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142 results about "Transferase inhibitor" patented technology
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Synergistic modulation of flt3 kinase using a flt3 inhibitor and a farnesyl transferase inhibitor
The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from compounds of Formula I′:Included within the present invention is both prophylactic and therapeutic methods for treating a subject at risk of (or susceptible to) developing a cell proliferative disorder or a disorder related to FLT3.
Owner:JANSSEN PHARMA NV
Isopentenyl pyrophosphate isomerase (IPI) and/or prenyl transferase inhibitors
Methods of treatment and prophylaxis of various diseases and disorders, and in particular diseases and disorders of lipid and bone metabolism, involving the administration of prenyl transferase (farnesyl pyrophosphate synthase) and / or isopentenyl pyrophosphate isomerase inhibitor compounds are disclosed.
Owner:UNIV OF SHEFFIELD
Medicinal composition
PCT No. PCT / JP96 / 02241 Sec. 371 Date Feb. 9, 1998 Sec. 102(e) Date Feb. 9, 1998 PCT Filed Aug. 8, 1996 PCT Pub. No. WO97 / 05902 PCT Pub. Date Feb. 20, 1997The present invention relates to an antitumor or anti-AIDS composition containing a protein-farnesyltransferase inhibitor and an agent which decreases farnesyl pyrophosphate in vivo as active ingredients.
Owner:BANYU PHARMA CO LTD
Synthesis of a glycosyltransferase inhibitor
Process for the preparation of animinosugar, and the intermediates thereof, having known activity as a glycosyltransferase inhibitor and used, for example, in the treatment of Gaucher's disease.
Owner:DIPHARMA FRANCIS
Continuous administration of l-dopa, dopa decarboxylase inhibitors, catechol-o-methyl transferase inhibitors and compositions for same
ActiveUS20140249228A1Improve efficiencyReduce the daily dosage of levodopaBiocideNervous disorderTolcaponeCarbidopa
Provided herein, in part, is a method of treating a neurological or movement disorder in a patient in need thereof, comprising subcutaneously administering to said patient a pharmaceutically acceptable composition comprising levodopa and optionally carbidopa and optionally entacapone or tolcapone, or pharmaceutically acceptable salts thereof, wherein said composition is administered substantially continuously, and compositions that can be used in the disclosed methods.
Owner:NEURODERM
Novel compounds as diacylglycerol acyltransferase inhibitors
This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia-related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as myocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders.
Owner:GLAXO SMITHKLINE LLC
Angiotensin I transferase inhibitor and preparation method and application thereof
InactiveCN102093471ANo side effectsImprove securityPeptide/protein ingredientsPeptide preparation methodsTransferase inhibitorSide effect
The invention relates to an angiotensin I transferase inhibitor and a preparation method and application thereof. The preparation method comprises the following steps of: performing enzymolysis on oyster serosity serving as a raw material to generate oyster protein enzymolysis solution; and further separating and purifying the oyster protein enzymolysis solution to obtain new peptide with an amino acid sequence of Vel Tyr Pro Trp Thr Gln Arg Phe. A test proves that the new peptide is the effective angiotensin I transferase inhibitor, has the advantages of no toxic or side effect, high safety, low cost, capability of industrialized production and the like, and can be widely applied to the preparation of medicaments for reducing blood pressure and health-care products.
Owner:DALIAN FISHERIES UNIVERSITY
Benzyl-substituted aniline compound and application thereof
ActiveCN103787902ASignificant farnesyltransferase inhibitory activityGood drug prospectsCarboxylic acid nitrile preparationOrganic compound preparationDiseaseTransferase inhibitor
The invention provides a benzyl-substituted aniline compound represented by a formula I shown in a drawing or pharmaceutically acceptable salts thereof, wherein R1 is independently selected from -COOH, -CONH2, H, -COOR5 (R5 is methyl or ethyl), -CN, -OH and -NH2COCH3, R2 and R3 are independently selected from C6-C10 aryl, C3-C6 cyclane and C1-C3 saturated alkyl or unsaturated alkyl respectively, and R4 is independently selected from -H, ethyl and acetyl. The compound and the pharmaceutically acceptable salts thereof, provided by the invention, can be used as farnesyltransferase inhibitors or can be used for preparing drugs for preventing or treating diseases related to farnesyltransferase, thereby having good medicine preparation prospects.
Owner:EAST CHINA UNIV OF SCI & TECH
Therapeutic agents for renal diseases and method for screening the same
InactiveUS20040185503A1High expressionSuppress generationBiocideCompound screeningRenal Tubular Epithelial CellsFatty acid
Owner:MITSUBISHI TANABE PHARMA CORP
Methods for inducing orexin neurons and agent for treating narcolepsy or eating disorder
ActiveUS20140349964A1Improve securityBiocideMicrobiological testing/measurementPluripotential stem cellSirtuin 1
The invention provides a method for producing an orexin neuron by culturing a pluripotent stem cell or a neural progenitor cell in the presence of N-acetyl-D-mannosamine and optionally in the presence of at least one inhibitor selected from the group consisting of a Sirtuin 1 inhibitor and an O-linked β-N-acetylglucosamine transferase inhibitor. The invention also provides a therapeutic agent for narcolepsy or eating disorders, such as anorexia, containing N-acetyl-D-mannosamine, which is based on the induction of orexin neuron in vivo.
Owner:THE UNIV OF TOKYO
Therapeutic use of farnesyltransferase inhibitors and methods of monitoring the efficacy thereof
InactiveUS20110195419A1Organic active ingredientsMicrobiological testing/measurementTransferase inhibitorFarnesyltransferase inhibitor
The therapeutic use of farnesyltransferase inhibitors (e.g., tipifarnib) for the treatment of sepsis is described. Methods useful to monitor the effectiveness of such treatment are also described.
Owner:FOURIE ANNE MADELEINE
UCH-L1 expression and cancer therapy
InactiveUS20050272068A1Reduce anti-proliferative effect of UCH-LImprove the level ofMicrobiological testing/measurementMaterial analysisTransferase inhibitorCancer therapy
Methods are provided of treating cancer with one or more farnesyl transferase inhibitors. Methods are provided for identifying cancers that are particularly susceptible to treatment with one or more farneseyl transferase inhibitors by identifying cancers that express low levels of UCH-L1.
Owner:THE BRIGHAM & WOMEN S HOSPITAL INC
Sustained release of apo a-i mimetic peptides and methods of treatment
InactiveUS20090081298A1Improve concentrationPowder deliveryPeptide/protein ingredientsSterol transportReverse cholesterol transport
A method including advancing a delivery device through a lumen of a blood vessel to a particular region in the blood vessel; and introducing a composition including a sustained-release carrier and an apolipoprotein A-I (apo A-I) synthetic mimetic peptide into a wall of the blood vessel at the particular region or a perivascular site, wherein the peptide has a property that renders the peptide effective in reverse cholesterol transport. A composition including an apolipoprotein A-I (apo A-I) synthetic peptide, or combination of an apo A-I synthetic mimetic peptide and an Acyl CoA cholesterol: acyltransferase (ACAT) inhibitor in a form suitable for delivery into a blood vessel, the peptide including an amino acid sequence in an order reverse to an order of various apo A-I mimetic peptides, or endogenous apo A-I analogs, or a chimera of helix 1 and helix 9 of endogenous apo A-I.
Owner:ABBOTT CARDIOVASCULAR
O-glcnac transferase inhibitors and uses thereof
ActiveUS20120108605A1Inhibit O-GlcNAcylationBiocideSenses disorderAutoimmune conditionAutoimmune disease
The present invention provides inhibitors of O-GIcNAc transferase. Typically, the inhibitors are quinolinone-6-sulfonamides. The invention also provides pharmaceutical compositions thereof and methods for using the same in diabetes and complications thereof, neurodegenerative diseases, cancers, autoimmune diseases, and inflammatory diseases.
Owner:PRESIDENT & FELLOWS OF HARVARD COLLEGE
Method and composition for reducing appearance of wrinkles
ActiveUS20070292537A1Reduce appearance problemsRelaxing facial skeletal musclesCosmetic preparationsBiocideTransferase inhibitorWrinkle skin
The present invention provides a cosmetic composition having a cosmetically acceptable vehicle and one or more gap junction inhibitors and / or one or more choline acetyl transferase (CAT) inhibitors in an amount effective for reducing the appearance of deep wrinkles on the skin. Also provided is a method of reducing the appearance of deep wrinkles on the skin, including the steps of topically applying to the skin the above cosmetic composition in an amount and for a period of time sufficient to reduce the appearance of deep wrinkles on the skin.
Owner:AVON PROD INC
Compositions and methods for targeting glioblastomas cells
InactiveUS8853274B1Relieve symptomsBiocideDipeptide ingredientsTransferase inhibitorGlioblastoma cell
A composition including a farnesyl transferase inhibitor (FTI) and a gamma-secretase inhibitor (GSI) is useful for producing an effect against a glioblastoma cell and / or for treating glioblastoma multiforme (GBM).
Owner:VANDERBILT UNIV
Combination of epigenetic factors and bispecific compounds targeting CD33 and CD3 in the treatment of myeloid leukemia
InactiveCN111888474AOrganic active ingredientsHybrid immunoglobulinsGranulocyte colony-stimulating factorMyeloid leukemia
Owner:AMGEN INC +1
Application of dihydromyricetin to prepare medicines treating Parkinson's syndrome as active composition
InactiveCN104116730ALow toxicityNo toxicityOrganic active ingredientsNervous disorderBlood drug concentrationEstrogens catechol
The invention provides a dihydromyricetin-containing plant extract and application thereof as a superactive catechol methylation transferase inhibitor. The dihydromyricetin-containing plant extract is applicable as a synergist of a medicine levodopa treating Parkinson's syndrome. In-vitro activity determination shows that IC50 of the plant extract inhibiting catechol methylation transferase can reach the micro-mole to nano-mole grade. Rat integral pharmacokinetic research shows that combined usage of dihydromyricetin and levodopa containing the dihydromyricetin-containing plant extract can substantially improve the plasma concentration of levodopa. Additionally, dihydromyricetin and the dihydromyricetin-containing plant extract are high in safety, do not generate active intermediates through metabolism activation, do not combine with a biomacromolecule to form a toxic adduct, and therefore dihydromyricetin and the dihydromyricetin-containing plant extract do not cause liver and kidney toxicity, and are expected to have good application prospect in auxiliary treatment of Parkinson's syndrome.
Owner:DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
Sustained release of apo A-I mimetic peptides and methods of treatment
InactiveUS8044021B2Organic active ingredientsPowder deliveryReverse cholesterol transportCholesterol
A method including advancing a delivery device through a lumen of a blood vessel to a particular region in the blood vessel; and introducing a composition including a sustained-release carrier and an apolipoprotein A-I (apo A-I) synthetic mimetic peptide into a wall of the blood vessel at the particular region or a perivascular site, wherein the peptide has a property that renders the peptide effective in reverse cholesterol transport. A composition including an apolipoprotein A-I (apo A-I) synthetic peptide, or combination of an apo A-I synthetic mimetic peptide and an Acyl CoA cholesterol: acyltransferase (ACAT) inhibitor in a form suitable for delivery into a blood vessel, the peptide including an amino acid sequence in an order reverse to an order of various apo A-I mimetic peptides, or endogenous apo A-I analogs, or a chimera of helix 1 and helix 9 of endogenous apo A-I.
Owner:ABBOTT CARDIOVASCULAR
Iminosugar in crystalline form
Iminosugar, which possesses known activity as a glycosyltransferase inhibitor, and is used, for example, in the treatment of Gaucher's disease, in crystalline form, a process for its preparation and a pharmaceutical composition thereof.
Owner:DIPHARMA FRANCIS
WecA gene knock-out train, its preparing method, application and method for screening M.tuberculosis (MTB) N-acetylglucosamine-1-phosphate transferase inhibitor
InactiveCN101984047AHigh potencyOvercoming the killing of normal cellsBacteriaMicrobiological testing/measurementMycobacterium smegmatisTraditional Chinese medicine
N-acetylglucosamine-1-phosphate transferase is a key component for synthesis of cell wall of M.tuberculosis (MTB), and wec A gene is an encoding gene of the N-acetylglucosamine-1-phosphate transferase, the invention constructs a wec A gene knock-out strain MJ2008 (Mycobacterium smegmatis), CGMCC 3417 and takes the MJ2008 strain as a cell model for screening the N-acetylglucosamine-1-phosphate transferase in a high throughout so as to screen out the effective N-acetylglucosamine-1-phosphate transferase inhibitor from a combined compound library and the traditional Chinese medicine and prepare the anti-tuberculosis drug with a high efficiency; additionally, in human cells, there has no homologue of the MTB N-acetylglucosamine-1-phosphate transferase, accordingly, the developed anti-tuberculosis drug targeting the N-acetylglucosamine-1-phosphate transferase has no harm to the human body and overcomes the disadvantage of killing normal cells of antibacterial agents.
Owner:DALIAN MEDICAL UNIVERSITY
Treatment of mitochondrial disorders using a farnesyl transferase inhibitor
InactiveUS20100331363A1Avoid cell deathIncreased insulin secretionBiocideNervous disorderAntioxidantDepressant
Methods and pharmaceutical compositions comprising a low dose of a farnesyl transferase inhibitor useful in the treatment of proteinopathies are provided. These low doses are below the doses used in oncological treatments for which these compounds were initially designed. The treatment includes administering to a subject an amount of a farnesyl transferase inhibitor, wherein the amount administered is sufficient to cause an improvement in mitochondrial health in said subject. Treatments in accordance with the present invention may also include an acetylcholinesterase inhibitor, an activator of neurotrophic receptors, an NMDA anatagonist, an amyloid deposit inhibitor, an antipsychotic agent, an antidepressant, an anxiolytic, or an antioxidant.
Owner:ASTRAZENECA AB
Application of vanillin in preparation of nicotinamide-N-methyltransferase inhibitor
PendingCN112494467AInhibit expressionInhibitory activityKetone active ingredientsAntineoplastic agentsApoptosisPharmaceutical medicine
The invention discloses an application of vanillin in preparation of a nicotinamide-N-methyltransferase inhibitor. The inhibitor is prepared from traditional Chinese medicine monomer vanillin and pharmaceutically acceptable auxiliary materials. According to the invention, proliferation of various colorectal cancer cell strains is inhibited by inhibiting the expression of NNMT and enzyme activity in vitro and vivo, and an anti-tumor effect is achieved. Studies show that vanillin can weaken the drug resistance of colorectal cancer cell strains to 5-FU caused by high expression of NNMT in vitro,so that the chemotherapy sensitivity is enhanced; the apoptosis of the colorectal cancer cell strains with high expression of NNMT is increased by inducing ROS production and mitochondrial damage in cells; and the inhibitory effect of 5-fluorouracil on tumor proliferation and the apoptosis rate can be improved, so as to enhance the chemotherapy effect. The vanillin can be used as an NNMT inhibitorfor preparing anti-colorectal cancer drugs or adjuvant chemotherapy drugs, and has a good application prospect.
Owner:ZHEJIANG UNIV
N-Myristoyl Transferase Inhibitors
ActiveUS20110312921A1Rapid onset of activityLow toxicityBiocideNervous disorderTransferase inhibitorN-myristoyltransferase
The present invention relates to N-heterocyclic sulphonamide compounds, in particular pyrazole sulphonamide compounds, and their use as N-myristoyl transferase inhibitors.
Owner:DUNDEE UNIV OF
Novel nicotinamide ribose phosphate transferase inhibitor as well as synthetic method and application thereof
InactiveCN104557863ASynthetic raw materials are cheapEasy to routeOrganic active ingredientsOrganic chemistryTransferase inhibitorStructural formula
The invention discloses a novel nicotinamide ribose phosphate transferase inhibitor as well as a synthetic method and application thereof. The novel nicotinamide ribose phosphate transferase inhibitor is a compound or pharmaceutically acceptable salts thereof shown in the structural formula I in the specification. The novel nicotinamide ribose phosphate transferase inhibitor is prepared from cheap synthetic raw materials, concise in route, simple in operation and suitable for industrial production; the obtained compound is excellent in antitumor activity and is expected to be developed as a new antitumor drug.
Owner:GUANGZHOU INST OF BIOMEDICINE & HEALTH CHINESE ACAD OF SCI +1
Bionic nano-drug co-loaded with JTC801 and DNA methylated transferase inhibitor and preparation method and application thereof
PendingCN113304123APromote enrichmentRapid enrichmentOrganic active ingredientsNervous disorderEnzyme inhibitorTransferase
The invention provides a bionic nano-drug co-loaded with JTC801 and a DNA methylated transferase inhibitor. The bionic nano-drug comprises an M1 type macrophage membrane, a nanoparticle core, the JTC801 and the DNA methylated transferase inhibitor, the JTC801 and the DNA methylated transferase inhibitor are simultaneously loaded in the nanoparticle core, and then the surface of the nanoparticle core is coated with the M1 type macrophage membrane; the enrichment of the M1 type macrophage bionic system at the tumor site is further promoted, the targeted amplification effect is achieved, on one hand, the nanoparticles are disguised as endogenous substances through the bionic effect of the M1 type macrophage cell membrane so that the nanoparticles are protected from being swallowed by the reticuloendothelial system; on the other hand, the macrophages can be rapidly enriched to tumor tissues due to recruitment effect, accumulation of drugs at tumor parts is increased, synchronous treatment of cancers and cancer-related pains is realized, and the drug is an innovation of synchronous treatment drugs for cancers and cancer-related pains, and has huge social and economic benefits.
Owner:ZHENGZHOU UNIV
Methods of treating or preventing an inflammatory disease or condition using glutaminyl cyclase inhibitors
Methods for the treatment and / or prevention of an inflammatory disease or disorder through administration of an inhibitor of a glutaminyl peptide cyclotransferase. Inflammatory diseases or disorders treated or prevented by methods disclosed herein include mild cognitive impairment (MCI), rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis, sepsis and peritonitus. Further provided are respective diagnostic methods, assays and kits.
Owner:VIVORYON THERAPEUTICS NV
Iminosugar in crystalline form
Iminosugar, which possesses known activity as a glycosyltransferase inhibitor, and is used, for example, in the treatment of Gaucher's disease, in crystalline form, a process for its preparation and a pharmaceutical composition thereof.
Owner:DIPHARMA FRANCIS
Method of treating inflammation with glutaminyl cyclase inhibitors
ActiveUS8338120B2Organic active ingredientsBiocideTransferase inhibitorMild cognitive impairment (MCI)
Provided herein are methods for the treatment and / or prevention of an inflammatory disease or disorder through administration of an inhibitor of a glutaminyl peptide cyclotransferase. Inflammatory diseases or disorders treated or prevented by methods disclosed herein include mild cognitive impairment (MCI), rheumatoid arthritis, atherosclerosis, restenosis and pancreatitis.
Owner:VIVORYON THERAPEUTICS NV
Application of acyl-coenzyme A: cholesterol acyltransferase-2 (ACAT2) inhibitor in liver cancer growth inhibition
ActiveCN103536922AOrganic active ingredientsMicrobiological testing/measurementMetaboliteIntracellular cholesterol
The invention relates to application of an acyl-coenzyme A: cholesterol acyltransferase-2 (ACAT2) inhibitor in liver cancer growth inhibition. Concretely, the inhibition of the activity of the ACAT2 can effectively inhibit the growth of human liver cancer cells and transplanted tumors respectively in cellular and animal levels, and the inhibitory effect is generated through accumulating intracellular cholesterol metabolites by blocking the secretion and excretion of ACAT2-mediated cholesterol metabolites. The accumulation of the cholesterol metabolites has effects on promoting the apoptosis of liver cancer cells and inhibiting the growth of liver cancer; the excretion of the cholesterol metabolites can remove the inhibitory effect.
Owner:CENT FOR EXCELLENCE IN MOLECULAR CELL SCI CHINESE ACAD OF SCI
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