Tanabe Seiyaku Company, Limited

Taku Nagao

Hiromichi Nakajima

Mikio Takeda

Tokuro Oh-ishi

Muneyoshi Ikezaki

Nobuo Ito

Masao Hoshiyama

Yasushi Okazaki

Hideo Nakai

Hiroshi Wada

Hideo Yabana

Isao Yamaguchi

Kohki Takashima

Hiroshi Narita

Hirozumi Inoue

Masanori Sato

Norihide Umino

Akiyoshi Kawai

Tetsuji Mori

Yoshiaki Akimoto

Yashushi Okazaki

Tokuro Ohishi

Novel 1,5-benzothiazepine derivatives of the formula: ##STR1## wherein X is hydrogen atom, a halogen atom or a lower alkyl group; R.sup.1 is a lower alkyl group or a lower alkoxy group; R.sup.2 is hydrogen atom, a lower alkyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted phenyl-lower alkyl grup or a diphenyl-lower alkyl group; R.sup.3 is a lower alkyl group or a substituted or unsubstituted phenyl-lower alkyl group, Q is single bond, or an alkylene or lower alkenylene group which may optionally be substituted by a lower alkoxy group or oxo group; R.sup.4 is (i) hydrogen atom, (ii) a lower alkyl group, (iii) an N-phenyl-N-lower alkylamino group, (iv) a phenyl, phenyloxy, phenylthio, benzenesulfonylamino, 1,4-benzoquinonyl or benzylthio group which may optionally have substituent, or (v) a heterocyclic group which may optionally have substituent; and n is 2 or 3, or a pharmaceutically acceptable salt thereof, which are useful as a calcium antagonist, and the process for preparing thereof.

1,5-benzothiazepine derivatives and preparation thereof

Disclosed is a method for producing a renal function-improving and diuretic effects on a warm-blooded animal which comprises administering to the warm-blooded animal a therapeutically effective amount of 2-(4-methoxyphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-8-chloro-2,3-dihy dro-1,5-benzothiazepin-4(5H)-one or a pharmaceutically acceptable acid addition salt thereof.

Method of producing renal function-improving effect and diuretic effect

Disclosed are a pharmaceutical composition for improving the constitution of lipids in blood, which comprises as an active ingredient 2-(4-methoxyphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-8-chloro-2,3-dihy dro-1,5-benzothiazepin-4(5H)-one or a pharmaceutically acceptable acid addition salt thereof, use of the compound for preparing the pharmaceutical composition and a method of improving the constitution of lipids in blood.

Pharmaceutical composition for improving constitution of lipids in blood

A novel thiazolidine derivative of the formula: ##STR1## wherein R.sup.1 is a substituted or unsubstituted phenyl group, R.sup.2 is hydrogen or a lower alkyl group, R.sup.3 is hydrogen, a lower alkyl group or a lower alkanoyl group, Q is a single bond or a lower alkylene group, Alk is a lower alkylene group, Y and Z are the same or different and are oxygen atom or sulfur atom and the group of the formula: ##STR2## is either ##STR3## or a pharmaceutically acceptable salt thereof, which is useful as a cardiotonic agent is disclosed together with processes for the preparation of the compound and a pharmaceutical composition containing said compound.

Thiazolidine derivatives

A novel thiazolidine derivative of the formula: ##STR1## wherein R.sup.1 is a substituted or unsubstituted phenyl group, Q is a single bond, a lower alkylene group or a lower alkenylene group, R.sup.2 and R.sup.3 are the same or different and each is hydrogen atom, a lower alkyl group, a cycloalkyl group, a lower alkanoyl group, a lower alkoxycarbonyl group, a lower alkylsulfonyl group, a benzoyl group, a phenyl group or a di(lower alkyl)phosphoryl group, Alk is a lower alkylene group, and Y and Z are the same or different and each is oxygen atom or sulfur atom, or a pharmaceutically acceptable salt thereof, which is useful as a cardiotonic agent is disclosed together with processes for the preparation of the compound and a pharmaceutical composition containing said compound.

N-substituted-2-[2-[2-(4-p

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 alkanoyl of one to 20 carbon atoms, benzoyl or lower alkyl-benzoyl, and processes for preparation thereof are disclosed. Said compound (I) and a pharmaceutically acceptable acid addition salt thereof are useful as a cardiotonic agent.

Novel benzylalcohol derivatives and processes for preparing same

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.

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Tokyo, Japan

Taku Nagao