US 8,986,652 B2 · Method of preparing [123I]iodooctyl fenbufen amide and application thereof

Abstract

The present invention provides a method of preparing [123I]Iodooctyl fenbufen amide with a radiochemical yield of 15%, a specific activity of 37 GBq/μmol and radiochemical purity of 95%. The present invention further provides a method of applying [123I]Iodooctyl fenbufen amide as tracer of single photon emission computer tomography (SPECT) to estimate the distribution of cyclooxygenase. By the binding characteristics of the iodine isotope-labeled compounds and the positive correlation of inflammation to tumor lesion, the present invention can estimate the tumor development and metastasis.

Claims3

Dependent claims

A method of detecting an early inflammatory lesion of a tumor comprising:

administering a compound of formula 1 as a tracer of an image-forming system, and
detecting the binding affinity of the compound of formula 1 with cyclooxygenase to produce a signal, wherein the cyclooxygenase is cyclooxygenase-1 (COX-1) or cyclooxygenase-2 (COX-2), wherein the signal is a hot spot displayed by radioactive accumulation and the tumor is a liver tumor.

Dependencies are inferred from the claim text.

Facts

Application

13/757,018Filed 1 Feb 2013

Priority

TW 101134033 A17 Sep 2012

Published

US 2014/0079633 A120 Mar 2014

Granted

24 Mar 2015

Term ends

Not estimatedThe source records don’t support an estimate.

Classification7 codes

A61K 51/04
Characterised by the carrier , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus: organic compounds
C07B 59/001
Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se: acyclic or carbocyclic compounds
C07C 231/02
Preparation of carboxylic acid amides: from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07C 231/12
Preparation of carboxylic acid amides: by reactions not involving the formation of carboxamide groups

Method of preparing [123I]iodooctyl fenbufen amide and application thereof

Life of this patent

Method of preparing [123I]iodooctyl fenbufen amide and application thereof

Life of this patent

Abstract

Claims3