| 摘要 |
1. A hydrate of 5-[4-[2-(N-methyl-N-(2pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione, maleic acid salt, characterised in that it: (i) comprises water in the range of from 0.3 to 0.6 molar equivalents; and (ii) provides an infra red spectrum containing peaks at 1757,1331.1290,1211 and 767 cm<-1>; and/or (iii) provides a Raman spectrum containing peaks at 1758,1610,1394,1316 and 1289 cm<-1>; and/or (iv) provides a solid state nuclear magnetic resonance spectrum containing chemical shifts substantially as set out in Table l; and/or (v) provides an X-ray powder diffraction (XRPD) pattern substantially as set out in Figure IV. 2. A hydrate according to Claim 1, wherein the water content is in the range of from 0.3 to 0.5 molar equivalents. 3. A hydrate according to Claim 1 or Claim 2, which provides an infra red spectrum substantially in accordance with Figure I. 4. A hydrate according to any one of Claims 1 to 3, which provides a Raman spectrum substantially in accordance with Figure II. 5. A hydrate according to any one of Claims 1 to 4, which provides a solid state nuclear magnetic resonance spectrum substantially in accordance with Figure III. 6. A hydrate according to any one of Claims 1 to 5, which provides an X-ray powder diffraction (XRPD) pattern substantially as set out in Figure IV. 7. A hydrate according to any one of Claims 1 to 6, in isolated form. 8. A hydrate according to any one of Claims 1 to 7, in pure form. 9. A hydrate according to any one of Claims 1 to 8, in crystalline form. 10. A compound in the form of a rehydratable form of a hydrate according to any one of Claims 1 to 9. 11. A process for preparing a hydrate according to Claim 1, characterised in that 5- [4- [2- (N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione, maleic acid salt is crystallised from aqueous ethanol. 12. A process according to Claim 11, wherein the aqueous ethanol contains from 2% to 15% of water by volume. 13 A pharmaceutical composition comprising an effective, non-toxic amount of a hydrate according to Claim 1 and a pharmaceutically acceptable carrier therefor. 14. A hydrate according to Claim 1, for use as an active therapeutic substance. 15. A hydrate according to Claim 1, for use in the treatment and/or prophylaxis of diabetes mellitus, conditions associated with diabetes mellitus and certain complications thereof. 16. The use of Hydrate for the manufacture of a medicament for the treatment and/or prophylaxis of diabetes mellitus, conditions associated with diabetes mellitus and certain complications thereof. 17. A method for the treatment and/or prophylaxis of diabetes mellitus, conditions associated with diabetes mellitus and certain complications thereof, in a human or non-human mammal which comprises administering an effective, non-toxic, amount of hydrate to a human or non-human mammal in need thereof. |
