Chugai Seiyaku Kabushiki Kaisha

Yasuhiro Ohba

Kazushige Sakai

Yoshiaki Kato

Isao Matsunaga

Osamu Cynshi

Tamotsu Yamazaki

Kunio Tamura

Shun-Ichi Hata

Mitsutaka Yoshida

Minoru Shindo

Noboru Kubodera

Shun-ichi Hata

Hiroyuki Nabata

Hiroyuki Nagano

Yugo Ikeda

Yasumi Uchida

Mitiro Takagi

Yasuyuki Shiraki

Yasushi Murakami

Masuo Koizumi

Shigeru Takanashi

Michitaka Akima

Yasuo Fujimura

Sadao Tanaka

Matsunaga Isao

Tanaka Sadao

Fujimura Yasuo

Kiyohiko Ito

Jinichiro Aono

Compounds represented by the general formula (I), as well as intermediates for the synthesis of thereof: ##STR1## where R.sup.1 is a hydrogen atom or an acyl group; R.sup.2 is a lower alkyl group; R.sup.3 is a hydrogen atom or a lower alkyl group; R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are a hydrogen atom or an optionally substituted alkyl, alkenyl, alkynyl or aryl group; R.sup.2 and R.sup.4, when taken together, may form a 5-membered ring; R.sup.5 and R.sup.6, when taken together, may form a cycloalkyl group or a heterocyclic group in which at least one methylene on the ring of a cycloalkyl group is substituted by an oxygen atom, a sulfur atom or an alkyl-substituted nitrogen atom, provided that R.sup.6 is not present if the ring formed by R.sup.2 and R.sup.4 taken together is a benzofuran ring. The compounds represented by the general formula (I) have a highly selective anti-oxidative activity and are useful as therapeutics of ischemic diseases such as arteriosclerosis and myocardial infarction.

4-alkoxy-2, 6-di-t-butylphenol derivatives

4,6-Di-t-butyl-dihydrobenzofuran-5-ol and its derivatives

Phenylpiperazine derivatives of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a straight- or branched-chain saturated or unsaturated alkyl group having 1 to 8 carbon atoms which may be substituted at any position by a hydroxyl group, a carboxyl group, a lower alkoxycarbonyl group or an oxo group; and R.sub.2 is a hydrogen atom, a halogen atom, a lower alkyl group or a sulfamoyl group, and a process for producing the same are disclosed. The derivatives of the formula have alpha blocking and serotonin antagonizing activities and are useful as a drug.

Phenyliperazine derivatives

Compounds of the formula ##STR1## (wherein R.sub.1 is a lower alkyl group, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, represent a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a trifluoromethyl group or a lower alkoxycarbonyl group; two adjacent groups of R.sub.2, R.sub.3 and R.sub.4 may combine to form a methylenedioxy group; n is an integer of 2 to 6) or salts thereof, are disclosed. These compounds are useful as agents for treating circulatory diseases because they have hypotensive action and are capable of increasing the cerebral blood flow, decreasing the heart rate and suppressing ventricular arrhythmia due to myocardial ischemia.

Method for treating circulatory diseases by using (2-lower

Pyrazoloindazole derivatives of the formula: ##STR1## [wherein R.sub.1 is a cyano group, carboxy group, a lower alkoxycarbonyl group or a group ##STR2## (wherein R.sub.2 and R.sub.3 are each a hydrogen atom, a lower alkyl group, a phenyl group which may have a substituent or when taken together with a nitrogen atom, form a heterocyclic ring); X.sup..crclbar. is a counter ion], a process for preparing the same and a pharamaceutical composition containing the same are disclosed. The compounds of the formula above have bronchodilating action and are useful as a medicine.

Pyrazoloindazole derivatives and pharmaceutical composition containing

Novel pyrazoloindazole derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxyl group or benzyloxyl group; R.sub.2 is a hydrogen atom, a halogen atom, a lower alkyl group or phenyl group (provided R.sub.1 and R.sub.2 are not hydrogen at the same time); and X.sup..crclbar. is a halide ion, a hydroxide ion, a methanesulfonate ion, a p-toluene sulfonate ion, a sulfate ion, a nitrate ion, a carbonate ion, an acetate ion, a benzoate ion or a salicylate ion, a process for preparing the derivatives, and a pharmaceutical composition containing the same are disclosed. The derivatives have good bronchodilating action for human without exhibiting substantially bad effects on the functioning of heart, and therefore, they are useful as a drug.

Pyrazoloindazole derivatives and bronchodilating composition

Dibenz[b,f][1,4]oxazepine derivatives of the formula ##STR1## (wherein R.sub.1 is a hydrogen atom or a lower alkyl group; R.sub.2 is a branched lower alkyl group; R.sub.3 is a hydrogen atom, a carboxyl group, a carbamoyl group, a lower alkoxycarbonyl group, or a lower alkoxy group; R.sub.4 and R.sub.5 are each a lower alkyl group or may, when taken together with a nitrogen atom, form a heterocyclic ring; and A is a lower alkylene group) or salts thereof, a process for preparing the same and pharmaceutical compositions comprising the same are disclosed. The derivatives of the formula above are effective to prevent and treat circulatory diseases, especially angina pectoris, and therefore, useful as medicines.

Dibenz[b,f][1,4]oxazepine derivatives, process for preparing the same,

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Kawasaki, Japan

Yasuhiro Ohba