DERIVATIVES OF CARBOXYLIC ACIDS (VARIANTS), PHARMACEUTICAL COMPOSITION AND METHOD FO SELECTIVE BINDING αβ-INTEGRIN IN MAMMAL Russian patent published in 2005 - IPC

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of carboxylic acids of the formula: wherein Y is taken independently in each case among the group comprising C(O), N, CR¹, C(R²)(R³), NR⁵, CH; q means a whole number from 3 to 10; A is taken among the group comprising NR⁶; E is taken among the group comprising NR⁷; J is taken among the group comprising O; T is taken among the group comprising (CH₂)_b wherein b = 0; M is taken among the group comprising C(R⁹)(R¹⁰), (CH₂)_u wherein u means a whole number from 0 to 3; L is taken among the group comprising NR¹¹ and (CH₂)_n wherein n means 0; X is taken among the group comprising CO₂H, tetrazolyl; W is taken among the group comprising C, CR¹⁵ and N; R¹, R², R³ and R¹⁵ are taken independently among th group comprising hydrogen atom, halogen atom, hydroxyl, alkyl, alkoxy-group, -CF₃, amino-group, -NHC(O)N(C₁-C₃-alkyl)-C(O)NH-(C₁-C₃-alkyl), -NHC(O)NH-(C₁-C₆-alkyl), alkylamino-, alkoxyalkoxy-group, aryl, aryloxy-, arylamino-group, heterocyclyl, heterocyclylalkyl, heterocyclylamino-group wherein heteroatom is taken among N atom or O atom, -NHSO₂-(C₁-C₃-alkyl), aryloxyalkyl; R⁴ is taken among the group comprising hydrogen atom, aryl, aralkyl, benzofuranyl, dihydrobenzofuranyl, dihydroindenyl, alkyl, benzodioxolyl, dihydrobenzodioxynyl, furyl, naphthyl, quinolinyl, isoquinolinyl, pyridinyl, indolyl, thienyl, biphenyl, 2-oxo-2,3-dihydro-1H-benzimidazolyl, pyrimidinyl and carbazolyl. Other values of radicals are given in the claimed invention. Also, invention relates to pharmaceutical composition used for inhibition binding α₄β₁-integrin in mammal based on these compounds. Invention provides preparing new compounds and pharmaceutical composition based on thereof in aims for treatment or prophylaxis of diseases associated with α₄β₁-integrin.

EFFECT: improved method for inhibition, valuable medicinal properties of compounds.

33 cl, 7 tbl, 42 ex