Patents Represented by Attorney, Agent or Law Firm Mark R. Daniel
  • Combination of an ace inhibitor and a diuretic
    Patent number: 5686451
    Abstract: Pharmaceutical formulations comprising as active ingredients an angiotensin converting enzyme (ACE) inhibitor at a dose level normally found effective as an antihypertensive and a diuretic at a dose level below its minimum effective dose, demonstrate greater efficacy than would be expected in returning the blood pressure of hypertensive patients to normotensive values.
    Type: Grant
    Filed: September 5, 1995
    Date of Patent: November 11, 1997
    Inventors: J. Krister Kristianson, Per Wold-Olsen
  • Endothelin antagonists
    Patent number: 5686478
    Abstract: Novel derivatives of the general structural Formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, complications of diabetes, migraine, bone resorption, and inflammatory diseases, including Raynaud's disease and asthma.
    Type: Grant
    Filed: July 7, 1994
    Date of Patent: November 11, 1997
    Assignee: Merck & Co. Inc.
    Inventors: William J. Greenlee, Thomas F. Walsh
  • Antifungal agent
    Patent number: 5686637
    Abstract: There is disclosed a novel compound having the formula ##STR1## which exhibits antifungal activity.
    Type: Grant
    Filed: January 10, 1995
    Date of Patent: November 11, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Gerald F. Bills, James E. Curotto, S. Dreikorn, Robert A. Giacobbe, Guy H. Harris, Suzanne Miller Mandala, Rosemary A. Thornton, Deborah L. Zink, Angeles Cabello Arroyo, Fernando Pelaez Perez, Teresa Diez Matas, Francisca Vicente Perez
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5686472
    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: October 27, 1993
    Date of Patent: November 11, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, S. Jane deSolms, Ta Jyh Lee, deceased
  • Acyloxyisopropyl carbamates as prodrugs for amine drugs
    Patent number: 5684018
    Abstract: This invention relates to novel acyloxyisopropyl carbamates as bioreversible prodrug moieties for amino drugs and to methods of synthesizng these compounds.
    Type: Grant
    Filed: December 13, 1994
    Date of Patent: November 4, 1997
    Assignee: Merck & Co., Inc.
    Inventor: Jose Alexander
  • Preparation of carboxyalkyl derivatives as inhibitors of matrix metalloproteinases
    Patent number: 5684152
    Abstract: Carboxy-peptidyl compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, coronary thrombosis associated with atherosclerotic plaque rupture, and aneurysmal aortic disease. This invention relates to a process of making the carboxy-peptidyl compounds of formula I.
    Type: Grant
    Filed: September 19, 1996
    Date of Patent: November 4, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Mitree M. Ponpipom, William K. Hagmann
  • Process for preparing side chain derivatives of cyclohexapeptidyl lipopeptides
    Patent number: 5684128
    Abstract: An improved process for the preparation of side chain derivatives of cyclohexapeptidyl lipopeptides represented by the formula ##STR1## wherein R.sup.1 is fully defined, is disclosed.
    Type: Grant
    Filed: February 20, 1996
    Date of Patent: November 4, 1997
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Frances A. Bouffard, James F. Dropinski, Akinlolu A. Adefarati, Jan S. Tkacz
  • Benzodiazepines
    Patent number: 5679672
    Abstract: Compounds of structures (I) and (Ia) are Class III antiarrhythmic agents ##STR1##
    Type: Grant
    Filed: May 14, 1996
    Date of Patent: October 21, 1997
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, David A. Claremon, Jason M. Elliott, Nigel Liverton, David C. Remy, Harold G. Selnick
  • Triterpene derivatives with immunosuppressant activity
    Patent number: 5679705
    Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.
    Type: Grant
    Filed: October 16, 1996
    Date of Patent: October 21, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, William H. Parsons, Kathleen M. Rupprecht
  • Device for dropwise delivery of a fluid contained in a flexible vial
    Patent number: 5673822
    Abstract: The present invention provides a device for the dropwise delivery of a fluid (6) contained in a flexible vial (4; 4'), the device comprising a tubular case (1) capable of surrounding the vial (4; 4'), which casing is provided with a bottom portion (2; 7) whose inner surface lies opposite the outer surface of the bottom wall (42; 42') of the vial (4; 4'), the bottom portion (2; 7) of the casing (1) being equipped with a resiliently displaceable tab (3; 8) which can be moved so as to press against the bottom wall (42; 42') of the vial (4; 4') in order to squeeze the vial (4; 4') and drive out a drop (60) of fluid.
    Type: Grant
    Filed: June 21, 1995
    Date of Patent: October 7, 1997
    Assignee: Laboratoires Merck Sharp & Dohme-Chibret
    Inventors: Patrice Chalmin, Jean Gazzola, Arthur Lifshey
  • Method for analyzing isomers of enalapril and enalaprilat
    Patent number: 5670655
    Abstract: The invention relates to a method for analyzing degenerates of enalapril maleate and enalaprilat, potent angiotensin converting enzyme inhibitors.
    Type: Grant
    Filed: September 10, 1996
    Date of Patent: September 23, 1997
    Assignee: Merck & Co. Inc.
    Inventors: Xue-Zhi Qin, Giuseppina Visentini, Qingxi Wang
  • 2,6-diaryl pyridazinones with immunosuppressant activity
    Patent number: 5670504
    Abstract: A class of 2,6-diarylpyridazinones of general structural formula I have been identified that exhibit exhibit immunosuppressant activity with human T-lymphocytes, and are useful as an immunosuppressants.
    Type: Grant
    Filed: February 23, 1995
    Date of Patent: September 23, 1997
    Assignee: Merck & Co. Inc.
    Inventors: Richard J. Bochis, Andrew Kotliar, William H. Parsons, Kathleen Rupprecht
  • Aza cyclohexapeptide compounds
    Patent number: 5668105
    Abstract: Compounds represented by the formula (Seq ID Nos. 1-6) ##STR1## wherein all substituents are fully defined, are disclosed. These compounds exhibit utilities as antibiotic and antifungal agents and for the treatment and prevention of Pneumocystis infections.
    Type: Grant
    Filed: March 12, 1996
    Date of Patent: September 16, 1997
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Frances A. Bouffard, Milton L. Hammond
  • Phenoxyphenylacetic acid derivatives
    Patent number: 5668176
    Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.
    Type: Grant
    Filed: October 18, 1996
    Date of Patent: September 16, 1997
    Assignee: Merck & Co. Inc.
    Inventors: Scott W. Bagley, Theodore P. Broten, Prasun K. Chakravarty, Daljit S. Dhanoa, Kenneth J. Fitch, William J. Greenlee, Nancy Jo Kevin, Gerard R. Kieczykowski, Douglas J. Pettibone, James R. Tata, Ralph A. Rivero, Thomas F. Walsh, David L. Williams, Jr., Jay M. Matthews, Richard B. Toupence
  • Substituted phthalazinones as neurotensin antagonists
    Patent number: 5668279
    Abstract: Novel substituted phthalazinones of the formula (I) ##STR1## are useful as neurotensin antagonists.
    Type: Grant
    Filed: April 6, 1995
    Date of Patent: September 16, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, Elizabeth M. Naylor, Anna Chen
  • 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.
  • Treatment of atherosclerosis with angiotensin II receptor blocking imidazoles
    Patent number: 5663186
    Abstract: A method of treatment for atherosclerosis and/or reducing cholesterol using an angiotensin II antagonist. This method of treatment can be used in conjunction with the treatment of hypertension. Substituted imidazoles such as ##STR1## are useful as angiotensin II receptor antagonists for this method of treatment. A method of treatment for atherosclerosis and/or reducing cholesterol using an angiotensin II receptor antagonist in combination with an HMG-Co A reductase inhibitor. A method of treatment for atherosclerosis and/or reducing cholesterol using an angiotensin II receptor antagonist in combination with an HMG-Co A reductase inhibitor and an angiotensin converting enzyme inhibitor. Also within the scope of this invention are pharmaceutical compositions for this method of use.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 2, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Edward B. Nelson, Charles S. Sweet
  • 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.
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5663193
    Abstract: The present invention is directed to non-peptide compounds which inhibit farnesyl-protein transferase (FPTase) and the farnesylation of the oncogene protein Ras. The invention also relates to the process for the preparation of a compound of this invention by cultivating a culture of Phoma sp. 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: July 17, 1996
    Date of Patent: September 2, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Carmen Cascales, Russell B. Lingham, Fernando Pelaez, Jon D. Polishook, Keith C. Silverman, Sheo B. Singh, Deborah L. Zink
  • Prodrugs of herpes TK inhibitors
    Patent number: 5663175
    Abstract: Certain prodrugs such as ##STR1## are useful in the inhibition of herpes virus thymidine kinase, the prevention or treatment of recurrent infection by herpes virus, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing or treating recurrent infection by herpes virus are also described.
    Type: Grant
    Filed: December 9, 1994
    Date of Patent: September 2, 1997
    Assignee: Merck & Co. Inc.
    Inventors: Richard L. Tolman, John D. Karkas, Derek Von Langen, Malcolm MacCoss