N-pyridin-3-yl or N-pyrazin-2-yl carboxamides
    2.
    发明授权
    N-pyridin-3-yl or N-pyrazin-2-yl carboxamides 有权
    N-吡啶-3-基或N-吡嗪-2-基甲酰胺

    公开(公告)号:US08410107B2

    公开(公告)日:2013-04-02

    申请号:US13267920

    申请日:2011-10-07

    IPC分类号: A61K31/4965 A61K31/44

    摘要: The present invention relates to compounds of formula I, wherein A, R1 to R7 are defined in the description, and to pharmaceutically acceptable salts thereof. The present invention also relates to the manufacture of such compounds or their pharmaceutically acceptable salts, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.

    摘要翻译: 本发明涉及式I化合物及其药学上可接受的盐,其中A,R 1至R 7在说明书中定义。 本发明还涉及这种化合物或其药学上可接受的盐的制备,含有它们的药物组合物及其作为用于治疗和/或预防可用HDL-胆固醇升高药物治疗的疾病的药物的用途,所述疾病例如血脂异常, 动脉粥样硬化和心血管疾病。

    METHOD OF TREATMENT AND/OR PREVENTION OF BRAIN, SPINAL OR NERVE INJURY
    7.
    发明申请
    METHOD OF TREATMENT AND/OR PREVENTION OF BRAIN, SPINAL OR NERVE INJURY 审中-公开
    治疗和/或预防脑,脊髓或神经损伤的方法

    公开(公告)号:US20110053954A1

    公开(公告)日:2011-03-03

    申请号:US12886691

    申请日:2010-09-21

    IPC分类号: A61K31/496 A61P25/00

    CPC分类号: A61K31/435

    摘要: The invention relates to a method of treatment and/or prevention of brain, spinal or nerve injury comprising administration to a person in need of such treatment, of a therapeutically effective amount of an NK-1 receptor antagonist compound of the formula wherein the meanings of R, R1, R2, R2′, R3, and R4 are explained in the specification and the pharmaceutically acceptable acid addition salts and the prodrugs thereof either alone or in combination with a magnesium salt. Exemplified is the use of N-(3,5-bis-trifluoromethyl-benzyl)-N-methyl-6-(4-methyl-piperazin-1-yl)-4-o-tolyl-nicotinamide. The invention also relates to pharmaceutical composition comprising one or more such NK-1 receptor antagonists, optionally in combination with a magnesium salt, and a pharmaceutically acceptable excipient for the treatment and/or prevention of brain, spinal or nerve injury.

    摘要翻译: 本发明涉及一种治疗和/或预防脑,脊髓或神经损伤的方法,包括向需要这种治疗的人施用治疗有效量的下式的NK-1受体拮抗剂化合物,其中, 说明书和其药学上可接受的酸加成盐及其前药单独或与镁盐组合说明了R,R 1,R 2,R 2',R 3和R 4。 举例说明了使用N-(3,5-双 - 三氟甲基 - 苄基)-N-甲基-6-(4-甲基 - 哌嗪-1-基)-4-邻甲苯基 - 烟酰胺。 本发明还涉及包含一种或多种这样的NK-1受体拮抗剂,任选与镁盐组合的药物组合物和用于治疗和/或预防脑,脊髓或神经损伤的药学上可接受的赋形剂。