Abstract: Tricyclicdicarboximides representatively prepared by the Diels-Alder condensation of a cyclic diene such as cycloheptatriene, cyclooctatetraene and the like with a dienophile such as substituted N-phenylmaleimide and the like are disclosed having pharmaceutical utility as minor tranquilizers and anti-convulsants. Also disclosed are processes for the preparation of such tricyclicdicarboximides; pharmaceutical compositions comprising such compounds and their salt, ester and amide derivatives, and methods of treatment comprising administering such compounds and compositions.
Type:
Grant
Filed:
August 12, 1976
Date of Patent:
December 6, 1977
Assignee:
Merck & Co., Inc.
Inventors:
Kenneth L. Shepard, William J. Paleveda, Jr.
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: Resolution of 1-methyl-4-(3-cyano-5H-dibenzo-[a,d]-cyclohepten-5-ylidene)piperidine provides a levorotary isomer (-) having major tranquilizer pharmaceutical utility and a dextrorotary isomer (+) having anticholinergic pharmaceutical utility. Also disclosed are pharmaceutical compositions comprising either isomer substantially free of the other; pharmaceutical compositions comprising preferred ratios of the (+) and (-) isomers; and methods of treatment comprising administering such compounds and compositions.
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, and for the prevention of thrombus formation.
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, and for the prevention of thrombus formation.
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:
May 24, 1976
Date of Patent:
November 22, 1977
Assignee:
Merck & Co., Inc.
Inventors:
Robert L. Smith, Ta-Jyh Lee, Edward J. Cragoe, Jr.
Abstract: Mercaptoalkylpyridines and various derivatives thereof have utility in the treatment of rheumatoid arthritis. The compounds useful in the method of treatment are generally prepared from known pyridine derivatives and, principally, from pyridoxine and related compounds.
Type:
Grant
Filed:
May 11, 1976
Date of Patent:
November 8, 1977
Assignee:
Merck & Co., Inc.
Inventors:
Tsung-Ying Shen, Howard Jones, Dennis M. Mulvey, Conrad P. Dorn
Abstract: Certain novel acyl cyanoguanidines, their preparation, pharmaceutical compositions and novel methods of treating inflammation and autoimmune diseases such as rheumatoid arthritis are disclosed.
Abstract: 11H-Pyrrolo[2,1-b][3]benzazepin-11-one and derivatives thereof are generally prepared by Friedel-Crafts ring closure of a N-styrylpyrrole-2-carboxylic acid derivative. They are useful intermediates in the synthesis of skeletal muscle relaxants and tranquilizers such as 11-(3-dimethylaminopropylidene)-2-cyano-11H-pyrrolo[2,1-b][3]benzazepine.
Type:
Grant
Filed:
June 29, 1976
Date of Patent:
November 1, 1977
Assignee:
Merck & Co., Inc.
Inventors:
Joseph G. Atkinson, Patrice C. Belanger, Clarence S. Rooney, Susan F. Britcher
Abstract: Paper products exhibiting markedly improved dry strength properties are produced by adding to the cellulose paper dispersion a chitin-based compound comprising chitosan alone or a graft copolymer of certain acrylic and/or diallylic monomers grafted onto the chitosan as a substrate.
Type:
Grant
Filed:
July 6, 1971
Date of Patent:
November 1, 1977
Assignee:
Calgon Corporation
Inventors:
Robert Clayton Slagel, Gloria DiMarco Sinkovitz
Abstract: This invention relates to 10-aza-11,12-secoprostaglandins and processes for their manufacture. These compounds have prostaglandin-like biological activity and are particularly useful as renal vasodilators.
Abstract: The invention is concerned with novel 16-aryloxy-, 16-alkoxy-, 16-arylthio- and 16-alkylthio-8-aza-9-dioxothia-11,12-seco-prostaglandins and processes for their preparation. These novel compounds are useful as pharmaceuticals since they can be used in animals for estrus synchronization and treatment of infertility due to persistence of luteal function.
Abstract: Methods of using aqueous hydraulic cement compositions containing polyamido-sulfonic compounds as flow-property-improving and turbulence-inducing additives are disclosed.
Type:
Grant
Filed:
March 4, 1977
Date of Patent:
October 11, 1977
Assignee:
Calgon Corporation
Inventors:
Sally Lee Adams, Michael M. Cook, Fred David Martin
Abstract: Heterocyclic dihydroanthracen imines are disclosed to be useful as minor tranquilizers, anticonvulsants, muscle relaxants and to be useful in the treatment of extrapyramidal disorders such as Parkinson's disease; also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions.
Type:
Grant
Filed:
April 7, 1975
Date of Patent:
October 4, 1977
Assignee:
Merck & Co., Inc.
Inventors:
Paul S. Anderson, Marcia E. Christy, Gerald S. Ponticello
Abstract: Preparation of S-3-X-4-(3-substituted amino-2-hydroxypropoxy)-1,2,5-thiadiazole beta adrenergic blocking agents using as starting material an optically active alkalmine in the sinister configuration, or a derivative of said alkamine, which is reacted with an 3-X-4-chloro(or RO-where R is hydrogen or an alkali metal)-1,2,5-thiadiazole. Certain3-morpholino-4-chloro(or RO-)-1,2,5-thiadiazoles and certain alkamines and their preparation also are described. Preferred alkamines are S-3,5-disubstituted oxazolidines.
Type:
Grant
Filed:
December 4, 1974
Date of Patent:
September 27, 1977
Assignee:
Charles E. Frosst & Co.
Inventors:
Leonard M. Weinstock, Roger J. Tull, Dennis M. Mulvey
Abstract: This invention relates to new derivatives of dibenzocycloheptenes and to processes for making them. More particularly, the invention includes 5H-dibenzo[a,d]-cycloheptenes and 10,11-dihydro-5H-dibenzo[a,d]cycloheptenes which are substituted at their 5-carbon atom with an aminopropyl or an aminopropylidene radical. The amino entity may be either primary or secondary and if secondary, the substituent may be either a lower alkyl or alkenyl radical having up to 6 carbon atoms, cycloalkyl having up to 8 carbon atoms or an aralkyl radical. The dibenzocycloheptene nucleus may be further substituted. The invention also includes the intermediates used for obtaining these products. Also included are derivatives such as acyl derivatives which yield the active compound under physiological conditions.