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1. 发明申请

WO2009080470A1 ALPHA-AMINOAMIDE DERIVATIVES USEFUL IN THE TREATMENT OF PSYCHIATRIC DISORDERS 审中-公开
标题翻译：用于治疗心理疾病的ALPHA-氨基腺苷衍生物
公开(公告)号：WO2009080470A1
公开(公告)日：2009-07-02
申请号：PCT/EP2008/066884
申请日：2008-12-05
申请人： NEWRON PHARMACEUTICALS S.P.A. , IZZO, Emanuela , FARAVELLI, Laura , BARBANTI, Elena , SALVATI, Patricia
发明人： IZZO, Emanuela , FARAVELLI, Laura , BARBANTI, Elena , SALVATI, Patricia
IPC分类号： A61K31/165 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/00
CPC分类号： A61K31/165
摘要： The present invention relates to pharmacotherapy of a psychiatric disorder which is schizophrenia and/or anxiety wherein schizophrenia includes schizophrenia related disorder 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 invention 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：本发明涉及精神障碍的精神病药物治疗，其中精神分裂症和/或焦虑症，其中精神分裂症包括精神分裂症相关疾病如短暂精神病，妄想症，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）。本发明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疾病。

2. 发明申请

WO2007144153A3 ALPHA-AMINOAMIDE DERIVATIVES USEFUL IN THE TREATMENT OF COGNITIVE DISORDERS 审中-公开
标题翻译：用于治疗认知障碍的ALPHA-氨基酰胺衍生物
公开(公告)号：WO2007144153A3
公开(公告)日：2008-03-13
申请号：PCT/EP2007005197
申请日：2007-06-13
申请人： NEWRON PHARM SPA , SALVATI PATRICIA , ROSSETTI STEFANO , BENATTI LUCA
发明人： SALVATI PATRICIA , ROSSETTI STEFANO , BENATTI LUCA
IPC分类号： A61K31/165 , A61P25/28
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 a-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。

3. 发明申请

WO2007147491A1 PROCESS FOR THE PRODUCTION OF 2- [4 - ( 3- AND 2-FLU0R0BENZYL0XY) BENZYLAMIN0] PROPAN AMIDES 审中-公开
标题翻译： 2- [4-（3-和2-氟代苄基）苯甲酰胺0]丙酰胺的制备方法
公开(公告)号：WO2007147491A1
公开(公告)日：2007-12-27
申请号：PCT/EP2007/005105
申请日：2007-06-08
申请人： NEWRON PHARMACEUTICALS S.P.A. , BARBANTI, Elena , CACCIA, Carla , SALVATI, Patricia , VELARDI, Francesco , RUFILLI, Tiziano , BOGOGNA, Luigi
发明人： BARBANTI, Elena , CACCIA, Carla , SALVATI, Patricia , VELARDI, Francesco , RUFILLI, Tiziano , BOGOGNA, Luigi
IPC分类号： C07C231/10 , C07C233/13 , 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。

4. 发明申请

WO2005040138A1 SUBSTITUTED BENZYLAMINOALKYLENE HETEROCYCLES 审中-公开
标题翻译：取代的苯甲酰氨基烯烃杂环化合物
公开(公告)号：WO2005040138A1
公开(公告)日：2005-05-06
申请号：PCT/EP2004/011104
申请日：2004-10-05
申请人： NEWRON PHARMACEUTICALS S.P.A. , SALVATI, Patricia , CACCIA, Carla , MELLONI, Piero , RESTIVO, Alessandra , SABIDO DAVID, Cibele , VALLESE, Stefania
发明人： SALVATI, Patricia , CACCIA, Carla , MELLONI, Piero , RESTIVO, Alessandra , SABIDO DAVID, Cibele , VALLESE, Stefania
IPC分类号： C07D261/02
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 NR 7 group; R 1 is C 3 -C 8 alkyl, or C 1 -C 8 alkyl substituted by phenoxy or phenyl, both phenoxy or phenyl being optionally substituted by one or more fluoro, chloro, trifluoromethyl, C 1 -C 6 alkyl, hydroxyl, C 1 -C 6 alkoxy; R 2 , R 3 are independently hydrogen, C 1 -C 6 alkyl, halogen, trifluoromethyl, hydroxy or C 1 -C 6 alkoxy; R 4 is hydrogen, C 1 -C 8 alkyl; R 5 , R 6 are independently hydrogen, C 1 -C 3 alkyl, optionally substituted by hydroxy or phenyl; R 7 is hydrogen or straight or branched C 1 -C 3 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 C 1 -C 6 alkyl, halogen, hydroxyl or C 1 -C 6 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; R 2，R 3独立地是氢，C 1 -C 6烷基，卤素，三氟甲基，羟基或C 1 -C 6烷氧基; R 4是氢，C 1 -C 8烷基; R 5，R 6独立地是氢，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抑制剂具有活性，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。

5. 发明申请

WO1997005111A1 N-(4-SUBSTITUTED-BENZYL)-2-AMINOLACTAM DERIVATIVES 审中-公开
标题翻译： N-（4-取代苄基）-2-氨基甲酰胺衍生物
公开(公告)号：WO1997005111A1
公开(公告)日：1997-02-13
申请号：PCT/EP1996002962
申请日：1996-07-05
申请人： PHARMACIA & UPJOHN S.P.A. , PEVARELLO, Paolo , AMICI, Raffaella , VARASI, Mario , MAJ, Roberto , SALVATI, Patricia
发明人： PHARMACIA & UPJOHN S.P.A.
IPC分类号： C07D211/74
CPC分类号： C07D207/273 , C07D205/085 , C07D211/76
摘要： Novel N-(4-substituted-benzyl)-2-aminolactams compounds, having antiepileptic, anti-Parkinson, neuroprotective, anti-depressant, antispastic and/or hypnotic activity, of general formula (I) wherein: m is zero, 1, 2 or 3; n is zero, 1, 2 or 3; X is -O-, -S-, -CH2- or -NH-; each of R and R1 independently is hydrogen, C1-C6 alkyl, halogen, hydroxy, C1-C4 alkoxy or trifluoromethyl; each of R2, R3 and R4 independently is hydrogen, C1-C6 alkyl optionally substituted by a hydroxy group, or C3-C7 cycloalkyl; and the pharmaceutically acceptable salts thereof, are disclosed.
摘要翻译：具有通式（I）的具有抗癫痫，抗帕金森综合征，神经保护作用，抗抑郁药，抗痉挛和/或催眠活性的新型N-（4-取代 - 苄基）-2-氨基内酰胺化合物，其中：m为0,1， 2或3; n为零，1,2或3; X是-O - ， - S - ， - CH 2 - 或-NH-; R和R 1各自独立地为氢，C 1 -C 6烷基，卤素，羟基，C 1 -C 4烷氧基或三氟甲基; R 2，R 3和R 4各自独立地为氢，任选被羟基取代的C 1 -C 6烷基或C 3 -C 7环烷基; 及其药学上可接受的盐。

6. 发明申请

WO2007071311A1 2 -PHENYLETHYLAMINO DERIVATIVES AS CALCIUM AND/OR SODIUM CHANNEL MODULATORS 审中-公开
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：WO2007071311A1
公开(公告)日：2007-06-28
申请号：PCT/EP2006/011443
申请日：2006-11-29
申请人： NEWRON PHARMACEUTICALS S.P.A. , THALER, Florian , NAPOLETANO, Mauro , SABIDO-DAVID, Cibele , MORIGGI, Ermanno , CACCIA, Carla , FARAVELLI, Laura , RESTIVO, Alessandra , SALVATI, Patricia
发明人： THALER, Florian , NAPOLETANO, Mauro , SABIDO-DAVID, Cibele , MORIGGI, Ermanno , CACCIA, Carla , FARAVELLI, Laura , RESTIVO, Alessandra , SALVATI, Patricia
IPC分类号： C07D237/06 , C07D295/18 , C07D307/52 , C07D295/08 , C07D309/06 , C07D307/14 , C07D261/08 , C07D213/30 , C07D213/38 , A61K31/33 , A61K31/165 , A61P25/00 , A61P9/00 , A61P13/00 , A61P27/00
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 of formula (I); wherein J, W, R, R 0 R 1 , R 2 , R 3 , and R 4 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，R 0，R 1，R 2，R 3和R 2 > 4 具有本说明书及其药学上可接受的盐中所定义的含义，含有它们作为活性成分的药物组合物及其作为钠和/或钙通道调节剂的用途，其可用于预防缓解和治愈多种病变，描述了上述机制已被描述为发挥病理作用的神经，精神，心血管，炎症，眼科，泌尿科和胃肠道疾病。

7. 发明申请

WO2005018627A8 ALPHA-AMINOAMIDE DERIVATIVES USEFUL AS ANTI-INFLAMMATORY AGENTS 审中-公开
标题翻译：可用作抗炎药物的ALPHA-氨基脲衍生物
公开(公告)号：WO2005018627A8
公开(公告)日：2005-09-01
申请号：PCT/IB2004001574
申请日：2004-04-22
申请人： NEWRON PHARM SPA , SALVATI PATRICIA , VENERONI ORIETTA , BARBANTI ELENA , RUGGERO FARIELLO , BENATTI LUCA
发明人： SALVATI PATRICIA , VENERONI ORIETTA , BARBANTI ELENA , RUGGERO FARIELLO , BENATTI LUCA
IPC分类号： A61K31/165 , A61K31/381 , A61P1/04 , A61P13/10 , A61P19/02
CPC分类号： A61K31/381 , A61K31/165
摘要： Methods of using certain a-aminoamide derivatives as anti-inflammatory agents. The anti-inflammatory agents of the invention are able to reduce or even stop inflammatory s conditions substantially without side effects.
摘要翻译：使用某些α-氨基酰胺衍生物作为抗炎剂的方法。本发明的抗炎剂能够基本上没有副作用减少甚至阻止炎性病症。

8. 发明申请

WO2004089353A8 METHODS FOR TREATMENT OF PARKINSON'S DISEASE 审中-公开
标题翻译：治疗帕金森病的方法
公开(公告)号：WO2004089353A8
公开(公告)日：2005-09-01
申请号：PCT/IB2004001408
申请日：2004-04-08
申请人： NEWRON PHARMACEUTICALS INC , RUGGERO FARIELLO , CATTANEO CARLO , SALVATI PATRICIA , BENATTI LUCA
发明人： RUGGERO FARIELLO , CATTANEO CARLO , SALVATI PATRICIA , BENATTI LUCA
IPC分类号： A61K31/16 , A61K45/06 , A61P25/16
CPC分类号： A61K31/165 , A61K31/137 , A61K31/16 , A61K31/473 , A61K31/4745 , A61K31/475 , A61K31/48 , A61K31/485 , A61K31/498 , A61K31/4985 , A61K31/55 , A61K45/06 , A61K2300/00
摘要： New uses of safinamide, safinamide derivatives and MAO-B inhibitors in novel types of treatment for Parkinson's Disease are described. More specifically, the invention relates to methods for treating Parkinson's Disease through the administration of safinamide, a safinamide derivative, or a MAO-B inhibitor, in combination with other Parkinson's Disease agents or treatments, such as levodopa/PDI or dopamine agonists.
摘要翻译：描述了safinamide，safinamide衍生物和MAO-B抑制剂在新型帕金森病治疗类型中的新用途。更具体地，本发明涉及通过与其他帕金森病药物或治疗如左旋多巴/ PDI或多巴胺激动剂的组合组合施用safinamide，safinamide衍生物或MAO-B抑制剂来治疗帕金森病的方法。

9. 发明申请

WO2003020273A2 PHARMACEUTICAL COMPOSITION COMPRISING GABAPENTIN OR AN ANALOGUE THEREOF AND AN $G(A)-AMINOAMIDE AND ITS ANALGESIC USE 审中-公开
标题翻译：包含GABAPENTIN或其类似物和ANG（A） - 氨基酰胺的药物组合物及其镇痛用途
公开(公告)号：WO2003020273A2
公开(公告)日：2003-03-13
申请号：PCT/EP2002/008910
申请日：2002-08-09
申请人： NEWRON PHARMACEUTICALS SPA , SALVATI, Patricia , VENERONI, Orietta , MAJ, Roberto , FARIELLO, Ruggero , BENATTI, Luca
发明人： SALVATI, Patricia , VENERONI, Orietta , MAJ, Roberto , FARIELLO, Ruggero , BENATTI, Luca
IPC分类号： A61K31/445
CPC分类号： A61K31/16 , A61K31/445 , A61K2300/00
摘要： There is disclosed a pharmaceutical composition comprising gabapentin or an analogue thereof (pregabalin or tiagabine) and an α-aminoamide and its analgesic use. A synergistic effect of the respective analgesic activities without concomitant increase of side effects was observed.
摘要翻译：公开了包含加巴喷丁或其类似物（普瑞巴林或噻加宾）和α-氨基酰胺及其镇痛用途的药物组合物。观察到各自镇痛活性的协同作用，但没有伴随副作用的增加。

10. 发明申请

WO1997005102A1 2-(4-SUBSTITUTED)-BENZYLAMINO-2-METHYL-PROPANAMIDE DERIVATIVES 审中-公开
标题翻译： 2-（4-取代的） - 苯甲酰胺-2-甲基丙酰胺衍生物
公开(公告)号：WO1997005102A1
公开(公告)日：1997-02-13
申请号：PCT/EP1996002961
申请日：1996-07-05
申请人： PHARMACIA & UPJOHN S.P.A. , PEVARELLO, Paolo , AMICI, Raffaella , VARASI, Mario , BONSIGNORI, Alberto , SALVATI, Patricia
发明人： PHARMACIA & UPJOHN S.P.A.
IPC分类号： C07C237/06
CPC分类号： C07C237/06 , C07C323/36
摘要： Novel 2-(4-substituted)-benzylamino-2-methyl-propanamides compounds, having CNS activity, of general formula (I) wherein: n is zero, 1, 2 or 3; X is -O-, -S-, -CH2- or -NH-; each of R and R1 independently is hydrogen, C1-C6 alkyl, halogen, hydroxy, C1-C4 alkoxy or trifluoromethyl; each of R2, R3 and R4 independently is hydrogen, C1-C6 alkyl or C3-C7 cycloalkyl; and the pharmaceutically acceptable salts thereof, are disclosed.
摘要翻译：具有通式（I）的CNS活性的新的2-（4-取代） - 苄基氨基-2-甲基 - 丙酰胺化合物，其中：n为0,1,2或3; X是-O - ， - S - ， - CH 2 - 或-NH-; R和R 1各自独立地为氢，C 1 -C 6烷基，卤素，羟基，C 1 -C 4烷氧基或三氟甲基; R2，R3和R4各自独立地为氢，C1-C6烷基或C3-C7环烷基; 及其药学上可接受的盐。

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