Patents by Inventor William C. Lumma

William C. Lumma has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Inhibitors of prenyl-protein transferase
    Patent number: 6355643
    Abstract: The present invention comprises unsubstituted and substituted piperazine-containing compounds having alkanoyl, alkylsulfonyl, alkylamido or alkoxycarbonyl substituents, and having the formula A, which inhibit prenyl-protein transferases. In particular, the invention relates to prenyl-protein transferase inhibitors which are efficacious in vivo as inhibitors of geranylgeranyl-protein transferase type I (GGTase-I) and that inhibit the cellular processing of both the H-Ras protein and the K4B-Ras protein. Such therapeutic compounds are useful in the treatment of cancer.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: March 12, 2002
    Assignee: Merck & Co., Inc.
    Inventors: William C. Lumma, John T. Sisko, Anthony M. Smith, Thomas J. Tucker, Christopher J. Dinsmore, Jeffrey M. Bergman
  • Inhibitors of prenyl-protein transferase
    Patent number: 6335343
    Abstract: The present invention comprises piperazine/piperazinone-containing compounds having multicyclic ring system substituents on one of the piperazine/piperazinone nitrogens, which inhibit prenyl-protein transferases, including farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: January 1, 2002
    Assignee: Merck & Co., Inc.
    Inventors: William C. Lumma, Jr., Anthony M. Smith, John T. Sisko
  • Inhibitors of prenyl-protein transferase
    Patent number: 6127390
    Abstract: The present invention is directed to compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: October 1, 1998
    Date of Patent: October 3, 2000
    Assignee: Merck & Co., Inc.
    Inventors: S. Jane deSolms, William C. Lumma, Jr., Anthony W. Shaw, John T. Sisko, Thomas J. Tucker
  • Fibrinogen receptor antagonist prodrugs
    Patent number: 5990107
    Abstract: Fibrinogen receptor antagonist alcohol prodrugs having the structure, for example, of ##STR1## more particularly, ##STR2##
    Type: Grant
    Filed: June 26, 1997
    Date of Patent: November 23, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Melissa S. Egbertson, George D. Hartman, William C. Lumma, John S. Wai, Steven D. Young
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5977134
    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.
    Type: Grant
    Filed: December 4, 1997
    Date of Patent: November 2, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Terrence M. Ciccarone, Wasyl Halczenko, John H. Hutchinson, William C. Lumma, Jr., Gerald E. Stokker, Craig A. Stump, Theresa M. Williams
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5939439
    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.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: August 17, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Samuel L. Graham, Lekhanh O. Tran, Ian M. Bell, S. Jane deSolms, Robert P. Gomez, Michelle Sparks Kuo, William C. Lumma, Jr., Debra S. Perlow, Anthony W. Shaw, John S. Wai, Steven D. Young
  • Benzoxazinones as inhibitors of HIV reverse transcriptase
    Patent number: 5811423
    Abstract: Certain benzoxazinones are useful in the inhibition of HIV reverse transcriptase (including its resistant varieties), the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: March 12, 1997
    Date of Patent: September 22, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Steven D. Young, Linda S. Payne, Susan F. Britcher, Lekhanh O. Tran, William C. Lumma, Jr.
  • Thrombin inhibitors
    Patent number: 5798377
    Abstract: A compound which inhibits human thrombin and where has the structure ##STR1## such as ##STR2##
    Type: Grant
    Filed: October 21, 1996
    Date of Patent: August 25, 1998
    Assignee: Merck & Co., Inc.
    Inventors: William C. Lumma, Thomas J. Tucker, Keith M. Witherup, Stephen F. Brady, Willie L. Whitter, Joseph P. Vacca, Craig Coburn, Jules A. Shafer
  • Pyridinone thrombin inhibitors
    Patent number: 5792779
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and have the following structure: ##STR1## for example: ##STR2##
    Type: Grant
    Filed: February 19, 1997
    Date of Patent: August 11, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Philip E. Sanderson, Terry A. Lyle, Joseph P. Vacca, William C. Lumma, Stephen F. Brady, Thomas J. Tucker
  • Alpha 1b adrenergic receptor antagonists
    Patent number: 5747490
    Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha 1b adrenergic receptor antagonists. These compounds display submicromolar affinity for the human alpha 1b adrenergic receptor subtype while displaying at least five-fold lower affinity for the human alpha 1d and alpha 1a adrenergic receptor subtypes, and many other G-protein coupled human receptors. One application of these compounds is in the treatment of hypertension. More specifically, these compounds display selectivity for lowering blood pressure without, for example, substantially affecting urethral pressure.
    Type: Grant
    Filed: September 19, 1996
    Date of Patent: May 5, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Mark G. Bock, Michael A. Patane, William C. Lumma
  • Piperidine and hexahydropyridazine thrombin inhibitors
    Patent number: 5714485
    Abstract: Compounds of the invention have the following structure: ##STR1##
    Type: Grant
    Filed: January 16, 1997
    Date of Patent: February 3, 1998
    Assignee: Merck & Co., Inc.
    Inventors: William C. Lumma, Roger M. Freidinger, Stephen F. Brady, Philip E. Sanderson, Dong-Mei Feng, Terry A. Lyle, Kenneth J. Stauffer, Thomas J. Tucker, Joseph P. Vacca
  • Benzoxazinones as inhibitors of HIV reverse transcriptase
    Patent number: 5665720
    Abstract: Certain benzoxazinones are useful in the inhibition of HIV reverse transcriptase (including its resistant varieties), the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: September 9, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Steven D. Young, Susan F. Britcher, Linda S. Payne, Lekhanh O. Tran, William C. Lumma, Jr.
  • Benzoxazinones as inhibitors of HIV reverse transcriptase
    Patent number: 5663169
    Abstract: Certain benzoxazinones are useful in the inhibition of HIV reverse transcriptase (including its resistant varieties), the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable saks, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: September 2, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Steven D. Young, Linda S. Payne, Susan F. Britcher, Lekhanh O. Tran, William C. Lumma, Jr.
  • Thrombin inhibitors
    Patent number: 5629324
    Abstract: Compounds of the invention have the following structure: ##STR1## for example ##STR2## These compounds inhibit thrombin and associated thrombosis.
    Type: Grant
    Filed: April 10, 1995
    Date of Patent: May 13, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Joseph P. Vacca, William C. Lumma, Stephen F. Brady, Thomas J. Tucker
  • Inhibitors of HIV reverse transcriptase
    Patent number: 5527819
    Abstract: Novel indole compounds inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 18, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Theresa M. Williams, Terrence M. Ciccarone, Walfred S. Saari, John S. Wai, William J. Greenlee, Suresh K. Balani, Mark E. Goldman, Anthony D. Theoharides, deceased, Jacob M. Hoffman, Jr., William C. Lumma, Jr., Joel R. Huff, Clarence S. Rooney, Philip E. Sanderson
  • Benzoxazinones as inhibitors of HIV reverse transcriptase
    Patent number: 5519021
    Abstract: Certain benzoxazinones are useful in the inhibition of HIV reverse transcriptase (including its resistant varieties), the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: May 21, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Steven D. Young, Susan F. Britcher, Linda S. Payne, Lekhanh O. Tran, William C. Lumma, Jr.
  • Pyrrolidine thrombin inhibitors
    Patent number: 5510369
    Abstract: Compounds of the invention have the following structure: ##STR1## for example ##STR2## These compounds inhibit thrombin and associated thrombosis.
    Type: Grant
    Filed: July 22, 1994
    Date of Patent: April 23, 1996
    Assignee: Merck & Co., Inc.
    Inventors: William C. Lumma, Roger M. Freidinger, Stephen F. Brady, Philip E. Sanderson, Dong-Mei Feng, Terry A. Lyle, Kenneth J. Stauffer, Thomas J. Tucker, Joseph P. Vacca
  • Diamino isothiazole-1-oxides and 1,1 dioxides as gastric secretion inhibitors
    Patent number: 5171860
    Abstract: This invention is directed to diamino isothiazole -1-oxides and -1,1-dioxides and related compounds as well as pharmaceutical compositions and methods useful in the treatment of gastric secretion in mammals.
    Type: Grant
    Filed: November 12, 1991
    Date of Patent: December 15, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Susan F. Britcher, William C. Lumma, Jr.
  • 2-substituted-1(4)-aryl piperazines and the process for their preparation
    Patent number: 5051422
    Abstract: This invention relates to novel 2-substituted-1(4)-aryl piperazines and to a process for their preparation. The compounds of this invention have been found to have cardiovascular, primarily antiarrhythmic effects and are of the following general formula I ##STR1## wherein R is hydrogen, lower alkyl or benzyl; and R.sub.1 and R.sub.2 are the same or independently hydrogen, lower alkyl, lower alkoxy or halogen;Z is ##STR2## --NR.sub.3 --CH.sub.2 --, --OCH.sub.2 --, --NR.sub.3 --, --O-- or --NR.sub.3 SO.sub.2 -- andQ is (C.sub.1 -C.sub.4) alkyl--SO.sub.2 --NR.sub.4 -- or ##STR3## R.sub.3 is hydrogen, lower alkyl, allyl or loweralkoxyloweralkyl; and included in the descriptors of the compounds of Formula I is the proviso that when R.sub.4 is methyl then ##STR4## must be in the 2 position of Formula I.
    Type: Grant
    Filed: September 15, 1989
    Date of Patent: September 24, 1991
    Assignee: Schering AG
    Inventors: William C. Lumma, Jr., Thomas K. Morgan, Jr., Gary B. Phillips
  • Derivatized alkanolamines as cardiovascular agents
    Patent number: 5051423
    Abstract: Novel derivatized alkanolamines of the following structural formula ##STR1## are described as useful cardiovascular agents. Most especially described is their usefulness as cardiovascular agents exhibiting an antiarrhythmic effect. Said antiarrhythmic effect is of a combination Class II/Class III variety. Pharmaceutical formulations containing such compounds are also described.
    Type: Grant
    Filed: July 13, 1988
    Date of Patent: September 24, 1991
    Assignee: Schering AG
    Inventors: Randall E. Lis, William C. Lumma, Jr., Thomas K. Morgan, Jr., Klaus Nickisch, Ronald A. Wohl