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17 条记录 (耗时 0.03 秒)

    Inactivation of genes of the MEP pathway
    6.
    发明授权
    Inactivation of genes of the MEP pathway 失效
    MEP途径的基因失活

    公开(公告)号：US07875279B2

    公开(公告)日：2011-01-25

    申请号：US10475510

    申请日：2002-04-13

    申请人： Hassan Jomaa ,  Matthias Eberl ,  Boran Altincicek

    发明人： Hassan Jomaa ,  Matthias Eberl ,  Boran Altincicek

    IPC分类号： A61K39/395 ,  A61K51/00 ,  A01N63/00 ,  C12P21/00

    CPC分类号： A61K35/68 ,  A61K31/66

    摘要： The invention relates to cells and organisms as well as to methods for producing said cells and organisms, according to which intermediates of the mevalonate-independent pathway for isoprenoid biosynthesis (MEP pathway) are enriched by deleting or inactivating genes. The derivatives can also be enriched by using enzyme inhibitors. The enriched intermediates may be used as substrates in enzyme activity tests. The inventive cells and organisms and the enriched intermediates can further be used in the production of medicaments.

    摘要翻译： 本发明涉及细胞和生物体，以及用于产生所述细胞和生物体的方法，根据该方法，通过缺失或失活基因来富集用于类异戊二烯生物合成（MEP途径）的甲羟戊酸非依赖性途径的中间体。 还可以通过使用酶抑制剂来富集衍生物。 富集的中间体可用作酶活性测试中的底物。 本发明的细胞和生物以及富集的中间体可进一步用于制备药物。

    Inactivation Of Genes Of The Mep Pathway
    7.
    发明申请
    Inactivation Of Genes Of The Mep Pathway 失效
    Mep途径的基因失活

    公开(公告)号：US20080206267A1

    公开(公告)日：2008-08-28

    申请号：US10475510

    申请日：2002-04-13

    申请人： Hassan Jomaa ,  Matthias Eberl ,  Boran Altincicek

    发明人： Hassan Jomaa ,  Matthias Eberl ,  Boran Altincicek

    IPC分类号： A61K39/00 ,  C12P13/02 ,  C12N15/74

    CPC分类号： A61K35/68 ,  A61K31/66

    摘要： The invention relates to cells and organisms as well as to methods for producing said cells and organisms, according to which intermediates of the mevalonate-independent pathway for isoprenoid biosynthesis (MEP pathway) are enriched by deleting or inactivating genes. The derivatives can also be enriched by using enzyme inhibitors. The enriched intermediates may be used as substrates in enzyme activity tests. The inventive cells and organisms and the enriched intermediates can further be used in the production of medicaments.

    摘要翻译： 本发明涉及细胞和生物体，以及用于产生所述细胞和生物体的方法，根据该方法，通过缺失或失活基因来富集用于类异戊二烯生物合成（MEP途径）的甲羟戊酸非依赖性途径的中间体。 还可以通过使用酶抑制剂来富集衍生物。 富集的中间体可用作酶活性测试中的底物。 本发明的细胞和生物以及富集的中间体可进一步用于制备药物。

    Organophosphoric Derivatives Useful as Anti-Parasitic Agents
    8.
    发明申请
    Organophosphoric Derivatives Useful as Anti-Parasitic Agents 失效
    有机磷衍生物可用作反寄生剂

    公开(公告)号：US20080312190A1

    公开(公告)日：2008-12-18

    申请号：US12158973

    申请日：2006-12-22

    申请人： Serge Van Calenbergh ,  Timothy Haemers ,  Vincent Devreux ,  Hassan Jomaa ,  Jochen Wiesner

    发明人： Serge Van Calenbergh ,  Timothy Haemers ,  Vincent Devreux ,  Hassan Jomaa ,  Jochen Wiesner

    IPC分类号： C07F9/6553 ,  A61K31/67 ,  A61P33/00 ,  A61P33/06

    CPC分类号： C07F9/3882 ,  A01N57/22 ,  C07F9/3808 ,  C07F9/4006 ,  C07F9/4056 ,  C07F9/655345 ,  Y02P20/55

    摘要： The present invention relates to novel phosphonic acid compounds having the structural formula (I): wherein: (a) R is a group of 1 to 5 substituents independently selected from the group consisting of fluoro, chloro, bromo, C1-4 alkoxy, C1-4 alkyl, hydroxy, formyl, trifluoromethoxy, phenyl, heterocyclic, heterocyclic-substituted methyl, aminomethyl, hydroxy methyl, bromomethyl, sulfonyl chloride, acetyl chloride, nitroso and cyano, (b) R1 is selected from the group consisting of hydrogen, C1-7 alkyl, C3-10 cycloalkyl, aryl, arylalkyl and heterocyclic, and (c) R2 is selected from the group consisting of hydroxy and hydroxy-protecting groups, and stereoisomer, solvates and salts thereof. These compounds are useful as anti-infectious and anti-parasitic agents, in particular anti-malaria agents.

    摘要翻译： 本发明涉及具有结构式（I）的新型膦酸化合物：其中：（a）R是1至5个独立地选自氟，氯，溴，C1-4烷氧基，C1 -4-烷基，羟基，甲酰基，三氟甲氧基，苯基，杂环，杂环取代的甲基，氨基甲基，羟基甲基，溴甲基，磺酰氯，乙酰氯，亚硝基和氰基，（b）R 1选自氢， 烷基，C 3-10环烷基，芳基，芳烷基和杂环基，和（c）R 2选自羟基和羟基保护基，以及它们的立体异构体，溶剂化物和盐。 这些化合物可用作抗感染和抗寄生虫剂，特别是抗疟剂。

    Organophosphoric derivatives useful as anti-parasitic agents
    9.
    发明授权
    Organophosphoric derivatives useful as anti-parasitic agents 失效
    有机磷衍生物可用作抗寄生虫药物

    公开(公告)号：US07638505B2

    公开(公告)日：2009-12-29

    申请号：US12158973

    申请日：2006-12-22

    申请人： Serge Van Calenbergh ,  Timothy Haemers ,  Vincent Devreux ,  Hassan Jomaa ,  Jochen Wiesner

    发明人： Serge Van Calenbergh ,  Timothy Haemers ,  Vincent Devreux ,  Hassan Jomaa ,  Jochen Wiesner

    IPC分类号： A01N57/00

    CPC分类号： C07F9/3882 ,  A01N57/22 ,  C07F9/3808 ,  C07F9/4006 ,  C07F9/4056 ,  C07F9/655345 ,  Y02P20/55

    摘要： The present invention relates to novel phosphonic acid compounds having the structural formula (I): wherein: (a) R is a group of 1 to 5 substituents independently selected from the group consisting of fluoro, chloro, bromo, C1-4 alkoxy, C1-4 alkyl, hydroxy, formyl, trifluoromethoxy, phenyl, heterocyclic, heterocyclic-substituted methyl, aminomethyl, hydroxy methyl, bromomethyl, sulfonyl chloride, acetyl chloride, nitroso and cyano, (b) R1 is selected from the group consisting of hydrogen, C1-7 alkyl, C3-10 cycloalkyl, aryl, arylalkyl and heterocyclic, and (c) R2 is selected from the group consisting of hydroxy and hydroxy-protecting groups, and stereoisomer, solvates and salts thereof. These compounds are useful as anti-infectious and anti-parasitic agents, in particular anti-malaria agents.

    摘要翻译： 本发明涉及具有结构式（I）的新型膦酸化合物：其中：（a）R是1至5个独立地选自氟，氯，溴，C1-4烷氧基，C1 -4-烷基，羟基，甲酰基，三氟甲氧基，苯基，杂环，杂环取代的甲基，氨基甲基，羟基甲基，溴甲基，磺酰氯，乙酰氯，亚硝基和氰基，（b）R 1选自氢， 烷基，C 3-10环烷基，芳基，芳烷基和杂环基，和（c）R 2选自羟基和羟基保护基，以及它们的立体异构体，溶剂化物和盐。 这些化合物可用作抗感染和抗寄生虫剂，特别是抗疟剂。

    Medicaments containing bisphosphonic acids and derivatives thereof for preventing and treating diseases and allergies
    10.
    发明申请
    Medicaments containing bisphosphonic acids and derivatives thereof for preventing and treating diseases and allergies 审中-公开
    含有双膦酸及其衍生物的药物用于预防和治疗疾病和过敏

    公开(公告)号：US20060040899A1

    公开(公告)日：2006-02-23

    申请号：US11121044

    申请日：2005-05-04

    申请人： Hassan Jomaa

    发明人： Hassan Jomaa

    IPC分类号： A61K31/675 ,  A61K31/663

    CPC分类号： A61K39/0008 ,  A61K2039/55511

    摘要： Provided are compounds and methods for the prevention and treatment of autoimmune disorders and of allergies using such compositions in which autoantigens or allergens previously used for treating autoimmune disorders and allergies are used in combination with bisphosphonates or the derivatives thereof. Bisphosphonic acids and derivatives thereof generally corresponding to Formula I illustrated below are useful in the production of pharmaceutical formulations that may be used for the prevention and treatment of various autoimmune diseases or allergies. The bisphosphonic acids and the derivatives thereof which are used are those represented by the Formula I: in which the variables A1, A2, A3, A4, R1, R2 and X are selected from a range of substituents as outlined in the specification.

    摘要翻译： 提供了使用这样的组合物预防和治疗自身免疫性疾病和过敏的化合物和方法，其中先前用于治疗自身免疫性疾病和过敏症的自身抗原或过敏原与双膦酸盐或其衍生物组合使用。 通常对应于下述式I的二膦酸及其衍生物可用于制备可用于预防和治疗各种自身免疫性疾病或过敏症的药物制剂。 所使用的双膦酸及其衍生物是由式I表示的那些：其中变量A1，A2，A3，A4，R1，R2和X选自说明书中概述的一系列取代基。