IP Library Granted Patent US 9,918,967
Granted Patent B2
US 9,918,967 · App. 14/640,712 · Granted Mar 20, 2018

Thiazole derivatives for treating dyskinesias caused by a chemical treatment

Inventors: Pierre-Etienne Chabrier de Lassauniere (Paris, FR); Michel Auguet (Palaiseau, FR); Brigitte Spinnewyn (Bures sur Yvette, FR)
Assignee: IPSEN PHARMA S.A.S.
A61K31/426A61K31/198A61K31/427C07D277/28
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Quick Facts
Patent No.
US 9,918,967
App. No.
14/640,712
Granted
Mar 20, 2018
Kind
B2
Abstract

The invention relates to the use of derivatives of thiazoles having general formula (I) for the preparation of a medicament for the treatment or prevention of dyskinesias caused by a chemical treatment. The invention also relates to a combination of thiazole derivatives having general formula (I) and at least one compound selected from among neuroleptics or products that act on the dopaminergic system for the treatment or prevention of dyskinesias caused by a chemical treatment.

Claims (20)

1. A composition consisting of:

(a) a compound of formula (I),

or a salt thereof, wherein:

A is an aryl radical (A1),

 wherein:

R 5 is hydrogen or alkyl, and

R 6 , R 7 , R 8 are each independently hydrogen, alkyl, cycloalkyl, hydroxy, or alkoxy;

B is hydrogen or alkyl;

n is an integer from 0 to 5;

R 1 and R 2 are each independently hydrogen, alkyl, or cycloalkyl;

R 3 and R 4 are each independently hydrogen or alkyl, or R 3 and R 4 , together with the nitrogen atom to which they are attached, form:

a heterocycle having 5 to 7 members, including 1 to 2 heteroatoms, wherein the members of the heterocycle include —CH 2 —, —NR 14 —, —O— or —S—;

R 14 is hydrogen, alkyl, —COR 15 , —COOR 15 , or —CONR 16 R 17 ;

R 15 is alkyl; and

R 16 and R 17 are each independently hydrogen or alkyl; and

(b) L-Dopa.

2. The composition of claim 1 comprising 4-[2-(aminomethyl)-1,3-thiazol-4-yl]-2,6-di(tert-butyl)phenol or its salt and L-Dopa.

3. The composition of claim 1 comprising 4{2-[(1R)-1-aminoethyl]-1,3-thiazol-4-yl}-2,6-di-tert-butylphenol or its salt and L-Dopa.

4. The composition of claim 1 comprising 4-{2-[(1S)-1-aminoethyl]-1,3-thiazol-4-yl}-2,6-di-tert-butylphenol or its salt and L-Dopa.

5. The composition of claim 1 , wherein the compound of Formula (I) is the only compound in the composition that is active in treating or preventing dyskinesia.

Assignments (2)
CHANGE OF NAME Recorded Sep 9, 2016
From: SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES, S.A.S.
To: IPSEN PHARMA S.A.S.
Reel/Frame 039689/0240 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 5, 2016
From: DE LASSAUNIERE, PIERRE-ETIENNE CHABRIER; AUGUET, MICHEL; SPINNEWYN, BRIGITTE
To: SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S)
Reel/Frame 039350/0288 →
Priority Claims (1)
FR 05 07303 · Jul 8, 2005 · national
Continuity (2)
Division 11995092
Related Publication 20150238468A1 · Aug 27, 2015