Title:
BASE ACETAMIDE GLYCERIN ETHER MOLECULE, CHEMICAL SYNTHESIS METHOD THEREFOR, AND APPLICATIONS THEREOF IN FIELD OF GENE THERAPY
Document Type and Number:
WIPO Patent Application WO/2018/085962
Kind Code:
A1
Abstract:
Disclosed in the present invention are a base acetamide glycerin ether molecule, a chemical synthesis method therefor, and applications thereof in the field of gene delivery. The molecule has an amphiphilic structure represented by formula (I), that is, a base-1-acetic acid is used as a hydrophilic head, and an amide bond is connected to glycerol aliphatic ether serving as a hydrophobic tail, so as to form an amphiphilic molecule. The Base group is common nature purine and a pyrimidine base, and the R group is a saturated or unsaturated aliphatic carbon chain. The compound can be prepared by means of an activated derivative of the base-1-acetic acid and 2, 3-dialkoxyl-1-propylamine, prices of the raw materials are low, and the synthesis method is simple. The compound can be used to prepare liposome and other supramolecular structures, and does not have obvious cytotoxicity. The base of the head of the compound can be combined with nucleic acid, and can carry the nucleic acid to enter a cell membrane. Accordingly, the compound has the potential of becoming a new non-cationic gene vector, and can be widely used in the field of gene therapy.
Inventors:
YANG ZHENJUN (CN)
WANG CHAO (CN)
SUN JING (CN)
WANG CHAO (CN)
SUN JING (CN)
Application Number:
PCT/CN2016/000712
Publication Date:
May 17, 2018
Filing Date:
December 27, 2016
Export Citation:
Assignee:
UNIV BEIJING (CN)
International Classes:
C07D473/34; A61K9/127; A61K48/00; C07D239/47; C07D239/54; C07D473/18; C12N15/88
Foreign References:
| CN103242243A | 2013-08-14 | |||
| CN103232510A | 2013-08-07 | |||
| CN102925487A | 2013-02-13 |
Other References:
SKWARCZYNSKI, M. ET AL.: "Thymine, adenine and lipoamino acid based gene delivery systems", CHEM. COMMUN, vol. 46, 5 March 2010 (2010-03-05), pages 3140 - 3142, XP055503104
CHEM. REV., vol. 109, 2009, pages 259 - 302
BIOMATERIALS, vol. 29, 2008, pages 3477 - 3496
MILANI ET AL., J. AM. CHEM. SOC., vol. 129, 2007, pages 11664 - 11665
TOTH ET AL., CHEM. COMMUN., vol. 46, 2010, pages 3140 - 3142
CHABAUD ET AL., BIOCONJUGATE CHEM., vol. 17, 2006, pages 466 - 472
MOREAU ET AL., J. AM. CHEM. SOC., vol. 126, 2004, pages 7533 - 7539
See also references of EP 3539964A4
CHEM. REV., vol. 109, 2009, pages 259 - 302
BIOMATERIALS, vol. 29, 2008, pages 3477 - 3496
MILANI ET AL., J. AM. CHEM. SOC., vol. 129, 2007, pages 11664 - 11665
TOTH ET AL., CHEM. COMMUN., vol. 46, 2010, pages 3140 - 3142
CHABAUD ET AL., BIOCONJUGATE CHEM., vol. 17, 2006, pages 466 - 472
MOREAU ET AL., J. AM. CHEM. SOC., vol. 126, 2004, pages 7533 - 7539
See also references of EP 3539964A4
Attorney, Agent or Firm:
KELONG INTERNATIONAL INTELLECTUAL PROPERTY AGENCY LTD. (CN)
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