Tanabe Seiyaku Company, Limited

Katsuo Ikezawa

Takeo Iwakuma

Yasuhiko Sasaki

Akio Odawara

Tatsuzo Ukita

Shinsuke Yamagata

Harumichi Kohno

Hideo Kikkawa

Tameo Iwasaki

Kazuhiko Kondo

Muneyoshi Ikezaki

Yasuo Sekine

Kazuaki Naito

Hirozumi Inoue

Kei Tsuzurahara

Norihide Umino

Masanori Sato

Osasi Takaiti

Tomofumi Uchida

Kunihiko Irie

Akira Tsunashima

Masakatsu Sugahara

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

A pyridine derivative of the formula (I): ##STR1## wherein A is group of the following formulae: ##STR2## (R.sup.1 and R.sup.2 are each H, or protected or unprotected OH, R.sup.31, R.sup.41 and R.sup.42 are protected or unprotected hydroxymethyl, R.sup.32 is H, lower alkyl, or protected or unprotected hydroxymethyl, R.sup.33 is substituted or unsubstituted lower alkyl, and the dotted line means the presence or absence of a double bond), R.sup.5 and R.sup.6 are H, or protected or unprotected amino, or both combine together with the adjacent nitrogen to form substituted or unsubstituted heterocycle, or a pharmaceutically acceptable salt thereof, these compounds showing excellent bronchoconstriction inhibitory activity and/or anti-inflammatory activity of airway, and being useful in the prophylaxis or treatment of asthma.

Pyridine derivatives

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.

Naphthalene derivatives, processes for preparing the same, and synthetic

Method for the treatment or prophylaxis of thromboses or asthma in warm-blooded animal which comprises administering an effective amount of a compound having the formula: ##STR1## wherein R.sup.1 is phenyl group or phenyl group substituted by a member selected from the group consisting of C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, halogen atom, trifluoromethyl, and nitro, or naphthyl group, and R.sup.2 is hydroxymethyl or a group of the formula: ##STR2## wherein R.sup.3 is hydrogen atom or C.sub.1 -C.sub.5 alkyl and R.sup.4 is C.sub.3 -C.sub.6 cycloalkyl, C.sub.2 -C.sub.6 alkoxycarbonyl-phenyl, carboxy-phenyl, C.sub.1 -C.sub.5 alkyl, or C.sub.1 -C.sub.5 alkyl having a substituent selected from C.sub.1 -C.sub.5 alkoxycarbonyl, carboxy, C.sub.2 -C.sub.6 alkoxycarbonyl-phenyl, carboxy-phenyl, C.sub.2 -C.sub.6 alkoxycarbonyl-(C.sub.3 -C.sub.6) cycloalkyl and carboxy-(C.sub.3 -C.sub.6) cycloalkyl, or a pharmaceutically acceptable salt thereof to said warm blooded animal.

Indan derivatives used for treating thromboses or asthma

There are disclosed a 4-aminophenol derivative of the formula: ##STR1## (wherein R.sup.1 and R.sup.2 each represent a lower alkyl group, Y represents a single bonding arm, a lower alkylene group or a lower alkenylene group, R.sup.3 represents a thienyl group or pyrrolyl group which may be also substituted with a lower alkyl group; benzothienyl group, indolyl group; or a phenol group which is substituted with 1 to 2 groups selected from a lower alkoxy group and a lower alkanoyloxy group; or Y-R.sup.3 represents integrally an alkyl group with 6 to 9 carbon atoms; or a hydrocarbon group with 5 to 14 carbon atoms having 2 or 3 double bonds) or a pharmacologically acceptable salt thereof, and processes for preparing the same.

4-aminophenol derivatives and processes for preparing the same

Indan derivatives of the formula: ##STR1## wherein R.sup.1 is substituted or unsubstituted phenyl, naphthyl or sulfur-containing heterocyclic group, and R.sup.2 is hydroxy-methyl or a group of the formula: ##STR2## wherein R.sup.3 is hydrogen atom or lower alkyl and R.sup.4 is cycloalkyl, lower alkoxycarbonyl-phenyl, carboxy-phenyl, nitrogen-containing heterocyclic group, lower alkyl, or lower alkyl having a substituent selected from lower alkoxycarbonyl, carboxy, lower alkoxycarbonyl-phenyl, carboxy-phenyl, lower alkoxycarbonyl-cycloalkyl and carboxy-cycloalkyl, or a pharmaceutically acceptable salt thereof, which are useful as a platelet aggregation-inhibiting agent and as an agent for the treatment, amelioration and/or prophylaxis of a variety of thrombosis or embolism, coronary and cerebral vascular smooth muscle vellication, asthma, and the like, processes for the preparation thereof, and pharmaceutical composition containing said compound as an active ingredient.

Indan derivatives and pharmaceutical preparation thereof

Novel indanoxyacetic acid derivatives of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group, a substituted or unsubstituted phenyl group, naphtyl group or a sulfur-containing heterocyclic group, R.sup.2 is hydroxy group or a protected hydroxy group, p is an integer of 2 or 3, and q is an integer of 0 or 1, and a salt thereof are disclosed. Said derivative (I) and a salt thereof are useful as a platelet aggregation-inhibiting agent and an agent for the treatment, amelioration and/or prophylaxis of a variety of thrombosis, embolism, coronary and cerebral vascular smooth muscl vellication, asthma, and the like.

Indanoxyacetic acid derivatives

There are disclosed are glycine derivative of the formula: ##STR1## (wherein R.sup.1 represents a substituted or unsubstituted phenyl group, R.sup.2 represents a carboxyl group which may be protected, Q represents a lower alkylene group and m represents 0 or 1) or a pharmacologically acceptable salt thereof and a process for preparing the same.

Glycine derivative and pharmaceutical preparation thereof

A novel carbostyril derivative of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof, and a process for preparing same. The compound (I) shows potent bronchodilating activity and is useful as a bronchodilator.

Bronchodilating

A novel 5,7-dihydroxytetrahydroisoquinoline derivative having the formula: ##STR1## wherein R is trimethoxyphenyl, is prepared either by hydrolysis of a compound having the formula: ##STR2## wherein R.sup.1 is an organic acyl group and R is same as above, or by catalytic hydrogenation of a compound having the formula: ##STR3## wherein R.sup.3 is hydrogen or benzyl and R is same as above. The 5,7-dihydroxytetrahydroisoquinoline derivative (I) or a pharmaceutically acceptable acid addition salt thereof is useful as a bronchodilator.

Growing community of inventors

Urawa, Japan

Katsuo Ikezawa