Takeda Chemical Industries, Inc.

Yoshihiro Sugiura

Kaneyoshi Kato

Koichi Kato

Yasuo Nagai

Giichi Goto

Akinobu Nagaoka

Ken-ichi Naruo

Hideki Takahashi

Tetsuji Imamoto

Tsuneo Asano

A compound represented by the formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 independently represent an optionally substituted aromatic group; Q represents an optionally substituted divalent aliphatic hydrocarbon group optionally containing O or S; R.sup.1 represents H, acyl group, etc.; and X represents an electron-withdrawing group, an optionally substituted aromatic group, a group of the formula: ##STR2## wherein R.sup.2 and R.sup.3 independently represent H, acyl group or an optionally substituted hydrocarbon group, etc., etc.; or salts thereof are useful as an excellent anti-neurodegenerative agent.

Aromatic hydroxamix acid compounds, their production and use

The compound ##STR1## wherein ring A represents a benzene ring;

Condensed heterocyclic compounds, their production and use

A compound of the formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 independently represent an optionally substituted aromatic group; P and Q independently represent a divalent aliphatic hydrocarbon group having at least 2 carbon atoms and optionally having either oxygen or sulfur in the carbon chain; R.sup.1 and R.sup.3 independently represent --CO--R, --CONH--R (R represents a hydrocarbon group or a heterocyclic group) or a hydrocarbon group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4, taken together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic group; and j represents 0 or 1, or a salt thereof, has excellent GnRH-receptor antagonizing activity and is useful as a prophylactic and therapeutic agent for hormone-dependent and other diseases.

Amine compounds, their production and use

The compound ##STR1## wherein ring A represents a benzene ring; Ar represents an aromatic group; R.sup.1 and R.sup.2 independently represent hydrogen, acyl or hydrocarbon group or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom represent a nitrogen-containing heterocyclic group; m represents an integer of 1 to 6; n represents an integer of 2 to 3; ----- represents a single bond or a double bond; X stands for --O-- or --NR.sup.3 -- in which R.sup.3 represents hydrogen, acyl or hydrocarbon group where ----- is a single bond or .dbd.N-- where ----- is a double bond has excellent GnRH receptor antagonizing activity, calcium antagonizing and monoamine-uptake inhibiting activities and and value as a prophylactic/therapeutic drug for sex hormone-dependent diseases and for central nervous system diseases.

The present invention relates to prevention or treatment a brain edema, an intracranial hemorrhage and a cerebral infarction by administering a pharmaceutically effective amount of a compound or a pharmaceutically acceptable salt thereof, for inhibiting a vascular permeability enhancer, which the compound is of the formula: ##STR1## wherein A is halogen, --X--R.sup.3 in which X is O, S, NH or NHNH, and R.sup.3 is H, acyl, a hydrocarbon group or an aromatic heterocyclic group, or --Y.dbd.R.sup.4 in which Y is N or NHN, and R.sup.4 is a divalent hydrocarbon group, and R.sup.1 is H, halogen, a hydrocarbon group, a heterocyclic group or --Z--R.sup.5 in which Z is O, S or NH, and R.sup.5 is H, a hydrocarbon group or an aromatic heterocyclic group;

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Nara, Japan

Yoshihiro Sugiura