Abstract: New taxoids of general formula (I), their preparation and pharmaceutical compositions containing them.In general formula (I),Ar represents an aryl radical,R represents a hydrogen atom or an acetyl, alkoxyacetyl or alkyl radical,R.sub.1 represents a benzoyl radical or a radical of formulaR.sub.2 --O--CO-- in which R.sub.2 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 antitumour activity.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
November 5, 1996
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Herv e Bouchard, Jean-Dominique Bourzat, Alain Commercon
Abstract: This invention relates to the process for the preparation of 2-amino 7-nitro benzothiazoles of formula (I) ##STR1## consisting in a) nitrating a derivative of formula (II) ##STR2## and b) reacting the compound of formula (III) ##STR3## so obtained with caustic ammonia.
Type:
Grant
Filed:
June 13, 1994
Date of Patent:
October 22, 1996
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Fran.cedilla.ois Audiau, Patrick Jimonet, Serge Mignani
Abstract: This invention relates to compounds having formula (I), ##STR1## wherein R.sub.1 is a hydrogen or halogen atom or an alkyl, alkoxy, alkylthio, nitro, hydroxy or cyano radical; R.sub.2 is an alkyl radical or a chain --CH(R.sub.5)--CO--R.sub.6 ; R.sub.3 is (a) a phenyl radical substituted by one or a plurality of substituents selected amongst the radicals -alk-SO.sub.3 H, -alk-PO.sub.3 H.sub.2, --CH.dbd.NOH, --CH--NO-alk-COOX, --S-alk-COOX, --SO-alk-COOX, --SO.sub.2 -alk-COOX, --CH.dbd.CH--COOX, -alk-CO--NHOH, --C(.dbd.NOH)--COOX, -alk-N(OH)--CO-alk,-alk-SO.sub.2 H, --CH.dbd.CH--SO.sub.3 H, --C(COOX).dbd.N--O-alk-COOX, tetrazolyalkyle or a group having a formula (I) or (b) a ring having the formula (A) ##STR2## wherein R.sub.9 is a radical .dbd.NOX, .dbd.NO-alk-COOX, .dbd.CH--COOX, -alk-COOX, -alk-SO.sub.2 H or -alk-S).sub.3 H, R.sub.10 is an oxygen or sulfur atom or a methylene or alkylimino radical and R.sub.11 is a methylene or ethylene radical, R.sub.
Type:
Grant
Filed:
April 6, 1994
Date of Patent:
October 8, 1996
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Marc Capet, Claude Cotrel, Marie-Christine Dubroeuco, Claude Guyon, Jean-Paul Martin
Abstract: This invention relates to compounds having the formula R.sub.1 -(CH.sub.2).sub.n -Het wherein R.sub.1 is a residue having the formula (B), (C), (D); Het represents a radical phenyl-4 tetrahydro-1,2,3,6 pyridyl-1 whose phenyl cycle is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical; a radical phenyl-4 piperazinyl-1 whose phenyl cycle is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical; R.sub.3 is a hydrogen atom or a phenyl radical; R.sub.4 is a hydrogen or halogen atom or a residue Het; R.sub.5 is a carbonyl or sulfonyl radical; R.sub.6 is a radical Si(CH.sub.3).sub.2 or C(CH.sub.3).sub.2 ; n equals 1, 2, 3 or 4; excepting {[(phenyl-4 tetrahydro-1,2,3,6 pyridyl-1)-2 ethyl] amino}-3 benzisothiazol-1,2 dioxyde-1,1; their salts, their preparation and medicaments containing them.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
October 8, 1996
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Dominique Damour, Richard Labaudiniere, Jean-luc Malleron, Serge Mignani
Abstract: This invention relates to taxoids of general formula (I), their preparation and the pharmaceutical compositions which contain them. The products of general formula (I) have notable antitumoral properties. In the general formula (I),Ar represents an aryl radical,R represents a hydrogen atom or an acetyl or alkoxyacetyl radical,R.sub.1 represents a benzoyl radical or a radical R.sub.2 --O--CO-- in which R.sub.2 represents an alkyl, alkenyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical, andR.sub.3 represents an alkyl, alkenyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted aryl (with the exception of unsubstituted phenyl) or heterocyclyl radical.
Type:
Grant
Filed:
March 2, 1994
Date of Patent:
September 17, 1996
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Herv e Bouchard, Jean-Dominique Bourzat, Alain Commer.cedilla.on, Jean-Pierre Pulicani
Abstract: Methods and devices for delivery of granulocyte-colony stimulating factor to a patient are disclosed. The method comprises continuous subcutaneous delivery of a solution comprising granulocyte-colony stimulating factor to the patient. Devices for continuous administration are also disclosed.
Type:
Grant
Filed:
January 20, 1995
Date of Patent:
September 10, 1996
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Anne Bousseau, Armand Frydman, Jean-Paul Plard, Gilles Spenlehauer, Michel Veillard
Abstract: New taxoids of general formula (I), their preparation and pharmaceutical compositions containing them.In general formula (I),Ar represents an aryl radical,R represents a hydrogen atom or an acetyl, alkoxyacetyl or alkyl radical,R.sub.1 represents a benzoyl radical or a radical of formula R.sub.2 --O--CO-- in which R.sub.2 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.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
August 27, 1996
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Herv e Bouchard, Jean-Dominique Bourzat, Alain Commercon
Abstract: New taxoids of general formula (I), their preparation and pharmaceutical compositions containing them.In general formula (I),Ar represents an aryl radicalR represents a hydrogen atom or an acetyl, alkoxyacetyl or alkyl radical,R.sub.1 represents a benzoyl radical or a radical of formula R.sub.2 --O--CO-- in which R.sub.2 represents an optionally substituted alkyl radical, an alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radicalThe new products of general formula (I) have a remarkable antitumour activity.
Abstract: Use of 2-amino-6-(trifluoromethoxy)benzothiazole, or a salt of this compound with a pharmaceutically acceptable acid, for obtaining a medicament intended for the treatment of motor neuron diseases, in particular amyotrophic lateral sclerosis, and especially amyotrophic lateral sclerosis with early bulbar involvement or the bulbar form of the disease.
Abstract: This invention relates to levogyral isomers of alkylammonium (amino-3 phenyl)-1 ethanesulphonate derivatives of formula (I) in which R+ denotes a tetraalkylammonium or trialkylphenylalkylammonium residue. The invention also concerns the preparation and use of said derivatives.
Abstract: The present invention relates to a pharmaceutical form based on cephalosporin. It relates in particularly to a tabletted pharmaceutical form.
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.sub.2 are phenyl radicals which can be substituted by a halogen atom or a methyl radical in position 2 or 3, R.sub.3 is a halogen atom or a hydroxy radical, 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:
April 16, 1996
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Daniel Achard, Serge Grisoni, Stephen Hanessian, Claude Moutonnier, Jean-Francois Peyronel, Michel Tabart, Alain Truchon
Abstract: This invention relates to a novel therapeutical use of phenzothiazine derivatives of general formula (I), ##STR1## wherein R is a straight or branched chain C.sub.1-5 alkyl radical, and R.sub.1 and R.sub.2, which are the same or different, are C.sub.1-2 alkyl radicals or form, together with the nitrogen atom to which they are attached, a pyrrolidinyl radical; and salts and stereoisomers thereof; having useful prophylactic and/or curative activity for the treatment of ischaemia and/or hypoxia.
Type:
Grant
Filed:
September 7, 1994
Date of Patent:
March 26, 1996
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Claude Garret, Jean Rataud, Jean-Marie Stutzmann
Abstract: The present invention relates to a novel 2-aminonaphthyridine compounds that are useful in preparing a 2-isoindolinyl napthyridine compound that exhibits remarkable anxiolytic, hypnotic, anticonvulsant, antiepileptic and muscle-relaxant properties. The invention is also directed to the optical isomers of the 2-amino napthyridine compounds and salts thereof, their preparation and the use of the 2-amino napthyridine compounds for preparing the 2-isoindolinyl napthyridine compound.
Abstract: The present invention relates to a new isoindolinone derivative of formula: ##STR1## in racemic form or in the form of its enantiomers, as well as its salts, its preparation and the pharmaceutical compositions which contain it.
Type:
Grant
Filed:
August 5, 1994
Date of Patent:
February 27, 1996
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Michel Barreau, Michel Cheve, Marie-Christine Dubroeucq, Gilles Dutruc-Rosset, Franco Manfre
Abstract: This invention relates to compounds having selective LTB.sub.4 antagonist properties. Therapeutic 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 formula ##STR1## wherein R.sub.4, X, R, Y, R', Q, m and n are herein defined, and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
October 6, 1994
Date of Patent:
February 20, 1996
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Norbert Dereu, Wolfram Hendel, Richard Labaudiniere
Abstract: This invention relates to novel perhydroisoindole derivatives of general formula (I), ##STR1## wherein radicals R are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl radical; R.sub.1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted 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 optionally 2-substituted phenyl; R.sub.4 is OH or fluorine when R.sub.5 is H, or R.sub.4 and R.sub.5 are OH or R.sub.4 and R.sub.5 together form a bond; isomeric forms and mixtures thereof; optionally salts thereof where applicable; and preparation thereof. The novel derivatives are particularly useful as P substance antagonists.
Type:
Grant
Filed:
October 11, 1994
Date of Patent:
January 16, 1996
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Daniel Achard, Serge Grisoni, Jean-Luc Malleron, Jean-Francois Peyronel, Michel Tabart
Abstract: This invention relates to novel derivatives of thiopyranopyrrole of general formula (I): ##STR1## in which R is hydrogen, allyl, or a radical having the structure: --CR.sub.a R.sub.b R.sub.c where R.sub.a and R.sub.b are hydrogen atoms or phenyl radicals optionally substituted (by halogen, alkyl, alkyloxy or nitro), and R.sub.c is defined as R.sub.a and R.sub.b or stands for an alkyl or alkyloxyalkyl radical, at least one of R.sub.a, R.sub.b and R.sub.c being a substituted or unsubstituted phenyl radical, and n is 0 to 2, in their stereoisomer forms, and mixtures thereof, and possibly the salts if they exist, and preparation thereof. The novel derivatives of the invention are particularly interesting as synthesis intermediates.
Type:
Grant
Filed:
November 17, 1993
Date of Patent:
January 16, 1996
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Daniel Achard, Claude Moutonnier, Jean-Francois Peyronel, Michel Tabart, Alain Truchon
Abstract: A method for preparing taxane derivatives having general formula (I), novel derivatives thereby obtained and compositions containing same. In general formula (I), R is t.butoxy or phenyl, R.sub.1 is hydrogen or acetyl, and Ar is substituted phenyl or optionally substituted .alpha. or .beta.-naphthyl. These novel taxane derivatives are useful as antileukemic and antitumoral agents.
Type:
Grant
Filed:
May 21, 1993
Date of Patent:
December 19, 1995
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Jean-Dominique Bourzat, Alain Commercon, Jean-Marc Paris
Abstract: Compounds of formula: ##STR1## in which R.sub.1 represents a hydrogen atom, an alkyl or alkoxycarbonyl radical or a phenyl radical, optionally substituted,R.sub.2 represents an alkoxy, optionally substituted cycloalkyloxy, cycloalkylalkyloxy, phenylalkyloxy, polyfluoroalkyloxy or cinnamyloxy radical or a radical --NR.sub.5 R.sub.6,R.sub.3 represents a phenylamino radical in which the phenyl ring is optionally substituted, an optionally substituted phenyl radical or a naphthyl, indolyl or quinolyl radical,R.sub.4 represents a substituted phenyl radical,R.sub.5 and R.sub.6, which may be identical or different, represent a hydrogen atom or an alkyl, optionally substituted phenyl, indanyl, cycloalkylalkyl, cycloalkyl or phenylalkyl radical, or alternatively R.sub.5 and R.sub.6, together with the nitrogen atom to which they are attached, form a heterocycle, their preparation and medicinal products containing them.
Type:
Grant
Filed:
October 8, 1992
Date of Patent:
December 12, 1995
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Jean-Dominique Bourzat, Marc Capet, Claude Cotrel, Claude Guyon, Franco Manfre, Gerard Roussel