Patents Represented by Attorney William H. Nicholson

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  • Process for 4a'(R),5'-dihydromevinolin
    Patent number: 4490546
    Abstract: Mevinolin is converted to its 4a',5'-dihydro derivative by a route involving protection of the 3',4'-double bond followed by reduction of the 4a',5'-double bond followed by deprotection of the 3',4'-positions.
    Type: Grant
    Filed: June 20, 1983
    Date of Patent: December 25, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Chan-Hwa Kuo
  • Dopamine .beta.-hydroxylase inhibitors
    Patent number: 4487761
    Abstract: Two fermentation isolates, C.sub.7 H.sub.9 NO.sub.4 and C.sub.6 H.sub.7 NO.sub.3, presumably trihydroxy, methyl-pyridine derivatives, are inhibitors of dopamine .beta.-hydroxylase. These natural product compounds are produced by fermentation of Streptoverticillium hiroshimense and each may prove useful as antihypertensive agents.
    Type: Grant
    Filed: April 5, 1982
    Date of Patent: December 11, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Lucille J. Cole, Leeyan Huang, Jerrold M. Liesch
  • (Hydroxybenzoyl)thiophenesulfonamide and acyl derivatives thereof for the topical treatment of elevated intraocular pressure
    Patent number: 4486444
    Abstract: (Hydroxybenzoyl)thiophenesulfonamide and acyl derivatives thereof are useful for the topical treatment of elevated intraocular pressure in ophthalmic compositions including drops and inserts.
    Type: Grant
    Filed: June 20, 1983
    Date of Patent: December 4, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Kenneth L. Shepard
  • 8-[2-Imidazolylmethyloxy(thio, or amino)]-imidazo[1,2-a]pyrazines and derivatives for treating hypertension
    Patent number: 4483858
    Abstract: 8-[2-Imidazolylmethyloxy(thio, or amino)]-imidazo[1,2-a]pyrazines and derivatives and acid addition salts thereof are central adrenergic receptor agonists and thereby useful as antihypertensives.
    Type: Grant
    Filed: October 25, 1982
    Date of Patent: November 20, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Walfred S. Saari
  • Process for 5-methyl-10,11-dihydro-5H-dibenzo[a,d]-cyclohepten-5,10-imine
    Patent number: 4477668
    Abstract: (+)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]-cyclohepten-5,10-imine, and its pharmaceutically acceptable salts is useful as an anxiolytic, antidepressant, anticonvulsant, muscle relaxant and in the treatment of mixed anxiety-depression, minimal brain dysfunction and extrapyramidal disorders such as Parkinson's disease. The racemate of the compound is produced by a four-step synthetic process in about 65% yield from 5H-dibenzo[a,d]cyclohepten-5-one.
    Type: Grant
    Filed: September 3, 1982
    Date of Patent: October 16, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Dean R. Bender, Sandor Karady, Theresa Rothauser
  • Benzothiazolesulfonamide derivatives for the topical treatment of elevated intraocular pressure
    Patent number: 4472417
    Abstract: Novel carbamates of 6(or 5)-hydroxy-2- benzothiazolesulfonamide are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions include drops and inserts.
    Type: Grant
    Filed: April 22, 1983
    Date of Patent: September 18, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Otto W. Woltersdorf, Jr.
  • Antihypercholesterolemic compounds
    Patent number: 4472426
    Abstract: Compounds of general structural formula: ##STR1## wherein Q is: ##STR2## or pharmaceutically acceptable salts, C.sub.1-3 alkyl esters or .alpha.-monoglyceride when Q is a dihydroxy acid are useful as antihypercholesterolemic agents for the treatment of atherosclerosis, familial hypercholesterolemia, hyperlipemia and like diseases. They also have useful antifungal activity.
    Type: Grant
    Filed: December 22, 1982
    Date of Patent: September 18, 1984
    Assignee: Merck & Co., Inc.
    Inventors: William F. Hoffman, Ta-Jyh Lee, Robert L. Smith, Alvin K. Willard
  • Benzothiazolesulfonamide derivatives for the topical treatment of elevated intraocular pressure
    Patent number: 4472418
    Abstract: Novel sulfamates of 6(or 5)-hydroxy-2-benzothiazolesulfonamide are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions include drops and inserts.
    Type: Grant
    Filed: April 22, 1983
    Date of Patent: September 18, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Otto W. Woltersdorf, Jr.
  • Benzothiazolesulfonamide derivatives for the topical treatment of elevated intraocular pressure
    Patent number: 4470991
    Abstract: Novel sulfonates of 6(or 5)-hydroxy-2-benzothiazolesulfonamide are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions include drops and inserts.
    Type: Grant
    Filed: April 22, 1983
    Date of Patent: September 11, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Otto W. Woltersdorf, Jr.
  • Compensating container, notably for pharmaceutical products
    Patent number: 4460090
    Abstract: The present invention relates to a container which is notably intended to hold pills, and it comprises on the one hand an external, rigid envelope 10 and on the other hand an internal envelope 11 enclosing the pills, this internal envelope being elastically deformable and capable of an increase in volume which is sufficient for absorbing the surplus pressure resulting from the packing of the pills when the lid is applied, without crushing the pills.In a first embodiment, the internal envelope 11 is cylindrical and it has a convex, deformable base 12.In a second embodiment, the internal envelope is a sleeve provided with at least one slit allowing its radial expansion.
    Type: Grant
    Filed: July 12, 1982
    Date of Patent: July 17, 1984
    Assignee: Laboratoires Merck Sharp & Dohme - Chibret
    Inventor: Jean-Claude Paoletti
  • Substituted pyranone inhibitors of cholesterol synthesis
    Patent number: 4459422
    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: June 10, 1982
    Date of Patent: July 10, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Alvin K. Willard, Frederick C. Novello, William F. Hoffman, Edward J. Cragoe, Jr.
  • 1-(3-Halo-2-pyridinyl) piperazine
    Patent number: 4456604
    Abstract: 1-(3-Halo-2-pyridinyl)piperazine and its acid addition salts are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressant agents and for treating sedation caused by antihypertensive therapy.
    Type: Grant
    Filed: July 12, 1982
    Date of Patent: June 26, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Walfred S. Saari
  • Benzothiazolesulfonamide derivatives for the topical treatment of elevated intraocular pressure
    Patent number: 4456599
    Abstract: Novel phosphates of 6(or 5)-hydroxy-2-benzothiazolesulfonamide are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions include drops and inserts.
    Type: Grant
    Filed: April 22, 1983
    Date of Patent: June 26, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Otto W. Woltersdorf, Jr.
  • 5-Hydroxy-2-benzothiazolesulfonamide for the topical treatment of elevated intraocular pressure
    Patent number: 4454148
    Abstract: 5-Hydroxy-2-benzothiazolesulfonamide is useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions including drops and inserts are disclosed.
    Type: Grant
    Filed: December 9, 1982
    Date of Patent: June 12, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Otto Woltersdorf, Jr., Harvey Schwam, Stuart R. Michelson, John M. Sondey
  • Antihypercholesterolemic compounds
    Patent number: 4450171
    Abstract: 6(R)-[2-(8'-acyloxy-2'-methyl-6'-methyl (or hydrogen)-polyhydronaphthyl-1')-ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H- pyran-2-ones are prepared by acylation of the corresponding 8'-hydroxy compounds. The products are strong inhibitors of the biosynthesis of cholesterol.
    Type: Grant
    Filed: June 14, 1982
    Date of Patent: May 22, 1984
    Assignee: Merck & Co., Inc.
    Inventors: William F. Hoffman, Robert L. Smith, Alvin K. Willard
  • Antihypercholesterolemic compounds
    Patent number: 4444784
    Abstract: 6(R)-[2-(8'-acyloxy-2'-methyl-6'-methyl (or hydrogen)-polyhydronaphthyl-1')-ethyl]-4 (R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-ones are prepared by acylation of the corresponding 8'-hydroxy compounds. The products are strong inhibitors of the biosynthesis of cholesterol.
    Type: Grant
    Filed: December 18, 1980
    Date of Patent: April 24, 1984
    Assignee: Merck & Co., Inc.
    Inventors: William F. Hoffman, Robert L. Smith, Alvin K. Willard
  • Purification and characterization of a protein fibroblast growth factor
    Patent number: 4444760
    Abstract: Acidic brain fibroblast growth factor isolated from bovine brain, is purified by a particular combination of protein purification techniques. The product is useful in the promotion of cell division (mitogenesis) such as in the promotion of wound healing.
    Type: Grant
    Filed: June 17, 1983
    Date of Patent: April 24, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Kenneth A. Thomas, Jr.
  • Treating sedation with 1-(3-substituted-2-pyridinyl) piperazines
    Patent number: 4442103
    Abstract: 1-(3-Substituted-2-pyridinyl)piperazines and their acid addition salts are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressant agents and for treating sedation caused by antihypertensive therapy.
    Type: Grant
    Filed: September 30, 1982
    Date of Patent: April 10, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Walfred S. Saari
  • Process for preparing inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase via a chiral synthon
    Patent number: 4440927
    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: May 3, 1982
    Date of Patent: April 3, 1984
    Assignee: Merck & Co., Inc.
    Inventor: John D. Prugh
  • Strain of Escherichia coli by bacterial conjugation
    Patent number: 4440748
    Abstract: A new strain of Escherichia coli which is enteropathogenic to both calves and piglets is produced by bacterial conjugation of two parents, one enteropathogenic solely to calves and one enteropathogenic solely to piglets. The new strain is useful in the preparation of a vaccine for use in both calves and piglets to prevent colibacillosis.
    Type: Grant
    Filed: April 3, 1982
    Date of Patent: April 3, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Amy C. Graham