| 摘要 |
N1-thiazolyl-N3-aminosulfonylphenyl-urea derivatives (I) and their salts, hydrates and/or solvates are new. N1-thiazolyl-N3-aminosulfonylphenyl-urea derivatives of formula (I) and their salts, hydrates and/or solvates are new. R<1> = 1-6C alkyl, optionally substituted by 1-3 of amino (optionally substituted by 1-2 1-6C alkyl or by one 6-10C aryl or 5-10C heteroaryl), hydroxymethyl, carboxy, 1-6C alkoxy, 1-6C alkoxycarbonyl, aminocarbonyl, 1-6C alkoxycarbonylamino, 6-10C aryl, 5-10C heteroaryl, 3-8C cycloalkyl or 5-8 membered heterocyclyl; or 5-8 membered heterocyclyl or phenyl, and all (hetero)aryl, cycloalkyl or (hetero)arylamino can be substituted by 1-3 of halo, nitro, hydroxy, amino, trifluoromethyl, 1-6C alkyl or benzyloxy; R<2> = H or 1-6C alkyl; R<1>+R<2> = (thio)morpholino, 4-R<3>-piperazino or 4-R<4>-piperidino; R<3> = H, 1-6C alkyl, 6-10C aryl, 5-10C heteroaryl, 3-8C cycloalkyl, 5-8 membered heterocyclyl, 1-6C alkyl- or alkoxy-carbonyl, 3-8C cycloalkylcarbonyl or 5-8 membered heterocyclylcarbonyl, where alkyl is optionally substituted by 1-3 of oxo, hydroxy, 1-6C alkoxycarbonylamino, mono or di (1-6C) alkylamino, 1-6C alkylcarbonyl, 6-10C aryl, 5-10C heteroaryl, 3-8C cycloalkyl, 5-8 membered heterocyclyl (optionally substituted by one 1-6C alkyl) or 1-6C alkoxy (optionally substituted by one hydroxy), and (hetero)aryl, heterocyclyl, cycloalkyl- or heterocyclyl-carbonyl may be substituted by 1-3 of halo, amino, nitro, cyano, carboxy, hydroxy, oxo, trifluoromethyl, 1-6C alkyl or alkoxy, 1-6C alkoxycarbonyl or phenyl; R<4> = H, hydroxy, carboxy, 6-10C aryl, 5-10C heteroaryl, 5-8 membered heterocyclyl, 3-8C cycloalkyl-, 5-8 membered heterocyclyl- or 1-6C alkoxy-carbonyl, where cylcoalkyl- and heterocyclyl-carbonyl are optionally substituted by 1 or 2 of 1-6C alkyl or alkoxy, or by hydroxyethyl. An Independent claim is also included for preparation of (I) by reacting 3-(((1,3-thiazol-2-ylamino)carbonyl)amino)benzene sulfonyl fluoride (II) with HNR<1>R<2> in inert solvent.
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