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    ErbB-2 selective small molecule kinase inhibitors
    2.
    发明授权
    ErbB-2 selective small molecule kinase inhibitors 失效
    ErbB-2选择性小分子激酶抑制剂

    公开(公告)号：US07427689B2

    公开(公告)日：2008-09-23

    申请号：US10343267

    申请日：2001-07-30

    申请人： Shaomeng Wang ,  Dajun Yang ,  Istvan Enyedy

    发明人： Shaomeng Wang ,  Dajun Yang ,  Istvan Enyedy

    IPC分类号： C07C205/00

    CPC分类号： A61K31/216 ,  A61K31/00 ,  A61K31/192

    摘要： A novel method for erbB-2 kinase inhibition by compounds identifies through computational modeling and data processing and/or rational and de novo drug design is provided the compounds bind erbB-2 kinase molecules and which can be used as erbB-2 kinase agonists or antagonists. These compounds are useful especially in the treatment of cancer, particularly breast cancer, and can be used alone or in combination with other chemotherapeutic agents, particularly with hercetin, a humanized anti-HER-2 antibody, or with radiation therapy. A specific compound which is exemplified is “compound B17”=methyl-(p-nitrophenyl)-2-propynoate.

    摘要翻译： 化合物的erbB-2激酶抑制的新方法通过计算建模和数据处理鉴定，和/或合理和从头药物设计提供了化合物结合erbB-2激酶分子，并且其可以用作erbB-2激酶激动剂或拮抗剂 。 这些化合物特别用于治疗癌症，特别是乳腺癌，并且可以单独使用或与其它化学治疗剂，特别是与赫氏原，人源化抗HER-2抗体或放射治疗组合使用。 例示的具体化合物是“化合物B17”=甲基 - （对硝基苯基）-2-丙炔酸酯。

    SMALL MOLECULE ANTAGONISTS OF BCL-2 FAMILY PROTEINS
    3.
    发明申请
    SMALL MOLECULE ANTAGONISTS OF BCL-2 FAMILY PROTEINS 有权

    公开(公告)号：US20090092684A1

    公开(公告)日：2009-04-09

    申请号：US12242380

    申请日：2008-09-30

    申请人： Shaomeng Wang ,  Dajun Yang ,  Liang Xu

    发明人： Shaomeng Wang ,  Dajun Yang ,  Liang Xu

    IPC分类号： A61K31/12 ,  A61P35/00 ,  A61K33/24 ,  A61K31/337

    CPC分类号： A61K31/11 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-XL, and the like). The present invention also provides compositions comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents). The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases) comprising administering a composition comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents) and/or techniques (e.g., radiation therapies, surgical interventions, and the like) to a subject or in vitro cells, tissues, and organs.

    SMALL MOLECULE ANTAGONISTS OF BCL2 FAMILY PROTEINS
    4.
    发明申请
    SMALL MOLECULE ANTAGONISTS OF BCL2 FAMILY PROTEINS 审中-公开
    BCL2家族蛋白的小分子拮抗剂

    公开(公告)号：US20100069344A1

    公开(公告)日：2010-03-18

    申请号：US12609761

    申请日：2009-10-30

    申请人： Shaomeng Wang ,  Dajun Yang ,  Liang Xu

    发明人： Shaomeng Wang ,  Dajun Yang ,  Liang Xu

    IPC分类号： A61K31/573 ,  A61P35/00

    CPC分类号： A61K31/11 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-XL, and the like). The present invention also provides compositions comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents). The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases) comprising administering a composition comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents) and/or techniques (e.g., radiation therapies, surgical interventions, and the like) to a subject or in vitro cells, tissues, and organs.

    摘要翻译： 本发明涉及Bcl-2家族蛋白质的天然存在和化学合成的小分子拮抗剂。 特别地，本发明提供了棉酚化合物（例如异构体，对映异构体，外消旋化合物，代谢物，衍生物，药学上可接受的盐，与酸或碱的组合等）和使用这些化合物作为抗 - Bcl-2家族蛋白（如Bcl-2，Bcl-XL等）的凋亡作用。 本发明还提供包含棉酚化合物和任选的一种或多种另外的治疗剂（例如抗癌/化学治疗剂）的组合物。 本发明还提供了治疗疾病和病症（例如，肿瘤疾病）的方法，包括施用包含棉酚化合物和任选的一种或多种另外的治疗剂（例如抗癌/化学治疗剂）和/或技术（例如，放射疗法， 外科手术等）到受试者或体外细胞，组织和器官。

    Small molecule inhibitors targeted at Bcl-2
    6.
    发明授权
    Small molecule inhibitors targeted at Bcl-2 有权
    针对Bcl-2的小分子抑制剂

    公开(公告)号：US07354928B2

    公开(公告)日：2008-04-08

    申请号：US10286085

    申请日：2002-11-01

    申请人： Shaomeng Wang ,  Dajun Yang ,  Istvan J. Enyedy

    发明人： Shaomeng Wang ,  Dajun Yang ,  Istvan J. Enyedy

    IPC分类号： A61K31/44 ,  A61K31/335 ,  A61K31/135 ,  A61K31/505 ,  A61K31/65

    CPC分类号： A61K45/06 ,  A61K31/00 ,  A61K31/122 ,  A61K31/395 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/444 ,  A61K31/452 ,  A61K31/473 ,  A61K31/4745 ,  A61K31/519 ,  A61K31/655 ,  A61K2300/00

    摘要： The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-XL. In particular, the present invention provides non-peptide cell permeable small molecules (e.g., tricyclo-dibenzo-diazocine-dioxides) that bind to a pocket in Bcl-2/Bcl-XL that block the anti-apoptotic function of these proteins in cancer cells and tumor tissues exhibiting Bcl-2 protein overexpression. In preferred embodiments, the small molecules of the present invention are active at the BH3 binding pocket of Bcl-2 family proteins (e.g., Bcl-2, Bcl-XL, and Mcl-1). The compositions and methods of the present invention are useful therapeutics for cancerous diseases either alone or in combination with chemotherapeutic or other drugs.

    摘要翻译： 本发明涉及Bcl-2家族蛋白质如Bcl-2和/或Bcl-X L的小分子拮抗剂。 特别地，本发明提供了结合Bcl-2 / Bcl-XLL中的口袋的非肽细胞可渗透的小分子（例如三环二苯并二氮杂二恶英），其阻断抗 这些蛋白在癌细胞和表达Bcl-2蛋白过表达的肿瘤组织中的凋亡功能。 在优选的实施方案中，本发明的小分子在Bcl-2家族蛋白（例如Bcl-2，Bcl-X L和Mcl-1）的BH3结合口袋上是有活性的。 本发明的组合物和方法单独或与化学治疗剂或其它药物组合用于癌性疾病的有用治疗剂。

    SMALL MOLECULE ANTAGONISTS OF BCL-2 FAMILY PROTEINS
    8.
    发明申请
    SMALL MOLECULE ANTAGONISTS OF BCL-2 FAMILY PROTEINS 审中-公开
    BCL-2家族蛋白的小分子拮抗剂

    公开(公告)号：US20090082424A1

    公开(公告)日：2009-03-26

    申请号：US12242388

    申请日：2008-09-30

    申请人： Shaomeng Wang ,  Dajun Yang ,  Liang Xu

    发明人： Shaomeng Wang ,  Dajun Yang ,  Liang Xu

    IPC分类号： A61K31/11 ,  A61K31/337 ,  A61P35/02 ,  A61P35/04 ,  A61P35/00

    CPC分类号： A61K31/11 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-XL, and the like). The present invention also provides compositions comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents). The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases) comprising administering a composition comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents) and/or techniques (e.g., radiation therapies, surgical interventions, and the like) to a subject or in vitro cells, tissues, and organs.

    摘要翻译： 本发明涉及Bcl-2家族蛋白质的天然存在和化学合成的小分子拮抗剂。 特别地，本发明提供了棉酚化合物（例如异构体，对映异构体，外消旋化合物，代谢物，衍生物，药学上可接受的盐，与酸或碱的组合等）和使用这些化合物作为抗 - Bcl-2家族蛋白（如Bcl-2，Bcl-XL等）的凋亡作用。 本发明还提供包含棉酚化合物和任选的一种或多种另外的治疗剂（例如抗癌/化学治疗剂）的组合物。 本发明还提供了治疗疾病和病症（例如，肿瘤疾病）的方法，包括施用包含棉酚化合物和任选的一种或多种另外的治疗剂（例如抗癌/化学治疗剂）和/或技术（例如，放射疗法， 外科手术等）到受试者或体外细胞，组织和器官。

    Small molecule antagonists of Bcl-2 family proteins
    9.
    发明授权
    Small molecule antagonists of Bcl-2 family proteins 有权
    Bcl-2家族蛋白的小分子拮抗剂

    公开(公告)号：US07432304B2

    公开(公告)日：2008-10-07

    申请号：US10729156

    申请日：2003-12-05

    申请人： Shaomeng Wang ,  Dajun Yang ,  Liang Xu

    发明人： Shaomeng Wang ,  Dajun Yang ,  Liang Xu

    IPC分类号： A61K31/12

    CPC分类号： A61K31/11 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-XL, and the like). The present invention also provides compositions comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents). The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases) comprising administering a composition comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents) and/or techniques (e.g., radiation therapies, surgical interventions, and the like) to a subject or in vitro cells, tissues, and organs.

    摘要翻译： 本发明涉及Bcl-2家族蛋白质的天然存在和化学合成的小分子拮抗剂。 特别地，本发明提供了棉酚化合物（例如异构体，对映异构体，外消旋化合物，代谢物，衍生物，药学上可接受的盐，与酸或碱的组合等）和使用这些化合物作为抗 - Bcl-2家族蛋白（例如Bcl-2，Bcl-XL等）的凋亡作用。 本发明还提供包含棉酚化合物和任选的一种或多种另外的治疗剂（例如抗癌/化学治疗剂）的组合物。 本发明还提供了治疗疾病和病症（例如，肿瘤疾病）的方法，包括施用包含棉酚化合物和任选的一种或多种另外的治疗剂（例如抗癌/化学治疗剂）和/或技术的组合物（例如，放射疗法， 外科手术等）到受试者或体外细胞，组织和器官。

    Small molecule antagonists of Bcl-2 family proteins
    10.
    发明授权
    Small molecule antagonists of Bcl-2 family proteins 有权
    Bcl-2家族蛋白的小分子拮抗剂

    公开(公告)号：US08163805B2

    公开(公告)日：2012-04-24

    申请号：US12242380

    申请日：2008-09-30

    申请人： Shaomeng Wang ,  Dajun Yang ,  Liang Xu

    发明人： Shaomeng Wang ,  Dajun Yang ,  Liang Xu

    IPC分类号： A61K31/12

    CPC分类号： A61K31/11 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-XL, and the like). The present invention also provides compositions comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents). The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases) comprising administering a composition comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents) and/or techniques (e.g., radiation therapies, surgical interventions, and the like) to a subject or in vitro cells, tissues, and organs.

    摘要翻译： 本发明涉及Bcl-2家族蛋白质的天然存在和化学合成的小分子拮抗剂。 特别地，本发明提供了棉酚化合物（例如异构体，对映异构体，外消旋化合物，代谢物，衍生物，药学上可接受的盐，与酸或碱的组合等）和使用这些化合物作为抗 - Bcl-2家族蛋白（如Bcl-2，Bcl-XL等）的凋亡作用。 本发明还提供包含棉酚化合物和任选的一种或多种另外的治疗剂（例如抗癌/化学治疗剂）的组合物。 本发明还提供了治疗疾病和病症（例如，肿瘤疾病）的方法，包括施用包含棉酚化合物和任选的一种或多种另外的治疗剂（例如抗癌/化学治疗剂）和/或技术（例如，放射疗法， 外科手术等）到受试者或体外细胞，组织和器官。