.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 5,811,423

« Back to Dashboard

Claims for Patent: 5,811,423

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.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc