发明名称 Cyclic amines as bromodomain inhibitors
摘要 The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
申请公布号 US9073878(B2) 申请公布日期 2015.07.07
申请号 US201314085545 申请日期 2013.11.20
申请人 Zenith Epigenetics Corp. 发明人 Fairfax David John;Duffy Bryan Cordell;Martin Gregory Scott;Quinn John Frederick;Liu Shuang;Wagner Gregory Steven;Young Peter Ronald
分类号 C07D239/91;C07D265/32;A61K45/06;C07D401/04;C07D401/14;A61K31/517 主分类号 C07D239/91
代理机构 Finnegan, Henderson, Farabow, Garrett & Dunner, LLP 代理人 Finnegan, Henderson, Farabow, Garrett & Dunner, LLP
主权项 1. A compound of Formula I: or a stereoisomer, tautomer, pharmaceutical acceptable salt, or hydrate thereof, wherein: W1 is selected from N and CR1;W2 is selected from N and CR2;W3 is selected from N and CR3;W4 is selected from N and CR4;each W may be the same or different from each other;A is selected from N and CH;R1, and R4 are each independently selected from hydrogen, alkyl, alkenyl, alkynyl, alkoxy, thioalkyl, aryloxy, aryl, amino, hydroxyl, and halogen;R2 and R3 are each independently selected from hydrogen, alkyl, alkenyl, alkynyl, alkoxy, thioalkyl, aryloxy, aryl, hydroxyl, and halogen; two adjacent substituents selected from R1, R2, R3, and R4 may be connected in a 5- or 6- membered ring to form a bicyclic carbocycle or bicyclic heterocycle; AR1 is a group selected from the following: B is a group selected from the following: each ring system may be substituted with one or more substituents independently selected from R10 and R11; R5 is selected from hydrogen, alkoxy, alkyl, thioalkyl, aryloxy, aryl, hydroxyl, and halogen; R6 is selected from hydrogen, alkoxy, alkyl, thioalkyl, aryloxy, aryl, and halogen; R7 is selected from hydrogen, alkyl, —SO2R12, —C(O)NR12R13, and —C(O)R12; R8 and R9 are independently selected from hydrogen, aryl, alkenyl, alkyl, —SO2R12, —C(O)NR12R13, and —C(O)R12; R10 and R11 are independently selected from hydrogen, halogen, alkyl, alkoxy, aryl, and hydroxyl; R12 and R13 are independently selected from hydrogen, aryl, and alkyl; Y is selected from NH, O, and S; and two adjacent substituents selected from R5, R6, R6, R9, R10, and R11 may be connected in a 5- or 6-membered ring to form a carbocycle or heterocycle.
地址 Calgary, Alberta CA