IP Library Granted Patent US 12,365,674
Granted Patent B2
US 12,365,674 · App. 17/422,642 · Granted Jul 22, 2025

Inhibitors of histone deacetylase useful for the treatment or prevention of HIV infection

Inventors: Dane James Clausen (Rahway, NJ); Joseph A. Kozlowski (Princeton, NJ); Jian Liu (Edison, NJ); Scott E. Wolkenberg (Wyndmoor, PA); Wengsheng Yu (Edison, NJ)
Assignee: Merck Sharp & Dohme LLC
C07D413/14A61K31/422A61K31/4709A61K45/06A61P31/18C07D413/12C07D417/14
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Quick Facts
Patent No.
US 12,365,674
App. No.
17/422,642
Granted
Jul 22, 2025
Kind
B2
Abstract

The present invention relates to Compounds of Formula I and pharmaceutically acceptable salts or prodrug thereof, wherein R 1 , R 2 , R 3 , R 4 , X and A are as defined herein. The present invention also relates to compositions comprising at least one compound of Formula I, and methods of using the compounds of Formula I for treating or preventing HIV infection in a subject.

Claims (10)

1. A compound selected from:

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

3. A method for inhibiting histone deacetylase (HDAC) in a subject in need thereof which comprises administering to the subject an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

4. A method for treating an infection by HIV or for treating or delaying the onset or progression of AIDS in a subject in need thereof, which comprises administering to the subject an effective amount of compound of claim 1 , or a pharmaceutically acceptable salt thereof.

5. The pharmaceutical composition of claim 2 , further comprising one or more additional therapeutic agents selected from lamivudine, abacavir, ritonavir, darunavir, atazanavir, emtricitabine, tenofovir, rilpivirine, doravirine, EFdA and lopinavir.

6. The method of claim 4 , further comprising administering to the subject one or more additional therapeutic agents selected from lamivudine, abacavir, ritonavir, darunavir, atazanavir, emtricitabine, tenofovir, rilpivirine, doravirine, EFdA and lopinavir, wherein the amounts administered are together effective to treat infection by HIV or to treat, prevent or delay the onset or progression of AIDS.

7. The pharmaceutical composition of claim 2 , wherein the composition is present in a tablet or capsule.

8. The pharmaceutical composition of claim 2 , wherein the composition is present in a liquid form preparation.

9. A pharmaceutically acceptable prodrug of the compound of claim 1 .

Assignments (2)
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 Jul 13, 2021
From: CLAUSEN, DANE JAMES; KOZLOWSKI, JOSEPH A.; LIU, JIAN; WOLKENBERG, SCOTT E.; YU, WENSHENG
To: MERCK SHARP & DOHME CORP.
Reel/Frame 056840/0870 →