Fujisawa Pharmaceutical Company, Ltd.

Reverse Proteomics Research Institute

Nishizaki Bioinformation Research Institute

Astellas Pharma Gmbh

Other

Ktn Biotec, Inc.

Tox K.k.

Akito Tanaka

Tomoyuki Nishizaki

Akira Yamazaki

Hisashi Takasugi

Shigetaka Nishino

Tomohiro Terada

Masayuki Haramura

Minoru Sakurai

Hiroaki Mizuno

Hidenori Nakajima

Tsuruki Tamura

Takaaki Shiyama

Takao Takaya

Takashi Nakano

Hideo Tsutsumi

Minoru Yoshida

Kiyotaka Ito

Sueharu Horinouchi

Hiroyoshi Sakai

Takeshi Tsutsumi

Minoru Furuya

Takatoshi Ishikawa

Tadashi Shimizu

Takeshi Kanno

8-[2-(2-Pentyl-cyclopropylmethyl)-cyclopropyl]-octanoic acid (DCP-LA) has an action to promote synthesis and regeneration of elastin, and is useful as an agent for the prophylaxis or improvement of wrinkles, and an anti-aging drug.

Elastin synthesis/regeneration promoting agent

8-[2-(2-pentyl-cyclopropylmethyl)-cyclopropyl]-octanoic acid has a protein tyrosine phosphatase 1B (PTP1B) inhibitory action, an Akt activating action, a GSK-3&#x3b2; phosphorylation promoting action, and a suppressive action on &#x3c4; protein phosphorylation induced by A&#x3b2;, and is useful as a therapeutic drug for Alzheimer-type dementia, an antidepressant and/or an anti-aging drug.

Inhibitor of &#x3c4; protein phosphorylation

The invention provides a phospholipid compound containing unsaturated fatty acid having a cyclopropane ring such as 8-[2-(2-pentyl-cyclopropylmethyl)-cyclopropyl]-octanoic acid (DCP-LA) and 8-(2-octylcyclopropyl)octanoic acid (DCP-OA) and the like, particularly 1,2-o-bis-[8-{2-(2-pentyl-cyclopropylmethyl)-cyclopropyl}-octanoyl]-sn-glycero-3-phosphatidylethanolamine (diDCP-LA-PE), which has a cognitive function improving effect and an anti-diabetes action, and which is useful as a medicine such as a therapeutic drug for dementia, a therapeutic drug for diabetes and the like.

Phospholipid compound containing unsaturated fatty acid derivative having cyclopropane ring

The present invention aims to provide a compound having an anticancer action comparable or superior to that of naftopidil. A compound represented by the formula (I) wherein each symbol is as defined in the SPECIFICATION, or a pharmaceutically acceptable salt thereof, particularly 1-((2-((2-methoxyphenyl)amino)ethyl)amino)-3-(1-naphthyloxy)propan-2-ol, or a pharmaceutically acceptable salt thereof. The compound shows a cell proliferation suppressive action on a wide range of cancer cells, is useful as an anti-cancer agent, and is useful for the prophylaxis and/or treatment of cancer.

Anticancer agent

The present invention aims to obtain an optical isomer of DCP-LA, which shows more superior activity and is suitable for clinical utilization, and provide an agent having a superior PKC-&#x3b5; activation action, a prophylactic and/or therapeutic agent for neurotransmitter release disorders, and a prophylactic and/or therapeutic agent for neuropsychiatric diseases, which contain the isomer as an active ingredient. A compound represented by the following formula: or a pharmaceutically acceptable salt thereof, and a selective PKC-&#x3b5; activator containing same as an active ingredient, and is the like.

PKC-&#x3b5; activator

A resin which is prepared by polymerizing a monomer component incorporating a hydrophilic spacer, and a ligand-immobilized solid phase carrier obtained by immobilizing a ligand to the resin, are capable of reducing the non-specific adsorption of substances, other than the target molecule for the ligand, which mingle in the sample, to the resin and/or the ligand. Therefore, target molecule search, identification and the like with less noise are enabled.

Affinity resin

A method to determine specificity of ligand binding includes comparing a solid phase carrier first extract obtained by pre-treating a sample with a ligand-immobilized solid phase carrier and a solid phase carrier second extract obtained by treating the pretreated sample again with a ligand-immobilized solid phase carrier in terms of the proteins contained therein, and identifying a protein whose content is remarkably decreased in the second extract compared to the first extract, in order to solve 1) the problem of the solubility of subject ligand, 2) the problem of the non-specific protein-denaturing effect of the subject ligand added, and the like, in antagonism experiments in target search using an affinity resin.

Method of calibrating ligand specificity

The present invention provides a method of suppressing the nonspecific interaction between molecules, characterized in that in a process to immobilize a molecule onto a solid phase carrier and analyze the specific interaction between the molecule and a molecule that specifically interacts with the molecule on the solid phase, the hydrophobic property of the solid phase surface in the solid phase carrier is regulated, particularly a hydrophilic spacer is interlaid at the time of immobilization of the molecule onto the solid phase carrier, which method makes it possible to suppress the nonspecific interaction between the molecules, and to reduce nonspecific adsorption to the solid phase.

Method of inhibiting nonspecific interaction between molecules on solid phase support

The present invention provides a pharmaceutical composition containing, as an active ingredient, a compound that specifically binds to KSRP or a functional fragment thereof, and a screening method for the compound. KSRP is a novel target protein for anticancer agents; a compound capable of regulating the expression and activity of such a protein and a pharmaceutical composition containing it are highly useful for proliferative diseases, particularly as anticancer agents. By providing the novel target protein, the mechanism behind the anticancer effect that has conventionally been unexplainable can be elucidated.

Target protein of anticancer agent and novel anticancer agent (spnal) corresponding thereto

The present invention provides a method of analyzing the specific interaction between a molecule to be analyzed and a molecule that specifically interacts with the former molecule on a solid phase using a molecule-immobilized solid phase support mixture prepared by binding the subject molecule to the solid phase support without specifying the binding position on the molecule side, particularly a method wherein the immobilization is conducted via a spacer introduced to the molecule without specifying the binding position on the molecule side, which method makes it possible to identify and select only a molecule that exhibits a specific interaction with a molecule to be analyzed, without an investigation of structure-activity correlation, which has conventionally been essential, and hence enables an analysis of the interaction between these molecules.

Method of immobilizing compound on solid phase support

A carboxylic acid compound having cyclopropane ring(s) of the formula (I): wherein R is alkyl or alkenyl optionally having one or more 1,2-cyclopropylene in a carbon chain and/or optionally having cyclopropyl at the end of a chain,X is a single bond or alkylene, wherein the total number of carbon less the number of cyclopropane ring is 10-25, and a pharmaceutically acceptable salt thereof are provided. The compound (I) shows an LTP-like potentiation of synaptic transmission, allows slow metabolism in the living body, show a stable LTP-like potentiation of synaptic transmission, and is useful as an agent for LTP-like potentiation of synaptic transmission, a cognition-enhancing drug or an agent for the prophylaxis and treatment of dementia, a learning and memory disorder and a neurotransmitter release disorder.

Carboxylic acid compound having cyclopropane ring

The present invention provides a method of analyzing the interaction between a ligand and a target molecule, which uses a solid support wherein the ligand is immobilized via a linker cleavable by photoirradiation, particularly a method of searching and purifying a target molecule. By intervening a linker specifically cleavable by photoirradiation between the ligand molecule and the solid support, release and elution of the target molecule from the solid support without using a ligand or salt at a high concentration can be enabled, and suppression of release and elution of a nonspecific protein can be enabled.

Solid support having ligand immobilized thereon by using photocleavable linker

The present invention relates to reduced FK228 of the formula (I) wherein Rand Rare the same or different and each is a hydrogen atom or a thiol-protecting group, or a salt thereof, and a histone deacetylase inhibitor containing this compound, an expression potentiator and a reactivation promoter of a transgene, and pharmaceutical agents containing them as active ingredients. The reduced FK228 or a salt thereof has a strong histone deacetylase inhibitory activity and this compound can be used for the prophylaxis or treatment of various diseases, in which histone deacetylation is involved, and for the gene therapy of such diseases.

Growing community of inventors

Tsukuba, Japan

Akito Tanaka