Toray Industries, Inc.

Keiichi Okimura

Tomohide Masuda

Hiroyuki Meguro

Katsuhiko Iseki

Mie Kaino

Yukihiro Nishio

Hideaki Inada

Hideyuki Tsutsui

Yuko Kubota

Syuji Udagawa

Yumiko Sekiya

Masashi Yamamoto

Tadaaki Ohgi

Eriko Aoki

Munetaka Kunishima

Tatsuya Fujita

Yuki Matsumura

Kennunettsu Asaba

Yutaka Nishimura

Kazuyuki Tokumaru

Yasufumi Goto

Kyohei Koshimoto

Ayumi Takashina

Shigeo Fujii

Masato Sanosaka

Yoshitaka Numajiri

A method produces a hairpin single-stranded RNA molecule capable of inhibiting expression of a target gene, the method including: (i) an annealing step of annealing a first single-stranded oligoRNA molecule and a second single-stranded oligoRNA molecule; and (ii) a ligation step of ligating 3′ end of the first single-stranded oligoRNA molecule and 5′ end of the second single-stranded oligoRNA molecule by an Rnl2 family ligase, wherein a sequence produced by ligating the first single-stranded oligoRNA molecule and the second single-stranded oligoRNA molecule includes a gene expression-inhibiting sequence for the target gene.

Method of producing hairpin single-stranded RNA molecule

A method produces a hairpin single-stranded RNA molecule capable of inhibiting expression of a target gene, including the step of reacting a first single-stranded oligo-RNA molecule represented by formula (I) with a second single-stranded oligo-RNA molecule represented by formula (II) in a mixed solvent including a buffer solution and a hydrophilic organic solvent in the presence of a dehydration condensation agent: 5′-Xc-Lx(I) and Lx-X—Y-Ly-Yc-3′ (II), wherein the dehydration condensation agent is selected from the group consisting of a triazine-based dehydration condensation agent, a uronium-based dehydration condensation agent including an N-hydroxy nitrogen-containing aromatic ring structure, a carbodiimide-based dehydration condensation agent, a 2-halopyridinium-based dehydration condensation agent, and a formamidinium-based dehydration condensation agent.

Method of producing hairpin single-stranded RNA molecules

A compound has a guanidine skeleton that inhibits the protease activity of MALT1 and exerts a therapeutic or prophylactic effect on autoimmune disease such as psoriasis or allergic disease such as atopic dermatitis. The guanidine derivative is typified by the following formula or a pharmacologically acceptable salt thereof. 

Guanidine derivative and medical use thereof

A compound has inhibitory activity on Discoidin Domain Receptor 1. The compound includes a urea derivative represented by the formula below or a pharmaceutically acceptable salt thereof. 

Urea derivative and use therefor

A compound has inhibitory activity on Discoidin Domain Receptor 1. A urea derivative is represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein, Ris trifluoromethyl, trifluoromethoxy, or pentafluorosulfanyl; each Ris independently a hydrogen atom or methyl which is optionally substituted by one hydroxyl or one saturated heterocyclyl having four to six ring-forming atoms; Ris a hydrogen atom, halogen atom, C-Calkyl, saturated heterocyclyl having four to six ring-forming atoms and optionally having an oxo group, or RO&#x2014;; and Ris phenyl, pyridyl, pyridazinyl, or pyrimidinyl, which phenyl, pyridyl, pyridazinyl, or pyrimidinyl is optionally substituted by one R.

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Kamakura, Japan

Keiichi Okimura