Substance FKI-0076 and process for producing the same
    31.
    发明授权
    Substance FKI-0076 and process for producing the same 失效
    物质FKI-0076及其制造方法

    公开(公告)号:US06790968B1

    公开(公告)日:2004-09-14

    申请号:US10169551

    申请日:2002-10-24

    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。

    Roselipin derivative
    32.
    发明授权
    Roselipin derivative 失效
    罗塞平衍生物

    公开(公告)号:US06512099B2

    公开(公告)日:2003-01-28

    申请号:US10096942

    申请日:2002-03-14

    IPC分类号: C07G1100

    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。

    Substances KF-1040 and process for producing of the same
    33.
    发明授权
    Substances KF-1040 and process for producing of the same 失效
    物质KF-1040及其制造方法

    公开(公告)号:US06432682B1

    公开(公告)日:2002-08-13

    申请号:US09581660

    申请日:2000-08-08

    IPC分类号: C12P1944

    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。

    Pyripyropene derivative having ACAT2 inhibiting activity and stable to metabolizing enzymes
    34.
    发明授权
    Pyripyropene derivative having ACAT2 inhibiting activity and stable to metabolizing enzymes 有权
    具有ACAT2抑制活性并且对代谢酶稳定的吡哆醛衍生物

    公开(公告)号:US09187492B2

    公开(公告)日:2015-11-17

    申请号:US13638332

    申请日:2011-03-25

    摘要: A compound effective in prevention and treatment of arteriosclerosis with a mechanism different from that of statin drugs has the following formula or a pharmaceutically acceptable salt, solvate, or hydrate thereof: wherein R1 is an aliphatic, alicyclic, or aromatic acyloxy group, or a group of the formula —O—CH(R7)—R8 where R7 is a lower alkoxy group and R8 is an aryl group, and R2 is carboxyl, a lower alkoxycarbonyl group, or an arylmethylcarbamoyl group, or a —CH2-acyloxy group and R3 is an aliphatic, alicyclic or aromatic acyloxy group, provided that at least one of R4 and R3 is a group other than acetoxy, or R2 and R3 taken together form a group of the formula —O—CH(R5)—O— where R5 is an aryl group.

    摘要翻译: 具有与他汀类药物不同的机制预防和治疗动脉硬化的化合物具有下式或其药学上可接受的盐,溶剂合物或水合物:其中R1是脂族,脂环族或芳族酰氧基或基团 的式-O-CH(R7)-R8,其中R7是低级烷氧基,R8是芳基,R2是羧基,低级烷氧基羰基或芳基甲基氨基甲酰基,或-CH2-酰氧基和R3 是脂族,脂环族或芳香族酰氧基,条件是R 4和R 3中的至少一个是除乙酰氧基以外的基团,或者R 2和R 3一起形成式-O-CH(R 5)-O-基团,其中R 5 是芳基。

    Pyripyropene Derivatives Having An ACAT2-Inhibiting Activity
    35.
    发明申请
    Pyripyropene Derivatives Having An ACAT2-Inhibiting Activity 有权
    具有ACAT2抑制活性的吡柔比星衍生物

    公开(公告)号:US20110184173A1

    公开(公告)日:2011-07-28

    申请号:US12810545

    申请日:2008-12-17

    IPC分类号: C07D401/14

    摘要: The present invention is a compound having the general formula (I), (II), or (III) or a pharmacologically acceptable salt, solvate, or hydrate thereof, and a pharmaceutical composition containing such a compound, or its pharmacologically acceptable ester, or other pharmacologically acceptable derivative thereof as an active ingredient. The compound has an excellent ACAT 2-inhibiting activity by a mechanism different from that of a statin drug and is useful as a therapeutic or prophylactic agent for obesity, adiposis, hyperlipidemia, hypercholesterolemia, disorder of lipid metabolism, and arteriosclerosis, as well as obesity-derived hyperlipidemia, hypercholesterolemia, disorder of lipid metabolism, arteriosclerosis, and hypertension.

    摘要翻译: 本发明是具有通式(I),(II)或(III)的化合物或其药理学上可接受的盐,溶剂化物或水合物,以及含有这种化合物或其药理学上可接受的酯的药物组合物,或 其他药理学上可接受的衍生物作为活性成分。 该化合物通过与他汀类药物不同的机制具有优异的ACAT 2抑制活性,并且可用作肥胖症,肥胖症,高脂血症,高胆固醇血症,脂质代谢紊乱和动脉硬化以及肥胖症的治疗或预防剂 衍生的高脂血症,高胆固醇血症,脂质代谢紊乱,动脉硬化和高血压。

    NOVEL COMPOUND, PROCESS FOR PRODUCTION THEREOF, AND USE THEREOF
    36.
    发明申请
    NOVEL COMPOUND, PROCESS FOR PRODUCTION THEREOF, AND USE THEREOF 审中-公开
    新型化合物,其生产方法及其用途

    公开(公告)号:US20100291622A1

    公开(公告)日:2010-11-18

    申请号:US12681202

    申请日:2008-09-12

    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。

    Fki-1366 substances and process for producing the same
    38.
    发明申请
    Fki-1366 substances and process for producing the same 审中-公开
    Fki-1366物质及其生产方法

    公开(公告)号:US20060252930A1

    公开(公告)日:2006-11-09

    申请号:US10548452

    申请日:2003-08-29

    IPC分类号: C07D267/22 C07K7/60

    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 the 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,并从培养物质中分离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 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。

    Selection media for beauveriolide I or beauveriolide III and process for selectively producing these substances
    39.
    发明授权
    Selection media for beauveriolide I or beauveriolide III and process for selectively producing these substances 失效
    选择培养基用于白藜芦醇I或白藜芦醇III及选择性生产这些物质的方法

    公开(公告)号:US06902925B2

    公开(公告)日:2005-06-07

    申请号:US10239831

    申请日:2001-04-10

    IPC分类号: C12N1/14 C12P17/14 C12P21/02

    CPC分类号: C12P17/14 C12N1/14 C12P21/02

    摘要: The present invention is a process for selective production of beauveriolide I substance or beauveriolide III substance, in which a beauveriolide producing microorganism strain FO-6979 or mutant thereof is cultured in a medium for fungi added with specific amino acid in order to produce beauveriolide I substance or beauveriolide III substance selectively with high yield; beauveriolide I substance or beauveriolide III substance is accumulated selectively in the cultured mass; and beauveriolide I substance or beauveriolide III substance is collected selectively with high yield from said cultured mass.

    摘要翻译: 本发明是一种选择性生产白化二醇I物质或白藜芦醇III物质的方法,其中产生微生物菌株FO-6979或其变异体的微生物菌株FO-6979或其突变体在添加有特定氨基酸的真菌培养基中培养以产生博美硼酸I物质 或白藜芦醇III物质选择性地高产量; 白藜芦醇I物质或白藜芦醇III物质在培养物中选择性积聚; 并且从所述培养物质中以高产率选择性地收集了硼莫单体I物质或白藜芦醇III物质。