Elizabeth E Sugg

5889182, Mar 30, 1999

Apr 14, 1997

8/817363

Milana Dezube - Chapel Hill NC
Gavin Charles Hirst - Marlboro MA
Ronald George Sherrill - Cary NC
Elizabeth Ellen Sugg - Durham NC
Jerzy Ryszard Szewczyk - Chapel Hill NC
Timothy Mark Willson - Durham NC

Glaxo Wellcome Inc. - Research Triangle Park NC

C07D22316
A61K 3153

540527

This invention relates to novel oxoazepine derivatives of Formula (I), R. sup. 1 R. sup. 2 NCOCH. sub. 2 N(R. sup. 3)COR. sup. 4 (I) to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine. More particularly, it relates to compounds which exhibit agonist activity for CCK-A receptors thereby enabling them to modulate the hormones gastrin and cholecystokinin (CCK) in mammals.

56461402, Jul 8, 1997

Oct 13, 1995

8/525659

Elizabeth Ellen Sugg - Research Triangle Park NC
Christopher Joseph Aquino - Research Triangle Park NC
Jerzy Ryszard Szewczyk - Research Triangle Park NC
Harry Finch - Stevenage, GB
Robin Arthur Ellis Carr - Stevenage, GB

Glaxo Wellcome Inc. - Research Triangle Park NC

C07D24312
A61K 3155

517221

This invention pertains to novel benzodiazepine compounds of formula (I) ##STR1## which exhibit agonistic activity for CCK-A receptors, enabling them to modulate the hormones gastrin and cholecystokinin (CCK) in mammals for use in medicine as anorectic agents in the regulation of appetite, the treatment of obesity and the maintenance of weight loss.

57804648, Jul 14, 1998

Apr 14, 1997

8/817364

Elizabeth Ellen Sugg - Durham NC

Glaxo Wellcome Inc. - Research Triangle Park NC

A61K 3155

514221

A pharmaceutical formulation in solid dosage form for oral administration which comprises a compound of the general Formula (I) ##STR1## or a physiologically acceptable salt or solvate thereof together with one or more pharmaceutically acceptable carriers wherein the formulation is encased in an enteric coating or capsule.

57958874, Aug 18, 1998

Oct 11, 1996

8/718552

Christopher Joseph Aquino - Long Beach WA
Milana Dezube - Chapel Hill NC
Ronald George Sherrill - Cary NC
Elizabeth Ellen Sugg - Durham NC
Jerzy Ryszard Szewczyk - Chapel Hill NC
Timothy Mark Willson - Durham NC

Glaxo Wellcome Inc. - Research Triangle Park NC

A01N 4362
C07D24324
C07D24312

514221

A method of inducing a Cholescystokinin-A receptor agonist response in a mammal by administering a compound of formula (I), ##STR1## where R. sup. 1 is C. sub. 1 -C. sub. 6 alkyl, C. sub. 3-6 cycloalkyl, phenyl, or substituted phenyl; R. sup. 2 is C. sub. 3-6 alkyl, C. sub. 3-6 cycloalkyl, C. sub. 3-6 alkenyl, benzyl, phenylC. sub. 1-3 alkyl or substituted phenyl; or NR. sup. 1 R. sup. 2 together form 1,2,3,4-tetrahydroquinoline or benzazepine mono-, di-, or trisubstituted independently with C. sub. 1-6 alkyl, C. sub. 1-6 alkoxy or halogen substituents; n is an integer selected from the grouping consisting of 0,1,2 or 3; p is the integer 0 or 1; q is the integer 0 or 1; r is the integer 0 or 1, provided that when q is 0 then r is 0; R. sup. 3, R. sup. 4, R. sup. 5 and R. sup. 8 are selected from a variety of substituents; X is nitrogen, nitroso or R. sup. 8 ; m is an integer selected from the group consisting of 0, 1, 2 or 3; Y and Z are hydrogen or halogen, novel intermediates, a pharmaceutical composition for treating obesity, gall bladder stasis, disorders of pancreatic secretion, methods for such treatment and processes for preparing compounds of formula (I).

58590072, Jan 12, 1999

Nov 14, 1996

8/722051

Christopher Joseph Aquino - Long Beach WA
Marcus Brackeen - Durham NC
Milana Dezube - Chapel Hill NC
Brad Richard Henke - Cary NC
Gavin Charles Hirst - Marlboro MA
Peter Walter Jeffs - Chapel Hill NC
Tanya Momtahen - Raleigh NC
Elizabeth Ellen Sugg - Durham NC
Edward Martin Suh - Chapel Hill NC
Timothy Mark Willson - Durham NC

Glaxo Wellcome Inc. - Research Triangle Park NC

A01N 4362
C07D24312

514221

Benzo�b!�1,4!diazepine compounds of formula (I), where R. sup. 1 is selected from C. sub. 1 C. sub. 6 alkyl, C. sub. 3 -C. sub. 6 cycloalkyl, phenyl, or substituted phenyl; R. sup. 2 is selected from C. sub. 3 -C. sub. 6 alkyl, C. sub. 3 C. sub. 6 cycloalkyl, C. sub. 3 -C. sub. 6 alkenyl, benzyl, phenylC. sub. 1 -C. sub. 3 alkyl of substituted phenyl; or NR. sup. 1 R. sup. 2 together form 1,2,3,4-tetrahydroquinoline or benzazepine, mono-, di-, or trisubstituted independently with C. sub. 1-6 alkyl C. sub. 1-6 alkoxy or halogen substituents; p is an integer 0 or 1; q is an integer 0 or 1; r is an integer 0 or 1; t is an integer 0 or 1, provided that when r is 0 then t is 0; R. sup. 3, R. sup. 5, and R. sup. 6 are independently hydrogen or C. sub. 1-6 alkyl; R. sup. 4 is C. sub.

53808720, Jan 10, 1995

Jul 14, 1992

7/914918

Elizabeth E. Sugg - Durham NC
Milana Dezube - Chapel Hill NC
Gavin C. Hirst - Carrboro NC

Glaxo Inc. - Research Triangle Park NC

C07D20920

548495

CCK modulators, e. g. agonists or antagonists, of the following formula (I): ##STR1## or a base-addtion salt thereof.

55084320, Apr 16, 1996

Jun 8, 1994

8/255592

Elizabeth E. Sugg - Durham NC
Milana Dezube - Chapel Hill NC
Gavin C. Hirst - Carrboro NC

Glaxo Wellcome Inc. - Research Triangle Park NC

C07D20920
C07D40312
A61K 3141
A61K 31405

548506

CCK modulators, e. g. agonists or antagonists, of the following formula (I): ##STR1## or a base-addtion salt thereof.

57391297, Apr 14, 1998

Oct 11, 1996

8/722191

Christopher Joseph Aquino - Long Beach WA
Elizabeth Ellen Sugg - Durham NC
Jerzy Ryszard Szewczyk - Chapel Hill NC

Glaxo Wellcome Inc. - RTP NC

A61K 3155

514221

Compounds of general formula (I) and physiologically salts thereof, processes for their preparation and their use as modulators of the effects of gastrin and CCK.