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公开(公告)号:US20100048665A1
公开(公告)日:2010-02-25
申请号:US12610660
申请日:2009-11-02
申请人: Florian THALER , Cibele Maria Sabido David , Sara Maestroni , Luca Francesco Raveglia , Patricia Salvati
发明人: Florian THALER , Cibele Maria Sabido David , Sara Maestroni , Luca Francesco Raveglia , Patricia Salvati
CPC分类号: C07D207/273 , A61K31/4015 , A61K31/4412 , A61K31/55 , C07D211/76
摘要: 3-aminopyrrolidone compounds and 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.
摘要翻译: 作为钠和/或钙通道调节剂有活性的3-氨基吡咯烷酮化合物及其药学上可接受的盐,因此可用于预防,减轻和治愈广泛范围的病症,包括但不限于心血管,炎症,眼科,泌尿,代谢 和胃肠道疾病。
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公开(公告)号:US07411091B2
公开(公告)日:2008-08-12
申请号:US10580367
申请日:2004-11-12
申请人: Florian Thaler , Cibele Maria Sabido David , Laura Faravelli , Stefania Gagliardi , Elena Colombo , Patricia Salvati
发明人: Florian Thaler , Cibele Maria Sabido David , Laura Faravelli , Stefania Gagliardi , Elena Colombo , Patricia Salvati
IPC分类号: C07C233/05 , C61K31/16 , C07D207/00
CPC分类号: C07D207/27 , C07C233/36
摘要: This invention is related to compounds and use of N-Acyl-N′-benzyl-alkylendiamino derivatives of the following general formula (I), wherein A is a straight or branched C2-C8 alkyl chain; X is a 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 are independently hydrogen or C1-C6 alkyl; R6 is a hydrogen or a straight or branched C1-C8 alkyl or linked to R5 can form a five to seven membered lactam; R7 is hydrogen or C1-C6 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, neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role
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公开(公告)号:US08063039B2
公开(公告)日:2011-11-22
申请号:US12610660
申请日:2009-11-02
申请人: Florian Thaler , Cibele Maria Sabido David , Sara Maestroni , Luca Francesco Raveglia , Patricia Salvati
发明人: Florian Thaler , Cibele Maria Sabido David , Sara Maestroni , Luca Francesco Raveglia , Patricia Salvati
IPC分类号: A61K31/55 , A61K31/4412 , A61K31/4015
CPC分类号: C07D207/273 , A61K31/4015 , A61K31/4412 , A61K31/55 , C07D211/76
摘要: A method for treating pain, migraine, inflammation, gastrointestinal tract disorders, disorders of the genito-urinary tract, ophthalmic diseases or obesity in a subject, the method including administering to the subject an effective amount of a compound of a general formula, specific examples of which include 3-(4-Butyloxy-benzylamino)-pyrrolidin-2-one, 3-[4-(4-trifluorobutyloxy)-benzylamino]-pyrrolidin-2-one, 3-(4-Pentyloxy-benzylamino)-pyrrolidin-2-one, 3-[4-(5-trifluoropentyloxy)-benzylamino]-pyrrolidin-2-one, and 3-(4-Phenylethyl-benzylamino)-pyrrolidin-2-one.
摘要翻译: 一种用于治疗受试者的疼痛,偏头痛,炎症,胃肠道疾病,泌尿系泌尿系疾病,眼科疾病或肥胖的方法,所述方法包括向受试者施用有效量的通式化合物,具体实例 其中包括3-(4-丁氧基 - 苄基氨基) - 吡咯烷-2-酮,3- [4-(4-三氟丁氧基) - 苄基氨基] - 吡咯烷-2-酮,3-(4-戊氧基 - 苄基氨基) - 吡咯烷 -2-酮,3- [4-(5-三氟戊基氧基) - 苄基氨基] - 吡咯烷-2-酮和3-(4-苯乙基 - 苄基氨基) - 吡咯烷-2-酮。
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公开(公告)号:US07968592B2
公开(公告)日:2011-06-28
申请号:US10579675
申请日:2004-11-16
申请人: Florian Thaler , Cibele Maria Sabido David , Sara Maestroni , Luca Francesco Raveglia , Patricia Salvati
发明人: Florian Thaler , Cibele Maria Sabido David , Sara Maestroni , Luca Francesco Raveglia , Patricia Salvati
IPC分类号: A61K31/55 , A61K31/4412 , A61K31/4015 , C07D223/12 , C07D223/10 , C07D211/76 , C07D207/273 , C07D207/26
CPC分类号: C07D207/273 , A61K31/4015 , A61K31/4412 , A61K31/55 , C07D211/76
摘要: 3-aminopyrrolidone compounds and 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.
摘要翻译: 作为钠和/或钙通道调节剂有活性的3-氨基吡咯烷酮化合物及其药学上可接受的盐,因此可用于预防,减轻和治愈广泛范围的病症,包括但不限于心血管,炎症,眼科,泌尿,代谢 和胃肠道疾病。
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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。
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