Joel E Shaffer

US Patent:

20030219825, Nov 27, 2003

Filed:

Dec 12, 2002

Appl. No.:

10/297976

Inventors:

Jill Haizlip - Durham NC, US
Diane Ignar - Durham NC, US
Channa Jayawickreme - Durham NC, US
Holly King - Durham NC, US
James Liacos - Durham NC, US
Kirsten Mills - Research Triangle Park NC, US
Jason Ruan - Cambridge MA, US
Howard Sauls Jr - Durham NC, US
Joel Shaffer - Durham NC, US

International Classification:

G01N033/53
G01N033/567
G01N033/543

US Classification:

435/007100, 435/007200, 436/518000

Abstract:

A method for screening candidate compounds for an ability to modulate the biological activity of a target. The method includes the steps of providing a substrate comprising a target and an indicator, the substrate adapted for receiving a plurality of candidate compounds; contacting the substrate with a plurality of candidate compound samples in a manner wherein an identity of each candidate compound can be determined and wherein the candidate compounds in the candidate compound samples interact with the target in the substrate; detecting a signal, the signal produced by the indicator upon interaction between the target and a candidate compound; and identifying a candidate compound as a modulator of the biological activity of the target based upon an amount of signal produced.

US Patent:

20080009019, Jan 10, 2008

Filed:

Jan 17, 2007

Appl. No.:

11/623983

Inventors:

Jill Haizlip - Durham NC, US
Diane Ignar - Durham NC, US
Channa Jayawickreme - Durham NC, US
Holly King - Durham NC, US
James Liacos - Durham NC, US
Kirsten Mills - Stevenage, GB
Jason Ruan - Cambridge MA, US
Howard Sauls - Durham NC, US
Joel Shaffer - Durham NC, US

Assignee:

SmithKline Beecham Corporation - Philadelphia PA

International Classification:

G01N 33/567
G01N 33/53
G01N 33/543

US Classification:

435007200, 435007100, 436518000

Abstract:

A method for screening candidate compounds for an ability to modulate the biological activity of a target. The method includes the steps of providing a substrate comprising a target and an indicator, the substrate adapted for receiving a plurality of candidate compounds; contacting the substrate with a plurality of candidate compound samples in a manner wherein an identity of each candidate compound can be determined and wherein the candidate compounds in the candidate compound samples interact with the target in the substrate; detecting a signal, the signal produced by the indicator upon interaction between the target and a candidate compound; and identifying a candidate compound as a modulator of the biological activity of the target based upon an amount of signal produced.

US Patent:

51873052, Feb 16, 1993

Filed:

Nov 26, 1990

Appl. No.:

7/617826

Inventors:

Stephen A. Thompson - Durham NC
Joel E. Shaffer - Chapel Hill NC

Assignee:

Glaxo Inc. - Research Triangle Park NC

International Classification:

C07C 6962
C07C 6966

US Classification:

560145

Abstract:

The present invention relates to the compounds of formula (I), ##STR1## wherein R. sup. 1 is C. sub. 1-8 alkyl; C. sub. 5-8 cycloalkyl;--(CH. sub. 2). sub. n --Si(CH. sub. 3). sub. 3, wherein n is 1 to 5; C. sub. 2-5 alkylenyl; arylmethylene; aryl; heteroaryl; or wherein such aryl or heteoaryl bears 1 to 3 substituents independently selected from halogen, amino, C. sub. 1-8 alkyl mono- or disubstituted amino, C. sub. 1-8 alkyl and C. sub. 1-8 alkoxy and R. sup. 2 is C. sub. 1-8 alkoxy, pharmaceutical formulations containing these compounds and their use as vasodilators and in the treatment of cardiovascular disorders.

US Patent:

50514318, Sep 24, 1991

Filed:

Aug 9, 1990

Appl. No.:

7/565297

Inventors:

Thomas N. Wheeler - Raleigh NC
Terrence P. Kenakin - Durham NC
Joel E. Shaffer - Chapel Hill NC

Assignee:

Glaxo Inc. - Research Triangle Park NC

International Classification:

C07D21364
A61K 3144

US Classification:

514344

Abstract:

Pyridones of formula (I) for treating congestive heart failure: ##STR1## wherein: R. sup. 1 and R. sup. 2 are a variety of phenyl substituents, L is a divalent alkylene or amide containing alkylene linking group. Pharmaceutical composition, methods for their use in treating cardiovascular conditions, processes used in synthesis and intermediates used in such processes.

US Patent:

50969048, Mar 17, 1992

Filed:

Jul 20, 1990

Appl. No.:

7/556230

Inventors:

Thomas N. Wheeler - Raleigh NC
Terrence P. Kenakin - Durham NC
Joel E. Shaffer - Chapel Hill NC

Assignee:

Glaxo Inc. - Research Triangle Park NC

International Classification:

A61K 3150
A61K 31535
C07D23714

US Classification:

514247

Abstract:

Pyridazinones of the following formula (I): ##STR1## where R. sup. 1 -R. sup. 4 are a variety of substituents and L is a linking group, a pharmaceutical composition for treating congestive heart failure, novel intermediates, methods for such treatment and processes for preparing compounds of formula (I).

US Patent:

50876317, Feb 11, 1992

Filed:

Dec 18, 1990

Appl. No.:

7/629936

Inventors:

Joel E. Shaffer - Chapel Hill NC
Stephen A. Thomson - Durham NC

Assignee:

Glaxo Inc. - Research Triangle Park NC

International Classification:

C07D29104
A61K 3141

US Classification:

514342

Abstract:

The present invention relates to the compounds of formula (I). ##STR1## wherein R. sup. 1 is C. sub. 1-8 alkyl, C. sub. 2-8 alkenyl, C. sub. 5-8 cycloalkyl, aryl-C. sub. 1-4 alkyl, aryl or heteroaryl; or aryl or heteroaryl which is mono-, di-, or trisubstituted independently with halogen, nitro, C. sub. 1-4 alkyl, C. sub. 1-4 alkoxy, trifluoromethyl, amino or C. sub. 1-4 alkyl mono or disubstituted amino, pharmaceutical formulations containing these compounds and their use as vasodilators in the treatment of cardiovascular disorders.

US Patent:

51532093, Oct 6, 1992

Filed:

Jun 13, 1991

Appl. No.:

7/714539

Inventors:

Thomas N. Wheeler - Raleigh NC
Terrence P. Kenakin - Durham NC
Joel E. Shaffer - Chapel Hill NC

Assignee:

Glaxo Inc. - Research Triangle Park NC

International Classification:

C07D21385
A61K 3144

US Classification:

514344

Abstract:

Pyridones of formula (I) for treating congestive heart failure: ##STR1## wherein: R. sup. 1 and R. sup. 2 are a variety of phenyl substituents, L is a divalent alkylene linking group. Pharmaceutical composition, methods for their use in treating cardiovascular conditions, processes used in synthesis and intermediates used in such processes.

US Patent:

52044637, Apr 20, 1993

Filed:

Sep 4, 1991

Appl. No.:

7/754835

Inventors:

Thomas N. Wheeler - Raleigh NC
Terrence P. Kenakin - Durham NC
Joel E. Shaffer - Chapel Hill NC

Assignee:

Glaxo Inc. - Research Triangle Park NC

International Classification:

C07D23714

US Classification:

544114

Abstract:

Pyridazinones of the following formula (I): ##STR1## where R. sup. 1 -R. sup. 4 are a variety of substituents and L is a linking group, a pharmaceutical composition for treating congestive heart failure, novel intermediates, methods for such treatment and processes for preparing compounds of formula (I).