Patents Represented by Attorney Mario A. Monaco

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  • Inhibitor of dihydrofolate reductase
    Patent number: 4258045
    Abstract: A group of aryl-Z-alkoxy-5-benzylpyrimidines wherein Z is oxy, thio, imino, carbonyl, carbamoyl, sulfonyl, sulfinyl or sulfamoyl has been prepared from 2,4-diamino-5-benzylpyrimidine via alkylation with either an aryl-Z-alkyl halide or a substituted glycidyl ether. These compounds are potent dihydrofolate reductase (DHFR) inhibitors which are useful as antibacterial, anti-protozoal and antitumor agents.
    Type: Grant
    Filed: November 30, 1979
    Date of Patent: March 24, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Martin Poe, William V. Ruyle
  • Process for the preparation of imino-bridged benzocycloheptapyridines
    Patent number: 4256889
    Abstract: Benzocycloheptapyridines with an imine bridge in the cycloheptane ring, derivatives and pharmaceutically acceptable salts thereof are useful as anxiolytics, antidepressants, anticonvulsants, muscle relaxants and in the treatment of mixed anxiety-depression, minimal brain dysfunction and extrapyramidal disorders such as Parkinson's disease. They are prepared, for example, by treatment of a benzo[5,6]cyclohepta[1,2-c]pyridin-11-one with ammonia to give the 11-imine, acylation of the imine, treatment of the protected imine with an alkyllithium to provide the 11-alkyl-11-acylamino compound, treatment with acid or base to cause ring closure to an 11-alkyl-6,11-acylimino compound followed by removal of the protecting group, either hydrolytically or hydrogenolytically.
    Type: Grant
    Filed: November 13, 1979
    Date of Patent: March 17, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Shepard, Daniel G. Brenner
  • Long-lasting agonists of enkephalin
    Patent number: 4254107
    Abstract: Novel peptides of the formula: ##STR1## wherein X is S or (CH.sub.2).sub.n and n is 0, 1 or 2, and R.sub.1 through R.sub.6 are various amino acid and other substituents; having long-lasting enkephalin agonist activity; useful in treating pain and in treating schizophrenia.
    Type: Grant
    Filed: November 27, 1979
    Date of Patent: March 3, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Daniel F. Veber, Roger M. Freidinger
  • Treatment of pain, fever, and inflammation with compositions containing 2-(substitutedpiperidinomethyl)propane and propene nitriles
    Patent number: 4254131
    Abstract: A method of treating pain, fever, and inflammation and pharmaceutical compositions for use therein, wherein the active ingredient comprises a compound of the formula: ##STR1## wherein A and R.sub.1 represent various substituents.
    Type: Grant
    Filed: August 21, 1979
    Date of Patent: March 3, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel
  • Bone char and activated carbon mixtures for sugar liquor purification
    Patent number: 4252571
    Abstract: An admixture of granular activated carbon (GAC) and bone char (BC) can be effectively employed to decolorize and to deash white cane sugar liquors. Use of this admixture in place of bone char exclusively results in significantly improved decolorization. The GAC/BC admixture can be effectively reactivated at a temperature within the limit of 900.degree. F. to 1200.degree. F.
    Type: Grant
    Filed: November 21, 1979
    Date of Patent: February 24, 1981
    Assignee: Calgon Corporation
    Inventor: Phillip B. Reilly
  • Tetrahydro-1H-1,4-diazepino(1,7-a)benzimidazoles useful as analgesic agents
    Patent number: 4252816
    Abstract: Substituted tetrahydro-1H-1,4-diazepino[1,7-a]benzimidazoles of the formula: ##STR1## and pharmaceutically acceptable salts thereof having thereapeutic activity as analgesic agents.
    Type: Grant
    Filed: December 3, 1979
    Date of Patent: February 24, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Walfred S. Saari, Joel R. Huff
  • 9,10-Dihydro-4H-benzo[4,5]cyclohepta [1,2-b]thiophen-4,9-imines
    Patent number: 4252810
    Abstract: 9,10-Dihydro-4H-benzo[4,5]cyclohepta [1,2-b]thiophen-4,9-imines, derivatives and pharmaceutically acceptable salts thereof are useful as antianxiety agents, as muscle relaxants and in the treatment of extrapyramidal disorders such as in Parkinson's disease.
    Type: Grant
    Filed: November 15, 1978
    Date of Patent: February 24, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Paul S. Anderson, Ben E. Evans
  • 2-{[4-(6-Substituted-2-pyrazinyl)- 1-piperazinyl]alkyl}-5-substituted-1,2,4-triazolo[4,3-a]pyridin-3(2H)-one analgesic agents
    Patent number: 4251530
    Abstract: 2-{[4-(6-Substituted-2-pyrazinyl)-1-piperazinyl]alkyl}-5-substituted-1,2,4- triazolo[4,3-a]pyridin-3(2H)ones useful as analgesic agents, having the following formula: ##STR1## wherein p1 n is 2 to 4; R is halo, methyl, methoxy, or CF.sub.3 ; andR.sub.1 is H or methyl;and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: February 19, 1980
    Date of Patent: February 17, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Walfred S. Saari, William C. Lumma
  • Treatment of pain, fever, and inflammation with compositions containing piperidinobutan-and 3-buten-2-ones
    Patent number: 4250184
    Abstract: A method of treating pain, fever, and inflammation and pharmaceutical compositions for use therein, wherein the active ingredient comprises a compound of the formula; ##STR1##
    Type: Grant
    Filed: July 20, 1979
    Date of Patent: February 10, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel
  • 2-(Substitutedpiperidylmethyl)propene and propane nitriles
    Patent number: 4247700
    Abstract: Antimicrobial agents suitable for use in aqueous systems for their preservation against biodeterioration include substitutedpiperidinomethyl-propenenitriles and propanenitriles. The unsaturated compounds are prepared by reaction of a suitable piperidine with cyano acetic acid and formaldehyde: the propane derivatives therefrom by nucleophilic addition. spThis application is a continuation-in-part of Ser. No. 795,693, filed May 11, 1977, now abandoned.
    Type: Grant
    Filed: February 5, 1979
    Date of Patent: January 27, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel
  • 1-[2-(Alkyl and arylsulfonyl)-2-propenyl and propyl] substituted piperidines useful as antimicrobial and antiinflammatory agents
    Patent number: 4244963
    Abstract: 1-[2-(Alkyl and arylsulfonyl)-2-propenyl and propyl] substituted piperidines of the formula: ##STR1## where A is ##STR2## and R.sub.1 -R.sub.5 are various substituents, are useful as antimicrobial and anti-inflammatory agents.
    Type: Grant
    Filed: September 27, 1979
    Date of Patent: January 13, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel
  • Orexigenic use of pyrrolo[2,1-b][3]benzazepines
    Patent number: 4242349
    Abstract: Pyrrolo[2,1-b][3]benzazepines with a piperidinylidene group in the 11-position have utility as appetite stimulants.
    Type: Grant
    Filed: October 1, 1979
    Date of Patent: December 30, 1980
    Assignee: Merck & Co., Inc.
    Inventor: David C. Remy
  • Piperazinyl-imidazo[1,2-a]pyrazines
    Patent number: 4242344
    Abstract: Piperazinyl-imidazo[1,2-a]pyrazines, derived from reactions between halo-imidazo[1,2-a]pyrazines with piperazine derivatives, are found to be active anorexic, antidepressant, antihypertensive, analgesic, antiarrhythmic, and/or anti-smoking agents.
    Type: Grant
    Filed: September 7, 1979
    Date of Patent: December 30, 1980
    Assignee: Merck & Co., Inc.
    Inventor: William C. Lumma
  • Preparation of 5(halophenyl)salicylic acid compounds
    Patent number: 4237315
    Abstract: A method of preparing compounds of the formula: ##STR1## wherein a novel palladium catalyst system is utilized comprising palladium together with C.sub.1-2 COO.sup.- ligands and halo ligands wherein the molar weight percent based on total ligand molar weight, of the C.sub.1-2 COO.sup.- ligand is from 30 to 60%; andwherein the ratio of the total molar weight of the ligands to the molar weight of palladium utilized is from 4:1 to 10:1; anda catalyst regeneration portion comprising from 0.1 to 8.0 parts of phosphomolybdenovanadic acid per part of palladium catalyst, and at least 20 parts of a solubilizing agent selected from ethylene carbonate, propylene carbonate, and sulfolane, per part of palladium catalyst.
    Type: Grant
    Filed: November 2, 1979
    Date of Patent: December 2, 1980
    Assignee: Merck & Co., Inc.
    Inventor: Ulf H. Dolling
  • 3-Hydroxymethyldibenzo[b,f]thiepins as prostaglandin antagonists
    Patent number: 4237160
    Abstract: Novel 3-hydroxymethyldibenzo[b,f]thiepin and derivatives are prepared and employed in the treatment and control of allergic conditions such as allergic asthma.
    Type: Grant
    Filed: November 27, 1979
    Date of Patent: December 2, 1980
    Assignee: Merck Sharp & Dohme (I.A.) Corp.
    Inventors: Pierre A. Hamel, Joshua Rokach
  • High molecular weight meningococcal group C vaccine and method for preparation thereof
    Patent number: 4235994
    Abstract: A vaccine against Group C meningococcal meningitis consisting of a polysaccharide of which at least 80% by weight has a molecular weight in excess of 1,000,000 daltons is prepared. The polysaccharide was isolated from Group C hexadecyl trimethylammonium bromide cell paste with 1.0M CaCl.sub.2 extraction and purified by phenol extraction, ultracentrifugation at 100,000 g. and ethanol fractionation (30%-45% v/v in ethanol).
    Type: Grant
    Filed: June 26, 1978
    Date of Patent: November 25, 1980
    Assignee: Merck & Co., Inc.
    Inventors: Thomas H. Stoudt, Dennis J. Carlo, Arpi Hagopian
  • Process for preparing indenyl acetic acids
    Patent number: 4233457
    Abstract: This invention relates to an improved process for preparing 5-fluoro-2-methyl-1-(p-methylsulfinylbenzylidene)-3-indenyl acetic acid.
    Type: Grant
    Filed: May 17, 1979
    Date of Patent: November 11, 1980
    Assignee: Merck & Co., Inc.
    Inventors: Robert F. Czaja, Edward J. J. Grabowski
  • Diazaditwistanes, and pharmaceutical compositions for treating pain in warm blooded animals containing them
    Patent number: 4232026
    Abstract: Certain 2- and/or 9- phenylalkyl-5,11-dimethyl-5,11-diazaditwistane compounds bind to opiate receptor sites and have central nervous system activities exemplified by analgesia.
    Type: Grant
    Filed: July 20, 1978
    Date of Patent: November 4, 1980
    Assignee: Merck & Co., Inc.
    Inventor: Jan ten Broeke
  • 10,11-Dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines
    Patent number: 4232158
    Abstract: 10,11-Dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines, derivatives and pharmaceutically acceptable salts thereof are useful as antianxiety agents, as muscle relaxants and in the treatment of extrapyramidal disorders such as in Parkinson's disease. They are prepared by treatment of a 5H-dibenzo[a,d]cyclohepten-5-one with ammonia to give the 5-imine, acylation of the imine, treatment of the protected imine with an organolithium to provide the 5-substituted-5-acylamino compound, treatment with acid or base to cause ring closure to a 5-substituted-5,10-acylimino compound followed by removal of the protecting group, either hydrolytically or hydrogenolytically.
    Type: Grant
    Filed: June 4, 1979
    Date of Patent: November 4, 1980
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Shepard, Daniel G. Brenner
  • Transdermal delivery of drugs
    Patent number: 4230105
    Abstract: An improved method for the topical administration of systemically or locally active drugs utilizes a bandage containing one or more layers including a drug useful in the treatment of disease and a heat-generating substance, each dispersed intimately throughout said bandage layers.
    Type: Grant
    Filed: November 13, 1978
    Date of Patent: October 28, 1980
    Assignee: Merck & Co., Inc.
    Inventor: Richard J. Harwood