Eisai Company, Limited

Kyoto University

Tokyo Institute of Technology

Green Tech Co., Ltd.

Eisai R&d Management Co., Ltd.

Nippon Zoki Pharmaceutical Co., Ltd.

The Doshisha

Nagoya Industrial Science Research Institute

National Center for Geriatrics and Gerontology

Atsuhiko Kubota

Kiyomi Yamatsu

Takashi Kosasa

Yoshiharu Yamanishi

Hiroo Ogura

Youichi Iimura

Hachiro Sugimoto

Norio Karibe

Takaharu Nakamura

Masahiro Yonaga

Kunizou Higurashi

Yutaka Tsuchiya

Shin Araki

Atsushi Sasaki

Hiroyuki Sugumi

Kiyomi Tamatsu

Michiko Ohtake

Satoshi Nagato

Takeru Kaneko

Kumi Uchikoshi

Takashi Takahashi

Ichiro Hijikuro

Michiaki Okuda

Isao Saito

Yoshikazu Inoue

Masataka Ueno

Takahiro Nakazawa

Shinichi Nakayama

Rie Tokizane

Kohshi Ueno

Sachiyuki Hamano

Yoshiharu Daiku

Yoichi Iimura

Tadao Shoji

Kunizo Higurashi

Masuhiro Ikeda

Michiko Kosasa

Kimie Takizawa

Satoru Ozaki

Yoko Sakata

Sachiyuki Hamazo

Yuki Fujita

Yoshio Takeuchi

Emiko Suzuki

Takeshi Kihara

Tetsuhiro Niidome

Toshiji Igarashi

Mitsuru Naiki

Naoki Asakawa

Jun Takahashi

Munekazu Iinuma

Takashi Doko

Taro Terauchi

Hidetaka Suzuki

Nariyasu Mano

Naoki Asai

Yukio Nishizawa

Shoei Furukawa

Tetsuo Ota

Tomonori Matsumoto

Tomohiro Miyasaka

Yasuo Ihara

Satoru Matsuda

Takeshi Uzuo

Akinori Akaike

Yuki Shinzaki

Yohei Oe

Tetsuo Shibata

Norio Shibata

Akihiko Takashima

Yoshiari Shimmyo

Yoshiyuki Soeda

Hiroyuki Osada

A tau aggregation inhibitor can sufficiently inhibit a tau protein from aggregating in cells. The inhibitor includes a 4-substituted catechol structure compound, having, at position 4 of its catechol ring, an electron-donating substituent R other than a hydrocarbon group, or a salt thereof. The 4-substituted catechol structure compound is preferably 4-aminocatechol or 1,2,4-benzenetriol. Examples of tauopathies to which this inhibitor is applicable include AD, Down's syndrome, frontotemporal dementia, cotricobasal degeneration (CBD) and progressive supranuclear palsy (PSP).

Tau aggregation inhibitor

Provided is a novel therapeutic means for Alzheimer's disease. In particular, provided is a compound represented by the following general formula (I): ora salt thereof.

Pyrazole derivative

Provided is a novel therapeutic means for Alzheimer's disease. In particular, provided is a compound represented by the following general formula (I): [wherein Arrepresents 2-methoxy-4-(2-pyridylmethoxy)phenyl etc. and Arrepresents a 1H-indol-6-yl group etc.] or a salt thereof.

An object of the present invention is to provide a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof and to provide a pharmaceutical agent which contains said compound as an active ingredient and has a highly safe neurotrophic factor-like activity or an alleviating action for side effect induced by administration of anti-cancer agents. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof which is the compound of the present invention is specifically represented by the formula (1): (In the formula, Y is &#x2014;O&#x2014;, &#x2014;NR&#x2014; or &#x2014;S&#x2014;, R is hydrogen atom, alkyl group, dialkylaminoalkyl group or the like and W is a substituent such as dialkylaminoalkyl group) and has a quite high usefulness as a pharmaceutical agent such as a preventive or therapeutic agent for dementia, Alzheimer's disease, Parkinson's disease, depression, etc., a treating or repairing agent for spinal cord injury.

Trans-2-decenoic acid derivative and pharmaceutical agent containing the same

The present invention provides a novel compound that is structurally similar to curcumin and has a suppressive effect on A&#x3b2; aggregation, a degradative effect on A&#x3b2; aggregates, an inhibitory effect on &#x3b2;-secretase, and a protective effect on neurons. The novel compound is a compound represented by the following general formula (Ia) or a salt thereof: wherein Rrepresents a 4-hydroxy-3-methoxyphenyl group or the like, and Rrepresents a 1H-indol-6-yl group or the like.

Curcumin derivative

The present invention provides a novel indoline derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or a salt thereof represented by the following formula (1) that has an excellent butyrylcholinesterase inhibitory activity. In the formula, Rrepresents an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a heteroaryl group, an arylalkyl group, a heteroarylalkyl group, a cycloalkylalkyl group, a heterocycloalkylalkyl group, a dihydrofurylalkyl group, an alkenyl group, a tetrahydronaphthyl group, or an indanyl group; Rrepresents a hydrogen atom, an alkyl group, an arylalkyl group, a cycloalkylalkyl group, a heteroarylalkyl group, a heterocycloalkylalkyl group, an aryl group, or an acyl group; Reach independently represents a hydrogen atom, an alkyl group, or a dialkylaminocarbonyl group; Reach independently represents a hydrogen atom or an alkyl group; and Rrepresents a hydrogen atom or an alkyl group. Each functional group may have a substituent. 

Indoline derivatives

To develop a highly safe measure to treat Alzheimer's disease using a secretase-inhibiting substance, there is provided a compound represented by the following general formula (I) or a salt thereof: wherein A represents a phenyl group or the like, Rrepresents a chlorine atom, a bromine atom, or a nitro group or the like, R, R, R, and Reach represent a hydrogen atom or the like, and L represents CH&#x2014;CHor CH&#x2550;CH.

Therapeutic agent for Alzheimer's disease

According to the present invention, there is provided a method of screening for a substance useful for transdifferentiation of microglia into neurons, a method of producing neurons, and a method of treating a neurologic disorder.

Method of screening for substances useful for transdifferentiation of microglia into neurons

The present invention provides a novel compound exhibiting an excellent suppressing effect to cell injury caused by radicals and neurotoxicity induced by excitatory nuerotransmitters such as glutamate. Specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein Z represents a bivalent organic group and the like of from 2 to 3 carbon atom(s) which may have a substituent; and Rrepresents a carboxyl group and the like.

Atisane compounds and use thereof

Fluorides of 4-substituted piperidine derivatives

The present invention provides a novel compound useful as a medicament, an acetylcholinesterase inhibitor, and an agent for preventing, treating and improving various kinds of senile dementia, Alzheimer-type senile dementia, cerebrovascular dementia or attention deficit hyperactivity disorder, namely, 1-benzyl-4-&lsqb;(5,6-dimethoxy-2-fluoro-1-indanone)-2-yl&rsqb;methylpiperidine represented by the following formula:

1-benzyl-4&lsqb;(5,6-dimethoxy-2-fluoro-1-indanon)-2-yl&rsqb;methylpiperidine

The cyclic amide derivative is defined by the formula (I) or a salt thereof: R1-(CH2)n-Z in which R1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an integer of 1 to 10 and Z is ##STR1## R2 being an aryl, a substituted aryl, a cycloalkyl or a heterocyclic group, m being an integer of 1 to 6, R3 being hydrogen or a lower alkyl, R4 being an aryl or a substituted aryl, a cycloalkyl or a heterocyclic group, p being an integer of 1 to 6, provided that the cyclic amide compound is quinazoline-on or quinazoline-dion, R2 and R4 are neither aryl nor substituted aryl. The cyclic amide compound is pharmacologically effective to prevent and treat diseases due to insufficiency of the central choline functions.

Cyclic amide derivatives

The cyclic amide derivative is defined by the formula (I) or a salt thereof: R.sup.1 --(CH.sub.2)n-Z in which R.sup.1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an integer of 1 to 10 and Z is ##STR1## R.sup.2 being an aryl, a substituted aryl, a cycloalkyl or a heterocyclic group, m being an integer of 1 to 6, R.sup.3 being hydrogen or a lower alkyl, R.sup.4 being an aryl or a substituted aryl, a cycloalkyl or a heterocyclic group, p being an integer of 1 to 6, provided that the cyclic amide compound is quinazoline-on or quinazoline-dion, R.sup.2 and R.sup.4 are neither aryl nor substituted aryl. The cyclic amide compound is pharmacologically effective to prevent and treat diseases due to insufficiency of the central choline functions.

Bicyclic amide derivatives, compositions and methods of treatment

A piperdine derivative having the formula (I) or a pharmacologically acceptable salt thereof:

Piperidine derivative and pharmaceutical composition

Growing community of inventors

Kyoto, Japan

Hachiro Sugimoto