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36 条记录 (耗时 0.02 秒)

    Cyclipostins, process for their preparation and use thereof
    1.
    发明授权
    Cyclipostins, process for their preparation and use thereof 有权
    Cyclipostins，其制备和使用的方法

    公开(公告)号：US06756402B2

    公开(公告)日：2004-06-29

    申请号：US09886044

    申请日：2001-06-22

    申请人： Laszlo Vertesy ,  Klaus Ehrlich ,  Michael Kurz ,  Joachim Wink

    发明人： Laszlo Vertesy ,  Klaus Ehrlich ,  Michael Kurz ,  Joachim Wink

    IPC分类号： A61K31335

    CPC分类号： C12R1/465 ,  C07F9/65744 ,  C12P9/00

    摘要： The invention relates to compounds of formula I in which R1, R2, E, X1, X2, and X3 have the meaning as described in the specification and claims, obtained by culturing Streptomyces species HAG 004107 (DSM 13381), and their physiologically tolerable salts and chemical equivalents. The invention furthermore relates to a process for the preparation of the cyclipostins, the microorganism HAG 004107 (DSM 13381), the use of the cyclipostins and their physiologically tolerable salts and chemical equivalents as pharmaceuticals, in particular as inhibitors of lipases, and pharmaceutical preparations which contain cyclipostin or a physiologically tolerable salt or equivalent thereof.

    摘要翻译： 本发明涉及式Iin化合物，其中R 1，R 2，E，X 1，X 2和X 3具有如说明书和权利要求书中所述的含义，通过培养链霉菌种类HAG 004107（DSM 13381）， 及其生理上可耐受的盐和化学当量。 本发明还涉及一种制备环肽酶，微生物HAG 004107（DSM 13381），环肽素及其生理上可耐受的盐和化学等价物作为药物，特别是作为脂肪酶抑制剂的药物制剂的方法，以及药物制剂 含有Cycipostin或生理上可耐受的盐或其等同物。

    Pluraflavins and derivatives thereof, process for their preparation and use thereof
    2.
    发明授权
    Pluraflavins and derivatives thereof, process for their preparation and use thereof 有权
    多夫肝素及其衍生物，其制备方法和用途

    公开(公告)号：US06500936B2

    公开(公告)日：2002-12-31

    申请号：US09784035

    申请日：2001-02-16

    申请人： Laszlo Vertesy ,  Klaus Ehrlich ,  Martin Knauf ,  Joachim Wink ,  Francis P. Barbone ,  Elaine A. Powers ,  Elizabeth A. Cashman

    发明人： Laszlo Vertesy ,  Klaus Ehrlich ,  Martin Knauf ,  Joachim Wink ,  Francis P. Barbone ,  Elaine A. Powers ,  Elizabeth A. Cashman

    IPC分类号： A61K3135

    CPC分类号： C12R1/01 ,  C07H17/04 ,  C12P19/26 ,  C12P19/60

    摘要： The invention relates to a compound of formula (I) wherein R1 is a sugar; R2 is —CH2—O—(R7)m, R7 representing a sugar, or is —COOH; R3 is an epoxide-comprising group, or is C1-C6-alkyl or C2-C6-alkenyl, unsubstituted or substituted by at least one OH; R5 is H, C1-C6-alkyl, C2-C6-alkenyl or C2-C6-alkynyl; R4R6, R8 and R10 independently of one another are H; C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, —X2H, or —X2R12, or R4 and R6 together and/or R8 and R10 together are =X2; X2 is O, NH, N—C1-C6-alkyl, N—C2-C6-alkenyl, N-C2-C6-alkynyl or S; R12 is C1-C6-alkyl, C2-C6—alkenyl, C2-C6-alkynyl, aryl or acyl; and m and n are 1 or 2; in any of its stereochemical forms and mixtures of these forms in any ratio, and a physiologically acceptable salt or derivative thereof. The compounds are obtainable from a culture of the microorganism Actinomycetales species HAG 003959, DSM 12931, by fermentation. Accordingly, the invention relates to a process for their preparation and to the use of the compounds as pharmaceuticals, for example as antitumor agents.

    摘要翻译： 本发明涉及式（I）化合物，其中R1是糖; R2是-CH2-O-（R7）m，R7代表糖，或是-COOH; R3是含环氧化物的基团，或是未被取代或被至少一个OH取代的C1-C6-烷基或C2-C6-烯基; R5是H，C1-C6-烷基，C2-C6-烯基或C2-C6-炔基; R4R6，R8和R10彼此独立地为H; C1-C6-烷基，C2-C6-烯基，C2-C6-炔基，-X2H或-X2R12或R4和R6一起和/或R8和R10一起为= X2; X 2是O，NH，N-C 1 -C 6 - 烷基，N-C 2 -C 6 - 烯基，N-C 2 -C 6 - 炔基或S; R 12是C 1 -C 6烷基，C 2 -C 6 - 烯基，C 2 -C 6炔基，芳基或酰基; m和n为1或2; 其任何立体化学形式和这些形式的任何比例的混合物及其生理上可接受的盐或其衍生物。 这些化合物可通过发酵从放线菌种类HAG 003959，DSM 12931的培养物中获得。 因此，本发明涉及其制备和使用化合物作为药物的方法，例如作为抗肿瘤剂。

    Cephaibols: novel antiparasitics from Acremonium tubakii, process for their production, and use thereof
    10.
    发明授权
    Cephaibols: novel antiparasitics from Acremonium tubakii, process for their production, and use thereof 有权
    头孢唑醇：来自Acremonium tubakii的新型抗寄生虫药，其生产方法及其用途

    公开(公告)号：US07067112B2

    公开(公告)日：2006-06-27

    申请号：US10411144

    申请日：2003-04-11

    申请人： Laszlo Vertesy ,  Michael Kurz ,  Matthias Schiell ,  Joachim Hofmann

    发明人： Laszlo Vertesy ,  Michael Kurz ,  Matthias Schiell ,  Joachim Hofmann

    IPC分类号： A61K49/00 ,  A61K38/10 ,  C07K7/08

    CPC分类号： C07K7/08 ,  A61K38/00

    摘要： The invention relates to compounds of the formula I AcPhe-Aib-Aib-Aib-x-w-Leu-y-Aib-Hyp-Gln-z-Hyp-Aib-Pro-R   (I) in which R is Phe-ol or Phe-al and w, x, y, and z have the following meanings: a) w is Gly or Ala; x is Aib and y and z are Iva; b) w is Gly; x, y and z are Iva; c) w is Gly; x and z are Aib and y is Iva; d) w is Gly; x, y and z are Aib; or e) w is Gly; x and y are Aib and z is Iva; or of the formula II AcPhe-Iva-Gln-Aib-lle-Thr-Aib-Leu-Aib-x-Gln-Aib-Hyp-Aib-Pro-Phe-Ser,   (II) wherein x is Hyp or Pro, which are synthesized by Acremonium tubakii FH 1685 DSM 12774 during fermentation and released into the culture medium, a process for the isolation of the cephaibols from the culture medium, and their purification, and the use of the cephaibols as pharmacologically active compounds, in particular for the control of parasites.

    摘要翻译： 本发明涉及式I化合物<？in-line-formula description =“In-line Formulas”end =“lead”→AcPhe-Aib-Aib-Aib-xw-Leu-y-Aib-Hyp-Gln -z-Hyp-Aib-Pro-R（I）<？in-line-formula description =“In-line Formulas”end =“tail”？>其中R是Phe-ol或Phe-al，w，x ，y和z具有以下含义：a）w是Gly或Ala; x是Aib，y和z是Iva; b）w是Gly; x，y和z是Iva; c）w是Gly; x和z是Aib，y是Iva; d）w是Gly; x，y和z是Aib; 或e）w是Gly; x和y是Aib，z是Iva; AcPhe-Iva-Gln-Aib-Lle-Thr-Aib-Leu-Aib-x-Gln-Aib，或者式II <？in-line-formula description =“In-line Formulas”end =“lead” -Hyp-Aib-Pro-Phe-Ser，（II）<？在线公式描述=“在线公式”end =“tail”？>其中x是Hyp或Pro，它们是由Acremonium tubakii FH 1685 DSM 12774在发酵过程中释放到培养基中，从培养基中分离头孢胆素的方法及其纯化，以及将头孢唑醇用作药物活性化合物，特别是用于控制寄生虫的方法。