Joseph G Burkhart

US Patent:

6953788, Oct 11, 2005

Filed:

Dec 19, 1997

Appl. No.:

08/893080

Inventors:

Alan M. Warshawsky - Cincinnati OH, US
Joseph T. Tsay - Cincinnati OH, US
Michael J. Janusz - Oregonia OH, US
Jian Shen - Cincinnati OH, US
Gary A. Flynn - Tucson AZ, US
Ramalinga M. Dharanipragada - Tucson AZ, US
Joseph P. Burkhart - Plainfield IN, US
Douglas W. Beight - Indianapolis IN, US
Meena V. Patel - Chicago IL, US

Assignee:

Aventis Pharmaceuticals Inc. - Bridgewater NJ

International Classification:

C07D243/00
C07D401/00
C07D223/12
A61K031/55
A61P019/02

US Classification:

51421203, 51421208, 514218, 540492, 540524, 540527

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.

US Patent:

63131617, Nov 6, 2001

Filed:

Oct 26, 1999

Appl. No.:

9/426993

Inventors:

Norton P. Peet - Cincinnati OH
J. O'Neal Johnston - Milford OH
Joseph P. Burkhart - West Chester OH

Assignee:

Merrell Pharmaceuticals Inc. - Bridgewater NJ

International Classification:

A61K 31352
A61K 31382
C07D31178
C07D31194
C07D33504

US Classification:

514432

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.

US Patent:

62653814, Jul 24, 2001

Filed:

Jan 28, 2000

Appl. No.:

9/491814

Inventors:

Norton P. Peet - Cincinnati OH
Michael R. Angelastro - Mason OH
Joseph P. Burkhart - West Chester OH

Assignee:

Merrell Pharmaceuticals, Inc. - Bridgewater NJ

International Classification:

A61K 3800

US Classification:

514 18

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.

US Patent:

54911362, Feb 13, 1996

Filed:

Mar 18, 1994

Appl. No.:

8/210796

Inventors:

Norton P. Peet - Cincinnati OH
J. O'Neal Johnston - Milford OH
Joseph P. Burkhart - West Chester OH

Assignee:

Merrell Dow Pharmaceuticals Inc. - Cincinnati OH

International Classification:

A61K 3158

US Classification:

514172

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 aromarase, 19-hydroxylase and as treatment for various estrogen dependent/mediated disorders including hormonal dependent breast cancer.

US Patent:

58498664, Dec 15, 1998

Filed:

Jun 7, 1995

Appl. No.:

8/481666

Inventors:

H. Michael Kolb - Cincinnati OH
Joseph P. Burkhart - West Chester OH
Michel J. Jung - Pfaffenhoffen, FR
Fritz E. Gerhart - late of Kehl Leutesheim, DE
Eugene L. Giroux - Cincinnati OH
Bernhard Neises - Offenburg-Griesheim, DE
Daniel G. Schirlin - Lampertheim, FR

Assignee:

Merrell Pharmaceuticals Inc. - Cincinnati OH

International Classification:

C07C 4900
C07C23300
C07K 500
C07K 700

US Classification:

530323

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.

US Patent:

45888256, May 13, 1986

Filed:

Mar 13, 1985

Appl. No.:

6/712318

Inventors:

Joseph P. Burkhart - West Chester OH
Gene W. Holbert - Loveland OH

Assignee:

Merrell Dow Pharmaceuticals Inc. - Cincinnati OH

International Classification:

C07D30724
C07D30730
C07F 718

US Classification:

549475

Abstract:

This application relates to a stereospecific process for preparing specific enantiomers of 4-amino-4,5-dihydro-2-furancarboxylic acid and C. sub. 1-6 lower alkyl esters thereof. These compounds are. gamma. -aminobutyric acid transaminase inhibitors useful in the treatment of epilepsy.

US Patent:

59728973, Oct 26, 1999

Filed:

Jun 26, 1997

Appl. No.:

8/882764

Inventors:

Norton P. Peet - Cincinnati OH
Joseph P. Burkhart - West Chester OH
Shujaath Mehdi - West Chester OH

Assignee:

Merrell Pharmaceuticals Inc. - Bridgewater NJ

International Classification:

A61K 3805
C07D20709

US Classification:

514 19

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.

US Patent:

59488867, Sep 7, 1999

Filed:

Nov 25, 1997

Appl. No.:

8/978096

Inventors:

Norton P. Peet - Cincinnati OH
Joseph P. Burkhart - Plainfield IN
Shujaath Mehdi - West Chester OH

Assignee:

Hoechst Marion Roussel, Inc. - Bridgewater NJ

International Classification:

C07K 500

US Classification:

530330

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.