POLYMORPHS
First Claim
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1. Anhydrous polymorph A of the compound 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, characterised in that it melts at 206±
- 3°
C.
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Abstract
The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.
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13 Claims
- 1. Anhydrous polymorph A of the compound 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, characterised in that it melts at 206±
-
5. Polymorph C of the compound 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, characterised in that it loses water at a temperature of 30-100°
- C. and in the DSC diagram it exhibits further thermal effects at approx. 150°
C. and 175°
C. - View Dependent Claims (6, 9, 10)
- C. and in the DSC diagram it exhibits further thermal effects at approx. 150°
-
7. Anhydrous polymorph D of the compound 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, characterised in that it melts at 150±
- 3°
C.
- 3°
-
8. Anhydrous polymorph E of the compound 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, characterised in that it melts at 175±
- 3°
C.
- 3°
-
11. A method for the treatment of patients with type I and type II diabetes mellitus, prediabetes or reduced glucose tolerance, rheumatoid arthritis, obesity, or calcitonin-induced osteoporosis, as well as patients in whom an allograft transplant has been carried out, the method comprising the step of administering a pharmaceutical composition comprising at least one of the polymorphs A, B, and C, and one or more inert carriers, diluents, or carriers and diluents.
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12. A pharmaceutical composition comprising at least one of the polymorphs A, B, and C, and one or more inert carriers, diluents, or carriers and diluents.
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13. A medicament containing 0.1% to 0.5% or 0.5% to 1.5% or 1% to 3% of one of the polymorphs A, B or C, in addition to one or more inert carriers.
Specification