# US 10,869,875 B2 · Oxysterols and Hedgehog signaling

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- Number: US 10,869,875 B2
- Document ID: US10869875B2
- Status: Granted
- Kind: B2
- Application number: 15/771,005
- Filed: 2016-10-25
- Published: 2018-11-01
- Granted: 2020-12-22
- Earliest claimed: 2015-10-26
- Assignees: Max Biopharma, Inc.
- Applicants: Max Biopharma, Inc.
- Inventors: Frank Stappenbeck; Yi Chiao Fan; Feng Wang; Farhad Parhami
- Web page: https://patentgrep.com/patent/US10869875B2

## CPC

- A61K 31/575: substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- C07J 9/00: Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
- C07J 7/002: {not substituted in position 16}
- 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)
- C07J: STEROIDS (seco-steroids C07C)

## Abstract

Described herein are compounds and pharmaceutical compositions containing such compounds which inhibit Hedgehog signaling. Also described herein are methods for using such Hedgehog signaling inhibitors, alone or in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of Hedgehog signaling.

## Claims

### Claim 1

A compound having the structure of Formula (I):
wherein:
R1 is substituted or unsubstituted C1-C8alkyl;
R6 is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;
is a single or double bond;
R2, R3, R4, and R5 are independently hydrogen, deuterium, or —OH;
R7 is hydrogen, substituted or unsubstituted C1-C8alkyl, or —C(O)NR8R9; and
R8 and R9 are independently hydrogen or substituted or unsubstituted C1-C8alkyl; or a pharmaceutically acceptable salt or solvate thereof.

### Claim 2 (depends on 1)

The compound of claim 1, wherein R2, R3, R4, and R5 are independently hydrogen or deuterium.

### Claim 3 (depends on 2)

The compound of claim 2, wherein R2, R3, R4, and R5 are each hydrogen.

### Claim 4 (depends on 1)

The compound of claim 1, wherein R1 is unsubstituted C1-C8alkyl.

### Claim 5 (depends on 4)

The compound of claim 4, wherein R1 is —CH3.

### Claim 6 (depends on 1)

The compound of claim 1, wherein R6 is substituted or unsubstituted pyridyl.

### Claim 7 (depends on 6)

The compound of claim 6, wherein R6 is unsubstituted pyridyl.

### Claim 8 (depends on 1)

The compound of claim 1, wherein R7 is hydrogen.

### Claim 9 (depends on 1)

The compound of claim 1, wherein R7 is substituted or unsubstituted C1-C8alkyl.

### Claim 10 (depends on 9)

The compound of claim 9, wherein R7 is —CH3.

### Claim 11 (depends on 1)

The compound of claim 1 having the structure:
or a pharmaceutically acceptable salt or solvate thereof.

### Claim 12 (depends on 1)

The compound of claim 1 having the structure:
or a pharmaceutically acceptable salt or solvate thereof.

### Claim 13 (depends on 1)

The compound of claim 1 having the structure:
or a pharmaceutically acceptable salt or solvate thereof.

### Claim 14 (depends on 1)

The compound of claim 1 having the structure:
or a pharmaceutically acceptable salt or solvate thereof.

### Claim 15 (depends on 1)

The compound of claim 1 having the structure:
or a pharmaceutically acceptable salt or solvate thereof.

### Claim 16 (depends on 1)

A pharmaceutical composition comprising a compound of claim 1, or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable excipient.

### Claim 17 (depends on 1)

A method of treating a disease, disorder or condition associated with an aberrant activation of Hedgehog signaling pathway in a mammal comprising locally or systemically administering to the mammal a therapeutically effective amount of a compound according to claim 1, or a pharmaceutically acceptable salt or solvate thereof wherein the disease is a cancer selected from basal cell carcinoma, melanoma, leukemia, multiple myeloma, stomach cancer, pancreatic cancer, bladder cancer, prostate cancer, ovarian cancer, bone cancer, brain cancer, lung cancer, breast cancer, liver cancer, colon cancer, rhabdomyosarcoma, and skin cancer.

### Claim 18 (depends on 1, 17)

The method of claim 17, wherein the therapeutically effective amount of a compound according to claim 1, or a pharmaceutically acceptable salt or solvate thereof, is co-administered with an anti-tumor agent.

### Claim 19 (depends on 18)

The method of claim 18, wherein the anti-tumor agent is selected from a chemotherapeutic agent, a hormonal therapeutic agent, an immunotherapeutic agent, a STAT 3 inhibitor, and a Janus Kinase inhibitor.