Abstract: 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.
Abstract: New formulations of spiramycin suitable for oral administration, particularly for children, comprise spiramycin and potassium acesulfame. These formulations mask the bitterness of spiramycin without adversely affecting the bioavailability or stability of the spiramycin. Preparation by wet granulation followed by dry state mixing is also disclosed.
Abstract: The present invention relates to a process for the preparation of (1R,2R)-N-methyl -2-(3-pyridyl)tetrahydrothiopyran-2-carbothioamide 1-oxide of formula: ##STR1## which is particularly useful as an antihypertensive and as a cardioprotective agent.
Abstract: A method for the treatment of mitochondrial diseases, including Kearns-Sayre syndrome, MERRF syndrome, MELAS syndrome and Leber's disease, is carried out by administering to a patient in need of treatment an effective amount of riluzole or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
July 11, 1996
Date of Patent:
November 11, 1997
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Jean-Christophe Delumeau, Michel Martinet, Michel Reibaud, Jean-Marie Stutzmann
Abstract: A method for preparing taxane derivatives of general formula (I) by esterifying protected baccatin III or protected 10-deacetyl baccatin III with an acid of general formula (II). In general formulae (I) and (II), Ar is an aryl radical; R.sub.1 and R.sub.2 which are the same or different, are a hydrogen atom, an alkyl, phenylalkyl, phenyl, alkoxyphenyl or dialkoxyphenyl radical, or R.sub.1 or R.sub.2, together with the carbon atom to which they are attached, form a 4-7 membered ring; R.sub.3 is an acetyl radical or a hydroxy function protective grouping, and R.sub.4 is a hydroxy function protective grouping; R is a phenyl radical or a radical of formula R.sub.5 --O-- wherein R.sub.5 -- is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, phenyl or saturated or unsaturated nitrogenous heterocylcyl radical. The products of general formula (I) are particularly useful for preparing taxol, Taxotere and analogues thereof having remarkable antitumor properties.
Type:
Grant
Filed:
April 28, 1995
Date of Patent:
November 11, 1997
Assignee:
Rhone-Poulenc Rorer, S.A.
Inventors:
Jean-Noel Denis, Andrew-Elliot Greene, Alice Kanazawa
Abstract: Thiazolidine derivatives of formula (I), in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined in the specification. The invention also concerns the salts of these derivatives, the preparation thereof and drugs containing same.
Type:
Grant
Filed:
December 19, 1996
Date of Patent:
November 11, 1997
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Marc Capet, Marie-Christine Dubroeucq, Claude Guyon, Franco Manfre
Abstract: .beta.-phenylisiserine-(2R,3S), salts and preparation thereof through the action of ammonia on .beta.-phenylglycidic-(2R,3R) acid and its use in the preparation of taxane derivatives of general formula: ##STR1## wherein R is hydrogen or --COCH.sub.3 ;and R.sub.1 is phenyl or --O--C(CH.sub.3).sub.3.
Abstract: The invention discloses nanoparticles offering an extended time before capture by the reticulo-endothelial system. Said particles are composed of an ethylene and/or propylene polyoxide polylactic copolymer optionally mixed with a polylactic polymer.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
November 4, 1997
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Gilles Spenlehauer, Didier Bazile, Michel Veillard, Christian Prud'Homme, Jean-Paul Michalon
Abstract: A method according to the invention is directed to the preparation of a 2-azadihydroxybicyclo?2.2.1!heptane compound of formula ##STR1## wherein * represents an R chirality, *' represents an S chirality, R is hydrogen or, respectively, a group of formula ##STR2## wherein R.sub.1 is alkyl and Ar is optionally substituted aryl, comprising bishydroxylating a bicyclo?2.2.1!heptene compound of formula ##STR3## wherein *, *' and R are as previously defined, in the presence of about 0.1 mol to about 5 mol % of a metal osmate compound or about 0.06 mol % to about 0.07 mol % osmium tetroxide, and an oxidizing agent capable of regenerating osmium tetroxide.The invention is also directed to the treatment of the (1R) diastereomer of the 2-azadihydroxybicyclo?2.2.1!heptane compound (I) wherein R is a group of formula II with L-tartaric acid, and the L-tartaric acid salt product thereof. Furthermore, the invention is directed to using the (1R) diastereomer of the 2-azadihydroxybicyclo?2.2.
Type:
Grant
Filed:
October 16, 1996
Date of Patent:
November 4, 1997
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Michael O'Brien, Patrick Leon, Denis Largeau, Matthew Powers, Thierry Durand
Abstract: Method for the preparation of .beta.-phenylisoserine derivatives of general formula (I) involving the action of an anhydride and hydrogen with a product of general formula (II). The products of general formula (I) are especially useful in the preparation of taxoids having outstanding antitumour properties. In general formulae (I) and (II), Ar is an aryl radical, Ph is a phenyl radical or an optionally substituted .alpha. or .beta.-naphtyl, R is a hydrogen atom or an alkyl radical optionally substituted by a phenyl radical and R.sub.1 is an optionally substituted phenyl radical or a R.sub.2 --O radical wherein R.sub.2 is an alkyl, alkenyl, cycloalkyl, phenyl or heterocyclyl.
Abstract: The present invention concerns yeasts of the genus Kluyveromyces having one or more genetic modifications of at least one gene coding for a protease, said gene reducing or modifying the proteolytic actively of said yeasts, as well as their use as a cellular host for the secretion of recombinant proteins.
Abstract: Disclosed is a compound of formula VII: ##STR1## where Ar represents an optionally substituted phenyl or .alpha.- or .beta.-naphthyl radical; R.sub.3 represents hydrogen, a C.sub.1-4 alkyl radical, a C.sub.2-4 alkenyl radical, an aralkyl radical, or an aryl radical; and R.sub.4 represents hydrogen, a C.sub.1-4 alkyl radical, a C.sub.2-4 alkenyl radical, an aralkyl radical, or an aryl radical; or alternatively R.sub.3 and R.sub.4, together with the carbon atom to which they are linked, form a 4- to 7-membered ring; and R.sub.5 represents an C.sub.1-4 alkyl radical substituted with at least one chlorine atom. The compound of formula VI may be used to manufacture a compound of formula VIII: ##STR2## where Ar, R.sub.3, R.sub.4 and R.sub.5 are defined above; G.sub.1 represents a group protecting the hydroxyl function; and where appropriate, G.sub.2 represents a group protecting the hydroxyl function.
Abstract: Compounds having the formula (I) wherein R and R.sub.1, similar or different, represent a hydrogen or halogen atom or a radical alkyl, alkoxy, amino, acylamino, phenylureido, --N.dbd.CH--N(R.sub.2)R.sub.3, nitro, imidazolyl, phenyl, SO.sub.3 H or cyano; R.sub.2 and R.sub.3 which may be similar or different, represent each an alkyl radical; the invention also relates to the salts of such compounds, their preparation, intermediates for preparing them and drugs containing them.
Abstract: This invention relates to an application of riluzole or the pharmaceutically acceptable salts in the preparation of drugs for the treatment of Parkinson's disease and parkinsonian syndromes.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
October 7, 1997
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Alain Boireau, Adam Doble, Pierre Dubedat, Erik Louvel, Mireille Meunier, Jean-Marie Miquet, Jean-Marie Stutzmann
Abstract: Compounds of formula (I), wherein R is an oxygen or sulphur atom or an NH or N-alk radical, and each of R.sub.1 and R.sub.2, which are the same or different, is a hydrogen or halogen atom or an alkyl, alkoxy, amino, acylamino, --NH--CO--NH--Ar,--N.dbd.CH--N(alk)alk', nitro, cyano, phenyl, imidazolyl or SO.sub.3 H radical, the preparation thereof, and drugs containing such compounds, are disclosed.
Abstract: The present invention relates to a novel process for the preparation of 7-trialkylsilylbaccatin III of general formula: ##STR1## in which the symbols R, which may be identical or different, represent alkyl radicals containing 1 to 4 carbon atoms which are optionally substituted with a phenyl radical, starting with 10-deacetylbaccatin III of formula: ##STR2## In the general formula (I), each of the symbols R preferably represents a straight or branched alkyl radical containing 1 to 4 carbon atoms. Even more particularly, each of the symbols R represents an ethyl radical.
Abstract: Novel derivatives of 1R- or 1S-2-azabicyclo?2.2.1!heptane with the general formula (I) or (I'), their preparation and their application. ##STR1## In the general formulas (I) and (I'), R represents a hydrogen atom or a group with the formula ##STR2## respectively, in which R.sub.1 represents an alkyl group containing 1-4 carbon atoms and Ar represents an optionally substituted phenyl or .alpha.- or .beta.-naphthyl group.The novel products with the general formula (I) are particularly useful for the preparation of adenosine agonists.
Abstract: This invention relates to a pharmaceutical composition comprising as active principle, docetaxel or a taxoid derived from docetaxel, one or more unsaturated phospholipids and a small amount of one or more negative phospholipids, allow the active principle to be formulated in high concentration and are suitable for administration by injection.
Abstract: New polypeptides having granulocyte colony stimulating activity, preparation thereof and pharmaceutical compositions containing said polypeptides.
Abstract: Stable, pharmaceutical ketoprofen salts for oral administration are provided in oily solutions to avoid direct contact of acid forms of ketoprofen with the gastric or duodenal mucus membranes. Sodium, arginine, lysine and/or N-methylglucamine salts of ketoprofen are disclosed in solutions of polyoxyethyenatide vegetable oil, castor oil, esters of fatty acids and/or polyols. These oily solutions of ketoprofen may be administered orally in capsule form.