Hokuriku Pharmaceutical Co., Ltd.

Hokuriku Seiyaku Co., Ltd.

Nobuo Ogawa

Hideo Kato

Eiichi Koshinaka

Yasuo Ito

Yasuo Itoh

Hiroyuki Nishino

Jun Sakaguchi

Kazuya Mitani

Kagari Yamagishi

Tomio Suzuki

Yasuo Itho

Toshihiko Yoshida

Sakae Kurata

Shunichiro Sakurai

Kouji Morikawa

Noriyuki Yagi

Hiroyuki Sawanishi

Shingo Yasuda

Benzenesulfonamide derivatives and use thereof

Tricyclic compounds and method for treating allergic diseases

Novel polycyclic compounds represented by the following formula: A--(CH.sub.2).sub.n --COOR.sup.1, wherein R.sup.1 represents a hydrogen atom or a lower alkyl group; n represents an integer of from 0 to 5; and A is a group represented by the following formula: ##STR1## wherein X represents a hydrogen atom or a halogen atom; and Y represents a methylene group, an oxygen atom, or a sulfur atom, or A is a group represented by the following formula: ##STR2## and pharmacologically acceptable salts thereof are disclosed. Also disclosed are a method for preparing the same, a pharmaceutical composition comprising the same, an antiallergic agent and an agent for bronchial asthma comprising the same, and a method for treatment of an allergic disease or bronchial asthma comprising the step of administering the same.

Piperazinealkanoic acid and a pharmaceutical composition comprising the

A piperidine derivative represented by the following general formula (I): ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each independently represents a hydrogen atom, a halogen atom, a lower alkyl group, or a lower alkoxy group; R.sub.3 represents a hydrogen atom or a lower alkyl group; X represents an oxygen atom or a sulfur atom; Y represents an alkylene group having 1 to 7 carbon atoms which may be optionally substituted with a lower alkyl group, or Y represents an --A--O--B-- group wherein A and B are the same or different and each independently represents an alkylene group having 1 to 3 carbon atoms which may be optionally substituted with a lower alkyl group is disclosed. Also disclosed are a pharmacologically acceptable salt of a compound of formula (I), an antihistaminic and antiallergic agent comprising a compound of formula (I), a pharmaceutical composition comprising a compound of formula (I), and a method for the treatment of an allergic disease by administering a compound of formula (I).

Piperidine derivative, method for preparation thereof, and a

A thiazetoquinoline-3-carboxylic acid derivative represented by the general formula (I) ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl group; R.sub.2 is a fluorine atom or a chlorine atom; R.sub.3 is a hydrogen atom, a lower alkyl group, a lower alkanoyl group, a halogenated lower alkanoyl, or alkoxycarbonyl group; and R.sub.4 is a hydrogen atom or a lower alkyl group, and a pharmacologically acceptable salt thereof, a process for preparation thereof, a pharmaceutical composition comprising the same, and a method for the treatment of an infectious disease by administering the same, are disclosed.

Thiazetoquinoline-3-carboxylic acid derivative and a pharmaceutical

A piperidine derivative represented by the following general formula (I): ##STR1## wherein R represents a hydrogen atom or a lower alkyl group; X represents --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, or --CH.sub.2 O--; Y represents an alkylene group having 1 to 5 carbon atoms which may be optionally substituted with a lower alkyl group, or Y represents an --A--O--B-- group wherein A and B are the same or different and each independently represented an alkylene group having 1 to 3 carbon atoms which may be optionally substituted with a lower alkyl group is disclosed. Also disclosed are a pharmacologically acceptable salt of a compound of formula (I), a method for preparation of a compound of formula (I), an antihistaminic and antiallergic agent comprising a compound of formula (I), a pharmaceutical composition comprising a compound of formula (I), and a method for the treatment of an allergic disease by administering a compound of formula (I).

Piperidine derivatives and pharmaceutical compositions comprising the

Amide-compounds represented by the formula (I): ##STR1## wherein R.sub.1 represents hydrogen, lower alkoxy, hydroxy, lower alkyl, halogen, amino which can be substituted by lower alkyl, nitro, cyano, sulfamoyl which can be substituted by lower alkyl, R.sub.2 represents hydrogen, lower alkoxy, hydroxy, lower alkyl, halogen, amino, nitro, wherein R.sub.1 and R.sub.2 can be combined to form methylenedioxy, R.sub.3 means hydrogen, lower alkyl, halogen, or amino, R.sub.4 and R.sub.5 may be the same or different and each represents lower alkyl or wherein R.sub.4 and R.sub.5 may be combined together with nitrogen to form 1-pyrrolidinyl or piperidino, and pharmacologically-acceptable acid-addition salts thereof, which exhibit excellent effects in the activation of gastric motor function, a process for preparation pharmaceutical compositons thereof, as well as a method for the treatment of a subject suffering from an ailment associated with inadequate gastric motor function by administrating such a compound to the said subject, are all disclosed.

Amide compounds, process for preparing the same, and composition for

Phenoxyethylamine derivatives represented by the general formula (I): ##STR1## wherein R.sub.1 and R.sub.5 represent lower-alkyl, R.sub.2 and R.sub.3, which may be the same or different, each represents hydrogen or lower-alkyl, or ##STR2## represents a 5- or 6-membered ring system which may include nitrogen, oxygen or sulfur as a ring membered atom, R.sub.4 represents hydrogen or lower-alkyl, and n represents an integer selected from 1 to 3, their optical isomers and pharmacologically-acceptable acid addition salts, which exhibit excellent .alpha..sub.1 -blocking activity, a process for their preparation, pharmaceutical compositions thereof, and a method for the treatment of a subject afflicted with hypertension or dysuria by administrating such a compound, are all disclosed.

Phenoxyethylamine derivatives, for preparing the same and composition

Novel pyrazine derivatives useful for treatment of bronchial asthma, allergic gastorenteric trouble, hay fever urticaria, allertic rhinitis, and allergic conjunctivitis, and pharmaceutical compositions thereof, are disclosed. The compounds have the formula I as follows: ##STR1## wherein R represents hydrogen or ##STR2## wherein R.sub.1 and R.sub.2 may be the same or different and each independently represents hydrogen, straight or branched-chain lower-alkyl, or cycloalkyl having three to six carbon atoms inclusive, phenyl which may be substituted with halogen, lower-alkyl, or lower-alkoxy, or wherein R.sub.1 and R.sub.2 together represent alkylene of four to six carbon atoms, inclusive, optionally interrupted by one or two nitrogen atoms or one oxygen atom and said ring being optionally substituted by straight or branched-chain lower-alkyl having one to six carbon atoms inclusive, hydroxy, or phenyl, and pharmaceutically-acceptable salts thereof.

Pyrazine-2-carboxamide derivatives useful in treating allergic disease

Certain 4'-alkyl-2-methyl-3-pyrrolidinopropiophenones, acid addition salts thereof, their method of preparation, pharmaceutical compositions embodying the same, and a method of muscle relaxation therewith, are disclosed.

Derivatives of 3-pyrrolidinopropiophenone and a process for preparation

Novel alpha-aminoalkyl-alpha-alkylphenylacetonitrile derivatives useful for treatment of cartino vaso diseases, a peripheral circulatory insufficiency and cerebral circulation failure are disclosed.

Pharmaceutical alpha-aminoalkyl-alpha-alkylphenylacetonitriles

The invention is concerned with the novel piperazinylquinoline-3-carboxylic acids represented by formula (I) ##STR1## or a pharmacologically-acceptable salt thereof, a process for the preparation of them, and a pharmaceutical composition which contains these new compounds as active ingredient and can be used as the therapeutic agent against bacteria.

6-Fluoro-1, 4-dihydro-4-oxo-7-substituted

Derivatives of N-substituted flavone-8-carboxamides represented by general formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom, a methyl group or an ethyl group, R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkoxyl group, a halogen atom or a nitro group, R.sub.3 represents a hydrogen atom or a lower alkyl group, k represents 0, 1, 2, or 3, m represents 0 or 1; X and Y, which must be different, represent a hydrogen atom or methyl group. A represents an amino group having the formula ##STR2## wherein, R.sub.4 and R.sub.5, which may be the same or different, represent a lower alkyl group or a cyclic amino group together with the nitrogen atom and with or without an oxygen atom, R.sub.6 represents a lower alkyl group and n represents 2 or 3, are disclosed, as well as pharmaceutical compositions thereof and method of treating therewith. The N-substituted flavone-8-carboxamides derivatives are useful as agents for treatment of dysurea.

N-substituted flavone-8-carboxamides

1-(3,4,5-Trimethoxycinnamoyl)-4-aminocarbonylethyl-substituted piperazine derivatives represented by general formula (I): ##STR1## wherein R is a straight- or branched-chain alkyl group having 1 to 6 carbon atoms or a cycloalkyl group having 5 to 7 carbon atoms, and pharmaceutically acceptable acid addition salts thereof are disclosed. The 1-(3,4,5-trimethoxycinnamoyl)-4-aminocarbonylethyl-substituted piperazine derivatives are useful as vasodilator agents.

1-(3,4,5-Trimethoxycinnamoyl)-4-alkylaminocarbonylethyl piperazines

A process is provided for preparing 2-arylpiperazine derivatives and more particularly, 2-phenylpiperazine derivatives of the formula ##STR1## wherein R represents a group selected from the group consisting of a halogen atom, a lower alkyl group (having carbon atoms of 1 to about 8, preferably 1 to 4), a lower alkoxy group (having carbon atoms of 1 to about 8, preferably 1 to 4), a nitro group, a cyano group, a benzyloxy group, a hydroxy group and when n is 2 R is a methylenedioxy group, and n represents 1, 2 or 3.

Growing community of inventors

Katsuyama, Japan

Nobuo Ogawa