公开(公告)号：EP1889540B1

公开(公告)日：2011-11-02

申请号：EP06756816.2

申请日：2006-05-31

申请人： Meiji Seika Pharma Co., Ltd. ,  The Kitasato Institute

发明人： GOTO, Kimihiko, c/o Meiji Seika Kaisha, Ltd. ,  HORIKOSHI, Ryo, c/o Meiji Seika Kaisha, Ltd. ,  TSUCHIDA, Mariko, c/o Meiji Seika Kaisha, Ltd. ,  OYAMA, Kazuhiko, c/o Meiji Seika Kaisha, Ltd. ,  OMURA, Satoshi ,  TOMODA, Hiroshi ,  SUNAZUKA, Toshiaki

IPC分类号： A01N43/90

CPC分类号： C07D493/04 ,  A01N43/90

摘要： Disclosed is a composition used as a pest control agent which contains a compound represented by the formula (I) below or an agriculturally and horticulturally acceptable salt thereof as an active ingredient and an agriculturally and horticulturally acceptable carrier.

摘要翻译： 本发明公开了一种用作有害生物防除剂的组合物，其包含由下式（I）表示的化合物或其农业和园艺上可接受的盐作为活性成分和农业和园艺学上可接受的载体。

公开(公告)号：EP1950219B1

公开(公告)日：2011-06-22

申请号：EP06821966.6

申请日：2006-10-13

申请人： THE KITASATO INSTITUTE ,  Aphoenix, Inc.

发明人： OMURA, Satoshi ,  SUNAZUKA, Toshiaki ,  NAGAI, Kenichiro ,  SHIMA, Hideaki ,  YAMABE, Haruko

IPC分类号： C07H17/08 ,  A61K31/7048 ,  A61P1/04 ,  A61P29/00

CPC分类号： C07H17/08

摘要： Compounds represented by the general formula [I] (wherein each symbol is as defined in the description) or pharmacologically acceptable salts thereof; and pharmaceutical compositions containing the compounds or the salts as the active ingredient.

摘要翻译： 由通式[I]表示的化合物（其中每个符号如说明书中所定义）或其药理学上可接受的盐; 以及含有该化合物或盐作为活性成分的药物组合物。

公开(公告)号：EP1988171A1

公开(公告)日：2008-11-05

申请号：EP06714669.6

申请日：2006-02-21

申请人： THE KITASATO INSTITUTE

发明人： TOMODA, Hiroshi ,  OMURA, Satoshi ,  MASUMA, Rokuro

IPC分类号： C12P7/62 ,  A61K31/225 ,  A61K45/00 ,  A61P35/00 ,  C07C69/604 ,  C12N1/14

CPC分类号： C07C69/604 ,  A61K31/225 ,  A61K45/06 ,  C12P7/6436

摘要： The present invention relates to FKI-2342 substance which is produced by a process comprising culturing a microorganism belonging to genus Aspergillus and having ability to produce FKI-2342 substance represented by the general formula (I), accumulating FKI-2342 substance in a cultured mass, and isolating FKI-2342 substance from the cultured mass. The obtained FKI-2342 substance is expected to enhance an action of DNA damaging type anticancer agent or radiation therapy and to reduce side effects in the treatment with using the DNA damaging type anticancer agent or the radiation therapy.

摘要翻译： 本发明涉及通过包括培养属于曲霉属的微生物并具有产生由通式（I）表示的FKI-2342物质的能力的方法生产的FKI-2342物质，其在培养物质中积累FKI-2342物质 ，并从培养物质中分离出FKI-2342物质。 预期获得的FKI-2342物质可增强DNA损伤型抗癌剂或放射治疗的作用，并减少使用DNA损伤型抗癌剂或放射治疗的治疗副作用。

公开(公告)号：EP1160330B1

公开(公告)日：2006-08-09

申请号：EP99973760.4

申请日：1999-03-08

申请人： THE KITASATO INSTITUTE

发明人： OMURA, Satoshi ,  TOMODA, Hiroshi ,  TAKAHASHI, Yoko

IPC分类号： C12P13/00 ,  C12N1/20 ,  C07F15/02 ,  C12P9/00 ,  A61K31/295 ,  C12R1/465

CPC分类号： C12P13/008 ,  C07F15/025 ,  C12P9/00 ,  C12R1/465

摘要： Novel substances WK-5344A and WK-5344B having an effect of inhibiting cholesteryl ester transfer protein; and a process for producing the same which comprises culturing a microorganism belonging to the genus Streptomyces and being capable of producing the substances WK-5344A and WK-5344B in a medium, thus accumulating the substances WK-5344A and WK-5344B in the culture and collecting the substances WK-5344A and WK-5344B therefrom. Because of showing a potent inhibitory activity on cholesteryl ester transfer protein, these substances are useful in preventing and treating human diseases induced by the accumulation of cholesterol.

公开(公告)号：EP1659116A1

公开(公告)日：2006-05-24

申请号：EP03748519.0

申请日：2003-08-29

申请人： THE KITASATO INSTITUTE

发明人： OMURA, Satoshi ,  TOMODA, Hiroshi ,  MASUMA, Rokuro ,  Arai, Masayoshi

IPC分类号： C07D273/00 ,  C12N1/14 ,  C12P17/14 ,  A61K31/395 ,  A61P31/10

CPC分类号： C12P17/14 ,  A61K31/395 ,  C07D273/00 ,  C12R1/645

摘要： A microorganism belonging to Beauveria sp. and having ability to produce FKI-1366 substance A and/or FKI-1366 substance B and/or FKI-1366 substance C (Beauveria sp. FKI-1366 FERM BP-08459) is cultured in a medium, accumulating FKI-1366 substance A and/or FKI-1366 substance B and/or FKI-1366 substance C in the culture liquid and isolating FKI-1366 substance A and/or FKI-1366 substance B and/or FKI-1366 substance C from said cultured mass. Since the thus obtained FKI-1366 substance A and/or FKI-1366 substance B and/or FKI-1366 substance C or composition thereof have activity to enhance azole antifungal agent, the substance has an action against various fungal infections such as deep-seated mycosis and other fungal infections in the low concentration within short term. Consequently, the substance is useful for reducing frequency of appearance of resistant microorganisms and overcoming resistance, and is expected as a medicament.

摘要翻译： 属于白僵菌的微生物 并且在培养基中培养产生FKI-1366物质A和/或FKI-1366物质B和/或FKI-1366物质C（白僵菌FKI-1366FERM BP-08459）的能力，将FKI-1366物质A 和/或FKI-1366物质B和/或FKI-1366物质C，并从所述培养物质分离FKI-1366物质A和/或FKI-1366物质B和/或FKI-1366物质C。 由于如此获得的FKI-1366物质A和/或FKI-1366物质B和/或FKI-1366物质C或其组合物具有增强唑类抗真菌剂的活性，所以该物质具有针对各种真菌感染的作用，例如深层次 短期内低浓度的真菌病和其他真菌感染。 因此，该物质可用于降低抗性微生物的出现频率并克服抗性，并且预期作为药物。

公开(公告)号：EP1454905A1

公开(公告)日：2004-09-08

申请号：EP01274937.0

申请日：2001-12-11

申请人： THE KITASATO INSTITUTE

发明人： OMURA, Satoshi ,  SHIOMI, Kazuro ,  MASUMA, Rokuro

IPC分类号： C07D309/38 ,  C12P17/06 ,  C12N1/14 ,  A61K31/351 ,  A61P33/10 ,  A61P31/04

CPC分类号： C12R1/645 ,  C07D309/38 ,  C12P17/06

摘要： The present invention is comprised of culturing microorganism having ability to produce FKI-1083 substance represented by the formula:
in a medium, accumulating FKI-1083 substance in the cultured medium, and isolating FKI-1083 substance from the cultured mass. The thus obtained FKI-1083 substance has growth inhibitory activities against microorganisms, nematodes and arthropods, and is useful as anthelmintic and insecticide.

摘要翻译： 本发明包括在培养基中培养具有由式：CHEM>表示的FKI-1083物质的能力的微生物，在培养基中积聚FKI-1083物质，并从培养物质中分离FKI-1083物质。 由此获得的FKI-1083物质对微生物，线虫和节肢动物具有生长抑制活性，可用作驱肠虫和杀虫剂。

公开(公告)号：EP1270728A1

公开(公告)日：2003-01-02

申请号：EP01906278.5

申请日：2001-02-23

申请人： KYOWA HAKKO KOGYO CO., LTD. ,  THE KITASATO INSTITUTE

发明人： ENDO, Hirofumi, Kyowa Hakko Kogyo Co. Ltd. ,  YAMAGUCHI, Hiroyuki, Tokyo Res. Lab. Kyowa Hakko ,  KANDA, Yutaka, Pharm. Res. Inst. Kyowa Hakko ,  HASHIMOTO, Shinichi, Tokyo Res. Lab. Kyowa Hakko ,  OMURA, Satoshi ,  IKEDA, Haruo

IPC分类号： C12N15/54 ,  C12N15/53 ,  C12N9/10 ,  C12N9/14 ,  C12N1/21 ,  C07C327/30 ,  C12P17/08

CPC分类号： C12N15/52 ,  C07C327/30

摘要： According to the present invention, 22,23-dihydroavermectin B1a, which is useful as a medicine, a veterinary drug, and a pesticide, can be directly fermented and produced. This can obviate the need for the complicated and difficult conventional processes for purifying avermectin B1a at an industrial level and for chemically modifying avermectin B1a and can significantly decrease cost and time required in the industrial production of 22,34-dihydroavermectin B1a. The production of the formulation containing only 22,23-dihydroavermectin B1a, which is highly effective as a medicine, is also realized.

摘要翻译： 根据本发明，可以直接发酵和制造可用作药物，兽药和农药的22,23-二氢阿凡曼菌素B1a。 这可以避免需要复杂且困难的用于纯化工业水平的除虫菌素B1a和用于化学改性除虫菌素B1a的常规方法，并且可以显着降低工业生产22,34-二氢阿凡曼菌素B1a所需的成本和时间。 也可以实现仅含有作为药物高度有效的22,23-二氢阿凡曼明B1a的制剂的生产。

公开(公告)号：EP3441399A1

公开(公告)日：2019-02-13

申请号：EP18194117.0

申请日：2013-06-13

申请人： Meiji Seika Pharma Co., Ltd. ,  The Kitasato Institute

发明人： MITOMI, Masaaki ,  SAKAI, Masayo ,  HORIKOSHI, Ryo ,  ONOZAKI, Yasumichi ,  NAKAMURA, Satoshi ,  OMURA, Satoshi ,  SUNAZUKA, Toshiaki ,  HIROSE, Tomoyasu ,  SHIOMI, Kazuro ,  MASUMA, Rokuro

IPC分类号： C07K11/02 ,  A01N43/72 ,  A01P5/00 ,  A01P7/02 ,  A01P7/04 ,  C07C231/12 ,  C07C235/12 ,  C07C269/06 ,  C07C271/22 ,  C07D273/08 ,  C07B51/00 ,  C07B61/00

摘要： An objective of the present invention is to provide novel cyclic depsipeptide derivatives and harmful organism control agents including the same as each other. Specifically, the present invention provides compounds represented by formula (1) or stereoisomers thereof, harmful organism control agents containing them, and a process for producing them.

公开(公告)号：EP2939668A1

公开(公告)日：2015-11-04

申请号：EP13869345.2

申请日：2013-12-26

申请人： The Kitasato Institute ,  Tokushima University ,  Nobelpharma Co., Ltd.

发明人： OMURA, Satoshi ,  NAKANO, Hirofumi ,  YAMAJI, Kenzaburo ,  YAMAMOTO, Tsuyoshi ,  KIDO, Hiroshi ,  YAMANE, Kazuhiko ,  SUNAZUKA, Toshiaki ,  HIROSE, Tomoyasu

IPC分类号： A61K31/015 ,  A61K31/122 ,  A61P1/14 ,  A61P13/02 ,  A61P31/16 ,  A61P35/00 ,  A61P43/00

CPC分类号： C07C69/95 ,  A61K8/355 ,  A61K8/368 ,  A61K8/37 ,  A61K8/40 ,  A61K8/42 ,  A61K31/122 ,  A61K31/136 ,  A61K31/166 ,  A61K31/192 ,  A61K31/198 ,  A61K31/216 ,  A61K31/235 ,  A61K31/37 ,  A61K31/47 ,  A61K2800/782 ,  A61Q19/00 ,  A61Q19/08 ,  C07C50/38 ,  C07C66/00 ,  C07C235/66 ,  C07C235/84 ,  C07C251/32 ,  C07C251/40 ,  C07D493/20

摘要： The present invention to provide a novel pyruvate dehydrogenase kinase inhibitors. A pyruvate dehydrogenase kinase inhibitor comprising a compound represented by the general formula (I) as an active ingredient (wherein, ring A represents a 6-membered aromatic hydrocarbon ring optionally substituted with 2-4 substituents,
R 1 and R 4 , which are the same or different, represent a hydrogen atom, a hydroxyl group, an optionally substituted C1-6 alkyl group, R 2 and R 3 , which are the same or different, represent a hydrogen atom, a carboxyl group, an optionally substituted C1-6 alkyl group, an optionally substituted C6-10 aryl group, or a group represented by -C (=R 9 )-R 10 ), a pharmaceutical composition for treatment or prophylaxis of diseases or disorders that pyruvate dehydrogenase kinase relates to its development or aggravation, and a cosmetic composition, and the like.

摘要翻译： 本发明提供了一种新的丙酮酸脱氢酶激酶抑制剂。 丙酮酸脱氢酶激酶抑制剂，其包含由通式（I）表示的化合物作为活性成分（其中，环A表示任选被2-4个取代基取代的6元芳族烃环，R 1和R 4是 相同或不同，表示氢原子，羟基，任选取代的C 1-6烷基，R 2和R 3相同或不同，表示氢原子，羧基，任选取代的C 1-6 烷基，任选取代的C 6-10芳基或由-C（= R 9）-R 10表示的基团），用于治疗或预防丙酮酸脱氢酶激酶涉及其发展或恶化的疾病或病症的药物组合物 ，和化妆品组合物等。

公开(公告)号：EP2752416A1

公开(公告)日：2014-07-09

申请号：EP12828060.9

申请日：2012-08-31

申请人： The Kitasato Institute

发明人： OMURA, Satoshi ,  TAKAHASHI, Yoko ,  NAKASHIMA, Takuji ,  OTOGURO, Kazuhiko ,  SHIOMI, Kazuro ,  IWATSUKI, Masato ,  MATSUMOTO, Atsuko

IPC分类号： C07D493/18 ,  A61K31/366 ,  A61P33/00 ,  C12N1/20 ,  C12P1/06 ,  C12R1/01

CPC分类号： C07D493/16 ,  C07D493/18 ,  C12P17/181 ,  C12R1/01

摘要： [Problem]
The present invention addresses the problem of providing an anti-trypanosomal drug having a novel skeleton, in order to solve issues that occur with conventional technologies.
[Solution]
The present invention is based on the discovery of a microbe that produces an anti-trypanosomal drug having a novel skeleton. Specifically, this invention provides: a compound indicated by formula (I) having a trypanosomal inhibitory activity; an analog thereof; a production method therefor; and a Lechevalieria sp. K10-0216 strain that produces said compound.

摘要翻译： 本发明解决提供具有新骨架的抗锥虫药物的问题，以解决常规技术中出现的问题。 [解决方案]本发明是基于产生具有新骨架的抗锥虫药物的微生物的发现。 具体地，本发明提供：具有锥虫体抑制活性的式（I）表示的化合物; 其类似物; 一种生产方法; 和Lechevalieria sp。 产生所述化合物的K10-0216菌株。