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41.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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公开(公告)号：US20120122947A1
公开(公告)日：2012-05-17
申请号：US13294315
申请日：2011-11-11
Applicant: Shaomeng Wang , Yujun Zhao , Wei Sun , Sanjeev Kumar , Lance Leopold , Laurent Debussche , Cedric Barriere , Jean-Christophe Carry , Kwame Amaning
Inventor： Shaomeng Wang , Yujun Zhao , Wei Sun , Sanjeev Kumar , Lance Leopold , Laurent Debussche , Cedric Barriere , Jean-Christophe Carry , Kwame Amaning
IPC: A61K31/407 , A61P35/00 , A61P35/02 , C07D487/10
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。
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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。
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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
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：US20110112052A1
公开(公告)日：2011-05-12
申请号：US12945511
申请日：2010-11-12
Applicant: Shaomeng Wang , Shanghai Yu , Wei Sun , Sanjeev Kumar Shangary , Duxin Sun , Peng Zou , Donna McEachern , Yujun Zhao
Inventor： Shaomeng Wang , Shanghai Yu , Wei Sun , Sanjeev Kumar Shangary , Duxin Sun , Peng Zou , Donna McEachern , Yujun Zhao
IPC: C07D487/10 , A61K31/407 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/675 , A61P1/00 , A61P35/04
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.
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作为p53和MDM2之间的相互作用的拮抗剂的螺 - 羟吲哚，以及它们作为治疗癌症和其它疾病的治疗剂的用途。
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Patent Agency Ranking
公开(公告)号：US20100317661A1
公开(公告)日：2010-12-16
申请号：US12815113
申请日：2010-06-14
Applicant: Shaomeng Wang , Dongguang Qin , Jianyong Chen , Shanghai Yu
Inventor： Shaomeng Wang , Dongguang Qin , Jianyong Chen , Shanghai Yu
IPC: A61K31/5377 , C07D487/10 , A61K31/407 , C12N5/00 , A61P35/00 , A61P17/14 , A61P1/00 , A61K31/496 , A61K31/4178
CPC classification number: C07D487/10 , C07D491/107 , C12N5/0693 , C12N2501/48
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).
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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。
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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
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。
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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
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。
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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。
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