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1. 发明申请

WO2022216552A2 NOVEL HEPATOSELECTIVE POLYADENYLATING POLYMERASES INHIBITORS AND THEIR METHOD OF USE 审中-公开
公开(公告)号：WO2022216552A2
公开(公告)日：2022-10-13
申请号：PCT/US2022/023110
申请日：2022-04-01
申请人： BARUCH S. BLUMBERG INSTITUTE
发明人： DU, Yanming , BLOCK, Timothy M. , ZHOU, Tianlun , HWANG, Nicky
IPC分类号： C07D401/14 , C07D403/14 , C07D491/12 , C07D491/147 , C07D221/10 , C07D455/06 , C07D471/04 , C07D471/14 , C07D491/052 , C07D495/04
摘要： Described herein are hepatoselective inhibitors of PAPD 5 and 7 having a disease-modifying action in the treatment of diseases associated with PAPD 5 and 7 that include disease such as hepatitis B and liver cancer. Compositions comprising same; and methods of making and using same are also described herein.

2. 发明申请

WO2018013508A1 SUBSTITUTED AMINOTHIAZOLES 审中-公开
标题翻译：取代的氨基噻唑
公开(公告)号：WO2018013508A1
公开(公告)日：2018-01-18
申请号：PCT/US2017/041443
申请日：2017-07-11
申请人： BARUCH S. BLUMBERG INSTITUTE
发明人： DU, Yanming , LU, Huagang , ROGOWSKY, John , KINNEY, William, A. , CUCONATI, Andrea
IPC分类号： C07D277/42 , C07D495/04
摘要： Described herein are substituted aminothiazoles, compositions comprising same; and methods of making and using same.
摘要翻译：本文描述了取代的氨基噻唑，包含其的组合物; 以及制作和使用它们的方法。

3. 发明申请

WO2022087023A1 METHODS AND KITS FOR DIAGNOSING AND TREATING CANCERS 审中-公开
公开(公告)号：WO2022087023A1
公开(公告)日：2022-04-28
申请号：PCT/US2021/055688
申请日：2021-10-19
申请人： BARUCH S. BLUMBERG INSTITUTE
发明人： PESTELL, Richard, G. , LI, Zhiping , JIAO, Xuanmao , WAYNE ASHTON, Anthony
IPC分类号： G01N33/574 , G01N33/537 , A61P35/00
摘要： Methods and/or kits for aiding, preventing, treating, or ameliorating the negative effects for a patient suffering from cancer are disclosed herein. In accordance with an aspect of the invention, that includes determining a sensitivity of one or more cancer cells by administering an immunohistochemical stain configured to determine an abundance of DACH1a gene.

4. 发明申请

WO2021126856A1 METHODS, KITS AND COMPOSITIONS FOR REDUCING CARDIOTOXICITY ASSOCIATED WITH CANCER THERAPIES 审中-公开
公开(公告)号：WO2021126856A1
公开(公告)日：2021-06-24
申请号：PCT/US2020/065128
申请日：2020-12-15
申请人： BARUCH S. BLUMBERG INSTITUTE
发明人： PESTELL, Richard, G. , WAYNE ASHTON, Anthony
IPC分类号： C07K14/705 , C07K14/715 , C07K14/52 , A61P35/00
摘要： Described herein are methods for administering a chemotherapeutic agent to a patient in need thereof comprising administering an effective amount of a CCR5 antagonist contemporaneously with an effective amount of a chemotherapeutic agent. Also described are kits and compositions useful to implement the methods.

5. 发明申请

WO2020072492A1 BENZAMIDE DERIVATIVES AS CGAS-STING PATHWAY AGONISTS 审中-公开
公开(公告)号：WO2020072492A1
公开(公告)日：2020-04-09
申请号：PCT/US2019/054065
申请日：2019-10-01
申请人： BARUCH S. BLUMBERG INSTITUTE
发明人： CHANG, Jinhong , DU, Yanming , GUO, Ju-tao
IPC分类号： C07D471/04
摘要： Pharmaceutical compositions of the invention comprise functionalized benzamide derivatives useful as cyclic GMP-AMP synthase- Stimulator of interferon gene (cGAS-STING) pathway agonists, and useful for treating viral diseases and boost antitumor immunity.

6. 发明申请

WO2015191179A1 TTP INHIBITIORS OF LOW DENSITY LIPPROTEIN SECRETION FOR THE MANAGEMENT OF DISEASES ASSOCIATED WITH ELEVATED BLOOD LDL LEVELS 审中-公开
标题翻译：低浓度LIPPROTEIN分泌的TTP抑制剂与高脂血症LDL水平相关的疾病管理
公开(公告)号：WO2015191179A1
公开(公告)日：2015-12-17
申请号：PCT/US2015/028730
申请日：2015-05-01
申请人： BARUCH S. BLUMBERG INSTITUTE
发明人： CUCONATI, Andrea , BLOCK, Timothy, M.
IPC分类号： A61K31/70 , C07D239/70
CPC分类号： A61K31/519
摘要： The present invention provides for the novel method for the inhibition of microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion having Formulas I-XI in lowering serum lipids and in the prevention and treatment of related disease. Regulation of the VLDL/LDL pathway as a therapeutic means to reduce hyperlipidemia is supported from studies in liver cells and in an animal model. Accordingly, the inhibition of regulation described herein is identified as a new therapeutic target for treatment of cardiovascular disease or diseases associated with cardiovascular disease such as hyperlipidemia. Treatment of cardiovascular disease and associated conditions or diseases with the novel TTP inhibitors of the invention reduces MTP protein associated lipid production without side effects that occur with other methods of MTP protein associated lipid inhibition. We describe small molecules (disubstituted tetrahydro-tetrazolo(l,5a)pyrimidine (TTP) and a method of their use to inhibit the secretion of ApoB and LDLs from liver derived cells in tissue culture and in animal models. We further describe how to use these small molecules in the management of diseases associated with elevations of circulating LDLs.
摘要翻译：本发明提供了抑制具有式I-XI的微粒体甘油三酯转移蛋白（MTP）和/或载脂蛋白B（Apo B）分泌物在降低血清脂质中的预防和治疗相关疾病的新方法。 VLDL / LDL途径的调节作为减少高脂血症的治疗手段得益于肝细胞和动物模型的研究。因此，本文所述的调节抑制被鉴定为用于治疗与心血管疾病如高脂血症相关的心血管疾病或疾病的新治疗靶标。使用本发明的新型TTP抑制剂治疗心血管疾病和相关病症或疾病可减少MTP蛋白相关的脂质生成，而不伴随MTP蛋白相关脂质抑制的其他方法发生副作用。我们描述了小分子（二取代四氢 - 四唑（1,5）嘧啶（TTP））及其在组织培养和动物模型中用于抑制来自肝源细胞的ApoB和LDL分泌的方法，我们进一步描述如何使用这些小分子治疗与循环低密度脂蛋白升高相关的疾病。

7. 发明申请

WO2022226422A2 METHODS, KITS AND COMPOSITIONS FOR REDUCING CHROMOSOMAL INSTABILITY IN CANCER CELLS 审中-公开
公开(公告)号：WO2022226422A2
公开(公告)日：2022-10-27
申请号：PCT/US2022/026221
申请日：2022-04-25
申请人： BARUCH S. BLUMBERG INSTITUTE
发明人： PESTELL, Richard G. , DU, Yanming
IPC分类号： C07D493/22 , C07D311/04 , C07D311/22 , C07D311/26 , A61K31/136 , A61K31/353 , A61K31/4709 , A61K31/517 , A61K31/704 , A61K31/713 , A61K39/00 , A61K45/06
摘要： Described herein are methods for administering a chemotherapeutic agent to a patient in need thereof. Such methods may treat, prevent, or ameliorate tumor CIN associated with administration of a chemotherapeutic agent., resulting in therapeutic resistance, tumor progression and death also described are kits and compositions useful to implement the methods.

8. 发明申请

WO2021222156A1 COMPOUNDS AND COMPOSITIONS FOR TREATING HEMATOLOGIC MALIGNANCIES 审中-公开
公开(公告)号：WO2021222156A1
公开(公告)日：2021-11-04
申请号：PCT/US2021/029275
申请日：2021-04-27
申请人： THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA , BARUCH S. BLUMBERG INSTITUTE
发明人： ROBERTSON, Erle S. , PEI, Yonggang , DU, Yanming
IPC分类号： A61K31/35 , A61K31/352 , C07D311/02 , C07D311/78 , A61K31/366 , C07D493/08 , A61P35/02
摘要： The present disclosure relates, in part, to certain compounds comprising brusatol derivatives, or a pharmaceutically acceptable salt, solvate, or polymorph thereof, which are useful for the treatment of hematological malignancies, including but not limited to leukemia and lymphoma. In certain embodiments, the present disclosure relates to pharmaceutical compositions of the compounds of the present disclosure.

9. 发明申请

WO2015193484A1 TAGGED HEPADNAVIRUS E ANTIGEN AND ITS USE IN SCREENING ANTIVIRAL SUBSTANCES 审中-公开
标题翻译：标记的HEPADNAVIRUS E抗原及其在筛选抗病毒物质中的用途
公开(公告)号：WO2015193484A1
公开(公告)日：2015-12-23
申请号：PCT/EP2015/063838
申请日：2015-06-19
申请人： DREXEL UNIVERSITY , BARUCH S. BLUMBERG INSTITUTE , F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GUO, Haitao , CAI, Dawai , CUCONATI, Andrea , JI, Changhua
IPC分类号： C07K14/005 , G01N33/576
CPC分类号： C07K14/005 , C07K2319/40 , C07K2319/42 , C12N2730/10122 , C12N2730/10151 , C12N2830/006 , G01N33/502 , G01N2333/02
摘要： The present invention relates to methods and uses for screening anti-hepadnaviral substances, wherein the substances are screened for the capacity to inhibit covalently closed circular (ccc) DNA of a hepadnavirus, like hepatitis B virus. The methods and uses take advantage of cells comprising a nucleic sequence encoding a tagged hepadnavirus e antigen, like Hepatitis B virus e antigen (HBeAg). Furthermore, the present invention provides nucleic acid sequences encoding a tagged hepadnavirus e antigen and proteins encoded thereby. Also kits for use in the screening methods are provided.
摘要翻译：本发明涉及用于筛选抗肝炎军事病毒物质的方法和用途，其中所述物质被筛选以抑制乙型肝炎病毒如乙型肝炎病毒的共价闭合的环状（ccc）DNA。所述方法和用途利用了包含编码标记的肝炎病毒e抗原（例如乙型肝炎病毒e抗原（HBeAg））的核酸序列的细胞。此外，本发明提供了编码标记的肝炎链球菌病毒e抗原的核酸序列和由其编码的蛋白质。还提供了用于筛选方法的试剂盒。

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