Rhone-Poulenc Sante

Rhone-Poulenc Industries

Rhone-Poulenc Rorer S.a.

Jean-Louis Fabre

Claude James

Daniel Farge

Daniel Lave

Thierry Dupechez

Jean-Pierre Bastart

Francois Debarre

Jean-Pierre Bastard

The invention provides new compositions containing taxane derivatives, consisting of solutions of such derivatives in a solvent mixture composed of ethanol and polysorbate. These compositions are used to prepare perfusions.

Compositions containing taxane derivatives

This invention relates to compositions containing taxane derivatives, consisting of a solution of such derivatives in a surfactant. These compositions can be used to prepare perfusion solutions.

New compositions containing taxane derivatives

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

1H,3H-pyrrolo[1,2-c]thiazole derivatives having anti-allergic and

Thiazolo[3,2-a]pyrimidine derivative of the formula: ##STR1## wherein R represents phenyl, alkyl of 1 through 4 carbon atoms, alkyl of 1 through 4 carbon atoms substituted by 1 through 3 halogen atom, alkenyl of 2 through 4 carbon atoms, or cycloalkyl of 3 through 6 carbon atoms and R.sub.1 represents hydrogen, or R and R.sub.1 each represent phenyl or unsubstituted alkyl of 1 through 4 carbon atoms, or R and R.sub.1 together represent an alkylene radical of 4 or 5 carbon atoms, and R.sub.2 and R.sub.3 each represent hydrogen or unsubstituted alkyl of 1 through 4 carbon atoms, or R and R.sub.1 each represent hydrogen, and one of R.sub.2 and R.sub.3 represents hydrogen and the other represents unsubstituted alkyl of 1 through 4 carbon atoms, or R.sub.2 and R.sub.3 both represent unsubstituted alkyl of 1 through 4 carbon atoms, are new compounds possessing pharmacological properties. They are especially useful in the treatment of rheumatic disease or allergic states, or as analgesics. Processes for the preparation of the compounds are described.

2,3,6,7-Tetrahydrothiazolo[3,2-a]pyrimidine derivatives having

Compounds of the formula: ##STR1## wherein R represents hydrogen or an alkyl radical, R.sub.1 represents a hydroxy, amino or alkoxy radical or an alkylamino or dialkylamino group, the various alkyl radicals and the alkoxy radical being optionally substituted by a dialkylamino group, the alkyl radicals of the said dialkylamino groups optionally being linked together to form a heterocyclyl radical with 5 or 6 atoms in the ring, and A represents the thieno[2,3-b]thien-2-yl or thieno[3,2-b]thien-2-yl radical, the A--CO-- grouping being attached to the 3- or 4-position of the phenyl ring, have been found to possess useful pharmacological properties and are particularly active as analgesics, antipyretics, agents for inhibiting platelet aggregation and as anti-inflammatory agents.

Thienothienylcarbonyl-phenylalkanoic acids and derivatives thereof

Compounds of the formula: ##STR1## wherein the symbols X each represent hydrogen or methoxy, R represents hydrogen or carboxymethyl, the symbols R.sub.1 each represent hydrogen or together represent a valency bond and the symbols R.sub.2 each represent hydrogen or together represent a valency bond, the pair of symbols R.sub.2 having the same significance as the pair of symbols R.sub.1, and when the symbols R.sub.1 and R.sub.2 represent hydrogen the symbol X also represents hydrogen, are new compounds possessing antiviral activity.

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Paris, France

Jean-Louis Fabre