US2019092754A1PendingUtilityA1

5-(n-benzyl tetrahydroisoquinolin-6-yl) pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication

Assignee: VIIV HEALTHCARE UK NO 5 LTDPriority: Aug 11, 2015Filed: Nov 28, 2018Published: Mar 28, 2019
Est. expiryAug 11, 2035(~9 yrs left)· nominal 20-yr term from priority
A61P 31/18C07D 401/14A61K 31/4725A61K 31/5365A61K 31/444A61K 2300/00C07D 401/04
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Claims

Abstract

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.

Claims

exact text as granted — not AI-modified
We claim: 
     
         1 . A compound of Formula I 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof wherein: 
         R 1  is hydrogen, C 1-6 alkyl, or C 3-7 cycloalkyl; 
         R 2  is tetrahydroisoquinolinyl and is substituted with 1 R 6  substituent and also with 0-3 halo or C 1-6 alkyl substituents; 
         R 3  is azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, homopiperidinyl, homopiperazinyl, or homomorpholinyl, and is substituted with 0-3 substituents selected from cyano, halo, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 alkoxy, and C 1-6 haloalkoxy; 
         R 4  is C 1-6 alkyl or C 1-6 haloalkyl; 
         R 5  is C 1-6 alkyl; 
         R 6  is Ar 1 , (Ar 1 ) C 1-6 alkyl, (chromanyl)C 1-6 alkyl, cyanoC 3-7 cycloalkyl or (dihydrobenzodioxinyl) C 1-6 alkyl; and 
         Ar 1  is phenyl substituted with 0-5 substituents selected from cyano, halo, C 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 haloalkyl, hydroxy, C 1-6 alkoxy, C 1-6 haloalkoxy, (hydroxy)C 1-6 alkoxy-(C 1-6 alkoxy)C 1-6 alkoxy, phenoxy, benzyloxy, carboxy, phenyl, and cyanoC 3-7 cycloalkyl.

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