发明名称 NITROGEN-CONTAINING HETEROCYCLIC COMPOUND
摘要 PROBLEM TO BE SOLVED: To obtain a new compound comprising a specific nitrogen-containing heterocyclic compound, having an inhibiting action against cGMP phosphodiesterase and helpful for the prevention and treatment of ishemic heart disease, angina pectoris, high blood pressure, heart failure, asthma or the like. SOLUTION: This new compound is expressed by formula I (wherein, R1-R4 are each H, a halogen, a lower alkyl or the like; R5 is H, OH, hydrazino or the like; R6 is H, amino, a lower alkyl or the like), and is e.g. a 2,6- dichloro-4-(3,4-methylenedioxybenzyl)aminoquinoline of formula II. The compound of formula I is obtained by making a quinoline derivative of formula III (wherein, R5a is H, a halogen or a group directly combining with a quinoline skeleton through a carbon atom) act on phosphorus oxychloride, if needed, in the presence of phosphorus pentoxide, followed by heatup. When orally administering the compound of formula I as a medicament, one to three doses containing the compound of formula I of 10-100 mg/day/adult is/are taken a day. In the case of injection, 3-1,000μg/(kg body weight) of the compound of formula I is preferably administered.
申请公布号 JP2000264877(A) 申请公布日期 2000.09.26
申请号 JP20000070130 申请日期 2000.03.14
申请人 EISAI CO LTD 发明人 TAKASE YASUTAKA;WATANABE NOBUHISA;MATSUI MAKOTO;IKUTA HIRONORI;KIMURA TEIJI;SAEKI TAKAO;ADACHI HIDEYUKI;TOKUMURA CHUICHI;MOCHIDA HISATOSHI;AKITA YASUNORI;SODA SHIGERU
分类号 C07D215/42;A61K31/415;A61K31/4184;A61K31/4427;A61K31/443;A61K31/445;A61K31/454;A61K31/4706;A61K31/4709;A61K31/496;A61K31/505;A61K31/517;A61K31/519;A61P9/00;A61P9/04;A61P9/10;A61P9/12;A61P11/06;A61P37/00;A61P43/00;C07D215/48;C07D235/06;C07D235/08;C07D239/78;C07D239/84;C07D239/86;C07D239/88;C07D239/90;C07D239/94;C07D239/95;C07D239/96;C07D401/04;C07D401/12;C07D401/14;C07D403/12;C07D405/06;C07D405/12;C07D405/14;C07D413/12;C07D471/04;C07D491/04;C07D491/056;C07D521/00;(IPC1-7):C07D215/42;A61K31/470 主分类号 C07D215/42
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