ENANTIOMERALLY PURE (-) 2- 1- (7-METHYL-2- (MORPHOLIN-4-IL) -4-OXO-4H-PYRIDO 1,2-a PYRIMIDIN-9-IL) BENZOIC ACID, ITS APPLICATION IN PHARMACOTHERAPY AND PHARMACEUTICAL COMPOSITION CONTAINING ITS

摘要

1. Enantiomerically pure (-) 2- [1- (7-methyl-2- (morpholin-4-yl) -4-oxo-4H-pyrido [1,2-a] pyrimidin-9-yl) ethylamino] benzoic acid or a pharmaceutically acceptable salt thereof. ! 2. The pure enantiomer according to claim 1, characterized in that the enantiomer is in enantiomeric excess (e.i.) ≥95%. ! 3. The pure enantiomer according to claim 1, characterized in that the enantiomer is in enantiomeric excess (e.i.) ≥99.8%, for example 99.9%. ! 4. The pure enantiomer according to claim 1, characterized in that the enantiomer is in a solid state. ! 5. The pure enantiomer according to claim 1, characterized in that the enantiomer is in a partially crystalline state. ! 6. The pure enantiomer according to claim 1, characterized in that the enantiomer is in an essentially crystalline state. ! 7. The pure enantiomer according to claim 1, characterized in that it has peaks of XRPD (X-ray powder diffraction patterns) at the following approximate values of d: 6.8, 5.9 and 3.91 Å. ! 8. The pure enantiomer according to claim 1, characterized in that it has XRPD peaks at the following approximate d values: 6.8, 6.1, 5.9, 4.98, 4.41, 4.26 and 3.91 Å. ! 9. (-) 2 - [(1R) -1- (7-methyl-2- (morpholin-4-yl) -4-oxo-4H-pyrido [1,2-a] pyrimidin-9-yl) ethylamino ] benzoic acid according to claim 7 or 8, characterized in that it has an XRPD diffraction pattern essentially as shown in FIG. ! 10. The method of obtaining the pure enantiomer according to any one of claims 1 to 9, which includes the separation of the two enantiomers methyl-2 - {[- 1- (7-methyl-2-morpholin-4-yl-4-oxo-4H-pyrido [ 1,2-a] pyrimidin-9-yl) ethyl] amino} benzoate by chiral chromatography followed by hydrolysis of methyl ether and crystallization. !eleven. The pure enantiomer according to claim 1 or a pharmaceutically acceptable salt thereof for use in pharmacotherapy. ! 12. Pharmaceutical composition containing the pure enantiomer �