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1. 发明授权

US06245734B1 Physiologically active polyoxypeptin and deoxypolyoxypeptin and anticancer drugs containing the same 失效
标题翻译：生理活性多羟脯氨酸和含有相同抗氧化素的抗癌药物
公开(公告)号：US06245734B1
公开(公告)日：2001-06-12
申请号：US09445581
申请日：1999-12-13
申请人： Tomio Takeuchi , Kazuo Umezawa , Shinichi Kondo , Yoko Ikeda , Hiroshi Naganawa , Masa Hamada
发明人： Tomio Takeuchi , Kazuo Umezawa , Shinichi Kondo , Yoko Ikeda , Hiroshi Naganawa , Masa Hamada
IPC分类号： A01N6100
CPC分类号： C12R1/465 , A61K38/00 , C07K7/06
摘要： As novel substances having an activity of inducing an apoptosis even on the apoptosis-resistant cancer cells, there are obtained polyoxypeptin and deoxypolyoxypeptin represented by the following general formula (I) wherein R denotes a hydroxyl group for polyoxypeptin, or R denotes a hydrogen atom for deoxypolyoxypeptin, by cultivation of Streptomyces sp. MK498-98F14 strain. Polyoxypeptin and deoxypolyoxypeptin are physiologically active substances which have an activity of inducing apoptosis on a human pancreatic adenocarcinoma cell, AsPC-1 cell.
摘要翻译：作为具有诱导细胞凋亡抗性的癌细胞的细胞凋亡的活性的新物质，可以举出以下通式（I）表示的多羟脯氨酸和脱氧多肽，其中R表示多羟脯氨酸的羟基，或R表示氢原子，脱氧脱氧蛋白，通过培养链霉菌 MK498-98F14菌株。多核苷酸和脱氧多肽抗氧化素是具有诱导人胰腺癌细胞AsPC-1细胞凋亡活性的生理活性物质。

2. 发明授权

US5003055A Anthracycline derivatives having inhibitory activity against reverse transcriptase of human immunodeficiency virus 失效
标题翻译：对人类免疫缺陷病毒逆转录酶具有抑制活性的蒽环类衍生物
公开(公告)号：US5003055A
公开(公告)日：1991-03-26
申请号：US248417
申请日：1988-09-23
申请人： Tomio Takeuchi , Shinichi Kondo , Daishiro Ikeda , Yoshiyuki Koyama , Keiichi Ajito , Kazuo Umezawa , Sonoko Hirose
发明人： Tomio Takeuchi , Shinichi Kondo , Daishiro Ikeda , Yoshiyuki Koyama , Keiichi Ajito , Kazuo Umezawa , Sonoko Hirose
IPC分类号： C07C65/21 , C07H17/08
CPC分类号： C07H17/08 , C07C65/21
摘要： As new compounds are now provided 14-O-(3,4-disubstituted benzoyl)adriamycins which are of low cytotoxicity and exhibit a high activity inhibitory to the reverse transcriptase of human immunodeficiency virus (HIV) and which can inhibit propagation of HIV.

3. 发明授权

US06566394B1 Salicylamide derivatives 失效
标题翻译：水杨酰胺衍生物
公开(公告)号：US06566394B1
公开(公告)日：2003-05-20
申请号：US10049158
申请日：2002-05-30
申请人： Tomio Takeuchi , Kazuo Umezawa , Sakino To-E , Naoki Matsumoto , Tsutomu Sawa , Takeo Yoshioka , Naoki Agata , Shin-ichi Hirano , Kunio Isshiki
发明人： Tomio Takeuchi , Kazuo Umezawa , Sakino To-E , Naoki Matsumoto , Tsutomu Sawa , Takeo Yoshioka , Naoki Agata , Shin-ichi Hirano , Kunio Isshiki
IPC分类号： A61K31336
CPC分类号： C07D303/36 , C07C237/38 , C07C237/40
摘要： Salicylamide derivatives represented by formulae (1a) and (1b); intermediates in the production thereof; a process for producing the same; and drugs containing the same as the active ingredient. The salicylamide derivatives represented by formulae (1a) and (1b) are useful as anti-inflammatory agents and immunosuppressive agents which exert an effect of inhibiting the activation of NF-&kgr;B with little side effects.
摘要翻译：由式（1a）和（1b）表示的水杨酰胺衍生物; 中间体在其生产中; 其制造方法; 和含有与活性成分相同的药物。由式（1a）和（1b）表示的水杨酰胺衍生物可用作具有抑制NF-κB活化的副作用的抗炎剂和免疫抑制剂。

4. 发明授权

US4873225A 1-n-(4-amino-3-fluoro-2-hydroxybutyryl)-kanamycins 失效
标题翻译： 1-正（4-氨基-3-氟-2-羟基丁酰） - 卡那霉素
公开(公告)号：US4873225A
公开(公告)日：1989-10-10
申请号：US158628
申请日：1988-02-22
申请人： Sumio Umezawa , Tsutomu Tsuchiya , Tomio Takeuchi , Kazuo Umezawa , Yoshiaki Takahashi , Tetsuo Shitara , Yoshihiko Kobayashi , Yasushi Takagi
发明人： Sumio Umezawa , Tsutomu Tsuchiya , Tomio Takeuchi , Kazuo Umezawa , Yoshiaki Takahashi , Tetsuo Shitara , Yoshihiko Kobayashi , Yasushi Takagi
IPC分类号： C07H15/234 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07H15/236
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-hydroxybutyryl}-2',3'-dideoxykanamycin A; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-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-3-fluoro-2-hydroxybutyryl}-kanamycin B; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-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-hydroxybutyryl}-5,3'-dideoxy-5-fluorokanamycin B; and 1-N{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-5,3',4'-trideoxy-5-fluorokanamycin B, which are all useful as antibacterial agent in the therapeutic treatment of bacterial infections.

5. 发明授权

US08524747B2 Pharmaceutical compositions 失效
标题翻译：药物组合物
公开(公告)号：US08524747B2
公开(公告)日：2013-09-03
申请号：US13000442
申请日：2009-06-25
申请人： Kazuo Umezawa , Yuichi Ishikawa , Shigeru Nishiyama , Miyuki Tachibana , Ayumi Kaneda
发明人： Kazuo Umezawa , Yuichi Ishikawa , Shigeru Nishiyama , Miyuki Tachibana , Ayumi Kaneda
IPC分类号： A61K31/44
CPC分类号： C07D211/88 , A61K31/45
摘要： The object of the present invention is to provide a pharmaceutical composition that inhibits expression of iNOS and COX-2 without inhibiting NF-κB. The pharmaceutical composition that inhibits expression of iNOS and COX-2 without inhibiting NF-κB contains DTCM glutarimide of the Formula (I) as an effective ingredient, thereby being able to inhibit nitric oxide (NO) production and prostaglandin production.
摘要翻译：本发明的目的是提供抑制iNOS和COX-2的表达而不抑制NF-κB的药物组合物。抑制iNOS和COX-2的表达而不抑制NF-κB的药物组合物含有式（I）的DTCM戊二酰亚胺作为有效成分，从而能够抑制一氧化氮（NO）产生和前列腺素的产生。

6. 发明申请

US20090291153A1 Health food, Method for producing the same and dried Product and Extract 审中-公开
标题翻译：保健食品，生产方法和干燥产品和提取物
公开(公告)号：US20090291153A1
公开(公告)日：2009-11-26
申请号：US10577328
申请日：2005-04-14
申请人： Kazuo Umezawa , Izumi Takei , Seiji Shibahara , Itaru Kojima , Takashi Koyano , Chika Ishii
发明人： Kazuo Umezawa , Izumi Takei , Seiji Shibahara , Itaru Kojima , Takashi Koyano , Chika Ishii
IPC分类号： A61K36/24 , A61P3/10
CPC分类号： A61K31/455 , A23L33/105 , A23V2002/00 , A61K36/24 , A23V2250/21 , A23V2200/328
摘要： Conophylline, contained in leaves of Ervatamia microphylla or Tabernaemontana divaricata, can induce non-tumor cells to differentiate into insulin-producing cells and thereby to produce insulin and also to lower blood glucose levels. Thus, in the present invention, dried products and extracts of leaves of Ervatamia microphylla or Tabernaemontana divaricata, which contain conophylline, are used as health foods for preventing and improving diabetes and obesity or health foods for lowering blood glucose levels.
摘要翻译：茶叶中含有的叶绿素（Ervatamia microphylla）或Tabernaemontana divaricata，可诱导非肿瘤细胞分化成胰岛素生成细胞，从而产生胰岛素，降低血糖水平。因此，本发明中，作为防止和改善用于降低血糖水平的糖尿病和肥胖症或健康食品的健康食品，使用干燥产品和含有茶碱的小叶螨的叶子的提取物或者Tabernaemontana divaricata的叶子提取物。

7. 发明授权

US08178135B2 Aqueous solution of conophylline and/or conophyllidine 有权
标题翻译：茶碱和/或叶绿素碱的水溶液
公开(公告)号：US08178135B2
公开(公告)日：2012-05-15
申请号：US12281940
申请日：2007-03-05
申请人： Kazuo Umezawa , Mikio Fujii
发明人： Kazuo Umezawa , Mikio Fujii
IPC分类号： A61K36/00
CPC分类号： A61K36/24 , A23L33/105 , A61K31/475 , C07D491/22
摘要： PROBLEMS TO BE SOLVED BY THE INVENTIONTo provide aqueous solutions of conophylline and/or conophyllidine; methods for purifying conophylline and/or conophyllidine from the aqueous solutions; methods for producing the aqueous solutions, water-soluble compositions containing conophylline and/or a conophyllidine useful for food compositions or pharmaceutical compositions or methods for preparing the same; as well as food compositions or pharmaceutical compositions containing the water-soluble compositions.MEANS OF SOLVING THE PROBLEMSIt has been found that conophylline and/or conophyllidine can be efficiently extracted from a plant producing conophylline and/or conophyllidine with an acidic aqueous solution having a pH equal to or less than 4. The extract thus obtained, i.e., aqueous solution of conophylline, and/or conophyllidine is useful for production of, for instance, food compositions, pharmaceutical compositions, etc.
摘要翻译：本发明要解决的问题提供茶碱和/或叶绿素碱的水溶液; 从水溶液中纯化茶碱和/或叶绿素的方法; 制备水溶液的方法，含有可用于食品组合物或药物组合物的茶碱和/或叶绿素的水溶性组合物或其制备方法; 以及含有水溶性组合物的食品组合物或药物组合物。解决问题的手段已经发现，可以用pH等于或小于4的酸性水溶液从产生茶碱和/或叶绿素的植物中有效地提取茶碱和/或叶肉氨酸。由此得到的提取物，茶碱水溶液和/或叶绿素碱可用于生产例如食品组合物，药物组合物等。

8. 发明申请

US20110213001A1 PHARMACEUTICAL COMPOSITIONS 失效
标题翻译：药物组合物
公开(公告)号：US20110213001A1
公开(公告)日：2011-09-01
申请号：US13000442
申请日：2009-06-25
申请人： Kazuo Umezawa , Yuichi Ishikawa , Shigeru Nishiyama , Miyuki Tachibana , Ayumi Kaneda
发明人： Kazuo Umezawa , Yuichi Ishikawa , Shigeru Nishiyama , Miyuki Tachibana , Ayumi Kaneda
IPC分类号： A61K31/4422 , C07D221/00 , A61P35/00 , A61P19/02 , A61P29/00 , A61P25/16
CPC分类号： C07D211/88 , A61K31/45
摘要： The object of the present invention is to provide a pharmaceutical composition that inhibits expression of iNOS and COX-2 without inhibiting NF-κB. The pharmaceutical composition that inhibits expression of iNOS and COX-2 without inhibiting NF-κB contains DTCM glutarimide of the Formula (I) as an effective ingredient, thereby being able to inhibit nitric oxide (NO) production and prostaglandin production.
摘要翻译：本发明的目的是提供抑制iNOS和COX-2的表达而不抑制NF-κB的药物组合物。抑制iNOS和COX-2表达而不抑制NF-κB的药物组合物含有式（I）的DTCM戊二酰亚胺作为有效成分，从而能够抑制一氧化氮（NO）的产生和前列腺素的产生。

9. 发明申请

US20100286184A1 AQUEOUS SOLUTION OF CONOPHYLLINE AND/OR CONOPHYLLIDINE 有权
标题翻译：对映体和/或对羟苯胺的水溶液
公开(公告)号：US20100286184A1
公开(公告)日：2010-11-11
申请号：US12281940
申请日：2007-03-05
申请人： Kazuo Umezawa , Mikio Fujii
发明人： Kazuo Umezawa , Mikio Fujii
IPC分类号： A61K31/475 , A61P3/10
CPC分类号： A61K36/24 , A23L33/105 , A61K31/475 , C07D491/22
摘要： PROBLEMS TO BE SOLVED BY THE INVENTION To provide aqueous solutions of conophylline and/or conophyllidine; methods for purifying conophylline and/or conophyllidine from the aqueous solutions; methods for producing the aqueous solutions, water-soluble compositions containing conophylline and/or a conophyllidine useful for food compositions or pharmaceutical compositions or methods for preparing the same; as well as food compositions or pharmaceutical compositions containing the water-soluble compositions. MEANS OF SOLVING THE PROBLEMS It has been found that conophylline and/or conophyllidine can be efficiently extracted from a plant producing conophylline and/or conophyllidine with an acidic aqueous solution having a pH equal to or less than 4. The extract thus obtained, i.e., aqueous solution of conophylline, and/or conophyllidine is useful for production of, for instance, food compositions, pharmaceutical compositions, etc.
摘要翻译：本发明要解决的问题提供茶碱和/或叶绿素碱的水溶液; 从水溶液中纯化茶碱和/或叶绿素的方法; 制备水溶液的方法，含有可用于食品组合物或药物组合物的茶碱和/或叶绿素的水溶性组合物或其制备方法; 以及含有水溶性组合物的食品组合物或药物组合物。解决问题的手段已经发现，可以用pH等于或小于4的酸性水溶液从产生茶碱和/或叶绿素的植物中有效地提取茶碱和/或叶肉氨酸。由此得到的提取物，茶碱水溶液和/或叶绿素碱可用于生产例如食品组合物，药物组合物等。

10. 发明申请

US20060167086A1 Medicinal composition 审中-公开
标题翻译：药用成分
公开(公告)号：US20060167086A1
公开(公告)日：2006-07-27
申请号：US10545234
申请日：2004-02-16
申请人： Kazuo Umezawa , Kuniki Kato , Yoshikazu Suzuki , Yutaka Horiguchi , Jun Nakashima , Hiroyuki Hata , Hiroyuki Namba , Izumi Takei , Ryouichi Horie
发明人： Kazuo Umezawa , Kuniki Kato , Yoshikazu Suzuki , Yutaka Horiguchi , Jun Nakashima , Hiroyuki Hata , Hiroyuki Namba , Izumi Takei , Ryouichi Horie
IPC分类号： A61K31/336
CPC分类号： C07D303/36 , A61K31/336 , Y02A50/406
摘要： (−)-DHM2EQ, which is useful as an antitumor agent and an anti-inflammatory agent, can be directly obtained by optically resolving (±)-DHM2EQ using an optically active column packed with an optical resolving agent containing, for example, amylose tris(3,5-dimethylphenylcarbamate) as an active ingredient. The (−)-DHM2EQ obtained by optical resolution using the optically active column or pharmacologically acceptable salt thereof is useful as a pharmaceutical composition for improving various symptoms.
摘要翻译：（ - ） - DHM2EQ，其可用作抗肿瘤剂和抗炎剂，可以通过光学拆分（±）-DHM2EQ直接获得，该光学活性色谱柱装有光学拆分剂，该光学拆分剂含有例如直链淀粉三（3,5-二甲基苯基氨基甲酸酯）作为活性成分。使用光学活性柱或其药学上可接受的盐通过光学拆分获得的（ - ） - DHM2EQ可用作改善各种症状的药物组合物。

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