Patents Assigned to Rhone-Poulenc Rorer Pharmaceuticals Inc.
  • Patent number: 5561134
    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
  • Patent number: 5561143
    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
  • Patent number: 5556990
    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
  • Patent number: 5552528
    Abstract: Bovine .beta.-endothelial cell growth factor (.beta.-ECGF) having an apparent molecular weight of 20,000 daltons can be purified at least 16,300 fold from bovine brain using heparin-Sepharose affinity chromatography. ECGF is useful for, among other purposes, diagnostic applications and has potential in the treatment of damaged blood vessels or other endothelial cell-lined structures.
    Type: Grant
    Filed: November 3, 1994
    Date of Patent: September 3, 1996
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Wilson Burgess, Thomas Maciag
  • Patent number: 5541109
    Abstract: This invention provides a unique SH3 binding domain core motif of the sequence RPLPXXP and cDNA clones encoding proteins which interact with the SH3 domain of c-src, as well as the amino acid sequences which mediate this binding.Another embodiment of this invention is a method of identifying SH3-binding proteins and elucidating the sequences which mediate binding. This method may be used as an assay to select compounds which bind to this site and which inhibit or enhance the binding of the SH3 domain.
    Type: Grant
    Filed: April 19, 1994
    Date of Patent: July 30, 1996
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: George H. Searfoss, III, Yuri D. Ivashchenko, Michael C. Jaye, Victoria J. South, Stephen M. French, Christopher Cheadle, George A. Ricca
  • Patent number: 5534532
    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: January 25, 1995
    Date of Patent: July 9, 1996
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Robert A. Groneberg, John R. Regan, Kent W. Neuenschwander, Anthony C. Scotese
  • Patent number: 5530100
    Abstract: Recovery of the 52/48 kDa tryptic fragment of vWF or peptide subfragments thereof produced in the form of inclusion bodies from recombinant host cells is carried out by providing a washed recombinant host cell suspension, adding a detergent and subjecting the cells to mechanical disruption. A second detergent is added, followed by another mechanical disruption and centrifugation to a pellet. The pellet is resuspended in a buffer and subjected to another mechanical disruption. Inclusion bodies are washed, resuspended and then recovered. In addition, endotoxins and DNA are removed from inclusion bodies containing the 52/48 kDa tryptic fragment of vWF or peptide subfragments thereof by mechanically disrupting the inclusion bodies in an aqueous buffer containing a detergent. A washed pellet is formed from these mechanically disrupted inclusion bodies and dissolved in a denaturant.
    Type: Grant
    Filed: May 7, 1990
    Date of Patent: June 25, 1996
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Thomas L. J. Darling, Lida Y. Akhnana, Jonathan J. Mitschelen, Michael E. Hrinda
  • Patent number: 5506341
    Abstract: A method of improving the therapeutic activity of von Willebrand Factor obtained from materials comprising said Factor comprising incubating said Factor at a temperature of about 20.degree. C. to about 55.degree. C. for about 1 to about 30 hours.
    Type: Grant
    Filed: May 16, 1994
    Date of Patent: April 9, 1996
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Jack Newman, David L. Farb
  • Patent number: 5494918
    Abstract: This invention relates to polycyclic compounds containing two mono- and/or bicyclic rings and a basic tertiary amino group capable of forming an ammonium ion at biological pH and which reduces 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: October 7, 1994
    Date of Patent: February 27, 1996
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Kent Neuenschwander, Dilip Amin, Anthony C. Scotese, Robert L. Morris
  • Patent number: 5480883
    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: December 10, 1993
    Date of Patent: January 2, 1996
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Alfred P. Spada, Michael R. Myers, Martin P. Maguire, Paul E. Persons
  • Patent number: 5476851
    Abstract: This invention relates to pyrazolo[3,4-g]quinoxaline compounds exhibiting protein tyrosine kinase inhibition activity of the formula: ##STR1## where: ------ may be a double bond;R, R.sub.2, R.sub.3 and R.sub.4 are as described in claim 1;a pharmaceutically acceptable salt thereof.More specifically, compounds of this invention are novel as selective inhibitors of the PDGF-R protein tyrosine kinase and can be applied as potential therapeutic agents for various disease states which are characterized by uncontrolled cellular proliferation. Further, the present invention provides pharmaceutical compositions and a method for treating such disorders comprising the administration to a patient of a PDGF receptor inhibiting effective amount of a pyrazolo[3,4-g]quinoxaline compound exhibiting protein tyrosine kinase inhibition activity. Processes for the preparation of pyrazolo[3,4-g]quinoxaline compounds are also described.
    Type: Grant
    Filed: September 8, 1994
    Date of Patent: December 19, 1995
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals, Inc.
    Inventors: Michael R. Myers, Paul E. Persons, Cuong Q. Ly, Alfred P. Spada
  • Patent number: 5468898
    Abstract: This invention relates to bicyclic aryl compounds having selective LTB.sub.4 antagonist properties and comprising an amido substituent, a substituent group having a terminal carboxylic acid or derivative thereof and a lipophilic substituent, and to methods for the treatment of disorders which result from LTB.sub.4 activity and pharmaceutical compositions including such compounds.
    Type: Grant
    Filed: April 23, 1993
    Date of Patent: November 21, 1995
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Fu-Chih Huang, Wan K. Chan, Charles A. Sutherland, Robert A. Galemmo, Jr.
  • Patent number: 5455260
    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 21, 1993
    Date of Patent: October 3, 1995
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Robert A. Groneberg, John R. Regan, Kent W. Neuenschwander, Anthony C. Scotese
  • Patent number: 5451596
    Abstract: This invention relates to a class of novel polycyclic compounds containing a cycloalkyl ring having substituted thereon a primary amine and which is further linked or bridged to two mono- and/or bicyclic rings and which reduces 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 29, 1992
    Date of Patent: September 19, 1995
    Assignee: Rhone Poulenc Rorer Pharmaceuticals Inc.
    Inventors: John W. Ullrich, Terence J. Kiesow, Kent W. Neuenschwander, Keith S. Learn, William P. Dankulich, Anthony C. Scotese
  • Patent number: 5441946
    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: April 14, 1994
    Date of Patent: August 15, 1995
    Assignee: Rhone-Poulenc-Rorer Pharmaceuticals, Inc.
    Inventors: Henry W. Pauls, Yong-Mi Choi, Dilip V. Amin
  • Patent number: 5413782
    Abstract: In a method in which an ionizable pharmaceutical material, such as theophylline, having a pharmaceutically-active anionic group is bonded to an anion exchange resin having cationic groups bonded to displacable anionic groups by bringing said material and said resin into contact with each other under conditions such that the pharmaceutically-active anionic group of said material is bonded to the cationic group of said resin and replaces the anionic group thereof, the improvement comprising effecting said contact in an environment which is substantially free of carbon dioxide and/or bicarbonate ion, a pharmacologically active composition comprising said pharmaceutically active anion and said resin, including a composition in which at least about 40% of the binding capacity of the resin comprises said pharmaceutically active anion, and a sustained release pharmaceutical composition, including enteric coated particles of the composition, and stabilizing said composition by maintaining it in an environment substan
    Type: Grant
    Filed: November 10, 1992
    Date of Patent: May 9, 1995
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Mark P. Warchol, Zofia J. Chrzan
  • Patent number: 5409930
    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: November 8, 1993
    Date of Patent: April 25, 1995
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Alfred P. Spada, Martin P. Maquire, Paul E. Persons, Michael R. Myers
  • Patent number: 5408041
    Abstract: The present invention relates to the development of bone growth factors as therapeutics for the prevention and treatment of pathological conditions involving bone tissue. The present invention provides biologically active proteinaceous factors comprising polypeptides containing the amino acid sequence M-A-G-L-G-D-E-F-G-D, [SEQ ID NO: 1], (X) F E T L F G A/V E D V I/D A L Q F V C G D, [SEQ ID NO: 2], or A-Y-I-P-I-E-T-L-E-G-I/G-E-L-V-D/Q-T-G/L-Q-F, [SEQ ID NO: 3], or biologically active fragments or sequence analogues thereof. Among the biological properties of the proteinaceous materials of the present invention is the capability to promote the growth and/or differentiation of osteoblastic cells.
    Type: Grant
    Filed: January 13, 1994
    Date of Patent: April 18, 1995
    Assignees: Rhone-Poulenc Rorer Pharmaceuticals Inc., OsteoSA Inc.
    Inventors: Gregory R. Mundy, Gloria E. Gutierrez, Ian R. Garrett, Massimo Sabatini, Elzbieta Izbicka, Wilson Burgess, Gregg R. Crumley, Clarence C. Morse, Timothy R. Arnett
  • Patent number: 5395846
    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: June 25, 1993
    Date of Patent: March 7, 1995
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Robert L. Morris, Kent W. Neuenschwander, Keith S. Learn, Anthony C. Scotese
  • Patent number: 5385912
    Abstract: This invention relates to polycyclic compounds containing two mono- and/or bicyclic rings and a basic tertiary amino group capable of forming an ammonium ion at biological pH and which reduces 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.The compounds of this invention are described by the formula ##STR1## where Ar I is phenylene or naphthylene, Ar II is phenyl or naphthyl and A is 1-azabicyclo[2.2.2]octan-3-yl.
    Type: Grant
    Filed: October 13, 1992
    Date of Patent: January 31, 1995
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Kent Neuenschwander, Dilip Amin, Anthony C. Scotese, Robert L. Morris