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    Substituted 2-pyrrolidinone activators of PKC
    41.
    发明授权
    Substituted 2-pyrrolidinone activators of PKC 失效
    PKC的取代的2-吡咯烷酮激活剂

    公开(公告)号：US5962504A

    公开(公告)日：1999-10-05

    申请号：US149609

    申请日：1998-09-08

    Applicant: Alan P. Kozikowski ,  Shaomeng Wang ,  Lixin Qiao

    Inventor： Alan P. Kozikowski ,  Shaomeng Wang ,  Lixin Qiao

    IPC: A61K31/4015 ,  A61P35/00 ,  A61P43/00 ,  C07D207/26 ,  C07D498/04 ,  A61K31/40

    CPC classification number: C07D207/26

    Abstract: Compounds of formula I: ##STR1## wherein R.sub.1 and R.sub.2 have any of the values defined in the specification, and their pharmaceutically acceptable salts, are PKC activators and are useful for treating diseases, such as, for example, cancer. Also disclosed are pharmaceutical compositions comprising compounds of formula I, processes for preparing compounds of formula I, and intermediates useful for preparing compounds of formula I.

    Abstract translation: 式I化合物：其中R 1和R 2具有说明书中定义的任何值及其药学上可接受的盐，是PKC激活剂，并且可用于治疗疾病，例如癌症。 还公开了包含式I化合物，式I化合物的方法和可用于制备式I化合物的中间体的药物组合物。

    Small molecule antagonists of Bcl-2 family proteins
    47.
    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

    Applicant: Shaomeng Wang ,  Dajun Yang ,  Liang Xu

    Inventor： Shaomeng Wang ,  Dajun Yang ,  Liang Xu

    IPC: A61K31/12

    CPC classification number: A61K31/11 ,  A61K45/06 ,  A61K2300/00

    Abstract: 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.

    Abstract translation: 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。

    Matriptase, a serine protease and its applications
    48.
    发明授权
    Matriptase, a serine protease and its applications 有权
    Matriptase，丝氨酸蛋白酶及其应用

    公开(公告)号：US07960163B2

    公开(公告)日：2011-06-14

    申请号：US12040467

    申请日：2008-02-29

    Applicant: Robert B. Dickson ,  Chen-Yong Lin ,  Michael Johnson ,  Shaomeng Wang ,  Istvan Enyedy

    Inventor： Robert B. Dickson ,  Chen-Yong Lin ,  Michael Johnson ,  Shaomeng Wang ,  Istvan Enyedy

    IPC: C12N9/00 ,  C12N9/50 ,  C12N1/20 ,  C12N15/00 ,  C07H21/04

    CPC classification number: A61K49/0039 ,  A61K38/00 ,  A61K49/0056 ,  A61K49/0058 ,  A61K51/10 ,  C12Q1/37 ,  G01N33/573 ,  G01N2333/96433 ,  G01N2500/20

    Abstract: The invention is directed to a method of detecting a malignancy or a pre-malignant lesion in breast or other tissue, or a pathologic condition, by detecting the presence of single-chain or two-chain forms of matriptase in the tissue. The invention is further directed to a method of treating malignancies, which have the phenotype of matriptase production by administering a tumor formation inhibiting effective amount of concentrate of Bowman-Birk inhibitor (BBIC), or other matriptase inhibitor. The invention also is directed to nucleic acids encoding a matriptase protein or fragments thereof, and their use for structure elucidation and modeling to identify other inhibitors of matriptase, as well as to methods of identifying matriptase modulating agents, including activators and inhibitors.

    Abstract translation: 本发明涉及通过检测组织中单链或双链形式的matriptase的存在来检测乳腺或其他组织或病理状况中的恶性肿瘤或恶性前病变的方法。 本发明进一步涉及通过施用抑制有效量的Bowman-Birk抑制剂（BBIC）浓缩物或其它片剂酶抑制剂的肿瘤形成来治疗恶性肿瘤的方法，所述恶性肿瘤具有基质酶产生的表型。 本发明还涉及编码matriptase蛋白质或其片段的核酸，以及其用于结构阐明和建模以鉴定其它抑制剂的用途，以及鉴定片段酶调节剂（包括活化剂和抑制剂）的方法。

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