Patents Represented by Attorney Raymond M. Speer
  • Patent number: 5149838
    Abstract: Disclosed is a process for the enantioselective synthesis of the compound of Formula I and related compounds. The process comprises the synthesis of the benzofuranyl carboxaldehyde; introduction of the benzylic amine functionality with control of the absolute stereochemistry; preparation of the azetidinone fragment and its coupling to the benzofuranyl amine fragments. The carboxylic acid in Formula I is liberated using heterogenous palladium catalyzed de-allylation of the allyl esters. Compounds I have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents.
    Type: Grant
    Filed: September 20, 1991
    Date of Patent: September 22, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Guy R. Humphrey, Ann M. Madar, Andrew S. Thompson
  • Patent number: 5143624
    Abstract: Poly(diallylamine) blended with poly(N-methylolacrylamide) effectively detackifies over-sprayed paint in the circulating water of a wet paint spray booth operation. After detackification the dispersed paint is flocculated with hydrolyzed polyacrylamide, the paint waste is removed, and the clarified water is recirculated back into the paint spray booth operation.
    Type: Grant
    Filed: May 2, 1991
    Date of Patent: September 1, 1992
    Assignee: Calgon Corporation
    Inventor: Lewis D. Morse
  • Patent number: 5141954
    Abstract: A new carbazate represented by the formula ##STR1## is found to be antifungal and especially useful in the treatment of mycotic infections caused by the Cryptococcus species.
    Type: Grant
    Filed: July 30, 1991
    Date of Patent: August 25, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Arthur A. Patchett, Frank VanMiddlesworth
  • Patent number: 5137884
    Abstract: N-tetrazolyl beta-lactams of the Formula: ##STR1## and the pharmaceutically acceptable salts thereof wherein R.sup.2 is hydrogen, alkyl having 1 to 6 carbon atoms or carboalkoxy having 2 to 7 carbon atoms; andZ is ##STR2## and W is ##STR3## thus forming a zwitterion, or Z is ##STR4## wherein R.sup.1 is benzyl, phenyloxymethyl or ##STR5## wherein Y is alkoxy or substituted alkoxy having 1 to 6 carbon atoms wherein the substituent on the alkoxy group is --COOH; andW is ##STR6## wherein R.sup.3 is H, M or --CH.sub.2 COOM, wherein M is a pharmaceutically acceptable cation are disclosed. The compounds are useful as antibiotics.
    Type: Grant
    Filed: November 16, 1983
    Date of Patent: August 11, 1992
    Assignee: Merck & Co., Inc.
    Inventors: W. Alexander Andrus, Burton G. Christensen, James V. Heck
  • Patent number: 5137657
    Abstract: An orthophosphate salt and sodium silicate, when used in a 3:1 ratio by weight, and in a concentration of 0.1 to 100 mg/L, are found to have a synergistic effect in controlling the corrosion of carbon steel in an aqueous system, e.g., a municipal water supply system. The synergistic combination is also useful in reducing lead solubility and leaching, and in stabilizing soluble iron and manganese and their reaction products.
    Type: Grant
    Filed: April 24, 1991
    Date of Patent: August 11, 1992
    Assignee: Merck & Co., Inc.
    Inventor: Bennett P. Boffardi
  • Patent number: 5110799
    Abstract: A series of carboxyl-containing N-alkyldipeptides have been found to posess antiviral potency--specifically against herpes simplex virus--by selectively inhibiting the viral ribonucleotide reductase enzyme.
    Type: Grant
    Filed: July 28, 1989
    Date of Patent: May 5, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Richard L. Tolman, Wallace T. Ashton, Mu T. Wu
  • Patent number: 5104800
    Abstract: A process for the one-step conversion of cephalosporin C and derivatives thereof to the corresponding 7-aminocephalosporanic acid and derivatives comprising treating said cephalosporin C and derivatives with a cephalosporin C amidase enzyme of a recited sequence, the DNA encoding said enzyme, and expression thereof in a suitable host, e.g., Bacillus species under the control of a suitable promoter.
    Type: Grant
    Filed: June 27, 1989
    Date of Patent: April 14, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Mark S. Crawford, David B. Finkelstein, John A. Rambosek
  • Patent number: 5093356
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of the 5-lipoxygenase enzyme. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
    Type: Grant
    Filed: January 16, 1990
    Date of Patent: March 3, 1992
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Yves Girard, Pierre Hamel, Daniel Delorme
  • Patent number: 5091300
    Abstract: Anti-hepatitis B virus surface protein (anti-HBS) antibody is adsorbed onto the surface of a substratum. Hepatitis B virus PreS2+S (PreS2+S) protein is then adsorbed onto the same surface through the interaction of the anti-HBS antibody with the "S" portion of the PreS2+S protein. The coated surface is then incubated concomitantly with the test sample and a radiolabelled antibody specific for the "PreS2" portion of the PreS2+S protein.
    Type: Grant
    Filed: August 3, 1989
    Date of Patent: February 25, 1992
    Assignee: Merck & Co., Inc.
    Inventors: William M. Hurni, William J. Miller
  • Patent number: 5087376
    Abstract: Multifunctional scale inhibitor compositions, alone or together with polymeric structures, are described which are characterized by having, in addition to a phosphonomethylamino group, a sulfonic acid and/or carboxylic acid group. By incorporating several types of functional groups into a single molecule, control of scale formation and deposition under more severe conditions than normally encountered can be attained.
    Type: Grant
    Filed: October 15, 1990
    Date of Patent: February 11, 1992
    Assignee: Calgon Corporation
    Inventors: Beverly Bendiksen, Leonard J. Persinski, Raymond J. Schaper
  • Patent number: 5076939
    Abstract: A novel method of treating circulating water containing over-sprayed water-based or solvent-based paint, such as in a paint spray booth operation, comprises adjusting the alkalinity of the paint spray booth water by adding an alkalinity source thereto, contacting the oversprayed paint with the alkalinity-adjusted water and with an alumina coated silica sol added to the water, adding an effective amount of a polymer floccing agent to the water, and removing resulting sludge from the water.
    Type: Grant
    Filed: May 2, 1991
    Date of Patent: December 31, 1991
    Assignee: Calgon Corporation
    Inventors: W. Eugene Hunter, Lewis D. Morse
  • Patent number: 5076941
    Abstract: Monofluorophosphate salts, especially sodium monofluorophosphate (Na.sub.2 PO.sub.3 F), when added to potable water sources in concentrations between 0.1 mg/L and 500 mg/L, significantly reduces lead (Pb) leaching into said water, producing the double benefit of reducing lead solubility and thus content in drinking water, while at the same time adding fluoride to that drinking water, with the anticaries benefit that fluoridation provides.
    Type: Grant
    Filed: October 15, 1990
    Date of Patent: December 31, 1991
    Assignee: Calgon Corp.
    Inventors: Bennett P. Boffardi, Ann M. Sherbondy
  • Patent number: 5075436
    Abstract: A multistep process is described for selectively obtaining 1-.beta.-methylcarbapenem intermediates in high overall yield. The desired 1-.beta.-methyl chirality is obtained through the hydrogenation of certain bicyclic .beta.-lactam ring structures containing an exocyclic methylene double bond alpha to the .beta.-lactam ring, in the presence of a metallic nickel hydrogenation catalyst. The hydrogenation results in a mixture of .alpha.- and .beta.-methyl isomers having a high .beta./.alpha.epimeric molar ratio. New 1-.beta.-methylcarbapenem intermediates containing the exocyclic double bond are also described.
    Type: Grant
    Filed: January 19, 1989
    Date of Patent: December 24, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Ichiro Shinkai, Anthony O. King, Lelia M. Fuentes
  • Patent number: 5073205
    Abstract: An improved method for detackifying over-sprayed paint, lacquer or enamel entrained in the circulating water of paint spray booths comprises maintaining in the wash water a small amount of an N-methylolacrylamide copolymer with methyldiallylamine.
    Type: Grant
    Filed: May 2, 1991
    Date of Patent: December 17, 1991
    Assignee: Merck & Co., Inc.
    Inventor: Lewis D. Morse
  • Patent number: 5064835
    Abstract: Novel hydroxymacrolide derivatives of the general structural Formula I: ##STR1## have been prepared from (a) suitable precursor(s) by selective reduction of the ketone at C-2. These macrolide immunosuppressants are useful in a human host for the treatment of autoimmune diseases (such as juvenile-onset diabetes melitus, multiple sclerosis and rheumatoid arthritis), infectious diseases and/or the prevention of rejection of foreign organ transplants, e.g. bone marrow and heart transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses such as: psoriasis, atopical dermatitiis, contact dermatitis and further eczematous dermatitises, seborrhoeic dermatitis, Lichen planus, Pemphigus, bullous Pemphigoid, Epidermolysis bullosa, urticaria, angioedemas, vasculitides, erythemas, cutaneous eospinphilias, Lupus erythematosus or Alopecia areata.
    Type: Grant
    Filed: March 1, 1990
    Date of Patent: November 12, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Richard J. Bochis, Huyn O. Ok, Matthew J. Wyvratt
  • Patent number: 5042472
    Abstract: A powder inhaler device not requiring a propellant is disclosed which comprises a unit dose package and delivery system which is breath actuated and permits a patient to inhale through the mouth a medication in powder form for administration to the bronchia and lungs. The powder dose is contained in a compartment of the device which is sealed off from the environment by a peel-off piece of lidding material. The compartment has two apertures: one over which the mouth of the patient is placed to receive the powder medication by inhalation; and the other which permits ingress of air to aerosolize the powder medication.
    Type: Grant
    Filed: October 15, 1990
    Date of Patent: August 27, 1991
    Assignee: Merck & Co., Inc.
    Inventor: Leonid Bunin
  • Patent number: 5030645
    Abstract: (S)-.alpha.-fluoromethylhistidine, a potent, selective, mechanism-based inhibitor of mammalian histidine carboxylase, the enzyme responsible for biosynthesis of histamine in mammals, is useful in the treatment of asthma.
    Type: Grant
    Filed: October 15, 1990
    Date of Patent: July 9, 1991
    Assignee: Merck & Co., Inc.
    Inventor: Janos Kollonitsch
  • Patent number: 5021426
    Abstract: Various 3-substituted cyproheptadine derivatives are useful in the treatment of infection by Plasmodium falciparum and in the treatment of malaria either as compounds, pharmaceutically acceptable salts, or pharmaceutical composition ingredients in combination with antimalarial agents or compounds. Methods of treating malaria and methods of treating infection by Plasmodium falciparum are also described.
    Type: Grant
    Filed: February 26, 1990
    Date of Patent: June 4, 1991
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gabriel F. Eilon, Paul A. Friedman, David C. Remy
  • Patent number: 5017603
    Abstract: The controlled aerobic fermentation of the fungal organism Fusarium lateritium var. longum produces xanthomegnin. Xanthomegnin has been discovered to have potent parasiticidal, anthelminthic, and insecticidal activity.
    Type: Grant
    Filed: March 21, 1990
    Date of Patent: May 21, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Dan A. Ostlind, Sagrario Mochales
  • Patent number: 5006466
    Abstract: Virginiamycin M.sub.1 having the Formula: ##STR1## and virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## Virginiamycin M.sub.1 and the analogs I-IV are antagonists of cholecystokinin (CCK) and gastrin. Cholecystokinin antagonists are useful as analgesics and in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems in animals, especially humans. Gastrin antagonists are useful in blocking the receptors for gastrin in humans and may function as agents for the treatment of ulcers, tumors or other gastrointestinal disorders. The compounds of Formulae I-IV are antibiotics and are useful as antimicrobial agents in animals including man and are useful as food additives to promote feed utilization in animals. Virginiamycin M.sub.1 and the analogs of Formula I, III and IV are produced by the controlled aerobic fermentation of a strain of Streptomyces olivaceus, ATCC No. 53527, while the analog of Formula II is produced by chemical synthesis.
    Type: Grant
    Filed: October 26, 1989
    Date of Patent: April 9, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Yiu-kuen T. Lam, Otto D. Hensens, Raymond S. Chang, Cheryl D. Schwartz, Deborah L. Zink