2-CYANOPYRIMIDINE-4-YL CARBAMATE, OR A UREA DERIVATIVE, OR ITS SALT AND A PHARMACEUTICAL COMPOSITION CONTAINING THEM Russian patent published in 2023 - IPC C07D239/28 C07D401/12 C07D403/12 C07D405/12 C07D413/12 A61K31/421 A61K31/505 A61P19/10 

FIELD: pharmaceutical industry.

SUBSTANCE: group of inventions relates to pharmaceutical chemistry, namely to a compound of formula 1 or to a compound selected from a group consisting of 1-(4-(2-cyanopyrimidine-4-yl)tetrahydro-2H-piran-4-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)urea and 1-(1-(2-cyanopyrimidine-4-yl)cyclohexyl)-3-(4'-ethyl-[1,1'-diphenyl]-4-yl)urea, their pharmaceutically acceptable salts, pharmaceutical composition and reagent based on them. In formula 1, A is a chemical bond, -CH₂- or -C(CH₃)₂-, L is -(CH₂)m-O-, -(CH₂)_n-NH-, -CH(CH₃)-NH- or -N(CH₃)-, m is 1 or 2, n is 0, 1 or 2, Ar is an aromatic ring selected from a group consisting of phenyl, phenoxyphenyl, pyridinylphenyl, indazolylphenyl, morphololphenyl, piperazinylphenyl, piperidinylphenyl, pyrazolylphenyl, benzyl-phenyl, phenylaminophenyl, diphenyl, piperazinyl-diphenyl, morpholinyl-diphenyl, naphthyl, benzodioxolyl, furanyl, indazolyl, quinoxalinyl and indanyl, and the aromatic ring is selectively replaced by substituents in the amount of one to three, selected from a group consisting of halogen, cyano, hydroxy, trifluoromethyl, C₁~C₄ alkyl, C₃~C₆ cycloalkyl, C₁~C₄ alkoxy, hydroxy- C₁~C₄ alkyl, C₁~C₄ alkoxy- C₁~C₄ alkyl, hydroxycarbonyl- C₁~C₄ alkyl, C₁~C₄ alkoxycarbonyl C₁~C₄ alkyl, C₁~C₄ alkoxy- C₁~C₄ alkoxy alkyl, alkylcarboxylic- C₁~C₄ alkyl, amino-C₁~C₄ alkoxy, mono - or di- C₁~C₄ alkylamino C₁~C₄ alkoxy, aminosulfonyl, C₁~C₄ alkyl-sulfonyl, trifluoromethysulfonyl, C₃~C₆ cycloalkylcarbonyl, mono - or di- C₁~C₄ alkylamino, C₁~C₄ alkylcarbonylamino, methanesulfonylamido, C₁~C₄ alkylarbonyl, hydroxycarbonyl, mono- or di- C₁~C₄ alkylaminocarbonyl, oxolanyl- C₁~C₄ alkylaminocarbonyl, di- C₁~C₄ alkylamino- C₁~C₄ alkylaminocarbonyl, imidazolyl- C₁~C₄ alkylaminocarbonyl, C₁~C₄ alkoxy- C₁~C₄ alkylaminocarbonyl, C₃~C₆ cycloalkylcarbonyl, pyrrolidinylcarbonyl, triazolyl- C₁~C₄ alkylaminocarbonyl, C₁~C₄ alkoxycarbonyl alkynyl, hydroxycarbonyl- C₂~C₄ alkynyl, hydroxy- C₁~C₄ alkylphenyl- C₁~C₄ alkynyl and C₁~C₄ alkoxy- C₁~C₄ alkylphenoxymethyl.

EFFECT: derivatives of 2-cyanopyrimidine-4-ilcarbamate and urea derivatives that selectively inhibit cathepsin K and can be used in the treatment of osteoporosis.

<Formula 1>

12 cl, 7 tbl, 192 ex