Title:
The beta substitution gamma amino acid and similar object as a chemotherapeutic drug
Document Type and Number:
Japanese Patent JP6271766
Kind Code:
B2
Abstract:
β-Substituted γ-amino acids, β-substituted γ-amino acid derivatives, and β-substituted γ-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates, capable of passing through the blood-brain barrier, and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an increased efficacy on a variety of tumor types.
Inventors:
Jean De Leit, Bernd
Fisher, Wolf-Nicholas
Coller, Kelly Jay.
Fisher, Wolf-Nicholas
Coller, Kelly Jay.
Application Number:
JP2016567476A
Publication Date:
January 31, 2018
Filing Date:
February 03, 2015
Export Citation:
Assignee:
Quadriga Biosciences, Inc.
International Classes:
C07C229/42; A61K31/197; A61K31/255; A61K31/27; A61K31/41; A61K31/662; A61P35/00; C07C237/30; C07C239/20; C07C271/46; C07C291/04; C07C309/66; C07D257/04; C07F9/30
Foreign References:
| WO2013033569A1 |
Attorney, Agent or Firm:
Hidesaku Yamamoto
Natsuki Morishita
Takatoshi Iida
Daisuke Ishikawa
Kensaku Yamamoto
Natsuki Morishita
Takatoshi Iida
Daisuke Ishikawa
Kensaku Yamamoto