| 摘要 |
Aryl alkenamides derivatives of Formula I or a pharmaceutically acceptable salt thereof are novel MCP-1 antagonists and are thus useful in the treatment of inflammation, atherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection V=O, S, NH or a bond; Ar can be unsubstituted or substituted benzimidazole, phenyl, biphenyl, pyridyl, naphthyl, quinoline, isoquinoline or indole; n=2-6; m=1-3; X=O (oxygen), S (sulfur), =CH2, =NH or H2; R1 and R2 can independently be hydrogen, lower alkyl of from 1-4 carbon atoms, -(CH2)nOR6, -(CH2)nNR3R4, -(CH2)n'CONR3R4, -(CH2)n'COOR6, -(CH2)rAr', where n'=0-6 r=0-4 R3 and R4 can independently be hydrogen, lower alkyl of from 1-4 carbon atoms, -(CH2)nOR6, or -(CH2)m-Ar', which can be unsubstituted or substituted with up to 3 substitutents, where "Ar'" is phenyl, pyridyl, or indole; R3 and R4 may also be taken together to form a cyclic ring of 3-8 atoms which may also contain oxygen or the group NR5 where R5 can be hydrogen, lower alkyl of from 1-4 carbon atoms, cycloalkyl of from 5-12 carbon atoms, or -(CH2)m-Phenyl, which can be unsubstituted or substituted with up to 3 substitutents; R6 can be hydrogen, lower alkyl or (CH2)m-Phenyl; m=1-3; R1 and R2 may be also taken together to form a ring of 3-8 atoms which may also contain oxygen or the group NR5, which ring may be substituted on one or more carbon atoms with the group NR3R4; the subtituents are defined as: halogen, nitro, CF3, alkyl of from 1-12 carbon atoms; -(CH2)rOR6 -(CH2)rNR3R4 -(CH2)rCONR3</su
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