Compound inhibitor of Dipeptidyl peptidase IV (DP IV) or CD26, Pharmaceutical composition containing same and their use for preparing the composition

摘要

Compound inhibitor of Dipeptidyl peptidase IV (DP IV, CD26) or formula (1), and pharmaceutically acceptable salts, tautu00f3meros stereoisomers, where X1 is selected from Oxygen, sulfur, sulfinilo, sulfonyl and methylene; x2 is selected from - or - S -, - and - methylene carbonyl; X3 is NR5 or or Tiocarbonilo; r1 is Hydrogen or Nitrile; R2 and R3 are independently H and Lower alkyl,Or can be co - P - (CH2); R4 is R4A when X3 is - When r4b NR5 and X3 is a carbonyl group or tiocarbonilo; R4A is r6r7nc (= o), r6r7nc (= S), R8 (CH2) QC (= o) - (CH2) QC (R8 = S), R8 (CH2) qso2, R8 (CH2) QOC (= S) and R8 (CH2) (= OR); r4b QOC is r6r7n; R5 is H or alkyl of C1 - 6; R6 and R7 are each Independent. Dently R8 (CH2) or jointly are Q - (CH2) 2 - Z - (CH2) 2 - or - chr9 - Z2 - CH2 - chr10 - R8 is H, alkyl,;Benzofusionado cycloalkyl, acyl, dialcyl Carbamoyl, dialquilamino, N - alquilpiperidililo, optionally substituted aryl, aroilo - alquilbencilo optionally substituted, optionally substituted, optionally substituted heteroaryl arilsulfonilo and optionally substituted; R9 and R10 are independent DID H, carbamoilo, Hydroxymethyl and cianometilo; Z1 is a Covalent Bond, - (CH2) -, - O -,SOT -, and - N - ((CH2) qr8); Z2 is an Ortho phenylene Group optionally substituted; M is 1 - 3; n is 0 - 4 is 2 - 5; P; Q is 0 - 3; R is 1 or 2; and t is 0 - 2, provided that when x2 is CH2, NH is r8ch2o X3 is R4 and R8 (CO) then it is not nitrofenilo substituted phenyl or not. Pharmaceutical composition comprising at least one of said compounds.Use for preparing a composition useful for the treatment of Type 2 diabetes, impaired glucose tolerance, Growth Hormone deficiency, polycystic ovary syndrome, and Autoimmune and inflammatory diseases.