IP Library Granted Patent US 10,138,206
Granted Patent B2
US 10,138,206 · App. 15/517,665 · Granted Nov 27, 2018

Amorphous form of lomitapide mesylate

Inventors: Shekhar Bhaskar Bhirud (Mumbai, IN); Samir Naik (Thane, IN); Sushanta Mishra (Bolangir, IN); Vipin Pandey (Thane, IN); Deepak S. Patekar (Navi Mumbai, IN)
Assignee: GLENMARK PHARMACEUTICALS LIMITED
C07D211/58A61K9/143A61K9/145A61K9/146A61K9/1623A61K31/4468A61K9/4866C07B2200/13
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Quick Facts
Patent No.
US 10,138,206
App. No.
15/517,665
Granted
Nov 27, 2018
Kind
B2
Abstract

Provided is novel amorphous form of lomitapide mesylate salt and process for preparation thereof.

Claims (7)

1. A process for the preparation of an amorphous form of lomitapide mesylate free of alkyl mesylates comprising

(a) providing a solution of lomitapide mesylate in a non-hydroxylic solvent; and

(b) isolating the amorphous form of lomitapide mesylate by

combining the solution obtained in (a) with an antisolvent followed by optional cooling to precipitate amorphous form of lomitapide mesylate, wherein the amorphous form of lomitapide mesylate has purity greater than 99.5% and a DSC endothermic peak at about 113±3° C. as shown in FIG. 2 ; wherein the non-hydroxylic solvent is ethyl acetate and the antisolvent is heptane.

2. The process as claimed in claim 1 , wherein the lomitapide mesylate in step (a) is prepared by treating lomitapide with methane sulfonic acid.

3. Lomitapide mesylate free of alkyl mesylates in amorphous form wherein the amorphous form of lomitapide mesylate has purity greater than 99.5% and has a DSC endothermic peak at about 113±3° C., prepared by a process of claim 1 .

4. The process as claimed in claim 2 , wherein the lomitapide treated with methanesulfonic acid is a crystalline lomitapide characterized by an X-ray powder diffraction (XRPD) spectrum having peak reflections at about 10.9, 13.7, 18.1, 18.9 and 21.9±0.2 degrees 2 theta.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 27, 2019
From: GLENMARK PHARMACEUTICALS LIMITED
To: GLENMARK LIFE SCIENCES LIMITED
Reel/Frame 050179/0351 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 12, 2017
From: BHIRUD, SHEKHAR BHASKAR; NAIK, SAMIR; MISHRA, SUSHANTA; PANDEY, VIPIN; PATEKAR, DEEPAK S.
To: GLENMARK PHARMACEUTICALS LIMITED
Reel/Frame 041981/0772 →
Priority Claims (1)
IN 3209/MUM/2014 · Oct 9, 2014 · national
Continuity (1)
Related Publication 20170305858A1 · Oct 26, 2017