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 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: Methods of inhibiting cell proliferation in a patient suffering from such disorder comprising the use of a styryl-substituted heteroaryl compound wherein the heteroaryl group is a monocyclic ring with 1 or 2 heteroatoms, or a bicyclic ring with 1 to about 4 heteroatoms, said compound optionally substituted or polysubstituted, with the proviso that when said ring is polysubstituted, the substituents do not have a common point of attachment to said ring, and those compounds wherein no substituent on the heteroaryl group is a carboxy group or an ester group, and pharmaceutical compositions comprising such compounds.
Type:
Grant
Filed:
April 16, 1991
Date of Patent:
April 12, 1994
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Alfred P. Spada, Paul E. Persons, Alexander Levitzki, Chaim Gilon
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: 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: 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: 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 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: This invention is directed to certain dibenzofurancarboxamides and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinctic activity void of any significant D.sub.2 receptor binding properties. This invention also describes novel processes necessary for their preparation.
Type:
Grant
Filed:
May 29, 1992
Date of Patent:
September 21, 1993
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Raymond D. Youssefyeh, Henry F. Campbell, Donald E. Kuhla, John E. Airey, Scott I. Klein, Matthew R. Powers
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: Monocyclic aryl compounds having selective LTB.sub.4 antagonists properties and comprising an amido substituent, a substituent group having a terminal carboxylic acid or derivative thereof and a lipophilic substituent, therapeutic compositions and methods of treatment of disorders which result from LTB.sub.4 activity using the monocyclic aryl compounds are disclosed.
Type:
Grant
Filed:
September 10, 1990
Date of Patent:
August 3, 1993
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Fu-Chih Huang, Wan K. Chan, Charles A. Sutherland, Robert A. Galemmo, Jr., Michael N. Chang
Abstract: This invention relates to the stereospecific process for the preparation, separation and purification of hexahydrodibenzofurans which are used in the preparation of the 5HT.sub.3 compounds. More specifically, the present invention relates to a process for the preparation of substantially optically pure cishexahydrodibenzofuran compounds including at least two chiral fused ring centers which comprises the acidic catalyzed stereospecific ring closure by the intra-molecular inversion of a gamma, i.e. 2', carbon atom of a 2-[(2'-leaving group)cycloalkyl]phenol.
Type:
Grant
Filed:
July 6, 1992
Date of Patent:
July 27, 1993
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Abstract: This invention is directed to a method for stereoselectively preparing a syn-dihydroxylated compound comprising reacting a 3-hydroxyket-1-one and a sterically hindered dialkylated borane to form a complex at about -50.degree. C. to about 0.degree. C., and reducing the complex with hydride at about -25.degree. C. to about 50.degree. C.
Type:
Grant
Filed:
September 2, 1992
Date of Patent:
June 8, 1993
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Abstract: This invention relates to compounds which are derivatives of cyclopentane which are useful as antihypertensive agents, to pharmaceutical compositions including such compounds, and to their use in treating hypertension.
Type:
Grant
Filed:
November 15, 1990
Date of Patent:
June 8, 1993
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
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.