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公开(公告)号：EP2527352B1
公开(公告)日：2015-10-28
申请号：EP12180101.3
申请日：2004-01-30
IPC分类号： C07H19/06 , A61K31/7072 , A61P31/04 , A61P31/06 , C07D405/14 , C07D403/08 , C07D403/14
CPC分类号： C07H19/067 , A61K31/7072 , C07D403/08 , C07D403/14 , C07D405/14 , C07H15/26 , C07H19/06 , Y02P20/55
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2.发明公开
公开(公告)号：EP2902403A1
公开(公告)日：2015-08-05
申请号：EP14197812.2
申请日：2004-01-30
IPC分类号： C07H19/06 , A61K31/7072 , A61P31/04 , A61P31/06 , C07D405/14 , C07D403/08 , C07D403/14 , C07H15/26 , C07H19/067
CPC分类号： C07H19/067 , A61K31/7072 , C07D403/08 , C07D403/14 , C07D405/14 , C07H15/26 , C07H19/06 , Y02P20/55
摘要： Caprazene-1"'-ester derivatives of the formula (III)
wherein Me is methyl group, R 2 is a straight chain or a substantially straight chain alkyl group of 5-21 carbon atoms or a straight chain or a substantially straight chain alkenyl group of 5-21 carbon atoms or an alkynyl group of 5-21 carbon atoms and A is hydrogen atom or an amino-protecting group which is an alkoxycarbonyl group or an aralkyloxycarbonyl group, or a pharmaceutically acceptable acid addition salt thereof.
The novel caprazene derivatives exhibit excellent antibacterial activities against a variety of bacteria including acid-fast bacteria.摘要翻译： 其中Me为甲基的式（III）的吡啶-1“ - 酯衍生物，R 2为5-21个碳原子的直链或基本上直链的烷基，或直链或基本上直链的烯基 5-21个碳原子的炔基或5-21个碳原子的炔基，A是氢原子或作为烷氧基羰基或芳烷氧基羰基的氨基保护基，或其药学上可接受的酸加成盐，新的癸酰衍生物 对各种细菌（包括耐酸菌）表现出优异的抗菌活性。
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3.发明授权CONAGENIN FOR THE TREATMENT OF ULCEROUS COLITIS AND/OR CROHN'S DISEASE 失效Conagenin用于治疗溃疡性结肠炎和/或节段性回肠炎
公开(公告)号：EP0987022B1
公开(公告)日：2006-01-25
申请号：EP98912719.6
申请日：1998-04-08
发明人： ISHIZUKA, Masaaki , MAEDA, Kenji , TAKEUCHI, Tomio , SHIRAISHI, Tadayoshi , FUKUSHIMA, Masakazu
IPC分类号： A61K31/198 , A61P1/04
CPC分类号： A61K31/198 , Y10S514/885 , Y10S514/925 , Y10S514/926
摘要： Preventives and remedies for ulcerous colitis and/or Crohn's disease containing as the active ingredient conagenin or a pharmaceutically acceptable salt thereof and having prominent therapeutic effects and a high safety.
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公开(公告)号：EP1211259B1
公开(公告)日：2003-11-19
申请号：EP00951962.0
申请日：2000-08-11
IPC分类号： C07H19/067 , C12P17/16 , C12N1/20 , A61K31/7072 , A61P31/04
CPC分类号： C07H19/06 , C12P17/16 , Y10S435/886
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公开(公告)号：EP0930310B1
公开(公告)日：2003-03-26
申请号：EP96917702.1
申请日：1996-06-17
发明人： HIRANO, Shin-ichi , MASE, Toshiyuki , AGATA, Naoki , IGUCHI, Hiroshi , MATSUMOTO, Naoki , YOSHIOKA, Takeo , TONE, Hiroshi , KUMAGAI, Hiroyuki , ISHIZUKA, Masaaki , TAKEUCHI, Tomio
IPC分类号： C07D311/76 , A61K31/35
CPC分类号： C07D311/76
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6.发明授权A process for the preparation of 2'-deoxy-2'-halocoformycins or stereoisomers thereof 失效一种用于2'-脱氧-2'- halocoformycin或其立体异构体的制备方法
公开(公告)号：EP0794194B1
公开(公告)日：2001-12-12
申请号：EP97400511.8
申请日：1997-03-06
IPC分类号： C07H19/23 , C07H19/052
CPC分类号： C07H19/052 , C07H19/23
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7.发明授权Fluorine-containing anthracycline derivatives having hydroxyl group(s) mono- or di-o-aminoalkanoylated in the sugar moiety thereof 失效在糖残基单 - 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
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
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公开(公告)号：EP0653207B1
公开(公告)日：1997-09-24
申请号：EP93900436.2
申请日：1992-12-25
发明人： KONDO, Shinichi , IKEDA, Yoko Crescent Ikejiri Ohashi 502, 19 -16 , HAMADA, Masa , TAKEUCHI, Tomio , HOSHINO, Hiroo
IPC分类号： A61K31/16
CPC分类号： A61K31/16
摘要： D-β-Lysylmethanediamine represented by formula (I) or a salt or hydrate thereof has an activity of inhibiting the infection with AIDS virus or HIV, and hence an AIDS virus infection inhibitor containing the same as an active ingredient is prospective as one of the remedies for AIDS which is thought to be difficult to cure.
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9.发明公开Threo-3-amino-2-hydroxypentanoic acid and threo (2R,3S), (2S,3R)-3-(p-methoxy-benzyloxycarbonyl) amino-2-hydroxy-pentanoic acid 失效（2R，3S），（2S，3R）-3-（对 - 甲氧基 - 苄氧基羰基）氨基-2-羟基 - 戊酸的3-烯丙基-3-氨基-2-羟基戊酸和苏氨酸。
公开(公告)号：EP0672648A1
公开(公告)日：1995-09-20
申请号：EP95106762.8
申请日：1990-04-13
发明人： Takeuchi, Tomio , Aoyagi, Takaaki , Hamada, Masa , Naganawa, Hiroshi , Muraoka, Yasuhiko , Ogawa, Keiji , Nagai, Machiko , Tsuda, Makoto
IPC分类号： C07C229/22 , C07C271/22 , C07K5/08
CPC分类号： C07C229/22 , A61K38/00 , C07C271/22 , C07K5/0202 , C07K7/02
摘要： Threo-3-amino-2-hydoxypentanoic acid and threo (2R,3S), (2S,3R)-3-(p-methoxy-benzyloxycarbonyl) amino-2-hydoxy-pentanoic acid.
摘要翻译： （2R，3S），（2S，3R）-3-（对甲氧基 - 苄氧基羰基）氨基-2-羟基 - 戊酸的苏氨基-3-氨基-2-羟基戊酸和苏氨酸。
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10.发明公开2'-DEOXY-2'-FLUOROCOFORMYCIN AND STEREOISOMERS THEREOF 失效2-DEOXY-2-FLUORCOFORMYCIN UND STEREOISOMERE DAVON。
公开(公告)号：EP0643069A1
公开(公告)日：1995-03-15
申请号：EP92923538.0
申请日：1992-11-13
发明人： TAKEUCHI, Tomio No. 701 New Fuji Mansion , UMEZAWA, Sumio 1-1-709, Shinjuku 5-chome , TSUCHIYA, Tsutomu 1-17-201, Eda Higashi 3-chome , TAKAHASHI, Yoshiaki 201 Yaguchi Heim
IPC分类号： C07H19/23 , C07H19/052 , C07H5/02 , C07H5/04
摘要： 2'-Deoxy-2'-fluorocoformycin and 2'-deoxy-8-epi-2'-fluorocoformycin have now been synthesized by a multistage reaction via 3,5-di-O-benzoyl-2-deoxy-2-fluoro-α- and -β-D-ribofuranosyl bromide. Also 2'-deoxy-2'-epi-2'-fluorocoformycin and 2'-deoxy-8,2'-diepi-2'-fluorocoformycin have been synthesized from 3,5-di-O-benzoyl-2-deoxy-2-fluoro-α-D-arabinofuranosyl bromide by a multistage reaction. These four 2'-fluorocoformycin derivatives are novel compounds and have a potent enzyme inhibiting activity against adenosine deaminase. In particular, they are useful for treating acute lymphocytic leukemia in virtue of the above activity. Other novel compounds also obtained include various intermediates useful for the synthesis of the above derivatives.
摘要翻译： 2'-脱氧-2'-氟霉素和2'-脱氧-8-表-2-fluorocoformycin已经通过多步反应通过3,5-二-O-苯甲酰基-2-脱氧-2-氟 - α和β-D-呋喃核糖基溴。 还从3,5-二-O-苯甲酰基-2-脱氧-α-脱氧-2'-氟代霉素和2'-脱氧-8,2'-二哌啶-2'-氟霉素合成了2'-脱氧-2'-外 - 2-氟-α-D-阿拉伯呋喃糖基溴通过多级反应。 这四种2'-氟霉素衍生物是新型化合物，对腺苷脱氨酶具有强效的酶抑制活性。 特别地，由于上述活性，它们可用于治疗急性淋巴细胞性白血病。 还得到的其它新化合物包括可用于合成上述衍生物的各种中间体。
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