IP Library › Granted Patent US 11,453,641
Granted Patent B2
US 11,453,641 · App. 17/357,593 · Granted Sep 27, 2022

Methods of treating neurofibromatosis with N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-benzamide

Inventor: Erwin Irdam (Melrose, MA)
Assignee: Warner-Lambert Company LLC
C07C237/28A61K9/0053A61K9/20A61K9/48C07B2200/13
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Quick Facts
Patent No.
US 11,453,641
App. No.
17/357,593
Granted
Sep 27, 2022
Kind
B2
Abstract

The present disclosure relates to: a) a crystalline composition of essentially pure Form IV of N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide; b) pharmaceutical compositions comprising the crystalline composition of essentially pure Form IV of N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide, and, optionally, a pharmaceutically acceptable carrier; and c) methods of treating a tumor, a cancer, or a Rasopathy disorder by administering the crystalline composition of essentially pure Form IV of N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide to a subject in need thereof.

Claims (6)

1. A method of treating Neurofibromatosis in a patient in need thereof comprising administering a pharmaceutical composition comprising 1 mg to 4 mg N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide Form IV characterized by an XRPD pattern having peaks at 4.6±0.2, 13.5±0.2 and 16.7±0.2 degrees two theta.

2. The method of claim 1 wherein the pharmaceutical composition comprises 1 mg N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide.

3. The method of claim 1 wherein the pharmaceutical composition comprises 2 mg N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide.

4. The method of claim 1 wherein the pharmaceutical composition comprises 3 mg N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide.

5. The method of claim 1 wherein the pharmaceutical composition comprises 4 mg N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide.

6. A method of treating Neurofibromatosis in a patient in need thereof comprising administering a pharmaceutical composition comprising 1 mg to 4 mg N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide Form IV characterized by an XRPD pattern substantially as shown in FIG. 1A .

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 9, 2022
From: IRDAM, ERWIN
To: WARNER-LAMBERT COMPANY LLC
Reel/Frame 059210/0478 →
Continuity (2)
Continuation 17178022 · Feb 17, 2021
Related Publication 20220259142A1 · Aug 18, 2022
Cited By (8)
US 12,220,390 US 12,257,215 US 12,263,146 US 12,295,925 US 12,324,791 US 12,357,597 US 12,383,517 US 12,661,330