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
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