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Claims for Patent: 5,519,021

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Claims for Patent: 5,519,021

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)
Application Number:08/460,026
Patent Claims: 1. A compound of the formula: ##STR79## 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, unsubstimted or substituted with

(i) A, or

(ii) aryl, unsubstituted or substituted with A,

or pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition useful for inhibiting HIV reverse transcription, comprising an effective amount of a compound of Formula II, ##STR80## and a pharmaceutically acceptable carder, wherein X is halo;

X.sup.1 is trihalomethyl; pentahaloethyl;

Z is O;

R is

(a) C.sub.1-8 alkyl, unsubstimted 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, unsubstimted or substituted with

(i) A, or

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

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

(i) A, or

(ii) aryl, unsubstimted or substituted with A,

or pharmaceutically acceptable salt thereof.

3. A compound, which is

(-) 6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxa zin-2-one,

(-) 6-chloro-4-phenylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2 -one,

(+/-) 6-chloro-4-(2-cyanophenyl)ethynyl-4-(1,1,1-trifluoromethyl)-1,4-dihydro-2H -3,1

(+/-) 4-(1-chloro-1,1-difluoromethyl)-4-(2-phenylethynyl)-6-chloro-1,4-dihydro-2 H-3,1-benzoxazin-2-one, or

(+/-) 4-(2-[dimethylaminomethyl]ethynyl)-4-trifluoromethyl-6-chloro-1,4-dihydro- 2H-3,1-benzoxazin-2-one, or a pharmaceutically acceptable salt thereof.

4. A pharmaceutical composition useful for inhibiting HIV reverse transcriptase, comprising an effective amount of a compound as in any of claims 1 or 3, and a pharmaceutically acceptable carrier.

5. A pharmaceutical composition useful for treating infection by HIV or for treating AIDS or ARC, comprising an effective amount of a compound of claim 1, 2 or 3, and a pharmaceutically acceptable carrier.
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