Antidiabetic agents

Details Antidiabetic agents Antidiabetic agents

2007-01-30

2007-01-30

Shameem, Golam M. M. (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C548S530000, C548S540000

Reexamination Certificate

active

11106594

ABSTRACT:
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 R3CO, groups R4COOC(R5)(R6)OCO, methoxycarbonyl, ethoxycarbonyl and benzyloxycarbonyl; R1is selected from H, C1–C6alkyl residues, (CH2)aNHW1, (CH2)bCOW2, (CH2)cOW3, CH(Me)OW4, (CH2)d—C6H4—W5and (CH2)eSW6, where a is 2–5, b is 1–4, c is 1–2, d is 1–2, e is 1–3, W1is COW6, CO2W6or SO2W6, W2is OH, NH2, OW6or NHW6, W3is H or W6, W4is H or W6, W5is H, OH or OMe, and W6is C1–C6alkyl, optionally substituted phenyl, optionally substituted heteroaryl or benzyl and R2is selected from H and (CH2)n—C5H3N—Y, where n is 2–4 and Y is H, F, Cl, NO2or CN, or R1and R2together are —(CH2)p— where p is 3 or 4; R3is selected from H, C1–C6alkyl and phenyl; R4is selected from H, C1–C6alkyl, benzyl and optionally substitued phenyl; R5and R6are each independently selected from H and C1–C6alkyl or together are —(CH2)m—, where m is 4–6; R7is selected from pyridyl and optionally substituted phenyl; R8is selected from H and C1–C3alkyl; and R9is selected from H, C1–C6alkyl, C1–C6alkoxy and phenyl.

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