ACETAMIDINE DERIVATIVES AND THEIR USE AS INHIBITORS FOR THE NITRIC OXIDE SYNTHASE

摘要

A class of acetamidine derivatives of general formula (I), methods for the manufacture thereof in therapy, particularly as inhibitors of nitric oxide synthase, is disclosed or a salt thereof, wherein R<1> is hydrogen, a C1-6 hydrocarbyl group optionally substituted by halo, halo, nitro, cyano or a group XR<3> wherein X is oxygen, C(O)m wherein m is 1 or 2, S(O)n wherein n is 0, 1 or 2, or a group NR<4> wherein R<4> is hydrogen or C1-6 alkyl; and R<3> is hydrogen, C1-6 alkyl, or a group NR<5>R<6> wherein R<5> and R<6> are independently hydrogen or C1-6 alkyl, provided that R<3> is not NR<5>R<6> when X is oxygen or S(O)n; R<1a> and R<1b> are independently selected from hydrogen or halo; R<2> is a C1-14 hydrocarbyl group which may optionally contain one or two heteroatoms, the group R<2> being optionally substituted by one or more groups independently selected from halo; N3; nitro; CF3; ZR<7> wherein Z is oxygen, C(O)m', wherein m' is 1 or 2, S(O)n', wherein n' is 0, 1 or 2, or a group NR<8> wherein R<8> is hydrogen or C1-6 alkyl and R<7> is hydrogen, C1-6 alkyl or a group NR<9>R<10> wherein R<9> and R<10> are independently hydrogen or C1-6 alkyl; or R<2> is substituted by a group (a), wherein R<11> has a definition the same as for R<1>; with the proviso that when R<1> is a C1-6 alkyl group and R<2> is a C1-14 hydrocarbyl substituted by two groups ZR<7> wherein one group ZR<7> is CO2H, the other group ZR<7> is not NH2.