PYRIDOXAZINONE DERIVATIVES AS TNAP INHIBITORS Russian patent published in 2020 - IPC C07D498/04 A61K31/4353 A61K31/553 A61P19/00 

FIELD: chemistry.

SUBSTANCE: invention refers to a compound of general formula (I):

or its pharmacologically acceptable salt. In formula (I): R¹ represents a hydrogen atom, a C1-6 alkyl group (where the alkyl group is optionally substituted with one to three groups which can be identical or different and are selected from the following substitutes: hydroxyl group, C1–6 alkoxy group, C6–10 aryl group optionally substituted with one or two C1–6 alkoxy groups), C6–10 aryl group or 3–10-member heterocyclyl group containing from one to four nitrogen atoms, R ² and R³ are identical or different and each represents a hydrogen atom, a C1–6 alkyl group (where the alkyl group is optionally substituted with one to three groups which can be identical or different and are selected from the following substitutes: a hydroxyl group, an aminocarbonyl group optionally substituted with one or two groups which can be identical or different C1–6 alkyl groups), 3–10-member heterocyclyl group containing from one to four nitrogen atoms, 3–10-member heterocyclylcarbonyl group containing from one to four nitrogen or oxygen atoms, an aminocarbonyl group (where the aminocarbonyl group is optionally substituted with one or two groups which can be identical or different C1–6 alkyl groups), or R² and R³, which are C1–6 alkyl groups, are optionally linked to each other to form 3–6-member saturated carbocyclic ring, R⁴ and R⁵ are identical or different and each represents a hydrogen atom or a C1–6 alkyl group, R⁶ is a hydrogen atom, each of substitutes R⁷, which can be identical or different, is a C1-6 alkoxy group (where the alkoxy group is optionally substituted with one to three halogen groups which can be identical or different), or halogen group, X is -CH = or -C(-R⁷)=, m is integer from 1 to 4. Also disclosed are a compound of formula (Ia), a pharmaceutical composition, a TNAP inhibitor, a method of treating, a TNAP inhibition method, use of the compound to produce a pharmaceutical composition.

EFFECT: disclosed compounds have tissue-specific alkaline phosphatase (TNAP) inhibiting activity and can be used to treat an elastic pseudo-xanthoma and other diseases.

22 cl, 2 tbl, 69 ex