Patent number: 7169806
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; R1 is selected from H, C1–C6alkyl residues, (CH2)aNHW1, (CH2)bCOW2, (CH2)cOW3, CH(Me)OW4, (CH2)d—C6H4—W5 and (CH2)eSW6, where a is 2–5, b is 1–4, c is 1–2, d is 1–2, e is 1–3, W1 is COW6, CO2W6 or SO2W6, W2 is OH, NH2, OW6 or NHW6, W3 is H or W6, W4 is H or W6, W5 is H, OH or OMe, and W6 is C1–C6 alkyl, optionally substituted phenyl, optionally substituted heteroaryl or benzyl and R2 is selected from H and (CH2)n—C5H3N—Y, where n is 2–4 and Y is H, F, Cl, NO2 or CN, or R1 and R2 together are —(CH2)p— where p is 3 or 4; R3 is selected from H, C1–C6 alkyl and phenyl; R4 is selected from H, C1–C6 alkyl, benzy
Type:
Grant
Filed:
April 15, 2005
Date of Patent:
January 30, 2007
Assignee:
Ferring BV
Inventor:
David Michael Evans
Patent number: 7098238
Abstract: A pharmaceutical composition comprising a compound of formula (I) wherein X is an electron withdrawing group, Y1 is hydrogen, alkyl, alkenyl, alkynyl, aryl, heterocyclyl, —SO2R4, —CO2R4, —CONHR4 or —COR4, and each of R1, R2 and R4, which may be the same or different, is hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl or heterocyclyl, or a compound of formula (II) wherein each of Y2 and Y3, which may be the same or different, is hydrogen, alkyl, alkenyl, alkynyl, aryl, heterocyclyl, —SO2R9, —CO2R9, —CONHR9 or —COR9, Z is hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclyl, —CH?C(NHR10)CH((CH2)mCO2R11)(C?O)CH3 or —CH2(C?O)CH((CH2)mCO2R11)(C?O)CH3, R8 is —(CH2)nCO2R12, each of R5 to R7 and R9 to R12, which may be the same or different, is hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl or heterocyclyl, and each of m and n, which may be the same or different, is 1 to 6 or a compound of formula (III) wherein each of Y4 to Y6, which may be the same or
Type:
Grant
Filed:
February 26, 2001
Date of Patent:
August 29, 2006
Assignee:
Medical Research Council
Inventors:
Joseph Floyd Clark, Thomas Andrew Daniel Cadoux-Hudson, Christopher Joseph Schofield