TH87142A - (5Z) -5- (6-quinosalinylmethylidene) -2- (2,6-dichlorophenyl) amino) -1,3-thiazole-4 ( 5H) - transfer - Google Patents

Abstract

DC60 (08/08/49) The invented compound is (5Z)-5-(6-quinosalinylmethylidine)-2-[(2,6-dichlorophenyl)amino]-1,3-thiazole-4(5H)-one and/or its pharmacologically acceptable salts, hydrates, solvates and products. Also invented is a pharmacological mixture containing this compound, a method for preparing this compound and its pharmacologically acceptable salts, hydrates, solvates and products. Also invented is a method for using this compound as an hYAK3 protein inhibitor. The invented compound is (5Z)-5-(6-quinosalinylmethylidine)-2-[(2,6-dichlorophenyl)amino]-1,3-thiazole-4(5H)-one and/or its pharmacologically acceptable salts, hydrates, solvates and products. Its pharmaceutical acceptance, including the development of pharmaceutical mixtures containing this compound, methods for preparing this compound and its pharmaceutically acceptable salts, hydrates, solvates, and products, and methods for using this compound as an hYAK3 protein inhibitor, are all aspects of its development.

Claims (37)

1. Compound (5Z)-5-(6-quinosalinylmethylidine)-2-[(2,6-dichlorophenyl)amino]-1,3-thiazole-4(5H)-one 2. Pharmaceutically acceptable salts, hydrates, solaves and products of the compounds of claim 1. 3. Compound (5Z)-5-(6-quinosalinylmethylidine)-2-[(2,6-dichlorophenyl)amino]-1,3-thiazole-4(5H)-one meglumine 4. Pharmaceutically acceptable hydrates and solvattes of the compounds of claim 3. 5. Monosodium salt of the compound of claim 1. 6. Monosodium salt conforming to claim 5 is a hydrate. 7. Compounds of claim 6 in which the hydrate contains less than 5.25% water of the solution. 8. A pharmaceutical mixture containing the compounds of claim I and a pharmaceutically acceptable carrier. 9. A pharmaceutical mixture containing the pharmacologically acceptable salts, hydrates, solvates, and products of the compounds of claim I and a pharmacologically acceptable carrier. 10. The compound conforming to claim 3 is a hydrate. 11. The hydrated compound of claim 10 is the monohydrate. 12. Compounds of claim 11 that contain hydrated water of solution 1 plus or minus 10%. 13. Compounds of claim 11 in which the hydrate contains less than 1% of the solvation water. 14. The compound of claim 3 is an anhydrate. 15. A pharmaceutical mixture containing the compounds of claim 3 and a pharmaceutically acceptable carrier. 16. A pharmaceutical mixture containing the pharmaceutically acceptable hydrate and solvate of the compounds of claim 3 and a pharmaceutically acceptable carrier. 17. A pharmaceutical mixture containing the compounds of claim number 4 and a pharmaceutically acceptable carrier. 18. The process for preparing a pharmaceutical mixture containing a pharmaceutically acceptable carrier or diluent and the resulting quantity of the compound of claim 1, which involves the combination of the compound of claim 1 with a pharmaceutically acceptable carrier or diluent. 19. The process for preparing pharmaceutical mixtures containing pharmaceutically acceptable carriers or diluents and the resulting quantities of pharmaceutically acceptable salts, hydrates, solvates and/or products of the compounds of claim 1, which involves the incorporation of pharmaceutically acceptable salts, hydrates, solvates and/or products of the compounds of claim 1 into the pharmaceutically acceptable carriers or diluents. 20. The process for preparing a pharmaceutical mixture containing a pharmaceutically acceptable carrier or diluent and the resulting quantity of the compound of claim 3, which involves the combination of the compound of claim 3 with a pharmaceutically acceptable carrier or diluent. 21. The process for preparing pharmaceutical mixtures containing a pharmaceutically acceptable carrier or diluent and the resulting amount of the pharmaceutically acceptable hydrate, solvate and/or productus of the compound of claim 3, which involves the integration of the pharmaceutically acceptable hydrate, solvate and/or productus of the compound of claim 3 with a pharmaceutically acceptable carrier or diluent. 22. The use in therapeutic doses of the compounds of claim 1 and/or their pharmaceutically acceptable salts, hydrates, solvates and products for hYAK3 inhibition in patients. 23. Application of claim #22, which states that the patient is a human being. 24. Use of therapeutic doses of the compounds of claim 3 and/or their pharmaceutically acceptable hydrates and solvates for hYAK3 inhibition in patients. 25. Application of claim 24, which states that the patient is a human being. 26. The use in therapeutic doses of the compounds of claim 1 and/or one or more pharmaceutically acceptable salts, hydrates, solvates and their products, and in one or more pharmaceutically acceptable carriers, diluents and excipients in patients for the treatment or prevention of hematopoietic deficiency, particularly in the treatment of erythroid deficiency. 27. The use of claim 26, in which erythroid and hematopiatic system deficiency is selected from a group comprising anemia, congenital anemia, spinal cord development abnormalities, congenital anemia, spinal cord reduction, and cytopenia. 28. The use in therapeutic doses of the compounds of claim 3 and/or their pharmaceutically acceptable hydrates, solvates and products, and one or more pharmaceutically acceptable carriers, diluents and excipients in patients for the treatment or prevention of hematopoietic deficiency, particularly in the treatment of erythroid deficiency. 29. The use of claim 28, in which erythroid and hematopoietic system deficiencies are selected from a group comprising anemia, congenital anemia, spinal cord dysfunction, congenital anemia, spinal cord reduction, and cytopenia. 30. The use in therapeutic doses of the compounds of claim I and/or one or more of their pharmaceutically acceptable salts, hydrates, solvates and pharmaceutically acceptable products and carriers, diluents and pharmaceutically acceptable excipients in patients for the treatment or prevention of disease of a select group of anemia, congenital anemia, spinal cord dysfunction, congenital anemia, spinal cord reduction and cytopenia. 31. The use in therapeutic doses of the compounds of claim 3 and/or their hydrates, and their pharmaceutically acceptable solvates, and one or more pharmaceutically acceptable carriers, diluents, and excipients in patients for the treatment or prevention of a selected disease from the group comprising anemia, congenital anemia, spinal cord dysfunction, congenital spinal cord reduction, and cytopenia. 32. Application of Claim 27, which states that the patient is a human being. 33. Application of Claim 29, which states that the patient is a human being. 34. The use in therapeutic doses of a) the compounds of claim I and/or their pharmaceutically acceptable salts, hydrates, solves and products, and b) EPO or its derivatives for the treatment of hematopoietic disorders in patients requiring such treatment. 35. The use in therapeutic doses of a) the compounds of claim 3 and/or their pharmaceutically acceptable hydrates and solvates, and b) EPO or its derivatives, for the treatment of hematopoietic deficiency in patients requiring such treatment. 36. The compound of claim 3 in crystalline form. 37. The compound of claim 36 with the IR band of Figure 3.