Rhone-poulenc Sante

Daniel Lave

Claude James

Jean-Louis Fabre

Daniel Farge

Francoise Soler

New derivatives of formula (I) in which R.sub.1 =H, halogen, alkyl, alkyloxy, CF.sub.3, NH.sub.2, alkylamino, dialkylamino, OH, CH, phenyl or phenoxy, Ar=phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, thienyl, thieno[2,3-b]thienyl or thieno[3,2-b]thienyl (these groups optionally substituted with halogen, alkyl, alkyloxy, CF.sub.3, NH.sub.2, alkylamino, dialkylamino, OH or CN), p=0, 1 or 2, and

1H, 3H-pyrrolo[1,2-c]thiazole-7-carboxamide derivatives and

A compound of the general formula I: ##STR1## in which Ar is a pyridyl, quinolinyl, isoquinolinyl, naphthyridinyl, pyrimidyl, quinazolinyl, thiazolyl, benzothiazolyl, imidazolyl, benzimidazolyl, oxazolyl, benzoxazolyl, thienyl, benzothienyl or naphthyl group; optionally substituted with one or more halogen or alkyl, alkyloxy, alkylthio, trifluoromethyl, amino, alkylamino, dialkylamino, hydroxy, cyano, alkylsulphinyl, alkylsulphonyl, sulphamido, alkylsulphamido, dialkylsulphamido, alkylcarbonyl, benzoyl, alkyloxycarbonyl, carboxy, phenoxycarbonyl, alkylcabonyloxy, benzoyloxy, alkylcarbonylamino, benzamido, phenyl, benzyl, phenoxy or phenylthio group, provided that (i) when Ar is a pyridyl group, the pyridyl group must be substituted, (ii) an alkyl moiety contains 1 to 4 straight- or branched chain carbon atoms; (iii) a phenyl moiety may be unsubstituted or substituted with one or more halogen or alkyl, alkyloxy, alkylthio, trifluoromethyl, amino, alkylamino, dialkylamino, hydroxy, cyano, phenyl or benzyl group in separate enantiomeric form or mixtures thereof, or a pharmaceutically acceptable salt thereof is useful in the treatment of all pathological conditions in which PAF-acether may be implicated directly or indirectly.

1H, 3H-pyrrolo (1,2-C) thiazole derivatives and pharmaceutical

A compound of the general formula I; ##STR1## in which R is hydrogen or a halogen or an alkyl, alkyloxy, alkylthio, trifluoromethyl, amino, alkylamino, dialkylamino, hydroxy, cyano, carboxy, alkylsulphinyl, alkylsulphonyl, sulphamido, alkylsulphamido, dialkylsulphamido, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, phenylcarbamoyl, diphenylcarbamoyl, pyridylcarbamoyl, dipyridylcarbamoyl, benzyl, alkylcarbonyl, benzoyl, alkyloxycarbonyl, phenoxycarbonyl, alkylcarbonyloxy, benzoyloxy, alkylcarbonylamino, benzamido, phenyl, phenoxy or phenylthio group, X is oxygen or sulphur or an imino, alkylimino, phenylimino, benzylimino, sulphinyl, sulphonyl, carbonyl, carbonylmethylene, methylenecarbonyl, carbonylvinylene or vinylenecarbonyl group, or X represents a valency bond or a straight-chain alkylene group containing 1 to 4 carbon atoms and Ar is a phenyl, naphthyl, pyridyl, quinolinyl, isoquinolinyl, thienyl, benzothienyl, thieno[3,2-b]thien-2-yl or thieno[2,3-b]thien-2-yl group, it being possible for the group Ar to be unsubstituted or substituted with one or more halogen or alkyl, alkyloxy, alkylthio, trifluoromethyl, amino, alkylamino, dialkylamino, hydroxy, cyano, carboxy, alkylsulphinyl, alkylsulphonyl, sulphamido, alkylsulphamido, dialkylsulphamido, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, phenylcarbamoyl, diphenylcarbamoyl, pyridylcarbamoyl, dipyridylcarbamoyl, benzyl, alkylcarbonyl, benzoyl, alkyloxycarbonyl, phenoxycarbonyl, alkylcarbonyloxy, benzoyloxy, alkylcarbonylamino or benzamido group; each alkyl moiety containing 1 to 4 straight- or branched-chain carbon atoms; the compound being in separate enantiomeric form or mixtures thereof or a pharmaceutically acceptable salt thereof is useful in the treatment of all the pathological conditions in which PAF-acether may be directly or indirectly implicated.

1H,3H-pyrrol[1,2-c]thiazole derivatives and pharmaceutical compositions

The invention provides novel pyrrole derivatives of formula: ##STR1## in which R'=H, alkyl or phenyl optionally substituted by halogen, alkyl, alkyloxy or alkylthio, Z=0 or S, p=0 or 1, and

Anti-thrombotic ortho-condensed pyrrole derivatives, compositions, and

Antithrombotics of the formula ##STR1## in which A=S, SO or SO.sub.2, R.sub.3 =H, alkyl or substituted or unsubstituted phenyl, X=O, S, NH or variously substituted nitrogen, p is 0 or 1 and y=H, NH.sub.2, or various substituted amines.

Pyrrolo[1,2-c]-1,3-thiazines

Pyrrolidine derivatives of the formula: ##STR1## wherein X represents an oxygen or sulphur atom, R represents a hydrogen atom or an alkyl radical, R.sub.o represents a hydrogen atom, an alkyl radical or a phenyl radical optionally substituted by a halogen atom or by an alkyl, alkoxy, alkylthio or nitro radical, A represents a nitrogen atom or a radical .dbd.CH--, the symbol Y represents a hydrogen or halogen atom or an alkyl, alkoxy, alkylthio, alkylcarbonyl, nitro, amino, alkylcarbonylamino, alkylamino, dialkylamino, alkylsulphinyl, alkylsulphonyl, alkoxycarbonyl, cyano, trifluoromethyl, hydroxy, mercapto, alkylcarbonyloxy or alkylcarbonylthio radical, n represents zero or 1, and p represents 1, 2 or 3, it being understood that the alkyl and alkoxy radicals, and alkyl and alkoxy moieties of any of the aforementioned groups, contain from 1 to 4 carbon atoms are new therapeutically useful compounds, more particularly useful as antidepressants.

Substituted phenyl piperazinyl pyrrolidin-2-ones and related compounds

Antithrombotics of the formula: ##STR1## wherein A is S, SO or SO.sub.2 ; R.sub.3 is H, alkyl or substituted or unsubstituted phenyl; p is zero or 1; X is O, S, N or variously substituted nitrogen; Y is H or various substituted amines.

Pyrrolo[1,2-c]thiazoles useful as antithrombotic agents

The invention provides new derivatives of the formula: ##STR1## in which either (a) Y=COOH or a radical of the formula (II), in which R.sub.2 =alkyl or benzyl, A=a sulphur atom, m=1, n=0, R=pyridin-3-yl and R.sub.1 =H, or (b) Y=CN, COOH or a radical of the formula ##STR2## defined as above, A=S, O or CH.sub.2, m=1 or 2 and n=0, 1 or 2, (m+n) being 1, 2 or 3, R=H, alkyl or phenyl (optionally substituted by halogen, alkyl, alkoxy or CF.sub.3) and R.sub.1 =a radical of the formula ##STR3## in which p=0 or 1, the alkyl radicals and alkyl portions being straight-chain or branched-chain and containing 1 to 4 carbon atoms each. Processes for the production of these compounds are described. They are useful as intermediates for the preparation of new medicaments.

Pyridin-3-yl substituted ortho-fused pyrrole derivatives

New compounds of the formula ##STR1## in which R.sub.1 and R.sub.2 =H or alkyl and

Growing community of inventors

Paris, France

Daniel Lave