32 results about "Phosphatase inhibitor" patented technology

The invention relates to the field of biotechnology and medicine, and more particularly to a polypeptide having the amino acid sequence SEQ ID NO: 1 and being capable of inhibiting RAS-GTPase activity, to the use of said polypeptide to produce a drug for treating stomach cancer or rectal cancer in a dose of 0.81-3.00 mg / kg, as well as to a drug based on said polypeptide for the treatment of stomach cancer or rectal cancer, and to a method for treating stomach cancer or rectal cancer by intraperitoneally administering said drug to a subject in an amount of 150 ml twice at an interval of 7 days.

The invention belongs to the field of medical chemistry, and particularly discloses a protein tyrosine phosphatase (PTPN) inhibitor as shown in a formula 1, a pharmaceutical composition and application of the PTPN inhibitor. The invention discloses a method for treating related diseases such as cancers and metabolic diseases by using the protein tyrosine phosphatase inhibitor. # imgabs0 #

The invention belongs to the field of medical chemistry, and particularly discloses a protein tyrosine phosphatase inhibitor, such as type 2 non-receptor protein tyrosine phosphatase (PTPN2) and / or type 1 non-receptor protein tyrosine phosphatase (PTPN1) inhibitor, a pharmaceutical composition and application thereof. The invention discloses a method for treating related diseases such as cancers and metabolic diseases by using the protein tyrosine phosphatase inhibitor.

Disclosed herein are apyrase inhibitors of Formula (I). Also disclosed herein are methods for using the disclosed inhibitors, including in methods for protecting crops from pests. In one aspect the apyrase inhibitors are useful for enhancing the activity of pesticides for the protection of crops from pathogens and to support crop yield.

The present invention relates to a benzo ring-containing compound as a PTPN1 and / or PTPN2 inhibitor and use thereof, and particularly relates to a compound of formula (I), a tautomer thereof, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, a method for preparing same, and use thereof in the preparation of a medicament for treating a PTPN1 and / or PTPN2-related disease.

The present invention relates to a double bond substituent containing compound serving as a PTPN1 and / or PTPN2 inhibitor, and a use thereof, and in particular to a compound represented by formula (I), a tautomer, a stereoisomer, or a pharmaceutically acceptable salt thereof, and a preparation method therefor, and a use in the preparation of a drug for treating diseases related to PTPN1 and / or PTPN2.

The utility model discloses a distributing and mixing device for phosphatase inhibitors, which relates to the technical field of distributing and mixing devices for inhibitors and comprises a magnetic stirrer, a mixing bottle is mounted on the magnetic stirrer, supports are arranged on two sides of the magnetic stirrer, and a proportioning component is arranged between the two supports. Proportioning the phosphatase inhibitor with a solvent when the phosphatase inhibitor is diluted; a stirring assembly is arranged at the bottom end of the proportioning assembly and is used for diluting and stirring the phosphatase inhibitor and the solvent. According to the invention, centralized treatment of distribution and mixing of the phosphatase inhibitor is realized, the step that an operator needs to quantitatively transfer a reagent by using a pipette for many times is reduced, and the operation steps of an experimenter are simplified. The problem that an operator needs to continuously and accurately sample, stir and dropwise add the phosphatase inhibitor in the distribution and mixing process is solved, the operation difficulty and steps of the operator are simplified, and operation is more concentrated and convenient.

The invention relates to a benzoring-containing compound serving as a PTPN1 and / or PTPN2 inhibitor and application thereof, in particular to a compound shown in a formula (I), a tautomer, a stereoisomer or pharmaceutically acceptable salt of the compound, a preparation method of the compound, and application of the compound to preparation of drugs for treating PTPN1 and / or PTPN2 related diseases. (I)

The invention discloses a method for extracting high-purity liver cell membranes of pelteobagrus fulvidraco. The method comprises the following steps: firstly, cutting the liver into pieces to obtain large liver tissues; digesting the large liver tissue for multiple times by using isopyknic protease liquid; adding an extraction reagent 1 containing a protease inhibitor and a phosphatase inhibitor into the digested small tissues and cell precipitates, and ultrasonically crushing to obtain homogenate; performing low-speed centrifugation on the homogenate for multiple times to collect supernate, and performing high-speed centrifugation for multiple times to collect clear liquid; carrying out ultracentrifugation to collect the precipitate, and resuspending; obtaining a coarse cell membrane suspension; adding the coarse cell membrane suspension into a centrifugal tube, then adding a sucrose density gradient buffer solution until the centrifugal tube is filled with the coarse cell membrane suspension, and carrying out ultracentrifugation; and resuspending the cell membrane precipitate to obtain the pelteobagrus fulvidraco liver cell membrane. Immunoblotting verification on the cell membrane and other organelles extracted by the method shows that the cell membrane extracted by the method conforms to the expected effect of high purity, and other organelles contained in the cell membrane have few impurities.

The invention relates to a compound containing double bond substitution as a PTPN1 and / or PTPN2 inhibitor and application thereof, in particular to a compound shown in a formula (I), a tautomer, a stereoisomer or pharmaceutically acceptable salt of the compound, a preparation method of the tautomer, the stereoisomer or the pharmaceutically acceptable salt of the compound, and application of the tautomer, the stereoisomer or the pharmaceutically acceptable salt in preparation of drugs for treating PTPN1 and / or PTPN2 related diseases.

The present disclosure relates, in part, to crystalline forms of (R)-1'-(3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl)-3H-spiro[benzofuran-2,4'-piperidin]-3-amine, salts thereof, and variants thereof.

Provided herein are methods of using a combination comprising protein tyrosine phosphatase non-receptor type 2 (PTPN2) and / or protein tyrosine phosphatase non-receptor type 1 (PTPN1) and an additional therapeutic agent to treat a disease (e.g., cancer or metabolic disease) that produces an advantageous response to PTPN1 or PTPN2 inhibitor treatment.

The disclosure is in part directed to crystalline forms of (R)-1'-(3 -(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4- b|pyrazin-6-yl)-3H-spiro[benzofuran-2,4'-piperidin]-3 -amine, its salt, and variants thereof.

The invention provides new pyrazine derivatives of formula (I):or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein. The invention also provides pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

The present disclosure relates to an oily flowable formulation comprising a first active compound # imgabs0 # having structure (I) and a lipophilic solvent, a first dispersant and a rheology modifier. The formulation comprises particles of the first active compound having a median particle size of 0.1 to 20 microns as measured by light scattering. The formulation may further comprise an emulsifier, a second dispersant, and / or an agriculturally active compound such as an acaricide, an antimicrobial agent, a fungicide, a herbicide, an insecticide, a molluscicide, or a nematicide, or a combination thereof. Also disclosed are agricultural compositions comprising the formulations and methods of using the same.

The present application relates to the technical field of pharmacy, in particular to application of compound Diaporterpene C in preparation of mycobacterium tuberculosis tyrosine phosphatase inhibitor. The present application provides application of compound Diaporterpene C in preparation of mycobacterium tuberculosis tyrosine phosphatase inhibitor, the compound can significantly inhibit the activity of key virulence factor tyrosine phosphatase MptpA and MptpB of mycobacterium tuberculosis, can be used as tyrosine phosphatase inhibitor with MptpA and / or MptpB as target, and can be further developed as anti-tuberculosis drug. The compound shows good anti-tuberculosis activity by inhibiting pathogenic signal pathway of pathogenic bacteria, and has important clinical application potential and development value in tuberculosis treatment.

The present disclosure relates to novel compounds including formula (X) and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure.

Collapsing focal segmental glomerulosclerosis (collapsing FSGS), also known as collapsing glomerulopathy (CG), is the most aggressive variant of FSGS and is characterized by rapid progression to end-stage kidney disease (ESKD). The inventors used the telomerase-induced mouse model of CG (i-TERTci mice) to identify mechanisms to inhibit CG pathogenesis. They found that inactivation of WIP1 phosphatase, a p53 target acting in a negative feedback loop, blocks disease initiation in i-TERTci mice. They found that pharmacologic inhibition of WIP1 enzymatic activity in either telomerase mice with CG or in Tg26 mice promotes partial remission of proteinuria and ameliorates renal histopathologic features. Their findings suggest that targeting WIP1 may be an effective therapeutic strategy for patients with CG. Thus, the present invention relates to a method of preventing or treating glomerular disease (e.g. focal segmental glomerulosclerosis, in particular collapsing glomerulopathy) in a subject in need thereof, comprising the step of administering to said subject a Wild-type p53-induced phosphatase 1 (WIP1) inhibitor.

The present disclosure relates to a formulation comprising an aqueous suspension of a first active compound having the following structure; and a dispersant, a freezing point inhibitor and a buffer or a partially neutralized base such that the pH of the formulation is from about 6 to about 11. The formulation comprises particles of the first active compound having a volume weighted median particle size of greater than 0.01 to 20 microns as measured by light scattering. The formulation may further comprise a viscosity modifier, a biocide, a defoamer, a surfactant and / or an agriculturally active compound such as an acaricide, an antimicrobial agent, a fungicide, a herbicide, an insecticide, a molluscicide or a nematicide or a combination thereof. Also disclosed are agricultural compositions comprising the formulations and methods of using the same. # imgabs0 #

The invention discloses a Homoaconitic acid extracted from tremella fuciformis as well as an extraction method and application of the Homoaconitic acid, and belongs to the field of research and development of natural medicines. The lappaconitic acid is obtained from tremella sporocarp through extraction, separation and purification for the first time, and the lappaconitic acid can serve as a novel phosphatase inhibitor to be used for developing drugs for treating bone diseases, cancers and inflammations or developing products for improving soil or water eutrophication.

Provided are methods of using molecules as described herein in supporting crop viability and yield, such as by protecting crops from pests. In some cases, the methods inhibit apyrase enzymes by contacting such enzymes with a compound of the formula (I), wherein G, Z, and R1 are as described herein. In further embodiments, an apyrase inhibitor as described herein is used in combination with one or more pesticide to treat a crop at risk of disease.

Disclosed herein are adenosine triphosphate biphosphatase inhibitors of formula (I): # imgabs0 #. Also disclosed herein are methods of using the disclosed inhibitors, including methods for protecting crop plants from pest attack. In one aspect, the adenosine triphosphate biphosphatase inhibitors may be used to enhance the activity of insecticides to protect crops from pathogens and to support crop yield.

The present invention provides enrichment, detection methods and applications of GPC-3 complexes in blood samples. The enrichment method includes A. collecting peripheral blood from liver cancer patients, placing it in an anticoagulant tube and mixing the whole blood; B. adding multiple volumes of red blood cell lysis solution, pipetting and mixing, lysing on ice, centrifuging and discarding the red supernatant. If the cell pellet is still red, repeat this step; C. washing the pellet 1-2 times, adding PBS or normal saline to resuspend the pellet, centrifuging and discarding the supernatant; D. counting white blood cells, adding PBS to resuspend the cell pellet, taking an appropriate amount to fill the pool, letting it stand for 2-3 minutes, and manually counting the white blood cells using the four large squares in the four corners of the low-power microscope. The calculation formula is as follows: WBC / L=N / 4*10 5 *10 4 , and calculate the number of white blood cells per milliliter of the original suspension, WBC / ml original suspension = N / 4*10 4 *Dilution factor; E. Add lysis buffer containing 1% protease inhibitor and 1% phosphatase inhibitor to the obtained cells, refrigerate and let stand for a certain period of time, and then centrifuge to obtain the supernatant as the sample to be tested to achieve GPC-3 enrichment.

Disclosed herein are apyrase inhibitors of Formula (I): (I). Also disclosed herein are methods for using the disclosed inhibitors, including in methods for protecting crops from pests. In one aspect the apyrase inhibitors are useful for enhancing the activity of pesticides for the protection of crops from pathogens and to support crop yield.

Disclosed herein are apyrase inhibitors of Formula (I): (I). Also disclosed herein are methods for using the disclosed inhibitors, including in methods for protecting crops from pests. In one aspect the apyrase inhibitors are useful for enhancing the activity of pesticides for the protection of crops from pathogens and to support crop yield.

Expression of a phosphatase inhibitor in heart cells can be used to treat cardiac disorders, e.g., heart failure. Decreasing phosphatase activity can improve β-adrenergic responsiveness.

Described herein is a method of determining if a kinase inhibitor is a phosphatase enhancer or inhibitor, the method including providing a phosphorylated target kinase substrate; contacting the kinase inhibitor, the phosphorylated target kinase substrate and the phosphatase under conditions for dephosphorylation of the target kinase substrate by the phosphatase; quantitating dephosphorylation of the phosphorylated target kinase substrate in the presence and absence of the kinase inhibitor; and determining the kinase inhibitor is a phosphatase enhancer when its presence increases the rate of dephosphorylation of the target kinase, or determining the kinase inhibitor is a phosphatase inhibitor when its presence decreases the rate of dephosphorylation of the target kinase.

Disclosed herein are embodiments of water dispersible granules (and compositions / formulations thereof) comprising a first active compound having structure (I), a dispersant, and optionally a dust inhibitor. # imgabs0 #

Derivatives, including deuterated derivatives, of the SHP-1 inhibitor compound 2-(2,5- dichlorophenyl)benzoquinone (which is also referred to as 2-(2,5-dichlorophenyl)cyclohexa-2,5- diene- 1,4-dione, Tyrosine Phosphatase Inhibitor 1 or TPI-1; CAS Registry No. 79756-69-7) are provided. The TPI-1 derivatives can be used in treatment of diseases such as cancer.