Patents Represented by Attorney Francis P. Bigley
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Patent number: 5698566Abstract: 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: GrantFiled: November 2, 1995Date of Patent: December 16, 1997Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, David A. Claremon, Jason M. Elliott, Gerald S. Ponticello, David C. Remy, Harold G. Selnick
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Patent number: 5696111Abstract: This invention is concerned with novel compounds represented by structural formula I and II. ##STR1## which are antiarrhythmic agents.Type: GrantFiled: May 16, 1996Date of Patent: December 9, 1997Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, David A. Claremon, Nigel Liverton, Harold G. Selnick
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Patent number: 5691331Abstract: This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia.Type: GrantFiled: June 7, 1995Date of Patent: November 25, 1997Assignee: Merck & Co., Inc.Inventors: David A. Claremon, Roger M. Freidinger, Nigel Liverton, Harold G. Selnick, Garry R. Smith
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Patent number: 5638657Abstract: 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: GrantFiled: March 1, 1996Date of Patent: June 17, 1997Assignee: Merck & Co., Inc.Inventors: John R. Archer, David E. Cumpstey, Richard H. Gray, Stephen Owen
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Patent number: 5633251Abstract: 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: GrantFiled: August 17, 1995Date of Patent: May 27, 1997Assignee: Merck & Co., Inc.Inventors: David A. Claremon, Nigel Liverton, Harold G. Selnick
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Patent number: 5631251Abstract: 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: GrantFiled: June 7, 1995Date of Patent: May 20, 1997Assignee: Merck & Co., Inc.Inventors: John Butcher, David A. Claremon, Nigel Liverton, Harold G. Selnick
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Patent number: 5624057Abstract: 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: GrantFiled: May 1, 1995Date of Patent: April 29, 1997Assignee: Merck & Co., Inc.Inventor: Arthur L. Lifshey
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Patent number: 5597818Abstract: Benzodiazepine analogs have been found to be useful in treating cardiac abnormalities.Type: GrantFiled: March 20, 1995Date of Patent: January 28, 1997Assignee: Merck & Co., Inc.Inventors: Michael C. Sanguinetti, Joseph J. Salata, Joseph J. Lynch, Jr.
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Patent number: 5582838Abstract: 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: GrantFiled: December 22, 1994Date of Patent: December 10, 1996Assignee: Merck & Co., Inc.Inventors: Gerald S. Rork, James D. Pipkin
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Patent number: 5550126Abstract: 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: GrantFiled: January 30, 1995Date of Patent: August 27, 1996Assignee: Merck Sharp and Dohme LimitedInventors: David C. Horwell, John Hughes, Geoff N. Woodruff
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Patent number: 5543154Abstract: 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: GrantFiled: October 21, 1994Date of Patent: August 6, 1996Assignee: Merck & Co., Inc.Inventors: Gerald S. Rork, James D. Pipkin
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Patent number: 5541208Abstract: 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: GrantFiled: January 24, 1994Date of Patent: July 30, 1996Assignee: Merck & Co., Inc.Inventors: Maria L. Garcia, Robert A. Giacobbe, Otto D. Hensens, Seok H. Lee, Owen B. McManus, Deborah L. Zink
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Patent number: 5525596Abstract: 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: GrantFiled: October 21, 1994Date of Patent: June 11, 1996Assignee: Merck & Co., Inc.Inventor: Gerold L. Mosher
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Patent number: 5522512Abstract: 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: GrantFiled: May 9, 1994Date of Patent: June 4, 1996Assignee: Merck & Co., Inc.Inventors: John R. Archer, David E. Cumpstey, Richard H. Gray, Stephen Owen
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Patent number: 5516491Abstract: 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: GrantFiled: July 28, 1994Date of Patent: May 14, 1996Assignee: Merck & Co., Inc.Inventors: Gary S. Kath, Gregory W. King, Kevin Chapman
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Patent number: 5506228Abstract: 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: GrantFiled: February 23, 1995Date of Patent: April 9, 1996Assignee: Merck & Co., Inc.Inventors: Richard Norton, Mohammed K. A. Ibraham
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Patent number: 5504332Abstract: 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: GrantFiled: August 26, 1994Date of Patent: April 2, 1996Assignee: Merck & Co., Inc.Inventors: Eric W. Richmond, Bruce R. Buchanan, Mark A. Baxter, Andy Duff, Oksana M. Tully, Samuel A. Thornton
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Patent number: 5494895Abstract: 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: GrantFiled: July 22, 1993Date of Patent: February 27, 1996Assignee: 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
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Patent number: 5489024Abstract: 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: GrantFiled: August 8, 1994Date of Patent: February 6, 1996Assignee: Merck & Co., Inc.Inventor: Leonid Bunin
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Patent number: 5484923Abstract: 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: GrantFiled: May 31, 1994Date of Patent: January 16, 1996Assignee: Merck & Co., Inc.Inventors: Dongwei Cai, Richard Desmond, Yao-Jun Shi, David M. Tschaen, Thomas R. Verhoeven