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Chirally pure isomers of itraconazole and inhibitors of lanosterol 14A-demethylase for use as angiogenesis inhibitors

An angiogenesis and itraconazole technology is applied in the field of a chiral pure isomer of itraconazole as an angiogenesis inhibitor and an inhibitor of lanosterol 14A-demethylase, and can solve toxic, Difficult to use, unstable, etc.

Inactive Publication Date: 2010-05-19
THE JOHN HOPKINS UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In addition, many substances that seem promising in vitro have been shown to be relatively ineffective when used in vivo
Likewise, a variety of these substances have been found to be unstable, toxic or difficult to use

Method used

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  • Chirally pure isomers of itraconazole and inhibitors of lanosterol 14A-demethylase for use as angiogenesis inhibitors
  • Chirally pure isomers of itraconazole and inhibitors of lanosterol 14A-demethylase for use as angiogenesis inhibitors
  • Chirally pure isomers of itraconazole and inhibitors of lanosterol 14A-demethylase for use as angiogenesis inhibitors

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Experimental program
Comparison scheme
Effect test

Embodiment

[0211] 1. Synthesis of stereoisomers of itraconazole and azalanstat

[0212] General Experimental

[0213] Thin-layer chromatography was performed on Merck precoated silica gel 60F-254 plate and visualized with 254 nm (nanometer) ultraviolet light (UV light), or with iodine Or ammonium molybdate cerium stain (ceric ammonium molybdate stain) to stain. Silica gel (200-400 mesh, Merck) was used in flash chromatography. Reagents were purchased from Aldrich, Acros or Lancaster. Melting points were recorded on a Mel-Temp II instrument without calibration. Varian Unity-400 (400MHz) from the Department of Pharmacology and Molecular Sciences at Johns Hopkins University 1 H, 100MHz 13 C) The machine collects the NMR data. 1 HNMR spectra were obtained in deuterochloroform (CDCl 3 ) and tetramethylsilane (TMS, δ=0.00, 1 H) or chloroform (δ=7.27, 1 H), or, in DMSO-d 6 With tetramethylsilane (TMS, δ=0.00, 1 H) as an internal reference. 13 CNMR spectra are proton decoupled and ar...

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Abstract

Described herein are methods of inhibiting angiogenesis, and treating or preventing a disease or disorder (or symptoms thereof) associated with angiogenesis, wherein an anti-angiogenesis compound is administered to a subject.

Description

[0001] Related applications [0002] This application claims priority to US Provisional Application Serial No. 60 / 922,059, filed April 5, 2007. The entire content of the provisional application is incorporated herein by reference. Background technique [0003] Angiogenesis can be defined as the development of blood supply to specific areas of tissue. The development of the blood supply may be part of normal embryonic development, represent revascularization of a wound bed, or involve stimulation of blood vessel growth from inflammatory or malignant cells. Sometimes, angiogenesis is defined as the proliferation of new capillaries to existing blood vessels. New growth of soft tissue requires new vascularization, and the concept of angiogenesis is a key element of tissue growth, and especially a key point of entry for pathological tissue growth. [0004] Angiogenesis is a fundamental process required for embryonic development, subsequent growth, and tissue repair. Angiogenesi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/497A61K31/415
CPCC12Q1/25A61K9/0024G01N2500/00A61K31/415A61K31/497A61K9/0019A61P27/02A61P35/00Y02A50/30
Inventor J·刘C·R·张J·徐J·陆S·巴特
Owner THE JOHN HOPKINS UNIV SCHOOL OF MEDICINE
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