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公开(公告)号：US20100291622A1
公开(公告)日：2010-11-18
申请号：US12681202
申请日：2008-09-12
Applicant: Hiroshi Tomoda , Junji Inokoshi , Rokuro Masuma , Satoshi Omura
Inventor： Hiroshi Tomoda , Junji Inokoshi , Rokuro Masuma , Satoshi Omura
IPC: C12P29/00 , C07C237/26 , C07C49/727 , C12N1/20
CPC classification number: C07C235/82 , C07C49/755 , C07C62/38 , C07C2603/52 , C12P7/24 , C12P29/00
Abstract: The present invention provides compounds which exhibit an inhibitory effect on undecaprenyl diphosphate synthase of microbes and thereby they are expected to be used clinically as pharmaceutical agents for infectious diseases caused by bacteria.The process comprises culturing a microbe belonging to Penicillium and having ability of producing an FKI-3368 substance in or on a nutrient medium to accumulate the FKI-3368 substance in the nutrient medium and collecting the FKI-3368 substance from the culture.
Abstract translation: 本发明提供了对微生物的十碳六烯基二磷酸合成酶具有抑制作用的化合物，因此预期其可以临床用作由细菌引起的感染性疾病的药剂。 该方法包括培养属于青霉属的微生物，并具有在营养培养基中或培养基上产生FKI-3368物质的能力，以在营养培养基中积累FKI-3368物质，并从培养物中收集FKI-3368物质。
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公开(公告)号：US20110105769A1
公开(公告)日：2011-05-05
申请号：US12867435
申请日：2009-02-12
Applicant: Hiroshi Tomoda , Ryuji Uchida , Rokuro Masuma , Satoshi Omura
Inventor： Hiroshi Tomoda , Ryuji Uchida , Rokuro Masuma , Satoshi Omura
IPC: C07D407/10 , C12P17/06 , C12N1/14
CPC classification number: A61K36/06 , C07D311/92 , C12P17/162 , C12R1/80
Abstract: This invention relates to substance FKI-3864 represented by the following formula [I] having an inhibitory activity on the synthesis of triacylglycerols and a method for preparing the same. The substance FKI-3864 can be prepared by a method comprising culturing a microorganism which belongs to the genus Penicillium and is capable of producing the substance FKI-3864, and particularly Penicillium pinophilum FKI-3864 (FERM BP-11093) so as to accumulate the substance FKI-3864 in the culture and collecting the substance FKI-3864 from the culture. The substance has an inhibitory activity on the synthesis of intracellular triacylglycerols and is useful for prevention or treatment of obesity.
Abstract translation: 本发明涉及具有对三酰基甘油合成抑制活性的下式[I]表示的物质FKI-3864及其制备方法。 物质FKI-3864可以通过包括培养属于青霉属的微生物并能够产生物质FKI-3864，特别是嗜热青霉FKI-3864（FERM BP-11093）的方法来制备，以便积累 培养物质FKI-3864，从培养物中收集物质FKI-3864。 该物质对细胞内三酰基甘油的合成具有抑制活性，可用于预防或治疗肥胖症。
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公开(公告)号：US20070032545A1
公开(公告)日：2007-02-08
申请号：US10570991
申请日：2004-03-24
Applicant: Satoshi Omura , Hiroshi Tomoda , Rokuro Masuma
Inventor： Satoshi Omura , Hiroshi Tomoda , Rokuro Masuma
IPC: A61K31/366 , C12P17/08 , C12N1/16 , C07D309/38
CPC classification number: C07D309/38 , C12P17/06
Abstract: A microorganism belonging to filamentous fungi, capable of producing antibiotic FKI-1778A and/or FKI-1778B and/or FKI-1778C and/or FKI-1778D is cultured in a culture medium to thereby accumulate the antibiotic FKI-1778A and/or FKI-1778B and/or FKI-1778C and/or FKI-1778D in the culture mixture. The antibiotic FKI-1778A and/or FKI-1778B and/or FKI-1778C and/or FKI-1778D is collected from the culture mixture. The thus obtained substance is promising as drugs, veterinary medicines or agrichemicals having a growth inhibiting activity to microorganisms, nematodes and arthropods or as drugs exhibiting a growth inhibiting activity to carcinoma cells.
Abstract translation: 在培养基中培养属于丝状真菌的能够产生抗生素FKI-1778A和/或FKI-1778B和/或FKI-1778C和/或FKI-1778D的微生物，从而累积抗生素FKI-1778A和/或FKI -1778B和/或FKI-1778C和/或FKI-1778D。 从培养混合物中收集抗生素FKI-1778A和/或FKI-1778B和/或FKI-1778C和/或FKI-1778D。 由此获得的物质有希望作为对微生物，线虫和节肢动物具有生长抑制活性的药物，兽药或农药或作为对癌细胞具有生长抑制活性的药物。
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4.发明授权
公开(公告)号：US5807721A
公开(公告)日：1998-09-15
申请号：US567066
申请日：1995-12-04
Applicant: Satoshi Omura , Hiroshi Tomoda , Rokuro Masuma
Inventor： Satoshi Omura , Hiroshi Tomoda , Rokuro Masuma
IPC: A61K31/44 , A61P3/06 , C07D321/12 , C07D493/04 , C12N9/99 , C12P17/18 , C12R1/66 , C12N1/14
CPC classification number: C07D493/04 , C12P17/181 , C12R1/66 , Y10S435/913
Abstract: A FO-1289 substance of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are hydrogen or acyl. A process for the production thereof comprises culturing the novel microorganism Aspergillus sp. FO-1289 FERM BP-4242 in a nutrient medium, accumulating the FO-1289 substance thus produced in the medium, and isolating the FO-1289 substance therefrom. Particular species of the FO-1289 substance comprise FO-1289A, in which R.sub.1, R.sub.2 and R.sub.3 are acetyl and R.sub.4 is hydrogen; FO-1289B, wherein R.sub.1 is propionyl, R.sub.2 and R.sub.3 are acetyl and R.sub.4 is hydrogen; FO-1289C, wherein R.sub.1 and R.sub.3 are acetyl, R.sub.2 is propionyl and R.sub.4 is hydrogen; and FO-1289D, wherein R.sub.1 and R.sub.2 are acetyl, R.sub.3 is propionyl and R.sub.4 is hydrogen.
Abstract translation: 其中R1，R2，R3和R4是氢或酰基的式“IMAGE”的FO-1289物质。 其生产方法包括培养微生物曲霉菌 FO-1289 FERM BP-4242在营养培养基中积聚由此在培养基中产生的FO-1289物质，并从其中分离FO-1289物质。 FO-1289物质的特定物种包括FO-1289A，其中R1，R2和R3是乙酰基，R4是氢; FO-1289B，其中R1是丙酰基，R2和R3是乙酰基，R4是氢; FO-1289C，其中R1和R3是乙酰基，R2是丙酰基，R4是氢; 和FO-1289D，其中R1和R2是乙酰基，R3是丙酰基，R4是氢。
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公开(公告)号：US08378125B2
公开(公告)日：2013-02-19
申请号：US12867435
申请日：2009-02-12
Applicant: Hiroshi Tomoda , Ryuji Uchida , Rokuro Masuma , Satoshi Omura
Inventor： Hiroshi Tomoda , Ryuji Uchida , Rokuro Masuma , Satoshi Omura
IPC: C07D311/78
CPC classification number: A61K36/06 , C07D311/92 , C12P17/162 , C12R1/80
Abstract: This invention relates to substance FKI-3864 represented by the following formula [I] having an inhibitory activity on the synthesis of triacylglycerols and a method for preparing the same. The substance FKI-3864 can be prepared by a method comprising culturing a microorganism which belongs to the genus Penicillium and is capable of producing the substance FKI-3864, and particularly Penicillium pinophilum FKI-3864 (FERM BP-11093) so as to accumulate the substance FKI-3864 in the culture and collecting the substance FKI-3864 from the culture. The substance has an inhibitory activity on the synthesis of intracellular triacylglycerols and is useful for prevention or treatment of obesity.
Abstract translation: 本发明涉及具有对三酰基甘油合成抑制活性的下式[I]表示的物质FKI-3864及其制备方法。 物质FKI-3864可以通过包括培养属于青霉属的微生物并能够产生物质FKI-3864，特别是嗜热青霉FKI-3864（FERM BP-11093）的方法来制备，以便积累 培养物质FKI-3864，从培养物中收集物质FKI-3864。 该物质对细胞内三酰基甘油的合成具有抑制活性，可用于预防或治疗肥胖症。
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Patent Agency Ranking
公开(公告)号：US07514455B2
公开(公告)日：2009-04-07
申请号：US10489964
申请日：2002-06-10
Applicant: Satoshi Omura , Kazuro Shiomi , Hiroshi Tomoda , Rokuro Masuma , Kiyoshi Kita
Inventor： Satoshi Omura , Kazuro Shiomi , Hiroshi Tomoda , Rokuro Masuma , Kiyoshi Kita
IPC: C07D211/84 , A61K31/4415
CPC classification number: A61K31/44 , C07D213/69 , C12P17/12 , C12R1/80
Abstract: An electron transport system complex II inhibitor comprising 2-pyridinol derivative represented by the general formula [I] wherein R is alkyl or alkenyl optionally having substituent containing halogen, or its tautomer 2-pyridone derivative represented by the general formula [II] wherein R is alkyl or alkenyl optionally having substituent containing halogen, or salt thereof as an active ingredient. The compound inhibits the complex II strongly with nM order activity. Consequently, 2-pyridinol derivative or its tautomer, 2-pyridone derivative, are useful as the complex II inhibitor.
Abstract translation: 一种电子传递系统络合物II抑制剂，其包含由通式[I]表示的2-吡啶醇衍生物，其中R是任选具有含卤素取代基的烷基或烯基，或其通式[II]表示的互变异构体2-吡啶酮衍生物，其中R为 任选具有含卤素取代基的烷基或链烯基或其盐作为活性成分。 该化合物以nM顺序活性强烈地抑制复合体II。 因此，2-吡啶酚衍生物或其互变异构体2-吡啶酮衍生物可用作复合物II抑制剂。
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公开(公告)号：US07132447B2
公开(公告)日：2006-11-07
申请号：US10491131
申请日：2001-12-11
Applicant: Satoshi Omura , Kazuro Shiomi , Rokuro Masuma
Inventor： Satoshi Omura , Kazuro Shiomi , Rokuro Masuma
IPC: A61K31/35
CPC classification number: C12R1/645 , C07D309/38 , C12P17/06
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US06486197B1
公开(公告)日：2002-11-26
申请号：US09509770
申请日：2000-08-03
Applicant: Satoshi Omura , Kazuro Shiomi , Rokuro Masuma , Yuzuru Iwai
Inventor： Satoshi Omura , Kazuro Shiomi , Rokuro Masuma , Yuzuru Iwai
IPC: A61K3135
CPC classification number: C07D493/04 , C12P17/18 , C12P17/181
Abstract: The present invention is to obtain novel FT-0554 substance which is useful for treatment of helminthiasis. The present invention comprising the steps of culturing the microorganism belonging to fungi having producing activity of FT-0554 substance represented by the following formula [I] subjected ho accumulation of FT-0554 substance in the cultured medium, and isolating FT-0554 substance from the said cultured mass. The medicament useful for treatment of parasitic infection, specifically helminthiasis can be obtained.
Abstract translation: 本发明是获得可用于治疗蠕虫病的新型FT-0554物质。 本发明包括以下步骤：培养具有由下式[I]表示的具有FT-0554物质的具有生物活性的真菌的微生物，使FT-0554物质在培养基中积聚，并将FT-0554物质从 说培养的群众。 可以获得用于治疗寄生虫感染，特别是蠕虫病的药物。
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公开(公告)号：US20110021848A1
公开(公告)日：2011-01-27
申请号：US12933162
申请日：2009-03-12
Applicant: Satoshi Omura , Kazuro Shiomi , Rokuro Masuma , Hideaki Ui , Takayuki Nagai , Haruki Yamada
Inventor： Satoshi Omura , Kazuro Shiomi , Rokuro Masuma , Hideaki Ui , Takayuki Nagai , Haruki Yamada
CPC classification number: C12R1/885 , A61K31/045 , C07C35/44 , C07C2603/40 , C12P7/02
Abstract: The present invention includes wickerol and a method for producing the wickerol. In the method for producing the wickerol, Trichoderma atroviride strain FKI-3737 (FERM ABP-11099 corresponding to FERM BP-11099) belonging to filamentous fungi is cultured in a medium, and the wickerol is accumulated in a culture, and then the produced wickerol is isolated and purified from the culture. A substance having inhibitory activity against influenza virus replication and containing the wickerol as an active ingredient, and an anti-influenza drug containing the wickerol as an active ingredient are obtained.
Abstract translation: 本发明包括柳氮磺吡啶和柳氮磺胺的制造方法。 在生产柳叶刀的方法中，将属于丝状真菌的木霉菌菌株FKI-3737（对应于FERM BP-11099的FERM ABP-11099）在培养基中培养，并将wickerol积聚在培养物中，然后生产的wickerol 从培养物中分离纯化。 获得具有针对流感病毒复制的抑制活性且含有作为活性成分的柳叶刀的物质，以及含有柳叶刀作为有效成分的抗流感药物。
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公开(公告)号：US07541336B2
公开(公告)日：2009-06-02
申请号：US10532662
申请日：2002-11-12
Applicant: Satoshi Omura , Kazuro Shiomi , Rokuro Masuma
Inventor： Satoshi Omura , Kazuro Shiomi , Rokuro Masuma
Abstract: 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.
Abstract translation: 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。
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