Abstract: Compounds of 5H dibenzo[a,d]-cycloheptenes and 10,11-dihydro-5H-dibenzo[a,d]cycloheptenes which are substituted at their 5-carbon atom with an N-cyanoaminopropyl or an N-cyanoaminopropylidene radical.
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: Disclosed are 2,3,5,6-tetrahydro-8H-imidazo-[2,1-c][1,4]thiazines, analogues and derivatives thereof which are effective in inhibiting indoleamine-N-methyl transferase and thus useful in the treatment of mental aberrations, such as schizophrenia. Also disclosed are processes for the preparation of such imidazothiazines; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions.
Abstract: Tetrafluoro derivatives of 10,11-dihydro-5H-dibenzo[a,d]cycloheptene-5-propylamine and 10,11-dihydro-5H-dibenzo[a,d]cycloheptene-.DELTA.-5-.gamma.-propylamine, useful as antidepressants, are prepared from the known 10,11-dihydro-5H-dibenzo[a,d]cycloheptene-10,11-dione by fluorination at the 10,11- position using sulfur tetrafluoride followed by introduction of the amino propylidine or the amino propyl substituent at the 5- position by reaction of the 5-keto or 5-halo-10,10,11,11-tetrafluoro derivative with the appropriate Grignard reagent.
Abstract: A cigarette filter containing menthol or other smoke-flavoring agent, and having improved shelf life and delivery rates for the smoke-flavoring agent, is obtained by first impegnating a granular activated carbon with a pore-modifying agent capable of blocking the most retentive portions of the activated carbon, by being held in preference to the smoke-flavoring agent which is added later. The pore-modifying agent is employed in amounts such that the less retentive portions of the activated carbon are not blocked but remain available for adsorption of the smoke-flavoring agent. A preferred pore-modifying agent is sucrose. Subsequently, the activated carbon is impregnated with the smoke-flavoring agent. The granular activated carbon is then formed into a filter.
Abstract: S,S'-bis(pyridylmethyl)-carbonodithioates and derivatives thereof have utility in the treatment of rheumatoid arthritis. The compound useful in the method of treatment is prepared from known pyridine derivatives and, principally, from pyridoxine and related compounds.
Type:
Grant
Filed:
May 16, 1974
Date of Patent:
July 27, 1976
Assignee:
Merck & Co., Inc.
Inventors:
Tsung-Ying Shen, Howard Jones, Dennis M. Mulvey, Conrad P. Dorn
Abstract: Hexa- and heptapeptides of formula W-[X-Pro-Phe-Phe-Y-Z].sub.n H prepared by standard synthetic peptide techniques are anti-inflammatory, anti-rheumatoid arthritic and anti-ulcer agents.
Type:
Grant
Filed:
January 21, 1975
Date of Patent:
July 27, 1976
Assignee:
Merck & Co., Inc.
Inventors:
Arthur F. Wagner, Frederick W. Holly, Tsau-Yen Lin, Tsung-Ying Shen, Ralph F. Hirschmann
Abstract: Process for preparing 5-fluoro-2-methyl-1-(p-methylsulfinylbenzylidene)-indene-3-acetic acid by reacting fluorobenzene with an acid halide, to form an indanone, reaction of the indanone with a methylthio (or methylsulfinyl) benzyl compound to form 5-fluoro-2-methyl-1-(p-methylthiobenzyl) or (p-methylsulfinylbenzyl)-indene and reacting said indene with a glyoxylic acid.This invention relates to new processes for preparing 5-fluoro-2-methyl-1-(p-methylsulfinylbenzylidene)-indene-3-acetic acid, to intermediates thereof and processes for said intermediates.
Type:
Grant
Filed:
July 5, 1974
Date of Patent:
July 20, 1976
Assignee:
Merck & Co., Inc.
Inventors:
Roger J. Tull, Robert F. Czaja, Richard F. Shuman, Seemon H. Pines
Abstract: The new 1-alkyl-4-(10-oxo or -hydroxy-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)piperidine compounds are prepared from the corresponding 10-desoxy compounds having a double bond at the 10,11-position by a process involving bromination, dehydrobromination of the resulting dibromo compound, followed by enamine formation and hydrolysis to give the desired 10-oxo compound. The compounds prepared in this manner are active as antihistamines and as appetite stimulants.
Abstract: The 2-aminomethyl-5-hydroxy-4H-pyran-4-ones of the present invention are disclosed to have pharmaceutical utility as skeletal muscle relaxants. Also disclosed are processes for the preparation of such pyranones; pharmaceutical compositions comprising such compounds; and method of treatment comprising administering such compounds and compositions when a muscle relaxant effect is indicated.
Type:
Grant
Filed:
January 22, 1975
Date of Patent:
July 6, 1976
Assignee:
Merck & Co., Inc.
Inventors:
Joseph G. Atkinson, Joshua Rokach, Clarence S. Rooney
Abstract: Deuterated functional group-containing hydrocarbons prepared by treating the non-labelled substrate in the liquid state with deuterium gas in the presence of a Group VII or VIII metal catalyst with heating between ambient to 300.degree. C. The labelled compounds are especially useful in reaction mechanism studies, as tracers in separation process studies, in the investigation of the physical properties of labelled compounds and in other specialized research work.
Abstract: A method of inhibiting corrosion and scale formation in an aqueous system is disclosed which comprises the step of treating the said system with 0.1 to 500 parts per million by weight of the total aqueous content of the said system, of a composition which may additionally include zinc and which comprises a polymer selected from the group consisting of:Polymers having recurring units of the formula: ##EQU1## WHEREIN M.sup.+ may be H.sup.+, alkali metal cation, or quaternary ammonium cation of the formula: ##EQU2## wherein for all of the above formulas, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are each independently selected from the group consisting of hydrogen, alkyl of from one to 10 carbon atoms, and substituted alkyl of from one to 10 carbon atoms, where the substituent is hydroxyl; carbonyl; and carboxylic acid groups, and alkali metal ion and ammonium salts thereof; andWherein n is an integer of from 2 to 100; and polymers having recurring units of the formula: ##EQU3## WHEREIN R.sub.
Type:
Grant
Filed:
March 11, 1974
Date of Patent:
June 22, 1976
Assignee:
Calgon Corporation
Inventors:
Bennett P. Boffardi, Michael M. Cook, Paul H. Ralston
Abstract: Aqueous hydraulic cement compositions containing phosphonobutane tricarboxylic acid as a flow-property-improving and turbulence-inducing additive and its use in cementing wells is disclosed.
Type:
Grant
Filed:
February 27, 1975
Date of Patent:
June 22, 1976
Assignee:
Calgon Corporation
Inventors:
Leonard J. Persinski, Fred David Martin, Sally Lee Adams
Abstract: This invention concerns 2,3,5,6-dibenzobicyclo-[5.1.0]octanes which may be substituted at the 4-position by either halogen, ketonic oxygen or hydroxyl. These compounds are prepared from 5H-dibenzo[a,d]cyclohepten-5-one by reaction with ethyl trichloroacetate in the presence of sodium methoxide to give 8,8-dichloro-2,3,5,6-dibenzobicyclo[5.1.0]octan-4-one which is reduced to the corresponding 4-hydroxy compound. The resulting 4-hydroxy compound is dehalogenated and converted to the corresponding 4-chloro or 4-keto compound. The 4-substituted compounds are useful in preparing other compounds of our invention.4-Dialkylaminopropylidenedibenzobicyclo[5.1.0]-octane compounds and 4-dialkylaminopropyldibenzobicyclo[5.1.0]octane compounds, useful as antidepressant agents, are prepared from, respectively, dibenzobicyclo[5.1.0]-octan-4-one by reaction with a dialkylaminopropyl Grignard reagent followed by dehydration of the resulting carbinol or by reaction of a 4-halo-2,3,5,6-dibenzobicyclo[5.1.
Abstract: The new 1-alkyl-4-(10-oxo or -hydroxy-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-piperidine compounds are prepared from the corresponding 10-desoxy compounds having a double bond at the 10,11-position by a process involving bromination, dehydrobromination of the resulting dibromo compound, followed by enamine formation and hydrolysis to give the desired 10-oxo compound. The compounds prepared in this manner are active as antihistamines and as appetite stimulants.
Abstract: A watchman's tour recording system which includes a watchman's unit having a clock means for producing digital time signals, a station identification signal producing means for producing digital station signals, at least two digital bit storage or memory means and special address means arranged to direct the digital time and station identification signals into predetermined locations in the memory means so that their storage capabilities are most effectively utilized. Novel photoelectric station identification signal generating means are also disclosed.
Type:
Grant
Filed:
September 10, 1974
Date of Patent:
May 25, 1976
Assignee:
Merck & Co., Inc.
Inventors:
William Grove Lawrence, Wolfgang Juergen Sauter
Abstract: Process for preparing .beta.-D-glucosyluronic acid derivatives of pharmaceutical acids by the controlled hydrolysis of the corresponding 2,3,4-tri-O-acyl .beta.-D-glucopyranosidyl uronate esters of the free acids.
Abstract: A process for the controlled manufacture of cells and vaccines in which reproducable real time quantitative assays are utilized to ascertain the physical and chemical state of the system, in order to more efficiently manage the system, so that cell sheet formation may be determined and the vaccine may be harvested at its maximum titre, thereby resulting in significantly increased yields and decreased production costs.
Type:
Grant
Filed:
December 6, 1974
Date of Patent:
May 25, 1976
Assignee:
Merck & Co., Inc.
Inventors:
William J. Miller, Raymond E. Spier, William J. McAleer