Nishizaki Bioinformation Research Institute

Other

Ktn Biotec, Inc.

Tox K.k.

Tomoyuki Nishizaki

Akito Tanaka

Takashi Nakano

Takeshi Kanno

Tadashi Shimizu

The present invention provides a therapeutic drug for diabetes containing 1,2-dioleoyl-sn-glycerol-3-phosphoethanolamine (DOPE) as an active ingredient, particularly a therapeutic drug for diabetes that exhibits a GLUT4 endocytosis suppressive action by suppressing activation of PKC&#x3b1; and the like.

GLUT4 endocytosis inhibitor

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

The present invention provides a prophylactic and/or therapeutic drug for diabetes, which contains 8-[2-(2-pentyl-cyclopropylmethyl)-cyclopropyl]-octanoic acid (DCP-LA) as an active ingredient, particularly a prophylactic and/or therapeutic drug for diabetes, which promotes sugar intake into the cells, and the like.

Agent for treating diabetes

The present invention provides an anti-cancer agent, a cancer cell death inducing agent, a protein phosphatase 2A activation enhancing agent, a protein tyrosine phosphatase 1B activation enhancing agent and the like, each containing 1,2-dipalmitoleoyl-sn-glycero-3-phosphoethanolamine as an active ingredient.

Anti-cancer agent containing a diacylphosphatidylethanolamine as an active ingredient

The combined use of 1,2-dilinoleoyl-sn-glycero-3-phosphocholine and 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine affords a superior anti-depressive action, an improving effect on the cognitive function associated with depression, an improving effect on the stress-induced suppression of Akt activation, and a suppressive action on the stress-induced GSK-3&#x3b2; activation. Therefore, the present invention can provide an antidepressant combination drug, an agent for improving cognitive function associated with depression, an agent for improving stress-induced suppression of Akt activation and an agent for suppressing stress-induced GSK-3&#x3b2; activation.

Antidepressant combination drug

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 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.

Growing community of inventors

Kobe, Japan

Tomoyuki Nishizaki