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    FXR modulators
    5.
    发明授权
    FXR modulators 失效

    公开(公告)号：US07511043B2

    公开(公告)日：2009-03-31

    申请号：US10794228

    申请日：2004-03-04

    申请人： Jonathan Houze ,  Sharon McKendry ,  Joshua Gergely ,  Yi Xia ,  Bei Shan ,  Frank Kayser

    发明人： Jonathan Houze ,  Sharon McKendry ,  Joshua Gergely ,  Yi Xia ,  Bei Shan ,  Frank Kayser

    IPC分类号： A61K31/497 ,  C07D241/36

    CPC分类号： C07D209/48 ,  C07C233/75 ,  C07C237/22 ,  C07C311/19 ,  C07C311/29 ,  C07C2601/14 ,  C07D241/44 ,  C07D279/02

    摘要： The present invention provides compounds, pharmaceutical compositions and methods that are useful in modulating the farnesoid X receptor (FXR). As FXR is involved in negatively controlling the expression level of cholesterol 7α-hydroxylase (cyp7a), the rate-limiting enzyme involved in the oxidative metabolism of cholesterol into bile acids, the compounds described herein find utility in treating diseases associated with abnormally high or low cholesterol levels. In certain aspects, the FXR modulators (e.g., antagonists) described herein block the negative feed-back downregulation of cyp7a expression produced by certain cholic acids, the endogenous ligands for FXR. Moreover, as FXR forms heterodimers with the retinoid X receptor (RXR) in some cell types, modulation of the level of FXR activity in cells has a wide range of effects on a variety of biological processes which are mediated by RXR or other RXR-interacting proteins such as PPARγ and PPARα. Thus, compounds described herein are useful in treating other biological activities such as obesity, diabetes, lipid associated disorders, cancer, inflammatory disorders, disorders involving a disrupted or dysfunctional epidermal barrier, and various other metabolic disorders.

    Sulfonylated pyrrole-2-indolinone derivatives as kinase inhibitors
    7.
    发明申请
    Sulfonylated pyrrole-2-indolinone derivatives as kinase inhibitors 审中-公开
    磺酰化吡咯-2-二氢吲哚酮衍生物作为激酶抑制剂

    公开(公告)号：US20050032871A1

    公开(公告)日：2005-02-10

    申请号：US10653470

    申请日：2003-09-03

    申请人： Peng Tang ,  Chung Wei ,  Yi Xia

    发明人： Peng Tang ,  Chung Wei ,  Yi Xia

    IPC分类号： A61K31/404 ,  C07D403/06 ,  C07D413/14 ,  C07D43/02

    CPC分类号： C07D403/06 ,  C07D413/14

    摘要： The present invention relates to compounds having the following chemical structure (Formula I): where the substituents R1-R10 are defined herein. The compounds of this invention are useful in treating disorders related to abnormal kinase activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

    摘要翻译： 本发明涉及具有以下化学结构（式I）的化合物：其中取代基R 1 -R 10在本文中定义。 本发明的化合物可用于治疗与异常激酶活性相关的疾病。 还公开了包含这些化合物的药物组合物，利用包含这些化合物的药物组合物治疗疾病的方法及其制备方法。