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1. 发明授权

EP1200421B1 PROCESS FOR PRODUCING ISOCOUMARINS AND INTERMEDIATES FOR THE SAME 有权
标题翻译：法生产ISOCOUMARINEN及其中间体
公开(公告)号：EP1200421B1
公开(公告)日：2008-08-27
申请号：EP00940911.1
申请日：2000-06-30
申请人： MERCIAN CORPORATION , ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
发明人： Tsuchida, Toshio , Nagai, Hazuki , Nakashima, Takashi , Yoshida, Masashi , Konuki, Kaname , Kuroda, Asako , Isshiki, Kunio , Takeuchi, Tomio
IPC分类号： C07D311/76 , C07C69/78
CPC分类号： C07D311/76 , C07C67/31 , C07C67/343 , C07C67/46 , C07C69/92 , Y02P20/55 , C07C69/88
摘要： Provided is a process for producing an isocoumarin-3-yl-acetic acid derivative, characterized by reacting a homophthalic acid derivative represented by formula (a): (wherein Rc, R2 and R are mainly protecting groups) with a malonic acid derivating represented by formula (IV): (wherein R is an organic group including a lower alkyl group; R3 is a protecting group for a carboxyl group; and X is a halogen atom or a -OM group (wherein M is alkaline metal or alkaline earth metal)). According to the above process, various isocoumarin-3-yl-acetic acid derivatives can efficiently be provided.

2. 发明公开

EP1200421A1 PROCESS FOR PRODUCING ISOCOUMARINS AND INTERMEDIATES FOR THE SAME 有权
标题翻译：法生产ISOCOUMARINEN及其中间体
公开(公告)号：EP1200421A1
公开(公告)日：2002-05-02
申请号：EP00940911.1
申请日：2000-06-30
申请人： MERCIAN CORPORATION , ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
发明人： Tsuchida, Toshio , Nagai, Hazuki , Nakashima, Takashi , Yoshida, Masashi , Konuki, Kaname , Kuroda, Asako , Isshiki, Kunio , Takeuchi, Tomio
IPC分类号： C07D311/76 , C07C69/78
CPC分类号： C07D311/76 , C07C67/31 , C07C67/343 , C07C67/46 , C07C69/92 , Y02P20/55 , C07C69/88
摘要： Provided is a process for producing an isocoumarin-3-yl-acetic acid derivative, characterized by reacting a homophthalic acid derivative represented by formula (a): (wherein Rc, R2 and R are mainly protecting groups) with a malonic acid derivating represented by formula (IV): (wherein R is an organic group including a lower alkyl group; R3 is a protecting group for a carboxyl group; and X is a halogen atom or a -OM group (wherein M is alkaline metal or alkaline earth metal)). According to the above process, various isocoumarin-3-yl-acetic acid derivatives can efficiently be provided.

3. 发明授权

EP0356330B1 Pharmaceutical composition for inhibiting infection with virus causative of acquired human immunodeficiency syndrome 失效
标题翻译：药物预防感染与负责艾滋病病毒
公开(公告)号：EP0356330B1
公开(公告)日：1999-10-13
申请号：EP89402315.9
申请日：1989-08-21
申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
发明人： Takeuchi, Tomio , Kondo, Shinichi , Hoshino, Hiroo
IPC分类号： A61K31/71
CPC分类号： A61K31/70 , C07H15/244 , Y10S514/934

4. 发明授权

EP0308977B1 Anthracycline derivatives having inhibitory activity against reverse transcriptase of human immunodeficiency virus 失效
标题翻译：具有抗人类免疫缺陷病毒的逆转录酶抑制活性的蒽环类衍生物。
公开(公告)号：EP0308977B1
公开(公告)日：1993-12-08
申请号：EP88115741.6
申请日：1988-09-23
申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
发明人： Takeuchi, Tomio , Kondo, Shinichi , Ikeda, Daishiro , Koyama, Yoshiyuki , Ajito, Keiichi , Umezawa, Kazuo , Hirose, Sonoko
IPC分类号： C07H15/252 , C07C65/01 , C07D319/08 , A61K31/70
CPC分类号： C07H17/08 , C07C65/21

5. 发明授权

EP0296040B1 Actinonin derivatives having physiological activities 失效
标题翻译：具有生理活动的ACTINONIN衍生物
公开(公告)号：EP0296040B1
公开(公告)日：1993-04-28
申请号：EP88401437.4
申请日：1988-06-10
申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI , MEIJI SEIKA KAISHA LTD.
发明人： Shibahara, Seiji , Takahashi, Yukiko , Matsuhashi, Yuji , Hachisu, Mitsugu , Kondo, Shinichi , Takeuchi, Tomio , Aoyagi, Takaaki
IPC分类号： C07D207/08 , A61K31/40
CPC分类号： C07D207/08

6. 发明公开

EP0474553A1 Actinonin derivatives 失效
标题翻译：放线菌素衍生物
公开(公告)号：EP0474553A1
公开(公告)日：1992-03-11
申请号：EP91402360.1
申请日：1991-09-04
申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI , MEIJI SEIKA KAISHA LTD.
发明人： Shibahara, Seiji, Pharmaceutical Research Center , Koyama, Yoshiyuki, Pharmaceutical Research Center , Inoue, Shigeharu, Pharmaceutical Research Center , Hachisu, Mitsugu, Pharmaceutical Research Center , Kondo, Shinichi , Aokagi, Takaaki , Takeuchi, Tomio
IPC分类号： C07D207/08 , C07D207/16
CPC分类号： C07D207/08 , C07D207/16
摘要： A novel actinonin derivative and a salt thereof are provided, which are useful as enzyme inhibitors and particularly have strong inhibitory activities against enkephalinase and angiotensin-converting enzymes. This actinonin derivative is represented by general formula (I):

wherein R¹ is sulfoxymethyl or carboxyl or a substituted carboxyl group selected from carboxamide, hydroxyamino-carbonyl and alkoxycarbonyl groups; and R² is hydroxyl, alkoxy, hydroxyamino or sulfoxyamino group.
摘要翻译：提供了一种新的放线菌素衍生物及其盐，它们可用作酶抑制剂，特别是对脑啡肽酶和血管紧张素转化酶具有强抑制活性。该放线菌素衍生物由通式（I）表示：其中R 1是磺氧甲基或羧基或选自羧酰胺，羟氨基 - 羰基和烷氧羰基的取代羧基; 和R 2是羟基，烷氧基，羟基氨基或亚磺酰氨基。

7. 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。

8. 发明公开

EP0420552A2 New antifungal antibiotic, and the production and uses of same 失效
标题翻译： Antifungales Antibiotikum und seine Herstellung und Verwendung。
公开(公告)号：EP0420552A2
公开(公告)日：1991-04-03
申请号：EP90310433.9
申请日：1990-09-24
申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
发明人： Takeuchi, Tomio , Hamada, Masa , Kondo, Shinichi , Sezaki, Masaji , Gomi, Shuichi
IPC分类号： C07H15/244 , A61K31/71 , C12P19/56
CPC分类号： C07H15/244
摘要： A new antibiotic, dexylosylbenanomicin A (formula I) is provided, which exhibits an antifungal activity and is useful as a therapeutic antifungal agent. Dexylosylbenanomicin A may be produced either by chemical conversion of a known antifungal and antiviral antibiotic, benanomicin A, or by cultivation of a benanomicin-producing MH193-16F4 strain of actinomycetes (identifiable as FERM BP-2051).
摘要翻译：提供了一种新的抗生素，具有抗真菌活性的dexylosylbenanomicin A（式I），可用作治疗性抗真菌剂。可以通过已知的抗真菌和抗病毒抗生素，苯那霉素A的化学转化或通过培养产生苯丙氨酸的MH193-16F4菌株的放线菌（可鉴定为FERM BP-2051）来生产脱甲基叶绿素组氨酸A. w

9. 发明公开

EP0335369A3 New anthracycline derivatives and processes for the preparation of the same 失效
标题翻译：新的蒽醌衍生物及其制备方法
公开(公告)号：EP0335369A3
公开(公告)日：1990-03-28
申请号：EP89105540.2
申请日：1989-03-29
申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
发明人： Takeuchi, Tomio , Umezawa, Sumio , Tsuchiya, Tsutomu , Umezawa, Kazuo , Takagi, Yasushi CI Mansion Higashi Totsuka , Miyake, Toshiaki
IPC分类号： C07H15/252 , A61K31/70
CPC分类号： C07H15/252
摘要： As new anthracycline derivatives are now produced 7-O-(2,6-dideoxy-2-fluoro-a-L-mannopyranosyl)-daunomycinone and -adriamycinone, their 4-demethoxy derivatives and 14-0-ester derivatives of the adriamycinone compounds of them, as well as 4-demethoxy-7-0-(2,6-dideoxy-2-fluoro-α-L-talopyranosyl)-daunomycinone and -adriamycinone and 14-0-ester derivatives of the adriamycinone compound thereof which )exhibit excellent antitumor activities and are useful as antitumor agents. These new anthracycline derivatives may be produced by various processes.

10. 发明公开

EP0356330A1 Pharmaceutical composition for inhibiting infection with virus causative of acquired human immunodeficiency syndrome 失效
标题翻译： Arzneimittel zur Verhinderung einer Infektion mitdemfürAIDS verantwortlichen Virus。
公开(公告)号：EP0356330A1
公开(公告)日：1990-02-28
申请号：EP89402315.9
申请日：1989-08-21
申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
发明人： Takeuchi, Tomio , Kondo, Shinichi , Hoshino, Hiroo
IPC分类号： A61K31/71
CPC分类号： A61K31/70 , C07H15/244 , Y10S514/934
摘要： Pharmaceutical compositions containing at least one of benanomicins A and B and their salts are now provided, which are useful to inhibit the infection of human T-cells with HIV, namely a virus causative of acquired human immunodeficiency syndrome (AIDS). Thus, benanomicins A and B as well as their salts are useful as antiviral agent against HIV.
摘要翻译：现在提供含有至少一种贝那霉素A和B及其盐的药物组合物，其可用于抑制HIV感染人T细胞，即获得性人体免疫缺陷综合征（AIDS）病毒的病毒。因此，苯那霉素A和B及其盐可用作抗HIV的抗病毒剂。

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