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1. 发明授权

US07250389B1 Antifungal compound and process for producing the same 失效
标题翻译：抗真菌化合物及其制备方法
公开(公告)号：US07250389B1
公开(公告)日：2007-07-31
申请号：US09601655
申请日：1999-02-08
申请人： Osamu Sakanaka , Koichi Mitomo , Takayoshi Tamura , Yasushi Murai , Katsuharu Iinuma , Takeshi Teraoka , Kikuko Kuzuhara , Haruki Mikoshiba , Makoto Taniguchi
发明人： Osamu Sakanaka , Koichi Mitomo , Takayoshi Tamura , Yasushi Murai , Katsuharu Iinuma , Takeshi Teraoka , Kikuko Kuzuhara , Haruki Mikoshiba , Makoto Taniguchi
IPC分类号： A01N504/14 , C07D405/00
CPC分类号： C07D405/12 , A01N43/24 , A01N43/40 , A01N43/54 , C07D321/00 , Y02P20/55
摘要： Disclosed are novel compounds useful for prevention or control of diseases derived from fungi, a process for producing the same, and novel antifungal agents using the novel compounds. The compounds useful for prevention and treatment of diseases derived from fungi according to the present invention include novel compounds represented by formula (I). The compounds represented by formula (I) have potent antifungal activity against diseases derived from fungi, and do not have phytotoxicity to mammals and agricultural and garden plants, from which diseases should be eliminated, and, even when applied to agricultural and garden plants, have high photostability. wherein R1 represents isobutyryl, tigloyl, isovaleryl, or 2-methylbutanoyl; R2 represents a hydrogen atom, an aromatic carboxylic acid residue, or a protective group of amino; and R3 represents a hydrogen atom, nitro, amino, acylamino, or N,N-dialkylamino, excluding the case where, when R1 represents isobutyryl, tigloyl, isovaleryl, or 2-methylbutanoyl with R3 representing a hydrogen atom, R2 represents a 3-hydroxypicolinic acid residue, 3-hydroxy-4-methoxypicolinic acid residue, or a 3,4-dimethoxypicolinic acid residue.
摘要翻译：公开了可用于预防或控制来自真菌的疾病的新化合物，其制备方法和使用该新化合物的新型抗真菌剂。用于预防和治疗根据本发明的真菌的疾病的化合物包括由式（I）表示的新化合物。由式（I）表示的化合物对从真菌衍生的疾病具有有效的抗真菌活性，并且对哺乳动物和农业和园艺植物没有植物毒性，应从其中消除疾病，甚至在应用于农业和花园植物时也具有高光稳定性其中R 1表示异丁酰基，二酰基，异戊酰基或2-甲基丁酰基; R 2表示氢原子，芳族羧酸残基或氨基的保护基; 并且R 3表示氢原子，硝基，氨基，酰氨基或N，N-二烷基氨基，不同之处在于当R 1表示异丁酰基时，二酰基，异戊酰基，或代表氢原子的R 3的2-甲基丁酰基，R 2表示3-羟基吡啶甲酸残基，3-羟基-4-甲氧基吡啶甲酸残基，或3- 4-二甲氧基吡啶甲酸残余物。

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