Eisai R&d Management Co., Ltd.

Mamoru Takaishi

Toshihiko Kaneko

Yuichi Suzuki

Koichi Ito

Koki Kawano

Noritaka Kitazawa

Teiji Kimura

Takehiko Miyagawa

Hiroaki Hagiwara

Takeo Sasaki

Eriko Doi

Nobuaki Sato

Takashi Doko

Takafumi Motoki

Tasuku Ishida

Kunitoshi Takeda

Yoichi Kita

Kogyoku Shin

Afzal Khan

Noboru Yamamoto

Yu Yoshida

Paschalis Dimopoulos

Daisuke Shinmyo

Daiju Hasegawa

Toshiyuki Uemura

Yoshinori Takahashi

Ikuo Kushida

Nobuhiro Sato

Alan James Braunton

Tomoyuki Shibuguchi

Alan Braunton

A compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof works as an mGluR2 antagonist, and is applicable as a therapeutic agent for neurological disorders related to glutamate dysfunction and diseases involving the mGluR2, such as Alzheimer's disease: 

Tetrahydroimidazo(1,5-D)[1,4]oxazepine derivative

Disclosed is a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, which is effective as a therapeutic or prophylactic agent for a disease induced by A&#x3b2;, wherein Arrepresents an imidazolyl group which may be substituted with a C1-6 alkyl group, or the like; Arrepresents a phenyl group which may be substituted with a C1-6 alkoxy group, or the like; Xrepresents a double bond, or the like; and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, or the like.

Polycyclic compound

The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; R is monofluoromethyl or difluoromethyl; and pharmaceutically acceptable salts thereof; which compound has an A&#x3b2; production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A&#x3b2; and typified by Alzheimer-type dementia. 

Fused aminodihydrothiazine derivatives

A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a Caryl group or the like, L is &#x2014;NRCO&#x2014; or the like (wherein Ris a hydrogen atom or the like), Ring B is a Caryl group or the like, X is a Calkylene group or the like, Y is a single bond or the like, Z is a Calkylene group or the like, Rand Rare each independently a hydrogen atom or the like, and R, R, Rand Rare independently a hydrogen atom, a halogen atom or the like, has an A&#x3b2; production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A&#x3b2; and typified by Alzheimer-type dementia.

A compound represented by the general formula: wherein Ring A is a Caryl group or the like, L is &#x2014;NRCO&#x2014; or the like (wherein Ris a hydrogen atom or the like), Ring B is a Caryl group or the like, X is a Calkylene group or the like, Y is a Calkylene group or the like, Z is an oxygen atom or the like, Rand Rare each independently a hydrogen atom or the like, and R, R, Rand Rare independently a hydrogen atom, a halogen atom or the like, or a pharmaceutically acceptable salt thereof, or a solvate thereof, has an A&#x3b2; production inhibitory effect or a BACE1 inhibitory effect and is useful as a therapeutic agent for a neurodegenerative disease caused by A&#x3b2; and typified by Alzheimer-type dementia.

Fused aminodihydrothiazine derivative

The present invention relates to a novel two cyclic cinnamide compound and a pharmaceutical agent comprising the compound as an active ingredient. The two cyclic cinnamide compound represented by the general formula (I): whereinrepresents a single bond or a double bond; Arrepresents a phenyl group or pyridinyl group that may be substituted with 1 to 3 substituents; Rand Reach represent a C1-6 alkyl group, a hydroxyl group, or the like; Zrepresents a methylene group or vinylene group, which may be substituted with 1 or 2 substituents selected from Substituent Group A1, an oxygen atom, or an imino group that may be substituted with a substituent selected from Substituent Group A1; and p, q, and r each represent an integer of 0 to 2, which has an effect of reducing A&#x3b2;40 and A&#x3b2;42 production, and thus is particularly useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A&#x3b2; such as Alzheimer's disease or Down's syndrome.

Two cyclic cinnamide compound

The present invention relates to a compound represented by formula (I): wherein Rrepresents a C1-3 alkyl group, Rrepresents a hydrogen atom or a C1-3 alkyl group, Ar represents a phenyl group or the like which may be substituted with 1 to 3 substituents, X represents an oxygen atom or the like, n and m are the same or different and integers of 0 to 2, or a pharmacologically acceptable salt, and use thereof as a medicament.

Bicyclic oxomorpholine derivative

The present invention provides a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein Ar1 represents an imidazolyl group that may be substituted with a C1-6 alkyl group, or the like, Ar2 represents a phenyl group that may be substituted with a C1-6 alkoxy group, or the like, X1 represents a double bond or the like, and Het represents an imidazolyl group that may be substituted with a C1-6 alkyl group, or the like, which is effective as a therapeutic or prophylactic agent for a disease caused by A&#x3b2;.

Multi-cyclic cinnamide derivatives

A compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein Arrepresents an imidazolyl group or the like which may be substituted with a C1-6 alkyl group, Arrepresents a phenyl group or the like which may be substituted with a C1-6 alkoxy group, Xrepresents a double bond or the like and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, is effective as a therapeutic or prophylactic agent for a disease caused by A&#x3b2;.

Imidazoyl pyridine compounds and salts thereof

The present invention relates to a compound represented by Formula (I): (wherein Arrepresents an imidazolyl group which may be substituted with 1 to 3 substituents; Arrepresents a pyridinyl group, a pyrimidinyl group, or a phenyl group which may be substituted with 1 to 3 substituents; Xrepresents (1) &#x2014;C&#x2261;C&#x2014; or (2) a double bond etc. which may be substituted; Rand Rrepresent, for example, a C1-6 alkyl group or C3-8 cycloalkyl group which may be substituted) or a pharmacologically acceptable salt thereof and to the use thereof as pharmaceutical agents.

Cinnamide compound

The present invention provides a most suitable prodrug of a cinnamide compound. The prodrug is represented by Formula (I) wherein Rand Reach denote a C1-6 alkyl group or the like; Xdenotes a methoxy group or a fluorine atom; Y denotes a phosphono group or the like; and A denotes a cyclic lactam derivative.

Prodrug of cinnamide compound

The present invention provides a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein Arrepresents an imidazolyl group that may be substituted with a C1-6 alkyl group, or the like, Arrepresents a phenyl group that may be substituted with a C1-6 alkoxy group, or the like, Xrepresents a double bond or the like, and Het represents an imidazolyl group that may be substituted with a C1-6 alkyl group, or the like, which is effective as a therapeutic or prophylactic agent for a disease caused by A&#x3b2;.

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Tsukuba, Japan

Mamoru Takaishi