# US 10,117,846 B2 · Prodrugs of fumarates and their use in treating various diseases

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- Number: US 10,117,846 B2
- Document ID: US10117846B2
- Status: Granted
- Kind: B2
- Application number: 15/704,219
- Filed: 2017-09-14
- Published: 2018-03-08
- Granted: 2018-11-06
- Earliest claimed: 2013-03-14
- Assignees: Alkermes Pharma Ireland Limited
- Applicants: Alkermes Pharma Ireland Limited
- Inventors: Tarek A. Zeidan; Scott Duncan; Christopher P. Hencken; Thomas Andrew Wynn; Carlos N. Sanrame
- Web page: https://patentgrep.com/patent/US10117846B2

## CPC

- A61K 31/225: Polycarboxylic acids
- A61P 17/06: Antipsoriatics
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07C 219/08: having at least one of the hydroxy groups esterified by a carboxylic acid having the esterifying carboxyl group bound to an acyclic carbon atom of an acyclic unsaturated carbon skeleton
- C07C 229/16: to carbon atoms of hydrocarbon radicals substituted by amino or carboxyl groups, e.g. ethylenediamine-tetra-acetic acid, iminodiacetic acids
- C07C 233/18: having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
- C07C 233/91: with carbon atoms of the carboxamide groups bound to acyclic carbon atoms
- C07C 235/88: having the nitrogen atom of at least one of the carboxamide groups further acylated
- C07C 279/08: being further substituted by singly-bound oxygen atoms
- C07C 317/18: with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
- C07C 317/28: with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
- C07D 207/06: with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
- C07D 207/40: 2,5-Pyrrolidine-diones
- C07D 209/52: condensed with a ring other than six-membered
- C07D 211/06: having no double bonds between ring members or between ring members and non-ring members
- C07D 211/38: Halogen atoms or nitro radicals
- C07D 295/088: to an acyclic saturated chain
- C07D 491/113: with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
- 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
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.

## Claims

### Claim 1

A pharmaceutical composition comprising a compound of Formula (Ia), or a pharmaceutically acceptable salt thereof:
wherein:
R1 is unsubstituted C1-C6 alkyl;
La is unsubstituted C1-C6 alkyl linker; and
R2 is H, unsubstituted C1-C6 alkyl, unsubstituted C2-C6alkenyl, or unsubstituted C2-C6 alkynyl; and
a pharmaceutically acceptable carrier.

### Claim 2 (depends on 1)

The composition of claim 1, wherein R1 is methyl.

### Claim 3 (depends on 1)

The composition of claim 1, wherein La is an unsubstituted C1-C3 alkyl.

### Claim 4 (depends on 3)

The composition of claim 3, wherein La is an unsubstituted C2 alkyl.

### Claim 5 (depends on 1)

The composition of claim 1, wherein R2 is an unsubstituted C1-C6 alkyl, unsubstituted C2-C6 alkenyl, or unsubstituted C2-C6 alkynyl.

### Claim 6 (depends on 5)

The composition of claim 5, wherein R2 is an unsubstituted C1-C6 alkyl.

### Claim 7 (depends on 6)

The composition of claim 6, wherein R2 is an unsubstituted C1-C3 alkyl.

### Claim 8 (depends on 7)

The composition of claim 7, wherein R2 is an unsubstituted C1-C2 alkyl.

### Claim 9 (depends on 8)

The composition of claim 8, wherein R2 is methyl.

### Claim 10 (depends on 1)

The composition of claim 1, wherein the compound of Formula (Ia) has the structure:
or a pharmaceutically acceptable salt thereof.