Patents Represented by Attorney, Agent or Law Firm Mark R. Daniel
  • Ophthalmic package and delivery device
    Patent number: 5624057
    Abstract: This invention consists of an ophthalmic storage and dispensing device formed by injection molding, consisting of a vial with thick rigid walls and a limited flexible area. The flexible area allows only a small displacement when squeezed providing a metered volume of dispensed liquid. It also has an integral molded dropper tip as well as an integral molded puncture membrane within the tip. A bottom plug, which serves as closure after filling, is sealed to the vial. The bottom plug is of varying size and shape so as to provide for varying internal liquid capacity in the same bottle. It can also have a separate cap which acts as both a seal break and reclosable mechanical liquid seal between usage periods. Both vial and cap offer a geometric shape which facilitates gripping and limits rolling.
    Type: Grant
    Filed: May 1, 1995
    Date of Patent: April 29, 1997
    Assignee: Merck & Co., Inc.
    Inventor: Arthur L. Lifshey
  • Modified pseudomonas exotoxin PE.sub.40
    Patent number: 5621078
    Abstract: Pseudomonas exotoxin 40 is modified by deleting or substituting one or more cysteine residues. Such a modified protein, when hybridized to TGF.alpha., exhibits altered biological activities from unmodified TGF.alpha. PE.sub.40, including decreased cell killing activity and increased receptor-binding activity.
    Type: Grant
    Filed: February 21, 1995
    Date of Patent: April 15, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Mark W. Riemen, Steven M. Stirdivant
  • Boronic acid compound
    Patent number: 5618934
    Abstract: The present invention is directed to a compound represented by the structural formula: ##STR1## wherein Z-- represents a negatively charged counterion.
    Type: Grant
    Filed: February 27, 1995
    Date of Patent: April 8, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Ann E. DeCamp, Edward J. J. Grabowski, Mark A. Huffman, Lyndon C. Xavier, Nobuyoshi Yasuda, Guo-Jie Ho, David J. Mathre
  • Dioxobutanoic acid derivatives as inhibitors of influenza endonuclease
    Patent number: 5618830
    Abstract: Dioxobutanoic acids substituted with piperidine or similar N-substituted saturated cycloalkyls are found to inhibit the cap-dependent endonuclease of influenza virus. These compounds are useful in the prevention or treatment of infection by influenza virus and the treatment of influenza, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating influenza and methods of preventing or treating infection by influenza virus are also described.
    Type: Grant
    Filed: September 29, 1995
    Date of Patent: April 8, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Harold G. Selnick, John J. Baldwin, Gerald S. Ponticello, Joanne E. Tomassini
  • Controlled-pH formulation for intravesicular instillation of TGF.alpha.PE.sub.40 ab
    Patent number: 5612313
    Abstract: A buffered intravesicular pharmaceutical dosage system for delivery of TGF.alpha.PE.sub.40 ab to a human bladder for bladder cancer chemotherapy, in which a buffer system of 100 mM phosphate at an initial pH of 7.8 maintains a pH range in the bladder of 6.5 to 7.8 that is sufficient to maximize interaction of TGF.alpha.PE.sub.40 ab with the EGF receptor expressed on the surface of bladder cancer cells and to prevent aggregation of the TGF.alpha.PE.sub.40 ab while in the bladder.
    Type: Grant
    Filed: June 27, 1996
    Date of Patent: March 18, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Dorothy Marquis-Omer, C. Russell Middaugh, Gautam Sanyal
  • Polymorphs of losartan and the process for the preparation of form II of losartan
    Patent number: 5608075
    Abstract: Polymorphic forms of Losartan (Formula I) ##STR1## and a process for the preparation of Form II of Losartan. Losartan is known to be useful in the treatment of hypertension.
    Type: Grant
    Filed: January 12, 1995
    Date of Patent: March 4, 1997
    Assignees: Merck & Co., Inc., E. I. Du Pont de Nemours & Company, The DuPont Merck Pharmaceutical Company
    Inventors: Gordon C. Campbell, Jr., Anil M. Dwivedi, Dorothy A. Levorse, James A. McCauley, Krishnaswamy S. Raghavan
  • Cannabinoid receptor agonists
    Patent number: 5605906
    Abstract: Disclosed are novel cannabinoid (CB2) receptor agonists, their compositions, and the methods of their preparation. The compounds are useful for lowering ocular intra ocular pressure, treating glaucoma, useful as antiinflammatory, immunosuppressive, analgesics agents, and as agents for treatment and prevention of emesis and nausea because of the activity on the cannabinoid receptor.
    Type: Grant
    Filed: March 24, 1995
    Date of Patent: February 25, 1997
    Assignee: Merck Frosst Canada, Inc.
    Inventor: Cheuk K. Lau
  • Pour-on formulations consisting of gylcols, glycerides and avermectin compounds
    Patent number: 5602107
    Abstract: There is disclosed a topical pour-on formulation containing glycols, glycerides, or their derivatives and an avermectin compound (active ingredient) which has been discovered to provide superior efficacy against endoparasites and ectoparasites when compared to conventional formulations and to maintain the concentration of the active compound in the milk of dairy animals below a safe concentration for human consumption. The formulation contains the avermectin active ingredient and at least 50% of the glycol or glyceride.
    Type: Grant
    Filed: November 20, 1995
    Date of Patent: February 11, 1997
    Assignee: Merck & Co., Inc.
    Inventor: Hoo-Kyun Choi
  • Peptides
    Patent number: 5599686
    Abstract: Assays which comprise oligopeptides and which are useful for determining free PSA protease activity in vitro and in vivo are described. Such oligopeptides comprise amino acid sequences that are recognized and proteolytically cleaved by free prostrate specific antigen (PSA). Also described are assays useful in identifying inhibitors of free PSA.
    Type: Grant
    Filed: June 28, 1994
    Date of Patent: February 4, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Deborah DeFeo-Jones, Victor M. Garsky, Raymond E. Jones, Allen I. Oliff
  • Antifungal agents
    Patent number: 5597806
    Abstract: There are disclosed novel compounds having the formula ##STR1## which exhibit antifungal activity.
    Type: Grant
    Filed: May 9, 1995
    Date of Patent: January 28, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Wendy H. Clapp, Guy H. Harris, Gerald F. Bills, James E. Curotto, Anne W. Dombrowski, Sarah J. Driekorn, Myra B. Kurtz, Maria S. Meinz, Janet C. Onishi, Jon D. Polishook, Stanley L. Streicher, John R. Thompson, Marie Williams, Deborah L. Zink
  • Methods of treating cardiac arrhythmia
    Patent number: 5597818
    Abstract: Benzodiazepine analogs have been found to be useful in treating cardiac abnormalities.
    Type: Grant
    Filed: March 20, 1995
    Date of Patent: January 28, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Michael C. Sanguinetti, Joseph J. Salata, Joseph J. Lynch, Jr.
  • Antiarrhythmic benzodiazepines
    Patent number: 5595990
    Abstract: Benzo-(1,5)-diazepine derivatives with an amide or urea function in the 3-position are useful in the treatment of arrhythmia.
    Type: Grant
    Filed: March 27, 1995
    Date of Patent: January 21, 1997
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, David A. Claremon, Jason M. Elliott, Nigel Liverton, David C. Remy, Harold G. Selnick
  • Ruthenium-phosphine complex catalysts for asymmetric hydrogenations
    Patent number: 5596113
    Abstract: .beta.- or .gamma.-Ketoesters and .beta.- or .gamma.-ketoamides are asymmetrically reduced with a Ru(II)-BINAP derived catalyst at about 40.degree. C. and about 50 N/mm.sup.2 of hydrogen in the presence of a strong acid.
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: January 21, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Alan W. Douglas, Lisa DiMichele, Steven A. King, Thomas R. Verhoeven
  • Process of synthesizing N-acyl auxiliaries
    Patent number: 5594134
    Abstract: A process of synthesizing N-acyl auxiliary compounds is disclosed. A compound of the formula: ##STR1## is reacted with an anhydride in the presence of a lithium salt and an amine base to produce the N-acylated auxiliary.
    Type: Grant
    Filed: March 31, 1995
    Date of Patent: January 14, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Guo-Jie Ho, David J. Mathre
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5585359
    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 the farnesylation of Ras. Furthermore, these CAAX analogues differ from those previously described as inhibitors of Ras farnesyl 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 autoxidation 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.
    Type: Grant
    Filed: September 29, 1994
    Date of Patent: December 17, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Michael J. Breslin, S. J. deSolms, Samuel L. Graham, John H. Hutchinson, Gerald E. Stokker
  • Controlled release drug suspension delivery device
    Patent number: 5582838
    Abstract: A device is disclosed for the controlled delivery of a beneficial agent, the device consisting of (i) a core comprising at least two layers, wherein at least one layer comprises a beneficial agent and a polymer which forms microscopic gel beads upon hydration and at least one layer which comprises a polymer which forms microscopic gel beads upon hydration; and (ii) an impermeable, insoluble coating which adheres to and surrounds the core and contains apertures which provide an area for the hydration and release of the microscopic gel beads.
    Type: Grant
    Filed: December 22, 1994
    Date of Patent: December 10, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Gerald S. Rork, James D. Pipkin
  • Benzamide-containing inhibitors of farnesyl-protein transferase
    Patent number: 5578629
    Abstract: The present invention comprises peptidomimetic compounds which comprise a suitably substituted aminoalkylbenzamide moiety. The instant compounds inhibit the farnesyl protein transferase enzyme and the farnesylation of certain proteins. Furthermore, the instant farnesyl protein transferase inhibitors 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 autoxidation 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.
    Type: Grant
    Filed: March 29, 1995
    Date of Patent: November 26, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Terrence M. Ciccarone, Theresa M. Williams, Suzanne C. MacTough
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5576313
    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 treatment of cancer.
    Type: Grant
    Filed: August 29, 1994
    Date of Patent: November 19, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Thorsten E. Fisher, John S. Wai, J. Christopher Culberson, Walfred S. Saari
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5576293
    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 the farnesylation of Ras. Furthermore, these CAAX analogues differ from those previously described as inhibitors of Ras farnesyl 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 autoxidation 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.
    Type: Grant
    Filed: September 29, 1994
    Date of Patent: November 19, 1996
    Assignee: Merck & Co., Inc.
    Inventors: S. Jane deSolms, Victor M. Garsky, Elizabeth A. Giuliani, Robert P. Gomez, Samuel L. Graham, Gerald E. Stokker, Catherine M. Wiscount
  • Muscarine antagonists
    Patent number: 5574044
    Abstract: Compounds, 1,3-dihydro-1-{1-[piperidin-4-yl]piperidin-4-yl}-2H-benzimidazol-2-ones and 1,3-dihydro-1-{4-amino-1-cyclohexyl}-2H-benzimidazol-2-ones and derivatives thereof, their preparation, method of use and pharmaceutical compositions are described. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).
    Type: Grant
    Filed: October 27, 1994
    Date of Patent: November 12, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Wayne J. Thompson, Michael F. Sugrue, Richard W. Ransom, Pierre J. Mallorga, Ian M. Bell, Anthony M. Smith