Kyowa Hakko Kogyo Co., Ltd.

Yoshimasa Oiji

Hiroshi Takizawa

Katsuichi Shuto

Kazuhiro Kubo

Hiroyuki Obase

Tamotsu Hashimoto

Tatsuyuki Hirayama

Osamu Morita

Shunji Ichikawa

Kenji Ohmori

Hiroshi Tanaka

Shizuo Shiozaki

Etsuo Oshima

Toshiaki Kumazawa

Hiromasa Kato

Setsuya Sasho

Kei Okazaki

Tamotu Hashimoto

Masaaki Nito

Yutaka Enomoto

A furan derivative and a pharmaceutically acceptable salt thereof having gastrointestinal enterokinetic activity which is expected to be used in a broad spectrum of diseases associated with gastrointestinal dyskinesia.

Furan derivatives useful for the treatment of gastro-intestinal disorders

Disclosed are anti-dementia agents comprising an antiamnestically effective amount of a benzylpyridine derivative of the formula ##STR1## wherein R is an alkyl group. The invention also pertains to the treatment of dementia by administration of such anti-dementia agent.

Anti-dementia agent

Isoindolin-1-one compounds represented by the following formula (I); ##STR1## {wherein n represents an integer of 1 to 6; m represents 0 or 1; R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen or lower alkyl, and when m is 1, R.sub.1 and one of R.sub.2 and R.sub.3 may form a five-membered or six-membered ring over N atom; X represents hydrogen or hydroxy; Ar represents naphthyl, pyridyl or substituted phenyl represented by the formula (II); Ar and X may form a lactone ring; ##STR2## [wherein Y represents carboxyl, lower alkoxycarbonyl, carbamoyl, N,N-lower alkyl-substituted carbamoyl or amino represented by the formula (III): ##STR3## (wherein R.sub.6 and R.sub.7 are each independently hydrogen, lower alkyl or lower alkanoyl); R.sub.4 and R.sub.5 are each independently hydrogen, lower alkyl, cyano or halogen]} or a pharmaceutically acceptable acid addition salt or metal salt thereof have an excellent antiarrhythmic activity.

Isoindolin-1-one derivative and antiarrhythmic agent

A dibenz[b,e]oxepin compound having an antiallergic activity is represented by the following general formula: ##STR1## wherein R.sub.1 represents a cyano group, a 5-tetrazolyl group, a carbamoyl group or --CO.sub.2 R.sub.3 wherein R.sub.3 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms or a 1-(ethoxycarbonyloxy)ethyl group, and R.sub.2 represents a 4-alkylpiperazino group wherein the alkyl group has 1 to 5 carbon atoms, a 3-quinuclidinylamino group or --X--(CH.sub.2).sub.n --NR.sub.4 R.sub.5 wherein X represents --NH--, --S -- or --O--, R.sub.4 and R.sub.5 are same or different and each represents an alkyl group having 1 to 5 carbon atoms and n represents 2 or 3; and the pharmaceutically acceptable acid addition salts or metal salts thereof.

Dibenz[b,e]oxepin compounds

A novel [1] benzepino[3,4-b]pyridine derivative having antiulcer activity is represented by the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group, a halogenated alkyl group, an alkoxy group or a halogen atom; R.sup.2 represents ##STR2## wherein Y represents an amino group, a substituted amino group, a heterocyclic group or a substituted heterocyclic group; Z represents a hydrogen atom, an alkyl group or an acyl group; and m is an integer of 1-3, ##STR3## wherein Z' represents a hydrogen atom or an alkyl group; Y has the same meaning as defined above, and n is 0, 1 or 2; or ##STR4## wherein Z and n have the same meanings as defined above; X represents an oxygen atom or a sulfur atom. Also disclosed are pharmaceutically acceptable acid addition salts of the compound represented by the formula (I).

Antiulcer [1] benzepino[3,4-b]pyridine and compositions

Novel dibenz [b,e] oxepin derivatives represented by the general formula: ##STR1## wherein R.sub.11 represents an alkyl group containing 1 to 5 carbon atoms, an alkoxy group containing 1 to 5 carbon atoms, a halogen atom, a cyclohexyl group or a phenyl group; and R.sub.21 represents ##STR2## wherein X represents a hydrogen atom, a hydroxy group, an amino group or a substituted aralkyl group containing 7 to 20 carbon atoms, and n represents 0 or an integer of 1 to 3 ##STR3## wherein Y represents an alkylamino group containing 1 to 5 carbon atoms, an aralkyl group containing 7 to 20 carbon atoms, a substituted aralkyl group, an aralkyloxy group containing 7 to 20 carbon atoms, an aralkylamino group containing 7 to 20 carbon atoms, a heterocyclic ring or a substituted heterocyclic ring, and n has the same meaning as defined before; provided that when R.sub.11 represents an alkyl group, an alkoxy group or a halogen atom, X does not represent a hydrogen atom; and the pharmaceutically acceptable acid addition salts thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutical carrier and, as an active ingredient, an effective amount of dibenz [b,e] oxepin derivative represented by the following general formula: ##STR4## wherein R.sub.1 represents an alkyl group containing 1 to 5 carbon atoms, an alkoxy group containing 1 to 5 carbon atoms, a halogen atom, a cyclohexyl group or a phenyl group; and R.sub.2 represents ##STR5## wherein X represents a hydrogen atom, a hydroxy group, an amino group or a substituted aralkyl group containing 7 to 20 carbon atoms, and n has the same meaning as defined before ##STR6## wherein Y and n have the same meaning as defined above; and the pharmaceutically acceptable acid addition salts thereof. Compound I, represented by the general formula (I), has antichlolinergic, antihistaminergic, antiasthmatic and antiplatelet aggregation activities, and is therefore useful as a sposmolysant, an antihistaminic, an antiasthmatic agent and as a medicament for cardiovascular or cerebrovascular diseases, respectively.

Dibenz [b,e] oxepin derivatives

New amino-alcohol derivatives and processes for production thereof are disclosed. These compounds exhibit .alpha. and .beta.-adrenergic receptor blocking activity or they act to increase the flow of blood of certain organs.

Amino-alcohol derivatives

Novel dibenz [b,e] oxepin derivatives represented by the general formula: ##STR1## wherein R.sub.11 represents an alkyl group containing 1 to 5 carbon atoms, an alkoxy group containing 1 to 5 carbon atoms, a halogen atom, a cyclohexyl group or a phenyl group; and R.sub.21 represents ##STR2## wherein X represents a hydrogen atom, a hydroxy group, an amino group or a substituted aralkyl group containing 7 to 20 carbon atoms, and n represents 0 or an integer of 1 to 3 ##STR3## or (3) --NH--(CH.sub.2).sub.n --Y, wherein Y represents an alkylamino group containing 1 to 5 carbon atoms, an aralkyl group containing 7 to 20 carbon atoms, a substituted aralkyl group, an aralkyloxy group containing 7 to 20 carbon atoms, an aralkylamino group containing 7 to 20 carbon atoms, a heterocyclic ring or a substituted heterocyclic ring, and n has the same meaning as defined before; provided that when R.sub.11 represents an alkyl group, an alkoxy group or a halogen atom, X does not represent a hydrogen atom; and the pharmaceutically acceptable acid addition salts thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutical carrier and, as an active ingredient, an effective amount of a dibenz [b,e] oxepin derivative represented by the following general formula: ##STR4## wherein R.sub.1 represents an alkyl group containing 1 to 5 carbon atoms, an alkoxy group containing 1 to 5 carbon atoms, a halogen atom, a cyclohexyl group or a phenyl group; and R.sub.2 represents ##STR5## wherein X represents a hydrogen atom, a hydroxy group, an amino group or a substituted aralkyl group containing 7 to 20 carbon atoms, and n has the same meaning as defined before ##STR6## or (3) --NH--(CH.sub.2).sub.n --Y, wherein Y and n have the same meaning as defined above; and the pharmaceutically acceptable acid addition salts thereof. Compound I, represented by the general formula (I), has antichlolinergic, antihistaminergic, antiasthmatic and antiplatelet aggregation activities, and is therefore useful as a sposmolysant, an antihistaminic, an antiasthmatic agent and as a medicament for cardiovascular or cerebrovascular diseases, respectively.

A pharmaceutical composition, specifically a muscle relaxant acting at the same time as an anti-inflammatory and analgesic agent which composition comprises pharmaceutically acceptable carrier(s) and a benzo[b]furancarboxamide derivative represented by the general formula: ##STR1## wherein R represents a halogen atom, an alkyl group having 1-5 carbon atoms or an alkoxy group having 1-5 carbon atoms.

Pharmaceutical composition containing a benzofurancarboxamide derivative

The present invention relates to certain novel benzo[b]furan derivatives, namely, 5-substituted-2-substituted carbamoylmethyl-3-methyl benzo[b]furan having interesting pharmacological properties, in particular a muscle relaxant activity.

Growing community of inventors

Shizuoka, Japan

Yoshimasa Oiji