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    Rifamycins, their compositions and use as antibiotics
    1.
    发明授权
    Rifamycins, their compositions and use as antibiotics 失效
    利福霉素，其组合物和用作抗生素

    公开(公告)号：US4411896A

    公开(公告)日：1983-10-25

    申请号：US397379

    申请日：1982-07-12

    申请人： Thomas Schupp ,  Peter Traxler ,  Jakob Nuesch

    发明人： Thomas Schupp ,  Peter Traxler ,  Jakob Nuesch

    IPC分类号： C07D498/08 ,  C07D498/18 ,  C12P17/18 ,  A61K31/395 ,  C07D491/08

    CPC分类号： C07D498/08 ,  C07D498/18 ,  C12P17/189 ,  C12R1/365 ,  Y10S435/872 ,  Y10S435/886

    摘要： New antibiotically active compounds having the basic structure of rifamycin S, namely 3-hydroxyrifamycin S (formula A: X=>C.dbd.O; R.sup.1 =OH; R.sup.2 =H), 3,31-dihydroxy-rifamycin S (formula A: X=>C.dbd.O; R.sup.1 =R.sup.2 =OH) and 1-desoxy-1-oxarifamycin S (formula A: X=--O--; R.sup.1 =R.sup.2 =H) ##STR1## are formed by cultivating, under aerobic conditions, a strain of Nocardia mediterranei which is derived from Streptomyces mediterranei ATCC 13 685 as the parent strain and is characterized by the ability to produce at least one of the mentioned compounds. The recombinant strain Nocardia mediterranei DSM 1415 has proved suitable. The mentioned rifamycin S analogues have analogous antibiotic properties to this but have a wider range of action, especially against gram-negative bacteria.

    摘要翻译： 具有利福霉素S的基本结构的新的抗生素活性化合物即3-羟基喜树碱S（式A：X => C = O; R1 = OH; R2 = H），3,31-二羟基利福霉素S（式A：X （A = X = -O-; R 1 = R 2 = H）通过在有氧下培养形成（A），（C = O; R1 = R2 = OH）和1-脱氧-1-氧硫霉素S 条件，来自地衣链霉菌（Streptomyces mediterranei）ATCC13685作为亲本菌株的诺卡氏菌（Nocardia mediterranei）菌株，其特征在于产生至少一种所述化合物的能力。 重组菌诺卡氏菌DSM 1415已证明是合适的。 所提到的利福霉素S类似物具有类似的抗生素特性，但具有更广泛的作用范围，特别是针对革兰氏阴性细菌。

    Cobalamine derivatives useful for diagnosis and treatment of abnormal cellular proliferation
    3.
    发明申请
    Cobalamine derivatives useful for diagnosis and treatment of abnormal cellular proliferation 失效
    用于诊断和治疗异常细胞增殖的钴胺衍生物

    公开(公告)号：US20070155692A1

    公开(公告)日：2007-07-05

    申请号：US10583760

    申请日：2004-12-21

    申请人： Hans-Jorg Treichler ,  Roger Alberto ,  Robert Waibel ,  Martin Kuenzi ,  Jakob Nuesch ,  Stefan Mundwiler ,  Dave van Staveren

    发明人： Hans-Jorg Treichler ,  Roger Alberto ,  Robert Waibel ,  Martin Kuenzi ,  Jakob Nuesch ,  Stefan Mundwiler ,  Dave van Staveren

    IPC分类号： A61K31/714 ,  C07H23/00

    CPC分类号： C07H23/00 ,  A61K51/041 ,  A61K51/0482 ,  A61K51/0497

    摘要： The invention relates to cobalamin derivatives (a) having no binding affinity or low binding affinity to the transport protein transcobalamin II TCII) and (b) retaining activity as a vitamin B12 substitute, optionally carrying a therapeutic and/or diagnostic agent, such as a radioactive metal. These compounds have a much reduced accumulation rate in blood and benign organs, such as kidney and liver, compared to the accumulation rate in neoplastic tissues, and are more rapidly eliminated from blood. The invention further relates to a method of diagnosis and a method of treatment of a neoplastic disease or an infection by microorganisms in a mammal comprising (a) exposing the mammal to a period of a vitamin B12-free diet, and (b) subsequently applying a cobalamin derivative of the invention carrying a diagnostic and/or therapeutic agent. By selecting cobalamin derivatives acting as vitamin B12 substitutes, the risk of the formation of resistant offspring in neoplastic tissue is much reduced.

    摘要翻译： 本发明涉及对运输蛋白转铁蛋白II TCII没有结合亲和力或低结合亲和力的钴胺素衍生物（a））和（b）保留作为维生素B12替代物的活性，任选地携带治疗和/或诊断剂，例如 放射性金属。 与肿瘤组织中的积累率相比，这些化合物在血液和良性器官如肾脏和肝脏中的积聚速率大大降低，并且从血液中更快速地消除。 本发明还涉及一种诊断方法和治疗哺乳动物的微生物的肿瘤疾病或感染的方法，其包括（a）将哺乳动物暴露于不含维生素B12的饮食期间，以及（b）随后应用 携带诊断和/或治疗剂的本发明的钴胺素衍生物。 通过选择作为维生素B12替代物的钴胺素衍生物，在肿瘤组织中形成抗性后代的风险大大降低。

    Fermentation process for producing a rifamycin derivative
    5.
    发明授权
    Fermentation process for producing a rifamycin derivative 失效
    用于生产利福霉素衍生物的发酵方法

    公开(公告)号：US4298692A

    公开(公告)日：1981-11-03

    申请号：US112898

    申请日：1980-01-17

    申请人： Thomas Schupp ,  Peter Traxler ,  Jakob Nuesch

    发明人： Thomas Schupp ,  Peter Traxler ,  Jakob Nuesch

    IPC分类号： C07D498/08 ,  C07D498/18 ,  C12P17/18

    CPC分类号： C07D498/08 ,  C07D498/18 ,  C12P17/189 ,  C12R1/365 ,  Y10S435/872

    摘要： New antibiotically active compounds having the basic structure of rifamycin S, namely 3-hydroxyrifamycin S (formula A: X.dbd.>C.dbd.O; R.sup.1 .dbd.OH; R.sup.2 .dbd.H), 3,31-dihydroxyrifamycin S (formula A: X.dbd.>C.dbd.O; R.sup.1 .dbd.R.sup.2 .dbd.OH) and 1-desoxy-1-oxarifamycin S (formula A: X.dbd.--O--; R.sup.1 .dbd.R.sup.2 .dbd.H) ##STR1## are formed by cultivating, under aerobic conditions, a strain of Nocardia mediterranei which is derived from Streptomyces mediterranei ATCC 13 685 as the parent strain and is characterized by the ability to produce at least one of the mentioned compounds. The recombinant strain Nocardia mediterranei DSM 1415 has proved suitable. The mentioned rifamycin S analogues have analogous antibiotic properties to this but have a wider range of action, especially against gram-negative bacteria.

    摘要翻译： 具有利福霉素S的基本结构的新型抗生素活性化合物，即3-羟基喜树碱S（式A：X => C = O; R 1 = OH; R 2 = H），3,31-二羟基化合物S（式A：X = C = O; R1 = R2 = OH）和1-脱氧-1-氧硫霉素S（式A：X = -O-; R1 = R2 = H）通过在需氧条件下培养， 作为亲本菌株来源于地塞米松（Streptomyces mediterranei）ATCC13685的诺卡氏菌（Nocardia mediterranei）菌株，其特征在于产生至少一种所述化合物的能力。 重组菌诺卡氏菌DSM 1415已证明是合适的。 所提到的利福霉素S类似物具有类似的抗生素特性，但具有更广泛的作用范围，特别是针对革兰氏阴性细菌。

    Papulacandin derivatives and pharmaceutical compositions containing same
    6.
    发明授权
    Papulacandin derivatives and pharmaceutical compositions containing same 失效
    帕拉可坎因衍生物和含有它们的药物组合物

    公开(公告)号：US4278665A

    公开(公告)日：1981-07-14

    申请号：US844412

    申请日：1977-10-21

    申请人： Peter Traxler ,  Johannes Gruner ,  Jakob Nuesch

    发明人： Peter Traxler ,  Johannes Gruner ,  Jakob Nuesch

    IPC分类号： A01N63/02 ,  A61K31/70 ,  A61K31/7024 ,  A61P31/04 ,  C07H7/04 ,  C07H13/04 ,  C07H19/01 ,  C12P1/02 ,  C12P19/12 ,  C12P19/44 ,  C12P19/60 ,  C12R1/645 ,  A61K31/71 ,  C07H17/04

    CPC分类号： C07H19/01 ,  C12P19/12 ,  C12R1/645

    摘要： The new antibiotic "Papulacandin" is obtained by the cultivation of the microorganism Papularia sphaerosperma (Pers.) Hohnel, especially of the strain NRRL 8086, under aerobic conditions in an aqueous nutrient medium. There can also be used mutants of said microorganisms. Papulacandin consists of various components A, B, C, D and E, the more important of which are A and B, whose structures have been elucidated to a great extent: they contain only carbon, hydrogen and oxygen. Papulacandin and its components have a strong anti-fungal action, for instance against Candida albicans, and can be used for combating infections caused by pathogenic fungi.

    摘要翻译： 新的抗生素“Papulacandin”是通过在有氧条件下在含水营养培养基中培养微生物Papularia spherersperma（Pers。）Höhnel，特别是NRRL 8086菌株获得的。 还可以使用所述微生物的突变体。 帕拉坎卡因由各种组分A，B，C，D和E组成，其中更重要的是A和B，其结构在很大程度上被阐明：它们仅含有碳，氢和氧。 Papulacandin及其组分具有强烈的抗真菌作用，例如对抗白色念珠菌，并且可用于对抗致病真菌引起的感染。