1. A process for production of 5-ene-3-one of sterols, comprising steps of:
performing a reaction, by inclusion of sterol or a derivative thereof in a bilayer solution containing of an aqueous layer including a cholesterol oxidase-containing solution and a hydrocarbon-based solvent layer including a hydrocarbon-based solvent,
wherein the cholesterol oxidase-containing solution is a culturing solution for a Arthrobacter genus exhibiting a cholesterol oxidase activity.
2. The process for production of 5-ene-3-one of sterols according to claim 1, wherein the hydrocarbon-based solvent is at least one selected from n-butane, n-hexane, heptane and cycloalkanes.
3. The process for production of 5-ene-3-one of sterols according to claim 1, further comprising adding an alcohol to a reaction solution after the reaction is terminated.
4. The process for production of 5-ene-3-one of sterols according to claim 1, wherein the sterol is plant sterols.
5. The process for production of 5-ene-3one of sterols according to claim 1, wherein the Arthrobacter genus is Arthrobacter Simplex.
The claims below are in addition to those above.
All refrences to claim(s) which appear below refer to the numbering after this setence.
What is claimed is:
1. A compound of the formula (I):
59
or a pharmaceutically acceptable salt form or prodrug thereof, wherein:
Q is Q1,
(C1-C3 alkyl) OQ1,
(C1-C3 alkyl)-SQ1,
(C1-C3 alkyl)-S(O)Q1,
(C1-C3 alkyl)-S(O)2-Q1, or
(C1-C3 alkyl)-N(R20)Q1;
Q1 is C1-C8 alkyl substituted with 0-3 R1a;
C2-C8 alkenyl substituted with 0-3 R1a;
C2-C8 alkynyl substituted with 0-3 R1a;
C3-C10 cycloalkyl substituted with 0-3 R1b;
C3-C10 carbocycle substituted with 0-3 R1b;
C6-C10 aryl substituted with 0-3 R1b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R1b;
R1a, at each occurrence, is independently selected from H, C1-C6 alkyl, OR14, C1, F, Br, I, NR15R16, CF3;
C3-C10 carbocycle substituted with 0-3 R1b;
C6-C10 aryl substituted with 0-3 R1b; and
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R1b; R1b, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, C1-C4 haloalkyl-S, and (C1-C6 alkyl)-OC(O);
R2 is H, methyl, ethyl, propyl, or butyl;
R3 is H, C1-C6 alkyl, C(O)(C1-C6 alkyl), C (S)(C1-C6 alkyl), or C(O)NR21R22;
alternatively, R2 and OR3 are combined to form CO or CNOH;
R5 is H, OR14;
C1-C6 alkyl substituted with 0-3 R5b;
C1-C6 alkoxy substituted with 0-3 R5b;
C2-C6 alkenyl substituted with 0-3 R5b;
C2-C6 alkynyl substituted with 0-3 R5b;
C3-C10 cycloalkyl substituted with 0-3 R5c;
C3-C10 carbocycle substituted with 0-3 R5c;
C6-C10 aryl substituted with 0-3 R5c; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3R5c;
R5a is H, C1-C4 alkyl, or C2-C4 alkenyl;
alternatively, R5 and R5a may be combined to form a 3-7 membered cycloalkyl ring substituted with 0-3 R5c; optionally the cycloalkyl ring formed by combining R5 and R5a may be benzo fused, wherein the benzo fused ring may be substituted with 0-3 R5c; R5b, at each occurrence, is independently selected from:
H, C1-C6 alkyl, CF3, OR14, Cl, F, Br, I, O, CN, NO2, NR15R16, acetyl, SCH3, S(O)CH3, S(O)2CH3, C2-C6 alkenyl, C2-C6 alkynyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, C1-C4 haloalkyl-S,
C3-C10 cycloalkyl substituted with 0-3 R5c;
C3-C10 carbocycle substituted with 0-3 R5c;
C6-C10 aryl substituted with 0-3 R5c; and
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R5c;
R5c, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
R6 is H or C1-C6 alkyl;
W is (CR8R8a)p;
p is 0, 1, 2, 3,or 4;
R8 and R8a, at each occurrence, are independently selected from H, F, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl and C3-C8 cycloalkyl;
X is a bond;
C6-C10 aryl substituted with 0-3 RXb;
C3-C10 cycloalkyl substituted with 0-3 RXb;
C3-C10 carbocycle substituted with 0-3 RXb; or
5 to 10 membered heterocycle substituted with 0-2 RXb;
RXb, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
Y is a bond or (CR9R9a)tV(CR9R9a)u;
t is 0, 1, 2,or 3;
u is 0, 1, 2,or 3;
R9 and R9a, at each occurrence, are independently selected from H, F, C1-C6 alkyl or C3-C8 cycloalkyl;
V is a bond, C(O), O, S, S(O), S(O)2, N(R19), C(O)NR19b, NR19bC(O), NR19bS(O)2, S(O)2NR19b, C(O)O, or OC(O);
Z is H;
C1-C8 alkyl substituted with 0-2 R12;
C2-C4 alkenyl substituted with 0-2 R12;
C2-C4 alkynyl substituted with 0-2 R12;
C6-C10 aryl substituted with 0-4 R12b;
C3-C10 carbocycle substituted with 0-4 R12b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R12b;
Ring B is a 6, 7,or 8 membered lactam,
wherein the lactam is saturated, partially saturated or unsaturated;
wherein each additional lactam carbon is substituted with 0-2 R11; and,
optionally, the lactam contains a heteroatom selected from N, N(O), NH, N(R10), O, S, S(O), and S(O)2;
additionally, two R11 substituents on adjacent atoms may be combined to form C3-C6 carbocycle fused radical, a benzo fused radical, or a 5 to 6 membered heteroaryl fused radical,
wherein said 5 to 6 membered heteroaryl fused radical comprises 1-2 heteroatoms selected from N, O, and S;
wherein said benzo fused radical or 5 to 6 membered heteroaryl fused radical is substituted with 0-3 R13;
R10 is H, C(O)R17, C(O) OR17, C(O)NR18R19, S(O)2NR18R19, S (O)2R17;
C1-C6 alkyl substituted with 0-2 R10a;
C6-C10 aryl substituted with 0-4 R10b;
C3-C10 carbocycle substituted with 0-3 R10b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is optionally substituted with 0-3 R10b;
R10a, at each occurrence, is independently selected from H, C1-C6 alkyl, OR14, Cl, F, Br, I, O, CN, NO2, NR15R16, CF3;
aryl substituted with 0-4 R10b;
C3-C10 carbocycle substituted with 0-3 R10b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is optionally substituted with 0-3 R10b;
R10b, at each occurrence, is independently selected from H, OH, C1-C6 alkyl, C1-C4 alkoxy, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O) CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
R11, at each occurrence, is independently selected from H,
C1-C4 alkoxy, Cl, F, Br, I, O, CN, NO2, NR18R19, C(O)R17, C(O)OR17, C(O)NR18R19, S(O)2NR18R19, CF3;
C1-C6 alkyl substituted with 0-1 R11a;
C6-C10 aryl substituted with 0-3 R11b;
C3-C10 carbocycle substituted with 0-3 R11b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R11b;
R11a, at each occurrence, is independently selected from H, C1-C6 alkyl, OR14, Cl, F, Br, I, O, CN, NO2, NR15R16, CF3;
phenyl substituted with 0-3 R11b;
C3-C10 carbocycle substituted with 0-3 R11b; or 5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R11b; R11b, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, C1-C4 haloalkyl-S, benzyl, benzoyl, C(O)CH3, t-butoxycarbonyl, and 3,5-dimethyl-isoxazole-S(O)2;
R12 at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, C(O)NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
C6-C10 aryl substituted with 0-4 R12b;
C3-C10 carbocycle substituted with 0-4 R12b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R12b;
R12b, at each occurrence, is independently selected from H, OH, Cl ,F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
R13, at each occurrence, is independently selected from H, OH, C1-C6 alkyl, C1-C4 alkoxy, Cl, F, Br, I, CN, NO2, NR15R6, and CF3;
R14, at each occurrence, is independently selected from H, phenyl, benzyl, C1-C6 alkyl, and C2-C6 alkoxyalkyl;
R14ais H, phenyl, benzyl, or C1-C6 alkyl;
R15, at each occurrence, is independently selected from H, C1-C6 alkyl, phenyl, benzyl, phenethyl, (C1-C6 alkyl)-C(O), (C1-C6 alkyl)-OC(O) and (C1-C6 alkyl)-S(O)2;
R16, at each occurrence, is independently selected from H, OH, C1-C6 alkyl, phenyl, benzyl, phenethyl, (C1-C6 alkyl)-C(O), (C1-C6 alkyl)-OC(O) and (C1-C6 alkyl)-S(O)2;
alternatively, NR15R16 may be a heterocyclic ring selected from the group piperidinyl, morpholinyl, thiomorpholinyl, pyrrolidinyl, homopiperidinyl, piperazinyl, and N-methylpiperizinyl;
R17 is H, C1-C6 alkyl, or C2-C6 alkoxyalkyl, aryl substituted by 0-4 R17a, or aryl-CH2 wherein said aryl is substituted by by 0-4 R17a;
R17a is H, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, butoxy, OH, F, Cl, Br, I, CF3, OCF3, SCH3, S(O)CH3, S(O)2CH3, NH2, N(CH3)2, or C1-C4 haloalkyl;
R18, at each occurrence, is independently selected from H, C1-C6 alkyl, phenyl, benzyl, phenethyl, (C1-C6 alkyl)-C(O) and (C1-C6 alkyl)-S(O)2; alternatively, NR18R19 may be a heterocyclic ring selected from the group: piperidinyl, morpholinyl, thiomorpholinyl, pyrrolidinyl, homopiperidinyl, piperazinyl, and N-methylpiperizinyl; wherein said heterocyclic ring is substituted with 0-3 R11b;
R19, at each occurrence, is independently selected from H, OH, C1-C6 alkyl, phenyl, benzyl, phenethyl, (C1-C6 alkyl)-C(O) and (C1-C6 alkyl)-S(O)2;
R19b, at each occurrence, is independently selected from H and C1-C6 alkyl;
R20 is H, OH, C1-C4 alkyl, phenyl, benzyl, or phenethyl;
R21 at each occurrence, is independently selected from H, C1-C6 alkyl, phenyl, benzyl, and phenethyl; and
R22, at each occurrence, is independently selected from H, C1-C6 alkyl, phenyl, benzyl, and phenethyl.
2. A compound of claim 1, or a pharmaceutically acceptable salt form or prodrug thereof, wherein:
Q is Q1,
(C1-C3 alkyl)-OQ1,
(C1-C3 alkyl)-SQ1,
(C1-C3 alkyl)-S(O)Q1,
(C1-C3 alkyl)-S(O)2Q1, or
(C1-C3 alkyl)-N(R20)Ql;
Q1 is C1-C6 alkyl substituted with 0-3 R1a;
C2-C6 alkenyl substituted with 0-3 R1a;
C2-C6 alkynyl substituted with 0-3 R1a;
C3-C10 cycloalkyl substituted with 0-3 R1b;
C3-C10 carbocycle substituted with 0-3 R1b;
C6-C10 aryl substituted with 0-3 R1b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R1b;
R1a, at each occurrence, is independently selected from H,
C1-C6 alkyl, OR14, Cl ,F, Br, I, NR15R16, CF3;
C3-C10 carbocycle substituted with 0-3 R1b;
C6-C10 aryl substituted with 0-3 R1b; and
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R1b;
R1b, at each occurrence, is independently selected from H, OH, Cl ,F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, C1-C4 haloalkyl-S, and (C1-C6 alkyl)-OC(O);
R2 is H, methyl, ethyl, propyl, or butyl;
R3 is H, C1-C4 alkyl, C(O) (C1-C4 alkyl), C(S) (C1-C4 alkyl), or C(O) NR21R22;
R5 is H, OR14;
C1-C6 alkyl substituted with 0-3 R5b;
C1-C6 alkoxy substituted with 0-3 R5b;
C2-C6 alkenyl substituted with 0-3 R5b;
C2-C6 alkynyl substituted with 0-3 R5b;
C3-C10 cycloalkyl substituted with 0-3 R5c;
C3-C10 carbocycle substituted with 0-3 R5c;
C6-C10 aryl substituted with 0-3 R5c; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3R5c;
R5a is H, C1-C4 alkyl, or C2-C4 alkenyl;
alternatively, R5 and R5a may be combined to form a 3-7 membered cycloalkyl ring substituted with 0-3 R5c;
R5b, at each occurrence, is independently selected from:
H, C1-C6 alkyl, CF3, OR14, Cl, F, Br, I, O, CN, NO2, NR15R16, acetyl, SCH3, S(O)CH3, S(O)2CH3, C2-C6 alkenyl, C2-C6 alkynyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S,
C3-C10 cycloalkyl substituted with 0-3 R5c;
C3-C10 carbocycle substituted with 0-3 R5c;
C6-C10 aryl substituted with 0-3 R5c; and
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R5c;
R5c, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
R6 is H, methyl, or ethyl;
W is (CR8R8a)p;
p is 0, 1,or 2;
R8 and R8a, at each occurrence, are independently selected from H, F, methyl, and ethyl;
X is a bond;
phenyl substituted with 0-3 RXb;
C3-C6 cycloalkyl substituted with 0-3 RXb; or
5 to 6 membered heterocycle substituted with 0-2 RXb;
Rxb, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
Y is a bond or (CR9R9a)tV(CR9R9a)u;
t is 0, 1,or 2;
u is 0, 1,or 2;
R9 and R9a, at each occurrence, are independently selected from H, F, methyl, and ethyl;
V is a bond, C(O), O, S, S(O), S(O)2, N(R19)5490 , C(O)NH, NHC(O), NHS(O)2, or S(O)2NH;
Z is H, halo;
C1-C4 alkyl substituted with 0-2 R12;
C2-C4 alkenyl substituted with 0-2 R12;
C2-C4 alkynyl substituted with 0-2 R12;
C6-C10 aryl substituted with 0-4 R12b;
C3-C6 carbocycle substituted with 0-4 R12b; or
5 to 6 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-3 R12b;
Ring B is a 7 membered lactam,
wherein the lactam is saturated, partially saturated or unsaturated;
wherein each additional lactam carbon is substituted with 0-2 R11; and,
optionally, the lactam contains a heteroatom selected from N, NH, N(R10), O, S, S(O), and S(0)2;
additionally, two R11 substituents on adjacent atoms may be combined to form C3-C6 carbocycle fused radical, a benzo fused radical, or a 5 to 6 membered heteroaryl fused radical,
wherein said 5 to 6 membered heteroaryl fused radical comprises 1-2 heteroatoms selected from N, O, and S;
wherein said benzo fused radical or 5 to 6 membered heteroaryl fused radical is substituted with 0-3 R13;
R10 is H, C(O)R17, C(O)OR17, C(O)NR18R19, S(O)2NR18R19, S(0)2R17;
C1-C6 alkyl substituted with 0-2 R10a;
C6-C10 aryl substituted with 0-4 R10b;
C3-C10 carbocycle substituted with 0-3 R10b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is optionally substituted with 0-3
R10A, at each occurrence, is independently selected from H, C1-C6 alkyl, OR14, Cl, F, Br, I, O, CN, NO2, NR15R16, CF3, or aryl substituted with 0-4 R10b; R10b, at each occurrence, is independently selected from H, OH, C1-C6 alkyl, C1-C4 alkoxy, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(0)CH3, S(0)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
R11, at each occurrence, is independently selected from H, C1-C4 alkoxy, Cl, F, Br, I, O, CN, NO2, NR18R19, C(O)R17, C(O)OR17, C(O)NR18R19, S(O)2NR18R19, CF3;
C1-C6 alkyl substituted with 0-1 R11a;
C6-C10 aryl substituted with 0-3 R11b;
C3-C10 carbocycle substituted with 0-3 R11b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R11b;
R11a, at each occurrence, is independently selected from H, C1-C6 alkyl, OR14, Cl, F, Br, I, O, CN, NO2, NR15R16, CF3;
phenyl substituted with 0-3 R11b;
C3-C10 carbocycle substituted with 0-3 R11b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R11b;
R11b, at each occurrence, is independently selected from H, OH, C1,F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
R12 at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16,C(O)NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
C6-C10 aryl substituted with 0-4 R12b;
C3-C10 carbocycle substituted with 0-4 R12b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R12b;
R12b, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
R13, at each occurrence, is independently selected from H, OH, C1-C6 alkyl, C1-C4 alkoxy, C1,F, Br, I, CN, NO2, NR15R16, and CF3;
R14, at each occurrence, is independently selected from H, phenyl, benzyl, C1-C6 alkyl, and C2-C6 alkoxyalkyl;
R15, at each occurrence, is independently selected from H, C1-C6 alkyl, phenyl, benzyl, phenethyl, (C1-C6 alkyl)-C(O), (C1-C6 alkyl)-OC(O) and (C1-C6 alkyl)-S(O)2;
R16, at each occurrence, is independently selected from H, OH, C1-C6 alkyl, phenyl, benzyl, phenethyl, (C1-C6 alkyl)-C(O), (C1-C6 alkyl)-OC(O) and (C1-C6 alkyl)-S(O)2;
alternatively, NR15R16 may be a heterocyclic ring selected from the group piperidinyl, morpholinyl, thiomorpholinyl, pyrrolidinyl, homopiperidinyl, piperazinyl, and N-methylpiperizinyl;
R17 is H, aryl, aryl-CH2, C1-C6 alkyl, or C2-C6 alkoxyalkyl;
R18 at each occurrence, is independently selected from H, C1-C6 alkyl, phenyl, benzyl, phenethyl, (C1-C6 alkyl)-C(O) and (C1-C6 alkyl)-S(O)2;
R19, at each occurrence, is independently selected from H, OH, C1-C6 alkyl, phenyl, benzyl, phenethyl, (C1-C6 alkyl)-C(O) and (C1-C6 alkyl)-S(O)2;
alternatively, NR18R19 may be a heterocyclic ring selected from the group piperidinyl, morpholinyl, thiomorpholinyl, pyrrolidinyl, homopiperidinyl, piperazinyl, and N-methylpiperizinyl;
R20 is H, OH, C1-C4 alkyl, phenyl, benzyl, or phenethyl;
R21, at each occurrence, is independently selected from H, C1-C6 alkyl, phenyl, benzyl, and phenethyl; and
R22, at each occurrence, is independently selected from H, C1-C6 alkyl, phenyl, benzyl, and phenethyl.
3. A compound of claim 2 wherein Ring B is selected from:
60
wherein each benzo fused radical is substituted with 0-3 R13.
4. A compound of claim 1, of Formula (Ia):
61
or a pharmaceutically acceptable salt form or prodrug thereof, wherein:
Q is Q1,
(C1-C3 alkyl)-OQ1,
(C1-C3 alkyl)-SQ1,
(C1-C3 alkyl)-S(O)Q1,
(C1-C3 alkyl)-S(O)2Q1, or
(C1-C3 alkyl)-N(R20)Q1;
Q1 is C1-C6 alkyl substituted with 0-3 R1a;
C2-C6 alkenyl substituted with 0-3 R1a;
C2-C6 alkynyl substituted with 0-3 R1a;
C3-C10 cycloalkyl substituted with 0-3 R1b;
C3-C10 carbocycle substituted with 0-3 R1b;
C6-C10 aryl substituted with 0-3 R1b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R1b;
R1a, at each occurrence, is independently selected from H,
C1-C6 alkyl, OR14, Cl, F, Br, I, NR15R16, CF3;
C3-C10 carbocycle substituted with 0-3 R1b;
C6-C10 aryl substituted with 0-3 R1b; and
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R1b;
R1b, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, C1-C4 haloalkyl-S, and (C1-C6 alkyl)-OC(O);
R2 is H, methyl, or ethyl;
R5 is H, OR14;
C1-C6 alkyl substituted with 0-3 R5b;
C1-C6 alkoxy substituted with 0-3 R5b;
C2-C6 alkenyl substituted with 0-3 R5b;
C2-C6 alkynyl substituted with 0-3 R5b;
C3-C10 cycloalkyl substituted with 0-3 R5c;
C3-C10 carbocycle substituted with 0-3 R5c;
C6-C10 aryl substituted with 0-3 R5c; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3R5c;
R5a is H, C1-C4 alkyl, or C2-C4 alkenyl; alternatively, R5 and R5a may be combined to form a 3-7 membered cycloalkyl ring substituted with 0-3 R5c;
R5b, at each occurrence, is independently selected from:
H, C1-C6 alkyl, CF3, OR14, C1,F, Br, I, O, CN, NO2, NR15R16, acetyl, SCH3, S(O)CH3, S(O)2CH3, C2-C6 alkenyl, C2-C6 alkynyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S,
C3-C10 cycloalkyl substituted with 0-3 R5c;
C3-C10 carbocycle substituted with 0-3 R5c;
C6-C10 aryl substituted with 0-3 R5c; and
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R5c;
R5c, at each occurrence, is independently selected from H, OH, C1,F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
W is (CR8R8a)p;
p is 0, 1,or 2;
R8 and R8a, at each occurrence, are independently selected from H, F, methyl, and ethyl;
X is a bond;
phenyl substituted with 0-3 RXb;
C3-C6 cycloalkyl substituted with 0-3 RXb; or
5 to 6 membered heterocycle containing 1 to 3 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-2 RXb,
Rxb, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R 6, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
Y is a bond or (CR9R9a)tV(CR9R9a)u;
t is 0, 1,or 2;
u is 0, 1,or 2;
R9 and R9a, at each occurrence, are independently selected from H, F, methyl, and ethyl;
V is a bond, C(O), O, S, S(O), S(O)2, N(R19), C(O)NH, or NHC(O);
Z is H, halo;
C1-C4 alkyl substituted with 0-2 R12;
C2-C4 alkenyl substituted with 0-2 R12;
C2-C4 alkynyl substituted with 0-2 R12;
C6-C10 aryl substituted with 0-4 R12b;
C3-C6 carbocycle substituted with 0-4 R12b; or
5 to 6 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-3 R12b;
Ring B is selected from:
62
R10 is H, C(O)R17, C(O)OR17, C(O)NR18R19, S(O)2NR18R19, S(O)2R17;
C1-C6 alkyl substituted with 0-2 R10a;
C6-C10 aryl substituted with 0-4 R10b;
C3-C10 carbocycle substituted with 0-3 R10b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is optionally substituted with 0-3 R10b;
R10a, at each occurrence, is independently selected from H, C1-C6 alkyl, OR14, Cl, F, Br, I, O, CN, NO2, NR15R16, CF3, or aryl substituted with 0-4 R10b;
R10b, at each occurrence, is independently selected from H, OH, C1-C6 alkyl, C1-C4 alkoxy, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
R11, at each occurrence, is independently selected from H,
C1-C4 alkoxy, Cl, F, Br, I, O, CN, NO2, NR18R19, C(O)R17, C(O)OR17, C(O)NR18R19, S(O)2NR18R19, CF3;
C1-C6 alkyl substituted with 0-1 R11a;
C6-Cl0 aryl substituted with 0-3 R11b;
C3-C10 carbocycle substituted with 0-3 R11b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R11b;
R11a, at each occurrence, is independently selected from H, C1-C6 alkyl, OR14, Cl, F, Br, I, O, CN, NO2, NR15R16, CF3;
phenyl substituted with 0-3 R11b;
C3-C10 carbocycle substituted with 0-3 R11b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R11b; R11b, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, C1-C4 haloalkyl-S, benzyl, benzoyl, C(O)CH3, t-butoxycarbonyl, and 3,5-dimethyl-isoxazole-S(O)2;
R12 at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, C(O)NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
C6-C10 aryl substituted with 0-4 R12b;
C3-C10 carbocycle substituted with 0-4 R12b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R12b; R12b, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
R13, at each occurrence, is independently selected from H, OH, C1-C6 alkyl, C1-C4 alkoxy, Cl, F, Br, I, CN, NO2, NR15R16, and CF3;
R14, at each occurrence, is independently selected from H, phenyl, benzyl, C1-C6 alkyl, and C2-C6 alkoxyalkyl;
R15, at each occurrence, is independently selected from H, C1-C6 alkyl, phenyl, benzyl, phenethyl, (C1-C6 alkyl)-C(O), (C1-C6 alkyl)-OC(O) and (C1-C6 alkyl)-S(O)2;
R16, at each occurrence, is independently selected from H, OH, C1-C6 alkyl, phenyl, benzyl, phenethyl, (C1-C6 alkyl)-C(O), (C1-C6 alkyl)-OC(O) and (C1-C6 alkyl)-S(O)2; alternatively, NR15R16 may be a heterocyclic ring selected from the group piperidinyl, morpholinyl, thiomorpholinyl, pyrrolidinyl, homopiperidinyl, piperazinyl, and N-methylpiperizinyl;
R17 is H, C1-C6 alkyl, or C2-C6 alkoxyalkyl, aryl substituted by 0-4 R17a, or aryl-CH2-wherein said aryl is substituted by by 0-4 R17a;
R17a is H, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, butoxy, OH, F, C1,Br, I, CF3, OCF3, SCH3, S(O)CH3, S(O)2CH3, NH2, N(CH3)2, or C1-C4 haloalkyl;
R18, at each occurrence, is independently selected from H, C1-C6 alkyl, phenyl, benzyl, phenethyl, (C1-C6 alkyl)-C(O) and (C1-C6 alkyl)-S(O)2;
R19, at each occurrence, is independently selected from H, OH, C1-C6 alkyl, phenyl, benzyl, phenethyl, (C1-C6 alkyl)-C(O) and (C1-C6 alkyl)-S(O)2;
alternatively, NR18R19 may be a heterocyclic ring selected from the group: piperidinyl, morpholinyl, thiomorpholinyl, pyrrolidinyl, homopiperidinyl, piperazinyl, and N-methylpiperizinyl; wherein said heterocyclic ring is substituted with 0-3 R11b-; and
R20 is H, OH, C1-C4 alkyl, phenyl, benzyl, or phenethyl.
5. A compound, according to claim 4, of Formula (Ia):
63
wherein:
Ring B is selected from:
64
Q is Q1 or (C1-3 alkyl) -OQ1;
Q1 is C1-C6 alkyl substituted with 0-3 R1a;
C2-C6 alkenyl substituted with 0-3 R1a;
C2-C6 alkynyl substituted with 0-3 R1a;
C3-C10 cycloalkyl substituted with 0-3 R1b;
C3-C10 carbocycle substituted with 0-3 R1b;
C6-C10 aryl substituted with 0-3 R1b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R1b;
R1a, at each occurrence, is independently selected from H,
C1-C6 alkyl, OR14, Cl, F, Br, I, NR15R16, CF3;
C3-C10 carbocycle substituted with 0-3 R1b;
C6-C10 aryl substituted with 0-3 R1b; and
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R1b;
R1b, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, C1-C4 haloalkyl-S, and (C1-C6 alkyl)-OC(O);
R2 is H, methyl, or ethyl;
R5 is H, OR14;
C1-C6 alkyl substituted with 0-3 R5b;
C2-C6 alkenyl substituted with 0-3 R5b;
C2-C6 alkynyl substituted with 0-3 R5b;
C3-C6 cycloalkyl substituted with 0-3 R5c;
C3-C6 carbocycle substituted with 0-3 R5c;
phenyl substituted with 0-3 R5c; or
5 to 7 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 7 membered heterocycle is substituted with 0-3R5c;
R5a is H, C1-C4 alkyl, or C2-C4 alkenyl;
alternatively, R5 and R5a may be combined to form a C4-C7 cycloalkyl ring;
R5b, at each occurrence, is independently selected from:
H, C1-C6 alkyl, CF3, OR14, C1,F, Br, I, O, CN, NO2, NR15R16, acetyl, SCH3, S(O)CH3, S(O)2CH3, C2-C6 alkenyl, C2-C6 alkynyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S,
C3-C10 cycloalkyl substituted with 0-3 R5c;
C3-C10 carbocycle substituted with 0-3 R5c;
C6-C10 aryl substituted with 0-3 R5c; and
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R5c;
R5c, at each occurrence, is independently selected from H, OH, Cl ,F, Br, I, CN, NO2, NR15R16CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
W is (CR8R8a)p;
p is 0, 1,or 2;
R8 and R8a, at each occurrence, are independently selected from H, methyl, and ethyl;
X is a bond;
phenyl substituted with 0-3 RXb;
C3-C6 cyclolakyl substituted with 0-3 RXb; or
5 to 6 membered heterocycle containing 1 to 3 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-2 RXb;
RXb, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
Y is a bond or (CR9R9a)tV(CR9R9a)u;
t is 0, 1,or 2;
u is 0, 1,or 2;
R9 and R9a, at each occurrence, are independently selected from H, F, methyl, and ethyl;
V is a bond, C(O), O, S, S(O), S(O)2, N(R19), NHC(O), or C(O)NH;
Z is H, F, Cl, Br;
C1-C4 alkyl substituted with 0-2 R12;
C2-C4 alkenyl substituted with 0-2 R12;
C2-C4 alkynyl substituted with 0-2 R12;
C6-C10 aryl substituted with 0-4 R12b;
C3-C6 carbocycle substituted with 0-4 R12b; or
5 to 6 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-3 R12b;
R10 is C(O)R17, C(O)NR18R19, S(O)2R17;
C1-C6 alkyl substituted with 0-2 R10a;
phenyl substituted with 0-3 R10b; or
5 to 6 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is optionally substituted with 0-3 R10b;
R10a, at each occurrence, is independently selected from H, C1-C6 alkyl, OR14, Cl, F, Br, I, O, CN, NO2, NR15R16, CF3, or aryl substituted with 0-3 R10b;
R10b, at each occurrence, is independently selected from H, OH, C1-C6 alkyl, C1-C4 alkoxy, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
R11, at each occurrence, is independently selected from H, O, NR18R19, C(O)R17, C(O)OR17, C(O)NR18R19, S(O)2NR18R19, CF3;
C1-C6 alkyl substituted with 0-1 R11a;
phenyl substituted with 0-3 R11b,
C3-C6 carbocycle substituted with 0-3 R11b; or
5 to 7 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 7 membered heterocycle is substituted with 0-3 R11b;
R11a, at each occurrence, is independently selected from H, C1-C4 alkyl, OR14, Cl, F, Br, O, CN, NO2, NR15R16, CF3;
phenyl substituted with 0-3 R11b;
C3-C6 carbocycle substituted with 0-3 R11b; or
5 to 7 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 7 membered heterocycle is substituted with 0-3 R11b;
R11b, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, C1-C4 haloalkyl-S, benzyl, benzoyl, C(O)CH3, t-butoxycarbonyl, and 3,5-dimethyl-isoxazole-S(O)2;
R12 at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16,C(O)NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
C6-C10 aryl substituted with 0-4 R12b;
C3-C10 carbocycle substituted with 0-4 R12b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R12b;
R12b, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S((O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
R13, at each occurrence, is independently selected from H, OH, C1-C6 alkyl, C1-C4 alkoxy, Cl, F, Br, I, CN, NO2, NR15R16, and CF3;
R14, at each occurrence, is independently selected from H, phenyl, benzyl, C1-C6 alkyl, and C2-C6 alkoxyalkyl;
R15, at each occurrence, is independently selected from H, C1-C6 alkyl, phenyl, benzyl, phenethyl, (C1-C6 alkyl)-C(O), (C1-C6 alkyl)-OC(O) and (C1-C6 alkyl)-S(O)2;
R16, at each occurrence, is independently selected from H, OH, C1-C6 alkyl, phenyl, benzyl, phenethyl, (C1-C6 alkyl)-C(O), (C1-C6 alkyl)-OC(O) and (C1-C6 alkyl)-S(O)2;
alternatively, NR15R16 may be a heterocyclic ring selected from the group piperidinyl, morpholinyl, thiomorpholinyl, pyrrolidinyl, homopiperidinyl, piperazinyl, and N-methylpiperizinyl; and
R17 is H, C1-C6 alkyl, or C2-C6 alkoxyalkyl, aryl substituted by 0-4 R17a, or aryl-CH2 wherein said aryl is substituted by by 0-4 R17a;
R17a is H, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, butoxy, OH, F, Cl, Br, I, CF3, OCF3, SCH3, S(O)CH3, S(O)2CH3, NH2, N(CH3)2, or C1-C4 haloalkyl;
R18, at each occurrence, is independently selected from H, C1-C6 alkyl, phenyl, benzyl, phenethyl, (C1-C6 alkyl)-C(O) and (C1-C6 alkyl)-S(O)2;
R19, at each occurrence, is independently selected from H, OH, methyl, ethyl, propyl, butyl, phenyl, benzyl, and phenethyl; and
alternatively, NR18R19 may be a heterocyclic ring selected from the group: piperidinyl, morpholinyl, thiomorpholinyl, pyrrolidinyl, homopiperidinyl, piperazinyl, and N-methylpiperizinyl; wherein said heterocyclic ring is substituted with 0-3 R11b .
6. A compound of claim 5 wherein:
Q is Q1;
Q1 is C1-C6 alkyl substituted with 0-3 R1a;
C2-C6 alkenyl substituted with 0-3 R1a;
C2-C6 alkynyl substituted with 0-3 R1a;
C3-C10 cycloalkyl substituted with 0-3 R1b;
C3-C10 carbocycle substituted with 0-3 R1b;
C6-C10 aryl substituted with 0-3 R1b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R1b;
R1a, at each occurrence, is independently selected from H, C1-C6 alkyl, OR14, Cl ,F, Br, I, NR15R16, CF3;
C3-C10 carbocycle substituted with 0-3 R1b;
C6-C10 aryl substituted with 0-3 R1b; and
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R1b;
R1b, at each occurrence, is independently selected from H, OH, Cl ,F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, C1-C4 haloalkyl-S, and (C1-C6 alkyl)-OC(O);
R2 is H, methyl, or ethyl;
R5 is H, OR14;
C1-C6 alkyl substituted with 0-3 R5b;
C2-C6 alkenyl substituted with 0-3 R5b; or
C2-C6 alkynyl substituted with 0-3 R5b;
R5a is H, methyl, ethyl, propyl, butyl, or C2-C4 alkenyl; alternatively, R5 and R5a may be combined to form a C4-C7 cycloalkyl ring;
R5b at each occurrence, is independently selected from:
H, methyl, ethyl, propyl, butyl, CF3, OR14, Cl, F, Br, I, O, NR15R16,
C3-C7 cycloalkyl substituted with 0-3 R5c;
C3-7 carbocycle substituted with 0-3 R5c;
phenyl substituted with 0-3 R5c; and
5 to 7 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 7 membered heterocycle is substituted with 0-3 R5c;
R5c, at each occurrence, is independently selected from H, OH, Cl ,F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C4 alkyl, C1-C3 alkoxy, C1-C2 haloalkyl, and C1-C2 haloalkoxy;
W is (CHR8)p;
p is 0 or 1;
R8 is H, methyl, or ethyl;
X is a bond;
phenyl substituted with 0-2 RXb;
C5-C6 cycloalkyl substituted with 0-3 RXb; or
5 to 6 membered heterocycle containing 1 to 3 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-2 RXb;
RXb, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
Y is a bond, V, CH2V, VCH2, or CH2VCH2;
V is a bond, C(O), O, S, S(O), S(O)2, or N(R19);
Z is H, F, C1,Br,
C1-C4 alkyl substituted with 0-2 R12;
C2-C4 alkenyl substituted with 0-2 R12;
C2-C4 alkynyl substituted with 0-2 R12;
C6-C10 aryl substituted with 0-4 R12b;
C3-C6 carbocycle substituted with 0-4 R12b; or
5 to 6 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-3 R12b;
R10 is C(O)R17, C(O)NR18R19, S(O)2R17;
C1-C6 alkyl substituted with 0-2 R10a;
phenyl substituted with 0-3 R10b; or
5 to 6 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is optionally substituted with 0-3 R10b;
R10a, at each occurrence, is independently selected from H, C1-C6 alkyl, OR14, Cl, F, Br, I, O, CN, NO2, NR15R16, CF3, or aryl substituted with 0-3 R10b; R10b, at each occurrence, is independently selected from H, OH, C1-C6 alkyl, C1-C4 alkoxy, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
R11 at each occurrence, is independently selected from
H, O, NR18R19, C(O)R17, C(O)OR17, C(O)NR18R19, S(O)2NR18R19, CF3;
C1-C6 alkyl substituted with 0-1 R11a;
phenyl substituted with 0-3 R11b;
C3-C6 carbocycle substituted with 0-3 R11b; or
5 to 7 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 7 membered heterocycle is substituted with 0-3 R11b; wherein said 5 to 7 membered heterocycle is selected from pyridinyl, pyrimidinyl, triazinyl, furanyl, thienyl, thiazolyl, pyrrolyl, piperazinyl, piperidinyl, homopiperidinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, and tetrazolyl;
R11a, at each occurrence, is independently selected from H, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, Cl, F, O, NR15R16, CF3;
phenyl substituted with 0-3 R11b;
C3-C6 carbocycle substituted with 0-3 R11b; or
5 to 7 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 7 membered heterocycle is substituted with 0-3 R11b; wherein said 5 to 7 membered heterocycle is selected from pyridinyl, pyrimidinyl, triazinyl, furanyl, thienyl, thiazolyl, pyrrolyl, piperazinyl, piperidinyl, homopiperidinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, and tetrazolyl;
R11b, at each occurrence, is independently selected from H, OH, Cl, F, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, C1-C2 haloalkyl, C1-C2 haloalkoxy, benzyl, benzoyl, C(O)CH3, t-butoxycarbonyl, and 3,5-dimethyl-isoxazole-S(O)2;
R12 at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, C(O)NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
C6-C10 aryl substituted with 0-4 R12b;
C3-C10 carbocycle substituted with 0-4 R12b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R12b;
R12b, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
R13, at each occurrence, is independently selected from H, OH, C1-C6 alkyl, C1-C4 alkoxy, Cl, F, Br, I, CN, NO2, NR15R16, and CF3;
R14, at each occurrence, is independently selected from H, phenyl, benzyl, C1-C4 alkyl, and C2-C4 alkoxyalkyl;
R15, at each occurrence, is independently selected from H, methyl, ethyl, propyl, butyl, phenyl, benzyl, and phenethyl;
R16 at each occurrence, is independently selected from H, OH, methyl, ethyl, propyl, butyl, phenyl, benzyl, phenethyl, CH3CH2C(O), CH3C(O), CH3CH2OC(O), CH3OC(O), CH3CH2S(O)2 and CH3S(O)2;
R17 is H, C1-C4 alkyl, or C2-C4 alkoxyalkyl;
phenyl substituted by 0-2 R17a; or
benzyl substituted by 0-2 R17a;
R17a is H, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, butoxy, OH, F, Cl, Br, I, CF3, OCF3, SCH3, S(O)CH3, S(O)2CH3, NH2, N(CH3)2, or C1-C4 haloalkyl;
R18, at each occurrence, is independently selected from H, methyl, ethyl, propyl, butyl, phenyl, benzyl, and phenethyl;
R19, at each occurrence, is independently selected from H, OH, methyl, ethyl, propyl, and butyl; and
alternatively, NR18R19 may be a heterocyclic ring selected from the group: piperidinyl, morpholinyl, thiomorpholinyl, pyrrolidinyl, homopiperidinyl, piperazinyl, and N-methylpiperizinyl; wherein said heterocyclic ring is substituted with 0-3 R11b.
7. A compound of claim 6 wherein:
Q is Q1,
Q1 is C1-C6 alkyl substituted with 0-3 R1a;
C2-C6 alkenyl substituted with 0-3 R1a;
C2-C6 alkynyl substituted with 0-3 R1a;
C3-C6 cycloalkyl substituted with 0-3 R1b;
phenyl substituted with 0-3 R1b; or
5 to 6 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-3 R1b;
R1a, at each occurrence, is independently selected from
H, methyl, ethyl, propyl, butyl, OR14, Cl, F, Br, I, NR15R16, CF3;
C3-C6 carbocycle substituted with 0-3 R1b;
phenyl substituted with 0-3 R1b; and
5 to 6 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-3 R1b;
R1b, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, C1-C2 haloalkyl, C1-C2 haloalkoxy, (methyl)OC(O), (ethyl)OC(O), (propyl)OC(O), and (butyl)OC(O);
R2 is H or methyl;
R5 is H, OR14;
C1-C4 alkyl substituted with 0-1 R5b;
C2-C4 alkenyl substituted with 0-1 R5b; or
C2-C4 alkynyl substituted with 0-1 R5b;
R5a is H, methyl, ethyl, propyl, or butyl;
alternatively, R5 and R5a may be combined to form a cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl ring;
R5b, at each occurrence, is independently selected from:
H, methyl, ethyl, propyl, butyl, CF3, OR14, Cl, F, O, NR15R16,
C3-C7 cycloalkyl substituted with 0-3 R5c;
C3-C7 carbocycle substituted with 0-3 R5c;
phenyl substituted with 0-3 R5c; and
5 to 7 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 7 membered heterocycle is substituted with 0-3 R5c; wherein said 5 to 7 membered heterocycle is selected from pyridinyl, pyrimidinyl, triazinyl, furanyl, thienyl, thiazolyl, pyrrolyl, piperazinyl, piperidinyl, homopiperidinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, and tetrazolyl;
R5c, at each occurrence, is independently selected from H, OH, Cl, F, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, C1-C2 haloalkyl, and C1-C2 haloalkoxy;
W is a bond, CH2, or CH(CH3);
X is a bond;
phenyl substituted with 0-1 RXb;
C5-C6 cycloalkyl substituted with 0-1 RXb; or
5 to 6 membered heterocycle containing 1 to 3 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-1 RXb; wherein said 5 to 6 membered heterocycle is selected from pyridinyl, pyrimidinyl, triazinyl, furanyl, thienyl, thiazolyl, pyrrolyl, piperazinyl, piperidinyl, pyrazolyl, imidazolyl, oxazolyl, and isoxazolyl;
Rxb, at each occurrence, is independently selected from H, OH, Cl, F, Br, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, C1-C2 haloalkyl, and C1-C2 haloalkoxy;
Y is a bond, V, VCH2, or CH2V;
V is a bond, C(O), O, S, S(O), S(O)2, or N(R19);
Z is H, F, Cl, Br,
C1-C4 alkyl substituted with 0-2 R12;
C2-C4 alkenyl substituted with 0-2 R12;
C2-C4 alkynyl substituted with 0-2 R12;
C6-C10 aryl substituted with 0-4 R12b;
C3-C6 carbocycle substituted with 0-4 R12b; or
5 to 6 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-3 R12b;
R11, at each occurrence, is independently selected from H, NR18R19, CF3;
C1-C4 alkyl substituted with 0-1 R11a;
phenyl substituted with 0-3 R11b;
C3-C6 carbocycle substituted with 0-3 R11b; or
5 to 7 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 7 membered heterocycle is substituted with 0-3 R11b; wherein said 5 to 7 membered heterocycle is selected from pyridinyl, pyrimidinyl, triazinyl, furanyl, thienyl, thiazolyl, pyrrolyl, piperazinyl, piperidinyl, homopiperidinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, and tetrazolyl; isoxazolyl, and tetrazolyl;
R11b, at each occurrence, is independently selected from H, OH, Cl, F, NR15R16, CF3, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, C1-C2 haloalkyl, and C1-C2 haloalkoxy;
R12 at each occurrence, is independently selected from H, OH, Cl, F, Br, NR15R16, C(O)NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, C1-C2 haloalkyl, and C1-C2 haloalkoxy;
phenyl substituted with 0-4 R12b;
C3-C6 carbocycle substituted with 0-4 R12b; or
5 to 6 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-3 R12b;
R12b, at each occurrence, is independently selected from H, OH, Cl, F, Br, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, C1-C2 haloalkyl, and C1-C2 haloalkoxy;
R13, at each occurrence, is independently selected from H, OH, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, Cl, F, Br, CN, NR15R16, and CF3;
R14, at each occurrence, is independently selected from H, phenyl, benzyl, methyl, ethyl, propyl, and butyl;
R15, at each occurrence, is independently selected from H, methyl, ethyl, propyl, or butyl;
R16, at each occurrence, is independently selected from H, OH, methyl, ethyl, propyl, butyl, phenyl, benzyl, and phenethyl;
R18, at each occurrence, is independently selected from H, methyl, ethyl, propyl, butyl, phenyl, benzyl and, phenethyl; and
R19, at each occurrence, is independently selected from H, OH, methyl, ethyl, propyl, butyl, phenyl, benzyl and, phenethyl.
8. A compound of claim 7 wherein:
Q is CH3, CH2CH3, CH2CH2CH3, CH2CH2CH2CH3, CH2CH2CH2CH2CH3, CH2CH2CH2CH2CH2CH3, CH (CH3)2, CH(CH3)CH2CH3, CH2CH(CH3)2, CH2C(CH3)3,
CF3, CH2CF3, CH2CH2CF3, CH2CH2CH2CF3,
CHCH2, CH2CHCH2, CH2C(CH3)CH2, CH2CHC(CH3)2, CH2CH2CHCH2, CH2CH2C(CH3)CH2, CH2CH2CHC(CH3)2, cis-CH2CHCH(CH3), cis-CH2CH2CHCH(CH3), trans-CH2CHCH(CH3), trans-CH2CH2CHCH(CH3);
CCH, CH2CCH, CH2CC(CH3),
cyclopropyl-, cyclobutyl-, cyclopentyl-, cyclohexyl-, cyclopropyl-CH2, cyclobutyl-CH2, cyclopentyl-CH2, cyclohexyl-CH2, cyclopropyl-CH2CH2, cyclobutyl-CH2CH2, cyclopentyl-CH2CH2, cyclohexyl-CH2CH2,
phenyl-, 2-F-phenyl-, 3-F-phenyl-, 4-F-phenyl-, 4-methoxyphenyl-,4-ethoxyphenyl-, 4-propoxyphenyl-, phenyl-CH2, (2-F-phenyl)CH2, (3-F-phenyl)CH2, (4-F-phenyl)CH2, (2-Cl-phenyl)CH2, (3-Cl-phenyl)CH2, (4-Cl-phenyl)CH2,
(2,3-diF-phenyl)CH2, (2,4-diF-phenyl)CH2, (2,5-diF-phenyl)CH2, (2,6-diF-phenyl)CH2, (3,4-diF-phenyl)CH2, (3,5-diF-phenyl)CH2, (2,3-diCl-phenyl)CH2, (2,4-diCl-phenyl)CH2, (2,5-diCl-phenyl)CH2, (2,6-diCl-phenyl)CH2, (3,4-diCl-phenyl)CH2, (3,5-diCl-phenyl)CH2, (3-F-4-Cl-phenyl)CH2, (3-F-5-Cl-phenyl)CH2, (3-Cl-4-F-phenyl) CH2,
2-furanyl-CH2, 3-furanyl-CH2, 2-thienyl-CH2, 3-thienyl-CH2, 2-pyridyl-CH2, 3-pyridyl-CH2, 4-pyridyl-CH2, 1-imidazolyl-CH2, 2-oxazolyl-CH2, 4-oxazolyl-CH2, 5-oxazolyl-CH2, 3-isoxazolyl-CH2, 4-isoxazolyl-CH2, 5-isoxazolyl-CH2,
phenyl-CH2CH2, (2-F-phenyl)CH2CH2, (3-F-phenyl)CH2CH2, (4-F-phenyl)CH2CH2, (2-Cl-phenyl)CH2CH2, (3-Cl-phenyl)CH2CH2, (4-Cl-phenyl)CH2CH2, (2,3-diF-phenyl)CH2CH2, (2,4-diF-phenyl )CH2CH2, (2,5-diF-phenyl)CH2CH2, (2,6-diF-phenyl)CH2CH2, (3,4-diF-phenyl)CH2CH2, (3,5-diF-phenyl)CH2CH2, (2,3-diCl-phenyl)CH2CH2, (2,4-diCl-phenyl)CH2CH2, (2,5-diCl-phenyl)CH2CH2, (2,6-diCl-phenyl)CH2CH2, (3,4-diCl-phenyl)CH2CH2, (3,5-diCl-phenyl)CH2CH2, (3-F-4-Cl-phenyl)CH2CH2, (3-F-5-Cl-phenyl)CH2CH2;
furanyl-CH2CH2, thienyl-CH2CH2, pyridyl-CH2CH2, 1-imidazolyl-CH2CH2, oxazoly-CH2CH2, isoxazolyl-CH2CH2, 3,5-dimethylisoxazol-4-yl-CH2CH2, phenyl-propyl-;
benzyl-CH(NH2), benzyl-CH(NHC(O)O-tBu)-, benzyloxy-CH2, pyrrolidin-2-yl-, or 3-t-butoxycarbonylpyrrolidin-2-yl-;
R2 is H or methyl;
R5 is CH3, CH2CH3, CH2CH2CH3, CH(CH3)2, CH2CH2CH2CH3, CH(CH3)CH2CH3, CH2CH(CH3)2, CH2C(CH3)3, CH2CH2CH2CH2CH3, CH(CH3)CH2CH2CH3, CH2CH(CH3)CH2CH3, CH2CH2CH(CH3)2, CH(CH2CH3)2,
CF3, CH2CF3, CH2CH2CF3, CH2CH2CH2CF3, CH2CH2CH2CH2CF3,
CHCH2, CH2CHCH2, CH2CH2CHCH2, CHCHCH3, cis-CH2CHCH(CH3), trans-CH2CHCH(CH3), trans-CH2CHCH(C6H5), CH2CHC(CH3)2, cis-CH2CHCHCH2CH3, trans-CH2CHCHCH2CH3, cis-CH2CH2CHCH(CH3), trans-CH2CH2CHCH(CH3), trans-CH2CHCHCH2 (C6H5),
CCH, CH2CCH, CH2CC(CH3), CH2CC(C6H5), CH2CH2CCH, CH2CH2CC(CH3), CH2CH2CC(C6H5), CH2CH2CH2CCH, CH2CH2CH2CC(CH3), CH2CH2CH2CC(C6H5),
cyclopropyl-CH2, cyclobutyl-CH2, cyclopentyl-CH2, cyclohexyl-CH2, (2-CH3-cyclopropyl)CH2, (3-CH3-cyclobutyl)CH2, cyclopropyl-CH2CH2, cyclobutyl-CH2CH2, cyclopentyl-CH2CH2, cyclohexyl-CH2CH2, (2-CH3-cyclopropyl)CH2CH2, (3-CH3-cyclobutyl)CH2CH2,
phenyl-CH2, (2-F-phenyl)CH2, (3-F-phenyl)CH2, (4-F-phenyl)CH2, (3,5-diF-phenyl)CH2, 2-furanyl-CH2, 3-furanyl-CH2, 2-thienyl-CH2, 3-thienyl-CH2, 2-pyridyl-CH2, 3-pyridyl-CH2, 4-pyridyl-CH2, 1-imidazolyl-CH2, 2-oxazolyl-CH2, 4-oxazolyl-CH2, 5-oxazolyl-CH2, 3-isoxazolyl-CH2, 4-isoxazolyl-CH2, 5-isoxazolyl-CH2,
phenyl-CH2CH2, (2-F-phenyl)CH2CH2, (3-F-phenyl)CH2CH2, (4-F-phenyl)CH2CH2, furanyl-CH2CH2, thienyl-CH2CH2, pyridyl-CH2CH2, 1-imidazolyl-CH2CH2, oxazolyl-CH2CH2, isoxazolyl-CH2CH2;
methoxy, ethoxy, propoxy, or butoxy;
R5a is H;
alternatively, R5 and R5a may be combined to form cyclopentyl, cyclohexyl, or cycloheptyl;
W is a bond, CH2, or CH(CH3);
X is a bond;
65
Y is a bond, CH2V, V, or VCH2;
V is a bond, C(O), O, S, S(O), S(O)2, NH, or N(CH3);
Z is H, F, Cl, Br, methyl, ethyl, n-propyl, i-propyl, n-butyl, i-butyl, s-butyl, t-butyl,
cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl,
phenyl, 2-F-phenyl, 3-F-phenyl, 4-F-phenyl, 2-Cl-phenyl, 3-Cl-phenyl, 4-Cl-phenyl, 2,3-diF-phenyl, 2,4-diF-phenyl, 2,5-diF-phenyl, 2,6-diF-phenyl, 3,4-diF-phenyl, 3,5-diF-phenyl, 2,3-diCl-phenyl, 2,4-diCl-phenyl, 2,5-diCl-phenyl, 2,6-diCl-phenyl, 3,4-diCl-phenyl, 3,5-diCl-phenyl, 3-F-4-Cl-phenyl, 3-F-5-Cl-phenyl, 3-Cl-4-F-phenyl, 2-MeO-phenyl, 3-MeO-phenyl, 4-MeO-phenyl, 2-Me-phenyl, 3-Me-phenyl, 4-Me-phenyl, 2-MeS-phenyl, 3-MeS-phenyl, 4-MeS-phenyl, 2-CF3O-phenyl, 3-CF3O-phenyl, 4-CF3O-phenyl,
furanyl, thienyl, pyridyl, N-oxide-pyridinyl, 2-Me-pyridyl, 3-Me-pyridyl, 4-Me-pyridyl, 1-imidazolyl, oxazolyl, isoxazolyl, 1-benzimidazolyl, morpholino, N-piperinyl,
phenyl-CH2, (2-F-phenyl)CH2, (3-F-phenyl)CH2, (4-F-phenyl)CH2, (2-Cl-phenyl)CH2, (3-Cl-phenyl)CH2, (4-Cl-phenyl)CH2, (2,3-diF-phenyl)CH2, (2,4-diF-phenyl)CH2, (2,5-diF-phenyl)CH2, (2,6-diF-phenyl)CH2, (3,4-diF-phenyl)CH2, (3,5-diF-phenyl)CH2, (2,3-diCl-phenyl)CH2, (2,4-diCl-phenyl)CH2, (2,5-diCl-phenyl)CH2, (2,6-diCl-phenyl)CH2, (3,4-diCl-phenyl)CH2, (3,5-diCl-phenyl)CH2, (3-F-4-Cl-phenyl)CH2, (3-F-5-Cl-phenyl)CH2, (3-Cl-4-F-phenyl)CH2, (2-MeO-phenyl)CH2, (3-Me-e-phenyl)CH2, (4-MeO-phenyl)CH2, (2-PhO-phenyl) CH2, (3-PhO-phenyl)CH2, (4-PhO-phenyl)CH2, (2-Me-phenyl)CH2, (3-Me-phenyl)CH2, (4-Me-phenyl)CH2, (2-MeS-phenyl)CH2, (3-MeS-phenyl)CH2, 4-MeS-phenyl)CH2, (2-CF3O-phenyl)CH2, (3-CF3O-phenyl)CH2, (4-CF3O-phenyl)CH2, (furanyl)CH2, (thienyl)CH2, (pyridyl)CH2, (2-Me-pyridyl)CH2, (3-Me-pyridyl)CH2, (4-Me-pyridyl)CH2, (1-imidazolyl)CH2, (oxazolyl)CH2, (isoxazolyl)CH2, (1-benzimidazolyl)CH2, (cyclopropyl)CH2, (cyclobutyl)CH2, (cyclopentyl)CH2, (cyclohexyl)CH2, (morpholino)CH2, (N-pipridinyl)CH2,
phenyl-CH2CH2, (phenyl)2CHCH2, (2-F-phenyl)CH2CH2, (3-F-phenyl)CH2CH2, (4-F-phenyl)CH2CH2, (2-Cl-phenyl)CH2CH2, (3-Cl-phenyl)CH2CH2, (4-Cl-phenyl)CH2CH2, (2,3-diF-phenyl)CH2CH2, (2,4-diF-phenyl)CH2CH2, (2,5-diF-phenyl)CH2CH2, (2,6-diF-phenyl)CH2CH2, (3,4-diF-phenyl)CH2CH2, (3,5-diF-phenyl)CH2CH2, (2,3-diCl-phenyl)CH2CH2, (2,4-diCl-phenyl)CH2CH2, (2,5-diCl-phenyl)CH2CH2, (2,6-diCl-phenyl)CH2CH2, (3,4-diCl-phenyl)CH2CH2, (3,5-diCl-phenyl)CH2CH2, (3-F-4-Cl-phenyl)CH2CH2, (3-F-5-Cl-phenyl)CH2CH2, (3-Cl-4-F-phenyl)CH2CH2, (2-MeO-phenyl)CH2CH2, (3-MeO-phenyl)CH2CH2, (4-MeO-phenyl)CH2CH2, (2-Me-phenyl)CH2CH2, (3-Me-phenyl)CH2CH2, (4-Me-phenyl)CH2CH2, (2-MeS-phenyl)CH2CH2, (3-MeS-phenyl)CH2CH2, (4-MeS-phenyl)CH2CH2, (2-CF3O-phenyl)CH2CH2, (3-CF3O-phenyl)CH2CH2, (4-CF3O-phenyl)CH2CH2, (furanyl)CH2CH2,(thienyl)CH2CH2, (pyridyl)CH2CH2, (2-Me-pyridyl)CH2CH2, (3-Me-pyridyl)CH2CH2, (4-Me-pyridyl)CH2CH2, (imidazolyl)CH2CH2, (oxazolyl)CH2CH2, (isoxazolyl)CH2CH2, (benzimidazolyl)CH2CH2, (cyclopropyl)CH2CH2, (cyclobutyl)CH2CH2, (cyclopentyl)CH2CH2, (cyclohexyl)CH2CH2, (morpholino)CH2CH2, or (N-pipridinyl)CH2CH2;
R11, at each occurrence, is independently selected from H, methyl, ethyl, n-propyl, i-propyl, n-butyl, i-butyl, s-butyl, t-butyl, phenyl, benzyl, phenethyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, cycloheptylmethyl, cyclopropylethyl, cyclobutylethyl, cyclopentylethyl, cyclohexylethyl, 2-F-phenyl-, 3-F-phenyl, 4-F-phenyl, 4-Cl-phenyl, 4-CH3-phenyl, 4-MeO-phenyl-, 4-CF3-phenyl, (4-F-phenyl)CH2, (4-Cl-phenyl)CH2, (4-CH3-phenyl)CH2, (4-CF3-phenyl)CH2, (4-F-phenyl)CH2CH2, (4-Cl-phenyl)CH2CH2, (4-CH3-phenyl)CH2CH2, (4-CF3-phenyl)CH2CH2, pyridin-2-yl-, pyridin-3-yl-, 4-CF3-pyridin-2-yl-, 4-CH3-pyridin-2-yl-, thiazol-2-yl-, azapan-1-yl, N,N-dimethylamino, N,N-diethylamino, N,N-dipropylamino, and N,N-dibutylamino; and
R13, at each occurrence, is independently selected from H, MeO, F, and Cl.
9. A compound, according to claim 5, of Formula (Ic);
66
or a pharmaceutically acceptable salt form or prodrug thereof.
10. A compound, according to claim 6, of Formula (Ic);
67
or a pharmaceutically acceptable salt form or prodrug thereof.
11. A compound, according to claim 7, of Formula (Ic);
68
or a pharmaceutically acceptable salt form or prodrug thereof.
12. A compound, according to claim 8, of Formula (Ic);
69
or a pharmaceutically acceptable salt form or prodrug thereof.
13. A compound, according to claim 5, of Formula (Id);
70
or a pharmaceutically acceptable salt form or prodrug thereof.
14. A compound, according to claim 6, of Formula (Id);
71
or a pharmaceutically acceptable salt form or prodrug thereof.
15. A compound, according to claim 7, of Formula (Id);
72
or a pharmaceutically acceptable salt form or prodrug thereof.
16. A compound, according to claim 8, of Formula (Id);
73
or a pharmaceutically acceptable salt form or prodrug thereof.
17. A compound, according to claim 5, of Formula (Ie);
74
or a pharmaceutically acceptable salt form or prodrug thereof.
18. A compound, according to claim 6, of Formula (Ie);
75
or a pharmaceutically acceptable salt form or prodrug thereof.
19. A compound, according to claim 7, of Formula (Ie);
76
or a pharmaceutically acceptable salt form or prodrug thereof.
20. A compound, according to claim 8, of Formula (Ie);
77
or a pharmaceutically acceptable salt form or prodrug thereof.
21. A compound of selected from:
3-(2(R)-Cyclopentylmethyl-3 (S)-hydroxyl-1-oxo-5-phenylpentyl) amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Cyclopentylmethyl-3(S)-hydroxyl-1-oxo-5-phenylpentyl)amino-1-methyl-5-(4-fluoro-phenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Benzyl-3( S)-hydroxyl-1-oxo-5-phenylpentyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Isopropyl-3(S)-hydroxyl-1-oxo-5-phenylpentyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2 (R)-Cyclopentylmethyl-3(S)-hydroxyl-1-oxo-4-(3,5-difluorophenoxy)butyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Isobutyl-3(S)-hydroxyl-1-oxo-4-(3,5-difluorophenoxy)butyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2 (R)-Cyclopentylmethyl-3(S)-hydroxyl-1-oxo-4-phenoxybutyl)amino-7-chloro-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Isobutyl-3(S)-hydroxyl-1-oxo-4-phenoxybutyl)amino-7-chloro-1-methyl-5-(4-fluorophenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Methyl-3(S)-hydroxyl-1-oxo-4-cyclohexyloxybutyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Isobutyl-3(S)-hydroxyl-1-oxo-4-cyclohexyloxybutyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Methyl-3(S)-hydroxyl-1-oxo-4-phenoxybutyl)amino-7-chloro-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2 (R)-Isobutyl-3(S)-hydroxyl-1-oxo-4-phenoxybutyl)amino-7-chloro-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Benzyl-3(S)-hydroxyl-1-oxo-4-cyclohexyloxybutyl)amino-7-chloro-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Cyclopentylmethyl-3(S)-hydroxyl-1-oxo-4-cyclohexyloxybutyl)amino-7-chloro-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Isobutyl-3(S)-hydroxyl-1-oxo-4-cyclohexyloxybutyl)amino-7-chloro-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Isopropyl-3(S)-hydroxyl-1-oxo-4-cyclohexyloxybutyl)amino-7-chloro-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Methoxy-3(S)-hydroxyl-1-oxo-4-(4-trifluoromethylbenzyloxy)butyl)amino-7-chloro-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Methyl-3(S)-hydroxyl-1-oxo-4-(2,4-difluorobenzyloxy)butyl)amino-7-chloro-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Vinyl-3(S)-hydroxyl-1-oxo-4-benzyloxybutyl)amino-7-chloro-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Methyl-3(S)-hydroxyl-1-oxo-4-cyclohexyloxybutyl)amino-7-chloro-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Isobutyl-3(S)-hydroxyl-1-oxo-5-phenylpentyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Isobutyl-3(S)-hydroxyl-1-oxo-3-cyclopropylpropyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Isobutyl-3(S)-hydroxyl-1-oxo-heptyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(R)-(2(R)-Isobutyl-3(S)-hydroxyl-1-oxo-heptyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(S)-(2(R)-Isobutyl-3(S)-hydroxyl-1-oxo-heptyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Isobutyl-3(S)-hydroxyl-1-oxo-nonyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Isobutyl-3(S)-hydroxyl-1-oxo-hexyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Isobutyl-3(S)-hydroxyl-1-oxo-4-phenylbutyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Methyl-3(S)-hydroxyl-1-oxo-5-phenylpentyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Methyl-3(S)-hydroxyl-1-oxo-6-phenylhexyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Isobutyl-3(S)-hydroxyl-1-oxo-butyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Isobutyl-3(S)-hydroxyl-1-oxo-octyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Methyl-3(S)-hydroxyl-1-oxo-heptyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Methyl-3(S)-hydroxyl-1-oxo-3-phenylpropyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Methyl-3(S)-hydroxyl-1-oxo-5,5-dimethylhexyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Methyl-3(S)-hydroxyl-1-oxo-hexyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2(R)-Methyl-3(S)-hydroxyl-1-oxo-3-(4-propoxyphenyl)propyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
2-(R)-cyclopropylmethyl-3-(S)-hydroxylheptanoic acid (2-oxo-1-(3-phenoxybenzyl)azapan-3-(S)-yl) amide;
2(R)-cyclopropylmethyl-5-(3,5-difluorophenyl)-3-(S)-hydroxypentanoic acid (2-oxo-1-(3-phenoxybenzyl)azapan-3-(S)-yl)amide;
4-cyclopentyl-2-(R)-cyclopropylmethyl-3-(S)-hydroxybutanoic acid (2-oxo-1-(3-phenoxybenzyl)azapan-3-(S)-yl) amide;
2-(R)-cyclopropylmethyl-3-(S)-hydroxyheptanioc acid (1-(5-bromo-3-pyridinyl)methyl-2-oxo-azapan-3-(S)-yl) amide;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-5-(2-fluorophenyl)-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-5-(azapan-1-yl)-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-5-(3,5-difluorophenyl)-3(S)-hydroxyl-1-oxopentyl)amino-1-methyl-5-(pyridn-2-yl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxopentyl)amino-1-methyl-5-(4-chlorophenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-5-(4-methoxyphenyl)l-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-5-(4-methoxyphenyl)-1-methyl-2,3-dihydro-1H-1,4-benxodiazepin-2-one;
3-(S)-(4-cyclopentyl-2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxobutyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(S)-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxohept-6-enyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxohept-6-enyl)amino-1-methyl-5-(4-trifluoromethyl-phenyl)-2,3-dihydro-H-1,4-benzodiazepin-2-one;
3-(S)-(2-(R)-cyclopropylmethyl-5-(3,5-dimethylisoxazol-4-yl)-3-(S)-hydroxyl-1-oxopentyl)amino-1-methyl-5-phenyl-2, 3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-7-chloro-1-methyl-5-phenyl-2, 3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclpropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-(pyridin-2-yl)-2,3-dihydro-1H-1,4 benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-5-(4-fluorophenyl)-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(4-trifouoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(5-cyclopentyl-2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxopentyl)amino-1-methyl-5-(pyridin-2-yl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-iso-butyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(S)-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxo-5-(thiophen-2-yl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(S)-(2-(R)-cyclopropylmethyl-5-(furan-2-yl)3-(S)-hydroxyl-1-oxopentyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(5-cyclopentyl-2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxopentyl)amino-5-(4-fluorophenyl)-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(S)-(2-(R)-cyclopropylmethyl-5-(3,5-difluorophenyl)-3-(S)-hydroxy-1-oxopentyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(S)-(3-(S)-hydroxyl-2-(R)-(thiophen-2-yl)methyl-1-oxoheptyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(S)-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-7-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-7-methoxy-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(S)-(2-(R)-cyclobutylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(S)-(2-(R)-(3,5-difluorobenzyl)-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-phenyl-2,3-dihydor-1H-1,4-benzodiaxepin-2-one;
3-(S)-(2-(R)-(furan-2-yl)methyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxl-1-oxo-5-pheylpentyl)amino-1-methyl-5-(pyridin-2-yl)-2,3-dihydro-1H-benzodiazepin-2-one;
3-(2-(R)-iso-butyl-3-(S)-hydroxyl-1-oxoheptyl)amino-5-(4-fluorophenyl)-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-iso-butyl-3-(S)-hydroxyl-1-oxoheptyl)amino-5-(4-fluorophenyl)-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxo-5-phenylpentyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-5-(furan-2-yl)-3-(S)-hydroxyl-1-oxopentyl)amino-1-methyl-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(5-cyclopentyl-2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxopentyl)amino-1-methyl-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxooctyl)amino-1-methyl-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxononyl)amino-1-methyl-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(4-trifluoromethyl(pyridin-2-yl))-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclobutylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(40trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopentylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(4-methyl-2-pyridiyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(4-methyl-2-pyridyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxobutyl)amino-1-methyl-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(S)-(2-(R)-(3-butenyl)-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(S)-(2-(R)-(3-methylbutyl)3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(S)-(2-(R)-ethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(S)-(2-(R)-propyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-phenyl-2,3-dihydro-1,4-benzodiazepin-2-one;
3-(S)-(2-(R)-butyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(4-(S)-amino-3-(R)-hydroxyl-2-(R)-methyl-1-oxo-5-phenylpentyl)amino-7-chloro-5-(2-fluorophenyl)-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(4-(S)-(tert-butoxycarbonylamino-3-(R)-hydroxyl-2-(R)-methyl-1-oxo-5-phenylpentyl)amino-7-chloro-5-(2-fluorophenyl)-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(3-(tert-butoxycarbonylpyrrolidin-2-(R)-yl)-3-(R)-hydroxyl-2-(R)-methyl-1-oxopropyl)amino-7-chloro-5-(2-fluorophenyl)-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one; 3-(3-(R)-hydroxyl-2-(R)-methyl-1-oxo-3-(pyrrolidin-2-(R)-yl)propyl)-amino-7-chloro-5-(2-fluorophenyl)-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(4-benzyloxy-3-(R)-hydroxyl-2-(R)-iso-propyl-1-oxobutyl-amino-7-chloro-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
2-(4-(S)-amino-3-(S)-hydroxyl-2-(S)-methyl-1-oxo-5-phenylpentyl)amino-7-chloro-5-(2-flourophenyl)-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
2-(4-(S)-(tert-butoxycarbonylamino-3-(S)hydroxyl-2-(S)-methyl-1-oxo-5-phenylpentyl)amino-7-chloro-5-(2-fluorophenyl)-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(thiazol-2-yl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl) amino-1-cyclopropylmethyl-5-(thiazol-2-yl)-2,3-dihydro-1H-1,4benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl) amino-1-cyclopropylmethyl-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-benzyl-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-(3-phenoxybenzyl)-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-(3-pyridinylmethyl)-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(S)-cyclopropylmethyl-3-(R)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(S)-cyclopropylmethyl-3-(R)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(R)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(S)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(S)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-3-(S)-methyl-1-oxoheptyl)amino-1-methyl-5-(4-trifluoromethyl-phenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-(3-phenoxybenzyl)-5-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmehtyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-benzyl-5-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(3-(S)-acetoxy-2-(R)-iso-butyl-1-oxoheptyl)amino-5-(4-fluorophenyl)-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(S)-(5-cyclopentyl-2-(R)-cyclopropylmethyl-3-(S)-methoxy-1-oxopentyl)amino-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
1-(1-hydroxypentyl)cyclohexanecarboxylic acid(5-(4-fluorophenyl)-1-methyl-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)amide;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-5-methyl-5H, 7H-dibenzob,dazepin-6-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxooctyl)amino-5-methyl-5H, 7H-dibenzob,dazepin-6-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxononyl)amino-5-methyl-5H, 7H-dibenzob,dazepin-6-one;
3-(2-(R)-cyclopropylmethyl-5-(furan-2-yl)-3-(S)-hydroxyl-1-oxopentyl)amino-5-methyl-5H, 7H-dibenzob,dazepin-6-one;
2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-heptanoic acid (2-oxo-1-(3-phenylamino-benzyl)azapan-3-(S)-yl) amide;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-5-cyclopentyl-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-5-benzyl-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-5-benzyl-1-butyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-5-cycloheptyl-1-methyl -2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cycloropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-benzyl-5-cycloheptyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-butyl-5-cycloheptyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-(2-pyridinylmethyl)-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-(3-pyridinylmethyl)-5-(2-fluorophenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(S)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxopentyl)amino-1-(3-pyridinylmethyl)-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-1(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(N,N-dibutylamino)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-n-butyl-5-t-butyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-(2-oxo-3,3-dimethylbutyl)-5-n-butyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-benzyl-5-t-butyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-(2-picolyl)-5-n-butyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-Isobutyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-homopiperidino-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-1,3-dioxoheptyl)amino-1-methyl-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one; and
1-pentyrylcyclohexanecarboxylic acid (5-(4-fluorophenyl)-1-methyl-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-3-yl) amide.
22. A compound of claim 21 wherein the stereochemistry of carbon 3 in lactam ring B is of the S configuration.
23. A compound of claim 21 wherein the stereochemistry of carbon 3 in lactam ring B is of the R configuration.
24. A compound of Formula (Ib)
78
wherein:
Ring B is selected from:
79
Q1 is C1-C6 alkyl substituted with 0-3 R1a;
C2-C6 alkenyl substituted with 0-3 R1a;
C2-C6 alkynyl substituted with 0-3 R1a;
C3-C10 cycloalkyl substituted with 0-3 R1b;
C3-C10 carbocycle substituted with 0-3 R1b;
C6-C10 aryl substituted with 0-3 R1b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R1b;
R1a, at each occurrence, is independently selected from H, C1-C6 alkyl, OR14, Cl, F, Br, I, NR15R16, CF3;
C3-C10 carbocycle substituted with 0-3 R1b;
C6-C10 aryl substituted with 0-3 R1b; and
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R1b;
R1b, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, C1-C4 haloalkyl-S-, and (C1-C6 alkyl)-OC(O);
R5 is OR14;
C1-C6 alkyl substituted with 0-3 R5b;
C2-C6 alkenyl substituted with 0-3 R5b; or
C2-C6 alkynyl substituted with 0-3 R5b;
R5a is H, methyl, ethyl, propyl, butyl, or C2-C4 alkenyl;
alternatively, R5 and R5a may be combined to form a C4-C7 cycloalkyl ring;
R5b, at each occurrence, is independently selected from:
H, methyl, ethyl, propyl, butyl, CF3, OR14, Cl, F, Br, I, O, NR15R16,
C3-C7 cycloalkyl substituted with 0-3 R5c;
C3-C7 carbocycle substituted with 0-3 R5c;
phenyl substituted with 0-3 R5c; and
5 to 7 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 7 membered heterocycle is substituted with 0-3 R5c;
R5c, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C4 alkyl, C1-C3 alkoxy, C1-C2 haloalkyl, and C1-C2 haloalkoxy;
W is (CHR8)p;
p is 0 or 1;
R8 is H, methyl, or ethyl;
X is a bond;
phenyl substituted with 0-2 RXb;
C5-C6 cycloalkyl substituted with 0-3 RXb; or
5 to 6 membered heterocycle containing 1 to 3 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-2 RXb;
RXb, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
Y is a bond, V, CH2V, VCH2, or CH2VCH2;
V is a bond, C(O), O, S, S(O), S(O)2, or
N(R19);
Z is H, F, Cl, Br,
C1-C4 alkyl substituted with 0-2 R12;
C2-C4 alkenyl substituted with 0-2 R12;
C2-C4 alkynyl substituted with 0-2 R12;
C6-C10 aryl substituted with 0-4 R12b;
C3-C6 carbocycle substituted with 0-4 R2b; or
5 to 6 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-3 R12b;
R11, at each occurrence, is independently selected from
H, O, NR18R19, C(O)R17, C(O)OR17, C(O)NR18R19,
S(O)2NR18R19, CF3;
C1-C6 alkyl substituted with 0-1 R11a;
phenyl substituted with 0-3 R11b;
C3-C6 carbocycle substituted with 0-3 R11b; or
5 to 7 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 7 membered heterocycle is substituted with 0-3 R11b; wherein said 5 to 7 membered heterocycle is selected from pyridinyl, pyrimidinyl, triazinyl, furanyl, thienyl, thiazolyl, pyrrolyl, piperazinyl, piperidinyl, homopiperidinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, and tetrazolyl;
R11a, at each occurrence, is independently selected from H, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, Cl, F, O, NR15R16, CF3;
phenyl substituted with 0-3 R11b;
C3-C6 carbocycle substituted with 0-3 R11b; or
5 to 7 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 7 membered heterocycle is substituted with 0-3 R11b; wherein said 5 to 7 membered heterocycle is selected from pyridinyl, pyrimidinyl, triazinyl, furanyl, thienyl, thiazolyl, pyrrolyl, piperazinyl, piperidinyl, homopiperidinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, and tetrazolyl;
R11b, at each occurrence, is independently selected from H, OH, Cl, F, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, C1-C2 haloalkyl, and C1-C2 haloalkoxy;
R12 at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, C(O)NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
C6-C10 aryl substituted with 0-4 R12b;
C3-C10 carbocycle substituted with 0-4 R12b; or
5 to 10 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 10 membered heterocycle is substituted with 0-3 R12b;
R12b, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, and C1-C4 haloalkyl-S;
R13, at each occurrence, is independently selected from H, OH, C1-C6 alkyl, C1-C4 alkoxy, Cl, F, Br, I, CN, NO2, NR15R16, and CF3;
R14, at each occurrence, is independently selected from H, phenyl, benzyl, C1-C4 alkyl, and C2-C4 alkoxyalkyl;
R15, at each occurrence, is independently selected from H, methyl, ethyl, propyl, butyl, phenyl, benzyl, and phenethyl;
R16, at each occurrence, is independently selected from H, OH, methyl, ethyl, propyl, butyl, phenyl, benzyl, phenethyl, CH3CH2C(O), CH3C(O), CH3CH2OC(O), CH3OC(O), CH3CH2S(O)2 and CH3S(O)2;
R17 is H, phenyl, benzyl, C1-C4 alkyl, or C2-C4 alkoxyalkyl;
R18, at each occurrence, is independently selected from H, methyl, ethyl, propyl, butyl, phenyl, benzyl, and phenethyl; and
R19, at each occurrence, is independently selected from H, OH, methyl, ethyl, propyl, and butyl.
25. A compound of claim 24 wherein:
Q1 is C1-C6 alkyl substituted with 0-3 R1a;
C2-C6 alkenyl substituted with 0-3 R1a;
C2-C6 alkynyl substituted with 0-3 R1a;
C3-C6 cycloalkyl substituted with 0-3 R1b;
phenyl substituted with 0-3 R1b; or
5 to 6 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-3 R1b;
R1a, at each occurrence, is independently selected from
H, methyl, ethyl, propyl, butyl, OR14, Cl, F, Br, I, NR15R16, CF3;
C3-C6 carbocycle substituted with 0-3 R1b;
phenyl substituted with 0-3 R1b; and
5 to 6 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-3 R1b;
R1b, at each occurrence, is independently selected from H, OH, Cl, F, Br, I, CN, NO2, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, C1-C2 haloalkyl, C1-C2 haloalkoxy, (methyl)OC(O), (ethyl)OC(O), (propyl)OC(O), and (butyl)OC(O);
R5 is OR14;
C1-C4 alkyl substituted with 0-1 R5b;
C2-C4 alkenyl substituted with 0-1 R5b; or
C2-C4 alkynyl substituted with 0-1 R5b;
R5a is H, methyl, ethyl, propyl, or butyl;
alternatively, R5 and R5a may be combined to form a cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl ring;
R5b, at each occurrence, is independently selected from:
H, methyl, ethyl, propyl, butyl, CF3, OR14, Cl, F, O, NR15R16,
C3-C7 cycloalkyl substituted with 0-3 R5c;
C3-C7 carbocycle substituted with 0-3 R5c;
phenyl substituted with 0-3 R5c; and
5 to 7 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 7 membered heterocycle is substituted with 0-3 R5c; wherein said 5 to 7 membered heterocycle is selected from pyridinyl, pyrimidinyl, triazinyl, furanyl, thienyl, thiazolyl, pyrrolyl, piperazinyl, piperidinyl, homopiperidinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, and tetrazolyl;
R5c, at each occurrence, is independently selected from H, OH, Cl, F, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, C1-C2 haloalkyl, and C1-C2 haloalkoxy;
W is a bond, CH2, or CH(CH3);
X is a bond;
phenyl substituted with 0-1 RXb;
C5-C6 cycloalkyl substituted with 0-1 RXb; or
5 to 6 membered heterocycle containing 1 to 3 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-1 RXb; wherein said 5 to 6 membered heterocycle is selected from pyridinyl, pyrimidinyl, triazinyl, furanyl, thienyl, thiazolyl, pyrrolyl, piperazinyl, piperidinyl, pyrazolyl, imidazolyl, oxazolyl, and isoxazolyl;
Rxb, at each occurrence, is independently selected from H, OH, Cl, F, Br, NR15R16 CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, C1-C2 haloalkyl, and C1-C2 haloalkoxy;
Y is a bond, V, VCH2, or CH2V;
V is a bond, C(O), O, S, S(O), S(O)2, or N(R19);
Z is H, F, Cl, Br,
C1-C4 alkyl substituted with 0-2 R12;
C2-C4 alkenyl substituted with 0-2 R12;
C2-C4 alkynyl substituted with 0-2 R12;
C6-C10 aryl substituted with 0-4 R12b;
C3-C6 carbocycle substituted with 0-4 R12b; or
5 to 6 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-3 R12b;
R11, at each occurrence, is independently selected from H, NR18R19, CF3;
C1-C4 alkyl substituted with 0-1 R11a;
phenyl substituted with 0-3 R11b;
C3-C6 carbocycle substituted with 0-3 R11b; or
5 to 7 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 7 membered heterocycle is substituted with 0-3 R11b; wherein said 5 to 7 membered heterocycle is selected from pyridinyl, pyrimidinyl, triazinyl, furanyl, thienyl, thiazolyl, pyrrolyl, piperazinyl, piperidinyl, homopiperidinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, and tetrazolyl;
R11a, at each occurrence, is independently selected from H, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, Cl, F, O, NR15R16, CF3;
phenyl substituted with 0-3 R11b;
C3-C6 carbocycle substituted with 0-3 R11b; or
5 to 7 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 7 membered heterocycle is substituted with 0-3 R11b; wherein said 5 to 7 membered heterocycle is selected from pyridinyl, pyrimidinyl, triazinyl, furanyl, thienyl, thiazolyl, pyrrolyl, piperazinyl, piperidinyl, homopiperidinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, and tetrazolyl;
R11b, at each occurrence, is independently selected from H, OH, Cl, F, NR15R16, CF3, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, C1-C2 haloalkyl, and C1-C2 haloalkoxy;
R12 at each occurrence, is independently selected from H, OH, Cl, F, Br, NR15R16, C(O)NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, C1-C2 haloalkyl, and C1-C2 haloalkoxy;
phenyl substituted with 0-4 R12b;
C3-C6 carbocycle substituted with 0-4 R12b; or
5 to 6 membered heterocycle containing 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulphur, wherein said 5 to 6 membered heterocycle is substituted with 0-3 R12b;
R12b, at each occurrence, is independently selected from H, OH, Cl, F, Br, NR15R16, CF3, acetyl, SCH3, S(O)CH3, S(O)2CH3, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, C1-C2 haloalkyl, and C1-C2 haloalkoxy;
R13, at each occurrence, is independently selected from H, OH, methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, Cl, F, Br, CN, NR15R16, and CF3;
R14, at each occurrence, is independently selected from H, phenyl, benzyl, methyl, ethyl, propyl, and butyl;
R15, at each occurrence, is independently selected from H, methyl, ethyl, propyl, or butyl;
R16, at each occurrence, is independently selected from H, OH, methyl, ethyl, propyl, butyl, phenyl, benzyl, and phenethyl;
R18, at each occurrence, is independently selected from H, methyl, ethyl, propyl, butyl, phenyl, benzyl and, phenethyl; and
R19, at each occurrence, is independently selected from H, OH, methyl, ethyl, propyl, butyl, phenyl, benzyl and, phenethyl.
26. A compound of claim 25 wherein:
Q1 is CH3, CH2CH3, CH2CH2CH3, CH2CH2CH2CH3, CH2CH2CH2CH2CH3, CH2CH2CH2CH2CH2CH3, CH(CH3)2, CH(CH3)CH2CH3, CH2CH(CH3)2, CH2C(CH3)3,
CF3, CH2CF3, CH2CH2CF3, CH2CH2CH2CF3,
CHCH2, CH2CHCH2, CH2C(CH3)CH2, CH2CHC(CH3)2, CH2CH2CHCH2, CH2CH2C(CH3)CH2, CH2CH2CHC(CH3)2, cis-CH2CHCH(CH3), cis-CH2CH2CHCH(CH3), trans-CH2CHCH(CH3), trans-CH2CH2CHCH(CH3);
CCH, CH2CCH, CH2CC(CH3),
cyclopropyl-, cyclobutyl-, cyclopentyl-, cyclohexyl-, cyclopropyl-CH2, cyclobutyl-CH2, cyclopentyl-CH2, cyclohexyl-CH2, cyclopropyl-CH2CH2, cyclobutyl-CH2CH2, cyclopentyl-CH2CH2, cyclohexyl-CH2CH2,
phenyl-, 2-F-phenyl-, 3-F-phenyl-, 4-F-phenyl-, 4-methoxyphenyl-,4-ethoxyphenyl-, 4-propoxyphenyl-, phenyl-CH2, (2-F-phenyl)CH2, (3-F-phenyl)CH2, (4-F-phenyl)CH2, (2-Cl-phenyl)CH2, (3-Cl-phenyl)CH2, (4-Cl-phenyl)CH2,
(2,3-diF-phenyl)CH2, (2,4-diF-phenyl)CH2, (2,5-diF-phenyl)CH2, (2,6-diF-phenyl)CH2, (3,4-diF-phenyl)CH2, (3,5-diF-phenyl)CH2, (2,3-diCl-phenyl)CH2, (2,4-diCl-phenyl)CH2, (2,5-diCl-phenyl)CH2, (2,6-diCl-phenyl)CH2, (3,4-diCl-phenyl)CH2, (3,5-diCl-phenyl)CH2, (3-F-4-Cl-phenyl)CH2, (3-F-5-Cl-phenyl)CH2, (3-Cl-4-F-phenyl)CH2,
2-furanyl-CH2, 3-furanyl-CH2, 2-thienyl-CH2, 3-thienyl-CH2, 2-pyridyl-CH2, 3-pyridyl-CH2, 4-pyridyl-CH2, 1-imidazolyl-CH2, 2-oxazolyl-CH2, 4-oxazolyl-CH2, 5-oxazolyl-CH2, 3-isoxazolyl-CH2, 4-isoxazolyl-CH2, 5-isoxazolyl-CH2,
phenyl-CH2CH2, (2-F-phenyl)CH2CH2, (3-F-phenyl)CH2CH2, (4-F-phenyl)CH2CH2, (2-Cl-phenyl)CH2CH2, (3-Cl-phenyl)CH2CH2, (4-Cl-phenyl)CH2CH2, (2,3-diF-phenyl)CH2CH2, (2,4-diF-phenyl)CH2CH2, (2,5-diF-phenyl)CH2CH2, (2,6-diF-phenyl)CH2CH2, (3,4-diF-phenyl)CH2CH2, (3,5-diF-phenyl)CH2CH2, (2,3-diCl-phenyl)CH2CH2, (2,4-diCl-phenyl)CH2CH2, (2,5-diCl-phenyl)CH2CH2, (2,6-diCl-phenyl)CH2CH2, (3,4-diCl-phenyl)CH2CH2, (3,5-diCl-phenyl)CH2CH2, (3-F-4-Cl-phenyl)CH2CH2, (3-F-5-Cl-phenyl)CH2CH2;
furanyl-CH2CH2, thienyl-CH2CH2, pyridyl-CH2CH2, 1-imidazolyl-CH2CH2, oxazolyl-CH2CH2, isoxazolyl-CH2CH2, 3,5-dimethylisoxazol-4-yl-CH2CH2, phenyl-propyl-;
benzyl-CH(NH2), benzyl-CH(NHC(O)O-tBu)-, benzyloxy-CH2, pyrrolidin-2-yl-, or 3-t-butoxycarbonylpyrrolidin-2-yl-;
R5 is CH3, CH2CH3, CH2CH2CH3, CH(CH3)2, CH2CH2CH2CH3, CH(CH3)CH2CH3, CH2CH(CH3)2, CH2C(CH3)3, CH2CH2CH2CH2CH3, CH(CH3)CH2CH2CH3, CH2CH(CH3)CH2CH3, CH2CH2CH(CH3)2, CH(CH2CH3)2,
CF3, CH2CF3, CH2CH2CF3, CH2CH2CH2CF3, CH2CH2CH2CF3,
CHCH2, CH2CHCH2, CH2CH2CHCH2, CHCHCH3, cis-CH2CHCH(CH3), trans-CH2CHCH(CH3), trans-CH2CHCH(C6H5), CH2CHC(CH3)2, cis-CH2CHCHCH2CH3, trans-CH2CHCHCH2CH3, cis-CH2CH2CHCH(CH3), trans-CH2CH2CHCH(CH3), trans-CH2CHCHCH2(C6H5),
CCH, CH2CCH, CH2CC(CH3), CH2CC(C6H5), CH2CH2CCH, CH2CH2CC(CH3), CH2CH2CC(C6H5), CH2CH2CH2CCH, CH2CH2CH2CC(CH3), CH2CH2CH2CC(C6H5),
cyclopropyl-CH2, cyclobutyl-CH2, cyclopentyl-CH2, cyclohexyl-CH2, (2-CH3-cyclopropyl)CH2, (3-CH3-cyclobutyl)CH2, cyclopropyl-CH2CH2, cyclobutyl-CH2CH2, cyclopentyl-CH2CH2, cyclohexyl-CH2CH2, (2-CH3-cyclopropyl)CH2CH2, (3-CH3-cyclobutyl)CH2CH2,
phenyl-CH2, (2-F-phenyl)CH2, (3-F-phenyl)CH2, (4-F-phenyl)CH2, (3,5-diF-phenyl)CH2, 2-furanyl-CH2, 3-furanyl-CH2, 2-thienyl-CH2, 3-thienyl-CH2, 2-pyridyl-CH2, 3-pyridyl-CH2, 4-pyridyl-CH2, 1-imidazolyl-CH2, 2-oxazolyl-CH2, 4-oxazolyl-CH2, 5-oxazolyl-CH2, 3-isoxazolyl-CH2, 4-isoxazolyl-CH2, 5-isoxazolyl-CH2,
phenyl-CH2CH2, (2-F-phenyl)CH2CH2, (3-F-phenyl)CH2CH2, (4-F-phenyl)CH2CH2, furanyl-CH2CH2, thienyl-CH2CH2, pyridyl-CH2CH2, 1-imidazolyl-CH2CH2, oxazolyl-CH2CH2, isoxazolyl-CH2CH2;
methoxy, ethoxy, propoxy, or butoxy;
R5a is H;
alternatively, R5 and R5a may be combined to form cyclopentyl, cyclohexyl, or cycloheptyl;
W is a bond, CH2, or CH(CH3);
X is a bond;
80
Y is a bond, CH2V, V, or VCH2;
V is a bond, C(O), O, S, S(O), S(O)2, NH, or N(CH3);
Z is H, F, Cl, Br, methyl, ethyl, n-propyl, i-propyl, n-butyl, i-butyl, s-butyl, t-butyl,
cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl,
phenyl, 2-F-phenyl, 3-F-phenyl, 4-F-phenyl, 2-Cl-phenyl, 3-Cl-phenyl, 4-Cl-phenyl, 2,3-diF-phenyl, 2,4-diF-phenyl, 2,5-diF-phenyl, 2,6-diF-phenyl, 3,4-diF-phenyl, 3,5-diF-phenyl, 2,3-diCl-phenyl, 2,4-diCl-phenyl, 2,5-diCl-phenyl, 2,6-diCl-phenyl, 3,4-diCl-phenyl, 3,5-diCl-phenyl, 3-F-4-Cl-phenyl, 3-F-5-C1-phenyl, 3-Cl-4-F-phenyl, 2-MeO-phenyl, 3-MeO-phenyl, 4-MeO-phenyl, 2-Me-phenyl, 3-Me-phenyl, 4-Me-phenyl, 2-MeS-phenyl, 3-MeS-phenyl, 4-MeS-phenyl, 2-CF3O-phenyl, 3-CF3O-phenyl, 4-CF3O-phenyl,
furanyl, thienyl, pyridyl, 2-Me-pyridyl, 3-Me-pyridyl, 4-Me-pyridyl, 1-imidazolyl, oxazolyl, isoxazolyl, 1-benzimidazolyl, morpholino, N-piperinyl,
phenyl-CH2, (2-F-phenyl)CH2, (3-F-phenyl)CH2, (4-F-phenyl)CH2, (2-C1-phenyl)CH2, (3-Cl-phenyl)CH2, (4-Cl-phenyl)CH2, (2,3-diF-phenyl)CH2, (2,4-diF-phenyl)CH2, (2,5-diF-phenyl)CH2, (2,6-diF-phenyl)CH2, (3,4-diF-phenyl)CH2, (3,5-diF-phenyl)CH2, (2,3-diCl-phenyl)CH2, (2,4-diCl-phenyl)CH2, (2,5-diCl-phenyl)CH2, (2,6-diCl-phenyl)CH2, (3,4-diCl-phenyl)CH2, (3,5-diCl-phenyl)CH2, (3-F-4-Cl-phenyl)CH2, (3-F-5-Cl-phenyl)CH2, (3-Cl-4-F-phenyl)CH2, (2-MeO-phenyl)CH2, (3-MeO-phenyl)CH2, (4-MeO-phenyl)CH2, (2-PhO-phenyl)CH2, (3-PhO-phenyl)CH2, (4-PhO-phenyl)CH2, (2-Me-phenyl)CH2, (3-Me-phenyl)CH2, (4-Me-phenyl)CH2, (2-MeS-phenyl)CH2, (3-MeS-phenyl)CH2, 4-MeS-phenyl)CH2, (2-CF3O-phenyl)CH2, (3-CF3O-phenyl)CH2, (4-CF3O-phenyl)CH2, (furanyl)CH2, (thienyl)CH2, (pyridyl)CH2, (2-Me-pyridyl)CH2, (3-Me-pyridyl)CH2, (4-Me-pyridyl)CH2, (1-imidazolyl)CH2, (oxazolyl)CH2, (isoxazolyl)CH2, (1-benzimidazolyl)CH2, (cyclopropyl)CH2, (cyclobutyl)CH2, (cyclopentyl)CH2, (cyclohexyl)CH2, (morpholino)CH2, (N-pipridinyl)CH2,
phenyl-CH2CH2, (phenyl)2CHCH2, (2-F-phenyl)CH2CH2, (3-F-phenyl)CH2CH2, (4-F-phenyl)CH2CH2, (2-Cl-phenyl)CH2CH2, (3-Cl-phenyl)CH2CH2, (4-Cl-phenyl)CH2CH2, (2,3-diF-phenyl)CH2CH2, (2,4-diF-phenyl)CH2CH2, (2,5-diF-phenyl)CH2CH2, (2,6-diF-phenyl)CH2CH2, (3,4-diF-phenyl)CH2CH2, (3,5-diF-phenyl)CH2CH2, (2,3-diCl-phenyl)CH2CH2, (2,4-diCl-phenyl)CH2CH2, (2,5-diCl-phenyl)CH2CH2, (2,6-diCl-phenyl)CH2CH2, (3,4-diCl-phenyl)CH2CH2, (3,5-diCl-phenyl)CH2CH2, (3-F-4-Cl-phenyl)CH2CH2, (3-F-5-Cl-phenyl)CH2CH2, (3-Cl-4-F-phenyl)CH2CH2, (2-MeO-phenyl)CH2CH2, (3-MeO-phenyl)CH2CH2, (4-MeO-phenyl)CH2CH2, (2-Me-phenyl)CH2CH2, (3-Me-phenyl)CH2CH2, (4-Me-phenyl)CH2CH2, (2-MeS-phenyl)CH2CH2, (3-MeS-phenyl)CH2CH2, (4-MeS-phenyl)CH2CH2, (2-CF3O-phenyl)CH2CH2, (3-CF3O-phenyl)CH2CH2, (4-CF3O-phenyl)CH2CH2, (furanyl)CH2CH2, (thienyl)CH2CH2, (pyridyl)CH2CH2, (2-Me-pyridyl)CH2CH2, (3-Me-pyridyl)CH2CH2, (4-Me-pyridyl)CH2CH2, (imidazolyl)CH2CH2, (oxazolyl)CH2CH2, (isoxazolyl)CH2CH2, (benzimidazolyl)CH2CH2, (cyclopropyl)CH2CH2, (cyclobutyl)CH2CH2, (cyclopentyl)CH2CH2, (cyclohexyl)CH2CH2, (morpholino)CH2CH2, or (N-pipridinyl)CH2CH2;
R11, at each occurrence, is independently selected from H, methyl, ethyl, n-propyl, i-propyl, n-butyl, i-butyl, s-butyl, t-butyl, phenyl, benzyl, phenethyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, cycloheptylmethyl, cyclopropylethyl, cyclobutylethyl, cyclopentylethyl, cyclohexylethyl, 2-F-phenyl-, 3-F-phenyl, 4-F-phenyl, 4-Cl-phenyl, 4-CH3-phenyl, 4-MeO-phenyl-, 4-CF3-phenyl, (4-F-phenyl)CH2, (4-Cl-phenyl)CH2, (4-CH3-phenyl)CH2, (4-CF3-phenyl)CH2, (4-F-phenyl)CH2CH2, (4-Cl-phenyl)CH2CH2, (4-CH3-phenyl)CH2CH2, (4-CF3-phenyl)CH2CH2, pyridin-2-yl-, pyridin-3-yl-, 4-CF3-pyridin-2-yl-, 4-CH3-pyridin-2-yl-, thiazol-2-yl-, azapan-1-yl, N,N-dimethylamino, N,N-diethylamino, N,N-dipropylamino, and N,N-dibutylamino; and
R13, at each occurrence, is independently selected from H, MeO, F, and Cl.
27. A compound, according to claim 24, of Formula (If);
81
or a pharmaceutically acceptable salt form or prodrug thereof.
28. A compound, according to claim 25, of Formula (If);
82
or a pharmaceutically acceptable salt form or prodrug thereof.
29. A compound, according to claim 26, of Formula (If);
83
or a pharmaceutically acceptable salt form or prodrug thereof.
30. A compound, according to claim 24, of Formula (Ig);
84
or a pharmaceutically acceptable salt form or prodrug thereof.
31. A compound, according to claim 25, of Formula (Ig);
85
or a pharmaceutically acceptable salt form or prodrug thereof.
32. A compound, according to claim 26, of Formula (Ig);
86
or a pharmaceutically acceptable salt form or prodrug thereof.
33. A compound, according to claim 24, of Formula (Ih);
87
or a pharmaceutically acceptable salt form or prodrug thereof.
34. A compound, according to claim 25, of Formula (Ih);
88
or a pharmaceutically acceptable salt form or prodrug thereof.
35. A compound, according to claim 26, of Formula (Ih);
89
or a pharmaceutically acceptable salt form or prodrug thereof.
36. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.
37. A method for the treatment of neurological disorders associated with -amyloid production comprising administering to a host in need of such treatment a therapeutically effective amount of a compound of claim 1.
38. A method for inhibiting -secretase activity comprising administering to a host in need of such inhibition a therapeutically effective amount of a compound of claim 1 that inhibits -secretase activity.
39. A compound, according to claim 5, of Formula (Ii);
90
or a pharmaceutically acceptable salt form or prodrug thereof.
40. A compound, according to claim 6, of Formula (Ii);
91
or a pharmaceutically acceptable salt form or prodrug thereof.
41. A compound, according to claim 5, of Formula (Ij);
92
or a pharmaceutically acceptable salt form or prodrug thereof.
42. A compound, according to claim 6, of Formula (Ij);
93
or a pharmaceutically acceptable salt form or prodrug thereof.
43. A compound, according to claim 5, of Formula (Ik);
94
or a pharmaceutically acceptable salt form or prodrug thereof.
44. A compound, according to claim 6, of Formula (Ik);
95
or a pharmaceutically acceptable salt form or prodrug thereof.
45. A compound of claim 1 or a pharmaceutically acceptable salt form or prodrug thereof, is selected from:
(2R,3S)-N-1-butyl-5-(methylethyl)-2-oxo(3H-benzof1,4-diazepin-3-yl)-2-(cyclopropylmethyl)-3-hydroxyheptanamide;
(2R,3S)-2-(cyclopropylmethyl)-3-hydroxy-N-5-(methylethyl)-2-oxo-1-benzyl(3H-benzof1,4-diazepin-3-yl)heptanamide;
(2R,3S)-2-(cyclopropylmethyl)-3-hydroxy-N-5-methyl-1-(3-(4-methylphenyl)sulfonylaminophenyl)-methyl-2-oxo(3H-benzof1,4-diazepin-3-yl)heptanamide;
3-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-t-butyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
(2R,3S)-2-(cyclopropylmethyl)-3-hydroxy-N-1-(3-(4-methylphenyl)sulfonylaminophenyl)methyl-2-oxo(3H,4H,5H-benzof1,4-diazaperhydroepin-3-yl)heptanamide;
3-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-piperizinyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
7-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-5-(2-diethylaminoethyl)-6,7-dihydro-5H-dibenzoazepin-6-one;
7-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-5-(3-hydroxypropyl)-6,7-dihydro-5H-dibenzoazepin-6-one;
3-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-(benzyl-5-(2,2-dimethylpropyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-n-butyl-5-n-butyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-benzyl-5-n-butyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(3,4-dihydro-1H-isoquinolin-2-yl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(2,2-dimethylpropyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
7-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-5-n-butyl-6,7-dihydro-5H-dibenzoazepin-6-one;
3-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl) amino-1-(2-ethylbutyl)-5-n-butyl-2, 3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-pyrrolidin-1-yl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
7-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl) amino-5-benzyl-6,7-dihydro-5H-dibenzoazepin-6-one;
3-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-ethoxy-2, 3-dihydro-H-1,4-benzodiazepin-2-one;
3-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-butyl-5-(2,2-dimethylpropyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-(2-pyridinylmethyl N-oxide)-5-(4-trifluoromethyl)phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-(3-pyridinylmethyl N-oxide)-5-(4-trifluoromethyl)phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(S)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxopentyl)amino-1-(3-pyridinylmethyl)-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-(2-(diethylamino)ethyl)-5-(4-trifluoromethylphenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxopentyl)amino-1-(3-pyridinylmethyl N-oxide)-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
(2R,3S)-N-(8-bromo-1,5-dimethyl-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)-2-(cyclopropylmethyl)-3-hydroxyheptanamide;
6-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1,4-dibenzyl-hexahydro-5H-1,4-diazepin-5-one;
6-(2-(R)-cyclopropylmethyl-3-(S)-hydroxy-1-oxohetptyl)amino-4-benzyl-1-(4-chlorophenyl)sulfonyl-hexahydro-5H-1,4-diazepin-5-one;
6-(2-(R)-cyclopropylmethyl-3-(S)-hydroxy-1-oxopentyl)amino-4-benzyl-1-(4-chlorophenyl)sulfonyl-hexahydro-5H-1,4-diazepin-5-one;
(2R,3S)-2-(cyclopropylmethyl)-N-(1-3-(4-fluorophenoxy)phenylmethyl-2-oxo(3H,4H,5H-benzofazaperhydroepin-3-yl))-3-hydroxyheptanamide;
(2R,3S)-2-(cyclopropylmethyl)-3-hydroxy-N-2-oxo-1-benzyl(3H,4H,5H-benzofazaperhydroepin-3-yl)heptanamide;
3-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(4-benzylpiperizin-1-yl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(4-methanesulfonyl-piperazin-1-yl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(4-methylpiperazin-1-yl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(4-acetylpiperazin-1-yl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(4-(3,5-dimethyl-isoxazole-4-sulfonyl)-piperazin-1-yl-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
3-(R,S)-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(4-benzoylpiperazin-1-yl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one;
4-3-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxy-heptanoylamino)-1-methyl-2-oxo-2,3-dihydro-1H-benzoe1,4diazepin-5-yl-piperazine-1-carboxylic acid tert-butyl ester; and
3-(2-(R)-cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-(3-pyridinylmethyl N-oxide)-5-(4-trifluoromethyl)phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one-4-N-oxide.