Abstract: An improved method for the topical administration of systemically or locally active drugs utilizes a bandage containing one or more layers including a drug useful in the treatment of disease and a heat-generating substance, each dispersed intimately throughout said bandage layers.
Abstract: This invention relates to novel interphenylene 9-thia-11-oxo-12-azaprostanoic acid compounds, salts, and derivatives thereof. These compounds are exceptionally potent renal vasodilators and antihypertensives which are active when administered orally but which have a more specific type of biological activity than that of many of the natural prostaglandins and their synthetic analogs or derivatives.
Type:
Grant
Filed:
August 30, 1978
Date of Patent:
September 30, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Ta-jyh Lee, John B. Bicking
Abstract: A rigid blister package includes a rigid thermoformed plastic cover piece and a flexible backing sheet, a score line for opening said package, and a slide fastener for reclosing the blister package, along with stops to hold the slide fastener in the open or closed position.
Type:
Grant
Filed:
November 16, 1978
Date of Patent:
September 23, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Arthur Jaeger, Richard Gunderlock, Richard J. Harwood
Abstract: This invention relates to an apparatus for slicing cylindrically shaped columns of gels. More particularly, it relates to an apparatus for firmly holding cylindrical columns of acrylamide gel while making a longitudinal slice through the entire length of the column.
Type:
Grant
Filed:
November 13, 1978
Date of Patent:
March 25, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Edward C. O'Rourke, W. Wardle Fullerton
Abstract: This invention relates to a novel diagnostic kit for use in radiographic bone scanning. More particularly, it relates to a kit comprising ingredients employed in the preparation of an intravenous injection of a complex of Technetium-99m, stannous ion, and an organic phosphonate identified as triethylene tetramine hexa (methylene phosphonic acid).
Type:
Grant
Filed:
October 3, 1977
Date of Patent:
February 5, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Richard E. Rolleston, Jacques A. Nadeau
Abstract: Novel interphenylene derivatives of 11,12-secoprostaglandins are prepared by the stepwise alkylation of the ethyl ester or the t-butyl ester of acetoacetic acid. One such method involves treatment of the t-butyl ester of acetoacetic acid with a strong base to form the anion followed by treatment with ethyl p-(3-bromopropyl)benzoate to produce ethyl 4-(4-tert-butoxycarbonyl-5-oxo-hexyl)benzoate, subsequently reacting the anion of the thus-formed benzoate with 1-chloro-4-acetoxynonane to produce ethyl 4-(4-acetyl-4-tert-butoxycarbonyl-8-acetoxytridecyl)benzoate followed by decarboxylation and alkaline hydrolysis to produce the desired product 4-(4-acetyl-8-hydroxytridecyl)benzoic acid which is useful as a pharmaceutical in the treatment of patients with renal failure and in the prevention of transplant rejection.
Abstract: Invention relates to improved processes for preparing 5-fluoro-2-methyl-1-(p-methylsulfinylbenzylidene)-indenyl-3-acetic acid, to intermediates thereof, and to the preparation of said intermediates.
Abstract: This invention relates to 9-thia- , 9-oxothia, and 9-dioxothia-11,12-seco-prostaglandins and processes for their manufacture. These compounds have prostaglandin-like biological activity and are particularly useful for the treatment of skin diseases such as psoriasis, for the prevention of thrombus formation, in stimulating the production of growth hormone in intact animals, and as regulators of the immune response.
Type:
Grant
Filed:
October 25, 1977
Date of Patent:
May 22, 1979
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., John B. Bicking, Robert L. Smith
Abstract: Novel interphenylene derivatives of 11,12-secoprostaglandins are prepared by the stepwise alkylation of the ethyl ester or the t-butyl ester of acetoacetic acid. One such method involves treatment of the t-butyl ester of acetoacetic acid with a strong base to form the anion followed by treatment with ethyl p-(3-bromopropyl)benzoate to produce ethyl 4-(4-tert-butoxycarbonyl-5-oxo-hexyl)benzoate, subsequently reacting the anion of the thus-formed benzoate with 1-chloro-4-acetoxynonane to produce ethyl 4-(4-acetyl-4-tert-butoxycarbonyl-8-acetoxytridecyl)benzoate followed by decarboxylation and alkaline hydrolysis to produce the desired product 4-(4-acetyl-8-hydroxytridecyl)benzoic acid which is useful as pharmaceutical in the treatment of patients with renal failure and in the prevention of transplant rejection.
Abstract: Novel interphenylene derivatives of 11,12-secoprostaglandins are prepared by the stepwise alkylation of the ethyl ester or the t-butyl ester of acetoacetic acid. One such method involves treatment of the t-butyl ester of acetoacetic acid with a strong base to form the anion followed by treatment with ethyl p-(3-bromopropyl)benzoate to produce ethyl 4-(4-tert-butoxycarbonyl-5-oxo-hexyl)benzoate, subsequently reacting the anion of the thus-formed benzoate with 1-chloro-4-acetoxynonane to produce ethyl 4-(4-acetyl-4-tert-butoxycarbonyl-8-acetoxytridecyl)benzoate followed by decarboxylation and alkaline hydrolysis to produce the desired product 4-(4-acetyl-8-hydroxytridecyl)benzoic acid which is useful as a pharmaceutical in the treatment of patients with renal failure and in the prevention of transplant rejection.
Abstract: This invention relates to 9-thia-, 9-oxothia, and 9-dioxothia-11,12-seco-prostaglandins and processes for their manufacture. These compounds have prostaglandin-like biological activity and are particularly useful for the treatment of skin diseases such as psoriasis, for the prevention of thrombus formation, in stimulating the production of growth hormone in intact animals, and as regulators of the immune response.
Type:
Grant
Filed:
October 25, 1977
Date of Patent:
December 5, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., John B. Bicking, Robert L. Smith
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.
Abstract: Invention relates to improved processes for preparing 5-fluoro-2-methyl-1-(p-methylsulfinylbenzylidene)-indenyl-3-acetic acid, to intermediates thereof, and to the preparation of said intermediates.
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.
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.
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
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:
May 30, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., John B. Bicking, Robert L. Smith
Abstract: This invention relates to 8-aza-9-ozo(and dioxo)-thia-11,12-secoprostaglandins and processes for their manufacture. These compounds have prostaglandin-like biological activity and are particularly useful as renal vasodilators, for the prevention of thrombus formation, to induce growth hormone release, and as regulators of the immune response.
Abstract: New substituted indenyl methyl sulfonic acids and derivatives thereof which have anti-inflammatory, antipyretic and analgesic activity. Also included are methods of preparing said indenyl compounds, pharmaceutical compositions having said indenyl compounds as an active ingredient and methods of treating inflammation by administration of said indenyl compounds.
Abstract: Novel 8-aza-9-dioxothiaprostanoic acid compounds, their salts, and derivatives, are prepared from ethyl 7-(3-hydroxymethyl-2-isothiazolidinyl)-5-heptynoate S,S-dioxide by first hydrogenating the triple bond over a Lindlar catalyst, followed by mild oxidation, to produce the corresponding 3-formyl compound, which is condensed with the ylide prepared from dimethyl-(2-oxoheptyl)phosphonate to produce the .alpha.,.beta.-unsaturated ketone, followed by reduction to the corresponding carbinol, and ester hydrolysis. The compounds are useful especially for the treatment of patients with poorly functioning kidneys, as hypotensives, or as platelet aggregation inhibitors.
Type:
Grant
Filed:
February 17, 1977
Date of Patent:
May 2, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., James H. Jones, John B. Bicking