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109 条记录 (耗时 0.028 秒)

    Salt forms of (2S)-(4E)-N-Methyl-5-[(5-Isopropoxy)pyridin-3-yl]-4-penten-2-amine
    86.
    发明公开
    Salt forms of (2S)-(4E)-N-Methyl-5-[(5-Isopropoxy)pyridin-3-yl]-4-penten-2-amine 审中-公开
    （2S） - （4E）-N-甲基-5 - [（5-异丙氧基）吡啶-3-基] -4-戊烯-2-氨基

    公开(公告)号：EP2357174A1

    公开(公告)日：2011-08-17

    申请号：EP11150475.9

    申请日：2007-05-08

    申请人： AstraZeneca AB ,  Targacept, Inc.

    发明人： Bohlin, Martin Hans ,  Dull, Gary M. ,  Eriksson, Caroline ,  Miller, Craig H. ,  Munoz, Julio A. ,  Sebhatu, Tesfai

    IPC分类号： C07D213/65 ,  A61K31/44 ,  A61P25/00

    CPC分类号： C07D213/65

    摘要： Phosphoric acid, edisylic acid (1,2-ethanedisulfonic acid), citric acid, orotic acid (uracil-6-carboxylic acid), R-mandelic acid, sulfuric acid, 1,5-naphthalenedisulfonic acid, D-aspartic acid, and lysine monohydrochloride salts of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine, and methods for their preparation, pharmaceutical compositions comprising said salts, and use, are disclosed. The salts can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders.

    摘要翻译： 磷酸，乙二酸（1,2-乙烷二磺酸），柠檬酸，乳清酸（尿嘧啶-6-羧酸），R-扁桃酸，硫酸，1,5-萘二磺酸，D-天冬氨酸和赖氨酸 （2S） - （4E）-N-甲基-5- [3-（5-异丙氧基吡啶）基] -4-戊烯-2-胺的单盐酸盐及其制备方法，包含所述盐的药物组合物和使用 ，被披露。 盐可以施用于易患或患有诸如中枢神经系统疾病的病症和障碍的患者，以治疗和/或预防这些疾病。

    HETEROARYL-SUBSTiTUTED DIAZATRICYCLOALKANES, METHODS FOR ITS PREPARATION AND USE THEREOF
    90.
    发明授权
    HETEROARYL-SUBSTiTUTED DIAZATRICYCLOALKANES, METHODS FOR ITS PREPARATION AND USE THEREOF 有权
    杂芳基DIAZATRICYCLOALKANE，方法及其及其应用

    公开(公告)号：EP1917265B1

    公开(公告)日：2010-09-29

    申请号：EP06813627.4

    申请日：2006-08-21

    申请人： Targacept, Inc.

    发明人： MAZUROV, Anatoly ,  MIAO, Lan ,  KLUCIK, Jozef

    IPC分类号： C07D471/18 ,  A61K31/439 ,  A61P25/00

    CPC分类号： C07D471/18 ,  C07D471/14

    摘要： The present invention relates to amide and urea derivatives of heteroaryl- substituted diazatricycloalkanes, of the Formula (I) with the definition as set out in the description pharmaceutical compositions including the compounds, methods of preparing the compounds, and methods of treatment using the compounds. More specifically, the methods of treatment involve modulating the activity of the α7 nAChR subtype by administering one or more of the compounds to treat or prevent disorders mediated by the α7 nAChR subtype. The diazatricycloalkanes typically consist of a 1-azabicyclooctane fused to pyrrolidine ring. The substituent heteroaryl groups are 5- or 6-membered ring heteroaromatics, such as 3-pyridinyl and 5-pyrimidinyl moieties, which are attached directly to the diazatricycloalkane. The secondary nitrogen of the pyrrolidine moiety is substituted with an arylcarbonyl (amide type derivative) or an arylaminocarbonyl (N- arylcarbamoyl) (urea type derivative) group. The compounds are beneficial in therapeutic applications requiring a selective interaction at certain nAChR subtypes. That is, the compounds modulate the activity of certain nAChR subtypes, particularly the α7 nAChR subtype, and do not have appreciable activity toward muscarinic receptors. Radiolabeled versions of the compounds can be used in diagnostic methods.