Kyowa Hakko Kirin Co., Limited

Kyowa Hakko Kogyo Co., Ltd.

Jun-ichi Saito

Yutaka Kanda

Yuichi Takahashi

Shiro Akinaga

Tomoyuki Nishikawa

Michihiko Suzuki

Yukimasa Shiotsu

Takahiro Nakajima

Shinji Nara

Shiro Soga

Junichiro Yamamoto

Takayuki Nakashima

Masayoshi Nakoji

Jiro Kajita

Asana Makino

Hiroshi Nakagawa

Taiji Oashi

Fumikazu Shinohara

Yasuo Kouda

An oligonucleotide having improved affinity for AGO2 is disclosed. The oligonucleotide has a nucleotide residue or a nucleoside residue represented by formula (I) wherein Xis an oxygen atom or the like, Ris formula (IIA), wherein Ris halogen or the like, and Ris a hydrogen atom or the like, or formula (IVA) wherein Yis a nitrogen atom or the like, and Yis CH or the like, or the like, Ris a hydrogen atom, hydroxy, halogen, or optionally substituted lower alkoxy, and Ris a hydrogen atom or the like at the 5' end thereof, and the nucleotide residue or the nucleoside residue binds to an adjacent nucleotide residue through the oxygen atom at position 3. A method for improving the knockdown activity of an oligonucleotide wherein the oligonucleotide has a knockdown activity against an mRNA encoding a protein involved in a disease. 

Oligonucleotide

An oligonucleotide having a nucleotide residue or a nucleoside residue represented by formula (I) {wherein Xis an oxygen atom or the like, Ris formula (IIA) (wherein Ris halogen or the like, and Ris a hydrogen atom or the like), formula (IVA) (wherein Yis a nitrogen atom or the like, and Yis CH or the like), or the like, Ris a hydrogen atom, hydroxy, halogen, or optionally substituted lower alkoxy, and Ris a hydrogen atom or the like, or formula (VI) (wherein n2 is 1, 2 or 3)} at the 5' end thereof, wherein the nucleotide residue or the nucleoside residue binds to an adjacent nucleotide residue through the oxygen atom at position 3, is provided. 

Oligonucleotide having non-natural nucleotide at 5'-terminal thereof

The present invention provides Hsp90 family protein inhibitors comprising, as an active ingredient, a benzoyl compound represented by general formula (I): (wherein n represents an integer of 0 to 10; Rrepresents substituted or unsubstituted lower alkoxy, substituted or unsubstituted lower alkoxycarbonyl, CONRRor the like; Rrepresents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group or the like; Rand R, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl or the like; and Rand R, which may be the same or different, each represent a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like) or a prodrug thereof, or a pharmaceutically acceptable salt of said benzoyl compound or said prodrug.

Hsp90 family protein inhibitors

Growing community of inventors

Sunto-gun, Japan

Jun-ichi Saito