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Pyridin-3-ylacetic acid derivatives as inhibitors of human immunodeficiency virus replication
专利权人:
ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド;ヘルスケア;ヴィーブ;ユーケー(ナンバー5)リミテッド
发明人:
キャドウ,ジョン エフ.,ナイドゥ,ビー.ナラシムフル,ロマイン,ジェフリー リー,シヴァプラカサン,プラサンナ,サン.ローラン,デニス アール.,キャドウ,ジョン エフ.,ナイドゥ,ビー.ナラシムフル,ロマイン,ジェフリー リー,シヴァプラカサン,プラサンナ,サン.ローラン,デニス アール.
申请号:
JP2018506098
公开号:
JP2018522052A
申请日:
2016.08.03
申请国别(地区):
JP
年份:
2018
代理人:
摘要:
Disclosed are compounds of formula I, including pharmaceutically acceptable salts, pharmaceutical compositions containing the compounds, methods of making the compounds and their use in the inhibition of HIV integrase and treatment of those infected with HIV or AIDS. Has been. In compounds of formula I, R1 is selected from H, alkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, (alkoxy) alkoxyalkyl, or (R6) alkyl, R2 is one R7 substituent, as well as halo, Phenyl substituted with 0 to 3 substituents selected from alkyl, haloalkyl, alkoxy, and haloalkoxy, or R2 is tetrahydroisoquinolinyl, ((Ar1) alkyl) tetrahydroisoquinolinyl Or (N-alkoxycarbonyl) tetrahydroisoquinolinyl, R3 is selected from tetrahydroisoquinolinyl or decahydroisoquinolinyl and selected from halo, alkyl, and haloalkyl Substituted with three substituents, or R3 is a [5-7.3-7.0-2] fused or bridged bicyclic amine, and Substituted with 0-3 alkyl substituents, or R3 is selected from azetidinyl, pyrrolidinyl, piperidinyl, or homopiperidinyl and contains a spirocyclic moiety, wherein the spirocyclic moiety is attached Forming C3-7 cycloalkanes, tetrahydrofuranyl, tetrahydropyranyl, pyrrolidinyl, N-alkylpyrrolidinyl, piperidinyl, N-alkylpiperidinyl, homopiperidinyl, or N-alkylpiperidinyl containing carbon atoms And wherein the spirocyclic moiety is substituted with 0 to 3 halo or alkyl substituents, R4 is selected from alkyl or haloalkyl, and R5 is H, alkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl. , (Alkoxy) alkoxyalkyl, or (R6) alkyl. , R6 is selected from (oxetanyl) oxy, ((oxetanyl) alkoxy) alkyl, (tetrahydropyranyloxy) alkyl, ((tetrahydropyranyl) alkoxy) alkyl, or (R8) (R9) N, and R7 is ( Ar1) alkoxy or ((Ar1) alkyl) HNCO, R8 is selected from hydrogen, alkyl, (cycloalkyl) alkyl, alkoxyalkyl, (tetrahydropyranyl) alkyl, tetrahydropyranyl, or alkoxyphenyl, R9 (R8) (R9) N is selected from hydrogen or alkyl or taken together is selected from azetidinyl, pyrrolidinyl, piperidinyl, (spirocyclobutyl) piperidinyl, piperazin
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