US2016304535A1PendingUtilityA1

Polycyclic carbamoylpyridone derivative having hiv integrase inhibitory activity

71
Assignee: SHIONOGI & COPriority: Apr 28, 2005Filed: Jun 29, 2016Published: Oct 20, 2016
Est. expiryApr 28, 2025(expired)· nominal 20-yr term from priority
A61K 9/20A61P 31/12A61P 43/00A61P 31/18A61P 31/00A61P 37/02A61K 31/4985C07D 471/14C07D 498/14A61K 31/5365C07D 471/04C07D 471/22C07D 498/22A61K 45/06A61K 9/0053A61K 31/551C07D 498/04C07D 498/20A61K 31/519
71
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Claims

Abstract

The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z 1 is NR 1 ; R 1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO 2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R 2 is optionally substituted aryl; R 3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R 4 and Z 2 part taken together forms a ring, to forma polycyclic compound, including e.g., a tricyclic or tetracyclic compound.

Claims

exact text as granted — not AI-modified
1 - 58 . (canceled) 
     
     
         57 . A compound of the formula: 
       
         
           
           
               
               
           
         
         wherein, 
         ring A is 
       
       
         
           
           
               
               
           
         
         Z═O; 
         wherein any two groups of R 32-39  together may form a carbocycle; 
         the stereochemistry of an asymmetric carbon represented by * shows R- or S-configuration, or a mixture thereof; 
         R is halogen; 
         m is an integer from 0 to 3; 
         R X  is hydrogen; 
         R 1  is hydrogen or lower alkyl; 
         R 3  is hydrogen, halogen, hydroxy, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted lower alkenyloxy, optionally substituted aryl, optionally substituted aryloxy, optionally substituted heterocyclic group, optionally substituted heterocycleoxy or optionally substituted amino; 
         R 14  is hydrogen; and, 
         or a pharmaceutically acceptable salt thereof. 
       
     
     
         58 . A pharmaceutical composition comprising the compound of  claim 57  or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier or diluent.

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