Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Yoichi Iimura

Takashi Kosasa

Yoshiharu Yamanishi

Yuichi Suzuki

Noboru Yamamoto

Hachiro Sugimoto

Koichi Ito

Koki Kawano

Teiji Kimura

Satoshi Nagato

Yoshihiko Norimine

Shinji Hatakeyama

Tetsuhiro Niidome

Tetsuyuki Teramoto

Yoshio Takeuchi

Emiko Suzuki

Makoto Komatsu

Toshihiko Kaneko

Afzal Khan

Piotr Pawel Graczyk

Gurpreet Singh Bhatia

Daisuke Shinmyo

Nobuyuki Kurusu

Manami Kimura

Yoshihisa Kaneda

Yukie Yoshikawa

Tetsuo Shibata

Norio Shibata

The present invention provides novel compounds of formula (I) and their use in the inhibition of c-Jun N-terminal kinases. The present invention further provides the use of these compounds in medicine, in particular in the prevention and/or treatment of neurodegenerative disorders related to apoptosis and/or inflammation. 

JNK inhibitors

The present invention provides an excellent sigma receptor binding agent and/or acetylcholinesterase inhibitor containing an (1-indanone)-(1,2,3,6-tetrahydropyridine) compound. More specifically, it provides an (1-indanone)-(1,2,3,6-tetrahydropyridine) compound represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate thereof:  In the formula (I), R, R, Rand Rare the same as or different from each other.

(1-Indanone)-(1,2,3,6-tetrahydropyridine) compounds

The present invention provides a novel compound having an excellent acetylcholinesterase inhibitory effect. That is, it provides a compound represented by formula: (wherein Rand Rrepresent substituents), a pharmacologically acceptable salt thereof or hydrates thereof.

4-substituted piperidine compound

The present invention provides a novel compound having a superior acetylcholinesterase inhibitory action. It provides a compound represented by the formula:(In the formula, Rrepresents a group represented by the formula:(wherein, R, R, Rand Rare the same as or different from each other and each represents a hydrogen atom, an optionally substituted Calkoxy group and the like; and m represents an integer from 0 to 6) and the like; and Rrepresents a hydrogen atom, an optionally substituted Calkyl group, an optionally substituted Calkenyl group or an optionally substituted Calkynyl group), a salt thereof or a hydrate of them.

The present invention provides a novel compound having a superior calcium antagonism, in particular, a neuron-selective calcium antagonism. Namely, it provides a compound represented by the following formula, a salt thereof or a hydrate of them.In the formula, Ar indicates an optionally substituted 5- to 14-membered aromatic ring etc.; the ring A indicates any one ring selected from a piperazine, a homopiperazine, a piperidine and the like; the ring B indicates an optionally substituted Con hydrocarbon ring etc.; E indicates a single bond, a group represented by the formula &#x2014;CO&#x2014;, etc.; X indicates a single bond, an oxygen atom etc.; Rindicates a hydrogen atom, a halogen atom, a hydroxyl group etc.; and D, D, Wand Ware the same as or different from each other and each represents a single bond or an optionally substituted Calkylene chain.

Piperazine compound and pharmaceutical composition containing the compound

N,N-substituted cyclic amine derivatives

Acetylcholinesterase inhibitors containing 1-benzyl-pyridinium salts

Fluorides of 4-substituted piperidine derivatives

Nitrile compound

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 present invention provides a novel industrially or economically preferable process for production of a hydrogen halogenide salt of a Donepezil derivative having an excellent pharmacological action as medicament, namely, reaction of 1-indanone derivative with carbonate ester to obtain 2-alkoxycarbonyl-1-indanone derivative, followed by reaction with halogenated (4-pyridyl)methyl or a salt thereof and decarboxylation successively to obtain 2-(4-pyridyl)methyl-1-indanone derivative, then reaction with halogenated benzyl to obtain quaternary ammonium salt, then reduction, and synthetic intermediates thereof.

Process for production of donepezil derivative

Growing community of inventors

Ibaraki, Japan

Yoichi Iimura