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    Piperidinyl alkyne orexin receptor antagonists
    5.
    发明授权
    Piperidinyl alkyne orexin receptor antagonists 有权
    哌啶基炔炔食欲素受体拮抗剂

    公开(公告)号：US08940898B2

    公开(公告)日：2015-01-27

    申请号：US14354454

    申请日：2012-10-19

    申请人： Scott D. Kuduk ,  Jason W. Skudlarek

    发明人： Scott D. Kuduk ,  Jason W. Skudlarek

    IPC分类号： C07D211/68 ,  A61K31/47 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D417/06 ,  C07D417/14

    CPC分类号： C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D417/06 ,  C07D417/14

    摘要： The present invention is directed to piperidinyl alkyne compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the piperidinyl alkyne compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

    摘要翻译： 本发明涉及作为食欲素受体拮抗剂的哌啶基炔化合物。 本发明还涉及本文所述的哌啶基炔化合物在治疗或预防涉及食欲素受体的神经和精神病症和疾病中的用途。 本发明还涉及包含这些化合物的药物组合物。 本发明还涉及这些药物组合物在预防或治疗涉及食欲素受体的疾病中的用途。

    Nitrogenous heterocyclic derivative and medicine containing the same as an active ingredient
    10.
    发明授权
    Nitrogenous heterocyclic derivative and medicine containing the same as an active ingredient 失效
    含氮杂环衍生物和含有与活性成分相同的药物

    公开(公告)号：US08410276B2

    公开(公告)日：2013-04-02

    申请号：US13016849

    申请日：2011-01-28

    申请人： Yoshikazu Takaoka ,  Shiro Shibayama ,  Rena Nishizawa

    发明人： Yoshikazu Takaoka ,  Shiro Shibayama ,  Rena Nishizawa

    IPC分类号： C07D211/68 ,  A61K31/445

    CPC分类号： C07D413/12 ,  A61K31/00 ,  C07D211/58 ,  C07D231/12 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14

    摘要： A compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof: (wherein each symbol is as defined in the description.) The compounds represented by formula (I) has the antagonistic activity against CCR5, so they are useful in preventing and/or treating CCR5-related diseases, for example, various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, inflammatory bowel disease such as ulcerative colitis, etc.), immunological diseases (autoimmune diseases, rejection in organ transplantation (rejection of graft of solid organ, rejection of graft of pancreatic islet cells in therapy for diabetes, graft-versus-host disease, etc.), immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (infection with human immunodeficiency virus, acquired immunodeficiency syndrome, infection with RSV, etc.), allergic diseases (atopic dermatitis, urticaria, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis, etc.), cardiovascular diseases (arteriosclerosis, ischemic reperfusion injury, etc.), acute respiratory distress syndrome, shock accompanying bacterial infection, diabetes, cancer metastasis and so on.

    摘要翻译： 由式（I）表示的化合物，其盐，其N-氧化物，其溶剂合物或其前药：（其中各符号如说明书中所定义）。式（I）表示的化合物具有拮抗作用 因此它们可用于预防和/或治疗CCR5相关疾病，例如各种炎性疾病（哮喘，肾炎，肾病，肝炎，关节炎，类风湿关节炎，鼻炎，结膜炎，炎性肠病如溃疡性结肠炎） 等等），免疫疾病（自身免疫性疾病，器官移植排斥反应（实体器官移植排斥反应，胰岛细胞移植对糖尿病的治疗排斥反应，移植物抗宿主病等），免疫抑制，牛皮癣， 多发性硬化症等），感染性疾病（人类免疫缺陷病毒感染，获得性免疫缺陷综合征，RSV感染等），过敏性疾病（特应性皮炎，荨麻疹，过敏性 急性呼吸窘迫综合征，伴随细菌感染的休克，糖尿病，癌症转移等），心血管疾病（动脉硬化，缺血再灌注损伤等）。