IP Library Granted Patent US 11,311,544
Granted Patent B2
US 11,311,544 · App. 17/393,553 · Granted Apr 26, 2022

Treatment of congenital adrenal hyperplasia

Inventor: Dimitri E. Grigoriadis (San Diego, CA)
Assignee: Neurocrine Biosciences, Inc.
A61K31/519A61K31/427A61K31/4985
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Quick Facts
Patent No.
US 11,311,544
App. No.
17/393,553
Granted
Apr 26, 2022
Kind
B2
Abstract

CRF 1 receptor antagonists have the potential to directly inhibit ACTH release in patients with CAH and thereby allow normalization of androgen production while using lower, more physiologic doses of hydrocortisone, and thus reducing treatment-associated side effects.

Claims (28)

1. A method of treating Congenital Adrenal Hyperplasia (CAH), said method comprising administering to a subject in need thereof already being treated with a glucocortocoid, an effective amount of a CRF 1 receptor antagonist, wherein the CRF 1 receptor antagonist is 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-(2-propyn-1-yl)-2-thiazolamine (SSR-125543), or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the glucocorticoid is hydrocortisone.

3. The method of claim 1 , wherein the glucocorticoid is prednisone.

4. The method of claim 1 , wherein the glucocorticoid is prednisolone.

5. The method of claim 1 , wherein the glucocorticoid is dexamethasone.

6. The method of claim 1 , further comprising administering a salt-wasting, mineralocorticoid to the subject.

7. The method of claim 6 , wherein the salt-wasting, mineralocorticoid is fludrocortisone.

8. The method of claim 1 , wherein the dose of the glucocorticoid is decreased by 10% or more following administration of the CRF 1 receptor antagonist.

9. The method of claim 1 , wherein the dose of the glucocorticoid is decreased by 15% or more following administration of the CRF 1 receptor antagonist.

10. The method of claim 1 , wherein the dose of the glucocorticoid is decreased by 20% or more following administration of the CRF 1 receptor antagonist.

11. The method of claim 1 , wherein the dose of the glucocorticoid is decreased by 30% or more following administration of the CRF 1 receptor antagonist.

12. The method of claim 1 , wherein the dose of the glucocorticoid is decreased by 40% or more following administration of the CRF 1 receptor antagonist.

13. The method of claim 1 , wherein the dose of the glucocorticoid is decreased by 50% or more following administration of the CRF 1 receptor antagonist.

14. The method of claim 1 , wherein the CAH is classical CAH.

15. The method of claim 1 , wherein the CAH is caused by 21-α hydroxylase deficiency.

16. The method of claim 1 , wherein the CAH is caused by 11β-hydroxylase deficiency.

17. The method of claim 1 , wherein the subject has a mutation in the CYP21A2 gene located on chromosome 6p21.

18. The method of claim 1 , wherein the subject does not have a mutation of the 11β-hydroxylase gene CYP11B1 (11β-OH CAH).

19. The method of claim 1 , wherein the CRF 1 receptor antagonist is administered at bedtime.

20. The method of claim 1 , wherein the CRF 1 receptor antagonist is 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-(2-propyn-1-yl)-2-thiazolamine (S SR-125543).

21. The method of claim 1 , wherein 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-(2-propyn-1-yl)-2-thiazolamine (SSR-125543), or a pharmaceutically acceptable salt thereof, is administered in the form of a liquid formulation.

22. The method of claim 1 , wherein 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-(2-propyn-1-yl)-2-thiazolamine (SSR-125543), or a pharmaceutically acceptable salt thereof, is administered in the form of a solid formulation.

23. The method of claim 1 , wherein 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-(2-propyn-1-yl)-2-thiazolamine (SSR-125543), or a pharmaceutically acceptable salt thereof, is administered in the form of a semi-solid formulation.

24. The method of claim 1 , wherein 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-(2-propyn-1-yl)-2-thiazolamine (SSR-125543), or a pharmaceutically acceptable salt thereof, is administered in the form of a tablet, powder, granule or capsule.

25. The method of claim 24 , wherein 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-(2-propyn-1-yl)-2-thiazolamine (SSR-125543), or a pharmaceutically acceptable salt thereof, is administered in the form of a capsule.

26. The method of claim 1 , wherein the subject is an adult.

27. The method of claim 1 , wherein the subject is a child.

28. The method of claim 1 , wherein the subject is a female.

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 Aug 5, 2021
From: GRIGORIADIS, DIMITRI E.
To: NEUROCRINE BIOSCIENCES, INC.
Reel/Frame 057086/0747 →
Continuity (7)
Continuation 17074845 · Oct 20, 2020
Continuation 16227127 · Dec 20, 2018
Continuation 15113362
Provisional Application 61929941 · Jan 21, 2014
Provisional Application 61981033 · Apr 17, 2014
Provisional Application 62069155 · Oct 27, 2014
Related Publication 20210361659A1 · Nov 25, 2021
Cited By (3)
US 12,383,536 US 12,582,634 US 12,686,680