IP Library › Granted Patent US 8,097,592
Granted Patent B2
US 8,097,592 · App. 12/296,056 · Granted Jan 17, 2012

Cocrystal of C-glycoside derivative and L-proline

Assignees: Astellas Pharma Inc.; Kotobuki Pharmaceutical Co. Ltd.
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 8,097,592
App. No.
12/296,056
Granted
Jan 17, 2012
Kind
B2
Abstract

A cocrystal of (1S)-1,5-anhydro-1-[3-(1-benzothien-2-ylmethyl)-4-fluorophenyl]-D-glucitol and L-proline. It is a cocrystal of known compound A, which has a constant quality, is superior in storage stability, has no moisture absorptivity, and is suitable as a crystal of a drug substance used for preparing pharmaceuticals.

Claims (6)

1. A cocrystal of (1S)-1,5-anhydro-1-[3-(1-benzothien-2-ylmethyl)-4-fluorophenyl]-D-glucitol and L-proline having peaks at 2θ(°) of 4.14, 8.98, 12.4, 16.5, 17.5, 18.7, 20.5 and 21.5 measured by X-ray powder diffraction.

2. The cocrystal according to claim 1 , having an endothermic peak at 201 to 213° C. measured by differential scanning calorimetry (DSC analysis).

3. The cocrystal according to claim 2 , wherein the molar ratio of (1S)-1,5-anhydro-1-[3-(1-benzothien-2-ylmethyl)-4-fluorophenyl]-D-glucitol and L-proline is 1:1.

4. A solid pharmaceutical composition comprising the cocrystal according to claim 1 , and a pharmaceutically acceptable excipient.

5. A solid pharmaceutical composition comprising the cocrystal according to claim 1 in a dose effective to treat diabetes.

6. A method for treating diabetes comprising administering an effective therapeutic dose of the cocrystal according to claim 1 to patients in need thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 6, 2008
From: IMAMURA, MASAKAZU; NAKANISHI, KEITA; SHIRAKI, RYOTA; ONDA, KENICHI; SASUGA, DISUKE; YUDA, MASAMICHI
To: ASTELLA PHARMA INC.; KOTOBUKI PHARMACEUTICAL CO., LTD.
Reel/Frame 021637/0401 →
Priority Claims (1)
JP 2006-103711 · Apr 5, 2006 · national
Continuity (1)
Related Publication 20090143316A1 · Jun 4, 2009