Patent ID: 6384048
Filing Date: 2002-05-07
Classification: A61P,C07D

Abstract:
A compound of the formula I in whichR1 is 1-4C-alkyl, R2 is 1-4C-alkyl or hydroxy-1-4C-alkyl, R3 is hydrogen or halogen, one of the substituents R4a and R4b is hydrogen and the other is hydrogen, hydroxyl, 1-4C-alkoxy, 1-4C-alkoxy-1-4C-alkoxy, 1-4C-alkylcarbonyloxy or the radical R4â€², or R4a and R4b together are O (oxygen), where, R4â€² is â€”Oâ€”(CH2)mS(O)nâ€”R9, â€”S(O)nâ€”(CH2)mâ€”OH, â€”S(O)nâ€”(CH2)mâ€”Oâ€”R9, â€”S(O)nâ€”(CH2)mâ€”S(O)pâ€”R9, â€”O-alk1-S(O)nâ€”R9, â€”S(O)nâ€”R9, â€”S(O)n-alk1-OH, â€”S(O)n-alk1-O-R9 or â€”S(O)n-alk1-S(O)p-R9, in which R9 is 1-7C-alkyl, halo-1-4C-alkyl, hydroxy-1-4C-alkyl, 1-4C-alkoxy-1-4C-alkyl, carboxy-1-4C-alkyl, 1-4C-alkoxycarbonyl-1-4C-alkyl or di-1-4C-alkylamino-1-4C-alkyl, Ar or Ar-1-4C-alkyl, where Ar is phenyl or substituted phenyl having one, two or three identical or different substituents selected from the group consisting of 1-4C-alkyl, 1-4C-alkoxy, 1-4C-alkylcarbonyl, 1-4C-alkoxycarbonyl, halogen, trifluoromethyl, difluoromethoxy, trifluoromethoxy, amino, 1-4C-alkoxycarbonylamino, 1-4C-alkoxy-1-4C-alkoxycarbonylamino and nitro, alk1 is 1-4C-alkyl-, hydroxyl-, oxo-, carboxyl-, halogen-, amino-, 1-4C-alkoxycarbonylamino- or phenyl-substituted 2-7C-alkylene or 3-4C-alkenylene, m is an integer from 2 to 7, n is the number 0, 1 or 2 and p is the number 0, 1 or 2, one of the substituents R5a and R5b is hydrogen and the other is hydrogen, hydroxyl, 1-4C-alkoxy, 1-4C-alkoxy-1-4C-alkoxy, 1-4C-alkylcarbonyloxy or the radical R5â€², or R5a and R5b together are O (oxygen) where R5â€² is â€”Oâ€”(CH2)qâ€”S(O)râ€”R10, â€”S(O)râ€”(CH2)qâ€”OH, â€”S(O)râ€”(CH2)qâ€”Oâ€”R10, â€”S(O)r(CH2)qâ€”S(O)tâ€”R10, â€”O-alk2-S(O)râ€”R10, â€”S(O)râ€”R10, â€”S(O)r-alk2-OH, â€”S(O)ralk2-Oâ€”R10 or â€”S(O)r-alk2-S(O)tâ€”R10, in whichR10 is 1-7C-alkyl, halo-1-4C-alkyl, hydroxy-1-4C-alkyl, 1-4C-alkoxy-1-4C-alkyl, carboxy-1-4C-alkyl, 1-4C-alkoxycarbonyl-1-4C-alkyl or di-1-4C-alkylamino-1-4C-alkyl, Ar or Ar-1-4C-alkyl, where Ar is phenyl or substituted phenyl having one, two or three identical or different substituents selected from the group consisting of 1-4C-alkyl, 1-4C-alkoxy, 1-4C-alkylcarbonyl, 1-4C-alkoxycarbonyl, halogen, trifluoromethyl, difluoromethoxy, trifluoromethoxy, amino, 1-4C-alkoxycarbonylamino, 1-4C-alkoxy-1-4C-alkoxycarbonylamino and nitro, alk2 is 1-4C-alky-, hydroxyl-, oxo-, carboxyl-, halogen-, amino-, 1-4C-alkoxycarbonylamino- or phenyl-substituted 2-7C-alkylene or 3-4C-alkenylene, q is an integer from 2 to 7, r is the number 0, 1 or 2 and t is the number 0, 1 or 2, R6 is hydrogen, halogen, 1-4C-alkyl, 1-4C-alkoxy, 1-4C-alkoxycarbonylamino, 1-4C-alkoxy-1-4C-alkoxycarbonylamino or trifluoromethyl, R7 is hydrogen, halogen, 1-4C-alkyl or 1-4C-alkoxy and R8 is hydrogen or 1-4C-alkyl, and its salts, where one of the substituents R4a and R4b has to be R4â€² and/or one of the substituents R5a and R5b has to be R5â€².