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5-(N-BENZYL TETRAHYDROISOQUINOLIN-6-YL) PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
专利权人:
发明人:
申请号:
EP16758283.2
公开号:
EP3334716A1
申请日:
2016.08.10
申请国别(地区):
EP
年份:
2018
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.
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