Eisai R&d Management Co., Ltd.

Eisai Company, Limited

Noritaka Kitazawa

Koki Kawano

Teiji Kimura

Koichi Ito

Toshihiko Kaneko

Mamoru Takaishi

Hiroaki Hagiwara

Takehiko Miyagawa

Takeo Sasaki

Nobuaki Sato

Atsushi Sasaki

Kohshi Ueno

Tadashi Okabe

Eriko Doi

Atsuhiko Kubota

Keiko Takahashi

Manabu Matsunaga

Makoto Komatsu

Takashi Doko

Akiharu Kajiwara

Satoshi Nagato

Kogyoku Shin

Atsushi Kamada

Yuichi Suzuki

Kazumasa Nara

Noboru Yamamoto

Yu Yoshida

Masataka Ueno

Shinichi Hamaoka

Daisuke Shinmyo

Daiju Hasegawa

Toshiyuki Uemura

Yoshimasa Machida

Norio Minami

Naoyuki Shimomura

Yoshiharu Yamanishi

Kozo Akasaka

Masahiro Yonaga

Toshikazu Shimizu

Ikuo Kushida

Yuki Komatsu

Kunizo Higurashi

Atsushi Nagaoka

Toru Watanabe

Shinji Hatakeyama

Takahisa Hanada

Takuma Minamisono

Tatsuto Fukushima

Shinichi Tsukuba Res Lab Eisai Co Ltd Hamaoka

Tadashi c/o Tsukuba Research Laboratories Okabe

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

A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein Ring A represents a five-membered aromatic heterocyclic group or the like fused with a non-aromatic ring group, which may be substituted, Ring B represents a phenyl group or the like which may be substituted, X1 represents a single bond or the like, R1 and R2 each represent a C1-6 alkyl group or the like, m represents an integer of 0 to 3, and n represents an integer of 0 to 2, is effective as a therapeutic agent for a disease caused by A&#x3b2;. 

Nitrogen-containing fused heterocyclic compounds and their use as beta amyloid production inhibitors

The present invention provides a crystal of a 1.5 D-tartrate of a compound represented by the formula (1) having an A production inhibitory effect, characterized in that the crystal has a diffraction peak at a diffraction angle (20.2) of 23.2 in powder X-ray diffractometry; a crystal of a disulfate of the compound of the formula (1), characterized in that the crystal has a diffraction peak at a diffraction angle (20.2) of 17.1 in powder X-ray diffractometry; various other salts of the compound of the formula (1); crystal polymorphs of these salts; and the like, which are expected to be used as drug substances. 

Salt of tetrahydrotriazolopyridine derivative and crystal thereof

The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Rand Rare the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R' represents 1 to 4 independent hydrogen atoms and the like; and R&#x2033; represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.

Selective estrogen receptor modulator

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

The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like;&#x2003;&#x2003;(I-1)formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Rand Rare the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R' represents 1 to 4 independent hydrogen atoms and the like; and R&#x2033; represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.

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;.

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.

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Tsukuba, Japan

Noritaka Kitazawa