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    • 9. 发明授权
    • Guanidino compounds
    • 胍基化合物
    • US06716840B2
    • 2004-04-06
    • US10118730
    • 2002-04-08
    • Daniel ChuRustum S. BoyceDavid DuhlBryan H. Chang
    • Daniel ChuRustum S. BoyceDavid DuhlBryan H. Chang
    • A61K315375
    • C07D209/46C07D209/48C07D217/24C07D235/08C07D235/10
    • 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.
    • 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。