发明名称 Tumor necrosis factor inhibitors
摘要 The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-α mediated conditions.
申请公布号 US9096607(B2) 申请公布日期 2015.08.04
申请号 US201414279506 申请日期 2014.05.16
申请人 The Trustees Of The University Of Pennsylvania 发明人 Greene Mark I.;Murali Ramachandran;Cheng Xin;Ottenbrite Raphael;Xiao Yingxin
分类号 A61K31/15;C07D311/82;C07D493/10;C07C251/86;A61K31/352;A61K31/365 主分类号 A61K31/15
代理机构 Baker & Hostetler LLP 代理人 Baker & Hostetler LLP
主权项 1. A method treating rheumatoid arthritis, psoriasis, ankylosing spondylitis, Crohn's disease, or ulcerative colitis, comprising treating a patient in need of such treatment with an effective amount of a compound having a structure of Formula (IIA), or a pharmaceutically acceptable salt thereof: wherein R6, R7, R8, and R9 are each independently alkyl, hydroxyl, alkoxy, NR13R14, halogen, nitro, cyano, borono, aryl, aryloxy, —(CH2)nCOOR15, —O(CH2)nCOOR16, —OC(O)R17, —CR18═NOH, —CR19R20NHOH, —SO3H, —SO2R21, —SO2NHR22, —O(CH2)mOR23, —C(OH)═NOH, —C(O)NR24OH, CHR25N(COR26)OH, or C(O)R27; or R8 and R9 together form —O—, —NHC(O)—, —C(O)NH—, —C(O)O—, —NR29—, or —S(O)2NH; R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26, R28, and R29 are each independently hydrogen, alkyl, or aryl, and R27 is alkyl or aryl; X is absent or is —O—, —NR28— or —S—; n and m are independently 0, 1, 2, 3, 4, 5, or 6; and t and u are independently 0, 1, 2, or 3.
地址 Philadelphia PA US