发明名称 TRPV3 modulators
摘要 Disclosed herein are modulators of TRPV3 of formula (I); wherein G1, X1, X2, X3, X4, X5, G2, Z1, Ra, Rb, u, and p are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
申请公布号 US9156788(B2) 申请公布日期 2015.10.13
申请号 US201313761862 申请日期 2013.02.07
申请人 AbbVie Inc. 发明人 Bayburt Erol K.;Clapham Bruce;Cox Phil B.;Daanen Jerome F.;Gomtsyan Arthur;Kort Michael E.;Kym Philip R.;Voight Eric A.
分类号 A61K31/444;C07D213/30;C07D239/26;C07D401/04;C07D405/12;C07D213/50;C07D401/12 主分类号 A61K31/444
代理机构 代理人
主权项 1. A compound according to formula (I):or a pharmaceutically acceptable salt thereof, wherein Ra and Rb are absent; u is 0; X3 is O; X4 is (CH2)m and X5 is (CH2)n; m and n are each 2; each Z1 group is an optional substituent on any substitutable carbon atom of the ring containing X3, X4, and X5, and is independently alkyl, O(alkyl), oxo, halogen, haloalkyl, or OH; two Z1 groups that are resided on the same carbon atom, together with the carbon atom to which they are attached optionally form a 4-6 membered monocyclic heterocycle ring containing one or two oxygen atoms; p is 0; —X1 is —OH and X2 is hydrogen; G1 is unsubstituted pyrimidinyl or pyridinyl; G2 is G2d wherein G2d is aryl, optionally substituted with 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of Gd, alkyl, alkenyl, alkynyl, halogen, haloalkyl, —CN, —OC(O)Rf, —OC(O)N(Rf)2, —S(O)2Re, —S(O)2N(Rf)2, —C(O)Rf, —C(O)ORf, —C(O)N(Rf)2, —N(Rf)2, —N(Rf)C(O)Rf, —N(Rf)S(O)2Re, —N(Rf)C(O)O(Re), —N(Rf)C(O)N(Rf)2, —(CR1aR1b)q—ORf, —(CR1aR1b)q—OC(O)Rf, —(CR1aR1b)q—OC(O)N(Rf)2, —(CR1aR1b)q—S(O)2Re, —(CR1aR1b)q—S(O)2N(Rf)2, —(CR1aR1b)q—C(O)Rf, —(CR1aR1b)q—C(O)ORf, —(CR1aR1b)q—C(O)N(Rf)2, —(CR1aR1b)q—N(Rf)2, —(CR1aR1b)q—N(Rf)C(O)Rf, —(CR1aR1b)q—N(Rf)S(O)2Re, —(CR1aR1b)q—N(Rf)C(O)O(Re), —(CR1aR1b)q—N(Rf)C(O)N(Rf)2, and —(CR1aR1b)q—CN;R1a and R1b, are the same or different, and at each occurrence are each independently hydrogen, alkyl, or haloalkyl;each occurrence of Rf is independently hydrogen, alkyl, haloalkyl, Gd, or —(CR1aR1b)q-Gd;each occurrence of Re is independently alkyl, haloalkyl, Gd, or —(CR1aR1b)q-Gd;q, at each occurrence, is independently 1, 2, or 3;each occurrence of Gd is independently aryl, heteroaryl, cycloalkyl, heterocycle, or cycloalkenyl; and is each optionally substituted with 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of alkyl, alkenyl, alkynyl, halogen, haloalkyl, —CN, —OC(O)Rj, —OC(O)N(Rj)2, —S(O)2Rk, —S(O)2N(Rj)2, —C(O)Rj, —C(O)ORj, —C(O)N(Rj)2, —N(Rj)2, —N(Rj)C(O)Rj, —N(Rj)S(O)2Rk, —N(Rj)C(O)O(Rk), —N(Rj)C(O)N(Rj)2, —(CR1aR1b)q—ORj, —(CR1aR1b)q—OC(O)Rj, —(CR1aR1b)q—OC(O)N(Rj)2, —(CR1aR1b)q—S(O)2Rk, —(CR1aR1b)q—S(O)2N(Rj)2, —(CR1aR1b)q—C(O)Rj, —(CR1aR1b)q—C(O)ORj, —(CR1aR1b)q—C(O)N(Rj)2, —(CR1aR1b)q—N(Rj)2, —(CR1aR1b)q—N(Rj)C(O)Rj, —(CR1aR1b)q—N(Rj)S(O)2Rk, —(CR1aR1b)q—N(Rj)C(O)O(Rk), —(CR1aR1b)q—N(Rj)C(O)N(Rj)2, and —(CR1aR1b)q—CN;each occurrence of Rj is independently hydrogen, alkyl, or haloalkyl; andeach occurrence of Rk is independently alkyl or haloalkyl.
地址 North Chicago IL US