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292 条记录 (耗时 0.029 秒)

    PROCESS FOR PREPARING PYRIDOÝ2,3-D¨PYRIMIDIN-7-ONE AND 3,4-DIHYDROPYRIMIDOÝ4,5-D¨PYRIMIDIN-2(1H)-ONE DERIVATIVES
    82.
    发明公开
    PROCESS FOR PREPARING PYRIDOÝ2,3-D¨PYRIMIDIN-7-ONE AND 3,4-DIHYDROPYRIMIDOÝ4,5-D¨PYRIMIDIN-2(1H)-ONE DERIVATIVES 审中-公开
    METHOD FOR PRODUCING吡啶并| 2,3-D嘧啶-7-酮和3,4-二氢嘧啶| 4,5-D嘧啶-2（1H） - 酮衍生物

    公开(公告)号：EP1865959A2

    公开(公告)日：2007-12-19

    申请号：EP06739572.3

    申请日：2006-03-24

    申请人： GLAXO GROUP LIMITED

    发明人： CALLAHAN, James, Francis ,  BOEHM, Jeffrey ,  WAN, Zehong ,  YAN, Hongxing

    IPC分类号： A61K31/519 ,  C07D487/02

    CPC分类号： C07D487/04 ,  C07D471/04

    摘要： The present invention is directed to a novel method of preparing of 2,4,8- trisubstituted pyrido[2,3-d]pyrimidin-7-one pharmacophores of Formula (II) or (Ha) wherein GHs CH2 Or NH: G2 is CH or nitrogen; Rx is chloro, bromo, iodo, or O-S(O)2CF3; Rg is a C1 10 alkyl; m is 0, or an integer having a value of 1 , or 2; R3 is a C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted. which comprises reacting a compound of the formula: wherein Ry is chloro, bromo, iodo, O-S(O)2CF3; and Rg is a C1-10 alkyl; with a olefin forming reagent in a suitable base to yield a compound of Formula (II), or (Ha) wherein m=0 and oxidizing the sulphur as necessary or desired.

    Reactions of polymorphs of N-methyl-N-(3-(3-(2-thienylcarbonyl)-pyrazol-(1,5-alpha)-pyrimidin-7-yl)phenyl)acetamide
    88.
    发明公开
    Reactions of polymorphs of N-methyl-N-(3-(3-(2-thienylcarbonyl)-pyrazol-(1,5-alpha)-pyrimidin-7-yl)phenyl)acetamide 审中-公开
    苯基多巴胺多聚甲醛N-甲基-N-（3-（3-（2-噻吩基羰基） - 吡唑 - （1,5-α） - 嘧啶-7-基）苯基）乙酰胺

    公开(公告)号：EP1477169A1

    公开(公告)日：2004-11-17

    申请号：EP04013998.2

    申请日：2000-09-01

    申请人： Neurocrine Biosciences, Inc.

    发明人： Thiele, William, J. ,  O'Donnell, Patrick, B.

    IPC分类号： A61K31/519 ,  C07D487/02 ,  C07D487/04 ,  A61K31/505

    CPC分类号： C07D487/04

    摘要： Polymorphs of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide (Compound (1)), and use of the same as a sedative-hypnotic, anxiolytic, anticonvulsant, and skeletal muscle relaxant agent. Processes for making the same, as well as related compositions and methods are also disclosed, particularly with regard to treatment of insomnia. A polymorph Form I possessing exception physical and heat stability is provided. A polymorph Form II, is also provided.

    摘要翻译： N-甲基-N-（3-Ä2-噻吩基羰基-1H-吡唑并[1,5-a]嘧啶-7-基]苯基）乙酰胺（化合物（1））的多晶型物，并使用它们作为镇静催眠药 ，抗焦虑药，抗惊厥药和骨骼肌松弛剂。 还公开了制备方法以及相关组合物和方法，特别是关于治疗失眠的方法。 提供了具有异常物理和热稳定性的多晶型物I。 还提供了多晶型II。