163 results about "Protein Tyrosine Phosphatase 1B" patented technology

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.

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.

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.

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.

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.

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.

The invention discloses a phloroglucinol derivative capable of inhibiting PTP1B activity, and a preparation method and applications thereof, and more specifically relates to a phloroglucinol compound which is obtained via extraction and separation from Eugenia jambolana Lam seeds, a preparation method thereof, and applications of the phloroglucinol compound in preparing drugs used for treating diabetes and obesity, or inhibitors of protein tyrosine phosphatase 1B (PTP1B). The general molecular formula of the phloroglucinol compound is represented by formula I, wherein R1 is used for representing methyl or hydrogen, R2 is used for representing methyl or hydrogen, R1 and R2 are used for representing the same or the different groups, and R3 is used for representing an alkane or olefin side chain containing 12 to 26 carbon atoms. The phloroglucinol compound is a novel compound with excellent PTP1B inhibition effect; the PTP1B inhibition activity IC50 value ranges from 0.42 to 3.16<mu>M; the phloroglucinol compound can be used for preparing PTP1B inhibitors, and drugs used for treating diabetes, obesity, and complications of diabetes and obesity.

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.

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.

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.

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.

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.

The invention discloses 3-(2-carboxylbenzoyl)-oleanolic acid or physiologically acceptable salt of the same, application of the same and a pharmaceutical composition containing the compound. The compound has inhibition effect on protein tyrosine phosphatase 1B (PTP1B) and 11beta-hydroxysteriod dehydrogenase 1 (11beta-HSD1), has antagonism effect on a glucocorticoid receptor (GR), has agonistic effect on nuclear receptor LXRa: RXRa heterodimer, and can also strengthen the expression of glucose transporter 4 (Glut4) at the same time. A whole animal experiment shows that the compound has hypoglycemic activity. Therefore, the 3-(2-carboxylbenzoyl)-oleanolic acid or the physiologically acceptable salt of the same can be used for treating diabetes, obesity and complicating diseases thereof caused by insulin resistance.

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.

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.

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.

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.

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).

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.