Patents Represented by Attorney William H. Nicholson

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  • Ophthalmic compositions of carbonic anhydrase inhibitors for topical application in the treatment of elevated intraocular pressure
    Patent number: 4438123
    Abstract: Although dibasic carbonic anhydrase inhibitors (C.A.I.) can be administered systemically by oral or intravenous routes, attempts to administer them topically were inadvisable because of their elevated pH. The mono-alkali metal salts in the treatment of intraocular hypertension especially the sodium and potassium salts, of dibasic salt-forming C.A.I. are as effective in lowering intraocular pressure as dialkali metal salts of dibasic C.A.I. while having a pH more in harmony with ocular pH. They are found particularly useful when administered in conjunction with an ophthalmologically acceptable water-soluble polymer such as hydroxypropylcellulose in an aqueous carrier.
    Type: Grant
    Filed: December 22, 1981
    Date of Patent: March 20, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Robert L. Smith
  • Hypocholesterolemic fermentation products and process of preparation
    Patent number: 4432996
    Abstract: Substances isolated after cultivation of a micoorganism belonging to the genus Penicillium in a culture medium comprises compounds which have strucures: ##STR1## Together with salts and esters of the carboxylic acid, these compounds form a class of highly active hypocholesterolemic and hypolipemic medicaments.
    Type: Grant
    Filed: May 17, 1982
    Date of Patent: February 21, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Vincent P. Gullo, Tony Y. K. Lam, Richard L. Monaghan
  • Method of use of enantiomers of trans-indeno[1,2-b]-1,4-oxazines
    Patent number: 4431647
    Abstract: The (R,R)-enantiomers of trans-indeno[1,2-b]-1,4-oxazines demonstrate dopaminergic activity, whereas the (S,S)-enantiomers demonstrate .alpha.-adrenergic antagonist activity. They are prepared by cyclization of the appropriate chiral 2-amino-1-hydroxyindane.
    Type: Grant
    Filed: August 2, 1982
    Date of Patent: February 14, 1984
    Assignee: Merck & Co., Inc.
    Inventor: David E. McClure
  • 5-Benzothiazolesulfonamide derivatives for the topical treatment of elevated intraocular pressure
    Patent number: 4426388
    Abstract: Novel carboxylic acid esters of 5-hydroxy-2-benzothiazolesulfonamide are shown to be 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: April 2, 1982
    Date of Patent: January 17, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Otto W. Woltersdorf, Jr.
  • Treatment of giardiasis and trichomoniasis
    Patent number: 4424220
    Abstract: Fluorouracil and emimycin are useful in the treatment of giardiasis and trichomoniasis.
    Type: Grant
    Filed: September 22, 1982
    Date of Patent: January 3, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Ching C. Wang
  • Hexahydronaphth[1,2-b]-1,4-oxazines
    Patent number: 4420480
    Abstract: Hexahydronaphth[1,2-b]-1,4-oxazines have dopaminergic activity and display .alpha..sub.2 -adrenergic receptor antagonism. They are useful in the treatment of parkinsonism, depression and hypertension. An important method of preparation is by ring closure of the appropriate 2-chloroacetamidotetrahydronaphthalen-1-ol and reduction of the resulting cyclic amide carbonyl group.
    Type: Grant
    Filed: August 30, 1982
    Date of Patent: December 13, 1983
    Assignee: Merck & Co., Inc.
    Inventor: James H. Jones
  • Benzothiazolesulfonamide derivatives for the topical treatment of elevated intraocular pressure
    Patent number: 4416890
    Abstract: Novel carboxylic acid esters of 6-hydroxy-2-benzothiazolesulfonamide are shown to be 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: May 21, 1982
    Date of Patent: November 22, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Otto W. Woltersdorf, Jr.
  • Dibenzo[a,d]cycloocten-5,12-imines
    Patent number: 4414154
    Abstract: Dibenzo[a,d]cycloocten-5,12-(and 6,12)-imines, derivatives and pharmaceutically acceptable salts thereof are useful as anxiolytics, antidepressants, anticonvulsants, muscle relaxants and in the treatment of mixed anxiety-depression, minimal brain dysfunction and extrapyramidal disorders such as Parkinson's disease.
    Type: Grant
    Filed: October 22, 1981
    Date of Patent: November 8, 1983
    Assignee: Merck & Co. Inc.
    Inventors: Paul S. Anderson, Marcia E. Christy, Ben E. Evans, David C. Remy
  • Anti-emetic esters of cyproheptadine-3-carboxylic acid and structurally related compounds
    Patent number: 4412999
    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 migrane 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: April 14, 1982
    Date of Patent: November 1, 1983
    Assignee: Merck & Co., Inc.
    Inventors: David C. Remy, Bradley V. Clineschmidt
  • Ophthalmic formulations of 5-fluoro-2-methyl-1-(p-methylthiobenzylidene)-3-indenylacetic acid
    Patent number: 4402979
    Abstract: This invention relates to ophthalmic preparations which include 5-fluoro-2-methyl-1-(p-methylthiobenzylidene)-3-indenylacetic acid or ophthalmologically acceptable salts thereof as the active entity for reducing or controlling inflammation of the eye.
    Type: Grant
    Filed: October 28, 1981
    Date of Patent: September 6, 1983
    Assignees: Merck & Co., Inc. & Laboratories, Merck, Sharp & Dohme-Chibret
    Inventors: Tsung-Ying Shen, Philippe Conquet, Jean-Claude Le Douarec
  • Treatment of giardiasis and trichomoniasis
    Patent number: 4401671
    Abstract: Fluorouracil and emimycin are useful in the treatment of giardiasis and trichomoniasis.
    Type: Grant
    Filed: February 10, 1982
    Date of Patent: August 30, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Ching C. Wang
  • Allylsulfoxide enzyme inhibitors
    Patent number: 4400395
    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 18, 1982
    Date of Patent: August 23, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Raymond A. Firestone
  • 5-Alkyl or hydroxyalkyl substituted-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines and anticonvulsant use thereof
    Patent number: 4399141
    Abstract: 5-Substituted-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines, derivatives and pharmaceutically acceptable salts thereof are useful as anticonvulsants.
    Type: Grant
    Filed: June 12, 1981
    Date of Patent: August 16, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Paul Anderson, Marcia E. Christy, Ben E. Evans
  • Treatment of gray matter edema
    Patent number: 4394385
    Abstract: The invention relates to the treatment of gray matter edema in the brain or spinal chord by the administration of benzofuranyloxyacetic acids, indeno[5,4-b]furancarboxylic acids, their analogs and salts thereof.
    Type: Grant
    Filed: January 29, 1982
    Date of Patent: July 19, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Edward J. Cragoe, Jr.
  • Treatment of gray matter edema
    Patent number: 4389417
    Abstract: The invention relates to the treatment of gray matter edema in the brain or spinal chord by the administration of (indanyloxy)acetic acids, and analogs and salts thereof.
    Type: Grant
    Filed: December 30, 1981
    Date of Patent: June 21, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Robert S. Bourke, Edward J. Cragoe, Jr.
  • Allylsulfoxide enzyme inhibitors
    Patent number: 4388475
    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 7, 1980
    Date of Patent: June 14, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Raymond A. Firestone
  • Phenyl hydroxypropyl sulfoxide enzyme inhibitors
    Patent number: 4388326
    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 7, 1980
    Date of Patent: June 14, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Raymond A. Firestone
  • Hypocholesterolemic fermentation products and process of preparation
    Patent number: 4387242
    Abstract: Substances isolated after cultivation of a microorganism belonging to the genus Aspergillus in a culture medium include a compound with structural formula: ##STR1## Together with the corresponding free acid of the above ester, its salts and lactone, compound I is a member of a class of hypocholesterolemic and hypolipemic medicaments.
    Type: Grant
    Filed: August 21, 1981
    Date of Patent: June 7, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Tony Y. K. Lam
  • 6-Hydroxy-2-benzothiazolesulfonamide for the topical treatment of elevated intraocular pressure
    Patent number: 4386098
    Abstract: 6-Hydroxy-2-benzothiazolesulfonamide is useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions including drops and inserts are disclosed.
    Type: Grant
    Filed: November 3, 1981
    Date of Patent: May 31, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Otto Woltersdorf, Jr., Stuart R. Michelson, John M. Sondey, Harvey Schwam
  • Process for preparation of 9-(dihalobenzyl)adenines
    Patent number: RE31429
    Abstract: 9-(Dihalobenzyl)adenines are prepared uncontaminated with other positional isomers in a series of mild transformations starting from 4,5,6-triaminopyrimidine and proceeding via 7-(N-formyl-N-dihalobenzyl)amino[1,2,5]-thiadiazolo[3,4-d]pyrimidine. The resulting compounds have anticoccidial activity and are useful in controlling cecal and/or intestinal coccidiosis when administered in minor quantities to animals, in particular to poultry usually in admixture with animal sustenance.
    Type: Grant
    Filed: October 23, 1979
    Date of Patent: October 25, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Robert Tull, deceased, George D. Hartman, Leonard M. Weinstock