Patent ID: 6451805
Filing Date: 2002-09-17
Classification: C07D

Abstract:
A substituted pyrazole compound of the formula (I): in whichR1 represents pyrimidinyl, is optionally substituted by 1 to 3 substituents independently selected from the group consisting of amino, azido, formyl, mercaptyl, carboxyl, hydroxyl, straight-chain or branched acyl having up to 6 carbon atoms, straight-chain or branched alkoxy having up to 6 carbon atoms, straight-chain or branched alkylthio having up to 6 carbon atoms, straight-chain or branched alkoxycarbonyl having up to 6 carbon atoms, nitro, cyano, halogen, phenyl, and alkyl having up to 6 carbon atoms, which alkyl is optionally substituted by hydroxyl, amino, azido, carboxyl, straight-chain or branched acyl having up to 5 carbon atoms, straight-chain or branched alkoxy having up to 5 carbon atoms, straight-chain or branched alkoxycarbonyl having up to 5 carbon atoms, straight-chain or branched acylamino having up to 5 carbon atoms, or a radical of the formula â€”OR4; â€ƒin which R4 represents straight-chain or branched acyl having up to 5 carbon atoms, or a group of the formula â€”SiR5R6R7; â€ƒin which R5, R6 and R7 independently represent aryl having 6 to 10 carbon atoms or alkyl having up to 6 carbon atoms; or the pyrimidinyl is substituted by a radical of the formula: â€”S(O)câ€”NR9R10, â€ƒin which a, b and bâ€² independently represent a number 0, 1, 2 or 3; R8 represents hydrogen or straight-chain or branched alkyl having up to 4 carbon atoms; c represents a number 1 or 2; and R9 and R10 independently represent hydrogen, straight-chain or branched alkyl having up to 10 carbon atoms, which alkyl can be optionally substituted by cycloalkyl having 3 to 8 carbon atoms or by optionally halogen substituted aryl having 6 to 10 carbon atoms, aryl having 6 to 10 carbon atoms, which aryl is optionally substituted by halogen, or cycloalkyl having 3 to 7 carbon atoms; R2 and R3, together with the carbon atoms to which they are attached and the double bond joining said carbon atoms, form a pyridinyl ring, which is optionally substituted by 1 to 3 substituents independently selected from the group consisting. of formyl, carboxyl, hydroxyl, mercaptyl, straight-chain or branched acyl having up to 6 carbon atoms, straight-chain or branched alkylthio having up to 6 carbon atoms, straight-chain or branched alkoxy having up to 4 carbon atoms, straight-chain or branched alkoxycarbonyl having up to 6 carbon atoms, nitro, cyano, azido, halogen, straight-chain or branched alkyl having up to 6 carbon atoms, or straight-chain or branched alkoxy having up to 6 carbon atoms, which allyl or alkoxy is optionally substituted by hydroxyl, amino, carboxyl, straight-chain or branched acyl having up to 5 carbon atoms, straight-chain or branched alkoxy having up to 5 carbon atoms, or straight-chain or branched alkoxycarbonyl having up to 5 carbon atoms; or the pyridinyl is optionally substituted by a group of the formula â€”NR12R13 or â€”S(O)câ€²NR9â€²R10â€²; â€ƒin which R12 and R13 independently represent hydrogen or straight-chain or branched alkyl having up to 6 carbon atoms; or R12 represents hydrogen; and R13 represents formyl; câ€² represents a number 1 or 2; and R9â€² and R10â€² independently represent hydrogen, straight-chain or branched alkyl having up to 10 carbon atoms, which alkyl can be optionally substituted by cycloalkyl having 3 to 8 carbon atoms or by optionally halogen substituted aryl having 6 to 10 carbon atoms, aryl having 6 to 10 carbon atoms, which aryl is optionally substituted by halogen, or cycloalkyl having 3 to 7 carbon atoms; or the pyridinyl is optionally substituted by phenyl, which phenyl is optionally substituted by 1 or 2 substituents independently selected from the group consisting of halogen, straight-chain or branched alkyl having up to 6 carbon atoms, and straight-chain or branched alkoxy having up to 6 carbon atoms; and/or the pyridinyl is optionally substituted by a group of the formula â€”N&boxH;CHâ€”NR14R15; â€ƒin which R14 and R15 independently represent hydrogen, phenyl or straight-chain or branched alkyl having up to 6 carbon atoms; A represents phenyl, which is optionally substituted by 1 to 3 substituents independently selected from the group consisting of amino, mercaptyl, hydroxyl, formyl, carboxyl, straight-chain or branched acyl having up to 6 carbon atoms, straight-chain or branched alkylthio having up to 6 carbon atoms, straight-chain or branched alkyloxyacyl having up to 6 carbon atoms, straight-chain or branched alkoxy having up to 6 carbon atoms, straight-chain or branched aloxycarbonyl having up to 6 carbon atoms, nitro, cyano, trifluoromethyl, azido, halogen, phenyl, or straight-chain or branched alkyl having up to 6 carbon atoms, which alkyl is optionally substituted by hydroxyl, carboxyl, straight-chain or branched acyl having up to 5 carbon atoms, straight-chain or branched alkoxy having up to 5 carbon atoms, or straight-chain or branched alkoxycarbonyl having up to 5 carbon atoms; or â€ƒthe phenyl group A is optionally substituted by a group of the formula â€”(CO)dâ€”NR16R17; â€ƒin which d represents a number 0 or 1; and R16 and R17 independently represent hydrogen, phenyl, benzyl, straight-chain or branched alkyl having up to 5 carbon atoms, or straight-chain or branched acyl having up to 5 carbon atoms; and a purified stereoisomes thereof or a salt thereof.