Patents by Inventor Joseph P. Burkhart

Joseph P. Burkhart 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).

  • 3-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase
    Patent number: 6953788
    Abstract: The present invention relates to certain novel 3-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase. Pharmaceutical compositions containing said compounds as well as methods of treating various disease states responding to inhibition of matrix metalloproteinase are also claimed herein.
    Type: Grant
    Filed: December 19, 1997
    Date of Patent: October 11, 2005
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Alan M. Warshawsky, Joseph T. Tsay, Michael J. Janusz, Jian Shen, Gary A. Flynn, Ramalinga M. Dharanipragada, Joseph P. Burkhart, Douglas W. Beight, Meena V. Patel
  • Elastase inhibitors
    Patent number: 6693072
    Abstract: This invention relates to compounds which are inhibitors of elastase, particularly human neutrophil elastase. The inhibitors are short, synthetic peptides in which the P2 moiety is substituted with various nitrogen-containing heterocyclic groups. As inhibitors of human neutrophil elastase, the compounds are useful in the treatment of a patient afflicted with a neutrophil associated inflammatory disease.
    Type: Grant
    Filed: December 20, 2000
    Date of Patent: February 17, 2004
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Steven L. Gallion, William A. Metz Jr., Joseph P. Burkhart, Michael R. Angelastro, Norton P. Peet
  • Novel elastase inhibitors
    Publication number: 20030096759
    Abstract: This invention relates to compounds which are inhibitors of elastase, particularly human neutrophil elastase. The inhibitors are short, synthetic peptides in which the P2 moiety is substituted with various nitrogen-containing heterocyclic groups. As inhibitors of human neutrophil elastase, the compounds are useful in the treatment of a patient afflicted with a neutrophil associated inflammatory disease.
    Type: Application
    Filed: December 20, 2000
    Publication date: May 22, 2003
    Inventors: Steven L. Gallion, William A. Metz, Joseph P. Burkhart, Michael R. Angelastro, Norton P. Peet
  • 20-fluoro-17(20)-vinyl steroids
    Patent number: 6413951
    Abstract: The invention relates to 20&xgr;-fluoropregna-4,17(20)-dien-3-on-21-oic acid ethyl ester, 20&xgr;-fluoro-3&bgr;-hydroxypregna-5,17(20)-dien-21-oic acid ethyl ester, 20&xgr;-fluoro-21-hydroxypregna-4,17 (20)-dien-3-one, 20&xgr;-fluoropregna-5,17(20)-dien-3&bgr;,21-diol and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17,20 lyase, 5&agr;-reductase and C17-hydroxylase, and to the use of these compounds in the treatment of androgen and estrogen mediated or dependent disorders, including benign prostatic hyperplasia, prostate cancer, breast cancer and DHT-mediated disorders such as acne and hirsutism. Treatment of disorders related to the over synthesis of cortisol, for example, Cushing's Syndrome are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide.
    Type: Grant
    Filed: June 21, 2001
    Date of Patent: July 2, 2002
    Assignee: Aventis Pharmaceuticals, Inc.
    Inventors: Norton P. Peet, Philip M. Weintraub, Joseph P. Burkhart, Cynthia A. Gates
  • 20-Fluoro-17(20)-vinyl steroids
    Publication number: 20020019548
    Abstract: The invention related to 20&xgr;-fluoropregna-4,17(20)-dien-3-on-21-oic acid ethyl ester, 20&xgr;-fluoro-3&bgr;-hydroxypregna-4,17(20)-dien-21-oic acid ethyl ester, 20&xgr;-fluoro-21-hydroxypregna-4,17(20)-dien-3-one, 20&xgr;-fluoropregna-4,17(20)-dien-3&bgr;,21-diol and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17,20 lyase, 5&agr;-reductase and C17-hydroxylase, and to the use of these compounds in the treatment of androgen and estrogen mediated or dependent disorders, including benign prostatic hyperplasia, prostate cancer, breast cancer and DHT-mediated disorders such as acne and hirsutism. Treatment of disorders related to the over synthesis of cortisol, for example, Cushing's Syndrome are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide.
    Type: Application
    Filed: June 21, 2001
    Publication date: February 14, 2002
    Inventors: Norton P. Peet, Philip M. Weintraub, Joseph P. Burkhart, Cynthia A. Gates
  • 2,19-methyleneoxy and 2,19-methylenethio bridged steroids as aromatase, 19-hydroxylase inhibitors and methods of their use in the treatment of estrogen mediated disorders
    Patent number: 6313161
    Abstract: The present invention is directed to a method of using a certain compounds which are 2,19-methyleneoxy or 2,19 methylenethio bridged steroids, and related steroidal compounds as inhibitors of the enzyme steroid aromatase, 19-hydroxylase and as treatment for various estrogen dependent/mediated disorders including hormonal dependent breast cancer.
    Type: Grant
    Filed: October 26, 1999
    Date of Patent: November 6, 2001
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Norton P. Peet, J. O'Neal Johnston, Joseph P. Burkhart
  • Orally-active elastase inhibitors
    Patent number: 6265381
    Abstract: This invention relates to novel morpholinourea and related derivatives of pentafluoroethyl peptides which are orally active elastase inhibitors. These compounds are useful in the treatment of various inflammatory diseases and emphysema.
    Type: Grant
    Filed: January 28, 2000
    Date of Patent: July 24, 2001
    Assignee: Merrell Pharmaceuticals, Inc.
    Inventors: Norton P. Peet, Michael R. Angelastro, Joseph P. Burkhart
  • Acylated enol derivative of &agr;-ketoesters and &agr;-ketoamides
    Patent number: 6172044
    Abstract: This invention relates to acylated enol derivatives of &agr;-ketoesters and &agr;-ketoamides. The compounds of this invention are either prodrugs of known elastase inhibitors or are elastase inhibitors in their own right and are useful in the treatment of various inflammatory diseases, including cystic fibrosis and emphysema.
    Type: Grant
    Filed: May 3, 1999
    Date of Patent: January 9, 2001
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Norton P. Peet, Joseph P. Burkhart, Shujaath Mehdi
  • Peptidase inhibitors
    Patent number: 6130315
    Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.
    Type: Grant
    Filed: August 24, 1998
    Date of Patent: October 10, 2000
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: H. Michael Kolb, Joseph P. Burkhart, Michael J. Jung, Fritz E. Gerhart, deceased, Eugene L. Giroux, Bernhard Neises, Daniel G. Schirlin
  • Polyfluoroalkyl tryptophan tripeptide thrombin inhibitors
    Patent number: 6069232
    Abstract: This invention relates to polyfluoroalkyl tryptophan tripeptides and to compositions containing them. The compounds are highly selective thrombin inhibitors which provide anticoagulant effects useful in the treatment of thrombin conditions and in preventing the coagulation of stored whole blood and blood products.
    Type: Grant
    Filed: August 26, 1996
    Date of Patent: May 30, 2000
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: J. Anthony Malikayl, Joseph P. Burkhart, Robert J. Broersma, Norton P. Peet
  • Perfluoroalkyl ketone inhibitors of elastase and processes for making the same
    Patent number: 6008196
    Abstract: This invention relates to compounds which are inhibitors of elastase, particularly human neutrophil elastase, and to novel processes for making the same. As inhibitors of human neutrophil elastase, the compounds are useful in the treatment of a patient afflicted with a neutrophil associated inflammatory disease.
    Type: Grant
    Filed: November 22, 1996
    Date of Patent: December 28, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Timothy T. Curran, Joseph P. Burkhart, Michael R. Angelastro, Norton P. Peet, William A. Metz, Jr.
  • Methods and compositions using .DELTA..sup.16 unsaturated C.sub.17 heterocyclic steroids useful as steroid C.sub.17-20 lyase inhibitors
    Patent number: 5977094
    Abstract: The present invention relates to methods and compositions using .DELTA..sup.16 unsaturated steroids which are useful as steroid C.sub.17-20 lyase inhibitors.
    Type: Grant
    Filed: May 6, 1998
    Date of Patent: November 2, 1999
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Norton P. Peet, Joseph P. Burkhart, Cynthia A. Gates
  • Acylated enol derivatives as prodrugs of elastase inhibitors
    Patent number: 5972897
    Abstract: This invention relates to acylated enol derivatives of known elastase inhibitors. These compounds are useful in the treatment of various inflammatory diseases, including cystic fibrosis and emphysema or as prodrugs of compounds which are useful in the treatment of said diseases.
    Type: Grant
    Filed: June 26, 1997
    Date of Patent: October 26, 1999
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Norton P. Peet, Joseph P. Burkhart, Shujaath Mehdi
  • .increment..sup.16 unsaturated C.sub.17 heterocyclic steroids useful as steroid C.sub.17-20 lyase inhibitors
    Patent number: 5965548
    Abstract: The present invention relates to .DELTA..sup.16 unsaturated steroids which are useful as steroid C.sub.17-20 lyase inhibitors.
    Type: Grant
    Filed: May 6, 1998
    Date of Patent: October 12, 1999
    Assignee: Merrel Pharmaceuticals, Inc.
    Inventors: Norton P. Peet, Joseph P. Burkhart, Cynthia A. Gates
  • Acylated enol derivatives of .alpha.-ketoesters and .alpha.-ketoamides
    Patent number: 5948886
    Abstract: This invention relates to acylated enol derivatives of .alpha.-ketoesters and .alpha.-ketoamides. The compounds of this invention are either prodrugs of known elastase inhibitors or are elastase inhibitors in their own right and are useful in the treatment of various inflammatory diseases, including cystic fibrosis and emphysema.
    Type: Grant
    Filed: November 25, 1997
    Date of Patent: September 7, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Norton P. Peet, Joseph P. Burkhart, Shujaath Mehdi
  • Peptidase inhibitors
    Patent number: 5849866
    Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: December 15, 1998
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: H. Michael Kolb, Joseph P. Burkhart, Michel J. Jung, Fritz E. Gerhart, deceased, Eugene L. Giroux, Bernhard Neises, Daniel G. Schirlin
  • Orally-active elastase inhibitors
    Patent number: 5714470
    Abstract: This invention relates to novel morpholinourea and related derivatives of pentafluoroethyl peptides which are orally active elastase inhibitors. These compounds are useful in the treatment of various inflammatory diseases and emphysema.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: February 3, 1998
    Assignee: Merrell Pharmaceuticals, Inc.
    Inventors: Norton P. Peet, Michael R. Angelastro, Joseph P. Burkhart
  • Acylated enol derivatives as prodrugs of elastase inhibitors
    Patent number: 5698523
    Abstract: This invention relates to acylated enol derivatives of known elastase inhibitors. These compounds are useful in the treatment of various inflammatory diseases, including cystic fibrosis and emphysema or as prodrugs of compounds which are useful in the treatment of said diseases.
    Type: Grant
    Filed: June 25, 1996
    Date of Patent: December 16, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Norton P. Peet, Joseph P. Burkhart, Shujaath Mehdi
  • 16 unsaturated C17 heterocyclic steroids useful as steroid C17-20 lyase inhibitors
    Patent number: 5677293
    Abstract: The present invention relates to .DELTA..sup.16 unsaturated C.sub.17 heterocyclic steroids which are useful as steroid C.sub.17-20 lyase inhibitors.
    Type: Grant
    Filed: July 15, 1996
    Date of Patent: October 14, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Norton P. Peet, Joseph P. Burkhart, Cynthia A. Gates
  • Prolyl endopeptidase inhibitors
    Patent number: 5661167
    Abstract: The present invention relates to compounds of formula 1, ##STR1## including all of its stereoisomers, compositions, and processes for preparation of the same. The compounds of the present invention are also useful in their pharmacological activities as they directly act as inhibitors of prolyl endopeptidase and thereby provide a methods for memory enhancement, preventing or slowing the affects of amnesia or memory deficits.
    Type: Grant
    Filed: December 2, 1996
    Date of Patent: August 26, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Norton P. Peet, Shujaath Mehdi, Joseph P. Burkhart