| 摘要 |
Compounds which are 1-(2'-aminoacyl)-2-cyanopyrrolidine derivatives according to general formula (1) are DP-IV inhibitors for treatment of impaired glucose tolerance or type 2 diabetes; wherein A is selected from groups (2, 3 and 4); X is selected from aminoacyl groups corresponding to the natural amino acids, acyl groups R<3>CO, groups R<4>COOC(R<5>)(R<6>)OCO, methoxycarbonyl, ethoxycarbonyl and benzyloxycarbonyl; R<1> is selected from H, C1-C6 alkyl residues, (CH2)aNHW<1>, (CH2)bCOW<2>, (CH2)cOW<3>, CH(Me)OW<4>, (CH2)d-C6H4-W<5> and (CH2)eSW<6>, where a is 2-5, b is 1-4, c is 1-2, d is 1-2, e is 1-3, W<1> is COW<6>, CO2W<6> or SO2W<6>, W<2> is OH, NH2, OW<6> or NHW<6>, W<3> is H or W<6>, W<4> is H or W<6>, W<5> is H, OH or OMe, and W<6> is C1-C6 alkyl, optionally substituted phenyl, optionally substituted heteroaryl or benzyl and R<2> is selected from H and (CH2)n-C5H3N-Y, where n is 2-4 and Y is H, F, Cl, NO2 or CN, or R<1> and R<2> together are -(CH2)p-where p is 3 or 4; R<3> is selected from H, C1-C6 alkyl and phenyl; R<4> is selected from H, C1-C6 alkyl, benzyl and optionally substitued phenyl; R<5> and R<6> are each independently selected from H and C1-C6 alkyl or together are -(CH2)m-, where m is 4-6; R<7> is selected from pyridyl and optionally substituted phenyl; R<8> is selected from H and C1-C3 alkyl; and R<9> is selected from H, C1-C6 alkyl, C1-C6 alkoxy and phenyl.
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