| 摘要 |
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 (alpha4beta1) 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 |
