Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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

A technology of pharmacy, compound, applied in the field of drug synthesis

Inactive Publication Date: 2019-03-12
ABBISKO THERAPEUTICS CO LTD
View PDF3 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently, no SGLT-1 / SGLT-2 protein inhibitors are on the market, and the fastest-developing one is Sanofi's Sotagliflozin, which has reached the third phase of clinical trials. The compound patent is WO2008042688A2 (Apr 10, 2008)
In addition, in 2015, Korea HANMIPHARM.CO., LTD disclosed a compound patent WO2015174695A1 (Nov 19, 2015), and Jiangsu Hansoh Pharmaceutical Co., Ltd. disclosed a compound patent WO2015032272A1 (Mar 12, 2015). of protein inhibitors have not entered the clinical stage

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • SGLTs (sodium-dependent glucose transporters 2) inhibitor, preparation method thereof and pharmaceutical application of inhibitor
  • SGLTs (sodium-dependent glucose transporters 2) inhibitor, preparation method thereof and pharmaceutical application of inhibitor
  • SGLTs (sodium-dependent glucose transporters 2) inhibitor, preparation method thereof and pharmaceutical application of inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0110] Example 1 (1S, 2S, 3S, 4R, 5S)-1-(hydroxymethyl)-5-(7-(4-methoxybenzyl)-4-methyl-2,3-dihydro-1H Preparation of -inden-5-yl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol

[0111]

[0112] Step 1: Preparation of (6-bromo-7-methyl-2,3-dihydro-1H-inden-4-yl)(4-methoxyphenyl)methanone

[0113]

[0114] N 2 Under protection, 6-bromo-7-methyl-2,3-dihydro-1H-indene-4-carboxylic acid (6.9 g, 27.1 mmol) was dissolved in DCM (30 mL), the solution was cooled to 0 °C, then Will (COCl) 2 (3.5 mL, 41.4 mmol) in DMF (0.10 mL) was slowly added dropwise. The reaction solution was stirred overnight at room temperature. After the reaction solution was concentrated, the oil pump was pumped dry for half an hour. The resulting product was dissolved in DCM (50 mL), then cooled to 0 °C, anisole (3.5 g, 32.4 mmol) and AlCl were added 3 (4.5 g, 33.8 mmol). After the reaction solution was warmed to room temperature, it was stirred at room temperature for 4 hours. The reaction solution w...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

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.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and in particular relates to a SGLTs protein inhibitor, its preparation method and pharmaceutical application. technical background [0002] Diabetes is caused by genetic factors, immune dysfunction, microbial infection and its toxins, free radical toxins, mental factors and other pathogenic factors acting on the body to cause hypofunction of pancreatic islets and insulin resistance (Insulin Resistance, IR), etc. A series of metabolic disorder syndromes such as sugar, protein, fat, water and electrolytes, clinically characterized by hyperglycemia, typical cases may show polyuria, polydipsia, polyphagia, weight loss, etc., that is, "three more and one less". "symptom. Abnormal blood sugar levels can lead to serious long-term complications, including cardiovascular disease, chronic renal failure, retinal damage, nerve damage, microvascular damage, and obesity, among others. In the early stage of dia...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/01C07H1/00C07D493/08A61P3/10A61P27/02A61P25/00A61P13/12A61P5/50A61P9/12A61P3/06A61P3/04A61P9/10A61K31/7048A61K31/35A61K31/36A61K31/381A61K31/357A61K31/538A61K31/404
CPCC07H19/01A61P3/04A61P3/06A61P3/10A61P5/50A61P9/10A61P9/12A61P13/12A61P25/00A61P27/02C07D493/08C07H1/00
Inventor 赵保卫周夏君陈椎
Owner ABBISKO THERAPEUTICS CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com