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    PROCESS FOR THE PRODUCTION OF 2-Ý4-(3- OR 2-FLUOROBENZYLOXY)BENZYLAMINO¨PROPANAMIDES WITH HIGH PURITY DEGREE
    1.
    发明公开
    PROCESS FOR THE PRODUCTION OF 2-Ý4-(3- OR 2-FLUOROBENZYLOXY)BENZYLAMINO¨PROPANAMIDES WITH HIGH PURITY DEGREE 有权
    PROCESS FOR制备2- [4-（3-或2-氟苄氧基）苄基氨基] PROPANAMIDEN高纯度

    公开(公告)号：EP2229351A1

    公开(公告)日：2010-09-22

    申请号：EP08860373.3

    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： 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-(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： 一种用于与具有高纯度，即，与二苄基衍生物杂质的含量低于0.03％，以获得治疗活性2- [4-（3-和2-（氟苄氧基）苄基氨基] -propanamides和与药学上可接受的酸及其盐的过程 （重量）。该方法通过提交船基中间体与还原剂的还原反应在有机溶剂中的量，以允许悬浮液的船舶上的（还原反应的相当大的部分中和存在下）形成开展 基地。

    N-ACYL-N -BENZYL-ALKYLENDIAMINO DERIVATIVES
    5.
    发明授权
    N-ACYL-N -BENZYL-ALKYLENDIAMINO DERIVATIVES 有权
    N-酰基-N-苄基 - 烷基氨基酰胺衍生物

    公开(公告)号：EP1689708B1

    公开(公告)日：2007-06-27

    申请号：EP04803133.0

    申请日：2004-11-12

    申请人： Newron Pharmaceuticals S.p.A.

    发明人： THALER, Florian ,  SABIDO DAVID, Cibele, Maria ,  FARAVELLI, Laura ,  GAGLIARDI, Stefania c/o Nikem Research S.r.l ,  COLOMBO, Elena ,  SALVATI, Patricia

    IPC分类号： C07D207/267 ,  A61K31/165 ,  C07C233/36 ,  A61K31/4015

    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 C2-C8 alkyl chain; X is a methylene, oxygen, sulphur or a NR7 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, 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 are independently hydrogen or C1-C6 alkyl; R6 is a hydrogen or a straight or branched C1-C8 alkyl or linked to R5 can form a five to seven membered lactam; R7 is 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, 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： 本发明涉及下列通式（I）的N-酰基-N'-苄基 - 亚烷基二氨基衍生物的化合物和用途，其中A是直链或支链的C2-C8烷基链; X是亚甲基，氧，硫或NR7基团; R 1为任选被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亚炔基链，所述芳环任选被一个或多个C 1 -C 4烷基，卤素，三氟甲基 ，羟基或C 1 -C 4烷氧基; R2，R3独立地为氢，C1-C3烷基链，卤素，三氟甲基，羟基或C1-C4烷氧基; R4，R5独立地为氢或C1-C6烷基; R6是氢或直链或支链C1-C8烷基或与R5连接可形成5-7元内酰胺; R 7是氢或C 1 -C 6烷基; 及其药学上可接受的盐，其作为钠和/或钙通道调节剂是有活性的，因此可用于预防，缓解和治疗广泛范围的病状，包括但不限于神经学，精神病学，心血管疾病，炎症，眼科，泌尿科 ，代谢和胃肠疾病，其中上述机制已被描述为起病理作用。

    PROCESS FOR THE PRODUCTION OF 2-[4-(3- OR 2-FLUOROBENZYLOXY)BENZYLAMINO]PROPANAMIDES WITH HIGH PURITY DEGREE
    7.
    发明公开
    PROCESS FOR THE PRODUCTION OF 2-[4-(3- OR 2-FLUOROBENZYLOXY)BENZYLAMINO]PROPANAMIDES WITH HIGH PURITY DEGREE 审中-公开
    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。

    ALPHA-AMINOAMIDE DERIVATIVES USEFUL IN THE TREATMENT OF PSYCHIATRIC DISORDERS
    8.
    发明公开
    ALPHA-AMINOAMIDE DERIVATIVES USEFUL IN THE TREATMENT OF PSYCHIATRIC DISORDERS 审中-公开
    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。

    N-ACYL-N -BENZYL-ALKYLENDIAMINO DERIVATIVES
    9.
    发明公开
    N-ACYL-N -BENZYL-ALKYLENDIAMINO DERIVATIVES 有权
    N-酰基-N-苄基ALKYLENDIAMINODERIVATE

    公开(公告)号：EP1689708A1

    公开(公告)日：2006-08-16

    申请号：EP04803133.0

    申请日：2004-11-12

    申请人： Newron Pharmaceuticals S.p.A.

    发明人： THALER, Florian ,  SABIDO DAVID, Cibele, Maria ,  FARAVELLI, Laura ,  GAGLIARDI, Stefania c/o Nikem Research S.r.l ,  COLOMBO, Elena ,  SALVATI, Patricia

    IPC分类号： C07D207/267 ,  A61K31/165 ,  C07C233/36 ,  A61K31/4015

    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 C2-C8 alkyl chain; X is a methylene, oxygen, sulphur or a NR7 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, 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 are independently hydrogen or C1-C6 alkyl; R6 is a hydrogen or a straight or branched C1-C8 alkyl or linked to R5 can form a five to seven membered lactam; R7 is 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, neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.