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1. 发明授权

US06358957B1 Phenylahistin and the phenylahistin analogs, a new class of anti-tumor compounds 有权
标题翻译：苯基黑曲霉素和亚硫酸钠类似物，一类新的抗肿瘤化合物
公开(公告)号：US06358957B1
公开(公告)日：2002-03-19
申请号：US09440316
申请日：1999-11-12
申请人： Kenji Fukumoto , Shinkichi Kohno , Kaneo Kanoh , Tohru Asari , Hiroshi Kawashima , Hirokatsu Sekiya , Kazunori Ohmizo , Takeo Harada
发明人： Kenji Fukumoto , Shinkichi Kohno , Kaneo Kanoh , Tohru Asari , Hiroshi Kawashima , Hirokatsu Sekiya , Kazunori Ohmizo , Takeo Harada
IPC分类号： C07D24106
CPC分类号： C07D403/06 , A61K31/496
摘要： A compound, its pharmaceutically acceptable salts, and/or its pro-drug esters, in isolated form, and methods for isolating, for formulating, and for administering the compound, salt, and/or pro-drug ester as an antitumor agent, wherein the compound, salt, or pro-drug ester has the following structure: wherein: R1, R2, R5, R7,and R8 are each separately selected from the group consisting of a hydrogen atom, a halogen atom, and saturated C1-C24 alkyl, unsaturated C1-C24 alkenyl, cycloalkyl, cycloalkenyl, alkoxy, cycloalkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, amino, substituted amino, nitro, substituted nitro, phenyl, and substituted phenyl groups, R3, R4, and R6 are each separately selected from the group consisting of a hydrogen atom, a halogen atom, and saturated C1-C12 alkyl, unsaturated C1-C12 alkenyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, amino, substituted amino, nitro, and substituted nitro groups, X1 and X2 are separately selected from the group consisting of an oxygen atom, and a sulfur atom, and the dashed bond represents a bond selected from the group consisting of a carbon-carbon single bond and a carbon-carbon double bond. Most preferably, R3 and R4 are hydrogen, and each are involved in hydrogen bonds, and/or the dashed bond is a double bond, such that the chemical backbone of the compound substantially retains a substantially planar conformation.
摘要翻译：分离形式的化合物，其药学上可接受的盐和/或其前药酯，以及用于分配，配制和施用作为抗肿瘤剂的化合物，盐和/或前药酯的方法，其中化合物，盐或前药酯具有以下结构：其中：R 1，R 2，R 5，R 7和R 8各自独立地选自氢原子，卤素原子和饱和C 1 -C 24烷基，不饱和C 1 -C 24烯基，环烷基，环烯基，烷氧基，环烷氧基，芳基，取代的芳基，杂芳基，取代的杂芳基，氨基，取代的氨基，硝基，取代的硝基，苯基和取代的苯基，R 3，R 4和R 6 分别选自氢原子，卤素原子和饱和C 1 -C 12烷基，不饱和C 1 -C 12烯基，环烷基，烷氧基，环烷氧基，芳基，取代的芳基，杂芳基，取代的杂芳基，氨基，取代的氨基，硝基和取代的硝基，X1和 X2分别选自氧原子和硫原子，虚键表示选自碳 - 碳单键和碳 - 碳双键的键。最优选地，R 3和R 4是氢，并且各自参与氢键，和/或虚线键是双键，使得化合物的化学主链基本上保持基本上平面的构象。

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