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3837 results about "Enzyme inhibitor" patented technology

An enzyme inhibitor is a molecule that binds to an enzyme and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. They are also used in pesticides. Not all molecules that bind to enzymes are inhibitors; enzyme activators bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.

Bacterial glutamine synthetases and methods of use

Compositions and methods for conferring herbicide resistance to and improving nitrogen utilization of bacteria, plants, plant cells, tissues and seeds are provided. Compositions comprising a coding sequence for a polypeptide that confers resistance or tolerance to herbicidal glutamine synthetase inhibitors are provided. The coding sequences can be used in DNA constructs or expression cassettes for transformation and expression in plants. Compositions also comprise transformed bacteria, plants, plant cells, tissues, and seeds. In particular, isolated polynucleotides corresponding to herbicidal glutamine synthetase inhibitor-resistant polynucleotides are provided. Additionally, polypeptides corresponding to the polynucleotides are encompassed. In particular, the present invention provides for isolated polynucleotides comprising a variant of SEQ ID NO:1, wherein the variant polynucleotide encodes a polypeptide that is resistant to inhibition by herbicidal glutamine synthetase inhibitor.
Owner:BASF AGRICULTURAL SOLUTIONS SEED LLC

Indole and azaindole inhibitors of fructose-1,6-bisphosphatase

InactiveUS6054587AReduce riskFasting hyperglycemiaPhosphorus organic compoundsFructoseNitrogen
Novel indole and azaindole compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is described: and pharmaceutically acceptable prodrugs and salts thereof.
Owner:METABASIS THERAPEUTICS INC

Benzimidazole inhibitors of fructose 1,6-bisphosphatase

Novel benzimidazole compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is described
Owner:METABASIS THERAPEUTICS INC

Specific kinase inhibitors

Resorcylic acid lactones having a C5-C6 cis double bond and a ketone at C7 and other compounds capable of Michael adduct formation are potent and stable inhibitors of a subset of protein kinases having a specific cysteine residue in the ATP binding site.
Owner:KOSAN BIOSCI

Purine inhibitors of fructose 1,6-bisphosphatase

InactiveUS6284748B1Reduce riskFasting hyperglycemiaBiocideOrganic active ingredientsFructosePurine
Novel purine compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is described.whereinA is selected from the group consisting of -NR82, -NHSO2R3, -OR5, -SR5, halo, lower alkyl, -CON(R4)2, guanidino, amidino, -H, and perhaloalkyl;E is selected from the group consisting of -H, halo, lower alkylthio, lower perhaloalkyl, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, -CN, and -NR72;X is selected from the group consisting of -alk-NR-, alkylene, alkenylene, alkynylene, arylene, heteroarylene, -alk-NR-alk-, -alk-O-alk-, -alk-S-alk-, -alk-S-, alicyclicene, heteroalicyclicene, 1,1-dihaloalkylene, -C(O)-alk-, -NR-C(O)-NR'-, -alk-NR-C(O)-, -alk-C(O)-NR-, -Ar-alk-, and -alk-Ar-, all optionally substituted, wherein each R and R' is independently selected from -H and lower alkyl, and wherein each "alk" and "Ar" is an independently selected alkylene or arylene, respectively;Y is selected from the group consisting of -H, alkyl, alkenyl, alkynyl, aryl, alicyclic, heteroalicyclic, aralkyl, aryloxyalkyl, alkoxyalkyl, -C(O)R3, -S(O)2R3, -C(O)-OR3, -CONHR3, -NR22, and -OR3, all except H are optionally substituted; andpharmaceutically acceptable prodrugs and salts thereof.
Owner:METABASIS THERAPEUTICS INC

Method of prevention and treatment of aging, age-related disorders and/or age-related manifestations including atherosclerosis, peripheral vascular disease, coronary artery disease, osteoporosis, arthritis, type 2 diabetes, dementia, alzheimers disease and cancer

InactiveUS20060275294A1Halogenated hydrocarbon active ingredientsBiocideAbnormal tissue growthSTAT Transcription Factors
This invention relates to a method for prevention and treatment of aging, age-related disorders and / or age-related manifestations 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, age-related disorders and / or age-related manifestations 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

Stent coatings containing HMG-CoA reductase inhibitors

InactiveUS20030077310A1Hydrolysis can be preventedAvoid accessStentsSurgeryHMG-CoA reductaseDepressant
Stents with coatings comprising a combination of a restenosis inhibitor comprising an HMG-CoA reductase inhibitor and a carrier. Also provided are methods of coating stents with a combination of an HMG-CoA reductase inhibitor and a carrier. A preferred example of a restenosis inhibitor is cerivastatin. The stent coatings have been shown to release restenosis inhibitors in their active forms.
Owner:ZIMMER ORTHOBIOLIGICS

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

InactiveUS20060078533A1BiocidePeptide/protein ingredientsInterleukin 6STAT Transcription Factors
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

Bone graft

An improved demineralized bone matrix (DBM) or other matrix composition is provided that has been mixed with a stabilizing agent that acts as (1) a diffusion barrier, (2) a enzyme inhibitor, (3) a competitive substrate, or (4) a masking moiety. A diffusion barrier acts as a barrier so as to protect the osteoinductive factors found in DBM from being degraded by proteolytic and glycolytic enzymes at the implantation site. Stabilizing agents may be any biodegradable material such as starches, modified starches, cellulose, dextran, polymers, proteins, and collagen. As the stabilizing agents degrades or dissolves in vivo, the osteoinductive factors such as TGF-β, BMP, and IGF are activated or exposed, and the activated factors work to recruit cells from the preivascular space to the site of injury and to cause differentiation into bone-forming cells. The invention also provides methods of preparing, testing, and using the inventive improved osteodinductive matrix compositions.
Owner:WARSAW ORTHOPEDIC INC

Combinations for HCV treatment

InactiveUS20060003942A1Improve pharmacokineticsImproving the pharmacokinetics of Hepatitis C NS3/4ABiocideOrganic active ingredientsHcv treatmentMonooxygenase
The present invention relates to co-administering a Hepatitis C virus NS3 / 4A protease inhibitor and a cytochrome P450 monooxygenase inhibitor. The combination acts by interfering with the life cycle of the hepatitis C virus and is therefore useful as an antiviral therapy. As such, the combination may be used for treating or preventing Hepatitis C infections in patients. The invention also relates to compositions comprising the combination of inhibitors. The invention also relates to kits and pharmaceutical packs comprising a Hepatitis C virus NS3 / 4A protease inhibitor and a cytochrome P450 monooxygenase inhibitor. The invention also relates to processes for preparing these compositions, combinations, kits, and packs.
Owner:VERTEX PHARMA INC

Biological markers predictive of anti-cancer response to epidermal growth factor receptor kinase inhibitors

The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with an EGFR kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an EGFR kinase inhibitor, comprising assessing whether the tumor cell has undergone an epithelial to mesenchymal transition (EMT), by determining the expression level of epithelial and / or mesenchymal biomarkers, wherein tumor cells that have undergone an EMT are substantially less sensitive to inhibition by EGFR kinase inhibitors. Improved methods for treating cancer patients with EGFR kinase inhibitors that incorporate the above methodology are also provided. Additionally, methods are provided for the identification of new biomarkers that are predictive of responsiveness of tumors to EGFR kinase inhibitors. Furthermore, methods for the identification of agents that restore the sensitivity of tumor cells that have undergone EMT to inhibition by EGFR kinase inhibitors are also provided.
Owner:OSI PHARMA LLC

Baby Care Skin Protectant Compositions for Diaper Rash

The present invention provides a comprehensive solution to skin problems of infants and incontinent adults related to diaper rash, also known as diaper dermatitis. This is based on certain novel divalent metal and quaternary ammonium complexes (ion-pairs) of zeolites (that are made by an in-situ process), which in synergistic combination with certain other compositions, provide a comprehensive treatment for diaper rash that encompasses the following aspects: (1) deactivation of lipase and protease enzymes on skin surface, (2) the controlled-release delivery of skin protectant compositions, such as divalent metal zinc cation, (3) trapping of acidic and alkaline chemicals deposited on skin from body exudates and enzyme activity, (4) controlled-release delivery of anti-inflammatory agents, and COX and LOX enzyme inhibitors, (5) controlled-release delivery of antibacterial and antifungal compositions, and (6) absorption of excess moisture in the diaper zone.
Owner:BIODERM RES

Combinations comprising HCV protease inhibitor(s) and HCV polymerase inhibitor(s), and methods of treatment related thereto

Disclosed are medicaments, pharmaceutical compositions, pharmaceutical kits, and methods based on combinations of at least one HCV protease inhibitor and at least one HCV polymerase inhibitor but not HCV-796; for concurrent or consecutive administration in treating or ameliorating one or more symptoms of HCV, or disorders associated with HCV in a subject in need thereof.
Owner:SCHERING CORP

Nutritional intervention composition containing a source of proteinase inhibitor extending post meal satiety

The invention relates to a nutritional intervention composition in powder form that is taken before a meal and that extends post meal satiety. The compositions of the invention are comprised of at least one protein, C12-18 fatty acids, preferably oleic acid, all of which stimulate CCK release in the body, and a source of proteinase inhibitor which acts to prevent the deactivation of CCK. The subject compositions preferably additionally contain a source of calcium and are advantageous in that they utilize a source of proteinase inhibitor as opposed to the more costly extracts. The source of proteinase inhibitor is advantageously an extract of potato, soy, or beans containing about 10 weight percent of proteinase inhibitor. The powder compositions are mixed with a suitable liquid, preferably water, prior to ingestion.
Owner:ANAYA PERSONAL CARE PROD LLC +1

Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme

The present invention relates to compounds that are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.
Owner:ABBVIE INC

Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme

The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.
Owner:ABBVIE INC

Topical Antiviral Formulations

The present invention relates to formulations of nucleotide reverse transcriptase inhibitors (N(t)RTIs), preferably [2-(6-Amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid (tenofovir, PMPA), or a physiologically functional derivative thereof, suitable for topical application and their use in the prevention of HIV infections.
Owner:EASTERN VIRGINIA MEDICAL SCHOOL +1

Dimeric IAP inhibitors

ActiveUS20060194741A1Increased cell deathIncreased apoptotic activityBiocideOrganic active ingredientsSmac mimeticsApoptosis
Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac / DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of LAP. Also disclosed are methods of using these peptidomimetics for therapeutic purposes. In various embodiments of the invention the Smac mimetics of the invention are combined with chemotherapeutic agents, including, but not limited to topoisomerase inhibitors, kinase inbhibitors, NSAIDs, taxanes and platinum containing compounds use broader language
Owner:MEDIVIR AB

Fused heterobicyclic kinase inhibitors

InactiveUS20070208053A1Low toxicityDisrupting virus life-cycleAntibacterial agentsBiocideNervous systemAllergy
Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X5, X7, R1, and Q1 are defined herein, inhibit kinase enzymes and are useful for the treatment and / or prevention of hyperproliferative diseases such as cancer. The compounds are also useful in the treatment of inflammation, allergy, asthma, disease and conditions of the immune system, disease and conditions of the nervous system, cardiovascular diseases, disease and conditions of the eye, dermatological diseases, osteoporosis, diabetes, multiple sclerosis, and infections.
Owner:OSI PHARMA INC

Phosphatidylinositol 3 kinase inhibitors

Provided are compounds according to Formula (I):or stereoisomer, prodrug, polymorph, or pharmaceutically acceptable salt forms thereof, wherein X, Y, R1, R6, R7, and R8 are as defined, and which compounds are effective inhibitors of PI3-kinase and / or other medically and clinically relevant kinases. Also provided are pharmaceutical compositions and methods of using the compounds and compositions as PI3-kinase and kinase inhibitors. More particularly, the compounds of the invention provide treatments and therapeutics for human diseases regulated by, or associated with, the activity of, PI3-kinases and / or protein kinases, or mutant or variant forms thereof.
Owner:PROGENICS PHARMA INC

Biological markers predictive of anti-cancer response to epidermal growth factor receptor kinase inhibitors

The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with an EGFR kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an EGFR kinase inhibitor, comprising assessing whether the tumor cell has undergone an epithelial to mesenchymal transition (EMT), by determining the expression level of epithelial and / or mesenchymal biomarkers, wherein tumor cells that have undergone an EMT are substantially less sensitive to inhibition by EGFR kinase inhibitors. Improved methods for treating cancer patients with EGFR kinase inhibitors that incorporate the above methodology are also provided. Additionally, methods are provided for the identification of new biomarkers that are predictive of responsiveness of tumors to EGFR kinase inhibitors. Furthermore, methods for the identification of agents that restore the sensitivity of tumor cells that have undergone EMT to inhibition by EGFR kinase inhibitors are also provided.
Owner:OSI PHARMA INC
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