Patent ID: 6365736
Filing Date: 2002-04-02
Classification: A61P,C07D

Abstract:
A compound of formulae Ia and/or Ib, including tautomeric or isomeric forms or salts: in whichX means O or S, R1 means NO2, cyano, CF3, â€”OCF3, â€”SO2NR7R8, â€”CONR7R8, â€”NR9â€”C(&boxH;NR10)â€”R11, â€”NHâ€”CSâ€”NR7R8, â€”NHâ€”COâ€”NR7R8, NR12R13, or â€”COâ€”R14; or C6-10 aryl which optionally is substituted with halogen, cyano C1-4 alkyl, â€”Sâ€”R9, â€”OR9, â€”NR7R8 or CONR7R8; or a 5- or 6-membered heteroaryl ring with 1 to 4 heteroatoms selected from oxygen, nitrogen or sulfur, which optionally is substituted with â€”OR9, â€”SR9, halogen, C1-4-alkyl, NR7R8 or CONR7R8; or C1-6 alkyl which is substituted with halogen, â€”OR9, â€”SR9, â€”NR7R8, â€”NR7â€²R8â€², &boxH;NR7, &boxH;NOC1-6 alkyl, &boxH;N-NHaryl, phenyl, C3-7 cycloalkyl or 5- or 6-membered heteroaryl; or C2-6 alkenyl which is substituted with halogen, CONH2, C/N or phenyl; or C2-6 alkynyl, which is substituted with halogen, CONH2, C/N or phenyl; or C3-7 cycloalkyl, R2 means hydrogen or R1 and R2 together with two adjacent carbon atoms form a 5-, 6-, 7- or 8-membered ring, which is monocyclic or bicyclic, saturated or unsaturated, and which is optionally substituted with â€”NR7R8, â€”NR7â€²R8â€² or C1-4 alkyl, R3 means hydrogen, halogen, â€”Sâ€”R9 or â€”Oâ€”R9 or, independently has one of meanings of R1, R4 means hydrogen or acyl, R5 means hydrogen, R6 means C3-7 cycloalkyl, C6-10 aryl, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl radicals, which are each optionally substituted with halogen, OH, Oâ€”C1-6 alkyl, SH, Sâ€”C1-6 alkyl, NR15R16, 5- or 6-membered heteroaryl with 1-3 N, O or S atoms, phenyl or C3-7 cycloalkyl, R7 and R8 mean hydrogen, C1-6 alkyl, phenyl optionally substituted with halogen or C1-4 alkyl, benzyl optionally substituted with halogen or C1-4 alkyl or C3-7 cycloalkyl, R7â€² means hydrogen, C1-6 alkyl optionally substituted with OH, phenyl, cyano, COOâ€”C1-4 alkyl or carbonyl, R8â€² means C1-6 alkyl, which is substituted with C3-7 cycloalkyl, indanyl, C6-10 aryl or 5- or 6-membered heteroaryl with 1-3 nitrogen, oxygen or sulfur atoms, whereby the aryl and heteroaryl radicals are optionally substituted with halogen, C1-4 alkyl, C1-4 alkoxy, CF3, NO2, NH2, N(C1-4 alkyl)2, SO2CH3, â€”Oâ€”CH2â€”O, SO2NH2, OH or COOâ€”C1-4 alkyl or indanyl or 1,2,3,4-tetrahydronaphthyl, or R7â€² and R8â€² together with the nitrogen atom form a 5- to 7-membered saturated heterocycle, which optionally contains another oxygen, nitrogen or sulfur atom and is optionally substituted with C1-4 alkyl, phenyl, benzyl or benzoyl or forms an unsaturated 5-membered heterocycle, which contains a further 1-3 N atoms and is optionally substituted with phenyl, C1-4 alkyl, halogen or CH2â€”OH, R9, R10 and R15, R16 mean hydrogen or C1-6 alkyl, R11 means C1-6 alkyl, â€”NH2, â€”NHâ€”CH3, â€”NHâ€”CN, C6-10 aryl optionally substituted with halogen, C1-4 alkyl or CF3, or 5- or 6-membered heteroaryl with 1 to 4 nitrogen, sulfur or oxygen atoms that is optionally substituted with halogen, C1-4 alkyl or CF3, m means 0, 1 or 2, R12, R13 together with the nitrogen atom form a saturated 5-, 6- or 7-membered ring, which optionally contains another nitrogen, oxygen or sulfur atom and is optionally substituted with C1-4 alkyl, phenyl, benzyl or benzoyl, and R14 means hydrogen, phenyl, C1-6 alkyl optionally substituted with CO2H, CO2â€”C1-6 alkyl, hydroxy, C1-4 alkoxy, halogen, NR7R8, NR12R13, CONR7R8 or phenyl, or C2-6 alkenyl optionally substituted with phenyl, cyano, CONR7R8 or CO2C1-4 alkyl.