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1. 发明专利

JP2014528450A 肝細胞癌を含む癌の阻害剤、および肝炎ウイルス複製の阻害剤としての置換アミノチアゾール有权
标题翻译：的癌症抑制剂，包括肝细胞癌，和如肝炎病毒复制的抑制剂取代的氨基噻唑
公开(公告)号：JP2014528450A
公开(公告)日：2014-10-27
申请号：JP2014534680
申请日：2012-10-04
申请人：インスティテュートフォーヘパタイティスアンドウィルスリサーチInstitute For Hepatitis And Virus Research , インスティテュートフォーヘパタイティスアンドウィルスリサーチInstitute For Hepatitis And Virus Research
发明人：キュコナティ，アンドレア , シュー，シャイアドン , ブロック，ティモシー，エム．
IPC分类号： C07D277/20 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K31/519 , A61P1/16 , A61P31/12 , A61P35/00 , A61P35/02 , A61P35/04 , C07D277/42 , C07D417/04 , C07D417/12 , C07D417/14 , C07D475/08 , C07D495/04
CPC分类号： C07D417/14 , A61K31/425 , A61K31/426 , C07D277/42 , C07D417/04 , C07D417/12 , C07D487/04 , C07D495/04
摘要：置換アミノチアゾール誘導体を含む、本発明の薬学的組成物を、提示する。置換アミノチアゾール誘導体は、無制御な細胞成長と関連する疾患の治療において、疾患修飾作用を有する。このような疾患には、肝細胞癌等の癌、および肝炎ウイルスによるウイルス感染が挙げられる。【選択図】なし
摘要翻译：包括取代的氨基噻唑衍生物，本发明的药物组合物，呈现。在的与不受控制的细胞生长，疾病减轻作用相关的疾病的治疗取代的氨基噻唑衍生物。这样的疾病，肝细胞癌和类似物，和由肝炎病毒病毒感染的癌症。系统技术领域

3. 发明申请

US20140249154A1 SUBSTITUTED AMINOTHIAZOLES AS INHIBITORS OF CANCERS, INCLUDING HEPATOCELLULAR CARCINOMA, AND AS INHIBITORS OF HEPATITIS VIRUS REPLICATION 审中-公开
标题翻译：取代的氨基酸作为癌症的抑制剂，包括肝细胞癌和作为乙型肝炎病毒复制的抑制剂
公开(公告)号：US20140249154A1
公开(公告)日：2014-09-04
申请号：US14349014
申请日：2012-10-04
申请人： The Institute for Hepatitis and Virus Research
发明人： Andrea Cuconati , Xiaodong Xu , Timothy M. Block
IPC分类号： C07D495/04 , C07D487/04 , C07D417/04 , C07D277/42 , C07D417/14 , C07D417/12
CPC分类号： C07D417/14 , A61K31/425 , A61K31/426 , C07D277/42 , C07D417/04 , C07D417/12 , C07D487/04 , C07D495/04 , Y02A50/463
摘要： Pharmaceutical compositions of the invention are presented which comprise substituted aminothiazoles derivatives. The substituted aminothiazoles derivatives have a disease-modifying action in the treatment of diseases associated with unregulated cell growth. Such diseases include cancers such as hepatocellular carcinoma, and viral infections from a hepatitis virus.
摘要翻译：本发明的药物组合物包括取代的氨基噻唑衍生物。取代的氨基噻唑衍生物在治疗与未调节的细胞生长相关的疾病中具有疾病修饰作用。这些疾病包括癌症如肝细胞癌和肝炎病毒的病毒感染。

4. 发明申请

US20150011569A1 NOVEL P13K p110 INHIBITORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：新型P13K p110抑制剂及其使用方法
公开(公告)号：US20150011569A1
公开(公告)日：2015-01-08
申请号：US14364751
申请日：2012-12-14
申请人： PHILADELPHIA HEALTH & EDUCATION CORPORATION d/b/a Drexel University College of Medicine , INSTITUTE FOR HEPATITIS AND VIRUS RESEARCH
发明人： Peter D. Katsikis , William A. Kinney , Harold R. Almond , Noshena Khan
IPC分类号： A61K31/52 , A61K45/06 , C07D473/34
CPC分类号： A61K31/52 , A61K45/06 , C07D473/34 , C07D519/00
摘要： The invention includes compositions that regulated PI3K p110 delta and are useful as an anti-viral therapy. The invention includes a method of inhibiting p110 delta, a component of PI3K p110 delta signaling pathway, or any combination thereof in a cell as an anti-viral therapeutic approach for treating a viral infection, for example influenza. The invention includes a method of modulating PI3K p110 delta in a cell infected with a virus by contacting the cell with an effective amount of a composition comprising an inhibitor of PI3K p110 delta.
摘要翻译：本发明包括调节PI3Kp110δ并可用作抗病毒治疗的组合物。本发明包括抑制作为用于治疗病毒感染（例如流感）的抗病毒治疗方法的细胞中的p110δ，PI3Kp110δ信号通路的成分或其任何组合的方法。本发明包括通过使细胞与有效量的包含PI3Kp110δ的抑制剂的组合物接触来调节感染病毒的细胞中的PI3Kp110δ的方法。

5. 发明申请

WO2013126640A2 BENZODIAZEPINE COMPOUNDS WITH ANTI-FLAVIVIRUS ACTIVITY 审中-公开
标题翻译：苯并噻唑类化合物具有抗病毒活性
公开(公告)号：WO2013126640A2
公开(公告)日：2013-08-29
申请号：PCT/US2013/027241
申请日：2013-02-22
申请人： INSTITUTE FOR HEPATITIS AND VIRUS RESEARCH
发明人： CUCONATI, Andrea , CHANG, Jinhong , BLOCK, Timothy, M. , JU-TAO, Guo
IPC分类号： C12Q1/70
CPC分类号： A61K31/5513 , C07D243/24 , C12Q1/6897 , C12Q1/70 , G01N2500/04 , G01N2500/10 , Y02A50/385 , Y02A50/387
摘要： The present invention describes a unique antiviral screen system. The assay is based on quantitatively monitoring viral activation of host cell beta-interferon (IFN-β) gene expression in a HEK293 -derived reporter cell line expressing a firefly luciferase gene under the control of a human IFN-β promoter. Unlike the traditional high throughput antiviral assays that measure either the reduction of viral components/yields or cytopathic effect, the readout of the reporter assay in the present invention is the virus-induced host cellular innate immune response. Hence, the assay allows for identification of compounds that inhibit virus infection. In addition, because induction of IFN is one of the most common attributes of viruses, the assay is applicable to all the viruses that are able to infect the reporter cell line and induce IFN- β expression. Compounds that interfere with viral mediated activation of the interferon pathway in a primary screen, can be further screened with virus-specific assay to confirm their antiviral activity.
摘要翻译：本发明描述了一种独特的抗病毒屏幕系统。该测定基于定量监测来自表达在人IFN-β启动子控制下的萤火虫萤光素酶基因的HEK293衍生的报道细胞系中宿主细胞β-干扰素（IFN-β）基因表达的病毒活化。不同于测量病毒成分/产量或细胞病变效应的降低的传统高通量抗病毒测定法，本发明中报道分析的读出是病毒诱导的宿主细胞先天免疫应答。因此，该测定允许鉴定抑制病毒感染的化合物。另外，由于IFN的诱导是病毒最常见的属性之一，所以该测定适用于能够感染报道细胞系并诱导IFN-β表达的所有病毒。可以用病毒特异性测定进一步筛选干扰原代筛选中的干扰素途径的病毒介导的激活的化合物，以证实其抗病毒活性。

6. 发明申请

WO2013052613A1 SUBSTITUTED AMINOTHIAZOLES AS INHIBITORS OF CANCERS, INCLUDING HEPATOCELLULAR CARCINOMA, AND AS INHIBITORS OF HEPATITIS VIRUS REPLICATION 审中-公开
标题翻译：取代的氨基酸作为癌症的抑制剂，包括肝细胞癌和作为乙型肝炎病毒复制的抑制剂
公开(公告)号：WO2013052613A1
公开(公告)日：2013-04-11
申请号：PCT/US2012/058674
申请日：2012-10-04
申请人： INSTITUTE FOR HEPATITIS AND VIRUS RESEARCH
发明人： CUCONATI, Andrea , XU, Xiaodong , BLOCK, Timothy, M.
IPC分类号： A61K31/425 , A61K31/426 , C07D417/00 , C07D417/02
CPC分类号： C07D417/14 , A61K31/425 , A61K31/426 , C07D277/42 , C07D417/04 , C07D417/12 , C07D487/04 , C07D495/04 , Y02A50/463
摘要： Pharmaceutical compositions of the invention are presented which comprise substiuted aminothiazoles derivatives. The substiuted aminothiazoles derivatives have a disease-modifying action in the treatment of diseases associated with unregulated cell growth. Such diseases include cancers such as hepatocellular carcinoma, and viral infections from a hepatitis virus.
摘要翻译：本发明的药物组合物包括取代的氨基噻唑衍生物。取代的氨基噻唑衍生物在治疗与未调节的细胞生长相关的疾病中具有改善疾病的作用。这些疾病包括癌症如肝细胞癌和肝炎病毒的病毒感染。

7. 发明申请

WO2010027996A9 NOVEL IMINO SUGAR DERIVATIVES DEMONSTRATE POTENT ANTIVIRAL ACTIVITY AND REDUCED TOXICITY 审中-公开
公开(公告)号：WO2010027996A9
公开(公告)日：2010-03-11
申请号：PCT/US2009/055658
申请日：2009-09-02
申请人： INSTITUTE FOR HEPATITIS AND VIRUS RESEARCH , BLOCK, Timothy, M. , CHANG, Jinhong , XU, Xiaodong
发明人： BLOCK, Timothy, M. , CHANG, Jinhong , XU, Xiaodong
IPC分类号： A01N43/42 , A61K31/47
摘要： lmino sugars, such as deoxynojιrimycin(DNJ), are glucose analogues that selectively inhibit cellular a-glucosidase I and Il (enzymes that process N-linked glycans in glycoprotein) and exhibit broad spectrwn antiviral activities against many enveloped 5 viruses. In order to develop' imino sugars with more potent antiviral activity as well as improved toxicity profile, OSL-95II was modified by diversifying the nitrogen linked alkylated side chain. Furthermore, these new compounds were shown to be active againstDengue virus (DV) and West Nile virus (WNV) infection in BHK cells where potentantι-DV activity having submicromolar EC50 values and SI of greater than 900. Thesecompounds represent a new generation of iminio sugars and their analogues, having IS application in the clinical treatment of infection ofbv and other members of flavivirdae.

8. 发明申请

WO2010027996A1 NOVEL IMINO SUGAR DERIVATIVES DEMONSTRATE POTENT ANTIVIRAL ACTIVITY AND REDUCED TOXICITY 审中-公开
标题翻译：新型三嗪糖衍生物衍生物抗病毒活性和降低毒性
公开(公告)号：WO2010027996A1
公开(公告)日：2010-03-11
申请号：PCT/US2009/055658
申请日：2009-09-02
申请人： INSTITUTE FOR HEPATITIS AND VIRUS RESEARCH , BLOCK, Timothy, M. , CHANG, Jinhong , XU, Xiaodong
发明人： BLOCK, Timothy, M. , CHANG, Jinhong , XU, Xiaodong
IPC分类号： A01N43/42 , A61K31/47
CPC分类号： A61K31/47 , A61K31/7056 , C07D211/46 , Y02A50/393 , A61K2300/00
摘要： lmino sugars, such as deoxynojιrimycin(DNJ), are glucose analogues that selectively inhibit cellular a-glucosidase I and Il (enzymes that process N-linked glycans in glycoprotein) and exhibit broad spectrwn antiviral activities against many enveloped 5 viruses. In order to develop' imino sugars with more potent antiviral activity as well as improved toxicity profile, OSL-95II was modified by diversifying the nitrogen linked alkylated side chain. Furthermore, these new compounds were shown to be active againstDengue virus (DV) and West Nile virus (WNV) infection in BHK cells where potentantι-DV activity having submicromolar EC50 values and SI of greater than 900. Thesecompounds represent a new generation of iminio sugars and their analogues, having IS application in the clinical treatment of infection ofbv and other members of flavivirdae.
摘要翻译：诸如脱氧核糖核苷酸（DNJ）的葡萄糖是选择性抑制细胞α-葡萄糖苷酶I和II（在糖蛋白中加工N-连接聚糖的酶）的葡萄糖类似物，并且对许多包膜的5种病毒表现出广泛的抗病毒活性。为了开发具有更强效抗病毒活性的亚氨基糖以及改进的毒性特征，OSL-95II通过使氮连接的烷基化侧链多样化而被修饰。此外，这些新化合物被证明对BHK细胞中的登革热病毒（DV）和西尼罗病毒（WNV）感染具有活性，其中具有亚微摩尔EC 50值和SI大于900的有效β-DV活性。该化合物代表新一代亚氨基糖类及其类似物，具有IS应用于临床治疗紫薇和其他成虫的感染。

9. 发明申请

WO2014089296A2 FUNCTIONALIZED BENZAMIDE DERIVATIVES AS ANTIVIRAL AGENTS AGAINST HBV INFECTION 审中-公开
标题翻译：功能化的苯甲酸衍生物作为抗HBV感染的抗病毒药物
公开(公告)号：WO2014089296A2
公开(公告)日：2014-06-12
申请号：PCT/US2013/073319
申请日：2013-12-05
申请人： INSTITUTE FOR HEPATITIS AND VIRUS RESEARCH , PHILADELPHIA HEALTH & EDUCATION CORPORATION d/b/a DREXEL UNIVERSITY COLLEGE OF MEDICINE
发明人： XU, Xiaodong , BLOCK, Timothy, M. , GUO, Ju-Tao , DU, Yanming
IPC分类号： A61M31/00
CPC分类号： C07C233/66 , C07C233/75 , C07C235/64 , C07C2602/10 , C07D317/46 , C07D317/68 , C07D319/18 , C07D321/10 , C07D333/68 , C07D333/70 , C07D333/72 , C07D495/04
摘要： Pharmaceutical compositions of the invention comprise functionalized benzamide derivatives useful as pregenomic RNA encapsidation inhibitors, useful for the treatment of Hepatitis B virus (HBV) infection.
摘要翻译：本发明的药物组合物包含可用作治疗乙型肝炎病毒（HBV）感染的预先基因组RNA包封抑制剂的官能化苯甲酰胺衍生物。

10. 发明申请

WO2008154373A1 2-AMINO-2,7-DIDEOXY-ALPHA-D-GLYCERO-D-GLUCO-HEPTOPYRANOSYL INHIBITORS OF POSITIVE SENSE SINGLE-STRANDED RNA ENVELOPE VIRUSES 审中-公开
标题翻译：阳性感应单链RNA包膜病毒的2-氨基-2,7-二脱氧-α-D-谷氨酰-D-谷氨酰 - 赖氨酸残基
公开(公告)号：WO2008154373A1
公开(公告)日：2008-12-18
申请号：PCT/US2008/066104
申请日：2008-06-06
申请人： INSTITUTE FOR HEPATITIS AND VIRUS RESEARCH , BIRK, Alexander, V. , DUBOVI, Edward, J. , SZETO, Hazel, H.
发明人： BIRK, Alexander, V. , DUBOVI, Edward, J. , SZETO, Hazel, H.
IPC分类号： A61K31/70
CPC分类号： C07D309/14 , C07H15/23
摘要： The present invention is directed to compounds, compositions and methods comprising the aminoglycoside moiety represented by Formula (II) for treating and preventing the spread of positive sense single-stranded RNA envelope viral infections. One embodiment of the present invention uses geneticin or its analogs, including 2-amino-2,7-dideoxy-alpha-D-glycero-D-gluco-heptopyranose, as the antiviral agent. The compounds, compositions and methods of the present invention are applicable to infections resulting from Hepatitis C virus, West Nile virus, Yellow Fever virus, Dengue virus, Bovine Viral Diarrhea virus, Equine Arteritis virus, and/or Sindbis virus.
摘要翻译：本发明涉及包含由式（II）表示的氨基糖苷部分用于治疗和预防阳性单链RNA包膜病毒感染的扩散的化合物，组合物和方法。本发明的一个实施方案使用遗传霉素或其类似物，包括2-氨基-2,7-二脱氧-α-D-甘油-D-葡庚糖 - 吡喃葡萄糖作为抗病毒剂。本发明的化合物，组合物和方法适用于丙型肝炎病毒，西尼罗病毒，黄热病病毒，登革热病毒，牛病毒性腹泻病毒，马动脉炎病毒和/或辛德比斯病毒引起的感染。

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