Invention Grant
US09040488B2 Imino sugar derivatives demonstrate potent antiviral activity and reduced toxicity
有权
亚氨基糖衍生物表现出强大的抗病毒活性和降低的毒性
- Patent Title: Imino sugar derivatives demonstrate potent antiviral activity and reduced toxicity
- Patent Title (中): 亚氨基糖衍生物表现出强大的抗病毒活性和降低的毒性
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Application No.: US13061734Application Date: 2009-09-02
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Publication No.: US09040488B2Publication Date: 2015-05-26
- Inventor: Timothy M. Block , Jinhong Chang , Xiaodong Xu
- Applicant: Timothy M. Block , Jinhong Chang , Xiaodong Xu
- Applicant Address: US PA Doylestown US PA Philadelphia
- Assignee: Baruch S. Blumberg Institute,Drexel University
- Current Assignee: Baruch S. Blumberg Institute,Drexel University
- Current Assignee Address: US PA Doylestown US PA Philadelphia
- Agent Joseph F. Aceto
- International Application: PCT/US2009/055658 WO 20090902
- International Announcement: WO2010/027996 WO 20100311
- Main IPC: C07D211/46
- IPC: C07D211/46 ; A61K31/445 ; A61K31/47 ; A61K31/7056

Abstract:
Imino sugars, such as deoxynojirimycin (DNJ), are glucose analogues that selectively inhibit cellular α-glucosidase I and II (enzymes that process N-linked glycans in glycoprotein) and exhibit broad spectrum antiviral activities against many enveloped viruses. Previously we have reported a novel DNJ derivative, OSL-95II, with antiviral activity and reduced cytotoxicity. 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. The antiviral activities were initially tested in bovine viral diarrhea virus (BVDV) infected MDBK cells, yielding several imino sugar derivatives with novel structure and superior antiviral activity and toxicity profile. Furthermore, these new compounds were shown to be active against Dengue virus (DV) and West Nile virus (WNV) infection in BHK cells where potent anti-DV activity having submicromolar EC50 values and SI of greater than 900. These compounds represent a new generation of iminio sugars and their analogues, having application in the clinical treatment of infection of DV and other members of flaviviridae.
Public/Granted literature
- US20110189771A1 Novel Imino Sugar Derivatives Demonstrate Potent Antiviral Activity and Reducted Toxicity Public/Granted day:2011-08-04
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