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    • 3. 发明申请
    • SUBSTITUTED BENZYLAMINOALKYLENE HETEROCYCLES
    • 取代的苯甲酰氨基烯烃杂环化合物
    • WO2005040138A1
    • 2005-05-06
    • PCT/EP2004/011104
    • 2004-10-05
    • NEWRON PHARMACEUTICALS S.P.A.SALVATI, PatriciaCACCIA, CarlaMELLONI, PieroRESTIVO, AlessandraSABIDO DAVID, CibeleVALLESE, Stefania
    • SALVATI, PatriciaCACCIA, CarlaMELLONI, PieroRESTIVO, AlessandraSABIDO DAVID, CibeleVALLESE, Stefania
    • C07D261/02
    • C07D261/02A61K31/341A61K31/422A61K31/426C07D213/38C07D233/64C07D235/14C07D249/08C07D261/08C07D263/32C07D277/28C07D307/14C07D307/38C07D307/52C07D307/81C07D309/04C07D319/12C07D333/20
    • This invention is related to compounds of general formula (I) wherein X is oxygen or sulphur or a NR 7 group; R 1 is C 3 -C 8 alkyl, or C 1 -C 8 alkyl substituted by phenoxy or phenyl, both phenoxy or phenyl being optionally substituted by one or more fluoro, chloro, trifluoromethyl, C 1 -C 6 alkyl, hydroxyl, C 1 -C 6 alkoxy; R 2 , R 3 are independently hydrogen, C 1 -C 6 alkyl, halogen, trifluoromethyl, hydroxy or C 1 -C 6 alkoxy; R 4 is hydrogen, C 1 -C 8 alkyl; R 5 , R 6 are independently hydrogen, C 1 -C 3 alkyl, optionally substituted by hydroxy or phenyl; R 7 is hydrogen or straight or branched C 1 -C 3 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 C 1 -C 6 alkyl, halogen, hydroxyl or C 1 -C 6 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.
    • 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; R 2,R 3独立地是氢,C 1 -C 6烷基,卤素,三氟甲基,羟基或C 1 -C 6烷氧基; R 4是氢,C 1 -C 8烷基; R 5,R 6独立地是氢,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抑制剂具有活性,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。
    • 10. 发明申请
    • PROLINAMIDE DERIVATIVES AS SODIUM AND/OR CALCIUM CHANNEL BLOCKERS OR SELECTIVE MAO-B INHIBITORS
    • 丙氨酰胺衍生物作为钠和/或钙通道阻断剂或选择性MAO-B抑制剂
    • WO2005040108A1
    • 2005-05-06
    • PCT/EP2004/011105
    • 2004-10-05
    • NEWRON PHARMACEUTICALS S.P.A.CACCIA, CarlaLA PORTA, ElenaMAESTRONI, SaraMELLONI, PieroSABIDO DAVID, CibeleSALVATI, Patricia
    • CACCIA, CarlaLA PORTA, ElenaMAESTRONI, SaraMELLONI, PieroSABIDO DAVID, CibeleSALVATI, Patricia
    • C07D207/16
    • C07D401/12C07D207/16C07D211/60C07D223/06
    • This invention is related to novel prolinamide derivatives and analogues of general formula (I) wherein Q is C 3 -C 8 alkyl, or C 1 -C 8 alkyl substituted by phenoxy or saturated or unsaturated 5 to 7 membered ring optionally containing one or more heteroatoms chosen independently from nitrogen, oxygen or sulphur, the rings being optionally substituted by one or more halogen atoms, trifluoromethyl, C 1 -C 6 alkyl, hydroxyl, C 1 -C 6 alkoxy; X is an oxygen, sulphur or a NR 5 group; R, R 1 are independently hydrogen, C 1 -C 6 alkyl, halogen, trifluoromethyl, hydroxy or C 1 -C 6 alkoxy; R 2 is hydrogen or hydroxyl; R 3 R 4 R 5 are independently hydrogen or straight or branched C 1 -C 3 alkyl; n is an integer from 1 to 3 and a pharmaceutically acceptable salt or prodrug thereof, that areactive as sodium and/or calcium channel modulators and/or as selective MAOB 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.
    • 本发明涉及新的脯氨酰胺衍生物和通式(I)的类似物,其中Q为C 3 -C 8烷基或被苯氧基或饱和或不饱和5至7元环任选地含有一个或多个独立地选自以下的杂原子取代的C 1 -C 8烷基: 氮,氧或硫,所述环任选被一个或多个卤素原子,三氟甲基,C 1 -C 6烷基,羟基,C 1 -C 6烷氧基取代; X是氧,硫或NR 5基团; R 1,R 2独立地是氢,C 1 -C 6烷基,卤素,三氟甲基,羟基或C 1 -C 6烷氧基; R 2是氢或羟基; R 3 R 4独立地是氢或直链或支链C 1 -C 3烷基; n是1至3的整数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MAOB抑制剂起作用,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,眼科,泌尿系,代谢和胃肠道疾病,其中上述机制已被描述为发挥病理作用。