IP Library Granted Patent US 9,757,381
Granted Patent B2
US 9,757,381 · App. 15/191,820 · Granted Sep 12, 2017

Compounds, compositions and methods useful for cholesterol mobilization

Inventors: Jean-Louis Henri Dasseux (Toulouse, FR); Ronald Barbaras (Seilh, FR)
Assignee: CERENIS THERAPEUTICS HOLDING SA
A61K31/5377A61K9/0053A61K31/155A61K31/194A61K31/198A61K31/20A61K31/201A61K31/353A61K31/4365A61K31/506A61K31/575A61K31/7032C07D319/18C07D401/04C07D401/14C07D471/04C07D493/04C07D495/04C07D513/04G01N33/92G01N2800/52
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Quick Facts
Patent No.
US 9,757,381
App. No.
15/191,820
Granted
Sep 12, 2017
Kind
B2
Abstract

The invention relates to classes of pharmaceutically-active heterocyclic compounds and pharmaceutically acceptable salts, and hydrates thereof, and compositions comprising the same. The invention also relates to methods for treating or preventing a disease or disorder, which comprises administering a therapeutically or prophylactically effective amount a compound described herein.

Claims (25)

1. A method for treating a hepatic steatosis, comprising administering to a subject in need thereof an effective amount of a compound of Formula (II):

or a pharmaceutically acceptable salt thereof, wherein

each R 9 is independently —H, -hydrocarbyl, -aryl, -aralkyl, -heteroaryl, -heterocyclyl, —C(O)O(alkyl), —OC(O)(alkyl), —C(O)NH 2 , —C(O)NH(alkyl), —C(O)N(alkyl)(alkyl), —NHC(O)(alkyl), N(alkyl)C(O)(alkyl), or —SO 2 NH 2 ;

each R 10 is independently —H, —OH, —NH 2 , —NH(alkyl), —N(alkyl)(alkyl), hydrocarbyl, —O-alkyl, —O-alkenyl, aryl, —O-aryl, aralkyl, —O-aralkyl, heteroaryl, —O-heteroaryl, heterocyclyl,

—O-heterocyclyl, halo, —OCF 3 , —C(O)O(alkyl), —OC(O)(alkyl), —C(O)NH 2 , —C(O)NH(alkyl), —C(O)N(alkyl)(alkyl), —NHC(O)(C 2 -C 10 -alkyl), —N(alkyl)C(O)(alkyl), —OC(O)O(alkyl), —OC(O)NH 2 , —OC(O)NH(alkyl), —OC(O)N(alkyl)(alkyl), —CHNH, —CHN(alkyl), or —SO 2 NH 2 ;

each of Q 1 , Q 2 , and Q 3 is independently CR 10 or N;

X is CHR 10 , S, O, or NR 9 ; and

each m is independently an integer from 0-3.

2. The method of claim 1 , wherein the compound has the structure:

or a pharmaceutically acceptable salt of any of the foregoing.

3. The method of claim 1 , wherein R 9 is H and R 10 is OH.

4. The method of claim 3 , wherein each m is 1.

5. The method of claim 1 , wherein the compound has the structure:

6. The method of claim 1 , wherein the hepatic steatosis is alcoholic hepatic steatosis or non-alcoholic hepatic steatosis.

7. The method of claim 1 , wherein the compound or pharmaceutically acceptable salt thereof is present in a composition that further comprises a pharmaceutically acceptable vehicle or carrier.

8. The method of claim 7 , wherein the composition is formulated for oral administration.

9. The method of claim 7 , wherein the composition is in the form of a tablet or capsule.

10. The method of claim 7 , wherein the compound or pharmaceutically acceptable salt thereof is present in the composition in an amount of about 1 mg to about 1,000 mg.

11. A method for treating a hepatic steatosis, comprising administering to a subject in need thereof an effective amount of a compound having the structure:

or a pharmaceutically acceptable salt of any of the foregoing.

12. The method of claim 11 , wherein the hepatic steatosis is alcoholic hepatic steatosis or non-alcoholic hepatic steatosis.

13. The method of claim 11 , wherein the compound or pharmaceutically acceptable salt thereof is a present in a composition that further comprises a pharmaceutically acceptable vehicle or carrier.

14. The method of claim 13 , wherein the composition is formulated for oral administration.

15. The method of claim 13 , wherein the composition is in the form of a tablet or capsule.

16. The method of claim 13 , wherein the compound or pharmaceutically acceptable salt thereof is present in the composition in an amount of about 1 mg to about 1,000 mg.

Assignments (9)
CHANGE OF ADDRESS FOR REEL/FRAME 039679/0959 Recorded Dec 26, 2018
From: CERENIS THERAPEUTICS HOLDING SA
To: CERENIS THERAPEUTICS HOLDING SA
Reel/Frame 047984/0074 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 8, 2016
From: KOVALSKY, DMITRY; KOCHUBEY, VALERY; RODIN, OLEG GENNADIEVICH
To: ASINEX
Reel/Frame 039679/0836 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 8, 2016
From: GEOFFROY, OTTO
To: ALCHEM LABORATORIES CORP.
Reel/Frame 039679/0854 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 8, 2016
From: ALCHEM LABORATORIES CORP.
To: CERENIS THERAPEUTICS SA
Reel/Frame 039679/0858 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 8, 2016
From: RZEPIELA, ANNA
To: PYXIS DISCOVERY
Reel/Frame 039679/0893 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 8, 2016
From: ASINEX
To: PYXIS DISCOVERY
Reel/Frame 039679/0905 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 8, 2016
From: ONICIU, DANIELA CARMEN; DASSEUX, JEAN-LOUIS HENRI; BARBARAS, RONALD
To: CERENIS THERAPEUTICS SA
Reel/Frame 039679/0939 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 8, 2016
From: PYXIS DISCOVERY
To: CERENIS THERAPEUTICS SA
Reel/Frame 039679/0951 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 8, 2016
From: CERENIS THERAPEUTICS SA
To: CERENIS THERAPEUTICS HOLDING SA
Reel/Frame 039679/0959 →
Continuity (6)
Continuation 14729908 · Jun 3, 2015
Division 13673799 · Nov 9, 2012
Division 13276238 · Oct 18, 2011
Provisional Application 61444212 · Feb 18, 2011
Provisional Application 61394136 · Oct 18, 2010
Related Publication 20160361318A1 · Dec 15, 2016