IP Library › Patent Application 15113362
Patent Application
App. No. 15/113,362

CRF1 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF CONGENITAL ADRENAL HYPERPLASIA

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Patent No.
US None
App. No.
15/113,362
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 (21)

1 . A method for treating Congenital Adrenal Hyperplasia (CAH) by administering to a subject in need thereof a CRF 1 receptor antagonist having a dissociation half-life in excess of 30 minutes.

2 . The method of claim 1 wherein the CRF 1 receptor antagonist has a dissociation half-life in excess of 40 minutes.

3 . The method of claim 1 wherein the CRF 1 receptor antagonist has a dissociation half-life in excess of 50 minutes.

4 . The method of claim 1 wherein the CRF 1 receptor antagonist is Compound I (NBI-77860; 2,5-dimethyl-3-[2-methyl-4-(methyloxy)phenyl]-N-[(1S)-1-(3-methyl-1,2,4-oxadiazol-5-yl)propyl]pyrazolo[1,5-a]pyrimidin-7-amine).

5 . The method of claim 1 wherein the CRF 1 receptor antagonist is NBI-30775, NBI-34041, SSR-126374, SSR-125543, antalarmin (N-butyl-N-ethyl-2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[3,2-e]pyrimidin-4-amine), or DMP904.

6 . The method of any one of claims 1 - 5 wherein the CRF 1 receptor antagonist is administered at bedtime.

7 . The method of any one of claims 1 - 5 wherein the CRF 1 receptor antagonist is administered at or before the expected circadian release of ACTH.

8 . The method of claim 7 wherein the CRF 1 receptor antagonist is administered 3-4 hours before the expected circadian release of ACTH.

9 . A method for reducing 17-OHP and ACTH levels in a subject who has Congenital Adrenal Hyperplasia (CAH), said method comprising administering to the subject a CRF 1 receptor antagonist at bedtime.

10 . The method of claim 9 , wherein the CRF 1 receptor antagonist is administered at or before the expected circadian release of ACTH.

11 . The method of claim 9 , wherein the CRF 1 receptor antagonist is administered 3-4 hours before the expected circadian release of ACTH.

12 . The method of any one of claims 9 - 11 , wherein the CRF 1 receptor antagonist is Compound I (NBI-77860; 2,5-dimethyl-3-[2-methyl-4-(methyloxy)phenyl]-N-[(1S)-1-(3-methyl-1,2,4-oxadiazol-5-yl)propyl]pyrazolo[1,5-a]pyrimidin-7-amine).

13 . The method of any one of claims 9 - 11 , wherein the CRF 1 receptor antagonist is NBI-30775, NBI-34041, SSR-126374, SSR-125543, antalarmin (N-butyl-N-ethyl-2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[3,2-e]pyrimidin-4-amine), or DMP904.

14 . A CRF 1 receptor antagonist for use in treating Congenital Adrenal Hyperplasia (CAH), wherein the CRF 1 receptor antagonist has a dissociation half-life in excess of 30 minutes.

15 . The CRF 1 receptor antagonist of claim 14 , wherein the CRF 1 receptor antagonist has a dissociation half-life in excess of 40 minutes.

16 . The CRF 1 receptor antagonist of claim 14 , wherein the CRF 1 receptor antagonist has a dissociation half-life in excess of 50 minutes.

17 . The CRF 1 receptor antagonist of claim 14 , wherein the CRF 1 receptor antagonist is Compound I (NBI-77860; 2,5-dimethyl-3-[2-methyl-4-(methyloxy)phenyl]-N-[(1S)-1-(3-methyl-1,2,4-oxadiazol-5-yl)propyl]pyrazolo[1,5-a]pyrimidin-7-amine).

18 . The CRF 1 receptor antagonist of claim 14 , wherein the CRF 1 receptor antagonist is NBI-30775, NBI-34041, SSR-126374, SSR-125543, antalarmin (N-butyl-N-ethyl-2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[3,2-e]pyrimidin-4-amine), or DMP904.

19 . The CRF 1 receptor antagonist of any one of claims 14 - 18 , wherein the CRF 1 receptor antagonist is suitable for administration at bedtime.

20 . The CRF 1 receptor antagonist of any one of claims 14 - 18 , wherein the CRF 1 receptor antagonist is suitable for administration at or before the expected circadian release of ACTH.

21 . The CRF 1 receptor antagonist of any one of claims 14 - 18 , wherein the CRF 1 receptor antagonist is suitable for administration 3-4 hours before the expected circadian release of ACTH.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 16, 2019
From: GRIGORIADIS, DIMITRI E.
To: NEUROCRINE BIOSCIENCES, INC.
Reel/Frame 048034/0449 →