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

A class of compounds containing alkoxyphenyl and diene fluoroadamantane structures and uses thereof

A compound, alkyl technology, applied in the field of drugs related to thrombosis, can solve problems such as high bleeding risk

Active Publication Date: 2016-03-16
邳州市润宏实业有限公司
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage of these drugs is the greater risk of bleeding

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
  • A class of compounds containing alkoxyphenyl and diene fluoroadamantane structures and uses thereof
  • A class of compounds containing alkoxyphenyl and diene fluoroadamantane structures and uses thereof
  • A class of compounds containing alkoxyphenyl and diene fluoroadamantane structures and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027]

[0028] 2.46g (10mmol) compound II and 2.62g (10mmol) PPh 3 Dissolve in 20 mL of dry THF and reflux overnight under nitrogen protection. After the reaction mixture was cooled to room temperature, a white cloudy solution was obtained. Cooled to -78°C under nitrogen protection, slowly added 6.25mL (10mmol, 1.6M) n-BuLi n-hexane solution dropwise. After the dropwise addition was completed, stirring was continued for one hour, and a solution prepared by dissolving compound 1.28 g (10 mmol) III in 2 mL THF was added dropwise. After the dropwise addition was complete, the reaction mixture was slowly warmed to room temperature and then refluxed for 1 hour. The reaction mixture was poured into ice water, stirred, extracted with 50 mL×3 dichloromethane, the combined extracts were washed with brine, and dried over anhydrous sodium sulfate. The desiccant was removed by suction filtration, 0.50 g of iodine was added to the filtrate, and stirred overnight at room temperature....

Embodiment 2-6

[0032] Referring to the method of Example 1, the following compounds with general formula I were synthesized.

[0033]

[0034]

Embodiment 7

[0035] The preparation of embodiment 7 reference compound D1

[0036] In order to fully illustrate the beneficial effects of the compounds of the present invention, the applicant recorded the following compound D1 (unpublished) found during the experiment as a pharmacodynamic reference compound.

[0037]

[0038] The synthesis method is as follows:

[0039]

[0040] 2.47g (10mmol) compound II and 2.62g (10mmol) PPh 3 Dissolve in 20 mL of dry THF and reflux overnight under nitrogen protection. After the reaction mixture was cooled to room temperature, a white cloudy solution was obtained. Cooled to -78°C under nitrogen protection, slowly added 6.25mL (10mmol, 1.6M) n-BuLi n-hexane solution dropwise. After the dropwise addition was completed, stirring was continued for one hour, and a solution prepared by dissolving compound 1.28 g (10 mmol) III in 2 mL THF was added dropwise. After the dropwise addition was complete, the reaction mixture was slowly warmed to room temp...

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 the field of medicine related to the thrombotic diseases, in particular to a class of PAR-1 antagonist containing an alcoxyl phenyl group and diene fluoro adamantane structure and a preparation method and application of the class of PAR-1 antagonist containing the alcoxyl phenyl group and diene fluoro adamantane structure. Please see the formula in the specification, wherein the R is selected from the H alkyl group or C1-C5 alkyl group and the C3-C8 naphthenic base.

Description

technical field [0001] The invention relates to the field of drugs related to thrombosis diseases. Specifically, the present invention relates to a class of PAR-1 antagonists containing alkoxyphenyl and dienyl fluoroadamantane structures that have a therapeutic effect on thrombotic diseases and their preparation methods, pharmaceutical compositions containing them and in the treatment of Use in thrombotic diseases. Background technique [0002] Protease Activated Acceptor-1 (PAR-1) is a new target of anti-platelet antithrombotic drugs discovered recently. Protease-activated receptor 1 is also called thrombin receptor. After thrombin is activated by the coagulation chain, it acts on platelets through PAR-1 receptors to activate platelets, causing platelet aggregation and causing thrombus and coagulation. The thrombus induced by PAR-1 is rich in platelet components, which is the main cause of arterial thrombus. PAR-1 antagonists can block thrombin from activating platelets,...

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 Patents(China)
IPC IPC(8): C07D207/335A61K31/402A61P7/02A61P9/10
CPCC07D207/335
Inventor 蔡子洋
Owner 邳州市润宏实业有限公司
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