发明名称 Substituted triazole derivatives as oxytocin antagonists
摘要 The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction.;
申请公布号 US9394278(B2) 申请公布日期 2016.07.19
申请号 US201514691319 申请日期 2015.04.20
申请人 Ixchelsis Limited 发明人 Brown Alan Daniel;Calabrese Andrew Antony;Ellis David
分类号 C07D401/04;C07D401/14 主分类号 C07D401/04
代理机构 Mueting, Raasch & Gebhardt, P.A. 代理人 Mueting, Raasch & Gebhardt, P.A.
主权项 1. A compound of formula (I): wherein: m is 2 and n is 1;X is selected from O, NH, N(C1-C6)alkyl, NC(O)(C1-C6)alkyl, N(SO2(C1-C6)alkyl), S and SO2;R1 is phenyl or napthylwherein said phenyl or napthyl is optionally substituted with one or more substituents independently selected from halo, (C1-C6)alkyl, (C1-C6)alkoxy,(C1-C6)alkoxy(C1-C6)alkyl, cyano, CF3, NH(C1-C6)alkyl, N((C1-C6)alkyl)2, CO(C1-C6)alkyl, C(O)O(C1-C6)alkyl, C(O)NH(C1-C6)alkyl, C(O)N((C1-C6)alkyl)2, C(O)OH and C(O)NH2;R2 is selected from:(i) H and hydroxy;(ii) (C1-C6)alkyl, which is optionally substituted by O(C1-C6)alkyl or phenyl;(iii) O(C1-C6)alkyl, which is optionally substituted by O(C1-C6)alkyl;(iv) NH(C1-C6)alkyl, said alkyl group being optionally substituted by O(C1-C6)alkyl; and(v) N((C1-C6)alkyl)2, one or both of said alkyl groups being optionally substituted by O(C1-C6)alkyl;R3 is selected from H, (C1-C6)alkyl and (C1-C6)alkoxy(C1-C6)alkyl;R4, R5, R6 and R7 are each independently selected from H, halo, hydroxy, CN, (C1-C6)alkyl, NH(C1-C6)alkyl, N((C1-C6)alkyl)2 and O(C1-C6)alkyl;R8 is selected from H, (C1-C6)alkyl, (C1-C6)alkoxy(C1-C6)alkyl, CH2OH, CH2NH2, CH2NH(C1-C6)alkyl, CH2N((C1-C6)alkyl)2, CN, C(O)NH2, C(O)NH(C1-C6)alkyl and C(O)N((C1-C6)alkyl)2; a tautomer thereof or a pharmaceutically acceptable salt of said compound or tautomer.
地址 Sandwich, Kent GB