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1. 发明申请

US20070066688A1 Cyclopentyl derivatives 有权
标题翻译：环戊基衍生物
公开(公告)号：US20070066688A1
公开(公告)日：2007-03-22
申请号：US10580366
申请日：2004-11-12
申请人： Piero Melloni , Cibele Sabido David , Alessandra Restivo , Roberto Forlani , Patricia Salvati
发明人： Piero Melloni , Cibele Sabido David , Alessandra Restivo , Roberto Forlani , Patricia Salvati
IPC分类号： A61K31/165 , C07C237/20
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是亚甲基，氧，硫或NR 7基团; R 1是直链或支链C 1 -C 8烷基或C 3 -C 8烷基亚烷基或C 3 -C 8亚炔基链，任选被CF 3，苯基，苯氧基或萘基取代，芳环任选地被一个或多个C 1 -C 4烷基，卤素，三氟甲基，羟基或C 1 -C 4亚烷基取代 >烷氧基; R 2，R 3，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 7独立地是氢或C 1〜 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，并且可用于预防，减轻和治愈广泛范围的病症，包括但不限于神经性，精神病学，心血管疾病，炎症性，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。

2. 发明授权

US07649005B2 Substituted benzylaminoalkylene heterocycles 有权
标题翻译：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。

3. 发明申请

US20070135496A1 Substituted benzylaminoalkylene heterocycles 有权
公开(公告)号：US20070135496A1
公开(公告)日：2007-06-14
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 , A61K31/421 , A61K31/42 , A61K31/4172 , A61K31/381 , A61K31/35 , A61K31/343 , A61K31/34
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.

4. 发明授权

US07265244B2 Cyclopentyl derivatives 有权
标题翻译：环戊基衍生物
公开(公告)号：US07265244B2
公开(公告)日：2007-09-04
申请号：US10580366
申请日：2004-11-12
申请人： Piero Melloni , Cibele Maria Sabido David , Alessandra Restivo , Roberto Forlani , Patricia Salvati
发明人： Piero Melloni , Cibele Maria Sabido David , Alessandra Restivo , Roberto Forlani , Patricia Salvati
IPC分类号： C07C233/58 , C07C237/20
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-C6alkyl; 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是亚甲基，氧，硫或NR 7基团; R 1是直链或支链C 1 -C 8烷基或C 3 -C 8烷基亚烷基或C 3 -C 8亚炔基链，任选被CF 3，苯基，苯氧基或萘基取代，芳环任选地被一个或多个C 1 -C 4烷基，卤素，三氟甲基，羟基或C 1 -C 4烷基取代，烷氧基; R 2，R 3，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 7独立地是氢或C 1〜 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，并且可用于预防，减轻和治愈广泛范围的病症，包括但不限于神经性，精神病学，心血管疾病，炎症性，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。

5. 发明申请

US20100210631A1 SUBSTITUTED 2-[2-(PHENYL) ETHYLAMINO] ALKANEAMIDE DERIVATIVES AND THEIR USE AS SODIUM AND/OR CALCIUM CHANNEL MODULATORS 有权
标题翻译：取代的2- [2-（苯基）乙酰胺]烷基胺衍生物及其作为钠和/或钙通道调节剂的用途
公开(公告)号：US20100210631A1
公开(公告)日：2010-08-19
申请号：US12663926
申请日：2008-05-14
申请人： Piero Melloni , Alessandra Restivo , Emanuela Izzo , Simona Francisconi , Elena Colombo , Cibele Sabido-David
发明人： Piero Melloni , Alessandra Restivo , Emanuela Izzo , Simona Francisconi , Elena Colombo , Cibele Sabido-David
IPC分类号： A61K31/551 , C07C237/20 , A61K31/165 , C07C321/26 , A61P25/00 , A61P25/28 , A61P25/16 , A61P9/10 , A61P25/18 , A61P25/22 , A61P25/30 , A61P25/24 , A61K31/445 , A61K31/519 , A61P29/00
CPC分类号： A61K31/381 , A61K31/137 , A61K31/165 , A61K31/40 , A61K31/4515 , A61K31/519 , A61K31/5513 , C07C237/06 , C07C237/08 , C07C237/20 , C07C317/28 , C07C321/26 , C07C323/25 , C07C327/42 , C07C327/44 , C07D207/16 , C07D295/182 , C07D333/20
摘要： Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them are useful as sodium and/or calcium channel modulators for preventing, alleviating and curing pathologies wherein the above mechanisms play a pathological role. The compounds may be particularly used for the prevention, alleviation, and curing of, for example, neurological, cognitive, psychiatric, inflammatory, urogenital, and gastrointestinal diseases.
摘要翻译：取代的2- [2-（苯基）乙基氨基]烷酰胺衍生物，其药学上可接受的盐和含有它们的药物组合物可用作用于预防，减轻和治愈其中上述机制发挥病理作用的病症的钠和/或钙通道调节剂。这些化合物可以特别用于预防，缓解和治愈例如神经，认知，精神，炎症，泌尿生殖和胃肠道疾病。

6. 发明授权

US08519000B2 Substituted 2-[2-(phenyl) ethylamino] alkaneamide derivatives and their use as sodium and/or calcium channel modulators 有权
标题翻译：取代的2- [2-（苯基）乙基氨基]烷酰胺衍生物及其作为钠和/或钙通道调节剂的用途
公开(公告)号：US08519000B2
公开(公告)日：2013-08-27
申请号：US12663926
申请日：2008-05-14
申请人： Piero Melloni , Alessandra Restivo , Emanuela Izzo , Simona Francisconi , Elena Colombo , Cibele Sabido-David
发明人： Piero Melloni , Alessandra Restivo , Emanuela Izzo , Simona Francisconi , Elena Colombo , Cibele Sabido-David
IPC分类号： A61K31/165 , C07C237/08 , C07C233/05 , C07C233/65
CPC分类号： A61K31/381 , A61K31/137 , A61K31/165 , A61K31/40 , A61K31/4515 , A61K31/519 , A61K31/5513 , C07C237/06 , C07C237/08 , C07C237/20 , C07C317/28 , C07C321/26 , C07C323/25 , C07C327/42 , C07C327/44 , C07D207/16 , C07D295/182 , C07D333/20
摘要： Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them are useful as sodium and/or calcium channel modulators for preventing, alleviating and curing pathologies wherein the above mechanisms play a pathological role. The compounds may be particularly used for the prevention, alleviation, and curing of, for example, neurological, cognitive, psychiatric, inflammatory, urogenital, and gastrointestinal diseases.
摘要翻译：取代的2- [2-（苯基）乙基氨基]烷酰胺衍生物，其药学上可接受的盐和含有它们的药物组合物可用作用于预防，减轻和治愈其中上述机制发挥病理作用的病症的钠和/或钙通道调节剂。这些化合物可以特别用于预防，缓解和治愈例如神经，认知，精神，炎症，泌尿生殖和胃肠道疾病。

7. 发明申请

US20080319057A1 2-Phenylethylamino Derivatives as Calcium and/or Sodium Channel Modulators 有权
标题翻译： 2-苯基乙基氨基衍生物作为钙和/或钠通道调节剂
公开(公告)号：US20080319057A1
公开(公告)日：2008-12-25
申请号：US12158491
申请日：2006-11-29
申请人： Florian Thaler , Mauro Napoletano , Cibele Sabido-David , Ermanno Moriggi , Carla Caccia , Laura Faravelli , Alessandra Restivo , Patricia Salvati
发明人： Florian Thaler , Mauro Napoletano , Cibele Sabido-David , Ermanno Moriggi , Carla Caccia , Laura Faravelli , Alessandra Restivo , Patricia Salvati
IPC分类号： A61K31/341 , C07C237/20 , A61K31/165 , C07D307/54
CPC分类号： C07D285/06 , C07C237/06 , C07C237/20 , C07C2601/02 , C07D211/58 , C07D213/30 , C07D213/38 , C07D213/64 , C07D231/12 , C07D233/64 , C07D261/12 , C07D295/185 , C07D307/14 , C07D307/52 , C07D333/20 , C07D405/12 , C07D409/12 , C07D413/12
摘要： 2-Phenylethylamino substituted carboxamide derivatives of formula (I); wherein J, W, R0, R1, R2, R3, and R4 have the meanings as defined in the specification and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and their use as sodium and/or calcium channel modulators useful in preventing alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urology, and gastrointestinal diseases where the above mechanisms have been described as playing a pathological role, are described.
摘要翻译：式（I）的2-苯基乙基氨基取代的甲酰胺衍生物; 其中J，W，R 0，R 1，R 2，R 3和R 4具有如本说明书中所定义的含义及其药学上可接受的盐，含有它们作为活性成分的药物组合物及其作为钠和/或钙通道调节剂用于预防描述了将上述机制描述为发挥病理作用的各种病症，包括神经，精神，心血管，炎症，眼科，泌尿科和胃肠疾病。

8. 发明授权

US08470877B2 2-phenylethylamino derivatives as calcium and/or sodium channel modulators 有权
标题翻译： 2-苯基乙基氨基衍生物作为钙和/或钠通道调节剂
公开(公告)号：US08470877B2
公开(公告)日：2013-06-25
申请号：US13359285
申请日：2012-01-26
申请人： Florian Thaler , Mauro Napoletano , Cibele Sabido-David , Ermanno Moriggi , Carla Caccia , Laura Faravelli , Alessandra Restivo , Patricia Salvati
发明人： Florian Thaler , Mauro Napoletano , Cibele Sabido-David , Ermanno Moriggi , Carla Caccia , Laura Faravelli , Alessandra Restivo , Patricia Salvati
IPC分类号： C07D209/14
CPC分类号： C07D285/06 , C07C237/06 , C07C237/20 , C07C2601/02 , C07D211/58 , C07D213/30 , C07D213/38 , C07D213/64 , C07D231/12 , C07D233/64 , C07D261/12 , C07D295/185 , C07D307/14 , C07D307/52 , C07D333/20 , C07D405/12 , C07D409/12 , C07D413/12
摘要： 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.
摘要翻译：提出了2-苯基乙基氨基取代的甲酰胺衍生物及其作为钠和/或钙通道调节剂用于预防，减轻和治愈广泛范围病理学的用途。

9. 发明授权

US07855227B2 2-phenylethylamino derivatives as calcium and/or sodium channel modulators 有权
标题翻译： 2-苯基乙基氨基衍生物作为钙和/或钠通道调节剂
公开(公告)号：US07855227B2
公开(公告)日：2010-12-21
申请号：US12158491
申请日：2006-11-29
申请人： Florian Thaler , Mauro Napoletano , Cibele Sabido-David , Ermanno Moriggi , Carla Caccia , Laura Faravelli , Alessandra Restivo , Patricia Salvati
发明人： Florian Thaler , Mauro Napoletano , Cibele Sabido-David , Ermanno Moriggi , Carla Caccia , Laura Faravelli , Alessandra Restivo , Patricia Salvati
IPC分类号： A61K31/34 , C07D209/14
CPC分类号： C07D285/06 , C07C237/06 , C07C237/20 , C07C2601/02 , C07D211/58 , C07D213/30 , C07D213/38 , C07D213/64 , C07D231/12 , C07D233/64 , C07D261/12 , C07D295/185 , C07D307/14 , C07D307/52 , C07D333/20 , C07D405/12 , C07D409/12 , C07D413/12
摘要： 2-Phenylethylamino substituted carboxamide derivatives of formula (I); wherein J, W, R0, R1, R2, R3, and R4 have the meanings as defined in the specification and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and their use as sodium and/or calcium channel modulators useful in preventing alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urology, and gastrointestinal diseases where the above mechanisms have been described as playing a pathological role, are described.
摘要翻译：式（I）的2-苯基乙基氨基取代的甲酰胺衍生物; 其中J，W，R 0，R 1，R 2，R 3和R 4具有如本说明书中所定义的含义及其药学上可接受的盐，含有它们作为活性成分的药物组合物及其作为钠和/或钙通道调节剂用于预防描述了将上述机制描述为发挥病理作用的各种病症，包括神经，精神，心血管，炎症，眼科，泌尿科和胃肠疾病。

10. 发明授权

US08129427B2 2-phenylethylamino derivatives as calcium and/or sodium channel modulators 有权
标题翻译： 2-苯基乙基氨基衍生物作为钙和/或钠通道调节剂
公开(公告)号：US08129427B2
公开(公告)日：2012-03-06
申请号：US12878831
申请日：2010-09-09
申请人： Florian Thaler , Mauro Napoletano , Cibele Sabido-David , Ermanno Moriggi , Carla Caccia , Laura Faravelli , Alessandra Restivo , Patricia Salvati
发明人： Florian Thaler , Mauro Napoletano , Cibele Sabido-David , Ermanno Moriggi , Carla Caccia , Laura Faravelli , Alessandra Restivo , Patricia Salvati
IPC分类号： A61K31/34 , C07D209/14
CPC分类号： C07D285/06 , C07C237/06 , C07C237/20 , C07C2601/02 , C07D211/58 , C07D213/30 , C07D213/38 , C07D213/64 , C07D231/12 , C07D233/64 , C07D261/12 , C07D295/185 , C07D307/14 , C07D307/52 , C07D333/20 , C07D405/12 , C07D409/12 , C07D413/12
摘要： 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.
摘要翻译：提出了2-苯基乙基氨基取代的甲酰胺衍生物及其作为钠和/或钙通道调节剂用于预防，减轻和治愈广泛范围病理学的用途。

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