Patent ID: 6414009
Filing Date: 2002-07-02
Classification: A61P,C07D

Abstract:
A 1-Benzyl-3-(substituted heteroaryl)-fused pyrazole derivative of the formula (IV-I) in which A4 represents phenyl, which is optionally substituted up to 3 times in an identical or different manner by halogen, hydroxyl, cyano, carboxyl, nitro, trifluoromethyl, trifluoromethoxy, azido, straight-chain or branched alkyl, alkoxy or alkoxycarbonyl having in each case up to 6 carbon atoms, R69 represents a radical of the formula wherein R72 denotes a radical of the formula â€”CH(OH)â€”CH3 or straight-chain or branched alkyl having 2 to 6 carbon atoms, which is substituted once to twice by hydroxyl or straight-chain or branched alkoxy having up to 4 carbon atoms, or denotes formyl, straight-chain or branched acyl having up to 6 carbon atoms, nitro or straight-chain or branched alkyl having up to 6 carbon atoms, which is substituted by amino, azido or by a radical of the formula â€”OR73, wherein R73 denotes straight-chain or branched acyl having up to 5 carbon atoms or a group of the formula â€”SiR74R75R76, wherein R74, R76 and R76 are identical or different and denote aryl having 6 to 10 carbon atoms or straight-chain or branched alkyl having up to 6 carbon atoms, R78 denotes hydrogen or straight-chain or branched alkyl having up to 3 carbon atoms and R79 denotes hydrogen or straight-chain or branched alkyl having up to 4 carbon atoms, or R72 denotes a group of the formula wherein R80 denotes hydrogen or straight-chain or branched alkyl having up to 4 carbon atoms, R81 denotes hydrogen or straight-chain or branched alkyl having up to 4 carbon atoms and a4 denotes the number 1, 2 or 3, b4 and b4â€² are identical or different and denote the number 0, 1, 2 or 3, c4 denotes the number 1 or 2 and R82 and R83 are identical or different and denote hydrogen or straight-chain or branched alkyl having up to 10 carbon atoms, which is optionally substituted by cycloalkyl having 3 to 8 carbon atoms or by aryl having 6 to 10 carbon atoms, which in its turn can be substituted by halogen, or denote aryl having 6 to 10 carbon atoms, which is optionally substituted by halogen, or denote cycloalkyl having 3 to 7 carbon atoms, or R82 and R83, together with the nitrogen atom, form a 5- to 7-membered saturated heterocyclic ring, which can optionally contain a further oxygen atom or a radical â€”NR84, wherein R84 denotes hydrogen, straight-chain or branched alkyl having up to 4 carbon atoms or a radical of the formula or denotes benzyl or phenyl, wherein the ring systems are optionally substituted by halogen, or R72 denotes a group of the formula â€”CH2â€”OR85, wherein R85 denotes hydrogen or straight-chain or branched alkyl having up to 3 carbon atoms, R70 and R71 together form a radical of the formula wherein R86 denotes hydrogen, halogen, hydroxyl, nitro, amino, trifluoromethyl or straight-chain or branched alkyl or alkoxy having in each case up to 4 carbon atoms, or a group of the formula â€”S(O)c4â€²NR82â€²R83â€², wherein c4â€², R82â€² and R83â€² have the abovementioned meaning of c4, R82 and R83 and are identical to or different from these, or an isomer or salt thereof, with the proviso that R72, in the case of the phenyl ring and in the position directly adjacent to the heteroatom, may represent the group of the formula â€”CH2â€”OR85 only if A4 either represents phenyl, which is substituted by cyano, nitro, trifluoromethyl, azido, carboxyl or straight-chain or branched alkoxycarbonyl having up to 6 carbon atoms, or is substituted at least twice by the radicals listed above, or R86 represents nitro, amino, trifluoromethyi or represents the group of the formula â€”S(O)c4NR82â€²R83â€².