Patents Represented by Attorney Paul D. Matukaitis
  • Patent number: 5650412
    Abstract: Compounds of formula ##STR1## are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in 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: October 26, 1995
    Date of Patent: July 22, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Byeong Moon Kim, Joseph P. Vacca
  • Patent number: 5484724
    Abstract: The DNA encoding glucan synthesis gene 1 (GLS1) is cloned and used in an in vitro assay to screen for compounds that modulate 1,3.beta.-D glucan synthase activity.
    Type: Grant
    Filed: May 26, 1994
    Date of Patent: January 16, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Mohamed El-Sherbeini, Joseph A. Clemas
  • Patent number: 5409911
    Abstract: This invention relates to a prostaglandin-bisphosphonate compound of the formula: ##STR1## and its pharmaceutically acceptable salts. The claimed compounds are effective as delivery agents of prostaglandins to treat osteoporosis and related bone diseases. The claimed compounds also simultaneously deliver a bisphosphonate which inhibits bone resorption and delivers prostaglandins which increase bone formation in vivo.
    Type: Grant
    Filed: September 11, 1992
    Date of Patent: April 25, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Peter C. Tyler, Robert N. Young, Gideon A. Rodan
  • Patent number: 5401832
    Abstract: Acidic fibroblast growth factor (aFGF) is isolated and purified from human brain tissue. The distinctive and complete amino acid sequences of both bovine and human aFGFs are determined and herein disclosed. Unique genes coding for these disclosed amino acid sequences are constructed. The bovine gene is derived from reverse translation of the aFGF amino acid sequence with unique restriction sites included while the human gene is derived by specific point mutations of the bovine gene. Each gene construct is inserted into an expression vector which is used to transform an appropriate host. The transformed host cells produce recombinant aFGF (r-aFGF), human or bovine, which is purified and has activity equivalent to the native protein. Both recombinant and purified brain-derived human and bovine aFGF are active mitogens for mesoderm and neuroectoderm-derived cells in culture, and promote wound healing of soft tissue, cartilaginous tissue and musculo-skeletal tissue.
    Type: Grant
    Filed: September 25, 1992
    Date of Patent: March 28, 1995
    Assignee: Merck & Co., Inc.
    Inventors: David L. Linemeyer, Linda J. Kelly, Guillermo Gimenez-Gallego, Kenneth A. Thomas, Jr.
  • Patent number: 5397791
    Abstract: Fibrinogen receptor antagonists having the formula ##STR1## for example ##STR2##
    Type: Grant
    Filed: August 9, 1993
    Date of Patent: March 14, 1995
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John D. Prugh, Wasyl Halczenko, Melissa Egbertson, Nathan Ihle
  • Patent number: 5391752
    Abstract: Anti-ulcer agents having a methylsulfinyl bridge between a substituted pyridine moiety and a substituted benzimidazole moiety are prepared by oxidizing the corresponding compounds, having a methylthio bridge, with magnesium monoperoxyphthalate in a suitable solvent. The reaction may be run in an aromatic hydrocarbon solvent, wherein the product may crystallize out of the reaction solution and may be directly isolated by filtration.
    Type: Grant
    Filed: February 22, 1993
    Date of Patent: February 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Robert S. Hoerrner, Joel J. Friedman, Joseph S. Amato, Thomas M. Liu, Ichiro Shinkai, Leonard M. Weinstock
  • Patent number: 5389631
    Abstract: Fibrinogen receptor antagonists of the ##STR1## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets wherein G is: ##STR2## for example, ##STR3##
    Type: Grant
    Filed: March 22, 1993
    Date of Patent: February 14, 1995
    Assignee: Merck & Co., Inc.
    Inventors: David A. Claremon, Nigel Liverton
  • Patent number: 5387504
    Abstract: Monospecific antibodies are produced which are specific for fragments of the connective tissue protein aggrecan, generated by specific stromelysin cleavage. These monospecific antibodies are used in an assay system to detect polypeptide fragments of aggrecan, produced by the specific cleavage of aggrecan by stromelysin. The presence of aggrecan polypeptide fragments demonstrates stromelysin activity. Elevations of stromelysin occur in osteoarthritis, rheumatoid arthritis, atherosclerotic lesions, gout, inflammatory bowel disease (IBD), idiopathic pulmonary fibrosis (IPF), certain cancers, joint injuries, and numerous inflammatory diseases. The monospecific antibodies and the assay system are used to quantitate aggrecan polypeptide fragments as a readout of stromelysin activity and to evaluate potential stromelysin inhibitors.
    Type: Grant
    Filed: September 30, 1992
    Date of Patent: February 7, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Richard A. Mumford, Michael W. Lark, Ellen B. K. Bayne, Lori A. Hoerrner
  • Patent number: 5385932
    Abstract: This invention relates to compounds of formulae I and II ##STR1## which are metabolites of tetrahydrosimvastatin and 5-hydroxy-tetrahydrosimvastatin and which are HMG--CoA reductase inhibitors.
    Type: Grant
    Filed: February 18, 1992
    Date of Patent: January 31, 1995
    Assignee: Merck & Co., Inc.
    Inventor: Stanley Vickers
  • Patent number: 5380728
    Abstract: 17.beta.-N-monosubstituted-carbamoyl-4-aza-5.alpha.-androst-1-en-3-ones of the formula: ##STR1## wherein the dotted line can represent a double bond when present,R.sup.1 is selected from hydrogen, methyl and ethyl andR.sup.2 is CONHC(CH.sub.3).sub.2 CHO, andRa is methyl,are described as being useful for the treatment of benign prostatic hypertrophy.
    Type: Grant
    Filed: February 10, 1993
    Date of Patent: January 10, 1995
    Assignee: Merck & Co., Inc.
    Inventor: Gary H. Rasmusson
  • Patent number: 5376383
    Abstract: The instant invention is directed to a method for enhancing the lowering of plasma cholesterol level in a subject in need thereof which comprises the time-controlled administration of a nontoxic therapeutically effective amount of an HMG-CoA reductase inhibitor to said subject which surprisingly affords an equivalent or improved reduction of plasma cholesterol levels while significantly reducing the amount of HMG-CoA reductase inhibitor circulating in the bloodstream of the subject as compared to the same parameters when the oral administration of a conventional rapid release dosage form is utilized.
    Type: Grant
    Filed: February 1, 1993
    Date of Patent: December 27, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Alfred W. Alberts, Edward M. Scolnick, Arnold J. Repta
  • Patent number: 5376396
    Abstract: A beverage stabilizing system which is a blend of gellan gum and carboxymethylcellulose. The blend provides a weak, stabilizing gel structure suitable for beverage products.
    Type: Grant
    Filed: April 27, 1993
    Date of Patent: December 27, 1994
    Assignee: Merck & Co., Inc.
    Inventor: Ross C. Clark
  • Patent number: 5376748
    Abstract: A class of optionally 4-substituted 3-nitro-2-oxo-1,2,3,4-tetrahydroquinoline derivatives are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA receptor antagonist.
    Type: Grant
    Filed: January 7, 1993
    Date of Patent: December 27, 1994
    Assignee: Merck Sharp & Dohme Limited
    Inventors: William R. Carling, Julian D. Smith, Paul D. Leeson
  • Patent number: 5374622
    Abstract: A fibrinogen receptor antagonist of the formulaAc-Cys-Asn-Pro-(L-AMF)-Gly-Asp-Cys-OHorAc-Cys-Asn-(DiMeTzl)-(L-AMF)-Gly-Asp-Cys-OH.
    Type: Grant
    Filed: January 28, 1993
    Date of Patent: December 20, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Ruth F. Nutt, Stephen F. Brady, Daniel F. Veber, Mark E. Duggan
  • Patent number: 5372829
    Abstract: The present invention is a procedure for preparing cooked foods which involve the use of a gellan gum batter to coat a food substrate to impart qualities which are typically associated with fried foods, including crispness and juiciness. The coated food is then fried and frozen. Food products resulting from the procedure of the present invention contain low levels of fat and yet have the desirable qualities of fried foods.
    Type: Grant
    Filed: January 15, 1993
    Date of Patent: December 13, 1994
    Assignee: Merck & Co., Inc.
    Inventors: William F. Chalupa, George R. Sanderson
  • Patent number: 5369125
    Abstract: This invention relates to compounds of structural formula (I): ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal agents. These compounds are also inhibitors of farnesyl protein transferase and farnesylation of the oncogene protein Ras and thus useful in treating cancer.
    Type: Grant
    Filed: March 19, 1993
    Date of Patent: November 29, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Gregory D. Berger, James D. Bergstrom, Tesfaye Biftu, Robert L. Bugianesi, Robert M. Burk, Narindar N. Girotra, C. H. Kuo, William H. Parsons, Mitree M. Ponpipom, Lori L. Whiting
  • Patent number: 5364948
    Abstract: This invention relates to compounds of structural formula (I) isolated from an aerobic fermentation of Trichoderma viride MF5628, ATCC 74084: ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents. These compounds are also potent antifungal agents. Additionally, they inhibit farnesyl protein transferase and farnesylation of the oncogene protein Ras and are thus useful in treating cancer. This invention also relates to a process for obtaining compounds of structural formula (I).
    Type: Grant
    Filed: February 9, 1993
    Date of Patent: November 15, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Guy H. Harris, Deborah Zink, E. Tracy T. Jones, Yu L. Kong
  • Patent number: 5364776
    Abstract: Incubation of ##STR1## with a preparation from mammalian organ yields as biotransformation products the 5-(1-hydroxy)ethyl pyridinone analog as well as the 5-(1-hydroxy)ethyl pyridyl and the 5-(2-hydroxy)ethyl pyridyl derivatives.
    Type: Grant
    Filed: February 24, 1992
    Date of Patent: November 15, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Suresh K. Balani, Laura R. Kauffman, Anthony D. Theoharides
  • Patent number: 5360736
    Abstract: A live, attenuated varicella zoster virus vaccine is produced with enhanced yield of VZV. The new process makes mass production of a live VZV vaccine more practical.
    Type: Grant
    Filed: June 4, 1992
    Date of Patent: November 1, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Philip J. Provost, David L. Krah, Paul A. Friedman
  • Patent number: 5358956
    Abstract: Novel fibrinogen receptor antagonists of the formula: ##STR1## are provided in which the claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating thrombus formation.
    Type: Grant
    Filed: October 14, 1992
    Date of Patent: October 25, 1994
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, Wasyl Halczenko