Patents by Inventor Heinz W. Pauls

Heinz W. Pauls 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).

  • N-acylpyrrolidin-2-ylalkylbenzamidine derivatives as inhibitors of factor Xa
    Patent number: 7361663
    Abstract: This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing Factor Xa. The present invention is also directed to compositions containing said derivatives, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.
    Type: Grant
    Filed: October 16, 2003
    Date of Patent: April 22, 2008
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Mark Czekaj, Scott I. Klein, Heinz W. Pauls
  • 4-(3-aminomethylphenyl)piperidin-1-yl]-[5-(2-fluorophenylethynyl)furan-2-yl]-methanone as an inhibitor of mast cell tryptase
    Publication number: 20040192734
    Abstract: The present invention extends to the compound of formula (I): 1
    Type: Application
    Filed: December 22, 2003
    Publication date: September 30, 2004
    Applicant: AVENTIS PHARMACEUTICALS INC.
    Inventors: Heinz W. Pauls, Suzanne Aldous, Gregory H. Merriman, Robert A. Farr, Adam W. Sledeski
  • Substituted oxoazaheterocyclyl compounds
    Publication number: 20040102450
    Abstract: This invention is directed to oxoazaheterocycyl compounds which inhibit Factor Xa, to oxoazaheterocycyl compounds which inhibit both Factor Xa and Factor IIa, to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds, to a method of directly inhibiting Factor Xa and to a method of simultaneously directly inhibiting Factor Xa and Factor IIa..
    Type: Application
    Filed: July 25, 2003
    Publication date: May 27, 2004
    Applicant: AVENTIS PHARMACEUTICALS INC.
    Inventors: William R. Ewing, Michael R. Becker, Yong Mi Choi-Sledeski, Heinz W. Pauls, Wei He, Stephen M. Condon, Roderick S. Davis, Barbara A. Hanney, Alfred P. Spada, Christopher J. Burns, John Z. Jiang, Aiwen Li, Michael R. Myers, Wan F. Lau, Gregory B. Poli, Mark A. Bobko, Robert L. Morris, Joseph M. Karpinski, Timothy F. Gallagher, Kent W. Neuenschwander, Robert D. Groneberg, Jean-Francois Sabuco
  • N-acylpyrrolidin-2-ylalkylbenzamidine derivatives as inhibitors of factor Xa
    Publication number: 20040087570
    Abstract: This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing Factor Xa. The present invention is also directed to compositions containing said derivatives, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.
    Type: Application
    Filed: October 16, 2003
    Publication date: May 6, 2004
    Applicant: AVENTIS PHARMA DEUTSCHLAND GMBH
    Inventors: Mark Czekaj, Scott I. Klein, Heinz W. Pauls
  • Methods of treating insulin resistance syndrome and diabetes
    Publication number: 20030176390
    Abstract: This invention is directed to methods of treating insulin resistance syndrome and diabetes in a patient in need thereof, comprising administering to said patient a pharmaceutically effective amount of a compound derived from adenosine and analogues thereof, or a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable prodrug thereof, an N-oxide thereof, a hydrate thereof or a solvate thereof, or a pharmaceutical composition comprising such compound.
    Type: Application
    Filed: May 14, 2002
    Publication date: September 18, 2003
    Inventors: Andreas Herling, Gerhard Jaehne, Martin P. Maguire, Alfred P. Spada, Michael R. Myers, Yong Mi Choi-Sledeski, Heinz W. Pauls, William R. Ewing
  • N-acylpyrrolidin-2-ylalkylbenzamidine derivatives as inhibitors of factor Xa
    Publication number: 20030092698
    Abstract: This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing Factor Xa. The present invention is also directed to compositions containing said derivatives, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.
    Type: Application
    Filed: May 10, 2002
    Publication date: May 15, 2003
    Inventors: Mark Czekaj, Scott I Klein, Heinz W. Pauls
  • Sulfonic acid or sulfonylamino N-(heteroaralkyl)-azaheterocyclylamide compounds
    Publication number: 20020013310
    Abstract: The compounds of formula I herein 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, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
    Type: Application
    Filed: July 30, 2001
    Publication date: January 31, 2002
    Inventors: Yong Mi Choi-Sledeski, Heinz W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong, Julian Levell
  • Substituted N-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides
    Patent number: 6323227
    Abstract: This invention relates to compounds of formula which inhibit Factor Xa, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of patients suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.
    Type: Grant
    Filed: February 26, 1999
    Date of Patent: November 27, 2001
    Assignee: Aventis Pharmaceuticals Products Inc.
    Inventors: Scott I. Klein, Kevin R. Guertin, Alfred P. Spada, Heinz W. Pauls, Yong Gong, Daniel G. McGarry
  • Sulfonic acid sulfonylamino n-(heteroaralkyl)-azaheterocyclylamide compounds
    Patent number: 6281227
    Abstract: The compounds of formula I herein 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, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
    Type: Grant
    Filed: December 2, 1999
    Date of Patent: August 28, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Yong Mi Choi-Sledeski, Heinz W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong, Julian Levell
  • Substituted sulfonic acid N-[(aminoiminomethyl)phenylalkyl]-azaheterocyclylamide compounds
    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
  • Substituted sulfonic acid n-?(aminoiminomethyl)phenylalkyl!-azaheterocyclamide compounds
    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
  • Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors
    Patent number: 5158936
    Abstract: Thiol protease inhibitors are disclosed having the formula: ##STR1## or an optical isomer thereof, or a pharmaceutically acceptable salt thereof, wherein:n is 0 or 1;m is 0, 1 or 2;X is H or an N-protecting group;each Y is independently an optionally protected .alpha.-amino acid residue;R is an optionally protected .alpha.-amino acid side chain that is H or CH.sub.3 or that is bonded to the .alpha.-carbon atom to which it is attached by a methylene, methine or phenyl radial; andR' is optionally substituted aryl.
    Type: Grant
    Filed: May 15, 1991
    Date of Patent: October 27, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Alexander Krantz, Heinz W. Pauls, Roger A. Smith, Robin W. Spencer
  • Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors
    Patent number: 5055451
    Abstract: Thiol protease inhibitors are disclosed having the formula: ##STR1## or an optical isomer thereof, or a pharmaceutically acceptable salt thereof, wherein:n is 0 or 1;m is 0, 1 or 2;X is H or an N-protecting group;each Y is independently an optionally protected .alpha.-amino acid residue;R is an optionally protected .alpha.-amino acid side chain that is H or CH.sub.3 or that is bonded to the .alpha.-carbon atom to which it is attached by a methylene, methine or phenyl radical; andR' is optionally substituted aryl.
    Type: Grant
    Filed: December 7, 1987
    Date of Patent: October 8, 1991
    Assignee: Syntex Inc.
    Inventors: Alexander Krantz, Heinz W. Pauls, Roger A. Smith, Robin W. Spencer
  • Process for preparing .alpha.-L N-acetyl daunosaminide
    Patent number: 4514561
    Abstract: The present invention is a unique method for the regioselective addition of a functional group to an allylic alcohol moiety which is particularly useful in the preparation of cis-hydroxyamino sugars.
    Type: Grant
    Filed: April 15, 1983
    Date of Patent: April 30, 1985
    Assignee: Research Corporation
    Inventors: Bertram Fraser-Reid, Heinz W. Pauls