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Details for Patent: 9,273,065

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Details for Patent: 9,273,065

Title:Substituted pyrido[1',2':4,5]pyrazino[1,2-a]pyrimidines as HIV integrase inhibitors
Abstract: The present invention is directed to a class of substituted pyrido[1'2':4,5]pyrazino[1,2-a]-pyrimidines useful as intermediates in the production of anti-HIV agents. The compounds have the formula (I-24b): ##STR00001## wherein R.sup.e is one or two halogen; R.sup.z is C.sub.1-8alkyl; R.sup.z is hydrogen, C.sub.3-6cycloalkyl, heterocyclyl, or C.sub.1-8alkyl optionally substituted with hydroxy, C.sub.3-6cycloalkyl, alkoxy, heterocyclyl, heteroaryl, C.sub.6-14aryl, or amino, wherein said amino may be optionally substituted with --C(O)C.sub.1-8alkyl or C.sub.1-8alkyl; and P.sup.1 is C.sub.6-14arylC.sub.1-8alkyl; 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:Apr 30, 2015
Application Number:14/700,679
Claims:1. A compound of formula (I-24b) ##STR00211## wherein: R.sup.e is one or two halogen; R.sup.z is C.sub.1-8alkyl; R.sup.z1 is hydrogen, C.sub.3-6cycloalkyl, heterocyclyl, or C.sub.1-8alkyl optionally substituted with hydroxy, C.sub.3-6cycloalkyl, alkoxy, heterocyclyl, heteroaryl, C.sub.6-14aryl, or amino, wherein said amino may be optionally substituted with --C(O)C.sub.1-8alkyl or C.sub.1-8alkyl; and P.sup.1 is C.sub.6-14arylC.sub.1-8alkyl; or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1, wherein R.sup.e is one or two fluorine.

3. The compound of claim 1, wherein R.sup.z is methyl.

4. The compound of claim 1, wherein R.sup.z1 is C.sub.3-6cycloalkyl.

5. The compound of claim 1, wherein R.sup.z1 is C.sub.3cycloalkyl.

6. A compound which is: ##STR00212##

7. A process for the preparation of a compound of formula (I-24b) ##STR00213## wherein R.sup.e is one or two halogen; R.sup.z is C.sub.1-8alkyl; R.sup.z1 is hydrogen, C.sub.3-6cycloalkyl, heterocyclyl, or C.sub.1-8alkyl optionally substituted with hydroxy, C.sub.3-6cycloalkyl, alkoxy, heterocyclyl, heteroaryl, C.sub.6-14aryl, or amino, wherein said amino may be optionally substituted with --C(O)C.sub.1-8alkyl or C.sub.1-8alkyl; and P.sup.1 is C.sub.6-14arylC.sub.1-8alkyl; comprising condensing a compound of the formula ##STR00214## wherein R.sup.e is one or two halogen; R.sup.50 is C.sub.1-8alkyl; and P.sup.1 is C.sub.6-14arylC.sub.1-8alkyl; with a compound of the formula ##STR00215## wherein R.sup.z is C.sub.1-8alkyl; R.sup.z1 is hydrogen, C.sub.3-6cycloalkyl, heterocyclyl, or C.sub.1-8alkyl optionally substituted with hydroxy, C.sub.3-6cycloalkyl, alkoxy, heterocyclyl, heteroaryl, C.sub.6-14aryl, or amino, wherein said amino may be optionally substituted with --C(O)C.sub.1-8alkyl or C.sub.1-8alkyl; to form a compound of the formula (I-24b).

8. The process of claim 7, further comprising a step of replacing the C.sub.6-14arylC.sub.1-8alkyl of P.sup.1 with hydrogen.
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