发明名称 PHENYLTHIAZOLE AND THIAZOLINE DERIVATIVES AND THEIR USE AS ANTIPARASITICS
摘要 The present invention provides a new class of antiparatisitcs. The compounds found with the present invention are substituted thiazole- and thiazoline derivatives. The present invention is based on the discovery that such compounds have been found to have antiparasitic activity. The present invention relates to 4-phenyl thiazole derivatives of the following general formula (I): X in formula (I) may be N-R<6> or a bond. R<1> in formula (I) may be (1-8C)alkyl, (2-8C)alkenyl, (2-8C)alkynyl, (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, (6-14C)aryl, (3-13C)heteroaryl, (6-14C)aryl(1-8C)alkyl or (3-13C)heteroaryl(1-8C)alkyl. R<2> in formula (I) may be SO2NR<7>R<8>, CONR<7>R<8> or NR<7>R<8> R<3> and R<4> in formula (I) may independently be selected from H, halogen, (1-8C)alkyl, hydroxy, (1-8) alkoxy, cyano, nitro, (1-8C) alkoxycarbonyl, (1-8C)(di)alkylamino and (6-14C)(di)arylamino, or R<3> and R<4> are joined together in a 5-7 membered carbocyclic or heterocyclic ring. R<5> in formula (I) may be a halogen atom, (1-8C)alky, hydroxy, (1-8C)alkoxy, cyano, nitro, (1-8C)alkoxycarbonyl, (1-8C)(di)alkylamino or (6-14C)(di)arylamino. "n" may be 0-3. R<6> in formula (I) may be H or (1-8C)alkyl, (2-8C)alkenyl, (2-8C)alkynyl, (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, (6-14C)aryl, (3-13C)heteroaryl, (6-14C)aryl(1-8C)alkyl or (3-13C)heteroaryl(1-8C)alkyl. R<7> and R<8> in formula (I) may independently be selected from H, (1-8C)alkyl, (2-8C)alkenyl, (2-8C)alkynyl, (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, (6-14C)aryl, (3-13C)heteroaryl, (6-14C)aryl(1-8C)alkyl and (3-13C)heteroaryl(1-8C)alkyl, or R<7> and R<8> are joined together in a (2-7C) heterocycloalkyl ring.
申请公布号 WO02051410(A3) 申请公布日期 2003.07.31
申请号 WO2001EP15119 申请日期 2001.12.19
申请人 AKZO NOBEL N.V.;FRUECHTEL, JOERG;KOCH, SANDRA;NEWTON, TREVOR;MICULKA, CHRISTIAN;MCCONNELL, DARRYL;HOFMANN, JOACHIM 发明人 FRUECHTEL, JOERG;KOCH, SANDRA;NEWTON, TREVOR;MICULKA, CHRISTIAN;MCCONNELL, DARRYL;HOFMANN, JOACHIM
分类号 A61K31/351;A61K31/426;A61K31/427;A61K31/4439;A61K31/4725;A61K31/496;A61K31/517;A61K45/06;A61P33/00;A61P33/02;C07D277/42;C07D417/12 主分类号 A61K31/351
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