1.-13. (canceled)
14. A compound of Formula (I):
and pharmaceutically acceptable salts, solvates or prodrugs thereof,
wherein:
X, Y, Z each, independently of one another, are N or CR2, with the proviso that if Z is N, Y is CR2, and if Y is N, Z is CR2,
T, Q are S, O or CR5, with the proviso that if T is S or O, Q is CR5, and if Q is S or O, T is CR5,
—– denotes the presence or absence of a bond, with the proviso that one of the two dashed lines is always a bond, whereas the other one is always absent,
R1, R2, R5 each, independently of one another, are H, A, Hal, OH, SH, CN, NH2, NO2,
R3 is H or A,
R4 is A, Ar or A-Ar, or
R3 and R4 together with the C atom to which they are attached, may form Ar, or cyclic A which may be unsubstituted or substituted by COO(LA) or CONH(LA),
Ar is a mono- or bicyclic aromatic homo- or heterocycle having 1 to 4 N, O andor S atoms and 5 to 10 skeleton atoms, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by Hal, A, OH, SH, OA, NH2, NHA, NA2, NO2, CN, OCN, SCN, COOH, COOA, CONH2, CONHA, CONH(LAr), CONA2, NHCOA, NHCO(LAr), NHCONHA, NHCONH2, NHSO2A, CHO, COA, SO2NH2, SO2A andor SO2Hal,
A is unbranched or branched, linear or cyclic alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 C atoms, in which one or two CH2 groups may be replaced by an O or S atom andor by an NH, N(LA), SO2, CONH, NHCO or \u2014CH\u2550CH\u2014 group, and in which 1-3 H atoms may be replaced by Hal, and in which one or two CH3 groups may be replaced by OH, SH, NH2, NH(LA), N(LA)2, NHCOOH, NHCONH2, N3, NO2 or CN,
LA is unbranched or branched, linear alkyl having 1, 2, 3 or 4 C atoms,
LAr is a monocyclic aromatic homo- or heterocycle having 1 or 2 N, O andor S atoms and 5 to 7 skeleton atoms, which may be unsubstituted or mono-, di- or trisubstituted by Hal, LA, OH, O(LA), NH2 or NH(LA),
Hal is F, Cl, Br or I.
15. The compounds according to claim 14 which conforms to Formulae (II):
and pharmaceutically acceptable salts, solvates or prodrugs thereof,
in which T is S or O, and the remaining substituents have the meaning indicated for Formula (I) according to claim 14.
16. The compounds according to claim 1 which conforms to Formulae (III):
and pharmaceutically acceptable salts, solvates or prodrugs thereof,
in which Q is S or O, and the remaining substituents have the meaning indicated for Formula (I) according to claim 14.
17. The compounds according to claim 1 which conform to Formulae (IV):
and pharmaceutically acceptable salts, solvates or prodrugs thereof,
in which T is S or O, and the remaining substituents have the meaning indicated for Formula (I) according to claim 14.
18. The compounds according to claim 1 which conforms to Formulae (V):
and pharmaceutically acceptable salts, solvates or prodrugs thereof,
in which Q is S or O, and the remaining substituents have the meaning indicated for Formula (I) according to claim 14.
19. The compounds according to claim 14, in which the residues not designated in greater detail have the meaning indicated for the Formula (I) according to claim 1, but in which:
in Subformula A
T, Q are S,
R5 is H or methyl,
in Subformula B
T, Q are O,
R5 is H or methyl,
in Subformula C
X, Y, Z are CH,
in Subformula D
X, Y, Z are CH,
T, Q are S,
R5 is H or methyl,
in Subformula E
Y, Z are CH,
X is N,
T, Q are S,
R5 is H or methyl,
in Subformula F
X, Y, Z are CH,
T, Q are S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
in Subformula G
X, Y, Z are CH,
T, Q are S,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula H
Y, Z are CH,
X is N,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula J
Y, Z are CH,
X is N,
T, Q are S,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula K
Y, Z are CH,
X is N,
T, Q are O,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula L
X, Y, Z are CH,
T, Q are S,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula M
X, Y, Z are CH,
T, Q are S,
R5 is H,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula N
X, Y, Z are CH,
T, Q are S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula O
Y, Z are CH,
X is N,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula P
Y, Z are CH,
X is N,
T, Q are S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula Q
Y, Z are CH,
X is N,
T, Q are O,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula R
X, Y, Z are CH,
T, Q are S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula S
X, Y, Z are CH,
T, Q are S,
R5 is H,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula T
X, Y, Z are CH,
T, Q are S,
R5 is H,
R3 is hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F,
in Subformula U
X, Y, Z are CH,
T, Q are S,
R5 is H,
R3 is H,
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula V
X, Y, Z are CH,
T, Q are S,
R5 is H,
R3 and R4 together with the C atom to which they are attached, form piperidinyl, phenyl, pyrrolidinyl, tetrahydrofuranyl, each of which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F,
in Subformula W
X, Z are CH,
Y is CR2,
R2 is methyl,
T, Q are S,
R5 is H,
R3 is H,
and the remaining residues have the meaning as indicated for Formula (I) above,
and pharmaceutically acceptable salts, solvates or prodrugs thereof.
20. The compounds according to claim 15, in which the residues not designated in greater detail have the meaning indicated for the Formula (I) according to claim 1, but in which:
in Subformula A
T is S,
R5 is H or methyl,
in Subformula B
T is O,
R5 is H or methyl,
in Subformula C
X, Y, Z are CH,
in Subformula D
X, Y, Z are CH,
T is S,
R5 is H or methyl,
in Subformula E
Y, Z are CH,
X is N,
T is S,
R5 is H or methyl,
in Subformula F
X, Y, Z are CH,
T is S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
in Subformula G
X, Y, Z are CH,
T is S,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula H
Y, Z are CH,
X is N,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula J
Y, Z are CH,
X is N,
T is S,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula K
Y, Z are CH,
X is N,
T is O,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula L
X, Y, Z are CH,
T is S,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula M
X, Y, Z are CH,
T is S,
R5 is H,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula N
X, Y, Z are CH,
T is S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula O
Y, Z are CH,
X is N,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula P
Y, Z are CH,
X is N,
T is S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula Q
Y, Z are CH,
X is N,
T is O,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula R
X, Y, Z are CH,
T is S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula S
X, Y, Z are CH,
T is S,
R5 is H,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula T
X, Y, Z are CH,
T is S,
R5 is H,
R3 is hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F,
in Subformula U
X, Y, Z are CH,
T is S,
R5 is H,
R3 is H,
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula V
X, Y, Z are CH,
T is S,
R5 is H,
R3 and R4 together with the C atom to which they are attached, form piperidinyl, phenyl, pyrrolidinyl, tetrahydrofuranyl, each of which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F,
in Subformula W
X, Z are CH,
Y is CR2,
R2 is methyl,
T is S,
R5 is H,
R3 is H,
and the remaining residues have the meaning as indicated for Formula (I),
and pharmaceutically acceptable salts, solvates or prodrugs thereof.
21. The compounds according to claim 16, in which the residues not designated in greater detail have the meaning indicated for the Formula (I) according to claim 1, but in which:
in Subformula A
Q is S,
R5 is H or methyl,
in Subformula B
Q is O,
R5 is H or methyl,
in Subformula C
X, Y, Z are CH,
in Subformula D
X, Y, Z are CH,
Q is S,
R5 is H or methyl,
in Subformula E
Y, Z are CH,
X is N,
Q is S,
R5 is H or methyl,
in Subformula F
X, Y, Z are CH,
Q is S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
in Subformula G
X, Y, Z are CH,
Q is S,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula H
Y, Z are CH,
X is N,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula J
Y, Z are CH,
X is N,
Q is S,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula K
Y, Z are CH,
X is N,
Q is O,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula L
X, Y, Z are CH,
Q is S,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula M
X, Y, Z are CH,
Q is S,
R5 is H,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula N
X, Y, Z are CH,
Q is S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula O
Y, Z are CH,
X is N,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula P
Y, Z are CH,
X is N,
Q is S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula Q
Y, Z are CH,
X is N,
Q is O,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula R
X, Y, Z are CH,
Q is S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula S
X, Y, Z are CH,
Q is S,
R5 is H,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula T
X, Y, Z are CH,
Q is S,
R5 is H,
R3 is hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F,
in Subformula U
X, Y, Z are CH,
Q is S,
R5 is H,
R3 is H,
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula V
X, Y, Z are CH,
Q is S,
R5 is H,
R3 and R4 together with the C atom to which they are attached, form piperidinyl, phenyl, pyrrolidinyl, tetrahydrofuranyl, each of which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F,
in Subformula W
X, Z are CH,
Y is CR2,
R2 is methyl,
Q is S,
R5 is H,
R3 is H,
and the remaining residues have the meaning as indicated for Formula (I),
and pharmaceutically acceptable salts, solvates or prodrugs thereof.
22. The compounds according to claim 17, in which the residues not designated in greater detail have the meaning indicated for the Formula (I) according to claim 1, but in which
in Subformula A
T is S,
R5 is H or methyl,
in Subformula B
T is O,
R5 is H or methyl,
in Subformula C
X, Y, Z are CH,
in Subformula D
X, Y, Z are CH,
T is S,
R5 is H or methyl,
in Subformula E
Y, Z are CH,
X is N,
T is S,
R5 is H or methyl,
in Subformula F
X, Y, Z are CH,
T is S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
in Subformula G
X, Y, Z are CH,
T is S,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula H
Y, Z are CH,
X is N,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula J
Y, Z are CH,
X is N,
T is S,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula K
Y, Z are CH,
X is N,
T is O,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula L
X, Y, Z are CH,
T is S,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula M
X, Y, Z are CH,
T is S,
R5 is H,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula N
X, Y, Z are CH,
T is S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula O
Y, Z are CH,
X is N,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula P
Y, Z are CH,
X is N,
T is S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula Q
Y, Z are CH,
X is N,
T is O,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula R
X, Y, Z are CH,
T is S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula S
X, Y, Z are CH,
T is S,
R5 is H,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula T
X, Y, Z are CH,
T is S,
R5 is H,
R3 is hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F,
in Subformula U
X, Y, Z are CH,
T is S,
R5 is H,
R3 is H,
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula V
X, Y, Z are CH,
T is S,
R5 is H,
R3 and R4 together with the C atom to which they are attached, form piperidinyl, phenyl, pyrrolidinyl, tetrahydrofuranyl, each of which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F,
in Subformula W
X, Z are CH,
Y is CR2,
R2 is methyl,
T is S,
R5 is H,
R3 is H,
and the remaining residues have the meaning as indicated for Formula (I),
and pharmaceutically acceptable salts, solvates or prodrugs thereof.
23. The compounds according to claim 18, in which the residues not designated in greater detail have the meaning indicated for the Formula (I) according to claim 1, but in which:
in Subformula A
Q is S,
R5 is H or methyl,
in Subformula B
Q is O,
R5 is H or methyl,
in Subformula C
X, Y, Z are CH,
in Subformula D
X, Y, Z are CH,
Q is S,
R5 is H or methyl,
in Subformula E
Y, Z are CH,
X is N,
Q is S,
R5 is H or methyl,
in Subformula F
X, Y, Z are CH,
Q is S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
in Subformula G
X, Y, Z are CH,
Q is S,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula H
Y, Z are CH,
X is N,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula J
Y, Z are CH,
X is N,
Q is S,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula K
Y, Z are CH,
X is N,
Q is O,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula L
X, Y, Z are CH,
Q is S,
R5 is H or methyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula M
X, Y, Z are CH,
Q is S,
R5 is H,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula N
X, Y, Z are CH,
Q is S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula O
Y, Z are CH,
X is N,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula P
Y, Z are CH,
X is N,
Q is S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula Q
Y, Z are CH,
X is N,
Q is O,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula R
X, Y, Z are CH,
Q is S,
R5 is H or methyl,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula S
X, Y, Z are CH,
Q is S,
R5 is H,
R3 is H, hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula T
X, Y, Z are CH,
Q is S,
R5 is H,
R3 is hydroxymethyl, aminomethyl, azidomethyl or cyanomethyl,
R4 is phenyl or benzyl, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F,
in Subformula U
X, Y, Z are CH,
Q is S,
R5 is H,
R3 is H,
R4 is benzylamino-methyl, wherein the phenyl ring may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F; or
R4 is aminomethyl, (fluoro-benzoylamino)-benzyl, (benzoylamino)-benzyl, (chloro-azabenzoylamino)-benzyl, pyrrolidinyl, (thiophenylmethyl)amino-ethyl, (indolylmethyl)amino-methyl, (1-phenyl-ethylamino)-methyl, benzyloxy-methyl, phenylamino-methyl, isobutyl, (bis-furan-3-ylmethyl-amino)-methyl, furanylmethyl)aminomethyl, pyrrolylmethyl)aminomethyl, thiophenyl-methyl, (sulfamoyl-phenyl)-methyl, cyclohexenyl-methyl, benzoylamino-methyl, 1-hydroxy-1-phenyl-methyl, (furanylmethylsulfanyl)-methyl or benzenesulfonylamino-methyl,
in Subformula V
X, Y, Z are CH,
Q is S,
R5 is H,
R3 and R4 together with the C atom to which they are attached, form piperidinyl, phenyl, pyrrolidinyl, tetrahydrofuranyl, each of which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by methyl, methoxy, CF3, OCF3, amino, Cl or F,
in Subformula W
X, Z are CH,
Y is CR2,
R2 is methyl,
Q is S,
R5 is H,
R3 is H,
and the remaining residues have the meaning as indicated for Formula (I),
and pharmaceutically acceptable salts, solvates or prodrugs thereof.
24. The compound according to claim 14, wherein the compound is selected from the group consisting of:
3-(7H-Pyrrolo2,3-dpyrimidin-4-ylamino)-furan-2-carboxylic acid 3-chloro-benzylamide,
3-(7H-Pyrrolo2,3-dpyrimidin-4-ylamino)-thiophene-2-carboxylic acid 2-(3-fluoro-phenyl)-ethyl-amide,
3-(7H-Pyrrolo2,3-dpyrimidin-4-ylamino)-thiophene-2-carboxylic acid phenethyl-amide,
3-(7H-Pyrrolo2,3-dpyrimidin-4-ylamino)-thiophene-2-carboxylic acid 2-(3-chloro-phenyl)-ethyl-amide,
3-(7H-Pyrrolo2,3-dpyrimidin-4-ylamino)-thiophene-2-carboxylic acid 2-(4-fluoro-phenyl)-ethyl-amide,
3-(7H-Pyrrolo2,3-dpyrimidin-4-ylamino)-thiophene-2-carboxylic acid 2-(4-bromo-phenyl)-ethyl-amide,
3-(7H-Pyrrolo2,3-dpyrimidin-4-ylamino)-thiophene-2-carboxylic acid (2-o-tolyl-ethyl)-amide,
3-(7H-Pyrrolo2,3-dpyrimidin-4-ylamino)-thiophene-2-carboxylic acid (2-benzylamino-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (2-benzylamino-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(4-fluoro-phenyl)-ethyl-amide,
3-(7H-Pyrrolo2,3-dpyrimidin-4-ylamino)-thiophene-2-carboxylic acid piperidin-3-ylamide,
5-Methyl-3-(7H-pyrrolo2,3-dpyrimidin-4-ylamino)-thiophene-2-carboxylic acid 3-chloro-benzylamide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid pyrrolidin-3-ylamide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (2-cyclohex-1-enyl-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(4-sulfamoyl-phenyl)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(3-trifluoromethyl-phenyl)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(3-chloro-phenyl)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (2-thiophen-2-yl-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(3-fluoro-phenyl)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(4-fluoro-phenyl)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(furan-2-ylmethylsulfanyl)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (2-o-tolyl-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(3-methoxy-phenyl)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(4-bromo-phenyl)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(4-methoxy-phenyl)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (2-benzylamino-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 3-chloro-benzylamide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (2-phenylamino-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (4-chloro-phenyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (4-methoxy-phenyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (4-fluoro-phenyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(4-methoxy-benzylamino)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid {2-(pyridin-2-ylmethyl)-amino-ethyl}-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (2-amino-ethyl)-amide,
S-3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (2-hydroxy-1-phenyl-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid {2-(thiophen-3-ylmethyl)-amino-ethyl}-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(bis-furan-3-ylmethyl-amino)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(2-trifluoromethoxy-benzylamino)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(3-methoxy-benzylamino)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(3-trifluoromethoxy-benzylamino)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(4-trifluoromethoxy-benzylamino)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(4-trifluoromethyl-benzylamino)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid {2-(furan-3-ylmethyl)-amino-ethyl}-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid {2-(1H-pyrrol-2-ylmethyl)-amino-ethyl}-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(3-methyl-benzylamino)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(3-chloro-benzylamino)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(2-fluoro-benzylamino)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid {2-(1H-indol-5-ylmethyl)-amino-ethyl}-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(2-methoxy-benzylamino)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(4-fluoro-benzylamino)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(3-chloro-4-fluoro-benzylamino)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (2-benzyloxy-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (2-benzoylamino-ethyl)-amide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid (2-benzylamino-ethyl)-amide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid ((S)-2-hydroxy-1-phenyl-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (2-azido-1-phenyl-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (2-amino-1-phenyl-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (2-amino-2-phenyl-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid ((S)-1-benzyl-2-hydroxy-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 3-amino-benzylamide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(4-chloro-3-trifluoromethyl-benzylamino)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 3-methoxybenzylamide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 4-chloro-3-trifluoromethyl-benzylamide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (2-hydroxy-2-phenyl-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 3-(4-fluoro-benzoylamino)-benzylamide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid pyrrolidin-3-ylamide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid piperidin-3-ylamide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-amino-1-(3-fluoro-phenyl)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-amino-1-(2-methoxy-phenyl)-ethyl-amide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid 2-amino-1-(3-fluoro-phenyl)-ethyl-amide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid 2-amino-1-(2-methoxy-phenyl)-ethyl-amide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid 2-amino-1-(3,4-dimethoxy-phenyl)-ethyl-amide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid 3-amino-benzylamide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid benzylamide 3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-amino-1-(3,4-dimethoxy-phenyl)-ethyl-amide, 2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid ((S)-2-azido-1-phenyl-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid ((R)-2-cyano-1-phenyl-ethyl)-amide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid (cyano-phenyl-methyl)-amide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid ((S)-1-hydroxymethyl-3-methyl-butyl)-amide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid ((S)-1-hydroxymethyl-2-phenyl-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid ((R)-2-carbamoyl-1-phenyl-ethyl)-amide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid 3-chloro-4-trifluoromethyl-benzylamide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (2-amino-1-p-tolyl-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-amino-1-(3-methoxy-phenyl)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-amino-1-(3-chloro-phenyl)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-amino-1-(3,4-dichloro-phenyl)-ethyl-amide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid (2-amino-1-p-tolyl-ethyl)-amide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid 2-amino-1-(3-methoxy-phenyl)-ethyl-amide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid 2-amino-1-(3,4-dichloro-phenyl)-ethyl-amide,
2-Chloro-N-3-({3-(1H-pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carbonylamino}-methyl)-phenyl-isonicotinamide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid 2-amino-1-(3-chloro-phenyl)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(1-phenyl-ethylamino)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-amino-1-(4-trifluoromethyl-phenyl)-ethyl-amide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid 2-amino-1-(4-trifluoromethyl-phenyl)-ethyl-amide,
(S)-3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid2-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-1-phenyl-ethyl-amide,
(S)-2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid2-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-1-phenyl-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(4-methyl-benzylamino)-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 2-(3-chloro-4-methoxy-benzylamino)-ethyl-amide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid ((R)-2-cyano-1-phenyl-ethyl)-amide,
2-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-3-carboxylic acid ((S)-2-amino-1-phenyl-ethyl)-amide,
2-Pyrrolidin-1-yl-N-3-({3-(1H-pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carbonyl-amino}-methyl)-phenyl-isonicotinamide,
2-Dimethylamino-N-3-({3-(1H-pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carbonyl-amino}-methyl)-phenyl-isonicotinamid,
2-(4-Methyl-piperazin-1-yl)-N-3-({3-(1H-pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carbonyl-amino}-methyl)-phenyl-isonicotinamide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 1-(3-fluoro-phenyl)-2-methylamino-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid 1-(3-chloro-phenyl)-2-methylamino-ethyl-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (2-methylamino-1-phenyl-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid ((S)-2-amino-1-phenyl-ethyl)-amide,
3-(1H-Pyrrolo2,3-bpyridin-4-ylamino)-thiophene-2-carboxylic acid (S)-2-amino-1-(3-fluoro-phenyl)-ethyl-amide,
3-(7H-Pyrrolo2,3-dpyrimidin-4-ylamino)-thiophene-2-carboxylic acid benzylamide,
3-(7H-Pyrrolo2,3-dpyrimidin-4-ylamino)-thiophene-2-carboxylic acid 2-(3-fluorophenyl)-ethyl-amide,
3-(7H-Pyrrolo2,3-dpyrimidin-4-ylamino)-furan-2-carboxylic acid 3-chloro-benzylamide,
3-(7H-Pyrrolo2,3-dpyrimidin-4-ylamino)-thiophene-2-carboxylic acid 2-(3-chloro-phenyl)-ethyl-amide,
3-(5-Methyl-7H-pyrrolo2,3-dpyrimidin-4-ylamino)-thiophene-2-carboxylic acid 3-chloro-benzylamide.
and pharmaceutically acceptable salts, solvates or prodrugs thereof.
25. A pharmaceutical composition comprising a compound according to claim 1, or a pharmaceutically acceptable salt, solvate or prodrug thereof, as active ingredient, together with a pharmaceutically acceptable carrier.
26. A pharmaceutical composition comprising a compound according to claim 4, or a pharmaceutically acceptable salt, solvate or prodrug thereof, as active ingredient, together with a pharmaceutically acceptable carrier.
27. A method for the treatment of a hyperproliferative disease comprising, adminstering a compound of claim 1, or a pharmaceutically acceptable salt, solvate or prodrug thereof, to a patient presenting at least one symptom of said hyperproliferative disease under conditions such that at least one symptom of said hyperproliferative disease is substantially improved.
28. A method for the treatment of a hyperproliferative disease comprising, adminstering a compound of claim 4, or a pharmaceutically acceptable salt, solvate or prodrug thereof, to a patient presenting at least one symptom of said hyperproliferative disease under conditions such that at lease one symptom of said hyperproliferative disease is substantially improved.
29. The method of claim 27 wherein said hyperproliferative disease is selected from the group consisting of cancer, inflammation, pancreatitis or kidney disease, pain, benign hyperplasia of the skin, restenosis, prostate, diseases related to vasculogenesis or angiogenesis, tumor angiogenesis, skin diseases selected from psoriasis, eczema, and sclerodema, diabetes, diabetic retinopathy, retinopathy of prematurity, age-related macular degeneration, hemangioma, glioma, melanoma and Kaposi’s sarcoma.
30. The method of claim 28 wherein said hyperproliferative disease is selected from the group consisting of cancer, inflammation, pancreatitis or kidney disease, pain, benign hyperplasia of the skin, restenosis, prostate, diseases related to vasculogenesis or angiogenesis, tumor angiogenesis, skin diseases selected from psoriasis, eczema, and sclerodema, diabetes, diabetic retinopathy, retinopathy of prematurity, age-related macular degeneration, hemangioma, glioma, melanoma and Kaposi’s sarcoma.
31. Set (kit) consisting of separate packs of:
a) an effective amount of a compound according to claim 1 or a pharmaceutically acceptable salt, solvate or prodrug thereof, and
b) an effective amount of a further medicament active ingredient.
32. Set (kit) consisting of separate packs of:
c) an effective amount of a compound according to claim 4 or a pharmaceutically acceptable salt, solvate or prodrug thereof, and
d) an effective amount of a further medicament active ingredient.
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 method of fabricating a turbine blade assembly for a gas turbine engine, the turbine blade assembly including a platform, a turbine airfoil extending radially outward from the platform, a shank extending radially inward from the platform, and a dovetail extending from the shank, the platform including a leading edge, a trailing edge, a pressure edge, and a suction edge, said method comprising:
forming the platform pressure edge into a plurality of arcs to facilitate reducing stress concentrations; and
forming the platform suction edge into a plurality of arcs complementary to the pressure edge.
2. A method in accordance with claim 1 wherein forming the platform pressure edge further comprises forming the platform pressure edge into at least two substantially linear segments separated by at least one arc.
3. A method in accordance with claim 1 wherein forming the platform pressure edge further comprises forming the platform pressure edge into at least one concave arc and at least one convex arc.
4. A method in accordance with claim 1 wherein forming the platform pressure edge further comprises:
forming the platform pressure edge into at least two substantially linear portions separated by at least one convex arc; and
forming the platform suction edge into at least two substantially linear portions separated by at least one concave arc.
5. A turbine blade assembly for a gas turbine engine, said turbine blade assembly comprising:
a platform;
a turbine airfoil extending radially outward from said platform;
a shank extending radially inward from said platform; and
a dovetail extending from said shank, said platform comprising a leading edge and a trailing edge separated by a pressure edge and an opposite suction edge, said pressure edge comprising a plurality of arcs extending between said leading edge and said trailing edge, said suction edge comprising a plurality of arcs extending between said leading and trailing edges.
6. A turbine blade assembly in accordance with claim 5 wherein said pressure edge arcs and said suction edge arcs configured to reduce stresses induced to said turbine blade assembly.
7. A turbine blade assembly in accordance with claim 5 wherein said pressure edge further comprises at least two substantially linear portions.
8. A turbine blade assembly in accordance with claim 5 wherein said pressure edge arcs comprises at least one concave arc and at least one convex arc.
9. A turbine blade assembly in accordance with claim 5 wherein said pressure edge further comprises at least three substantially linear portions separated by at least one concave arc and by at least one convex arc.
10. A turbine blade assembly in accordance with claim 5 wherein said turbine airfoil comprises a pressure side, a suction side, and a high-c portion, said platform suction edge further comprises a first substantially linear portion extending from said leading edge to adjacent said turbine airfoil high-c portion.
11. A turbine blade assembly in accordance with claim 5 wherein said turbine airfoil comprises a pressure side, a suction side, and a turbine airfoil trailing edge, said platform pressure edge further comprises at least one substantially linear portion extending from said trailing edge to adjacent said turbine airfoil trailing edge.
12. A turbine blade assembly in accordance with claim 5 wherein at least one of said pressure edge and said suction edge further comprises a first portion angularly displaced from said leading edge by about 102 degrees, and a second portion angularly displaced from said trailing edge by about 117 degrees.
13. A gas turbine engine comprising at least one turbine blade assembly comprising:
a platform;
a turbine airfoil extending radially outward from said platform;
a shank extending radially inward from said platform; and
a dovetail extending from said shank, said platform comprising a leading edge and a trailing edge separated by a pressure edge and an opposite suction edge, said pressure edge comprising a plurality of arcs extending between said leading edge and said trailing edge, said suction edge comprising a plurality of arcs extending between said leading and trailing edges.
14. A gas turbine engine in accordance with claim 13 wherein said pressure edge arcs and said suction edge arcs configured to reduce stresses induced to said turbine blade assembly.
15. A gas turbine engine in accordance with claim 13 wherein said pressure edge further comprises at least two substantially linear portions.
16. A gas turbine engine in accordance with claim 13 wherein said pressure edge arcs comprise at least one concave arc and at least one convex arc.
17. A gas turbine engine in accordance with claim 13 wherein said pressure edge further comprises at least three substantially linear portions separated by at least one concave arc and by at least one convex arc.
18. A gas turbine engine in accordance with claim 13 wherein said turbine airfoil comprises a pressure side, a suction side, and a high-c portion, said platform suction edge further comprises a first substantially linear portion extending from said leading edge to adjacent said turbine airfoil high-c portion.
19. A gas turbine engine in accordance with claim 13 wherein said turbine airfoil comprises a pressure side, a suction side, and a turbine airfoil trailing edge, said platform pressure edge further comprises at least one substantially linear portion extending from said trailing edge to adjacent said turbine airfoil trailing edge.
20. A gas turbine engine in accordance with claim 13 wherein at least one of said pressure edge and said suction edge further comprises a first portion angularly displaced from said leading edge by about 102 degrees, and a second portion angularly displaced from said trailing edge by about 117 degrees.