Patent ID: 6166027
Filing Date: 2000-12-26
Classification: A61P,C07D

Abstract:
A 1-Heterocyclyl-methyl-substituted pyrazole of the formula (II-I) ##STR359## in which R.sup.20 represents a 6-membered aromatic heterocyclic ring having up to 3 nitrogen atoms, which is optionally substituted up to 3 times in an identical or different manner by formyl, carboxyl, hydroxyl, mercaptyl, straight-chain or branched acyl, alkoxy, alkylthio or alkoxycarbonyl having in each case up to 6 carbon atoms, nitro, cyano, azido, halogen, phenyl and/or by a group of the formula--NR.sup.23 R.sup.24whereinR.sup.23 and R.sup.24 are identical or different and denote hydrogen or straight-chain or branched acyl having up to 6 carbon atoms or straight-chain or branched alkyl having up to 6 carbon atoms, which is optionally substituted by cycloalkyl having 3 to 6 carbon atoms, hydroxyl, amino or by straight-chain or branched alkoxy, acyl or alkoxycarbonyl having in each case up to 5 carbon atoms,orR.sup.23 and R.sup.24, together with the nitrogen atom, form a 3- to 7-membered saturated or partly unsaturated heterocyclic ring, which can optionally additionally contain an oxygen or sulphur atom or a radical of the formula --NR.sup.25,whereinR.sup.25 denotes hydrogen or straight-chain or branched alkyl having up to 4 carbon atoms,and/or is substituted by straight-chain or branched alkyl having up to 6 carbon atoms, which in its turn can be substituted by hydroxyl, amino, halo 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 ---OR.sup.26 ,whereinR.sup.26 denotes straight-chain or branched acyl having up to 5 carbon atoms or a group of the formula --SiR.sup.27 R.sup.28 R.sup.29,whereinR.sup.27, R.sup.28 and R.sup.29 are identical or different and denote aryl having 6 to 10 carbon atoms or alkyl having up to 6 carbon atoms,and/or is optionally substituted by a radical of the formula ##STR360## wherein b2 and b2' are identical or different and denote the number 0, 1, 2 or 3,a2 denotes the number 1, 2 or 3,R.sup.30 denotes hydrogen or straight-chain or branched alkyl having up to 4 carbon atoms,c2 denotes the number 1 or 2 andR.sup.31 and R.sup.32 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, ordenote aryl having 6 to 10 carbon atoms, which is optionally substituted by halogen, ordenote cycloalkyl having 3 to 7 carbon atoms, orR.sup.31 and R.sup.32, 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 --NR.sup.33,whereinR.sup.33 denotes hydrogen, straight-chain or branched alkyl having up to 4 carbon atoms or a radical of the formula ##STR361## or denotes benzyl or phenyl, wherein the ring systems are optionally substituted by halogen,R.sup.21 and R.sup.22, including the double bond, form a 5-membered aromatic heterocyclic ring having a heteroatom from the series consisting of S, N and/or O, or a phenyl ring, which are optionally substituted up to 3 times in an identical or different manner by formyl, mercaptyl, carboxyl, hydroxyl, amino, straight-chain or branched acyl, alkylthio, alkoxy or alkoxycarbonyl having in each case up to 6 carbon atoms, nitro, cyano, azido, 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, or are optionally substituted by a group of the formula --S(O).sub.c2.NR.sup.31' R.sup.32' wherein c.sub.2., R.sup.31 ' and R.sup.32 ' have the abovementioned meaning of c2, R.sup.- and R.sup.32 and are identical to or different from these,A.sup.2 represents phenyl or 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, which is optionally substituted up to 3 times in an identical or different manner by 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,and/or is substituted by a group of the formula --(CO).sub.d2 --NR.sup.34 R.sup.35,whereind2 denotes the number 0 or 1,R.sup.34 and R.sup.35 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, and an isomer, salt and N-oxide thereof.