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    PYRIMIDINE CARBOXAMIDE DERIVATIVES
    2.
    发明申请
    PYRIMIDINE CARBOXAMIDE DERIVATIVES 审中-公开
    吡咯烷酰胺衍生物

    公开(公告)号：WO2013032522A1

    公开(公告)日：2013-03-07

    申请号：PCT/US2012/000373

    申请日：2012-08-29

    申请人： APAC PHARMACEUTICAL LLC. ,  MAEHR, Hubert

    发明人： MAEHR, Hubert

    IPC分类号： C07D239/24 ,  A61K31/505 ,  A61P29/00

    CPC分类号： C07D239/28 ,  C07C235/78 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42

    摘要： The invention relates to a compound of the formula wherein the substituents are as defined herein, and a pharmaceutically acceptable salt of the compound of formula (1). The compounds of formula (1) and their salts possess inflammation inhibiting properties and are therefore useful in the treatment and prevention of conditions related to inflammations such as inflammatory joint diseases. The compounds of formula (1) are also useful for the treatment of diseases where chronic inflammation is the underlying cause. This application relates to compounds of formula (1), methods for their preparation, pharmaceutical compositions comprising these compounds, and their use for the preparation of a medicament for the treatment of humans and animals.

    摘要翻译： 本发明涉及下式化合物，其中取代基如本文所定义，和式（1）化合物的药学上可接受的盐。 式（1）的化合物及其盐具有炎症抑制性质，因此可用于治疗和预防与诸如炎性关节疾病的炎症有关的病症。 式（1）的化合物也可用于治疗慢性炎症是其根本原因的疾病。 本申请涉及式（1）化合物，其制备方法，包含这些化合物的药物组合物及其用于制备治疗人和动物的药物的用途。

    MATRIX METALLOPROTEINASE INHIBITORS
    10.
    发明申请
    MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
    基质金属蛋白酶抑制剂

    公开(公告)号：WO2005016868A3

    公开(公告)日：2005-05-19

    申请号：PCT/EP2004009087

    申请日：2004-08-12

    申请人： GLAXO GROUP LTD ,  HOLMES IAN ,  WATSON STEPHEN PAUL

    发明人： HOLMES IAN ,  WATSON STEPHEN PAUL

    IPC分类号： C07C233/51 ,  C07C235/34 ,  C07C235/78 ,  C07C255/57 ,  C07D209/08 ,  C07D333/24 ,  C07C235/00 ,  C07C255/00

    CPC分类号： C07C235/78 ,  C07C233/51 ,  C07C235/34 ,  C07C255/57 ,  C07C2601/14 ,  C07D209/08 ,  C07D333/24

    摘要： Compounds of Formula (I), wherein R represents optionally substituted -C4-12 alkyl, -C2-10alkylcycloalkyl, -C2-6 alkyl heterocycloalkyl, -C2-6alkylaryl, optionally substituted 5- or 6- membered aryl or heteroaryl, except pyridinyl. Z represents a bond, CH2, O, S, SO, SO2, NR , OCR R , CR R O, or Z, R and Q together form an optionally substituted fused tricyclic group; Q represents an optionally substituted 5- or 6- membered aryl or heteroaryl ring; X represents COR ; R represents CONH2, CO2H, CO2R , SO2R or SO2NR R , except that R ; may not represent CO2R when X is CONH2 ; R represents OR , or NR R ; R and R each independently represents H, C1-6 alkyl or C1-4 alkylaryl; R represents H or C1-6 alkyl; R represents C1-6 alkyl; R and R each independently represents H or C1-6 alkyl or R and R together with the nitrogen atom to which they are attached form a 5- or 6- membered ring which may optionally include 1 or more further heteroatoms selected from O, S and N; and physiologically functional derivatives thereof with the exception of [3-(acetylamino)-4-cyclohexylphenyl]-butanedioic acid and 3-(acetylamino)-4-cyclohexylphenyl]-butanedioic acid diethyl ether; butanedioic acid [3-methoxy-4-(phenylmethoxy)phenyl]; butanedioic acid [4-(phenylmethoxy)phenyl]; with the proviso that when R represents C4-12 alkyl, Z is other than a bond, O or CH2; and physiologically functional derivatives thereof , processes for their preparation, pharmaceutical formulations containing them and their use as inhibitors of matrix metallproteinase enzymes (MMPs) are described.

    摘要翻译： 式（I）化合物，其中R 1表示任选取代的-C 4-12烷基，-C 2-10烷基环烷基，-C 2-6烷基杂环烷基，-C 2-6烷基芳基，任选取代的5-或6-元芳基或杂芳基， 除了吡啶基。 Z表示键，CH 2，O，S，SO，SO 2，NR 4，OCR 4 R 5，CR 4 R 5 O或Z，R 1和Q一起形成 任选取代的稠合三环基团; Q代表任选取代的5元或6元芳基或杂芳基环; X代表COR 3; R 2代表CONH 2，CO 2 H，CO 2 R 7，SO 2 R 7或SO 2 NR 8 R 9，除了R 2; 当X是CONH 2时可能不代表CO 2 R 7; R 3表示OR 6或NR 8 R 9; R 4和R 5各自独立地表示H，C 1-6烷基或C 1-4烷基芳基; R6代表H或C1-6烷基; R 7表示C 1-6烷基; R 8和R 9各自独立地表示H或C 1-6烷基或者R 8和R 9与它们所连接的氮原子一起形成5-或6-元环，其可任选地 包括1个或多个选自O，S和N的其他杂原子; 以及除[3-（乙酰氨基）-4-环己基苯基] - 丁二酸和3-（乙酰氨基）-4-环己基苯基] - 丁二酸二乙酯以外的其生理学功能衍生物; 丁二酸[3-甲氧基-4-（苯基甲氧基）苯基]; 丁二酸[4-（苯基甲氧基）苯基]; 条件是当R 1代表C 4-12烷基时，Z不是键，O或CH 2; 及其生理功能衍生物，其制备方法，含有它们的药物制剂以及它们作为基质金属蛋白酶（MMP）抑制剂的用途。