IP Library Granted Patent US 8,309,579
Granted Patent B2
US 8,309,579 · App. 13/193,114 · Granted Nov 13, 2012

N-hydroxyamide derivatives and use thereof

Assignee: Merck Serono SA
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Quick Facts
Patent No.
US 8,309,579
App. No.
13/193,114
Granted
Nov 13, 2012
Kind
B2
Abstract

The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.

Claims (30)

1. An N-hydroxyamide derivative of Formula (I),

wherein:

A is C(B);

B is H or B forms a bond with either R 5 or R 7 ;

R 1 is selected from H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 -cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C 3 -C 8 -cycloalkyl C 1 -C 6 alkyl, heterocycloalkyl C 1 -C 6 alkyl, heteroaryl C 1 -C 6 alkyl, amino or alkoxy;

R 2 is selected from H, substituted C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 4 : cycloalkyl, C 6 -C 8 -cycloalkyl, heterocycloalkyl, alkoxy, aryl or heteroaryl;

R 3 is selected from H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl;

R 4 , R 5 , R 6 and R 7 are independently selected from H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl; or R 4 and R 7 form together a —CH 2 — linkage; and

n is an integer selected from 1, 2, 3, 4, 5 and 6;

or pharmaceutically acceptable salts thereof,

wherein carbons (2) and (3) are two chiral centers, chiral center (2) has a configuration selected from “S” and “R” and chiral center (3) has an “S”.

2. The N-hydroxyamide derivative according to claim 1 having a Formula (Ia):

wherein A is CH;

R 1 is selected from H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 -cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C 3 -C 8 -cycloalkyl C 1 -C 6 alkyl, heterocycloalkyl C 1 -C 6 alkyl, heteroaryl C 1 -C 6 alkyl, amino or alkoxy;

R 2 is selected from H, substituted C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 4 -cycloalkyl, C 6 -C 8 -cycloalkyl, heterocycloalkyl, alkoxy, aryl or heteroaryl;

R 3 is selected from H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl;

R 4 , R 5 , R 6 and R 7 are independently selected from H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl; or R 4 and R 7 form together a —CH 2 — linkage; and

n is an integer selected from 1, 2, 3, 4, 5 and 6;

or pharmaceutically acceptable salts thereof,

wherein carbons (2) and (3) are two chiral centers, chiral center (2) has a configuration selected from “S” and “R” and chiral center (3) has an “S” configuration.

3. The N-hydroxyamide derivative according to claim 1 , wherein R 1 is selected from aryl and heteroaryl.

4. The N-hydroxyamide derivative according to claim 1 ,

wherein R 2 is selected from H, substituted C 1 -C 6 alkyl, C 2 -C 6 alkenyl and C 2 -C 6 alkynyl.

5. The N-hydroxyamide derivative according to claim 1 , wherein R 3 is H.

6. The N-hydroxyamide derivative according to claim 1 , wherein R 4 , R 5 and R 7 are H.

7. The N-hydroxyamide derivative according to claim 2 , wherein R 1 is selected from aryl and heteroaryl.

8. The N-hydroxyamide derivative according to claim 2 , wherein R 2 is selected from H, substituted C 1 -C 6 alkyl, C 2 -C 6 alkenyl and C 2 -C 6 alkynyl.

9. The N-hydroxyamide derivative according to claim 2 , wherein R 3 is H.

10. The N-hydroxyamide derivative according to claim 2 , wherein R 4 , R 5 and R 7 are H.

11. A pharmaceutical composition comprising at least one N-hydroxyamide derivative according to claim 1 and a pharmaceutically acceptable carrier, diluent or excipient.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 1, 2011
From: SWINNEN, DOMINIQUE; GONZALEZ, JEROME
To: LABORATOIRES SERONO S.A.
Reel/Frame 027003/0280 →
CHANGE OF NAME Recorded Oct 1, 2011
From: LABORATOIRES SERONO SA
To: MERCK SERONO SA
Reel/Frame 027003/0338 →
Priority Claims (1)
EP 05111228 · Nov 24, 2005 · regional
Continuity (3)
Division 12094921
Provisional Application 60740211 · Nov 28, 2005
Related Publication 20110281891A1 · Nov 17, 2011