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113 results about "Viral protease" patented technology

Viral proteases are enzymes (endopeptidases EC 3.4.2) encoded by the genetic material (DNA or RNA) of viral pathogens. The role of these enzymes is to catalyze the cleavage of specific peptide bonds in viral polyprotein precursors or in cellular proteins. In most cases these proteolytic events are essential for the completion...

Colon targeted delivery system

InactiveUS6039975ADrageesPlasticizerMedicine
A novel delivery system for targeting drugs to the colon is herein described. The system is a tablet comprised of three parts: 1) an outer enteric coating, 2) an inner semi-permeable polymer membrane containing a plasticizer and 3) a central core comprising swelling excipients and an active ingredient. The novel dosage form described herein will release the drug consistently in the colon by a time-dependent explosion mechanism. This delivery system is particularly suitable for delivering viral protease inhibitors to the colon.
Owner:F HOFFMANN LA ROCHE & CO AG

Resistance-repellent retroviral protease inhibitors

Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.
Owner:SEQUOIA PHARMACEUTICALS INC

Pyrrolidine derivatives for use in treating heaptitis c virus infection

InactiveUS20060142204A1Good biological propertiesIncrease biological penetrationAntibacterial agentsBiocideDiseaseProteinase activity
The present invention relates to novel hepatitis C virus (“HCV”) protease inhibitors or other flavivirus protease inhibitors having the general structure (I) or (II), pharmaceutical compositions containing one or more such inhibitors, methods for preparing such inhibitors, uses of these compounds to treat hepatitis C and related disorders together with their use for their activity towards NS3 serine protease, intermediary compounds for the method of preparation of said compounds and screening methods. The invention specifically discloses novel chemical compounds as inhibitors of the HCV serine protease.
Owner:GENOSCI PHARMA

Resistant-repellent retroviral protease inhibitors

Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.
Owner:SEQUOIA PHARMACEUTICALS INC

.alpha.- and .beta.-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors

.alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Owner:GD SEARLE & CO

Modified Foot-And-Mouth Disease Virus 3C Proteases, Compositions And Methods Thereof

This application is directed generally to foot-and-mouth disease virus (FMDV) 3C proteases that have been modified by mutating a polynucleotide sequence coding for the FMDV 3C protease. The modified FMDV proteases exhibit proteolytic activity on FMDV P1 precursor protein and exhibit a reduction in one or more toxic or inhibitory properties associated with an unmodified FMDV 3C protease on a host cell used to recombinantly produce it. Vectors carrying polynucleotides encoding modified FMDV 3C protease sequences can induce production of FMDV virus-like particles in a host cell when expressed in the host cell. The modified FMDV 3C proteases can generally be used to produce immunogenic FMDV preparations capable of inducing an immune response against FMDV.
Owner:THE GOVERNMENT OF THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SEC OF HOMELAND SECURITY

Resistance-repellent retroviral protease inhibitors

InactiveUS20050209301A1Prevent slow emergenceSlow emergenceBiocideOrganic chemistryRetroviral protease inhibitorViral protease
Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.
Owner:SEQUOIA PHARMACEUTICALS INC

Α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors

α- and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Owner:GD SEARLE & CO

Recombinant human serum transferrins containing peptides for inducing apoptosis in HIV-1 infected cells

A mammalian protein, like the human serum transferrin (HST), is modified with an inserted peptide sequence flanked at both ends by cleavage sites. The peptide insert contains a motif known to induce apoptosis in cells and the cleavage sites are specific for the viral protease of HIV-1. The delivery of such recombinant transferrin into an HIV-1 infected cell results in the release of the peptide which then induces apoptosis. The peptide is inserted into surface exposed loops of the N-terminal lobe of the HST containing the RGD motif flanked by two modified p17 / p24 HIV-1 protease cleavage sites. When delivered to the infected cell the cleavage of the loop inserted sequences by the HIV-1 protease results in the release of the central RGD-containing peptide sequences. Peptides containing the RGD motif (arginine, glycine, aspartic acid) have been shown to induce cell apoptosis even in small concentrations.
Owner:TOMYCZ NESTOR D

Alpha- and beta-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors

alpha- and beta-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Owner:GD SEARLE & CO

Α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors

α- and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Owner:GD SEARLE & CO

Inhibitors of coronavirus protease and methods of use thereof

This invention provides organic boron-containing compounds, compositions thereof, and methods of using such compounds and compositions for inhibiting coronavirus protease(s) and for treating infections.
Owner:FULCRUM PHARMA +1

Macrocyclic compounds as antiviral agents

A class of macrocyclic compounds of formula (I), wherein R1, R3, R4, Ra, Rb, A, Z, Y, X, M, W, n and m are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes 5 for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection. Formula (I):
Owner:MERCK SHARP & DOHME LLC

Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors

Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
Owner:GD SEARLE & CO

Resistance-repellent retroviral protease inhibitors

Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.
Owner:SEQUOIA PHARMACEUTICALS INC

Structure and application of Enterovirus 71 3C protease

The invention discloses a structure and application of an Enterovirus 71 (EV71) 3C protease and belongs to the field of RNA virus protein. The invention also discloses an application of the 3C protease and a substrate binding groove thereof in drug design. The protein provided by the invention has a special substrate binding groove and new EV71 virus 3C protease drugs are designed according to the spatial structure of the substrate binding groove, thus the inhibitors aiming at the EV71 virus 3C protease, which are more specific and have better effect, can be obtained, potential drug candidates can be provided for the clinical treatment of hand, foot and mouth disease and the EV71 virus 3C protease has very high application value.
Owner:INST OF MICROBIOLOGY - CHINESE ACAD OF SCI

3D-Structure model of SARS coronavirus 3CL protease and anti-SARS drugs

InactiveUS20060142383A1BiocideHydrolasesCinanserinProteinase activity
The present invention discloses 3D-structure of SARS-CoV Viral 3CL Protease obtained through molecular simulation. The 3D-structure is used as a drug target for screening the existing medical database CMC (Comprehensive Medicinal Chemistry, MDL Information System, Inc.), and a group of compounds which have the activity of inhibiting SARS-CoV virus 3CL Protease are found. Cinanserin was tested at molecular and viral levels, and it was found to be able to inhibit the SARS-CoV viral 3CL protease and SARS-CoV viruses. Cinanserin analogs were synthesized and tested at molecular and viral levels, they were found to be able to inhibit the SARS-CoV virus 3CL Protease and SARS-CoV viruses, and may be used for treating and / or preventing SARS-CoV virus infection.
Owner:SHANGHAI LEAD DISCOVERY PHARMA +1

HIV-1 virus protease inhibitor drug resistance mutation detection kit and method

The invention relates to an HIV-1 protease inhibitor drug resistance mutation detection method and a kit. Specifically, the invention also discloses a probe for detection of human immunodeficiency virus protease gene drug resistance mutation, and the probe includes a probe for detection of protease gene D30N mutation, a probe for detection of protease gene V32I mutation, a probe for detection of protease gene M46I and M46L mutation, a probe for detection of protease gene I47V and I47A mutation, a probe for detection of protease gene G48V mutation, a probe for detection of protease gene I50V mutation, a probe for detection of protease gene I54V mutation, a probe for detection of protease gene V82A, V82F, V82T and V82S mutation, a probe for detection of protease gene I84V mutation, a probe for detection of protease gene N88D mutation, and a probe for detection of protease gene L90M mutation.
Owner:ZHEJIANG UNIV

Drug screening model of targeting coronavirus protease and application thereof

The present invention provides a novel cell-based drug screening model of targeting coronavirus protease. In the processing products of the coronavirus polyprotein 1a(1ab), nsp3, nsp4 and nsp6 contain transmembrane (TM) domains which can mediate the protein to locate on the cell endoplasmic reticulum (ER) membrane. Using the characteristics that nsp3, nsp4 and nsp6 contain transmembrane domains and the protein is located in the cell, the present invention constructs a eukaryotic expression DNA construct by secretion reporter gene, wherein the eukaryotic expression DNA construct consists of coronavirus proteases - protease recognition sites - secretion reporter genes. After cell transfection, the expression products of the active releasing reporter gene are cut by the coronavirus protease and are secreted into the cellular supernatant; the activity of the coronavirus protease is detected by the activity of the reporter genes in the cellular supernatant and is used for coronavirus drug screening.
Owner:INST OF RADIATION MEDICINE ACAD OF MILITARY MEDICAL SCI OF THE PLA

Activatable toxin complexes comprising a cleavable inhibitory peptide

The present invention relates to activatable toxin complexes which include a cleavable inhibitory peptide. More specifically, the complexes comprise a cell targeting domain, a toxin catalytic domain, a specific protease cleavage site and an inhibitory peptide domain. The inhibitory peptide prevents the catalytic domain from exerting toxic effects until its release from the complex by the action of a protease, such a viral protease, at the protease cleavage site. Further provided are pharmaceutical compositions comprising the complexes and use thereof for treating infections and malignant disease.
Owner:RAMOT AT TEL AVIV UNIV LTD

Application of MERS-CoV 3CLpro (Middle East respiratory syndrome coronavirus 3C-like protease) as deubiquitinating enzyme and interferon inhibitor

The invention relates to the field of biomedicine, in particular to application of MERS-CoV 3CLpro (Middle East respiratory syndrome coronavirus 3C-like protease) as a deubiquitinating enzyme and interferon inhibitor. The invention provides a novel deubiquitinating enzyme and interferon inhibitor; the new understanding of the functionality of human coronavirus proteinase can be expanded; theoretical basis can be provided for the research on coronavirus and host antiviral natural immunization and the research on antiviral drugs using viral proteinase as a target.
Owner:ACADEMY OF MILITARY MEDICAL SCI

Substituted quinoline-2-formaldehyde-phenylhydrazone derivative, and preparation method and application thereof

The present invention relates to a substituted-quinoline-2-formaldehyde-phenylhydrazone derivative and a preparation method and application thereof, and in particular relates to a novel 4-acyl-quinoline-2-formaldehyde-phenylhydrazone derivative, and a preparation method and application thereof to preparation of therapeutic drugs for dengue fever and dengue hemorrhagic fever caused by dengue virus. A structure of the compound is shown as a formula 1. The compound can be used as a protease inhibitor for a dengue virus NS2B-NS3, so as to block further proliferation of the dengue virus in a host.
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI +1
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