BETA-AMINO TETRAHIDROIMIDAZO (1,2-A) PIRAZINI I TETRAHIDROTRIAZOLO (4,3-A) PIRAZINI KAO INHIBITORI DIPEPTIDIL PEPTIDAZE ZA LIJEČENJE ILI PREVENCIJU DIJABETESA
SCOTT D. EDMONDSON,MIHAEL H. FISHER,DOOSEOP KIM,MALCOLM MACCOSS,EMMA R. PARMEE,ANN E. WEBER,JINYOU XU
申请号:
HRP20031098
公开号:
HRP20031098B1
申请日:
2003.12.30
申请国别(地区):
HR
年份:
2012
代理人:
摘要:
A compound of tetrahidroimidazol [1,2-a] pyrazines and tetrahidrotriazol [4,3-a] pyrazines of formula (1), where ar is phenyl is replaced or not replaced with 1 - 5 of R3, R3 are independently selected from the Group comprising alkyl Halogen; C1 - 6, which is linear or ramific Ado and is replaced or not replaced with 1 - 5 halogens; oalquilo C1 - 6Which is linear or branched and is replaced or not replaced with 1 - 5 halogens; and CN; X is selected from the Group comprising N and CR2; R1 and R2 are independently selected from the group consisting of hydrogen, alkyl; ns; C1 - 10, which is linear or branched and is not Sustituid Or replaced with 1 - 5 halogens or phenylThat is not replaced or substituted with 1 - 5 independently selected from Halogen substituents, CN, Oh, R4, or4, nhso2r4, so2r4, CO2H and co2alquilo C1 - 6 - 6, where the co2alquilo C1 is linear or branched; that is not replaced or substituted phenyl substituents independientement with 1 - 5 E selected from Halogen, CN, Oh, R4, or4, nhso2r4, so2r4, CO2H and co2alquilo C1 - 6Where the co2alquilo C1 - 6 is a linear or branched and heterocycle; 5 or 6 members, which may be saturated or unsaturated, comprising 1 to 4 independently heteroatoms selected from N, s and o, the unsubstituted or substituted with Heterocyclic substituents independently 1 - 3 I selected from OXO, halogen, alkyl oalquilo C1 and C1 - 6 - 6Where the alkyl oalquilo C1 and C1 - 6 - 6 are linear or branched and are optionally substituted with 1 - 5 Halogen alkyl; R4 is C1 - 6, which are linear or branched out and is replaced or not replaced with 1 - 5 groups independently selected from Halogen, CO2H and co2alquilo C1 - 6Where the co2alquilo C1 - 6 is linear or branched; and their pharmaceutically acceptable Salts and their individual Diastereomers. The compounds of formula (1) are inhibitors of Dipeptidyl peptidase IV ( "inhibitors of DP IV ") and are useful in the Treatment or prevention of diseases in which Dipeptidyl peptidase IV is i