IP Library Granted Patent US 11,358,711
Granted Patent B2
US 11,358,711 · App. 17/025,371 · Granted Jun 14, 2022

Tetracyclic heterocycle compounds useful as HIV integrase inhibitors

Inventors: Thomas H. Graham (Quincy, MA); Tao Yu (Edison, NJ); Yonglian Zhang (Metuchen, NJ); John A. McCauley (Maple Glen, PA)
Assignee: Merck Sharp & Dohme Corp.
B64C27/48A61K31/18A61K31/407A61K31/4188A61K31/4439A61K31/4985A61K31/519A61K31/5365A61K31/553A61K31/7076A61P31/18B64C11/08C07D498/16C07D498/22A61K2300/00C12N15/1132C12N2740/16011
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Quick Facts
Patent No.
US 11,358,711
App. No.
17/025,371
Granted
Jun 14, 2022
Kind
B2
Abstract

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

Claims (28)

1. A method for the treatment of infection by HIV or for the treatment, or delay in the onset or progression of AIDS in a subject in need thereof, which comprises administering to the subject an effective amount of a compound having the structure:

or a pharmaceutically acceptable salt thereof, and doravirine, or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 comprising

or a pharmaceutically acceptable salt thereof, and doravirine, or a pharmaceutically acceptable salt thereof.

3. The method of claim 1 comprising

or a pharmaceutically acceptable salt thereof, and doravirine, or a pharmaceutically acceptable salt thereof.

4. The method of claim 1 comprising

or a pharmaceutically acceptable salt thereof, and doravirine, or a pharmaceutically acceptable salt thereof.

5. The method of claim 1 comprising

or a pharmaceutically acceptable salt thereof, and doravirine, or a pharmaceutically acceptable salt thereof.

6. The method of claim 1 comprising

or a pharmaceutically acceptable salt thereof, and doravirine, or a pharmaceutically acceptable salt thereof.

7. The method of claim 1 comprising

or a pharmaceutically acceptable salt thereof, and doravirine, or a pharmaceutically acceptable salt thereof.

8. A method for the treatment of infection by HIV or for the treatment, or delay in the onset or progression of AIDS in a subject in need thereof, which comprises administering to the subject an effective amount of a compound having the structure:

or a pharmaceutically acceptable salt thereof, and 4′-ethynyl-2-fluoro-2′-deoxyadenosine, or a pharmaceutically acceptable salt thereof.

9. The method of claim 8 comprising

or a pharmaceutically acceptable salt thereof, and 4′-ethynyl-2-fluoro-2′-deoxyadenosine, or a pharmaceutically acceptable salt thereof.

10. The method of claim 8 comprising

or a pharmaceutically acceptable salt thereof, and 4′-ethynyl-2-fluoro-2′-deoxyadenosine, or a pharmaceutically acceptable salt thereof.

11. The method of claim 8 comprising

or a pharmaceutically acceptable salt thereof, and 4′-ethynyl-2-fluoro-2′-deoxyadenosine, or a pharmaceutically acceptable salt thereof.

12. The method of claim 8 comprising

or a pharmaceutically acceptable salt thereof, and 4′-ethynyl-2-fluoro-2′-deoxyadenosine, or a pharmaceutically acceptable salt thereof.

13. The method of claim 8 comprising

or a pharmaceutically acceptable salt thereof, and 4′-ethynyl-2-fluoro-2′-deoxyadenosine, or a pharmaceutically acceptable salt thereof.

14. The method of claim 8 comprising

or a pharmaceutically acceptable salt thereof, and 4′-ethynyl-2-fluoro-2′-deoxyadenosine, or a pharmaceutically acceptable salt thereof.

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 Sep 18, 2020
From: GRAHAM, THOMAS H.; YU, TAO; ZHANG, YONGLIAN; MCCAULEY, JOHN A.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 053818/0383 →