Check patentability & draft patents in minutes with Patsnap Eureka AI!

FXa inhibitors containing bisamide structure as well as preparation method and application thereof

A technology of dicyclohexylcarbodiimide and compounds, applied in the field of pharmaceuticals and FXa inhibitors containing bisamide structure

Active Publication Date: 2015-06-03
栾勇
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

DVT also puts patients at high risk of developing pulmonary thromboembolism

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
  • FXa inhibitors containing bisamide structure as well as preparation method and application thereof
  • FXa inhibitors containing bisamide structure as well as preparation method and application thereof
  • FXa inhibitors containing bisamide structure as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] The synthesis of embodiment 1 compound I-1

[0022]

[0023] A. Synthesis of Compound III

[0024] Compound II (1.26g, 10mmol) and triethylamine (3.04g, 30mmol) were dissolved in 10mL of dry DMF, stirred under cooling in an ice-water bath, slowly added dropwise from triphenylchloromethane (TrCl; 3.07g, 11mmol) and 10 mL of dry DMF solution. After the addition was complete, the resulting reaction mixture was stirred at room temperature for 3 hours, and TLC showed that the reaction was complete. The reaction mixture was poured into 120 mL of ice water, CH 2 Cl 2 (50mL×3) was extracted, and the extract phases were combined, washed with brine, and dried over anhydrous sodium sulfate. The desiccant was removed by suction filtration, the filtrate was evaporated to dryness on a rotary evaporator, and the obtained residue was purified by column chromatography to obtain compound III, a white solid, ESI-MS, m / z=369 ([M+H] + ).

[0025] B. Synthesis of Compound V-1

[0...

Embodiment 2-8

[0032] Referring to the method of Example 1, the compounds listed in the following table were synthesized.

[0033]

Embodiment 7

[0034] The synthesis of embodiment 7 reference compound D-1

[0035] Compound D-1 is also a compound designed by the inventors during the research process (unpublished as of the filing date).

[0036]

[0037] A. Synthesis of Compound III

[0038] Compound II (1.26g, 10mmol) and triethylamine (3.04g, 30mmol) were dissolved in 10mL of dry DMF, stirred under cooling in an ice-water bath, slowly added dropwise from triphenylchloromethane (TrCl; 3.07g, 11mmol) and 10 mL of dry DMF solution. After the addition was complete, the resulting reaction mixture was stirred at room temperature for 3 hours, and TLC showed that the reaction was complete. The reaction mixture was poured into 120 mL of ice water, CH 2 Cl 2 (50mL×3) was extracted, and the extract phases were combined, washed with brine, and dried over anhydrous sodium sulfate. The desiccant was removed by suction filtration, the filtrate was evaporated to dryness on a rotary evaporator, and the obtained residue was pu...

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 medicines related to venous thrombotic diseases and in particular relates to FXa inhibitors containing a bisamide structure, a preparation method of the FXa inhibitors and an application of the FXa inhibitors to preparation of medicines related to venous thrombotic diseases. The FXa inhibitors have a structure shown in a general formula I in the specification, wherein in the general formula I, R is selected from C1-C3 alkyl and C3-C6 cycloalkyl.

Description

technical field [0001] The invention relates to the field of drugs for the treatment of venous thrombosis diseases. More specifically, the present invention relates to a class of FXa inhibitors containing a bisamide structure that has a therapeutic effect on venous thrombosis, its preparation method, and its use in pharmacy. Background technique [0002] Deterioration of coagulation ability is unstable angina, cerebral infarction, cerebral embolism, myocardial infarction, pulmonary infarction, pulmonary embolism, thromboangiitis obliterans, deep vein thrombosis, disseminated intravascular coagulation syndrome, after valve replacement An important factor in thrombosis during revascularization, reocclusion after revascularization, or thrombosis during cardiopulmonary bypass. In the arterial system, abnormal thrombosis is mainly related to coronary arteries, cerebrovascular and peripheral blood vessels, and diseases related to thrombotic closure of these vessels mainly include...

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
IPC IPC(8): C07D471/04A61P7/02
CPCC07D471/04
Inventor 蔡子洋
Owner 栾勇
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

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

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com