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LIPID DERIVATIVE FOR NUCLEIC ACID INTRODUCTION meetings

Foreign code F190009702
File No. S2017-0623-C0
Posted date Jan 23, 2019
Country WIPO
International application number 2018JP007736
International publication number WO 2018190017
Date of international filing Mar 1, 2018
Date of international publication Oct 18, 2018
Priority data
  • P2017-078458 (Apr 11, 2017) JP
Title LIPID DERIVATIVE FOR NUCLEIC ACID INTRODUCTION meetings
Abstract The present invention addresses the problem of providing lipid particles that do not have a positive charge at the pH of a body fluid (usually in the neutral range) and are capable of more efficiently expressing the effect of an encapsulated drug, and a lipid for forming said lipid particles. The problem can be solved by a phospholipid represented by general formula (1): [in the formula, R1 and R2 are the same or different and represent a chain hydrocarbon group. m represents 1 or 2. n represents 1 or 2. p represents an integer of 1-4.] and lipid particles containing the same.
Outline of related art and contending technology BACKGROUND ART
RNA interfering agents including, small interfering RNA(siRNA) recent attractive drug are receiving great attention as seeds.This seed is effective to sequentially have been found, in vivo RNA was administered from the outside of the original activity may require a delivery system with a very high degree.This is, RNA and quickly receive the enzymatic degradation does not pass through the cell membrane due to a little.Therefore, to a practical use of RNA interference, is inevitably accompanied by the development of a delivery system.
RNA such as the system the delivery of the drug, the drug is encapsulated in lipid particles are known to be administered.However, administration of a nucleic acid having a negative charge, usually, the electrostatic interaction in order to cause the one having a positive charge is used and therefore, a fear of cytotoxicity (Patent Document 1).
Scope of claims (In Japanese)請求の範囲 [請求項1]
一般式(1):
[化1]

[式中、R 1及びR 2は同一又は異なって、鎖式炭化水素基を示す。mは1又は2を示す。nは1又は2を示す。pは1~4の整数を示す。]
で表されるリン脂質。

[請求項2]
前記鎖式炭化水素基が不飽和鎖式炭化水素基である、請求項1に記載のリン脂質。

[請求項3]
前記鎖式炭化水素基の炭素数が12~24である、請求項1又は2に記載のリン脂質。

[請求項4]
前記m及び前記nが共に2である、請求項1~3のいずれかに記載のリン脂質。

[請求項5]
前記pが1又は2である、請求項1~4のいずれかに記載のリン脂質。

[請求項6]
請求項1~5のいずれかに記載のリン脂質(リン脂質A)を含有する、脂質粒子。

[請求項7]
薬物を内包する、請求項6に記載の脂質粒子。

[請求項8]
前記薬物がポリヌクレオチドである、請求項7に記載の脂質粒子。

[請求項9]
さらに、コレステロールを含有する、請求項6~8のいずれかに記載の脂質粒子。

[請求項10]
前記リン脂質Aが不飽和鎖式炭化水素基を有するリン脂質であり、且つ、さらに、飽和鎖式炭化水素基を有するリン脂質(リン脂質B)を含有する、請求項6~9のいずれかに記載の脂質粒子。

[請求項11]
前記リン脂質Bの含有量が、前記リン脂質A 100モルに対して30~70モルである、請求項10に記載の脂質粒子。

[請求項12]
請求項1~5のいずれかに記載のリン脂質を含有するアルコール溶液と、水溶性薬物を含有する酸性水溶液とを混合する工程を含む、脂質粒子の製造方法。

[請求項13]
前記水溶性薬物がポリヌクレオチドである、請求項12に記載の製造方法。

[請求項14]
前記アルコール溶液が溶媒としてブタノールを含有する溶液である、請求項12又は13に記載の製造方法。

[請求項15]
請求項1~5のいずれかに記載のリン脂質及び薬物を含有する脂質粒子を含有する、医薬。

  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • NIPPON FINE CHEMICAL CO., LTD.
  • SHIZUOKA PREFECTURAL UNIVERSITY CORPORATION
  • Inventor
  • ASAI, Tomohiro
  • OKU, Naoto
  • MAEDA, Noriyuki
  • FUKATA, Naofumi
  • TOMITA, Koji
IPC(International Patent Classification)

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