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    Heterocyclic derivatives which inhibit factor Xa
    1.
    发明申请
    Heterocyclic derivatives which inhibit factor Xa 审中-公开
    抑制因子Xa的杂环衍生物

    公开(公告)号：US20020193375A1

    公开(公告)日：2002-12-19

    申请号：US10180337

    申请日：2002-06-27

    申请人： ZENECA LIMITED

    发明人： Peter Warner ,  Roger James ,  Thorsten Nowak

    IPC分类号： A61K031/53 ,  A61K031/513 ,  A61K031/501 ,  A61K031/497 ,  A61K031/444 ,  A61K031/4439

    CPC分类号： C07D213/82

    摘要： The invention relates to heterocyclic derivatives, or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The, invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, formula (I).

    摘要翻译： 本发明涉及具有抗血栓形成和抗凝血性质的杂环衍生物或其药学上可接受的盐，因此可用于治疗人或动物的方法。 本发明还涉及制备杂环衍生物的方法，含有它们的药物组合物及其制备用于生产抗血栓形成或抗凝血作用的药物（式（I））的用途。

    Use of compounds for the elevation of pyruvate dehydrogenase activity
    2.
    发明申请
    Use of compounds for the elevation of pyruvate dehydrogenase activity 失效
    使用化合物来提高丙酮酸脱氢酶活性

    公开(公告)号：US20040009979A1

    公开(公告)日：2004-01-15

    申请号：US10277957

    申请日：2002-10-23

    申请人： ZENECA LIMITED

    发明人： Roger J. Butlin ,  Thorsten Nowak ,  Jeremy N. Burrows ,  Michael H. Block

    IPC分类号： A61K031/53 ,  A61K031/50 ,  A61K031/501 ,  A61K031/497 ,  A61K031/506

    CPC分类号： C07D295/192 ,  A61K31/167 ,  C07C235/16 ,  C07C317/40 ,  C07C317/42 ,  C07C317/44 ,  C07C323/65 ,  C07D295/096 ,  C07D295/13 ,  C07D295/15 ,  C07D295/205 ,  C07D295/24 ,  C07D295/26

    摘要： The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs; in formula (I), Ring C is phenyl or a carbon linked heteroaryl ring substituted as defined within; R1 is an ortho substituent as defined within; n is 1 or 2; A-B is a linking group as defined within; R2 and R3 are as defined within; R4 is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are also described. 1

    摘要翻译： 使用式（I）化合物及其盐; 和所述式（I）化合物的药学上可接受的体内可切割前药; 和所述化合物或所述前药的药学上可接受的盐; 在式（I）中，环C是苯基或被定义为碳原子的杂芳基环; R 1是如上所定义的邻位取代基; n为1或2; A-B是定义的连接基团; R 2和R 3如上所定义; R 4是羟基，氢，卤素，氨基或甲基; 在制备用于升高温血动物（例如人）中PDH活性的药物中的用途。 还描述了制备式（I）化合物的药物组合物，方法和方法。