Patent ID: 6162809
Filing Date: 2000-12-19
Classification: A61P,C07D

Abstract:
A compound of the formula I in whichR is hydrogen, 1-4C-alkyl, halogen, trifluoromethyl, 1-4C-alkoxycarbonyl, carboxyl or cyano,R1 is hydrogen or 1-4C-alkyl,R2 is hydrogen or 1-4C-alkyl,R3 is hydrogen, 1-4C-alkyl, 1-4C-alkoxy or halogen,R4 is a mono- or di-1-4C-alkylcarbamoyl or -thiocarbamoyl radical, an N-1-4C-alkyl-N'-cyanoamidino radical, a 1-N-1-4C-alkylamino-2-nitroethylene radical, an N-2-propynyl-N'-cyanoamidino radical, an aminosulfonylamidino radical, the radical --N(R7)R8 or an R9- and R10-substituted cyclic system or bicyclic system which is selected from the group consisting of benzene, naphthalene, furan, thiophene, pyrrole, oxazole, isoxazole, thiazole, thiazoline, isothiazole, imidazole, imidazoline, pyrazole, triazole, tetrazole, thiadiazole, thiadiazole-1-oxide, oxadiazole, pyridine, pyridine-N-oxide, pyrimidine, triazine, pyridone, benzimidazole, imidazopyridine, benzothiazole, benzoxazole and quinoline,R5 is hydrogen, 1-4C-alkyl, 1-4C-alkoxy or halogen,R6 is hydrogen or 1-4C-alkyl,R7 is 1-7C-alkyl, 3-7C-cycloalkyl or Ar-1-4C-alkyl andR8 is 1-7C-alkyl, 3-7C-cycloalkyl or Ar-1-4C-alkyl, whereAr is phenyl, furyl, naphthyl, tetrahydronaphthyl or R11-, R12- and R13-substituted phenyl, or in whichR7 and R8 together, and including the nitrogen atom to which both are bonded, are an unsubstituted or substituted 5- or 6-membered ring hetero(bi)cyclic system, which is selected from the group consisting of piperidine, piperazine, morpholine, indoline, 1,2,3,4-tetrahydroquinoline and 1,2,3,4-tetrahydroisoquinoline, wherea substituted piperidino radical is substituted by one, two or three identical or different substituents selected from the group consisting of 1-4C-alkyl, 1-4C-alkoxycarbonyl, hydroxy-1-4C-alkyl, phenyl, R11-, R12- and R13-substituted phenyl, phenyl-1-4C-alkyl, benzoyl, halogen-substituted benzoyl and carboxyl,a substituted piperazino radical can be substituted in the 2-, 3-, 5- or 6-position by a 1-4C-alkyl radical and is substituted in the 4-position by a substituent selected from the group consisting of 1-4C-alkyl, 3-7C-cycloalkyl, 3-7C-cycloalkyl-1-4C-alkyl, 1-4C-alkoxycarbonyl-1-4C-alkyl, carbamoyl, --C.sub.p H.sub.(2p-2) --R14 and --C.sub.q H.sub.2q --R14,a substituted morpholino radical is substituted by one or two identical or different 1-4C-alkyl radicals,a substituted indolin-1-yl radical, substituted in the 2- and/or 3-position by a carboxyl group or by one or two identical or different 1-4C-alkyl radicals, or substituted in the benzo moiety by one or two identical or different substituents selected from the group consisting of 1-4C-alkyl, halogen and nitro,a substituted 1,2,3,4-tetrahydroquinoline radical is substituted by one or two identical or different substituents selected from the group consisting of 1-4C-alkyl and halogen,a substituted 1,2,3,4-tetrahydroisoquinoline radical is substituted by one or two identical or different substituents selected from the group consisting of 1-4C-alkyl, carboxyl and phenyl,R9 is hydrogen, 1-4C-alkyl, hydroxyl, 1-4C-alkoxy, halogen, nitro, guanidino, carboxyl, 1-4C-alkoxycarbonyl, R15-substituted 1-4C-alkyl or --N(R16)R17,R10 is hydrogen, 1-4C-alkyl, hydroxyl, 1-4C-alkoxy, halogen or trifluoromethyl,R11 is hydrogen, 1-4C-alkyl, hydroxyl 1-4C-alkoxy, 1-4C-alkylcarbonyl, halogen, 1-4C-alkylamino or nitro,R12 is hydrogen, 1-4C-alkyl, hydroxyl, 1-4C-alkoxy, halogen or nitro, andR13 is hydrogen or trifluoromethyl,R14 is an R9- and R10-substituted cyclic system or bicyclic system which is selected from the group consisting of benzene, naphthalene, furan, thiophene, pyrrole, oxazole, isoxazole, thiazole, thiazoline, isothiazole, imidazole, imidazoline, pyrazole, triazole, tetrazole, thiadiazole, oxadiazole, pyridine, pyridine-N-oxide, pyrimidine, benzimidazole and quinoline,R15 is hydroxyl, 1-4C-alkoxy, carboxyl, 1-4C-alkoxycarbonyl or --N(R16)R17, whereR16 is hydrogen, 1-4C-alkyl or --CO--R18 andR17 is hydrogen or 1-4C-alkyl, or whereR16 and R17, together and including the nitrogen atom to which both are bonded, are a piperidino or morpholino radical,R18 is hydrogen, 1-4C-alkyl or 1-4C-alkoxy,W is CH or N,X is O (oxygen), N-1-4C-alkyl or S,Y is O (oxygen), N-1-4C-alkyl, S, SO or SO.sub.2,Z is O (oxygen), N-1-4C-alkyl, S, SO or SO.sub.2,m is a number from 1 to 7,n is the number 0, 1 or 2,r is a number from 2 to 4,t is the number 0 or 1,u is a number from 0 to 4,v is the number 0 or 1,p is a number from 2 to 4 andq is a number from 0 to 4or a salt thereof, wheret and/or v are not the number 1 if m is the number 1,Z is not SO or SO.sub.2 if u is the number 0, and whereR4 is not --N(R7)R8 or an N (nitrogen)-bonded cyclic system or bicyclic system if Z is O, S, SO or SO.sub.2, v is the number 1 and u is the number 0.