Toray Industries, Inc.

Katsuhiko Iseki

Naoki Izumimoto

Yasuhiro Morita

Shunsuke Iwano

Shuji Udagawa

Yuji Osada

Tomoya Miyoshi

Tadamasa Arai

Kei Takahashi

Keiichi Okimura

Motohiro Shiraki

Yuji Sugawara

Hideaki Inada

Hirozumi Takahashi

Chihiro Yoshida

Tetsuro Koreeda

Masanori Murakami

Yoko Baba

Keiyu Oshida

Hidetoshi Noda

Tadaaki Ohgi

Hajimu Kurumatani

Eriko Aoki

Hideyuki Tsutsui

Munetaka Kunishima

Mitsuko Miyamoto

Tatsuya Fujita

Masato Sanosaka

Eriko Higashi

Fuko Matsuda

Hideyuki Tsutsiu

Kyohei Koshimoto

Ayumi Takashina

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 crystal of ethane disulfonate of (S)-1-(4-(dimethylamino)piperidin-1-yl)-3-hydroxy-3-(1-methyl-1H-imidazol-2-yl)propan-1-one, having peaks at diffraction angles 2&#x3b8;)(&#xb0; of 12.6&#xb1;0.2, 16.0&#xb1;0.2, 17.7&#xb1;0.2, 18.5&#xb1;0.2, and 21.3&#xb1;0.2 in powder X-ray diffraction; and the crystal of ethane disulfonate of (S)-1-(4-(dimethylamino)piperi din-1-yl)-3-hydroxy-3-(1-methyl-1H-imidazol-2-yl)propan-1-one, having an endothermic peak at 173&#xb0; C. to 177&#xb0; C. in simultaneous thermogravimetric-differential thermal analysis.

Crystals of cyclic amine derivative and pharmaceutical use thereof

Crystals of a compound that exhibits an analgesic action against neuropathic pain and/or fibromyalgia syndrome are useful as pharmaceuticals. The crystals may be of (S)-1-(4-(dimethylamino)piperidin-1-yl)-3-hydroxy-3-(1-methyl-1H-imidazol-2-yl)propan-1-one or a pharmacologically acceptable salt thereof.

A cyclic amine derivative represented by a general formula (I) or a pharmacologically acceptable salt thereof: wherein n represents 1 or 3, Rrepresents an alkyl group having 1 to 6 carbon atoms unsubstituted, substituted with a halogen atom or substituted with an alkyloxy group having 1 to 4 carbon atoms and Rrepresents a hydrogen atom or a halogen atom.

Cyclic amine derivative and pharmaceutical use thereof

A compound exerts an analgesic effect against pain, in particular, neuropathic pain and/or fibromyalgia syndrome. A cyclic amine derivative represented by the following general formula, or a pharmacologically acceptable salt thereof:  Methods using the compound including the cyclic amine derivative or a pharmacologically acceptable salt thereof to treat pain, neuropathic pain and fibromyalgia syndrome.

A compound exerts a strong analgesic effect against pain, in particular, neuropathic pain and/or fibromyalgia syndrome. A cyclic amine derivative represented by general formula or a pharmacologically acceptable salt thereof:  A method of treating neuropathic pain includes administering a therapeutically effective amount of the cyclic amine derivative to a mammal. A method of treating fibromyalgia syndrome includes administering a therapeutically effective amount of the cyclic amine derivative to a mammal.

A compound exerts a strong analgesic effect against pain, in particular, neuropathic pain and/or fibromyalgia syndrome. The cyclic amine derivative is represented by formula, a prodrug thereof or a pharmacologically acceptable salt thereof: wherein A represents a group represented by Formula (IIa), (IIb) or (IIc): wherein

The present invention aims to provide a therapeutic agent for chronic renal failure, comprising as an effective ingredient a compound represented by General Formula (1) or a pharmaceutically acceptable salt thereof. That is, the present invention provides provision of a drug comprising as an effective ingredient a compound represented by General Formula (1) or a pharmaceutically acceptable salt thereof, which drug is useful not only for amelioration of renal function, but also for amelioration of anemia, activation of SOD and excretion of uremic substances.

Therapeutic agent for chronic renal failure

A method relieves both nociceptive pain and neuropathic pain and has fewer side effects. The compound includes cyclohexane derivatives represented by the following compound, or pharmaceutically acceptable salts thereof or prodrugs thereof. 

Cyclohexane derivative and pharmaceutical use thereof

A compound has a strong analgesic action against both nociceptive pain and neuropathic pain and has less side effects, and is medically useful. The compound includes cyclohexane derivatives represented by the following compound, or pharmaceutically acceptable salts thereof or prodrugs thereof. 

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Kamakura, Japan

Katsuhiko Iseki