公开(公告)号：US20100291622A1

公开(公告)日：2010-11-18

申请号：US12681202

申请日：2008-09-12

申请人： Hiroshi Tomoda ,  Junji Inokoshi ,  Rokuro Masuma ,  Satoshi Omura

发明人： Hiroshi Tomoda ,  Junji Inokoshi ,  Rokuro Masuma ,  Satoshi Omura

IPC分类号： C12P29/00 ,  C07C237/26 ,  C07C49/727 ,  C12N1/20

CPC分类号： C07C235/82 ,  C07C49/755 ,  C07C62/38 ,  C07C2603/52 ,  C12P7/24 ,  C12P29/00

摘要： 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.

摘要翻译： 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。

公开(公告)号：US20110105769A1

公开(公告)日：2011-05-05

申请号：US12867435

申请日：2009-02-12

申请人： Hiroshi Tomoda ,  Ryuji Uchida ,  Rokuro Masuma ,  Satoshi Omura

发明人： Hiroshi Tomoda ,  Ryuji Uchida ,  Rokuro Masuma ,  Satoshi Omura

IPC分类号： C07D407/10 ,  C12P17/06 ,  C12N1/14

CPC分类号： A61K36/06 ,  C07D311/92 ,  C12P17/162 ,  C12R1/80

摘要： 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.

摘要翻译： 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。

公开(公告)号：US20070032545A1

公开(公告)日：2007-02-08

申请号：US10570991

申请日：2004-03-24

申请人： Satoshi Omura ,  Hiroshi Tomoda ,  Rokuro Masuma

发明人： Satoshi Omura ,  Hiroshi Tomoda ,  Rokuro Masuma

IPC分类号： A61K31/366 ,  C12P17/08 ,  C12N1/16 ,  C07D309/38

CPC分类号： C07D309/38 ,  C12P17/06

摘要： 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.

摘要翻译： 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。

公开(公告)号：US5807721A

公开(公告)日：1998-09-15

申请号：US567066

申请日：1995-12-04

申请人： Satoshi Omura ,  Hiroshi Tomoda ,  Rokuro Masuma

发明人： Satoshi Omura ,  Hiroshi Tomoda ,  Rokuro Masuma

IPC分类号： A61K31/44 ,  A61P3/06 ,  C07D321/12 ,  C07D493/04 ,  C12N9/99 ,  C12P17/18 ,  C12R1/66 ,  C12N1/14

CPC分类号： C07D493/04 ,  C12P17/181 ,  C12R1/66 ,  Y10S435/913

摘要： 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.

摘要翻译： 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。

公开(公告)号：US08378125B2

公开(公告)日：2013-02-19

申请号：US12867435

申请日：2009-02-12

申请人： Hiroshi Tomoda ,  Ryuji Uchida ,  Rokuro Masuma ,  Satoshi Omura

发明人： Hiroshi Tomoda ,  Ryuji Uchida ,  Rokuro Masuma ,  Satoshi Omura

IPC分类号： C07D311/78

CPC分类号： A61K36/06 ,  C07D311/92 ,  C12P17/162 ,  C12R1/80

摘要： 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.

摘要翻译： 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。

公开(公告)号：US07514455B2

公开(公告)日：2009-04-07

申请号：US10489964

申请日：2002-06-10

申请人： Satoshi Omura ,  Kazuro Shiomi ,  Hiroshi Tomoda ,  Rokuro Masuma ,  Kiyoshi Kita

发明人： Satoshi Omura ,  Kazuro Shiomi ,  Hiroshi Tomoda ,  Rokuro Masuma ,  Kiyoshi Kita

IPC分类号： C07D211/84 ,  A61K31/4415

CPC分类号： A61K31/44 ,  C07D213/69 ,  C12P17/12 ,  C12R1/80

摘要： 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.

摘要翻译： 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。

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：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。

公开(公告)号：US07794991B2

公开(公告)日：2010-09-14

申请号：US11795683

申请日：2005-10-03

申请人： Satoshi Omura ,  Hiroshi Tomoda ,  Rokuro Masuma

发明人： Satoshi Omura ,  Hiroshi Tomoda ,  Rokuro Masuma

IPC分类号： C12P17/06 ,  C07D311/94

CPC分类号： C12P17/181 ,  C07D493/04 ,  C12R1/66

摘要： The present invention relates to novel stemphones having enhancing effect of β-lactam antibiotic used as an antibacterial agent, and a process for production thereof. The process is comprised of culturing microorganism belonging to genus Aspergillus and having ability to produce stemphones, the microorganism of which is Aspergillus sp. FKI-2136 NITE BP-83, accumulating the stemphones in the cultured mass, and isolating the stemphones from the cultured mass. Since the obtained stemphones have an action enhancing activity of β-lactam antibiotic used as an antibacterial agent by combining with β-lactam antibiotic, the stemphones are expected to be useful as the therapeutic agent for MRSA infection and infectious diseases caused by multi-drug resistant microorganisms including β-lactam antibiotic resistance.

摘要翻译： 本发明涉及用作抗菌剂的β-内酰胺抗生素具有增强作用的新颖的话筒及其生产方法。 该方法包括培养属于曲霉菌属的微生物，并且具有产生茎杆菌的能力，其微生物是曲霉属（Aspergillus sp。）。 FKI-2136 NITE BP-83，将培养物质中的茎干积累起来，并从培养物质中分离茎干。 由于所获得的手机具有通过与β-内酰胺抗生素结合用作抗菌剂的β-内酰胺抗生素的作用增强活性，因此预期该手段可用作MRSA感染和多因素引起的感染性疾病的治疗剂， 耐药微生物包括β-内酰胺抗生素抗性。

公开(公告)号：US20080160587A1

公开(公告)日：2008-07-03

申请号：US11795683

申请日：2005-10-03

申请人： Satoshi Omura ,  Hiroshi Tomoda ,  Rokuro Masuma

发明人： Satoshi Omura ,  Hiroshi Tomoda ,  Rokuro Masuma

IPC分类号： C12P17/06 ,  C07D311/02 ,  C12N1/14

CPC分类号： C12P17/181 ,  C07D493/04 ,  C12R1/66

摘要： The present invention relates to novel stemphones having enhancing effect of β-lactam antibiotic used as an antibacterial agent, and a process for production thereof. The process is comprised of culturing microorganism belonging to genus Aspergillus and having ability to produce stemphones, the microorganism of which is Aspergillus sp. FKI-2136 NITE BP-83, accumulating the stemphones in the cultured mass, and isolating the stemphones from the cultured mass. Since the obtained stemphones have an action enhancing activity of β-lactam antibiotic used as an antibacterial agent by combining with β-lactam antibiotic, the stemphones are expected to be useful as the therapeutic agent for MRSA infection and infectious diseases caused by multi-drug resistant microorganisms including β-lactam antibiotic resistance.

摘要翻译： 本发明涉及具有增强β-内酰胺抗生素作为抗菌剂作用的新颖的手柄及其生产方法。 该方法包括培养属于曲霉菌属的微生物，并且具有产生茎杆菌的能力，其微生物是曲霉属（Aspergillus sp。）。 FKI-2136 NITE BP-83，将培养物质中的茎秆积累起来，并从培养物质中分离茎秆。 由于所获得的话筒具有通过与β-内酰胺抗生素结合用作抗菌剂的β-内酰胺抗生素的作用增强活性，因此预期该手段可用作MRSA感染和由多重耐药性引起的感染性疾病的治疗剂 微生物包括β-内酰胺抗生素抗性。