SUBSTITUTED ACRYLAMIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION BASED ON SAID DERIVATIVE Russian patent published in 2010 - IPC C07D207/325 C07C237/22 C07C323/63 C07D207/327 C07D207/404 C07D213/30 C07D213/56 C07D215/14 C07D239/96 C07D295/14 C07D307/66 A61K31/166 A61K31/341 A61K31/381 A61K31/402 A61K31/44 A61P3/14 A61P19/10 

FIELD: chemistry.

SUBSTANCE: in formula (I') , R⁵ is any group selected from a group comprising C₁-C₆ alkoxy group, which can be substituted with one group selected from a group of β substitutes, phenyloxy group which can be substituted with one group selected from a group of γ substitutes, C₁-C₆ halogenalkoxy group and C₃-C₆ cycloalkyloxy group; R⁶ is a substitute in a benzene ring which is selected from a group of α substitutes; R⁷ is a hydrogen atom, C₁-C₆ halogenalkyl group, C₁-C₆ hydroxyalkyl group which can be substituted with a hydroxy-protective group, C₁-C₆ alkyl group which can be substituted with one group selected from a group of β substitutes, or a phenyl group which can be substituted with one hydroxy group; m equals 1; n equals 1 or 2; numbers in each benzene ring denote the number of the position of each substitute; the group of substitutes includes hydroxyl groups, nitro groups, cyano groups, C₁-C₆ dialkylamino groups, acetamide groups, halogen atoms, C₁-C₆ alkyl groups, which can be substituted with one group selected from a group of β substitutes, C₁-C₆ halogen alkyl groups, C₃-C₁₀ cycloalkyl groups, 6-member heterocyclic groups with an N atom or O atom as a heteroatom, C₃-C₆ cycloalkenyl groups, phenyl group which can be substituted with one group selected from a group of γ substitutes, 5-6-member heteroaryl groups with 1-3 N atoms as heteroatoms which can be substituted wit one or more groups selected from a group of γ substitutes, C₁-C₆ alkoxy groups, C₁-C₆ halogenalkoxy groups, C₃-C₁₀ cycloalkoxy groups, phenyloxy group, C₁-C₆ alkylthio groups, C₁-C₆ halogenalkylthio groups, C₁-C₆ alkylsulphonyl groups and C₁-C₆ alkylcarbonyl groups; the group of β substitutes includes C₁-C₆ alkoxycarbonyl groups, C₃-C₁₀ cycloalkyl groups which can be substituted with one group selected from a group of γ substitutes, C₃-C₆ cycloalkenyl groups, C₆-C₁₀ aryl groups which can be substituted with one or more groups selected from a group of γ substitutes, 5-6-member heteroaryl groups with one N, O or S heteroatom, 9-member heteroaryl groups with two heteroatoms selected from N and S, C₁-C₆ alkoxy group and C₆-C₁₀ aryloxy group; and the group of γ substitutes include cyano groups, C₁-C₆ dialkylamino groups, C₁-C₆ cyclic amino groups, halogen atoms, C₁-C₆ alkyl groups, C₃-C₁₀ cycloalkyl grous, C₁-C₆ halogenalkyl groups, C₁-C₆ alkoxy groups and C₁-C₆ alkylenedioxy groups. The invention also relates to compounds or pharmaceutically acceptable salts thereof, selected from: 4-(2-cyclopropylethoxy)-N-(2-(4-ethoxyphenyl)-1-{[(2-hydroxyethyl)amino]carbonyl}vinyl)benzamide, 4-(2-cyclopropylethoxy)-N-(2-[4-(cyclopropyloxy)phenyl]-1-{[(2-hydroxyethyl)amino]carbonyl}vinyl)benzamide, 4-(2-cyclopropylethoxy)-N-(2-[4-(difluoromethoxy)phenyl]-1-{[(2-hydroxyethyl)amino]carbonyl}-vinyl)-benzamide. Other compounds are given in the formula of invention. The invention also relates to a pharmaceutical composition which can inhibit bone resorption, which contains the disclosed compound, to use of the disclosed compound as a medicinal agent for inhibiting bone resorption, for preparing a medicinal agent for lowering concentration of calcium in the blood, for preparing a medicinal agent for inhibiting reduction of bone mass, to a medicinal agent for inhibiting bone resorption in form of the disclosed compound, to a method of inhibiting bone resorption, a method of lowering concentration of calcium in the blood, a method of inhibiting reduction of bond mass, involving addition of an effective amount of the disclosed compound.

EFFECT: more effective use of the compounds.

22 cl, 6 tbl, 116 ex