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公开(公告)号：US07098241B2
公开(公告)日：2006-08-29
申请号：US10732633
申请日：2003-12-10
申请人： Adelbert Grossmann , Frank Herting , Matthias Koerner , Klaus-Peter Kuenkele , Anja Limberg , Olaf Mundigl , Ulrich Tibes
发明人： Adelbert Grossmann , Frank Herting , Matthias Koerner , Klaus-Peter Kuenkele , Anja Limberg , Olaf Mundigl , Ulrich Tibes
IPC分类号： A61K31/38 , C07D333/22
CPC分类号： C07D409/12 , C07D333/38 , C07D413/12
摘要： The (R) and (S) enantiomers of a compound of formula I are novel antiproliferative therapeutic agents. These compounds have HDAC inhibitor activity and are useful in the treatment of cancer. Also disclosed are methods of making and using compounds of formula (I), as well as pharmaceutical compositions containing compounds of formula (I).
摘要翻译： 式I化合物的（R）和（S）对映异构体是新的抗增殖治疗剂。 这些化合物具有HDAC抑制剂活性，可用于治疗癌症。 还公开了制备和使用式（I）化合物的方法，以及含有式（I）化合物的药物组合物。
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公开(公告)号：US06512123B2
公开(公告)日：2003-01-28
申请号：US10127100
申请日：2002-04-22
IPC分类号： C07D20982
CPC分类号： C07C259/06 , C07D209/88 , C07D313/12
摘要： Compounds of formula I wherein R1, R2, A, X, Y and Z have the meanings provided in the specification, and their enantiomers, diastereoisomers, racemates, pharmaceutically acceptable salts and mixtures thereof. These compounds have HDAC inhibitory activity for inhibiting cell proliferation. Also provided is a process of manufacturing these compounds.
摘要翻译： R1，R2，A，X，Y和Z中的式I化合物具有说明书中提供的含义及其对映异构体，非对映异构体，外消旋体，药学上可接受的盐及其混合物。 这些化合物具有抑制细胞增殖的HDAC抑制活性。 还提供了制造这些化合物的方法。
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3.发明授权Tricyclic lactam and sultam derivatives and their use as histone deacetylase inhibitors 失效三环内酰胺和苏丹衍生物及其作为组蛋白脱乙酰酶抑制剂的用途公开(公告)号：US07091229B2
公开(公告)日：2006-08-15
申请号：US10470121
申请日：2002-01-24
IPC分类号： A61K31/425 , A61K31/403 , C07D275/06 , C07D209/56
CPC分类号： C07D275/06 , C07D209/92
摘要： A compound of formula (I) wherein A and B are optionally substituted cyclohexenyl or phenyl groups, X is carbonyl or sulfonyl, and Y is 5–7 atoms-linker, is useful as histone deacetylase inhibitors, particularly for inhibiting cell proliferation.
摘要翻译： 式（I）的化合物，其中A和B为任选取代的环己烯基或苯基，X为羰基或磺酰基，Y为5-7个原子的连接体，可用作组蛋白脱乙酰酶抑制剂，尤其用于抑制细胞增殖。
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公开(公告)号：US06531472B2
公开(公告)日：2003-03-11
申请号：US10006173
申请日：2001-12-04
IPC分类号： A61K3140
CPC分类号： C07D295/116 , C07C259/06 , C07C2601/02 , C07C2602/10 , C07D213/50 , Y02P20/55
摘要： The present invention provides compounds of formula I and pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, X and Y have the meanings defined in the specification. The compounds have histone deacetylase (HDAC) inhibitory activity which is useful in cancer treatment. Also provided is a process for making a compound of formula I by reacting a compound of formula III with a compound of formula IV wherein A is a displaceable group and PG is a protecting group.
摘要翻译： 本发明提供式I化合物和药学上可接受的盐，其中R1，R2，R3，R4，R5，X和Y具有本说明书中定义的含义。 该化合物具有可用于癌症治疗的组蛋白脱乙酰酶（HDAC）抑制活性。 还提供了通过使式III化合物与式IV化合物反应制备式I化合物的方法，其中A是可置换基团，PG是保护基团。
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公开(公告)号：US09783570B2
公开(公告)日：2017-10-10
申请号：US14127085
申请日：2012-06-28
CPC分类号： C07K1/165 , C07K1/18 , C07K1/20 , C07K1/36 , C07K14/5443 , C07K2319/30
摘要： Herein is reported a method for obtaining a polypeptide in monomeric form comprising the steps of a) providing a solution comprising the polypeptide m monomeric form and m aggregated form, wherein the ratio of monomeric to aggregated form is 4:1 or less as determined by size exclusion chromatography, b) performing a mixed-mode chromatography in bind-and-elute mode, or a hydrophobic interaction chromatography in flow-through mode, or a size-exclusion chromatography, and c) performing a weak cation exchange chromatography in bind-and-elute mode or flow-through mode, and thereby obtaining the polypeptide m monomeric form.
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公开(公告)号：US20110086026A1
公开(公告)日：2011-04-14
申请号：US12843225
申请日：2010-07-26
申请人： Josef Endl , Maria Elena Fuentes , Yvo Graus , Adelbert Grossmann , Sebastian Neumann , Paul Parren , Frank Rebers , Joerg Thomas Regula , Ralf Schumacher , Stefan Seeber , Jan Olaf Stracke , Kay-Gunnar Stubenrauch , Jan Van De Winkel , Martine Van Vugt , Sandra Vereecken-Verploegen
发明人： Josef Endl , Maria Elena Fuentes , Yvo Graus , Adelbert Grossmann , Sebastian Neumann , Paul Parren , Frank Rebers , Joerg Thomas Regula , Ralf Schumacher , Stefan Seeber , Jan Olaf Stracke , Kay-Gunnar Stubenrauch , Jan Van De Winkel , Martine Van Vugt , Sandra Vereecken-Verploegen
IPC分类号： A61K39/395 , C07H21/00 , C07K16/00 , A61P11/06 , A61P37/02 , C12N5/10 , C12P21/02 , C12N15/63 , C12N1/00
CPC分类号： C07K16/2866 , C07K2317/21 , C07K2317/56 , C07K2317/76
摘要： An antibody binding to IL-13Rα1, inhibiting IL-13 bioactivity and comprising a variable heavy and a variable light chain, characterized in that the variable heavy chain amino acid sequence CDR3 of said antibody is selected from the group consisting of the heavy chain CDR3 sequences of SEQ ID NO: 1, 3, 5, 7 or 9 is useful in the treatment of asthma and allergic diseases.
摘要翻译： 与IL-13Rα1结合的抗体，抑制IL-13生物活性并包含可变重链和可变轻链的抗体，其特征在于所述抗体的可变重链氨基酸序列CDR3选自重链CDR3序列 的SEQ ID NO：1,3,5,7或9可用于治疗哮喘和过敏性疾病。
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公开(公告)号：US20100203589A1
公开(公告)日：2010-08-12
申请号：US12765229
申请日：2010-04-22
IPC分类号： C12P21/02
CPC分类号： C07K14/48
摘要： The invention relates to a method for producing biologically active β-NGF from the proform proNGF. After expressing the proform of the β-NGF in a prokaryotic host cell, the recombinant protein is isolated in the form of insoluble inactive aggregates (inclusion bodies). After the solubilization thereof in a strong denaturing agent and the subsequent conversion thereof into the natural conformation, which is determined by the disulfide bridges present in the natural β-NGF, biologically active β-NGF is obtained by subsequently splitting-off the prosequence.
摘要翻译： 本发明涉及从前体proNGF生产生物活性的NGF的方法。 在原核宿主细胞中表达生物素-NGF的形式后，重组蛋白以不溶性非活性聚集体（包涵体）的形式分离。 在将其溶解在强变性剂中并随后转化成通过存在于天然和/或生长因子中的二硫键确定的天然构象后，通过随后分离前体 。
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公开(公告)号：US07541163B2
公开(公告)日：2009-06-02
申请号：US11838730
申请日：2007-08-14
申请人： Phillip A. Patten , Sridhar Viswanathan , Torben Lauesgaard Nissen , Anne Vogt , Harald Kropshofer , Ralf Schumacher , Stephan Fischer , Stefan Seeber , Adelbert Grossmann , Friederike Hesse
发明人： Phillip A. Patten , Sridhar Viswanathan , Torben Lauesgaard Nissen , Anne Vogt , Harald Kropshofer , Ralf Schumacher , Stephan Fischer , Stefan Seeber , Adelbert Grossmann , Friederike Hesse
CPC分类号： A61K38/212 , A61K47/60 , C07K14/56 , Y02A50/463
摘要： The present invention provides interferon-alpha polypeptides and conjugates, and nucleic acids encoding the polypeptides. The invention also includes compositions comprising these polypeptides, conjugates, and nucleic acids; cells containing or expressing the polypeptides, conjugates, and nucleic acids; methods of making the polypeptides, conjugates, and nucleic acids; and methods of using the polypeptides, conjugates, and nucleic acids.
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公开(公告)号：US20070025966A1
公开(公告)日：2007-02-01
申请号：US11531557
申请日：2006-09-13
申请人： Phillip Patten , Sridhar Viswanathan , Torben Nissen , Anne Vogt , Harald Kropshofer , Ralf Schumacher , Stephan Fischer , Stefan Seeber , Adelbert Grossmann , Friederike Hesse , Andreas Schaubmar , Roberto Falkenstein , Hans Koll , Markus Dembowski
发明人： Phillip Patten , Sridhar Viswanathan , Torben Nissen , Anne Vogt , Harald Kropshofer , Ralf Schumacher , Stephan Fischer , Stefan Seeber , Adelbert Grossmann , Friederike Hesse , Andreas Schaubmar , Roberto Falkenstein , Hans Koll , Markus Dembowski
CPC分类号： A61K38/212 , A61K47/60 , C07K14/56 , Y02A50/463
摘要： The present invention provides interferon-alpha polypeptides and conjugates, and nucleic acids encoding the polypeptides. The invention also includes compositions comprising these polypeptides, conjugates, and nucleic acids; cells containing or expressing the polypeptides, conjugates, and nucleic acids; methods of making the polypeptides, conjugates, and nucleic acids; and methods of using the polypeptides, conjugates, and nucleic acids.
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10.发明申请公开(公告)号：US20140142283A1
公开(公告)日：2014-05-22
申请号：US14127085
申请日：2012-06-28
CPC分类号： C07K1/165 , C07K1/18 , C07K1/20 , C07K1/36 , C07K14/5443 , C07K2319/30
摘要： The present invention relates to methods for obtaining a polypeptide in a monomeric form, the method comprising a) providing a solution containing the polypeptide in monomeric form and in aggregated form, wherein the ratio of monomeric to aggregated form is 4:1 or less, as determined by size exclusion chromatography, b) performing mixed-mode chromatography in bind-and-elute mode, or hydrophobic interaction chromatography in flow-through mode, or a size-exclusion chromatography, and c) performing a weak cation exchange chromatography in bind-and-elute mode or flow-through mode, and thereby obtaining the polypeptide in monomeric form.
摘要翻译： 本发明涉及以单体形式获得多肽的方法，所述方法包括：a）提供含有单体形式和聚集形式的多肽的溶液，其中单体与聚集形式的比例为4:1或更低，如 通过尺寸排阻色谱法确定，b）以结合 - 洗脱模式进行混合模式色谱法，或以流通模式或尺寸排阻色谱法进行疏水相互作用层析，以及c）在结合 - 洗脱模式或流通模式，从而获得单体形式的多肽。
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