IP Library Granted Patent US 9,469,634
Granted Patent B2
US 9,469,634 · App. 14/047,515 · Granted Oct 18, 2016

Non-nucleoside reverse transcriptase inhibitors

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Quick Facts
Patent No.
US 9,469,634
App. No.
14/047,515
Granted
Oct 18, 2016
Kind
B2
Abstract

Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R 1 , R 2 , R E , L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Claims (14)

1. A compound

2. A pharmaceutical composition comprising an effective amount of the compound according to claim 1 and a pharmaceutically acceptable carrier.

3. The pharmaceutical composition of claim 2 further comprising a second HIV antiviral agent selected from the group consisting of HIV protease inhibitors, HIV integrase inhibitors, non-nucleoside HIV reverse transcriptase inhibitors, nucleoside HIV reverse transcriptase inhibitors, HIV fusion inhibitors, and HIV entry inhibitors.

4. A method for the treatment of infection by HIV in a subject in need thereof which comprises administering to the subject an effective amount of the compound according to claim 1 .

5. The method of claim 4 further comprising administering to the subject a second HIV antiviral agent selected from the group consisting of HIV protease inhibitors, HIV integrase inhibitors, non-nucleoside HIV reverse transcriptase inhibitors, nucleoside HIV reverse transcriptase inhibitors, HIV fusion inhibitors, and HIV entry inhibitors.

6. A method for the treatment of AIDS in a subject in need thereof which comprises administering to the subject an effective amount of the compound according to claim 1 .

7. The method of claim 6 further comprising administering to the subject a second HIV antiviral agent selected from the group consisting of HIV protease inhibitors, HIV integrase inhibitors, non-nucleoside HIV reverse transcriptase inhibitors, nucleoside HIV reverse transcriptase inhibitors, HIV fusion inhibitors, and HIV entry inhibitors.

8. A compound that is a pharmaceutically acceptable salt of

9. A pharmaceutical composition comprising an effective amount of the compound according to claim 8 and a pharmaceutically acceptable carrier.

10. The pharmaceutical composition of claim 9 further comprising a second HIV antiviral agent selected from the group consisting of HIV protease inhibitors, HIV integrase inhibitors, non-nucleoside HIV reverse transcriptase inhibitors, nucleoside HIV reverse transcriptase inhibitors, HIV fusion inhibitors, and HIV entry inhibitors.

11. A method for the treatment of infection by HIV in a subject in need thereof which comprises administering to the subject an effective amount of the compound according to claim 8 .

12. The method of claim 11 further comprising administering to the subject a second HIV antiviral agent selected from the group consisting of HIV protease inhibitors, HIV integrase inhibitors, non-nucleoside HIV reverse transcriptase inhibitors, nucleoside HIV reverse transcriptase inhibitors, HIV fusion inhibitors, and HIV entry inhibitors.

13. A method for the treatment of AIDS in a subject in need thereof which comprises administering to the subject an effective amount of the compound according to claim 8 .

14. The method of claim 13 further comprising administering to the subject a second HIV antiviral agent selected from the group consisting of HIV protease inhibitors, HIV integrase inhibitors, non-nucleoside HIV reverse transcriptase inhibitors, nucleoside HIV reverse transcriptase inhibitors, HIV fusion inhibitors, and HIV entry inhibitors.

Assignments (4)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 23, 2014
From: ARRINGTON, KENNETH L.; BURGEY, CHRISTOPHER; GILFILLAN, ROBERT; PATEL, MEHUL; HAN, YONGXIN
To: MERCK SHARP & DOHME CORP.
Reel/Frame 033799/0932 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 23, 2014
From: LI, CHUN SING; LUO, YUNFU; LEI, ZHIYU; LI, YAOZONG
To: WUXI APPTEC (SHANGHAI) CO., LTD.
Reel/Frame 033800/0297 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 23, 2014
From: WUXI APPTEC (SHANGHAI) CO., LTD.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 033800/0708 →