Title:
腫瘍画像化のためのアミノ酸アナログ
Document Type and Number:
Japanese Patent JP5341136
Kind Code:
B2
Abstract:
The invention provides novel amino acid compounds of use in detecting and evaluating brain and body tumors. These compounds combine the advantageous properties of 1-amino-cycloalkyl-1-carboxylic acids, namely, their rapid uptake and prolonged retention in tumors with the properties of halogen substituents, including certain useful halogen isotopes including fluorine-18, iodine-123, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77 and bromine-82. In one aspect, the invention features amino acid compounds that have a high specificity for target sites when administered to a subject in vivo. Preferred amino acid compounds show a target to non-target ratio of at least 5:1, are stable in vivo and substantially localized to target within 1 hour after administration. An especially preferred amino acid compound is [18F]-1-amino-3-fluorocyclobutane-1-carboxylic acid (FACBC). In another aspect, the invention features pharmaceutical compositions comprised of an alpha -amino acid moiety attached to either a four, five, or a six member carbon-chain ring. In addition, the invention features analogs of alpha -aminoisobutyric acid.
Inventors:
Mark M. Goodman
Timothy Shoup
Timothy Shoup
Application Number:
JP2011121052A
Publication Date:
November 13, 2013
Filing Date:
May 30, 2011
Export Citation:
Assignee:
Emory University
International Classes:
A61K51/00; C07C229/48; A61K51/04; C07B59/00; C07C45/30; C07C45/59; C07C229/20; C07C229/30; C07F13/00; C07F17/00
Other References:
Biophysical Journal,1983年,Vol.43, No.3,p.261-267
Attorney, Agent or Firm:
Hidesaku Yamamoto
Takaaki Yasumura
Natsuki Morishita
Takaaki Yasumura
Natsuki Morishita