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Serving hundreds of leading biopharmaceutical companies globally:

Citi
Daiichi Sankyo
Express Scripts
Cerilliant
Federal Trade Commission
Dow
Covington
Baxter
Johnson and Johnson

Generated: May 21, 2018

DrugPatentWatch Database Preview

Details for Patent: 5,665,720

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Title: Benzoxazinones as inhibitors of HIV reverse transcriptase
Abstract:Certain benzoxazinones are useful in the inhibition of HIV reverse transcriptase (including its resistant varieties), the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
Inventor(s): Young; Steven D. (Lansdale, PA), Britcher; Susan F. (Norristown, PA), Payne; Linda S. (Lansdale, PA), Tran; Lekhanh O. (West Chester, PA), Lumma, Jr.; William C. (Pennsburg, PA)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Filing Date:Jun 02, 1995
Application Number:08/458,529
Claims:1. A pharmaceutical composition comprising a compound of the formula ##STR82## wherein: X is halo,

X.sup.1 is trihalomethyl, or pentahaloethyl;

Z is O;

R is

(a) C.sub.1-8 alkyl, unsubstituted or substituted with A, and A is halo, C.sub.3-6 cycloalkyl, CN, hydroxy, C.sub.1-4 alkoxy, C.sub.2-4 alkynyl-C.sub.1-4 alkoxy, aryloxy, C.sub.1-4 alkylcarbonyl, nitro, di(C.sub.1-2 alkyl)amino, C.sub.1-4 alkylamino-C.sub.1-2 alkyl, heterocycle, or arylthio;

(b) C.sub.2-2 alkenyl, unsubstituted or substituted with

(i) A, or

(ii) aryl, unsubstituted or substituted with A;

(c) C.sub.2-5 alkynyl, unsubstituted or substituted with

(i) A, or

(ii) aryl, unsubstituted or substituted with A; or

(d) C.sub.3-4 cycloalkyl, unsubstituted or substituted with

(i) A, or

(ii) aryl, unsubstituted or substituted with A,

in admixture with a nucleoside analog having biological activity against HIV reverse transcriptase,

or a pharmaceutically acceptable salt of any of the above.

2. A pharmaceutical composition comprising the compound ##STR83## in admixture with the compound ##STR84## and, optionally, one or more of the HIV reverse transcriptase inhibitors selected from the group consisting of AZT, ddI and ddC,

or a pharmaceutically acceptable salt of any of the above.

3. A pharmaceutical composition comprising the compound ##STR85## in admixture with one or more HIV reverse transcriptase inhibitors selected from the group consisting of AZT, ddI and ddC,

or pharmaceutically acceptable salt of any of the above.

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Serving hundreds of leading biopharmaceutical companies globally:

Queensland Health
Chinese Patent Office
Dow
Express Scripts
Harvard Business School
Daiichi Sankyo
US Department of Justice
Federal Trade Commission
Colorcon

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