Patent ID: 6387940
Filing Date: 2002-05-14
Classification: A61P,C07D

Abstract:
A 3-Heterocyclyl-substituted pyrazole derivative of the formula (III-I) in whichR42 represents a saturated 6-membered heterocyclic ring having up to 2 heteroatoms from the series consisting of S, N and/or O or represents a 5-membered aromatic or saturated heterocyclic ring having 2 to 3 heteroatoms from the series consisting of S, N and/or O, which can also be bonded via a nitrogen atom and which are optionally substituted up to 3 times in an identical or different manner by formyl, phenyl, mercaptyl, carboxyl, trifluoromethyl, hydroxyl, straight-chain or branched acyl, alkoxy, alkylthio or alkoxycarbonyl having in each case up to 6 carbon atoms, nitro, cyano, halogen, phenyl or straight-chain or branched alkyl having up to 6 carbon atoms, which in its turn can be substituted by hydroxyl, halogen, trifluoromethyl, amino, carboxyl, straight-chain or branched acyl, alkoxy, alkoxycarbonyl or acylamino having in each case up to 5 carbon atoms or by a radical of the formula â€”OR45, wherein R45 denotes straight-chain or branched acyl having up to 5 carbon atoms or a group of the formula â€”SiR46R47R48, wherein R46, R47 and R48 are identical or different and denote aryl having 6 to 10 carbon atoms or alkyl having up to 6 carbon atoms, and/or can be substituted by a radical of the formula â€ƒwherein a3, b3 and b3â€² denote the number 0, 1, 2 or 3, R49 denotes hydrogen or straight-chain or branched alkyl having up to 4 carbon atoms, c3 denotes the number 1 or 2 and R50 and R51 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 â€ƒdenote aryl having 6 to 10 carbon atoms, which is optionally substituted by halogen, or â€ƒdenote cycloalkyl having 3 to 7 carbon atoms, or â€ƒR50 and R51, 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€”NR52, wherein R52 denotes hydrogen, straight-chain or branched alkyl having up to 4 carbon atoms or a radical of the formula â€ƒor denotes benzyl or phenyl, wherein the ring systems are optionally substituted by halogen, R43 and R44, including the double bond, form a 5-membered aromatic heterocyclic ring having one heteroatom from the series consisting of N, S and/or O, or a phenyl ring, which are optionally substituted up to 3 times in an identical or different manner by formyl, carboxyl, hydroxyl, amino, straight-chain or branched acyl, alkoxy or alkoxycarbonyl having in each case up to 6 carbon atoms, nitro, cyano, halogen, phenyl or straight-chain or branched alkyl having up to 6 carbon atoms, which in its turn can be substituted by hydroxyl, amino, carboxyl, straight-chain or branched acyl, alkoxy or alkoxycarbonyl having in each case up to 5 carbon atoms, â€ƒand/or are optionally substituted by a group of the formula â€”S(O)c3NR50â€²R51â€², wherein c3, R50â€² and R51â€² have the abovementioned meaning of c3, R50 and R51 and are identical to or different from these, A3 represents a 5- to 6-membered aromatic or saturated heterocyclic ring having up to 3 heteroatoms from the series consisting of S, N and/or O or phenyl, which are optionally substituted up to 3 times in an identical or different manner by amino, mercaptyl, hydroxyl, formyl, carboxyl, straight-chain or branched acyl, alkylthio, alkyloxyacyl, alkoxy or alkoxycarbonyl having in each case up to 6 carbon atoms, nitro, cyano, trifluoromethyl, azido, halogen, phenyl or straight-chain or branched alkyl having up to 6 carbon atoms, which in its turn can be substituted by hydroxyl, carboxyl, straight-chain or branched acyl, alkoxy or alkoxycarbonyl having in each case up to 5 carbon atoms, â€ƒand/or is substituted by a group of the formula (â€”CO)d3â€”NR53R54, wherein d3 denotes the number 0 or 1, R53 and R54 are identical or different and denote hydrogen, phenyl, benzyl or straight-chain or branched alkyl or acyl having in each case up to 5 carbon atoms, or an isomer or salt thereof.