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    CYCLOPENTYL DERIVATES
    8.
    发明公开
    CYCLOPENTYL DERIVATES 有权
    CYCLOPENTYLDERIVATE

    公开(公告)号：EP1687259A1

    公开(公告)日：2006-08-09

    申请号：EP04819587.9

    申请日：2004-11-12

    申请人： Newron Pharmaceuticals S.p.A.

    发明人： MELLONI, Piero ,  SABIDO DAVID, Cibele Maria ,  RESTIVO, Alessandra ,  FORLANI, Roberto c/o Nikem Research S.r.I. ,  SALVATI, Patricia

    IPC分类号： C07C237/24 ,  A61K31/16 ,  A61P25/00 ,  A61P29/00 ,  A61P13/00

    CPC分类号： C07C237/24 ,  C07C2601/08

    摘要： This invention is related to novel cyclopentyl derivatives of the following general Formula (I), wherein X is methylene, oxygen, sulphur or a NR7 group; R1 is a straight or branched C1-C8 alkyl or C3-C8 alkenylene or C3-C8 alkynylene chain, optionally substituted with CF3, phenyl, phenoxy or naphthyl, the aromatic rings optionally substituted by one or more C1-C4 alkyl, halogens, trifluoromethyl, hydroxy or C1-C4 alkoxy groups; R2, R3 are independently hydrogen, a C1-C3 alkyl chain, halogen, trifluoromethyl, hydroxy or C1-C4 alkoxy groups; R4, R5, R6, R7 are independently hydrogen or C1-C6 alkyl; and the pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators and therefor 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： 本发明涉及以下通式（I）的新环戊基衍生物：其中X为亚甲基，氧，硫或NR 7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独立地是氢或C 1 -C 6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理学，包括但不限于神经性，精神病学，心血管，炎症，眼科，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。

    SUBSTITUTED BENZYLAMINOALKYLENE HETEROCYCLES
    9.
    发明公开
    SUBSTITUTED BENZYLAMINOALKYLENE HETEROCYCLES 有权
    取代的苯基氨基亚烷基杂环化合物

    公开(公告)号：EP1673356A1

    公开(公告)日：2006-06-28

    申请号：EP04790126.9

    申请日：2004-10-05

    申请人： Newron Pharmaceuticals S.p.A.

    发明人： SALVATI, Patricia ,  CACCIA, Carla ,  MELLONI, Piero ,  RESTIVO, Alessandra ,  SABIDO DAVID, Cibele ,  VALLESE, Stefania, Nikem

    IPC分类号： C07D261/02 ,  C07D307/14 ,  C07D307/38 ,  C07D319/12 ,  C07D213/38 ,  C07D233/54 ,  C07D249/02 ,  C07D277/10 ,  C07D327/04 ,  C07D333/20 ,  C07D307/81 ,  C07D235/14 ,  A61K31/341 ,  A61K31/422 ,  A61K31/426

    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NR7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独立地为氢，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C1-C3烷基; R7是氢或直链或支链C1-C3烷基; Het是含有一个或多个独立地选自氮，氧和硫的杂原子的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二环基团，所述单环或双环基团任选被C1 -C6烷基，卤素，羟基或C1-C6烷氧基; 及其药学上可接受的盐或前药，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，缓解和治疗多种病症，包括但不限于 ，神经系统疾病，精神疾病，心血管疾病，炎症，眼科，泌尿系统疾病，代谢疾病和胃肠疾病，其中上述机制被描述为起病理作用。