What is claimed is:
1. A sunshade arrangement for a transparent part of a motor vehicle, the sunshade arrangement comprising:
at least one sunshade element which is adapted for mounting on the transparent part, the at least one sunshade element being extendable in a lengthwise direction to an extent corresponding to a distance to at least one of a front edge and a rear edge of the transparent part;
wherein the at least one sunshade element is movable in said lengthwise direction both in an at least partially extended position and also in a retracted position.
2. The sunshade arrangement as claimed in claim 1, wherein the at least one sunshade element is attached to a cross member which is movable in said lengthwise direction in an installed condition on a motor vehicle.
3. The sunshade arrangement as claimed in claim 2, wherein the at least one sunshade element comprises first and second extendible sunshade elements, the second extendible sunshade element being provided for covering a part of the transparent motor vehicle part which is uncovered by the first extendible sunshade element and being supported on one of a front edge and a rear edge of the cross member.
4. The sunshade arrangement as claimed in claim 2, further comprising a drive for moving said at least one sunshade element and the cross member.
5. The sunshade arrangement as claimed in claim 1, wherein a drive is provided which extends or retracts the at least one sunshade element.
6. The sunshade arrangement as claimed in claim 2, wherein one of the cross member and the at least one sunshade element is adapted to be movably supported on at least one of the front edge and rear edge of the transparent motor vehicle part.
7. The sunshade arrangement as claimed in claim 1, wherein the at least one sunshade element is divided in a transverse direction of the transparent motor vehicle part into at least two independent sunshade component elements.
8. The sunshade arrangement as claimed in claim 3, wherein the cross member is movable both with the at least one sunshade element in the extended position and also with the at least one sunshade element accommodated on the cross member.
9. The sunshade arrangement as claimed in claim 2, wherein the cross member is sized to match to the transparent motor vehicle part.
10. The sunshade arrangement as claimed in claim 2, wherein the cross member comprises two legs, the two legs having leg ends which are movably supported, and a middle section of the cross member being located higher than the leg ends.
11. The sunshade arrangement as claimed in claim 10, wherein a sunshade element is provided on each leg of the cross member.
12. A motor vehicle roof with a sunshade arrangement and a transparent roof section, the sunshade arrangement comprising:
at least one sunshade element which is located under the roof section, the at least one sunshade element being extendible to at least one of a front edge and a rear edge of a roof cutout containing the transparent roof section;
wherein the at least one sunshade element is movable in a lengthwise direction of the motor vehicle, both in an at least partially extended position and also in a retracted position.
13. The motor vehicle roof as claimed in claim 12, wherein the roof section is a fixed glass roof.
14. The motor vehicle roof as claimed in claim 12, wherein the roof section has at least one openable transparent cover.
15. The motor vehicle roof as claimed in claim 12, wherein the at least one sunshade element is attached to a cross member which is movable in the lengthwise direction of the motor vehicle.
16. The motor vehicle roof as claimed in claim 15, wherein the cross member is movably supported on side guide rails of the motor vehicle roof.
17. The motor vehicle roof as claimed in claim 15, wherein the cross member and the at least one sunshade element are removable as a unit from the motor vehicle roof.
18. The motor vehicle roof as claimed in claim 12, wherein the at least one sunshade element is divided in a transverse direction of the transparent motor vehicle part into at least two independent sunshade component elements.
19. The motor vehicle roof as claimed in claim 18, wherein at least one of the component elements is a pull-out shade or an awning.
The claims below are in addition to those above.
All refrences to claim(s) which appear below refer to the numbering after this setence.
1. A compound having formula I
or a pharmaceutically acceptable salt thereof, wherein
A1 is R1 or R2, wherein A1 is unsubstituted or substituted with one or two OH, CN, C1-alkyl, C2-alkyl, C3-alkyl, C4-alkyl, C5-alkyl, cycloalkane, ORA or NRARA;
RA is H or alkyl;
R1 is cycloalkane or cycloalkene each of which is unfused or fused with R1A;
R1A is benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R2 is heterocycloalkane or heterocycloalkene; each of which is unfused or fused with R2A;
R2A is benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
A2 is OR4, NHR4, N(R4)2, SR4, S(O)R4, SO2R4 or R5;
wherein each R4 is C1-alkyl, C2-alkyl or C3-alkyl; each of which is substituted with
R5 is C1-alkyl, C2-alkyl, C3-alkyl, C4-alkyl or C5-alkyl; each of which is substituted with R10, and further unsubstituted or substituted with one or two or three of independently selected OR10, NHR10, N(R10)2, SR10, S(O)R10, SO2R10 or CF3;
wherein each R10 is R10A, R10B or R10C; each of which must be attached at a carbon atom;
R10A is phenyl which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which are unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which are unfused or fused with benzene. heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R10C is cycloalkyl, cycloalkenyl, heterocycloalkyl or heterocycloalkenyl; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
wherein each R10 is independently unsubstituted or substituted with one or two or three of independently selected, R11, OR11, SR11, S(O)R11, SO2R11, NH2, NHR11, N(R11)2, C(O)R11, C(O)OR11, C(O)NH2, C(O)NHR11, C(O)N(R11)2, NHC(O)R11, NR11C(O)R11, NHSO2R11, NR11SO2R11, NHC(O)OR11, NR11C(O)OR11, NHSO2NH2, NHSO2NHR11. NHSO2N(R11)2, SO2NH2, SO2NHR11, SO2N(R11)2, NHC(O)NH2, NHC(O)NH R11, NHC(O)N(R11)2, NR11C(O)N(R11)2, NO2, OH, (O), C(O)H, C(O)OH, CN, CF3, OCF3, CF2CF3, F, Cl, Br or I;
wherein each R11 is R12, R13, R14 or R15;
R12 is phenyl which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R13 is heteroaryl which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R14 is cycloalkyl, cycloalkenyl, heterocycloalkyl or heterocycloalkenyl; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R15 is alkyl, alkenyl or alkynyl; each of which is unsubstituted or substituted with one or two of independently selected R16, OR16, SR16, S(O)2R16, C(O)OH, NH2, NHR16 N(R16)2, C(O)R16, C(O)NH2, C(O)NHR16, C(O)N(R16)2, NHC(O)R16, NR16C(O)R16, NHC(O)OR16, NR16C(O)OR16, OH, F, Cl, Br or I;
wherein each R16 is R17 or R17A;
R17 is alkyl, alkenyl or alkynyl; each of which is unsubstituted or substituted with one or two of independently selected R18, C(O)OH, NH2, NHR18 or N(R18)2, C(O)R18, C(O)NH2, C(O)NHR16, C(O)N(R13)2, NHC(O)R18, NR18C(O)R18, F, Cl, Br or I;
R17A is phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
wherein each R18 is phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl or heterocycloalkenyl;
wherein each of the moieties represented by R12, R13, R14, R17A, and R18 are independently unsubstituted or substituted with one or two or three or four of independently selected R19, OR19, SR19, S(O)R19, SO2R19, C(O)R19, CO(O)R19, OC(O)R19, OC(O)R19, NH2, NHR19, N(R19)2, NHC(O)R19, NR19C(O)R19, NHS(O)2R19, NR19S(O)2R19, NHC(O)OR19, NR19C(O)OR19, NHC(O)NH2, NHC(O)NHR19, NHC(O)N(R19)2, NR19C(O)NHR19, NR19C(O)N(R19)2, C(O)NH2, C(O)NHR19, C(O)N(R19)2, C(O)NHOH, C(O)NHOR19, C(O)NHSO2R19, C(O)NR19SO2R19, SO2NH2, SO2NHR19, SO2N(R19)2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR19, C(N)N(R19)2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I;
wherein each R19 is R20, R21, R22 or R23;
R20 is phenyl which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R21 is heteroaryl which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R22 is cycloalkyl, cycloalkenyl, heterocycloalkyl or heterocycloalkenyl; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R23 is alkyl, alkenyl or alkynyl; each of which is unsubstituted or substituted with one or two of independently selected R24, OR24, SR24, S(O)2R24, C(O)OH, NH2, NHR24 N(R24)2, C(O)R24, C(O)NH2, C(O)NHR24, C(O)N(R24)2, NHC(O)R24, NR24C(O)R24, NHC(O)OR24, NR24C(O)OR24, NHS(O)2R24, NR24S(O)2R24, OH, F, Cl, Br or I;
wherein each R24 is R24A or R24B;
R24A is phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl or heterocycloalkenyl each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R24B is alkyl, alkenyl or alkynyl each of which is unsubstituted or substituted with one or two of independently selected R25, OR25, SR25, S(O)2R25, C(O)OH, NH2, NHR25N(R25)2, C(O)R25, C(O)NH2, C(O)NHR25, C(O)N(R25)2, NHC(O)R25, NR25C(O)R25, NHC(O)OR25, NR25C(O)OR25, OH, F, Cl, Br or I;
wherein each R25 is alkyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl or heterocycloalkenyl; each of which is unsubstituted or substituted with NH2, NH(CH3), N(CH3)2, OH or OCH3;
wherein each of the moieties represented by R20, R21, R22, and R24A are independently unsubstituted or substituted with one or two of independently selected R26, OR26, alkenyl, alkynyl, phenyl, OH, (O), C(O)OH, CN, CF3, OCF3, CF2CF3, F, Cl, Br or I; and
R26 is alkyl.
2. The compound of claim 1, wherein A1 is unsubstituted R1 or unsubstituted R2;
R1 is cycloalkane, which is unfused;
R2 is heterocycloalkane, which is unfused; and
A2 is R5;
or a pharmaceutically acceptable salt thereof
3. The compound of claim 2, wherein A1 is unsubstituted R1; and
R1 is cyclohexane, which is unfused;
or a pharmaceutically acceptable salt thereof.
4. The compound of claim 3, wherein R5is C1-alkyl, C2-alkyl or C3-alkyl;
or a pharmaceutically acceptable salt thereof.
5. The compound of claim 4, wherein
R10A is phenyl which is unfused or fused with heterocycloalkane, which is fused heterocycloalkane;
R10B is
R10C is heterocycloalkyl, which is unfused;
wherein R10 is substituted with F and further unsubstituted or substituted with one or two of independently selected R11, OR11, SR11, S(O)R11, SO2R11, NH2, N(R11)2, C(O)R11, C(O)OR11, C(O)NHR11, C(O)N(R11)2, NHC(O)R11, NHSO2R11, NR11SO2R11, NHC(O) OR11, NHSO2N(R11)2, NO2, OH, (O), C(O)OH, F, Cl or Br;
wherein each R11 is R12, R13, R14 or R15;
R12 is phenyl which is unfused or fused with benzene, heteroarene, heterocycloalkane or heterocycloalkene;
R13 is heteroaryl, which is unfused;
R14 is cycloalkyl, heterocycloalkyl or heterocycloalkenyl; each of which is unfused or fused with benzene, cycloalkane, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene;
R15 is alkyl which is unsubstituted or substituted with one or two of independently selected R16, OR16, SR16, S(O)2R16, C(O)OH, NH2, NHR16N(R16)2, C(O)R16, C(O)NHR16, NHC(O)R16, NHC(O)OR16, OH, F, Cl, Br or I;
wherein each R16 is R17 or R17A;
R17 is alkyl which is unsubstituted or substituted with R18;
R17A is phenyl, heteroaryl, cycloalkyl, heterocycloalkyl or heterocycloalkenyl each of which is unfused or fused with benzene or heterocycloalkane;
R18 is phenyl or heterocycloalkyl, which is unfused;
wherein the moieties represented by R12, R13, R14, R17A, and R18 are independently unsubstituted or substituted with one or two of independently selected R19, OR19, SR19, SO2R19, C(O)R19, CO(O)R19, NHR19, N(R19)2, NHC(O)R19, NHS(O)2R19, C(O)NH2, C(O)NHR19, C(O)N(R19)2, C(O)H, OH, (O), CN, CF3, F, Cl, Br or I;
wherein each R19 is R20, R21, R22 or R23;
R20 is phenyl, which is unfused;
R21 is heteroaryl, which is unfused;
R22 is cycloalkyl or heterocycloalkyl; each of which is unfused or fused with benzene:
R23 is alkyl which is unsubstituted or substituted with R24, OR24, NHR24 N(R24)2, NHS(O)2R24 or OH;
wherein each R24 is R24A or R24B;
R24A is phenyl, cycloalkyl, heterocycloalkyl or heterocycloalkenyl, which is unfused or fused with heterocycloalkane;
R24B is alkyl, which is unsubstituted or substituted with OR25, OH, F, Cl, Br or I;
R25 is alkyl, which is unsubstituted or substituted with NH2;
wherein the moieties represented by R20, R21, R22, and R24A are independently unsubstituted or substituted with one or two of independently selected R26, OR26 (O), F, Cl, Br or I; and
R26 is alkyl;
or a pharmaceutically acceptable salt thereof.
6. The compound of claim 4, wherein R10 is phenyl which is unfused;
or a pharmaceutically acceptable salt thereof.
7. The compound of claim 6, wherein R10 is substituted with C(O)R11, C(O)NH2, C(O)NHR11, C(O)N(R11)2, NHC(O)R11 or NR11C(O)R11 and is further unsubstituted or substituted with one or two or three of independently selected R11, OR11, SR11, S(O)R11, SO2R11, NH2, NHR11, N(R11)2, C(O)OR11, C(O)NH2, C(O)NHR11, C(O)N(R11)2, NHC(O)R11, NR11C(O)R11, NHSO2R11, NR11SO2R11, NHC(O)OR11, NR11C(O)OR11, NHSO2NH2, NHSO2NHR11, NHSO2N(R11)2, SO2NH2, SO2NHR11, SO2N(R11)2, NHC(O)NH2, NHC(O)NHR11, NHC(O)N(R11)2, NR11C(O)N(R11)2, NO2, OH, (O), C(O)H, C(O)OH, CN, CF3, OCF3, CF2CF3, F, Cl, Br or I;
or a pharmaceutically acceptable salt thereof.
8. The compound of claim 3, wherein
R5 is Cl-alkyl which is substituted with R10, and further unsubstituted or substituted with CF3;
R10 is R10A, R10B or R10C; each of which must be attached at a carbon atom;
R10A is phenyl which is unfused or fused with heterocycloalkane, which is fused with heterocycloalkane;
R10B is
R10C is heterocycloalkyl, which is unfused;
wherein R10 is substituted with C(O)R11, C(O)NHR11, C(O)N(R11)2 or NHC(O)R11, and is further unsubstituted or substituted with one or two or three of independently selected R11, OR11, SR11, S(O)R11, SO2R11, NH2, N(R11)2, C(O)R11, C(O)OR11, C(O)NHR11, C(O)N(R11)2, NHC(O)R11, NHSO2R11, NR11SO2R11, NHC(O)OR11, NHSO2N(R11)2, NO2, OH, (O), C(O)OH, F, Cl, Br or I;
wherein each R11 is R12, R13, R14 or R15;
R12 is phenyl which is unfused or fused with benzene, heteroarene, heterocycloalkane or heterocycloalkene;
R13 is heteroaryl, which is unfused;
R14 is cycloalkyl, heterocycloalkyl or heterocycloalkenyl; each of which is unfused or fused with benzene, cycloalkane, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene;
R15 is alkyl, which is unsubstituted or substituted with one or two of independently selected R16, OR16, SR16, S(O)2R16, C(O)OH, NH2, NHR16 N(R16)2, C(O)R16, C(O)NHR16, NHC(O)R16, NHC(O)OR16, OH, F, Cl, Br or I;
wherein each R16 is R17 or R17A;
R17 is alkyl, which is unsubstituted or substituted with R18;
R17A is phenyl, heteroaryl, cycloalkyl, heterocycloalkyl, heterocycloalkenyl each of which is unfused or fused with benzene or heterocycloalkane;
R18 is phenyl or heterocycloalkyl, which is unfused;
wherein the moieties represented by R12, R13, R14, R17A, and R18 are independently unsubstituted or substituted with one or two independently selected R19, OR19, SR19, SO2R19, C(O)R19, CO(O)R19, NHR19, N(R19)2, NHC(O)R19, NHS(O)2R19, C(O)NH2, C(O)NHR19, C(O)N(R19)2, C(O)H, OH, (O), CN, CF3, F, Cl, Br or I;
wherein each R19 is R20, R21, R22 or R23;
R20 is phenyl, which is unfused;
R21 is heteroaryl, which is unftused;
R22 is cycloalkyl,or heterocycloalkyl each of which is unfused or fused with benzene;
R23 is alkyl which is unsubstituted or substituted with one or two of independently selected R24 OR24, NHR24 N(R24)2, NHS(O)2R24, OH, F, Cl, Br or I;
wherein each R24 is R24A or R24B;
R24A is phenyl, cycloalkyl, heterocycloalkyl or heterocycloalkenyl; each of which is unfused or fused with heterocycloalkane;
R24B is alkyl which is unsubstituted or substituted with OR25, OH, F, Cl, Br or I;
R25 is alkyl each of which is unsubstituted or substituted with NH2;
wherein the moieties represented by R20, R21, R22, and R24A are independently unsubstituted or substituted with one or two of independently selected R26, OR26, (O), F, Cl, Br or I; and
R26 is alkyl;
or a pharmaceutically acceptable salt thereof.
9. The compound of claim 3, wherein R10 is R10A, wherein is R10A is phenyl which is unfused and substituted with F, and further substituted with C(O)R11, C(O)NH2, C(O)NHR11, C(O)N(R11)2, NHC(O)R11 or NR11C(O)R11 and is further unsubstituted or substituted with one or two or three of independently selected R11, OR11, SR11, S(O)R11, SO2R11, NH2, NHR11, N(R11)2, C(O)R11, C(O)OR11, C(O)NH2, C(O)NHR11, C(O)N(R11)2, NHC(O)R11, NR11C(O)R11, NHSO2R11, NR11SO2R11, NHC(O)OR11, NR11C(O)OR11, NHSO2NH2, NHSO2NHR11, NHSO2N(R11)2, SO2NH2, SO2NHR11, SO2N(R11 )2, NHC(O)NH2, NHC(O)NHR11, NHC(O)N(R11)2, NR11C(O)N(R11)2, NO2, OH, (O), C(O)H, C(O)OH, CN, CF3, OCF3, CF2CF3, F, Cl, Br or I;
or a pharmaceutically acceptable salt thereof.
10. The compound of claim 4, wherein R10 is R10A, wherein is R01A is phenyl which is unfused and substituted with F, and further substituted with NHC(O)R11, wherein R11 is R15;
or a pharmaceutically acceptable salt thereof.
11. The compound of claim 10, wherein R15 is alkyl, which is unsubstituted or substituted with one or two of independently selected R16, OR16, SR16, S(O)2R16, C(O)OH, NH2, NHR16 N(R16)2, C(O)R16, C(O)NHR16, NHC(O)R16, NHC(O)OR16, OH, F, Cl, Br or I;
wherein each R16 is R17 or R17A;
R17 is alkyl, which is unsubstituted or substituted with one or two of independently selected R18;
R17A is phenyl, heteroaryl, cycloalkyl, heterocycloalkyl, heterocycloalkenyl each of which is unfused or fused with benzene or heterocycloalkane;
wherein each R18 is phenyl or heterocycloalkyl;
wherein each of the moieties represented by R17A and R18 are independently unsubstituted or substituted with one or two or three or four of independently selected R19, OR19, SR19, SO2R19, C(O)R19, CO(O)R19, NHR19, N(R19)2, NHC(O)R19, NHS(O)2R19, C(O)NH2, C(O)NHR19, C(O)N(R19)2, C(O)H, OH, (O), CN, CF3, F, Cl, Br or I;
wherein each R19 is R20, R21, R22 or R23;
R20 is phenyl which is unfused;
R21 is heteroaryl which is unfused;
R22 is cycloalkyl or heterocycloalkyl; each of which are unfused or fused with benzene;
R23 is alkyl, which is unsubstituted or substituted with one or two of independently selected R24, OR24, NHR24 N(R24)2, NHS(O)2R or OH;
wherein each R24 is R24A or R24B;
R24A is unsubstituted phenyl, cycloalkyl, heterocycloalkyl or heterocycloalkenyl each of which is unfused or fused with heterocycloalkane;
R24B is alkyl, which is unsubstituted or substituted with one or two of independently selected OR25 or OH;
wherein each R25 is alkyl unsubstituted or substituted with NH2;
wherein each R20 is unsubstituted or substituted with one or two of independently selected R26, OR26, (O), F, Cl, Br or I; and
R26 is alkyl;
or a pharmaceutically acceptable salt thereof.
12. The compound of claim 4, wherein R10 is R10A, wherein R10A is phenyl which is unfused and substituted with F, and further substituted with R11, wherein R11 is phenyl, pyrrolyl, azabicylclo(3.1.0)hexanyl, hexahydro-1H-isoindolyl, 1,3-oxazolidinyl, azepanyl, piperidinyl, imidazolidinyl, thiazolidinyl, thiazinyl, azetidinyl, 1,6-dihydropyridazyl. tetrahydropyrimidin(2H)-yl or azabicylo(2.2.1)hept-2-yl; each of which are independently unsubstituted or substituted with one or two or three of independently selected R19, OR19, SR19, SO2R19, C(O)R19, CO(O)R19, NHR19, N(R19)2, NHC(O)R19, NHS(O)2R19, C(O)NH2, C(O)NHR19, C(O)N(R19)2, C(O)H, OH, (O), CN, CF3, F, Cl, Br or I;
wherein each R19 is R20, R21, R22 or R23;
R20 is phenyl, which is unfused;
R21 is heteroaryl, which is unfused;
R22 is cycloalkyl,or heterocycloalkyl each of which is unfused or fused with benzene;
R23 is alkyl which is unsubstituted or substituted with one or two of independently selected R24, OR24, NHR24N(R24)2, NHS(O)2R19, OH, F, Cl, Br or I;
wherein each R24 is R24A or R24B;
R24A is phenyl, cycloalkyl, heterocycloalkyl or heterocycloalkenyl; each of which is unfused or fused with heterocycloalkane;
R24B is alkyl which is unsubstituted or substituted with OR25, OH, F, Cl, Br or I;
R25 is alkyl each of which is unsubstituted or substituted with NH2;
wherein the moieties represented by R20, R21, R22, and R24A are independently unsubstituted or substituted with one or two of independently selected R26, OR26, (O), F Cl, Br or I; and
R26 is alkyl,
or a pharmaceutically acceptable salt thereof.
13. The compound of claim 4, wherein R10 is substituted with F, and further substituted with R14 wherein each R10 is independently unsubstituted or substituted with one or two or three of independently selected R11, OR11, SR11, S(O)R11, SO2R11, NH2, NHR11, N(R11)2, C(O)R11, C(O)OR11, C(O)NH2, C(O)NHR11, C(O)N(R11)2, NHC(O)R11, NR11C(O)R11, NHSO2R11, NR11SO2R11, NHC(O)OR11, NR11C(O)OR11, NHSO2NH2, NHSO2NHR11, NHSO2N(R11)2, SO2NH2, SO2NHR11, SO2N(R11)2, NHC(O)NH2, NHC(O)NHR11, NHC(O)N(R11)2, NR11C(O)N(R11)2, NO2, OH, (O), C(O)H, C(O)OH, CN, CF3, OCF3, CF2CF3, F, Cl, Br or I;
wherein R14 is pyrrolidinyl, azetidinyl, pyrrolyl, 1,3-oxazolidinyl, azepanyl, piperidinyl, imidazolidinyl, tetrahydropyrimidin(2H)-yl, azabicyclo(2.2.1)heptyl or 1.6-dihydropyridazyl; each of which unfuised or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; and
wherein the moiety represented by R14 is substituted with one or two (O) substituents;
or a pharmaceutically acceptable salt thereof
14. A compound having formula (Ik),
or a pharmaceutically acceptable salt thereof, wherein R101, R102, R103, R104, and R105, are independently selected from H, R11, OR11, SR11, S(O)R11, SO2R11, NH2, N(R11)2, C(O)R11, C(O)OR11, C(O)NHR11, C(O)N(R11)2, NHC(O)R11, NHSO2R11, NR11SO2R11, NH C(O)OR11, NHSO2N(R11)2, NO2, OH, (O), C(O)OH, F, Cl or Br; wherein each R11 is R12, R13, R14 or R15;
R12 is phenyl which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R13 is heteroaryl which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene. heterocycloalkane or heterocycloalkene;
R14 is cycloalkyl, cycloalkenyl, heterocycloalkyl or heterocycloalkenyl; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R15 is alkyl, alkenyl or alkynyl; each of which is unsubstituted or substituted with one or two of independently selected R16, OR16, SR16, S(O)2R16, C(O)OH, NH2, NHR16N(R16)2, C(O)R16, C(O)NH2, C(O)NHR16, C(O)N(R16)2, NHC(O)R16, NR16C(O)R16, NHC(O)OR16, NR16C(O)OR16, OH, F, Cl, Br or I;
wherein each R16 is R17or R17A;
R17 is alkyl, alkenyl or alkynyl; each of which is unsubstituted or substituted with one or two of independently selected R18, C(O)OH, NH2, NHR18 or N(R18)2, C(O)R18, C(O)NH2, C(O)NHR18, C(O)N(R18)2, NHC(O)R18, NR18C(O)R18, F, Cl, Br or I;
R17A is phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
wherein each R18 is phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl or heterocycloalkenyl;
wherein each of the moieties represented by R12, R13, R14, R17A, and R18 are independently unsubstituted or substituted with one or two or three or four of independently selected R19, OR19, SR19, S(O)R19, SO2R19, C(O)R19, CO(O)R19, OC(O)R19, OC(O)O R19, NH2, NHR19, N(R19)2, NHC(O)R19, NR19C(O)R19, NHS(O)2R19, NR19S(O)2R19, NHC(O)OR19, NR19C(O)OR19, NHC(O)NH2, NHC(O)NHR19, NHC(O)N(R19)2, NR19C(O)NHR19, NR19C(O)N(R19)2, C(O)NH2, C(O)NHR19, C(O)N(R19)2, C(O)NHOH, C(O)NHOR19, C(O)NHSO2R19, C(O)NR19SO2R19, SO2NH2, SO2NHR19, SO2N(R19)2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR19, C(N)N(R19)2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I;
wherein each R19 is R20, R21, R22 or R23;
R20 is phenyl which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R21 is heteroaryl which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R22 is cycloalkyl, cycloalkenyl, heterocycloalkyl or heterocycloalkenyl; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfised or fused with benzene, heteroarene. cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R23 is alkyl, alkenyl or alkynyl; each of which is unsubstituted or substituted with one or two of independently selected R24, OR24, SR24, S(O)2R24, C(O)OH, NH2, NHR24 N(R24)2, C(O)R24, C(O)NH2, C(O)NHR24, C(O)N(R24)2, NHC(O)R24, NR24C(O)R24, NHC(O)OR24, NR24C(O)OR24, NHS(O)2R24, NR24S(O)2R24, OH, F, Cl, Br or I;
wherein each R24 is R24A or R24B;
R24A is phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl or heterocycloalkenyl each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R24B is alkyl, alkenyl or alkynyl each of which is unsubstituted or substituted with one or two of independently selected R25, OR25, SR25, S(O)2R25, C(O)OH, NH2, NHR25N(R25)2, C(O)R25, C(O)NH2, C(O)NHR25, C(O)N(R25)2, NHC(O)R25, NR25C(O)R25, NHC(O)OR25, NR25C(O)OR25, OH, F, Cl, Br or I;
wherein each R25 is alkyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl or heterocycloalkenyl; each of which is unsubstituted or substituted with NH2, NH(CH3), N(CH3)2, OH or OCH3;
wherein each of the moieties represented by R20, R21, R22, and R24A are independently unsubstituted or substituted with one or two of independently selected R26, OR26, alkenyl, alkynyl, phenyl, OH, (O), C(O)OH, CN, CF3, OCF3, CF2CF3, F, Cl, Br or I; and
R26 is alkyl.
15. The compound of claim 14, wherein R1C3 is F; or a pharmaceutically acceptable salt thereof.
16. The compound of claim 15, wherein R101, R104 and R105 are H; or a pharmaceutically acceptable salt thereof.
17. The compound of claim 15, wherein R102 is NHC(O)R11; or a pharmaceutically acceptable salt thereof.
18. The compound of claim 17, wherein R11 is R15, wherein R15 is alkyl, unsubstituted or substituted with one or two of independently selected R16, OR16, SR16, S(O)2R16, C(O)OH, NH2, NHR16N(R16)2, C(O)R16, C(O)NHR16, NHC(O)R16, NHC(O)OR16, OH or Cl;
wherein each R16 is R17 or R17A:
R17 is alkyl, which is unsubstituted or substituted with one or two of independently selected R18;
R17A is phenyl, heteroaryl, cycloalkyl, heterocycloalkyl, heterocycloalkenyl each of which is unfused or fused with benzene or heterocycloalkane;
wherein each R18 is phenyl or heterocycloalkyl;
wherein each of the moieties represented by R17A and R18 are independently unsubstituted or substituted with one or two or three or four of independently selected R19, OR19, SR19, SO2R19, C(O)R19, CO(O)R19, NHR19, N(R19)2, NHC(O)R19, NHS(O) 2R19, C(O)NH2, C(O)NHR19, C(O)N(R19)2, C(O)H, OH, (O), CN, CF3, F, Cl, Br or I;
wherein each R19 is R20, R21, R22 or R23:
R20 is phenyl which is unfused;
R21 is heteroaryl which is unfused;
R22 is cycloalkyl or heterocycloalkyl; each of which are unfused or fused with benzene;
R23 is alkyl, which is unsubstituted or substituted with one or two of independently selected R24, OR24, NHR24N(R24)2, NHS(O)2R24 or OH;
wherein each R24 is R24A or R24B;
R24A is unsubstituted phenyl, cycloalkyl, heterocycloalkyl or heterocycloalkenyl each of which is unfused or fused with heterocycloalkane;
R24B is alkyl, which is unsubstituted or substituted with one or two of independently selected OR25 or OH;
wherein each R25 is alkyl unsubstituted or substituted with NH2;
wherein each R20 is unsubstituted or substituted with one or two of independently selected R26, OR26, (O), F or Cl; and
R26 is alkyl; or a pharmaceutically acceptable salt thereof.
19. The compound of claim 16, wherein R102 is NHC(O)R11.
20. The compound of claim 15, wherein R102 is R11, wherein R11 is selected from pyrrolidinyl, oxazolyl, imidazolidinyl, isothiazolidinyl, piperidinyl, piperazinyl and azepanyl, wherein R104 is substituted with one or two (O) substituents; or a pharmaceutically acceptable salt thereof.
21. The compound of claim 20, wherein R11 is pyrrolidinyl; or a pharmaceutically acceptable salt thereof.
22. The compound of claim 16, wherein R102 is R11, wherein R11 is selected from pyrrolidinyl, oxazolyl, imidazolidinyl, isothiazolidinyl, piperidinyl, and azepanyl, wherein R104 is substituted with one or two (O) substituents; or a pharmaceutically acceptable salt thereof.
23. The compound of claim 22, wherein R11 is pyrrolidinyl; or a pharmaceutically acceptable salt thereof.
24. A compound according to claim 15 selected from
2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)benzoic acid;
4-(3-amino-4-fluorobenzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-((2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)amino)-4-oxobutanoic acid;
1-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)pyrrolidine-2,5-dione;
4-(3-(1,4-diazepan-1-ylcarbonyl)-4-fluorobenzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(3-(aminomethyl)-4-fluorobenzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(3-((dimethylamino)methyl)-4-fluorobenzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(4-fluoro-3-((isopropylamino)methyl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(3-((cyclohexylamino)methyl)-4-fluorobenzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(4-fluoro-3-((tetrahydro-2H-pyran-4-ylamino)methyl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(4-fluoro-3-((methyl((1-methylpyrrolidin-3-yl)methyl)amino)methyl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(4-fluoro-3-((methyl(((2R)-1-methylpyrrolidin-2-yl)methyl)amino)methyl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(4-fluoro-3-pyrimidin-2-ylbenzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(4-fluoro-3-pyridin-3-ylbenzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(4-fluoro-3-pyridin-4-ylbenzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
N,N-diethyl-2\u2032-fluoro-5\u2032-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)-1,1\u2032-biphenyl-2-carboxamide;
N-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)-3-piperidin-1-ylpropanamide;
N-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)-3-(4-methylpiperazin-1-yl)propanamide;
2-amino-N-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)acetamide;
3-cyclohexyl-N-(2-uoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)propanamide;
N-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)piperidine-3-carboxamide;
4-(4-fluoro-3-(2-oxopyrrolidin-1-yl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
N-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophihalazin-1-yl)methyl)phenyl)azetidine-3-carboxamide;
N-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)-2-morpholin-4-ylacetamide;
N-(2\u2032-fluoro-5\u2032-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)-1,1\u2032-biphenyl-3-yl)acetamide;
4-((6-fluoro-3\u2032-(methylsulfonyl)-1,1\u2032-biphenyl-3-yl)methyl)-5,6,7,8-tetrahydrophthalazin-1(21)-one;
4-((6-fluoro-3\u2032-(pyrrolidin-1-ylcarbonyl)-1,1\u2032-biphenyl-3-yl)methyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-((6-fluoro-4\u2032-(pyrrolidin-1-ylcarbonyl)-1,1\u2032-biphenyl-3-yl)methyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
N,N-diethyl-2\u2032-fluoro-5\u2032-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)-1,1\u2032-biphenyl-3-carboxamide;
2\u2032-fluoro-N,N-dimethyl-5\u2032-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)-1,1\u2032-biphenyl-4-carboxamide;
N-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)-4-(4-methoxyphenyl)-4-oxobutanamide;
1-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)-3,4-dimethyl-1H-pyrrole-2,5-dione;
3-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)-3-azabicyclo(3.1.0)hexane-2,4-dione;
2-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)hexahydro-1H-isoindole-1,3(2H)-dione;
1-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)-3,3-dimethylpyrrolidine-2,5-dione;
4-(4-fluoro-3-(2-methyl-5-oxopyrrolidin-1-yl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(4-fluoro-3-(2-oxo-1,3-oxazolidin-3-yl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(4-fluoro-3-(2-oxoazepan-1-yl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
1-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)piperidine-2,6-dione;
4-(4-fluoro-3-(2-oxoimidazolidin-1-yl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(3-(1,1-dioxidoisothiazolidin-2-yl)-4-fluorobenzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(4-fluoro-3-(2-oxoazetidin-1-yl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(4-fluoro-3-(2-oxopiperidin-1-yl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(4-fluoro-3-(3-methyl-2-oxoimidazolidin-1-yl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(4-fluoro-3-(2-oxotetrahydropyrimidin-1(2H)-yl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(3-(3-tert-butyl-2-oxoimidazolidin-1-yl)-4-fluorobenzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(4-fluoro-3-((1S,4R)-3-oxo-2-azabicyclo(2.2.1)hept-2-yl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
N-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)-N-methylmethanesulfonamide;
N-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)-2-hydroxy-2-methylpropanamide;
(3aS,4R,7S,7aR)-5-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)-2,2-dimethyltetrahydro-4,7-methano(1,3)dioxolo(4,5-c)pyridin-6(3aH)-one;
4-(3-(1,1-dioxido-1,2-thiazinan-2-yl)-4-fluorobenzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
N-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)-2-(2-oxopyrrolidin-1-yl)acetamide;
N-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)-5-methyl-1-phenyl-1H-pyrazole-4-carboxamide;
N-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)-5-oxohexanamide;
N-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophihalazin-1-yl)methyl)phenyl)-3-methoxypropanamide;
N-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)-N\u2032-phenylpentanediamide;
4-(4-fluoro-3-((4-pyrimidin-2-ylpiperazin-1-yl)carbonyl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one; or
4-(4-fluoro-3-(2-oxopyrrolidin-1-yl)phenyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
or a pharmaceutically acceptable salt thereof.
25. The compound of claim 15 selected from
4-((2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophihalazin-1-yl)methyl)phenyl)amino)-4-oxobutanoic acid;
1-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)pyrrolidine-2,5-dione;
4-(4-fluoro-3-(2-oxopyrrolidin-1-yl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
N-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)-3-(4-methylpiperazin-1-yl)propanamide;
3-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)-3-azabicyclo(3.1.0)hexane-2,4-dione;
1-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophlhalazin-1-yl)methyl)phenyl)-3,3-dimethylpyrrolidine-2,5-dione;
4-(4-fluoro-3-(2-oxo-1,3-oxazolidin-3-yl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(4-fluoro-3-(3-methyl-2-oxoimidazolidin-1-yl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(4-fluoro-3-(2-oxoazepan-1-yl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
1-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)methyl)phenyl)piperidine-2,6-dione;
4-(3-(1,1-dioxidoisothiazolidin-2-yl)-4-fluorobenzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
4-(4-fluoro-3-(2-oxopiperidin-1-yl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one; or
4-(4-fluoro-3-((4-pyrimidin-2-ylpiperazin-1-yl)carbonyl)benzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one;
or a pharmaceutically acceptable salt thereof.
26. A compound having formula (Iv),
or a pharmaceutically acceptable salt thereof, wherein R101, R102, R103, R104, and R105, are independently selected from H, R11, OR11, SR11, S(O)R11, SO2R11, NH2, N(R11)2, C(O)R11, C(O)OR11, C(O)NHR11, C(O)N(R11)2, NHC(O)R11, NHSO2R11, NR11SO2R11, NH C(O)OR11, NHSO2N(R11)2, NO2, OH, (O), C(O)OH, F, Cl or Br; wherein each R11 is R12, R13, R14 or R15;
R12 is phenyl which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R13 is heteroaryl which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R14 is cycloalkyl, cycloalkenyl, heterocycloalkyl or heterocycloalkenyl; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene. heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R15 is alkyl, alkenyl or alkynyl; each of which is unsubstituted or substituted with one or two of independently selected R16, OR16, SR16, S(O)2R16, C(O)OH, NH2, NHR16N(R16)2, C(O)R16, C(O)NH2, C(O)NHR16, C(O)N(R16)2, NHC(O)R16, NR16C(O)R16, NHC(O)OR16, NR16C(O)OR16, OH, F, Cl, Br or I;
wherein each R16 is R17 or R17A;
R17 is alkyl, alkenyl or alkynyl; each of which is unsubstituted or substituted with one or two of independently selected R18, C(O)OH, NH2, NHR18 or N(R18)2, C(O)R18, C(O)NH2, C(O)NHR18, C(O)N(R18)2, NHC(O)R18, NR18C(O)R18, F, Cl, Br or I;
R17A is phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl each of which is unfused or fused with benzene, heteroarene, cycloalkane. cycloalkene, heterocycloalkane or heterocycloalkene;
wherein each R18 is phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl or heterocycloalkenyl;
wherein each of the moieties represented by R12, R13, R14, R17A, and R18 are independently unsubstituted or substituted with one or tho or three or four of independently selected R19, OR19, SR19, S(O)R19, SO2R19, C(O)R19, CO(O)R19, OC(O)R19, O C(O)R19, NH2, NHR19, N(R19)2, NHC(O)R19, NR19C(O)R19, NHS(O)2R19, NR19S(O)2R19, NHC(O)OR19, NR19C(O)OR19, NHC(O)NH2, NHC(O)NHR19, NHC(O)N(R19)2, NR19C(O)NHR19, NR19C(O)N(R19)2, C(O)NH2, C(O)NHR19, C(O)N(R19)2, C(O)NHOH, C(O)NHOR19, C(O)NHSO2R19, C(O)NR19SO2R19, SO2NH2, SO2NHR19, SO2N(R19)2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR19, C(N)N(R19)2, CNOH, CNOCH3, OH, (O), CN, N3, NO2. CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I;
wherein each R19 is R20, R21, R22 or R23;
R20 is phenyl which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R21 is heteroaryl which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R22 is cycloalkyl, cycloalkenyl, heterocycloalkyl or heterocycloalkenyl; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R23 is alkyl, alkenyl or alkynyl; each of which is unsubstituted or substituted with one or two of independently selected R24, OR24, SR24, S(O)2R24, C(O)OH, NH2, NHR24 N(R24)2, C(O)R24, C(O)NH2, C(O)NHR24, C(O)N(R 24)2, NHC(O)R24, NR24C(O)R24, NHC(O)OR24, NR24C(O)OR24, NHS(O)2R24, NR24S(O)2R24, OH, F, Cl, Br or I;
wherein each R24 is R24A or R24B;
R24A is phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl or heterocycloalkenyl each of which is unfused or fused with benzene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene;
R24B is alkyl, alkenyl or alkynyl each of which is unsubstituted or substituted with one or two of independently selected R25, OR25, SR25, S(O)2R25, C(O)OH, NH2, NHR25N(R25)2, C(O)R25, C(O)NH2, C(O)NHR25, C(O)N(R25)2, NHC(O)R25, NR25C(O)R25, NHC(O)OR25, NR25C(O)OR25, OH, F, Cl, Br or I;
wherein each R25 is alkyl, phenyl, heteroaryl, cycloalkyl. cycloalkenyl, heterocycloalkyl or heterocycloalkenyl ; each of which is unsubstituted or substituted with NH2, NH(CH3), N(CH3)2, OH or OCH3;
wherein each of the moieties represented by R20, R21, R22, and R24A are independently unsubstituted or substituted with one or two of independently selected R26, OR26, alkenyl, alkynyl, phenyl, OH, (O), C(O)OH, CN, CF3, OCF3, CF2CF3, F, Cl, Br or I; and
R26 is alkyl.
27. The compound of claim 26, wherein R103 is F; or a pharmaceutically acceptable salt thereof.
28. The compound of claim 27 selected from
8-(4-fluorobenzyl)-2,3,4,6-tetrahydropyrido(2,3-d)pyridazin-5(1H)-one;
8-(4-fluoro-3-(2-oxoazetidin-1-yl)benzyl)-2,3,4,6-tetrahydropyrido(2,3-d)pyridazin-5(1H)-one;
8-(3-chloro-4-fluorobenzyl)-2,3,4,6-tetrahydropyrido(2,3-d)pyridazin-5(1H)-one
8-(4-fluoro-3-(2-oxopyrrolidin-1-yl)benzyl)-2,3,4,6-tetrahydropyrido(2,3-d)pyridazin-5(1H)-one;
methyl 2-fluoro-5-((5-oxo-1,2,3,4,5,6-hexahydropyrido(2,3-d)pyridazin-8-yl)methyl)benzoate;
8-(3-amino-4-fluorobenzyl)-2,3,4,6-tetrahydropyrido(2,3-d)pyridazin-5(1H)-one;
2-fluoro-5-((S-oxo-1,2,3,4,5,6-hexahydropyrido(2,3-d)pyridazin-8-yl)methyl)benzoic acid;
N-ethyl-2-fluoro-5-((5-oxo-1,2,3,4,5,6-hexahydropyrido(2,3-d)pyridazin-8-yl)methyl)benzamide;
N-cyclobutyl-2-fluoro-5-((5-oxo-1,2,3,4,5,6-hexahydropyrido(2,3-d)pyridazin-8-yl)methyl)benzamide;
2-fluoro-5-((5-oxo-1,2,3,4,5,6-hexahydropyrido(2,3-d)pyridazin-8-yl)methyl)-N-(2-pyrrolidin-1-ylethyl)benzamide;
8-(4-fluoro-3-((4-(morpholin-4-ylcarbonyl)piperazin-1-yl)carbonyl)benzyl)-2,3,4,6-tetrahydropyrido(2,3-d)pyridazin-5(1H)-one;
N-(2-fluoro-5-((5-oxo-1,2,3,4,5,6-hexahydropyrido(2,3-d)pyridazin-8-yl)methyl)phenyl)-N\u2032-phenylpentanediamide;
1-(2-fluoro-5-((5-oxo-1,2,3,4,5,6-hexahydropyrido(2,3-d)pyridazin-8-yl)methyl)phenyl)pyrrolidine-2,5-dione;
N-(2-fluoro-5-((5-oxo-1,2,3,4,5,6-hexahydropyrido(2,3-d)pyridazin-8-yl)methyl)phenyl)-3-methoxypropanamide;
N-(2-fluoro-5-((5-oxo-1,23,4,5,6-hexahydropyrido(2,3-d)pyridazin-8-yl)methyl)phenyl)-5-oxohexanamide;
N-(2-fluoro-5-((5-oxo-1,2,3,4,5,6-hexahydropyrido(2,3-d)pyridazin-8-yl)methyl)phenyl)-3-phenoxypropanamide;
N-(2-fluoro-5-((5-oxo-1,2,3,4,5,6-hexahydropyrido(2,3-d)pyridazin-8-yl)methyl)phenyl)-4-oxo-4-phenylbutanamide;
2-(4-(benzyloxy)phenoxy)-N-(2-fluoro-5-((5-oxo-1,2,3,4,5,6-hexahydropyrido(2,3-d)pyridazin-8-yl)methyl)phenyl)acetamide;
N-(2-fluoro-5-((5-oxo-1,2,3,4,5,6-hexahydropyido(2,3-d)pyridazin-8-yl)methyl)phenyl)-2-(4-methoxyphenoxy)acetamide;
N-cyclopropyl-2-fluoro-5-((5-oxo-1,2,3,4,5,6-hexahydropyrido(2,3-d)pyridazin-8-yl)methyl)benzamide;
8-(3-((4-(2-ethoxyethyl)piperazin-1-yl)carbonyl)-4-fluorobenzyl)-2,3,4,6-tetrahydropyrido(2,3-d)pyridazin-5(1H)-one; or
2-fluoro-5-((5-oxo-1,2,3,4,5,6-hexahydropyrido(2,3-d)pyridazin-8-yl)methyl)-N-(2-piperidin-1-ylethyl)benzamide;
or a pharmaceutically acceptable salt thereof.
29. The compound 1-(2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin 1-yl)methyl)phenyl)pyrrolidine-2,5-dione; or a pharmaceutically acceptable salt thereof
30. The compound 4-(3-(1,4-diazepan-1-ylcarbonyl)-4-fluorobenzyl)-5,6,7,8-tetrahydrophthalazin-1(2H)-one; or a pharmaceutically acceptable salt thereof.
31. The compound 4-((2-fluoro-5-((4-oxo-3,4,5,6,7,8-hexahydrophthalazin 1-yl)methyl)phenyl)amino)-4-oxobutanoic acid; or a pharmaceutically acceptable salt thereof
32. A pharmaceutical composition comprising a compound of claim 1 and pharmaceutically acceptable excipient.
33. A method of treating cancer in a mammal comprising administering thereto a therapeutically acceptable amount of a compound of claim 1.
34. A method for decreasing tumor volume in a mammal comprising administering thereto a therapeutically acceptable amount of a compound of claim 1.
35. A method of treating cancer in a mammal comprising administering thereto a therapeutically acceptable amount of a compound of claim I in combination with radiotherapy.
36. A method of treating cancer in a mammal comprising administering thereto a therapeutically acceptable amount of a compound of claim I in combination with a chemotherapeutic agent selected from temozolomide, dacarbazine, cyclophosphamide, carmustine, melphalan, lomustine, carboplatin, cisplatin, 5-FU \xb1leucovorin, gemcitabine, methotrexate, bleomycin, irinotecan, camptothecin, or topotecan.