Eisai R&d Management Co., Ltd.

Eriko Doi

Toshihiko Kaneko

Koichi Ito

Koki Kawano

Noritaka Kitazawa

Teiji Kimura

Mamoru Takaishi

Hiroaki Hagiwara

Takehiko Miyagawa

Takeo Sasaki

Nobuaki Sato

Kogyoku Shin

Takashi Doko

Fumihiro Ozaki

Motohiro Soejima

Yoshihiko Norimine

Noboru Yamamoto

Yu Yoshida

Ikuo Kushida

Tasuku Ishida

Kiyoaki Kobayashi

Daiju Hasegawa

Nobuyuki Kurusu

Compounds represented by formula (I) and pharmaceutically acceptable salts thereof have excellent sodium channel inhibitory action and are useful as therapeutic agents and analgesics for various kinds of neuralgia, neuropathy, epilepsy, insomnia, premature ejaculation and the like. wherein Q represents ethylene, etc., R, Rand Rrepresent hydrogen, etc., Xrepresents Calkylene, etc., Xrepresents Calkylene, etc., Arepresents a 5- to 6-membered heterocyclic group, etc., and Arepresents Caryl, etc.

Bicycloamine derivatives

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

An amorphous object of (3E)-1-[l(s)-1-(4-fluorophenyl)ethyl]-3-[3-methoxy-4-(4methyl-1H-imidazol-1-yl)benzylidene]piperidine-2-one, which is represented by the formula (1) and has A&#x3b2;-production inhibitory activity. The amorphous object has such satisfactory properties that it has excellent solubility, is stable, does not readily become a crystalline form, and has low hygroscopicity. It is hence suitable for use in pharmaceutical preparations.

Amorphous object of cinnamide compound

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 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;.

Multi-cycle cinnamide derivatives

The present invention relates to a process for preparing a compound of formula (6a): wherein Arrepresents an imidazolyl group which may be substituted with 1 to 3 substituents shown below; Arrepresents a pyridinyl group, a pyrimidinyl group or a phenyl group which may be substituted with 1 to 3 substituents; and Rrepresents a group selected from certain substituents.

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. The object of the present invention is to find a therapeutic or preventive agent for diseases caused by A&#x3b2;. According to the present invention, a therapeutic or preventive agents for diseases caused by A&#x3b2; can be provided.

The present invention relates to a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein R, R, R, and Rare the same or different and each represent a hydrogen atom or a C1-6 alkyl group; Xrepresents a C1-6 alkylene group that may be substituted; Xrepresents a methoxy group or a fluorine atom; Xrepresents an oxygen atom or a methylene group, provided that Xis only an oxygen atom when Xis a methoxy group; and Arrepresents an aryl group, pyridinyl group, aryloxy group, or pyridinyloxy group that may have a substituent such as a halogen atom; and to use of the compound or salt as a pharmaceutical agent.

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Tsukuba, Japan

Eriko Doi