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2. 发明申请

WO2005054206A1 HISTIDINE DERIVATIVES 审中-公开
公开(公告)号：WO2005054206A1
公开(公告)日：2005-06-16
申请号：PCT/EP2004/012944
申请日：2004-11-15
申请人： NEWRON PHARMACEUTICALS S.P.A. , MELLONI, Piero , SABIDO DAVID, Cibele, Maria , FARAVELLI, Laura , MAESTRONI, Sara , DONDIO, Giulio , SALVATI, Patricia
发明人： MELLONI, Piero , SABIDO DAVID, Cibele, Maria , FARAVELLI, Laura , MAESTRONI, Sara , DONDIO, Giulio , SALVATI, Patricia
IPC分类号： C07D233/64
CPC分类号： C07D233/64
摘要： This invention is related to novel histidine derivatives of the following general formula (I), wherein X is methylene, oxygen, sulphur or a NR 8 group; R 1 is a straight or branched C 1 -C 8 alkyl or C 3 -C 8 alkenylene or C 3 -C 8 alkynylene chain, optionally substituted with CF 3 , phenyl, phenoxy or naphthyl, the aromatic rings optionally substituted by one or more C 1 -C 4 alkyl, halogens, trifluoromethyl, hydroxy or C 1 -C 4 alkoxy groups; R 2 , R 3 are independently hydrogen, a C 1 -C 3 alkyl chain, halogen, trifluoromethyl, hydroxy or C 1 -C 4 alkoxy groups; R 4 , R 5 , R 6 , R 7 , R 8 are independently hydrogen or C 1 -C 4 alkyl; and the pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, psychiatric, cardiovascular, inflammatory, ophtalmic, urologic, metabolic and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
摘要翻译：本发明涉及以下通式（I）的新型组氨酸衍生物，其中X为亚甲基，氧，硫或NR 8基团; R 1是任选被CF 3，苯基，苯氧基或萘基取代的直链或支链C 1 -C 8烷基或C 3 -C 8亚烯基或C 3 -C 8亚炔基，任选被一个或多个C 1 -C 4烷基取代的芳环，卤素，三氟甲基，羟基或C 1 -C 4烷氧基; R 2，R 3独立地是氢，C 1 -C 3烷基链，卤素，三氟甲基，羟基或C 1 -C 4烷氧基; R 4，R 5，R 6，R 7，R 8独立地是氢或C 1 -C 4烷基; 其作为钠和/或钙通道调节剂具有活性的药学上可接受的盐，因此可用于预防，减轻和治愈广泛范围的病症，包括但不限于神经，精神，心血管，炎症，眼底，泌尿系统，代谢和胃肠道疾病，其中上述机制被描述为发挥病理作用。

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