IP Library › Granted Patent US 8,865,729
Granted Patent B2
US 8,865,729 · App. 13/140,853 · Granted Oct 21, 2014

Salt forms of a xanthine compound

Inventors: Peter Sieger (Mittelbiberach, DE); Waldemar Pfrengle (Biberach an der Riss, DE)
Assignee: Boehringer Ingelheim International GmbH
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Quick Facts
Patent No.
US 8,865,729
App. No.
13/140,853
Granted
Oct 21, 2014
Kind
B2
Abstract

The present invention relates to novel salt forms of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, a DPP-4 inhibitor and their use in pharmaceutical compositions useful in the treatment of type 2, diabetes, as well as their production.

Claims (11)

1. A salt of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine and a pharmaceutically acceptable acid in a 1:1 stoichiometry in the form of an organic solvate, hydrate, or mixed hydrate/organic solvate thereof.

2. An acid addition salt of 1-[(4-methyl-quinazolin-2-yl)-methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine with an acid selected from hydrochloric acid, hydrobromic acid, phosphoric acid, nitric acid, sulfuric acid, acetic acid, 2,2-dichloroacetic acid, adipic acid, D-ascorbic acid, L-ascorbic acid, D-aspartic acid, L-aspartic acid, benzenesulfonic acid, benzoic acid, 4-acetamido-benzoic acid, (+)-camphoric acid, (−)-camphoric acid, (+)-camphor-10-sulfonic, (−)-camphor-10-sulfonic, capric acid (decanoic acid), caproic acid (hexanoic acid), caprylic acid (octanoic acid), carbonic acid, cinnamic acid, citric acid, cyclamic acid, dodecylsulfuric acid, ethane-1,2-disulfonic acid, ethanesulfonic acid, 2-hydroxy-ethanesulfonic acid, formic acid, fumaric acid, galactaric acid, gentisic acid, D-glucoheptonic acid, L-glucoheptonic acid, D-gluconic acid, L-gluconic acid; D-glucuronic acid, L-glucuronic acid, glutamic acid, glutaric acid, 2-oxo-glutaric acid, glycerophosphoric acid, glycolic acid, hippuric acid, isobutyric acid, D-lactic acid, L-lactic acid, lactobionic acid, lauric acid, maleic acid, D-malic acid, L-malic acid, malonic acid, D-mandelic acid, L-mandelic acid, methanesulfonic acid, naphthalene-1,5-disulfonic acid, naphthalene-2-sulfonic acid, 1-hydroxy-2-naphthoic acid, nicotinic acid, oleic acid, orotic acid, oxalic acid, palmitic acid, pamoic acid (embonic acid), propionic acid, D-pyroglutamic acid, L-pyroglutamic acid, salicyclic acid, 4-aminosalicyclic acid, sebacic acid, stearic acid, succinic acid, D-tartaric acid, L-tartaric acid, thiocyanic acid, p-toluenesulfonic acid and undecylenic acid,

in the form of an organic solvate, hydrate, or mixed hydrate/organic solvate thereof.

3. The salt according to claim 2 , which is selected from the group consisting of a besylate salt, a hydrobromide salt, a benzoate salt, an esylate salt, a fumarate salt, a mesylate salt, a salicylate salt, a tosylate salt, a hydrochloride salt, a glycolate salt, a malonate salt and a gentisate salt.

4. The salt according to claim 2 , in the form of a solvate.

5. The salt according to claim 2 , in the form of an organic solvate.

6. The salt according to claim 2 , in the form of a hydrate.

7. The salt according to claim 2 , in the form of a mixed hydrate/organic solvate.

8. The salt according to claim 2 , in crystalline, partially crystalline, amorphous or polymorphous form.

9. A pharmaceutical composition comprising a salt according to claim 1 , optionally together with one or more pharmaceutically acceptable carriers and/or diluents.

10. The pharmaceutical composition according to claim 9 , further comprising one or more other active substances.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 27, 2011
From: SIEGER, PETER; PFRENGLE, WALDEMAR
To: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Reel/Frame 026972/0012 →
Priority Claims (1)
EP 08172785 · Dec 23, 2008 · regional
Continuity (1)
Related Publication 20120129874A1 · May 24, 2012