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

Medicine for treating pancreatitis, and preparation method thereof

A pharmacy and compound technology, applied in the field of medicines for the treatment of pancreatitis and their preparation, can solve problems such as being unable to meet actual needs and the like

Inactive Publication Date: 2018-07-20
MUDANJIANG MEDICAL UNIV
View PDF0 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the products currently on the market cannot meet the actual needs, so it is very necessary to develop a new drug product that can be used for the treatment of pancreatitis

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
  • Medicine for treating pancreatitis, and preparation method thereof
  • Medicine for treating pancreatitis, and preparation method thereof
  • Medicine for treating pancreatitis, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0085] Embodiment 1: synthetic compound I-1

[0086] 5-((2-methoxypyridin-4-yl)methyl)-2-(thien-3-yl)-6,7-dihydro-5H-pyrimidine[4,5-b][1,4 ] Zinc

[0087]

[0088] Step 1. Synthesis of 2-chloro-6,7-dihydro-5H-pyrimidine[4,5-b][1,4] Zinc

[0089]Add 60.0 mmol of 1,2-dibromoethane, 60.0 mmol of sodium hydroxide, and 0.75 g of benzyltriethylammonium chloride to a solution of 15.0 mmol of 5-amino-2-chloropyrimidin-4-ol in 200 mL of dichloromethane , and stirred at room temperature for 20 hours. After the reaction, the reaction mixture was poured into 300 mL of water, then extracted with ethyl acetate, the organic layer was washed with brine and water, and dried with anhydrous sodium sulfate to obtain 2-chloro-6,7-dihydro-5H-pyrimidine[ 4,5-b][1,4] 2.0 g of oxazine, yield 78.2%. LC-MS: m / z172.0(M+1) + .

[0090] Step 2. Synthesis of 2-(thiophen-3-yl)-6,7-dihydro-5H-pyrimidine[4,5-b][1,4] Zinc

[0091] Under nitrogen protection, 2-chloro-6,7-dihydro-5H-pyrimidine[4...

Embodiment 2

[0096] Embodiment 2: synthetic compound 1-2

[0097] 4-(3-(4-Methyl-2-(thiophen-3-yl)-6,7-dihydro-5H-pyrimidine[4,5-b][1,4] Azin-5-yl)propyl)-2-cyanopyridine

[0098]

[0099] According to the method of Example 1, the difference is that 4-methyl-5-amino-2-chloropyrimidin-4-ol is used instead of 5-amino-2-chloropyrimidin-4-ol, and 4-(3-bromopropane Base)-2-cyanopyridine in place of 4-(bromomethyl)-2-methoxypyridine to give 4-(3-(4-methyl-2-(thiophen-3-yl)-6,7- Dihydro-5H-pyrimidine[4,5-b][1,4] Oxyzin-5-yl)propyl)-2-cyanopyridine, the total yield of three steps is 51.3%.

[0100] LC-MS: m / z 378.1 (M+1) + .

[0101] Proton spectrum (400MHz, DMSO) δ8.84(d,1H),8.24(s,1H),8.01(d,1H),7.92(s,1H),7.78(d,1H),7.04(d,1H) , 4.25(t,2H), 3.55(t,2H), 3.47(t,2H), 2.65(t,2H), 2.31(s,3H), 2.02(m,2H).

Embodiment 3

[0102] Embodiment 3: synthetic compound 1-3

[0103] 2-(5-phenylfuryl-3-yl)-5-(3-(pyridin-4-yl)propyl)-6,7-dihydro-5H-pyrimidine[4,5-b][1 ,4] Zinc

[0104]

[0105] According to the method of Example 1, the difference is that 5-phenylfuran-3-boronic acid is used instead of thiophene-3-boronic acid, and 4-(3-bromopropyl)-pyridine is used instead of 4-(bromomethyl)-2- Methoxypyridine to give 2-(5-phenylfuryl-3-yl)-5-(3-(pyridin-4-yl)propyl)-6,7-dihydro-5H-pyrimidin[4, 5-b][1,4] oxazine, the three-step total yield is 49.1%.

[0106] LC-MS: m / z 399.1 (M+1) + .

[0107] Hydrogen spectrum (400MHz, DMSO) δ8.65(d,2H),8.24(s,1H),8.14(d,2H),7.61(t,2H),7.51(s,1H),7.40(t,1H) , 7.24(d,2H), 6.31(s,1H), 4.26(t,2H), 3.54(t,2H), 3.48(t,2H), 2.65(t,2H), 2.02(m,2H).

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 new pyrimido-oxazine compound. With the compound, the increment of amylase-lipase activity of sera of rats with acute pancreatitis can be remarkably inhibited, and the watercontent of pancreatic tissues of the rats with acute pancreatitis can be remarkably reduced, so that the compound has a favorable treatment effect on acute pancreatitis. In addition, compared with anexisting medicine gabexate, the treatment effect is more remarkable.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, specifically, the invention relates to a medicine for treating pancreatitis and a preparation method thereof, and the invention also relates to the use of the medicine. Background technique [0002] Pancreatitis is an inflammation of the pancreas and can be divided into acute pancreatitis and chronic pancreatitis. Pancreatic juice contains digestive enzymes such as amylase (to break down carbohydrates), trypsin (to break down proteins), and lipase (to break down fats). Pancreatitis refers to a state in which pancreatic juice cannot flow smoothly due to excessive intake of alcohol or gallstones, and the pancreas is self-digested by the above-mentioned enzymes. It can be broadly classified into a mild type in which interstitial edema and peripancreatic fat necrosis are seen, and a severe type in which extensive necrosis of peripancreatic and intrapancreatic fat, pancreatic parenchymal necrosis, ...

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): C07D498/04A61K31/5383A61P1/18
CPCC07D498/04
Inventor 宋先旭吴妍李宏海杨文萍郝琳娜刘爽姜宏春宋先东朱敏王梅
Owner MUDANJIANG MEDICAL UNIV
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