Fujisawa Pharmaceutical Company, Ltd.

Other

Nippon Shokubai Co., Ltd.

Yoshinari Sato

Teruaki Matuo

Tsutomu Toyonaka Teraji

Takatomo Ogahara

Ikuo Ueda

Masaaki Matsuo

Youichi Shiokawa

Kazuo Okumura

Suminori Umio

Shizuo Maeno

Hitoshi Mitsui

Ikuyo Katsumi

Seiichiro Tabuchi

Kazuo Sakane

Masakazu Kobayashi

Osamu Nakaguti

Naoko Yamamoto

Yuichi Satoh

Benzodiazepine derivatives of the formula:

1,4-benzodiazepinones and their uses as CCK antagonists

Benzodiazepine derivatives

The invention relates to novel cholecystokinin antagonists of the formula ##STR1## wherein R.sup.1 is aryl or substituted aryl, and a pharmaceutically acceptable salt thereof useful as cholecystokinin antagonists.

Tricyclic compounds having cholecystokinin antagonist activity

The invention relates to a compound of the formula ##STR1## wherein R.sup.1 is aryl which may have suitable substituent(s), X is --O-- or ##STR2## in which R.sup.3 is hydrogen or lower alkyl, A is a bond or lower alkylene which may have lower alkyl group(s), and R.sup.2 is arylcarbamoyl which may have halogen or lower alkoxy, or a pharmaceutically acceptable salt thereof, useful as a cholecystokinin antagonist.

Tricyclic compounds

Intermediates of the formula: ##STR1## wherein R.sup.1 is tetrazolyl or imidazolyl, each of which may have an imino protective group,

Tricyclic benzodiazepine derivates, their preparation, and

A compound of the formula ##STR1## the process for its preparation and intermediate thereof. The compound is useful as a cholecystokinin antagonist.

The invention relates to novel cholecystokinin antagonists of the formula ##STR1## wherein R.sup.1 is aryl which may have suitable substituent(s), X is --O-- or ##STR2## in which R.sup.3 is hydrogen or lower alkyl, A is bond; or methylene, ethylene, trimethylene, tetramethylene, pentamethylene or hexamethylene, each of which may have lower alkyl group(s), and

The invention relates to a compound of the formula: ##STR1## wherein R.sup.1 is aryl which may have suitable substituents(s), X is --O-- or ##STR2## in which R.sup.3 is hydrogen or lower alkyl, A is a bond or lower alkylene which may have lower alkyl group(s), and

Tricyclo benzodiazepines are cholecystokinin antagonists.

This invention relates to new benzodiazepine derivatives and pharmaceutically acceptable salts thereof. More particularly, it relates to new benzodiazepine derivatives and pharmaceutically acceptable salts thereof which are cholecystokinin (CCK) antagonists and therefore can be used as therapeutical agents for emesis, pancreatitis, satiety and appetite control, pain control, insulinoma, gastroparesis, acute obstructive cholecystitis, irritable bowel disease, carcinoma of pancreas, etc.

New triazine derivatives represented by the formula: ##STR1## wherein R.sup.1 is hydrogen or halogen;

Triazine derivatives, and pharmaceutical compositions comprising the same

New triazine derivatives represented by the formula: ##STR1## wherein R.sup.1 is aryl, pyridyl, thienyl, 1,2,3,4-tetrahydroquinolyl or 1,3,4,5-tetrahydro-2H-1-benzazepinyl, optionally substituted with lower alkyl, lower alkoxy, halogen, nitro or oxo, R.sup.2 is hydrogen, lower alkyl or carbamoyl substituted with lower alkyl or ar(lower)alkyl, and Z is a group selected from ##STR2## and pharmaceutically acceptable salt thereof, processes for preparation thereof and pharmaceutical compositions comprising the same of antihypertensive and antithrombotic activity.

New triazine derivatives represented by the formula: ##STR1## wherein R.sup.1 is hydrogen; halogen or hydrazinocarbonyl(lower)alkyl;

New triazine derivatives represented by the formula: ##STR1## wherein R.sup.1 is a 1,2,3,4-tetrahydroquinolyl, 2-oxo-1,2,3,4-tetrahydroquinolyl, 2-oxo-1,2-dihydroquinolyl, indolyl, 2-oxoindolinyl, benzothiazolyl, 2-oxobenzothiazolinyl, 3,4-dihydro-1H-2,1-benzothiazinyl in which the S atom being optionally oxidized, or 3-oxo-2,3-dihydro-4H-1,4-benzoxazinyl, each of which may have one or more substituent(s) selected from lower alkyl, hydroxy(lower)alkyl, lower alkylamino, lower alkanoyl, cyclic lower alkanoyl, lower alkoxy(lower)alkyl, lower alkylamino(lower)alkanoyl, benzyl, benzyloxy(lower)alkyl, lower alkoxycarbonyl(lower)alkyl and 4-(2-hydroxyethyl)piperazin-1-yl-carbonylmethyl;

Growing community of inventors

Takaishi, Japan

Yoshinari Sato