[EN] PYRAZOLOPYRIDYL COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS [FR] COMPOSÉS PYRAZOLOPYRIDYLE À UTILISER EN TANT QU'INHIBITEURS DE L'ALDOSTÉRONE SYNTHASE
摘要 方便地访问各种2-芳基化吡唑并[1,5-一个]吡啶吡唑并经由[1,5-一个]吡啶-2-基三氟甲磺酸酯使用被描述的Suzuki-Miyaura交叉偶联反应。合成了15种2-芳基吡唑并[1,5- a ]吡啶衍生物,产率为52-95%。 方便地访问各种2-芳基化吡唑并[1,5-一个]吡啶吡唑并经由[1,5-一个]吡啶-2-基三氟甲磺酸酯使用被描述的Suzuki-Miyaura交叉偶联反应。合成了15种2-芳基吡唑并[1,5- a ]吡啶衍生物,产率为52-95%。
The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
本发明提供了作为血浆激肽酶抑制剂并具有相同理想特性的化合物及其组合物。
[EN] PYRIMIDINE PDE10 INHIBITORS<br/>[FR] INHIBITEURS PYRIMIDINES DE PDE10
申请人:MERCK SHARP & DOHME
公开号:WO2013028590A1
公开(公告)日:2013-02-28
The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
[EN] NOVEL COMPOUNDS AND COMPOSITIONS FOR INHIBITION OF FASN<br/>[FR] NOUVEAUX COMPOSÉS ET COMPOSITIONS POUR L'INHIBITION DE FASN
申请人:FORMA THERAPEUTICS INC
公开号:WO2014164749A1
公开(公告)日:2014-10-09
The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
本发明涉及用于抑制FASN的化合物和组合物,其合成、应用和解毒剂。本发明的一个示例化合物如下所示:
[EN] COMPOUNDS FOR THE TREATMENT OF KINASE-DEPENDENT DISORDERS<br/>[FR] COMPOSÉS POUR LE TRAITEMENT DE TROUBLES DÉPENDANT DE LA KINASE
申请人:EXELIXIS INC
公开号:WO2020247418A1
公开(公告)日:2020-12-10
Disclosed herein are compounds of Formula (I) which inhibit, regulate and/or modulate tyrosine kinase receptors, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities, compositions containing the compounds, methods of using the compounds to treat kinase-dependent diseases and conditions, and methods for making the compounds.
PYRAZOLOPYRIDYL COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS
申请人:MERCK SHARP & DOHME CORP
公开号:US20140288094A1
公开(公告)日:2014-09-25
This invention relates to pyrazolopyridyl compounds of the structural formula:
or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.