IP Library Granted Patent US 11,891,373
Granted Patent B2
US 11,891,373 · App. 17/494,938 · Granted Feb 6, 2024

Crystalline forms of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate

Inventors: Eric Christian Hansen (Pawcatuck, CT); Christopher Scott Seadeek (West Lafayette, IN); Anil Mahadeo Rane (Mystic, CT)
Assignee: Pfizer Inc.
C07D401/04A61K31/4439C07B2200/13
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Quick Facts
Patent No.
US 11,891,373
App. No.
17/494,938
Granted
Feb 6, 2024
Kind
B2
Abstract

This invention relates to a crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate, and to pharmaceutical compositions thereof, to intermediates and methods for the production and isolation of such crystalline forms and compositions, and to methods of using such crystalline forms and compositions in the treatment of abnormal cell growth in mammals, especially humans.

Claims (8)

1. A crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea imidazole complex (1:1), having the structure:

2. A process for preparing a crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate, having the structure:

and having a powder X-ray diffraction pattern comprising peaks at 2θ values of: 11.6, 12.1 and 19.6 °2θ±0.2 °2θ, said process comprising treating 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea imidazole complex (1:1) with maleic acid.

3. The process of claim 2 , wherein the reaction is conducted in a solvent, which solvent is isopropanol.

4. The process of claim 2 , wherein the maleic acid is added as a solution in isopropanol.

5. The crystalline form of claim 1 , having a powder X-ray diffraction pattern comprising peaks at 2⊖ values essentially the same as shown in FIG. 4 .

6. The crystalline form of claim 1 , having a powder X-ray diffraction pattern consisting of peaks at 2⊖ values essentially the same as shown in FIG. 4 .

7. The crystalline form of claim 1 , having a powder X-ray diffraction pattern consisting essentially of peaks at 2⊖ values essentially the same as shown in FIG. 4 .

Assignments (2)
ASSIGNEE ADDRESS CORRECTION Recorded Mar 20, 2023
From: PFIZER INC.
To: PFIZER INC.
Reel/Frame 063119/0087 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 10, 2021
From: RANE, ANIL MAHADEO
To: PFIZER INC.
Reel/Frame 058071/0272 →