发明名称 NASAL AGENT
摘要 PROBLEM TO BE SOLVED: To obtain a nasal agent having excellent Na-H exchange-inhibiting activities, absorbability in vivo from the nasal mucous membrane, and properties of transmigration to the heart, and useful for therapy of cardiac infarction, arrhythmia or the like by including an aminoguanidine hydrazone having an aromatic heterocycle. SOLUTION: This nasal agent contains a compound of formula I [A-ring is a 5-or 6-membered (substituted) aromatic heterocycle; ring-B is a 5-or 6-membered (substituted) aromatic family or heterocycle; R1 is H, OH or a lower alkyl; and (n) is 0 or 1], e.g. (±)-7-(2-chlorophenyl)-5-guanidinoimino-4- methyl-5,6,7,8-tetrahydroquinoline, its prodrug or its salt. The compound of formula I is preferably obtained by condensing 1 mol compound of formula II with 1-2 mol compound of the formula H2N-N=C(NH2)(NHR1) in the presence of (1/10)-10 molar times of a catalyst (e.g. triethylamine) in a solvent (e.g. methanol) at 0-180 deg.C.
申请公布号 JP2001048865(A) 申请公布日期 2001.02.20
申请号 JP20000170437 申请日期 2000.06.02
申请人 TAKEDA CHEM IND LTD 发明人 OMAE MASAFUMI;TAKADA SHIGEYUKI;SHIRAISHI MITSURU;FUKUMOTO MASAJI
分类号 C07D215/38;A61K9/72;A61K31/47;A61P9/04;A61P9/06;A61P9/10;A61P9/12;(IPC1-7):C07D215/38 主分类号 C07D215/38
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