110 results about "Viral protease" patented technology

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.

The invention relates to sulfonamide-containing hydroxyethylamine protease inhibitor compounds, their process of making, composition and method of use for inhibiting retroviral proteases such as human immunodeficiency virus.

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.

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.

.alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

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.

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.

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.

The invention provides methods of synthesizing a viral protease inhibitor in high yield, without using expensive catalysts or challenging reaction conditions.

alpha- and beta-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

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.

A class of macrocyclic compounds of formula (I), wherein R¹, R³, R⁴, R^a, R^b, 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):

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.

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.

The invention provides methods of synthesizing compounds in an asymmetric or enantioenriched fashion, wherein the compounds are useful intermediates in the synthesis of viral protease inhibitors.

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.

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.

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.

This invention pertains to materials and methods for the treatment of patients with coronavirus infection and the control of zoonotic disease outbreaks using broad-spectrum non-covalent coronavirus protease inhibitors.

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.

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.

This invention relates to a method for producing a tobacco etch virus protease by means of genetic engineering and the application thereof, beloning to the genetic engineering field. The preparation of his-tagged recombinant tobacco etch virus protease comprises the expression of the soluble tobacco etch virus protease with his-tag in E.coli, and one-step purification through Ni2+ affinity chromatography. The protease can specificly identify and excise the substrates with excision sites of tobacco etch virus protease, with high efficiency and low cost. It can be used as the tool protease in spcificly excising proteins, polypeptides and recombinant fused proteins, which can be used in research of bio-pharmacy manufacturing, genetic engineering, biochemistry, molecular biology, and so on.