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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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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。
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公开(公告)号：US08445473B2
公开(公告)日：2013-05-21
申请号：US12937114
申请日：2009-04-13
Applicant: Shaomeng Wang , Haiying Sun , Zaneta Nikolovska-Coleska
Inventor： Shaomeng Wang , Haiying Sun , Zaneta Nikolovska-Coleska
IPC: C07D403/04 , C07D403/02 , C07D235/06
CPC classification number: C07D487/04
Abstract: The invention relates to heteroaryl-substituted 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的杂芳基取代的双环模拟物。 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：US08202902B2
公开(公告)日：2012-06-19
申请号：US12270374
申请日：2008-11-13
Applicant: Shaomeng Wang , Haiying Sun , Dongguang Qin , Zaneta Nikolovska-Coleska , Jianfeng Lu , Su Qiu , Yuefeng Peng , Qian Cai
Inventor： Shaomeng Wang , Haiying Sun , Dongguang Qin , Zaneta Nikolovska-Coleska , Jianfeng Lu , Su Qiu , Yuefeng Peng , Qian Cai
IPC: A01N47/10 , A61K31/27 , C07D225/00
CPC classification number: A61K38/191 , C07D487/04 , C07D519/00
Abstract: The invention relates to bivalent 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的二价模拟物，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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公开(公告)号：US07960372B2
公开(公告)日：2011-06-14
申请号：US11800220
申请日：2007-05-04
Applicant: Shaomeng Wang , Haiying Sun , Dongguang Qin , Zaneta Nikolovska-Coleska , Jianfeng Lu , Su Qiu , Yuefeng Peng , Qian Cai
Inventor： Shaomeng Wang , Haiying Sun , Dongguang Qin , Zaneta Nikolovska-Coleska , Jianfeng Lu , Su Qiu , Yuefeng Peng , Qian Cai
IPC: A61K31/545 , C07D225/00 , C07D403/00
CPC classification number: C07D519/00 , A61K38/191 , C07D487/04
Abstract: The invention relates to bivalent 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的二价模拟物，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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Patent Agency Ranking
公开(公告)号：US07910621B2
公开(公告)日：2011-03-22
申请号：US10594200
申请日：2005-03-22
Applicant: Jianyong Chen , Zaneta Nikolovska-Coleska , Dajun Yang , Shaomeng Wang , Haiying Sun , Liang Xu , Zengjian Hu
Inventor： Jianyong Chen , Zaneta Nikolovska-Coleska , Dajun Yang , Shaomeng Wang , Haiying Sun , Liang Xu , Zengjian Hu
IPC: A61K31/352 , C07D311/30
CPC classification number: C07C235/84 , C07C50/28 , C07C50/30 , C07D311/30
Abstract: The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of XIAP family proteins. In particular, the present invention provides embelin and other XIAP inhibitors and methods of using these compounds as antagonists of the anti-apoptotic effects of XIAP family member proteins. The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases).
Abstract translation: 本发明涉及XIAP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，本发明提供了塞林和其他XIAP抑制剂以及使用这些化合物作为XIAP家族蛋白的抗凋亡作用的拮抗剂的方法。 本发明还提供了治疗疾病和病理（例如肿瘤性疾病）的方法。
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公开(公告)号：US20080269140A1
公开(公告)日：2008-10-30
申请号：US10586271
申请日：2005-01-18
Applicant: Shaomeng Wang , Haiying Sun , Zaneta Nikolovska-Coleska , Chao-Yie Yang , Liang Xu
Inventor： Shaomeng Wang , Haiying Sun , Zaneta Nikolovska-Coleska , Chao-Yie Yang , Liang Xu
CPC classification number: C07K5/0806 , C07D487/04 , C07K5/0808 , C07K5/0827
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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公开(公告)号：US20080021095A1
公开(公告)日：2008-01-24
申请号：US10594200
申请日：2005-03-22
Applicant: Jianyong Chen , Zaneta Nikolovska-Coleska , Dajun Yang , Shaomeng Wang , Haiying Sun , Liang Xu , Zengjian Hu
Inventor： Jianyong Chen , Zaneta Nikolovska-Coleska , Dajun Yang , Shaomeng Wang , Haiying Sun , Liang Xu , Zengjian Hu
IPC: A61K31/353 , A61K31/122 , A61P35/00 , C07C49/603 , C07D311/30 , C12N5/06
CPC classification number: C07C235/84 , C07C50/28 , C07C50/30 , C07D311/30
Abstract: The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of XIAP family proteins. In particular, the present invention provides embelin and other XIAP inhibitors and methods of using these compounds as antagonists of the anti-apoptotic effects of XIAP family member proteins. The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases).
Abstract translation: 本发明涉及XIAP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，本发明提供了塞林和其他XIAP抑制剂以及使用这些化合物作为XIAP家族蛋白的抗凋亡作用的拮抗剂的方法。 本发明还提供了治疗疾病和病理（例如肿瘤性疾病）的方法。
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19.发明授权Process for the preparation of small molecule inhibitors of MDM2 and intermediates used therein 失效制备MDM2的小分子抑制剂的方法及其中使用的中间体公开(公告)号：US08742121B2
公开(公告)日：2014-06-03
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: C07D401/02 , C07D487/10 , C07D209/04
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：US20120289494A1
公开(公告)日：2012-11-15
申请号：US13469928
申请日：2012-05-11
Applicant: Shaomeng Wang , Wei Sun , Angelo Aguilar , Carlos Garcia-Echeverria
Inventor： Shaomeng Wang , Wei Sun , Angelo Aguilar , Carlos Garcia-Echeverria
IPC: A61K31/407 , A61K31/5377 , A61P35/00 , A61K31/438 , A61K31/41 , C07D487/10 , C07D471/20
CPC classification number: C07D487/10
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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