Abstract: This invention relates to an optically active hydroquinine (amino-3 phenyl)-1 ethanesulfonate (form A), preparation thereof and its use as an intermediate in the preparation of cholecystokinine and gastrin antagonists.
Abstract: The invention relates to the application of riluzole or the pharmaceutically acceptable salts of this compound in the treatment of neuro-AIDS.
Abstract: Perhydroisoindole derivatives of formula I, wherein the substituents are as defined in the specification, are particularly suitable as substance P antagonists. Several processes for preparing the compounds are also taught.
Type:
Grant
Filed:
January 29, 1996
Date of Patent:
April 29, 1997
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Daniel Achard, Serge Grisoni, Evelyne James-Surcouf, Jean-Luc Malleron, Anne Morgat, Jean-Fran.cedilla.ois Peyronel, Jean-Fran.cedilla.ois Sabuco, Michel Tabart
Abstract: Method of preparation of 6-fluoro-2-halogen quinoline of general formula (I) wherein R is a hydrogen atom or an alkyl radical and Hal and Hal' are identical or different halogen atoms. The invention is characterized in that a halogenating agent is made to act on hydroxy-1 quinoline of general formula (II) wherein Hal is defined as above and R.sub.1 is defined as R excepting a hydrogen atom, the acid function being optionally released if a 6-fluoro-2-halogen quinoline is to be obtained for which R is a hydrogen atom.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
April 29, 1997
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Herve Garcia, Roland Jacquot, Patrick Leon
Abstract: This invention relates to a method of preparing taxane derivatives of formula (I) by esterification of protected baccatin III or 10-deacetylbaccatin III by means of an acid of formula (VII), elimination of protection groupings and acylation of the amine function of the side chain. The products of formula (I) have remarkable antitumor and antileukemia properties. In formulae (I) and (VII): Ar stands for aryl, R is hydrogen or acetyl, R.sub.1 is a benzoyl radical or an R.sub.2 --O--CO-- radical in which R.sub.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, R.sub.3 is a trihalomethyl radical or phenyl substituted by a trihalomethyl radical, R.sub.4 is a hydrogen atom or is the same as R.sub.1.
Type:
Grant
Filed:
April 5, 1995
Date of Patent:
April 15, 1997
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Alain Commercon, Eric Didier, Elie Fouque
Abstract: This invention relates to a method of preparing taxane derivatives of general formula (I) by esterification of protected baccatine III or 10-deacetylbaccatine III by means of an acid of general formula (VII), elimination of protection groupings of the ester obtained, and acylation of the amine function of the side chain. In formulae (I) and (VII): Ar stands for aryl, R is hydrogen or acetyl, R.sub.1 is benzoyl or R.sub.2 --CO--O-- in which R.sub.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, R.sub.3 and R.sub.4 may be the same or different and represent hydrogen, alkyl, alkenyl, aralkyl, aryl or alkoxy, and R.sub.5 is an alkyl radical substituted by one or more chlorine atoms (2,2,2-trichloroethyl, (2-trichloromethylisopropyl).
Abstract: The present invention relates to DNA sequences comprising all or part of the K. lactis TAL1 gene promoter or of a derivative thereof and having a transcriptional promoter activity. It also relates to the use of these sequences for expression of recombinant genes.
Abstract: The present invention relates to a preparation of serum-human albumin having a colorimetry index lower than 0.2 resulting from the expression, in a eukaryotic or prokaryotic host, of an exogenous DNA sequence.
Type:
Grant
Filed:
July 27, 1994
Date of Patent:
March 18, 1997
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
J er ome Becquart, Reinhard Fleer, G erard Jung
Abstract: This invention relates to compositions of formula: ##STR1## and their salts, their preparation and the medicaments containing them.
Type:
Grant
Filed:
June 27, 1994
Date of Patent:
March 11, 1997
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Marc Capet, Claude Cotrel, Claude Guyon, Michel Joannic, Franco Manfre, G erard Roussel, Marie-Christine Dubroeuco, Michel Cheve, Gilles Dutruc-Rosset
Abstract: This invention relates to a method for preparing .beta.-phenylisoserine and analogues thereof having general formula (I) ##STR1## from an aromatic aldehyde and an .alpha.-methylarylamine-S, and through a lactam of general formula (II) as described herein. The acids of general formula (I) (R.dbd.H) may be used to prepare taxane derivatives having remarkable antitumoral and antileukaemic activity.
Abstract: This invention relates to novel anhydrides of general formula (I), ##STR1## wherein Ar is an aryl radical, and either R.sub.1 is C.sub.6 H.sub.5 --CO or (CH.sub.3).sub.3 C--O--CO, R.sub.2 is a hydrogen atom and R.sub.3 is a hydroxy function protective grouping, or R.sub.1 is (CH.sub.3).sub.3 C--O--CO and R.sub.2 together form a saturated 5 or 6-membered heterocyclic ring; preparation thereof; and uses thereof for preparing taxane derivatives having general formula (III), ##STR2## wherein R=H, acetyl; R.sub.1 is C.sub.6 --H.sub.5 --CO or (CH.sub.3).sub.3 C--O--CO), and having antitumoral properties.
Abstract: This invention relates to a method for the preparation of taxane derivatives having the formula (I) and pharmaceutical compositions which contain the derivatives thus obtained. In formula (I), R is hydrogen or acetyl, R.sub.1 is benzoyl or R.sub.2 --O--CO wherein R.sub.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl and Het is a 5-membered optionally substituted aromatic heterocycle (thiophene, tiazole, furan, pyrrole, imidazole, oxazole, isoxazole, pyrazole). The products of formula (I) have remarkable antitumor and antileukemia properties.
Abstract: The present invention concerns aqueous pharmaceutical compositions based on 1,4-substituted derivatives of piperidine characterized in that the composition contains a solubilizing agent and does not contain a surfactant. The solubilizing agent for the active principle is polyethylene glycol.
Abstract: This invention concerns a process for enzymatically preparing a compound of formula (1) ##STR1## from the compound of formula (2) ##STR2## by way of a microorganism or an acellular preparation derived from this microorganism. The microorganism and acellular preparation oxidizes the 2-3 bond of the macrolactones' D-proline into dehydroproline.
Abstract: The invention relates to a process for preparing taxoids of formula I herein that includes the steps of esterifying a baccatin III derivative of the formula VI herein, acylating the compound obtained, and optionally removing a protecting group to give the desired taxoid product.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
December 24, 1996
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Herv e Bouchard, Jean-Dominique Bourzat, Alain Commercon
Abstract: New Baccatin III derivatives are disclosed for use in making taxoid compounds having formula (I) illustrated herein that exhibit antitumor activity.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
December 3, 1996
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Herv e Bouchard, Jean-Dominique Bourzat, Alain Commercon
Abstract: The invention relates to a process for preparing taxoids of formula I herein that includes comprising the steps of esterifying a baccatin III derivative of the formula VI herein, treating the compound obtained in acidic medium, and optionally removing a protecting group to give the desired taxoid product.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
December 3, 1996
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Herv e Bouchard, Jean-Dominique Bourzat, Alain Commercon
Abstract: This invention relates to process for the preparation of a taxane derivative of general formula (I): ##STR1## and use of the product obtained for the preparation of taxane derivatives of general formula (II): ##STR2## In the general formula (I), R.sub.1 is an acetyl radical or a protective grouping G.sub.1 is a protective grouping and R is a t-butoxy or phenyl radical. In the general formula (II), R is a t-butoxy or phenyl radical and R'.sub.1 is a hydrogen atom or an acetyl radical.
Abstract: The invention relates to a process for preparing taxoids of formula I herein that includes the steps of esterifying a baccatin III derivative of the formula VI herein, treating the compound obtained in acidic medium, and optionally removing a protecting group to give the desired taxoid product.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
November 19, 1996
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Herv e Bouchard, Jean-Dominique Bourzat, Alain Commer.cedilla.on