EASTMAN, KYLE J.,KADOW, JOHN F.,PARCELLA, KYLE E.,NAIDU, B. NARASIMHULU,WANG, TAO,YIN, ZHIWEI,ZHANG, ZHONGXING
申请号:
CA2994791
公开号:
CA2994791A1
申请日:
2016.08.10
申请国别(地区):
CA
年份:
2017
代理人:
摘要:
Disclosed are compounds of Formula (I), including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS. In the compounds of formula (I), R1 is selected from hydrogen, alkyl, or cycloalkyi R2 is selected from tetrahydroisoquinolinyl and is substituted with 1 R6 substituent and also with 0-3 halo or alkyl substituents R3 is selected from azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, homopiperidinyl, homopiperazinyl, or homomorpholinyl, and is substituted with 0-3 substituents selected from cyano, halo, alkyl, haloalkyi, alkoxy, and haloalkoxy R4 is selected from alkyl or haloalkyi R5 is alkyl R6 is selected from Ar1, (Ar1)alkyl, (chromanyl)alkyl, cyanocycloalkyl or (dihydrobenzodioxinyl)alkyl and Ar1 is phenyl substituted with 0-5 substituents selected from cyano, halo, alkyl, cycloalkyi, haloalkyi, hydroxy, alkoxy, haloalkoxy, (hydroxy)alkoxy, (alkoxy)alkoxy, phenoxy, benzyloxy, carboxy, phenyl, and cyanocycloalkyl.