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17 条记录 (耗时 0.046 秒)

    4-imidazolyl substituted pyrimidine derivatives with CDK inhibitory activity
    5.
    发明授权
    4-imidazolyl substituted pyrimidine derivatives with CDK inhibitory activity 失效
    具有CDK抑制活性的4-咪唑基取代的嘧啶衍生物

    公开(公告)号：US07442697B2

    公开(公告)日：2008-10-28

    申请号：US10507169

    申请日：2003-03-06

    申请人： Nicholas John Newcombe ,  Andrew Peter Thomas

    发明人： Nicholas John Newcombe ,  Andrew Peter Thomas

    IPC分类号： C07D403/04 ,  A61K31/505

    CPC分类号： C07D403/04 ,  C07D405/14

    摘要： Compounds of the formula (I): wherein R1, R2, R3, R4, R5 and p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man.

    摘要翻译： 式（I）化合物：其中R 1，R 2，R 3，R 4，R 4，R p和p如上所定义，并且描述了药学上可接受的盐和体内可水解的酯。 还描述了它们的制备方法及其作为药物的用途，特别是用于在温血动物如人中产生细胞周期抑制（抗细胞增殖）作用的药物。

    Pyrimidine compounds
    8.
    发明授权
    Pyrimidine compounds 失效
    嘧啶化合物

    公开(公告)号：US07446105B2

    公开(公告)日：2008-11-04

    申请号：US10507163

    申请日：2003-03-06

    申请人： Nicholas John Newcombe ,  Andrew Peter Thomas

    发明人： Nicholas John Newcombe ,  Andrew Peter Thomas

    IPC分类号： C07D403/04 ,  A61K31/506

    CPC分类号： C07D403/04

    摘要： Compounds of the formula (I) wherein R1, R2, R3, R4, R5, R6 and p are as defined within and pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man.

    摘要翻译： 其中R 1，R 2，R 3，R 4，R 4，R 4，R 4， 其中，R 6和R 6定义如上，其中药学上可接受的盐和体内可水解的酯被描述。 还描述了它们的制备方法及其作为药物的用途，特别是用于在温血动物如人中产生细胞周期抑制（抗细胞增殖）作用的药物。

    Pyridyl-and pyrimidyl-heterocyclic compounds inhibiting oxido squalene-cyclase
    10.
    发明授权
    Pyridyl-and pyrimidyl-heterocyclic compounds inhibiting oxido squalene-cyclase 失效
    抑制氧化角鲨烯环化酶的吡啶基和嘧啶基杂环化合物

    公开(公告)号：US06335341B1

    公开(公告)日：2002-01-01

    申请号：US09463326

    申请日：2000-01-24

    申请人： Michael Clyde Johnson ,  Nicholas John Newcombe

    发明人： Michael Clyde Johnson ,  Nicholas John Newcombe

    IPC分类号： C07D40106

    CPC分类号： C07D401/04 ,  C07D401/12 ,  C07D401/14

    摘要： This invention concerns heterocyclic derivatives which are useful in inhibiting oxido-squalene cyclase, processes for their preparation and pharmaceutical compositions containing them. The present invention is also concerned with heterocyclic derivatives capable of inhibiting cholesterol biosynthesis and hence in lowering cholesterol levels in blood plasma. The present invention also relates to methods of using such heterocyclic derivatives in treating or preventing diseases and medical conditions such as hypercholesterolemia, atherosclerosis and other medical conditions associated with elevated cholesterol levels. In formula (I): G is selected from CH or N; R1 is selected from hydrogen, halogeno, (1-6C)alkyl, halogeno(1-6C)alkyl, cyano, nitro, (1-6C)alkoxycarbonyl, and NR3R4 wherein R3 and R4 are independently selected from hydrogen and (1-6C)alkyl, and wherein up to 3 R1 groups may be present; T1 is selected from CH or N; T2 and T2 are independently selected from N and CR, wherein R is selected from hydrogen, hydroxyl and (C1-4)alkyl and wherein either ring containing T2 or T3 is optionally substituted with an oxo group; R2 is selected from hydrogen or (1-4C)alkyl; Q is selected from SO2, CO and CH2; AR is selected from a five or six-membered heterocycle containing up to 3 heteroatoms selected from nitrogen, oxygen and sulphur, phenyl, phenyl (2-6)alkenyl and naphthyl in which any Ar group is optionally substituted by one or more substituents selected from (1-6C)alkyl, halogeno, halogeno (1-6C)alkyl, (1-6C)alkoxy, (1-6C)alkoxycarbonyl, cyano, (1-6C)alkylamido, nitro, NR3R4 wherein R3 and R4 are independently selected from hydrogen and (1-4C)alkyl; provided that both T2 and T3 are not N and that when T2 is CR then T1 is not CH.

    摘要翻译： 本发明涉及可用于抑制氧化 - 角鲨烯环化酶，其制备方法和含有它们的药物组合物的杂环衍生物。 本发明还涉及能够抑制胆固醇生物合成并因此降低血浆中胆固醇水平的杂环衍生物。 本发明还涉及使用这种杂环衍生物治疗或预防疾病和医学病症如高胆固醇血症，动脉粥样硬化和与升高的胆固醇水平相关的其它医学病症的方法。 在式（I）中：G选自CH或N; R 1选自氢，卤代，（1-6C）烷基，卤代（1-6C）烷基，氰基，硝基，（1-6C）烷氧基羰基和NR 3 R 4，其中R 3和R 4独立地选自氢和（1-6C ）烷基，并且其中可以存在多达3个R 1基团; T1选自CH或N; T2和T2独立地选自N和CR，其中R选自氢，羟基和（C 1-4）烷基，并且其中任何含有T 2或T 3的环任选被氧代基取代; R2选自氢或（1-4C）烷基; Q选自SO2，CO和CH2; AR选自含有至多3个选自氮，氧和硫的杂原子的五元或六元杂环，苯基，苯基（2-6）烯基和萘基，其中任何Ar基团任选被一个或多个选自以下的取代基取代： （1-6C）烷基，卤代，卤代（1-6C）烷基，（1-6C）烷氧基，（1-6C）烷氧基羰基，氰基，（1-6C）烷基酰氨基，硝基，NR3R4，其中R3和R4独立选择 由氢和（1-4C）烷基取代; 条件是T2和T3都不是N，当T2是CR时，T1不是CH。