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: This invention relates to di[(1 R)-(-)-camphosulfonic acid) salt of [1S-[1.alpha.,2.beta.,3.beta.,4.alpha.,(S*)]]-4-[7-[[2-(3-chloro-2-thienyl )-1-ethylethyl]amino]3 H-imidazo[4,5-b]pyridin-3-yl]-N-ethyl-2,3-dihydroxycyclopentanecarboxamide , and a process for preparing the compound, comprising reacting a reaction mixture of (-)-1.beta.-N-ethyl-2.alpha.,3.alpha.-isopropylidenedioxy-4.beta.-[3-amino -4-[2-(5-chloro-2-thienyl)-(1R)-1-ethylethyl]amino-2-pyridyl]aminocyclopent anecarboxamide and formamidine acetate, and then treating the reaction mixture with (1 R)-(-)-10-camphorsulfonic acid.The salt is useful in purifying [1 S-[1.alpha.,2.beta.,3.beta.,4.alpha.,(S*)]]-4-[7-[[2-(3-chloro-2-thienyl)- 1-ethylethyl]amino]-3 H-imidazo[4,5-b]pyridin-3-yl]-N-ethyl-2,3-dihydroxycyclopentanecarboxamide which possesses adenosine agonist activity and is useful as an anti-hypertensive, cardioprotective, anti-ischemic, and antilipolytic agent.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
July 29, 1997
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Alfred P. Spada, Cynthia A. Fink, Michael R. Myers, Laurence W. Reilly, Benoit J. Vanasse
Abstract: This invention relates to aromatic oligomeric compounds useful in the treatment of cardiovascular, bone metabolic, hypolipidaemic, neuronal, gastrointestinal and elastase-mediated connective tissue degradation disorders and disorders which may be treated by agents effective in binding DNA, to processes for preparation of such oligomeric compounds, to pharmaceutical compositions including such oligomeric compounds, and to their use in the treatment of such disorders.
Type:
Grant
Filed:
September 10, 1993
Date of Patent:
November 5, 1996
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
John R. Regan, Daniel G. McGarry, Michael N. Chang, Jeffrey N. Barton, Jack Newman, Schmuel Ben-Sasson
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:
October 3, 1994
Date of Patent:
October 1, 1996
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Alfred P. Spada, Cynthia A. Fink, Michael R. Myers
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 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: 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: This invention relates to compounds which are steroidyl derivatives of 4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one and the corresponding ring-opened hydroxy acid form thereof which are useful as antihypercholesterolemic agents, to pharmaceutical compositions including such compounds, and to their use in treating hypercholesterolemia.
Type:
Grant
Filed:
February 5, 1991
Date of Patent:
June 1, 1993
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Daniel G. McGarry, Francis A. Volz, John R. Regan, Michael N. Chang
Abstract: Disclosed are tetrahydro-pyrido-indoles having the general formula ##STR1## which are antagonists towards the neuropeptides cholexystokinin and gastrin processing valuable activities for the treatment of cholecystokinin or gastrin-related disorders of the gastrointestinal, central nervous and appetite regulatory systems and their pharmaceutical compositions and processes for their preparation.
Type:
Grant
Filed:
August 24, 1990
Date of Patent:
November 10, 1992
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Bruce F. Molino, Paul R. Darkes, William R. Ewing
Abstract: This invention relates to a series of bicyclic benzomonoazacyclic carboxamide compounds of the general formula: ##STR1## Where Z is tertiary amine, which are useful for the method of treating patients suffering from gastrointestinal disorders, and of pharmaceutical composition including an effective 5HT3 - antagonists amount of said compounds therein.
Type:
Grant
Filed:
April 6, 1990
Date of Patent:
November 5, 1991
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Jeffrey C. Pelletier, Raymond D. Youssefyeh, Henry F. Campbell