Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Makoto Kotake

Naoki Yoneda

Tomohiro Matsushima

Toshiyuki Matsuoka

Akifumi Kimura

Tetsuya Kawahara

Jean-Christophe P Harmange

Mark Spyvee

Kenzo Muramoto

Kazutoshi Miyake

Hitoshi Oinuma

Satoshi Yamamoto

Atsushi Inoue

Yoshiyuki Kawakami

Kenichi Chiba

Shinsuke Hirota

Hiroshi Shirota

Hong Du

Mamoru Saito

Fabian Gusovsky

Shinji Suda

Yoshiharu Mizui

Isao Tanaka

Masaki Goto

Yoshihito Eguchi

Yoshikazu Kuboi

John (Yuan) Wang

Hideki Sakurai

Masanori Fujita

Takatoshi Kawai

Masayuki Namiki

Takeshi Sudo

Megumi Kawada

Yong-Chun Shen

Richard S Clark

Fumihiro Ozaki

Nobuaki Sato

Hideyuki Adachi

Fumiyoshi Matsuura

Itaru Tsukada

Yimin Jiang

Shigeru Souda

Toru Watanabe

Seiichi Kobayashi

Mitsuaki Miyamoto

Kazuo Okano

Makoto Okita

Akiharu Kajiwara

Ieharu Hishinuma

Masanobu Shinoda

Roch Boivin

Hiroshi Tanaka

Atsushi Kamada

Yoshio Fukuda

Taro Terauchi

Masanori Mizuno

Xiang-Yi Li

Yu Yoshida

Yoichi Kita

Yoshimitsu Naoe

Shuichi Suzuki

Jesse Chow

Osamu Ito

Motoji Kogushi

Charles-André Lemelin

Hiroko Kobayashi

Masayoshi Ohkuro

Ken-ichi Chiba

Naoto Ono

Syuhei Miyazawa

Yoshiaki Oohashi

Kenji Hayashi

Tsutomu Kawata

Kogyoku Shin

Nobuyuki Mori

Kunitoshi Takeda

Takafumi Motoki

Yoshiaki Ohashi

Keiichi Sorimachi

Takashi Musha

Takashi Fukuyama

Yoshihisa Kobayashi

Yasuaki Kamada

Toshiyuki Ohfusa

Ray Wood

Tomoyuki Shibuguchi

Takashi Musya

Tsutomu Kawada

Taro Asaba

Toshiki Kurokawa

Hironori Fukumoto

Katsunobu Osada

John (yuan) Wang

Provided are compounds represented by the following formulas (I), (II), (III) and (IV) having orexin type 2 receptor-activating activity, or their pharmaceutically acceptable salts. 

Substituted piperidine compounds and their use

Compounds represented by formulae (I) to (XXII) or pharmaceutically acceptable salts thereof: 

Pyranodipyridine compound

The present invention provides methods for the use of compounds having formula (I) in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis, wherein R-R, t, X, Y, Z, and n are as defined herein.

Macrocyclic compounds useful as pharmaceuticals

The present invention provides compositions comprising compounds having formula (I): 

Salts and crystals of 1-cyclopropylmethyl-4-[2-(3,3,5,5-tetramethylcyclohexyl)phenyl]piperazine have excellent cell adhesion inhibitory action and cell infiltration inhibitory action, and are useful as therapeutic or prophylactic agents for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome, rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis.

Crystal and salt of 1-cyclopropylmethyl-4-[2-(3,3,5,5-tetramethylcyclohexyl)phenyl]piperazine

The present invention provides compounds having formula (I): 

In one aspect, the present invention provides compounds having formula (1) or (100), a salt thereof or a hydrate of the foregoing, which compounds exhibit excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and are useful as therapeutic or prophylactic agents for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome; rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis.  wherein R10 represents optionally substituted cycloalkyl, etc., R20-23 represent hydrogen, alkyl, alkoxy, etc., R30-32 represent hydrogen, alkyl, oxo, etc., and R40 represents optionally substituted alkyl, etc.

1,2-di(cyclic)substituted benzene compounds

A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and is useful as a therapeutic or prophylactic agent for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome, rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. 

A 2-iminoimidazole derivative represented by the formula: {wherein R, Rand Rrepresent hydrogen, optionally substituted Calkyl, etc.; Rrepresents hydrogen, Calkyl, Calkyloxycarbonyl, etc.; Yrepresents a single bond, &#x2014;CH&#x2014;, etc.; Yrepresents a single bond, &#x2014;CO&#x2014;, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R&#x2013;Rrepresent hydrogen, Calkyl, hydroxyl, Calkoxy, etc., and Rand Ror Rand Rmay bond together to form a 5- to 8-membered heterocycle], etc.}or salt thereof.

2-iminoimidazole derivatives (2)

A 2-iminopyrrolidine derivative represented by the formula: {wherein ring B represents a benzene ring, pyridine ring, etc.; R&#x2013;Rrepresent hydrogen, halogen, Calkyl, etc.; Rrepresents hydrogen, Calkyl, Calkoxy-Calkyl, etc.; Rrepresents hydrogen, Calkyl, Calkyloxycarbonyl, etc.; Yrepresents a single bond, &#x2014;CH&#x2014;, etc.; Yrepresents a single bond, &#x2014;CO&#x2014;, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R&#x2014;Rrepresent hydrogen, Calkyl, hydroxyl, Calkoxy, etc.; and Rand Ror Rand Rmay bond together to form a 5- to 8-membered heterocyclic ring], etc.},or a salt thereof.

2-iminopyrrolidine derivatives

The present invention relates to a substituted thiazolo[3,2-a] azepine derivative having inhibitory activity against angiotensin I converting enzyme and neutral endpeptidase and is represented by the following general formula (I): ##STR1##

Substituted thiazolo[3,2-a]azepine derivatives

Substituted thiazolo �3,2-a!azepine derivatives

The present invention relates to an amino acid derivative having an angiotensin I-converting enzyme inhibition activity, a vasopressin antagonism and an atrial natriuretic peptide hydrolase inhibition activity. This amino acid derivative is represented by the following general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or an acyl group; R.sup.2 represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, an ary group which may have a substituent, a heteroaryl group which may have a substituent, an arylalkyl group which may have a substituent or a heteroarylalkyl group which may have a substituent;

Amino acid derivative

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Tsukuba, Japan

Makoto Kotake