B. NARASIMHULU NAIDU,DENIS R. ST. LAURENT,JEFFREY LEE ROMINE,JOHN F. KADOW,PRASANNA SIVAPRAKASAM,B NARASIMHULU NAIDU,DENIS R ST LAURENT,JOHN F
申请号：
BR112018002403
公开号：
BR112018002403A2
申请日:
2016.08.03
申请国别(地区):
BR
年份:
2018
代理人:
摘要：
Compounds of formula (I), including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their uses for inhibiting HIV integrase and treating those infected with HIV or AIDS are described. In the compounds of formula (I), R 1 is selected from H, alkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, (alkoxy) alkoxyalkyl or (R 6) alkyl； R 2 is phenyl substituted with 1 substituent of R 7 and with 0 to 3 substituents selected from halo, alkyl, haloalkyl, alkoxy and haloalkoxy； or R2 is selected from tetrahydroisoquinolinyl, ((ar1) alkyl) tetrahydroisoquinolinyl or ((n-alkoxycarbonyl) tetrahydroisoquinolinyl； r3 is selected from tetrahydroisoquinolinyl or decahydroisoquinolinyl and is substituted with 0 to 3 substituents selected from halo, alkyl and haloalkyl, or r 3 is a bridged or fused bicyclic amine [5-7.3-7.0-2] and is substituted with 0 to 3 alkyl substituents； or r 3 is selected from azetidinyl, pyrrolidinyl, piperidinyl or homopiperidinyl and contains a spirocyclic moiety in which the spirocyclic moiety, including the carbon atom to which it is attached, forms C 3-7 cycloalkane, tetrahydrofuranyl, tetrahydropyranyl, pyrrolidinyl, nylinyl piperidinyl, n-alkylapiperidinyl, homopiperidinyl or n-alkylapiperidinyl and wherein the spirocyclic moiety is substituted with 0 to 3 halo or alkyl substituents； r4 is selected from alkyl or haloalkyl R 5 is selected from H, alkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, (alkoxy) alkoxyalkyl or (R 6) alkyl； R6 is selected from (oxetanyl) oxide, ((oxetanyl) alkoxy) alkyl, (tetrahydropyranyloxy) alkyl, (tetrahydropyranyl) alkoxy) alkyl or (rg) (r9) n； R7 is selected from (ar1) alkoxy or ((ar1) alkyl) hnco； R 8 is selected from hydrogen, alkyl, (cycloalkyl) alkyl, alkoxyalkyl, (tetrahydropyanyl) alkyl, tetrahydropyanyl or alkoxyphenyl； R 9 is selected from hydrogen or alkyl； or (r 8) (r 9) n together is selected from azetidinyl, pyrrolidinyl, piperidinyl, (spirocyclobu
