Guanidino compounds
    4.
    发明授权
    Guanidino compounds 失效
    胍基化合物

    公开(公告)号:US06716840B2

    公开(公告)日:2004-04-06

    申请号:US10118730

    申请日:2002-04-08

    IPC分类号: A61K315375

    摘要: Compounds having the general structure I are provided: X and Y are independently selected from the group consisting of CH2, N, NR9, C═O, C═S, S═O, SO2, S, O, (CR6R7)n, C(═O)—(CR6R7)n, and C(═S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of and L is selected from the group consisting of N, O, S, S═O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r”) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.

    摘要翻译: 提供具有通式结构I的化合物:X和Y独立地选自CH 2,N,NR 9,C = O,C = S,S = O,SO 2,S,O, (R 6 R 7)n,C(= O) - (CR 6 R 7)n和C(= S) - (CR 6 R 7)n,其中n为1 W选自N,O,S,S = O,SO 2,C(O),NC(O),NC(S),OC (O),OC(S),C(NR 10),C(NOR 10))和共价键。 Z 1,Z 2和Z 3独立地选自取代的碳和氮。 式I化合物是黑皮质素-4受体(“MC-4r”)的激动剂,因此可能具有控制人类MC-4r作用相关疾病如肥胖和II型糖尿病的有用性质。

    Therapeutic Macrolide Compounds and Their Use
    10.
    发明申请
    Therapeutic Macrolide Compounds and Their Use 审中-公开
    治疗性大环内酯类化合物及其用途

    公开(公告)号:US20110237566A1

    公开(公告)日:2011-09-29

    申请号:US13130144

    申请日:2009-11-24

    摘要: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain macrolide compounds (for convenience, collectively referred to herein as “MC compounds”), which, inter alia, are useful in treatment of cancer. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to treat proliferative conditions such as cancer, and in the treatment of diseases and conditions that are mediated by the regulation (e.g. inhibition) of cell proliferation, optionally in combination with another agent.

    摘要翻译: 本发明一般涉及治疗化合物的领域,更具体地涉及某些大环内酯类化合物(为方便起见,本文统称为“MC化合物”),其尤其可用于治疗癌症。 本发明还涉及包含这些化合物的药物组合物,以及这些化合物和组合物在体外和体内的用途,以治疗增殖性疾病如癌症,以及治疗由调节介导的疾病和病症 (例如抑制)细胞增殖,任选与另一种试剂组合。