Patents Represented by Attorney William H. Nicholson

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  • Furopyridine sulfonamides and their opthalmological compositions
    Patent number: 4808595
    Abstract: Furopyridine sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and disorders associated therewith such as glaucoma.
    Type: Grant
    Filed: May 5, 1988
    Date of Patent: February 28, 1989
    Assignee: Merck & Co., Inc.
    Inventor: Jacob M. Hoffman, Jr.
  • Substituted thieno[2,3-b]thiophene-2-sulfonamides as antiglaucoma agents
    Patent number: 4806562
    Abstract: Thieno[2,3-b]thiophene-2-sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma.
    Type: Grant
    Filed: May 4, 1988
    Date of Patent: February 21, 1989
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John D. Prugh
  • Amino-2-hydroxypropyloximinoheterocycle .alpha.-blockers
    Patent number: 4803286
    Abstract: Certain amino-2-hydroxypropyloximinoheterocycles are .beta.-adrenoceptor antagonists useful in the treatment of elevated intraocular pressure, hypertension, angina and arrhythmia.
    Type: Grant
    Filed: August 19, 1987
    Date of Patent: February 7, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello, David C. Remy, David A. Claremon, Stella W. King
  • Substituted thieno[2,3-B]furan-2-sulfonamides as antiglaucoma agents
    Patent number: 4798831
    Abstract: Thieno[2,3-b]furan-2-sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma.
    Type: Grant
    Filed: May 4, 1988
    Date of Patent: January 17, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John D. Prugh, George D. Hartman, Wasyl Halczenko
  • Thieno thiopyran sulfonamide derivatives, pharmaceutical compositions and use
    Patent number: 4797413
    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 26, 1987
    Date of Patent: January 10, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello, Marcia E. Christy
  • Closure counter
    Patent number: 4792664
    Abstract: A closure counter for counting how many times a screw cap closure has been closed and opened is described, which is back in its initial position after N closing and opening operations.The closure counter includes an open-bottomed housing (10) and a likewise open-bottomed cap-shaped counting unit (11) arranged in the housing for rotation about its longitudinal axis (12), the rotary motion relative to the housing (10) is limited to a fraction 1/N of one full rotation, and a display unit (13) is arranged for rotation about the longitudinal axis (12) of the counting unit (11), the rotation of the display unit (13) relative to the counting unit (11) being allowed in only one direction by a ratchet (14), the click motion likewise corresponds to the fraction 1/N of one full rotation, and there is sliding fit between the housing (10) and the display unit (13).
    Type: Grant
    Filed: December 24, 1986
    Date of Patent: December 20, 1988
    Assignee: Chibret Pharmazeutische GmbH
    Inventor: Walter Schwab
  • 2-Sulfamoylbenzo(b)thiophene derivatives pharmaceutical compositions and use
    Patent number: 4788192
    Abstract: Novel 2-sulfamoylbenzo[b]thiopenes and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.
    Type: Grant
    Filed: March 12, 1987
    Date of Patent: November 29, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Shepard, Samuel L. Graham
  • Dopamine agonists for treating elevated intraocular pressure
    Patent number: 4774243
    Abstract: Topical ocular administration of a dopamine agonist is effective in lowering abnormally elevated intraocular pressure and is useful in the prevention and treatment of glaucoma and related ocular diseases.
    Type: Grant
    Filed: December 24, 1985
    Date of Patent: September 27, 1988
    Assignee: Merck & Co., Inc.
    Inventor: John J. Baldwin
  • Chiral synthesis of (+)-trans-1a,2,3,4a,5,6-hexahydro-9-hydroxy-4-propyl-4H-naphth[1,2-b]-1, 4-oxazine
    Patent number: 4758661
    Abstract: (+)-trans-1a,2,3,4a,5,6-Hexahydro-9-hydroxy-4-propyl-4H-naphth[1,2-b]-1,4-o xazine is elaborated by a series of process steps that retain the enantiomeric purity of the starting material, D-aspartic acid. The product is a direct acting dopaminergic agent, useful in the treatment of Parkinson's disease.
    Type: Grant
    Filed: June 24, 1986
    Date of Patent: July 19, 1988
    Assignee: Merck & Co., Inc.
    Inventors: David G. Melillo, David J. Mathre, Robert D. Larsen
  • Substituted thieno[2,3-b]pyrrole-5-sulfonamides as antiglaucoma agents
    Patent number: 4751231
    Abstract: Thieno[2,3-b]pyrrole-5-sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma.
    Type: Grant
    Filed: September 16, 1987
    Date of Patent: June 14, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Wasyl Halczenko, George D. Hartman
  • Diastereocontrolled synthesis of 2-amino alcohols
    Patent number: 4743694
    Abstract: The addition of organolithium to dimethylhydrazones of certain ethers of a-hydroxyaldehydes results in the synthesis of threo- or erythro- intermediates readily convertible to threo- or erythro-2-amino alcohols.
    Type: Grant
    Filed: April 11, 1986
    Date of Patent: May 10, 1988
    Assignee: Mercek & Co., Inc.
    Inventor: David A. Claremon
  • Thienopyridine sulfonamides and their ophthalmological formulation
    Patent number: 4731368
    Abstract: Thienopyridine sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and disorders associated therewith such as glaucoma.
    Type: Grant
    Filed: December 8, 1986
    Date of Patent: March 15, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Jacob M. Hoffman, Jr., Kenneth L. Shepard
  • Biosoluble ocular insert
    Patent number: 4730013
    Abstract: Ocular inserts with or without pharmacologically active agents comprising low molecular weight polymers have a lower propensity to cause blurred vision compared with inserts prepared from high molecular weight hydroxypropyl cellulose. When an enteric coating material is included as a constituent of the matrix there is provided a means for controlling and predicting dissolution rates of the insert to yield a prolonged residence time.
    Type: Grant
    Filed: March 2, 1987
    Date of Patent: March 8, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Joseph V. Bondi, Richard J. Harwood
  • Substituted thiophene-2-sulfonamide antiglaucoma agents
    Patent number: 4721794
    Abstract: Thiophene-2-sulfonamides with a 5-alkyl-S(O).sub.n -substituent are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
    Type: Grant
    Filed: July 30, 1986
    Date of Patent: January 26, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Shepard, Samuel L. Graham
  • Anti-depressant spiro hexahydro arylquinolizine derivatives, composition, and method of use therefor
    Patent number: 4710504
    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: April 4, 1986
    Date of Patent: December 1, 1987
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Joel R. Huff, Joseph P. Vacca, Steven D. Young, Jane deSolms, James P. Guare, Jr.
  • Substituted pyranone inhibitors of cholesterol synthesis
    Patent number: 4710513
    Abstract: 6-Phenyl-, phenylalkyl- and phenylethenyl-4-hydroxytetrahydropyran-2-ones in the 4(R)-trans stereoisomeric forms are potent inhibitors of cholesterol synthesis by virtue of their ability to inhibit the enzyme, 3-hydroxy-3-methylglutaryl-coenzyme A reductase.
    Type: Grant
    Filed: March 14, 1984
    Date of Patent: December 1, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Alvin K. Willard, Frederick C. Novello, William F. Hoffman, Edward J. Cragoe, Jr.
  • Substituted hexahydro arylquinolizines as .alpha..sub.2 blockers
    Patent number: 4690928
    Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.6 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, antidiabetics, antiobesity and platelet aggregation inhibitors.
    Type: Grant
    Filed: July 14, 1986
    Date of Patent: September 1, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Joel R. Huff, Joseph P. Vacca, John J. Baldwin
  • Substituted benzo[b]furo- and benzo[b]thieno quinolizines
    Patent number: 4686226
    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, antiobesity and platelet aggregation inhibitors and modifiers of gastrointestinal motility.
    Type: Grant
    Filed: September 3, 1985
    Date of Patent: August 11, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Joel R. Huff, John J. Baldwin, Yojiro Sakurai, Joseph P. Vacca, James P. Guare, Jr.
  • 3-O-benzyl-2,4,6-tridooxy-6-iodo-alpha-D-erythro-hexopyranide useful for preparing inhibitors of 3-hydroxy-3-methylglutaryl coenzyme a reductase
    Patent number: 4683314
    Abstract: Totally synthetic analogs of the known inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase, compactin and mevinolin, are prepared from a chiral synthon derived from D-glucose which has the same chirality as the natural products.
    Type: Grant
    Filed: April 28, 1986
    Date of Patent: July 28, 1987
    Assignee: Merck & Co., Inc.
    Inventor: John D. Prugh
  • Analogs of substance P and eledoisin
    Patent number: 4680283
    Abstract: Analogs of substance P and eledoisin which are conformationally constrained by the presence of a lactam in the peptide chain demonstrate greater selectivity and increased protease stability and are useful as analgesic, anti-inflammatory, antihypertensive, central nervous system agents, and stimulants of lachrymal secretion. The compounds are prepared by standard peptide synthetic procedures.
    Type: Grant
    Filed: August 20, 1986
    Date of Patent: July 14, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Daniel F. Veber, Roger Freidinger