Samuel Karl Graham

US Patent:

7034026, Apr 25, 2006

Filed:

Apr 8, 2002

Appl. No.:

10/473788

Inventors:

Stanley F. Barnett - North Wales PA, US
Samuel L. Graham - Schwenksville PA, US
David C. Remy - North Wales PA, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 31/498
C07D 241/42

US Classification:

514249, 544353

Abstract:

The present invention is directed to compounds comprising a 2,3-diphenylquinoxaline moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

US Patent:

7994325, Aug 9, 2011

Filed:

Mar 14, 2006

Appl. No.:

11/885926

Inventors:

Daniel V. Paone - Lansdale PA, US
Diem N. Nguyen - Harleysville PA, US
Anthony W. Shaw - Harleysville PA, US
Christopher S. Burgey - Philadelphia PA, US
Thomas J. Tucker - North Wales PA, US
Samuel L. Graham - Schwenksville PA, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

A61K 31/444
C07D 211/86

US Classification:

546193, 546198, 546199, 514318

Abstract:

Compounds of Formula I:.

US Patent:

58721363, Feb 16, 1999

Filed:

Mar 27, 1997

Appl. No.:

8/827483

Inventors:

Neville J. Anthony - Hatfield PA
Robert P. Gomez - Perkasie PA
Samuel L. Graham - Schwenksville PA

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 3144
C07D21168
C07D21180
C07D21302

US Classification:

514341

Abstract:

The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

US Patent:

59394390, Aug 17, 1999

Filed:

Dec 22, 1997

Appl. No.:

8/995744

Inventors:

Neville J. Anthony - Hatfield PA
Samuel L. Graham - Schwenksville PA
Lekhanh O. Tran - Norristown PA
Ian M. Bell - Harleysville PA
S. Jane deSolms - Norristown PA
Robert P. Gomez - Perkasie PA
Michelle Sparks Kuo - Gwynedd Valley PA
William C. Lumma - Pennsburg PA
Debra S. Perlow - East Greenville PA
Anthony W. Shaw - Lansdale PA
John S. Wai - Harleysville PA
Steven D. Young - Lansdale PA

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D40104
A61K 3144

US Classification:

514333

Abstract:

The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

US Patent:

45446679, Oct 1, 1985

Filed:

Feb 9, 1984

Appl. No.:

6/578463

Inventors:

Kenneth L. Shepard - North Wales PA
Samuel L. Graham - Lansdale PA

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 3134
C07D30782

US Classification:

514470

Abstract:

Novel 2-sulfamoylbenzo[b]furans and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in compositions including opthalmic drops and inserts.

US Patent:

56611617, Aug 26, 1997

Filed:

Sep 14, 1995

Appl. No.:

8/527972

Inventors:

Neville J. Anthony - Hatfield PA
Terrence M. Ciccarone - Telford PA
S. Jane deSolms - Norristown PA
Samuel L. Graham - Schwenksville PA
Gerald E. Stokker - Gwynedd Valley PA
Catherine M. Wiscount - Allentown PA

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 3140
A61K 31415
C07D20716
C07D40106

US Classification:

514326

Abstract:

The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit farnesyl-protein transferase. Furthermore, these CAAX analogues differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid antoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.

US Patent:

61037230, Aug 15, 2000

Filed:

Oct 13, 1998

Appl. No.:

9/170951

Inventors:

Jeffrey M. Bergman - Telford PA
Christopher J. Dinsmore - Schwenksville PA
Samuel L. Graham - Schwenksville PA

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 31504
A61K 31553
C07D48708
C07D49808

US Classification:

514249

Abstract:

The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

US Patent:

48409634, Jun 20, 1989

Filed:

Dec 7, 1984

Appl. No.:

6/679431

Inventors:

Kenneth L. Shepard - North Wales PA
Samuel L. Graham - Harleysville PA

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 3140
C07D20910

US Classification:

514418

Abstract:

Novel 2-sulfamoyl-1H-indoles and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in pharmaceutical compositions designed for systemic or topical ophthalmic administration.