FURO- AND THIENO-PYRIDINE CARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS
    14.
    发明公开
    FURO- AND THIENO-PYRIDINE CARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS 审中-公开
    FURO-UND THIENO-吡啶羧酰胺 - 维生素D

    公开(公告)号:EP3036238A1

    公开(公告)日:2016-06-29

    申请号:EP14766267.0

    申请日:2014-08-22

    CPC分类号: C07D495/04 C07D491/048

    摘要: The present disclosure describes furo-and thieno-pyridine carboxamide compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: X is S or 0; A
    5 is N or C-R
    5 . Cy
    A is a 5 to 6 membered monocyclic heteroaryl group, wherein the ring atoms of the heteroaryl group forming Cy
    A consist of carbon atoms and 1, 2, or 3 heteroatoms selected from N, 0 and S, and wherein the 5 to 6 membered monocyclic heteroaryl group forming Cy
    A is unsubstituted or substituted with 1, 2, or 3 R
    A ; Cy
    B is C
    6-10 aryl, C
    3-7 cycloalkyl, 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl wherein the ring atoms of the ring atoms of the heteroaryl or heterocycloalkyl forming Cy
    B consist of carbon atoms and 1, 2 or 3 heteroatoms selected from 0, N and S, and wherein each of said C
    6-10 aryl, C
    3-7 cycloalkyl, 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl forming Cy
    B is unsubstituted or substituted with 1, 2, 3, 4 or 5 R
    B ; R
    2 is H, halogen or NH
    2 ; and R
    5 , R
    6 and R
    7 are as defined in claim 1; The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.

    摘要翻译: 本公开描述了呋喃和噻吩并吡啶甲酰胺化合物,以及它们的组合物和使用方法。 该化合物抑制Pim激酶的活性,并且可用于治疗与Pim激酶活性相关的疾病,包括例如癌症和其它疾病。

    AZETIDINE AND CYCLOBUTANE DERIVATIVES AS JAK INHIBITORS
    19.
    发明公开
    AZETIDINE AND CYCLOBUTANE DERIVATIVES AS JAK INHIBITORS 有权
    AZETIDIN- UND CYCLOBUTANDERATE ALS JAK-INHIBITOREN

    公开(公告)号:EP2288610A1

    公开(公告)日:2011-03-02

    申请号:EP09718650.6

    申请日:2009-03-10

    摘要: The method includes the steps of performing in-vitro liver, intestinal and/or expressed enzyme assays with selected ethnobotanical substances, for both humans and a variety of animal species, to produce an array of resulting chemical entities, such as metabolites, for the human and the animals. Comparisons are then made between the chemical entities from the human in-vitro studies and the animal in-vitro studies to determine the closest match. The animal with the closest match is then used for an in-vivo study. If a match is present between the animal in-vivo results and the human in-vitro results, the matched chemical entity is isolated or synthesized and then further tested to determine the suitability of the matched chemical entity as a treatment drug.

    摘要翻译: 本发明涉及氮杂环丁烷和环丁烷衍生物,以及它们的组合物,使用方法和制备方法,其是用于治疗JAK相关疾病(包括例如炎性和自身免疫性疾病)的JAK抑制剂,以及 作为癌症。