ANILINE DERIVATIVES POSSESSING AN INHIBITORY EFFECT OF NITRIC OXIDE SYNTHASE

摘要

Compounds represented by the general formula (1):(see formula I)(where R1 is SR6 or NR7R8, where R6 is typically an alkylgroup having 1 - 6 carbon atoms, R7 is a hydrogen atom, analkyl group having 1 - 6 carbon atoms or a nitro group,and R8 is a hydrogen atom or an alkyl group having 1 - 6carbon atoms; R2 and R3 are each typically a hydrogen atomor an alkyl group having 1 - 6 carbon atoms; R4 is ahydrogen atom, an alkyl group having 1 - 6 carbon atoms oran amidino group of which the amine portion may besubstituted by an alkyl or nitro group; R5 is a hydrogenatom or an alkyl group having 1 - 6 carbon atoms; Y1, Y2,Y3 and Y4 which may be the same or different are eachtypically a hydrogen atom, a halogen atom or an alkoxygroup having 1 - 6 carbon atoms; n and m are each aninteger of 0 or 1), or possible stereoisomers or opticallyactive forms of the compounds or pharmaceuticallyacceptable salts thereof. The compounds possess a potentnitric oxide synthase inhibiting activity and are usefulas therapeutics of cerebrovascular diseases.