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14 条记录 (耗时 0.024 秒)

    COMPOUNDS FOR THE INHIBITION OF DGAT1 ACTIVITY
    3.
    发明公开
    COMPOUNDS FOR THE INHIBITION OF DGAT1 ACTIVITY 审中-公开
    化合物用于抑制活性DGAT1

    公开(公告)号：EP2032547A1

    公开(公告)日：2009-03-11

    申请号：EP07733145.2

    申请日：2007-06-08

    申请人： AstraZeneca AB

    发明人： BENNETT, Stuart, Norman, Lile ,  BUTLIN, Roger, John ,  PLOWRIGHT, Alleyn

    IPC分类号： C07D271/10

    CPC分类号： C07D271/113

    摘要： Compounds of formula (I), or salts thereof, which inhibit acetyl CoA(acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein, for example, R1 is optionally substituted phenyl or naphthyl; Ring A is selected from (3-6C)cycloalkyl, (5-12C)bicycloalkyl and phenyl; n is 0, 1 or 2; R2 is, for example, hydrogen, fluoro, chloro or hydroxy; Ring B is selected from (3-6C)cycloalkyl, (5-12C)bicycloalkyl and phenyl; L1 is a direct bond or a defined linker group and R3 is, for example, hydroxy, carboxy or (1-6C)alkoxycarbonyl; together with processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.

    N-HETEROARYL-PYRIDINESULFONAMIDE DERIVATIVES AND THEIR USE AS ENDOTHELIN ANTAGONISTS
    6.
    发明授权
    N-HETEROARYL-PYRIDINESULFONAMIDE DERIVATIVES AND THEIR USE AS ENDOTHELIN ANTAGONISTS 失效
    N-杂芳基PYRIDINSULFONAMIDDERIVATE及其作为内皮素

    公开(公告)号：EP0832082B1

    公开(公告)日：2001-11-21

    申请号：EP96919941.3

    申请日：1996-06-03

    申请人： AstraZeneca AB

    发明人： BRADBURY, Robert, Hugh ,  BUTLIN, Roger, John ,  JAMES, Roger

    IPC分类号： C07D401/12 ,  A61K31/495

    CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D413/14

    摘要： The invention concerns pharmaceutically useful compounds of formula (I), in which A?1, A2, A3, A4, B1¿, m, Ar, W, X, Y, Z and R1 have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

    AMIDES AS INHIBITORS FOR PYRUVATE DEHYDROGENASE
    10.
    发明授权
    AMIDES AS INHIBITORS FOR PYRUVATE DEHYDROGENASE 有权
    酰胺类作为抑制剂的磷酸脱氢酶

    公开(公告)号：EP1214287B1

    公开(公告)日：2008-07-02

    申请号：EP00954797.7

    申请日：2000-08-30

    申请人： AstraZeneca AB

    发明人： BUTLIN, Roger, John ,  PEASE, Janet, Elizabeth ,  BLOCK, Michael, Howard ,  NOWAK, Thorsten ,  BURROWS, Jeremy, Nicholas ,  CLARKE, David, Stephen

    IPC分类号： C07C211/32 ,  C07D295/22 ,  C07D295/18 ,  C07D209/08 ,  C07D211/58 ,  A61K31/495 ,  A61P3/10

    CPC分类号： C07D295/185 ,  C07D209/08 ,  C07D211/32 ,  C07D211/58 ,  C07D295/192 ,  C07D295/26

    摘要： A compound of formula (I) wherein: Ring A is a nitrogen linked mono or bicyclic heterocyclic ring as defined within; R?1 and R2¿ are independently C¿1-3?alkyl optionally substituted by fluoro or chloro; or R?1 and R2¿ together with the carbon atom to which they are attached, form a C¿3-5?cylcoalkyl ring optionally substituted by fluoro; R?3¿ is as defined within; and n is 0-5; wherein the values of R3 may be the same or different; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.

    摘要翻译： 式（I）化合物，其中：环A是如本文所定义的氮连接的单环或双环杂环; R 1和R 2'独立地为任选被氟或氯取代的C 1-3 - 烷基; 或R 1和R 2'与它们所连接的碳原子一起形成任选被氟取代的C 3〜5的环烷基环; R？3是如在其中定义的; 并且n是0-5; 其中R3的值可以相同或不同; 或其药学上可接受的盐或体内可水解的酯。 还描述了式（I）化合物在温血动物例如人中产生PDH活性升高中的用途。 详细描述了用于制备式（I）化合物的药物组合物，方法和工艺。