IP Library Granted Patent US 9,713,619
Granted Patent B2
US 9,713,619 · App. 14/729,908 · Granted Jul 25, 2017

Compounds, compositions and methods useful for cholesterol mobilization

Inventors: Daniela Carmen Oniciu (Toulouse, FR); Jean-Louis Henri Dasseux (Toulouse, FR); Ronald Barbaras (Seilh, FR); Oleg Gennadievich Rodin (Moscow, RU); Anna Rzepiela (Rijswijsk, NL)
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
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 9,713,619
App. No.
14/729,908
Granted
Jul 25, 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 composition comprising an effective amount of a compound or pharmaceutically acceptable salt of a compound of Formula (XI):

or a pharmaceutically acceptable salt thereof, wherein

R 11a is H, hydrocarbyl, aralkyl, heteroaryl, heterocyclyl, —C(O)(alkyl), —C(O)O(alkyl), —C(O)NH 2 , —C(O)NH(alkyl), —C(O)N(alkyl)(alkyl), or —SO 2 NH 2 ;

each of R 11b and R 11c is independently H, hydrocarbyl, aryl, aralkyl, heteroaryl, heterocyclyl, —C(O)(alkyl), —C(O)O(alkyl), —C(O)NH 2 , —C(O)NH(alkyl), —C(O)N(alkyl)(alkyl), or —SO 2 NH 2 ;

each of X 1 and X 2 is independently CHR 10 , S, O, NR 9 , or N-acyl;

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), —OC(O)O(alkyl), or —SO 2 NH 2 ;

each R 10 is independently —H, —OH, —NH 2 , —NH(alkyl), —N(alkyl)(alkyl), hydrocarbyl, —O-hydrocarbyl, 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)(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 ; and

each m is independently an integer from 0-3;

and a pharmaceutically acceptable vehicle or carrier.

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

or a pharmaceutically acceptable salt thereof.

3. The composition of claim 1 , wherein the composition is formulated for oral administration.

4. The composition of claim 1 , wherein the composition is in the form of a tablet or capsule.

5. The composition of claim 1 , wherein the compound or salt thereof is present in an amount of about 1 mg to about 1,000 mg.

6. A composition comprising an effective amount of a pharmaceutically acceptable carrier or vehicle and a compound of Formula (XI):

or a pharmaceutically acceptable salt thereof, wherein

R 11a is aryl;

each of R 11b and R 11c is independently H, hydrocarbyl, aryl, aralkyl, heteroaryl, heterocyclyl, —C(O)(alkyl), —C(O)O(alkyl), —C(O)NH 2 , —C(O)NH(alkyl), —C(O)N(alkyl)(alkyl), or —SO 2 NH 2 ;

each of X 1 and X 2 is independently CHR 10 , S, O, NR 9 , or N-acyl;

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), —OC(O)O(alkyl), or —SO 2 NH 2 ;

each R 10 is independently —H, —OH, —NH 2 , —NH(alkyl), —N(alkyl)(alkyl), hydrocarbyl, —O-hydrocarbyl, 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)(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 ; and

each m is independently an integer from 0-3.

7. The composition of claim 6 , wherein the composition is formulated for oral administration.

8. The composition of claim 6 , wherein the composition is in the form of a tablet or capsule.

9. The composition of claim 6 , wherein the compound or salt thereof is present 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 (5)
Division 13673799 · Nov 9, 2012
Division 13276238 · Oct 18, 2011
Provisional Application 61444212 · Feb 18, 2011
Provisional Application 61394136 · Oct 18, 2010
Related Publication 20150344455A1 · Dec 3, 2015