Patents Represented by Attorney Mario A. Monaco

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  • 6-Bromocholesterol derivatives
    Patent number: 4430321
    Abstract: Novel 6-bromo derivatives of cholesterol have the formula ##STR1## Such compounds are prepared from the known 6-iodocholesterol by treatment with cuprous bromide.These compounds, labelled with radioisotopes of Br-82 or Br-77, are localized in the adrenal, mammary and ovary tissue of female mammals and in the adrenal or prostate tissue of males when administered to such individuals. This provides a method for imaging adrenal, ovary or prostate tissue which is superior to use of the prior art 6-iodo-cholesterol.
    Type: Grant
    Filed: January 15, 1982
    Date of Patent: February 7, 1984
    Assignee: Merck Frosst Canada Inc.
    Inventors: Richard J. Flanagan, Leonard I. Wiebe
  • Synergistic treatment of adult canine heartworm with thiacetarsamide and ivermectin
    Patent number: 4430329
    Abstract: There is disclosed a method for the treatment of adult canine heartworm which involves treating a dog infected with adult heartworm first with thiacetarsamide and then, following a period of from 3 to 6 weeks, with ivermectin. The thiacetarsamide which has some activity against the adult heartworm has this activity potentiated or synergized by the ivermectin.
    Type: Grant
    Filed: May 17, 1982
    Date of Patent: February 7, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Lyndia S. Blair
  • Fluorinated cyclic hexapeptide somatostatin analogs
    Patent number: 4427661
    Abstract: Fluorinated somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven of the ring amino acids of somatostatin and the Lys side chain is monofluorinated in the .gamma. or .delta. positions. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method.
    Type: Grant
    Filed: July 30, 1982
    Date of Patent: January 24, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Curley, Ralph F. Hirschmann
  • [(Alkoxycarbonyl)oxy]alkyl esters of methyldopa
    Patent number: 4426391
    Abstract: Novel prodrugs of methyldopa which are [(alkoxycarbonyl)oxy]alkyl esters of methyldopa are disclosed. Also, pharmaceutical compositions containing these compounds are disclosed. Upon administration to warm-blooded animals, these prodrugs liberate methyldopa along with innocuous side products.
    Type: Grant
    Filed: September 15, 1982
    Date of Patent: January 17, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, Chung Shih
  • 5-Benzothiazolesulfonamide derivatives for the topical treatment of elevated intraocular pressure
    Patent number: 4426388
    Abstract: Novel carboxylic acid esters of 5-hydroxy-2-benzothiazolesulfonamide are shown to be useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions including drops and inserts are also disclosed, as well as methods for preparing the novel compounds.
    Type: Grant
    Filed: April 2, 1982
    Date of Patent: January 17, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Otto W. Woltersdorf, Jr.
  • Treatment of giardiasis and trichomoniasis
    Patent number: 4424220
    Abstract: Fluorouracil and emimycin are useful in the treatment of giardiasis and trichomoniasis.
    Type: Grant
    Filed: September 22, 1982
    Date of Patent: January 3, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Ching C. Wang
  • Process for the whole broth extraction of avermectin
    Patent number: 4423211
    Abstract: A process for the whole broth extraction of avermectins wherein the pH of the whole broth is adjusted with mineral acid and then contacted with a solvent extractant so that the avermectic active component is taken up by the solvent. The now avermectin rich extractant is then processed through a solvent concentration step and the avermectin isolated by conventional crystallization. The extractant is then recycled with appropriate make-up to extract a subsequent batch of whole broth.
    Type: Grant
    Filed: December 21, 1981
    Date of Patent: December 27, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Carl Bagner, Arthur S. Wildman
  • Processes for the interconversion of avermectin compounds
    Patent number: 4423209
    Abstract: There is disclosed a process for converting avermectin compounds (formerly identified as C-076 compounds) of the A-type, into avermectin compounds of the B-type. The process is carried out on the naturally occuring avermectin compounds as well as on derivatives thereof. The process involves selectively cleaving the 5-methoxy group, converting it into the hydroxy group, through the intermediate 5-keto group.
    Type: Grant
    Filed: February 26, 1982
    Date of Patent: December 27, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Helmut H. Mrozik
  • Hexahydronaphth[1,2-b]-1,4-oxazines
    Patent number: 4420480
    Abstract: Hexahydronaphth[1,2-b]-1,4-oxazines have dopaminergic activity and display .alpha..sub.2 -adrenergic receptor antagonism. They are useful in the treatment of parkinsonism, depression and hypertension. An important method of preparation is by ring closure of the appropriate 2-chloroacetamidotetrahydronaphthalen-1-ol and reduction of the resulting cyclic amide carbonyl group.
    Type: Grant
    Filed: August 30, 1982
    Date of Patent: December 13, 1983
    Assignee: Merck & Co., Inc.
    Inventor: James H. Jones
  • Hypocholesteremic fermentation products and process of preparation
    Patent number: 4420491
    Abstract: Substances isolated after cultivation of a microorganism belonging to the genus Aspergillus in a culture medium comprise compounds which have structures: ##STR1## Together with salts and esters of the carboxylic acid, these compounds form a class of highly active hypocholesteremic and hypolipemic medicaments.
    Type: Grant
    Filed: May 28, 1981
    Date of Patent: December 13, 1983
    Assignee: Merck & Co., Inc.
    Inventors: George Albers-Schonberg, Henry Joshua, Maria B. Lopez
  • Amino derivatives of chloro nitro amino pyrazines useful as adjuncts to radiation therapy
    Patent number: 4418062
    Abstract: 2-Substituted amino derivatives of 6-amino-3-chloro-5-nitropyrazin-2-yl are prepared by converting 3-amino-5,6-dichloropyrazinecarboxylic acid to 5,6-dichloro-3-nitropyrazinamine and treating said compound with an amine to produce the corresponding 2-substituted amino compound.
    Type: Grant
    Filed: July 19, 1982
    Date of Patent: November 29, 1983
    Assignee: Merck & Co., Inc.
    Inventor: George D. Hartman
  • Benzothiazolesulfonamide derivatives for the topical treatment of elevated intraocular pressure
    Patent number: 4416890
    Abstract: Novel carboxylic acid esters of 6-hydroxy-2-benzothiazolesulfonamide are shown to be useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions including drops and inserts are also disclosed, as well as methods for preparing the novel compounds.
    Type: Grant
    Filed: May 21, 1982
    Date of Patent: November 22, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Otto W. Woltersdorf, Jr.
  • Di(alkylamino) derivatives of chloronitropyrazines useful as adjuncts to radiation therapy
    Patent number: 4416882
    Abstract: Di(alkylamino) derivatives of chloronitropyrazines are prepared from dichloronitropyrazinamine by diazotization of the amine followed by halogen exchange to produce an intermediate dichloro-halo nitropyrazine followed by reaction with one or two moles of an alkyl amine to effect replacement of one or two of the pyrazine halogens.
    Type: Grant
    Filed: July 19, 1982
    Date of Patent: November 22, 1983
    Assignee: Merck & Co., Inc.
    Inventor: George D. Hartman
  • Substance and process for its production
    Patent number: 4415669
    Abstract: There is disclosed a macrolide isolated from the fermentation broth of a microorganism identified as MA-5285 which morphological analysis reveals to be a strain of Streptomyces hygroscopicus. The compound's structure is presented based upon analytical studies. The compound has insecticidal and antiparasitic activity.
    Type: Grant
    Filed: December 7, 1981
    Date of Patent: November 15, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Sebastian Hernandez
  • Dibenzo[a,d]cycloocten-5,12-imines
    Patent number: 4414154
    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: November 8, 1983
    Assignee: Merck & Co. Inc.
    Inventors: Paul S. Anderson, Marcia E. Christy, Ben E. Evans, David C. Remy
  • N-Acyl derivatives of 6-alkylamino 5-chloro-3-nitropyrazinamines for radiation therapy
    Patent number: 4414215
    Abstract: N-Acyl derivatives of 6-(alkylamino)-5-chloro-3-nitro-pyrazinamines are disclosed to have activity in increasing the sensitivity of tumor cells to radiation. Also disclosed are methods of preparing such compounds and pharmaceutical compositions including such compounds.
    Type: Grant
    Filed: July 19, 1982
    Date of Patent: November 8, 1983
    Assignee: Merck & Co., Inc.
    Inventor: George D. Hartman
  • 22-Hydroxy derivatives of C-076 compounds, pharmaceutical compositions and method of use
    Patent number: 4412991
    Abstract: There is disclosed novel derivatives of C-076 compounds wherein the 22-position, normally substituted, is substituted with a hydroxy group. The compounds are isolated from the C-076 fermentation broth of Streptomyces avermitilis. The compounds have potent anthelmintic, insecticidal, and acaricidal activity and compositions for that use are also disclosed.
    Type: Grant
    Filed: August 28, 1981
    Date of Patent: November 1, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Robert E. Ormond
  • Anti-emetic esters of cyproheptadine-3-carboxylic acid and structurally related compounds
    Patent number: 4412999
    Abstract: Certain esters of cyproheptadine-3-carboxylic acid and its bioisosteres are peripherally selective dopamine antagonists useful in the treatment of emesis caused by stimulation of dopamine receptors of the chemoreceptor trigger zone, as well as emesis and nausea resulting from other causes including post operative emesis, chronic pediatric vomiting, radiotherapy and chemotherapy induced emesis, and nausea associated with migrane attacks and dysmenorrhea or arising idiopathically.They are also useful in the treatment of gastrointestinal disorders, such as gastro-oesophageal reflux caused by stimulation of dopamine receptors in the stomach or other causes and dyspepsia arising from delayed gastric emptying, post prandial dyspepsia or dyspepsia of unknown etiology.
    Type: Grant
    Filed: April 14, 1982
    Date of Patent: November 1, 1983
    Assignee: Merck & Co., Inc.
    Inventors: David C. Remy, Bradley V. Clineschmidt
  • Process for removal of homogeneous catalyst group VIII metals from process streams
    Patent number: 4413118
    Abstract: Organic sulfur compounds containing a carbon-sulfur double bond are used to remove homogeneous catalyst group VIII metals from chemical process streams.
    Type: Grant
    Filed: March 2, 1981
    Date of Patent: November 1, 1983
    Assignee: Merck & Co., Inc.
    Inventors: F. Edward Roberts, Victor J. Grenda
  • 6-Amidino-9-substituted benzyl purines
    Patent number: 4407802
    Abstract: This invention is concerned with 6-(substituted amidino-9-substituted benzyl purine derivatives and in particular 6-(aminomethylideneamino)-9-substituted benzyl purines. The compounds are active anticoccidial agents and suitable compositions and methods are described for the administration of such compounds to poultry for the prevention and treatment of coccidiosis.
    Type: Grant
    Filed: September 28, 1981
    Date of Patent: October 4, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Donald W. Graham, Gary H. Rasmusson, Richard L. Tolman