Abstract: Novel anticoccidial poultry compositions comprising an anticoccidially effective amount of a compound of the formula: ##STR1## wherein n is 3, 4 or 5 and R is hydrogen or an acyl radical derived from a non-toxic carboxylic acid or a non-toxic acid addition salt thereof methods of combatting poultry coccidiosis, novel compounds and methods of preparing these novel compounds.
Type:
Grant
Filed:
December 29, 1976
Date of Patent:
June 13, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Richard A. Dybas, Donald W. Graham, Jeannette E. Brown
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: 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
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:
November 22, 1976
Date of Patent:
April 18, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., John B. Bicking, Robert L. Smith
Abstract: The new 4-aminomethyldibenzobicyclo[5.1.0]octane compounds of the present invention are prepared from the corresponding 4-halo compounds by reaction with a metal cyanide to produce the corresponding 4-cyano compound, which is reduced with an alkali metal aluminum hydride to produce the desired 4-aminomethyl compound. These new aminomethyldibenzobicyclo[5.1.0]octane compounds are converted to the corresponding secondary and tertiary amino derivatives.These new compounds are useful as antiarrhythmic agents and can be used to overcome cardiac irregularities.
Abstract: The compound 6-chloro-2-(1'-piperazinyl)pyrazine, its N-oxides and acid-addition salts are disclosed having pharmacological activity as anorexic agents.
Type:
Grant
Filed:
June 15, 1976
Date of Patent:
April 4, 1978
Assignee:
Merck & Co., Inc.
Inventors:
William C. Lumma, Jr., Walfred S. Saari
Abstract: Compounds of the formula: ##STR1## and their N-oxides and acid-addition salts are disclosed having pharmacological activity as anorexic agents.
Type:
Grant
Filed:
March 4, 1977
Date of Patent:
March 28, 1978
Assignee:
Merck & Co., Inc.
Inventors:
William C. Lumma, Jr., Walfred S. Saari
Abstract: Compounds of the formula: ##STR1## and their N-oxides and acid-addition salts are disclosed having pharmacological activity as anorexic agents.
Type:
Grant
Filed:
September 24, 1976
Date of Patent:
March 7, 1978
Assignee:
Merck & Co., Inc.
Inventors:
William C. Lumma, Jr., Walfred S. Saari
Abstract: 1-Methyl-4-(2-carboxy-thioxanthen-9-ylidene)-piperidine is disclosed to have pharmaceutical utility as an appetite stimulant and an antihistamine with low antiserotonin and anticholinergic activity. Also disclosed are processes for the preparation of such compound; pharmaceutical compositions comprising such compound; and methods of treatment comprising administering such compound and compositions.
Abstract: 6,11-Dihydro-5H-Pyrrolo[2,1-b][3]benzazepin-11-one and derivatives thereof are generally prepared by Friedel-Crafts ring closure of a N-phenethylpyrrole-2-carboxylic acid halide. They are useful intermediates in the synthesis of skeletal muscle relaxants and tranquilizers such as 11-(3-dimethylaminopropylidene)-6,11-dihydro-5H-pyrrolo[2,1-b][3]benzazepi ne.
Type:
Grant
Filed:
June 29, 1976
Date of Patent:
February 21, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Joshua Rokach, Joseph G. Atkinson, Clarence S. Rooney
Abstract: This invention relates to a colloid-forming composition useful in medical diagnosis. More particularly, it relates to an improved kit useful as a diagnostic aid comprising colloid-forming reagent solutions.It further relates to a kit useful in medical diagnosis which comprises in combination a lyophilized Stannous-phytate complex and a buffered calcium chloride solution.
Abstract: Tetrafluoro derivatives of 10,11-dihydrodibenzo[a,d]cyclohepten-5-aminomethyl compounds and the corresponding N-substituted derivatives thereof, useful as antiarrhythmic agents, are prepared from tetrafluoro derivatives of 10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-one by reduction to the corresponding 5-ol compound and subsequently converting said 5-ol compound to the corresponding 5-halo and the 5-aminomethyl derivatives by reactions known in the prior art.
Abstract: Novel cholecalciferol and dihydrotachysterol.sub.3 derivatives produced against metabolic conversions at the 25-position, their preparation, pharmaceutical compositions, methods of treating steroid-induced osteoporosis, senile osteoporosis and secondary hyperparathyroidism, especially that induced by an insufficient amount of calcium in relationship to the amount of phosphate, novel intermediates and their preparation are disclosed.
Type:
Grant
Filed:
September 13, 1976
Date of Patent:
January 17, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Howard Jones, Shu Shu Yang, David P. Jacobus
Abstract: A novel tetrapeptide L-2-ketopiperidine-6-carbonyl-L-histidyl-L-thiazolidine-4-carbonyl-.beta.- alanin-amide, (L-Kpc-L-His-L-Tca-.beta.-ala-NH.sub.2), is a stimulant of the central nervous system. It is preparable by standard peptide synthetic procedures.
Type:
Grant
Filed:
January 24, 1977
Date of Patent:
January 3, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Daniel F. Veber, Ruth F. Nutt, Ralph F. Hirschmann
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:
November 22, 1976
Date of Patent:
January 3, 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:
March 22, 1976
Date of Patent:
January 3, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., John B. Bicking, Robert L. Smith
Abstract: Substituted 9,10-dihydroanthracen-9,10-imines are disclosed to be minor tranquilizers, anticonvulsnts, 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:
October 28, 1976
Date of Patent:
December 20, 1977
Assignee:
Merck & Co., Inc.
Inventors:
Paul S. Anderson, Marcia E. Christy, Gerald S. Ponticello
Abstract: The new 4-aminomethyldibenzobicyclo[ 5.1.0] octane compounds of the present invention are prepared from the corresponding 4-halo compounds by reaction with a metal cyanide to produce the corresponding 4-cyano compound, which is reduced with an alkali metal aluminum hydride to produce the desired 4-aminomethyl compound. These new aminomethyldibenzobicyclo[ 5.1.0] octane compounds are converted to the corresponding secondary and tertiary amino derivatives.These new compounds are useful as antiarrhythmic agents and can be used to overcome cardiac irregularities.