Patents by Inventor Alfred P. Spada

Alfred P. Spada has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 6057320
    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: June 25, 1997
    Date of Patent: May 2, 2000
    Assignee: Aventis Pharmaceuticals Products Inc.
    Inventors: Alfred P. Spada, Michael R. Myers, Martin P. Maguire, Paul E. Persons
  • Patent number: 6034093
    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 specifically, they are inhibitors of the activity of Factor Xa. 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, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
    Type: Grant
    Filed: August 6, 1998
    Date of Patent: March 7, 2000
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: William R. Ewing, Michael R. Becker, Yong Mi Choi-Sledeski, Heinz W. Pauls, Daniel G. McGarry, Roderick S. Davis, Alfred P. Spada
  • Patent number: 5958918
    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 inhibitors of the activity of Factor Xa. 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, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
    Type: Grant
    Filed: November 21, 1997
    Date of Patent: September 28, 1999
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: William R. Ewing, Michael R. Becker, Henry W. Pauls, Daniel L. Cheney, Jonathan Stephen Mason, Alfred P. Spada, Yong Mi Choi-Sledeski
  • Patent number: 5795889
    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 9, 1995
    Date of Patent: August 18, 1998
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Alfred P. Spada, Michael R. Myers, Martin P. Maguire, Paul E. Persons
  • Patent number: 5736554
    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: May 31, 1995
    Date of Patent: April 7, 1998
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Alfred P. Spada, Cynthia A. Fink, Michael R. Myers
  • Patent number: 5731315
    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 specifically, they are inhibitors of the activity of Factor Xa. 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, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: March 24, 1998
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: William R. Ewing, Michael R. Becker, Yong Mi Choi-Sledeski, Heinz W. Pauls, Daniel G. McGarry, Roderick S. Davis, Alfred P. Spada
  • Patent number: 5721237
    Abstract: This invention relates to a method for the selective treatment of cell growth and differentiation characterized by activity of the human epidermal growth factor receptor type 2 (HER2). More specifically, this invention relates to the use of substituted or unsubstituted mono- or bi-cyclic aryl, heteroaryl, cycloalkyl or heterocycloalkyl compounds in selectively regulating cell growth. Pharmaceutical compositions useful for the selective treatment of cell growth and differentiation are also described.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: February 24, 1998
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Michael R. Myers, Alfred P. Spada, Martin P. Maguire, Paul E. Persons
  • Patent number: 5714493
    Abstract: This invention relates to the treatment of intimation in a patient suffering from such disorder. More specifically, the invention relates to mono- and/or bicyclic aryl or heteroaryl quinazoline compounds in the treatment of inflammation.
    Type: Grant
    Filed: June 4, 1996
    Date of Patent: February 3, 1998
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals, Inc.
    Inventors: Michael R. Myers, Alfred P. Spada, Martin P. Maguire, Paul E. Persons, Asher Zilberstein, Chin-Yi Jenny Hsu, Susan E. Johnson
  • Patent number: 5710158
    Abstract: This invention relates to the modulation and/or inhibition of cell signaling, cell proliferation, cell inflammatory response, the control of abnormal cell growth and cell reproduction. More specifically, this invention relates to the use of mono- and/or bicyclic aryl or heteroaryl quinazoline compounds in inhibiting cell proliferation, including compounds which are useful protein tyrosine kinase (PTK) inhibitors. The method of treating cell proliferation using said quinazoline compounds and their use in pharmaceutical compositions is described.
    Type: Grant
    Filed: April 19, 1994
    Date of Patent: January 20, 1998
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Michael R. Myers, Alfred P. Spada, Martin P. Maguire, Paul E. Persons
  • Patent number: 5677329
    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: May 19, 1995
    Date of Patent: October 14, 1997
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals, Inc.
    Inventors: Alfred P. Spada, Paul E. Persons, Alexander Levitzki, Chaim Gilon, Aviv Gazit
  • Patent number: 5656643
    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
  • Patent number: 5656655
    Abstract: A method of inhibiting cell proliferation in a patient suffering from such disorder comprising the administration to the patient of a pharmaceutically effective amount of a pharmaceutical composition containing, in admixture with a pharmaceutically acceptable carrier, a compound, or a pharmaceutically acceptable salt thereof, of the formula ##STR1## wherein the radicals are defined in the specification.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: August 12, 1997
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals, Inc.
    Inventors: Alfred P. Spada, Paul E. Persons, Alexander Levitzki, Chaim Gilon, Aviv Gazit
  • Patent number: 5652366
    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
  • Patent number: 5646153
    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
  • Patent number: 5612353
    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
  • Patent number: 5597837
    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 11, 1994
    Date of Patent: January 28, 1997
    Assignee: Rh one-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Alfred P. Spada, Paul E. Persons
  • 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: 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: 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: RE36256
    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, 1997
    Date of Patent: July 20, 1999
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals, Inc.
    Inventors: Alfred P. Spada, Michael R. Myers, Martin P. Maguire, Paul E. Persons