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1.发明授权Effector conjugates, methods for their preparation and their pharmaceutical use 失效效应物缀合物，其制备方法及其药物用途公开(公告)号：US07605136B2
公开(公告)日：2009-10-20
申请号：US10728098
申请日：2003-12-05
CPC分类号： C07D417/04 , A61K47/6809 , A61K47/6851 , C07D309/10 , C07D417/14 , C07D493/04 , C07F7/1804 , Y02P20/55
摘要： Conjugates of epothilones and epothilone derivatives (as effectors) with suitable saccharides or saccharide derivatives (as recognition units) are described. Their production is carried out by the recognition units being reacted with suitable linkers, and the compounds that are produced are conjugated to the effectors. The pharmaceutical use of the conjugates for treating proliferative or angiogenesis-associated processes is described.
摘要翻译： 描述了具有合适的糖或糖衍生物（作为识别单元）的埃坡霉素和埃坡霉素衍生物（作为效应物）的缀合物。 它们的生产由识别单元与合适的接头反应进行，所生产的化合物与效应物共轭。 描述了缀合物用于治疗增殖或血管生成相关过程的药物用途。
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2.发明申请New effector conjugates, methods for their preparation and their pharmaceutical use 审中-公开新的效应物缀合物，其制备方法及其药物用途公开(公告)号：US20060276413A1
公开(公告)日：2006-12-07
申请号：US11500460
申请日：2006-08-08
IPC分类号： A61K31/7052 , A61K31/427 , C07D417/02
CPC分类号： C07D417/04 , A61K47/6809 , A61K47/6851 , C07D309/10 , C07D417/14 , C07D493/04 , C07F7/1804 , Y02P20/55
摘要： Conjugates of epothilones and epothilone derivatives (as effectors) with suitable saccharides or saccharide derivatives (as recognition units) are described. Their production is carried out by the recognition units being reacted with suitable linkers, and the compounds that are produced are conjugated to the effectors. The pharmaceutical use of the conjugates for treating proliferative or angiogenesis-associated processes is described.
摘要翻译： 描述了具有合适的糖或糖衍生物（作为识别单元）的埃坡霉素和埃坡霉素衍生物（作为效应物）的缀合物。 它们的生产由识别单元与合适的接头反应进行，所生产的化合物与效应物共轭。 描述了缀合物用于治疗增殖或血管生成相关过程的药物用途。
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3.发明申请New effector conjugates, process for their production and their pharmaceutical use 审中-公开新的效应物缀合物，其生产过程及其药物用途公开(公告)号：US20080166362A1
公开(公告)日：2008-07-10
申请号：US12000258
申请日：2007-12-11
申请人： Markus Berger , Gerhard Siemeister , Ulrich Klar , Jorg Willuda , Andreas Menrad , Klaus Bosslet
发明人： Markus Berger , Gerhard Siemeister , Ulrich Klar , Jorg Willuda , Andreas Menrad , Klaus Bosslet
IPC分类号： A61K39/395 , C07D417/00 , C07K16/00 , A61P25/00 , A61K35/04 , A61P19/00 , A61P29/00 , A61K31/425
CPC分类号： C07D493/04 , A61K47/6809 , A61K47/6851 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/14
摘要： Conjugates of epothilones and epothilone derivatives (as effectors) with suitable biomolecules (as recognition units) are described. Their production is carried out by the effectors being reacted with suitable linkers, and the compounds that are produced are conjugated to the recognition units. The pharmaceutical use of the conjugates for treating proliferative or angiogenesis-associated processes is described.
摘要翻译： 描述了具有合适的生物分子（作为识别单元）的埃坡霉素和埃坡霉素衍生物（作为效应物）的缀合物。 它们的生产通过与合适的接头反应的效应器进行，并且所生成的化合物与识别单元缀合。 描述了缀合物用于治疗增殖或血管生成相关过程的药物用途。
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4.发明申请New effector conjugates, process for their production and their pharmaceutical use 审中-公开新的效应物缀合物，其生产过程及其药物用途公开(公告)号：US20050234247A1
公开(公告)日：2005-10-20
申请号：US11045503
申请日：2005-01-31
申请人： Ulrich Klar , Joerg Willuda , Andreas Menrad , Klaus Bosslet
发明人： Ulrich Klar , Joerg Willuda , Andreas Menrad , Klaus Bosslet
IPC分类号： A61K39/00 , A61P19/00 , A61P25/00 , A61P29/00 , A61P35/00 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/14 , C07D493/04 , C07D493/08 , C07F9/28 , C07K16/00
CPC分类号： C07D493/04 , A61K2039/505 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , Y02P20/55
摘要： Conjugates of epothilones and epothilone derivatives (as effectors) with suitable biomolecules (as recognition units) are described. Their production is carried out by the effectors being reacted with suitable linkers, and the compounds that are produced are conjugated to the recognition units. The pharmaceutical use of conjugates for treating proliferative or angiogenesis-associated processes is described.
摘要翻译： 描述了具有合适的生物分子（作为识别单元）的埃坡霉素和埃坡霉素衍生物（作为效应物）的缀合物。 它们的生产通过与合适的接头反应的效应器进行，并且所生成的化合物与识别单元缀合。 描述了缀合物用于治疗增殖性或血管生成相关过程的药物用途。
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5.发明申请New effector conjugates, process for their production and their pharmaceutical use 失效新的效应物缀合物，其生产过程及其药物用途公开(公告)号：US20070088060A1
公开(公告)日：2007-04-19
申请号：US11509557
申请日：2006-08-25
申请人： Markus Berger , Gerhard Siemeister , Ulrich Klar , Jorg Willuda , Andreas Menrad , Klaus Bosslet
发明人： Markus Berger , Gerhard Siemeister , Ulrich Klar , Jorg Willuda , Andreas Menrad , Klaus Bosslet
IPC分类号： A61K31/427
CPC分类号： C07D493/04 , A61K47/6809 , A61K47/6851 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/14
摘要： Conjugates of epothilones and epothilone derivatives (as effectors) with suitable biomolecules (as recognition units) are described. Their production is carried out by the effectors being reacted with suitable linkers, and the compounds that are produced are conjugated to the recognition units. The pharmaceutical use of the conjugates for treating proliferative or angiogenesis-associated processes is described.
摘要翻译： 描述了具有合适的生物分子（作为识别单元）的埃坡霉素和埃坡霉素衍生物（作为效应物）的缀合物。 它们的生产通过与合适的接头反应的效应器进行，并且所生成的化合物与识别单元缀合。 描述了缀合物用于治疗增殖或血管生成相关过程的药物用途。
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6.发明授权Effector conjugates, process for their production and their pharmaceutical use 失效效应物缀合物，其制备方法及其药物用途公开(公告)号：US07129254B2
公开(公告)日：2006-10-31
申请号：US10631011
申请日：2003-07-31
申请人： Markus Berger , Gerhard Siemeister , Ulrich Klar , Jorg Willuda , Andreas Menrad , Klaus Bosslet
发明人： Markus Berger , Gerhard Siemeister , Ulrich Klar , Jorg Willuda , Andreas Menrad , Klaus Bosslet
IPC分类号： A61K31/425 , A61K31/44 , C07D277/20 , C07D417/08
CPC分类号： C07D493/04 , A61K47/6809 , A61K47/6851 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/14
摘要： Conjugates of epothilones and epothilone derivatives (as effectors) with suitable biomolecules (as recognition units) are described. Their production is carried out by the effectors being reacted with suitable linkers, and the compounds that are produced are conjugated to the recognition units. The pharmaceutical use of the conjugates for treating proliferative or angiogenesis-associated processes is described.
摘要翻译： 描述了具有合适的生物分子（作为识别单元）的埃坡霉素和埃坡霉素衍生物（作为效应物）的缀合物。 它们的生产通过与合适的接头反应的效应器进行，并且所生成的化合物与识别单元缀合。 描述了缀合物用于治疗增殖或血管生成相关过程的药物用途。
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7.发明授权Effector conjugates, process for their production and their pharmaceutical use 失效效应物缀合物，其制备方法及其药物用途公开(公告)号：US07335775B2
公开(公告)日：2008-02-26
申请号：US11509557
申请日：2006-08-25
申请人： Markus Berger , Gerhard Siemeister , Ulrich Klar , Jorg Willuda , Andreas Menrad , Klaus Bosslet
发明人： Markus Berger , Gerhard Siemeister , Ulrich Klar , Jorg Willuda , Andreas Menrad , Klaus Bosslet
IPC分类号： C07D277/20 , C07D417/08
CPC分类号： C07D493/04 , A61K47/6809 , A61K47/6851 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/14
摘要： Conjugates of epothilones and epothilone derivatives (as effectors) with suitable biomolecules (as recognition units) are described. Their production is carried out by the effectors being reacted with suitable linkers, and the compounds that are produced are conjugated to the recognition units. The pharmaceutical use of the conjugates for treating proliferative or angiogenesis-associated processes is described.
摘要翻译： 描述了具有合适的生物分子（作为识别单元）的埃坡霉素和埃坡霉素衍生物（作为效应物）的缀合物。 它们的生产通过与合适的接头反应的效应器进行，并且所生成的化合物与识别单元缀合。 描述了缀合物用于治疗增殖或血管生成相关过程的药物用途。
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8.发明申请New effector conjugates, process for their production and their pharmaceutical use 失效新的效应物缀合物，其生产过程及其药物用途公开(公告)号：US20050026971A1
公开(公告)日：2005-02-03
申请号：US10631011
申请日：2003-07-31
申请人： Markus Berger , Gerhard Siemeister , Ulrich Klar , Jorg Willuda , Andreas Menrad , Klaus Bosslet
发明人： Markus Berger , Gerhard Siemeister , Ulrich Klar , Jorg Willuda , Andreas Menrad , Klaus Bosslet
IPC分类号： A61K47/48 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/14 , C07D493/04 , A61K31/427 , C07D417/02
CPC分类号： C07D493/04 , A61K47/6809 , A61K47/6851 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/14
摘要： Conjugates of epothilones and epothilone derivatives (as effectors) with suitable biomolecules (as recognition units) are described. Their production is carried out by the effectors being reacted with suitable linkers, and the compounds that are produced are conjugated to the recognition units. The pharmaceutical use of the conjugates for treating proliferative or angiogenesis-associated processes is described.
摘要翻译： 描述了具有合适的生物分子（作为识别单元）的埃坡霉素和埃坡霉素衍生物（作为效应物）的缀合物。 它们的生产通过与合适的接头反应的效应器进行，并且所生成的化合物与识别单元缀合。 描述了缀合物用于治疗增殖或血管生成相关过程的药物用途。
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公开(公告)号：US20060292139A1
公开(公告)日：2006-12-28
申请号：US11135155
申请日：2005-05-23
申请人： Mathias Gehrmann , Gerhard Seemann , Klaus Bosslet , Jorg Czech
发明人： Mathias Gehrmann , Gerhard Seemann , Klaus Bosslet , Jorg Czech
IPC分类号： A61K39/395 , C07K16/12
CPC分类号： C12Y302/01031 , A01K2217/05 , A61K38/00 , C07K14/705 , C07K16/18 , C07K2319/00 , C07K2319/02 , C12N9/00 , C12N9/2434 , C12N15/62
摘要： The invention relates to compounds which contain an antigen binding region which is bound to at least one enzyme which is able to metabolize a compound (prodrug) which has little or no cytotoxicity to a cytotoxic compound (drug), where the antigen binding region is composed of a single polypeptide chain. It is advantageous for covalently bonded carbohydrates to be present on the polypeptide chain.
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10.发明申请Monoclonal antibodies (MAbs) against tumor-associated antigens, the preparation and use thereof 审中-公开针对肿瘤相关抗原的单克隆抗体（MAb），其制备和应用公开(公告)号：US20060159682A1
公开(公告)日：2006-07-20
申请号：US10942929
申请日：2004-09-17
IPC分类号： A61K39/395 , C07K16/28
CPC分类号： C07K16/3084 , A61K38/00 , A61K47/68 , A61K47/6815 , A61K47/6817 , A61K47/6851 , A61K51/1045 , C07K16/30 , C07K2317/24 , C07K2317/56 , C07K2317/76 , C07K2319/00 , C07K2319/30
摘要： The invention relates to murine monoclonal antibodies (MAbs), A, B, C and D, which are directed against tumor-associated antigens. The nearly complete nucleotide sequences of the V genes of these MAbs are described, so that the relevant variable domains can be put together to give chimeric MAbs, or “humanized” MAbs are obtained by inserting the hypervariable regions (complementarity determining regions ═CDR) into a human MAb framework. Antibody constructs of this type can be employed in human therapy and in vivo diagnosis without the disadvantages observed with murine MAbs.
摘要翻译： 本发明涉及针对肿瘤相关抗原的鼠单克隆抗体（MAb），A，B，C和D。 描述了这些MAb的V基因的几乎完整的核苷酸序列，使得相关的可变结构域可以放在一起以产生嵌合的MAb，或者通过将高变区（互补决定区-CDR）插入到 人类的MAb框架。 这种类型的抗体构建体可以用于人类治疗和体内诊断，而不存在用鼠MAb观察到的缺点。
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