Abstract: Pilocarpinium 2-naphthalenesulfonate, pilocarpinium 2,5-dihydroxybenzoate, pilocarpinium dihydrogenphosphate, pilocarpinium 2-chloro-4,6-disulfamoylphenoxide, and pilocarpinium 3,5-di-tert-butylsalicylate, novel compounds effective in the treatment of glaucoma.
Abstract: 10,11-Furo and 10,11-bis-(hydroxyalkyl) derivatives of cyproheptadine are disclosed having anticholinergic activity but with diminished or eliminated antiserotonin and antihistamine activity. 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.
Abstract: 2-Aminomethylphenol products and their non-toxic, pharmaceutically acceptable salts useful in the treatment of edema and inflammation are disclosed. The products may be prepared by treating an N-(2-hydroxybenzyl)carboxamide with an aqueous solution of an acid or a base.
Type:
Grant
Filed:
May 7, 1976
Date of Patent:
August 23, 1977
Assignee:
Merck & Co., Inc.
Inventors:
Everett M. Schultz, Edward J. Cragoe, Jr.
Abstract: (2-oxo-3-butenyl)dimethylamine monomers which may be used in the preparation of high molecular weight water-soluble cationic polymers which may be used as flocculants, drainage and retention aids, or conductive polymers.
Abstract: Cationic, electrically conductive polymers are mixed with multifunctional anionic compounds and/or anionic polymers to form a polysalt complex which exhibits markedly improved properties. Specifically, solvent holdout to parafinic solvents and to toluene are considerably improved, and the tackiness of the resulting film is notably decreased. The polysalt products also exhibit very good filmability on plastic substrates whereas the cationic polymer alone normally forms very poor films on such substrates.
Type:
Grant
Filed:
October 27, 1976
Date of Patent:
August 9, 1977
Assignee:
Calgon Corporation
Inventors:
Andrew Jackson Sharpe, Jr., Robert H. Windhager, Kathleen Seese Hearp
Abstract: Methods of using aqueous hydraulic cement compositions containing phosphonobutane tricarboxylic acid as a flow-property-improving and turbulence-inducing additive are disclosed.
Type:
Grant
Filed:
April 14, 1976
Date of Patent:
August 9, 1977
Assignee:
Calgon Corporation
Inventors:
Leonard J. Persinski, Fred David Martin, Sally Lee Adams
Abstract: Use of oil soluble cationic polymers as flocculants for the purification of used motor oil. Polymers useful in the process of the instant invention include oil soluble polymers such as fatty acid salts of cationic polymers.
Abstract: Methods of using aqueous hydraulic cement compositions containing sulfonated copolymers of styrene-maleic anhydride as flow-property-improving and turbulence-inducing additives are disclosed.
Type:
Grant
Filed:
April 14, 1976
Date of Patent:
July 19, 1977
Assignee:
Calgon Corporation
Inventors:
Leonard J. Persinski, Fred David Martin, Sally Lee Adams
Abstract: A new heterocycle, 5,11-diazatetracyclo[6.2.2.0.sup.2,7.0.sup.4.9 ]dodecane, is prepared by heating an endo-diazatricyclo[6.2.2.0.sup.2,7 ]dodec-11-ene substituted in the 7 and 11 positions with electron withdrawing groups. 2,9-Bis-phenylacetyl derivatives of the new heterocycle and closely related derivatives are potent analgesic agents.
Type:
Grant
Filed:
April 14, 1976
Date of Patent:
July 5, 1977
Assignee:
Merck & Co., Inc.
Inventors:
Jan ten Broeke, Edward J. J. Grabowski, Lars M. Flataker, Michael H. Fisher, Arthur A. Patchett
Abstract: This invention relates to 8-aza-9-oxo(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: Cyproheptadine derivatives substituted with a trifluoromethylthio or trifluoromethylsulfonyl group in one of the benzo rings and having a hydroxyalkyl or cycloalkylalkyl group on the piperidine nitrogen are potent antipsychotic agents, with a low propensity to induce extrapyramidal side effects that are experienced with most major tranquilizers. The tranquilizing activity is predominantly in the levorotatory enantiomers, whereas the dextrorotatory enantiomers have anticholinergic activity. Each enantiomer is useful as a source of the other by racemization. The novel compounds are prepared by treatment of the corresponding iodo or bromo compound with bis(trifluoromethylthio)mercury and copper powder.
Abstract: Cyproheptadine derivatives substituted with a trifluoromethylthio group in one of the benzo rings and certain derivatives thereof are potent antipsychotic agents, with a low propensity to induce extrapyramidal side effects experienced with most major tranquilizers, and platelet aggregation inhibitors useful as antithrombotic agents. The antipsychotic activity resides in the levorotatory enantiomer whereas both enantiomers are platelet aggregation inhibitors. The novel compounds are prepared by treatment of the corresponding iodo compound with trifluoromethylthiocopper formed from bis-(trifluoromethylthio)mercury and copper powder.
Abstract: A method of inhibiting indoleamine-N-methyl transferase comprises the administration to a host of a therapeutically effective amount of a 3-hydrocarbyl-2-imino-thiazolidine or thiazoline or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
May 3, 1976
Date of Patent:
June 14, 1977
Assignee:
Merck & Co., Inc.
Inventors:
Norman R. Hunter, Clarence S. Rooney, Joshua Rokach, Edward J. Cragoe, Jr.
Abstract: This invention relates to novel 9-thia-, 9-oxothia-, and 9-dioxothia-11-oxo-12-azaprostanoic 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, as platelet aggregation inhibitors, and for the treatment of certain autoimmune diseases.
Type:
Grant
Filed:
May 24, 1976
Date of Patent:
May 10, 1977
Assignee:
Merck & Co., Inc.
Inventors:
Robert L. Smith, Ta-Jyh Lee, Edward J. Cragoe, Jr.
Abstract: An apparatus is described which, in addition to testing each ear of a human subject separately for extent of hearing and frequency detection, also permits the delivery, preferably by electronic means for pre-set arrangement, of a series of intermittent long and short signals in different combinations, by means of which the subject can be tested for auditory memory and hearing side dominance.
Abstract: The N-oxide of 10,11-dihydro-3-carboxycyproheptadine is disclosed to have pharmaceutical utility as an appetite stimulant and as an anthihistaminic agent. 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: 1-Methyl-4-[2-(trifluoromethylthio)thioxanthen-9-ylidene]piperidine and the corresponding 2-trifluoromethylsulfonyl compound are antipsychotic agents. They are prepared by dehydration of the corresponding 9-hydroxy-9-piperidyl compounds.
Abstract: This invention relates to aryloxy-, and 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.