Eisai R&d Management Co., Ltd.

Daisuke Iida

Masato Ueda

Tetsuya Kawahara

Junichi Nagakawa

Hitoshi Harada

Shuhei Miyazawa

Nobuhisa Watanabe

Atsuhiko Kubota

Masanobu Shinoda

Shinsuke Hirota

Hiroki Terauchi

Keigo Tanaka

Richard S Clark

Yoshihiko Kotake

Osamu Asano

Hideaki Fujisaki

Naoki Yoneda

Fumiyoshi Matsuura

Hiroshi Azuma

Norio Murai

Nobuyuki Yasuda

Masahiro Yasuda

Takashi Fukuyama

Makoto Nakagawa

Wataru Itano

So Yasui

Toshiyuki Ohfusa

Yasuaki Kamada

Yasuhiro Kabasawa

Kazuo Hirota

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 compound represented by the formula (I) or a salt thereof: wherein a ring Z is a 5 to 6-membered heteroaromatic ring having one or two heteroatoms in the ring; Xis a hydrogen atom, a hydroxy group, a hydroxy Calkyl group, &#x2014;B(OH), a boronate ester group, a cyclic boronate ester group, a boranyl group, a cyclic boranyl group, &#x2014;BFM, &#x2014;Sn(R)(R)(R), a leaving group, a carboxy group, a formyl group, or &#x2014;NRR; and Xis a hydrogen atom or &#x2014;COR.

Hetero-fused cyclic 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

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 having excellent adenosine receptor (A, A, Areceptor) antagonistic action, of the following formula, a salt thereof or a solvate of them: wherein, Rand R, same or different, each represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, an aromatic hydrocarbon cyclic group, an acyl group or an alkylsulfonyl group, which groups may be substituted (except the hydrogen atom); Rrepresents a hydrogen atom, a halogen atom, a cyano group, an alkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon cyclic group, a nitrogen atom, an oxygen atom or a sulfur atom, which groups may be substituted (except the hydrogen atom, the halogen atom and the cyano group); Rrepresents an aromatic hydrocarbon cyclic group which may be substituted, and Rrepresents an aromatic hydrocarbon cyclic group which may be substituted.

Pyrimidine compound and medicinal composition thereof

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Tsukuba, Japan

Daisuke Iida