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Last Updated: May 10, 2024

Details for Patent: 7,858,788


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Title:Bicyclic carbamoylpyridone derivative having HIV integrase inhibitory activity
Abstract: Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and an agent, particularly an anti-HIV agent. A compound represented by the formula: ##STR00001## (wherein Z.sup.1 is NR.sup.4 (R.sup.4 is hydrogen, optionally substituted lower alkyl etc.), O or CH.sub.2; Z.sup.2 is optionally substituted lower alkylene or optionally substituted lower alkenylene, each may be intervened by a heteroatom group selected from group consisting O, S, SO, SO.sub.2, NR.sup.5 (R.sup.5 is selected independently from the same substituent group of R.sup.4) --N.dbd. and .dbd.N--; R.sup.1 is hydrogen or lower alkyl; X is a single bond, a heteroatom group selected from O, S, SO, SO.sub.2 and NH, or lower alkylene or lower alkenylene each may be intervened by the heteroatom group; R.sup.2 is optionally substituted aryl; R.sup.3 is hydrogen, halogen, hydroxy, optionally substituted alkyl group etc.)
Inventor(s): Yoshida; Hiroshi (Osaka, JP), Kawasuji; Takashi (Osaka, JP), Taoda; Yoshiyuki (Osaka, JP)
Assignee: Shionogi & Co., Ltd. (Osaka, JP)
Filing Date:Feb 20, 2006
Application Number:11/884,686
Claims:1. A compound represented by the formula: ##STR00042## (wherein, R.sup.1 is hydrogen or lower alkyl; X is a single bond, a heteroatom group selected from 0, S, SO, SO.sub.2 and NH, or lower alkylene or lower alkenylene each may be intervened by the heteroatom group; R.sup.2 is optionally substituted aryl; R.sup.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.sup.4 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted aryl, optionally substituted aryl lower alkyl, optionally substituted aryloxy, optionally substituted heterocycle, optionally substituted heterocycle lower alkyl, optionally substituted heterocycleoxy, hydroxy, optionally substituted amino, optionally substituted phosphoric acid residue, aryl substituted with optionally substituted phosphoric acid residue, aralkyl substituted with optionally substituted phosphoric acid residue, hydroxy substituted with optionally substituted phosphoric acid residue, amino substituted with optionally substituted phosphoric acid residue or lower alkyl substituted with optionally substituted phosphoric acid residue (the lower alkyl may be intervened by a heteroatom group selected from group consisting O, S, SO, SO.sub.2, NR.sup.a (R.sup.a is hydrogen or lower alkyl), --N.dbd. and .dbd.N--)), or a pharmaceutically acceptable salt thereof.

2. A compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is hydrogen; X is lower alkylene; R.sup.2 is phenyl, or phenyl substituted with at least halogen; and R.sup.3 is hydrogen, halogen, hydroxy, lower alkyl, lower alkenyl, lower alkoxy, lower alkenyloxy or optionally substituted amino.

3. A pharmaceutical composition, containing a compound as defined in claim 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent.

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