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    • 10. 发明申请
    • PYRIDO[4,3-b]INDOLE AND PYRIDO[3,4-b]INDOLE DERIVATIVES AND METHODS OF USE
    • 吡咯并[4,3-b]吲哚和吡咯并[3,4-b]吲哚衍生物及其使用方法
    • US20140206711A1
    • 2014-07-24
    • US14000179
    • 2012-02-17
    • Sarvajit ChakravartyBarry Patrick HartRajendra Parasmal Jain
    • Sarvajit ChakravartyBarry Patrick HartRajendra Parasmal Jain
    • C07D471/04
    • A61K31/437A61K31/4709A61K31/4745A61K31/55A61K45/06C07D471/04A61K2300/00
    • This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. The compounds may bind to and antagonize receptor α2B, α1B or α2A. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption, or to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. The compounds may also be used to treat diseases or conditions that are expected to be responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular, renal disorders or type 2 diabetes is particularly described.
    • 本公开涉及吡啶并[4,3-b]吲哚和吡啶并[3,4-b]吲哚衍生物。 还提供了包含化合物的药物组合物,以及在多种治疗应用中使用化合物的方法,包括治疗认知障碍,精神病性障碍,神经递质介导的病症和/或神经元病症。 该化合物可以结合并拮抗受体α2B,α1B或α2A。 这些化合物可用于治疗,例如(i)降低血压和/或(ii)促进肾血流量和/或(iii)降低或抑制钠再吸收,或调节血糖水平,增加胰岛素分泌和 治疗或预期对胰岛素生产增加有反应的疾病或病症。 所述化合物也可用于治疗预期对血压降低有反应的疾病或病症。 具体描述了使用该化合物治疗心血管,肾脏疾病或2型糖尿病。