Abstract: 6-(1-Piperazinyl)quinoxaline and pharmaceutically acceptable salts thereof have serotoninmimetic activity. It is prepared by reducing the nitro group of 1-(3-amino-4-nitrophenyl)piperazine followed by treatment with glyoxal.
Type:
Grant
Filed:
June 15, 1977
Date of Patent:
May 23, 1978
Assignee:
Merck & Co., Inc.
Inventors:
William C. Lumma, Jr., Walfred S. Saari
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: Novel pharmaceutical compositions are disclosed which comprise a hypotensive agent and a phenyl hydrazino substituted propionic acid decarboxylase inhibitor. The compositions have enhanced anti-hypertensive activity.
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: 3-(1-Piperazinyl)-pyrido[2,3-b]pyrazines and pharmaceutically acceptable salts thereof have serotoninmimetic activity. They are prepared by treating 3-halo-pyrido[2,3-b]pyrazines with piperazine.
Type:
Grant
Filed:
April 25, 1977
Date of Patent:
April 4, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Walfred S. Saari, William C. Lumma, Jr.
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: Novel 2-(4-substituted-1,2,5-thiadiazol-3-yloxy)acetaldehydes are disclosed. These acetaldehydes are useful as intermediates for preparing certain .beta.-adrenergic blocking agents.
Abstract: Novel functional ionene polymer compositions have been prepared which have been found to be useful in a wide variety of applications, including, among others, as wet and dry strength additives, corrosion inhibitors, and electroconductive coatings, and which comprise recurring units of the formula: ##STR1##
Abstract: The invention disclosed herein relates to novel partially cross-linked, fully quaternized poly-[(methylimino)trimethylene] polymers wherein a minor proportion (1% to 20%) of the nitrogen atoms in adjacent poly-[(methylimino)trimethylene] linear chains are, by quaternization, joined through trimethylene or 2-hydroxy-trimethylene bridges, the non-cross-linked nitrogens in the said linear chains being fully quaternized with lower alkyl or trialkylammoniopropyl groupings; and to the novel process for preparing these partially cross-linked, fully quaternized polymers which comprises reacting poly-[(methylimino)trimethylene] with 0.01 to 0.2 equivalents of 1,3-dihalo-propane or 1,3-dihalo-2-hydroxypropane per equivalent of tertiary amine in said poly-[(methylimino)trimethylene], and subsequently reacting the resulting product with excess alkyl halide or 3-halopropyltrialkylammonium halide.
Abstract: New fluoro derivatives of aralkylamine compounds, particularly 2-(2-phenyl-1,1,2,2-tetrafluoroethyl)benzylamine, as well as the N-alkyl and the N,N-dialkyl derivatives thereof are prepared by reaction of 2-bromobenzonitrile with benzylmagnesium chloride to produce 2'-bromo-2-phenylacetophenone; oxidation of said acetophenone with selenous acid to produce 2-bromobenzil; conversion of the benzil compound by treatment with sulfur tetrafluoride to the corresponding 2-bromo-.alpha.,.alpha.-.alpha.',.alpha.'-tetrafluorobibenzyl;followed by reaction of the 2-bromobibenzyl compound with a metal cyanide to produce the corresponding 2-(2-phenyl-1,1,2,2-tetrafluoroethyl)benzonitrile. This nitrile compound is then reduced with lithium aluminum hydride to produce the corresponding benzylamine, which is then converted, if desired, to the N-alkyl and/or N,N-dialkyl 2-(2-phenyl-1,1,2,2-tetrafluoroethyl)benzylamine.
Type:
Grant
Filed:
February 20, 1976
Date of Patent:
January 31, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Edward L. Engelhardt, Marcia E. Christy
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: 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: Novel pharmaceutical compositions comprising hydrazino-phenylpropionic acid decarboxylase inhibitors and certain benzimidazole and benzoxazole alanines are disclosed. The compositions have enhanced hypotensive activity.
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: Aqueous hydraulic cement compositions containing polyamido-sulfonic compounds as flow-property-improving and turbulence-inducing additives and their use in cementing wells is disclosed.
Type:
Grant
Filed:
April 20, 1977
Date of Patent:
March 28, 1978
Assignee:
Calgon Corporation
Inventors:
Sally Lee Adams, Fred David Martin, Michael M. Cook