Patents Represented by Attorney Harry E. Westlake, Jr.

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  • Substituted phenoxy-tridecenoic acids/esters
    Patent number: 4126629
    Abstract: This invention relates to aryloxy-, alkoxy-, arylthio-, and alkylthio-11,12-seco-prostaglandins and to processes for their manufacture. These compounds have prostaglandin-like activity and are particularly useful in fertility control such as for estrus synchronization in animals and postcoital contraceptive agents in humans.
    Type: Grant
    Filed: September 9, 1976
    Date of Patent: November 21, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., John B. Bicking
  • Method of preparing magnesium oxide impregnated activated carbon
    Patent number: 4125482
    Abstract: A novel impregnated activated carbon, containing from about 1.0 percent to about 15.0 percent by weight of MgO, has been found to be useful in a method of decolorizing a crude vegetable oil or a degummed vegetable oil, and removing organic acids therefrom, as well as in a process for making a refined edible vegetable oil wherein a crude vegetable oil is degummed, passed through the impregnated activated carbon, and subjected to steam distillation at reduced pressure. A novel method of preparing the MgO impregnated activated carbon has also been discovered.
    Type: Grant
    Filed: March 22, 1977
    Date of Patent: November 14, 1978
    Assignee: Merck & Co., Inc.
    Inventor: Rabindra K. Sinha
  • Novel substituted pyridines, their preparation and pharmaceutical use
    Patent number: 4125618
    Abstract: Novel substituted (3-loweralkylamino-2-R,o-propoxy)pyridines, their pharmaceutically acceptable salts and their preparation are disclosed. These pyridines have pharmaceutical properties such as anti-hypertensive activity of rapid onset.
    Type: Grant
    Filed: March 7, 1977
    Date of Patent: November 14, 1978
    Assignee: Merck & Co., Inc.
    Inventor: John J. Baldwin
  • Trifluoromethylimidazoles and a method for their preparation
    Patent number: 4125530
    Abstract: 4(5)-Trifluoromethylimidazoles having optional substituents in the 1 and 2 positions are provided. The novel 4(5)-trifluoromethylimidazoles are prepared by reacting a 1,1-dihalo-3,3,3-trifluoroacetone compound with an appropriate carboxaldehyde and ammonia. The 4(5)-trifluoromethylimidazoles are useful as anti-gout and anti-hyperuricemic agents.
    Type: Grant
    Filed: February 2, 1977
    Date of Patent: November 14, 1978
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Frederick C. Novello
  • Polynucleotides active as inducers of interferon production in living animal cells
    Patent number: 4124702
    Abstract: Polynucleotides which are multistranded are active as inducers of interferon production in living animal cells. They may be:A. Synthetically complexed polymers of two homopolynucleotides.B. A nucleic acid released by phenol from a ribonucleic acid complex elaborated by the growth of Penicillium funiculosum.C. A ribonucleic acid from reovirus type 3 virions.D. Replicative forms of nucleic acids.
    Type: Grant
    Filed: December 14, 1976
    Date of Patent: November 7, 1978
    Assignee: Merck & Co., Inc.
    Inventors: George P. Lampson, Alfred A. Tytell, Arthur K. Field, Maurice R. Hilleman
  • Method of microencapsulation
    Patent number: 4123382
    Abstract: Solids are added to a suspension of heat softened ethylcellulose capsules and are then encapsulated within the soft capsule. Cooling permits recovery of the desired encapsulated product.
    Type: Grant
    Filed: May 25, 1973
    Date of Patent: October 31, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Lewis D. Morse, William G. Walker, Paul A. Hammes
  • Novel N-carboxy-alpha-amino acid anhydrides
    Patent number: 4120971
    Abstract: N-carboxyanhydrides of hydroxyphenylalanines are disclosed. The compounds have antihypertensive activity.
    Type: Grant
    Filed: March 1, 1977
    Date of Patent: October 17, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Walfred S. Saari, Joel R. Huff
  • Certain quaternary ammonium-3-cyanopyridines
    Patent number: 4119630
    Abstract: Novel cyano substituted (3-loweralkylamino-2-acyl-O-propoxy)pyridines, their pharmaceutically acceptable salts and their preparation are disclosed. The pyridines are vasodilators having antihypertensive activity of rapid onset and extended duration and reduced tendency to cause undesirable tachychardia; they are also .beta.-adrenergic blocking agents.
    Type: Grant
    Filed: July 20, 1977
    Date of Patent: October 10, 1978
    Assignee: Merck & Co., Inc.
    Inventor: John J. Baldwin
  • 3-Amino-2-oxy-propoxy-substituted isothiazoles
    Patent number: 4119718
    Abstract: Isothiazoles having a 3-amino-2-acycloxy-propoxy or a 3-amino-2-hydroxy-propoxy substituent and 2-(3-amino-2-hydroxypropyl) isothiazole-3-ones are disclosed. These compounds have .beta.-adrenergic blocking activity.
    Type: Grant
    Filed: May 2, 1977
    Date of Patent: October 10, 1978
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello
  • Substituted (3-loweralkylamino-2-r.sub.1 o-propoxy)pyridines, their preparation and use
    Patent number: 4119721
    Abstract: Novel cyano substituted (3-loweralkylamino-2-acyl-O-propoxy)pyridines, their pharmaceutically acceptable salts and their preparation are disclosed. The pyridines are vasodilators having antihypertensive activity of rapid onset and extended duration and reduced tendency to cause undesirable tachychardia; they are also .beta.-adrenergic blocking agents.
    Type: Grant
    Filed: March 7, 1977
    Date of Patent: October 10, 1978
    Assignee: Merck & Co., Inc.
    Inventor: John J. Baldwin
  • Somatostatin analogs
    Patent number: 4115554
    Abstract: Somatostatin analogs having the structural formula: ##STR1## wherein R is H, COOH,A is (Asn).sub.n, .alpha.-Abu, Pro, Ala wherein n = 0 or 1,B is Phe, Tyr,C and D are independently Thr, Val,E is Ser, Pro, Ala, Gly,Wherein at least one of A and E is Pro and the ring formed by the peptide backbone contains 35 to 38 atoms and pharmaceutically acceptable non-toxic acid addition salts thereof are prepared by the solid phase method. These peptides have the property of inhibiting the release of insulin, glucagon and growth hormone and decreasing gastric secretion in humans and animals. The compounds are particularly useful in the treatment of diabetes and gastric ulcers.
    Type: Grant
    Filed: August 29, 1977
    Date of Patent: September 19, 1978
    Assignee: Merck & Co., Inc.
    Inventor: Daniel F. Veber
  • Pyrrolo[2,1-b] [3]benzazepines useful for producing a skeletal muscle relaxing or tranquilizing effect
    Patent number: 4112112
    Abstract: 11-Aminopropylidene-Pyrrolo[2,1-b] [3]benzazepines are disclosed to have pharmaceutical utility as skeletal muscle relaxants and tranquilizers. They are prepared by a Grignard reaction on pyrrolo[2,1-b] [3]benzazapin-11-ones followed by dehydration, or by a Wittig reaction on the same ketones.
    Type: Grant
    Filed: June 6, 1977
    Date of Patent: September 5, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Clarence Stanley Rooney, Joshua Rokach, Joseph George Atkinson
  • Interphenylene 8-aza-9-dioxothia-11,12-secoprostaglandins
    Patent number: 4112236
    Abstract: Interphenylene 8-aza-9-dioxothia-11,12-secoprostaglandins are prepared by the two-stage alkylation of the anion of a lower alkyl sulfonamide, R.sup.1 SO.sub.2 NH.sub.2, using first a compound of the formula: ##STR1## and second, a compound of the formula: ##STR2## The compounds produced have renal vasodilatory activity when administered orally and are therefore useful for treating patients with renal impairment.
    Type: Grant
    Filed: April 4, 1977
    Date of Patent: September 5, 1978
    Assignee: Merck & Co., Inc.
    Inventors: John B. Bicking, Edward J. Cragoe, Jr.
  • Process for the preparation of 4-methylthiazole
    Patent number: 4111948
    Abstract: Process for desulfurization of thiazoles including the removal of the mercapto group from 2-mercaptothiazoles and 2-mercaptobenzothiazoles and their derivatives by the oxidation with oxygen in the presence of an oxidation catalyst.
    Type: Grant
    Filed: November 26, 1976
    Date of Patent: September 5, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Henry S. Kao, William A. Sklarz, Leonard M. Weinstock
  • Process of isolating cyclohexane-free ethylcellulose microcapsules
    Patent number: 4107072
    Abstract: Ethylcellulose walled microcapsules, obtained from cyclohexane medium are heavily solvated with cyclohexane and tend to form lumps even after drying. Displacements of cyclohexane by pentane, hexane, heptane or octane or mixtures thereof during the isolation of the microcapsules gives a dry product which is essentially all discrete dry microcapsules.
    Type: Grant
    Filed: May 25, 1973
    Date of Patent: August 15, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Lewis D. Morse, Melvin J. Boroshok, Roy W. Grabner
  • Inhibition of indoleamine-N-methyl transferase by 2-iminopyridines
    Patent number: 4105769
    Abstract: A method of inhibiting indoleamine-N-methyl transferase comprises the administration to a host of a therapeutically effective amount of 1-alkyl-2-iminopyrrolidines or 1-alkyl-2-iminopyridines or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: January 24, 1977
    Date of Patent: August 8, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Clarence S. Rooney, Joshua Rokach, Edward J. Cragoe, Jr.
  • 3-Lower alkoxycyproheptadines as serotonin inhibitors
    Patent number: 4104398
    Abstract: The levorotatory enantiomers of 3-loweralkoxy-cyproheptadines are potent antiserotonin agents with a lower order of antihistaminic activity and substantially free of any anticholinergic activity. They are prepared by treatment of the levorotatory enantiomer of 3-iodocyproheptadine with an alkali metal lower alkoxide in the presence of copper powder.
    Type: Grant
    Filed: August 12, 1976
    Date of Patent: August 1, 1978
    Assignee: Merck & Co., Inc.
    Inventor: David C. Remy
  • Cardiotonic agent
    Patent number: 4103004
    Abstract: A novel peptide designated anthopleurin-C, hereinafter also referred to as AP-C, obtained from the sea anemone Anthopleura elegantissima is found to possess cardiotonic activity.
    Type: Grant
    Filed: August 29, 1977
    Date of Patent: July 25, 1978
    Assignee: University of Hawaii
    Inventors: Ted R. Norton, Midori Kashiwagi, Shoji Shibata
  • 3-Thiazolidinyl heptanoic acids
    Patent number: 4102888
    Abstract: This invention relates to novel 8-aza-9-oxo-11-thia-, -11-oxothia-, and -11-dioxothia-prostanoic acid compounds, salts, and derivatives thereof and also to processes for the preparation of such compounds. These compounds have prostaglandin-like biological activity and are particularly useful as renal vasodilators, for the treatment of certain autoimmune diseases, and in preventing thrombus formation.
    Type: Grant
    Filed: April 20, 1977
    Date of Patent: July 25, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Robert L. Smith, Ta-Jyh Lee, Edward J. Cragoe, Jr.
  • 11,12-Secoprostaglandins
    Patent number: 4097504
    Abstract: This invention relates to 11,12-secoprostaglandins and processes for their manufacture. These compounds have prostaglandin-like biological activity and are particularly useful as renal vasodilators, for the treatment of hypertension, for the prevention of thrombus formation, in preventing gastric secretion, and as regulators of the immune response.
    Type: Grant
    Filed: December 17, 1976
    Date of Patent: June 27, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., John B. Bicking, Robert L. Smith