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21. 发明授权

US5238953A N-imidazolyl derivatives of substituted tetrahydrocarbazole and cyclohept (B) indole 失效
标题翻译：取代四氮唑并环己酮（B）吲哚的N-咪唑衍生物
公开(公告)号：US5238953A
公开(公告)日：1993-08-24
申请号：US824240
申请日：1992-01-21
申请人： Paolo Cozzi , Antonio Pillan , Maurizio Pulici , Patricia Salvati , Angelo D. Volpi
发明人： Paolo Cozzi , Antonio Pillan , Maurizio Pulici , Patricia Salvati , Angelo D. Volpi
IPC分类号： A61K31/415 , A61P7/02 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/02 , A61P15/00 , A61P25/04 , A61P43/00 , C07D403/10 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： The invention provides new N-imidazolyl derivatives of substituted tetrahydrocarbazoles and cyclopent[b]indoles of general formula (I) ##STR1## wherein n is 1 or 2;p is an integer of 1 to 4;A is a straight or branched C.sub.1 -C.sub.4 alkylene chain;B is a direct linkage, a straight or branched, unsaturated or saturated C.sub.1 -C.sub.4 alkylene chain;Q is a direct linkage or a straight or branched C.sub.1 -C.sub.4 alkylene chain;each of R.sub.1 and R.sub.2 independently is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfonyl, halogen or trihalomethyl;each of R.sub.3 and R.sub.5, independently is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.4 is --OR.sub.6 or --N(R.sub.6,R.sub.7) group, wherein each of R.sub.6 and R.sub.7 independently is hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or benzyl; or a pharmaceutically acceptable salt thereof, which are useful in the treatment of a disease state in which an enhancement of TxA.sub.2 synthesis exerts a pathogenic effect.

22. 发明授权

US4882347A "N-imidazolyl derivatives of bicyclic compounds and pharmaceutical compositions containing the same" 失效
标题翻译： “双环化合物的N-咪唑基衍生物和含有相同的”
公开(公告)号：US4882347A
公开(公告)日：1989-11-21
申请号：US201909
申请日：1988-06-02
申请人： Paolo Cozzi , Corrado Ferti , Patricia Salvati , Germano Carganico , Antonio Pillan
发明人： Paolo Cozzi , Corrado Ferti , Patricia Salvati , Germano Carganico , Antonio Pillan
IPC分类号： C07D233/60 , A61K31/415 , A61P13/02 , A61P15/00 , C07D233/61 , C07D405/04
CPC分类号： A61K31/415 , Y10S514/866
摘要： A pharmaceutical compositon having activity against nephropathies comprising, as an active agent, a therapeutically effective amount of a compound of formula (I) ##STR1## wherein (a) ##STR2## wherein Y completes a single bond or is oxygen or a --CH.sub.2 -- group and the symbol ##STR3## represents a single bond or (b) ##STR4## ##STR5## and the symbol ##STR6## represents a double bond; one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is --CH.sub.2 OH, C.sub.2 -C.sub.4 acyl, ##STR7## in which each of R.sub.1, R.sub.8 and R.sub.9 is independently hydrogen or C.sub.1 -C.sub.4 alkyl and the others are independently chosen from hydrogen, hydroxy, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and --COOR, wherein R.sub.7 is as defined above, and one of R.sub.5 and R.sub.6 is hydrogen and the other is hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl; or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier and/or diluent.
摘要翻译：具有抗肾病活性的药物组合物，其包含作为活性剂的治疗有效量的式（I）化合物（I），其中（a）其中Y完成单键或氧或氧 -CH 2 - 基，符号表示单键或（b），符号表示双键; R 1，R 2，R 3和R 4中的一个是-CH 2 OH，C 2 -C 4酰基，其中R 1，R 8和R 9各自独立地为氢或C 1 -C 4烷基，其余各自独立地选自氢，羟基，卤素，C 1 -C 4烷基，C 1 -C 4烷氧基和-COOR，其中R 7如上所定义，R 5和R 6之一是氢，另一个是氢，C 1 -C 6烷基或苯基; 或其药学上可接受的盐; 和药学上可接受的载体和/或稀释剂。

23. 发明授权

US4500712A Ergoline derivatives 失效
标题翻译：二元醇衍生物
公开(公告)号：US4500712A
公开(公告)日：1985-02-19
申请号：US438259
申请日：1982-11-01
申请人： Luigi Bernardi , Aldemio Temperilli , Daniela Ruggieri , Giuliana Arcari , Patricia Salvati
发明人： Luigi Bernardi , Aldemio Temperilli , Daniela Ruggieri , Giuliana Arcari , Patricia Salvati
IPC分类号： A61K31/48 , A61P1/04 , A61P9/12 , C07D457/02 , C07D457/12 , C07D457/04
CPC分类号： C07D457/02 , C07D457/12
摘要： There are provided ergoline derivatives of formula ##STR1## wherein R.sub.1 .dbd.H, CH.sub.3 ; R.sub.2 .dbd.H or halogen atom, or CH.sub.3,CN, alkyl- or phenyl-thio; R.sub.3 .dbd.H, OCH.sub.3 ; R.sub.4 .dbd.C.sub.1 -C.sub.4 hydrocarbon group; X.dbd.O, S, NH; A.dbd.CO, SO.sub.2 ; B.dbd.C.sub.1 -C.sub.4 hydrocarbon group, aryl, aralkyl, heterocyclic ring group, alkoxy, aryloxy; n.dbd.0, 1, 2; and pharmaceutically acceptable salts thereof.A process for preparing said compounds is also provided. The compounds show anti-hypertensive activity and are active on the gastroenteric system.
摘要翻译：提供式（Ⅰ）的麦角灵衍生物，其中R1 = H，CH3; R2 = H或卤素原子，或CH3，CN，烷基或苯基 - 硫基; R3 = H，OCH3; R4 = C1-C4烃基; X = O，S，NH; A = CO，SO2; B = C1-C4烃基，芳基，芳烷基，杂环基，烷氧基，芳氧基; n = 0,1,2; 及其药学上可接受的盐。还提供了制备所述化合物的方法。这些化合物显示出抗高血压活性，并且对胃肠系统有活性。

24. 发明授权

US08741957B2 Alpha-aminoamide derivatives useful in the treatment of cognitive disorders 有权
标题翻译：可用于治疗认知障碍的α-氨基酰胺衍生物
公开(公告)号：US08741957B2
公开(公告)日：2014-06-03
申请号：US12304455
申请日：2007-06-13
申请人： Patricia Salvati , Stefano Rossetti , Luca Benatti
发明人： Patricia Salvati , Stefano Rossetti , Luca Benatti
IPC分类号： A61K31/165 , A61K31/404 , A61K31/085 , A61K31/135 , A61K31/341 , A61K31/402
CPC分类号： A61K31/404 , A61K31/085 , A61K31/135 , A61K31/165 , A61K31/341 , A61K31/402
摘要： The present invention is in the field of pharmacotherapy of cognitive deficits in learning and memory by administering an α-aminoamide, particularly safinamide. Examples of disturbances in cognition that can be treated with compounds of the invention are the ones associated with disorders such as autism, dyslexia, attention deficit hyperactivity disorder, schizophrenia, obsessive compulsive disorders, psychosis, bipolar disorders, depression, Tourette's syndrome, Mild Cognitive Impairment (MCI) and disorders of learning in children, adolescents and adults, Age Associated Memory Impairment, Age Associated Cognitive Decline, Alzheimer's Disease, Parkinson's Disease, Down's Syndrome, traumatic brain injury Huntington's Disease, Progressive Supranuclear Palsy (PSP), HIV, stroke, vascular diseases, Pick's or Creutzfeldt-Jacob diseases, multiple sclerosis (MS), other white matter disorders and drug-induced cognitive worsening.
摘要翻译：本发明通过给予α-氨基酰胺，特别是safinamide，在学习和记忆中的认知缺陷的药物治疗领域。可以用本发明化合物治疗的认知障碍的例子是与自闭症，阅读困难，注意缺陷多动障碍，精神分裂症，强迫症，精神病，双相情感障碍，抑郁症，Tourette综合征，轻度认知障碍（MCI）和儿童，青少年和成年人学习障碍，年龄相关记忆障碍，年龄相关认知衰退，阿尔茨海默病，帕金森病，唐氏综合征，创伤性脑损伤亨廷顿病，进行性核核麻痹（PSP），艾滋病毒，中风，血管疾病，Pick's或Creutzfeldt-Jacob疾病，多发性硬化症（MS），其他白质病症和药物诱导的认知恶化。

25. 发明授权

US08445539B2 Alpha-aminoamide derivatives useful in the treatment of psychiatric disorders 有权
标题翻译：用于治疗精神疾病的α-氨基酰胺衍生物
公开(公告)号：US08445539B2
公开(公告)日：2013-05-21
申请号：US12816143
申请日：2010-06-15
申请人： Emanuela Izzo , Laura Faravelli , Elena Barbanti , Patricia Salvati
发明人： Emanuela Izzo , Laura Faravelli , Elena Barbanti , Patricia Salvati
IPC分类号： A61K31/165
CPC分类号： A61K31/165
摘要： The disclosure relates to pharmacotherapy of a psychiatric disorder which is schizophrenia and/or anxiety, wherein schizophrenia includes schizophrenia related disorders such as brief psychotic disorders, delusional disorders, schizoaffective disorders, and schizophreniform disorders, and anxiety includes panic disorders, obsessive-compulsive disorders (OCD), post-traumatic stress disorders (PTSD), social phobia or social anxiety disorders, specific phobia, and generalized anxiety disorders (GAD). The compounds of the disclosure are useful for the treatment of the above psychiatric disorders alone or in combination with other therapeutical agents effective in the treatment of schizophrenia and/or anxiety disorders.
摘要翻译：本公开涉及精神障碍和/或焦虑症的精神障碍的药物治疗，其中精神分裂症包括精神分裂症相关的疾病，例如短暂性精神病，妄想障碍，分裂情感障碍和精神分裂症样症状，焦虑包括恐慌症，强迫症（强迫症） OCD），创伤后应激障碍（PTSD），社交恐惧症或社会焦虑症，特定恐惧症和广泛性焦虑症（GAD）。本公开的化合物可用于单独或与治疗精神分裂症和/或焦虑症有效的其它治疗剂组合治疗上述精神障碍。

26. 发明申请

US20120220592A1 2-PHENYLETHYLAMINO DERIVATIVES AS CALCIUM AND/OR SODIUM CHANNEL MODULATORS 有权
标题翻译：作为钙和/或钠通道调节剂的2-苯乙烯胺衍生物
公开(公告)号：US20120220592A1
公开(公告)日：2012-08-30
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： A61K31/165 , A61K31/433 , A61K31/44 , A61K31/445 , A61K31/5375 , A61P25/00 , A61P25/06 , A61P25/28 , A61P25/18 , A61P25/08 , A61P25/30 , A61P29/00 , A61P1/00 , A61P13/00 , A61P27/02 , A61P1/16 , A61P37/00 , A61P5/00 , A61P9/00 , A61K31/42
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。

27. 发明申请

US20100197799A1 HYDROXYLAMINE DERIVATIVES 审中-公开
标题翻译：羟基胺衍生物
公开(公告)号：US20100197799A1
公开(公告)日：2010-08-05
申请号：US12760007
申请日：2010-04-14
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： A61K31/13 , C07C239/20 , A61P25/16 , A61P25/28
CPC分类号： C07C239/20 , A61K31/13 , C07C239/12 , C07C2602/10
摘要： This invention is related to hydroxylamino derivatives of the following 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 the compounds and to pharmaceutical compositions containing them.
摘要翻译：本发明涉及以下通式（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相关的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，涉及制备该化合物的方法和含有该化合物的药物组合物。

28. 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。

29. 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。

30. 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。

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