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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

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。

4. 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。

5. 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。

6. 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。

7. 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。

8. 发明申请

US20100267835A1 Methods of treating disorders of trigeminalvascular activation 审中-公开
标题翻译：治疗三叉神经血管活化障碍的方法
公开(公告)号：US20100267835A1
公开(公告)日：2010-10-21
申请号：US12688192
申请日：2010-01-15
申请人： Patricia Salvati , Marcello Calabresi , Luciano Dho , Orietta Veneroni , Piero Melloni
发明人： Patricia Salvati , Marcello Calabresi , Luciano Dho , Orietta Veneroni , Piero Melloni
IPC分类号： A61K31/165 , A61P29/00
CPC分类号： A61K31/165
摘要： Alpha-aminoamide derivatives useful in the treatment of disorders of trigeminalvascular activation are disclosed.
摘要翻译：公开了可用于治疗三叉神经血管活化障碍的α-氨基酰胺衍生物。

9. 发明申请

US20060079570A1 Alpha-aminoamide derivatives useful as antimigraine agents 有权
标题翻译：可用作抗偏头痛药物的α-氨基酰胺衍生物
公开(公告)号：US20060079570A1
公开(公告)日：2006-04-13
申请号：US10541195
申请日：2003-11-18
申请人： Patricia Salvati , Marcello Calabresi , Luciano Dho , Orietta Veneroni , Piero Melloni
发明人： Patricia Salvati , Marcello Calabresi , Luciano Dho , Orietta Veneroni , Piero Melloni
IPC分类号： A61K31/381 , A61K31/165
CPC分类号： A61K31/165
摘要： α-Aminoamide derivatives useful as antimigraine agents, particularly for the treatment of head pain conditions such as migraine, cluster headache or other severe headache, are disclosed. The antimigraine agents of the invention are able to reduce or even stop the pain deriving from such conditions without, virtually, any side effects.
摘要翻译：公开了用作抗偏头痛药物的α-氨基酰胺衍生物，特别是用于治疗头痛症状如偏头痛，丛集性头痛或其他严重头痛。本发明的抗偏头痛药物能够减少甚至阻止从这些病症产生的疼痛，而实际上没有任何副作用。

10. 发明授权

US07709523B2 Alpha-aminoamide derivatives useful as antimigraine agents 有权
标题翻译：可用作抗偏头痛药物的α-氨基酰胺衍生物
公开(公告)号：US07709523B2
公开(公告)日：2010-05-04
申请号：US10541195
申请日：2003-11-18
申请人： Patricia Salvati , Marcello Calabresi , Luciano Dho , Orietta Veneroni , Piero Melloni
发明人： Patricia Salvati , Marcello Calabresi , Luciano Dho , Orietta Veneroni , Piero Melloni
IPC分类号： A61K31/381 , A61K31/165 , A61P25/06
CPC分类号： A61K31/165
摘要： α-Aminoamide derivatives useful as antimigraine agents, particularly for the treatment of head pain conditions such as migraine, cluster headache or other severe headache, are disclosed. The antimigraine agents of the invention are able to reduce or even stop the pain deriving from such conditions without, virtually, any side effects.
摘要翻译：公开了用作抗偏头痛药物的α-氨基酰胺衍生物，特别是用于治疗头痛症状如偏头痛，丛集性头痛或其他严重头痛。本发明的抗偏头痛药物能够减少甚至阻止从这些病症产生的疼痛，而实际上没有任何副作用。

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