Patents Represented by Attorney William H. Nicholson

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  • Method for tablet preparation
    Patent number: 4898736
    Abstract: Dose uniformity in formulations of highly potent drugs may be achieved by distributing a solution of the active ingredient over a directly compressible tableting vehicle with subsequent evaporation of the solvent, followed by tableting.
    Type: Grant
    Filed: March 9, 1988
    Date of Patent: February 6, 1990
    Assignee: Merck & Co., Inc.
    Inventor: Ashok V. Katdare
  • Substituted thieno[2,3-b]thiophene-2-sulfonamides as antiglaucoma agents
    Patent number: 4894390
    Abstract: Aromatic sulfonamides useful in the treatment of elevated intraocular pressure having the structural formula: ##STR1## wherein A, R, R.sup.1, and R.sup.2 are as hereinafter defined, as well as the pharmaceutically and ophthalmologically acceptable salts thereof.
    Type: Grant
    Filed: October 21, 1988
    Date of Patent: January 16, 1990
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John D. Prugh
  • 7,8-dihydro-4-(1-pierazinyl)-6H-thiopyrano-[3,2-d] pyrimidines as .beta.-blockers
    Patent number: 4889856
    Abstract: 7,8-Dihydro-4-(1-piperazinyl)-6H-thiopyranopyrimidines have .beta.-adrenergic blocking properties and are thus useful in the treatment of cardiovascular ailments known to be amenable to .beta.-blocker therapy. Certain of the compounds are useful in the treatment of elevated intraocular pressure by topical ocular administration.
    Type: Grant
    Filed: August 31, 1987
    Date of Patent: December 26, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Richard L. Tolman, Arthur F. Wagner, John J. Baldwin, Adolph Pietruszkiewicz
  • Use of specific N-methyl-D-aspartate receptor antagonists in the prevention and treatment of neurodegeneration
    Patent number: 4888347
    Abstract: Specific N-methyl-D-aspartate receptor antagonists are useful in the prevention and treatment of neurodegeneration in various pathological states.
    Type: Grant
    Filed: December 24, 1986
    Date of Patent: December 19, 1989
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Geoffrey N. Woodruff, Erik H. F. Wong, John A. Kemp
  • Substituted thieno[3,2-b]thiophene-2-sulfonamides as topically active carbonic anhydrase inhibitors
    Patent number: 4876271
    Abstract: Novel substituted thieno[3,2-b]thiophene-2-sulfonamides are prepared by novel synthetic processes. These compounds are useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.
    Type: Grant
    Filed: December 20, 1988
    Date of Patent: October 24, 1989
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John D. Prugh
  • Polyhydro derivatives of 10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine
    Patent number: 4870080
    Abstract: 10,11-Dihydro-5H-dibenzo[a,d] cyclohepten-5,10-imines and derivatives thereof wherein one or the other or both benzo rings are hydrogenated are active anticonvulsants and atagonists of N-methyl-D-aspartate.
    Type: Grant
    Filed: May 5, 1988
    Date of Patent: September 26, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Theresa R. Lamanec, Terry A. Lyle
  • Derivatives of 5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine
    Patent number: 4870079
    Abstract: Fluoro-and hydroxy-derivatives of 5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines wherein the substituents are on non-benzenoid carbons are active anticonvulsants and antagonists of N-methyl-D-aspartate.
    Type: Grant
    Filed: March 30, 1988
    Date of Patent: September 26, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Susan F. Britcher, Wayne J. Thompson, Terry A. Lyle, Sandor L. Varga
  • Process for preparing 10,11-dihydro-11-exo-hydroxy-5-methyldibenzo[a,d]cyclohepten-5,10-imine
    Patent number: 4869791
    Abstract: 10,11 Dihydro-11-exo-hydroxy-5-methyldibenzo[a,d]cyclohepten-5,10-imine is prepared in a four step synthesis which uses an electrochemical cyclization to form the 5,10-imine bridge in about a 50% yield.
    Type: Grant
    Filed: June 24, 1988
    Date of Patent: September 26, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Sandor Karady, Leonard M. Weinstock
  • Substituted aromatic sulfonamides as antiglaucoma agents, compositions and use
    Patent number: 4863922
    Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
    Type: Grant
    Filed: June 15, 1988
    Date of Patent: September 5, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello, Marcia E. Christy
  • [3R]-3-amino-1-hydroxy pyrrolidin-2-one and its use as a neuroprotective agent
    Patent number: 4863953
    Abstract: The present invention provides R(+)-3-amino-1-hydroxypyrrolidin-2-one of formula I: ##STR1## or pharmaceutically acceptable acid addition salt thereof, which compound is useful as an anticonvulsant agent and in the treatment and/or prevention of neurodegenerative disorders.
    Type: Grant
    Filed: November 18, 1988
    Date of Patent: September 5, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Paul D. Leeson, Brian J. Williams
  • Ophthalmological composition of the type which undergoes liquid-gel phase transition
    Patent number: 4861760
    Abstract: The present invention relates to a pharmaceutical composition intended for contacting with a physiological liquid characterized in that said composition is intended to be administered as a non-gelled liquid form and is intended to gel in situ, this composition containing at least one polysaccharide in aqueous solution, of the type which undergoes liquid-gel phase transition gelling in situ under the effect of an increase in the ionic strength of said physiological liquid.
    Type: Grant
    Filed: September 25, 1986
    Date of Patent: August 29, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Claude Mazuel, Marie-Claire Friteyre
  • Thiophene sulfonamide antiglaucoma agents
    Patent number: 4847289
    Abstract: Aryl (or aralkyl)-sulfonylthiophene-2-sulfonamides containing a basic functional group as a substituent are efficacious in the treatment of elevated intraocular pressure and glaucoma following topical ocular administration.
    Type: Grant
    Filed: June 8, 1987
    Date of Patent: July 11, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Charles M. Habecker, Samuel L. Graham, Wasyl Halczenko, George D. Hartman, Harvey Schwam, Gerald S. Ponticello, Kenneth L. Shepard
  • 2-Sulfamoyl-1H-indole derivatives for the treatment of elevated intraocular pressure
    Patent number: 4840963
    Abstract: Novel 2-sulfamoyl-1H-indoles and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in pharmaceutical compositions designed for systemic or topical ophthalmic administration.
    Type: Grant
    Filed: December 7, 1984
    Date of Patent: June 20, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Shepard, Samuel L. Graham
  • Preparation of n-formamidoyl[(s)-1-t-butoxy-3-methyl-2-amino)]1,2,3,4 tetrahydrobenzo [b]furo [2,3-c]pyridine and derivatives
    Patent number: 4835276
    Abstract: The present invention is directed to an enantioselective synthesis of 1,3,4,6,7,12b(S)-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin-2-one which is an intermediate in the production of the .alpha..sub.2 -adrenergic antagonist (2R,12bS)-N-(1,3,4,6,7,12-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin-2-yl) -N-methyl-2-hydroxy-ethanesulfonamide hydrochloride.
    Type: Grant
    Filed: July 3, 1986
    Date of Patent: May 30, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Ralph P. Volante, Richard Desmond, Ichiro Shinkai
  • Controlled release combination of carbidopa/levodopa
    Patent number: 4832957
    Abstract: A matrix or monolithic drug delivery system for the controlled release of carbidopa and levodopa consists of the two drugs uniformly dispersed in a polymer vehicle at a concentration that is greater than the solubility of either drug in the polymer. Treatment of parkinsonism with the controlled release formulation provides several advantages over treatment with the standard carbidopa/levodopa combinations presently employed.
    Type: Grant
    Filed: July 25, 1988
    Date of Patent: May 23, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Robert E. Dempski, Edward C. Scholtz, Donald W. Nibbelink, Scott A. Reines
  • .alpha..sub.2 -adrenoceptor antagonistic arylquinolizines
    Patent number: 4824849
    Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, platelet aggregation inhibitors, antiobesity agents, and modifiers of gastrointestinal motility.
    Type: Grant
    Filed: August 28, 1987
    Date of Patent: April 25, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Joel R. Huff, Joseph P. Vacca, Steven D. Young, Jane deSolms, James P. Guare, Jr.
  • Substituted aromatic sulfonamides as antiglaucoma agents
    Patent number: 4820848
    Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
    Type: Grant
    Filed: April 4, 1988
    Date of Patent: April 11, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Gerald S. Ponticello, Charles N. Habecker
  • Process for the geometric stereoselective dehydration of 3-(9-chloro-5,6-dihydro-11H-11-hydroxy-pyrrolo-(2,1-B)(3)-benzazepin-11- yl)-N,N-dimethyl-1-propanamine
    Patent number: 4820818
    Abstract: The muscle relaxant (E)-3-(9-chloro-5,6-dihydro-11H-pyrrolo[2,1-b][3]benzazepin-11-ylidene-N,N -dimethyl-1-propanamine is prepared by the geometric stereoselective dehydration of the intermediate carbinol with acidic agents and organic bases and low temperatures.
    Type: Grant
    Filed: May 2, 1988
    Date of Patent: April 11, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Ruth V. Wattley, Gerard R. Kieczykowski
  • Enantioselective synthesis of 1,3,4,6,7,12b(S)-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin-2-one
    Patent number: 4814452
    Abstract: An enantioselective synthesis of 1,3,4,6,7,12b(S)-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin-2-one provides a key intermediate for the preparation of the .alpha..sub.2 -adrenergic antagonist (2R,12bS)-N-(1,3,4,6,7,12-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin-2-yl) -N-methyl-2-hydroxyethanesulfonamide hydrochloride, useful as an anti-depressant.
    Type: Grant
    Filed: July 3, 1986
    Date of Patent: March 21, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Ralph P. Volante, Edward Corley, Ichiro Shinkai
  • Alkanesulfonamides as antiglaucoma agents
    Patent number: 4812463
    Abstract: Alkane sulfonamides with an electron withdrawing function .beta. to the sulfonamide group are topically effective carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma.
    Type: Grant
    Filed: December 10, 1987
    Date of Patent: March 14, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Samuel L. Graham, Thomas H. Scholz