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37 results about "SGLT Inhibitors" patented technology

Indole derivatives

Novel indole derivatives of formula (I) or a pharmaceutically acceptable salt thereof:wherein R1 is fluorine, or chlorine, and R2 is hydrogen, or fluorine, which are SGLT inhibitors and are useful for treatment or prevention of diabetes and related conditions.
Owner:MITSUBISHI TANABE PHARMA CORP

Application of galactooligosaccharides and derivatives of galactooligosaccharides as SGLT inhibitor

The invention belongs to the field of marine medicine, and particularly relates to an application of oligosaccharides containing D-galactose and L-galactose and derivatives of the oligosaccharides asa sodium-glucose cotransporter (SGLT) inhibitor. The galactooligosaccharides and derivatives are prepared by the following steps: by using red algae polysaccharide containing the D- / L-galactose as a raw material, performing degradation by using a physical method, a chemical method, a bioenzyme method or any combination of the above methods to prepare the galactooligosaccharides and the derivativesof the galactooligosaccharides with different degrees of polymerization, wherein the molecular skeleton contains the D-galactose and the L-galactose and derivatives thereof. The raw material of the product provided by the invention is from the red algae polysaccharide, and has the advantages of rich resources, a simple preparation process, high safety, clear targets and easy industrialization, the oligosaccharides and the derivatives are used as the SGLT1 and 2 inhibitor, and has broad application prospects in the development of medicines for treating diseases such as diabetes mellitus, obesity, diabetic nephropathy and glucose and lipid metabolism disorder and functional foods for improving non-alcoholic fatty liver diseases.
Owner:OCEAN UNIV OF CHINA

C-aryl glucoside derivative, as well as medical composition, preparation method and application thereof

The invention relates to a C-aryl glucoside derivative, as well as a medical composition, a preparation method and application thereof. The preparation method comprises the following steps of: method I, in a solvent, under the action of alkali, performing a deacetylation protecting group reaction on compounds 1-f; method II: 1, performing a Mitsunobu reaction on components 2-g and (as shown in the description); and 2, performing a deacetylation protecting group reaction on the compounds 2-f obtained in the step 1; and method III: 1, mixing compounds 3-g and (as shown in the description), and performing a nucleophilic substitution reaction; and 2, performing a deacetylation protecting group reaction on the compounds 3-f obtained in the step 1. The medical composition comprises the C-aryl glucoside derivative, salt and / or prodrug of the C-aryl glucoside derivative which are / is acceptable in pharmacy, and auxiliary materials. The invention further relates to the C- aryl glucoside derivative, and application of salt or medical compositions of the C- aryl glucoside derivative, which is acceptable in pharmacy, for preparing SGLT inhibitors. The C- aryl glucoside derivative disclosed by the invention provides a new direction for research of the SGLT inhibitors. (As shown in the description)
Owner:SHANGHAI DE NOVO PHARMA

Combination therapy comprising sglt inhibitors and dpp4 inhibitors

The present invention relates to combination therapy comprising a DPP4 inhibitor and an SGLT inhibitor. The combination of the present invention leads to increase plasma GLP-1 level and the combination is useful for prevention or treatment of conditions such as diabetes and diseases related to diabetes.
Owner:MITSUBISHI TANABE PHARMA CORP

Inhibitor probes for imaging sodium-glucose cotransporters in health and disease

Radiolabeled tracers for binding to sodium / glucose cotransporters (SGLTs), and their synthesis, are provided. The tracers are high-affinity inhibitors of SGLTs, glycosides labeled with radioactive halogens. Also provided are in vivo and in vitro techniques for using the tracers as analytical tools to study the biodistribution and regulation of SGLTs in health and disease, and to evaluate therapeutic interventions. The ability to monitor radiolabel tracer disposition in real time enables the design of new SGLT inhibitors with lower metabolism and higher efficiency.
Owner:RGT UNIV OF CALIFORNIA

Glucopyranose-substituted pyrazole compound and preparation method thereof

The invention relates to a glucopyranose-substituted pyrazole compound as a drug intermediate, and a preparation method and a use thereof. Specifically, the invention relates to a key intermediate forpreparation of a compound of a novel SGLTs inhibitor for treatment of diabetes, and a preparation method and a use thereof.
Owner:YABAO PHARMA GRP CO LTD +1

Synthetic processes of intermediates for preparation of SGLT inhibitor

The invention discloses a method for preparing a compound 1 and a compound 2, the structure of the compound 1 and the structure of the compound 2 are shown in the specification.The method comprises the following steps: 1) carrying out selective dibromination on 2, 3-dihydrobenzofuran-7-aniline serving as a raw material by using a bromination reagent to obtain 4, 6-dibromo-2, 3-dihydrobenzofuran-7-aniline; 2) subjecting the 4, 6-dibromo-2, 3-dihydrobenzofuran-7-aniline obtained in the step 1) to a Sandmeyer reaction for chlorination to give 4, 6-dibromo-7-chloro-2, 3-dihydrobenzofuran; 3-1) performing selective bromine removal on the 4, 6-dibromo-7-chloro-2, 3-dihydrobenzofuran obtained in the step 2) by using a strong base, adding a formylation reagent to give the compound 1; and 3-2) performing selective bromine removal on the 4, 6-dibromo-7-chloro-2, 3-dihydrobenzofuran obtained in the step 2) by using a strong base and then reacting with 4-cyclopropylbenzaldehyde to give the compound 2.
Owner:DAEWOONG PHARM CO LTD

SGLTs (sodium-dependent glucose transporters 2) inhibitor, preparation method thereof and pharmaceutical application of inhibitor

The invention relates to a SGLTs (sodium-dependent glucose transporters 2) inhibitor with a structure as shown in a formula (I), a preparation method thereof and a pharmaceutical application of the inhibitor. The series compound can be widely applied to treatment of diseases such as diabetes, diabetic retinopathy, diabetic neuropathy, diabetic nephropathy, insulin resistance, hyperglycemia, hyperinsulinemia, elevated level of fatty acid or glycerol, hyperlipemia, obesity, hypertriglyceridemia, X syndrome, diabetic complications or atherosclerosis or hypertension, and can be hopefully developedinto a new-generation SGLTs inhibitor.
Owner:ABBISKO THERAPEUTICS CO LTD

Process for the preparation of SGLT inhibitor compounds

ActiveUS10508128B2Easily available cost effectiveSaccharide with carbocyclic radicalsSugar derivativesArylHalogen
The present invention DISCLOSES a novel process for preparing sodium glucose transporters 2 (SGLT2) inhibitor compounds of Formula IX.Wherein, R is halogen, alkyl or alkoxy group; andAr is aryl group, substituted or unsubstituted monocyclic polycyclic or heterocyclic ring selected from the residues A, B, C or D as given below,
Owner:INDOCO REMEDIES

Methods of using alpha-methylglucoside (AMG) as an indicator for glucose absorption and excretion

Presented here are methods using alpha-methylglucoside (AMG) in vivo as an indicator for glucose absorption from the gastrointestinal (GI) system or glucose excretion in the urine after oral administration of AMG. The methods find use in, for example, but not limited to, determining the effect of a sodium-dependent glucose transporter (SGLT) inhibitor in an animal, comparing the differences in the effects of a first and second SGLT inhibitor in an animal, and diagnosing a disease associated with glucose absorption from the gastrointestinal (GI) system or glucose excretion from the kidney in an animal.
Owner:JANSSEN PHARMA NV

Composition and application and medicine thereof

The invention relates to the technical field of medicines, and particularly discloses a composition, application thereof and a medicine. The composition comprises an SGLT inhibitor and a tyrosine kinase activity inhibitor. The present invention provides a composition containing an SGLT inhibitor and a tyrosine kinase activity inhibitor. Based on the inhibition effect of TKI on tyrosine kinase of receptors such as VEGFR (vascular endothelial growth factor receptor), EGFR (epidermal growth factor receptor), HER2 (human epidermal growth factor receptor 2) and the like, an in-vitro anti-tumor test shows that SGLT inhibitors such as sofogliflozin, SY-009, Licogliflozin and the like can generate a synergistic inhibition effect on tumors when being combined with a tyrosine kinase activity inhibitor; in addition, the curative effect of TKI drugs can be remarkably enhanced, the drug resistance can be reversed, and the compound can be used for cancer treatment and preparation of anti-cancer drugs.
Owner:NEWISH TECH (BEIJING) CO LTD

Preparation method of SGLTs inhibitor and key intermediate thereof

The invention relates to a preparation method of an SGLTs inhibitor and a key intermediate of the SGLTs inhibitor. The SGLTs inhibitor is (1S, 2S, 3S, 4R, 5S)-5-(3-((2, 3-dihydrobenzo [b] [1, 4] dioxin-6-yl)methyl)-4-ethyl phenyl)-1-(hydroxymethyl)-6, 8-dioxabicyclo [3.2.1] octane-2, 3, 4-triol. According to the preparation method, 6-(2-ethyl-5-iodobenzyl)-2, 3-dihydrobenzo [b] [1, 4] dioxin is taken as a raw material, silyl is taken as a protecting group, and six-step reaction is carried out to prepare the product. The preparation method disclosed by the invention is simple to operate, high in yield of each step and stable in process, can adapt to industrial production requirements, solves the problem of drug accessibility, and is beneficial to acceleration of clinical development of the SGLTs inhibitor and drug marketing.
Owner:YOUNGENE THERAPEUTICS CO LTD

Use of alpha-methylglucoside (AMG) as an indicator for glucose absorption and excretion

Presented here are methods using alpha-methylglucoside (AMG) in vivo as an indicator for glucose absorption from the gastrointestinal (GI) system or glucose excretion in the urine after oral administration of AMG. The methods find use in, for example, but not limited to, determining the effect of a sodium-dependent glucose transporter (SGLT) inhibitor in an animal, comparing the differences in the effects of a first and second SGLT inhibitor in an animal, and diagnosing a disease associated with glucose absorption from the gastrointestinal (GI) system or glucose excretion from the kidney in an animal.
Owner:JANSSEN PHARMA NV

Amine solvate of sodium-glucose linked transporter inhibitor, and preparation method and application thereof

ActiveUS20190135848A1Treating and delaying developmentTreating and delaying and attackOrganic active ingredientsSenses disorderD-GlucoseGlucose polymers
Disclosed are an amine solvate of a sodium-glucose linked transporter (SGLT) inhibitor, and a preparation method and application thereof. The SGLT inhibitor is (1S,2S,3S,4R,5S)-5-(3-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)methyl)-4-ethylbenzyl)-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol. Further provided is a crystalline compound of the amine solvate, a pharmaceutical composition comprising the amine solvate, and an application of the amine solvate in preparing an SGLT-inhibiting pharmaceutical product.
Owner:YOUNGENE THERAPEUTICS CO LTD

Amine solvate of sodium-glucose linked transporter inhibitor, and preparation method and application thereof

Disclosed are an amine solvate of a sodium-glucose linked transporter (SGLT) inhibitor, and a preparation method and application thereof. The SGLT inhibitor is (1S,2S,3S,4R,5S)-5-(3-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)methyl)-4-ethylbenzyl)-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol. Further provided is a crystalline compound of the amine solvate, a pharmaceutical composition comprising the amine solvate, and an application of the amine solvate in preparing an SGLT-inhibiting pharmaceutical product.
Owner:YOUNGENE THERAPEUTICS CO LTD

C- aryl glycosid derivatives, pharmaceutical composition, preparation process and uses thereof

This invention relates to a kind of C-aryl glycoside derivatives, its pharmaceutical compositions, preparation methods, and uses thereof. The preparation method comprises: method 1: in a solvent, deprotecting the acetyl protecting groups of compound 1-f in the presence of a base; method 2: 1) compound 2-g reacts withvia Mitsunobu reaction; 2) deprotecting the acetyl protecting groups of compound 2-f obtained from step 1; method 3: 1) compound 2-g reacts withvia nucleophilic substitution reaction; 2) deprotecting the acetyl protecting groups of compound 3-f obtained from step 1. The pharmaceutical composition comprises a kind of C-aryl glycoside derivatives; it's pharmaceutically acceptable salts and / or prodrugs thereof and excipient thereof. This invention further relates to a kind of C-aryl glycoside derivatives, it's pharmaceutically acceptable salts or pharmaceutical compositions thereof for the use in preparation of a SGLT inhibitor. The C-aryl glycoside derivatives of this invention provides a new direction for the study of SGLT inhibitors.
Owner:SHANGHAI DE NOVO PHARMA

Method for producing intermediate useful for synethesis of SGLT inhibitor

The present invention relates to a method for producing an intermediate useful for the synthesis of a diphenylmethane derivative that can be used as a SGLT inhibitor. A method for synthesizing a compound of formula 7 according to the present invention has solved the problem of an existing synthesis process which requires an additional process due to the synthesis of Grignard reagent and the management of a related substance. In addition, the process can be simplified by minimizing the formation of the related substance and eliminating the need for reprocessing of reaction products, thereby becoming capable of maximizing a yield of a diphenylmethane derivative.
Owner:DAEWOONG PHARM CO LTD
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