NOVEL 2-PYRIDINECARBOXAMIDE DERIVATIVES, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF TREATMENT
    5.
    发明公开
    NOVEL 2-PYRIDINECARBOXAMIDE DERIVATIVES, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF TREATMENT 审中-公开
    新的2-PYRIDINCARBONSÄUREAMIDDERIVATE,用这类化合物和治疗方法组合物

    公开(公告)号:EP2931718A4

    公开(公告)日:2016-06-08

    申请号:EP13865833

    申请日:2013-12-12

    摘要: Novel pyridine-2-carboxamide derivatives of formula I and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are effective as glucokinase activating agents. Pharmaceutical compositions and methods of treatment are also included. The present invention relates to novel pyridine-2-carboxamide derivatives and salts thereof which are effective as glucokinase activating agents. Moreover, it relates to compositions containing such compounds, and methods of treatment.

    摘要翻译: 式的新的吡啶-2-甲酰胺衍生物I和药学上可接受的盐是游离缺失盘用于治疗或预防2型糖尿病和类似的条件是有用的。 该化合物是有效的葡糖激酶活化剂。 因此药物组合物和治疗方法也包括在内。 本发明涉及新的吡啶-2-甲酰胺衍生物及其盐可有效作为葡糖激酶活化剂。 更过地,它涉及COMPOSITIONS CONTAINING测试的化合物,和治疗的方法。

    FACTOR IXA INHIBITORS
    7.
    发明公开
    FACTOR IXA INHIBITORS 审中-公开
    FAKTOR-IXA-缝边

    公开(公告)号:EP2934538A4

    公开(公告)日:2016-06-08

    申请号:EP13873301

    申请日:2013-12-16

    摘要: The present invention provides a compound of Formula (I) wherein R1 is H or C1-6 alkyl, R2, is H or C1-6 alkyl or CH2OH, R3 is H or C1-6 alkyl, and R4 is H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, then R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl or —CH2OH, and when R2, R3, and R4 are H, then R1 is C1-6 alkyl; A is 1) a 9-10 membered bicyclic heterocycle having 1-3 heteroatoms independently selected from N, S and O, which 9-10 membered bicyclic heterocycle is unsubstituted or substituted with R5 and unsubstituted or substituted with R6 and unsubstituted or substituted with NH2, or 2) a 6-9 membered monocyclic or bicyclic carbocyclic ring system unsubstituted or substituted with R5, unsubstituted or substituted with R6, and unsubstituted or substituted with —CH2NH2; and B is 1) a 5- or 6-membered monocyclic heterocycle having 1 or 2 heteroatoms independently selected from N, S or O, which is unsubstituted or substituted on a carbon or nitrogen atom with R7, unsubstituted or substituted on a carbon or nitrogen atom with R8, and unsubstituted or substituted on a carbon or nitrogen atom with R9, or 2) an 8- or 9-membered fused bicyclic heterocycle having 1, 2 or 3 nitrogen atoms which is unsubstituted or substituted on a carbon or nitrogen atom with R7, and unsubstituted or substituted on a carbon or nitrogen atom with R8; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses.

    摘要翻译: 本发明提供式(I)化合物,其中R 1为H或C 1-6烷基,R 2为H或C 1-6烷基或CH 2 OH,R 3为H或C 1-6烷基,R 4为H或C 1-6 烷基,条件是当R 1,R 2和R 3为H时,R 4为C 1-6烷基,当R 1,R 2和R 4为H时,R 3为C 1-6烷基,当R 1,R 3和R 4为H ,R2是C1-6烷基或-CH2OH,当R2,R3和R4是H时,R1是C1-6烷基; A是1)具有1-3个独立地选自N,S和O的杂原子的9-10元双环杂环,其中9-10元双环杂环是未取代的或被R 5取代且未被取代或被R 6取代且未取代或被NH 2取代 ,或2)未被取代或被未取代或被R 6取代的R 5取代的未取代或被-CH 2 NH 2取代的6-9元单环或双环碳环系统; 且B为1)具有1或2个独立地选自N,S或O的杂原子的5或6元单环杂环,其未取代或在碳或氮原子上被取代或未取代或在碳或氮上取代的R7取代 具有R 8的未取代或取代的碳原子或氮原子上的取代基,或2)具有1,2或3个氮原子的8或9元稠合双环杂环,其未被取代或在碳原子或氮原子上被取代, R7,并且在碳或氮原子上未被取代或取代为R8; 和包含一种或多种所述化合物的药物组合物,以及使用所述化合物治疗或预防血栓形成的方法。