BENZENE OR THIOPHEN DERIVATIVE AND USING IT AS VAP-1 INHIBITOR Russian patent published in 2014 - IPC C07C243/32 C07C243/34 C07C281/02 C07C281/06 C07D213/74 C07D233/88 C07D237/20 C07D239/42 C07D241/20 C07D241/24 C07D265/36 C07D333/36 C07D401/04 C07D409/06 C07D277/38 C07D417/04 C07D487/08 A61K31/175 A61K31/44 A61K31/4965 A61K31/4164 A61K31/426 A61K31/505 A61K31/538 A61K31/4439 A61K31/381 A61K31/4436 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound presented by formula

,

wherein A¹ means benzene or heterocycle specified in a group consisting of pyridine, pyrazine, imidazole, thiazole, pyrimidine, thiophen, pyridazine, benzoxazine and oxobenzoxazine; A² means benzene, if needed substituted by fluorine, or thiophen; B¹ means hydrogen, lower alkyl, if needed substituted by piperazinyl or morpholino, halogen-substituted lower alkyl, lower alkoxy substituted by carbamoyl, acylamino, carbamoyl or lower alkylcarbonyloxy (provided A¹ means thiazole, B¹ does not mean acylamino); B² means hydrogen or a functional group containing at least one nitrogen atom specified in a group consisting of acylamino, pyrrolidinyl, morpholino, piperidinyl, if needed substituted by acyl, piperazinyl, if needed substituted by lower alkyl or acyl, pyrazolyl, diazabicyclo[2.2.1]heptyl, if needed substituted by acyl, and di-(lower alkyl)amino, if needed substituted by amino or acylamino (provided A¹ means thiazole, B² does not mean acylamino); Y means a group presented by formula

,

wherein J means ethylene or lower alkynylene; L means a bond; M means a bond; X means -(CH₂)_m-, -(CH₂)_m-O- or -(CH₂)_m-NR²- (wherein m is an integer of 0 to 3, and R² means hydrogen); D means -NR³-, wherein R³ means hydrogen; and E means amino, or its pharmaceutically acceptable salt. The compounds of formula (I) are used for preparing a pharmaceutical agent or a pharmaceutical composition for treating or preventing the VAP-1 related diseases.

EFFECT: benzene or thiophen derivative as a VAP-1 inhibitor.

13 cl, 25 tbl, 125 ex