Tanabe Seiyaku Company, Limited

Shinsuke Yamagata

Katsuo Ikezawa

Tatsuzo Ukita

Tameo Iwasaki

Kazuhiko Kondo

Hideo Kikkawa

Naphthalene derivatives of the formula &lsqb;I&rsqb;:

Naphthalene derivates, process for the preparation thereof, and intermediates therefor

Naphthalene derivatives of the formula [I]: wherein R.sup.1 and R.sup.2 are the same or different and are each H, protected or unprotected OH, one of R.sup.3 and R.sup.4 is protected or unprotected hydroxymethyl, and the other is H, lower alkyl, or protected or unprotected hydroxymethyl, R.sup.5 and R.sup.6 are the same or different and are each H, substituted or unsubstituted lower alkyl, substituted or unsubstituted phenyl or protected or unprotected NH.sub.2, or both combine together with the adjacent N to form substituted or unsubstituted heterocyclic group, and pharmaceutically acceptable salts thereof, these compounds showing excellent bronchoconstriction inhibitory activity, and hence, being useful in the prophylaxis or treatment of asthma.

Naphthalene derivatives, process for the preparation therof, and

Naphthalene derivatives of the formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are each H, protected or unprotected OH, one of R.sup.3 and R.sup.4 is protected or unprotected hydroxymethyl, and the other is H, lower alkyl, or protected or unprotected hydroxymethyl, R.sup.5 and R.sup.6 are the same or different and are each H, substituted or unsubstituted lower alkyl, substituted or unsubstituted phenyl or protected or unprotected NH.sub.2, or both combine together with the adjacent N to form substituted or unsubstituted heterocyclic group, and pharmaceutically acceptable salts thereof, these compounds showing excellent bronchoconstriction inhibitory activity, and hence, being useful in the prophylaxis or treatment of asthma.

Naphthalene derivatives, process for the preparation thereof, and

Naphthalene derivative of the formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen atom, hydroxy group, cyclo-lower alkyloxy group, substituted or unsubstituted lower alkoxy group, or both combine each other to form lower alkylenedioxy group, R.sup.3 is substituted or unsubstituted nitrogen-containing 6-membered heterocyclic group, and groups of the formulae: --OR.sup.4 and --OR.sup.5 are the same or different and are protected or unprotected hydroxy group, processes for preparing thereof, and synthetic intermediates therefor, these compounds have excellent bronchodilating activity, and are useful in the prophylaxis and treatment of asthma.

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Mishima-gun, Japan

Shinsuke Yamagata