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36 results about "Translocator protein 2" patented technology

Substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2h-pyrido[2,1-a]isoquinolin-2-ol compounds and methods relating thereto

ActiveUS20080167337A1BiocideNervous disorderIsoquinolineVesicular monoamine transporter 2
Substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol compounds are disclosed that are inhibitors of the vesicular monoamine transporter 2 (VMAT2). The compounds of this invention have the structure:wherein R1 is as defined herein, including stereoisomers and pharmaceutically acceptable salts and solvates thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use in a subject in need thereof.
Owner:NEUROCRINE BIOSCI INC

Thiazole derivatives as SGLT2 inhibitors and pharmaceutical composition comprising same

ActiveUS8586550B2Prevention and/or treatment of metabolic disordersReduce usageBiocideSaccharide with heterocyclic radicalsSodium dependentSGLT2 Inhibitor
The present invention relates to a novel compound with thiazole ring having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes.
Owner:THE GREEN CROSS CORP

Thiazole Derivatives as SGLT2 Inhibitors and Pharmaceutical Composition Comprising Same

The present invention relates to a novel compound with thiazole ring having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes.
Owner:THE GREEN CROSS CORP

Anti-system asc amino acid transporter 2 (ASCT2) antibody

An object of the present invention is to provide a monoclonal antibody which is useful for treating or diagnosing a disease relating to system ASC amino acid transporter 2 (hereinafter, referred to as “ASCT2”) or a method using the antibody. The present invention provides a monoclonal antibody which specifically recognizes a native three-dimensional structure of an extracellular region of ASCT2 and binds to the extracellular region, or an antibody fragment thereof; a hybridoma which produces the antibody; a DNA which encodes the antibody; a vector which contains the DNA; a transformant obtainable by introducing the vector; a process for producing an antibody or an antibody fragment thereof using the hybridoma or the transformant; and a therapeutic agent using the antibody or the antibody fragment thereof, and a diagnostic agent using the antibody or the antibody fragment thereof.
Owner:KYOWA HAKKO KIRIN CO LTD

Anti system asc amino acid transporter 2 (ASCT2) antibody

An object of the present invention is to provide a monoclonal antibody which is useful for treating or diagnosing a disease relating to system ASC amino acid transporter 2 (ASCT2) or a method using the antibody. The present invention provides a monoclonal antibody which specifically recognizes a native three-dimensional structure of an extracellular region of system ASC amino acid transporter 2 (ASCT2) and binds to the extracellular region, or an antibody fragment thereof; a hybridoma which produces the antibody; a DNA which encodes the antibody; a vector which contains the DNA; a transformant obtainable by introducing the vector; a process for producing an antibody or an antibody fragment thereof using the hybridoma or the transformant; and a therapeutic agent using the antibody or the antibody fragment thereof, and a diagnostic agent using the antibody or the antibody fragment thereof.
Owner:KYOWA HAKKO KIRIN CO LTD

1-(beta-d-pyranoglucosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene and l-phenylalanine eutectic compound and preparation method thereof

The invention discloses an eutectic compound of 1-(beta-D-pyranoglucosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene and L-phenylalanine and a preparation method thereof. Specifically speaking, the invention discloses the eutectic compound shown in a formula (Ia) and formed by L-phenylalanine and a sodium-glucose co-transporter 2 (SGLT-2) inhibitor shown in a formula (I), i.e., 1-(beta-D-pyranoglucosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene. The XRD characteristic peaks of the eutectic compound are shown in a figure 1. The preparation method comprises the following steps: mixing an aqueous solution of L-phenylalanine with an ethanol solution of the compound I; carrying out heating for dissolving of the two substances; then carrying out stirring, cooling and crystallization; and subjecting a filtrate to ethanol water recrystallization so as to obtain the eutectic compound. The formula (I) and the formula (Ia) are described in the specification.
Owner:JIANGSU HANSOH PHARMA CO LTD +1

Method for dual inhibition of SGLT1 and SGLT2 using diphenylmethane derivatives

The present invention relates to a method for dual inhibition of sodium-dependent glucose cotransporter 1 (SGLT1) and sodium-dependent glucose cotransporter 2 (SGLT2) present in the intestine and kidney by using the compound of formula I or a pharmaceutically acceptable salt or a prodrug thereof:wherein ring A, ring B, X and Y have the same meanings as defined in the specification.
Owner:THE GREEN CROSS CORP

Preparation method suitable for industrial production of empagliflozin

The invention belongs to the technical field of organic synthesis route design and medicine and chemical engineering, particularly relates to a synthesis method of a sodium-glucose cotransporter 2(SGLT2) inhibitor, and more particularly relates to a preparation method of empagliflozin. The empagliflozin is synthesized by taking (3S)-3-[4-[(2-chloro-5-iodophenyl) methyl] phenoxy] tetrahydrofuran and glucono delta-lactone as initial raw materials through a series of substep reactions such as protection, addition, substitution, deprotection and reduction. In the synthesis steps disclosed by the invention, a staged target product does not need to be separated and purified after each step of reaction, and the target product is finally obtained by directly subjecting a high-purity reaction intermediate to subsequent steps. The preparation method is simple in process, simple and convenient to operate and good in industrial prospect.
Owner:XUZHOU WANBANG JINQIAO PHARMA +1

Glucoside derivatives and pharmaceutical compositions thereof

The invention provides glucoside derivatives and pharmaceutical compositions thereof. The invention discloses chemical compounds as shown in general formula (I), pharmaceutically-acceptable salts thereof, easily-hydrolytic lipid prodrug thereof or isomers thereof, and the pharmaceutical compositions containing the chemical compounds which is used as sodium-glucose cotransporter 2 inhibitor used for treating or suspending relative diseases like diabetes mellitus, diabetic retinopathy, diabetic neuropathy, diabetic nephropathy and insulin resistance.
Owner:JIANGSU ATOM BIOSCI & PHARMA CO LTD

Benzimidazole derivatives and medical uses thereof

The present invention provides benzimidazole derivatives represented by the following formula (I) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an inhibitory activity on sodium-dependent nucleoside transporter 2 and are useful for a disease associated with an abnormality of plasma uric acid level. The compounds of the present invention are useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; R1 and R2 are H, a halogen atom, cyano group, optionally substituted alkyl group, optionally substituted aryl group or the like; R3 is H, a halogen atom, optionally substituted alkyl group or the like; R4 and R5 are H, a halogen atom, OH or the like; and R6 and RX are H or OH: RY is F or OH.
Owner:KISSEI PHARMA

SGLT2 as biomarker for diagnosing chronic kidney disease and monitoring the disease status after treatment

The present invention relates to a method for diagnosis of a chronic kidney disease in a subject by detecting the expression level of a sodium-glucose linked transporter 2 (SGLT2) protein in urine samples. A method for monitoring progression of a chronic kidney disease in a patient is also provided.
Owner:NAT DEFENSE MEDICAL CENT

Preparation method of sodium-glucose cotransporter 2 inhibitor

ActiveCN107686496ASaccharide with carbocyclic radicalsSugar derivativesSodium-Glucose Cotransporter 2 InhibitorPalladium
The invention discloses a preparation method of a sodium-glucose cotransporter 2 inhibitor. The preparation method specifically relates to a reaction step for converting a compound of a formula III into a compound of a formula II by a 'one-pot method' in a palladium carbon / acid or 1,2-dichlorobenzene catalytic system, wherein the definition of each substituent in the formula II and the formula IIIare the same as that in the description. The method has simple operation and low cost, and is suitable for large-scale production.
Owner:JIANGSU HENGRUI MEDICINE CO LTD

Novel SGLT2 inhibitor compounds and pharmaceutical composition thereof

The invention discloses novel SGLT2 inhibitor compounds shown in a formula (I), pharmaceutically acceptable salts, easily hydrolyzed pre-drug esters or isomers and a pharmaceutical composition which contains the compounds as an inhibitor of a sodium-glucose co-transporter (SGLT). The pharmaceutical composition is used for treating or delaying related diseases such as diabetes, diabetic retinopathy, diabetic neuropathy, diabetic nephropathy, insulin resistance, hyperglycemia, hyperinsulinemia, rise of fatty acid or glycerinum, hyperlipemia, obesity, hypertriglyceridemia, X syndrome, diabetic complications, atherosclerosis, hypertension and the like. The formula is shown in the description.
Owner:JIANGSU ATOM BIOSCI & PHARMA CO LTD

Agent for treating retinopathy

It is to provide an agent for treating and / or ameliorating retinopathy caused by glucose. It is an agent for treating retinopathy caused by glucose comprising sodium / glucose cotransporter2 inhibitor (SGLT2 inhibitor) as an active ingredient, and is used at a normal dosage amount, or at a lower dosage whereby no lowering in blood sugar is observed.
Owner:CARNA HEALTH SUPPORT LLC

Anti-system ASC amino acid transporter 2 (ASCT2) antibody

An object of the present invention is to provide a monoclonal antibody which is useful for treating or diagnosing a disease relating to system ASC amino acid transporter 2 (hereinafter, referred to as “ASCT2”) or a method using the antibody. The present invention provides a monoclonal antibody which specifically recognizes a native three-dimensional structure of an extracellular region of ASCT2 and binds to the extracellular region, or an antibody fragment thereof; a hybridoma which produces the antibody; a DNA which encodes the antibody; a vector which contains the DNA; a transformant obtainable by introducing the vector; a process for producing an antibody or an antibody fragment thereof using the hybridoma or the transformant; and a therapeutic agent using the antibody or the antibody fragment thereof, and a diagnostic agent using the antibody or the antibody fragment thereof.
Owner:KYOWA HAKKO KIRIN CO LTD

Novel c-aryl glucoside sglt2 inhibitors and pharmaceutical compositions comprising same

A novel C-aryl glucoside compound, or a pharmaceutically acceptable salt or a prodrug thereof having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney; and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly, diabetes, are provided.
Owner:THE GREEN CROSS CORP

Drug compound containing sodium-glucose synergic transport protein 2 inhibitor

The invention discloses a drug compound containing a sodium-glucose synergic transport protein 2 inhibitor. Specifically, the drug compound contains 1,6-dehydrated-1-C-{4-chlorine-3-[(3-fluorine-4-phenetyl) methyl] phenyl}-5-C-(hydroxymethyl)-beta-L-idose or a compound formed by the same with amino acid, pre-gelled starch and at least one pharmaceutically acceptable excipient. The drug compound disclosed by the invention has the characteristics of strong technical operability and quick and complete dissolution.
Owner:JIANGSU HENGRUI MEDICINE CO LTD

Novel c-aryl ansa sglt2 inhibitors

ActiveUS20140213642A1Prevention and/or treatment of metabolic disordersBiocideOrganic active ingredientsIntestinal structureDiabetes mellitus
Disclosed is a novel C-aryl ansa compound having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes. Also provided are a method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound.
Owner:THE GREEN CROSS CORP

Sodium-glucose cotransporter 2 (SGLT2) inhibitor and application thereof

The invention provides a sodium-glucose cotransporter 2 (SGLT2) inhibitor. The SGLT2 inhibitor is trilobatin, and the specific structure of the trilobatin is shown as the following formula (please seethe specifications for the formula); and the trilobatin and the SGLT2 interact with each other, the trilobatin is in hydrogen bond connection with ASn75 and Tyr290 sites of the SGLT2, and thus the trilobatin can significantly inhibit glucose reabsorption, lowers the overall blood glucose level of an experimental subject, and meanwhile, can further improve insulin resistance of the experimental subject effectively.
Owner:CHONGQING UNIV OF TECH
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