HIGH PURITY 2-[4-(3- OR 2-FLUOROBENZYLOXY)BENZYLAMINO] PROPANAMIDES AND METHODS OF USE THEREOF
    3.
    发明申请
    HIGH PURITY 2-[4-(3- OR 2-FLUOROBENZYLOXY)BENZYLAMINO] PROPANAMIDES AND METHODS OF USE THEREOF 有权
    高纯度2- [4-(3-或2-氟代苄基)苯甲酰胺]丙酰胺及其使用方法

    公开(公告)号:US20140051758A1

    公开(公告)日:2014-02-20

    申请号:US13961693

    申请日:2013-08-07

    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 C1-C5 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)苄基氨基]丙酰胺及其与具有高纯度的药学上可接受的酸的盐的方法,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%,该方法通过将希夫碱中间体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。

    USE OF (HALOBENZYLOXY) BENZYLAMINO-PROPANAMIDES FOR THE MANUFACTURE OF MEDICAMENTS ACTIVE AS SODIUM AND/OR CALCIUM CHANNEL SELECTIVE MODULATORS
    4.
    发明申请
    USE OF (HALOBENZYLOXY) BENZYLAMINO-PROPANAMIDES FOR THE MANUFACTURE OF MEDICAMENTS ACTIVE AS SODIUM AND/OR CALCIUM CHANNEL SELECTIVE MODULATORS 审中-公开
    (HALOBENZYLOXY)苯甲酰胺丙酰胺用于制备作为钠和/或钙通道选择性调节剂活性的药物的用途

    公开(公告)号:US20110184068A1

    公开(公告)日:2011-07-28

    申请号:US12939726

    申请日:2010-11-04

    IPC分类号: A61K31/167 A61P25/04

    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 as sodium 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.

    摘要翻译: 本发明涉及选择的(R)-2 - [(卤代苄氧基)苄基氨基] - 丙酰胺及其药学上可接受的盐在制备药物中的用途,其作为钠和/或钙通道调节剂选择性活性, 预防,缓解和治愈各种病症,包括疼痛,偏头痛,周围疾病,心血管疾病,影响所有身体系统的炎症过程,影响皮肤和相关组织的疾病,呼吸系统疾病,免疫和内分泌系统疾病 ,胃肠道,泌尿生殖,代谢和发作障碍,其中上述机制被描述为发挥病理作用。

    ALPHA-AMINOAMIDE DERIVATIVES USEFUL IN THE TREATMENT OF PSYCHIATRIC DISORDERS
    5.
    发明申请
    ALPHA-AMINOAMIDE DERIVATIVES USEFUL IN THE TREATMENT OF PSYCHIATRIC DISORDERS 有权
    用于治疗心理疾病的ALPHA-氨基腺苷衍生物

    公开(公告)号:US20110014304A1

    公开(公告)日:2011-01-20

    申请号:US12816143

    申请日:2010-06-15

    CPC分类号: A61K31/165

    摘要: The disclosure relates to pharmacotherapy of a psychiatric disorder which is schizophrenia and/or anxiety, wherein schizophrenia includes schizophrenia related disorders 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 disclosure 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治疗,其中精神分裂症包括精神分裂症相关的疾病,例如短暂性精神病,妄想障碍,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

    公开(公告)号:US07411091B2

    公开(公告)日:2008-08-12

    申请号:US10580367

    申请日:2004-11-12

    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