Meiji Seika Kaisha, Ltd.

Meji Seika Kaisha Ltd.

Sachiko Miyamoto

Yumiko Okada

Yasuo Ohtsuka

Kenichi Fushihara

Takashi Shishikura

Mami Kawaguchi

Sohjiro Shiokawa

Toshio Nishizuka

Seiji Tsutsumi

Toyoaki Ishikura

Hideo Kitagawa

Hiromi Takata

Maki Shiobara

Shin-Ichi Kitahara

Hanae Furukawa

Toshihiro Yamaguchi

Tricyclic triazolobenzazepine derivatives in the form or a prodrug are provided. The compounds according to the present invention are those represented by formula (I) and pharmacologically acceptable salts and solvates thereon. The compounds are useful as antiallergic agents and exhibit excellent bioavailability. wherein Rrepresents hydrogen, OH, alkyl or phenyl alkyl, 

Tricyclic triazolobenzazepine derivatives, process for producing the same, and antiallergic agents

A process for preparing a compound represented by formula (IIa')wherein Q represents group (i) as defined in the specification and Rto R, R, R, and Rare as defined in the specification, by (1) reacting a compound represented by formula (V)wherein Rto Rand Rare as defined in the specification. with a compound represented by RRC&#x2550;O wherein Rand Rare as defined in the specification; (2) reacting the compound prepared in (1) with a compound represented by R&#x2014;C(&#x2550;O)&#x2014;Rwherein Rand Reach independently represent a chlorine atom, 4-nitrophenyl, or 1-imidazolyl; and (3) reacting the compound prepared in (2) with a compound represented by ROH wherein Ris as defined in the specification.

Disclosed are novel crystalline 2-(1-isopropoxycarbonyloxy-2-methylpropyl)-7,8-dimethoxy-4(5H),10-dioxo-2H-1,2,3-triazolo[4,5-c][1]benzazepine and a pharmaceutical composition comprising the same.

Crystalline tricyclic triazolobenzazepine derivative

Tricyclic triazolobenzazepine derivatives, process for producing the same, and antiallergic

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Odawara, Japan

Sachiko Miyamoto