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163 results about "Protein Tyrosine Phosphatase 1B" patented technology
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Azole compound and medicinal use thereof
The present invention relates to an azole compound represented by the formula [I]wherein W is S or O; R is —COOR7, —X1-A1-COOR7 (R7 is H, alkyl) or tetrazolyl; R1, R2, R3 and R4 are H and the like; A is —(CH2)m—X— (X is —N(R8)—, —C(R9)(R10)—, —CO— or —CO—N(R8)—); B is aryl or aromatic heterocyclic group; R5 is H and the like; R6 is —(Y)s1-(A2)s-Z (Y is —O—, —S(O)t—, —N(R13)—, —N(R14)—CO—, —N(R14)—SO2—, —SO2—N(R14)— and the like, A2 is alkylene, and Z is cycloalkyl, aryl, aromatic heterocyclic group, indanyl, piperazinyl, a prodrug thereof or a pharmaceutically acceptable salt thereof. The compound [I] of the present invention has a protein tyrosine phosphatase 1B inhibitory activity, and is useful as a therapeutic agent for diabetes, a therapeutic drug for diabetic complications or a therapeutic drug for hyperlipidemia.
Owner:JAPAN TOBACCO INC
Azole compound and medicinal use thereof
The present invention relates to an azole compound represented by the formula [I]wherein W is S or O; R is —COOR7, —X1-A1-COOR7 (R7 is H, alkyl) or tetrazolyl; R1, R2, R3 and R4 are H and the like; A is —(CH2)m—X— (X is —N(R8)—, —C(R9)(R10)—, —CO— or —CO—N(R8)—); B is aryl or aromatic heterocyclic group; R5 is H and the like; R6 is —(Y)s1-(A2)s-Z (Y is —O—, —S(O)t—, —N(R13)—, —N(R14)—CO—, —N(R14)—SO2—, —SO2—N(R14)— and the like, A2 is alkylene, and Z is cycloalkyl, aryl, aromatic heterocyclic group, indanyl, piperazinyl, a prodrug thereof or a pharmaceutically acceptable salt thereof. The compound [I] of the present invention has a protein tyrosine phosphatase 1B inhibitory activity, and is useful as a therapeutic agent for diabetes, a therapeutic drug for diabetic complications or a therapeutic drug for hyperlipidemia.
Owner:JAPAN TOBACCO INC
Protein-tyrosine phosphatase inhibitors and uses thereof
The present invention is directed to compounds of formula (I),or a pharmaceutically suitable salt or prodrug thereof, which are useful for the selective inhibition of protein tyrosine phosphatase-1B (PTP1B), and are useful for the treatment of disorders caused by overexpressed or altered protein tyrosine phosphatase 1B.
Owner:ABBVIE INC
Application of magnolia bark preparation in preparing medicine for treating diabetes and obesity
InactiveCN101015597AInhibitory activityGood hypoglycemic effectMetabolism disorderSolution deliveryDiseaseDiabetes model
The application of Magnolia officinalis preparation for the production of medicaments for treating diabetes and obesity belongs to the field of medicinal application. The Magnolia officinalis preparation is extracted from Magnolia officinalis by soaking in ethanol with magnolol and honokiol as main ingredients. The preparation has effects of in-vitro inhibiting the activity of protein-tyrosine phosphatase 1B (PTP1B) and reducing blood sugar level in rat model of type 2 diabetes. The preparation can be made into powder, pill, capsule, tablet, oral liquid and injection. It can be used for treating diabetes, obesity, and diseases related to PTP1B.
Owner:JILIN UNIV
Oleanane-type triadic compound and its preparation method and medical application
The invention discloses an oleanane-type triad compound, and also provides its preparation method and medical application. Acid phosphatase 1B activity of oleanane-type (oleanane-type) triad compounds, structure: R1 is hydroxyl, acetoxy, R2 is carboxyl, hydroxymethylene, R3 is methyl, carboxyl, R4 For carboxyl, methyl. Multiple in vitro protein tyrosine phosphatase 1B inhibition experiments show that the compound has obvious PTP1B inhibitory activity and can be used in the preparation of medicines for diabetes, obesity and complications.
Owner:BEIHUA UNIV
Glycoside class compound of mango, preparation method, and application in area of medicine
This invention discloses compounds with natural product mangiferin as the frame. The general chemical structure of the compounds is shown in formula I, wherein, R1 and R2 are C1-20 linear or branched alkyl, benzyl, or substituted benzyl. The substituent is halogen, alkyl, etc. The compounds have strong inhibitive activity on protein tyrosine phosphatase 1B (PTP1B). This invention also discloses a method for preparing the compounds. The compounds can be used to treat diseases related to PTP1B inhibition, including diabetes type 2.
Owner:SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
Method for purifying effective ingredients of cicer ariethnum L. bean sprouts
ActiveCN102000138AIncrease contentEasy to purifyMetabolism disorderDigestive systemAlcoholAdditive ingredient
The invention relates to a method for purifying effective ingredients of cicer ariethnum L. bean sprouts. The method comprises the following steps of: selecting superior cicer ariethnum L.; germinating; picking the bean sprouts; drying; crushing; adding alcohol; heating for refluxing and extracting; collecting the extracting solution; recycling the alcohol under reduced pressure to obtain the extracting solution; then purifying with polyamide which is a macroporous resin; eluting with alcohol solution; concentrating under reduced pressure; and drying in vacuum to obtain the effective ingredients of the cicer ariethnum L. bean sprouts, such as total saponins and total isoflavones. The effective ingredients of the cicer ariethnum L. bean sprouts such as total saponins and total isoflavones proved by an in vitro sugar reducing experiment have inhibition effect to protein tyrosine phosphatase 1B and have good activity. The content of the effective ingredients of the cicer ariethnum L. bean sprouts, such as total saponins and total isoflavones is up to 52%, which has good repeatability. The resin can be reused.
Owner:XINJIANG TECHN INST OF PHYSICS & CHEM CHINESE ACAD OF SCI
Suppressive activity of mango aglycone on PTP1B and application thereof
InactiveCN101669934AHigh activityIncreased sensitivityOrganic active ingredientsMetabolism disorderDiseaseDiabetes model
The invention belongs to the technical field of biological pharmacy, and in particular relates to suppressive activity detection of tetrahydroxy norathyriol on protein-tyrosine-phosphatase (PTP) 1B, improvement of resistance function of insulin and accpication in medicament for PTP1B related diseases. Proved by in vitro enzyme suppression experiments, the invention testifies that mango aglycone is the competitive suppressant of restructuring humanized PTP1B with IC50 value being 9.2 mu m; mango aglycone can ensure the sensitivity of C57BL / 6 normal mouse and ob / ob diabetes model mouse on insulin to be obviously improved, and reduce blood sugar of experimental animals, which suggests that mango aglycone is a novel suppressant of PTP1B, and can be taken as potential lead compound to be applied in preparing medicament for curing insulin resistance related diabetes, obesity and other metabolic syndrome, tumor and other PTP1B related diseases.
Owner:NANJING UNIV
RNA interference mediated inhibtion of protein tyrosine phosphatase-1B (PTP-1B) gene expression using short interfering nucleic acid (siNA)
InactiveUS20060019913A1Improve bioavailabilityMinimize the possibilityCompounds screening/testingSugar derivativesProtein Tyrosine Phosphatase 1BDouble strand
This invention relates to compounds, compositions, and methods useful for modulating protein tyrosine phosphatase-1B (PTP-1B) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of PTP-1B gene expression and / or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of PTP-1B genes. Such small nucleic acid molecules are useful, for example, for treating, preventing, inhibiting, or reducing obesity, insulin resistance, diabetes (eg. type II and type I diabetes) in a subject or organism, and for any other disease, trait, or condition that is related to or will respond to the levels of PTP-1B in a cell or tissue, alone or in combination with other treatments or therapies.
Owner:SIRNA THERAPEUTICS INC
Protein tyrosine phosphatase inhibitors and methods of use thereof
The present invention provides compounds of Formula (I) and Formula (II) that are useful for modulating the biological activity of the protein tyrosine phosphatase-1b (PTP1B) enzyme. Compounds of this invention can be used to treat diseases and / or conditions in which the PTP1B enzyme is a factor. Such diseases and / or conditions include, but are not limited to, Type 1 diabetes, Type 2 diabetes, inadequate glucose tolerance, insulin resistance, obesity, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, low HDL levels, atherosclerosis, vascular restenosis, inflammatory bowel disease, pancreatitis, adipose cell tumors, adipose cell carcinoma, liposarcoma, dyslipidemia, cancer, and neurodegenerative diseases.
Owner:FALCON TECH PARTNERS LP
Phloroglucinol derivative capable of inhibiting PTP1B activity, and preparation method and applications thereof
Owner:NORTHEASTERN UNIV
Pharmaceutical uses of black-seed grass-seed oil of tuberculate fruit
The invention discloses a drug application of tumour-fruit black-seed grass-seed oil, which is characterized by the following: squeezing from tumour-fruit black-seed through normal method; extracting in the solvent; decompressing to remove solvent; testing the effect of protein tyrosine phosphatase 1B (PTP1B) inhibitor to resist lipid peroxidization and remove free radical of oxygen. The invention also provides an application in the antidiabetic drug and anti-oxidizing drug and health products.
Owner:新疆宝康药业有限公司
Compounds from an extract of Artemisia and methods for treating disorders
InactiveUS20070224301A1Avoid adjustmentInhibitory activityBiocideMetabolism disorderDiseaseProtein Tyrosine Phosphatase 1B
This invention comprises an extract of Artemisia dracunculus that can be used for the treatment and prevention of diabetes, diabetic complications, metabolic syndrome and other comorbidities that share the underlying commonality of insulin resistance. The invention includes the identity of six compounds from the extract that contribute to the activity of the extract by inhibiting protein tyrosine phosphatase-1B (PTP-1B) activity, phosphoenolpyruvate carboxykinase (PEPCK) gene expression or aldose reductase activity (ALR2). The compounds include 4,5-Di-O-caffeoylquinic acid, davidigenin, 6-demethoxycapillarisin, 2′,4-dihydroxy-4′-methoxydihydrochalcone, 2′,4′-dihydroxy-4-methoxdihydrochalcone and sakuranetin.
Owner:RUTGERS THE STATE UNIV
Method and composition for increasing insulin sensibility
InactiveCN101176786AIncreased sensitivityHigh biosecurityHydroxy compound active ingredientsHydrolasesDiseaseInsulin signalling
The present invention provides a use of SIRT1 protein or agonists or up-regulators thereof for manufacturing a composition which can increase insulin sensitivity. SIRT1 can be used to increase insulin sensitivity by down-regulating expression of protein tyrosine phosphatase 1B, a negative regulator of insulin action.
Owner:SHANGHAI INST OF BIOLOGICAL SCI CHINESE ACAD OF SCI
Use of pu'er tea in preparing medicament for treating or preventing diabetes
InactiveCN101411781AEnhance pharmacological effectsRich sourcesMetabolism disorderPlant ingredientsDiseaseDiabetes mellitus
The invention discloses Puerh tea and application of a preparation thereof to preparation of a medicine for treating or preventing diabetes. A product can inhibit the activity of protein tyrosine phosphatase 1B, and can be taken as a constituent of food, medicines or medicine compositions for diseases related to the protein tyrosine phosphatase 1B; and the product can be taken as food, a medicine or a medicine composition for treating a series of diseases related to the PTP1B such as diabetes, obesity and so on. The invention provides the Puerh tea and the novel application of the preparation thereof, and discloses good pharmaceutical prospect.
Owner:普洱市人民政府茶产业发展办公室科技服务中心
Protein-tyrosine-phosphatase 1B inhibitor and its preparation method and use
InactiveCN101260086AInhibitory activityOrganic active ingredientsOrganic chemistryDiseaseProtein Tyrosine Phosphatase 1B
The invention provides a PTP1B inhibitor. The concrete structure is as follows. The test shows that the inhibitor can effectively inhibit the activity of protein tyrosine phosphatase 1B (PTP1B), can be taken as insulin sensitizer, and is used to prevent, postpone or treat the related diseases resisted by insulin mediated by the PTP1B (particularly type II diabetes and obesity). The invention also provides a preparation method for the inhibitor.
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Kaurane-type diterpenoid compound as well as preparation method and medical application thereof
InactiveCN101786953AOrganic compound preparationMetabolism disorderMedicineProtein Tyrosine Phosphatase 1B
The invention relates to a kaurane-type diterpenoid compound which is a new compound and has the inhibitory activity of protein tyrosine phosphatase 1B (PTP1B). The invention also provides a preparation method and the medical application of the kaurane-type diterpenoid compound simultaneously. The kaurane-type diterpenoid compound which is prepared from feverfew herba siegesbeckiae by adopting extracting and separating processes has remarkable PTP1B inhibitory activity, can be applied to preparing medicines for treating diabetes, obesity and complications thereof and has important significant on the development and the utilization of Chinese medicinal plant resources.
Owner:BEIHUA UNIV
1-substituted-2-substituted-4- aryl substituted-butyl-2-alkene 1, 4-diketone compound, its preparation method and application
InactiveCN102234231AEffective treatmentOrganic active ingredientsOxygen-containing compound preparationDiketoneDiabetes mellitus
The invention discloses a 1-substituted-2-substituted-4- aryl substituted-butyl-2-alkene 1, 4-diketone compound, or its isomers, pharmacy-acceptable salts, preparation method and applications, and medicine compositions containing the compound. The protein-tyrosine phosphatase 1B inhibition test proves that the compound has good inhibitive activity of PTP1B, and can be used for treating diabetes mellitus, obesity and complications triggered by diabetes mellitus and obesity.
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Compound in cyclocarya paliurus and application thereof in medicament field
InactiveCN101570557AGood inhibitory effectEnhanced inhibitory effectOrganic active ingredientsSugar derivativesChemical structureChinese traditional
The invention relates to the technical field of medicaments, and in particular discloses a novel compound which is separated from cyclocarya paliurus and is used for treating diabetes and adiposis. Through various modern spectral analyses, particularly by applying various comprehensive analysis and X-diffraction analysis of advanced two-dimensional NMR spectrums, the chemical structure and the spatial configuration of the compound is defined, and the chemical structural formula of the compound is a formula (1). A protein tyrosine phosphatase 1B (PTP1B) inhibition experiment shows that the compound has remarkable PTP1B inhibitory effect. The compound can provide a lead compound for developing a novel medicament or a heath product for reducing glycemia and treating the adiposis, and has important values in developing and using Chinese herbal medicament resources.
Owner:SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
Ruthenium-containing complex for inhibiting protein tyrosine phosphatase 1B activity as well as preparation method of complex and protein tyrosine phosphatase 1B inhibitor
InactiveCN103360428AInhibitory activityMetabolism disorderGroup 8/9/10/18 element organic compoundsProtein Tyrosine Phosphatase 1BTyrosine
The invention discloses a ruthenium-containing complex for inhibiting protein tyrosine phosphatase 1B activity and a preparation method of the complex. The invention further discloses a protein tyrosine phosphatase 1B inhibitor which contains the ruthenium-containing complex. The ruthenium-containing complex for inhibiting protein tyrosine phosphatase 1B activity disclosed by the invention is a complex as shown in formula (1), wherein in the formula (1), A is one of structures as shown in formulas (2)-(8), and X is halogen. The ruthenium-containing complex has good protein tyrosine phosphatase 1B inhibiting activity.
Owner:INST OF CHEM CHINESE ACAD OF SCI
Novel medical application of isopentenyl isoflavone compounds in licorice roots
ActiveCN105582005ACosmetic preparationsOrganic active ingredientsProtein Tyrosine Phosphatase 1BLicorice roots
The invention discloses novel medical application of isopentenyl isoflavone compounds in licorice roots. Through systematic research on the chemical components and activity screening of the licorice roots, it is discovered that the isopentenyl isoflavone compounds including licoricidin, angustone A and glyasperin D of which the structures are similar have the significant activity on inhibition of cancer cell proliferation and inhibition of protein tyrosine phosphatase 1B (PTP1B), licoricidin and glyasperin D have the significant activity on inhibition of acetylcholine esterase (AChE), and glyasperin D also has the significant activity on inhibition of tyrosinase. On the basis of the discovery, the active compounds or salt, ester and solvent compounds, stereoisomers, tautomer and prodrugs which are acceptable in pharmacy of the active compounds and mixtures of the compounds can be used for preparing anti-cancer drugs, PTP1B inhibitors, antidiabetic drugs, tyrosinase inhibitors, freckle removing and whitening products, AChE inhibitors, anticholinesterase drugs and the like.
Owner:PEKING UNIV
3-(2-carboxylbenzoyl)-oleanolic acid, pharmaceutical composition of same and application of same in treating diabetes and/or obesity
InactiveCN101525366AEasy to synthesizeEasy to manufactureOrganic active ingredientsMetabolism disorderDiseaseWHOLE ANIMAL
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Genipin derivatives and their preparation method and use
ActiveCN107382951ALow toxicityShorten the overall cycleOrganic active ingredientsSugar derivativesProtein Tyrosine Phosphatase 1BStereochemistry
The invention provides genipin derivatives and their preparation method and use and specifically discloses genipin derivatives having novel structures shown in the formula I. The groups are defined in the specification. The invention also discloses a preparation method of the compounds and use of the compounds as protein tyrosine phosphatase 1B (PTP1B) inhibitors. The compounds produce good anti-diabetic effects and have an application value in preparation of drugs for treating type II diabetes.
Owner:SHANGHAI JIAO TONG UNIV
Preparation method of chickpea total saponin
ActiveCN101991635ALow priceImprove securityMetabolism disorderPlant ingredientsProtein Tyrosine Phosphatase 1BMass content
The invention relates to a preparation method of chickpea total saponin, comprising the following steps of: crushing and sieving chickpeas; adding solvent oil; degreasing by heating and refluxing; extracting by heating and refluxing; collecting an extracting solution; reducing pressure to recover ethanol; concentrating; purifying a concentrated solution by using macroporous resin; drying in vacuum; and obtaining a purifying product of the chickpea total saponin, wherein the mass content of the purifying product reaches 22-25 percent. Through an in-vitro hypoglycemic experiment, the obtained chickpea total saponin product has an inhibit function on protein-tyrosine-phosphatase 1B, and a result indicates that the chickpea total saponin has better activity; meanwhile, the preparation method has good reproduction quality, and resin can be repeatedly used.
Owner:XINJIANG TECHN INST OF PHYSICS & CHEM CHINESE ACAD OF SCI
Pinus dabeshanensis Cheng et Law bark extracts and preparation method thereof, and uses of Pinus dabeshanensis Cheng et Law bark extracts in pharmacy
ActiveCN107021942ASignificant PTP1B enzyme inhibitory activityOrganic active ingredientsMetabolism disorderProtein Tyrosine Phosphatase 1BDrug biological activity
The present invention belongs to the field of traditional Chinese medicines, and relates to Pinus dabeshanensis Cheng et Law bark extracts. According to the present invention, the diterpene compounds having structures defined in the specification and having protein-tyrosine phosphatase 1B (PTP1B) inhibition activity are extracted and separated from the bark of the Pinaceae Pinus plant Pinus dabeshanensis Cheng et Law, and the in vitro biological activity test results prove that the compounds have the significant PTP1B inhibition activity; and the obtained compounds can be used for preparing drugs for prevention, delaying or treatment of diabetes, obesity and complications thereof, and other PTP1B-mediated diseases.
Owner:FUDAN UNIV
PTP1B inhibitors and synthesis thereof, and application of PTP1B inhibitors to preparation of medicines for treating type 2 diabetes
ActiveCN102018692ALow costHigh yieldOrganic compound preparationMetabolism disorderTreatment effectProtein Tyrosine Phosphatase 1B
The invention relates to a chemical total synthesis method for six novel PTP1B inhibitors, and application of the PTP1B inhibitors to the preparation of medicines for treating type 2 diabetes. The active ingredients of the PTP1B inhibitors are one or more of six compounds with structural formulas shown in the specifications. The compound enhances the sensitivity of an insulin receptor by inhibiting the activity of protein tyrosine phosphatase 1B (PTP1B), and has good treatment effect on insulin-resistant type 2 diabetes.
Owner:INST OF OCEANOLOGY - CHINESE ACAD OF SCI
Blood glucose reduction use of kardiseed dreg extractive
The invention relates to a blood glucose reduction use of a kardiseed dreg extractive, namely the use of the kardiseed dreg extractive in preparation of a drug for treating glycuresis, drug screening a target-protein-tyrosine-phosphatase 1B inhibitor, functional foods or medicine composition for treating glycuresis. The kardiseed dreg extractive mentioned in the invention is obtained by means of ethanol extraction and chloroform extraction, and simultaneously the effects of the protein-tyrosine-phosphatase 1B inhibitor of the kardiseed dreg extractive and the drugs, functional foods and medicine compositions formed by the kardiseed dreg extractive for treating glycuresis are proved externally.
Owner:新疆宝康药业有限公司
Novel sulfonamide compound, preparation method, and use of novel sulfonamide compound as protein tyrosine phosphatase 1B inhibitor
The invention relates to a novel sulfonamide compound in a structure of a general formula I as shown in the specification, or pharmaceutically acceptable salt and a preparation method of the novel sulfonamide compound, and further relates to a drug composition containing the compound as shown as the general formula I or the pharmaceutically acceptable salt of the compound, and a use of the compound or the pharmaceutically acceptable salt for preparing a drug for preventing and / or treating symptoms or diseases such as hyperglycemia and diabetes mellitus type 2 since the compound as shown as the general formula I or the pharmaceutically acceptable salt of the compound has activity of inhibiting a protein tyrosine phosphatase 1B (PTP 1B).
Owner:QILU UNIV OF TECH
Pharmaceutical and food composition for preventing or treating diabetes or obesity
InactiveCN103249410AOrganic active ingredientsOrganic chemistryDiabetes mellitusStereocaulon alpinum
Owner:KOREA OCEAN RES & DEV INST
Three protein tyrosine phosphatase 1B (PTP1B) inhibitors and synthesis and application thereof
InactiveCN102020540ALow costHigh yieldOrganic chemistryMetabolism disorderSynthesis methodsProtein Tyrosine Phosphatase 1B
The invention relates to a chemical complete synthesis method for three novel PTP1B inhibitors and application of the PTP1B inhibitors in medicines for treating type II diabetes. The chemical structural formulas of the PTP1B inhibitors are shown as follows: a compound 6 (4, 5-di-(2, 3-dibromo-4, 5-dimethoxybenzyl)-1, 2-dimethoxyphenyl): groups connected with C of 2', 3', 2'' and 3'' sites of a benzene ring are bromine atoms, and C of 1, 2, 4', 5', 4'' and 5' sites is connected with methoxyl; a compound 7 (3-bromo-4, 5-di-(2, 3-dibromo-4, 5-dimethoxybenzyl)-1): the groups connected with C of 3, 2', 3', 2'' and 3'' sites of the benzene ring are bromine atoms, and C of 1, 2, 4', 5', 4'' and 5' sites is connected with the methoxyl; and a compound 8 (3-bromo-4, 5-di-(2, 3-dibromo-4, 5-dyhydroxylbenzyl)-1, 2-dihydroxybenzene): the groups connected with C of 3, 2', 3', 2'' and 3'' sites of the benzene ring are bromine atoms, and C of 1, 2, 4', 5', 4'' and 5'' is connected with hydroxyl. The three compounds enhance the sensitivity of an insulin receptor through inhibiting the activity of protein tyrosine phosphatase 1B and have good therapeutic action on insulin resistant type II diabetes.
Owner:INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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