2,3-METHANO-AMINO ACID COMPOUNDS, THEIR PRODUCING METHOD AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

摘要

PURPOSE: 2,3-methano-amino acid compounds, their producing method and a pharmaceutical composition containing the same are provided, which compounds have high selectivity to serine protease and induce the increase of TT and ACT in animals. CONSTITUTION: The 2,3-methano-amino acid compounds are represented by formula(I), in which n is 2 or 3; R1 is C3 to C8 cycloalkyl, optionally substituted phenyl or halogen, C3 to C8 cycloalkyl and optionally substituted linear or branched C1 to C6 alkyl optionally substituted by at least one of the same or different groups selected from optionally substituted phenyl; R2 is amino, amidino optionally substituted by at least one of the same or different groups selected from linear or branched C1 to C6 alkyl and hydroxy, guanidino optionally substituted by linear or branched C1 to C6 alkyl, or isothioureido optionally substituted by linear or branched C1 to C6 alkyl; Ar is aryl or single ring nitrogen-containing heteroaryl; X1 is hydroxy, amino or -NHR3( R3 is propargyl, iminomethyl, linear or branched C1 to C6 alkylsulfonyl, linear or branched aryl C1 to C6 alkylsulfonyl, -CONR3'R3", or CO2R3', CONR3'R3", hetero ring, aminosulfonyl, aryl, or linear or branched C1 to C6 alkyl optionally substituted by heteroaryl); and X1 is hydroxy group or substituted or unsubstituted amino group.