发明名称 Cold menthol receptor antagonists
摘要 Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows:; wherein A, L, R1, R2, R4, and R5 are defined herein.
申请公布号 US9096521(B2) 申请公布日期 2015.08.04
申请号 US201414152006 申请日期 2014.01.10
申请人 Janssen Pharmaceutica NV 发明人 Colburn Raymond W;Dax Scott L;Flores Christopher M;Ludovici Donald W;Xia Mingde;Xu Xiaoqing;Youngman Mark A;Zhu Bin
分类号 C07D217/02;C07D401/12;A61K31/47;C07D217/04;C07C237/20;C07D215/38 主分类号 C07D217/02
代理机构 代理人
主权项 1. A compound of Formula (I)wherein A is thienyl or C5-7cycloalkyl; R1 is one to three substituents selected from the group consisting of hydrogen, C1-4alkyl, C1-4alkoxy, fluoro, chloro, and hydroxy; L is —Z—(CH2)n— or —CH2—; n is 0 or 1; Z is NR3; R2 is hydrogen, C1-4alkyl, C1-4alkoxy, trifluoromethyl, chloro, fluoro, bromo, carboxy, or C1-4alkoxycarbonyl; R3 is hydrogen or C1-3alkyl; R4 is hydrogen or C1-4alkyl; R5 is isoquinolinyl; wherein R5 is optionally substituted with 1 to 2 substituents independently selected from the group consisting of C1-4alkyl, hydroxy, C1-4alkoxy, trifluoromethyl, chloro, fluoro, bromo, carboxy, C1-4alkoxycarbonyl, and cyano; and enantiomers, diastereomers, or a pharmaceutically acceptable salts thereof.
地址 Beerse BE