Tanabe Seiyaku Company, Limited

Hiromichi Nakajima

Taku Nagao

Mikio Takeda

Tokuro Oh-ishi

Nobuo Ito

Muneyoshi Ikezaki

Masao Hoshiyama

Yasushi Okazaki

Yashushi Okazaki

Novel 1,5-benzothiazepine derivative of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkanoyl and each of R.sup.2 and R.sup.3 is lower alkyl, and a pharmaceutically acceptable acid addition salt thereof are disclosed. Said derivative (I) and a salt thereof are useful as a hypotensive agent and/or a cerebral or coronary vasodilator.

Novel 9-chloro-1,5-benzothiazepine derivatives and their pharmaceutical

Novel 1,5-benzothiazepine derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.4 are:

1,5-benzothiazepine derivative

Novel 1,5-benzothiazepine derivatives of the formula: ##STR1## wherein R.sup.1 is lower alkyl or lower alkoxy, R.sup.2 is hydrogen atom or lower alkanoyl, each one of R.sup.3 and R.sup.4 is lower alkyl, Ring A is a substituted benzene ring of the formula: ##STR2## R.sup.a is lower alkyl, lower alkoxy, lower alkylthio or benzyloxy, each one of R.sup.b and R.sup.c is lower alkyl, lower alkoxy or halogen atom, and either one of R.sup.d and R.sup.e is fluorine atom and the other one is hydrogen atom, or a pharmaceutically acceptable acid addition salt thereof are disclosed. Said derivative (I) and its salt are useful as a hypotensive agent and/or a cerebral or coronary vasodilator.

1,5-benzothiazepine derivatives and their pharmaceutical use

Novel 1,5-benzothiazepine derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl, R.sup.2 is hydrogen, lower alkanoyl or benzyl, R.sup.3 is hydrogen or lower alkyl and either one of R.sup.4 and R.sup.5 is hydrogen and the other is chlorine, or a pharmaceutically acceptable acid addition salt thereof are disclosed. Said derivative (I) and its salt have a potent platelet aggregation-inhibiting activity.

1,5-benzothiazepine derivatives and processes for preparing the same

Novel 8-chloro-1,5-benzothiazepine derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl or a group of the formula: R.sup.4 CO--, each of R.sup.2 and R.sup.3 is lower alkyl and R.sup.4 is hydrogen or lower alkyl, and a pharmaceutically acceptable acid addition salt thereof are disclosed. Said derivative (I) and a pharmaceutically acceptable acid addition salt thereof are useful as hypotensive agents and/or coronary or cerebral vasodilators.

8-Chloro-1,5-benzothiazepine derivatives

A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl, R.sup.3 is hydrogen, lower alkyl or hydroxy-lower alkyl, R.sup.4 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkylthio or nitro, and A is lower alkylene, is disclosed. Said compound (I) and a pharmaceutically acceptable acid addition salt thereof are useful as cerebral or coronary vasodilators.

1,5-Benzothiazepin-4-one, their pharmaceutical compositoins, and methods

A compound of the formula: ##STR1## wherein R is lower alkyl, may be prepared, for example, by reducing a compound of the formula: ##STR2## wherein R is same as above. Other methods for preparing the compound [I] are also disclosed. The compound [I] and a pharmaceutically acceptable acid addition salt thereof are useful as anti-diabetic agents.

Novel benzylalcohol derivatives and processes for preparing the same

A compound having the formula: ##STR1## wherein Ring A is monohydroxyphenyl, or a pharmaceutically acceptable acid addition salt thereof is prepared by catalytic hydrogenation of a compound having the formula: ##STR2## wherein A' is monobenzyloxyphenyl, and Y is carbonyl or hydroxymethylene. The compound (I) in which Ring A is 4-hydroxyphenyl or 3-hydroxyphenyl is useful as a cardiotonic agent. On the other hand, the compound (I) in which Ring A is 2-hydroxyphenyl is useful as an anti-diabetic agent.

Novel benzylalcohol derivatives as antidiabetics and cardiotonics

Benzylalcohol amine derivatives

A compound of the formula: ##SPC1## Wherein Ring A' is dibenzyloxyphenyl and Y is carbonyl or hydroxymethylene, is subjected to catalytic hydrogenation. A compound of the formula: ##SPC2## Wherein Ring A is dihydroxyphenyl, is produced. The product is useful as a cardiotonic agent. It is also characterized by the high potency ratio of adrenergic .beta..sub.1 -receptor stimulating activity to adrenergic .beta..sub.2 -receptor stimulating activity.

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Urawa, Japan

Hiromichi Nakajima