IP Library Granted Patent US 11,116,763
Granted Patent B2
US 11,116,763 · App. 16/317,091 · Granted Sep 14, 2021

Meclozine derivatives and diclazuril derivatives for use in the prevention and/or the treatment of disorders associated to the inflammation induced by

Inventors: Nicolas Dupin (Paris, FR); Vincent Calvez (Paris, FR); Philippe Grange (Ozoir la Ferriere, FR); Anne-Geneviève Marcelin (Paris, FR)
Assignees: Universite de Paris; Assistance Publique—Hopitaux de Paris
A61K31/495A61K31/53A61K45/06A61P17/06A61P17/10A61K31/202A61K31/203
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 11,116,763
App. No.
16/317,091
Granted
Sep 14, 2021
Kind
B2
Abstract

The present invention relates to compounds of the following general formula (I) or (II) or a pharmaceutically acceptable salt and/or solvate thereof, for use in the prevention and/or the treatment of disorders associated to the inflammation induced by P. acnes , in particular in the prevention and/or the treatment of acne, psoriasis, chronic urticaria, urticaria pigmentosa, cutaneous autoinflammatory diseases, hidradenitis or atopic dermatis.

Claims (29)

1. A method for treating disorders associated to the inflammation induced by P. acnes comprising administering to a subject in need thereof an effective amount of a compound of following general formula (II):

or a pharmaceutically acceptable salt and/or solvate thereof, wherein:

X′, Y′ and Z′ are, independently of one another, CH, CH 2 , NH or N;

W′ is CHR′3, S═O or S;

R′ 1 and R′ 2 are, independently of one another, hydrogen atom, halo, —CN, —NO 2 , —CF 3 , —OR′ 7 , —NR′ 8 R′ 9 , or a (C 1 -C 6 )alkyl group;

R′ 3 is H, —CN, OR′ 10 , or a (C 1 -C 6 )alkyl group;

R′ 4 and R′ 5 , are, independently of one another, hydrogen atom or a group selected from halo, —NO 2 , —CN, —OR′ 11 , —NR′ 12 R′ 13 , —C(O)OR′ 14 , —S(O) 2 R′ 15 , or a (C 1 -C 6 )alkyl group optionally substituted with one or several groups selected from halo or —OR′ 16 ;

R′ 7 to R′ 16 are, independently of one another, hydrogen atom or a group selected from (C 1 -C 6 )alkyl, aryl, (C 1 -C 6 )alkyl-aryl, heterocycle, (C 1 -C 6 )alkyl-heterocycle, said group being optionally substituted with one or several groups selected from halo, (C 1 -C 6 )alkyl, CF 3 or —OR′ 17 ;

R′ 17 is hydrogen atom, halo or a (C 1 -C 6 )alkyl group.

2. The method of claim 1 , wherein said compound is a compound of the following general formula (IIa):

or a pharmaceutically acceptable salt and/or solvate thereof, wherein:

X′, Y′ and Z′ are, independently of one another, CH, CH 2 , NH, or N;

R′ 1 and R′ 2 are, independently of one another, hydrogen atom, halo, —CN, —NO 2 , —CF 3 , —OR′ 7 , —NR′ 8 R′ 9 , or a (C 1 -C 6 )alkyl group;

R′ 3 is H, —CN, OR′ 10 , or a (C 1 -C 6 )alkyl group;

R′ 4 and R′ 5 , are, independently of one another, hydrogen atom or a group selected from halo, —NO 2 , —CN, —OR′ 11 , —NR′ 12 R′ 13 , —C(O)OR′ 14 , —S(O) 2 R′ 15 , or a (C 1 -C 6 )alkyl group optionally substituted with one or several groups selected from halo or —OR′ 16 ;

R′ 7 to R′ 16 are, independently of one another, hydrogen atom, or a group selected from (C 1 -C 6 )alkyl, aryl, (C 1 -C 6 )alkyl-aryl, heterocycle, (C 1 -C 6 )alkyl-heterocycle, said group being optionally substituted with one or several groups selected from halo, (C 1 -C 6 )alkyl, CF 3 or —OR′ 17 ;

R′ 17 is hydrogen atom, halo or a (C 1 -C 6 )alkyl group.

3. The method of claim 1 , wherein X′, Y′, and Z′ are each a nitrogen atom.

4. The method of claim 1 , wherein R′ 3 is —CN, or OH.

5. The method of claim 1 , wherein and R′ 1 and R′ 2 are, independently of one another, hydrogen atom, halo, —CF 3 , —OH, or a (C 1 -C 6 )alkyl group.

6. The method of claim 1 , wherein R′ 5 is an hydrogen atom and R′ 4 is selected from the group consisting of hydrogen atom, halo, —CF 3 , —OH, and a (C 1 -C 6 )alkyl group.

7. The method of claim 1 , wherein said compound is a compound of the following general formula (IIb):

or a pharmaceutically acceptable salt and/or solvate thereof.

8. The method of claim 1 , wherein said compound is a compound of the following formula (IId):

or a pharmaceutically acceptable salt and/or solvate thereof.

9. The method of claim 1 , wherein said disorders associated to the inflammation induced by P. acnes are acne, psoriasis, chronic urticaria, urticaria pigmentosa, cutaneous autoinflammatory diseases, hidradenitis, or atopic dermatis.

10. A method for treating disorders associated to the inflammation induced by P. acnes comprising administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising at least one compound of claim 1 and at least one pharmaceutically acceptable excipient.

11. The method of claim 10 , wherein said composition further comprises another active principle selected from the group consisting of a topical antibiotic, topical anti-inflammatory, topical anti-seborrheic zinc derivative, cyclin, and isotretinoin.

12. The method of claim 10 , wherein said composition further comprises another active principle selected from the group consisting of erythromycine, dalacine, benzoyl peroxyde derivatives, isotretinoin, tretinoin, adapalene, zinc gluconate, cyclins, and isotretinoin.

Assignments (4)
CORRECTIVE ASSIGNMENT TO CORRECT THE PROPERTY NUMBER 16930208 PREVIOUSLY RECORDED AT REEL: 060390 FRAME: 0122. ASSIGNOR(S) HEREBY CONFIRMS THE CHANGE OF NAME. Recorded Jan 11, 2023
From: UNIVERSITE DE PARIS
To: UNIVERSITÉ PARIS CITÉ
Reel/Frame 062387/0489 →
CHANGE OF NAME Recorded Jun 20, 2022
From: UNIVERSITE DE PARIS
To: UNIVERSITÉ PARIS CITÉ
Reel/Frame 060390/0122 →
MERGER AND CHANGE OF NAME Recorded Dec 30, 2020
From: UNIVERSITE PARIS DESCARTES; UNIVERSITE PARIS DIDEROT PARIS 7; UNIVERSITÉ DE PARIS
To: UNIVERSITÉ DE PARIS
Reel/Frame 054871/0669 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 15, 2020
From: DUPIN, NICOLAS; CALVEZ, VINCENT; GRANGE, PHILIPE; MARCELIN, ANNE-GENEVIÈVE
To: UNIVERSITE PARIS DESCARTES; ASSISTANCE PUBLIQUE - HOPITAUX DE PARIS; INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM); CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS); SORBONNE UNIVERSITY
Reel/Frame 052939/0914 →
Priority Claims (1)
EP 16305912 · Jul 13, 2016 · regional
Continuity (1)
Related Publication 20190224191A1 · Jul 25, 2019