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Generated: July 25, 2017

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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), Payne; Linda S. (Lansdale, PA), Britcher; Susan F. (Norristown, PA), Tran; Lekhanh O. (West Chester, PA), Lumma, Jr.; William C. (Pennsburg, PA)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Application Number:08/815,780
Patent Claims: 1. A method of treating infection by HIV or of treating AIDS or ARC comprising administering to a mammal an effective amount of a compound of Formula I: ##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.2-4 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,

and one or more agent selected from the group consisting of: an AIDS antiviral, immunomodulator, antiinfective, vaccine, HIV protease inhibitor, and a nucleoside analog having biological activity against HIV reverse transcriptase.

2. A method of treating infection by HIV or of treating AIDS or ARC comprising administering to a mammal an effective amount of a compound of Formula: ##STR83## and one or more agent selected from the group consisting of: an AIDS antiviral, immunomodulator, antiinfective, vaccine, HIV protease inhibitor, and a nucleoside analog having biological activity against HIV reverse transcriptase.

3. A method of treating infection by HIV or of treating AIDS or ARC comprising administering to a mammal an effective amount of a compound of Formula I: ##STR84## 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.2-4 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;

an HIV protease inhibitor, and optionally, a nucleoside analog having biological activity against HIV reverse transcriptase or a pharmaceutically acceptable salt of any of the above.

4. A method of treating infection by HIV or of treating AIDS or ARC comprising administering to a mammal an effective amount of a compound of Formula I: ##STR85## 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.2-4 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;

a nucleoside analog having biological activity against HIV reverse transcriptase, and, optionally, an HIV protease inhibitor or a pharmaceutically acceptable salt of any of the above.

5. A method of treating infection by HIV or of treating AIDS or ARC comprising administering to a mammal an effective amount of a compound of Formula I: ##STR86## 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.2-4 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;

an HIV protease inhibitor, and a nucleoside analog having biological activity against HIV reverse transcriptase or a pharmaceutically acceptable salt of any of the above.

6. The method of treating infection by HIV or of treating AIDS or ARC as recited in claim 4 comprising administering to a mammal an effective amount of a compound of Formula: ##STR87## a HIV protease inhibitor, and a nucleoside analog having biological activity against HIV reverse transcriptase or a pharmaceutically acceptable salt of any of the above.
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