Patents Represented by Attorney J. Jerome Behan
  • Patent number: 4343802
    Abstract: 2-(3-Substituted amino-2-hydroxypropoxy)-3-substituted pyrazine compounds optionally having substituents in the 5 and/or 6 positions, possessing .beta.-adrenergic blocking properties are described. The products are prepared by reaction of a 2-chloro (or hydroxy) pyrazine with a 5-hydroxymethyl (or sulfonyloxymethyl) oxazolidine followed by acid hydrolysis.
    Type: Grant
    Filed: July 3, 1980
    Date of Patent: August 10, 1982
    Assignee: Merck, Sharp & Dohme (I.A.) Corp.
    Inventors: Burton K. Wasson, Leonard M. Weinstock
  • Patent number: 4215121
    Abstract: Organic chemical compounds based upon the urea molecule are disclosed which have potent gastric secretion inhibitory properties. The urea is substituted with a 6 membered heterocyclic substituent containing 2 or 3 heteroatoms, and also with a substituted amino alkyl group. Further substitution is also possible. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.
    Type: Grant
    Filed: November 8, 1978
    Date of Patent: July 29, 1980
    Assignee: Merck & Co., Inc.
    Inventor: William A. Bolhofer
  • Patent number: 4146642
    Abstract: Certain novel substituted imidazo [1,2-a] pyridines with a substituted amino group at the 2- or 3- position and a heterocyclic moiety on the pyrido portion of the molecule are active anthelmintic agents. The heterocyclic moiety is connected to the imidazo [1,2-a] pyridine molecule through an oxygen, sulfur, sulfinyl or sulfone. The novel compounds are prepared from the appropriately substituted 2-amino pyridine precursor. Compositions which utilize said novel imidazo [1,2-a] pyridines as the active ingredient thereof for the treatment of helminthiasis are also disclosed.
    Type: Grant
    Filed: May 30, 1978
    Date of Patent: March 27, 1979
    Assignee: Merck & Co., Inc.
    Inventors: Richard J. Bochis, Richard L. Tolman
  • Patent number: 4144338
    Abstract: Organic chemical compounds based upon the urea molecule are disclosed which have potent gastric secretion inhibitory properties. The urea is substituted with a 6 membered heterocyclic substituent containing 2 or 3 heteroatoms, and also with a substituted amino alkyl group. Further substitution is also possible. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.
    Type: Grant
    Filed: February 17, 1977
    Date of Patent: March 13, 1979
    Assignee: Merck & Co., Inc.
    Inventor: William A. Bolhofer
  • Patent number: 4134973
    Abstract: Carbohydrate derivatives of the antibiotic substance milbemycin, also identified as B-41, and of 13-hydroxy milbemycin are prepared. The carbohydrate groups are attached to the available hydroxy groups of milbemycin and to the hydroxy group synthesized at the 13-position. The reactions may be made selectively such that more than one carbohydrate group may be attached to a single position, or that multiple carbohydrate groups may be attached at different positions on the molecule. The described carbohydrate derivatives have antiparasitic activity.
    Type: Grant
    Filed: April 11, 1977
    Date of Patent: January 16, 1979
    Assignee: Merck & Co., Inc.
    Inventors: Michael H. Fisher, Richard L. Tolman
  • Patent number: 4096264
    Abstract: Certain novel substituted imidazo [1,2-a] pyridines with a substituted amino group at the 2- or 3-position are active anthelmintic agents. The novel compounds are prepared from the appropriate substituted 2-aminopyridine precursor. Compositions which utilize said novel imidazo [1,2-a] pyridines as the active ingredient thereof for the treatment of helminthiasis are also disclosed.
    Type: Grant
    Filed: August 26, 1976
    Date of Patent: June 20, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Richard J. Bochis, Peter Kulsa
  • Patent number: 4093657
    Abstract: The invention disclosed herein relates to a novel process for preparing the monomer, 3-[N-(3-chloropropyl)methylamino]-N,N,N-trimethyl-propan-1-aminium chlorid e, which comprises reacting N,N-bis(3-chloropropyl)methylamine with trimethylamine. The 3,3-ionene monomer thus obtained is a key intermediate for making the linear, unbranched, non-cross-linked polymer, poly-[{methyl-(3-trimethylammoniopropyl)imino}trimethylene dichloride], which is valuable as an oral bile acid sequestrant.
    Type: Grant
    Filed: April 9, 1976
    Date of Patent: June 6, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Erwin F. Schoenewaldt, Paul Sohar
  • Patent number: 4092413
    Abstract: The invention disclosed herein relates to antiandrogenic compositions active, in vivo, as inhibitors of the aggregation of mammalian blood platelets, and to the method of preventing, arresting or reversing blood platelet aggregation by the administration to mammals of such antiandrogenic compositions.
    Type: Grant
    Filed: June 23, 1977
    Date of Patent: May 30, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Glen E. Arth, Sumner Wood, Jr., deceased
  • Patent number: 4091104
    Abstract: Novel cyano substituted (3-loweralkylamino-2-R.sub.1 O-propoxy)pyridines, their pharmaceutically acceptable salts and their preparation are disclosed. The pyridines are vasodilators having antihypertensive activity of rapid onset and extended duration and reduced tendency to cause undesirable tachychardia; they are also .beta.-adrenergic blocking agents.
    Type: Grant
    Filed: March 7, 1977
    Date of Patent: May 23, 1978
    Assignee: Merck & Co., Inc.
    Inventor: John J. Baldwin
  • Patent number: 4071478
    Abstract: The invention disclosed herein relates to novel partially cross-linked, fully quaternized poly-[(methylimino)trimethylene] polymers wherein a minor proportion (1% to 20%) of the nitrogen atoms in adjacent poly-[(methylimino)trimethylene] linear chains are, by quaternization, joined through trimethylene or 2-hydroxy-trimethylene bridges, the non-cross-linked nitrogens in the said linear chains being fully quaternized with lower alkyl or trialkylammoniopropyl groupings; and to the novel process for preparing these partially cross-linked, fully quaternized polymers which comprises reacting poly-[(methylimino)trimethylene] with 0.01 to 0.2 equivalents of 1,3-dihalo-propane or 1,3-dihalo-2-hydroxypropane per equivalent of tertiary amine in said poly-[(methylimino)trimethylene], and subsequently reacting the resulting product with excess alkyl halide or 3-halopropyltrialkylammonium halide.
    Type: Grant
    Filed: June 7, 1976
    Date of Patent: January 31, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Tsung-Ying Shen, Arthur F. Wagner
  • Patent number: 4067987
    Abstract: Anthelmintically active 3-loweralkyl-1,2,4-oxadiazoles are stabilized by the formation of homogeneous mixtures thereof with water and with certain alcohols, the molar ratio of stabilizer to oxadiazole being adjusted to within 0.1:1 to 2:1 to achieve required stability.
    Type: Grant
    Filed: January 9, 1976
    Date of Patent: January 10, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Michael H. Fisher, George B. Smith, Dale R. Hoff
  • Patent number: 4066661
    Abstract: Substituted trichloroacetamidine derivatives are prepared by treating an appropriately substituted imidate with ammonia. The imidate intermediates are prepared by treating an appropriately substituted amine with an imidating reagent.
    Type: Grant
    Filed: June 1, 1976
    Date of Patent: January 3, 1978
    Assignee: Merck & Co., Inc.
    Inventor: George H. Denny
  • Patent number: 4065464
    Abstract: Substituted trichloroacetamidine derivatives are prepared by reacting trichloroacetamidine with an appropriately substituted compound also substituted with a suitable leaving group. The leaving groups are halogen, quaternary or tertiary amines, methanesulfonate, toluenesulfonate, and the like.
    Type: Grant
    Filed: June 1, 1976
    Date of Patent: December 27, 1977
    Assignee: Merck & Co., Inc.
    Inventors: George H. Denny, Walfred S. Saari
  • Patent number: 4065465
    Abstract: Substituted trichloroacetamidine derivatives are prepared by reacting an appropriately substituted amine with trichloroacetamidine or a trichloroacetimidate. The substituted amines are 3-aminomethyl indole and 2-acetoxy-3-phenoxy propylamine.
    Type: Grant
    Filed: June 1, 1976
    Date of Patent: December 27, 1977
    Assignee: Merck & Co., Inc.
    Inventor: George H. Denny
  • Patent number: 4064239
    Abstract: Novel substituted benzenedisulfonamides are disclosed which compounds are active anthelmintic agents being particularly useful against fascioliasis in sheep and cattle. Specifically the active compounds are 4-amino-1,3-benzenedisulfonamide with an unsaturated substituted alkyl group. Compositions and methods containing the novel substituted benzenedisulfonamides for use in anthelmintic therapy particularly against liver fluke are also disclosed.
    Type: Grant
    Filed: September 26, 1975
    Date of Patent: December 20, 1977
    Assignee: Merck & Co., Inc.
    Inventor: Helmut H. Mrozik
  • Patent number: 4062952
    Abstract: Substituted benzenedisulfonamides are disclosed, which are active anthelmintic agents being particularly useful against fascioliasis in sheep and cattle. Specifically the active compounds are 4-amino-1,3-benzenedisulfonamide compounds substituted at the 6-position with certain alkyl groups. Compositions and methods containing the novel substituted benzenedisulfonamides for use in anthelmintic therapy, particularly against liver fluke are also disclosed.
    Type: Grant
    Filed: November 24, 1975
    Date of Patent: December 13, 1977
    Assignee: Merck & Co., Inc.
    Inventor: Helmut H. Mrozik
  • Patent number: 4061732
    Abstract: The nutritional disease, lactic acidosis, is successfully prevented by orally administering to the animal an effective amount of a sulfur-containing peptide antibiotic. In particular thiopeptin and thiostrepton are particularly effective sulfur-containing peptide antibiotics useful against lactic acidosis.
    Type: Grant
    Filed: November 8, 1976
    Date of Patent: December 6, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Larry A. Muir, Albert Barreto
  • Patent number: 4055645
    Abstract: Novel pharmaceutical compositions are disclosed which comprise a hypotensive agent and a phenyl hydrazino substituted propionic acid decarboxylase inhibitor. The compositions have enhanced anti-hypertensive activity.
    Type: Grant
    Filed: February 13, 1976
    Date of Patent: October 25, 1977
    Assignee: Merck & Co., Inc.
    Inventor: Alexander Scriabine
  • Patent number: 4053602
    Abstract: 5-Deazariboflavin, its phosphate ester and non-toxic salts thereof and its novel bis(loweralkoxymethylene) derivatives have antiprotozoal and antiparasitic activity. They are particularly useful for controlling cecal and/or intestinal coccidiosis when administered in minor quantities to animals, in particular to poultry, usually in admixture with animal sustenance. The compounds are included in compositions useful for the prevention and treatment of coccidiosis in poultry.
    Type: Grant
    Filed: November 2, 1976
    Date of Patent: October 11, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Donald W. Graham, Edward F. Rogers, Wallace T. Ashton
  • Patent number: 4048183
    Abstract: Compounds useful in the treatment of asthma, the symptoms of allergy and in some instances in gout and hyperuricemia are described. The novel compounds are 1-substituted-1,2,4-triazoles being additionally substituted at the 3- and 5-positions with a pyridyl radical. Methods of preparing these tri-substituted triazoles are described.
    Type: Grant
    Filed: April 2, 1976
    Date of Patent: September 13, 1977
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Frederick C. Novello