IP Library Granted Patent US 12,071,414
Granted Patent B2
US 12,071,414 · App. 18/309,634 · Granted Aug 27, 2024

Apelin receptor agonists and methods of use thereof

Inventors: Layton H. Smith (Orlando, FL); Anthony B. Pinkerton (Rancho Santa Fe, CA); Paul Hershberger (Satellite Beach, FL); Patrick Maloney (Orlando, FL); Danielle McAnally (Gainesville, FL)
Assignee: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
C07D277/82A61P3/00A61P9/00C07D263/58C07D513/04
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Quick Facts
Patent No.
US 12,071,414
App. No.
18/309,634
Granted
Aug 27, 2024
Kind
B2
Abstract

Provided herein are agonists of the apelin receptor for the treatment of disease. The compounds disclosed herein are useful for the treatment of a range of cardiovascular, renal and metabolic conditions.

Claims (34)

1. A compound of formula:

or a pharmaceutically acceptable salt thereof,

wherein:

A is selected from the group consisting of substituted phenoxy and heteroaryl-oxy;

R 2 and R 3 are each independently selected from the group consisting of C 1 -C 6 haloalkyl, C 1 -C 6 haloalkoxy, optionally substituted C 1 -C 6 alkyl, and optionally substituted C 1 -C 6 alkoxy;

each R 5 -R 7 is independently selected from the group consisting of hydrogen, halogen, —CN, —C(O)—N(R 10 )—R 11 , —C(O)—O—R 12 , —SO 2 R 13 , C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted C 1 -C 6 alkoxy, C 1 -C 6 haloalkyl, C 1 -C 6 haloalkoxy, optionally substituted phenyl, and optionally substituted 5- or 6-membered heteroaryl;

each R 10 -R 12 is independently selected from the group consisting of hydrogen, optionally substituted C 1 -C 6 alkyl, optionally substituted C 3 -C 8 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted C 1 -C 6 alkoxy, C 1 -C 6 haloalkyl, C 1 -C 6 haloalkoxy, optionally substituted phenyl, optionally substituted amino, and optionally substituted 5- or 6-membered heteroaryl; and

R 13 is optionally substituted C 1 -C 6 alkyl, optionally substituted C 3 -C 8 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted C 1 -C 6 alkoxy, C 1 -C 6 haloalkyl, C 1 -C 6 haloalkoxy, optionally substituted phenyl, optionally substituted amino, or optionally substituted 5- or 6-membered heteroaryl.

2. The compound of claim 1 , wherein A is substituted phenoxy.

3. The compound of claim 2 , wherein R 2 and R 3 are each independently selected from the group consisting of C 1 -C 6 haloalkoxy and optionally substituted C 1 -C 6 alkoxy.

4. The compound of claim 3 , wherein R 2 and R 3 are each independently optionally substituted C 1 -C 6 alkoxy.

5. The compound of claim 4 , wherein R 2 and R 3 are each independently C 1 -C 6 alkoxy.

6. The compound of claim 5 , wherein R 2 and R 3 are each methoxy.

7. The compound of claim 6 , wherein R 5 and R 6 are each hydrogen.

8. The compound of claim 7 , wherein R 7 is —CN or —SO 2 R 13 ; and R 13 is optionally substituted C 1 -C 6 alkyl, optionally substituted C 3 -C 8 cycloalkyl, optionally substituted amino, or optionally substituted 5- or 6-membered heteroaryl.

9. The compound of claim 6 , wherein R 6 and R 7 are each hydrogen.

10. The compound of claim 9 , wherein R 5 is —CN or —SO 2 R 13 ; and R 13 is optionally substituted C 1 -C 6 alkyl, optionally substituted C 3 -C 8 cycloalkyl, optionally substituted amino, or optionally substituted 5- or 6-membered heteroaryl.

11. A compound of formula:

or a pharmaceutically acceptable salt thereof,

wherein:

A is selected from the group consisting of substituted phenoxy and heteroaryl-oxy;

R 1 and R 2 are each independently selected from the group consisting of C 1 -C 6 haloalkyl, C 1 -C 6 haloalkoxy, optionally substituted C 1 -C 6 alkyl, and optionally substituted C 1 -C 6 alkoxy;

each R 5 -R 7 is independently selected from the group consisting of hydrogen, halogen, —CN, —C(O)—N(R 10 )—R 11 , —C(O)—O—R 12 , —SO 2 R 13 , C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted C 1 -C 6 alkoxy, C 1 -C 6 haloalkyl, C 1 -C 6 haloalkoxy, optionally substituted phenyl, and optionally substituted 5- or 6-membered heteroaryl;

each R 10 -R 12 is independently selected from the group consisting of hydrogen, optionally substituted C 1 -C 6 alkyl, optionally substituted C 3 -C 8 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted C 1 -C 6 alkoxy, C 1 -C 6 haloalkyl, C 1 -C 6 haloalkoxy, optionally substituted phenyl, optionally substituted amino, and optionally substituted 5- or 6-membered heteroaryl; and

R 13 is optionally substituted C 1 -C 6 alkyl, optionally substituted C 3 -C 8 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted C 1 -C 6 alkoxy, C 1 -C 6 haloalkyl, C 1 -C 6 haloalkoxy, optionally substituted phenyl, optionally substituted amino, or optionally substituted 5- or 6-membered heteroaryl.

12. The compound of claim 11 , wherein A is substituted phenoxy.

13. The compound of claim 12 , wherein R 1 and R 2 are each independently selected from the group consisting of C 1 -C 6 haloalkoxy and optionally substituted C 1 -C 6 alkoxy.

14. The compound of claim 13 , wherein R 1 and R 2 are each independently optionally substituted C 1 -C 6 alkoxy.

15. The compound of claim 14 , wherein R 1 and R 2 are each independently C 1 -C 6 alkoxy.

16. The compound of claim 15 , wherein R 1 and R 2 are each methoxy.

17. The compound of claim 16 , wherein R 5 and R 6 are each hydrogen.

18. The compound of claim 17 , wherein R 7 is —CN or —SO 2 R 13 ; and R 13 is optionally substituted C 1 -C 6 alkyl, optionally substituted C 3 -C 8 cycloalkyl, optionally substituted amino, or optionally substituted 5- or 6-membered heteroaryl.

19. The compound of claim 16 , wherein R 6 and R 7 are each hydrogen.

20. The compound of claim 19 , wherein R 5 is —CN or —SO 2 R 13 ; and R 13 is optionally substituted C 1 -C 6 alkyl, optionally substituted C 3 -C 8 cycloalkyl, optionally substituted amino, or optionally substituted 5- or 6-membered heteroaryl.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 10, 2023
From: SMITH, LAYTON H.; PINKERTON, ANTHONY B.; HERSHBERGER, PAUL; MALONEY, PATRICK; MCANALLY, DANIELLE
To: SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTE
Reel/Frame 063607/0347 →
CHANGE OF NAME Recorded May 10, 2023
From: SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTE
To: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
Reel/Frame 063621/0644 →
Continuity (4)
Continuation 16869307 · May 7, 2020
Continuation 15568208
Provisional Application 62154025 · Apr 28, 2015
Related Publication 20230339872A1 · Oct 26, 2023