Polycyclic carbamoylpyridone derivative having hiv integrase inhibitory activity

Patent metadata

Field	Value
Publication number	US-2016304535-A1
Application number	US-201615196245-A
Country	US
Kind code	A1
Filing date	Jun 29, 2016
Priority date	Apr 28, 2005
Publication date	Oct 20, 2016
Grant date	—

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.

First claim

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.

Assignees

• Shionogi & Co
• Viiv Healthcare Co

Inventors

• Johns Brian A
• Kawasuji Takashi
• Taishi Teruhiko
• Taoda Yoshiyuki

Classifications

• A61K9/20

  Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)} · CPC title

• A61P31/12

  Antivirals · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P31/18

  for HIV · CPC title

• A61P31/00

  Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics · CPC title