专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 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.

3. 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。

4. 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。

5. 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。

6. 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。

7. 发明申请

US20110046129A1 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：US20110046129A1
公开(公告)日：2011-02-24
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： A61K31/5377 , C07C237/20 , A61K31/165 , C07D261/08 , A61K31/42 , C07D233/64 , A61K31/4174 , C07D307/16 , A61K31/341 , C07D285/06 , A61K31/433 , C07D231/12 , A61K31/415 , C07D213/64 , A61K31/44 , C07D211/34 , A61K31/445 , C07D295/112 , A61K31/5375 , C07D413/12 , A61P29/00 , A61P25/00 , A61P25/08 , A61P27/02 , A61P9/00
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。

8. 发明申请

US20090005436A1 Substituted Aminoalkyl- and Amidoalkyl-Benzopyran Derivatives 审中-公开
标题翻译：取代的氨基烷基 - 和酰胺基 - 苯并吡喃衍生物
公开(公告)号：US20090005436A1
公开(公告)日：2009-01-01
申请号：US11909095
申请日：2006-02-22
申请人： Angelo Carotti , Piero Melloni , Florian Thaler , Carla Caccia , Sara Maestroni , Patricia Salvati
发明人： Angelo Carotti , Piero Melloni , Florian Thaler , Carla Caccia , Sara Maestroni , Patricia Salvati
IPC分类号： A61K31/353 , C07D311/04 , A61P25/28
CPC分类号： C07D311/16 , C07D311/58
摘要： This invention is related to novel aminoalkyl- and amidoalkyl-benzopyran derivatives of the following general formula (I) wherein: the group is a substituent in position 6 or 7 wherein: R is an aromatic mono- or bi-cyclic carbocyclic ring or a mono- or bi-cyclic heterocyclic ring radical, said rings being optionally substituted by one or two substituents selected from (C1-C5) straight or branched alkyl, (C1-C5) straight or branched alkoxy, hydroxy, halogen and trifluoromethyl; m is zero or an integer from 1 to 3; n, p, R1 and R2 are as herein indicated and R3 and R4 are both hydrogen or taken together represent an oxygen atom, and the pharmaceutically acceptable salts thereof. The compounds that are active as selective and reversible MAO-B inhibitors in vitro and in vivo, are useful as medicaments for the prevention and the treatment of CNS degenerative disorders.
摘要翻译：本发明涉及以下通式（I）的新型氨基烷基 - 和酰氨基烷基 - 苯并吡喃衍生物，其中：该基团是6或7位的取代基，其中：R是芳族单环或双环碳环或单所述环任选被一个或两个选自（C1-C5）直链或支链烷基，（C1-C5）直链或支链烷氧基，羟基，卤素和三氟甲基的取代基取代; m为0或1〜3的整数; n，p，R1和R2如本文所示，R 3和R 4均为氢或一起代表氧原子，及其药学上可接受的盐。在体外和体内作为选择性和可逆MAO-B抑制剂活性的化合物可用作预防和治疗CNS退行性疾病的药物。

9. 发明申请

US20110184068A1 USE OF (HALOBENZYLOXY) BENZYLAMINO-PROPANAMIDES FOR THE MANUFACTURE OF MEDICAMENTS ACTIVE AS SODIUM AND/OR CALCIUM CHANNEL SELECTIVE MODULATORS 审中-公开
标题翻译：（HALOBENZYLOXY）苯甲酰胺丙酰胺用于制备作为钠和/或钙通道选择性调节剂活性的药物的用途
公开(公告)号：US20110184068A1
公开(公告)日：2011-07-28
申请号：US12939726
申请日：2010-11-04
申请人： Elena Barbanti , Florian Thaler , Carla Caccia , Ruggero Fariello , Patricia Salvati
发明人： Elena Barbanti , Florian Thaler , Carla Caccia , Ruggero Fariello , Patricia Salvati
IPC分类号： A61K31/167 , A61P25/04
CPC分类号： C07C237/06 , A61K31/00 , A61K31/165 , A61K45/06 , A61K2300/00
摘要： The invention relates to the use of selected (R)-2-[(halobenzyloxy)benzylamino]-propanamides and the pharmaceutically acceptable salts thereof for the manufacture of medicament, that are selectively active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, pain, migraine, periferal diseases, cardiovascular diseases, inflammatory processes affecting all body systems, disorders affecting skin and related tissues, disorders of the respiratory system, disorders of the immune and endocrinological systems, gastrointestinal, urogenital, metabolic and seizure disorders, where the above mechanisms have been described as playing a pathological role.
摘要翻译：本发明涉及选择的（R）-2 - [（卤代苄氧基）苄基氨基] - 丙酰胺及其药学上可接受的盐在制备药物中的用途，其作为钠和/或钙通道调节剂选择性活性，预防，缓解和治愈各种病症，包括疼痛，偏头痛，周围疾病，心血管疾病，影响所有身体系统的炎症过程，影响皮肤和相关组织的疾病，呼吸系统疾病，免疫和内分泌系统疾病，胃肠道，泌尿生殖，代谢和发作障碍，其中上述机制被描述为发挥病理作用。

10. 发明授权

US5637596A Azabicycloalkyl derivatives of imidazo[1,5-a]indol-3-one and process for their preparation 失效
标题翻译：咪唑并[1,5-a]吲哚-3-酮的氮杂双环烷基衍生物及其制备方法
公开(公告)号：US5637596A
公开(公告)日：1997-06-10
申请号：US578548
申请日：1996-01-24
申请人： Mario Varasi , Franco Heidempergher , Carla Caccia , Patricia Salvati
发明人： Mario Varasi , Franco Heidempergher , Carla Caccia , Patricia Salvati
IPC分类号： A61K31/41 , A61K31/435 , A61K31/439 , A61K31/46 , A61P1/00 , A61P1/08 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/36 , A61P43/00 , C07D451/04 , C07D451/14 , C07D453/02 , C07D519/00
CPC分类号： C07D453/02 , C07D451/04 , C07D451/14
摘要： Novel 5-HT.sub.3 receptor antagonist compounds having the general formula (I) ##STR1## wherein each of R, R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxy-carbonyl, nitro, --N(R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 alkanoyl; or a (R.sub.6 R.sub.7)N--SO.sub.2 group, in which each of R.sub.6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl; ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof, are provided.
摘要翻译： PCT No.PCT / EP95 / 01652 Sec。 371日期：1996年1月24日 102（e）日期1996年1月24日PCT 1995年5月2日PCT PCT。公开号WO95 / 32209 日期1995年11月30日具有通式（I）的图像的新型5-HT 3受体拮抗剂化合物（I）其中R，R 1和R 2可以相同或不同，为氢，卤素，羟基，氰基，C 1 -C 6烷基，CF 3，C 1 -C 6烷氧基，C 1 -C 6烷硫基，甲酰基，C 2 -C 6烷酰基，羧基，C 1 -C 6烷氧羰基，硝基，-N（R 4 R 5）是氢，C 1 -C 6烷基，甲酰基或C 2 -C 6烷酰基; 或（R6R7）N-SO2基团，其中R6和R7各自独立地为氢或C1-C6烷基; R3是a，a）或b）其中n是1或2的整数，R8是氢，未被取代或被苯基取代的C1-C6烷基，C2-C4烯基，C2-C4炔基，或C 2 -C 6烷酰基; 及其药学上可接受的盐。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式