DERIVATIVES OF THIOAMIDE AND PHARMACEUTICAL COMPOSITION Russian patent published in 2005 - IPC

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to compounds of the formula (I):

wherein X means group of the formula (X-1) wherein R₁₅ means halogen atom, (lower)-alkyl and perfluoro-(lower)-alkyl; R₁₆ means hydrogen, halogen atom and (lower)-alkyl; or X means group of the formula (X-2) wherein Het means 5- or 6-membered heteroaromatic ring comprising 1 or 2 heteroatoms as nitrogen (N) atom; R₁₅ and R₁₆ have values indicated above for (X-1); R₃₀ means hydrogen atom or (lower)-alkyl; p means a whole number from 0 to 1; or X means group of the formula (X-3) wherein R₁₈ means aryl; R₁₉ means unsubstituted arylalkyl or heteroarylalkyl representing 6-membered heteroaromatic ring comprising nitrogen (N) atom as a heteroatom; R₂₀ means unsubstituted (lower)-alkanoyl; Y means group of the formula (Y-1) wherein R₂₂ and R₂₃ mean independently from one another hydrogen atom, (lower)-alkyl, halogen atom or perfluoro-(lower)-alkyl and at least one of radicals R₂₂ and R₂₃ doesn't mean hydrogen atom; R₂₄ means hydrogen atom; or Y means group of the (Y-3) wherein R₂₅ means group of the formula: R₂₆-(CH₂)_e- wherein R₂₆ means (lower)-alkoxy-group, (lower)-alkylthio-group, (lower)-alkylsulfonyl; or R₂₆ means group of the formula: -NR₂₈R₂₉ wherein R₂₈ means hydrogen atom; R₂₉ means (lower)-alkanoyl or (lower)-alkylaminocarbonyl; Q means -(CH₂)_f- wherein e means a whole number from 0 to 4; f means a whole number from 1 to 3; a bond denoted as a dotted line can be hydrogenated optionally; and to its pharmaceutically acceptable salts and esters. Also, invention proposes a pharmaceutical composition designated for treatment or prophylaxis of rheumatic arthritis, cerebrospinal sclerosis, intestine inflammatory disease and asthma and containing compound of the formula (I) or its pharmaceutically acceptable salt or ester in combination with a compatible pharmaceutical carrier. Invention proposes derivatives of thioamide inhibiting interaction between α₄-comprising integrins and VCAM-1.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

20 cl, 1 tbl, 86 ex