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公开(公告)号:EP0432527B1
公开(公告)日:1997-02-05
申请号:EP90122217.4
申请日:1990-11-20
发明人: Aburaki, Shimpei , Yamasaki, Tetsuro , Oki, Toshikazu , Iimura, Seiji , Kamachi, Hajime , Kamei, Hideo , Naito, Takayuki
IPC分类号: C07H15/244 , A61K31/71 , C07C235/84
CPC分类号: C07H15/244 , C07C235/84 , C07C2603/90
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公开(公告)号:EP0408336B1
公开(公告)日:1994-09-07
申请号:EP90307579.4
申请日:1990-07-11
发明人: Ohkuma, Hiroaki , Tomita, Koji , Konishi, Masataka , Kamei, Hideo
IPC分类号: C07D309/32 , C12P17/06 , C12N1/20 , A61K31/35
CPC分类号: C07D309/32
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公开(公告)号:EP0408336A2
公开(公告)日:1991-01-16
申请号:EP90307579.4
申请日:1990-07-11
发明人: Ohkuma, Hiroaki , Tomita, Koji , Konishi, Masataka , Kamei, Hideo
IPC分类号: C07D309/32 , C12P17/06 , C12N1/20 , A61K31/35
CPC分类号: C07D309/32
摘要: The present invention relates to the antitumor antibiotic compound BU-3285T and its preparation. The compound is obtained by culturing a new strain of Chainia rosea and demonstrates both antitumor and antifungal activity. It also relates to the desulfated derivative of BU-3285T which is obtained by treatment of BU-3285T with sulfatase enzyme. BU-3285T desulfate possesses antitumor activity.
摘要翻译: 本发明涉及抗肿瘤抗生素化合物BU-3285T及其制备方法。 该化合物通过培养一种新的连翘蔷薇菌株获得,并表现出抗肿瘤和抗真菌活性。 它还涉及通过用硫酸酯酶处理BU-3285T获得的BU-3285T的脱硫衍生物。 BU-3285T硫酸盐具有抗肿瘤活性。
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公开(公告)号:EP0367189A2
公开(公告)日:1990-05-09
申请号:EP89120115.4
申请日:1989-10-30
CPC分类号: C07H17/04
摘要: The present invention relates to antitumor 4′-demethylepipodophyllotoxin glucosides having phosphate or sulfonate substituents on the sugar portion of the molecule.
摘要翻译: 本发明涉及在该分子的糖部分上具有磷酸酯或磺酸酯取代基的抗肿瘤剂4分钟 - 甲氧基表鬼臼毒素葡糖苷。
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公开(公告)号:EP0432527A3
公开(公告)日:1991-12-04
申请号:EP90122217.4
申请日:1990-11-20
发明人: Aburaki, Shimpei , Yamasaki, Tetsuro , Oki, Toshikazu , Iimura, Seiji , Kamachi, Hajime , Kamei, Hideo , Naito, Takayuki
IPC分类号: C07H15/244 , A61K31/71 , C07C235/84
CPC分类号: C07H15/244 , C07C235/84 , C07C2603/90
摘要: The present invention concerns neutral sugar derivatives (Formula I) of pradimicins, their use as antifungal agents, methods for their preparation, and intermediates for their synthesis.
wherein R¹ is selected from the group consisting of H, methyl, and hydroxymethyl, and when R¹ is methyl or hydroxymethyl, the resulting amino acid residue has the D -configuration; and R² is H or ß- D -xylosyl with the proviso that, when R¹ is methyl, R² is H; or a pharmaceutically acceptable salt thereof.摘要翻译: 本发明涉及普拉德霉素的中性糖衍生物(式I),它们作为抗真菌剂的用途,其制备方法及其合成中间体。 其中R 1选自H,甲基和羟甲基,当R 1为甲基或羟甲基时,所得氨基酸残基具有D-构型; 且R 2为H或β-D-木糖基,条件是当R 1为甲基时,R 2为H; 或其药学上可接受的盐。
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公开(公告)号:EP0401800A3
公开(公告)日:1991-04-10
申请号:EP90110729.2
申请日:1990-06-06
发明人: Ohnuma, Takeshi , Obata, Rika , Kamei, Hideo , Naito, Takayuki
CPC分类号: C07H17/04
摘要: The epipodophyllotoxin glucosides disclosed are acylated at herein one or both sugar hydroxyl groups. These compounds exhibit significant activity against P388 murine leukemia
wherein R² is H and R¹ is selected from the group consisting of (C₁₋₁₀)alkyl, (C₂₋₁₀)alkenyl, (C₅₋₆)cycloalkyl, 2-furyl, 2-thienyl, (C₆₋₁₀)aryl, and (C₇₋₁₄)aralkyl; or R¹ and R² are each (C₁₋₁₀)alkyl; or R¹, R² and the carbon to which they are attached together represent (C₅₋₆)cycloalkyl; one of R³ and R⁴ is H and the other is selected from the group consisting of (C₁₋₅)alkanoyl and benzoyl; or R³ and R⁴ are the same or different and are selected from the group consisting of (C₁₋₅)alkanoyl and benzoyl; R⁵ is H or a phosphate group.-
公开(公告)号:EP0367189A3
公开(公告)日:1991-04-10
申请号:EP89120115.4
申请日:1989-10-30
CPC分类号: C07H17/04
摘要: The present invention relates to antitumor 4′-demethylepipodophyllotoxin glucosides having phosphate or sulfonate substituents on the sugar portion of the molecule.
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公开(公告)号:EP0358197A2
公开(公告)日:1990-03-14
申请号:EP89116448.5
申请日:1989-09-06
摘要: The present invention provides antitumor fluoro-substituted 4'-demethylepipodophyllotoxin glucosides.
摘要翻译: 本发明提供抗肿瘤氟取代的4'-去甲表鬼臼毒素葡糖苷(I)。
其中R 2是H,R 1选自(C 1-10)烷基; (C 2-10)链烯基; (C 5-6)环烷基; 2-呋喃基; 2-噻吩基; (C 6-10)芳基; (C7-14)芳烷基; 和(C 8-14)芳烯基,其中每个芳环可以是未取代的或被一个或多个选自卤素,(C 1-8)烷基,(C 1-8)烷氧基,羟基,硝基和氨基的基团取代; 或R 1和R 2各自为(C 1-8)烷基; 或R 1和R 2和它们所连接的碳连接形成(C5-6)环烷基; R 3或R 4之一是OH,另一个是F; R 5为H或苯酚保护基; 而“IMAGE”代表α-或β-糖苷键。 -
公开(公告)号:EP0332080B1
公开(公告)日:1992-05-20
申请号:EP89103764.0
申请日:1989-03-03
发明人: Sugawara, Koko , Hatori, Masami , Kamei, Hideo , Konishi, Masataka , Oki, Toshikazu , Tomita, Koji
IPC分类号: C07D303/36 , C12P17/02 , C12N1/20 , A61K31/335
CPC分类号: C12R1/55 , C07D303/36 , C12P17/02
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公开(公告)号:EP0432527A2
公开(公告)日:1991-06-19
申请号:EP90122217.4
申请日:1990-11-20
发明人: Aburaki, Shimpei , Yamasaki, Tetsuro , Oki, Toshikazu , Iimura, Seiji , Kamachi, Hajime , Kamei, Hideo , Naito, Takayuki
IPC分类号: C07H15/244 , A61K31/71 , C07C235/84
CPC分类号: C07H15/244 , C07C235/84 , C07C2603/90
摘要: The present invention concerns neutral sugar derivatives (Formula I) of pradimicins, their use as antifungal agents, methods for their preparation, and intermediates for their synthesis.
wherein R¹ is selected from the group consisting of H, methyl, and hydroxymethyl, and when R¹ is methyl or hydroxymethyl, the resulting amino acid residue has the D -configuration; and R² is H or ß- D -xylosyl with the proviso that, when R¹ is methyl, R² is H; or a pharmaceutically acceptable salt thereof.摘要翻译: 本发明涉及普拉德霉素的中性糖衍生物(式I),它们作为抗真菌剂的用途,其制备方法及其合成中间体。 其中R 1选自H,甲基和羟甲基,当R 1为甲基或羟甲基时,所得氨基酸残基具有D-构型; 且R 2为H或β-D-木糖基,条件是当R 1为甲基时,R 2为H; 或其药学上可接受的盐。
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