| abstract |
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 R1 is hydrogen, a C¿1-6? 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 R4 is hydrogen or C¿1-6? alkyl; and R?3¿ is hydrogen, C¿1-6? alkyl, or a group NR?5R6¿ wherein R?5 and R6¿ are independently hydrogen or C¿1-6? alkyl, provided that R?3¿ is not NR5R6 when X is oxygen or S(O)¿n?; R?1a and R1b¿ are independently selected from hydrogen or halo; R2 is a C¿1-14? 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; N¿3?; 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 R8 is hydrogen or C¿1-6? alkyl and R?7¿ is hydrogen, C¿1-6? alkyl or a group NR?9R10¿ wherein R?9 and R10¿ are independently hydrogen or C¿1-6? alkyl; or R?2¿ is substituted by a group (a), wherein R11 has a definition the same as for R1; with the proviso that when R1 is a C¿1-6? alkyl group and R?2¿ is a C¿1-14? hydrocarbyl substituted by two groups ZR?7¿ wherein one group ZR7 is CO¿2?H, the other group ZR?7¿ is not NH¿2?. |