IP Library Granted Patent US 11,492,361
Granted Patent B2
US 11,492,361 · App. 16/948,873 · Granted Nov 8, 2022

Compounds useful in HIV therapy

Inventors: Richard M. Dunham (Research Triangle Park, NC); David Margolis (Chapel Hill, NC); Vincent Wing-Fai Tai (Research Triangle Park, NC); Jun Tang (Research Triangle Park, NC)
Assignees: GlaxoSmithKline Intellectual Property Development Limited; The University of North Carolina at Chapel Hill; ViiV Healthcare Company
C07D519/00A61P31/18
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Quick Facts
Patent No.
US 11,492,361
App. No.
16/948,873
Granted
Nov 8, 2022
Kind
B2
Abstract

The invention relates to compounds of Formula (I), salts thereof, combinations, pharmaceutical compositions thereof, as well as therapeutic methods of treatment and prevention.

Claims (41)

1. A compound represented by the Formula (I):

or a pharmaceutically acceptable salt or stereoisomer thereof, wherein:

R, R′, R″ and R′″ are each independently selected from H and CH 3 ;

X 1 and X 2 are each independently selected from the group consisting of O and S; and

L is a linker represented by the formula:

wherein:

Ar 12 and Ar 13 are each independently selected from (C 6 -C 14 )aryl;

Alk 3 is selected from:

and t and u are each independently selected from 1 to 12.

2. The compound according to claim 1 , wherein t and u are independently selected from 1 to 6.

3. The compound according to claim 2 , wherein t and u are independently selected from 1 to 4.

4. The compound according to claim 1 , wherein Alk 3 is:

5. The compound according to claim 4 , wherein Alk 3 is:

6. The compound according to claim 1 , wherein Ar 12 and Ar 13 are each Independently C 6-9 aryl.

7. The compound according to claim 6 , wherein Ar 12 and Ar 13 are each C 9 aryl.

8. A pharmaceutical composition comprising a compound according to claim 1 , or a pharmaceutically acceptable salt or stereoisomer thereof, and a pharmaceutically acceptable excipient.

9. The composition according to claim 8 , wherein said composition is adapted for parenteral administration.

10. A method of depleting latent HIV infected cells comprising administering to a subject a compound of claim 1 or a pharmaceutically acceptable salt or stereoisomer thereof.

11. A method of treating an HIV infection in a subject comprising administering to the subject a compound of claim 1 or a pharmaceutically acceptable salt or stereoisomer thereof.

12. A compound represented by the Formula (I):

or a pharmaceutically acceptable salt or stereoisomer thereof, wherein:

R, R′, R″ and R′″ are each independently selected from H and CH 3 ;

X 1 and X 2 are each independently selected from the group consisting of O and S; and

L is a linker represented by the formula:

wherein:

Ar 12 and Ar 13 are each independently selected from (C 6 -C 9 )aryl;

Alk 3 is selected from:

and t and u are each independently selected from 1 to 6.

13. The compound according to claim 12 , wherein Alk 3 is:

14. The compound according to claim 12 , wherein Ar 12 and Ar 13 are each C 9 aryl.

15. A pharmaceutical composition comprising a compound according to claim 12 , or a pharmaceutically acceptable salt or stereoisomer thereof, and a pharmaceutically acceptable excipient.

16. The composition according to claim 15 , wherein said composition is adapted for parenteral administration.

17. A method of depleting latent HIV infected cells comprising administering to a subject a compound of claim 12 or a pharmaceutically acceptable salt or stereoisomer thereof.

18. A method of treating an HIV infection in a subject comprising administering to the subject a compound of claim 12 or a pharmaceutically acceptable salt or stereoisomer thereof.

19. A combination comprising a compound according to claim 1 , a pharmaceutically acceptable salt or stereoisomer thereof and one or more pharmaceutical agents active against HIV.

20. A method of treating an HIV infection in a subject comprising administering to the subject a combination of claim 19 .

21. A method of depleting latent HIV infected cells comprising administering to a subject a combination of claim 19 .

22. A combination comprising a compound having the structure:

or a pharmaceutically acceptable salt thereof and one or more pharmaceutical agents active against HIV.

23. A method of treating an HIV infection in a subject comprising administering to the subject a combination of claim 22 .

24. A method of depleting latent HIV infected cells comprising administering to a subject a combination of claim 22 .

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 18, 2022
From: DE LA ROSA, MARTHA ALICIA; TAI, VINCENT WING-FAI; TANG, JUN; DUNHAM, RICHARD M.
To: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; VIIV HEALTHCARE COMPANY
Reel/Frame 060842/0281 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 18, 2022
From: MARGOLIS, DAVID
To: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL
Reel/Frame 060842/0363 →
Continuity (4)
Continuation 16897351 · Jun 10, 2020
Continuation 16621312
Provisional Application 62773563 · Nov 30, 2018
Related Publication 20210009609A1 · Jan 14, 2021