Baruch S. Blumberg Institute

Drexel University

Ortho-mcneil Pharmaceutical Corp.

Hepagene Therapeutics (hk) Limited

Arbutus Biopharma Corporation

Philadelphia Health and Education Corporation

Institute for Hepatitis and Virus Research

Janssen Pharmaceutica Nv

Enantigen Therapeutics, Inc.

Hepagene Therapeutics Limited

Xiaodong Xu

Timothy Michael Block

Andrea Cuconati

Ju-Tao Guo

Hong Ye

Tong Xiao

Yanming Du

Jinhong Chang

Todd C Henninger

Mark J Macielag

Steven David Paget

Xiaoqing Xu

Eugene B Grant

Huagang Lu

Michele Ann Weidner-Wells

Haitao Guo

Simon David Peter Baugh

Dawei Cai

Manomi A Tennakoon

Simon David Baugh

Eugene B Iii Grant

The present technology is directed to compounds, compositions, and methods related to inhibition of ASK1. In particular, the present compounds (e.g., compounds of Formula I as defined herein) and compositions may be used to treat ASK1-mediated disorders and conditions, including, e.g., fibrotic diseases and acute and chronic liver diseases, among others.

Urea derivatives as inhibitors of ASK1

The present technology is directed to compounds, compositions, and methods related to modulation of FXR. In particular, the present compounds and compositions may be used to treat FXR-mediated disorders and conditions, including, e.g., liver disease, hyperlipidemia, hypercholesteremia, obesity, metabolic syndrome, cardiovascular disease, gastrointestinal disease, and atherosclerosis, and renal disease.

Nitrogen-containing heterocyclic compounds as FXR modulators

The present technology is directed to compounds of formula (II) as well as compositions thereof and methods related to modulation of FXR. In particular, the present compounds and compositions may be used to treat FXR-mediated disorders and conditions, including, e.g., liver disease, hyperlipidemia, hypercholesteremia, obesity, metabolic syndrome, cardiovascular disease, gastrointestinal disease, and atherosclerosis, and renal disease. 

Heterocyclic containing cyclopropyl FXR modulators

Pharmaceutical compositions of the invention comprise alkylated imino sugars derivatives having a disease-modifying action in the treatment of diseases associated with glucosidase activity that include Viral hemorrhagic fevers, and any other diseases involving glucosidase activity.

Alkylated imino sugars exhibiting glucosidase inhibition and their method of use

Pharmaceutical compositions of the invention comprise substituted aminothiazoles derivatives having a disease-modifying action in the treatment of diseases associated with unregulated cell growth that include hepatocellular carcinoma, and infection with a hepatitis virus.

Substituted aminothiazoles as inhibitors of cancers, including hepatocellular carcinoma, and as inhibitors of hepatitis virus replication

The present invention provides novel compounds of formula (I) and methods of use thereof. In certain embodiments, the compounds of the invention are useful as nucleocapsid assembly inhibitors. In other embodiments, the compounds of the invention are useful as pregenomic RNA encapsidation inhibitors of Hepatitis B virus (HBV). In yet other embodiments, the compounds of the invention are useful for the treatment of viral infection, including HBV and related viral infections.

Antiviral agents against HBV infection

The present invention provides sulfamoylbenzamide derivatives, and pharmaceutical compositions thereof. In certain embodiments, the compounds and pharmaceutical compositions of the invention inhibit pregenomic RNA encapsidation. In other embodiments, the compounds and pharmaceutical compositions of the invention are useful for treating Hepatitis B virus (HBV) infection.

Sulfamoylbenzamide derivatives as antiviral agents against HBV infection

Pharmaceutical compositions of the invention comprise covalently closed circular DNA formation inhibitors having a disease-modifying action in the treatment of diseases associated with the formation of covalently closed circular DNA that include hepatitis B infection, and any disease involving formation of covalently closed circular DNA.

Inhibitors of hepatitis B virus covalently closed circular DNA formation and their method of use

Pharmaceutical compositions of the invention comprise triazolopyrimidines useful for the treatment of hepatitis virus in a patient.

Inhibitors of secretion of hepatitis B virus antigens

Pharmaceutical compositions of the invention comprise sulfamoylbenzamide derivative useful as pregenomic RNA encapsidation inhibitors, useful for the treatment of Hepatitis B virus (HBV) infection.

Imino sugars, such as deoxynojirimycin (DNJ), are glucose analogues that selectively inhibit cellular &#x3b1;-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.

Imino sugar derivatives demonstrate potent antiviral activity and reduced toxicity

A pharmaceutical composition comprising an effective amount of a compound of formulas (I-III) and a pharmaceutically acceptable carrier. Methods for treating a hepatitis virus in a patient comprising administering an effective amount of the compound of formulas (I-III) are also presented.

Substituted triazolo[1,5-A]pyrimidines as antiviral agents

The present invention relates to compounds having a structure according to Formula I wherein n, m, z, R, R, R, R, R, R, A, E, X, Y, a and b are as defined above;or an optical isomer, diastereomer or enantiomer thereof; a pharmaceutically acceptable salt, hydrate, or prodrug thereof.

Growing community of inventors

Doylestown, PA, United States of America

Xiaodong Xu