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FACTOR XIIa INHIBITORS

A kind of atomic and selected technology, applied in the field of producing the compound of the present invention, can solve the problems such as not suitable for long-term anticoagulation

Pending Publication Date: 2021-01-08
UNIV OF LEEDS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, if the infestin-4 or antibody approach is successful, they need to be administered intravenously, making them less suitable for long-term anticoagulation

Method used

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  • FACTOR XIIa INHIBITORS
  • FACTOR XIIa INHIBITORS
  • FACTOR XIIa INHIBITORS

Examples

Experimental program
Comparison scheme
Effect test

Embodiment and

[0457] Example and Synthesis

[0458] 1H-NMR: Spectra were acquired on a Bruker DRX 400MHz or Jeol ECS 400MHz spectrometer. Spectra were measured at 294K (unless otherwise stated) and chemical shifts (δ-values) are reported in parts per million (ppm) with reference to TMS (0.0 ppm), DMSO-d6 (2.50 ppm), CDCl3 (7.26 ppm). Coupling constants (J) in Hertz (Hz) Spectral splitting patterns specified as singlet (s), doublet (d), triplet (t), quartet (q), multiplet or more overlapping signals (m), broad signal (br); solvents are given in parentheses.

[0459] Acronym

[0460] The following abbreviations are used in the examples and in the rest of the specification.

[0461] ABCN: azobicyclohexanecarbonitrile; Boc: tert-butoxycarbonyl; Cbz: carbenzyloxy; DavePhos: 2-dicyclohexylphosphino-2′-(N,N-dimethylamino)biphenyl; dba: Tris(dibenzylideneacetone); DBU: 1,8-diazabicyclo[5.4.0]undec-7-ene; DCE: 1,2-dichloroethane; DCM: dichloromethane; DIAD: diisopropyl azodicarboxylate; dioxane...

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Abstract

This invention relates to compounds of formula (I). The compounds of formula (I) are modulators of Factor XII, specifically Factor XIIa. The compounds are inhibitors of Factor XIIa and may be useful as anticoagulants. The compounds of formula (I) may be used in methods of treatment (or prevention) of blood disorders related to bleeding or coagulation.

Description

technical field [0001] The present invention relates to compounds and methods of treatment (or prevention) using the compounds. The invention also relates to processes and methods for producing the compounds of the invention. Compounds of the invention are modulators of Factor XII (eg, Factor XIIa). In particular, the compounds are inhibitors of Factor XIIa and are useful as anticoagulants. Background technique [0002] Cardiovascular disease is the leading cause of death in developed countries, affecting millions of people worldwide each year. The disease is usually caused by atherosclerosis of the arterial wall, which develops over many years and is characterized by endothelial inflammation, subendothelial lipid deposition, macrophage infiltration, and plaque development. During the acute phase of the disease, atherosclerotic plaques become unstable and rupture, triggering thrombus formation. The development of thrombi (blood clots), which block blood vessels and there...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/12C07D401/14C07D401/12C07D403/14C07D405/12C07D241/04C07D471/04C07D211/14A61P7/02A61K31/496
CPCC07D403/12C07D401/14C07D401/12C07D403/14C07D405/12C07D241/04C07D471/04C07D211/14A61P7/02A61K31/496A61K31/506A61K31/445C07D413/12C07D211/60
Inventor 海伦·菲莉帕普理查德·福斯特科林·菲什威克夏洛特·雷维尔伊恩·尤尔罗格·泰勒阿兰·内勒菲利普·斯潘塞·法伦斯图尔特·克罗斯比安娜·霍普金斯马克·理查德·斯图尔特纳塔莉·路易丝·温菲尔德
Owner UNIV OF LEEDS
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