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1. 发明申请

WO1996040721A1 A CYTOTOXICITY-BASED GENETIC SELECTION SYSTEM (TOXSEL) 审中-公开
标题翻译：基于细胞毒性的遗传选择系统（TOXSEL）
公开(公告)号：WO1996040721A1
公开(公告)日：1996-12-19
申请号：PCT/US1996008356
申请日：1996-06-03
申请人： EMORY UNIVERSITY , PRESIDENT AND FELLOWS OF HARVARD COLLEGE
发明人： EMORY UNIVERSITY , PRESIDENT AND FELLOWS OF HARVARD COLLEGE , FU, Haian , COLLIER, R., John , DINGLEDINE, Raymond
IPC分类号： C07H21/04
CPC分类号： C12Q1/6897 , C12N15/1055 , G01N33/5014 , G01N2500/00
摘要： The invention provides a cytotoxicity-based genetic selection (TOXSEL) method and related testing kit for the identification and positive selection of molecules or mutations that are capable of disrupting a specific protein-protein interaction. The invention enables positive selection of molecules disruptive of specific protein-protein interactions by virtue of the presence in the TOXSEL system of a toxin reporter gene. A disrupted protein-protein interaction precludes expression of the toxin reporter gene and, consequently, allows survival of the host cell. TOXSEL technology enables large-scale screening for drugs or small molecules capable of disrupting specific protein-protein interactions critical in processes such as cellular signalling, carcinogenesis, etc. The positive selection of molecules or mutations capable of interfering with specific protein-protein interactions permits the identification of amino acid residues or motifs critical in the protein-protein interactions and permits the design of drugs for therapeutic or diagnostic applications.
摘要翻译：本发明提供基于细胞毒性的遗传选择（TOXSEL）方法和用于鉴定和阳性选择能够破坏特定蛋白质 - 蛋白质相互作用的分子或突变的相关检测试剂盒。本发明通过在毒素报告基因的TOXSEL系统中的存在能够正确选择破坏特定蛋白质 - 蛋白质相互作用的分子。破坏的蛋白质 - 蛋白质相互作用排除了毒素报告基因的表达，因此允许宿主细胞的存活。 TOXSEL技术可以大规模筛选能够破坏细胞信号传导，致癌作用等过程中特定蛋白质 - 蛋白质相互作用关键的药物或小分子。能够干扰特定蛋白质 - 蛋白质相互作用的分子或突变的阳性选择允许识别蛋白质 - 蛋白质相互作用中关键的氨基酸残基或基序，并允许药物设计用于治疗或诊断应用。

2. 发明申请

WO1993021769A1 DIPHTHERIA TOXIN RECEPTOR-BINDING REGION 审中-公开
公开(公告)号：WO1993021769A1
公开(公告)日：1993-11-11
申请号：PCT/US1993004166
申请日：1993-05-03
申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE
发明人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE , COLLIER, R., John , EISENBERG, David , FU, Haian , CHOE, Seunghyon
IPC分类号： A01N37/18
CPC分类号： C07K14/34 , A61K39/00 , C07K2319/00 , C07K2319/02 , C07K2319/55
摘要： The invention features a polypeptide consisting of amino acids 379-535 of diphtheria toxin, and portions thereof. This region, shown by X-ray crystallographic analysis to comprise the receptor binding domain of diphtheria toxin, is used as an immunogen and clinical therapeutic against diphtheria.
摘要翻译：本发明的特征在于由白喉毒素的氨基酸379-535组成的多肽及其部分。通过X射线晶体学分析显示的包含白喉毒素受体结合结构域的该区域被用作针对白喉的免疫原和临床治疗剂。

3. 发明申请

WO2010042500A2 HEAT SHOCK PROTEIN 90 INHIBITORS, METHODS OF PREPARING SAME, AND METHODS FOR THEIR USE 审中-公开
标题翻译：热休克蛋白90抑制剂，其制备方法及其使用方法
公开(公告)号：WO2010042500A2
公开(公告)日：2010-04-15
申请号：PCT/US2009/059677
申请日：2009-10-06
申请人： EMORY UNIVERSITY , MIN, Jaeki , DU, Yuhong , THEPCHATRI, Pahk , LIOTTA, Dennis C. , FU, Haian
发明人： MIN, Jaeki , DU, Yuhong , THEPCHATRI, Pahk , LIOTTA, Dennis C. , FU, Haian
IPC分类号： C07D215/18 , C07D215/16 , A61K31/47 , A61P35/00
CPC分类号： C07D215/16 , C07D211/14 , C07D211/52 , C07D213/74 , C07D215/18 , C07D233/88 , C07D295/104 , C07D317/66
摘要： Novel classes of molecular chaperone Heat shock protein 90 (Hsp90) inhibitors are disclosed. These compounds are useful in treating and preventing cancer and other Hsp90-related diseases and conditions, such as inflammation and neurodegenerative disorders. Methods of treating and preventing cancer and other Hsp90 related diseases and conditions are disclosed that include administering to the subject a therapeutically effective amount of an Hsp90 inhibitor. Methods of preparing the novel Hsp90 inhibitors are also provided.
摘要翻译：公开了新型的分子伴侣热休克蛋白90（Hsp90）抑制剂。这些化合物可用于治疗和预防癌症和其他Hsp90相关疾病和病症，例如炎症和神经变性疾病。公开了治疗和预防癌症和其他Hsp90相关疾病和病症的方法，其包括向受试者施用治疗有效量的Hsp90抑制剂。还提供了制备新型Hsp90抑制剂的方法。

4. 发明申请

WO2022026863A2 CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR (CFTR) MODULATORS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF 审中-公开
公开(公告)号：WO2022026863A2
公开(公告)日：2022-02-03
申请号：PCT/US2021/043956
申请日：2021-07-30
申请人： EMORY UNIVERSITY , CHILDREN'S HEALTHCARE OF ATLANTA, INC.
发明人： SORSCHER, Eric , FU, Haian , DAVIES, Huw , HONG, Jeong , DU, Yuhong , RAB, Andras , MANFREDI, Candela , YANG, Xun , REN, Zhi
IPC分类号： A61K31/353 , A61K31/36 , C07D311/68 , C07D498/04
摘要： This disclosure relates to compounds that are cystic fibrosis transmembrane conductance regulator (CFTR) modulators and pharmaceutical compositions containing the same. In certain embodiments, this disclosure relates to methods of managing a CFTR related disease or condition or respiratory distress comprising administering an effective amount of a CFTR modulator disclosed herein to a subject in need thereof.

5. 发明申请

WO2002067968A3 14-3-3 BINDING MOLECULES AS SENSITIZERS FOR ANTICANCER THERAPIES 审中-公开
公开(公告)号：WO2002067968A3
公开(公告)日：2002-09-06
申请号：PCT/US2002/004948
申请日：2002-02-20
申请人： EMORY UNIVERSITY , FU, Haian , MASTERS, Shane, C.
发明人： FU, Haian , MASTERS, Shane, C.
IPC分类号： A61K38/10
摘要： Methods are provided for enhancing the death of a neaplastic cell comprising the administration of a therapeutically effective concentration of a 14-3-3 antagonist and at least one antineoplastic therapeutic agent. The methods of the invention find use in improving the clinical outcome of a mammal having a neoplastic disorder and comprises administration to a mammal in need thereof at least one antineoplastic therapeutic agent in combination with a 14-3-3 antagonist. Further provided are pharmaceutical compositions having a therapeutically effective amount of a 14-3-3 antagonist and an antineoplastic therapeutic agent. Also provided are methods for identifying agents that selectively inhibit an interaction between a 14-3-3 polypeptide and a 14-3-3 ligand.

6. 发明申请

WO2015157382A1 TREATMENT OF NEURODEGENERATIVE DISEASES WITH ASPARAGINE ENDOPEPTIDASE (AEP) INHIBITORS AND COMPOSITIONS RELATED THERETO 审中-公开
标题翻译：治疗与ASPARAGINE内含肽（AEP）抑制剂和组合物相关的神经营养因子
公开(公告)号：WO2015157382A1
公开(公告)日：2015-10-15
申请号：PCT/US2015/024864
申请日：2015-04-08
申请人： EMORY UNIVERSITY
发明人： YE, Keqiang , FU, Haian , DU, Yuhong
IPC分类号： C07D271/12 , C07D285/14 , A61K31/4245 , A61K31/433 , A61K9/20 , A61K9/48 , A61K47/38
CPC分类号： C07D271/12 , A61K9/20 , A61K9/48 , A61K31/4015 , A61K31/426 , A61K31/433 , A61K31/47 , A61K31/496 , A61K31/519 , A61K31/522 , A61K31/5377 , C07D271/02 , C07D471/04 , C07D473/04 , Y02A50/395
摘要： This disclosure relates to asparagine endopeptidase inhibitors and compositions and uses related thereto. In certain embodiments, the asparagine endopeptidase inhibitors are useful for treating or preventing neurodegenerative diseases and cognitive disorders such as Alzheimer's Disease. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising an asparagine endopeptidase inhibitor and a pharmaceutically acceptable excipient. In certain embodiments, the disclosure relates to methods of treating or preventing a neurodegenerative disease comprising administering an effective amount of pharmaceutical composition a asparagine endopeptidase inhibitor disclosed herein to a subject in need thereof.
摘要翻译：本公开涉及天冬酰胺内肽酶抑制剂及其相关的组合物和用途。在某些实施方案中，天冬酰胺内肽酶抑制剂可用于治疗或预防神经变性疾病和认知障碍如阿尔茨海默病。在某些实施方案中，本公开涉及包含天冬酰胺内肽酶抑制剂和药学上可接受的赋形剂的药物组合物。在某些实施方案中，本公开涉及治疗或预防神经变性疾病的方法，其包括向有需要的受试者施用有效量的本文公开的天冬酰胺内肽酶抑制剂的药物组合物。

7. 发明申请

WO2020247914A1 KRAS G12V MUTANT BINDS TO JAK1, INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS RELATED THERETO 审中-公开
公开(公告)号：WO2020247914A1
公开(公告)日：2020-12-10
申请号：PCT/US2020/036607
申请日：2020-06-08
申请人： EMORY UNIVERSITY
发明人： FU, Haian , MO, Xiulei , TANG, Cong
IPC分类号： A61K38/08
摘要： This disclosure relates to the discovery that a G12V mutant of KRAS (hereinafter KRAS G12V) binds to JAK1, i.e., the existence of a KRAS G12V and JAK1 binding interaction. In certain embodiments, this disclosure relates to methods of disrupting the KRAS G12V and JAK1 interaction reversing KRAS G12V induced immune escape by cancer cells utilizing agents that prevent the binding of JAK1 to KRAS G12V.

8. 发明申请

WO2015157376A1 ASPARAGINE ENDOPEPTIDASE (AEP) INHIBITORS FOR MANAGING CANCER AND COMPOSITIONS RELATED THERETO 审中-公开
标题翻译：用于管理癌症和组合物的阿伐他汀内肽（AEP）抑制剂
公开(公告)号：WO2015157376A1
公开(公告)日：2015-10-15
申请号：PCT/US2015/024850
申请日：2015-04-08
申请人： EMORY UNIVERSITY
发明人： YE, Keqiang , FU, Haian , DU, Yuhong
IPC分类号： C07D473/04 , C07D473/06 , A61K31/52 , A61P35/00
CPC分类号： C07D473/06 , A61K31/4015 , A61K31/4168 , A61K31/433 , A61K31/47 , A61K31/496 , A61K31/519 , A61K31/522 , A61K31/5355 , A61K45/06 , C07D207/452 , C07D215/06 , C07D257/04 , C07D273/02 , C07D277/54 , C07D285/135 , C07D471/04
摘要： This disclosure relates to asparagine endopeptidase inhibitors for managing cancer and compositions related thereto. In certain embodiments, the asparagine endopeptidase inhibitors are substituted 3,7-dihydropurine-2,6-dione derivatives useful for treating or preventing metastasis, tumor growth, and/or cancer. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising an asparagine endopeptidase inhibitor and a pharmaceutically acceptable excipient. In certain embodiments, the disclosure relates to methods of treating a cancer comprising administering an effective amount of pharmaceutical composition a asparagine endopeptidase inhibitor disclosed herein to a subject in need thereof.
摘要翻译：本公开涉及用于管理癌症的天冬酰胺内肽酶抑制剂及其相关的组合物。在某些实施方案中，天冬酰胺内肽酶抑制剂是用于治疗或预防转移，肿瘤生长和/或癌症的取代的3,7-二氢嘌呤-2,6-二酮衍生物。在某些实施方案中，本公开涉及包含天冬酰胺内肽酶抑制剂和药学上可接受的赋形剂的药物组合物。在某些实施方案中，本公开涉及治疗癌症的方法，包括向有需要的受试者施用有效量的本文公开的天冬酰胺内肽酶抑制剂的药物组合物。

9. 发明申请

WO2008150899A1 COMBINATION THERAPIES FOR TREATMENT OF CANCER AND INFLAMMATORY DISEASES 审中-公开
标题翻译：治疗癌症和炎症疾病的组合治疗
公开(公告)号：WO2008150899A1
公开(公告)日：2008-12-11
申请号：PCT/US2008/065132
申请日：2008-05-29
申请人： EMORY UNIVERSITY , FU, Haian , LIOTTA, Dennis, C. , THOMAS, Shala, L. , SNYDER, James, P.
发明人： FU, Haian , LIOTTA, Dennis, C. , THOMAS, Shala, L. , SNYDER, James, P.
IPC分类号： A61K31/12 , A61K31/4164 , A61P35/00
CPC分类号： A61K45/06 , A61K31/12 , A61K31/4164 , A61K2300/00
摘要： The present invention is directed to combinations of compounds useful in the treatment and prevention of cancer and inflammatory conditions or diseases. In particular embodiments, the combinations comprise one or more compounds that are NF-κB inhibitors or p38 MAPK inhibitors. The invention further provides pharmaceutical compositions and methods of treatment using the combinations. In one embodiment, the NF -KB inhibitor is a curcumin analog.
摘要翻译：本发明涉及可用于治疗和预防癌症和炎性病症或疾病的化合物的组合。在具体实施方案中，组合包含一种或多种作为NF-κB抑制剂或p38MAPK抑制剂的化合物。本发明还提供药物组合物和使用这些组合的治疗方法。在一个实施方案中，NF-KB抑制剂是姜黄素类似物。

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