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    • 1. 发明申请
    • 3-AMINOPYRROLIDONE DERIVATIVES
    • 3-氨基吡咯烷酮衍生物
    • WO2005054190A1
    • 2005-06-16
    • PCT/EP2004/012957
    • 2004-11-16
    • NEWRON PHARMACEUTICALS S.p.A.THALER, FlorianSABIDO DAVID, Cibele, MariaMAESTRONI, SaraRAVEGLIA, Luca, FrancescoSALVATI, Patricia
    • THALER, FlorianSABIDO DAVID, Cibele, MariaMAESTRONI, SaraRAVEGLIA, Luca, FrancescoSALVATI, Patricia
    • C07D207/273
    • C07D207/273A61K31/4015A61K31/4412A61K31/55C07D211/76
    • This invention is related to compounds and use of 3-aminopyrrolidone derivatives and analogues of the following general formula (I), wherein m is an integer from 1 to 3; X is methylene, oxygen, sulphur or a NR 6 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, or phenyl 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 are independently hydrogen or C 1 -C 6 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 cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
    • 本发明涉及以下通式(I)的3-氨基吡咯烷酮衍生物和类似物的化合物和用途,其中m为1至3的整数; X是亚甲基,氧,硫或NR 6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亚炔基链,或苯基,任选被一个或多个C 1 -C 4 烷基,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独立地是氢或C 1 -C 6烷基; 和其药学上可接受的盐,其作为钠和/或钙通道调节剂是有活性的,因此可用于预防,缓解和治愈广泛范围的病理学,包括但不限于心血管,炎症,眼科,泌尿,代谢和胃肠道疾病 其中上述机制被描述为发挥病理作用。