Wichita State University

Kansas State University Research Foundation

Georgetown University

University of Iowa Research Foundation

The Ohio State University

William C Groutas

Kyeong-Ok Chang

Yunjeong Kim

Brent E Korba

Duy H Hua

Richard A Calderone

Radhakrishnan Padmanabhan

Linda J Saif

Rongze Kuang

Stanley Perlman

Compounds and treatment methods with compounds exhibiting antiviral activity and/or inhibition of viral replication against viruses, particularly those belonging to the picornavirus-like supercluster, including coronavirus having a formula: or a prodrug or pharmaceutically-acceptable salt thereof, where:

Deuterated protease inhibitors

Disclosed herein are protease transition state inhibitor/analogue prodrug compounds selected from the group consisting of esters, carbamates, ester phosphates, and pharmaceutically acceptable salts thereof. Compositions containing such prodrugs are also disclosed, along with methods of using such compounds therapeutically or prophylactically against calicivirus, picornavirus, and/or coronavirus infection, as well as other conditions, such as malaria, cancer, stroke, heart attack, neural degeneration, cataracts, and glaucoma through inhibition of the variety of proteases associated with progression of such conditions.

Protease transition state inhibitor prodrugs

Antiviral protease inhibitors are disclosed, along with related antiviral dipeptidyl compounds, macrocyclic derivatives thereof and methods of using the same to treat or prevent viral infection and disease from coronaviruses, caliciviruses, and picornaviruses.

Small molecule therapeutic inhibitors against picornaviruses, caliciviruses, and coronaviruses

Antiviral protease inhibitors, including peptidyl aldehydes, peptidyl &#x3b1;-ketoamides, peptidyl bisulfate salts, and peptidyl heterocycles, are disclosed, along with related antiviral compounds, and methods of using the same to treat or prevent viral infection and disease. The compounds possess broad-spectrum activity against viruses that belong to the picornavirus-like supercluster, which include important human and animal pathogens including noroviruses, enteroviruses, poliovirus, foot-and-mouth disease virus, hepatitis A virus, human rhinovirus (cause of common cold), human coronavirus (another cause of common cold), transmissible gastroenteritis virus, murine hepatitis virus, feline infectious peritonitis virus, and severe acute respiratory syndrome coronavirus.

Broad-spectrum antivirals against 3C or 3C-like proteases of picornavirus-like supercluster: picornaviruses, caliciviruses and coronaviruses

Antiviral protease inhibitors, including macrocylic transition state inhibitors and peptidomimetics are disclosed, along with related antiviral compounds, and methods of using the same to treat or prevent viral infection and disease. The compounds possess broad-spectrum activity against viruses that belong to the picornavirus-like supercluster, which include important human and animal pathogens including noroviruses, sapoviruses, enteroviruses, poliovirus, foot-and-mouth disease virus, hepatitis A virus, human rhinovirus (cause of common cold), human coronavirus (another cause of common cold), transmissible gastroenteritis virus, murine hepatitis virus, feline infectious peritonitis virus, and severe acute respiratory syndrome coronavirus.

Macrocyclic and peptidomimetic compounds as broad-spectrum antivirals against 3C or 3C-like proteases of picornaviruses, caliciviruses and coronaviruses

Novel classes of 1,2-benzisothiazolinone and isoindolinone compounds and compositions are disclosed. These compounds and compositions are useful in treating, preventing, and/or ameliorating viral, yeast, and fungal infections such as, for example, Hepatitis C Virus, Flavivirus infections,, and candidiasis.

1,2-benzisothiazolinone and isoindolinone derivatives

Novel classes of viral and fungal inhibitors are disclosed. These compounds are useful in treating, preventing, and/or ameliorating viral infections such as, for example, Hepatitis C Virus, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus, and fungal infections such as, for example, candidiasis.

Viral and fungal inhibitors

Sulfamide and bis-sulfamide amino acid derivatives as inhibitors of proteolytic enzymes

Substituted derivatives of 1,2,5-thiadiazolidin-3-one 1,1-dioxides, oligomers containing them, and methods of using them.

1,2,5, thiadiazolidin-3-one 1,1-dioxide derivatives

Isothiazolidin-3-one-1,1 dioxide, 3-oxo-1,2,5-thiadiazolidine-1,1,-dioxide and derivatives thereof, reduce or inhibit the activity of serine proteases. Such compounds are useful as anti-inflammatory and anti-metastatic agents.

Serine protease inhibitors

Certain amino-acid derivatives are disclosed as effective inhibitors of human leukocyte elastase and therefore useful in preventing the imbalance of this proteolytic enzyme in vivo. The compounds specifically are derivatives L-valine, L-norvaline, L-norleucine, and L-methionine methyl ester azolides succinimides or pyridones and sulfonate salts, and related compounds such as L-leucine and L-phenylalanine methyl ester derivatives. The compounds were found to be excellent inhibitors in that they embody both inhibitory and anti-oxidant or anti-inflammatory activity.

Growing community of inventors

Wichita, KS, United States of America

William C Groutas