发明名称 Compounds
摘要 The present invention is directed to novel retinoid-related orphan receptor gamma (RORγ) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by RORγ.
申请公布号 US9242972(B2) 申请公布日期 2016.01.26
申请号 US201314394113 申请日期 2013.04.25
申请人 Glaxo Group Limited 发明人 Birault Veronique;Campbell Amanda Jennifer;Harrison Stephen;Le Joelle;Shukla Lena
分类号 C07D213/76;C07D405/12;C07D413/12;A61K31/47;A61K31/5395;C07D413/14;C07D405/14 主分类号 C07D213/76
代理机构 代理人 Dinner Dara L.;Furman Theodore R.
主权项 1. A compound of formula (I), or a pharmaceutically acceptable salt thereof: wherein: R1 is each X1 is independently N or CRa; each X2 is independently N or CRb; X3 is N or CRc; each Ra is independently selected from H, CF3, halo, C1-4alkyl and C1-4alkoxy; each Rb is independently selected from H, CF3, halo, CH3 and OCH3; each Rc is independently selected from H, C1-4alkyl, C2-4alkenyl, C1-4alkoxy, CF3, halo, CN, C3-6cycloalkyl and C3-6heterocycloalkyl; R2 is selected from the group consisting of C3-5alkyl, —CH2C3-4cycloalkyl, and —CH2oxetanyl; each R3 is independently selected from the group consisting of C1-3alkyl, C1-3alkoxy, halo, OH and CH2OH; R4 is the group —X(CHR5)bR6; X is selected from the group consisting of O, CH2, CHOH and CHCH2OH; each R5 is independently selected from the group consisting of H, OH and CH2OH; R6 is isoxazole, tetrahydro-2H-pyran, tetrahydrofuran, —NHR7 or is a 5- or 6-membered heteroaryl group, wherein R6 may be unsubstituted or substituted with one or two substitutents independently selected from halo and CH3; R7 is oxetanyl or tetrahydrofuran, wherein R7 may be unsubstituted or substituted with one or two substitutents independently selected from halo and CH3; a is 0, 1 or 2; b is 0, 1 or 2; with the proviso that R1 contains one or two nitrogen atoms.
地址 Brentford, Middlesex GB