| 摘要 |
<p>EP--96517 A Pharmaceutical compsn. comprises 5-(p-aminophenyl)-2(1H) pyrazinone or a deriv. of formula (I) or its salts, together with a carrier. (R1-3 are H or 1-4C alkyl; R4 is H, or (1-6C) alkoxycarbonyl opt. substd. by NH2, OH, 1-4C alkoxy or COOH (when the substituent is not on the C atom adjacent to the) or CO(NR5)n-R6; n is 0 or 1; R6 is H or 1-6C alkyl, Ph or pyridinyl all opt. substd.; and R5 is H or 1-6C alkyl; or NR5R6 is piperidino, morpholino, piperazino or N-(1-6C) alkylpiperazino) Cpds. (I) are new except for (I; R1-R4 are H). Intermediates corresp. to (I), except that NHR4 is replaced by NO2 are new. - Cpds. (I) are inotropic agents and vasodilators, and so are useful for the treatment of congestative heart failure. Dose is 0.25-25 mg/kg daily. USAB- US4514568 A 5-(4-nitrophenyl) -2(1H)-pyrazinones of formula (I) are new. In (I), R1, R2 and R3 are each H or 1-4C alkyl (pref. R1=R2=R3=H). - (I) are prepd. by nitrating (III) with fuming HNO3 and H2SO4 in vol. ratio 6:1, at about -15 deg.C.. Yield about 80%.</p> |
