4-PYRIMIDINYL-N-ACYL-L-PHENYLALANINES AND PHARMACEUTICAL COMPOSITION Russian patent published in 2005 - IPC

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel 4-pyrimidinyl-N-acyl-L-phenylalanines of the formula (I)

or their pharmaceutically acceptable salts possessing ability to inhibit binding VCAM-1 with integrin VLA-4 (α4β1) or with cells expressing VLA-4 and useful in preparing medicinal agents used in treatment of, for example, rheumatic arthritis, cerebrospinal sclerosis, intestine inflammation and asthma. In compound of the formula (I) R₁ means group of the formula (Y-1): wherein R₂₂ and R₂₃ mean independently hydrogen atom, lower alkyl, lower alkoxy-group, halogen atom or perfluoro-lower alkyl and at least one among R₂₂ and R₂₃ doesn't mean hydrogen atom; R₂₄ means hydrogen atom, lower alkyl, lower alkoxy-group; or R₁ means group of the formula (Y-3) that means 3-7-membered cycle of the formula (Y-3): wherein R₂₅ means group of the formula: R₂₆-(CH₂)_e- wherein R₂₆ means lower alkoxy-group; Q means -(CH₂)_fN(R₂₇)-, -(CH₂)_f- wherein R₂₇ means hydrogen atom (H) or lower alkoxycarbonyl, and carbon atoms in cycle are unsubstituted; e means a whole number from 1 to 4; f means a whole number from 1 to 3; R₂ means hydrogen atom or lower alkyl; R₃ means hydrogen atom or lower alkyl; R₄ means hydrogen atom, lower alkyl, lower alkyl substituted with halide; R₅ means hydrogen atom or lower alkyl; R₆ means hydrogen atom, lower alkyl, lower alkylcarbonyloxy-lower alkyl, or R₆ means group of the formula (P-3): wherein R₃₂ means hydrogen atom; R₃₃ means lower alkyl; R₃₄ means lower alkyl wherein R₃₂ means hydrogen atom; R₃₃ means lower alkyl; R₃₄ means lower alkyl; h means a whole number from 0 to 2; g means a whole number from 0 to 2; h + g = 1-3; or R₆ means group of the formula (P-4):

wherein R₃₂, g and h have values given above; Q' means oxygen atom (O). Also, invention relates to pharmaceutical compositions.

EFFECT: valuable medicinal properties of compounds and compositions.

37 cl, 8 sch, 3 tbl, 42 ex