Patents Represented by Attorney Mario A. Monaco

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  • Soft tertiary amine esters of bio-affecting carboxylic acids
    Patent number: 4381307
    Abstract: Novel derivatives of known bio-affecting carboxylic acids R-COOH are disclosed, said derivatives having the structural formula ##STR1## wherein Y and Y' are each H or C.sub.1 -C.sub.4 alkyl; n is 0 or 1; R.sub.1 and R.sub.2 are each selected from a variety of unsubstituted or substituted hydrocarbon radicals, or are combined so that --NR.sub.1 R.sub.2 represents the residue of a saturated or unsaturated heterocyclic compound containing one secondary nitrogen atom; and R.sub.3 is H or one of a variety of other substituents. Salts and N-oxides of compounds of formula (I) and the corresponding diacyloxy derivatives of known bio-affecting carboxylic acids HOOC-R'-COOH are disclosed also.
    Type: Grant
    Filed: October 31, 1980
    Date of Patent: April 26, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Kenneth B. Sloan
  • (6a.alpha.,10a.alpha.,11a.alpha.)-2-(2-Pyridinyl)-1,3,4,6,6a,7,8,9,10,10 a,11,11a-dodecahydro-2H-pyrazino]1,2-b]isoquinoline and derivatives
    Patent number: 4381302
    Abstract: (6a.alpha.,10a.alpha.,11a.alpha.)-2-(2-pyridinyl)-1,3,4,6,6a,7,8,9,10,10a,1 1,11a-dodecahydro-2H-pyrazino[1,2-b]isoquinoline and derivatives or acid addition salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressant agents and for treating sedation caused by antihypertensive therapy.
    Type: Grant
    Filed: May 26, 1981
    Date of Patent: April 26, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Joel R. Huff, Stella W. King, Walfred S. Saari
  • Process for preparing Benzoxepino- or Benzthiapino[4,3-b]pyrrole-2-acetic acids
    Patent number: 4380645
    Abstract: Improved yields of Benzoxepino- or Benzthiapino[4,3-b]pyrrole-2-acetic acids have been achieved from processes based on modifications performed on a pyrrole carboxylic ester rather than on a pyrrole-.alpha.-oxoacetate.
    Type: Grant
    Filed: December 11, 1981
    Date of Patent: April 19, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Bruce E. Witzel, Paul E. Finke, Debra L. Allison
  • Novel C-076 compounds
    Patent number: 4378353
    Abstract: There are disclosed certain new compounds related to C-076 compounds which have been produced by a mutant of the culture that produced the original C-076 compounds and isolated from the fermentation broth thereof. The compounds retain the C-076 16-membered cyclic backbone, however, the groups attached thereto are considerably modified from the original C-076 compounds. The new compounds have been found to retain the biological activity of the parent C-076 compounds. The compounds are thus potent antiparasitic agents and compositions and methods for such uses are also disclosed.
    Type: Grant
    Filed: February 17, 1981
    Date of Patent: March 29, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Robert T. Goegelman, Vincent P. Gullo, Louis Kaplan
  • Long lasting agonists and antagonists of LH-RH
    Patent number: 4377515
    Abstract: Novel peptides of the formula: ##STR1## where A through G, X and Y are various amino acids and substituents; having long lasting LHRH agonist and antagonist activity; useful in promoting fertility, reducing fertility, respectively.
    Type: Grant
    Filed: October 1, 1979
    Date of Patent: March 22, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Daniel F. Veber, Roger M. Freidinger
  • 4-Aza-17.beta.-substituted-5.alpha.-androstan-3-one-reductase inhibitors
    Patent number: 4377584
    Abstract: 4-Aza-17.beta.-substituted-5.alpha.-androstan-3-ones and their A-homo analogs of the formula: ##STR1## where Formula (I) may also have the structure of partial Formulas (II) and/or (III);and pharmaceutically acceptable salts of the above compounds are active as testosterone 5.alpha.-reductase inhibitors, and thus useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.
    Type: Grant
    Filed: September 23, 1980
    Date of Patent: March 22, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Gary H. Rasmusson, David B. R. Johnston, Glen E. Arth, deceased
  • Preparation of aqueous alcoholic dispersions of pH sensitive polymers and plasticizing agents and a method of enteric coating dosage forms using same
    Patent number: 4377568
    Abstract: An enteric coating medium for solid medicinal dosage units is prepared by precipitation of a pH sensitive polymer from an alcoholic solution of such a polymer and a plasticizing agent to produce a suspension of fine particles of a mixture of polymer and plasticizing agent.
    Type: Grant
    Filed: August 12, 1981
    Date of Patent: March 22, 1983
    Assignee: Merck Sharp & Dohme (I.A.) Corp.
    Inventor: Sham K. Chopra
  • N -(Substituted)-2-aza-2'-hydroxy-5,6-benzotricyclo[6.3.0.sup.1,8.0.sup.4,1 1 ] undecane centrally-acting analgesics
    Patent number: 4376779
    Abstract: Novel N-(substituted) derivatives of 2-aza-2'-hydroxy-5,6-benzotricyclo[6.3.0.sup.1,8.0.sup.4,11 ] undecane of the formula: ##STR1## are centrally acting analgesics effective in the relief of pain.
    Type: Grant
    Filed: January 26, 1981
    Date of Patent: March 15, 1983
    Assignee: Merck Sharp & Dohme (I.A.) Corp.
    Inventors: Patrice C. Belanger, Robert N. Young
  • Use of piperazinyl-imidazo[1,2-a]pyrazines in sedation
    Patent number: 4376772
    Abstract: Piperazinyl-imidazo[1,2-a]pyrazines and their acid addition salts are selective .alpha..sub.2 -adrenergic receptor antagonists and are thereby useful for treating sedation caused by antihypertensive drug therapy.
    Type: Grant
    Filed: December 9, 1981
    Date of Patent: March 15, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Walfred S. Saari, Joel R. Huff
  • Pyridylmethyl esters of selected bio-affecting carboxylic acids
    Patent number: 4376767
    Abstract: Novel pharmaceutically useful derivatives of selected known bio-affecting carboxylic acids are disclosed, said derivatives having the structural formula ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are each hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkylthio, phenyl, or substituted phenyl having one or more substituents each of which is selected from the group consisting of C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, chloro and dialkylamino wherein the alkyl portions, which can be the same or different, each have 1 to 5 carbon atoms, with the proviso that when R.sub.1 is alkoxy or alkylthio, then R.sub.2 cannot be alkoxy or alkylthio; X and X', which can be the same or different, are each hydrogen, C.sub.1 -C.sub.5 alkyl, carboxy, C.sub.2 -C.sub.6 alkoxycarbonyl, halo, C.sub.1 -C.sub.
    Type: Grant
    Filed: January 2, 1981
    Date of Patent: March 15, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Kenneth B. Sloan
  • Hypocholesterolemic fermentation products
    Patent number: 4376863
    Abstract: Substances isolated after cultivation of a microorganism belonging to the genus Aspergillus in a culture medium include a compound with structural formula: ##STR1## compound I is a member of a class of hypocholesterolemic and hypolipemic medicaments.
    Type: Grant
    Filed: August 21, 1981
    Date of Patent: March 15, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Tony Y. K. Lam
  • Substituted pyranone inhibitors of cholesterol synthesis
    Patent number: 4375475
    Abstract: 6-Phenyl-, phenylalkyl- and phenylethenyl-4-hydroxytetrahydropyran-2-ones in the 4(R)-trans stereoisomeric forms are potent inhibitors of cholesterol synthesis by virtue of their ability to inhibit the enzyme, 3-hydroxy-3-methylglutaryl-coenzyme A reductase.
    Type: Grant
    Filed: February 11, 1981
    Date of Patent: March 1, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Alvin K. Willard, Frederick C. Novello, William F. Hoffman, Edward J. Cragoe, Jr.
  • Dibenzo[a,d]cycloocten-5,12-(and 6,12)-imines
    Patent number: 4374838
    Abstract: Dibenzo[a,d]cycloocten-5,12-(and 6,12)-imines, 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.
    Type: Grant
    Filed: October 22, 1981
    Date of Patent: February 22, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Paul S. Anderson, Marcia E. Christy, Ben E. Evans, David C. Remy
  • Process for the preparation of zomepirac and related compounds
    Patent number: 4374997
    Abstract: Zomepirac and its analogs have been prepared from a 5-aroyl-3-hydroxycarbonyl-4-substituted pyrrole-2-acetic acid via acidic decarboxylation.
    Type: Grant
    Filed: June 4, 1981
    Date of Patent: February 22, 1983
    Assignee: Merck & Co., Inc.
    Inventors: James B. Doherty, Debra L. Allison
  • Process for the preparation of cyclic hexapeptide
    Patent number: 4374060
    Abstract: There is disclosed a process for preparing a cyclic hexapeptide somatostatin analog, specifically cyclo (D-Trp-Lys-Val-Phe-N-Me-Ala-Tyr). The cyclic hexapeptide is synthesized in large quantities in a solution synthesis procedure. However, because of the unexpectedly rapid cyclization rate of this compound, conditions have been developed such that a much more concentrated solution, and thus smaller volumes of the reaction medium, may be employed than would be expected.
    Type: Grant
    Filed: July 15, 1981
    Date of Patent: February 15, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Ruth F. Nutt
  • 2-Pyridyl-1,2-benzisothiazolinone-1,1-dioxides and their use as selective protease inhibitors
    Patent number: 4369183
    Abstract: The invention concerns novel 2-aryl-1,2-benzisothiazolinone-1,1-dioxide compounds; methods for their preparation; pharmaceutical compositions containing them as an active ingredient; and methods of selectively inhibiting proteases, especially elastase, and of treating emphysema, rheumatoid arthritis, and various inflammatory diseases, for example, bronchial inflammation.
    Type: Grant
    Filed: February 2, 1981
    Date of Patent: January 18, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Howard Jones, Robert L. Clark, Morris Zimmerman
  • Cellulosic urea formaldehyde compositions
    Patent number: 4366096
    Abstract: Non-flammable reactive particle compositions useful in forming shaped articles prepared from flammable cellulosic materials and a type of urea/formaldehyde resin. Processes for their preparation and a method of rendering flammable reactive particles substantially inflammable.
    Type: Grant
    Filed: August 14, 1978
    Date of Patent: December 28, 1982
    Inventors: Carl C. Abrams, deceased, Bernice Abrams, administratrix, James R. Jones
  • Catalyst for the preparation of 4-cyanothiazole and process for preparing the catalyst
    Patent number: 4363751
    Abstract: An improved process for the preparation of 4-cyanothiazole from 4-methylthiazole using an ammoxidation catalyst composed of manganese, chromium and molybdenum is disclosed.
    Type: Grant
    Filed: May 20, 1981
    Date of Patent: December 14, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Stuart Bacher, Carlos B. Rosas, John J. Sharkey
  • Radial flow cell
    Patent number: 4362621
    Abstract: An improved radial flow cell, comprising two or more sets of inlet port-groove-dam devices for improving the efficiency of radial flows and an efficient filtration device consisting of a micropore membrane and a steel screen support of low retention volume, is useful for aseptic and continuous in-line filtration of heterogeneous mixtures containing high concentrations of solids especially those resulting from fermentation processes.
    Type: Grant
    Filed: April 27, 1981
    Date of Patent: December 7, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Robert W. Dobna, B. Allen Mayles, Thomas H. Stoudt
  • 2,4-Disubstituted-1,2,5-thiadiazol-3(2H)-one antimicrobials
    Patent number: 4362877
    Abstract: 2,4-Disubstituted-1,2,5-thiadiazol-3(2H)-one antimicrobials have broad spectrum antibacterial and antifungal activity. They are found to be especially useful in agriculture to protect plants against diseases such as leaf, stem, and fruit spotting, internal discoloration and decay of fruits and vegetables. These compounds are particularly active against diseases caused by the genera Pseudomonas, Xanthomonas, Erwinia, and Corynebacterium.
    Type: Grant
    Filed: April 21, 1980
    Date of Patent: December 7, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Richard A. Dybas, Bruce E. Witzel, Nathaniel Grier