PRODRUG OF TRIAZOLONE COMPOUND Russian patent published in 2016 - IPC C07D401/14 C07D403/04 A61K31/506 A61P7/02 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a new compound of formula (I) or its pharmaceutically acceptable salt possessing the properties of blood coagulation inhibitor. In the compound of formula (I) , R¹ represents 1) phenyl optionally substituted by one to three C₁-C₆alkyl groups, 2) C₁-C₆alkoxy or 3) C₂-C₆alkenyloxy; R² represents a hydrogen atom, C₁-C₆alkylcarbonyl or pyridylcarbonyl; each of R³ and R⁴ independently represents a hydrogen atom or C₁-C₆alkyl; A represents a single bond, oxygen atom, or a group presented by formula (II) , wherein each of R^a and R^b independently represents a hydrogen atom or C₁-C₆alkyl, whereas *1 and *2 mean a binding to carbonyl and R⁵, respectively, in formula (I), or a group presented by formula (III) , wherein each of R^c, R^d, R^e and R^f independently represents a hydrogen atom or C₁-C₆alkyl, whereas *1 and *2 are characterised by the same values described above; and R⁵ represents C₁-C₆alkyl or C₃-C₈cycloalkyl, whereas C₁-C₆alkyl or C₃-C₈cycloalkyl in R⁵ is independently substituted by one to three identical or different substitutes specified in a group of substitutes consisting of a halogen atom, C₁-C₆akyl and C₁-C₆alkoxy.

EFFECT: compounds can find application in the diseases caused by thrombus formation, such as thrombosis, deep-vein thrombosis, pulmonary embolism, cerebral infarction, myocardial infarction, acute coronary syndrome, vascular restenosis, disseminated intravascular coagulation, or malignant tumour.

16 cl, 6 dwg, 5 tbl, 68 ex