IP Library › Granted Patent US 12,304,911
Granted Patent B2
US 12,304,911 · App. 18/207,807 · Granted May 20, 2025

Substituted pyrido[2,1-a]isoquinolines as VMAT2 inhibitors

Inventors: Nicole Harriott (San Diego, CA); Nicholas Pagano (San Diego, CA); Byron A. Boon (San Diego, CA)
Assignee: Neurocrine Biosciences, Inc.
C07D471/04A61P25/18
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Quick Facts
Patent No.
US 12,304,911
App. No.
18/207,807
Granted
May 20, 2025
Kind
B2
Abstract

This disclosure relates generally to VMAT2 inhibitor compounds of Formula (Ia): and pharmaceutically acceptable salts thereof, as well as compositions and methods related thereto.

Claims (42)

1. A method for treating a neurological disease, a neurological disorder, a psychiatric disease, or a psychiatric disorder in a subject in need thereof, wherein the method comprises administering to the subject a compound of Formula (Ia):

or a pharmaceutically acceptable salt thereof;

wherein:

R 1 is:

wherein the neurological disease, the neurological disorder, the psychiatric disease, or the psychiatric disorder is selected from the group consisting of:

schizophrenia and schizoaffective disorder.

2. The method according to claim 1 , wherein the neurological disease, the neurological disorder, the psychiatric disease, or the psychiatric disorder is schizophrenia.

3. The method according to claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

4. The method according to claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

5. The method according to claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

6. The method according to claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

7. The method according to claim 2 , wherein the method comprises using the compound in adjunctive therapy.

8. The method according to claim 7 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

9. The method according to claim 7 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

10. The method according to claim 7 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

11. The method according to claim 7 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

12. The method according to claim 1 , wherein the neurological disease, the neurological disorder, the psychiatric disease, or the psychiatric disorder is schizoaffective disorder.

13. The method according to claim 12 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

14. The method according to claim 12 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

15. The method according to claim 12 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

16. The method according to claim 12 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

17. The method according to claim 12 , wherein the method comprises using the compound in adjunctive therapy.

18. The method according to claim 17 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

19. The method according to claim 17 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

20. The method according to claim 17 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

21. The method according to claim 17 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

Assignments (2)
CONFIRMATORY GRANT OF SECURITY INTEREST IN UNITED STATES PATENTS Recorded May 26, 2026
From: NEUROCRINE BIOSCIENCES, INC.
To: JPMORGAN CHASE BANK, N.A.
Reel/Frame 075670/0001 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 13, 2023
From: HARRIOTT, NICOLE; PAGANO, NICHOLAS; BOON, BYRON A.
To: NEUROCRINE BIOSCIENCES, INC.
Reel/Frame 063930/0106 →
Continuity (4)
Continuation 18096073 · Jan 12, 2023
Continuation PCTUS2022021080 · Mar 21, 2022
Provisional Application 63164135 · Mar 22, 2021
Related Publication 20240010647A1 · Jan 11, 2024
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