Isofagomine salts, methods of use and formulations
AssigneeTakeda Pharmaceutical Company Limited
InventorsHelge Reisch, Jeffrey Scott Depue, Fritz Blatter, Jennifer Robin, Michael Peter Hahn, Gaozhong Zhu, Muthuraman Meiyappan
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Abstract
The present invention relates generally to the field of pharmaceuticals, and specifically relates to isofagomine (IFG), novel salts thereof and preparation methods and uses of these, for example, in formulating pharmaceutical compositions for the treatment of Gaucher disease. Also provided are novel crystalline forms of isofagomine salts, methods for preparing the crystalline forms, and their use in formulating pharmaceutical compositions.
Claims18
A salt of isofagomine wherein the salt is selected from a quinate, maleate, fumarate, oxalate, malonate, succinate, cyclamate and ascorbate salt.
A salt of isofagomine wherein the salt is a crystalline form of isofagomine D-tartrate characterized by an x-ray diffraction pattern having three or more characteristic peaks at 2theta values selected from:
- 9.8°, ±0.2°, 10.5°±0.2°, 15°±0.2°, 15.3°±0.2°, 15.8°±0.2°, 17.4°±0.2°, 17.9°±0.2°, 18.5°±0.2°, 18.9°±0.2°, 19.6°±0.2°, 21.1°±0.2°, 21.7°±0.2°, 220° 0.2°, 24.2°±0.2°, 24.8°±0.2°, 26.6°±0.2°, 27.1°±0.2°, 27.4°±0.2°, 33.8°±0.2°, 35.7°±0.2°, 36.5°±0.2° and 37.5°±0.2°.
A method of producing an isofagomine salt comprising the steps of:
- i) dissolving an organic acid in a polar protic solvent to produce a solution 1;
- ii) dissolving isofagomine free base in a polar protic solvent to produce a solution 2;
- iii) combining solution 1 and solution 2, thereby forming a precipitate;
- and
- iv) isolating the precipitate corresponding to the isofagomine salt;
- wherein the organic acid is selected from quinic acid, fumaric acid, oxalic acid, malonic acid, D-tartaric acid, L-tartaric acid, succinic acid, cyclamic acid and ascorbic acid.
Dependencies are inferred from the claim text.