Takeda Pharmaceutical Company Limited

Tokyo Medical and Dental University

Institute of Science Tokyo

Ryosuke Tokunoh

Tetsuya Nagata

Takanori Yokota

Hideki Furukawa

Shigekazu Sasaki

Yoshihiro Banno

Tomohiro Seki

Kosuke Hidaka

Takatoshi Yogo

Yasuo Nakagawa

Kenichi Miyata

Ryoma Hara

Yusuke Adachi

Akio Uchida

Naoto Arimura

The object of the present invention is to provide a nucleic acid agent that can be efficiently delivered to the nervous system, particularly the central nervous system to which the BBB mechanism prevents drug delivery, and can produce an antisense effect on a target transcriptional product at the delivered site, and a composition comprising the same. Provided is a double-stranded nucleic acid complex formed by annealing a first nucleic acid strand capable of hybridizing to part of a target transcriptional product, and has an antisense effect on the target transcriptional product, to a second nucleic acid strand comprising a base sequence complementary to the first nucleic acid strand, and is bound to tocopherol or an analog thereof, cholesterol or an analog thereof, or a substituted or unsubstituted Calkyl group, a substituted or unsubstituted Calkenyl group, or a substituted or unsubstituted Calkoxy group.

BBB-crossing lipid ligand of hetero nucleic acid

Developed and provided is: a nucleic acid agent that is efficiently delivered to the central nervous system, to which drug delivery is inhibited by the blood brain barrier mechanism, and that provides an antisense effect to a target transcription product at the delivery site; and a composition containing such a nucleic acid agent. Provided is a double-stranded nucleic acid complex consisting of a first nucleic acid strand and a second nucleic acid strand that are annealed to each other; wherein the first nucleic acid strand hybridizes with part of a target transcription product and has an antisense effect on the target transcription product; and wherein the second nucleic acid strand includes a base sequence complementary to the first nucleic acid strand and is conjugated to a phosphatidylethanolamine or an analog thereof.

Nucleic acid complex

Provision of a prophylactic or therapeutic agent for diabetes, which has superior efficacy. A compound represented by the formula: wherein each symbol is as described in the specification, or a salt thereof.

Heterocyclic compound

The present invention provides a heterocyclic compound represented by the following formula (I), which has a glucagon antagonistic action and is useful for the prophylaxis or treatment of diabetes and the like, a compound represented by wherein ring A is an optionally substituted benzene ring and the like; Y is a nitrogen atom and the like; X is &#x2014;O&#x2014; and the like; Ris a hydrogen atom and the like; Rand Rare each independently a hydrogen atom and the like; Ris an optionally substituted hydrocarbon group and the like; Ris a hydrogen atom and the like; and Ris &#x2014;(CH)&#x2014;COOH and the like, or a salt thereof.

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Osaka, Japan

Ryosuke Tokunoh