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公开(公告)号：US20090082424A1
公开(公告)日：2009-03-26
申请号：US12242388
申请日：2008-09-30
Applicant: Shaomeng Wang , Dajun Yang , Liang Xu
Inventor： Shaomeng Wang , Dajun Yang , Liang Xu
IPC: A61K31/11 , A61K31/337 , A61P35/02 , A61P35/04 , A61P35/00
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。
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公开(公告)号：US20080248566A1
公开(公告)日：2008-10-09
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
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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公开(公告)号：US07432304B2
公开(公告)日：2008-10-07
申请号：US10729156
申请日：2003-12-05
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（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。
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公开(公告)号：US20080058322A1
公开(公告)日：2008-03-06
申请号：US11811019
申请日：2007-06-08
Applicant: Shaomeng Wang , Dajun Yang , Istvan Enyedy
Inventor： Shaomeng Wang , Dajun Yang , Istvan Enyedy
CPC classification number: 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
Abstract: 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.
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公开(公告)号：US20060211757A1
公开(公告)日：2006-09-21
申请号：US11360485
申请日：2006-02-22
Applicant: Shaomeng Wang , Ke Ding , Yipin Lu , Zaneta Nikolovska-Coleska , Su Qiu , Guoping Wang , Dongguang Qin , Sanjeev Kumar
Inventor： Shaomeng Wang , Ke Ding , Yipin Lu , Zaneta Nikolovska-Coleska , Su Qiu , Guoping Wang , Dongguang Qin , Sanjeev Kumar
IPC: A61K31/407 , C07D209/54
CPC classification number: C07D209/54 , C07D487/10 , C07D491/10
Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
Abstract translation: 本发明涉及作为p53和MDM2相互作用抑制剂的小分子。 本发明还涉及这些化合物用于抑制细胞生长，诱导细胞死亡，诱导细胞周期停滞和/或使细胞对另外的药剂敏化的用途。
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Patent Agency Ranking
46.发明授权Structure based discovery of inhibitors of matriptase for the treatment of cancer and other conditions 失效基于结构发现的matriptase抑制剂用于治疗癌症和其他病症公开(公告)号：US06677377B2
公开(公告)日：2004-01-13
申请号：US09885295
申请日：2001-06-21
Applicant: Chen-Yong Lin , Robert B. Dickson , Shaomeng Wang , Istvan Enyedy , Sheau-Ling Lee
Inventor： Chen-Yong Lin , Robert B. Dickson , Shaomeng Wang , Istvan Enyedy , Sheau-Ling Lee
IPC: A61K31155
CPC classification number: A61K31/655 , A61K31/155 , A61K31/341 , A61K31/404 , A61K31/505 , A61K49/0002 , G01N33/574 , G01N2333/96486
Abstract: The present invention relates to a method of inhibiting carcinoma progression wherein matriptase plays a role in a subject in need of such inhibition including administering to a subject an effective amount of a compound comprising two positively charged groups, which are the same or different. The groups are linked by a chemical group having a length of between 5 and 30 A, and preferably between 15 and 24 A. Diagnostic methods based on matriptase action and therapeutic methods involving inhibition of matriptase activity are provided.
Abstract translation: 本发明涉及一种抑制癌症进展的方法，其中底物酶在需要这种抑制的受试者中起作用，包括向受试者施用有效量的包含相同或不同的两个带正电基团的化合物。 这些基团通过长度为5至30A，优选15至24A的化学基团连接。提供了基于片段酶作用的诊断方法和涉及抑制matriptase活性的治疗方法。
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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。
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公开(公告)号：US08901117B2
公开(公告)日：2014-12-02
申请号：US13336047
申请日：2011-12-23
Applicant: Shaomeng Wang , Ke Ding , Yipin Lu , Zaneta Nikolovska-Coleska , Su Qiu , Guoping Wang , Dongguang Qin , Sanjeev Kumar
Inventor： Shaomeng Wang , Ke Ding , Yipin Lu , Zaneta Nikolovska-Coleska , Su Qiu , Guoping Wang , Dongguang Qin , Sanjeev Kumar
IPC: A61K31/5377 , A61K31/407 , A61K31/437 , A61K31/4985 , C07D209/54 , C07D491/10 , C07D487/10
CPC classification number: C07D209/54 , C07D487/10 , C07D491/10
Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
Abstract translation: 本发明涉及作为p53和MDM2相互作用抑制剂的小分子。 本发明还涉及这些化合物用于抑制细胞生长，诱导细胞死亡，诱导细胞周期停滞和/或使细胞对附加试剂敏感的用途。
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公开(公告)号：US08518984B2
公开(公告)日：2013-08-27
申请号：US12945511
申请日：2010-11-12
Applicant: Shaomeng Wang , Shanghai Yu , Wei Sun , Sanjeev Kumar , Duxin Sun , Peng Zou , Donna McEachern , Yujun Zhao
Inventor： Shaomeng Wang , Shanghai Yu , Wei Sun , Sanjeev Kumar , Duxin Sun , Peng Zou , Donna McEachern , Yujun Zhao
IPC: C07D487/10 , A61K31/4015
CPC classification number: C07D487/10 , A61K31/407 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/675 , A61K45/06 , C07D471/20 , C07D491/107 , C07D495/10 , C07F9/6561 , 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.
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50.发明申请PROCESS FOR THE PREPARATION OF SMALL MOLECULE INHIBITORS OF MDM2 AND INTERMEDIATES USED THEREIN 失效制备MDM2小分子抑制剂及其使用的中间体的方法公开(公告)号：US20130030173A1
公开(公告)日：2013-01-31
申请号：US13614751
申请日：2012-09-13
Applicant: Shaomeng Wang , Ke Ding , Guoping Wang
Inventor： Shaomeng Wang , Ke Ding , Guoping Wang
IPC: C07D487/10
CPC classification number: C07D209/54 , C07D487/10 , C07D491/10
Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
Abstract translation: 本发明涉及作为p53和MDM2相互作用抑制剂的小分子。 本发明还涉及这些化合物用于抑制细胞生长，诱导细胞死亡，诱导细胞周期停滞和/或使细胞对另外的药剂敏化的用途。
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