公开(公告)号：US20100273812A1

公开(公告)日：2010-10-28

申请号：US12159249

申请日：2008-04-14

Applicant: Shaomeng Wang ,  Yuefeng Peng ,  Haiying Sun ,  Qian Cai ,  Zaneta Nikolovska-Coleska ,  Jianfeng Lu ,  Su Qiu

Inventor： Shaomeng Wang ,  Yuefeng Peng ,  Haiying Sun ,  Qian Cai ,  Zaneta Nikolovska-Coleska ,  Jianfeng Lu ,  Su Qiu

IPC: A61K31/497 ,  C07D487/04 ,  A61K31/407 ,  A61K31/4025 ,  A61K31/4439 ,  A61P35/00 ,  C12N5/00

CPC classification number: G01N33/5011 ,  C07D487/04

Abstract: The invention relates to diazo bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.

Abstract translation: 本发明涉及作为细胞凋亡蛋白抑制剂抑制剂的Smac的重氮二环模拟物。 本发明还涉及这些模拟物用于诱导凋亡性细胞死亡和使细胞对细胞凋亡诱导剂敏感的用途。

公开(公告)号：US20100093645A1

公开(公告)日：2010-04-15

申请号：US10586269

申请日：2005-01-18

Applicant: Shaomeng Wang ,  Halying Sun ,  Zaneta Nikolovska-Coleska ,  Chao-Yie Yang ,  Liang Xu ,  Jlanyong Chen

Inventor： Shaomeng Wang ,  Halying Sun ,  Zaneta Nikolovska-Coleska ,  Chao-Yie Yang ,  Liang Xu ,  Jlanyong Chen

IPC: A61K38/06 ,  C07K5/087 ,  C12N5/06 ,  A61P35/00

CPC classification number: C07K5/0806 ,  A61K38/00 ,  C07K5/0808

Abstract: The invention relates to peptidomimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these peptidomimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.

Abstract translation: 本发明涉及作为细胞凋亡蛋白抑制剂抑制剂的Smac的肽模拟物。 本发明还涉及这些肽模拟物用于诱导凋亡性细胞死亡和使细胞对细胞凋亡诱导剂敏感的用途。

公开(公告)号：US07557251B2

公开(公告)日：2009-07-07

申请号：US11729638

申请日：2007-03-29

Applicant: Shaomeng Wang ,  Jianyong Chen ,  John F. W. Keana ,  Ming Guo

Inventor： Shaomeng Wang ,  Jianyong Chen ,  John F. W. Keana ,  Ming Guo

IPC: C07C39/12 ,  C07C39/38 ,  C07C39/10 ,  C07C53/08

CPC classification number: C07B57/00 ,  A61K31/192 ,  A61K31/78 ,  C07C45/516 ,  C07C45/79 ,  C07C45/85 ,  C07C47/57 ,  C07C51/487 ,  C07C53/08

Abstract: This invention relates to relates to methods for producing gossypol acetic acid co-crystals and (−)-gossypol acetic acid co-crystals. The invention also relates to pharmaceutical compositions comprising gossypol acetic acid co-crystals and (−)-gossypol acetic acid co-crystals and the use of gossypol acetic acid co-crystals and (−)-gossypol acetic acid co-crystals for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.

Abstract translation: 本发明涉及生产棉酚乙酸共晶体和（ - ） - 棉酚乙酸共晶体的方法。 本发明还涉及包含棉酚乙酸共晶和（ - ） - 棉酚乙酸共晶体的药物组合物，以及使用棉酚乙酸共晶体和（ - ） - 棉酚乙酸共晶体诱导细胞凋亡 细胞和致敏细胞诱导凋亡细胞死亡。

公开(公告)号：US20080132485A1

公开(公告)日：2008-06-05

申请号：US11632079

申请日：2005-07-11

Applicant: Shaomeng Wang ,  Haiying Sun ,  Zaneta Nikolovksa-Coleska ,  Chao-Yie Yang ,  Liang Xu ,  Naoyuki G. Saito ,  Jianyong Chen

Inventor： Shaomeng Wang ,  Haiying Sun ,  Zaneta Nikolovksa-Coleska ,  Chao-Yie Yang ,  Liang Xu ,  Naoyuki G. Saito ,  Jianyong Chen

IPC: A61K31/55 ,  A61P35/00 ,  C07D487/00 ,  A61K31/395 ,  A61K31/435 ,  C07D225/00 ,  C07D221/00

CPC classification number: C07D487/04 ,  C07D471/04

Abstract: The invention relates to conformationally constrained mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.

Abstract translation: 本发明涉及Smac的构象约束模拟物，其作为细胞凋亡蛋白抑制剂的抑制剂。 本发明还涉及这些模拟物用于诱导凋亡性细胞死亡和使细胞对细胞凋亡诱导剂敏感的用途。

公开(公告)号：US07355015B1

公开(公告)日：2008-04-08

申请号：US09936333

申请日：2000-03-10

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: C07K16/00 ,  C07K16/40 ,  A61K38/43

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。

公开(公告)号：US20060178435A1

公开(公告)日：2006-08-10

申请号：US11265576

申请日：2005-11-02

Applicant: Shaomeng Wang ,  Jianyong Chen ,  Zaneta Nikolovska-Coleska ,  Dajun Yang

Inventor： Shaomeng Wang ,  Jianyong Chen ,  Zaneta Nikolovska-Coleska ,  Dajun Yang

IPC: C07C50/32 ,  A61K31/12 ,  A61K31/122 ,  A61K31/22

CPC classification number: C07C50/30 ,  A45C11/00 ,  A45C11/04 ,  A45C13/42 ,  C07C39/14 ,  C07C46/00 ,  C07C50/32 ,  C07C67/08 ,  C07C67/29 ,  C07C69/017 ,  C07C69/21

Abstract: The invention relates to the compound apogossypolone and salts and prodrugs thereof. Apogossypolone functions as an inhibitor of Bcl-2 family proteins. The invention also relates to the use of apogossypolone for inhibiting hyperproliferative cell growth, for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.

Abstract translation: 本发明涉及化合物果糖酚及其盐和前药。 聚鸟苷酸作为Bcl-2家族蛋白的抑制剂起作用。 本发明还涉及用于抑制过度增殖细胞生长，用于诱导细胞凋亡和促进细胞诱导凋亡细胞死亡的用途。

公开(公告)号：US20060084647A1

公开(公告)日：2006-04-20

申请号：US11209998

申请日：2005-08-22

Applicant: Shaomeng Wang ,  Guoping Wang ,  Guozhi Tang ,  Renxiao Wang ,  Zaneta Nikolovska-Coleska ,  Dajun Yang ,  Liang Xu

Inventor： Shaomeng Wang ,  Guoping Wang ,  Guozhi Tang ,  Renxiao Wang ,  Zaneta Nikolovska-Coleska ,  Dajun Yang ,  Liang Xu

IPC: A61K31/5377 ,  A61K31/506 ,  A61K31/4709 ,  A61K31/47 ,  A61K31/445 ,  A61K31/165 ,  C07D413/02 ,  C07D401/02 ,  C07C317/32

CPC classification number: C07C205/38 ,  C07C39/10 ,  C07C39/15 ,  C07C39/17 ,  C07C39/367 ,  C07C43/23 ,  C07C43/295 ,  C07C49/747 ,  C07C49/82 ,  C07C49/83 ,  C07C49/84 ,  C07C65/105 ,  C07C235/60 ,  C07C235/64 ,  C07C311/29 ,  C07C311/46 ,  C07C317/22 ,  C07C317/40 ,  C07C317/44 ,  C07C2601/14 ,  C07C2603/74 ,  C07D211/16 ,  C07D213/70 ,  C07D215/227 ,  C07D215/233 ,  C07D217/06 ,  C07D263/56 ,  C07D277/64 ,  C07D307/84 ,  C07D321/12 ,  C07D333/60 ,  C07D333/76 ,  C07D401/12 ,  C07D405/12

Abstract: The invention relates to small molecules which function as inhibitors of anti-apoptotic Bcl-2 family member proteins (e.g., Bcl-2 and Bcl-xL). The invention also relates to the use of these compounds for inducing apoptotic cell death and sensitizing cells to the induction of apoptotic cell death.

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。

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。

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 -