Title:
CYCLIC GD (III) COMPLEX, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/173618
Kind Code:
A1
Abstract:
The present invention provides a cyclic Gd(III) complex, which has a chemical structure as shown in formula I, wherein a ring structure of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid, namely DOTA, is used as a parent ring, lipophilic groups R 'and R'' in formula I are respectively introduced to an α-position and a benzene ring structure of phenylacetic acid, and a chiral group R in formula I is introduced to a macrocyclic position of the DOTA. Using the chiral group R to increase the rigidity of the macrocyclic structure improves the stability of the complex, and the lipophilic groups R 'and R'' can bind to organic anion transport polypeptides in hepatocytes, so that the distribution of the cyclic Gd (III) complex in the liver and gallbladder when used as a contrast agent is greatly improved, that is, the targeting ability is good.
Inventors:
DAI LIXIONG (CN)
XU WEIYUAN (CN)
YE FANGFU (CN)
XU WEIYUAN (CN)
YE FANGFU (CN)
Application Number:
PCT/CN2022/100671
Publication Date:
September 21, 2023
Filing Date:
June 23, 2022
Export Citation:
Assignee:
WENZHOU INSTITUTE UNIV OF CHINESE ACADEMY OF SCIENCES (CN)
International Classes:
C07D257/02; A61K49/10
Domestic Patent References:
| WO2005065724A1 | 2005-07-21 |
Foreign References:
| CN114560821A | 2022-05-31 | |||
| CN101845112A | 2010-09-29 | |||
| CN109963839A | 2019-07-02 | |||
| CN114181164A | 2022-03-15 | |||
| US20100322855A1 | 2010-12-23 |
Other References:
AIME SILVIO, BOTTA MAURO, ERMONDI GIUSEPPE, TERRENO ENZO, ANELLI PIER LUCIO, FEDELI FRANCO, UGGERI FULVIO: "Relaxometric, Structural, and Dynamic NMR Studies of DOTA-like Ln(III) Complexes (Ln = La, Gd, Ho, Yb) Containing a p -Nitrophenyl Substituent", INORGANIC CHEMISTRY, AMERICAN CHEMICAL SOCIETY, EASTON , US, vol. 35, no. 10, 1 January 1996 (1996-01-01), Easton , US , pages 2726 - 2736, XP093092833, ISSN: 0020-1669, DOI: 10.1021/ic950981u
DIOURY FABIENNE, DUPRAT ARTHUR, DREYFUS GÉRARD, FERROUD CLOTILDE, COSSY JANINE: "QSPR Prediction of the Stability Constants of Gadolinium(III) Complexes for Magnetic Resonance Imaging", JOURNAL OF CHEMICAL INFORMATION AND MODELING, AMERICAN CHEMICAL SOCIETY , WASHINGTON DC, US, vol. 54, no. 10, 27 October 2014 (2014-10-27), US , pages 2718 - 2731, XP093092834, ISSN: 1549-9596, DOI: 10.1021/ci500346w
DIOURY FABIENNE, DUPRAT ARTHUR, DREYFUS GÉRARD, FERROUD CLOTILDE, COSSY JANINE: "QSPR Prediction of the Stability Constants of Gadolinium(III) Complexes for Magnetic Resonance Imaging", JOURNAL OF CHEMICAL INFORMATION AND MODELING, AMERICAN CHEMICAL SOCIETY , WASHINGTON DC, US, vol. 54, no. 10, 27 October 2014 (2014-10-27), US , pages 2718 - 2731, XP093092834, ISSN: 1549-9596, DOI: 10.1021/ci500346w
Attorney, Agent or Firm:
BEIJING GAOWO LAW FIRM (CN)
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