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    HETEROCYCLE-SUBSTITUTED 3-ALKYL AZETIDINE DERIVATIVES
    5.
    发明申请
    HETEROCYCLE-SUBSTITUTED 3-ALKYL AZETIDINE DERIVATIVES 审中-公开
    杂交取代的3-烷基亚氨基衍生物

    公开(公告)号：WO2007062193A1

    公开(公告)日：2007-05-31

    申请号：PCT/US2006/045328

    申请日：2006-11-22

    申请人： MERCK & CO., INC. ,  BAKER, Robert, K. ,  HALE, Jeffrey, J. ,  MIAO, Shouwu ,  RUPPRECHT, Kathleen, M.

    发明人： BAKER, Robert, K. ,  HALE, Jeffrey, J. ,  MIAO, Shouwu ,  RUPPRECHT, Kathleen, M.

    IPC分类号： C07D403/10 ,  C07D413/10 ,  A61K31/41 ,  A61K31/4245 ,  A61P3/04 ,  A61P25/30

    CPC分类号： C07D413/10 ,  C07D403/10

    摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CBl) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CBl receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro- inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

    摘要翻译： 结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。 本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，阿尔茨海默病，偏头痛，神经病，包括多发性硬化症和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症的中枢作用药物 脑血管意外，头部创伤，焦虑障碍，压力，癫痫，帕金森病，运动障碍和精神分裂症。 这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

    SELECTIVE S1P1/EDG1 RECEPTOR AGONISTS
    9.
    发明申请
    SELECTIVE S1P1/EDG1 RECEPTOR AGONISTS 审中-公开
    选择性S1P1 / EDG1受体激动剂

    公开(公告)号：WO2003061567A2

    公开(公告)日：2003-07-31

    申请号：PCT/US2003/001120

    申请日：2003-01-14

    申请人： MERCK & CO., INC. ,  DOHERTY, George, A. ,  FORREST, Michael, J. ,  HAJDU, Richard ,  HALE, Jeffrey, J. ,  LI, Zhen ,  MANDALA, Suzanne, M. ,  MILLS, Sander, G. ,  ROSEN, Hugh ,  SCOLNICK, Edward, M.

    发明人： DOHERTY, George, A. ,  FORREST, Michael, J. ,  HAJDU, Richard ,  HALE, Jeffrey, J. ,  LI, Zhen ,  MANDALA, Suzanne, M. ,  MILLS, Sander, G. ,  ROSEN, Hugh ,  SCOLNICK, Edward, M.

    IPC分类号： A61K

    CPC分类号： A61K31/66 ,  A61K31/00 ,  G01N33/566 ,  G01N2500/04

    摘要： The present invention encompasses a method of treating an immunoregulatory abnormality in a mammalian patient in need of such treatment comprising administering to said patient a compound which is an agonist of the S1P1/Edg1 receptor in an amount effective for treating said immunoregulatory abnormality, wherein said compound possesses a selectivity for the S1P1/Edg1 receptor over the S1PR3/Edg3 receptor, said compound administered in an amount effective for treating said immunoregulatory abnormality. Pharmaceutical compositions are included. The invention also encompasses a method of identifying candidate compounds that are agonists of the S1P1/Edg1 receptor and which possesses a selectivity for the S1P1/Edg1 receptor over the S1PR3/Edg3 receptor. The invention further encompasses a method of treating a respiratory disease or condition in a mammalian patient in need of such treatment comprising administering to said patient a compound which is an agonist of the S1P1/Edg1 receptor in an amount effective for treating said respiratory disease or condition, wherein said compound possesses a selectivity for the S1P1/Edg1 receptor over the S1PR3/Edg3 receptor.

    摘要翻译： 本发明包括在需要这种治疗的哺乳动物患者中治疗免疫调节异常的方法，包括以有效治疗所述免疫调节异常的量向所述患者施用作为S1P1 / Edg1受体激动剂的化合物，其中所述化合物 对S1P1 / Edg1受体具有S1PR3 / Edg1受体的选择性，所述化合物以有效治疗所述免疫调节异常的量给药。 包括药物组合物。 本发明还包括鉴定作为S1P1 / Edg1受体的激动剂的候选化合物的方法，并且其具有S1P1 / Edg1受体超过S1PR3 / Edg3受体的选择性。 本发明还包括治疗需要这种治疗的哺乳动物患者的呼吸系统疾病或病症的方法，包括向所述患者施用有效治疗所述呼吸系统疾病或病症的S1P1 / Edg1受体激动剂的化合物 其中所述化合物对S1P1 / Edg1受体具有超过S1PR3 / Edg3受体的选择性。