公开(公告)号：US06608185B1

公开(公告)日：2003-08-19

申请号：US09937335

申请日：2002-01-14

申请人： Satoshi Omura ,  Hiroshi Tomoda ,  Rokuro Masuma

发明人： Satoshi Omura ,  Hiroshi Tomoda ,  Rokuro Masuma

IPC分类号： C07H1500

CPC分类号： C07H15/10 ,  C12P19/44 ,  C12R1/645 ,  Y10S435/822

摘要： A microorganism which belongs to the genus Gliocladium and has the ability to produce stereoisomers KF-1040T4A and KF-1040T4B which are compounds represented by the following formula [I], and stereoisomers KF-1040T5A and KF-1040T5B which are compounds represented by the following formula [II], is cultivated in a culture medium to accumulate KF-1040T4A and/or KF-1040T4B and/or KF-1040T5A and/or KF-1040T5B in the culture medium, and the substance KF-1040T4A and/or KF-1040T4B and/or KF-1040T5A and/or KF-1040T5B are harvested from the culture medium. The obtained substances are useful for the prevention and treatment of the diseases relating to arteriosclerosis, obesity, thrombosis, inflammations and immunofunctional disorders.

摘要翻译： 属于Gliocladium属并且具有作为下述式[I]表示的化合物的立体异构体KF-1040T4A和KF-1040T4B以及由以下化合物表示的化合物的立体异构体KF-1040T5A和KF-1040T5B的微生物 将式[II]在培养基中培养以在培养基中积累KF-1040T4A和/或KF-1040T4B和/或KF-1040T5A和/或KF-1040T5B，并且物质KF-1040T4A和/或KF- 从培养基中收获1040T4B和/或KF-1040T5A和/或KF-1040T5B。 所获得的物质可用于预防和治疗与动脉硬化，肥胖症，血栓形成，炎症和免疫功能障碍有关的疾病。

公开(公告)号：US06586200B2

公开(公告)日：2003-07-01

申请号：US09937832

申请日：2002-05-21

申请人： Satoshi Omura ,  Akio Abe

发明人： Satoshi Omura ,  Akio Abe

IPC分类号： C12Q104

CPC分类号： C12Q1/18 ,  C12Q1/025 ,  G01N33/5014 ,  G01N33/721 ,  G01N2333/21 ,  G01N2333/235 ,  G01N2333/245 ,  G01N2333/25 ,  G01N2333/255

摘要： The present invention relates to a method for detecting substances specifically inhibiting a type III secretion mechanism and functions of the type III secretory proteins, within short time and large amounts thereof, without depending upon animal infectious experiments. Namely it relates to the method for detection of a type III secretory mechanism inhibitor comprising mixing a bacterium having the type III secretory mechanism and an erythrocyte suspension, adding the type III secretory mechanism inhibitor thereto, and detecting changes in the thus formed hemolytic activity. The method for detecting substances can be treated large amount of samples within short time by exhibiting the substances inhibiting the type III secretion mechanism or the functions of the type III secretory proteins as numerical index of the hemolytic activity of erythrocytes. Consequently, the present invention is useful for development of drugs.

公开(公告)号：US6077943A

公开(公告)日：2000-06-20

申请号：US143365

申请日：1998-08-28

申请人： Satoshi Omura ,  Masayasu Kato ,  Miichiro Arita

发明人： Satoshi Omura ,  Masayasu Kato ,  Miichiro Arita

IPC分类号： C07H17/08 ,  A01N43/04 ,  C07H1/06

CPC分类号： C07H17/08

摘要： A method of producing an N-demethyl-N-isopropyl-8,9-anhydroerythromycin A-6,9-hemiacetal or a salt thereof, characterized in that an N-demethylerythromycin A or a salt thereof is reacted with an isopropylating agent and subsequently treated under acidic conditions, and a method of producing a substantially pure crystal of an 8,9-anhydroerythromycin A-6,9-hemiacetal derivative represented formula (VI): ##STR1## wherein R.sup.1 and R.sup.2, whether identical or not, represent an alkyl having 1 to 6 carbon atoms, an alkenyl having 2 to 6 carbon atoms or an alkynyl having 2 to 6 carbon atoms; R.sup.3 represents hydrogen or a hydroxyl group; one of R.sup.4 and R.sup.5 represents hydrogen and the other represents a hydroxyl group, or R.sup.4 and R.sup.5 bind together to represent O.dbd.; R.sup.6 represents hydrogen or a hydroxyl group that may be substituted for; R.sup.7 represents hydrogen or a hydroxyl group; or a salt thereof, characterized in that a crude crystal of said 8,9-anhydroerythromycin A-6,9-hemiacetal derivative or a salt thereof is recrystallized as a solvation product from hydrated isopropanol.

摘要翻译： 一种N-去甲基-N-异丙基-8,9-去水红霉素A-6,9-半缩醛或其盐的制备方法，其特征在于N-去甲基红霉素A或其盐与异丙基化试剂反应，随后 在酸性条件下处理的方法，以及制备基本上纯的由9,9-脱水红霉素A-6,9-半缩醛衍生物衍生的结晶的方法，其中R 1和R 2相同或不相同，表示具有1 至6个碳原子，具有2至6个碳原子的烯基或具有2至6个碳原子的炔基; R3表示氢或羟基; R4和R5之一表示氢，另一个表示羟基，或R4和R5结合在一起代表O =; R6表示氢或可以被取代的羟基; R 7表示氢或羟基; 或其盐，其特征在于所述8,9-脱水红霉素A-6,9-半缩醛衍生物或其盐的粗结晶作为溶剂合物从水合异丙醇中重结晶。

公开(公告)号：US4948782A

公开(公告)日：1990-08-14

申请号：US158163

申请日：1988-02-18

申请人： Satoshi Omura ,  Zen Itoh

发明人： Satoshi Omura ,  Zen Itoh

IPC分类号： C07H17/08

CPC分类号： A61K31/70 ,  C07H17/08

摘要： A growth promoting composition for animals containing an erythromycin derivative wherein a dimethylamino radical of the 3'-position is converted into a primary amino radical, a secondary amino radical, a tertiary amino radical other than the dimethyl amino radical, or a quaternary ammonio radical.This composition does not exhibit the antimicrobial activity at all or show the extremely decreased antimicrobial activity, and has the excellent effect to improve the feed efficiency of domestic animals.

摘要翻译： 含有红霉素衍生物的动物的生长促进组合物，其中3'-位的二甲基氨基被转化为伯氨基，仲氨基，除二甲基氨基以外的叔氨基或季铵基。 该组合物完全不显示抗微生物活性或显示极度降低的抗微生物活性，并且对提高家畜的饲料效率具有优异的效果。

公开(公告)号：US4609645A

公开(公告)日：1986-09-02

申请号：US593461

申请日：1984-03-26

申请人： Satoshi Omura

发明人： Satoshi Omura

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61K35/74 ,  A61P31/04 ,  C07G11/00 ,  C07H17/08 ,  C12P1/06 ,  C12P19/62 ,  C12R1/465 ,  A61K31/71

CPC分类号： C07H17/08 ,  C12P19/62 ,  C12R1/465

摘要： Macrolides PTL-448 A and B, which can be prepared by aerobic cultivation of Streptomyces ambofaciens ATCC 15154 in the presence of a macrolide intermediate selected from protylonlide, 5-O-mycaminosylprotylonolide, 20-hydroxy-5-O-mycaminosylprotylonolide and 20-oxo-5-O-mycaminosylprotylonodide, and macrolides PTL-448 C and D, which can be prepared by acidic hydrolysis of PTL-448 A and B are useful antibiotics.

摘要翻译： 大环内酯类化合物PTL-448A和B，其可以通过需氧培养链霉菌（Streptomyces ambofaciens）ATCC 15154在大环内酯中间体制备，所述大环内酯类中间体选自阮内酰胺，5-O-碳霉糖基pro萜内酯，20-羟基-5-O- -5-O-碳霉糖基太子糖苷和大环内酯类PTL-448C和D，其可以通过PTL-448A和B的酸性水解制备是有用的抗生素。

公开(公告)号：US4493845A

公开(公告)日：1985-01-15

申请号：US434818

申请日：1982-10-18

申请人： Satoshi Omura ,  Yoshitake Tanaka ,  Yuzuru Iwai ,  Yoko Takahashi ,  Akira Nakagawa

发明人： Satoshi Omura ,  Yoshitake Tanaka ,  Yuzuru Iwai ,  Yoko Takahashi ,  Akira Nakagawa

IPC分类号： C07H17/08 ,  A61K31/325 ,  A61K31/35 ,  A61K35/74 ,  A61P31/04 ,  C07G11/00 ,  C12P1/06 ,  C12P17/18 ,  C07D491/08

CPC分类号： C12R1/465 ,  C12P1/06

摘要： Antibiotic AM-3603 which is also designated as irumamycin is represented by the following formula: ##STR1## This substance is active upon certain Gram-positive bacteria, phytopathogenic fungi and dermatophytes, and is of interest in treating various diseases of humans and animals caused by infectious bacteria and fungi and also useful for agricultural purposes. Antibiotic AM-3603 may be prepared by fermentation, in which a microorganism capable of producing AM-3603 is cultured in a medium to accumulate AM-3603 in the cultured broths, from which AM-3603 is recovered. A preferred strain is Streptomyces sp. AM-3603 (FERM-P 5619; NRRL 12518).

摘要翻译： 也被称为伊马利霉素的抗生素AM-3603由下式表示：该物质对某些革兰氏阳性菌，植物病原真菌和皮肤癣菌有活性，并且对于治疗人类和动物引起的各种疾病感兴趣 感染性细菌和真菌，也可用于农业目的。 抗生素AM-3603可以通过发酵制备，其中能够产生AM-3603的微生物在培养基中培养以在收集AM-3603的培养肉汤中积累AM-3603。 优选的菌株是链霉菌属（Streptomyces sp。）。 AM-3603（FERM-P 5619; NRRL 12518）。

公开(公告)号：US4296040A

公开(公告)日：1981-10-20

申请号：US97001

申请日：1970-11-23

申请人： Satoshi Omura ,  Haruo Tanaka ,  Itaru Takahashi ,  Shinzo Ishii ,  Kazuyuki Mineura ,  Kunikatsu Shirahata ,  Masaji Kasai

发明人： Satoshi Omura ,  Haruo Tanaka ,  Itaru Takahashi ,  Shinzo Ishii ,  Kazuyuki Mineura ,  Kunikatsu Shirahata ,  Masaji Kasai

IPC分类号： A61K31/35 ,  A61P31/04 ,  C07D493/08 ,  C12P17/18 ,  C12R1/465 ,  C07D311/78

CPC分类号： C07D493/08 ,  C12P17/181 ,  Y10S435/886

摘要： The present invention teaches a new antibiotic nanaomycin E represented by the formula: ##STR1## Nanaomycin E is active against Gram-positive bacteria, Trichophyton and Mycoplasma and may be used as antibacterial and therapeutic agents for humans and animals. Nanaomycin E is also a useful starting maerial for the preparation of nanaomycin A which latter nanaomycin has the highest activity among the various nanaomycin-type compounds. Nanaomycin E is produced by fermentation of a microorganism belonging to the genus Streptomyces and capable of producing nanaomycin E, especially Streptomyces rosa variant notoensis (FERM-P 2209; ATCC 31135) and recovering the same from the fermented liquor.

摘要翻译： 本发明教导了由下式表示的新型抗生素纳那霉素E：Nanaomycin E对革兰氏阳性菌，毛癣菌和支原体具有活性，可用作人和动物的抗菌剂和治疗剂。 纳豆霉素E也是制备纳诺霉素A的有用起始物，后者纳那霉素在各种纳诺霉素型化合物中活性最高。 纳豆霉素E是通过发酵属于链霉菌属的微生物产生的，并且能够产生纳诺霉素E，特别是罗氏变形链霉菌（FERM-P 2209; ATCC 31135），并从发酵液中回收。

公开(公告)号：US4218478A

公开(公告)日：1980-08-19

申请号：US1246

申请日：1979-01-05

申请人： Satoshi Omura ,  Ruiko Oiwa

发明人： Satoshi Omura ,  Ruiko Oiwa

IPC分类号： A61K31/165 ,  A61K31/16

CPC分类号： A61K31/165

摘要： Trichostatin (I) is disclosed to be useful as an antiprotozoal agent for the treatment of diseases in man and animals. Also disclosed are pharmaceutical compositions comprising trichostatin for treating protozoal infections. Trichostatin has the structure: ##STR1##

摘要翻译： 公开了曲古抑菌素（I）可用作治疗人和动物疾病的抗原虫药。 还公开了包含用于治疗原生动物感染的曲古抑菌素的药物组合物。 曲古抑菌素具有以下结构： I

公开(公告)号：US3995028A

公开(公告)日：1976-11-30

申请号：US606687

申请日：1975-08-21

申请人： Satoshi Omura ,  Iwao Umezawa ,  Keiki Satoh ,  Juichi Awaya ,  Kanki Komiyama ,  Ruiko Oiwa

发明人： Satoshi Omura ,  Iwao Umezawa ,  Keiki Satoh ,  Juichi Awaya ,  Kanki Komiyama ,  Ruiko Oiwa

IPC分类号： C07G11/00 ,  A61K35/74

CPC分类号： A61K36/06 ,  C07G11/00 ,  Y10S435/892

摘要： The present invention relates to a new antibiotic designated as OS-3256-B. OS-3256-B exhibits excellent inhibitory activities against animal tumors such as leukemia L-1210, Sarcoma-180 and Hela cells and gram-positive bacteria and is classified into the diazocompounds group. However, chromatographic analysis, Rf value and other experimental data reveal that OS-3256-B is a new compound of the type of azaamino acid derivatives. The present invention also provides a process for producing OS-3256-B by fermentation, in which OS-3256-B is produced by culturing a microorganism belonging to Streptomyces candidus var. azaticus in a culture medium conventionally used for culturing Streptomyces strain microorganisms.

摘要翻译： 本发明涉及一种称为OS-3256-B的新型抗生素。 OS-3256-B对动物肿瘤例如白血病L-1210，肉瘤180和Hela细胞和革兰氏阳性细菌具有优异的抑制活性，并被分类为重氮化合物组。 然而，色谱分析，Rf值等实验数据表明，OS-3256-B是一种新型的氮杂氨基酸衍生物化合物。 本发明还提供了通过发酵生产OS-3256-B的方法，其中OS-3256-B是通过培养属于Streptomyces candidus var。 通常用于培养链霉菌菌株微生物的培养基中的azaticus。

公开(公告)号：US3956487A

公开(公告)日：1976-05-11

申请号：US453041

申请日：1974-03-20

申请人： Toju Hata ,  Satoshi Omura ,  Michiko Katagiri ,  Juichi Awaya ,  Shimpei Kuyama ,  Shizuo Higashikawa ,  Kazuomi Yasui ,  Haruko Terada

发明人： Toju Hata ,  Satoshi Omura ,  Michiko Katagiri ,  Juichi Awaya ,  Shimpei Kuyama ,  Shizuo Higashikawa ,  Kazuomi Yasui ,  Haruko Terada

IPC分类号： C07H13/04 ,  A01N9/00

CPC分类号： C07H13/04

摘要： The antifungal antibiotic substance "F-1028" having the following formula, ##EQU1## or an acid salt thereof, a process for the production of the same by fermentation, and a fungicidal composition useful for agricultural and horticultural use.

摘要翻译： 具有下式的抗真菌抗生素物质“F-1028”，HCOH || HCNH 2 || HO 2 || CH 3 CHCONHCH ||| NH 2 CH 2或其酸式盐，通过发酵生产该方法 用于农业和园艺用途的杀真菌组合物。