IP Library Granted Patent US 11,452,726
Granted Patent B2
US 11,452,726 · App. 17/014,414 · Granted Sep 27, 2022

Salts of 2-fluoro-N-methyl-4-[7-(quinolin-6-yl-methyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide and processes related to preparing the same

Inventors: Lingkai Weng (Malvern, PA); Lei Qiao (Downingtown, PA); Jiacheng Zhou (Newark, DE); Pingli Liu (Newark, DE); Yongchun Pan (Newark, DE)
Assignees: Incyte Corporation; Inctye Holdings Corporation
A61K31/53C07D253/07C07D401/10C07D487/04
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Quick Facts
Patent No.
US 11,452,726
App. No.
17/014,414
Granted
Sep 27, 2022
Kind
B2
Abstract

The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.

Claims (8)

1. A process of preparing the hydrate of 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide dihydrochloric acid salt, comprising:

a) reacting a first mixture comprising 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide and water with at least two equivalents of hydrochloric acid in a solvent comprising water to form a second mixture; and

b) combining the second mixture with acetone.

2. The process of claim 1 , wherein step a) is carried out at a temperature of about 20 to about 30° C.

3. The process of claim 1 , wherein step a) and b) are carried out at about room temperature.

4. The process of claim 1 , wherein the hydrate of 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide dihydrochloric acid salt is crystalline.

5. The process of claim 4 , wherein the hydrate of 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide dihydrochloric acid salt has an X-ray powder diffraction pattern comprising characteristic peaks expressed in degrees 2θ at about 26.0, 24.7, 18.2, 29.3, and 7.8.

6. The process of claim 1 , wherein step a) is carried out at a temperature of about 50 to about 60° C.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 18, 2022
From: WENG, LINGKAI; ZHOU, JIACHENG; QIAO, LEI; LIU, PINGLI; PAN, YONGCHUN
To: INCYTE CORPORATION
Reel/Frame 060846/0454 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 18, 2022
From: INCYTE CORPORATION
To: INCYTE CORPORATION; INCYTE HOLDINGS CORPORATION
Reel/Frame 060846/0770 →
Continuity (7)
Continuation 16269871 · Feb 7, 2019
Continuation 15355630 · Nov 18, 2016
Continuation 14525381 · Oct 28, 2014
Continuation 13793864 · Mar 11, 2013
Division 12469360 · May 20, 2009
Provisional Application 61054995 · May 21, 2008
Related Publication 20210128568A1 · May 6, 2021