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    Non-peptide somatostatin receptor ligands
    3.
    发明授权
    Non-peptide somatostatin receptor ligands 失效
    非肽生长抑素受体配体

    公开(公告)号：US07189856B2

    公开(公告)日：2007-03-13

    申请号：US10289924

    申请日：2002-11-07

    申请人： Gideon Shapiro ,  Michael G. Natchus ,  Mark A. Lockwood ,  Simona Jurczyk

    发明人： Gideon Shapiro ,  Michael G. Natchus ,  Mark A. Lockwood ,  Simona Jurczyk

    IPC分类号： C07D27/104 ,  A61K31/41

    CPC分类号： C07D403/06

    摘要： Non-peptide somatostatin receptor ligands with conformationally restricted side chains exhibiting high binding affinity toward somatostatin receptors are provided. The compounds exhibit a high selectivity and act as agonists at human subtype 2 somatostatin receptors. The compounds are long acting for advantageous use as medicaments in peripheral diseases where somatostatinergic therapy is indicated. Furthermore, many of the compounds are lipophilic and are particularly useful for treating central nervous system and ophthalmic diseases where penetration of the blood brain and blood retinal barriers is required. It is a further object to describe the preferred stereoisomers of these somatostatin agonists and processes for their preparation. Further objects will become apparent from reading the following description.

    摘要翻译： 提供了具有对生长抑素受体具有高结合亲和力的构象限制性侧链的非肽生长抑素受体配体。 化合物表现出高选择性，并且作为人类2型生长抑素受体的激动剂。 化合物长效作为有益用途，作为指示生长抑素治疗的外周疾病中的药物。 此外，许多化合物是亲脂性的，并且特别可用于治疗中枢神经系统和需要渗透血脑屏障和血液视网膜屏障的眼科疾病。 另一个目的是描述这些生长抑素激动剂的优选立体异构体及其制备方法。 通过阅读以下描述，其他目的将变得显而易见。