Abstract: This invention relates to compounds having selective LTB.sub.4 antagonist properties, 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 general formula ##STR1## and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
February 17, 1993
Date of Patent:
November 22, 1994
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Norbert Dereu, Wolfram Hendel, Richard Labaudiniere
Abstract: This invention relates to adenosine derivatives and analogs which possess adenosine agonist activity and are useful as anti-hypertensive and anti-ischemic agents, to pharmaceutical compositions including such compounds, and to their use in treating hypertension and myocardial ischemia, and to methods and intermediates used in the preparation of such compounds.
Type:
Grant
Filed:
October 2, 1992
Date of Patent:
November 15, 1994
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Alfred P. Spada, Cynthia A. Fink, Michael R. Myers
Abstract: This invention is directed to a method for stereoselectively preparing a syn-dihydroxylated compound comprising reacting a 3-hydroxyket-1-one with a borohydride in the presence of titanium derivative.
Type:
Grant
Filed:
August 11, 1993
Date of Patent:
September 13, 1994
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Patrick Leon, Xavier Radisson, Viviane Massonneau
Abstract: Thioformamide derivatives of formula (I): ##STR1## wherein R represents alkyl; A represents optionally substituted pyrid-4-yl; Y represents ethylene or methylene or a direct bond and X represents an optionally substituted phenyl, pyridyl, furyl or thienyl group or optionally substituted alkyl, alkenyl or cycloalkyl, and salts thereof possessing useful pharmacological properties.
Abstract: This invention relates to N-arylcarbamoyl proline analogues which are useful as cholecystokinin and gastrin antagonists, to pharmaceutical compositions including such proline analogues, and to their use in preventing or treating cholecystokinin or gastrin related disorders.
Type:
Grant
Filed:
May 8, 1991
Date of Patent:
August 23, 1994
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Abstract: This invention relates to novel peptide and pseudopeptide derivatives and analogs of aspartic acid which are useful as inhibitors of platelet aggregation and thrombus formation in mammalian blood, to pharmaceutical compositions including such compounds, and to their use in inhibiting thrombus formation and platelet aggregation in mammals.
Type:
Grant
Filed:
March 30, 1992
Date of Patent:
July 26, 1994
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Scott I. Klein, Bruce F. Molino, Mark Czekaj, Charles Gardner, Michael R. Becker, Jeffrey M. Dener, Jeffrey C. Pelletier
Abstract: Disclosed are novel peptide and pseudopeptide derivatives and pharmaceutical compositions thereof that inhibit platelet aggregation and thrombus formation in mammalian blood.
Type:
Grant
Filed:
October 15, 1992
Date of Patent:
July 12, 1994
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Abstract: This invention relates to a method of lowering abnormally high serum cholesterol levels in the body without significantly reducing mevalonic metabolite synthesis and to novel pharmacological compositions containing as an active ingredient bisphosphonic acid and ester compounds containing a mono-, bi- or tricyclic ring linked with a bisphosphonate moiety through a basic amino alkylene group. This invention also provides novel bisphosphonate compounds and the processes for their preparation.
Type:
Grant
Filed:
May 1, 1992
Date of Patent:
May 31, 1994
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
John W. Ullrich, Raymond D. Youssefyeh, Daniel L. Cheney, Christopher J. Burns
Abstract: The invention provides compounds of formula (I) wherein R.sup.1 represents alkyl, R.sup.2 represents an acid-labile protecting group and X.sup.1 represents a halogen atom, which are useful in the synthesis of mevalonic acid derivatives.
Type:
Grant
Filed:
August 11, 1992
Date of Patent:
April 19, 1994
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Stanley F. Clark, Ronald H. Jones, Christopher G. Newton
Abstract: The present invention provides a fail-safe combination of chemical and physical means for rendering a blood product which comprises a labile blood protein free of viruses without incurring protein denaturation. The blood product is contacted with an effective amount of a selected chemical disinfectant, preferably, sodium thiocyanate in combination with a physical process, preferably, ultrafiltration. The blood product may be plasma, serum, plasma concentrate, cryoprecipitate, cryosupernatant, plasma fractionation precipitate or plasma fractionation supernatant containing viruses such as hepatitis or human immunodeficiency virus.
Type:
Grant
Filed:
September 25, 1991
Date of Patent:
April 5, 1994
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Michael E. Hrinda, Rose D'Alisa, George C. Tarr
Abstract: Novel compounds which are 2,6-methano-2H-1-benzoxocincarboxamides having 5-HT.sub.3 -antagonist properties including unique CNS, antiemetic and gastric prokinetic activities and which are void of any significant D.sub.2 receptor binding affinity, therapeutic compositions and methods of treatment of disorders which result from 5-HT.sub.3 activity using said compounds. Processes for their preparation and the preparation of their intermediates are also disclosed.
Type:
Grant
Filed:
August 5, 1992
Date of Patent:
February 22, 1994
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
John E. Airey, Matthew R. Powers, Walter Rodriguez, Raymond D. Youssefyeh
Abstract: The present invention is directed to the synthesis of 2-chloro-cis-[5a(S)-9a(S)-(5a,6,7,8,9,9a-hexahydro)]dibenzofuran-4-carboxy lic acid by an intramolecular Heck stereospecific synthesis substantially free of undesirable 8-chloro-2,6-methano-2H-3,4,5,6-tetrahydro-1-benzoxocin-10-carboxylic.
Type:
Grant
Filed:
April 30, 1993
Date of Patent:
January 11, 1994
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Abstract: A hydrazine derivative of formula (I), ##STR1## wherein A represents an optionally substituted phenyl, naphthyl or heteroaromatic group containing one or two nitrogen atoms, and R.sup.1 represents hydrogen, optionally substituted alkyl, or optionally substituted benzyl, phenethyl, or 1-naphthylmethyl, or pyrid-3-ylmethyl group, and salts thereof, possess useful pharmaceutical properties.
Type:
Grant
Filed:
August 7, 1992
Date of Patent:
January 4, 1994
Assignee:
Rhone-Poulenc Rorer Limited
Inventors:
Terance W. Hart, Brian W. Sharp, Roger J. A. Walsh
Abstract: Pure homogeneous glia maturation factor is disclosed with methods for producing it from neutral sources and by molecular cloning and genetic engineering.
Type:
Grant
Filed:
October 31, 1991
Date of Patent:
December 14, 1993
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Abstract: This invention relates to novel diaminoalkanoic acid derivatives that inhibit platelet aggregation and thrombus formation in mammalian blood thereby being useful in the prevention and treatment of thrombosis associated with disease states such as myocardial infarction, stroke, peripheral arterial disease and disseminated intravascular coagulation, to pharmaceutical compositions including such compounds, and to their use in inhibiting thrombus formation and platelet aggregation in mammals.
Type:
Grant
Filed:
December 16, 1991
Date of Patent:
November 2, 1993
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Abstract: Disclosed is a process for the preparation of 2-aryl-1-cyclohexene-1-carboxaldehydes from 1-arylcyclohexenes which are intermediates for trans-6-[(2-arylsubstituted cycloalkenyl and substituted cycloalkyl)alkenyl and alkyl]-3,4,5,6-tetrahydro-2H-pyran-2-ones.
Type:
Grant
Filed:
March 5, 1991
Date of Patent:
November 2, 1993
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Laurence W. Reilly, Jr., Ching T. Tsuei, Walter Rodriquez, Thomas Goetzen
Abstract: Disclosed are intermediates and a process of making an anticholesterolemic compound of the formula ##STR1## the corresponding ring-opened hydroxy acids derived therefrom and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
June 23, 1992
Date of Patent:
September 28, 1993
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Abstract: Compounds of formula: ##STR1## in which R.sub.1 represents a polyfluoroalkoxy radical and R.sub.2 represents an alkylthio, alkylsulphinyl or alkylsulphonyl radical, their salts, their preparation and the medicaments containing them.
Type:
Grant
Filed:
January 29, 1991
Date of Patent:
August 31, 1993
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Abstract: This invention provides a peptide fragment of human von Willebrand Factor (vWF) and sub-fragment thereof isolated as enzymtic digestion products from naturally occurring human vWF, or isolated from synthetic peptide mixtures or isolated from lysates of organisms capable of producing recombinant human vWF. The fragments and sub-fragments are useful in the prevention and treatment of cardiovascular disorders by virtue of their ability to inhibit the binding of vWF to platelets, heparin and/or collagen.
Type:
Grant
Filed:
May 7, 1990
Date of Patent:
August 24, 1993
Assignee:
Scipps Clinic and Research Foundation
Inventors:
Theodore S. Zimmerman, Yoshihiro Fujimura, Richard A. Houghten, Zaverio M. Ruggeri
Abstract: The present invention is directed to the synthesis of 2-chloro-cis-[5a(S)-9a(S)-(5a,6,7,8,9,9a-hexahydro)]dibenzofuran-4-carboxy lic acid by a stereospecific catalytic heteroannulation synthesis free of undesirable 8-chloro-2,6-methano-2H-3,4,5,6-tetrahydro-1-benzoxocin-10-carboxylic.
Type:
Grant
Filed:
April 30, 1993
Date of Patent:
January 3, 1995
Assignee:
Rhone Poulenc Rorer Pharmaceuticals Inc.