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Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta

ActiveUS7932260B2Inhibit growth and proliferationInhibit growthBiocideSenses disorderLeukocyte functionWhite blood cell

The invention provides a class of substituted quinazolinone compounds and methods of treating diseases mediated by PI3Kδ activity. The disclosed compounds are useful in treating diseases such as bone-resorption disorders; and cancer, especially hematopoietic cancers, lymphomas, multiple myelomas and leukemia. The compounds are also useful in disrupting or inhibiting cellular processes such as leukocyte function or accumulation, neutrophils function, lymphocyte proliferation, and endogenous immune responses.

Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta

Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta

Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta

Owner:ICOS CORP

5-substituted indazoles as kinase inhibitors

ActiveUS20090203690A1BiocideOrganic active ingredientsGlycogen synthase IGlycogen synthase

The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts,

wherein A, R₁, R₂, R₃and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.

5-substituted indazoles as kinase inhibitors

5-substituted indazoles as kinase inhibitors

5-substituted indazoles as kinase inhibitors

Owner:ABBVIE INC

Albumin fusion proteins

InactiveUS6905688B2Extended shelf lifeRetain activityFungiBacteriaDiseaseAlbumin

The present invention encompasses albumin fusion proteins. Nucleic acid molecules encoding the albumin fusion proteins of the invention are also encompassed by the invention, as are vectors containing these nucleic acids, host cells transformed with these nucleic acids vectors, and methods of making the albumin fusion proteins of the invention and using these nucleic acids, vectors, and/or host cells. Additionally the present invention encompasses pharmaceutical compositions comprising albumin fusion proteins and methods of treating, preventing, or ameliorating diseases, disordrs or conditions using albumin fusion proteins of the invention.

Albumin fusion proteins

Albumin fusion proteins

Albumin fusion proteins

Owner:HUMAN GENOME SCI INC

Bacterial expression of protease inhibitors and variants thereof

ActiveUS20050202535A1Reduce disulfide bondBacteriaPeptide/protein ingredientsProteinase activityProtease

The present invention provides compositions and methods related to expression of protease inhibitors and variants thereof in bacterial species. The present invention further provides fusion nucleic acids, vectors, fusion polypeptides, and processes for obtaining the protease inhibitors.

Bacterial expression of protease inhibitors and variants thereof

Bacterial expression of protease inhibitors and variants thereof

Bacterial expression of protease inhibitors and variants thereof

Owner:GENENCOR INT INC

Diaryl peptides as NS3-serine protease inhibitors of hepatitis C virus

InactiveUS6911428B2BiocideAntiviralsSerine Protease InhibitorsCrystallography

The present invention is directed to certain diaryl amide compounds as NS3-Serine protease inhibitors of hepatitis C virus. A particularly preferred compound is of the formula:

Diaryl peptides as NS3-serine protease inhibitors of hepatitis C virus

Diaryl peptides as NS3-serine protease inhibitors of hepatitis C virus

Diaryl peptides as NS3-serine protease inhibitors of hepatitis C virus

Owner:SCHERING CORP

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.

Imidazolidinones as NS3-serine protease inhibitors of hepatitis C virus

Imidazolidinones as NS3-serine protease inhibitors of hepatitis C virus

Imidazolidinones as NS3-serine protease inhibitors of hepatitis C virus

Owner:SCHERING CORP

Inhibitors of human phosphatidyl-inositol 3-kinase delta

InactiveUS6949535B2Inhibit growthPrevent proliferationAntibacterial agentsBiocideDiseaseLeukocyte function

Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.

Inhibitors of human phosphatidyl-inositol 3-kinase delta

Inhibitors of human phosphatidyl-inositol 3-kinase delta

Inhibitors of human phosphatidyl-inositol 3-kinase delta

Owner:ICOS CORP

Novel peptides as NS3-serine protease inhibitors of hepatitis C virus

InactiveUS20050176648A1BiocideDipeptide ingredientsSerine Protease InhibitorsHepatitis 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.

Novel peptides as NS3-serine protease inhibitors of hepatitis C virus

Novel peptides as NS3-serine protease inhibitors of hepatitis C virus

Novel peptides as NS3-serine protease inhibitors of hepatitis C virus

Owner:MERCK SHARP & DOHME CORP +1

Albumin fusion proteins

InactiveUS6926898B2Avoid lossExtended shelf lifeFungiBacteriaDiseaseAlbumin

The present invention encompasses albumin fusion proteins. Nucleic acid molecules encoding the albumin fusion proteins of the invention are also encompassed by the invention, as are vectors containing these nucleic acids, host cells transformed with these nucleic acids vectors, and methods of making the albumin fusion proteins of the invention and using these nucleic acids, vectors, and / or host cells. Additionally the present invention encompasses pharmaceutical compositions comprising albumin fusion proteins and methods of treating, preventing, or ameliorating diseases, disordrs or conditions using albumin fusion proteins of the invention.

Albumin fusion proteins

Albumin fusion proteins

Albumin fusion proteins

Owner:HUMAN GENOME SCI INC

Inhibitors of human phosphatidylinositol 3-kinase delta

InactiveUS20050261317A1Inhibit growth and proliferationAntibacterial agentsBiocideCancer cellLeukocyte function

Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K5, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.

Inhibitors of human phosphatidylinositol 3-kinase delta

Inhibitors of human phosphatidylinositol 3-kinase delta

Inhibitors of human phosphatidylinositol 3-kinase delta

Owner:ICOS CORP

Macrocyclic NS3-serine protease inhibitors of hepatitis C virus comprising N-cyclic P2 moieties

InactiveUS6846802B2BiocideAntiviralsSerine Protease InhibitorsHepatitis C virus

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.

Macrocyclic NS3-serine protease inhibitors of hepatitis C virus comprising N-cyclic P2 moieties

Macrocyclic NS3-serine protease inhibitors of hepatitis C virus comprising N-cyclic P2 moieties

Macrocyclic NS3-serine protease inhibitors of hepatitis C virus comprising N-cyclic P2 moieties

Owner:SCHERING CORP

Crop plant cystatin proteinase inhibitors encoding nucleic acids and methods of use

InactiveUS7205453B2Protease inhibitorsFermentationPlant cellNucleotide sequencing

Methods and compositions for modulating development and defense responses are provided. Nucleotide sequences encoding maize, soybean, wheat and rice cystatin proteins are provided. The sequences can be used in expression cassettes for modulating development, developmental pathways, and defense responses. Transformed plants, plant cells, tissues, and seed are also provided.

Crop plant cystatin proteinase inhibitors encoding nucleic acids and methods of use

Owner:PIONEER HI BRED INT INC

Methods of increasing endogenous erythropoietin (EPO)

InactiveUS20030153503A1Increase endogenous EPOIncrease endogenous EPO levelOrganic active ingredientsPeptide/protein ingredientsIn vivoBiology

The present invention relates to methods for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo. Methods for treating, pretreating or preconditioning, or preventing erythropoietin-associated conditions are also included. Compounds for use in these methods are provided, as are methods of identifying such compounds.

Methods of increasing endogenous erythropoietin (EPO)

Methods of increasing endogenous erythropoietin (EPO)

Methods of increasing endogenous erythropoietin (EPO)

Owner:FIBROGEN INC

Peptides as NS3-serine protease inhibitors of hepatitis C virus

InactiveUS7169760B2BiocideDipeptide ingredientsDiseaseSerine Protease Inhibitors

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.

Peptides as NS3-serine protease inhibitors of hepatitis C virus

Peptides as NS3-serine protease inhibitors of hepatitis C virus

Peptides as NS3-serine protease inhibitors of hepatitis C virus

Owner:DENDREON PHARMA LLC +1

Boron-containing small molecules

ActiveUS20090227541A1Antibacterial agentsBiocideBoron containingStereochemistry

This invention provides, among other things, novel compounds useful for treating bacterial infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.

Boron-containing small molecules

Boron-containing small molecules

Boron-containing small molecules

Owner:ANACOR PHARMA INC

Stabilization of hypoxia inducible factor (HIF) alpha

InactiveUS20030176317A1Improve heart functionPromote healingOrganic active ingredientsPeptide/protein ingredientsMedicineBiochemistry

The present invention relates to methods of stabilizing the alpha subunit of hypoxia inducible factor (HIF). The invention further relates to methods of preventing, pretreating, or treating conditions associated with HIF, including ischemic and hypoxic conditions. Compounds for use in these methods are also provided.

Stabilization of hypoxia inducible factor (HIF) alpha

Stabilization of hypoxia inducible factor (HIF) alpha

Stabilization of hypoxia inducible factor (HIF) alpha

Owner:FIBROGEN INC

Pyrazole compounds useful as protein kinase inhibitors

InactiveUS6989385B2BiocideSenses disorderArylPTK Inhibitors

This invention describes novel pyrazole compounds of formula IIc: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

Pyrazole compounds useful as protein kinase inhibitors

Pyrazole compounds useful as protein kinase inhibitors

Pyrazole compounds useful as protein kinase inhibitors

Owner:VERTEX PHARMA INC

Methods of isolating amyloid-inhibiting compounds and use of compounds isolated from Uncaria tomentosa and related plants

InactiveUS7285293B2Inhibition formationPromote mental alertnessBiocideNervous disorderAdditive ingredientFractionation

Assay-guided affinity fractionation and reverse phase high pressure liquid chromatography (HPLC) methodology to isolate, test and characterize the most active water-soluble ingredients within Cat's Claw, or Uncaria tomentos. These components appear to account for the majority of the amyloid or Aβ fibrillogenesis inhibitory activity. Individual fractions and / or compounds as isolated by HPLC are tested in relevant in vitro and / or animal models, and found to consistently demonstrate inhibition of amyloid or Aβ fibrillogenesis. Related extraction methods are disclosed.

Methods of isolating amyloid-inhibiting compounds and use of compounds isolated from Uncaria tomentosa and related plants

Methods of isolating amyloid-inhibiting compounds and use of compounds isolated from Uncaria tomentosa and related plants

Methods of isolating amyloid-inhibiting compounds and use of compounds isolated from Uncaria tomentosa and related plants

Owner:UNIV OF WASHINGTON +1

Kinase Inhibitor Phosphonate Conjugates

InactiveUS20070281907A1Increasing cellular accumulationImprove retentionBiocideOrganic active ingredientsKinaseStereochemistry

The invention is related to phosphorus substituted kinase inhibitory conjugates, compositions containing such conjugates, and therapeutic methods that include the administration of such conjugates, as well as to processes and intermediates useful for preparing such conjugates.

Kinase Inhibitor Phosphonate Conjugates

Kinase Inhibitor Phosphonate Conjugates

Kinase Inhibitor Phosphonate Conjugates

Owner:GILEAD SCI INC

Assays for measuring nucleic acid damaging activities

InactiveUS6214552B1Simple and accurate and reliable assayEfficient transferSugar derivativesMicrobiological testing/measurementElectrochemiluminescenceDouble strand

A method for assaying a sample for a nucleic acid damaging activity using at least one singular double-stranded nucleic acid with at least one electrochemiluminescent label, and a method for measuring an inhibitor of a nucleic acid damaging activity with at least one singular double-stranded nucleic acid using at least one electrochemiluminescent label, are disclosed.

Assays for measuring nucleic acid damaging activities

Assays for measuring nucleic acid damaging activities

Assays for measuring nucleic acid damaging activities

Owner:BIOVERIS CORP

1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase

ActiveUS20100015178A1Prevent immunosuppressionUseful in preparationBiocideSenses disorderDiseaseDioxygenase

The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.

1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase

1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase

1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase

Owner:INCYTE

Measles virus peptides with antifusogenic and antiviral activities

InactiveUS6013263AVirusesPeptide/protein ingredientsGp41Biology

The present invention relates to peptides which exhibit potent anti-retroviral activity. The peptides of the invention comprise DP178 (SEQ ID:1) peptide corresponding to amino acids 638 to 673 of the HIV-1LAI gp41 protein, and fragments, analogs and homologs of DP178. The invention further relates to the uses of such peptides as inhibitory of human and non-human retroviral, especially HIV, transmission to uninfected cells.

Measles virus peptides with antifusogenic and antiviral activities

Measles virus peptides with antifusogenic and antiviral activities

Measles virus peptides with antifusogenic and antiviral activities

Owner:TRIMERIS

Dual Variable Domain Immunoglobulins and Uses Thereof

ActiveUS20090304693A1High affinityAntibacterial agentsSenses disorderDiseaseVariable domain

The present invention relates to engineered multivalent and multispecific binding proteins, methods of making, and specifically to their uses in the prevention, diagnosis, and/or treatment of disease.

Dual Variable Domain Immunoglobulins and Uses Thereof

Owner:ABBVIE INC

Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases

InactiveUS20120225057A1BiocideSenses disorderActive agentAcute lymphocytic leukemia

Compounds of the present invention, alone and in combination with other active agents, find utility in the treatment of hyperproliferative diseases, mammalian cancers and especially human cancers including but not limited to for example malignant melanomas, myeloproliferative diseases, chronic myelogenous leukemia, acute lymphocytic leukemia, a disease caused by c-ABL kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.

Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases

Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases

Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases

Owner:DECIPHERA PHARMA LLC

Correction of alpha-1-antitrypsin genetic defects using spliceosome mediated RNA trans splicing

InactiveUS20060234247A1Reduce lungReduce liver pathologySugar derivativesMicrobiological testing/measurementDiseaseRNA Trans-Splicing

The present invention provides methods and compositions for generating novel nucleic acid molecules through targeted spliceosomal mediated RNA trans-splicing. The compositions of the invention include pre-trans-splicing molecules (PTMs) designed to interact with a SERPINA1 target precursor messenger RNA molecule (target pre-mRNA) and mediate a trans-splicing reaction resulting in the generation of a novel chimeric RNA molecule (chimeric RNA). In particular, the PTMs of the present invention include those genetically engineered to interact with SERPINA1 target pre-mRNA so as to result in correction of SERPINA1 genetic defects responsible for AAT deficiency. The PTMs of the invention may also comprise sequences that are processed out of the PTM to yield duplex siRNA molecules directed specifically to mutant SERPIN A1 mRNAs. Such duplexed siRNAs are designed to reduce the accumulation of toxic AAT protein in liver cells. The methods and compositions of the present invention can be used in gene therapy for correction of SERPINA1 disorders such as AAT deficiency.

Correction of alpha-1-antitrypsin genetic defects using spliceosome mediated RNA trans splicing

Correction of alpha-1-antitrypsin genetic defects using spliceosome mediated RNA trans splicing

Correction of alpha-1-antitrypsin genetic defects using spliceosome mediated RNA trans splicing

Owner:VIRXSYS

Lox and loxl2 inhibitors and uses thereof

ActiveUS20090053224A1Block enzymatic activitySlow tumor growthNervous disorderMuscular disorderAngiogenesis growth factorFibrosis

The present application relates to anti-LOX and anti-LOXL2 antibodies and their use in purification, diagnostic and therapeutic methods. Antibodies include monoclonal antibodies, humanized antibodies and functional fragments thereof. Anti-LOX and anti-LOXL2 antibodies can be used to identify and treat conditions such as a fibrotic condition, angiogenesis, or to prevent a transition from an epithelial cell state to a mesenchymal cell state.

Lox and loxl2 inhibitors and uses thereof

Lox and loxl2 inhibitors and uses thereof

Lox and loxl2 inhibitors and uses thereof

Owner:GILEAD BIOLOGICS

Genes encoding novel bacillus thuringiensis proteins with pesticidal activity against coleopterans

InactiveUS7605304B2Improve pesticidal activityStrong specificitySugar derivativesClimate change adaptationAureobasidium sp.Bacillus thuringiensis

The invention provides nucleic acids, and variants and fragments thereof, obtained from strains of Bacillus thuringiensis encoding δ-endotoxins having pesticidal activity against pests of the order Coleoptera. The invention further provides mutagenized nucleic acids that have been modified to encode endotoxins having improved pesticidal activity and/or altered pest specificity. Particular embodiments of the invention provide isolated nucleic acids encoding pesticidal proteins, expression cassettes comprising such nucleic acids, and transformed plants and seeds comprising a nucleic acid of the invention. These compositions find use in methods for controlling pests, especially plant pests.

Owner:EI DU PONT DE NEMOURS & CO

Azepine inhibitors of janus kinases

InactiveUS20090197869A1BiocideSenses disorderJanus kinase activityMedicine

The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.

Azepine inhibitors of janus kinases

Azepine inhibitors of janus kinases

Azepine inhibitors of janus kinases

Owner:INCYTE CORP

Inhibitors of serine proteases, particularly HCV NS3-NS4A protease

InactiveUS7273885B2Inhibit HCV replicationReduce riskBiocidePeptide/protein ingredientsHepatitis c viralSerine Protease Inhibitors

The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.

Inhibitors of serine proteases, particularly HCV NS3-NS4A protease

Inhibitors of serine proteases, particularly HCV NS3-NS4A protease

Inhibitors of serine proteases, particularly HCV NS3-NS4A protease

Owner:VERTEX PHARMA INC

Prevention of disulfide bond reduction during recombinant production of polypeptides

InactiveUS20090053786A1Reduce disulfide bondAnimal cellsBacteriaDisulfide bond reductionAntibody

The invention concerns methods and means for preventing the reduction of disulfide bonds during the recombinant production of disulfide-containing polypeptides. In particular, the invention concerns the prevention of disulfide bond reduction during harvesting of disulfide-containing polypeptides, including antibodies, from recombinant host cell cultures.

Prevention of disulfide bond reduction during recombinant production of polypeptides

Prevention of disulfide bond reduction during recombinant production of polypeptides

Prevention of disulfide bond reduction during recombinant production of polypeptides

Owner:GENENTECH INC

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