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545 results about "Enzyme Inhibitor Agent" patented technology
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Method of prevention and treatment of aging and age-related disorders including atherosclerosis, peripheral vascular disease, coronary artery disease, osteoporosis, arthritis, type 2 diabetes, dementia, alzheimer's disease and cancer
This invention relates to a method for prevention and treatment of aging and age-related disorders including atherosclerosis, peripheral vascular disease, coronary artery disease, osteoporosis, type 2 diabetes, dementia and some forms of arthritis and cancer in a subject comprising administering to said subject, separately, sequentially or simultaneously a therapeutically effective dosage of each component or combination of statins, bisphosphonates, cholesterol lowering agents or techniques, interleukin-6 inhibitor / antibody, interleukin-6 receptor inhibitor / antibody, interleukin-6 antisense oligonucleotide (ASON), gp130 protein inhibitor / antibody, tyrosine kinases inhibitors / antibodies, serine / threonine kinases inhibitors / antibodies, mitogen-activated protein (MAP) kinase inhibitors / antibodies, phosphatidylinositol 3-kinase (PI3K) inhibitors / antibodies, Nuclear factor κB (NF-κB) inhibitors / antibodies, IκB kinase (IKK) inhibitors / antibodies, activator protein-1 (AP-1) inhibitors / antibodies, STAT transcription factors inhibitors / antibodies, altered IL-6, partial peptides of IL-6 or IL-6 receptor, or SOCS (suppressors of cytokine signaling) protein, or a functional fragment thereof, administered separately, in sequence or simultaneously. Inhibition of the signal transduction pathway for Interleukin 6 mediated inflammation is key to the prevention and treatment of atherosclerosis, peripheral vascular disease, coronary artery disease, aging and age-related disorders including osteoporosis, type 2 diabetes, dementia and some forms of arthritis and tumors. Inhibition of Interleukin 6 mediated inflammation may be achieved indirectly through regulation of endogenous cholesterol synthesis and isoprenoid depletion or by direct inhibition of the signal transduction pathway utilizing interleukin-6 inhibitor / antibody, interleukin-6 receptor inhibitor / antibody, interleukin-6 antisense oligonucleotide (ASON), gp130 protein inhibitor / antibody, tyrosine kinases inhibitors / antibodies, serine / threonine kinases inhibitors / antibodies, mitogen-activated protein (MAP) kinase inhibitors / antibodies, phosphatidylinositol 3-kinase (PI3K) inhibitors / antibodies, Nuclear factor κB (NF-κB) inhibitors / antibodies, IκB kinase (IKK) inhibitors / antibodies, activator protein-1 (AP-1) inhibitors / antibodies, STAT transcription factors inhibitors / antibodies, altered IL-6, partial peptides of IL-6 or IL-6 receptor, or SOCS (suppressors of cytokine signaling) protein, or a functional fragment thereof. Said method for prevention and treatment of said disorders is based on inhibition of Interleukin-6 inflammation through regulation of cholesterol metabolism, isoprenoid depletion and / or inhibition of the signal transduction pathway.
Owner:OMOIGUI OSEMWOTA SOTA
4-oxoquinoline compound and use thereof as pharmaceutical agent
An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I]wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.
Owner:JAPAN TOBACCO INC
Acc inhibitors and uses thereof
The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
Owner:NIMBUS DISCOVERY INC +1
Macrocylic oximyl hepatitis c protease inhibitors
InactiveUS20080181868A1Inhibit serine protease activityInhibitory activityBiocidePeptide/protein ingredientsHepatitis c viralEnzyme Inhibitor Agent
The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof:
which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Owner:ENANTA PHARM INC
Sheddase inhibitors combined with cd30-binding immunotherapeutics for the treatment of cd30 positive diseases
The present invention is directed to pharmaceutical methods for the treatment of CD30 positive diseases, such as Hodgkin's disease, by administration of a combination of at least one sheddase inhibitor and at least one anti-CD30 immunotherapeutic.
Owner:INCYTE
Acyclic oximyl hepatitis c protease inhibitors
The present invention discloses compounds of formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof:which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Owner:ENANTA PHARM INC
Tank-binding kinase inhibitor compounds
Compounds having the following formula (I) and methods of their use and preparation are disclosed:
Owner:GILEAD SCI INC
Administration of HCV protease inhibitors in combination with food to improve bioavailability
InactiveUS20060281688A1Improve bioavailabilityBiocideDipeptide ingredientsEnzyme Inhibitor AgentEnhanced bioavailability
Methods of treating, preventing or ameliorating one or more symptoms of hepatitis C in a subject comprising the step of administering at least one HCV protease inhibitor in combination with food are provided. Also provided are methods of increasing bioavailability of an HCV protease inhibitor and methods of increasing serum levels of an HCV protease inhibitor in a subject. All methods comprise adminstering at least one HCV protease inhibitor in combination with food, the at least one HCV protease inhibitor selected from the group consisting of compounds of Formulae I-XXVI, described herein. Administration of compounds of the present invention in combination with food provides improved bioavailability and increased peak serum levels of the compounds as compared to administration without food.
Owner:MERCK SHARP & DOHME CORP
HCV NS3 Protease Inhibitors
InactiveUS20100099695A1Likelihood of moreSeverity of moreBiocideTripeptide ingredientsEnzyme Inhibitor AgentHcv hepatitis c virus
The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
Owner:MERCK SHARP & DOHME CORP +1
Substituted amide beta secretase inhibitors
Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
Owner:MERCK SHARP & DOHME LLC
Bi-Aryl Meta-Pyrimidine Inhibitors of Kinases
The invention provides methods of treating a disease selected from systemic sclerosis, rheumatoid arthritis, mastocytosis, and chronic eosinophilic leukemia comprising administering biaryl meta-pyrimidine compounds having the general structure (A) to a subject in need thereof. The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the JAK kinase family, and various other specific receptor and non-receptor kinases.
Owner:IMPACT BIOMEDICINES INC
Method and composition used for obtaining neuron-like cells from non-neuronal cells via reprogramming
ActiveCN105039258ALow costEasy to operateNervous disorderDrug screeningPTK InhibitorsEnzyme Inhibitor Agent
The invention discloses a method and a composition used for obtaining neuron-like cells from non-neuronal cells via reprogramming. The composition comprises a neuron-like characteristic chemical inducer; the neuron-like characteristic chemical inducer comprises an arbitrary combination of the following ingredients: 1) a cyclic adenosine monophosphate agonist; 2) neurogenic small molecules; 3) glycogen synthase kinase inhibitors, 4) TGF beta receptor inhibitors; 5) BET family bromodomain inhibitors; and 6) a selective inhibitor of Rho-associated, coiled-coil containing protein kinase and / or a p38 mitogen-activated protein kinase inhibitor; wherein 6) is a selective ingredient. The composition used for providing non-neuronal eukaryotic cells with neuron-like characteristics is capable of producing more than 90% TUJ1 positive cells in 16 days of induction. The neuron-like cells obtained via chemical induction possess neuronal specific expression profiles, are capable of generating action potential, and forming functional synapses via further maturation promotion.
Owner:PEKING UNIV +1
Hcv ns3 protease inhibitors
ActiveUS20140296136A1Likelihood of moreSeverity of moreOrganic active ingredientsTripeptide ingredientsEnzyme Inhibitor AgentHcv hepatitis c virus
The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
Owner:MERCK SHARP & DOHME LLC +2
Imidazopyridine Kinase Inhibitors
The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
Owner:GLAXO SMITHKLINE LLC
Immunoactive Compositions for Improved Oral Delivery of Vaccines and Therapeutic Agents
InactiveUS20080226682A1Raise the ratioImprove absorption and bioavailabilitySsRNA viruses negative-senseBiocideEnzyme Inhibitor AgentIsoflavones
The present invention concerns methods and compositions for improved oral delivery of bioactive agents, such as vaccines. In preferred embodiments, the compositions comprise at least one lectin, saponin, polyunsaturated fatty acid and / or isoflavone. In further embodiments, the compositions may further comprise at least one protease inhibitor, buffer and / or surfactant. In more preferred embodiments, the lectins, saponins, fatty acids, isoflavones and / or protease inhibitors may be derived from extracts, homogenates, finely ground powders or derivatives of plant or animal material, such as beans, nuts, peas, fish meal or krill. The relative amounts of various naturally occurring materials contained in the compositions may be selected to optimize the concentrations of one or more lectins, saponins, polyunsaturated fatty acids and / or isoflavones. The compositions are of use for oral delivery of a wide variety of bioactive agents, particularly protein or peptide based agents.
Owner:PEROS SYST TECH
Treatment of cancer using Anti-cd19 chimeric antigen receptor
PendingUS20190388471A1Enhances activity of CAR-expressingGood curative effectPolypeptide with localisation/targeting motifImmunoglobulin superfamilyDiseaseEnzyme Inhibitor Agent
The invention provides compositions and methods for treating diseases associated with expression of CD19, e.g., by administering a recombinant T cell comprising the CD19 CAR as described herein, in combination with a kinase inhibitor, e.g., a kinase inhibitor described herein. The invention also provides kits and compositions described herein.
Owner:THE TRUSTEES OF THE UNIV OF PENNSYLVANIA +1
Use of betulinic acid in preparing glycosidase inhibitor medicine
InactiveCN101416971ALow costRich sourcesOrganic active ingredientsMetabolism disorderLupeolDrug excipient
The invention provides the application of betulinic acid and salts thereof suitable for medical purpose in the preparation of a drug of a glycosidase inhibitor. The compound of the invention is the compound of lupeol type pentacyclic triterpene acid obtained by separating lagerstroemia plants. Pharmacological tests prove that the compound has obvious effect in inhibiting Alpha-glucosidase, the inhibitory activity of which exceeds acarbose 100% for initial therapy. Therefore, drug compositions made from the compound or the salts thereof suitable for medical purpose and drug excipients or carriers allowable for preparation can be applied to the preparation of drugs for preventing or treating Type II Diabetes, namely, noninsulin-dependent diabetes mellitus. The constitutional formula shown in formula (1) of the invention is shown as above.
Owner:ZHEJIANG UNIV
Anti-enterovirus 71 (EV71) caprolactam compounds, and preparation method and application thereof
The invention relates to a caprolactam anti-enterovirus 71 (EV71) 3C protease inhibitor with a structural formula shown as compounds (M). Each variable in the structure is defined as the specification. The compounds can effectively inhibit or block replication of enterovirus 71. The invention relates to discovery and application of compounds comprising a structure of formula (M), various optical isomers thereof, metabolites with pharmaceutically activity, pharmaceutically acceptable salts, solvates and prodrugs in preparing antiviral drugs for treating virus infections of hand-foot-and-mouth diseases. The invention also relates to an intermediate and a synthetic method for preparing the compounds having the structure of the formula (M).
Owner:NANKAI UNIV +2
MST1 kinase inhibitor and application thereof
The present invention relates to a kinase inhibitor comprising a compound of formula (I) or a pharmaceutically acceptable salt, solvate, ester, acid, metabolite or prodrug thereof. The present invention also relates to pharmaceutical compositions comprising the kinase inhibitor, and uses and methods of using these compound and compositions to inhibit tyrosine kinase activity of one or more selected from MST1 or mutations thereof in a cell or subject, and to prevent or treat disorders associated with MST1 or mutated kinase thereof in a subject.
Owner:HEFEI INSTITUTES OF PHYSICAL SCIENCE - CHINESE ACAD OF SCI
Arylalkoxyl hepatitis C virus protease inhibitors
The present invention discloses compounds of Formula I or II, or pharmaceutically acceptable salts, esters, or prodrugs thereof:which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering to the subject a pharmaceutical composition comprising a compound of the present invention.
Owner:ENANTA PHARM INC
Cathepsin cysteine protease inhibitors
This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
Owner:AXYX PHARMA INC +1
Phosphoinositide 3-kinase (P13K) inhibitor, pharmaceutical composition containing P13K inhibitor, and application of phosphoinositide kinase inhibitor and pharmaceutical composition
ActiveCN103483345AImprove effectivenessGood choiceOrganic active ingredientsOrganic chemistryKinase inhibitionEnzyme inhibitor
The invention discloses a phosphoinositide 3-kinase (P13K) inhibitor, a pharmaceutical composition containing the P13K inhibitor, and application of the P13K inhibitor and the pharmaceutical composition. The P13K inhibitor comprises a pyrimidine compound and a stereoisomer/hydrate/pharmaceutically-acceptable salt thereof. The pyrimidine compound has a general formula I of which the structure is shown in the specification. The P13K inhibitor and the pharmaceutical composition containing the same can be used for inhibiting PI3 Ks and treating proliferative diseases on which the PI3 Ks act. According to the invention, high-effectiveness and high-selectivity inhibitors for treating proliferative diseases on which PI3Ks act can be provided.
Owner:SUN YAT SEN UNIV
Cyclopropylamine spiro(hetero)cyclic compound, and pharmaceutical composition and application thereof
The invention relates to a preparation method for a cyclopropylamine spiro(hetero)cyclic compound and a composition containing the same, and application of the compound and the composition as an inhibitor for human lysine-specific demethylase (LSD1). The inhibitor is the cyclopropylamine spiro(hetero)cyclic compound as shown in a formula (I) which is described in the specification, or a pharmaceutically acceptable salt, predrug, solvate, polymorphic crystal or stable isotope derivative thereof. The compound can be used for treating or preventing diseases related to human lysine-specific demethylase, e.g., cancers and nerve diseases.
Owner:SHANGHAI DE NOVO PHARMA
Methods for treating inflammatory conditions or inhibiting JNK
This invention is generally directed to methods for treating or preventing a disease or disorder comprising administering to a patient in need thereof an effective amount of a Jun N-terminal kinase (JNK) inhibitor, such as an isothiazoloanthrone, isoxazoloanthrone, isoindolanthrone, or derivative thereof having the general formula: and pharmaceutically acceptable salts thereof, wherein Ro is -CH2-, -SO-, -O-, -SO2-, or -S-.
Owner:SIGNAL PHARMA LLC
Medicaments and methods combining a HCV protease inhibitor and an AKR competitor
InactiveUS20060276404A1Improve efficacyExtended durationBiocideDipeptide ingredientsDiseaseEnzyme Inhibitor Agent
Disclosed are medicaments, pharmaceutical compositions, pharmaceutical kits, and methods based on combinations of a hepatitis C virus (HCV) protease inhibitor and an aldo-keto reductase (AKR) competitor, for concurrent or consecutive administration in treating, preventing, or ameliorating one or more symptoms of HCV, treating disorders associated with HCV, or inhibiting cathepsin activity in a subject.
Owner:SCHERING CORP
Pentacyclic kinase inhibitors
The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I
wherein A, X, Y, Z, Ra, Rb, Rc, R1, R2, R3 and m are defined herein.
Owner:GENENTECH INC +2
F1F0-ATPase inhibitors and related methods
The present invention relates to a family of guanidine-based F1F0-ATPase inhibitors, e.g., mitochondrial F1F0-ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders.
Owner:RGT UNIV OF MICHIGAN
HCV NS3 protease inhibitors
The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.
Owner:MERCK SHARP & DOHME LLC +1
Macrocyclic kinase inhibitors
ActiveUS20070265333A1Prevent proliferationBiocideOrganic active ingredientsKinase inhibitionEnzyme inhibitor
A compound having a structure according to formula I
wherein R1, R2, R3, R4, and R5 are as defined herein, are useful as kinase inhibitors.
Owner:KOSAN BIOSCI
Aryl kinase inhibitor
The invention belongs to the technical field of medicines, in particular to an aryl kinase inhibitor represented by the general formula (I), pharmaceutically acceptable salts or stereisomers thereof, wherein R1, R2, R3, m, n, R5, Y, W, M, L or Q are defined in the specification. The invention further relates to a preparation method of the compounds, pharmaceutical preparations or pharmaceutical compositions comprising the compounds, and an application of the compounds for preparing medicines for treating and/or preventing ALK or c-Met mediated cancer related diseases.
Owner:SHANDONG XUANZHU PHARMA TECH CO LTD
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