IP Library Granted Patent US 10,898,461
Granted Patent B2
US 10,898,461 · App. 16/676,911 · Granted Jan 26, 2021

Salts of 3-[(dimethylamino)methyl]-N-{2-[4-(hydroxycarbamoyl) phenoxy]ethyli-1-benzofuran-2-carboxamide, related crystalline forms, method for preparing the same and pharmaceutical compositions containing the same

Inventors: Marina Gaillard (Orleans, FR); Philippe Letellier (Orleans, FR)
Assignee: Pharmacyclics LLC
A61K31/343A61K31/135A61K31/166A61K31/185C07D307/85G01N23/20G01V3/14
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Quick Facts
Patent No.
US 10,898,461
App. No.
16/676,911
Granted
Jan 26, 2021
Kind
B2
Abstract

Described herein are salts of 3-[(dimethylamino)methyl]-N-{2-[4-(hydroxycarbamoyl)phenoxy]ethyl}-1-benzofuran-2-carboxamide, in particular that of formula (I): wherein HA is naphthalene-1,5-disulfonic acid, naphthalene-2-sulfonic acid, oxalic acid, benzenesulfonic acid, or sulfuric acid, or hydrates thereof, and crystalline forms thereof characterized by the powder X-ray diffraction diagram and the 13C CP/MAS NMR solid state spectrum. Also described are compositions, methods of use and preparation thereof.

Claims (5)

1. A crystalline form of an abexinostat salt according to formula (Ia)

wherein HA is benzenesulfonic acid and wherein the crystalline form has a powder X-ray diffraction diagram exhibiting the following diffraction lines (Bragg angle 2 theta, express in degrees ±0.2°): 8.08; 10.03; 13.63; 15.00; 16.19; 17.73; 17.90; 18.77; 19.77; 21.98; 22.45.

2. The crystalline form of claim 1 characterized in that it has a powder X-ray diffraction diagram exhibiting the following diffraction lines (Bragg angle 2 theta, expressed in degrees ±0.2°): 8.08; 10.03; 11.86; 12.66; 13.63; 15.00; 16.19; 16.39; 16.52; 17.73; 17.90; 18.77; 19.77; 20.20; 20.86; 21.11 21.98; 22.45; 23.84; 26.13; 26.74; 27.44.

3. A pharmaceutical composition comprising the crystalline form of claim 1 as an active ingredient and one or more pharmaceutically acceptable carriers.

4. A pharmaceutical composition comprising the crystalline form of claim 2 as an active ingredient and one or more pharmaceutically acceptable carriers.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 17, 2020
From: GAILLARD, MARINA; LETELLIER, PHILIPPE
To: LES LABORATOIRES SERVIER
Reel/Frame 054684/0920 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 17, 2020
From: LES LABORATOIRES SERVIER
To: PHARMACYCLICS, INC.
Reel/Frame 054684/0924 →
MERGER AND CHANGE OF NAME Recorded Dec 17, 2020
From: PHARMACYCLICS, INC.; OXFORD AMHERST LLC; PHARMACYCLICS LLC
To: PHARMACYCLICS LLC
Reel/Frame 054684/0944 →
Priority Claims (2)
FR 14 58215 · Sep 3, 2014 · national
FR 14 58224 · Sep 3, 2014 · national
Continuity (2)
Continuation 15508609
Related Publication 20200069637A1 · Mar 5, 2020