Tanabe Seiyaku Company, Limited

Mikio Takeda

Taku Nagao

Hiromichi Nakajima

Tokuro Oh-ishi

Yasushi Honma

Kei Tsuzurahara

Kenji Tsujihara

Yoshihisa Arai

Hajime Tamaki

Hiroshi Wada

Takashi Ochiai

Hirozumi Inoue

Masaru Inage

Goro Hayashi

Seiichi Nurimoto

Tamio Morikawa

This invention relates to imidazolidinone compounds of the formula ##STR1## wherein Q is methylene group or a single bond:

Imidazolidinones as brain activators

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 nitrosourea compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl and R.sup.2 is lower alkyl or lower alkoxy-lower alkyl, which may be prepared by nitrosation of a compound of the formula: ##STR2## wherein R.sup.1 and R.sup.2 are the same as defined above. Said nitrosourea compound is useful as an anti-tumor or anti-leukemic agent.

Nitrosourea derivative and process for preparing same

A 2-pyridinecarboxamide derivative of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy, halogen, lower alkyl-thio or nitro and is in the 3rd-, 4th- or 5th-position of the pyridyl group, and R.sup.2 is hydrogen, lower alkyl, lower alkoxy, phenoxy, phenyl-lower alkyl, phenyl-lower alkenyl, or halogen. Said 2-pyridinecarboxamide derivative (I) or a pharmaceutically acceptable salt thereof is useful as an anti-allergic agent.

2-Pyridinecarboxamide derivatives compositions containing same and

N-(5-Tetrazolyl)-6-phenyl-2-pyridinecarboxamide derivatives of the formula: ##STR1## wherein R is hydrogen, a halogen, a lower alkyl or a lower alkoxy, and the phenyl ring A is a phenyl having a substituent selected from the group consisting of amino, a mono(lower)alkylamino, a di(lower)alkylamino, or a lower aliphatic acylamino, and a pharmaceutically acceptable salt thereof, and process for the preparation thereof. Said pyridinecarboxamide derivatives have excellent anti-allergic activities even by oral administration and are useful as an anti-allergic medicine.

Pyridinecarboxamide derivatives and process for the preparation thereof

A compound of the formula: ##SPC1## Wherein R.sup.1 is hydrogen, phenyl, alkyl of one to five carbon atoms, cycloalkyl of three to four carbon atoms, or alkyl of one to five carbon atoms having a substituent selected from the group consisting of phenyl, benzoyl and 4-fluorobenzoyl, R.sup.2 is hydrogen or alkyl of one to three carbon atoms, and R.sup.3 is hydrogen, alkanoyl of two to six carbon atoms, benzoyl or nicotinoyl, is disclosed. Several methods for preparing the compound (I) is also disclosed. The compound (I) and a pharmaceutically acceptable acid addition salt thereof are useful as analgesic agents.

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Urawa, Japan

Mikio Takeda