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    Small molecule inhibitors targeted at Bcl-2
    61.
    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：US06703382B2

    公开(公告)日：2004-03-09

    申请号：US09930237

    申请日：2001-08-16

    Applicant: Shaomeng Wang ,  Dajun Yang ,  Istvan J. Enyedy

    Inventor： Shaomeng Wang ,  Dajun Yang ,  Istvan J. Enyedy

    IPC: A61K31655

    CPC classification number: A61K31/655 ,  A61K31/675 ,  A61K31/70 ,  A61K33/24 ,  A61K45/06 ,  A61K2300/00

    Abstract: A method for promotion of cell death in tumor cells using tricylo-dibenzo-diazocine-dioxides that bind to a pocket of Bcl-2 and block the Bcl-2 anti-apoptotic function. A method of use of a compound of the general structural Formula (I) for use in treatment of cancer: wherein X and Y, and R and R1, and R2, R3, R4 and R5, and A and A1, have any of the values defined in the specification.

    Abstract translation: 使用结合Bcl-2的口袋并阻断Bcl-2抗凋亡功能的三羟甲基 - 二苯并二氮杂环己烷二氧化物促进肿瘤细胞中细胞死亡的方法。 使用通式（I）化合物用于治疗癌症的方法：其中X和Y，以及R和R 1，R 2，R 3，R 4和R 5以及A和A 1具有 规范中定义的值。

    Substituted 2-pyrrolidinone activators of PKC
    62.
    发明授权
    Substituted 2-pyrrolidinone activators of PKC 有权
    PKC的取代的2-吡咯烷酮激活剂

    公开(公告)号：US06284784B1

    公开(公告)日：2001-09-04

    申请号：US09339072

    申请日：1999-06-23

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

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

    IPC: A61K3140

    CPC classification number: C07D207/26

    Abstract: Compounds of formula I: wherein R1 and R2 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。

    Heregulin antagonists and methods for their use
    63.
    发明授权
    Heregulin antagonists and methods for their use 失效
    促胰岛素拮抗剂及其使用方法

    公开(公告)号：US6143740A

    公开(公告)日：2000-11-07

    申请号：US308396

    申请日：1999-08-16

    Applicant: Dajun Yang ,  Shaomeng Wang ,  Alan P. Kozikowski ,  Marc E. Lippman

    Inventor： Dajun Yang ,  Shaomeng Wang ,  Alan P. Kozikowski ,  Marc E. Lippman

    IPC: C07D498/18 ,  A61K31/34 ,  A61K31/395 ,  A61K31/495 ,  A61K31/496 ,  A61K31/551 ,  A61K31/655 ,  A61P35/00 ,  A61P43/00 ,  C07D498/08 ,  A61K31/33 ,  C07K1/00 ,  C07K16/00

    CPC classification number: A61K31/708 ,  A61K31/395 ,  A61K31/495 ,  A61K31/496 ,  A61K31/551 ,  A61K31/655 ,  A61K31/704 ,  A61K31/7076 ,  C07D498/08

    Abstract: The invention provides a method of inhibiting cancer cell growth, and thereby of treating cancer comprising administering to a mammal afflicted with cancer an effective amount of the compound of formula (I), wherein the variables of R.sub.1, and R.sub.2 have the meanings defined in the specification. The present invention also provides novel compounds of formula (I) as well as novel pharmaceutical compositions and intermediates useful for preparing compounds of formula (I). The figure illustrates the structure and binding activity of compounds of the invention and some of the rifamycin analogs.______________________________________ ##STR1## ______________________________________ Compounds R.sub.1 = ______________________________________ A1 --OH A2 --OH A3 --OH A4 --OH A5 --OH A6 --OH A7 --OH - A8 ##STR2## ______________________________________ Compounds R.sub.2 = ______________________________________ A1 #STR3## - A2 #STR4## - A3 #STR5## - A4 #STR6## - A5 #STR7## - A6 #STR8## - A7 #STR9## - A8 --H ______________________________________ Compounds IC.sub.50 (1) IC.sub.50 (2) ______________________________________ A1 10 uM 1 uM A2 10 uM 3 uM A3 10 uM 3 uM A4 50 uM 5 uM A5 >500 uM >50 uM A6 >500 uM >50 uM A7 >200 uM >50 uM A8 >500 M >50 uM ______________________________________

    Abstract translation: PCT No.PCT / US97 / 21474 Sec。 371日期1999年8月16日 102（e）1999年8月16日PCT 1997年11月19日PCT公布。 第WO98 / 21956号公报 日期1998年5月28日本发明提供抑制癌细胞生长，从而治疗癌症的方法，包括向患有癌症的哺乳动物施用有效量的式（I）化合物，其中R1和R2的变量具有 在本说明书中定义的含义。 本发明还提供新的式（I）化合物以及可用于制备式（I）化合物的新型药物组合物和中间体。 该图示出了本发明化合物和一些利福霉素类似物的结构和结合活性。 - 化合物R1 = -Al-OH-A2-OH-A3-OH-A4-OH-A5-OH-A6-OH-A7 -OH - - A8化合物R2 = 图像 - - A2 - - A3 - - A4 GE> - - A7 - - A8 -H - 化合物IC50（1）IC50（2） - A1 10 uM 1 uM - A2 10 uM 3 uM - A3 10 uM 3 uM - A4 50 uM 5 uM - A5> 500 uM> 50 uM - A6> 500 uM> 50 uM - A7> 200 uM> 50 uM - A8> 500 M> 50 uM -

    Bivalent diazo bicyclic Smac mimetics and the uses thereof
    65.
    发明授权
    Bivalent diazo bicyclic Smac mimetics and the uses thereof 有权
    二价重氮二环Smac模拟物及其用途

    公开(公告)号：US08815927B2

    公开(公告)日：2014-08-26

    申请号：US13503366

    申请日：2010-10-20

    Applicant: Shaomeng Wang ,  Haiying Sun

    Inventor： Shaomeng Wang ,  Haiying Sun

    IPC: C07D487/04 ,  C07D403/14 ,  C07D245/04 ,  C07D519/00

    CPC classification number: C07D519/00 ,  C07D487/04

    Abstract: The invention relates to diazo bicyclic Smac mimetics that are tethered through a covalent linker to give a bivalent species. Bivalent diazo bicyclic Smac mimetics function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs). The invention also relates to the use of bivalent diazo bicyclic Smac mimetics for inducing or sensitizing cells to the induction of apoptotic cell death. Thus, compounds of the invention are useful in the treatment, amelioration, or prevention of hyperproliferative diseases such as cancer.

    Abstract translation: 本发明涉及通过共价接头连接以产生二价物质的重氮二环Smac模拟物。 二价重氮双环Smac模拟物作为细胞凋亡蛋白抑制剂（IAP）的抑制剂起作用。 本发明还涉及二价重氮二环Smac模拟物用于诱导或致敏细胞诱导凋亡细胞死亡的用途。 因此，本发明的化合物可用于治疗，改善或预防过度增殖性疾病如癌症。

    Spiro-oxindole MDM2 antagonists
    66.
    发明授权
    Spiro-oxindole MDM2 antagonists 有权
    螺羟吲哚MDM2拮抗剂

    公开(公告)号：US08680132B2

    公开(公告)日：2014-03-25

    申请号：US13294315

    申请日：2011-11-11

    Applicant: Shaomeng Wang ,  Wei Sun

    Inventor： Shaomeng Wang ,  Wei Sun

    IPC: A61K31/4015 ,  C07D209/34

    CPC classification number: A61N5/10 ,  A61K31/407 ,  A61K45/06 ,  C07D487/10 ,  A61K2300/00

    Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.

    Abstract translation: 本文提供了药物化学领域中的化合物，组合物和方法。 本文提供的化合物和组合物涉及用作p53和MDM2之间相互作用的拮抗剂的螺 - 羟基吲哚，以及它们作为治疗癌症和其它疾病的治疗剂的用途。

    BIOMARKERS FOR GOSSYPOL CHEMOTHERAPY AND METHODS OF TREATING DISEASE
    68.
    发明申请
    BIOMARKERS FOR GOSSYPOL CHEMOTHERAPY AND METHODS OF TREATING DISEASE 审中-公开
    生物标记物治疗疾病和治疗疾病的方法

    公开(公告)号：US20120302629A1

    公开(公告)日：2012-11-29

    申请号：US13388610

    申请日：2010-07-28

    Applicant: Shaomeng Wang ,  Feng Jiang ,  Jianting Long ,  Longchuan Bai

    Inventor： Shaomeng Wang ,  Feng Jiang ,  Jianting Long ,  Longchuan Bai

    IPC: A61K31/11 ,  C12Q1/68 ,  A61P35/00 ,  A61K31/337 ,  A61P29/00 ,  A61P31/00 ,  A61P7/00 ,  A61P35/02 ,  G01N33/574 ,  A61P37/00

    CPC classification number: G01N33/57434 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/158 ,  G01N2800/52

    Abstract: The present invention provides a biomarker for selecting a patient for treatment with gossypol, wherein the biomarker comprises an elevated expression level of c-Myc, Mcl-1, or combination thereof, relative to the normal expression level of c-Myc, Mcl-1, or combination thereof. The present invention also provides methods for targeting patients for treatment with gossypol, wherein the patient has a disease, condition, or disorder that overexpresses c-Myc, Mcl-1, or combination thereof. The present invention also provides methods for treating or ameliorating a disease, condition, or disorder in a patient comprising determining the expression level of c-Myc, Mcl-1, or combination thereof in the patient and administering gossypol to the patient. In certain embodiments of the invention, the disease is cancer, and the cancer cells show elevated expression levels of c-Myc compared to non-cancerous cells. The invention also provides methods for overcoming Mcl-1-mediated chemoresistance comprising administering gossypol to a patient in need thereof.

    Abstract translation: 本发明提供了一种用于选择用棉酚处理的患者的生物标志物，其中相对于c-Myc，Mcl-1的正常表达水平，生物标志物包含c-Myc，Mcl-1或其组合的升高的表达水平 ，或其组合。 本发明还提供了靶向患者用棉酚治疗的方法，其中患者具有过表达c-Myc，Mcl-1或其组合的疾病，病症或病症。 本发明还提供了用于治疗或改善患者疾病，病症或障碍的方法，包括确定患者中c-Myc，Mcl-1或其组合的表达水平，并向患者施用棉酚。 在本发明的某些实施方案中，该疾病是癌症，与非癌细胞相比，癌细胞表现出c-Myc的升高的表达水平。 本发明还提供克服Mcl-1介导的化学耐药性的方法，包括向有需要的患者施用棉酚。

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