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. 发明申请

WO2013000651A8 FLUORINATED ARYLALKYLAMINOCARBOXAMIDE DERIVATIVES 审中-公开
公开(公告)号：WO2013000651A8
公开(公告)日：2013-01-03
申请号：PCT/EP2012/060006
申请日：2012-05-29
申请人： NEWRON PHARMACEUTICALS S.P.A. , PEVARELLO, Paolo
发明人： PEVARELLO, Paolo
IPC分类号： C07C237/06 , C07D209/08 , C07D217/06 , C07D265/36 , C07D295/185 , C07D295/182 , A61K31/165 , A61P25/00
摘要： Fluorinated arylalkylaminocarboxamide derivatives of formula (I) are described wherein W, J, n, R 1 , R 2 , R 2' , R 3 , R 4 , R 5 and R 6 have the meanings as defined in the specification and pharmaceutically salts thereof, pharmaceutical compositions containing them as active ingredients 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, ophtalmic, urolological, and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.

2. 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。

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

WO2009109334A1 (S)-(+)-2-[4-FLUORBENZYLOXY)BENZYLAMINO]PROPANAMIDE FOR USE IN THE TREATMENT OF MIXED OR COMBINED PAIN 审中-公开
标题翻译：（S） - （+） - 2- [4-氟苄氧基]苯甲酰胺]丙酰胺用于治疗混合或组合的疼痛
公开(公告)号：WO2009109334A1
公开(公告)日：2009-09-11
申请号：PCT/EP2009/001407
申请日：2009-02-27
申请人： NEWRON PHARMACEUTICALS S.P.A. , FARAVELLI, Laura , MARCHETTINI, Paolo , GIULIANI, Rodolfo , ROSSETTI, Stefano , BENATTI, Luca
发明人： FARAVELLI, Laura , MARCHETTINI, Paolo , GIULIANI, Rodolfo , ROSSETTI, Stefano , BENATTI, Luca
IPC分类号： A61K31/165 , A61P25/02 , A61P29/02 , A61K45/06
CPC分类号： A61K45/06 , A61K31/165 , A61K2300/00
摘要： (S)-(+)-2-[4-(2-Fluorobenzyloxy) benzylamino] propanamide (ralfϊnamide) and the salts thereof with pharmaceutically acceptable acids for use in the treatment of mixed or combined pain where a nociceptive component is combined with a neuropathic component, such as nerve compression and/or nerve entrapment syndromes, in particular, neuropathic low back pain (NLBP) or radicular low back pain (RLBP), alone or in combination with other therapeutic agents.
摘要翻译：（S） - （+） - 2- [4-（2-氟苄氧基）苄基氨基]丙酰胺（ralf？namide）及其与药学上可接受的酸的盐，用于治疗混合或组合的疼痛，其中伤害性成分组合具有神经性成分，例如神经压迫和/或神经阻滞综合征，特别是神经性下腰痛（NLBP）或根性背痛（RLBP），单独或与其它治疗剂组合。

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

WO2007144153A2 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：WO2007144153A2
公开(公告)日：2007-12-21
申请号：PCT/EP2007/005197
申请日：2007-06-13
申请人： NEWRON PHARMACEUTICALS S.P.A. , SALVATI, Patricia , ROSSETTI, Stefano , BENATTI, Luca
发明人： SALVATI, Patricia , ROSSETTI, Stefano , BENATTI, Luca
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。

8. 发明申请

WO2006102958A1 SUBSTITUTED AMINOALKYL- AND AMIDOALKYL-BENZOPYRAN DERIVATIVES 审中-公开
标题翻译：取代的氨基甲酰基和氨基二苯甲酮衍生物
公开(公告)号：WO2006102958A1
公开(公告)日：2006-10-05
申请号：PCT/EP2006/001572
申请日：2006-02-22
申请人： NEWRON PHARMACEUTICALS S.P.A. , CAROTTI, Angelo , MELLONI, Piero , THALER, Florian , CACCIA, Carla , MAESTRONI, Sara , SALVATI, Patricia
发明人： CAROTTI, Angelo , MELLONI, Piero , THALER, Florian , CACCIA, Carla , MAESTRONI, Sara , SALVATI, Patricia
IPC分类号： C07D311/08 , C07D311/58 , C07D311/74 , C07D405/12 , A61K31/37 , A61K31/353 , A61P25/00
CPC分类号： C07D311/16 , C07D311/58
摘要： This invention is related to novel aminoalkyl- and amidoalkyl- b enzopyran derivatives of the following general formula (I) wherein: the group (a) is a substituent in position 6 or 7 wherein: R is amono- or bi-cyclic (C 6 -C 10 ) aryl or a mono- or bi-cyclic (5-10) membered heteroaryl radical, said radicals rings being optionally substituted by one or two substituents selected from (C 1 -C 5 ) straight or branched alkyl, (C 1 -C 5 ) straight or branched alkoxy, hydroxy, halo and trifluoromethyl; m is zero or an integer from 1 to 3; n, p, R 1 and R 2 are as herein indicated and R 3 and R 4 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：（a）是位置6或7的取代基，其中：R是亚氨基或双环（C < 所述基团环任选地被一个或两个选自以下的取代基取代：（C 1 -C 10）芳基或单环或双环（5-10） C 1 -C 5 -C 5直链或支链烷基，（C 1 -C 5 -C 5）直链或支链烷氧基，羟基，卤素和三氟甲基; m为0或1〜3的整数; n，p，R 1和R 2 2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。在体外作为选择性和可逆的MAO-B抑制剂具有活性的化合物

9. 发明申请

WO2005054189A1 N-ACYL-N'-BENZYL-ALKYLENDIAMINO DERIVATIVES 审中-公开
标题翻译： N-乙酰基-N'-苄基-L-鸟氨酸衍生物
公开(公告)号：WO2005054189A1
公开(公告)日：2005-06-16
申请号：PCT/EP2004/012834
申请日：2004-11-12
申请人： NEWRON PHARMACEUTICALS S.P.A. , THALER, Florian , SABIDO DAVID, Cibele, Maria , FARAVELLI, Laura , GAGLIARDI, Stefania , COLOMBO, Elena , SALVATI, Patricia
发明人： THALER, Florian , SABIDO DAVID, Cibele, Maria , FARAVELLI, Laura , GAGLIARDI, Stefania , COLOMBO, Elena , SALVATI, Patricia
IPC分类号： C07D207/267
CPC分类号： C07D207/27 , C07C233/36
摘要： This invention is related to compounds and use of N-Acyl-N'-benzyl-alkylendiamino derivatives of the following general formula (I), wherein A is a straight or branched C 2 -C 8 alkyl chain; X is a methylene, oxygen, sulphur or a NR 7 group; R 1 is a straight or branched C 1 -C 8 alkyl or C 3 -C 8 alkenylene or C 3 -C 8 alkynylene chain, optionally substituted with CF 3 , phenyl, phenoxy or naphthyl, the aromatic rings optionally substituted by one or more C 1 -C 4 alkyl, halogens, trifluoromethyl, hydroxy or C 1 -C 4 alkoxy groups; R 2 , R 3 are independently hydrogen, a C 1 -C 3 alkyl chain, halogen, trifluoromethyl, hydroxy or C 1 -C 4 alkoxy groups; R 4 , R 5 are independently hydrogen or C 1 -C 6 alkyl; R 6 is a hydrogen or a straight or branched C 1 -C 8 alkyl or linked to R 5 can form a five to seven membered lactam; R 7 is hydrogen or C 1 -C 6 alkyl; and the pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators 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：本发明涉及以下通式（I）的N-酰基-N'-苄基 - 烷基二氨基衍生物的化合物和用途，其中A为直链或支链C 2 -C 8烷基链; X是亚甲基，氧，硫或NR 7基团; R 1是任选被CF 3，苯基，苯氧基或萘基取代的直链或支链C 1 -C 8烷基或C 3 -C 8亚烯基或C 3 -C 8亚炔基，任选被一个或多个C 1 -C 4烷基取代的芳环，卤素，三氟甲基，羟基或C 1 -C 4烷氧基; R 2，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独立地是氢或C 1 -C 6烷基; R 6是氢或直链或支链C 1 -C 8烷基或连接至R 5可以形成5至7元的内酰胺; R 7是氢或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，因此可用于预防，减轻和治愈广泛范围的病症，包括但不限于神经，精神，心血管，炎症，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。

10. 发明申请

WO2004048361A1 HALOTHENOYL-CYCLOPROPANE-1-CARBOXYLIC ACID DERIVATIVES 审中-公开
标题翻译：乙烯基环丙烷-1-羧酸衍生物
公开(公告)号：WO2004048361A1
公开(公告)日：2004-06-10
申请号：PCT/EP2003/013244
申请日：2003-11-25
申请人： NEWRON PHARMACEUTICALS S.P.A. , BENATTI, Luca , FARIELLO, Ruggero , SALVATI, Patricia , PELLICCIARI, Roberto , CACCIA, Carla
发明人： BENATTI, Luca , FARIELLO, Ruggero , SALVATI, Patricia , PELLICCIARI, Roberto , CACCIA, Carla
IPC分类号： C07D333/28
CPC分类号： C07D333/28
摘要： Compounds of formula (I) wherein R is hydroxy, linear or branched C 1 -C 6 alkoxy, phenoxy, benzyloxy, a group -N(R 1 R 2 ) wherein R 1 is hydrogen, linear or branched C 1 -C 4 alkyl, benzyl, phenyl and R 2 is hydrogen or linear or branched C 1 -C 4 alkyl, or R is a glycoside residue or a primary alkoxy residue from ascorbic acid, optionally having one or more hydroxy groups alkylated or acylated by linear or branched C 1 -C 4 alkyl or acyl groups; X is a halogen atom and n 1 or 2 are long lasting inhibitors of kynurenine 3-monooxygenase (KMO) and potent glutamate (GLU) release inhibitors.
摘要翻译：其中R是羟基，直链或支链C 1 -C 6烷氧基，苯氧基，苄氧基，基团-N（R 1 R 2）的式（I）化合物，其中R 1是氢，直链或支链C1- C4烷基，苄基，苯基和R 2是氢或直链或支链C 1 -C 4烷基，或R是来自抗坏血酸的糖苷残基或伯烷氧基残基，任选具有一个或多个羟基被烷基化或酰化直链或支链C 1 -C 4烷基或酰基; X是卤素原子，n 1或2是犬尿苷3-单加氧酶（KMO）和强力谷氨酸（GLU）释放抑制剂的长效抑制剂。

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