Abstract: The present invention relates to new lupane dervivatives of the general formula: ##STR1## to their salts, to their preparation and to the pharmaceutical compositions which contain them.
Type:
Grant
Filed:
May 12, 1994
Date of Patent:
November 21, 1995
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Romaine Bouboutou, Norbert Dereu, Michel Evers, Jean-Christophe Gueguen, Claude James, Christele Poujade, Daniel Reisdorf, Yves Ribeill, Francoise Soler
Abstract: This ivention relates to novel perhydroisoindole derivatives having formula (I), ##STR1## wherein the symbols R, which are the same or different, are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl radical, R' is a phenyl radical optionally 2-substituted by a C.sub.1-2 alkylk or alkyloxy radical, R" is a fluorine atom or a hydroxy radical, and R'" is a hydrogen atom, or else R' and R'" are hydroxy radicals, or R" and R'" together form a bond, and R.sup.o is a hydrogen atom or a protective radical; salts thereof whereever applicable; and preparation thereof. These products are synthetic intermediates for the preparation of derivatives having P substance antagonist activity.
Type:
Grant
Filed:
October 11, 1994
Date of Patent:
October 31, 1995
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Daniel Achard, Serge Grisoni, Jean-Luc Malleron, Jean-Francois Peyronel, Michel Tabart
Abstract: This invention relates to the process for the preparation of novel 1,4-substituted piperidine derivative based solid compositions in micronized or hydrophilic form.
Type:
Grant
Filed:
June 1, 1994
Date of Patent:
October 24, 1995
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Jean-Marc Bobee, Guillaume Conrath, Gabriel Gousset, Michel Ponsot, Michel Veillard
Abstract: Process for producing 10-deacetylbaccatin III from the various parts of the yew (Taxus sp.) by extraction and selective crystallization from a methanolic extract of the plant mass.
Abstract: This invention relates to derivatives of perhydroisoindol of formula: ##STR1## in which the radicals R are hydrogen atoms or together form a bond, the symbols R' are phenyl radicals which can be substituted by a halogen atom or a methyl radical in position 2 or 3, X is an oxygen atom or an NH radical, R.sub.1 is optionally substituted phenyl, or cyclohexadienyl, naphthyl, or heterocyclyl, R.sub.2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino, R.sub.3 is halogen or OH and R.sub.4 is H or halogen if R.sub.3 is halogen, in their isomer forms, or mixture thereof, and possibly also their salts when they exist, and preparation thereof. The derivatives of the invention are particularly interesting as P substance antagonist.
Type:
Grant
Filed:
November 17, 1993
Date of Patent:
September 19, 1995
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Daniel Achard, Serge Grisoni, Stephen Hanessian, Claude Moutonnier, Jean-Francois Peyronel, Michel Tabart, Alain Truchon
Abstract: The present invention relates to new taxoid-based compositions consisting of solutions of these derivatives in a surface-active agent.These solutions are used for preparing perfusion solutions.
Type:
Grant
Filed:
November 22, 1993
Date of Patent:
August 1, 1995
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Jean-Marc Bobee, Patrick de Lanty, Gilles Guerin, Michel Veillard
Abstract: Process for transforming (benzoyl-3-phenyl)-2-propionic-R(-) acid into an S(+) isomer through the action of a base either in situ during the splitting of racemic ketoprofen or on the crystallization mother liquor of a (benzoyl-3-phenyl)-2-propionic-S(+) acid salt.
Type:
Grant
Filed:
March 16, 1994
Date of Patent:
June 20, 1995
Assignee:
Rhone-Poulenc Rorer, S.A.
Inventors:
Claude Bertrand, Elie Fouque, Isidore Le Fur, Jean-Paul Richard
Abstract: This invention relates to the process for the preparation of a method for preparing derivatives of formula (I), ##STR1## wherein R is an alkyl, alkoxy, alkylthio, polyfluoroalkyl, polyfluoroalkoxy, alkenyl, phenyl, alkylsulphonyl, alkoxycarbonyl, amino, cyano, sulphonamide or dialkylcarbamyl radical, characterized in that a derivative of formula (II), ##STR2## wherein R has the same meaning as in formula (I), is reacted with nitronium tetrafluoroborate and derivatives of formula (II).
Type:
Grant
Filed:
June 13, 1994
Date of Patent:
June 13, 1995
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Francois Audiau, Patrick Jimonet, Serge Mignani
Abstract: This invention relates to compounds of formula (I): ##STR1## wherein R is a polyfluoroalkoxy, polyfluoroalkyl, alkoxy or alkyl radical and R.sub.1 is a hydrogen atom or an alkyl radical; salts thereof; the preparation thereof; and drugs containing same.
Type:
Grant
Filed:
December 7, 1993
Date of Patent:
April 4, 1995
Assignee:
Rhone Poulenc Rorer S.A.
Inventors:
Francois Audiau, Patrick Jimonet, Serge Mignani
Abstract: Compositions containing taxane derivatives, consist of a solution of such derivative in a surfactant consisting of polysorbate, polyethelene glycol or hydrogenated castor oil. These compositions can be used to prepare perfusion solutions essentially free of ethanol.
Abstract: Formulations of spiramycin granules may be conducted by preparing a solution of albumin in the presence of an antifoaming agent, separately preparing a suspension of spiramycin in the presence of an antifoaming agent, granulating and drying a mixture of one or more sugars and water, mixing the albumin solution and spiramycin suspension with heating to coagulate the albumin, evaporating the solvents to obtain spiramycin granules, and mixing the sugar granules and spiramycin granules. Oral spiramycin formulations prepared according to this method are also disclosed.
Type:
Grant
Filed:
July 16, 1993
Date of Patent:
April 4, 1995
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Ana Calvo, Luis A. Del Rio, Manuel Esteban, Robert Rona
Abstract: This invention relates to a process for obtaining 10-deacetylbaccatin III from various parts of yew (Taxus sp.) by extraction and selective crystallization starting with a methanolic extract of the vegetable matter.
Abstract: This invention relates to a process for obtaining 10-deacetylbaccatin III from various parts of yew (Taxus sp.) by extraction with a suitable organic solvent of the aqueous solution obtained after treating the appropriate part of yew with water, followed by selective crystallization of 10-deacetylbaccatin III.
Abstract: Process for preparing pure ascorbic acid from 2-keto-L-gulonic acid or its sodium salt, by carrying out the following successive steps:esterification of 2-keto-L-gulonic acid or its sodium saltlactonization to sodium ascorbateoptional separation of the sodium ascorbatedisplacement of the ascorbic acid from its saltseparation of the sodium sulphateseparation and purification of the ascorbic acid from its methanolic or aqueous-methanolic solution.
Type:
Grant
Filed:
December 23, 1993
Date of Patent:
February 21, 1995
Assignee:
Rhone Poulenc Rorer S.A.
Inventors:
Isidore Le Fur, Jean-Paul Richard, Gerard Wolff
Abstract: Heterogeneous intimate admixtures of sulfated heparinic polysaccharides, well suited for the prophylaxis/treatment of acute thrombotic episodes in a human patient, comprise immixture of sulfated polysaccharides having a weight average molecular weight less than that of heparin and which include from 9% to 20% of polysaccharide chains having a molecular weight less than 2,000 daltons and from 5% to 20% of polysaccharide chains having a molecular weight greater than 8,000 daltons, the ratio between the weight average molecular weight and the number average molecular weight thereof ranging from 1.3 to 1.6.
Abstract: Compounds of formula: ##STR1## in which R.sub.1 represents a hydrogen atom or an alkyl, alkoxycarbonyl or an unsubstituted or substituted phenyl radical,R.sub.2 represents a hydrogen atom or an unsubstituted or substituted alkyl radical,R.sub.3 represents an alkyl, phenylalkyl, indanyl, cycloalkylalkyl or an unsubstituted or substituted phenyl radical, orR.sub.2 and R.sub.3 form a heterocycle together with the nitrogen atom to which they are attached, andR.sub.4 represents an unsubstituted or substituted phenyl radical, a naphthyl, indolyl or quinolyl radical or a phenylamino radical in which the phenyl ring is unsubstituted or substituted, their preparation and medicaments containing them.
Type:
Grant
Filed:
July 8, 1992
Date of Patent:
January 17, 1995
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Jean-Dominique Bourzat, Marc Capet, Claude Cotrel, Claude Guyon, Franco Manfre, Gerard Roussel
Abstract: Process for the preparation of pearls based on a pharmaceutical active substance exhibiting an indefinite crystallization point.The said active substance is mixed in molten form with a pharmaceutical excipient promoting the solidification of the active substance, the melt is forced to pass through a nozzle which is subjected to a vibration, the pearls formed are allowed to fall in a tower countercurrentwise to a gas, and the pearls formed are collected in the bottom of the tower.
Type:
Grant
Filed:
July 21, 1992
Date of Patent:
January 10, 1995
Assignee:
Rhone-Poulenc Rorer, S.A.
Inventors:
Michel Deleuil, Pierre Labourt-Ibarre, Robert Rona, Eraclis Statiotis
Abstract: This invention relates to compounds of formula: ##STR1## in which R.sub.1 represents a hydrogen atom or an alkyl or alkoxycarbonyl radical or an unsubstituted or substituted phenyl radical,R.sub.2 represents an alkyl (1-8 C) or polyfluoroalkyl radical or an unsubstituted or substituted cycloalkyl radical,R.sub.3 represents an unsubstituted or substituted phenyl radical, a naphthyl, indolyl, quinolyl or phenylamino radical in which the phenyl ring is optionally substituted, or a quinolylamino radical, andm is 0 or 1, the process for preparing them and the medicaments containing them.
Type:
Grant
Filed:
June 25, 1992
Date of Patent:
December 20, 1994
Assignee:
Rhone-Poulenc Rorer, S.A.
Inventors:
Jean-Dominique Bourzat, Marc Capet, Claude Cotrel, Claude Guyon, Franco Manfre, Gerard Roussel
Abstract: This invention relates to compounds having selective LTB.sub.4 antagonist properties, compositions comprising said compounds and methods for the treatment of disorders involving LTB.sub.4 agonist-mediated activity utilizing said compositions wherein the compounds are described by the general formula ##STR1## and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
February 17, 1993
Date of Patent:
November 22, 1994
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Norbert Dereu, Wolfram Hendel, Richard Labaudiniere
Abstract: Method for preparing (dialkylamino-2 alkyl)sulphonyl-26 pristinamycin II.sub.B having general formula (I) ##STR1## by oxidation of (dialkylamino-2 alkyl)thio-26 pristinamycin II.sub.B with 3,5 to 20 of hydrogenperoxide equivalent, in the presence of alcaline metal tungstate, in a 2-phase medium, at a temperature between 10.degree. and 25.degree. C.