Kyowa Hakko Kirin Co., Limited

Dicerna Pharmaceuticals, Inc.

Kyowa Kirin Co., Ltd.

Tomoyuki Naoi

Takeshi Kuboyama

Tomohiro Era

Shintaro Hosoe

Toshihiko Ishii

Kaori Yagi

Junichi Enokizono

Kentarou Hatanaka

Akihiro Tokunaga

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).

The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) 

The present invention provides a composition for suppressing the expression of a KRAS gene, comprising a lipid particle containing, as a drug, a double-stranded nucleic acid having an antisense strand having a sequence of bases complementary to the sequence of at least 19 continuous bases of any one KRAS gene's mRNA of sequence Nos. 1 to 3; and a cationic lipid represented by the following formula (I): wherein  

RNAi pharmaceutical composition for suppressing expression of KRAS gene

The present invention provides a lipid nano-particles, which allow nucleic acids to be easily introduced into cells, comprising a cationic lipid represented by formula (I) (wherein: Rand Rare, the same or different, alkenyl, etc, and 

Lipid nano particles comprising cationic lipid for drug delivery system

The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: Rand Rare, the same or different, alkenyl, etc, and Xand Xare hydrogen atoms, or are combined together to form a single bond or alkylene, and Xis absent or is alkyl, etc, Y is absent or anion, a and b are, the same or different, 0 to 3, and Lis a single bond, etc, Ris alkyl, etc, Land Lare &#x2014;O&#x2014;, &#x2014;CO&#x2014;O&#x2014; or &#x2014;O&#x2014;CO&#x2014;), a composition comprising the cationic lipid and a nucleic acid, and a method for introducing a nucleic acid into a cell by using the composition comprising the cationic lipid and the nucleic acid, and the like. 

Growing community of inventors

Tokyo, Japan

Tomoyuki Naoi