Patents Represented by Attorney Francis P. Bigley
  • Patent number: 5698566
    Abstract: A series of novel spirocycles of general structural formula: ##STR1## or a pharmaceutically acceptable salt, hydrate or crystal form thereof are presented, whereinR.sup.1 =H.sub.3 CSO.sub.2 NH--, H.sub.3 CO--, alkylSO.sub.2 --, alkylCONH--, NO.sub.2 --;R.sup.2 =H, --OCH.sub.3 ;R.sup.3 and R.sup.4 taken together are .dbd.O, or R.sup.3 is H and R.sup.4 is OH;R.sup.5 =R.sup.6 taken together are --CH.sub.2 --CH.sub.2 --, .dbd.CH.sub.2 ;R.sup.7 is ##STR2## which are Class III antiarrhythmic agents and positive inotropic or cardiotonic agents.
    Type: Grant
    Filed: November 2, 1995
    Date of Patent: December 16, 1997
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, David A. Claremon, Jason M. Elliott, Gerald S. Ponticello, David C. Remy, Harold G. Selnick
  • Patent number: 5696111
    Abstract: This invention is concerned with novel compounds represented by structural formula I and II. ##STR1## which are antiarrhythmic agents.
    Type: Grant
    Filed: May 16, 1996
    Date of Patent: December 9, 1997
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, David A. Claremon, Nigel Liverton, Harold G. Selnick
  • Patent number: 5691331
    Abstract: This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 25, 1997
    Assignee: Merck & Co., Inc.
    Inventors: David A. Claremon, Roger M. Freidinger, Nigel Liverton, Harold G. Selnick, Garry R. Smith
  • Patent number: 5638657
    Abstract: A system and method for automatically feeding, inspecting and diverting tablets for continuous filling of tablet containers includes a tablet conveyor system which divides the tablets in a plurality of tablet streams for inspection by color, size and shape. Following the tablet inspection, each tablet passes through a tablet diverter which diverts the tablets to a recycle stream, reject stream or one of two bottle filling positions based upon instruction from the inspection. A bottle conveyor system is provided which feeds empty bottles into a bottle escapement mechanism which positions the empty bottles for filling. Filled bottles are moved from the bottle escapement mechanism to an exit conveyor. The entire system is computer controlled by various control mechanisms to enable the system to be fully operational without operator assistance.
    Type: Grant
    Filed: March 1, 1996
    Date of Patent: June 17, 1997
    Assignee: Merck & Co., Inc.
    Inventors: John R. Archer, David E. Cumpstey, Richard H. Gray, Stephen Owen
  • Patent number: 5633251
    Abstract: This invention is concerned with novel compounds represented by structural formula I ##STR1## where R.sup.1 is ##STR2## X and Y are independently hydrogen, fluoro, chloro, bromo, iodo, or trifluoromethyl;n is 0, 1 or 2; andR.sup.2 is hydrogen, fluoro, chloro, bromo, iodo, or trifluoromethyl, methyl, or methoxy;as the racemates, mixtures of enantiomers, individual diastereomers or individual enantiomers, and pharmaceutically acceptable crystal forms, salts, or hydrates thereof.
    Type: Grant
    Filed: August 17, 1995
    Date of Patent: May 27, 1997
    Assignee: Merck & Co., Inc.
    Inventors: David A. Claremon, Nigel Liverton, Harold G. Selnick
  • Patent number: 5631251
    Abstract: This invention is concerned with novel compounds represented by structural formula I ##STR1## Z is C.sub.0-6 alkyl; and R.sup.1 is phenyl or mono or disubstituted phenyl, where the substitutents are Cl, and CF.sub.3,or pharmaceutically acceptable salts, hydrates and crystal forms thereof which are useful in the treatment of arrhythmia.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: May 20, 1997
    Assignee: Merck & Co., Inc.
    Inventors: John Butcher, David A. Claremon, Nigel Liverton, Harold G. Selnick
  • 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
  • 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.
  • 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
  • Patent number: 5550126
    Abstract: Pharmaceutical compositions and methods of using CCK-ligands D,L-glutamic acid and D,L-aspartic acid as antipsychotic, antianxiety, and agents useful in treatment or prevention of withdrawal symptoms caused by withdrawal of chronic or long term use of diazepam, alcohol, cocaine or nicotine and antianxiety agents are described.
    Type: Grant
    Filed: January 30, 1995
    Date of Patent: August 27, 1996
    Assignee: Merck Sharp and Dohme Limited
    Inventors: David C. Horwell, John Hughes, Geoff N. Woodruff
  • Patent number: 5543154
    Abstract: A device for the controlled delivery of a beneficial agent as a gelatinous dispersion consisting of (i) a core which contains a beneficial agent, a polymer which forms gelatinous micoroscopic particles upon hydration and if desired an agent to modulate the hydration of the polymer; 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 a disperson comprising gelatinous microscopic particles.
    Type: Grant
    Filed: October 21, 1994
    Date of Patent: August 6, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Gerald S. Rork, James D. Pipkin
  • Patent number: 5541208
    Abstract: The present invention relates to compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof which are useful as potassium channel antagonists, particularly Maxi-K channel antagonists, and thus useful in treating Alzheimer's Disease and other cognitive disorders. This invention is also related to a method of making the compound of formula (I).
    Type: Grant
    Filed: January 24, 1994
    Date of Patent: July 30, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Maria L. Garcia, Robert A. Giacobbe, Otto D. Hensens, Seok H. Lee, Owen B. McManus, Deborah L. Zink
  • Patent number: 5525596
    Abstract: Intestional absorption of zwitterionic compounds is enhanced when the compound is delivered with the absorption enhancer palmitoyl carnitine chloride and the solubilizing agent .beta.-cyclodextrin when compared to delivery with palmitoyl carnitine chloride or .beta.-cyclodextrin alone.
    Type: Grant
    Filed: October 21, 1994
    Date of Patent: June 11, 1996
    Assignee: Merck & Co., Inc.
    Inventor: Gerold L. Mosher
  • Patent number: 5522512
    Abstract: A system and method for automatically feeding, inspecting and diverting tablets for continuous filling of tablet containers includes a tablet conveyor system which divides the tablets in a plurality of tablet streams for inspection by color, size and shape. Following the tablet inspection, each tablet passes through a tablet diverter which diverts the tablets to a recycle stream, reject stream or one of two bottle filling positions based upon instruction from the inspection. A bottle conveyor system is provided which feeds empty bottles into a bottle escapement mechanism which positions the empty bottles for filling. Filled bottles are moved from the bottle escapement mechanism to an exit conveyor. The entire system is computer controlled by various control mechanisms to enable the system to be fully operational without operator assistance.
    Type: Grant
    Filed: May 9, 1994
    Date of Patent: June 4, 1996
    Assignee: Merck & Co., Inc.
    Inventors: John R. Archer, David E. Cumpstey, Richard H. Gray, Stephen Owen
  • Patent number: 5516491
    Abstract: A disposable transportable reactor vessel can be prepared by modifying an eye-dropper pipette. A HDPE plug is inserted in one end of the pipette to permit selective passage of fluid while preventing resin flow. The pipette is looped into the shape of a u-tube and inserted into a holder such that the pipette is axially aligned with the holder to facilitate use in a robotic system.
    Type: Grant
    Filed: July 28, 1994
    Date of Patent: May 14, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Gary S. Kath, Gregory W. King, Kevin Chapman
  • Patent number: 5506228
    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. ##STR1## or a pharmaceutically acceptable salt, hydrate or crystal form thereof, wherein:when M is S, R.sup.1 and R.sup.2 are selected from the following combinations:when R.sup.2 is 4-chloro, then R.sup.1 is 4-OCH.sub.3,2 -CH.sub.3, 4-Cl, 4-CH3,3-Cl, 3-CH3, 2-Cl, 4-H, 4-Br, 3-NO.sub.2 ; andwhen R.sup.2 is H, then R.sup.1 is 4-OCH.sub.3, andwhen M is --SO.sub.2 --, then R.sup.2 is H and R.sup.1 is 4-OCH.sub.3.As an immunosuppressant, these compounds are useful in the treatment of autoimmune diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.
    Type: Grant
    Filed: February 23, 1995
    Date of Patent: April 9, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Richard Norton, Mohammed K. A. Ibraham
  • Patent number: 5504332
    Abstract: A method and system for determining the homogeneity of one or more components of a mixture of ingredients, especially, is presented. Most importantly, it can be used to determine homogeneity of a tabletted mixture of the produced pharmaceuticals, including active and inactive ingredients. The method and system monitor the pharmaceutical material during tablet manufacture as a powder mix, granular mix and compressed tablets. This system uses near infrared technology for analyzing the uniformity and mass balance of the pharmaceutical mixture to control the tablet manufacturing process. As part of the system and method, a NIR spectral library, consisting of a pharmaceutical materials spanning the normal process range for is developed. Assessment of uniformity is accomplished by comparison of future production with the library of acceptable material.
    Type: Grant
    Filed: August 26, 1994
    Date of Patent: April 2, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Eric W. Richmond, Bruce R. Buchanan, Mark A. Baxter, Andy Duff, Oksana M. Tully, Samuel A. Thornton
  • Patent number: 5494895
    Abstract: A thirty-nine amino acid peptide, Margatoxin (MgTX), is purified to homogeneity from venom of the scorpion Centruroides margaritatus. The gene encoding MgTX is constructed and this gene is expressed in E. coli, to produce recombinant MgTX. MgTX is a potent and selective inhibitor of a voltage-dependent K.sup.+ channel present in human lymphocytes. MgTX exhibits immunosuppressant activity with human T-lymphocytes, and is useful as an immunosuppressant, in modeling nonpeptidyl K.sup.+ channel blockers, and in establishing biochemical assays based on ligand binding or other protocols with which to screen for other novel modulators of voltage dependent K.sup.+ channels in lymphocytes and other tissues including the brain. As an immunosuppressant, MgTX is useful in the treatment of autoimmune diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.
    Type: Grant
    Filed: July 22, 1993
    Date of Patent: February 27, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Maria L. Garcia, Gloria C. Koo, Reid J. Leonard, Chiu-Chuan S. Lin, Robert S. Slaughter, Scott P. Stevens, Joanne M. Williamson
  • Patent number: 5489024
    Abstract: There is disclosed a medication container which is adapted to be side loaded with unit doses of medication during packaging operations. After being filled with the unit doses of medication, the container side is sealed. The medication doses can be removed by a user from the sealed container by means of a child resistant removable closure at one end of the container.
    Type: Grant
    Filed: August 8, 1994
    Date of Patent: February 6, 1996
    Assignee: Merck & Co., Inc.
    Inventor: Leonid Bunin
  • Patent number: 5484923
    Abstract: The present invention is directed to a process of making spirocycles of general structural formula: ##STR1## where R.sub.1 is selected from the group consisting of CO--C.sub.1-3 alkyl, cyano, carboxy, carboxy C.sub.1-6 alkyl ester, carboxamide, C.sub.1-6 alkyl sulfinyl, C.sub.1-6 alkyl sulfonyl, C.sub.1-6 methanesulfonamide and halogen; R.sub.2 is selected from the group consisting of keto or alcohol, R.sub.3 is cyano, resulting in compounds which are Class III antiarrhythmic.
    Type: Grant
    Filed: May 31, 1994
    Date of Patent: January 16, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Dongwei Cai, Richard Desmond, Yao-Jun Shi, David M. Tschaen, Thomas R. Verhoeven