Polymorphs
The invention relates to a polymorphic forms of (S)-3-(3-(1-methyl-2-oxo-5-(pyrazolo[1,5-a]pyridine-3-yl)-1H-imidazo[4,5-b]pyridine-3(2H)-yl)piperidin-1-yl)-3-oxopropanenitrile and their use as a therapeutic agent for the treatment of respiratory diseases.
1. A polymorph of (S)-3-(3-(1-methyl-2-oxo-5-(pyrazolo[1,5-a]pyridine-3-yl)-1H-imidazo[4,5-b]pyridine-3(2H)-yl)piperidin-1-yl)-3-oxopropanenitrile with the following diffraction angles (2Theta) based on cupric Kα1:
at approximately 8.25%;
at approximately 13.25%;
at approximately 15.40°;
at approximately 17.65°; and
at approximately 25.39°.
2. A polymorph according to claim 1 further characterised as having a XPRD diffractogram as shown in FIG. 2 .
3. A polymorph according to claim 1 further characterised as having a DSC endotherm onset of 239° C.
4. A process for the preparation of the claim 1 polymorph of (S)-3-(3-(1-methyl-2-oxo-5-(pyrazolo[1,5-a]pyridine-3-yl)-1H-imidazo[4,5-b]pyridine-3(2H)-yl)piperidin-1-yl)-3-oxopropanenitrile which comprises suspending the compound as Form I in aqueous THF and heating the resulting slurry between ambient temperature and about 50° C.
5. The process according to claim 4 in which the aqueous THF comprises about 5% water.
6. A pharmaceutical composition comprising a polymorph according to claim 1 with one or more pharmaceutically acceptable excipients.
7. A composition according to claim 6 in which the excipient comprises lactose.