发明名称 ORTHO SUBSTITUTED DIHYDROXY-2(1H)QUINAZOLINONE-1-ALKANOIC ACIDS
摘要 Cpds. of formula (I) and their quat. salts with alkyl halides, alkali (ne earth) metal salts and the amine salt, aminoalcohol salts and aminoacid salts are new. In (I) R1 is H, NH2 or N02; R2 is H, alkyl, cycloalkyl, cycloalkylalkyl, haloalkyl or bicycloalkyl; R3 and R4 are H, lower alkyl, or aryl (opt. substd. by alkyl, lower alkoxy or OH); R5 is H, lower alkyl, or opt. substd. benzyl, provided that when R5 is other than H, the cpd. is a quat. salt; X is benzyl, COOH, alkoxycarbonyl, CN, CONH2, methane sulphonyl, formyl, alkanoyl, aroyl, heteroaroyl or heteroaryl; and Y and Z are H or OH, at least one being OH and when both are OH, they are in the 5,6- or 6,7- posn. Intermediates of formula (II) are also new. (R6 is lower alkyl; and R7 is H or is absent). Cpds. (I) are renal vasodilators and cardiovascular agents, and some intermediates in their prepn. are cardiotonic agents. Dose is 15-300 mg/kg.
申请公布号 DE3376978(D1) 申请公布日期 1988.07.14
申请号 DE19833376978 申请日期 1983.09.29
申请人 ORTHO PHARMACEUTICAL CORPORATION 发明人 BANDURCO, VICTOR T.;LEVINE, SEYMOUR D.;MULVEY, DENNIS M.;TOBIA, ALFONSO J.
分类号 A61K;A61K31/395;A61K31/495;A61K31/505;A61K31/80;C07D;C07D239/00;C07D239/10;C07D239/22;C07D239/36;C07D239/72;C07D239/80;C07D401/06;C07D401/14;C07D405/06;C07D405/14;C07D409/06;C07D409/14;C07D417/06;C07D417/14;(IPC1-7):C07D239/80 主分类号 A61K
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