Synthelabo

Thomas A Purcell

Daniel J Galtier

Samir Jegham

Lydia Zard

Gilbert Lassalle

Gerard Defosse

Paul Howard Williams

Braham Shroot

Johannes Schoemaker

Pascal George

Jonathan Reid Frost

Jean-Claude Muller

Luc Even

Sergio Mallart

Christophe Philippo

Frederic Galli

Jean Claude Muller

Corinne Rousselle

Patrick Pasau

Regine Bartsch

Howard Williams

Itzchak Angel

G Erard Defosse

Fr Ed Galli

Jacques Comarmond

Luc Rivron

Benzenesulphonamide compounds of general formula (I), wherein R,is a hydrogen or halogen atom such as chlorine or fluorine, or a straight or branched C,alkyl or C,alkoxy group, each of R,, R,and R,, which are the same or different, is a hydrogen atom or a straight, branched or cyclic C,alkyl group, and R,is a hydrogen atom or a C,alkyl, C,fluoroalkyl or C,perfluoroalkyl group, in the form of enantiomers, diastereoisomers or mixtures thereof, including racemic mixtures, as well as pharmaceutically acceptable acid addition salts thereof, are provided for therapeutical use.

Benzenesulphonamide derivatives, preparation thereof and therapeutical uses thereof

A compound of formula (I): ##STR1## in which R.sub.1 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.4)alkyl group; and

Imidazol-4-ylpiperidine derivatives, their preparation and their

Compounds of formula (I) ##STR1## wherein R.sub.1 represents either a hydrogen atom, or a (C.sub.1 -C.sub.4)alkyl group, X represents either a sulphur atom, an oxygen atom or a methylene group, Z.sub.1 represents either a hydrogen atom, or a 1,1-dimethylethyl group, Z.sub.2 represents either a hydrogen atom, a triphenylmethyl group, or a phenylmethoxycarbonyl group, and n=1 or 2, and addition salts to inorganic or organic acids thereof as synthetic intermediates.

Imidazole derivatives useful as synthetic intermediates

A compound of formula (I) ##STR1## in which R.sub.3 and R.sub.4 together represent the residue of a dihydroxy compound, and

1-amino-4-(1H-imidazole)- aminobutaneboronic acid derivatives, their

Compounds of formula (I) ##STR1## wherein R represents a ##STR2## group in which R.sub.2 is a hydrogen atom, a (C.sub.1 -C.sub.4)alkoxycarbonyl group, a carboxylic group, a sodium carboxylate group, a --CH.sub.2 OR.sub.4 group R.sub.4 being a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group or a (C.sub.1 -C.sub.4)acyl group, an amide group of the formula --CONR.sub.5 R.sub.6, or a --CN.sub.4 R.sub.5 group, R.sub.5 being a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group and R.sub.6 being a hydrogen atom, a (C.sub.1 -C.sub.4)alkyl group, a hydroxy group or a (C.sub.1 -C.sub.4)alkoxy group, and R.sub.3 is a (C.sub.1 -C.sub.4)alkyl group, R.sub.1 represents either a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group, X represents either a sulphur atom, an oxygen atom or a methylene group, n=1 or 2 and Ar represents either a naphthalen-1-yl group substituted by a di(C.sub.1 -C.sub.4)alkylamino group, or a 6,7-di(C.sub.1 -C.sub.4)alkoxynaphthalen-1-yl group, or a quinolin-8-yl group substituted at 3 by a (C.sub.1 -C.sub.4)alkyl group, or a 1,2,3,4-tetrahydroquinolin-8-yl group substituted at 3 by a (C.sub.1 -C.sub.4)alkyl, or a 1H-indazol-7-yl group and pharmaceutically acceptable organic or inorganic salts thereof. Application in therapy.

1-[2-(arylsulphonylamino)-1-oxoethyl]piperidine derivatives, their

Compounds of the formula ##STR1## in which Y represents hydrogen, fluorine, chlorine, methyl or methoxy, R.sub.1 represents phenyl substituted by fluorine, methyl, methoxy, trifluoromethyl or phenyl, or R.sub.1 represents 2-thienyl, R.sub.2 represents methyl, and R.sub.3 represents (C.sub.1 -C.sub.4)-alkyl, or phenyl-(C.sub.1 -C.sub.2)-alkyl optionally substituted on the ring by 2 to 3 methoxy groups, or 2-(2-pyridyl)ethyl, or R.sub.2 and R.sub.3 form, with the adjacent nitrogen, 4-phenyl(1-piperidyl), 4-phenylmethyl(1-piperidyl), 1,2,3,4-tetrahydro-2-isoquinolyl, 6-methoxy-1,2,3,4-tetrahydro-2-isoquinolyl, 5,8-dimethoxy-1,2,3,4-tetrahydro-2-isoquinolyl, 6,7-dimethoxy 1,2,3,4-tetrahydro-2-isoquinolyl, 2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl, or 7,8-dimethoxy-2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl, and X represents carbonyl or sulphonyl, and their salts are useful as neuroprotective and antiiischaemic agents.

Benzoxazine derivatives and their application in therapy

A compound which is a piperidine derivative of formula (I) ##STR1## in which R represents hydrogen, or unbranched or branched C.sub.1 -C.sub.6 alkyl group; and

Piperidine derivatives, their preparation and their application in

The invention provides a compound which is a piperidine derivative of formula (I) ##STR1## in which R.sub.1 is hydrogen or straight or branched (C.sub.1 -C.sub.6) alkyl, R.sub.2 is hydrogen or straight or branched (C.sub.1 -C.sub.8) alkyl, Z and Z.sub.1 which may be the same or different, each is hydrogen, chlorine, hydroxyl, amino, nitro, hydroxymethyl, (C.sub.1 -C.sub.2) alkyl, (C.sub.1 -C.sub.8) alkoxy straight or branched (C.sub.1 -C.sub.5) alkoxycarbonyl or aryl (C.sub.1 -C.sub.2) alkoxy, Z is in position 4, 6 or 7 and Z and Z.sub.1 cannot both be hydrogen, or its addition salt with a pharmaceutically acceptable acid and its therapeutic application.

A compound which is a piperidine derivative of general formula (I) ##STR1## in which R.sub.1 represents a hydrogen atom, a linear or branched (C.sub.1-6)alkyl group or a cyclo(C.sub.3-8)alkyl group, X represents an oxygen atom, a sulphur atom or a group of general formula N--R.sub.3 in which R.sub.3 is a hydrogen atom, or a linear or branched (C.sub.1-8)alkyl, cyclo(C.sub.3-6)alkyl, cyclo(C.sub.3-6)alkylmethyl, (C.sub.1-4)alkoxy-(C.sub.1-4)alkyl, phenyl, pyridin-4-yl, pyridin-3-yl, pyridin-4-ylmethyl or pyridin-3-ylmethyl group and Z represents a hydrogen or fluorine atom and acid addition salts thereof with pharmaceutically acceptable acids, can be used for the treatment and prevention of disorders in which 5-HT receptors are involved.

Piperidine derivatives, their preparation and their therapeutic

A compound which is an N-(imidazolymethyl) diphenylazomethine derivative of the general formula (I) ##STR1## wherein R.sub.1 is chlorine or methyl,

N-(imidazolylmethyl)diphenylazomethines and compositions containing them

A compound, in the form of a pure optical isomer or a racemate, which is a dibenzo[be]oxepinacetic acid of the general formula (I) ##STR1## in which R1, R2 and R3, which may be the same or different, each represent hydrogen or methyl, XX represents a carbon-carbon bond or two hydrogen atoms, and YY represents a carbon-carbon bond or two hydrogen atoms, or a pharmaceutically acceptable salt thereof has useful therapeutic properties, especially as an anti-inflammatory.

Dibenzo[b,e]oxepinacetic acid derivatives and pharmaceutical

Compounds of general formula ##STR1## in which R.sub.1, taken separately, denotes a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, and

Dibenz[be]oxepin-acetic acid derivatives, the preparation thereof and

Imidazolidine derivatives of the formula: ##STR1## wherein R.sub.1 represents the hydroxy radical and R.sub.2 represents a grouping --NHSO.sub.2 CH.sub.3, --NHCOR' or --NHCONR'R', R' and R' independently of one another representing a hydrogen atom or an alkyl radical having from 1 to 4 carbon atoms, or alternatively R.sub.2 represents the hydroxy radical and R.sub.1 represents a grouping --NHSO.sub.2 CH.sub.3, --NHCOR' or ?NHCONR'R', R' and R' independently of one another representing a hydrogen atom or an alkyl radical having from 1 to 4 carbon atoms, and pharmacologically-acceptable acid addition salts thereof, are new therapeutically useful compounds. They are more particularly useful in the treatment of gastric hypersecretion or hyperacidity or glaucoma.

2-[4(3)-Amino-3(4)-hydroxyphenylimino]-imidazolines, useful in the

A method of treating a patient susceptible to thrombosis is provided which comprises treating the said patient with a compound of the formula ##STR1## wherein R' is H or CH.sub.3

Antithrombotic method

Compounds corresponding to the formula ##STR1## in which R' is a hydrogen atom or a methyl radical and R represents a radical ##STR2## in which Z is O, S, S.fwdarw.O, SO.sub.2 or NR.sub.1, in which R.sub.1 is a hydrogen atom or an alkyl, CONR.sub.2 R.sub.3, COOR.sub.2, COR.sub.2 or SO.sub.2 R.sub.2 radical, R.sub.2 and R.sub.3 each representing, independently of one another, a hydrogen atom, an alkyl radical having 1 to 4 carbon atoms, a phenyl radical or a CF.sub.3 radical, in the form of racemates or enantiomers if R' is CH.sub.3, and also, where appropriate, their addition salts with pharmaceutically acceptable acids. The compounds and salts are useful as anti-inflammatory agents, e.g. for treatment of arthritis. A process for preparing them and pharmaceutical compositions containing them are also claimed.

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Fontenay aux Roses, France

Thomas A Purcell