Patents Represented by Attorney William H. Nicholson

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  • 2-Substituted-3-sulfonamide-pyridine derivatives
    Patent number: 4569999
    Abstract: 2-Substituted-3-sulfonamidepyridine derivatives useful as hypotensives and as alpha and beta adrenergic blocking drugs as well as intermediates in the synthesis of other pharmacologically active pyridines. A process for preparing said derivatives is also described.
    Type: Grant
    Filed: July 2, 1984
    Date of Patent: February 11, 1986
    Assignee: Fabrica de Productos Quimicos y Farmaceuticos Abello, S.A.
    Inventors: M. Carmen G. Gil, Vicente G. Parra, Felix S. Alonso, Tomas T. Cebada
  • Substituted pyranone inhibitors of cholesterol synthesis
    Patent number: 4567289
    Abstract: The methyl, ethyl, n-propy, 2-(acetylamino)ethyl, or 1-(2,3-dihydroxy)propyl ester of E-(3R,5S)-7-(4'-fluoro-3,3',5-trimethyl[1,1'-biphenyl]-2-yl)-3,5-dihydroxy -6-heptenoic acid of structural formula: ##STR1## are HMG-CoA reductase inhibitors useful in the treatment of conditions associated with hypercholesterolemia.
    Type: Grant
    Filed: April 25, 1984
    Date of Patent: January 28, 1986
    Assignee: Merck & Co., Inc.
    Inventors: Alvin K. Willard, Frederick C. Novello, William F. Hoffman, Edward J. Cragoe, Jr.
  • Allylsulfoxide enzyme inhibitors
    Patent number: 4564635
    Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.
    Type: Grant
    Filed: October 23, 1984
    Date of Patent: January 14, 1986
    Assignee: Merck & Co., Inc.
    Inventor: Raymond A. Firestone
  • Process for preparing 5 pyridyl pyridine-2 (1H)-ones
    Patent number: 4563528
    Abstract: 5-Pyridinyl-6-R.sub.2 -3-R.sub.1 -2(1H)-pyridinones (I), where R.sub.2 is hydrogen or lower alkyl and R.sub.1 is a cyano, a carbamoyl or an amino group are prepared: by reaction of 1-R.sub.2 -1-oxo-2-pyridinyl-3-dialkylaminopropane (II) with malonamide under solid-liquid or liquid-liquid phase transfer catalysis conditions to obtain 1,2-dihydro-2-oxo-6-R.sub.2 -5-pyridinylnicotinamide (IV), or by reaction of II with cyanoacetamide under solid-liquid or liquid-liquid phase transfer catalysis conditions to obtain 1,2-dihydro-2-oxo-6-R.sub.2 -5-pyridinylnicotinonitrile (III) and partially hydrolizing III to yield IV; finally the carbamoyl group of IV is converted to amino and 1,2-dihydro-2-oxo-6-R.sub.2 -5-pyridinyl-3-aminopyridin-2-one are obtained.
    Type: Grant
    Filed: April 19, 1984
    Date of Patent: January 7, 1986
    Assignee: Fabrica De Productos Quimicos Y Farmaceuticos Abello, S.A.
    Inventors: Vicente Gomez Parra, Pedro Gonzalez Hernandez, Felix Sanchez Alonso, Tomas Torres Cebada
  • Device for preparing and dispensing a solution
    Patent number: 4559983
    Abstract: The invention relates to a device for preparing and dispensing a solution. A bottle containing a substance to be disolved is closed by a disc-shaped base having a rigid rod thereon and a deformable head. A tube of solvent is closed by an apertured slidable piston. Mixing is effected by placing the piston against the rigid rod and applying axial pressure which dispenses the solvent from the tube, through a capillary channel in the rod and into the bottle. Slots in the rod are revealed during this operation to allow the air to escape from the bottle. The deformable head also serves to pressurize the bottle to permit dispensing therefrom.
    Type: Grant
    Filed: December 21, 1983
    Date of Patent: December 24, 1985
    Assignee: Laboratoires Merck Sharp & Dohme Chibret
    Inventor: Jean-Claude Paoletti
  • Phenyl, trihalomethyl or heteroaryl sulfoxides having a latent allyl group bound to sulfur as enzyme inhibitors
    Patent number: 4558071
    Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.
    Type: Grant
    Filed: February 25, 1983
    Date of Patent: December 10, 1985
    Assignee: Merck & Co., Inc.
    Inventor: Raymond A. Firestone
  • Ophthalmic use of norfloxacin and related antibiotics
    Patent number: 4551456
    Abstract: Norfloxacin and related antibiotics are useful in the treatment of ocular infections by topical administration.
    Type: Grant
    Filed: November 14, 1983
    Date of Patent: November 5, 1985
    Assignee: Merck & Co., Inc.
    Inventor: Irving M. Katz
  • 2-Sulfamoylbenzo[b]furan derivatives for the treatment of elevated intraocular pressure
    Patent number: 4544667
    Abstract: Novel 2-sulfamoylbenzo[b]furans and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in compositions including opthalmic drops and inserts.
    Type: Grant
    Filed: February 9, 1984
    Date of Patent: October 1, 1985
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Shepard, Samuel L. Graham
  • Process for preparing tricyclic indoles
    Patent number: 4543415
    Abstract: An improved process for preparing 5-keto-1,3,4,5-tetrahydrobenz[c,d]indole and 6(1H)-oxo-3,4,5,6-tetrahydrocyclohept[c,d]indole is disclosed.
    Type: Grant
    Filed: May 19, 1980
    Date of Patent: September 24, 1985
    Assignee: Merck & Co., Inc.
    Inventor: Gerald S. Ponticello
  • 5-[Phenylsulfonyl(or sulfinyl)]thiophene-2-sulfonamides for the topical treatment of elevated intraocular pressure
    Patent number: 4542152
    Abstract: 5-[Phenylsulfonyl(or sulfinyl)]thiophene-2-sulfonamides are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions including drops and inserts are disclosed.
    Type: Grant
    Filed: June 20, 1983
    Date of Patent: September 17, 1985
    Assignee: Merck & Co., Inc.
    Inventor: Kenneth L. Shepard
  • Choline oxidase inhibitor
    Patent number: 4540575
    Abstract: New fermentation products useful in the treatment of tardive dyskinesia by inhibition of choline oxidase are produced by fermentation of a nutrient medium with a microorganism, Streptomyces hygroscopicus.
    Type: Grant
    Filed: May 6, 1983
    Date of Patent: September 10, 1985
    Assignee: Merck & Co., Inc.
    Inventors: Richard L. Monaghan, Yu-Lin Kong
  • Anti-emetic esters of cyproheptadine-3-carboxylic acid and structurally related compounds
    Patent number: 4522821
    Abstract: Certain esters of cyproheptadine-3-carboxylic acid and its bioisosteres are peripherally selective dopamine antagonists useful in the treatment of emesis caused by stimulation of dopamine receptors of the chemoreceptor trigger zone, as well as emesis and nausea resulting from other causes including post operative emesis, chronic pediatric vomiting, radiotherapy and chemotherapy induced emesis, and nausea associated with migraine attacks and dysmenorrhea or arising idiopathically.They are also useful in the treatment of gastrointestinal disorders, such as gastro-oesophageal reflux caused by stimulation of dopamine receptors in the stomach or other causes and dyspepsia arising from delayed gastric emptying, post prandial dyspepsia or dyspepsia of unknown etiology.
    Type: Grant
    Filed: August 8, 1983
    Date of Patent: June 11, 1985
    Assignee: Merck & Co., Inc.
    Inventors: David C. Remy, Bradley V. Clineschmidt
  • 6(or 5)-Hydroxybenzothiazole-2-sulfonamide-O-sulfate salts for the topical treatment of elevated intraocular pressure
    Patent number: 4510155
    Abstract: Novel O-sulfates of 6(or 5)-hydroxy-2-benzothiazolesulfonamide are useful for the topical treatment of elevated intraocular pressure. Opthalmic compositions include drops and inserts.
    Type: Grant
    Filed: June 2, 1983
    Date of Patent: April 9, 1985
    Assignee: Merck & Co., Inc.
    Inventors: Robert L. Smith, Samuel L. Graham
  • 4-[2-Pyridinylthio(oxy or amino)methyl]-1H-imidazoles and derivatives
    Patent number: 4505918
    Abstract: 4-[2-Pyridinylthio(oxy or amino)methyl]-1H-imidazoles and derivatives and acid addition salts thereof are selective central-adrenergic receptor agonists and thereby useful as antihypertensives.
    Type: Grant
    Filed: November 8, 1982
    Date of Patent: March 19, 1985
    Assignee: Merck & Co., Inc.
    Inventors: Joel R. Huff, Walfred S. Saari, John J. Baldwin
  • 2-[2-Pyridinyloxy(thio or amino)methyl]-1H-imidazoles and derivatives
    Patent number: 4506074
    Abstract: 2-[2-Pyridinyloxy(thio or amino)methyl]-1H-imidazoles and derivatives and acid addition salts thereof generally are selective .alpha..sub.2 -adrenergic receptor antagonists and .alpha..sub.1 -adrenergic receptor agonists and thereby useful as antidepressants and nasal decongestants.
    Type: Grant
    Filed: November 8, 1982
    Date of Patent: March 19, 1985
    Assignee: Merck & Co., Inc.
    Inventors: Joel R. Huff, Walfred S. Saari, John J. Baldwin
  • Ethers of hydroxybenzothiazole-2-sulfonamide for the topical treatment of elevated intraocular pressure
    Patent number: 4505923
    Abstract: Novel ethers of hydroxy-2-benzothiazolesulfonamide are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions include drops and inserts.
    Type: Grant
    Filed: October 31, 1983
    Date of Patent: March 19, 1985
    Assignee: Merck & Co., Inc.
    Inventors: Jacob M. Hoffman, Jr., Otto W. Woltersdorf, Jr.
  • Peripherally selective dopamine antagonists in the treatment of ocular hypertension
    Patent number: 4501749
    Abstract: Peripherally selective dopamine antagonists are useful in the treatment of ocular hypertension when administered topically to the eye.
    Type: Grant
    Filed: October 31, 1983
    Date of Patent: February 26, 1985
    Assignee: Merck & Co., Inc.
    Inventor: Bradley V. Clineschmidt
  • Benzothiazolesulfonamide derivatives for the topical treatment of elevated intraocular pressure
    Patent number: 4500538
    Abstract: Novel carbonates 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: March 14, 1983
    Date of Patent: February 19, 1985
    Assignee: Merck & Co., Inc.
    Inventor: Otto W. Woltersdorf
  • Benzothiazole-2-sulfonamide derivatives for the topical treatment of elevated intraocular pressure
    Patent number: 4499103
    Abstract: Novel 2-benzothiazolesulfonamides are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions including drops and inserts are also disclosed, as well as methods for preparing the novel compounds.
    Type: Grant
    Filed: March 17, 1983
    Date of Patent: February 12, 1985
    Assignee: Merck & Co., Inc.
    Inventor: S. Jane de Solms
  • Allylsulfoxide enzyme inhibitors
    Patent number: 4491590
    Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.
    Type: Grant
    Filed: May 26, 1983
    Date of Patent: January 1, 1985
    Assignee: Merck & Co., Inc.
    Inventor: Raymond A. Firestone