Patents Represented by Attorney Mario A. Monaco

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  • 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
  • Cyclic hexapeptide somatostatin analogs
    Patent number: 4486415
    Abstract: Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven of the ring amino acids of somatostatin. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method.
    Type: Grant
    Filed: August 15, 1983
    Date of Patent: December 4, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Roger Freidinger
  • N-Terminal substituted oligopeptide converting enzyme inhibitors
    Patent number: 4483850
    Abstract: N-Terminal substituted oligopeptides are disclosed. The compounds are angiotensin converting enzyme inhibitors useful as antihypertensives.
    Type: Grant
    Filed: February 18, 1983
    Date of Patent: November 20, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Arthur A. Patchett, William V. Ruyle
  • Isoefrotomycin, process of preparation, pharmaceutical composition and method of using same
    Patent number: 4482545
    Abstract: There is disclosed the novel compound isoefrotomycin which is synthesized from efrotomycin as a Michael adduct by treatment with a mixture of polar and nonpolar solvents. Isoefrotomycin is an effective antimicrobial agent and growth promotant in animals.
    Type: Grant
    Filed: October 13, 1983
    Date of Patent: November 13, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Richard J. Bochis, Ray S. Dewey
  • Pyrazine aldimine compounds as antimicrobial agents
    Patent number: 4479953
    Abstract: The instant invention is directed to a pyrazine compound represented by the formula ##STR1## wherein Z is --NH--, --NHSO.sub.2 --, --NHCO-- or --S--,Ar is a phenyl ring substituted by 1 or 2 substituents selected from the group consisting of halo, lower alkyl, lower alkoxy or nitro, andn is 0 or 1.
    Type: Grant
    Filed: August 25, 1983
    Date of Patent: October 30, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Arthur J. Friedman
  • Acyloxy derivatives of [phenylsulfonyl(or sulfinyl)]thiophenesulfonamide for the topical treatment of elevated intraocular pressure
    Patent number: 4477466
    Abstract: Novel acyloxy derivatives of [phenylsulfonyl(or sulfinyl)]thiophenesulfonamides 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: October 16, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Kenneth L. Shepard
  • Medicament container and transfer device
    Patent number: 4475914
    Abstract: The application discloses a combination medicament container and transfer device connected with a bellows type sleeve. The transfer device is a double ended spike having internal conduits optionally vented through a sterile hydropholic allowing two way transfer of liquid from an intravenous solution container and a medicament container of relatively insoluble medicament.
    Type: Grant
    Filed: August 30, 1982
    Date of Patent: October 9, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Joel B. Portnoff
  • Antihypertensive composition
    Patent number: 4472384
    Abstract: A pharmaceutical composition is disclosed which comprises the combination of interphenylene 9-thia-11-oxo-12-aza prostanoic acid derivatives and carboxyalkyl dipeptide derivatives.
    Type: Grant
    Filed: June 15, 1983
    Date of Patent: September 18, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Edward H. Blaine, Charles S. Sweet
  • Treatment of brain injury due to gray matter edema with (indanyloxy) butanoic acids
    Patent number: 4465850
    Abstract: The invention relates to the treatment and prevention of injury to the gray matter of the brain and to the spinal chord due to accidents, ischemic stroke, cardiac arrest, arrested breathing, Reye's syndrome and hydrocephalus by the administration of (indanyloxy)butanoic acids, their derivatives, analogs and salts thereof.
    Type: Grant
    Filed: September 30, 1982
    Date of Patent: August 14, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
  • 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.
  • 4a-Substituted avermectin compounds
    Patent number: 4457920
    Abstract: There are disclosed novel avermectin compounds wherein the 4-methyl group is substituted with hydroxy or various groups connected through the hydroxy oxygen atom. The hydroxy compounds are prepared by oxidation of the 4-methyl group and the hydroxy substituents prepared by a substitution process selective for primary alcohols. The compounds have utility as antiparasitic agents and compositions for that use are also disclosed.
    Type: Grant
    Filed: August 4, 1982
    Date of Patent: July 3, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Helmut H. Mrozik
  • 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.
  • N-(Alkenyl)-2-aza-2'-hydroxy-5,6-benzotricyclo[6.3.0.sup.1,8.0.sup.4,11 ] u n
    Patent number: 4454325
    Abstract: Novel N-(substituted) derivatives of 2-aza-2'-hydroxy-5,6-benzotricyclo[6.3.0.sup.1,8.0.sup.4,11 ] undecane of the formula: ##STR1## are centrally acting analgesics effective in the relief of pain.
    Type: Grant
    Filed: December 27, 1982
    Date of Patent: June 12, 1984
    Assignee: Merck Sharp & Dohme I.A. Corp.
    Inventor: Robert N. Young
  • 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
  • Anti-inflammatory/analgesic combination of .alpha.-fluoromethylhistidine and a selected non-steroidal anti-inflammatory drug (NSAID)
    Patent number: 4447443
    Abstract: Combinations of .alpha.-fluoromethylhistidine and a NSAID have been found to exhibit higher efficacy and shorter onset of action in the treatment of pain and inflammation.
    Type: Grant
    Filed: November 15, 1982
    Date of Patent: May 8, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Marvin M. Goldenberg
  • 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
  • Delivery of adjustable quantities of materials
    Patent number: 4444335
    Abstract: A delivery device and method making use of a plunger which can be controllable reciprocated within a housing to regulate the amount of material expelled from the housing. The plunger includes an adjustable stop collar which can be adjustably positioned, preferably by depressing the sides of the collar. In addition, a piston within the housing is sealably releasable from the plunger.
    Type: Grant
    Filed: September 14, 1981
    Date of Patent: April 24, 1984
    Assignee: Merck & Co., Inc.
    Inventors: William E. Wood, Roy A. Rosen
  • 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.