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|Title:||Substituted 10-hydroxy-9,11-dioxo-2,3,4a,5,9,11,13,13a-octahydro-1h-pyrido[1,2-.alpha- .]pyrrolo[1',2':3,4]imidazo[1,2-d]pyrazine-8-carboxamides|
|Abstract:||The present invention is directed to a class of substituted 10-hydroxy-9,11-dioxo-2,3,4a,5,9,11,13,13a-octahydro-1H-pyrido[1,2-a]pyrr- olo[1',2':3,4]imidazo[1,2-d]pyrazine-8-carboxamides useful as anti-HIV agents. The compounds have the formula (I-1-1): ##STR00001## wherein ring A is an optionally substituted hexahydro-1H-pyrrolo[1,2-c]-imidazole; R.sup.14 and R.sup.X are independently hydrogen or optionally substituted lower alkyl; R.sup.3 is selected from various groups; R.sup.1 is hydrogen or lower alkyl; R is halogen; m is 0, 1, 2 or 3; or a pharmaceutically acceptable salt thereof.|
|Inventor(s):||Johns; Brian A. (Research Triangle Park, NC), Kawasuji; Takashi (Osaka, JP), Taishi; Teruhiko (Osaka, JP), Taoda; Yoshiyuki (Osaka, JP)|
|Assignee:||Shionogi & Co., Ltd. (Osaka, JP) ViiV Healthcare Company (Research Triangle Park, NC)|
|Filing Date:||Feb 08, 2013|
|Claims:||1. A compound selected from the group consisting of: (4aR,13 aS)--N-[(2,4-Difluorophenyl)methyl]-10-hydroxy-9,11-dioxo-2,3,4a,5,9,11,1- 3,13a-octahydro-1H-pyrido[1,2-a]pyrrolo[1',2':3,4]imidazo[1,2-d]pyrazine-8- -carboxamide; (4aS,13 aR)--N-[(2,4-Difluorophenyl)methyl]-10-hydroxy-9,11-dioxo-2,3,4a,5,9,11,1- 3,13a-octahydro-1H-pyrido[1,2-a]pyrrolo[1',2':3,4]imidazo[1,2-c]pyrazine-8- -carboxamide; and (4aS,13 aR)--N-[(4-Fluorophenyl)methyl]-10-hydroxy-9,11-dioxo-2,3,4a,5,9,11,13,13- a-octahydro-1H-pyrido[1,2-a]pyrrolo[1',2':3,4]imidazo[1,2-d]pyrazine-8-car- boxamide; enantiomers thereof diastereomers thereof mixtures of enantiomers thereof mixtures of diastereomers thereof mixtures of enantiomers and diastereomers thereof and pharmaceutically acceptable salts thereof. |
2. A compound according to claim 1 wherein the pharmaceutically acceptable salt is a sodium salt.
3. A compound of the formula ##STR00210## or a pharmaceutically acceptable salt thereof.
4. A pharmaceutical composition comprising a compound of the formula ##STR00211## or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier or diluent.
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