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494 results about "Serine protease" patented technology
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Serine proteases (or serine endopeptidases) are enzymes that cleave peptide bonds in proteins, in which serine serves as the nucleophilic amino acid at the (enzyme's) active site. They are found ubiquitously in both eukaryotes and prokaryotes. Serine proteases fall into two broad categories based on their structure: chymotrypsin-like (trypsin-like) or subtilisin-like. In humans, they are responsible for coordinating various physiological functions, including digestion, immune response, blood coagulation and reproduction.
Peptides as NS3-serine protease inhibitors of hepatitis C virus
InactiveUS7012066B2Organic active ingredientsDigestive systemSerine Protease InhibitorsHepatitis C virus
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
Owner:DENDREON PHARMA INC +1
Imidazolidinones as NS3-serine protease inhibitors of hepatitis C virus
InactiveUS6838475B2Reduce frictionReduce wearBiocideOrganic active ingredientsSerine Protease InhibitorsHepacivirus
The present invention discloses novel imidazolidinones which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazolidinones as well as methods of using them to treat disorders associated with the HCV protease.
Owner:SCHERING CORP
(1R,2S,5S)-N-[(1S)-3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide as inhibitor of hepatitis C virus NS3/NS4a serine protease
The present invention discloses the compound of Formula 3 as an inhibitor of HCV protease, as well as methods for preparing the compound. In another embodiment, the invention discloses pharmaceutical compositions comprising the compound as well as methods of using them to treat disorders associated with the HCV protease.
![(1R,2S,5S)-N-[(1S)-3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide as inhibitor of hepatitis C virus NS3/NS4a serine protease](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/68ff82f9-3880-45b4-9833-0144a15a0351/US20050249702A1-20051110-C00001.png "(1R,2S,5S)-N-[(1S)-3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide as inhibitor of hepatitis C virus NS3/NS4a serine protease")
![(1R,2S,5S)-N-[(1S)-3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide as inhibitor of hepatitis C virus NS3/NS4a serine protease](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/68ff82f9-3880-45b4-9833-0144a15a0351/US20050249702A1-20051110-C00002.png "(1R,2S,5S)-N-[(1S)-3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide as inhibitor of hepatitis C virus NS3/NS4a serine protease")
![(1R,2S,5S)-N-[(1S)-3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide as inhibitor of hepatitis C virus NS3/NS4a serine protease](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/68ff82f9-3880-45b4-9833-0144a15a0351/US20050249702A1-20051110-C00003.png "(1R,2S,5S)-N-[(1S)-3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide as inhibitor of hepatitis C virus NS3/NS4a serine protease")
Owner:SCHERING CORP
Acylsulfonamide compounds as inhibitors of hepatitis C virus NS3 serine protease
ActiveUS20060046956A1Modulate activityInhibit HCVBiocideDipeptide ingredientsDiseaseHcv hepatitis c virus
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
Owner:MERCK SHARP & DOHME LLC
Novel peptides as NS3-serine protease inhibitors of hepatitis C virus
The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
Owner:MERCK SHARP & DOHME CORP +1
Macrocyclic NS3-serine protease inhibitors of hepatitis C virus comprising N-cyclic P2 moieties
The present invention discloses novel macrocyclic compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such macrocycles as well as methods of using them to treat disorders associated with the HCV protease.
Owner:SCHERING CORP
Five-membered heterocycles useful as serine protease inhibitors
The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and / or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and / or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
Owner:BRISTOL MYERS SQUIBB CO
Compounds useful in the complement, coagulat and kallikrein pathways and method for their preparation
The present invention is concerned with new compounds, and particularly those having a fused bicyclic ring substituted with an amidine moiety. These compounds are each potent inhibitors of Factor D of the alternate pathway of complement, C1s of the classical pathway of complement, Factors Xa, XIIa, VIIa and thrombin of the coagulation pathway, plasmin in the fibrinolytic pathway, and kallikrein and high molecular weight kininogen in the inflammatory pathways. These proteases, which have serine in their active site, are called serine proteases and they are pivotal to most of the processes of inflammation and coagulation. In fact, these various systems are interactive with one another and it is difficult to activate one pathway without it influencing the others.
Owner:BIOCRYST PHARM INC
3,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis C virus NS3 serine protease
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
Owner:SCHERING CORP
Macrocyclic inhibitors of hepatitis C virus NS3-serine protease
InactiveUS20050119168A1HCV infectionImprove overall utilizationBiocideAntiviralsDiseaseStructural formula
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as pharmaceutical compositions comprising such compounds and methods of using them to treat disorders associated with the HCV protease. The novel compounds typically include a 15-20 member macrocycle and have the general structure of structural Formula 1: wherein Z′, L′, M′, R1, X and D are defined herein.
Owner:MERCK SHARP & DOHME CORP
Cyclobutenedione-containing compounds as inhibitors of hepatitis C virus NS3 serine protease
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
Owner:SCHERING CORP
Novel peptides as NS3-serine protease inhibitors of hepatitis C virus
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
Owner:DENDREON PHARMA LLC +1
Transmembrane serine protease overexpressed in ovarian carcinoma and uses thereof
InactiveUS6942978B1Inhibit expressionTumor rejection antigen precursorsCell receptors/surface-antigens/surface-determinantsADAMTS ProteinsA-DNA
The present invention provides a TADG-12 protein and a DNA fragment encoding such protein. Also provided is a vector / host cell capable of expressing the DNA. The present invention further provides various methods of early detection of associated ovarian and other malignancies, and of interactive therapies for cancer treatment utilizing the DNA and / or protein disclosed herein.
Owner:BIOVENTURES LLC
Biarylmethyl indolines and indoles as antithromboembolic agents
The present invention provides compounds of Formula (I):or a stereoisomer or pharmaceutically acceptable salt or hydrate form thereof, wherein the variables A, B, L1, L2, X1, X2, X3, X4 and W are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and / or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and / or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and / or inflammatory disorders using the same.
Owner:BRISTOL MYERS SQUIBB CO
TADG-15: an extracellular serine protease overexpressed in carcinomas
The present invention provides DNA encoding a TADG-15 protein as well as a TADG-15 protein. Also provided is a vector capable of expressing the DNA of the present invention adapted for expression in a recombinant cell and regulatory elements necessary for expression of the DNA in the cell. The present invention further provides for methods of inhibiting TADG-15 expression and / or protease activity, methods of detecting TADG-15 mRNA and / or protein and methods of screening for TADG-15 inhibitors. Additionally, the present invention provides for cell-specific targeting via TADG-15 and methods of vaccinating an individual against TADG-15. The methods described are useful in the diagnosis, treatment and prevention of cancer, particularly breast and ovarian cancer.
Owner:UNIVERSITY OF ARKANSAS FOR MEDICAL SCIENCES
Compounds as NS3-serine protease inhibitors of hepatitis C virus
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
Owner:MERCK SHARP & DOHME CORP
Inhibitors of serine proteases, particularly hepatitis C virus NS3 protease
The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.
Owner:VERTEX PHARMA INC
Novel inhibitors of hepatitis C virus NS3/NS4a serine protease
InactiveUS20050153900A1Symptoms improvedOrganic active ingredientsBiocideDiseaseSerine Protease Inhibitors
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
Owner:SCHERING CORP
Inhibitors of serine proteases
InactiveUS20070105781A1Reduce riskReduce severityBiocideOrganic active ingredientsMedicinal chemistrySerine
Owner:VERTEX PHARMA INC
Direct determination of vitamin d in serum or plasma
ActiveUS20100068725A1Easy to controlPromote digestionBioreactor/fermenter combinationsBiological substance pretreatmentsSerum igeCompetitive binding
A method for quantitating vitamin D metabolites directly in blood plasma or serum, without the need for prior purification of the vitamin D metabolites, comprising a digestion of the serum proteins with a serine protease such as proteinase K and sequence of steps for inhibiting the proteinase K activity in the competitive binding analysis. The advantages of this method are its high accuracy over the whole range of physiologically relevant values and that it can be easily adapted for a fully automated analysis of serum and plasma samples.
Owner:IMMUNDIAGNOSTIK
Compositions and methods comprising serine protease variants
Owner:DANISCO US INC
Compounds as inhibitors of hepatitis C virus NS3 serine protease
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
Owner:MERCK SHARP & DOHME LLC
(Hetero)aryl-bicyclic heteroaryl derivatives, their preparation and their use as protease inhibitors
The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a partially unsaturated bicyclic heterocyclic ring structure, and B represents an aryl or a heteroaryl group. Preferred compounds of the present invention comprise a benzimidazole or indole nucleus. The compounds of this invention are inhibitors of serine proteases, Urokinase (uPA), Factor Xa (FXa), and / or Factor VIIa (FVIIa), and have utility as anti cancer agents and / or as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals.
Owner:AXYX PHARMA INC
Fluoropyrrolidines as dipeptidyl peptidase inhibitors
The present invention relates to novel compounds, their use for inhibiting serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV) and to methods for their production and their therapeutic utility.
Owner:SMITHKLINE BECKMAN CORP
Sushi peptide multimer
Endotoxin, also known as lipopolysaccharides (LPS), is the major mediator of septic shock due to Gram-negative bacterial infection. Chemically synthesized S3 peptide, derived from Sushi3 domain of Factor C, which is the endotoxin-sensitive serine protease of the limulus coagulation cascade, binds and neutralizes LPS activity. Fluorescent tagged-S3 is shown to detect LPS-containing bacteria. For large-scale production of S3 and to mimic other pathogen-recognizing molecules, tandem multimers of the S3 gene were constructed and expressed in E. coli. Tetramer of S3 for example is shown to display an enhanced inhibitory effect on LPS-induced activities. An affinity matrix based on tetramer of S3 is also shown to be particularly efficient at removing LPS.
Owner:NAT UNIV OF SINGAPORE
Substituted biaryl compounds as factor XIa inhibitors
The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and / or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and / or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and / or inflammatory disorders using the same.
Owner:BRISTOL MYERS SQUIBB CO
Method for modulating activity of HCV protease through use of a novel HCV protease inhibitor to reduce duration of treatment period
Methods are provided for using at least one novel hepatitis C (“HCV”) protease inhibitor in combination with at least one antiviral and / or immunomodulatory agent, which is different from the at least one HCV protease inhibitor, for treating a wide variety of diseases or disorders associated with hepatitis C virus by modulating the activity of HCV protease (for example HCV NS3 / NS4a serine protease) and reducing HCV viral load in a subject in a reduced treatment period. With the present invention, a hepatitis C viral load is reduced in a subject to a concentration of less than 6×10−5 HCV virions per milliliter of plasma in a time period of less than or equal to about 24 weeks. With the present invention, a hepatitis C viral production is suppressed with an effectiveness in a range of 0.7 to 0.997.
Owner:SCHERING CORP
Methods for treating hepatitis C
Methods of treating hepatitis C are provided comprising using a therapeutically effective amount of at least one novel hepatitis C (“HCV”) protease inhibitor or, alternatively, at least one antiviral or immuno-modulating HCV agent, which is not an HCV protease inhibitor, for a first treatment period. Subsequently, a combination of the at least one novel hepatitis C (“HCV”) protease inhibitor and the at least one antiviral or immuno-modulating HCV agent are administered in a therapeutically effective amount for a second treatment period. The methods are provided for treating a wide variety of diseases, disorders and symptoms associated with hepatitis C virus by modulating the activity of HCV protease (for example HCV NS3 / NS4a serine protease) in a subject.
Owner:SCHERING CORP
Six-membered heterocycles useful as serine protease inhibitors
The present invention provides compounds of Formula (I):or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, R3 and R11 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and / or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and / or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and / or inflammatory disorders using the same.
Owner:BRISTOL MYERS SQUIBB CO
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