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    PROCESS FOR THE PREPARATION OF 3,4-DISUBSTITUTED-THIAZOLIDIN-2-ONES
    2.
    发明申请
    PROCESS FOR THE PREPARATION OF 3,4-DISUBSTITUTED-THIAZOLIDIN-2-ONES 失效
    制备3,4代替噻唑烷-2-酮的方法

    公开(公告)号：US20080287683A1

    公开(公告)日：2008-11-20

    申请号：US12182918

    申请日：2008-07-30

    申请人： Jonathan B. DeCamp ,  Paul S. Watson ,  Jin She

    发明人： Jonathan B. DeCamp ,  Paul S. Watson ,  Jin She

    IPC分类号： C07D277/04

    CPC分类号： C07D277/14 ,  C07C319/06 ,  C07C323/58

    摘要： The present invention is directed to practical high-yielding synthetic processes for preparing 3,4-disubstituted-thiazolidin-2-ones, which do not compromise the absolute stereochemical integrity of the compounds. The present invention is also directed to novel compounds of 3,4-disubstituted-thiazolidin-2-ones. The compounds prepared by the present invention are useful in the synthesis and manufacture of compounds (such as latrunculins and/or their analogs) for treating diseases or conditions associated with inhibiting actin polymerization.

    摘要翻译： 本发明涉及用于制备3,4-二取代 - 噻唑烷-2-酮的实用的高产合成方法，其不损害化合物的绝对立体化学完整性。 本发明还涉及3,4-二取代 - 噻唑烷-2-酮的新化合物。 通过本发明制备的化合物可用于合成和制备用于治疗与抑制肌动蛋白聚合相关的疾病或病症的化合物（例如软核灰蛋白和/或其类似物）。

    Process for the preparation of 3,4-disubstituted-thiazolidin-2-ones
    3.
    发明授权
    Process for the preparation of 3,4-disubstituted-thiazolidin-2-ones 失效
    制备3,4-二取代 - 噻唑烷-2-酮的方法

    公开(公告)号：US07947850B2

    公开(公告)日：2011-05-24

    申请号：US12182918

    申请日：2008-07-30

    申请人： Jonathan B. DeCamp ,  Paul S. Watson ,  Jin She

    发明人： Jonathan B. DeCamp ,  Paul S. Watson ,  Jin She

    IPC分类号： C07C323/58

    CPC分类号： C07D277/14 ,  C07C319/06 ,  C07C323/58

    摘要： The present invention is directed to practical high-yielding synthetic processes for preparing 3,4-disubstituted-thiazolidin-2-ones, which do not compromise the absolute stereochemical integrity of the compounds. The present invention is also directed to novel compounds of 3,4-disubstituted-thiazolidin-2-ones. The compounds prepared by the present invention are useful in the synthesis and manufacture of compounds (such as latrunculins and/or their analogs) for treating diseases or conditions associated with inhibiting actin polymerization.

    摘要翻译： 本发明涉及用于制备3,4-二取代 - 噻唑烷-2-酮的实用的高产合成方法，其不损害化合物的绝对立体化学完整性。 本发明还涉及3,4-二取代 - 噻唑烷-2-酮的新化合物。 通过本发明制备的化合物可用于合成和制备用于治疗与抑制肌动蛋白聚合相关的疾病或病症的化合物（例如软核灰蛋白和/或其类似物）。

    Process for the preparation of 3,4-disubstituted-thiazolidin-2-ones
    4.
    发明授权
    Process for the preparation of 3,4-disubstituted-thiazolidin-2-ones 失效
    制备3,4-二取代 - 噻唑烷-2-酮的方法

    公开(公告)号：US07414137B2

    公开(公告)日：2008-08-19

    申请号：US11690048

    申请日：2007-03-22

    申请人： Jonathan B. DeCamp ,  Paul S. Watson ,  Jin She

    发明人： Jonathan B. DeCamp ,  Paul S. Watson ,  Jin She

    IPC分类号： C07D277/56

    CPC分类号： C07D277/14 ,  C07C319/06 ,  C07C323/58

    摘要： The present invention is directed to practical high-yielding synthetic processes for preparing 3,4-disubstituted-thiazolidin-2-ones, which do not compromise the absolute stereochemical integrity of the compounds. The present invention is also directed to novel compounds of 3,4-disubstituted-thiazolidin-2-ones. The compounds prepared by the present invention are useful in the synthesis and manufacture of compounds (such as latrunculins and/or their analogs) for treating diseases or conditions associated with inhibiting actin polymerization.

    摘要翻译： 本发明涉及用于制备3,4-二取代 - 噻唑烷-2-酮的实用的高产合成方法，其不损害化合物的绝对立体化学完整性。 本发明还涉及3,4-二取代 - 噻唑烷-2-酮的新化合物。 通过本发明制备的化合物可用于合成和制备用于治疗与抑制肌动蛋白聚合相关的疾病或病症的化合物（例如软核灰蛋白和/或其类似物）。

    Cytoskeletal active compounds, composition and use
    5.
    发明授权
    Cytoskeletal active compounds, composition and use 失效
    细胞骨架活性化合物，组成和用途

    公开(公告)号：US08039465B2

    公开(公告)日：2011-10-18

    申请号：US12695348

    申请日：2010-01-28

    申请人： John W. Lampe ,  Robert Plourde, Jr. ,  Jin She ,  Jason L. Vittitow ,  Paul S. Watson ,  Michael T. Crimmins ,  David J. Slade

    发明人： John W. Lampe ,  Robert Plourde, Jr. ,  Jin She ,  Jason L. Vittitow ,  Paul S. Watson ,  Michael T. Crimmins ,  David J. Slade

    IPC分类号： A61K31/54

    CPC分类号： C07D491/08 ,  C07D277/06 ,  C07D277/14 ,  C07D277/16 ,  C07D277/34 ,  C07D277/56 ,  C07D417/04 ,  C07D493/08 ,  C07D497/18

    摘要： The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.

    摘要翻译： 本发明涉及与天然的秋水仙素A或梭菌素B相关的合成细胞骨架活性化合物。本发明还涉及包含这些化合物和药学上可接受的载体的药物组合物。 本发明另外涉及预防或治疗与肌动蛋白聚合相关的疾病或病症的方法。 在本发明的一个实施方案中，该方法治疗增加的眼内压，例如原发性开角型青光眼。 该方法包括向受试者施用治疗有效量的式I或II的细胞骨架活性化合物，其中所述量有效影响细胞骨架，例如通过抑制肌动蛋白聚合。

    Branched linker for protein drug conjugates
    8.
    发明授权
    Branched linker for protein drug conjugates 有权

    公开(公告)号：US10294270B2

    公开(公告)日：2019-05-21

    申请号：US14001237

    申请日：2012-02-23

    申请人： Laurent Ducry ,  Bernhard Stump ,  Heilam Wong ,  Jin She ,  Gayle Allway

    发明人： Laurent Ducry ,  Bernhard Stump ,  Heilam Wong ,  Jin She ,  Gayle Allway

    IPC分类号： A61K47/60 ,  A61K47/64 ,  A61K47/65 ,  A61K47/68 ,  C07K5/062

    摘要： The present invention relates to method for connecting a protein and a drug to a protein drug conjugate, wherein the drug is linked to the protein through a specific branched linker, said branched linker comprises a peptide chain and is derived from o-hydroxy p-amino benzylic alcohol, wherein the peptide chain is connected to the phenyl ring via the p-amino group, the drug is connected to the phenyl ring via the benzylic alcohol moiety, and the protein is connected to the phenyl ring via the o-hydroxy group; further to a process for the preparation of said protein-drug-conjugates via various intermediates, to the pharmaceutical use of such protein drug conjugates, such as methods of controlling the growth of undesirable cells, to pharmaceutical compositions comprising such protein drug conjugates, and to intermediates of the preparation of the protein drug conjugates.

    Branched Linker for Protein Drug Conjugates
    9.
    发明申请
    Branched Linker for Protein Drug Conjugates 审中-公开
    蛋白质药物缀合物的分支连接子

    公开(公告)号：US20130324706A1

    公开(公告)日：2013-12-05

    申请号：US14001237

    申请日：2012-02-23

    申请人： Laurent Ducry ,  Bernhard Stump ,  Heilam Wong ,  Jin She ,  Gayle Phillips

    发明人： Laurent Ducry ,  Bernhard Stump ,  Heilam Wong ,  Jin She ,  Gayle Phillips

    IPC分类号： A61K47/48 ,  C07K5/062

    CPC分类号： C07K5/06043 ,  A61K47/60 ,  A61K47/64 ,  A61K47/65 ,  A61K47/6809 ,  A61K47/6845

    摘要： The present invention relates to method for connecting a protein and a drug to a protein drug conjugate, wherein the drug is linked to the protein through a specific branched linker, said branched linker comprises a peptide chain and is derived from o-hydroxy p-amino benzylic alcohol, wherein the peptide chain is connected to the phenyl ring via the p-amino group, the drug is connected to the phenyl ring via the benzylic alcohol moiety, and the protein is connected to the phenyl ring via the o-hydroxy group; further to a process for the preparation of said protein-drug-conjugates via various intermediates, to the pharmaceutical use of such protein drug conjugates, such as methods of controlling the growth of undesirable cells, to pharmaceutical compositions comprising such protein drug conjugates, and to intermediates of the preparation of the protein drug conjugates.

    摘要翻译： 本发明涉及将蛋白质和药物连接到蛋白质药物缀合物的方法，其中药物通过特定的支链接头与蛋白质连接，所述支链接头包含肽链，并衍生自邻羟基对氨基 苄基醇，其中肽链通过对氨基与苯环连接，药物通过苄醇部分连接到苯环，并且蛋白质通过邻羟基连接到苯环上; 进一步涉及通过各种中间体制备所述蛋白质 - 药物偶联物的方法，将这种蛋白质药物偶联物的药物用途，例如控制不期望细胞生长的方法用于包含这种蛋白质药物偶联物的药物组合物，以及 中间体制备蛋白质药物偶联物。

    Process for the preparation of Rho-kinase inhibitor compounds
    10.
    发明授权
    Process for the preparation of Rho-kinase inhibitor compounds 失效
    制备Rho激酶抑制剂化合物的方法

    公开(公告)号：US08158796B2

    公开(公告)日：2012-04-17

    申请号：US12470377

    申请日：2009-05-21

    申请人： Jin She ,  Jonathan Bryan deCamp ,  Paul S. Watson ,  David J. Slade

    发明人： Jin She ,  Jonathan Bryan deCamp ,  Paul S. Watson ,  David J. Slade

    IPC分类号： C07D217/22

    CPC分类号： C07D401/12 ,  C07C67/08 ,  C07C69/78

    摘要： The present invention is directed to practical high-yielding synthetic processes to prepare compounds of general Formula III, IV, V, VII, VIII, IX, X, XII, XIV, and XV. Such compounds are useful as final products or can be used as intermediates and be further modified to prepare other desired products such as rho-kinase inhibitors. The present invention is also directed to certain novel compounds and/or novel solid forms of certain compounds.

    摘要翻译： 本发明涉及制备通式III，IV，V，VII，VIII，IX，X，XII，XIV和XV的化合物的实际高产合成方法。 这些化合物可用作最终产物，或可用作中间体，并进一步修饰以制备其它所需产物如rho激酶抑制剂。 本发明还涉及某些新化合物和/或某些化合物的新型固体形式。