专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

11. 发明申请

US20070049643A1 Hydroxylamine derivatives 有权
标题翻译：羟胺衍生物
公开(公告)号：US20070049643A1
公开(公告)日：2007-03-01
申请号：US10582141
申请日：2004-12-10
申请人： Carla Caccia , Laura Girola , Petra Kaltofen , Daniele Losi , Patricia Salvati , Enrico Selva , Florian Thaler
发明人： Carla Caccia , Laura Girola , Petra Kaltofen , Daniele Losi , Patricia Salvati , Enrico Selva , Florian Thaler
IPC分类号： A61K31/13
CPC分类号： C07C239/20 , A61K31/13 , C07C239/12 , C07C2602/10
摘要： This invention is related to hydroxylamino derivatives of the general formula (I) wherein n is 0, 1 or 2; R1 and R2, independently of each other, are H, OH or OCH3; R3 is H or CH3; R4 is H, C1-C3 straight or branched alkyl or, together with R3, forms a five to seven-membered carbocyclic ring; and R5 and R6, independently of each other, are H or C1-C5 straight or branched alkyl and the pharmaceutically acceptable salts or prodrug thereof, for the preparation of medicaments useful for the prevention, treatment and diagnosis of CNS degenerative disorders related to protein misfolding and/or misaggregation. The invention also relates to novel compounds included in formula (I), to a method for preparing said compounds and to pharmaceutical compositions containing them.
摘要翻译：本发明涉及通式（I）的羟基氨基衍生物，其中n为0,1或2; R 1和R 2彼此独立地是H，OH或OCH 3; R 3是H或CH 3 N; R 4是H，C 1 -C 3直链或支链烷基，或与R 3'一起形成五至七元碳环; 和R 5和R 6彼此独立地是H或C 1 -C 5直链或支链烷基及其药学上可接受的盐或前药，用于制备可用于预防，治疗和诊断与蛋白质错折叠和/或解聚相关的CNS退行性疾病的药物。本发明还涉及式（I）中包括的新化合物，涉及制备所述化合物的方法和含有它们的药物组合物。

12. 发明授权

US5424328A Phenyl-imidazolidinone derivatives 失效
标题翻译：苯基咪唑啉酮衍生物
公开(公告)号：US5424328A
公开(公告)日：1995-06-13
申请号：US144514
申请日：1993-11-02
申请人： Mario Varasi , Franco Heidempergher , Carla Caccia , Claudio Arrigoni
发明人： Mario Varasi , Franco Heidempergher , Carla Caccia , Claudio Arrigoni
IPC分类号： C07D403/06 , A61K31/415 , A61K31/4178 , A61P1/00 , A61P1/08 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/20 , A61P25/26 , C07D233/32 , C07D233/54 , C07D233/56 , C07D233/61 , C07D401/06
CPC分类号： C07D233/64 , Y02P20/55
摘要： The invention relates to new derivatives of 1-imidazolylalkyl-3-phenyl-imidazolidin-2-ones of general formula (I) ##STR1## wherein n is 1, 2 or 3; 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; R.sub.3 is an imidazolyl group of formula ##STR2## wherein each of R.sub.8 and R.sub.10 which may be the same or different is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.9 is hydrogen, C.sub.1 -C.sub.6 alkyl or a nitrogen protecting group, or pharmaceutically acceptable salts thereof, which are useful in the treatment of CNS disorders, such as, e.g., anxiety and psychosis, and in the treatment of gut motility disorders, and/or emesis.
摘要翻译：本发明涉及通式（I）的单咪唑烷基-3-苯基 - 咪唑烷-2-酮的新衍生物，其中n为1,2或3; 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，其中R 4和R 5各自独立地是C 1 -C 6烷基甲酰基或C 2 -C 6烷酰基的C 1 -C 6烷氧基羰基，硝基，-N（R 4 R 5）或（R6R7）N-SO2基团，其中R6和R7各自独立地为氢或C1-C6烷基; R3是式IMAMA的咪唑基，其中R 8和R 10可以相同或不同的是氢或C 1 -C 6烷基，R 9是氢，C 1 -C 6烷基或氮保护基，或其药学上可接受的盐，其可用于治疗中枢神经系统疾病，例如焦虑和精神病，以及肠道运动障碍和/或呕吐的治疗。

13. 发明授权

US08278485B2 Process for the production of 2-[4-(3- and 2-fluorobenzyloxy) benzylamino] propanamides 有权
标题翻译：制备2- [4-（3-和2-氟苄氧基）苄氨基]丙酰胺的方法
公开(公告)号：US08278485B2
公开(公告)日：2012-10-02
申请号：US13288891
申请日：2011-11-03
申请人： Elena Barbanti , Carla Caccia , Patricia Salvati , Francesco Velardi , Tiziano Ruffilli , Luigi Bogogna
发明人： Elena Barbanti , Carla Caccia , Patricia Salvati , Francesco Velardi , Tiziano Ruffilli , Luigi Bogogna
IPC分类号： C07C231/12 , C07C233/09 , A61K31/165
CPC分类号： C07C231/12 , C07C231/18 , C07C237/06
摘要： A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]propanamides and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower than 0.03%, preferably lower than 0.01% by weight.The process is carried out by submitting the Schiff bases intermediates 2-[4-(3- and 2-fluorobenzyloxy)benzylideneamino]propanamides to catalytic hydrogenation in the presence of a heterogeneous catalyst in a protic organic solvent.
摘要翻译：一种获得治疗活性的2- [4-（3-和2-（氟苄氧基）苄氨基]丙酰胺及其与药学上可接受的酸的高纯度程度的盐，特别是二苄基衍生物杂质含量低于0.03％的方法，优选低于0.01重量％，该方法通过将席夫碱中间体2- [4-（3-和2-氟苄氧基）亚苄基氨基]丙酰胺在质子有机溶剂中的非均相催化剂存在下进行催化氢化来进行。

14. 发明申请

US20080096965A1 (Halobenzyloxy) Benzylamino-Propanamides as Sodium and/or Calcium Channel Selective Modulators 审中-公开
标题翻译：（Halobenzyloxy）苄基氨基 - 丙酰胺作为钠和/或钙通道选择性调节剂
公开(公告)号：US20080096965A1
公开(公告)日：2008-04-24
申请号：US11574751
申请日：2005-07-28
申请人： Elena Barbanti , Florian Thaler , Carla Caccia , Ruggero Fariello , Partricia Salvati
发明人： Elena Barbanti , Florian Thaler , Carla Caccia , Ruggero Fariello , Partricia Salvati
IPC分类号： A61K31/195 , A61P29/00
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 assodium 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）苄氨基] - 丙酰胺及其药学上可接受的盐在制备药物中的用途，所述药物是选择性活性的脯氨酸和/或钙通道调节剂，因此可用于预防，减轻和治愈各种病症，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病症，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。

15. 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.

16. 发明授权

US5874457A Imidazolylalkyl derivatives of imidazo�1,5-a!indol-3-one 失效
标题翻译：咪唑并[1,5-a]吲哚-3-酮的咪唑基烷基衍生物
公开(公告)号：US5874457A
公开(公告)日：1999-02-23
申请号：US578550
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： A61K31/415 , A61K31/4188 , A61P1/00 , A61P1/08 , A61P1/12 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/36 , A61P43/00 , C07D487/04
CPC分类号： C07D487/04 , Y02P20/55
摘要： Novel 5-HT.sub.3 receptor antagonist compounds having following formula (I) ##STR1## wherein n is 1, 2 or 3;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;R.sub.3 is an imidazolyl group of formula ##STR2## wherein each of R.sub.8 and R.sub.10 which may be the same or different is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.9 is hydrogen, C.sub.1 -C.sub.6 alkyl or a nitrogen protecting group; and the pharmaceutically acceptable salts thereof, are disclosed.
摘要翻译： PCT No.PCT / EP95 / 01651 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。出版物WO95 / 32204 日期：1995年11月30日具有下式（I）的新型5-HT 3受体拮抗剂化合物其中n为1,2或3; 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，其中R 4和R 5各自独立地为氢，C 1 -C 6烷基，甲酰基或C 2 -C 6烷酰基的C 1 -C 6烷氧羰基，硝基，-N（R 4 R 5）或（R6R7）N-SO2基团，其中R6和R7各自独立地为氢或C1-C6烷基; R 3是式（I）的咪唑基，其中R 8和R 10各自可以相同或不同，是氢或C 1 -C 6烷基，R 9是氢，C 1 -C 6烷基或氮保护基; 及其药学上可接受的盐。

17. 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。

18. 发明授权

US08076515B2 Process for the production of 2-[4-(3- and 2-fluorobenzyloxy) benzylamino] propanamides 有权
标题翻译：制备2- [4-（3-和2-氟苄氧基）苄氨基]丙酰胺的方法
公开(公告)号：US08076515B2
公开(公告)日：2011-12-13
申请号：US12338825
申请日：2008-12-18
申请人： Elena Barbanti , Carla Caccia , Patricia Salvati , Francesco Velardi , Tiziano Ruffilli , Luigi Bogogna
发明人： Elena Barbanti , Carla Caccia , Patricia Salvati , Francesco Velardi , Tiziano Ruffilli , Luigi Bogogna
IPC分类号： C07C231/12 , C07C233/09 , A61K31/165
CPC分类号： C07C231/12 , C07C231/18 , C07C237/06
摘要： A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]propanamides and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower than 0.03%, preferably lower than 0.01% by weight.The process is carried out by submitting the Schiff bases intermediates 2-[4-(3- and 2-fluorobenzyloxy)benzylideneamino]propanamides to catalytic hydrogenation in the presence of a heterogeneous catalyst in a protic organic solvent.
摘要翻译：一种获得治疗活性的2- [4-（3-和2-（氟苄氧基）苄氨基]丙酰胺及其与药学上可接受的酸的高纯度程度的盐，特别是二苄基衍生物杂质含量低于0.03％的方法，优选低于0.01重量％，该方法通过将席夫碱中间体2- [4-（3-和2-氟苄氧基）亚苄基氨基]丙酰胺在质子有机溶剂中的非均相催化剂存在下进行催化氢化来进行。

19. 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。

20. 发明授权

US07763751B2 Hydroxylamine derivatives 有权
标题翻译：羟胺衍生物
公开(公告)号：US07763751B2
公开(公告)日：2010-07-27
申请号：US10582141
申请日：2004-12-10
申请人： Carla Caccia , Laura Girola , Petra Karin Kaltofen , Daniele Losi , Patricia Salvati , Enrico Selva , Florian Thaler
发明人： Carla Caccia , Laura Girola , Petra Karin Kaltofen , Daniele Losi , Patricia Salvati , Enrico Selva , Florian Thaler
IPC分类号： C07C239/00 , A61K31/13
CPC分类号： C07C239/20 , A61K31/13 , C07C239/12 , C07C2602/10
摘要： This invention is related to hydroxylamino derivatives of the general formula (I) wherein n is 0, 1 or 2; R1 and R2, independently of each other, are H, OH or OCH3; R3 is H or CH3; R4 is H, C1-C3 straight or branched alkyl or, together with R3, forms a five to seven-membered carbocyclic ring; and R5 and R6, independently of each other, are H or C1-C5 straight or branched alkyl and the pharmaceutically acceptable salts or prodrug thereof, for the preparation of medicaments useful for the prevention, treatment and diagnosis of CNS degenerative disorders related to protein misfolding and/or misaggregation. The invention also relates to novel compounds included in formula (I), to a method for preparing said compounds and to pharmaceutical compositions containing them.
摘要翻译：本发明涉及通式（I）的羟基氨基衍生物，其中n为0,1或2; R 1和R 2彼此独立地是H，OH或OCH 3; R3是H或CH3; R4是H，C1-C3直链或支链烷基，或与R3一起形成五至七元碳环; 和R5和R6彼此独立地是H或C 1 -C 5直链或支链烷基及其药学上可接受的盐或前药，用于制备用于预防，治疗和诊断与蛋白质错折叠有关的CNS退行性病症的药物和/或散乱。本发明还涉及式（I）中包括的新化合物，涉及制备所述化合物的方法和含有它们的药物组合物。

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