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发明授权
US6008356A Pharmaceutically available protoberberine salts derivatives, and protoberberine salts derivatives, and protoberberine derivatives and salts thereof 失效
药学上可用的青蒿素盐衍生物和原香草精盐衍生物，以及原丁腈衍生物及其盐

Pharmaceutically available protoberberine salts derivatives, and protoberberine salts derivatives, and protoberberine derivatives and salts thereof
摘要：
The novel compounds of the following chemical formulae (I) and (II) exhibit in vitro antifungal activity against fungi including cutaneous filamentous fungus, such as Epidermophyton, Microsporum, Trichophyton, Sporothrix schenckii, Aspergillus or Candida. The compounds of the present invention exhibit in vitro antifungal activity at the concentration of 1-100 .mu.g/ml. ##STR1## wherein R.sup.1, R.sup.2, and R.sup.4 may be the same or different, and represent C.sub.1 -C.sub.5 alkoxy, R.sup.3 represents hydrogen or C.sub.1 -C.sub.10 alkyl, A.sup.- represents inorganic acid ion, organic acid ion or halide, R.sup.5 represents hydrogen, pyridylmethyl, substituted pyridylmethyl or a group having the following chemical formula(XI) ##STR2## wherein Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4 and Z.sup.5 may be the same or different and represent hydrogen, halogen, C.sub.1 -C.sub.5 alkyl, trifluoromethyl, phenyl, substituted phenyl, nitro, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylamino, acetylamino, C.sub.1 -C.sub.8 trialkyl ammonium, guanidinyl, methylthio, ethylthio, trifluoromethoxy, hydroxy, phenoxy, vinyl, carboxyl and C.sub.1 -C.sub.2 alkoxycarbonyl group.
摘要（中）：

以下化学式（I）和（II）的新化合物表现出对真皮的体外抗真菌活性，包括皮肤丝状真菌，如表皮癣菌，微孢子虫，毛癣菌，阵孢曲霉，曲霉或假丝酵母。 本发明的化合物以1-100μg/ ml的浓度显示体外抗真菌活性。 其中R1，R2和R4可以相同或不同，表示C1-C5烷氧基，R3表示氢或C1-C10烷基，A-表示无机酸离子，有机酸离子或卤化物，R5表示氢，吡啶基甲基，取代 吡啶基甲基或具有以下化学式（XI）的基团，其中Z 1，Z 2，Z 3，Z 4和Z 5可以相同或不同，表示氢，卤素，C 1 -C 5烷基，三氟甲基，苯基，取代的苯基，硝基， C4烷氧基，C1-C4烷基氨基，乙酰氨基，C1-C8三烷基铵，胍基，甲硫基，乙硫基，三氟甲氧基，羟基，苯氧基，乙烯基，羧基和C1-C2烷氧基羰基。

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