Mochida Pharmaceutical Co., Ltd.

Hodogaya Chemical Co., Ltd.

Kazumi Nishijima

Akira Kikuchi

Masayuki Ohashi

Hidemitsu Nishida

Toshiyuki Shudo

Kazutoshi Yanagibashi

Kazuo Kato

Ei Mochida

Ichiro Yamamoto

Tatsuto Notso

Hitoshi Inaba

Kikuo Ohtomo

Tatsuto Notsu

The invention relates to novel pyridocarbazole derivatives having highly selective action in inhibiting cyclic GMP-phosphodiesterase (hereinafter abbreviated as cGMP-PDE), processes for producing such derivatives, agents containing at least one of such derivatives as an active ingredient for preventing and/or treating pulmonary hypertension, ischemic heart diseases or diseases against which the cGMP-PDE inhibitory action is effective, and intermediates useful for the production of pyridocarbazole derivatives.

Pyridocarbazole derivatives having cgmp-pde inhibitory activity

Pyridocarbazole derivatives having cGMP-PDE inhibitory activity

The present invention relates to novel 4,5-dihydro-6H-imidazo[4,5,1-ij]quinolin-6-one-6-oxime-O-sulfonic acid compounds, processes for producing said compounds, intermediate compounds, i.e. novel 4,5-dihydro-6H-imidazo[4,5,1-ij]quinolin-6-one compounds and 4,5-dihydro-6H-imidazo[4,5,1-ij]quinolin-6-one-6-oxime compounds in the synthesis of said compounds, processes for producing said intermediate compounds, and pharmaceutical or veterinary compositions containing said compounds. The present invention is based on the selection of the substituents of 4,5-dihydro-6H-imidazo[4,5,1-ij]-quinolin-6-one-6-oxime-O-sulfonic acid compounds at 2-position, namely 2-(2-penten-3-yl)-, 2-cyclohexyl-, 2-naphthyl-, 2-thienyl-, etc. The compounds of the present invention containing these substituents have potent hypotensive, anti-oedematous and diuretic effects as well as an activity of removing ascites. The compounds of the present invention are extremely useful for treatment of diseases and disorders mentioned above.

4,5-dihydro-6H-imidazo[4,5,1-ij]quinolin-6-one-6-oxime-O-sulfonic acid

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Tokyo, Japan

Kazumi Nishijima