4-(4-CYANO-2-THIOARYL)-DIHYDROPYRIMIDINONES AND USING THEM Russian patent published in 2013 - IPC C07D239/22 C07D401/04 A61K31/506 A61K31/505 A61P11/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new 4-(4-cyano-2-thioaryl)- dihydropyrimidin-2-one derivatives of formula (I), a method for preparing and using them. In formula , , both A and E mean C-R⁷, wherein R⁷ mean hydrogen, Z means O, n means the number 0,1 or 2, R¹ means (C₁-C₆)-alkyl which may be substituted by the group hydroxy, (C₁-C₄)-alkoxy,(C₃-C₆)-cycloalkyl, phenyl or 5- or 6-member heteroaryl with two heteroatoms specified in nitrogen or sulphur, or may be substituted up to three times by fluorine, or means (C₃-C₆)-cycloalkyl or phenyl, R² means hydrogen, R³ means cyano or a group of formulas -C(=O)-R⁸, -C(=O)-O-R⁸ or -C(=O)-NH₂, wherein R⁸ means (C₁-C₆)-alkyl or (C₃-C₆)-alkenyl, R⁴ means methyl or ethyl, or R³ and R⁴ are linked to each other and together form an annulated group of formula (II), R⁹ means hydrogen, (C₁-C₆)-alkyl or (C₃-C₆)-cycloalkyl with (C₁-C₆)-alkyl may be substituted by a hydroxy group, aminocarbonylamino or (C₁-C₄)-acylamino, R⁵ means hydrogen or (C₁-C₆)-alkyl. The other group and radical values are specified in the patent claim.

EFFECT: compounds possess the properties of a neutrophil elastase (HNE) inhibitor and can find application in treating and/or preventing pulmonary arterial hypertension (PAH), chronic obstructive pulmonary disease (COPD), acute lung injury (ALI), acute respiratory distress syndrome (ARDS), pulmonary emphysema, mediated by neutrophil elastase (HNE) activity.

16 cl, 4 tbl, 10 dwg, 202 ex