公开(公告)号：US07670827B2

公开(公告)日：2010-03-02

申请号：US10535263

申请日：2003-06-11

申请人： Satoshi Omura ,  Haruo Ikeda ,  Yumiko Ogasawara

发明人： Satoshi Omura ,  Haruo Ikeda ,  Yumiko Ogasawara

IPC分类号： C12N1/21

CPC分类号： C12N1/20 ,  C12N15/52 ,  C12P17/181

摘要： In the present invention, a recombination of gene groups of nemadectin aglycon biosynthesis is performed for obtaining C-13 hydroxylnemadectin, to which sugar groups can be attached, and a production strain which produces C-13 hydroxylnemadectin is produced. Further, C-13 glycosylnemadectin producing strain is prepared by introducing aveBI-BVIII genes involving glycosidation of avermectin and biosynthesis of oleandrose. As described, C-13 hydroxylnemadectin and C-13 glycosidated nemadectin can be obtained effectively by using the producing strain prepared by means of the molecular genetic technology, and improvement in the biological activity thereof can be expected.

摘要翻译： 在本发明中，进行奈马替丁糖苷配基生物合成的基因组的重组，得到可以附着糖基的C-13羟基去神道菌素，生成产生C-13羟基神马丁的生产菌株。 此外，通过引入涉及除虫菌素糖基化和含有甘油糖的生物合成的aveBI-BVIII基因来制备C-13糖基胚乳肽生成菌株。 如上所述，可以通过使用通过分子遗传技术制备的生产菌株有效地获得C-13羟基去神道肽和C-13糖苷化的奈马克丁，并且可以预期其生物活性的改善。

公开(公告)号：US07630836B2

公开(公告)日：2009-12-08

申请号：US10156761

申请日：2002-05-29

申请人： Satoshi Omura ,  Haruo Ikeda ,  Jun Ishikawa ,  Hiroshi Horikawa ,  Tadayoshi Shiba ,  Yoshiyuki Sakaki ,  Masahira Hattori

发明人： Satoshi Omura ,  Haruo Ikeda ,  Jun Ishikawa ,  Hiroshi Horikawa ,  Tadayoshi Shiba ,  Yoshiyuki Sakaki ,  Masahira Hattori

IPC分类号： G01N33/48

CPC分类号： C07K14/36 ,  C12Q1/689

摘要： Novel polynucleotides derived from microorganisms belonging to actinomycetes and fragments thereof, polypeptides encoded by the polynucleotides and fragments thereof, polynucleotide arrays comprising the polynucleotides and fragments thereof, recording media in which the nucleotide sequences of the polynucleotide and fragments thereof have been recorded which are readable in a computer, and use of them.

摘要翻译： 衍生自属于放线菌及其片段的微生物的新型多核苷酸，由多核苷酸及其片段编码的多肽，包含多核苷酸及其片段的多核苷酸阵列，其中记录了多核苷酸及其片段的核苷酸序列已被记录的可记录的多核苷酸 一台电脑，并使用它们。

公开(公告)号：US07541336B2

公开(公告)日：2009-06-02

申请号：US10532662

申请日：2002-11-12

申请人： Satoshi Omura ,  Kazuro Shiomi ,  Rokuro Masuma

发明人： Satoshi Omura ,  Kazuro Shiomi ,  Rokuro Masuma

IPC分类号： A61K38/00 ,  A61K51/00

CPC分类号： C07K11/02 ,  A01N43/72 ,  C12P17/14 ,  C12R1/645

摘要： The present invention is comprised of culturing microorganism having ability to produce FKI-1033 substance represented by the formula: in a medium, accumulating FKI-1033 substance in the cultured medium, and isolating FKI-1033 substance from the cultured mass. The thus obtained FKI-1033 substance has ryanodine binding inhibition activity, insecticidal activity and anthelmintic activity, and is expected as useful drugs as agrochemicals, veterinary drugs and medicaments in effectiveness and toxicity.

摘要翻译： 本发明包括培养具有下式表示的FKI-1033物质的能力的微生物：在培养基中积聚FKI-1033物质的培养基中，并从培养物质中分离FKI-1033物质。 由此获得的FKI-1033物质具有兰诺定结合抑制活性，杀虫活性和驱虫活性，并且作为农药，兽药和药物的有效性和毒性被期待为有用的药物。

公开(公告)号：US20090130717A1

公开(公告)日：2009-05-21

申请号：US12084878

申请日：2006-05-16

申请人： Satoshi Omura ,  Hiroshi Tomoda ,  Yong-pil Kim ,  Hideaki Hanaki ,  Atsuko Matsumoto ,  Yoko Takahashi

发明人： Satoshi Omura ,  Hiroshi Tomoda ,  Yong-pil Kim ,  Hideaki Hanaki ,  Atsuko Matsumoto ,  Yoko Takahashi

IPC分类号： C12P19/44 ,  C07H15/10 ,  C12P13/02 ,  C12N1/20 ,  C07C59/62

CPC分类号： C07H11/04 ,  C07C323/59 ,  C12P13/02 ,  C12P19/26 ,  C12P19/44 ,  C12R1/465

摘要： A microorganism represented by a strain K04-0144 belonging to Streptomyces sp. having ability to produce K04-0144 substance is cultured in the medium, and the isolated K04-0144A substance, K04-0144B substance and K04-0144C substance therefrom have strong antibacterial activities against Gram-positive bacteria including methicillin-resistant Streptococcus aureus (MRSA), consequently these are useful as the therapeutic agents for infectious disease caused by MRSA as well as infectious diseases caused by multidrug including β-lactam antibiotics resistant bacteria. Further, similarly, since the novel K04-0144D substance isolated from the cultured liquid has the action for enhancing the effect of β-lactam antibiotics, which are utilized as the antibacterial agents, in combination with them, it is useful as the therapeutic agent for infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA) and multidrug including β-lactam antibiotics resistant bacteria.

摘要翻译： 属于Streptomyces sp。的菌株K04-0144所代表的微生物 在培养基中培养生产K04-0144物质的能力，分离的K04-0144A物质，K04-0144B物质和K04-0144C物质对革兰氏阳性菌（包括耐甲氧西林金黄色葡萄球菌（MRSA））具有很强的抗菌活性， 因此，这些可用作由MRSA引起的感染性疾病的治疗剂以及由多种药物（包括β-内酰胺抗生素抗性细菌）引起的感染性疾病。 此外，类似地，由于从培养液体中分离的新型K04-0144D物质具有增强作为抗菌剂的β-内酰胺抗生素与其组合的作用，因此可用作治疗剂 由耐甲氧西林金黄色葡萄球菌（MRSA）引起的感染性疾病和包括β-内酰胺抗生素抗性细菌在内的多种药物。

公开(公告)号：US20090093646A1

公开(公告)日：2009-04-09

申请号：US11911868

申请日：2006-03-15

申请人： Satoshi Omura ,  Hiroshi Tomoda ,  Rokuro Masuda

发明人： Satoshi Omura ,  Hiroshi Tomoda ,  Rokuro Masuda

IPC分类号： C07D493/22 ,  C12P17/18

CPC分类号： C12P17/06 ,  C07D493/04

摘要： The present invention relates to novel compound of stemphones obtained by culturing microorganism belonging to genus Aspergillus and having ability to produce compound of stemphones selected from the group consisting of stemphone D substance, stemphone E substance, stemphone E1 substance, stemphone E2 substance, stemphone E3 substance and stemphone F substance, accumulating the compound of stemphones in the cultured mass, and isolating the compound of stemphones from the cultured mass. Since the obtained compound has enhancing activity for imipenem and activity for reducing cytotoxicity, it can be expected to be useful as lead compounds for combination remedy for methicillin resistant Staphylococcus aureus (MRSA) infection.

摘要翻译： 本发明涉及通过培养属于曲霉属微生物的微生物获得的具有能够产生选自以下的干细胞的化合物的新型化合物：选自以下的组合：选自以下的组合：干扰素D物质，主体E物质， 和干扰素F物质，将培养物质中的电话的化合物积聚，并从培养的物质中分离出手机的化合物。 由于所得化合物对亚胺培南具有增强的活性和降低细胞毒性的活性，因此可预期作为用于耐甲氧西林金黄色葡萄球菌（MRSA）感染的组合治疗的铅化合物是有用的。

公开(公告)号：US20060287252A1

公开(公告)日：2006-12-21

申请号：US10571263

申请日：2004-02-09

申请人： Satoshi Omura ,  Akio Abe ,  Masato Iwatuki ,  Yoko Takahashi ,  Hiroshi Tomoda

发明人： Satoshi Omura ,  Akio Abe ,  Masato Iwatuki ,  Yoko Takahashi ,  Hiroshi Tomoda

IPC分类号： A61K38/04 ,  C12P21/04 ,  C12P17/00 ,  C07D403/02 ,  C07K5/04

CPC分类号： C12R1/465 ,  C07K5/1024 ,  C12P17/165

摘要： A microorganism belonging to the genus Streptomyces and being capable of producing substance K01-0509-A1 and/or substance K01-0509-A2 is cultured in a medium. Then, the substance K01-0509-A1 and/or the substance K01-0509-A2 having been thus accumulated in the liquid culture medium are collected from the medium. It is expected that the obtained substances are efficacious as drugs which are selectively effective on pathogenic gram-negative bacteria having the type III secretion system.

摘要翻译： 在培养基中培养属于链霉菌属的能够产生物质K01-0509-A1和/或物质K01-0509-A2的微生物。 然后，从介质中收集已经积累在液体培养基中的物质K01-0509-A1和/或物质K01-0509-A2。 预期所获得的物质作为对具有III型分泌系统的病原性革兰氏阴性细菌有选择性的药物是有效的。

公开(公告)号：US20050032883A1

公开(公告)日：2005-02-10

申请号：US10491131

申请日：2001-12-11

申请人： Satoshi Omura ,  Kazuro Shiomi ,  Rokuro Masuma

发明人： Satoshi Omura ,  Kazuro Shiomi ,  Rokuro Masuma

IPC分类号： A61P31/04 ,  A61P33/10 ,  C07D309/38 ,  C12P17/06 ,  A61K31/35

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： 本发明包括培养具有由下式表示的FKI-1083物质的能力的微生物：在培养基中积累FKI-1083物质并从培养物质中分离FKI-1083物质的培养基中。 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：US06790968B1

公开(公告)日：2004-09-14

申请号：US10169551

申请日：2002-10-24

申请人： Satoshi Omura ,  Hiroshi Tomoda ,  Rokuro Masuma ,  Masayoshi Arai

发明人： Satoshi Omura ,  Hiroshi Tomoda ,  Rokuro Masuma ,  Masayoshi Arai

IPC分类号： C07D30936

CPC分类号： C07D309/38 ,  C12P17/06

摘要： A microorganism having ability to produce FKI-0076 substance represented by the following formula [I] is cultured in a medium allowing for the accumulation of FKI-0076 substance in the culture liquid. The FKI-0076 substance from can then be isolated the cultured mass. Since the substance has the ability to enhance azole antifungal agents, it provides an action against various fungal infections such as deep-seated mycosis and other fungal infections in low concentration and within a short term. Consequently, the FKI-0076 is useful for reducing the frequency of appearance of resistant microorganisms. Further, usefulness for overcoming resistance is expected.

摘要翻译： 将能够产生下式[I]表示的FKI-0076物质的微生物培养在允许培养液中积累FKI-0076物质的培养基中。 然后可以将FKI-0076物质分离出培养的物质。 由于该物质具有增强唑类抗真菌剂的能力，因此可提供针对各种真菌感染的作用，例如低浓度和短期内的深层真菌病和其他真菌感染。 因此，FKI-0076可用于降低抗性微生物的出现频率。 此外，期望克服阻力的有用性。

公开(公告)号：US06512099B2

公开(公告)日：2003-01-28

申请号：US10096942

申请日：2002-03-14

申请人： Satoshi Omura ,  Hiroshi Tomoda

发明人： Satoshi Omura ,  Hiroshi Tomoda

IPC分类号： C07G1100

CPC分类号： C07H15/10 ,  C07C69/732 ,  C07H13/06

摘要： Roselipin derivatives which are represented by the following formula: [wherein R1 represents a hydrogen atom, mannose or acetylated mannose, R2 represents a hydrogen atom or a methyl group, and R3 represents a methyl group or a sugar alcohol], excluding a compound in which R1 is mannose, R2 is a hydrogen atom and R3 is arabinitol (roselipin 1A or 1B) and a compound in which R1 is acetylated mannose, R2 is a hydrogen atom and R3 is arabinitol (roselipin 2A or 2B), and which are useful for preventing and treating a disease of a human which is caused by accumulation of triacylglycerol can be obtained.

摘要翻译： 由下式表示的Roselipin衍生物：[其中R1表示氢原子，甘露糖或乙酰化甘露糖，R2表示氢原子或甲基，R3表示甲基或糖醇]，不包括其中 R1是甘露糖，R2是氢原子，R3是阿拉伯糖醇（roselipin 1A或1B）和R1是乙酰化甘露糖，R2是氢原子，R3是阿拉伯糖醇（roselipin 2A或2B）的化合物，它们可用于 可以获得预防和治疗由三酰基甘油积聚引起的人的疾病。

公开(公告)号：US06432682B1

公开(公告)日：2002-08-13

申请号：US09581660

申请日：2000-08-08

申请人： Satoshi Omura ,  Hiroshi Tomoda ,  Rokuro Masuma

发明人： Satoshi Omura ,  Hiroshi Tomoda ,  Rokuro Masuma

IPC分类号： C12P1944

CPC分类号： C07H15/10 ,  C12P7/06 ,  C12P17/06 ,  C12P19/44 ,  C12R1/645 ,  Y02E50/17 ,  Y10S435/822

摘要： A process for producing a substance KF-1040A represented by formula (I), and another substance KF-1040B represented by formula (II), which comprises culturing microorganisms capable of producing the substances KF-1040A and KF-1040B, thus accumulating these KF-1040A and/or KF-1040B in the liquid culture and harvesting the same from the culture. Because of the activities of inhibiting diacyloglycerol transferase and sphingomyelinase, the above substances are useful in preventing and treating arteriosclerosis, obesity, thrombus, inflammation and immune function-related diseases.

摘要翻译： 一种制备由式（I）表示的物质KF-1040A的方法和由式（II）表示的另一物质KF-1040B，其包括培养能产生物质KF-1040A和KF-1040B的微生物，从而积累这些KF -1040A和/或KF-1040B，并从培养物中收获。 由于抑制二甘油转移酶和鞘磷脂酶的活性，上述物质可用于预防和治疗动脉硬化，肥胖症，血栓，炎症和免疫功能相关疾病。