IP Library Granted Patent US 11,304,950
Granted Patent B2
US 11,304,950 · App. 17/081,694 · Granted Apr 19, 2022

Methods for treating testicular and ovarian adrenal rest tumors

Inventors: Alexis Howerton (San Francisco, CA); Hal Gerber (San Francisco, CA)
Assignee: SPRUCE BIOSCIENCES, INC.
A61K31/519A61K9/0053A61K9/20A61K9/48A61K45/06A61P5/06A61P5/08
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Quick Facts
Patent No.
US 11,304,950
App. No.
17/081,694
Granted
Apr 19, 2022
Kind
B2
Abstract

Provided herein are compounds and pharmaceutical compositions for the prevention and treatment of testicular adrenal rest tumors (TART) or ovarian adrenal rest tumors (OART).

Claims (27)

1. A method of treating or preventing testicular adrenal rest tumors (TART) or ovarian adrenal rest tumors (OART), comprising administering to a subject in need thereof a corticotropin-releasing factor type-1 (CRF 1 ) antagonist or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the subject has congenital adrenal hyperplasia (CAH).

3. The method of claim 1 , wherein the size of the tumors is reduced.

4. The method of claim 1 , wherein the number of the tumors is decreased.

5. The method of claim 1 , wherein both the size and the number of the tumors are reduced or decreased.

6. The method of claim 1 , wherein the CRF 1 antagonist comprises a compound having structural Formula (I):

or a pharmaceutically acceptable salt thereof,

wherein:

R 1 and R 2 are independently ethyl or n-propyl;

R 3 is hydrogen, Cl, Br, methyl, trifluoromethyl, or methoxy; and

R 4 is hydrogen, Br, R a R b N—, methoxymethyl, n-butyl, acetamido, pyridin-4-yl, morpholin-4-yl,

R a and R b are independently hydrogen, C 1 -C 3 alkyl, H 2 NCH 2 CH 2 —,

(CH 3 ) 3 COC(O)NHCH 2 CH 2 —, or CH 3 CH 2 CH 2 NHCH 2 CH 2 —.

7. The method of claim 6 , wherein R 3 is Cl, Br, or methyl.

8. The method of claim 6 , wherein R 4 is Br, R a R b N—, pyridin-4-yl, morpholin-4-yl, or

9. The method of claim 6 , wherein R 4 is morpholin-4-yl or

10. The method of claim 6 , wherein R 4 is hydrogen, Br, R a R b N— and R a and R b are independently C 1 -C 3 alkyl.

11. The method of claim 6 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

12. The method of claim 1 , wherein the CRF 1 antagonist, or a pharmaceutically acceptable salt thereof, is administered at a dose of about 5 mg/day to about 100 mg/day to the subject.

13. The method of claim 1 , wherein the CRF 1 antagonist, or a pharmaceutically acceptable salt thereof, is administered at a dose of about 10 mg/day to about 400 mg/day to the subject.

14. The method of claim 1 , wherein the CRF 1 antagonist, or a pharmaceutically acceptable salt thereof, is administered orally.

15. The method of claim 1 , wherein the CRF 1 antagonist, or a pharmaceutically acceptable salt thereof, is formulated as a capsule or tablet.

16. The method of claim 1 , further comprising administering to the subject an additional chemotherapeutic agent.

17. The method of claim 16 , wherein the additional chemotherapeutic agent is a glucocorticoid, a mineralocorticoid, an ACAT1 inhibitor, or an anti-androgen.

18. The method of claim 17 , wherein the glucocorticoid is beclomethasone, betamethasone, budesonide, cortisone, dexamethasone, hydrocortisone, methylprednisolone, prednisolone, prednisone, or triamcinolone.

19. The method of claim 6 , wherein R 3 is Cl, Br, methyl, or trifluoromethyl.

Assignments (2)
SECURITY INTEREST Recorded Jan 12, 2026
From: SPRUCE BIOSCIENCES, INC.
To: AVENUE CAPITAL MANAGEMENT II, L.P.
Reel/Frame 073442/0864 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 6, 2020
From: HOWERTON, ALEXIS; GERBER, HAL
To: SPRUCE BIOSCIENCES, INC.
Reel/Frame 054296/0458 →
Continuity (4)
Continuation PCTUS2019029486 · Apr 26, 2019
Provisional Application 62822815 · Mar 23, 2019
Provisional Application 62663951 · Apr 27, 2018
Related Publication 20210038604A1 · Feb 11, 2021
Cited By (6)
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