IP Library › Patent Application 13563767
Patent Application
App. No. 13/563,767

POLYMORPHS

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Quick Facts
Patent No.
US None
App. No.
13/563,767
Abstract

The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.

Claims (39)

1 . An isolated form of an 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., and further characterised in that it exhibits an X-ray powder diagram having inter alia characteristic reflexes at the following d values: 11.59 Å, 7.60 Å, 7.15 Å, 3.86 Å, 3.54 Å and 3.47.

2 . (canceled)

3 . An isolated form of an anhydrous polymorph B 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 exhibits an X-ray powder diagram having inter alia characteristic reflexes at the following d values: 11.25 Å, 9.32 Å, 7.46 Å, 6.98 Å and 3.77 Å.

4 - 13 . (canceled)

14 . The isolated form of polymorph A of claim 1 , further characterised in that the reflex at 11.59 Å in the X-ray powder diagram has a relative intensity of 100% and further characterized in that the X-ray powder diagram exhibits no reflexes having a relative intensity of 1% or more at the following d values: 11.25 Å, 9.32 Å, 7.46 Å, and 6.98 Å.

15 . The isolated form of polymorph B of claim 3 , further characterised in that the reflex at 11.3 Å in the X-ray powder diagram has a relative intensity of 100% and further characterized in that the X-ray powder diagram exhibits no reflexes having a relative intensity of 1% or more at the following d values: 11.59 Å, 7.60 Å, and 7.15 Å.

16 . An isolated form of an anhydrous polymorph B 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 according to claim 3 , further characterised in that at a temperature of 10-40° C. it transforms reversibly into the polymorph A, said polymorph A characterised in that it melts at 206±3° C., and further characterised in that it exhibits an X-ray powder diagram having inter alia characteristic reflexes at the following d values: 11.59 Å, 7.60 Å, 7.15 Å, 3.86 Å, 3.54 Å and 3.47.

17 . 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, said polymorph A characterised in that it melts at 206±3° C., and further characterised in that it exhibits an X-ray powder diagram having inter alia characteristic reflexes at the following d values: 11.59 Å, 7.60 Å, 7.15 Å, 3.86 Å, 3.54 Å and 3.47, unmixed with polymorph B, said polymorph B characterised in that it exhibits an X-ray powder diagram having inter alia characteristic reflexes at the following d values: 11.25 Å, 9.32 Å, 7.46 Å, 6.98 Å and 3.77 Å.

18 . Anhydrous polymorph B 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, said polymorph B characterised in that at a temperature of 10-40° C. it transforms reversibly into the polymorph A, and further characterised in that it exhibits an X-ray powder diagram having inter alia characteristic reflexes at the following d values: 11.25 Å, 9.32 Å, 7.46 Å, 6.98 Å and 3.77 Å, unmixed with polymorph A, said polymorph A characterised in that it exhibits an X-ray powder diagram having inter alia characteristic reflexes at the following d values: 11.59 Å, 7.60 Å, 7.15 Å, 3.86 Å, 3.54 Å and 3.47.

19 . An isolated form of an 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 by its lattice metrics:

Symmetry:

monocline

spatial group:

P

a:

16.16(2) Å

b:

17.02(1) Å

c:

18.18(2) Å

β:

100.95(6)°

cell volume:

  4907(11) Å 3

20 . An isolated form of an anhydrous polymorph B 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 by its lattice metrics:

Symmetry:

monocline

spatial group:

P2 1 /c (# 14)

a:

15.23(1) Å

b:

16.94(1) Å

c:

18.79(1) Å

β:

95.6(2)°

cell volume:

   4823(3) Å 3