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 8, 1995
Date of Patent:
August 12, 1997
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Alfred P. Spada, Martin P. Maguire, Paul E. Persons, Michael R. Myers
Abstract: The present invention relates to peptides capable of modulating the levels of GDP exchange on p21-GDP complexes, the nucleic acid sequences coding for said peptides, preparation thereof and pharmaceutical compositions containing them.
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: The present invention concerns novel polypeptides having NMDA receptor activity and genetic material permitting their expression. It also concerns a method for demonstrating and isolating ligands and/or modulators of the activity of these polypeptides and their utilization as drugs.
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:
May 11, 1995
Date of Patent:
July 8, 1997
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Alfred P. Spada, Michael R. Myers, Martin P. Maguire, Paul E. Persons
Abstract: Novel genetically engineered yeast strains of genus Kluyveromyces lactis, their preparation, and the use thereof for producing recombinant proteins, are described.
Abstract: The present invention concerns DNA sequences comprising all or part of the K.lactis RP28 ribosomal protein promoter gene or a derivative thereof, and having transcriptional promoter activity. The invention also relates to the use of said sequences for the expression of recombinant genes.
Abstract: DNA sequences comprising all or part of the ADH4 gene promoter of K. lactis or a derivative of the latter, and having transcriptional promoter activity. The invention also concerns the use of said sequences for the expression of recombined genes.
Abstract: The present invention relates to DNA sequences comprising all or part of the K. lactis TAL1 gene promoter or of a derivative thereof and having a transcriptional promoter activity. It also relates to the use of these sequences for expression of recombinant genes.
Abstract: The present invention relates to a preparation of serum-human albumin having a colorimetry index lower than 0.2 resulting from the expression, in a eukaryotic or prokaryotic host, of an exogenous DNA sequence.
Type:
Grant
Filed:
July 27, 1994
Date of Patent:
March 18, 1997
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
J er ome Becquart, Reinhard Fleer, G erard Jung
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 especially, they are Factor Xa inhibitors. 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, conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
March 18, 1997
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
William R. Ewing, Michael R. Becker, Henry W. Pauls, Daniel L. Cheney, Jonathan S. Mason, Alfred P. Spada
Abstract: Stable, highly purified Factor VIII protein formulations are provided in high ionic strength media which comprises: sodium chloride, potassium chloride or mixtures thereof; calcium chloride; and histidine as the buffering agent.
Type:
Grant
Filed:
December 27, 1994
Date of Patent:
February 25, 1997
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
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:
June 7, 1995
Date of Patent:
February 4, 1997
Assignee:
Rhone-Pouelnc Rorer S.A.
Inventors:
Michel Barreau, Michel Cheve, Marie-Christine Dubroeucq, Gilles Dutruc-Rosset, Franco Manfre
Abstract: This invention relates to a class of novel amino bi- and tri-carbocyclic alkane compounds having bis-aryl substitution which exhibit squalene synthase inhibition properties. The bi- and tri-carbocyclic alkane ring contains an amino group and the ring is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
Type:
Grant
Filed:
December 7, 1994
Date of Patent:
January 21, 1997
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Robert L. Morris, Kent W. Neuenschwander, Keith S. Learn, Anthony C. Scotese
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: This invention relates to a class of novel phosphonate derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis aryl cycloalkylamino and azacycloalkyl phosphonates. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
Type:
Grant
Filed:
May 4, 1995
Date of Patent:
October 8, 1996
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Henry W. Pauls, Yong-Mi Choi, Dilip V. Amin
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 a class of novel aliphatic amino bis-aryl compounds containing at least four carbon atoms and an amino group either substituted thereon or incorporated therein and is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
Type:
Grant
Filed:
May 22, 1995
Date of Patent:
October 1, 1996
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Robert A. Groneberg, John R. Regan, Kent W. Neuenschwander, Anthony C. Scotese
Abstract: This invention relates to a class of novel dicarboxy amide derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis-aryl and/or heteroaryl alkyl or cycloalkylamino dicarboxy amides. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
Type:
Grant
Filed:
December 16, 1994
Date of Patent:
September 17, 1996
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Henry W. Pauls, Yong-Mi Choi, Robert W. Studt, Martin P. Maguire, Alfred P. Spada, Don D. Cha