Yoshitomi Pharmaceutical Industries, Ltd.

Tsuguo Ikebe

Tetsuya Tahara

Osamu Yaoka

Ichiro Hakamada

Yutaka Maruyama

Shu Murakami

Michio Terasawa

Toru Nakao

Tomonori Imayoshi

Koretake Anami

Yohji Miura

Benzolactam compounds of the general formula ##STR1## or isomers thereof as well as salts thereof inclusive of hydrates and/or solvates forms thereof, and benzolactam compounds of the general formula ##STR2## wherein each of the symbols is as defined in the specification. The compound (I) exhibit antiamnesic activity, and are useful as brain function-improving drugs. The compounds (a) and (b) are useful as an intermediate for said compounds (I). Futher, the compound (a) show diuretic or antiulcer activity, and are useful as a diuretic or antiulcer agent.

Benzolactam compounds and pharmaceutical uses thereof

Piperidine compounds of the formula: ##STR1## or isomers thereof as well as pharmaceutically acceptable salts and/or hydrate forms thereof, and piperidine compounds of the formula: ##STR2## or isomers thereof as well as salt and/or hydrate forms thereof. In the above formulae, A represents a methylene group, an oxygen atom or a sulfur atom; B represents an oxygen atom or a sulfur atom; R.sup.1 and R.sup.2 independently represent a hydrogen atom, a lower alkyl group or an aralkyl group; R.sup.3 represents a hydrogen atom or an amino protecting group; Z represents an amino group or a protected amino group, a hydroxy group, or a reactive atom or group; m represents 1 or 2; and n represents the integer of 0 to 3. Piperidine compounds (I) possess an inhibitory activity against angiotensin-converting enzyme, and exhibit a long lasting hypotensive activity and are useful as antihypertensive agents. Piperidine compounds (II) are useful as intermediates for said piperidine compounds (I).

Piperidine compounds and pharmaceutical uses thereof

5-Hydroxyindole-3-carboxylic acid amide compounds, pharmaceutical

3-Indolecarboxamide compounds of the formula: ##STR1## inclusive of pharmaceutically acceptable acid addition salt and/or hydrate forms thereof, wherein R.sup.1 is hydrogen or C.sub.1-4 alkyl; each of R.sup.2 and R.sup.3 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, benzyloxy, C.sub.2-6 alkanoyloxy or hydroxy; R.sup.4 is hydrogen or C.sub.1-4 alkyl; R.sup.5 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy; R.sup.6 is hydrogen or C.sub.1-4 alkyl; X is oxygen, sulfur or direct bond; each of k and m is an integer of 1 to 3; and n is 1 or 2, are useful as drug for the prevention and treatment of various circulatory diseases.

3-indolecarboxamides for control of circulatory diseases

3-Indolecarboxamide compounds of the formula: ##STR1## inclusive of pharmaceutically acceptable acid addition salt and/or hydrate forms thereof, wherein R.sup.1 is C.sub.1-8 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-8 alkyl, allyl, propargyl, or phenyl or phenyl-C.sub.1-4 alkyl which may be optionally substituted, on the benzene ring, by at least one substituent selected from the group consisting of halogen, trifluoromethyl, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; R.sup.2 is H or C.sub.1-6 alkyl; R.sup.3 is H, halogen, C.sub.2-6 alkanoyloxy, benzoyloxy, C.sub.1-4 alkoxy, benzyloxy, hydroxy or C.sub.1-4 alkyl; R.sup.4 is H, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy; R.sup.5 is H or C.sub.1-4 alkoxy; A is ethylene or trimethylene, which may be optionally substituted by C.sub.1-4 alkyl; n is zero, 1 or 2; and m is zero or 1, are useful as drugs for the prevention and treatment of various allergic diseases.

Anti-allergic 3-indolecarboxamides

Benzo[f]quinoline derivatives which are useful as antihypertensive agents and are represented by the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl, R.sup.2 is hydrogen, lower alkyl, hydroxy-lower-alkyl or lower-alkoxy-lower-alkyl, R.sup.3 and R.sup.4 are the same or different and each is hydrogen, lower alkyl, halogen, lower alkoxy, benzyloxy or hydroxy, R.sup.5 and R.sup.6 are the same or different and each is hydrogen, straight or branched alkyl, aralkyl or cycloalkyl, or R.sup.5 and R.sup.6 together with the adjacent nitrogen atom form a heterocycle, and the dotted line in the ring is an optional bond between 1- and 2-positions, and pharmaceutically acceptable acid addition salts thereof.

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Oita, Japan

Tsuguo Ikebe