Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Satoshi Nagato

Koichi Ito

Yoshiharu Yamanishi

Masahiro Yonaga

Atsushi Sasaki

Kohshi Ueno

Youichi Iimura

Hachiro Sugimoto

Koki Kawano

Kiyomi Yamatsu

Norio Karibe

Hiroo Ogura

Takashi Kosasa

Kumi Uchikoshi

Yoshihiko Norimine

Masataka Ueno

Akiharu Kajiwara

Shinji Hatakeyama

Makoto Komatsu

Noritaka Kitazawa

Kozo Akasaka

Takahisa Hanada

Yukiko Sugaya

Yoshio Urawa

Hiroyuki Naka

Yoshimasa Machida

Norio Minami

Naoyuki Shimomura

Teiji Kimura

Yuichi Suzuki

Toshikazu Shimizu

Noboru Yamamoto

Yoichi Iimura

Yuki Komatsu

Takao Omae

Katsutoshi Nishiura

Kunizo Higurashi

Itaru Arimoto

Akio Kayano

Hiroyuki Amino

Terence Smith

Atsushi Nagaoka

Makoto Ogo

Anthony John Groom

Leanne Rivers

Atsuhiko Kubota

Masanori Mizuno

Hiroshi Ishihara

Ichirou Yoshida

Tetsuhiro Niidome

Tetsuyuki Teramoto

Tatsuto Fukushima

Takaki Kagaya

Mariko Komatsu

The present inventions provide a method for commercially producing a 1,2 -dihydropyridine-2-one compound represented by the following formula (III-a) wherein the ring A represents an optionally substituted 2-pyridyl group, the ring B represents an optionally substituted phenyl group, and the ring C represents an optionally substituted phenyl group. Further, the invention provides crystals of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2 -dihydropyridin-2-one and production processes therefore.

Method for producing 1,2-dihydropyridine-2-one compound

The present inventions provide a method for commercially producing a 1,2-dihydropyridine-2-one compound represented by the following formula (III-a) wherein the ring A represents an optionally substituted 2-pyridyl group, the ring B represents an optionally substituted phenyl group, and the ring C represents an optionally substituted phenyl group. Further, the invention provides crystals of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one and production processes therefore.

Method for producing 1, 2-dihydropyridine-2-one compound

The present invention provides a novel compound having an excellent AMPA receptor inhibitory action and/or kainate inhibitory action. A compound represented by the following formula, a salt thereof or hydrates thereof.  In the formula, Q indicates NH, O or S; and R, R, R, Rand Rare the same as or different from each other and each indicates hydrogen atom, a halogen atom, a Calkyl group or a group represented by the formula &#x2014;X-A (wherein X indicates a single bond, an optionally substituted Calkylene group etc.; and A indicates an optionally substituted Caromatic hydrocarbocyclic group or 5- to 14-membered aromatic heterocyclic group etc.).

1,2-dihydropyridine compounds, manufacturing method thereof and use thereof

An acid addition salt of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one or a hydrate thereof, wherein the acid is selected from the group consisting of benzenesulfonic acid, p-toluenesulfonic acid, hydrochloric acid, hydrobromic acid, sulfuric acid, methanesulfonic acid, fumaric acid, tartaric acid, succinic acid and benzoic acid. 

Salt of 1,2-dihydropyridine compound

The present invention provides a novel compound having an excellent AMPA receptor inhibitory action and/or kainate inhibitory action. A compound represented by the following formula, a salt thereof or hydrates thereof. In the formula, Q indicates NH, O or S; and R, R, R, Rand Rare the same as or different from each other and each indicates hydrogen atom, a halogen atom, a Calkyl group or a group represented by the formula &#x2014;X-A (wherein X indicates a single bond, an optionally substituted Calkylene group etc.; and A indicates an optionally substituted Caromatic hydrocarbocyclic group or 5- to 14-membered aromatic heterocyclic group etc.).

1,2-dihydropyridine compounds, process for preparation of the same and use thereof

Heterodiazinone derivatives

N,N-substituted cyclic amine derivatives

Nitrile compound

A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof:

Biphenyl derivatives

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

A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are defined in the specification, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis. The compounds exhibit dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism.

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

The cyclic amide derivative is defined by the formula (I) or a salt thereof: R.sup.1 --(CH2)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, 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.

Benzoxazine derivatives

The cyclic amide derivative is defined by the formula (I) or a salt thereof:

1,2,3,4 tetrahydropteridinone cyclic amide derivatives

Growing community of inventors

Chiba, Japan

Satoshi Nagato