# US 12,766,154 B2 · Ursodeoxycholic acid derivatives for the treatment of polycystic diseases

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- Number: US 12,766,154 B2
- Document ID: US12766154B2
- Status: Granted
- Kind: B2
- Application number: 18/353,525
- Filed: 2023-07-17
- Published: 2023-12-07
- Granted: 2026-10-20
- Earliest claimed: 2017-12-28
- Assignees: Administracion General De La Comunidad Autonoma De Euskadi; Universidad de Salamanca; Fundacio Institut D'Investigacio Biomedica De Bellvitge (Idibell); Universidad Del Pais Vasco/Euskal Herriko Unibertsitatea
- Applicants: Universidad Del Pais Vasco/Euskal Herriko Unibertsitatea; Administracion General De La Comunidad Autonoma De Euskadi; Fundacio Institut D'Investigacio Biomedica De Bellvitge (Idibell); Universidad De Salamanca
- Inventors: Jesus Maria Banales Asurmendi; Luis Bujanda Fernandez De Pierola; Alvaro Santos Laso; Fernando Pedro Cossio Mora; Ivan Rivilla De La Cruz; Francisco Javier Caballero Camino; Manel Esteller Badosa; Jose Juan Garcia Marin
- Web page: https://patentgrep.com/patent/US12766154B2

## CPC

- A61K 31/58: containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048})
- A61K 31/575: substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
- 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)

## Abstract

Compounds derived from ursodeoxycholic acid of formula (I) and to methods for obtaining same, as well as the use thereof in the treatment of polycystic diseases, particularly autosomal dominant polycystic liver disease, autosomal dominant polycystic kidney disease, or autosomal recessive polycystic kidney disease.

## Claims

### Claim 1

A compound of formula (I′):
wherein:
X is hydrogen or a C6-C10 aryl group;
Y is selected from:
—(CH2)n, wherein n is 1-5;
arylidene or heteroarylidene, wherein the arylidene or heteroarylidene are connect by (1,3)
or (1,4) bonds;
—C(O)—N(H)—CH2 (Ar)—, or
—Ar—C(O)—N(H)—CH2—(Ar)—, wherein Ar is arylidene
and
Z is selected from OH and optionally substituted C6-C10 aryl,
or a pharmaceutically acceptable stereoisomer, salt, or solvate thereof.

### Claim 2 (depends on 1)

The compound according to claim 1, wherein X is hydrogen.

### Claim 3 (depends on 1)

The compound according to claim 1, wherein Y is arylidene or heteroarylidene.

### Claim 4 (depends on 1)

The compound according to claim 1, wherein Y is —(CH2)n, where n is 1, 2, 3, or 4.

### Claim 5 (depends on 1)

The compound according to claim 1, wherein Z is OH or the optionally substituted C6-C10 aryl substituted by at least one of NH2 and a phenyl.

### Claim 6 (depends on 1)

The compound according to claim 1 selected from:

### Claim 7 (depends on 1)

A pharmaceutical composition comprising a compound of formula (I′) according to claim 1, or a stereoisomer, a salt, or a solvate thereof, and a pharmaceutically acceptable excipient or vehicle.

### Claim 8 (depends on 1)

A process for obtaining compounds of formula (I′) according to claim 1, comprising:
reacting ursodeoxycholic acid of formula (II):
with a compound of formula (III′):
wherein:
X is hydrogen or a C6-C10 aryl group;
Y is selected from:
—(CH2)n, wherein n is 1-5;
arylidene or heteroarylidene, wherein the arylidene or heteroarylidene are connect by (1,3)
or (1,4) bonds;
—C(O)—N(H)—CH2 (Ar)—, or
—Ar—C(O)—N(H)—CH2—(Ar)—, wherein Ar is arylidene
and where W is a precursor group of groups Z defined in claim 1, and
subsequently transforming groups W into the corresponding groups Z of formula (I′).