# US 11,304,950 B2 · Methods for treating testicular and ovarian adrenal rest tumors

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- Number: US 11,304,950 B2
- Document ID: US11304950B2
- Status: Granted
- Kind: B2
- Application number: 17/081,694
- Filed: 2020-10-27
- Published: 2021-02-11
- Granted: 2022-04-19
- Earliest claimed: 2018-04-27
- Assignees: Spruce Biosciences, Inc.
- Applicants: Spruce Biosciences, Inc.
- Inventors: Alexis Howerton; Hal Gerber
- Web page: https://patentgrep.com/patent/US11304950B2

## CPC

- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 31/5377: not condensed and containing further heterocyclic rings, e.g. timolol
- A61P 35/00: Antineoplastic agents
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/20: Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)}
- A61K 9/2004: {Excipients; Inactive ingredients}
- A61K 9/48: Preparations in capsules, e.g. of gelatin, of chocolate {(A61K9/0004 takes precedence; bite capsules A61K9/0056)}
- A61K 9/4841: {Filling excipients; Inactive ingredients}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 5/06: of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
- A61P 5/08: for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## 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

### Claim 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 (CRF1) antagonist or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

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

### Claim 3 (depends on 1)

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

### Claim 4 (depends on 1)

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

### Claim 5 (depends on 1)

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

### Claim 6 (depends on 1)

The method of claim 1, wherein the CRF1 antagonist comprises a compound having structural Formula (I):
or a pharmaceutically acceptable salt thereof,
wherein:
R1 and R2 are independently ethyl or n-propyl;
R3 is hydrogen, Cl, Br, methyl, trifluoromethyl, or methoxy; and
R4 is hydrogen, Br, RaRbN—, methoxymethyl, n-butyl, acetamido, pyridin-4-yl, morpholin-4-yl,
Ra and Rb are independently hydrogen, C1-C3alkyl, H2NCH2CH2—,
(CH3)3COC(O)NHCH2CH2—, or CH3CH2CH2NHCH2CH2—.

### Claim 7 (depends on 6)

The method of claim 6, wherein R3 is Cl, Br, or methyl.

### Claim 8 (depends on 6)

The method of claim 6, wherein R4 is Br, RaRbN—, pyridin-4-yl, morpholin-4-yl, or

### Claim 9 (depends on 6)

The method of claim 6, wherein R4 is morpholin-4-yl or

### Claim 10 (depends on 6)

The method of claim 6, wherein R4 is hydrogen, Br, RaRbN— and Ra and Rb are independently C1-C3alkyl.

### Claim 11 (depends on 6)

The method of claim 6, wherein the compound is
or a pharmaceutically acceptable salt thereof.

### Claim 12 (depends on 1)

The method of claim 1, wherein the CRF1 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.

### Claim 13 (depends on 1)

The method of claim 1, wherein the CRF1 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.

### Claim 14 (depends on 1)

The method of claim 1, wherein the CRF1 antagonist, or a pharmaceutically acceptable salt thereof, is administered orally.

### Claim 15 (depends on 1)

The method of claim 1, wherein the CRF1 antagonist, or a pharmaceutically acceptable salt thereof, is formulated as a capsule or tablet.

### Claim 16 (depends on 1)

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

### Claim 17 (depends on 16)

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

### Claim 18 (depends on 17)

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

### Claim 19 (depends on 6)

The method of claim 6, wherein R3 is Cl, Br, methyl, or trifluoromethyl.