Crystal forms of saxagliptin

Patent metadata

Field	Value
Publication number	US-9260389-B2
Application number	US-201314044204-A
Country	US
Kind code	B2
Filing date	Oct 2, 2013
Priority date	Apr 9, 2009
Publication date	Feb 16, 2016
Grant date	Feb 16, 2016

Abstract

The present invention relates to novel polymorphic forms of Saxagliptin Hydrochloride. The present invention also relates to methods of making polymorphic forms of Saxagliptin Hydrochloride.

First claim

The invention claimed is:

1. Crystalline Form I-S of Saxagliptin hydrochloride having a water content of not more than 1.5% w/w and a x-ray powder diffraction pattern comprising peaks at 6.7±0.2, 14.6±0.2, 15.2±0.2, 16.6±0.2 and 17.9±0.2 degrees two-theta and/or having an infrared spectrum comprising peaks at wavenumbers of 2907, 2853, 1637, 1589, 1462, 1391, 1318, 1045, 1014 and 775+/−2 cm-1, wherein the crystalline form is greater than 95% by weight.

2. Pharmaceutical composition comprising an crystalline form of Saxagliptin according to claim 1 in an effective amount.

3. A process for the preparation of crystalline Saxagliptin hydrochloride Form I-S according to claim 1 comprising the step of allowing Saxagliptin hydrochloride to crystallize from an alcohol in the presence of seed crystals of Saxagliptin hydrochloride Form I-S.

4. A method of treating diabetes and/or related diseases comprising administering to a patient a therapeutically effective amount of crystalline Saxagliptin hydrochloride according to claim 3 alone or in combination with one or more types of antidiabetic agents and/or one or more other types of therapeutic agents which may be administered orally or by injection.

5. A pharmaceutical composition comprising crystalline Saxagliptin hydrochloride according to claim 1 , wherein the equilibrium relative humidity of the composition is below 50%.

6. The pharmaceutical composition of claim 5 , wherein the equilibrium relative humidity of the composition is from 10% to 40%.

7. The crystalline Form I-S of Saxagliptin hydrochloride according to claim 1 having a x-ray powder diffraction pattern comprising peaks at 24.5±0.2 and 28.2±0.2 degrees two-theta.

8. The pharmaceutical composition according to claim 2 , formulated for use in treating diabetes and/or related diseases.

Assignees

• Pichler Arthur
• Wieser Josef
• Langes Christoph
• Vukicevic Milica
• Sandoz Ag

Inventors

• Pichler Arthur
• Wieser Josef
• Langes Christoph
• Vukicevic Milica

Classifications

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P3/00

  Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00) · CPC title

• A61P3/04

  Anorexiants; Antiobesity agents · CPC title

• A61K31/403

  condensed with carbocyclic rings, e.g. carbazole · CPC title

• C07D209/52 Primary

  condensed with a ring other than six-membered · CPC title