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51. 发明公开

EP1809271A2 (HALOBENZYLOXY) BENZYLAMINO-PROPANAMIDES AS SODIUM AND/OR CALCIUM CHANNEL SELECTIVE MODULATORS 有权
标题翻译：使用（R） - （HALOGENBENZYLOXY）苄基氨基PROPANAMIDEN钠和/或钙通道选择性调节剂
公开(公告)号：EP1809271A2
公开(公告)日：2007-07-25
申请号：EP05769799.7
申请日：2005-07-28
申请人： Newron Pharmaceuticals S.p.A.
发明人： BARBANTI, Elena , THALER, Florian , CACCIA, Carla , FARIELLO, Ruggero , SALVATI, Patricia
IPC分类号： A61K31/165 , A61K31/00 , A61K45/06 , A61P29/00 , A61P25/06 , A61P25/02 , A61P9/00 , A61P13/00 , A61P3/00 , A61P1/00 , A61P17/00 , A61P11/00 , A61P37/00 , A61P25/08 , A61P5/00
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.

52. 发明公开

EP1685103A1 3-AMINOPYRROLIDONE DERIVATIVES 有权
标题翻译： 3 AMINOPYRROLIDONDERIVATE
公开(公告)号：EP1685103A1
公开(公告)日：2006-08-02
申请号：EP04819593.7
申请日：2004-11-16
申请人： Newron Pharmaceuticals S.p.A.
发明人： THALER, Florian , SABIDO DAVID, Cibele, Maria , MAESTRONI, Sara , RAVEGLIA, Luca, Francesco , SALVATI, Patricia
IPC分类号： C07D207/273 , C07D211/76 , C07D223/12 , A61K31/4412 , A61K31/4015 , A61K31/55
CPC分类号： C07D207/273 , A61K31/4015 , A61K31/4412 , A61K31/55 , C07D211/76
摘要： This invention is related to compounds and use of 3-aminopyrrolidone derivatives and analogues of the following general formula (I), wherein m is an integer from 1 to 3; X is methylene, oxygen, sulphur or a NR6 group; R1 is a straight or branched C1-C8 alkyl or C3-C8 alkenylene or C3-C8 alkynylene chain, optionally substituted with CF3, phenyl, phenoxy or naphthyl, or phenyl the aromatic rings optionally substituted by one or more C1-C4 alkyl, halogens, trifluoromethyl, hydroxy or C1-C4 alkoxy groups; R2, R3 are independently hydrogen, a C1-C3 alkyl chain, halogen, trifluoromethyl, hydroxy or C1-C4 alkoxy groups; R4, R5, R6 are independently hydrogen or C1-C6 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 cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.

53. 发明授权

EP1423168B1 PHARMACEUTICAL COMPOSITION COMPRISING GABAPENTIN OR AN ANALOGUE THEREOF AND AN ALPHA-AMINOAMIDE AND ITS ANALGESIC USE 有权
标题翻译：加巴喷丁或其类似物和阿尔法氨基酰胺类镇痛使用该组合物的药物组合物
公开(公告)号：EP1423168B1
公开(公告)日：2006-02-08
申请号：EP02797573.9
申请日：2002-08-09
申请人： Newron Pharmaceuticals S.p.A.
发明人： SALVATI, Patricia , VENERONI, Orietta , MAJ, Roberto , FARIELLO, Ruggero , BENATTI, Luca
IPC分类号： A61P29/00 , A61P25/08 , A61K31/445 , A61K31/195 , A61K31/165
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.

54. 发明公开

EP1423168A2 PHARMACEUTICAL COMPOSITION COMPRISING GABAPENTIN OR AN ANALOGUE THEREOF AND AN $G(A)-AMINOAMIDE AND ITS ANALGESIC USE 有权
标题翻译：加巴喷丁或其类似物和阿尔法氨基酰胺类镇痛使用该组合物的药物组合物
公开(公告)号：EP1423168A2
公开(公告)日：2004-06-02
申请号：EP02797573.9
申请日：2002-08-09
申请人： Newron Pharmaceuticals S.p.A.
发明人： SALVATI, Patricia , VENERONI, Orietta , MAJ, Roberto , FARIELLO, Ruggero , BENATTI, Luca
IPC分类号： A61P29/00 , A61P25/08 , A61K31/445 , A61K31/195 , A61K31/165
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.

55. 发明授权

EP0842152B1 N-(4-SUBSTITUTED-BENZYL)-2-AMINOLACTAM DERIVATIVES 有权转让
标题翻译： N-（4-取代的苯基）-2-氨基己内酰胺衍生物
公开(公告)号：EP0842152B1
公开(公告)日：2001-01-31
申请号：EP96925667.6
申请日：1996-07-05
申请人： Newron Pharmaceuticals S.p.A.
发明人： PEVARELLO, Paolo , AMICI, Raffaella , VARASI, Mario , MAJ, Roberto , SALVATI, Patricia
IPC分类号： C07D211/74 , A61K31/395 , C07D205/085 , C07D223/12 , C07D207/273 , A61K31/445 , A61K31/40
CPC分类号： C07D207/273 , C07D205/085 , C07D211/76

56. 发明公开

EP1045830A1 ALPHA-AMINOAMIDE DERIVATIVES USEFUL AS ANALGESIC AGENTS 有权
标题翻译：用作镇痛药的α-氨基酰胺衍生物
公开(公告)号：EP1045830A1
公开(公告)日：2000-10-25
申请号：EP98966617.7
申请日：1998-12-12
申请人： Newron Pharmaceuticals S.p.A.
发明人： PEVARELLO, Paolo , VARASI, Mario , SALVATI, Patricia , POST, Claes
IPC分类号： C07C255/54 , A61K31/165
CPC分类号： C07C237/06 , A61K31/165 , C07C255/54
摘要： The use, in the manufacture of a medicament for use as an analgesic, of a compound which is an alpha-aminoamide of formula (I) wherein: A is a -(CH2)m-, -(CH2)n-X- or -(CH2)v-O- group wherein m is an integer of 1 to 4, n is zero or an integer of 1 to 4, X is -S- or -NH-, and v is zero or an integer of 1 to 5; s is 1 or 2; R is a furyl, thienyl, or pyridyl ring of a phenyl ring; R1 is hydrogen or C1-C4 alkyl; one of R2 and R3 is hydrogen and the other is hydrogen or C1-C4 alkyl optionally substituted by hydroxy or phenyl; or R2 and R3 taken together with the carbon atom to which they are linked form a C3-C6 cycloalkyl ring; or R2 and R3 are both methyl; R4 is hydrogen or C1-C4 alkyl ring; or a pharmaceutically acceptable salt thereof.
摘要翻译：（Ⅰ）的α-氨基酰胺化合物在制备用作镇痛剂的药物中的用途，其中：A是 - （CH 2）m - ， - （CH 2）n X - 或 - （ CH2）vO-基团，其中m是1至4的整数，n是0或1至4的整数，X是-S-或-NH-，并且v是0或1至5的整数; s是1或2; R为苯环的呋喃基，噻吩基或吡啶基环; R1是氢或C1-C4烷基; R2和R3之一是氢，另一个是氢或任选被羟基或苯基取代的C1-C4烷基; 或者R 2和R 3与它们连接的碳原子一起形成C 3 -C 6环烷基环; 或者R2和R3都是甲基; R4是氢或C1-C4烷基环; 或其药学上可接受的盐。

57. 发明授权

EP3257842B1 THERAPEUTIC USE OF 2-[4-(3- OR 2-FLUOROBENZYLOXY)BENZYLAMINO]PROPANAMIDES WITH HIGH PURITY DEGREE 无效转让
公开(公告)号：EP3257842B1
公开(公告)日：2020-11-18
申请号：EP17181175.5
申请日：2008-12-01
申请人： Newron Pharmaceuticals S.p.A.
发明人： BARBANTI, Elena , FARAVELLI, Laura , SALVATI, Patricia , CANEVOTTI, Renato , PONZINI, Francesco
IPC分类号： A61K31/165 , A61K31/197 , A61K31/198 , A61K45/06 , A61P25/00 , A61P1/00

58. 发明公开

EP3257842A1 PROCESS FOR THE PRODUCTION OF 2-[4-(3- OR 2-FLUOROBENZYLOXY)BENZYLAMINO]PROPANAMIDES WITH HIGH PURITY DEGREE 无效转让
标题翻译：生产高纯度2- [4-（3-或2-氟苯氧基）苄基氨基]丙酰胺的方法
公开(公告)号：EP3257842A1
公开(公告)日：2017-12-20
申请号：EP17181175.5
申请日：2008-12-01
申请人： Newron Pharmaceuticals S.p.A.
发明人： BARBANTI, Elena , FARAVELLI, Laura , SALVATI, Patricia , CANEVOTTI, Renato , PONZINI, Francesco
IPC分类号： C07C251/24 , A61K31/165 , A61P25/00 , A61K31/197 , A61K31/198 , A61K45/06
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 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：一种获得具有高纯度的治疗活性的2- [4-（3-和2-（氟苄氧基）苄基氨基]丙酰胺及其与可药用酸形成的盐的方法，特别是二苄基衍生物杂质含量低于0.03％通过使席夫碱中间体2- [4-（3-和2-氟苄氧基）亚苄基氨基]丙酰胺与选自硼氢化钠和钾的还原剂进行还原反应来进行该方法硼氢化物在合适量的选自C 1 -C 5低级链烷醇的有机溶剂中反应，允许在希夫碱在希夫碱的饱和溶液的悬浮液的还原反应过程的实质位置形成和存在于相同的有机溶剂。

59. 发明授权

EP2029524B1 PROCESS FOR THE PRODUCTION OF 2- [4 - ( 3- AND 2-FLUOROBENZYLOXY) BENZYLAMINO] PROPAN AMIDES 有权
标题翻译：用于生产2- [4 - （3-和2-氟苄氧基）苄基氨基] PROPANAMIDEN
公开(公告)号：EP2029524B1
公开(公告)日：2014-11-26
申请号：EP07764601.6
申请日：2007-06-08
申请人： Newron Pharmaceuticals S.p.A.
发明人： BARBANTI, Elena , CACCIA, Carla , SALVATI, Patricia , VELARDI, Francesco , RUFFILLI, Tiziano , BOGOGNA, Luigi
IPC分类号： C07C231/12 , C07C231/18
CPC分类号： C07C231/12 , C07C231/18 , C07C237/06

60. 发明公开

EP2222290A1 ALPHA-AMINOAMIDE DERIVATIVES USEFUL IN THE TREATMENT OF PSYCHIATRIC DISORDERS 有权转让
标题翻译： ALPHA-氨基酸衍生物ZER BEHANDLUNG PSYCHIATRISCHER ERKRANKUNGEN
公开(公告)号：EP2222290A1
公开(公告)日：2010-09-01
申请号：EP08864461.2
申请日：2008-12-05
申请人： Newron Pharmaceuticals S.p.A.
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：本公开涉及精神障碍和/或焦虑症的精神障碍的药物疗法，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。

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