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1. 发明授权

EP0230322B1 2,6-Dideoxy-2-fluoro-L-talopyranose and derivates thereof and the production of these compounds 失效
标题翻译： 2,6-二去氧-2-氟-L-三氟乙醇及其衍生物和这些化合物的生产
公开(公告)号：EP0230322B1
公开(公告)日：1993-07-21
申请号：EP87100856.1
申请日：1987-01-22
申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
发明人： Umezawa, Hamao , Umezawa, Sumio , Tsuchiya, Tsutomu , Takeuchi, Tomio , Takagi, Yasushi
IPC分类号： C07H5/02 , C07H15/04 , C07H13/04 , C07H15/252
CPC分类号： C07H5/02 , C07H13/04 , C07H15/04 , Y02P20/55

2. 发明授权

EP0761678B1 Fluorine-containing anthracycline derivatives having hydroxyl group(s) mono- or di-o-aminoalkanoylated in the sugar moiety thereof 失效
标题翻译：在糖残基单 - 或二 - 0 - aminoalkanoylaten羟基含氟蒽环类衍生物
公开(公告)号：EP0761678B1
公开(公告)日：1999-03-31
申请号：EP96420288.1
申请日：1996-09-06
申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
发明人： Takeuchi, Tomio, New Fuji Mansion 701, 1-11 , Umezawa, Sumio , Tsuchiya, Tsutomu , Takagi, Yasushi , Sohtome, Hiromi
IPC分类号： C07H15/252 , A61K31/70
CPC分类号： C07H15/252

3. 发明授权

EP0230013B1 New anthracycline derivatives, uses thereof as antitumor agent and production thereof 失效
标题翻译：新的蒽环衍生物，其作为抗菌剂及其生产的用途
公开(公告)号：EP0230013B1
公开(公告)日：1992-06-17
申请号：EP86117662.6
申请日：1986-12-18
申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
发明人： Umezawa, Hamao , Umezawa, Sumio , Tsuchiya, Tsutomu , Takeuchi, Tomio , Takagi, Yasushi
IPC分类号： C07H15/252 , A61K31/70
CPC分类号： C07H15/252 , Y02P20/55

4. 发明公开

EP0285526A2 1-N-(4-Amino-3-fluoro-2-hydroxybutyryl)-kanamycins 失效
标题翻译： 1-N-（4-氨基-3-氟-2-羟基丁基）卡那霉素。
公开(公告)号：EP0285526A2
公开(公告)日：1988-10-05
申请号：EP88420066.8
申请日：1988-02-24
申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
发明人： Umezawa, Sumio , Tsuchiya, Tsutomu , Takeuchi, Tomio , Umezawa, Kazuo , Takahashi, Yoshiaki , Shitara, Tetsuo , Kobayashi, Yoshihiko , Takagi, Yasushi
IPC分类号： C07H15/234 , A61K31/70
CPC分类号： C07H15/234
摘要： As new compound are now provided ten compounds, namely 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-kanamycin A; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybuty- ryl}-2',3'-dideoxykanamycin A; 1-N-{(2R,3R)-4-amino-fluoro-2-hydorxybutyryl}-2',3'-dideoxy-2'-fluorokanamycin A; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-5-deoxy-5-fluorokanamycin A; 1-N-((2R,3R)-4-amino-fluoro-2-hydrox- ybutyryl}-kanamycin B; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hy- droxybutyryl}-3'-deoxykanamycin B; 1-N-((2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-3',4'-dideoxykanamycin B; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-5-deoxy-5-fluorokanamycin B; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydrox- ybutyryl}-5,3'-dideoxy-5-fluorokanamycin B; and 1-N{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-5,3',4'-tride- oxy-5-fluorokanamycin B, which are all useful as antibacterial agent in the therapeutic treatment of bacterial infections.
摘要翻译：现在提供了新的化合物十个化合物，即1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} - 卡那霉素A; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -2'，3'-二脱氧卡那霉素A; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -2'，3'-二脱氧-2'-感染甲卡霉素A; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -5-脱氧-5-氟霉素A; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} - 卡那霉素B; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -3'-脱氧卡那霉素B; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -3'，4'-二脱氧卡那霉素B; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -5-脱氧-5-氟霉素B; 在B中的1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -5,3'-二脱氧-5-氟代烟酰胺; 和1-N（（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -5,3'，4'-三脱氧-5-氟卡那霉素B，它们都可用作治疗剂中的抗菌剂治疗细菌感染。

5. 发明公开

EP0761678A1 Fluorine-containing anthracycline derivatives having hydroxyl group(s) mono- or di-o-aminoalkanoylated in the sugar moiety thereof 失效
标题翻译：荧光e e mit rest mit mit mit rest rest rest rest rest rest rest rest rest rest rest rest rest rest rest rest rest rest rest rest rest
公开(公告)号：EP0761678A1
公开(公告)日：1997-03-12
申请号：EP96420288.1
申请日：1996-09-06
申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
发明人： Takeuchi, Tomio, New Fuji Mansion 701, 1-11 , Umezawa, Sumio , Tsuchiya, Tsutomu , Takagi, Yasushi , Sohtome, Hiromi
IPC分类号： C07H15/252 , A61K31/70
CPC分类号： C07H15/252
摘要： To provide novel fluorine-containing anthracycline derivatives having high antitumor activities and a solubility in water, there have now been synthesized a 7-O-(2,6-dideoxy-2-fluoro-3-O- or -4-O- or -3,4-di-O-aminoalkanoyl-α-L-talopyranosyl)daunomycinone or -adriamycinone of general formula (I) shown below, as well as a 7-O-(3-O- or -4-O-or -3,4-di-O-aminoalkanoyl-2,6-dideoxy-2,6,6,6-tetrafluoro-α-L-talopyranosyl- or -2,6-dideoxy-6,6,6-trifluoro-α-L-lyxo-hexopyranosyl)adriamycinone of general formula (II) shown below:-

wherein either one or both of A 1 and A 2 is or are an α-amino acid residue or an ω-amino acid residue and T denotes a fluorine or hydrogen atom. The novel fluorine-containing anthracycline derivatives of general formulae (I) and (II) are highly active against tumors and soluble in water, and they are useful as antitumor agents administrable in the form of injectable solution.
摘要翻译：为了提供具有高抗肿瘤活性和在水中的溶解性的新型含氟蒽环类衍生物，现在已经合成了7-O-（2,6-二脱氧-2-氟-3-O-或-4-O-或 -3,4-二-O-氨基链烷酰-α-L-吡喃葡萄糖基）道诺霉素酮或下列通式（I）的阿霉素酮，以及7-O-（3-O-或-4-O- -3,4-二-O-氨基烷酰基-2,6-二脱氧-2,6,6,6-四氟-α-L-吡喃木糖基或-2,6-二脱氧-6,6,6-三氟-α -L-赖肟基 - 六吡喃糖基）阿霉素酮，其如下所示： - CHEM>其中A 1和A 2中的任一个或两者是或是α-氨基酸残基或 ω-氨基酸残基，T表示氟或氢原子。通式（I）和（II）的新型含氟蒽环类衍生物对肿瘤和水溶性高度有活性，可用作以可注射溶液形式给药的抗肿瘤剂。

6. 发明公开

EP0285526A3 1-N-(4-Amino-3-fluoro-2-hydroxybutyryl)-kanamycins 失效
标题翻译： 1-N-（4-氨基-3-氟-2-羟）-kanamycins
公开(公告)号：EP0285526A3
公开(公告)日：1991-04-10
申请号：EP88420066.8
申请日：1988-02-24
申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
发明人： Umezawa, Sumio , Tsuchiya, Tsutomu , Takeuchi, Tomio , Umezawa, Kazuo , Takahashi, Yoshiaki , Shitara, Tetsuo , Kobayashi, Yoshihiko , Takagi, Yasushi
IPC分类号： C07H15/234 , A61K31/70
CPC分类号： C07H15/234
摘要： As new compound are now provided ten compounds, namely 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-kanamycin A; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybuty- ryl}-2',3'-dideoxykanamycin A; 1-N-{(2R,3R)-4-amino-fluoro-2-hydorxybutyryl}-2',3'-dideoxy-2'-fluorokanamycin A; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-5-deoxy-5-fluorokanamycin A; 1-N-((2R,3R)-4-amino-fluoro-2-hydrox- ybutyryl}-kanamycin B; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hy- droxybutyryl}-3'-deoxykanamycin B; 1-N-((2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-3',4'-dideoxykanamycin B; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-5-deoxy-5-fluorokanamycin B; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydrox- ybutyryl}-5,3'-dideoxy-5-fluorokanamycin B; and 1-N{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-5,3',4'-tride- oxy-5-fluorokanamycin B, which are all useful as antibacterial agent in the therapeutic treatment of bacterial infections.
摘要翻译：现在提供10种化合物，即1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} - 卡那霉素A; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁基} -2'，3'-双脱氧卡那霉素A; 1-N - {（2R，3R）-4-氨基 - 氟-2-羟基丁酰基} -2'，3'-二脱氧-2'-氟尿嘧啶A; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -5-脱氧-5-氟沙霉素A; 1 -N - （（2R，3R）-4-氨基 - 氟-2-羟基丁酰基} - 卡那霉素B; 1-N - {（2R，3R）-4-氨基-3-氟-2- （2R，3R）-4-氨基-3-氟-2-羟丁酰基} -3'，4'-双脱氧卡那霉素B; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟丁酰基} 3R）-4-氨基-3-氟-2-羟基丁酰基} -5-脱氧-5-氟沙霉素B; 1-N - {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -5,3'-二脱氧-5-氟沙霉素B;和1-N {（2R，3R）-4-氨基-3-氟-2-羟基丁酰基} -5,3'，4'-三氧代-5 氟隆霉素B，它们都可用作细菌感染治疗的抗菌剂。

7. 发明公开

EP0230322A2 2,6-Dideoxy-2-fluoro-L-talopyranose and derivates thereof and the production of these compounds 失效
标题翻译： 2,6-二脱氧-2-氟-L- talopyranose，它们的衍生物以及这些化合物的制备。
公开(公告)号：EP0230322A2
公开(公告)日：1987-07-29
申请号：EP87100856.1
申请日：1987-01-22
申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
发明人： Umezawa, Hamao , Umezawa, Sumio , Tsuchiya, Tsutomu , Takeuchi, Tomio , Takagi, Yasushi
IPC分类号： C07H5/02 , C07H15/04 , C07H13/04 , C07H15/252
CPC分类号： C07H5/02 , C07H13/04 , C07H15/04 , Y02P20/55
摘要： 2.6-Dideoxy-2-fluoro-L-talopyranose and I-substituted denvatives thereof. including methyl 2.6-dideoxy-2-fluoro-L-talopyranoside and 3.4-di-O-protected-2,6-dfdeoxy-2-fluoro-L-ta- lopyranosyl halides. are now provided and these new compounds are useful as intermediates for use in the synthesis of new compounds having antitumor activity. especially 7-O-(2.6-dideoxy-2-fluoro-α-L-talopyranosyl)daunomycinone or -adriamycinone. 2.6-Dideoxy-2-fluoro-L-talopyranose shows antibacterial activity. 2.6-Dideoxy-2-fluoro-L-talopyranose and the I-substituted derivatives thereof may be produced by a multi-stage process starting from L-fucose.

8. 发明公开

EP0230013A1 New anthracycline derivatives, uses thereof as antitumor agent and production thereof 失效
标题翻译： Anthracyclinderivate，ihre Verwendung als Antitumorsubstanzen und ihre Herstellung。
公开(公告)号：EP0230013A1
公开(公告)日：1987-07-29
申请号：EP86117662.6
申请日：1986-12-18
申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
发明人： Umezawa, Hamao , Umezawa, Sumio , Tsuchiya, Tsutomu , Takeuchi, Tomio , Takagi, Yasushi
IPC分类号： C07H15/252 , A61K31/70
CPC分类号： C07H15/252 , Y02P20/55
摘要： As new anthracycline derivatives are now provided 7-0-(2,6-dideoxy-2-fluoro-a-L-talopyranosyl)-daunomycinone and 7-0-(2,6-dideoxy-2-fluoro-a-L-talopyranosyl)adriamycinone which are useful as antitumor agent and also as antibacterial agent. Briefly, these new compounds may be produced by condensing a 2,6- dideoxy-2-fluoro-a-L-talopyranosyl halide with the 7-hydroxyl group of daunomycinone or adriamycinone.
摘要翻译：现在提供新的蒽环类衍生物7-O-（2,6-二脱氧-2-氟-α-L-吡喃葡萄糖基）道诺霉素酮和7-O-（2,6-二脱氧-2-氟-α-L-吡喃葡萄糖基）阿霉素，其可用作抗肿瘤剂，也可用作抗菌剂。简言之，这些新化合物可以通过将2,6-二脱氧-2-氟-α-L-吡喃葡萄糖基卤化物与道诺霉素酮或阿霉素酮的7-羟基缩合来制备。

9. 发明公开

EP0848010A1 Novel anthracycline derivatives having 4-amino-2,4,6-trideoxy-2-fluoro-alpha-L-talopyranosyl group 失效
标题翻译：蒽环类衍生物4-氨基-2,4,6-三脱氧-2-氟-α-L-塔吡喃糖基-Grope
公开(公告)号：EP0848010A1
公开(公告)日：1998-06-17
申请号：EP97403059.5
申请日：1997-12-16
申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
发明人： Takeuchi, Tomio , Umezawa, Sumio , Tsuchiya, Tsutomu , Takagi, Yasushi
IPC分类号： C07H15/252 , A61K31/70 , C07H15/12
CPC分类号： C07H15/12 , C07H15/252 , Y02P20/55
摘要： 7-O-(4-Amino-2,4,6-trideoxy-2-fluoro-α-L-talopyranosyl)-daunomycinone or -adriamycinone is now synthesized as a novel daunomycinone or adriamycinone derivative having the general formula
wherein R is a hydrogen atom or hydroxyl group. These novel compounds according to this invention exhibit excellent antitumor activities and have a high solubility in water, and hence they are useful as an antitumor agent.
摘要翻译： 7-O-（4-氨基-2,4,6-三脱氧-2-氟-α-L-吡喃葡萄糖基） - 日光霉素酮或阿德米霉素现在被合成为具有通式的新的道诺霉素酮或阿霉素酮衍生物，其中 R是氢原子或羟基。根据本发明的这些新化合物表现出优异的抗肿瘤活性并且在水中的溶解度高，因此它们可用作抗肿瘤剂。

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