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1. 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。

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

WO2009074478A1 PROCESS FOR THE PRODUCTION OF 2-[4-(3- OR 2-FLUOROBENZYLOXY)BENZYLAMINO]PROPANAMIDES WITH HIGH PURITY DEGREE 审中-公开
标题翻译：生产2- [4-（3-或2-氟代苄基）苯甲酰胺]丙二醛与高纯度度的方法
公开(公告)号：WO2009074478A1
公开(公告)日：2009-06-18
申请号：PCT/EP2008/066559
申请日：2008-12-01
申请人： NEWRON PHARMACEUTICALS S.P.A. , BARBANTI, Elena , FARAVELLI, Laura , SALVATI, PATRICIA , CANEVOTTI, Renato , PONZINI, Francesco
发明人： BARBANTI, Elena , FARAVELLI, Laura , SALVATI, PATRICIA , CANEVOTTI, Renato , PONZINI, Francesco
IPC分类号： C07C231/12 , C07C251/24 , C07C237/08 , A61K31/165 , A61P25/00
CPC分类号： C07C251/24 , A61K31/165 , A61K31/197 , A61K31/198 , A61K45/06 , C07C231/12 , C07C231/24 , C07C237/08
摘要： A process for obtaining therapeutically active 2-[4-(3- and 2-(flurobenzyloxy)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 a reduction reaction with a reducing agent selected from sodium borohydride and potassium borohydride in an appropriate amount of an organic solvent selected from C 1 -C 5 lower alkanols, allowing the formation and presence during a substantial position of the reduction reaction course of a suspension of the Schiff base into the saturated solution of the Schiff base into the same organic solvent.
摘要翻译：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度纯度的盐，特别是二苄基衍生物杂质的含量低于0.03％，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]丙酰胺与还原剂一起还原反应进行，所述还原剂选自硼氢化钠和钾硼氢化物在适当量的选自C 1 -C 5低级链烷醇的有机溶剂中，允许在希夫碱的悬浮液的还原反应过程的大部分位置的形成和存在进入席夫碱的饱和溶液进入相同的有机物溶剂。

4. 发明申请

WO2005054206A1 HISTIDINE DERIVATIVES 审中-公开
公开(公告)号：WO2005054206A1
公开(公告)日：2005-06-16
申请号：PCT/EP2004/012944
申请日：2004-11-15
申请人： NEWRON PHARMACEUTICALS S.P.A. , MELLONI, Piero , SABIDO DAVID, Cibele, Maria , FARAVELLI, Laura , MAESTRONI, Sara , DONDIO, Giulio , SALVATI, Patricia
发明人： MELLONI, Piero , SABIDO DAVID, Cibele, Maria , FARAVELLI, Laura , MAESTRONI, Sara , DONDIO, Giulio , SALVATI, Patricia
IPC分类号： C07D233/64
CPC分类号： C07D233/64
摘要： This invention is related to novel histidine derivatives of the following general formula (I), wherein X is methylene, oxygen, sulphur or a NR 8 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 , R 6 , R 7 , R 8 are independently hydrogen or C 1 -C 4 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, ophtalmic, 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）的新型组氨酸衍生物，其中X为亚甲基，氧，硫或NR 8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，R 6，R 7，R 8独立地是氢或C 1 -C 4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，眼底，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。

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。

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