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139 results about "Peptidase Inhibitors" patented technology
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Methods and compounds for producing dipeptidyl peptidase IV inhibitors and intermediates thereof
InactiveUS20050090539A1BiocideOrganic chemistryDipeptidyl peptidaseDipeptidyl-Peptidase IV Inhibitors
Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.
Owner:ASTRAZENECA AB
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
Pharmaceutical combination comprising an ibat inhibitor and a bile acid binder
InactiveUS20150031637A1Reduce generationEliminate the effects ofOrganic active ingredientsDipeptide ingredientsDipeptidyl peptidaseEnzyme inhibitor
Owner:ALBIREO
Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
Owner:MERCK SHARP & DOHME LLC
Pharmaceutical combination comprising an ibat inhibitor and a bile acid binder
InactiveUS20170182115A1Reduce generationEliminate the effects ofOrganic active ingredientsDipeptide ingredientsDipeptidyl peptidasePancreatic hormone
The present invention relates to a combination comprising a substance with inhibiting effect on the ileal bile acid transport system (I BAT) and at least one other active substance selected from an IBAT inhibitor; an enteroendocrine peptide or enhancer thereof; a dipeptidyl peptidase-IV inhibitor; a biguanidine; an incretin mimetic; a thiazolidinone; a PPAR agonist; a HMG Co-A reductase inhibitor; a bile acid binder; and a TGR5 receptor modulator; wherein the IBAT inhibitor compound and the at least one other active substance are adminstered simultaneously, sequentially or separately.
Owner:ALBIREO
Treatment of male sexual dysfunction
InactiveUS20020028799A1Increase heightSpeed up the processBiocideOrganic chemistryPhosphodiesterasePeptidase Inhibitors
The present invention relates to the use of neutral endopeptidase inhibitors (NEPi) and a combination of NEPi and phosphodiesterase type 5 (PDE5) inhibitor for the treatment of male sexual dysfunction, in particular MED.
Owner:PFIZER INC
Methods for identifying inhibitors of methionine aminopeptidases
InactiveUS6261794B1Microbiological testing/measurementPeptidesMethionine aminopeptidaseMethionine biosynthesis
Methods are provided for detecting methionine aminopeptidase (MAP) activity and for detecting inhibitors of MAP. The methods utilize a peptide comprising an N-terminal methionine which can be cleaved from the peptide by MAP, and a C-terminal detection moiety which is released by a second peptidase only if the N-terminal methionine has been cleaved from the peptide. When the peptide is combined with MAP and the second peptidase, the detection moiety is released, while the addition of a MAP inhibitor will inhibit the release of the detection moiety. Reaction mixes, peptides, and kits which are useful for practicing the methods are also provided.
Owner:SAINT LOUIS UNIVERSITY
Novel crystalline form of angiotensin receptor antagonist and neutral endopeptidase inhibitor supramolecular complex
ActiveCN105037289AGood water solubilityImprove stabilityOrganic chemistry methodsCarboxylic acid amide separation/purificationSolubilityWater soluble
The present invention discloses a novel crystalline form of an angiotensin receptor antagonist and neutral endopeptidase inhibitor supramolecular complex. The novel crystalline form of the supramolecular complex has high water solubility and good stability. Experiments show that the moisture absorption and intrinsic dissolution extent and speed are superior to those of a conventional crystalline supramolecular complex.
Owner:EAST CHINA UNIV OF SCI & TECH
Lipoglycopeptide antibiotics
Provided are novel lipoglycopeptides exhibiting bacterial signal peptidase inhibitory activity. Also provided are actinomycete strains that produce these lipoglycopeptides, methods of producing such lipoglycopeptides by culturing these strains, pharmaceutical compositions comprising these lipoglycopeptides, and methods of treating bacterial infections comprising contacting bacteria susceptible to treatment with the present bacterial signal peptidase inhibitor lipoglycopeptides. These lipoglycopeptides are useful in human and veterinary medicine.
Owner:ELI LILLY & CO
Amino hexatomic ring derivative and application thereof to medicine
The invention relates to an amino hexatomic ring derivative and application thereof to medicine, in particular to the amino hexatomic ring derivative shown in the general formula (I) (in the description), a stereoisomer thereof, a pharmaceutically acceptable salt thereof or a prodrug thereof, a drug composition comprising the derivative, and medical application to preparation of a dipeptidyl peptidase IV (DPP-IV) inhibitor. In the general formula (I), the definitions of the substituent groups are the same as those in the description.
Owner:SICHUAN HAISCO PHARMA CO LTD
Process for preparing a dipeptidyl peptidase IV inhibitor and intermediates employed therein
A process is provided for preparing a dipeptidyl peptidase IV inhibitor of the structurewhereinis treated with TFAA in isopropyl acetate to protect the tertiary hydroxyl group as a trifluoroacetate group to form 4(which is a novel intermediate)which is converted to acid chloride compound 5(which is a novel compound)using Vilsmeier reagent or other chloro reagent and coupled with compound 6 in a heterogeneous mixture of ethyl acetate and aqueous bicarbonate to give compound 7The N,O-bis(trifluoroacetyl) groups of compound 7 are deprotected to give free base compound 10.
Owner:ASTRAZENECA AB
Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
Owner:MERCK SHARP & DOHME CORP
Process for producing a dipeptidyl peptidase IV inhibitor
Owner:BRISTOL MYERS SQUIBB CO
Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
Owner:MERCK SHARP & DOHME LLC
Pyrrolidines 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
Amino six-membered ring derivative and application thereof in medicines
The invention relates to an amino six-membered ring derivative and an application thereof in medicines, and in particular, the invention relates to an amino six-membered ring derivative represented as the general formula (I), or a stereisomer thereof, a pharmaceutically-acceptable salt thereof, a pre-drug thereof, a drug composition comprising the derivative, and the application in a medicine of preparing a dipeptidyl peptidase IV (DPP-IV) inhibitor, wherein the substituent groups in the general formula (I) are defined as same as that in the specification.
Owner:SICHUAN HAISCO PHARMA CO LTD
Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
Owner:MERCK SHARP & DOHME CORP
Process for preparing dipeptidyl peptidase IV inhibitors and intermediates therefor
InactiveUS20050260712A1Procedure of process can be improvedReduce processing timeSugar derivativesBacteriaPhenylalanine dehydrogenaseDipeptidyl peptidase
A process for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV is provided which employs a BOC-protected amine of the structure prepared by subjecting an acid of the structure to reduce amination by treating the acid with ammonium formate, nicotinamide adenine dinucleotide, dithiothreitol and partially purified phenylalanine dehydrogenase / formate dehydrogenase enzyme concentrate (PDH / FDH) and without isolating treating the resulting amine of the structure 2 with di-tert-butyl dicarbonate to form the BOC-protected amine.
Owner:ASTRAZENECA AB
Novel alanyl-amino peptidase inhibitors for functionally influencing different cells and treating immunological, inflammatory, neuronal, and other diseases
The invention relates to medicinally used substances which specifically inhibit peptidases splitting ala-p-nitroanilide. The invention further relates to the use of at least one such substance or at least one pharmaceutical or cosmetic composition containing such a substance for preventing and treating diseases, especially diseases with an overshooting immune response (autoimmune diseases, allergies, and transplant rejections), other chronic inflammatory diseases, neuronal diseases, brain damages, skin diseases (acne and psoriasis, among others), tumor diseases, and special viral infections (including SARS).
Owner:INSTITUT FUR MEDIZINTECH MAGDEBURG IMTM +1
Enzyme stabilization
InactiveUS20080004200A1Organic detergent compounding agentsNon-surface-active detergent compositionsMicroorganismFlora
Liquid detergent compositions comprising a tripeptide enzyme inhibitors are provided. Methods of using the tripeptide enzyme inhibitor to stabilize liquid detergent compositions are also provided. Also provided are liquid detergent compositions wherein the tripeptide enzyme inhibitor at least inhibits the growth of at least one microbiological flora or fauna in the liquid detergent composition.
Owner:THE PROCTER & GAMBLE COMPANY
Methods of using small molecule compounds for neuroprotection
InactiveCN101365451AAvoid lostHeterocyclic compound active ingredientsTreatment choicesTranspeptidase Inhibitors
Methods are provided for preventing neurodegeneration and neuronal loss by administering compositions comprising small molecule compounds with the effect of preventing neurodegeneration and neuronal loss. In one aspect of the invention, the methods and compositions are also useful for treating neurodegenerative diseases. Small molecule compounds provide an important treatment option because of their stability, ease of use in both manufacture and formulation, ease of administration, and patient compliance. The small molecule compound compositions of the present invention may include topoisomerase II inhibitors, bacterial transpeptidase inhibitors, calcium channel antagonists, cyclooxygenase inhibitors, folic acid synthesis inhibitors, or sodium channel blockers and functional analogues thereof that have an effect on neurodegeneration. The compositions of the present invention may be administered prophylactically before the onset of clinical symptoms or after clinical symptoms of a neurodegenerative disease have manifested.
Owner:阿拉巴马大学董事会
Treating method for suppressing hair growth
InactiveUS7211278B2Excellent hair growth inhibitory effectStrong growth inhibitory effectCosmetic preparationsBiocideMalt GrainChymotrypsin
treating method for hair growth inhibition, which comprises administering (A) the extract of a plant of the family Juniperus or a malt. In addition, the present invention relates to a dermatologic composition for external use, which comprises (B) an elastase inhibitor or neutral endopeptidase inhibitor, and the above-described component (A) and / or (C) at least one proteolytic enzyme selected from the group consisting of papain, trypsin, chymotrypsin, pepsin, bromelain, ficin and pancreatin.
Owner:KAO CORP
Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
Owner:MERCK SHARP & DOHME CORP
Cell-based assay for identifying peptidase inhibitors
The present invention provides assays for the identification of inhibitors of endopeptidase toxins. The assays utilize genetically engineered yeast cells that contain a conditionally expressed endopeptidase toxin. When conditions for expression of the toxin are met, the toxin cleaves a yeast (natural or engineered) peptide product that is required for yeast survival. If the yeast is grown in the presence of an candidate substance that is an inhibitor of the toxin, the yeast survives, thereby providing a rapid and sensitive identification of the inhibitor.
Owner:VANDERBILT UNIV
Peptidyl nitril compounds as dipeptidyl peptidase i inhibitors
ActiveUS20180044328A1Overcome obstaclesImproved pharmacokinetic propertiesAntibacterial agentsNervous disorderDipeptidyl peptidasePeptidase Inhibitors
Owner:NEUPROZYME THERAPEUTICS APS
Process for preparing a dipeptidyl peptidase IV inhibitor and intermediates employed therein
A process is provided for preparing a dipeptidyl peptidase IV inhibitor of the structure wherein is treated with TFAA in isopropyl acetate to protect the tertiary hydroxyl group as a trifluoroacetate group to form 4 (which is a novel intermediate) which is converted to acid chloride compound 5 (which is a novel compound) using Vilsmeier reagent or other chloro reagent and coupled with compound 6 in a heterogeneous mixture of ethyl acetate and aqueous bicarbonate to give compound 7 The N,O-bis(trifluoroacetyl) groups of compound 7 are deprotected to give free base compound 10.
Owner:ASTRAZENECA AB
Pharmaceutical compositions comprising NEP-inhibitors, inhibitors of the endogenous endothelin producing system and AT1 receptor antagonists
InactiveUS20050288272A1Good curative effectImprove securityBiocideAnimal repellantsDepressantEssential hypertension
A combination therapy for cardiovascular diseases, in particular essential hypertension, pulmonary hypertension and / or congestive heart failure, involving administering a synergistic combination of at least one inhibitor of neutral endopeptidase, at least one inhibitor of the endogenous endothelin producing system, and at least one AT1 receptor antagonist.
Owner:SOLVAY PHARMA GMBH
Aminopeptidase N inhibitor, preparation method and application
The invention belongs to the technical field of drugs, and particularly relates to aminopeptidase N inhibitor, a preparation method and application to tumor resistance. The technical scheme includes that the aminopeptidase N inhibitor is chemically named as (S)-4-methyl-2-(3-naphthyl-1-ylmethyl-ureido)-valeryl group hydroxylamine. The constitutional formula (I) of the aminopeptidase N inhibitor is shown here. The pharmacodynamic effect of the aminopeptidase N inhibitor is evaluated by in-vitro APN (adiponectin) inhibitory experiments, in-vitro resistance to tumor cell invasion, antiangiogenesis and mouse in-vivo resistance to melanoma manual transfer and antiangiogenesis experiments.
Owner:WEIFANG BOCHUANG INT ACAD OF BIOTECH & MEDICINE
Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved
Owner:MERCK SHARP & DOHME CORP
Phenylalanine derivatives as depeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
Owner:MERCK SHARP & DOHME LLC
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