DERIVATIVES OF AMIDINO-AMINO-HALOGENATED ACIDS USEFUL AS INHIBITORS OF NITRICO-SINTASA OXIDE.

摘要

A compound of the formula (I): ** (Formula) ** or a pharmaceutically acceptable salt thereof. R1 is selected from the group consisting of hydrogen, C1-C10 alkyl, C2-C10 alkenyl and C2-C10 alkynyl; R2 is selected from the group consisting of hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, and R or Salfa-amino acid; R3 and R4 are independently selected from the group consisting of hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl and NO2; wherein R1, R2, R3 and R4 may optionally be substituted with substituents of the group consisting of C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, hydroxy, C1-C8 alkoxy, aryloxy, thiol, C1-C8 thioalkoxy, halogen, cyano, nitro, amino, carboxy, carboxy alkyl, carboxyaryl, amidino and guanidino; R11 is selected from the group consisting of hydroxyl or R or S alpha-amino acid; G is selected from the formula (CH2) p- (CX1X2) r- (CH2) sQ- (CH2) t- (CX3X4) u- (CH2 ) v, where p, r, s, t, u, v are independently 0 to 3 and Q is oxygen, C = O, S (O) a, where a is 0 to 2 or NR12 where R12 is hydrogen or C1-C10 alkyl which may be optionally substituted, when possible, with one or more substituents selected from the group consisting of C1-C10 alkyl, C1-C10 alkoxy, hydroxy, trifluoromethyl, nitro, cyano, amino and halogen; X1, X2, X3 and X4 are independently not present, or are hydrogen, halogen, C1-C10 alkyl, = CH2, C2-C10 alkenyl, or C2-C10 alkynyl, wherein C1-C10 alkyl, = CH2, C2 alkenyl C10 and C2-C10 aquinyl may be optionally substituted with one or more substituents of the group consisting of C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, hydroxy, C1-C8 alkoxy, aryloxy, thiol, C1-C8 thioalkoxy, halogen, cyano, nitro, amino, carboxy, carboxy alkyl, carboxyaryl, amidino, guanidino, trifluoromethyl; And is selected from the group consisting of heterocycle, C1-C10 haloalkyl, C1-C10 dihaloalkyl, C1C10 trihaloalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, C2-C10 alkenyl and C2-C10 alkynyl, each of which is optionally substituted with one or more substituents selected from the group consisting of halogen, hydroxy, trifluoromethyl, nitro, cyano, amino, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl and C1-C10 alkoxy; or Y may be NR9R10 where R9 and R10 are independently selected from the group consisting of hydrogen, C1-C10 alkyl, C3-C10 cycloalkyl, C2-C10 alkenyl, C2-C10 alkynyl, nitro, amino, aryl, and C1-C10 alkaryl ; with the proviso that G contains a halogen.