1,721,119 research outputs found
1,2,5-thiadiazolidin-3-one 1,1-dioxide derivatives
No full textWSU inventor: Groutas, William C., Dept. of Chemistry, College of Liberal Arts and SciencesApplication No: EP98942192A filed August 21, 1998. Patent No: EP1011668A1 granted June 28, 2000.Abstract not available for EP1011668A1. Abstract of corresponding document: WO9909977A1; Substituted derivatives of 1,2,5-thiadiazolidin-3-one 1,1-dioxides, oligomers containing them, and methods of using them, are disclosed
Novel serine protease inhibitors: Derivatives of isothiazolidin-3-one-1,1 dioxide and 3-oxo-1,2,5-thiadiazolidine-1,1-dioxide
No full textWSU inventor: Groutas, William C., Dept. of Chemistry, College of Liberal Arts and SciencesApplication No: EP95908003A filed January 3, 1995. Patent No: EP0739338A1 granted October 30, 1996.Abstract not available for EP0739338A1. Abstract of corresponding document: WO9518797A1: 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
Amino acid derivatives useful for deactivating enzymes
No full textWSU inventor: Groutas, William C., Dept. of Chemistry, College of Liberal Arts and SciencesApplication No: EP86109849A filed July 17, 1986. Patent No: EP0209855A2 granted January 28, 1987.Certain amino-acid derivatives having three or four carbon straight alkyl chains 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 L-valine, L-norvaline, L-norleucine, and L-methionine methyl ester azolides and sulfonate salts, and these compounds plus L-leucine and L-phenylalanine methyl ester sulfonate salts. The sulfonate salts were found to be excellent inhibitors in that they embody both inhibitory and anti-oxidant activity
Conformationally-constrained inhibitors of 3C or 3C-like proteases
No full textWSU inventor: Groutas, William C., Dept. of Chemistry, College of Liberal Arts and SciencesInternational Application No: PCT/US2022/014375 filed January 28, 2022. Patent No: WO/2022/165220 granted August 4, 2022.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
Protease transition state inhibitor prodrugs
No full textWSU inventor: Groutas, William C., Dept. of Chemistry, College of Liberal Arts and SciencesInternational Application No: PCT/US2017/044485 filed July 28, 2017. Patent No: WO/2018/023054 granted February 1, 2018.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
Small molecule therapeutic inhibitors against picornaviruses, caliciviruses, and coronaviruses
No full textWSU inventor: Groutas, William C., Dept. of Chemistry, College of Liberal Arts and SciencesInternational Application No: PCT/US2017/037920 filed June 16, 2017. Patent No: WO/2017/222935 granted December 28, 2017.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
Broad spectrum antivirals against coronavirus
No full textWSU inventor: Groutas, William C., Dept. of Chemistry, College of Liberal Arts and SciencesInternational Application No: PCT/US2021/024790 filed March 30, 2021. Patent No: WO/2021/202460 granted October 7, 2021.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: (I) where X comprises a cyclic moiety, R2 is a branched or unbranched alkyl, cycloalkyl, aryl, arylalkyl, alkenyl, alkynyl, amino acid side chain, bicyclic or tricyclic side chain, combinations, and substituted forms thereof, and Z is selected from the group consisting of C1-C6 hydroxyalkyl, aldehydes, alpha- ketoamides, and bisulfite salts, and in particular -CH2OH, -CHO, -CH(0H)S03-Na+, and - [0(C=0)Rw]S03-Na+
Broad spectrum antivirals against coronavirus
No full textWSU inventor: Groutas, William C., Dept. of Chemistry, College of Liberal Arts and SciencesApplication No: EP21781006A filed March 30, 2021. Patent No: EP4126816A1 granted February 8, 2023.Abstract not available for EP4126816A1 - abstract of corresponding document: WO2021202460A1Compounds exhibiting antiviral activity and/or inhibition of viral replication against viruses, particularly those belonging to the picornavirus-like supercluster, including coronavirus having a formula: (I) where X comprises a cyclic moiety, R is a branched or unbranched alkyl, cycloalkyl, aryl, arylalkyl, alkenyl, alkynyl, amino acid side chain, bicyclic or tricyclic side chain, combinations, and substituted forms thereof, and Z is selected from the group consisting of C-C hydroxyalkyl, aldehydes, alpha- ketoamides, and bisulfite salts, and in particular -CHOH, -CHO, -CH(0H)S0 Na, and - [0(C=0)R]S0 Na
Deuterated protease inhibitors
No full textWSU inventor: Groutas, William C., Dept. of Chemistry, College of Liberal Arts and SciencesApplication No: 17/343334 filed June 9, 2021. Patent No: US 20210380531 A1 granted December 9, 2021.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: ##STR00001## or a prodrug or pharmaceutically-acceptable salt thereof, where: each X comprises at least one cyclic moiety directly attached to the oxygen or connected via an alkyl linkage, where at least one of the linkage and/or the X moiety comprises a deuterium substitution; and Z is selected from the group consisting of aldehydes and bisulfite salts, or the ester or carbamate prodrugs thereof
Deuterated protease inhibitors
No full textWSU inventor: Groutas, William C., Dept. of Chemistry, College of Liberal Arts and SciencesInternational Application No: PCT/US2021/036625 filed June 9, 2021. Patent No: WO/2021/252634 granted December 16, 2021.Compounds and treatment methods with compounds exhibiting antiviral activity and/or inhibition of viral replication against viruses, particularly those belonging to the picornaviru s -like supercluster, including coronavirus having a formula: (I) or a prodrug or pharmaceutically-acceptable salt thereof, where: each X comprises at least one cyclic moiety directly attached to the oxygen or connected via an alkyl linkage, where at least one of the linkage and/or the X moiety comprises a deuterium substitution; and Z is selected from the group consisting of aldehydes and bisulfite salts, or the ester or carbamate prodrugs thereof
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