Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Tetsuya Kawahara

Isao Yamatsu

Kazuo Okano

Shuhei Miyazawa

Shinya Abe

Koukichi Harada

Hiroyuki Yoshimura

Mitsuaki Miyamoto

Naoyuki Shimomura

Richard S Clark

Shigeru Souda

Yoshimasa Machida

Kenzo Muramoto

Osamu Asano

Kouichi Katayama

Masanobu Shinoda

Satoshi Katayama

Kouji Yamada

Hiroshi Obaishi

Hajime Tsunoda

Yoshimori Sakuma

Takashi Inoue

Tsutomu Kawata

Takeshi Suzuki

Shigeki Hibi

Katsuya Tagami

Yasushi Okamoto

Makoto Kotake

Junsaku Nagaoka

Naoki Kobayashi

Tsutomu Yoshimura

Hiromasa Suzuki

Hirotoshi Numata

Fumihiro Ozaki

Takashi Yamanaka

Manabu Murakami

Naoki Yoneda

Fumiyoshi Matsuura

Atsushi Kamada

Kiyoshi Oketani

Shinsuke Hirota

Kenichi Chiba

Ryoichi Hashida

Toru Horie

Takashi Mori

Daisuke Iida

Kenichi Kusube

Masayoshi Ohkuro

Masato Ueda

Nobuaki Sato

Akiharu Kajiwara

Nobuhisa Watanabe

Ieharu Hishinuma

Atsuhiko Kubota

Junichi Nagakawa

Hitoshi Harada

Hiroshi Tanaka

Itaru Tsukada

Hideaki Fujisaki

Taro Terauchi

Hiroshi Shirota

Toshiyuki Matsuoka

Yoshimitsu Naoe

Shuichi Suzuki

Osamu Ito

Motoji Kogushi

Akifumi Kimura

Hiroko Kobayashi

Ken-ichi Chiba

Naoto Ono

Syuhei Miyazawa

Yoshiaki Oohashi

Hiroki Terauchi

Toshihiko Kaneko

Kenji Hayashi

Kozo Akasaka

Koichi Abe

Norihito Ohi

Kaname Miyamoto

Hiroshi Ishihara

Masayuki Tanaka

Hiromitsu Yokohama

Yoshinori Sakuma

Takashi Musha

So Yasui

Tohru Arai

Yasuaki Kamada

Toshiyuki Ohfusa

Hirsohi Shirota

Richar S Clark

Naoyuki Kimomura

Takashi Musya

Tsutomu Kawada

Osamu Takenaka

Jiro Sonoda

Sachiko Kikuchi

Ken-Ichi Chiba

The disclosure provides pyrazolo[1,5-a]pyrimidine compounds, and pharmaceutically acceptable salts thereof, having protease-activated receptor 2 (PAR2) inhibitory action, pharmaceutical compositions containing the same, and methods of treatment using the same.

Pyrazolo[1,5-a]pyrimidine compound

A novel chemical compound useful as a therapeutic or prophylactic agent for acid-related diseases is provided, which has an excellent inhibitory effect against gastric acid secretion, an excellent effect of maintaining the inhibitory effect against gastric acid secretion, thereby maintaining intragastric pH high for a long time, and having more safety and appropriate physicochemical stability. Provided is a compound represented by where Rand Rmay be the same or different and each represent a hydrogen atom or a C1-C6 alkyl group; Rrepresents (5,5-dimethyl-1,3-dioxan-2-yl)methoxy group, 5,7-dioxaspiro[2.5]oct-6-ylmethoxy group, 1,5,9-trioxaspiro[5.5]undec-3-ylmethoxy group, or (2,2-dimethyl-1,3-dioxan-5-yl)methoxy group; R, R, Rand Rrepresent a hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 haloalkyl group, C1-C6 alkoxy group or C1-C6 haloalkoxy group; and Wrepresents a single bond, methylene or ethylene group, a salt thereof or a solvate of these.

Benzimidazole compound

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

An object of the present invention is to provide a novel chemical compound useful as a therapeutic or prophylactic agent for acid-related diseases, having an excellent inhibitory effect against gastric acid secretion, an excellent effect of maintaining the inhibitory effect against gastric acid secretion, thereby maintaining intragastric pH high for a long time, and having more safety and appropriate physicochemical stability. Provided is a compound represented by 

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

Benzopiperidine derivatives

A benzothiazole derivative or a pharmacologically acceptable salt thereof of the following formula, as defined in the claims, which is useful as a preventive or therapeutic agent for diseases on which functions of suppressing leukotrienes and thromboxanes production are effective: ##STR1##

Benzothiazole compounds which are substituted by pyridymethyl

A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are useful in the pharmaceutical field, especially in treating allergic diseases. ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or an alkyl, R.sup.3 is hydrogen or a halogen, R.sup.4 is hydrogen or an alkyl, X is --OCO--, and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.

1,4-diazepine derivative and its pharmaceutical use

A glycerin derivative having the following formula (I) or (I') and a pharmacologically acceptable salt thereof are useful to treat diseases caused by the platelet activating factor. ##STR1##

Glycerin derivative and its pharmacological use

A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases. ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or an alkyl, R.sup.3 is hydrogen or a halogen, R.sup.4 is hydrogen or an alkyl, X is --OCO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.

A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases. ##STR1## in which R1 and R2 are hydrogen or an alkyl, R3 is hydrogen or a halogen, R4 is hydrogen or an alkyl, X is --OOO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.

A benzothiazole derivative or a pharmacologically acceptable salt thereof which is useful as a preventive or therapeutic agent for diseases on which functions of suppressing leukotrienes and thromboxanes production are effective. A benzothiazole derivative represented by the following general formula (I): ##STR1##

Pyridyl substituted benzothiazole compounds which have useful

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Ibaraki, Japan

Tetsuya Kawahara