Raymond E Gibson

US Patent:

6458935, Oct 1, 2002

Filed:

Jun 12, 2000

Appl. No.:

09/668637

Inventors:

H. Donald Burns - Harleysville PA
Terence G. Hamill - Lansdale PA
Raymond E. Gibson - Holland PA

Assignee:

Merck Co., Inc. - Rahway NJ

International Classification:

C07D40304

US Classification:

534 10, 544370, 558414

Abstract:

The present invention is directed toward radiolabeled farnesyl-protein transferase inhibitor compounds which are useful to label FPTase in assays, whether cell-based, tissue-based or in whole animal. The tracers can also be used in competitive binding assays to obtain information on the interaction of unlabeled FTIs with FPTase.

US Patent:

6939966, Sep 6, 2005

Filed:

Jul 19, 2002

Appl. No.:

10/484551

Inventors:

H. Donald Burns - Harleysville PA, US
Raymond E. Gibson - Holland PA, US
Terence G. Hamill - Lansdale PA, US
Takehiro Fukami - Hanamuro, JP

Assignee:

Merck & Co., Inc. - Rahway NJ
Banyu Pharmaceutical Co., Ltd.

International Classification:

C07D491/10
A61K049/00
A61K051/00

US Classification:

544331, 546 16, 424 181, 424 185, 424 189, 424 92

Abstract:

The present invention is directed to radiolabeled neuropeptide Y Y5 receptor antagonists which are useful for the labeling and diagnostic imaging of neuropeptide Y Y5 receptors in mammals.

US Patent:

7354935, Apr 8, 2008

Filed:

Sep 19, 2003

Appl. No.:

10/528888

Inventors:

H. Donald Burns - Harleysville PA, US
Wai-si Eng - Maple Glen PA, US
Raymond E. Gibson - Holland PA, US
Terence G. Hamill - Lansdale PA, US

Assignee:

Merck & Co. Inc. - Rahway NJ

International Classification:

A61K 31/445
C07D 401/12

US Classification:

514326, 546201

Abstract:

The present invention is directed to radiolabeled neurokinin-1 receptor antagonists which are useful for the labeling and diagnostic imaging of neurokinin-1 receptors in mammals.

US Patent:

7754188, Jul 13, 2010

Filed:

Jun 25, 2004

Appl. No.:

10/559228

Inventors:

H. Donald Burns - Harleysville PA, US
Alex M. Chen - Cranford NJ, US
Raymond E. Gibson - Holland PA, US
Mark T. Goulet - Westfield NJ, US
William K. Hagmann - Westfield PA, US
Terence G. Hamill - Lansdale PA, US
James P. Jewell - Jersey City NJ, US
Linus S. Lin - Westfield NJ, US
Ping Liu - Westfield NJ, US
Andrey V. Peresypkin - Cranford NJ, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

A61K 51/00
A61M 36/14

US Classification:

424 165, 424 189

Abstract:

The present invention relates to particular radiolabeled Cannabinoid-1 (CB1) receptor modulators, and methods of using these modulators for labeling and diagnostic imaging of Cannabinoid-1 receptors in mammals, particularly humans. In addition, intermediates useful for the synthesis of the radiolabeled Cannabinoid-1 receptor modulators are also disclosed, as well as the processes for synthesizing the radiolabeled Cannabinoid-1 receptor modulators. Still further, formulations of the radiolabeled Cannabinoid-1 receptor compounds are described.

US Patent:

44316275, Feb 14, 1984

Filed:

Dec 31, 1981

Appl. No.:

6/336340

Inventors:

William C. Eckelman - Rockville MD
Richard C. Reba - Silver Spring MD
Waclaw J. Rzeszotarski - Washington DC
Raymond E. Gibson - Arlington VA

Assignee:

Research Corporation - New York NY

International Classification:

A61K 4900
A61K 4300
C07D45302
G01N 3354

US Classification:

424 11

Abstract:

Compounds of the formula: ##STR1## wherein R is aryl, alkyl, cycloalkyl, phenyl, cyclopentyl, cyclohexyl, a ligand containing Tc-99m in chelated form or a ligand capable of chelating Tc-99m; R. sub. 1 is H or lower alkyl; X is in the ortho-, meta or para- position, and is selected from the group consisting of. sup. 125 I,. sup. 123 I,. sup. 127 I, I,. sup. 18 F,. sup. 75 Br,. sup. 77 Br, NH. sub. 2, and ##STR2## wherein R. sub. 2 is in the 2,3, or 4 position and is selected from the group consisting of H and lower alkyl, provided that when R is a ligand capable of chelating Tc-99m or containing Tc-99m in chelated form, X is not a radioisotope and may also be H or lower alkyl; Z. sup. crclbar. is an anion; or the free amine thereof; and denotes an asymmetric carbon atom.

US Patent:

62419641, Jun 5, 2001

Filed:

Sep 28, 1999

Appl. No.:

9/407822

Inventors:

H. Donald Burns - Harleysville PA
Terence G. Hamill - Lansdale PA
Raymond E. Gibson - Holland PA

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 5100
C07D40100
C07D21156
G01N 3353
G01N 33534

US Classification:

424 189

Abstract:

The present invention is directed to radiolabeled neurokinin-1 receptor antagonists which are useful for the labeling and diagnostic imaging of neurokinin-1 receptors in mammals.

US Patent:

60600381, May 9, 2000

Filed:

May 7, 1998

Appl. No.:

9/074346

Inventors:

Hugh D. Burns - Harleysville PA
Wai-Si Eng - Maple Glen PA
Raymond E. Gibson - Holland PA

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 5104
C07D24100

US Classification:

424 181

Abstract:

The present invention is directed toward radiolabeled farnesyl-protein transferase inhibitor compounds which are useful to label FPTase in assays, whether cell-based, tissue-based or in whole animal. The tracers can also be used in competitive binding assays to obtain information on the interaction of unlabeled FTIs with FPTase.

US Patent:

46440038, Feb 17, 1987

Filed:

Apr 3, 1985

Appl. No.:

6/719405

Inventors:

Waclaw J. Rzeszotarski - Washington DC
Raymond E. Gibson - Arlington VA
William C. Eckelman - Rockville MD
Richard C. Reba - Potomac MD

Assignee:

Research Corporation - New York NY

International Classification:

A61K 31435
C07D45302

US Classification:

514304

Abstract:

The present invention relates to antagonists of muscarinic acetylcholine receptors. More specifically, this invention contemplates highly selective antimuscarinic agents which are characterized as esters of 3-quinuclidinol and unsymmetrical alpha-disubstituted glycolic acids. These highly selective antimuscarinic agents permit efficacy at particular sites designated m. sub. 1 -AChR without affecting the muscarinic acetylcholine receptors of other tissues characterized by sites designated m. sub. 2 -AChR. Such efficacy requires lower quantities of the antagonist thereby lowering toxicity and other undesirable side effects.