Abstract: Compositions containing one or more nucleic acids and cationic polymers, and their use in gene therapy, particularly for in vivo nucleic acid transfer.
Type:
Grant
Filed:
February 28, 1997
Date of Patent:
January 11, 2000
Assignee:
Rhone-Poulenc Rorer SA
Inventors:
Jean-Paul Behr, Barbara Demeneix, Franck Lezoualch, Mojgan Mergny, Daniel Scherman, Otmane Boussif
Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
Type:
Grant
Filed:
July 28, 1993
Date of Patent:
August 10, 1999
Assignee:
Rhone-Poulenc Rorer Limited
Inventors:
Garry Fenton, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher, Michael John Ashton, David Charles Cook, Susan Jacqueline Hills, Ian Michael McFarlane, Nigel Vicker
Abstract: This invention relates to bis mono- and/or bicyclic aryl and/or heteroaryl compounds exhibiting protein tyrosine kinase inhibition activity. More specifically, it relates to the method of inhibiting abnormal cell proliferation in a patient suffering from a disorder characterized by such proliferation comprising the administration thereto of an EGF and/or PDGF receptor inhibiting effective amount of said bis mono- and/or bicyclic aryl and/or heteroaryl compound and to the preparation of said compounds and their use in pharmaceutical compositions used in this method.
Type:
Grant
Filed:
February 9, 1995
Date of Patent:
August 18, 1998
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Alfred P. Spada, Michael R. Myers, Martin P. Maguire, Paul E. Persons
Abstract: The invention relates to a process for the preparation of intermediates useful in the preparation of (1R,2R)-2-(3-pyridyl)-N-alkyltetrahydro-2H-thiopyran-2-carbothioamide 1-oxides, which possess useful pharmaceutical properties, for example antihypertensive properties, and to intermediates and pharmaceutical products prepared using said process.
Type:
Grant
Filed:
January 5, 1996
Date of Patent:
July 14, 1998
Assignee:
Rhone-Poulenc Rorer Limited
Inventors:
Philippe Pitchen, David Michael Thompson
Abstract: The invention is directed to a non-hygroscopic stable crystalline form of the antithrombotic compound N-?N-?N-(4-piperdin-4-yl)butanoyl)-N-ethylglycyl!-(L)-aspartyl!-(L)-.beta. -cyclohexyl-alanine amide, to processes for preparing said stable crystalline form, to a pharmaceutical composition thereof, and intermediates thereof, and the invention is directed also to processes for preparing a compound of the formula ##STR1## wherein: A, B, Z, E.sup.1, E.sup.2, G, R, m, n, and p are as defined herein.
Type:
Grant
Filed:
August 21, 1996
Date of Patent:
July 14, 1998
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Scott I. Klein, Bruce F. Molino, Mark Czekaj, Charles J. Gardner
Abstract: Novel farnesyl transferase inhibitors of general formula (I) ##STR1## preparation thereof and pharmaceutical compositions containing same. In general formula (I), R.sub.1 is Y--S--A.sub.1 -- (where Y is a hydrogen atom, an amino acid residue, a fatty acid residue, or an alkyl or alkoxycarbonyl radical, and A.sub.1 is a C.sub.1-4 alkylene radical optionally .alpha.-substituted in the >C(X.sub.1) (Y.sub.1,) grouping by an amino, alkylamino, alkanoylamino or alkoxycarbonylamino radical wherein the alkyl or alkanoyl portion contains 1-6 carbon atoms; each of X.sub.1 and Y.sub.1 is a hydrogen atom or X.sub.1 and Y.sub.1, taken toether with the carbon atom to which they are attached, form a >C.dbd.O grouping; R'.sub.1 is hydrogen or a C.sub.1-6 alkyl radical; X is an oxygen or sulphur atom; R.sub.2 is a C.sub.1-6 alkyl, alkenyl or alkynyl radical optionally substituted by hydroxy, alkoxy, mercapto, alkylthio, alkylsulphinyl or alkylsulphonyl.
Type:
Grant
Filed:
July 15, 1997
Date of Patent:
May 12, 1998
Assignee:
Phone-Poulenc Rorer SA.
Inventors:
Bernard Baudoin, Christopher Burns, Alain Commercon, Alain Le Brun
Abstract: The invention is directed to a novel compound of formula ##STR1## in which R is a hydroxyl, alkyloxy, phenylalkyloxy or --NH--CH.sub.2 --COOH radical, R' and R" are identical and are each a hydroxy or methoxy radical and R'" represents a hydrogen, bromine, chlorine or iodine atom or a nitro radical. The invention is also directed to the salts of said compounds and their use.
Type:
Grant
Filed:
November 19, 1996
Date of Patent:
May 5, 1998
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Jean-Jacques Debernard, Catherine Dubertret, Gerard Helynck, Jean Leboul, Jean-Paul Martin
Abstract: Compounds of the Formula ##STR1## wherein: K is N or N.fwdarw.O; Q is CH.sub.2 or O; T is ##STR2## or R.sub.3 O--CH.sub.2 ; X is a straight or branched chain alkylene, cycloalkylene or cycloalkenylene group, each of which is optionally substituted by at least one CH.sub.3, CH.sub.3 CH.sub.2, Cl, F, CF.sub.3 or CH.sub.3 O; Y is NR.sub.4, O or S; a=0 or 1; Z is of the formula ##STR3## Z.sub.1 is N, CR.sub.5, (CH).sub.m --CR.sub.5 or (CH).sub.m --N, m being 1 or 2; Z.sub.2 is N, NR.sub.6, O or S, n being 0 or 1; R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are independently H, alkyl, aryl or heterocyclyl; R.sub.a and R.sub.
Type:
Grant
Filed:
May 31, 1995
Date of Patent:
April 7, 1998
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Alfred P. Spada, Cynthia A. Fink, Michael R. Myers
Abstract: The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
Type:
Grant
Filed:
December 6, 1996
Date of Patent:
March 24, 1998
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
William R. Ewing, Michael R. Becker, Yong Mi Choi-Sledeski, Heinz W. Pauls, Daniel G. McGarry, Roderick S. Davis, Alfred P. Spada
Abstract: This invention relates to a method for the selective treatment of cell growth and differentiation characterized by activity of the human epidermal growth factor receptor type 2 (HER2). More specifically, this invention relates to the use of substituted or unsubstituted mono- or bi-cyclic aryl, heteroaryl, cycloalkyl or heterocycloalkyl compounds in selectively regulating cell growth. Pharmaceutical compositions useful for the selective treatment of cell growth and differentiation are also described.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
February 24, 1998
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Michael R. Myers, Alfred P. Spada, Martin P. Maguire, Paul E. Persons
Abstract: This invention relates to the treatment of intimation in a patient suffering from such disorder. More specifically, the invention relates to mono- and/or bicyclic aryl or heteroaryl quinazoline compounds in the treatment of inflammation.
Type:
Grant
Filed:
June 4, 1996
Date of Patent:
February 3, 1998
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals, Inc.
Inventors:
Michael R. Myers, Alfred P. Spada, Martin P. Maguire, Paul E. Persons, Asher Zilberstein, Chin-Yi Jenny Hsu, Susan E. Johnson
Abstract: This invention relates to the modulation and/or inhibition of cell signaling, cell proliferation, cell inflammatory response, the control of abnormal cell growth and cell reproduction. More specifically, this invention relates to the use of mono- and/or bicyclic aryl or heteroaryl quinazoline compounds in inhibiting cell proliferation, including compounds which are useful protein tyrosine kinase (PTK) inhibitors. The method of treating cell proliferation using said quinazoline compounds and their use in pharmaceutical compositions is described.
Type:
Grant
Filed:
April 19, 1994
Date of Patent:
January 20, 1998
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Michael R. Myers, Alfred P. Spada, Martin P. Maguire, Paul E. Persons
Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
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 process is described for the preparation of a compound of formula (IX) from 4-hydroxybutyl 3-pyridyl ketone. The compound of formula (IX) is an intermediate useful in the preparation of (1R,2R)-2-(3-pyridyl)-N-alkyl-tetrahydro-2H-thiopyran-2-carbothioamide 1-oxides which possess useful pharmaceutical properties, for example anti-hypertensive properties.
Type:
Grant
Filed:
April 24, 1996
Date of Patent:
November 18, 1997
Assignee:
Rhone-Poulenc Rorer Limited
Inventors:
Philippe Pitchen, Matthew Powers, Patrick Leon, Dominique Petre
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: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
October 21, 1997
Assignee:
Rhone-Poulenc Rorer Limited
Inventors:
Garry Fenton, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Keith Alfred James Stuttle, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher
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:
September 11, 1996
Date of Patent:
October 14, 1997
Assignee:
Rhone-Poulec Rorer S.A.
Inventors:
Michel Barreau, Michel Cheve, Marie-Christine Dubroeucq, Gilles Dutruc-Rosset, Franco Manfre
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.