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31.发明公开5-Deoxy-5-fluorokanamycin B derivatives and processes for the production thereof 失效5-Deoxy-5-fluorokanamycin-B-Derivate und Verfahren zu ihrer Herstellung。
公开(公告)号：EP0259014A2
公开(公告)日：1988-03-09
申请号：EP87306904.1
申请日：1987-08-04
IPC分类号： C07H15/236 , A61K31/70
CPC分类号： C07H15/234 , Y02P20/55
摘要： As new compounds are now provided 5-deoxy-5-fluorokanamycin B, 5,3'-dideoxy-5-fluorokanamycin B, 5,4'- dideoxy-5-fluorokanamycin B and 5,3',4'-trideoxy-5-fluorokanamycin B as well as 1-N-(3-amino-2-hydrox- ypropionyl)-or 1-N-(4-amino-2-hydroxybutyryl)-derivatives thereof which are all useful as antibacterial agents and exhibit improved antibacterial activities. These new compounds may be produced by synthetic processes starting from an appropriately N,O-protected 5-epi-kanamycin B, 3'-deoxy-5-epi-kanamycin B, 4'-deoxy-5-epi-kanamycin B or 3',4'-dideoxy-5-epi-kanamycin B derivative which is now prepared by a combination of reaction steps.
摘要翻译： 由于新化合物现在提供5-脱氧-5-氟乙酰霉素B，5,3'-二脱氧-5-氟沙卡他霉素B，5,4'-二脱氧-5-氟沙卡他霉素B和5,3'，4'-三脱氧-5 - 氟卡那霉素B以及1-N-（3-氨基-2-羟基丙酰基） - 或1-N-（4-氨基-2-羟基丁酰基）衍生物，它们都可用作抗菌剂并表现出改善的抗菌活性。 这些新化合物可以通过合适的方法从合适的N，O-保护的5-表卡那霉素B，3'-脱氧-5-表卡那霉素B，4'-脱氧-5-表卡那霉素B或3 '，4'-双脱氧-5-表卡那霉素B衍生物，其现在通过反应步骤的组合制备。
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公开(公告)号：EP0218440A2
公开(公告)日：1987-04-15
申请号：EP86307456.3
申请日：1986-09-29
发明人： Umezawa, Hamao , Nagatsu, Toshiharu , Takeuchi, Tomio , Sasaki, Fujinori CO-OP Shincho No. 203 , Morishima, Hajime , Sawasaki, Yoshio , Takezawa, Hiroshi
IPC分类号： C07C101/32 , A61K31/195 , C07C101/72
CPC分类号： A61K31/195
摘要： As new compounds N-methyl-3-(3,4-dihydroxyphenyl)serine alkyl esters. These are effective as a-adrenergic and β-adrenergic agenta to stimulate the a-adrenergic and β-adrenergic functions of the central nervous system of mammalian animals. Such compounds can be useful for therapeutic treatment of disorders as invoked by reduced biological activities or functions of the a-and/or β-adrenergic neurons. N-methyl-L-threo-3-(3,4-dihydroxyphenyl)serine (C 1 - Cs) alkyl esters are preferred amongst the new compounds of this invention.
摘要翻译： 作为新化合物N-甲基-3-（3,4-二羟基苯基）丝氨酸烷基酯。 这些作为α-肾上腺素能和β-肾上腺素能药物是有效的，以刺激哺乳动物中枢神经系统的α-肾上腺素能和β-肾上腺素能功能。 这样的化合物可用于治疗通过降低的生物活性或α和/或β-肾上腺素能神经元的功能引起的疾病。 在本发明的新化合物中，N-甲基-L-苏式-3-（3,4-二羟基苯基）丝氨酸（C1-C6）烷基酯是优选的。
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公开(公告)号：EP0086430B1
公开(公告)日：1985-11-06
申请号：EP83101145.7
申请日：1981-09-17
IPC分类号： C07C50/36
CPC分类号： C07D307/32 , C07C43/215 , C07C45/26 , C07D309/30 , C07H13/08 , C07H15/252 , Y02P20/55 , Y10S514/908 , C07C49/577
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34.发明公开A process for producing an optically active 3-(3,4-dihydroxphenyl) serine and a proteced derivative thereof 失效一种生产光学活性3-（3,4-二羟基苯基）丝氨酸及其保护衍生物的方法
公开(公告)号：EP0141613A3
公开(公告)日：1985-09-11
申请号：EP84307297
申请日：1984-10-24
发明人： Umezawa, Hamao , Takeuchi, Tomio , Nagatsu, Toshiharu , Hamada, Masa , Iwadare, Shuichi , Matsumoto, Ikuo , Morishima, Hajime
IPC分类号： C12P13/04 , C12P41/00 , C12R01/04 , C12R01/165 , C12R01/625 , C12R01/465
CPC分类号： C12P13/04 , C12P41/007 , Y10S435/826 , Y10S435/886 , Y10S435/908
摘要： N-acyl-DL-3-(3,4-dihydroxyphenyl)serine or a catecholic hydroxyl-protected derivative thereof is stereospecifically de-acylated by reaction with a microorganism of Streptomyces or Streptoverticillium having an acylase or with an extract of said microorganism containing said acylase, to produce L-3-(3,4-dihydroxyphenyl)serine or the hydroxyl-protected derivative thereof, with the N-acyl-D-3-(3,4-dihydroxyphenyl)serine compound remaining unaltered. The L-3-(3,4-dihydroxyphenyl)-serine compound so produced can be separated from the N-acyl-D-3-(3,4-dihydroxyphenyl)serine compound owing to its different properties.
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35.发明公开Tylosin derivatives, their preparation and pharmaceutical compositions containing them 失效泰乐菌素衍生物及其制备和含有它们的药物组合物
公开(公告)号：EP0132895A1
公开(公告)日：1985-02-13
申请号：EP84201085.2
申请日：1982-07-09
发明人： Umezawa, Hamao , Umezawa, Sumio , Tsuchiya, Tsutomu , Takeuchi, Tomio , Tanaka, Akihiro , Iwamoto, Hidenori , Sakamoto, Shuichi
CPC分类号： C07H17/08
摘要： A tylosin derivative represented by the general formula
wherein R. represents a hydrogen atom or a hydroxyl group and R. represents
(wherein R 9 and R 10 may be the same or different and selected from a hydrogen atom and C, to C. alkyl groups or which may together form an alkylene group having 3-7 carbon atoms) or -S-R 11 (wherein R " represents a furanyl group or a pyridyl group).摘要翻译： 由通式表示的泰乐菌素衍生物，其中R表示氢原子或羟基，并且R表示（其中R9和R10可以相同或不同并且选自氢原子和C，至C的烷基，或者 可以一起形成具有3-7个碳原子的亚烷基）或-S-R11（其中R“表示呋喃基或吡啶基）。
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36.发明公开N-methanesulfonic acid derivatives of 3-demethoxy-istamycin B and production thereof 失效N-Methansulfonsäure-Derivate von 3-Demethoxyistamycin-B und ihre Herstellung。
公开(公告)号：EP0130862A1
公开(公告)日：1985-01-09
申请号：EP84401075.1
申请日：1984-05-24
发明人： Umezawa, Hamao , Kondo, Shinichi
CPC分类号： C07H15/224
摘要： As new semi-synthetic antibiotic derivatives are provided N-methanesulfonic acid derivatives of 3-demethoxyistamycin B which are less toxic than the parent 3-demethoxyistamycin B but retain usefully high antibacterial activity of the parent antibiotic. The new derivatives are produced by a method of N-sulfomethylation where 3-demethoxyistamycin B is reacted with an aldehyde such as paraformaldehyde and sulfurous acid or sulfite reagent.
摘要翻译： 由于新的半合成抗生素衍生物提供3-脱甲氧基霉素B的N-甲磺酸衍生物，它们比亲本3-脱甲氧基霉素B毒性小，但保留有效的高抗菌活性。 新衍生物通过N-甲基磺酰化方法制备，其中3-脱甲氧基霉素B与醛如多聚甲醛和亚硫酸或亚硫酸盐试剂反应。
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公开(公告)号：EP0083931A2
公开(公告)日：1983-07-20
申请号：EP83100062.5
申请日：1983-01-05
IPC分类号： C07C103/52 , A61K37/02
CPC分类号： C07K5/0202
摘要： 3-Amino-2-hydroxy-4-phenylbutanoyl-leucyl-asparagines which are related to bestatin in their chemical structure and which are active to enhance the immune response in living animals are now provided.
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公开(公告)号：EP1593684B1
公开(公告)日：2016-11-02
申请号：EP04706817.6
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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39.发明公开
公开(公告)号：EP2902405A1
公开(公告)日：2015-08-05
申请号：EP14197814.8
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
摘要： Caprazol-1"'-amide derivatives of the formula (V) and caprazol-1"'- amide-3"'-ester derivatives from caprazol.
The novel caprazol derivatives now synthesized exhibit excellent antibacterial activities against a variety of bacteria including acid-fast bacteria.摘要翻译： 本发明新颖的吡唑衍生物对各种细菌（包括酸 - 磷酸酯）具有优异的抗菌活性， 快速细菌。
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40.发明授权COMPOSITIONS FOR TREATING OR PREVENTING MALARIA AND METHOD OF TREATING MALARIA 有权混合物用于治疗疟疾的治疗或预防疟疾和方法
公开(公告)号：EP1295881B1
公开(公告)日：2008-10-08
申请号：EP01925951.4
申请日：2001-04-26
发明人： TAKEUCHI, Tomio, New Fuji Mansion 701 , WATAYA, Yusuke , IINUMA, Munekazu , KIM, Hye-Sook , WATABE, Hiroomi , NAGANAWA, Hiroshi , TAKAHASHI, Yoshikazu
IPC分类号： C07D407/14 , A61K31/351 , A61P33/06
CPC分类号： C07D407/14 , A61K31/351 , Y02A50/411
摘要： An antibiotic SF2487 substance having the formula (I) or a salt thereof possesses an antimalarial activity against the proliferation of malarial parasites and is therefore useful as an antimalarial drug.
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