Substituted 6- (digidroksiboril) -2- {1- 3- (2-thienyl) propyl piperidin-4-yl} norleucine as an arginase inhibitors, pharmaceutical compositions, methods of making and using

摘要

1. Substituted 6- (dihydroxyboryl) -2- {1- [3- (2-thienyl) propyl] piperidin-4-yl} norleucine compound of general formula I or racemic mixture or the individual optical isomers, or pharmaceutically acceptable salts and / or hydrates thereof, wherein: R is hydrogen, alkyl; substituted alkyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, alkenyl, cycloalkenyl, alkynyl, acyl, aroyl, halo, heteroaroyl, alkylsulfonyl, arylsulfonyl, halogen, heteroarylsulfonyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl, heteroarylaminocarbonyl, geterotsiklilaminokarbonil, alkylaminothiocarbonyl, arylaminothiocarbonyl , heteroarylaminothiocarbonyl, heterocyclylaminothiocarbonyl optionally substituted aminosulfonyl, carbamoyl; R1 represents hydrogen, alkyl; substituted alkyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, alkenyl, cycloalkenyl, alkynyl, acyl, aroyl, halo, heteroaroyl, alkylsulfonyl, arylsulfonyl, halogen, heteroarylsulfonyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl, heteroarylaminocarbonyl, geterotsiklilaminokarbonil, alkylaminothiocarbonyl, arylaminothiocarbonyl , heteroarylaminothiocarbonyl, heterocyclylaminothiocarbonyl optionally substituted aminosulfonyl, carbamoyl; R2 is hydrogen, alkyl; substituted alkyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, alkenyl, cycloalkenyl, alkynyl, acyl, aroyl, halo, heteroaroyl, alkylsulfonyl, arylsulfonyl, halogen, heteroarylsulfonyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl, heteroarylaminocarbonyl, het