[EN] CANNABINOID RECEPTOR 1 ANTAGONISTS/INVERSE AGONISTS AND USES THEREOF [FR] ANTAGONISTES/AGONISTES INVERSES DU RÉCEPTEUR CANNABINOÏDE 1 ET LEURS UTILISATIONS
The present invention provides octahydro fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
本发明提供了八氢融合的阿扎德卡林化合物以及将这些化合物用作糖皮质激素受体调节剂的方法。
[EN] BICYCLIC INDAZOLE GLUCOCORTICOID RECEPTOR ANTAGONISTS<br/>[FR] ANTAGONISTES BICYCLIQUES DU RÉCEPTEUR DES GLUCOCORTICOÏDES D'INDAZOLE
申请人:CORCEPT THERAPEUTICS INC
公开号:WO2023122594A1
公开(公告)日:2023-06-29
The present disclosure provides compounds of Formula I, Ia, Ib, Ib-1, Ib-2, Ic, Ic-1, Id-1, and Id-2. Compounds of Formula I, Ia, Ib, Ib-1, Ib-2, Ic, Ic-1, Id-1, and Id-2 may be used in pharmaceutical formulations, and may be used for modulating glucocorticoid receptors.
[EN] FUSED AZATRICYCLIC DERIVATIVE, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF IN MEDICINE<br/>[ZH] 稠合的氮杂三环类衍生物、其制备方法及其在医药上的应用<br/>[FR] DÉRIVÉ AZATRICYCLIQUE CONDENSÉ, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION EN MÉDECINE
Identification of the Clinical Candidate (<i>R</i>)-(1-(4-Fluorophenyl)-6-((1-methyl-1<i>H</i>-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1<i>H</i>-pyrazolo[3,4-<i>g</i>]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist
作者:Hazel J. Hunt、Joseph K. Belanoff、Iain Walters、Benoit Gourdet、Jennifer Thomas、Naomi Barton、John Unitt、Timothy Phillips、Denise Swift、Emily Eaton
DOI:10.1021/acs.jmedchem.7b00162
日期:2017.4.27
The nonselective glucocorticoid receptor (GR) antagonist mifepristone has been approved in the U.S. for the treatment of selected patients with Cushing's syndrome. While this drug is highly effective, lack, of selectivity for GR leads to unwanted side effects in Sonic patients. Optimization pf the previously described fused azadecalin series of selective GR antagonists l'ed to the identification of CORT125134, which is currently being eValuateddp a phase 2 clinical study in patients with Cushing's syndrome.
[EN] HETEROARYL-KETONE FUSED AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS<br/>[FR] MODULATEURS DES RÉCEPTEURS DE GLUCOCORTICOÏDES CONSISTANT EN AZADÉCALINES À HÉTÉROARYLE CÉTONE FUSIONNÉ