Guanidino compounds
    3.
    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。

    Guanidino compounds
    9.
    发明授权
    Guanidino compounds 失效
    胍基化合物

    公开(公告)号:US07456183B2

    公开(公告)日:2008-11-25

    申请号:US10474331

    申请日:2002-04-08

    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 (formula I) and L is selected from the group consisting of N, O, 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-4r2) 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: 提供具有一般结构I的化合物。 X和Y独立地选自CH 2,N,NR 9,CO,CS,SO,SO 2,S ,(O) - (CR 6),(O) - (CR 6) C(-S) - (CR 6 R 7)N ,和C(-S) - (CR 6) 其中n为1,2或3.W选自(式I),L选自N,O,SO,SO 2, C(O),NC(O),NC(S),OC(O),OC(S),C(NR 10) ,和共价键。 Z 1,Z 2,Z 3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-4r2”)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。

    Processes of synthesizing dihydropyridophthalazinone derivatives
    10.
    发明授权
    Processes of synthesizing dihydropyridophthalazinone derivatives 有权
    合成二氢吡啶并酞嗪酮衍生物的方法

    公开(公告)号:US08765945B2

    公开(公告)日:2014-07-01

    申请号:US13023140

    申请日:2011-02-08

    IPC分类号: C07D237/36

    摘要: Provided herein are processes for synthesizing dihydropyridophthalazinone derivatives, such as for example, 5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one and its stereoisomers, which are potent poly(ADP-ribose)polymerase (PARP) inhibitors as well as novel synthetic intermediate compounds.

    摘要翻译: 本文提供了合成二氢吡啶并二氮杂萘酮衍生物的方法,例如5-氟-8-(4-氟苯基)-9-(1-甲基-1H-1,2,4-三唑-5-基) 9-二氢-2H-吡啶并[4,3,2-de]酞嗪-3(7H) - 酮及其立体异构体,它们是有效的聚(ADP-核糖)聚合酶(PARP)抑制剂以及新的合成中间体化合物。