Fki-1366 substances and process for producing the same
    41.
    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。

    Novel k99-5278 substance and a process for producing the same
    42.
    发明申请
    Novel k99-5278 substance and a process for producing the same 审中-公开
    新型k99-5278物质及其制备方法

    公开(公告)号:US20060014825A1

    公开(公告)日:2006-01-19

    申请号:US10492654

    申请日:2002-10-11

    摘要: The present invention relates to effective drugs for mycosis caused by so called fungi such as fungi and yeast. The present invention is comprised of culturing a microorganism belonging to genus Streptomyces and having ability to produce K99-5278A substance, K99-5278B substance and K99-5278C substance in a medium, accumulating K99-5278A substance, K99-5278B substance and K99-5278C substance in the cultured medium and isolating K99-5278A substance, K99-5278B substance and K99-5278C substance from the cultured mass. The thus obtained substances can be expected as a novel antifungal agent.

    摘要翻译: 本发明涉及由所谓的真菌如真菌和酵母引起的用于真菌病的有效药物。 本发明包括培养属于链霉菌属的微生物,并且能够在培养基中生产K99-5278A物质,K99-5278B物质和K99-5278C物质,积累K99-5278A物质,K99-5278B物质和K99-5278C 培养基中的物质,并从培养物质中分离K99-5278A物质,K99-5278B物质和K99-5278C物质。 可以预期由此获得的物质作为新颖的抗真菌剂。

    Selection media for beauveriolide I or beauveriolide III and process for selectively producing these substances
    43.
    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。

    K99-5041 substance and production thereof
    44.
    发明授权
    K99-5041 substance and production thereof 失效
    K99-5041物质及其生产

    公开(公告)号:US06747056B2

    公开(公告)日:2004-06-08

    申请号:US10359145

    申请日:2003-02-06

    IPC分类号: A61K3140

    CPC分类号: C07D207/32

    摘要: The present invention comprising culturing a microorganism which belongs to genus Streptomyces and has ability to produce K99-5041-C1x substance and/or K99-5041-C2x substance in a medium, accumulating K99-5041-C1x substance and/or K99-5041-C2x substance in the culture fluid, and isolating K99-5041-C1x substance and/or K99-5041-C2x substance form the cultured mass. Since the obtained K99-5041-C1x substance and/or K99-5041-C2x substance exhibit inhibitory activity against lanosterol synthase, these substances are expected to apply clinically for preventive and therapeutic agents caused by accumulation of cholesterol in humans and antifungal agents.

    摘要翻译: 本发明包括培养属于链霉菌属的微生物,并且能够在培养基中产生K99-5041-C1x物质和/或K99-5041-C2x物质,积累K99-5041-C1x物质和/或K99-5041- 培养液中的C2x物质,并从培养物质中分离K99-5041-C1x物质和/或K99-5041-C2x物质。 由于所获得的K99-5041-C1x物质和/或K99-5041-C2x物质对羊毛甾醇合酶表现出抑制活性,所以预期这些物质将临床应用于人类和抗真菌剂中胆固醇积聚引起的预防和治疗剂。

    Substance WK-5344A and wk-5344B and process for producing the same
    45.
    发明授权
    Substance WK-5344A and wk-5344B and process for producing the same 失效
    物质WK-5344A和wk-5344B及其制备方法

    公开(公告)号:US06512008B1

    公开(公告)日:2003-01-28

    申请号:US09857268

    申请日:2001-08-22

    IPC分类号: C12P1718

    摘要: The present invention relates to novel substance having inhibitory action on cholesteryl ester transfer protein, WK-5344A substance and WK-5344B substance, and process for production thereof. A microorganism belonging to genus Streptomyces having ability to produce WK-5344A substance and WK-5344B substance is cultured in a medium, and the WK-5344A substance and the WK-5344B substance are accumulated in the medium, then the WK-5344A substance and the WK-5344B substance are isolated from the said medium. Since the present substance shows significant inhibitory action on cholesteryl ester transfer protein, the substance is effective for prevention and treatment of diseases caused by accumulation of cholesterol in human.

    摘要翻译: 本发明涉及对胆固醇酯转移蛋白,WK-5344A物质和WK-5344B物质具有抑制作用的新物质及其生产方法。 在培养基中培养属于具有产生WK-5344A物质和WK-5344B物质的链霉菌属的微生物,将WK-5344A物质和WK-5344B物质累积在培养基中,然后将WK-5344A物质和 WK-5344B物质与所述介质分离。 由于本物质对胆固醇酯转移蛋白质具有显着的抑制作用,所以该物质对于预防和治疗由人胆固醇积累引起的疾病是有效的。

    "> 3, 3
    47.
    发明授权
    3, 3", 4"-Tri-O-acylspiramycin I 失效
    3,3“,4” - 三-O-酰基丝氨酸霉素I

    公开(公告)号:US4575497A

    公开(公告)日:1986-03-11

    申请号:US680347

    申请日:1984-12-11

    CPC分类号: C07H17/08

    摘要: 3, 3", 4"-Tri-O-acylspiramycin I represented by the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are the same or different groups, and at least one of the groups is a straight or branched chain alkylcarbonyl group represented by --COC.sub.m H.sub.2m+1 wherein m is an integer of 2-4 and the other group(s) are straight or branched chain alkylcarbonyl group(s) represented by --COC.sub.n H.sub.2n+1 wherein n is an integer of 1-4, and its pharmacologically acceptable acid addition salts.

    摘要翻译: 3,3“,4” - 由下式表示的三-O-酰基螺旋霉素I:其中R1,R2和R3是相同或不同的基团,并且至少一个基团是直链或支链 由-COCmH2m + 1表示的烷基羰基,其中m是2-4的整数,另一个基团是由-COC n H 2n + 1表示的直链或支链烷基羰基,其中n是1-4的整数, 及其药理学上可接受的酸加成盐。

    Pyripyropene derivatives having an ACAT2-inhibiting activity
    50.
    发明授权
    Pyripyropene derivatives having an ACAT2-inhibiting activity 有权
    具有抑制ACAT2活性的吡哆醛衍生物

    公开(公告)号:US08519128B2

    公开(公告)日:2013-08-27

    申请号:US12810545

    申请日:2008-12-17

    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。