Imidazole compound and liposome containing same

Patent metadata

Field	Value
Publication number	US-9795566-B2
Application number	US-201715406050-A
Country	US
Kind code	B2
Filing date	Jan 13, 2017
Priority date	Jul 17, 2014
Publication date	Oct 24, 2017
Grant date	Oct 24, 2017

Abstract

Provided are a novel imidazole compound which has a high stability of the compound itself; and a novel imidazole compound which is useful as a membrane-constituting lipid of liposomes. Disclosed are a compound represented by the following General Formula (1), and a liposome containing the same compound.

In the formula, Z is an imidazolyl group which may be substituted, L 1 is an alkylene group having 1 to 4 carbon atoms which may be substituted, X is an oxygen atom or a nitrogen-containing substituent, n is an integer of 2 to 4, m is an integer of 1 to 20, L 2 is a divalent linking group having 1 to 6 carbon atoms, Y is a nitrogen-containing group, R 1 and R 2 are a hydrogen group or an alkyl group having 1 to 6 carbon atoms, R 3 is a hydrogen atom or a substituent, and R 4 and R 5 are an alkyl group having 1 to 40 carbon atoms.

First claim

What is claimed is:

1. A compound represented by the following General Formula (1):

in Formula (1),
Z is an imidazolyl group which may have a substituent,
L 1 is an alkylene group having 1 to 4 carbon atoms which may have a substituent, and
X is an oxygen atom or a group represented by the following Formula (2),

* is a position of bonding,
n is an integer of 2 to 4,
m is an integer of 1 to 20,
L 2 is a divalent linking group having 1 to 6 carbon atoms, and
Y is a group represented by the following Formula (3),

R 1 and R 2 are the same or different and are a hydrogen atom or an alkyl group having 1 to 6 carbon atoms,
R 3 is a hydrogen atom or a substituent, and
R 4 and R 5 are the same or different and are an alkyl group having 1 to 40 carbon atoms.

2. The compound according to claim 1 , wherein L 1 is an alkylene group represented by the following Formula (4):

in the formula, * represents a position of bonding.

3. A liposome comprising the compound according to claim 1 .

4. A liposome comprising the compound according to claim 2 .

Assignees

• Fujifilm Corp

Inventors

• Oya Toyohisa
• ISHIYAMA Ayumi
• Nishikawa Naoyuki

Classifications

• A61K9/1272 Primary

  comprising non-phosphatidyl surfactants as bilayer-forming substances, e.g. cationic lipids or non-phosphatidyl liposomes coated or grafted with polymers (lipids as modifying agents {A61K47/543}) · CPC title

• A61K47/22

  Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones · CPC title

• C07D233/64 Primary

  with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine · CPC title

• A61K9/127

  Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant · CPC title

• C12N15/111

  General methods applicable to biologically active non-coding nucleic acids · CPC title