Kyowa Hakko Kirin Co., Limited

Kyowa Kirin Co., Ltd.

Shintaro Hosoe

Tomoyuki Naoi

Takeshi Kuboyama

Kentaro Hatanaka

Kaori Yagi

Keisuke Yamamoto

Tomohiro Tamura

Kimihisa Ueno

Tomohiro Era

Rina Nakamura

Hayato Yabuuchi

Nobuhiro Yagi

Michihiro Maemoto

The present invention provides a nucleic acid-containing lipid nanoparticle comprising an analog of a fatty acid ester of glycerol, and a nucleic acid, wherein the analog is not hydrolyzable by a lipase.

Nucleic acid-containing lipid nanoparticle

The present invention provides a compound represented by formula (I) usable as a cationic lipid that facilitates introduction of a nucleic acid, for example, into a cell, and a composition or the like containing the compound. 

Compound usable as cationic lipid

The present invention provides nucleic acid-containing lipid nanoparticles containing a lipid (lipid A) which has a hydrophilic unit having a single quaternary ammonium group, and three independent, optionally substituted hydrocarbon groups, a lipid derivative or fatty acid derivative of a water-soluble polymer, and a nucleic acid.

Nucleic acid-containing lipid nanoparticles

The present invention provides a compound represented by formula (I) or a pharmaceutically acceptable salt thereof as a cationic lipid, and the like. 

Compound as cationic lipid

The present invention provides a cationic lipid represented by the formula (I) wherein Rand Reach represents alkyl having 8 to 24 carbon atoms or the like; Rrepresents a hydrogen atom, alkyl having 1 to 3 carbon atoms, the formula (A) wherein Rand Reach represents a hydrogen atom or the like, and nrepresents an integer from 2 to 6, or the formula (B) wherein Rand Reach represents a hydrogen atom or the like, and nrepresents an integer from 1 to 6; nrepresents an integer from 0 to 4; and nrepresents an integer from 1 to 4, provided that the case where nis 0 and nis 1 is excluded, and a composition which contains the cationic lipid and a nucleic acid, or the like.

Cationic lipid

Provided are a cationic lipid which facilitates the introduction of a nucleic acid into, for example, a cell or the like; a composition containing the cationic lipid and a nucleic acid; a method for introducing a nucleic acid into a cell by using a composition containing the cationic lipid and the nucleic acid; and the like. The cationic lipid is, for example, a cationic lipid represented by formula (A): formula (A): (wherein Ris alkenyl or the like, Ris alkenyl or the like, Rand Rare each alkyl, or are combined together to form alkylene, or Rand Rare combined together to form alkylene, Ris a hydrogen atom or the like, or is combined together with Rto form alkylene, Xis alkylene, and Xis a single bond or alkylene).

A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, Ris a hydrogen atom and the like, X is the formula (b3) wherein Ris a hydrogen atom and the like, and the like, A is the formula (a18) wherein Ris a hydrogen atom and the like, and Rand Rare the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR&#x3b3; agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided. 

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Tokyo, Japan

Shintaro Hosoe