发明名称 TARTRATE SALTS OF THIAZOLIDINEDIONE DERIVATIVES
摘要 1. A compound 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione, L (+) tartrate salt or a solvate thereof. 2. A compound according to claim 1, characterised in that it provides: (i) an infrared spectrum substantially in accordance with Figure 1; (ii) a Raman spectrum substantially in accordance with Figure 2; (iii) an X-Ray powder diffraction pattern (XRPD) substantially in accordance with Table 1 or Figure 3; or (iv) a Solid State <13>C NMR spectrum substantially in accordance with Figure 4. 3. A compound according to claim 1, characterised in that it provides two or more of: (i) an infrared spectrum substantially in accordance with Figure 1; and (ii) a Raman spectrum substantially in accordance with Figure 2; and (iii) an X-Ray powder diffraction pattern (XRPD) substantially in accordance with Table 1 or Figure 3; and (iv) a Solid State <13>C NMR spectrum substantially in accordance with Figure 4. 4. A compound according to any one of claims 1 to 3, in purified form. 5. A compound according to any one of claims 1 to 3, in a solid dosage form. 6. A compound according to any one of claims 1 to 3, in a pharmaceutically acceptable form capable of being milled. 7. A compound according to any one of claims 1 to 3, in a pharmaceutically acceptable form having good flow properties. 8. A process for preparing the L (+) Tartrate or a solvate thereof, characterised in that 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione (Compound (I) or a salt thereof is reacted with a source of L (+) tartrate ion and thereafter, if required, a solvate of the resulting L (+) tartrate is prepared, and the L (+) Tartrate or a solvate thereof is recovered. 9. A pharmaceutical composition comprising 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyljthiazolidine-2,4-dione L (+) tartrate or a solvate thereof and a pharmaceutically acceptable carrier therefor. 10. A compound 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione L (+) tartrate or a solvate thereof for use as an active therapeutic substance. 11. A use of 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione L (+) tartrate or a solvate thereof, for the manufacture of a medicament for the treatment and/or prophylaxis of diabetes mellitus, conditions associated with diabetes mellitus and certain complications thereof.
申请公布号 EA005295(B1) 申请公布日期 2004.12.30
申请号 EA20030000232 申请日期 2001.08.03
申请人 SMITHKLINE BEECHAM P.L.C. 发明人 CHOUDARY, BERNADETTE, MARIE;CRAIG, ANDREW, SIMON;HO, TIM, CHIEN, TING;MACKENZIE, DONALD, COLIA;O'KEEFFE, DEIRDE
分类号 A61K31/4439;A61P3/08;A61P3/10;C07D417/12;(IPC1-7):C07D417/12;A61K31/44 主分类号 A61K31/4439
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