发明名称 SUBSTITUTED [1,2,4]TRIAZOLO[4,3-a]PYRAZINES AS BRD4 INHIBITORS
摘要 Method for treating AML and MM by administration of a compound of the formula (I);wherein the groups R1 to R3 have the meanings given in the specification.
申请公布号 US2016129001(A1) 申请公布日期 2016.05.12
申请号 US201614995578 申请日期 2016.01.14
申请人 Boehringer Ingelheim International GmbH 发明人 ENGELHARDT Harald;GIANNI Davide;SMETHURST Christian
分类号 A61K31/4985;A61K31/501;A61K31/5377 主分类号 A61K31/4985
代理机构 代理人
主权项 1. A method of treating AML or MM comprising administering to a patient having AML or MM a therapeutically effective amount of a compound of the formula (I) wherein, R1 is —C1-3alkyl or —C1-3haloalkyl; R2 is selected from —NHR4, —C1-5alkyl, —C1-5haloalkyl, halogen and —S—C1-3alkyl; R3 is a 5-12 membered heteroaryl, which group is substituted with —X—R10 and optionally further substituted with one or more groups independently selected from R9; R4 is selected from —C1-5alkyl and 5-12 membered heterocycloalkyl, which heterocycloalkyl can be optionally substituted with one or more groups independently selected from R5; R5 is selected from —C1-5alkyl, —C1-5haloalkyl and —C1-3alkylene-O—C1-3alkyl; R9 is selected from —C1-5alkyl, —O—C1-5alkyl, —N(C1-5alkyl)2, halogen, —C1-3alkylene-O—C1-3alkyl, —C1-5alkylene-N(C1-5alkyl)2 and 5-12 membered heterocycloalkyl, wherein the heterocycloalkyl group can be optionally substituted with one or more groups independently selected from ═O and —C1-3alkyl, or R9 is selected from —C6-10aryl and 5-12 membered heteroaryl, wherein the aryl and heteroaryl groups can be optionally and independently substituted with one or more groups selected from halogen, —C1-3alkyl, —O—C1-3alkyl, —C1-3haloalkyl-O—C1-3haloalkyl-N(C1-5alkyl)2 and —NH—C1-5alkyl; X is —C1-3alkylene- or —O—; R10 is —C6-10aryl or 5-12 membered heteroaryl, each of which groups can be optionally substituted with one or more groups selected from halogen, —C1-3alkyl, —O—C1-3alkyl, —C1-3haloalkyl and —O—C1-3haloalkyl; or a pharmaceutically acceptable salt thereof.
地址 Ingelheim am Rhein DE