Abstract: New taxoids of general formula (I), their preparation, and pharmaceutical compounds containing them.
In general formula (I), for example,
Ar represents an aryl radical,
R represents an alkoxyacetyl radical,
R1 represents a benzoyl radical or a radical of formula R2—O—CO— in which R2 represents an optionally substituted alkyl radical, an alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical. The new products of general formula (I) have a remarkable antitumor activity.
Abstract: The present invention relates to mixtures which can be isolated from grains of Eugenis Jambolana Lamarck, the preparation of such mixtures, the medicaments containing said mixtures or constituents of said mixtures, and the use of these mixtures and constituents for the preparation of a medicament.
Type:
Grant
Filed:
June 9, 1999
Date of Patent:
February 27, 2001
Assignees:
Rhone-Poulenc Rorer S.A., Institut Malgache de Recherches
Inventors:
Albert Rakoto Ratsimamanga, Suzanne Rakoto Ratsimamanga, Philippe Rasoanaivo, Jean Leboul, Jean Provost, Daniel Reisdorf
Abstract: The present invention relates to injectable compositions containing a dalfopristine/quinupristine combination comprising an aqueous solution containing the dalfopristine/quinopristine combination and an additive intended to avoid or reduce the intolerance effects at the site of injection.
Type:
Grant
Filed:
December 15, 1998
Date of Patent:
February 13, 2001
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Guillaume Conrath, Joël Vacus, Nicholas Paul Barker
Abstract: Peptides capable of inhibiting the transforming activity of activated p21 proteins, their preparation and compositions containing them are disclosed. Particular regions of the GAP protein have been identified and characterized that are involved in the transduction of activation signals of p21 proteins. Peptides derived from GAP protein but carrying an effector region rendered non-functional have been shown to inhibit the p21 signaling route. The products according to the invention are useful in pharmaceutical compositions to inhibit the transformation activity of ras genes whose transformation proceeds by a functional p21-GAP interaction.
Type:
Grant
Filed:
April 24, 1995
Date of Patent:
January 30, 2001
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Marc Duchesne, Fabien Schweighoffer, Bruno Tocque
Abstract: Novel taxoids of general formula (I), the preparation thereof and pharmaceutical compositions containing same, are disclosed. In general formula (I), Z is a hydrogen atom or a radical of general formula (H), wherein R.sub.1 is an optionally substituted benzoyl radical or a radical R.sub.2 --O--CO--, where R.sub.2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl or heterocyclyl radical; R.sub.3 is an alkyl, alkenyl, alkyl, cycloalkyl, phenyl, naphthyl or aromatic heterocyclic radical; R.sub.4 is a hydroxy radical or an alkoxy, alkenyloxy, optionally substituted alkynyloxy, alkanoyloxy, alkenoyloxy, alkynyloxy, alkoxyacetyl or alkyloxycarbonyloxy radical, or a cycloalkyloxy, cycloalkenyloxy, arylcarbonyloxy or heterocyclylcarbonyloxy radical; and R.sub.5 is an optionally substituted alkoxy radical or a cycloalkyloxy or cycloalkenyloxy radical.
Abstract: The present invention relates to a biosynthetic process for preparing cobalamines. More precisely, it relates to a process for amplifying the production of cobalamines and, more specifically, of coenzyme B.sub.12 by means of recombinant DNA techniques and/or by means of adding a novel cobalamine precursor.
Type:
Grant
Filed:
March 2, 1999
Date of Patent:
December 5, 2000
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Francis Blanche, Beatrice Cameron, Joel Crouzet, Laurent Debussche, Denis Thibaut, Elisabeth Remy
Abstract: This invention relates to a method for treating abnormal cell proliferation in the brain by administering a compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof: ##STR1## in which R represents a hydrogen atom or an acetyl, alkoxyacetyl or alkyl radical, R.sub.1 represents a benzoyl radical or a radical R.sub.2 --O--CO-- wherein R.sub.2 represents an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclylic radical, and Ar represents an aryl radical.
Abstract: This invention relates to the use of heterocyclic carboxamide compounds for preventing or reducing self-administration, by a human or animal patient, of a drug or a substance capable of giving rise to pharmacomania or to overuse. The preferred types of drugs or substances are nicotine, caffeine, benzodiazepines, narcotics, and hallucinogens.
Type:
Grant
Filed:
August 7, 1998
Date of Patent:
November 21, 2000
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Andrees Bohme, Marie-Christine Dubroeucq, Walter Fratta, Claude Guyon, Assunta Imperato, Franco Manfre
Abstract: This invention relates to stabilized nanoparticles which may be filtered under sterile conditions, comprising at least one hydrophobic, water-insoluble and non-water-dispersible polymer or copolymer (and optionally an active principle) which is emulsified in an aqueous solution or suspension comprising a phospholipid and a bile salt.
Type:
Grant
Filed:
September 9, 1997
Date of Patent:
November 14, 2000
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Marie-Christine Bissery, Michel Laborie, Joel Vacus, Thierry Verrecchia
Abstract: The present invention pertains to the use of compounds affecting the activity of transcription factors for the preparation of a pharmaceutical composition for the treatment of neurodegenerative diseases.
Type:
Grant
Filed:
April 25, 1996
Date of Patent:
October 31, 2000
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Jacques Mallet, Frederic Revah, Jean-Jacques Robert
Abstract: The invention relates to cells usable for the production of defective adenoviruses comprising, inserted into their genome, a portion of the region E4 of an adenovirus genome carrying the reading phase ORF6 under the control of a functional promoter.
Abstract: Yeast strains expressing human genes coding regulating cytochrome P450 expression, a method for making same and applications thereof are described.
Type:
Grant
Filed:
May 4, 1998
Date of Patent:
September 12, 2000
Assignees:
Centre National de la Recherche, Rhone-Poulenc Rorer S.A.
Abstract: A .beta.-phenylisoserine derivative of general formula (I): ##STR1## in the form of a salt or an ester, in which Ar represent an aryl radical, R represents a phenyl or naphthyl or a O--R.sub.1 radical and G.sub.1 represents --CH.sub.2 --Ph radical; and a method of using the same for making taxane derivatives.
Type:
Grant
Filed:
November 10, 1997
Date of Patent:
September 5, 2000
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Jean-Noel Denis, Andrew-Elliot Greene, Alice Kanazawa
Abstract: Cationic lipids of general formula (I), wherein m is an integer from 2 to 6 inclusive; n is an integer from 1 to 9 inclusive, preferably 1-5, where, when n is 2-9, a single R grouping other than hydrogen is present in the general formula, and m has variable or identical values within the groupings (a) or --(CH.sub.2).sub.m ; R is a hydrogen atom or a radical of general formula (II), wherein X or X.sup.1, which are the same or different, are an oxygen atom, a methylene grouping --(CH.sub.2).sub.q -- where q is 0, 1, 2 or 3, or an amino grouping --NH-- or NR.sup.1 --, where R is a C.sub.1-4 alkyl grouping; Y and Y.sup.1, which are the same or different, are a hydrogen atom or an optionally substituted C.sub.1-4 alkyl radical, and p is 0-5; and R.sub.6 is a cholesterol derivative or an alkylamino grouping --NR.sub.1 R.sub.2, where R.sub.1 and R.sub.2 are, independently of each other, a straight or branched, saturated or unsaturated C.sub.12-22 aliphatic radical.
Type:
Grant
Filed:
June 4, 1997
Date of Patent:
August 22, 2000
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Gerardo Byk, Daniel Scherman, Catherine Dubertret
Abstract: A compound of the formula ##STR1## in which Ra represents an -alk-COOalk' radical, a --CH.sub.2 --PO(Oalk).sub.2 radical, a --CH.dbd.CH--COOalk' radical or a phenyl radical substituted with an alkoxycarbonyl radical.
Type:
Grant
Filed:
July 13, 1999
Date of Patent:
August 8, 2000
Assignee:
Rhone-Poulenc Rorer, S.A.
Inventors:
Jean-Claude Aloup, Jean Bouquerel, Dominique Damour, Jean-Claude Hardy, Patrick Jimonet, Franco Manfre, Serge Mignani, Patrick Nemecek
Abstract: A compound of formula (II): ##STR1## in which R is a hydrogen atom or a carboxy, alkoxycarbonyl, --CO--NR.sub.4 R.sub.5, --PO.sub.3 H.sub.2 or --CH.sub.2 OH radical, and R.sub.1 is an -alk-NH.sub.2, -alk-NH--CO--R.sub.3, -alk-COOR.sub.4, -alk-CO--NR.sub.5 R.sub.6 or --CO--NH--R.sub.7 radical. The compounds of formula (II) can be used to prepare compounds of formula (I): ##STR2## in which R and R.sub.1 have the same meanings as above. The compounds of formula (I) have valuable pharmacological properties and are antagonists of the .alpha.-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor, also known as the quisqualate receptor. The compounds of formula (I) are also non-competitive antagonists of the N-methyl-D-aspartate (NMDA) receptor and more specifically are ligands for NMDA receptor glycine modulator sites.
Type:
Grant
Filed:
December 4, 1998
Date of Patent:
May 2, 2000
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Jean-Claude Aloup, Fran.cedilla.ois Audiau, Michel Barreau, Dominique Damour, Arielle Genevois-Borella, Jean-Claude Hardy, Patrick Jimonet, Franco Manfre, Serge Mignani, Patrick Nemecek, Yves Ribeill
Abstract: A method of preparing a taxoid of formula III by esterifying protected baccatin III or deacetylbaccatin III using an oxazolidinecarboxylic acid, or an acid halide, or an acid anhydride thereof.
Abstract: The present invention relates to recombinant adenoviruses having a cassette capable of integrating into the genome of infected cells, their preparation, pharmaceutical compositions containing them, and their use. In particular, the cassette contains at least one inverted terminal repeat (ITR) Sequence from AAV and a heterologous DNA Sequence.
Type:
Grant
Filed:
September 12, 1996
Date of Patent:
March 7, 2000
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Martine Latta, Patrice Denefle, Emmanuelle Vigne, Michel Perricaudet
Abstract: Process for the preparation of 4-acetoxy-2.alpha.-benzoyloxy-5.beta.,20-epoxy-1,7.beta., 10.beta.-trihydroxy-9-oxo-tax-11-en-13.alpha.-yl (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate trihydrate, characterized in that the 4-acetoxy-2.alpha.-benzoyloxy-5.beta.,20-epoxy-1,7.beta.,10.beta.-trihydro xy-9-oxo-tax-11-en-13.alpha.-yl (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate is crystallized from a mixture of water and an aliphatic alcohol containing 1 to 3 carbon atoms, and then the product obtained is dried under defined conditions of temperature, pressure and humidity.