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    Substituted benzylaminoalkylene heterocycles
    9.
    发明授权
    Substituted benzylaminoalkylene heterocycles 有权
    取代的苄基氨基亚烷基杂环

    公开(公告)号：US07649005B2

    公开(公告)日：2010-01-19

    申请号：US10575627

    申请日：2004-10-05

    申请人： Patricia Salvati ,  Carla Caccia ,  Piero Melloni ,  Alessandra Restivo ,  Cibele Sabido David ,  Stefania Vallese

    发明人： Patricia Salvati ,  Carla Caccia ,  Piero Melloni ,  Alessandra Restivo ,  Cibele Sabido David ,  Stefania Vallese

    IPC分类号： A61K31/44 ,  C07D213/02

    CPC分类号： C07D261/02 ,  A61K31/341 ,  A61K31/422 ,  A61K31/426 ,  C07D213/38 ,  C07D233/64 ,  C07D235/14 ,  C07D249/08 ,  C07D261/08 ,  C07D263/32 ,  C07D277/28 ,  C07D307/14 ,  C07D307/38 ,  C07D307/52 ,  C07D307/81 ,  C07D309/04 ,  C07D319/12 ,  C07D333/20

    摘要： This invention is related to compounds of general formula (I) wherein X is oxygen or sulphur or a NR7 group; R1 is C3-C8 alkyl, or C1-C8 alkyl substituted by phenoxy or phenyl, both phenoxy or phenyl being optionally substituted by one or more fluoro, chloro, trifluoromethyl, C1-C6 alkyl, hydroxyl, C1-C6 alkoxy; R2, R3 are independently hydrogen, C1-C6 alkyl, halogen, trifluoromethyl, hydroxy or C1-C6 alkoxy; R4 is hydrogen, C1-C8 alkyl; R5, R6 are independently hydrogen, C1-C3 alkyl, optionally substituted by hydroxy or phenyl; R7 is hydrogen or straight or branched C1-C3 alkyl; Het is a five to seven membered, saturated or unsaturated heteromonocyclic or an eight to ten membered, saturated or unsaturated heterobicyclic group, containing one or more heteroatoms chosen independently from nitrogen, oxygen and sulphur, said mono- or bicyclic groups being optionally substituted by C1-C6alkyl, halogen, hydroxyl or C1-C6 alkoxy; and the pharmaceutically acceptable salts or prodrug thereof, that are active as sodium and/or calcium channel modulators and/or as selective MAO-B inhibitors and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.

    摘要翻译： 本发明涉及通式（I）的化合物，其中X是氧或硫或NR 7基团; R 1是C 3 -C 8烷基或被苯氧基或苯基取代的C 1 -C 8烷基，苯氧基或苯基任选被一个或多个氟，氯，三氟甲基，C 1 -C 6烷基，羟基，C 1 -C 6烷氧基取代; R2，R3独立地是氢，C1-C6烷基，卤素，三氟甲基，羟基或C1-C6烷氧基; R4是氢，C1-C8烷基; R5，R6独立地为氢，任选被羟基或苯基取代的C 1 -C 3烷基; R 7是氢或直链或支链C 1 -C 3烷基; Het是五至七元饱和或不饱和杂单环或八至十元饱和或不饱和杂双环基团，其含有一个或多个独立地选自氮，氧和硫的杂原子，所述单 - 或双环基团任选被C 1 -C 1-6烷基，卤素，羟基或C 1 -C 6烷氧基; 其作为钠和/或钙通道调节剂和/或作为选择性MAO-B抑制剂是有活性的，因此可用于预防，缓解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，眼科，泌尿，代谢和胃肠疾病，其中上述机制已被描述为发挥病理作用。