利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

23 条记录 (耗时 0.023 秒)

    Benzamide derivatives as thrombin inhibitors
    3.
    发明授权
    Benzamide derivatives as thrombin inhibitors 失效
    苯甲酰胺衍生物作为凝血酶抑制剂

    公开(公告)号：US06670381B2

    公开(公告)日：2003-12-30

    申请号：US10044769

    申请日：2002-01-10

    申请人： Henry Anderson Kelly ,  Martin Pass ,  David Neil Smith

    发明人： Henry Anderson Kelly ,  Martin Pass ,  David Neil Smith

    IPC分类号： C07D21374

    CPC分类号： C07D213/74

    摘要： There are provided according to the invention novel compounds of formula (I) wherein R1 represents C1-4alkyl or C3-8cycloalkyl, R2 represents C1-4alkyl or C3-4alkenyl, R3 represents hydrogen, C1-3alkyl or halogen, and R4 represents C1-6alkyl, processes for preparing them, pharmaceutical formulations containing them and their use in therapy particularly as thrombin inhibitors.

    摘要翻译： 根据本发明提供新的式（I）化合物，其中R 1表示C 1-4烷基或C 3-8环烷基，R 2表示C 1-4烷基或C 3-4烯基，R 3表示氢，C1- 3烷基或卤素，R 4表示C 1-6烷基，其制备方法，含有它们的药物制剂及其在治疗中的用途，特别是作为凝血酶抑制剂。

    2,4,6-trisubstituted pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer
    4.
    发明授权
    2,4,6-trisubstituted pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer 失效
    2,4,6-三取代嘧啶作为磷脂酰肌醇（PI）3-激酶抑制剂及其在治疗癌症中的应用

    公开(公告)号：US07893063B2

    公开(公告)日：2011-02-22

    申请号：US11630881

    申请日：2005-07-07

    申请人： Martin Pass

    发明人： Martin Pass

    IPC分类号： C07D413/14 ,  A61K31/5377

    CPC分类号： C07D239/42 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04

    摘要： The invention concerns pyrimidine derivatives of Formula (I) wherein each of Qa, G1, G2, q, R3, r, R4, X1 and Qb have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the production of an anti-proliferative effect in a warm-blooded animal such as man.

    摘要翻译： 本发明涉及式（I）的嘧啶衍生物，其中Qa，G1，G2，q，R3，r，R4，X1和Qb中的每一个具有本说明书中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于在温血动物如人中产生抗增殖作用的药物中的用途。

    PYRIMIDINE DERIVATIVES
    7.
    发明申请
    PYRIMIDINE DERIVATIVES 审中-公开

    公开(公告)号：US20100267755A1

    公开(公告)日：2010-10-21

    申请号：US10477546

    申请日：2002-05-23

    申请人： Gianpaolo Bravi ,  Malcolm Clive Carter ,  Richard Howard Green ,  Jennifer Margaret Doughty ,  Charles David Hartley ,  Alan Naylor ,  Martin Pass ,  Jeremy John Payne ,  Neil Anthony Pegg

    发明人： Gianpaolo Bravi ,  Malcolm Clive Carter ,  Richard Howard Green ,  Jennifer Margaret Doughty ,  Charles David Hartley ,  Alan Naylor ,  Martin Pass ,  Jeremy John Payne ,  Neil Anthony Pegg

    IPC分类号： A61K31/505 ,  A61P29/00 ,  C07D239/42 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  A61K31/506

    CPC分类号： C07D239/42 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

    摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable salts thereof, in which: R1 and R2 are independently selected from the group consisting of H, C1-6alkyl, C1-2alkyl substituted by one to five fluorine atoms, C3-6alkenyl, C3-6alkynyl, C3-10cycloalkylC0-6alkyl, C4-12bridged cycloalkyl, A(CR7R8)n and B(CR7R8)n; R3 is selected from the group consisting of C1-6alkyl, NH2 and R10CONH; R4 is C1-2alkyl substituted by one to five fluorine atoms; R5 is selected from the group consisting of H, C1-4alkyl, C1-2alkyl substituted with one to five fluorine atoms, halogen and C3-10cycloalkylC0-6alkyl, with the proviso that when R6 is H R5 is not H. R6 is selected from the group consisting of H, C1-4alkyl, C1-2alkyl substituted with one to five fluorine atoms, halogen, C1-4alkoxy, CN, NO2, C1-6alkylOCO, NH2CO, C1-6alkylNHCO, NH2, C1-6alkylNH, (C1-6alkyl)2N, (C1-6alkyl)2NCO, C1-6alkylCONH, NH2SO2, C1-6alkylNHSO2, (C1-6alkyl)2NSO2, C1-6alkylSO2NH, ArSO2NH, C1-6alkylSO2, ArSO2, C3-10cycloalkylC0-6alkyl, C3-6alkenyl and C3-6alkynyl, with the proviso that when R5 is H R6 is not H. R7 and R8 are independently selected from H or C1-6alkyl; A is an unsubstituted 5- or 6-membered heteroaryl or an unsubstituted 6-membered aryl, or a 5- or 6-membered heteroaryl or a 6-membered aryl substituted by one or more R9; R9 is selected from the group consisting of hydroxy, halogen, C1-6alkyl, C1-6alkyl substituted by one more fluorine atoms, C1-6alkoxy, C1-6alkoxy substituted by one or more F, NH2SO2 and C1-6alkylSO2; R10 is selected from the group consisting of H, C1-6alkyl, C1-6alkoxy, C1-6alkylOC1-6alkyl, phenyl, HO2CC1-6alkyl, C1-6alkylOCOC1-6alkyl, C1-6alkylOCO, H2NC1-6alkyl, C1-6alkylOCONHC1-6alkyl and C1-6alkylCONHC1-6alkyl; B is selected from the group consisting of defines the point of attachment of the ring; and n is 0 to 4. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of pain, fever and inflammation of a variety of conditions and diseases.