Patents Represented by Attorney Frank M. Mahon
  • Patent number: 4388306
    Abstract: A complex of polyriboinosinic-polyribocytidylic acid (poly I:C) with poly-L-lysine hydrobromide ([lysine.HBr].sub.n) having a defined molecular weight is prepared which is about 5-15 times as resistant to hydrolysis by pancreatic ribonuclease as the parent poly I:C. A pharmaceutical solution, containing a relatively high concentration of the complex, prepared as described, induces significant antiviral levels of serum interferon in monkeys under conditions in which poly I:C itself induces little or no interferon. An important feature of this invention is that the product is a soluble material requiring no special solubilizing agent, thereby facilitating the preparation of solutions having the desired concentration. The product will hereinafter be designated as poly I:C/poly-L-lysine.
    Type: Grant
    Filed: February 8, 1982
    Date of Patent: June 14, 1983
    Assignee: Merck & Co., Inc.
    Inventors: A. Kirk Field, Alfred A. Tytell, George P. Lampson
  • Patent number: 4386066
    Abstract: A vesicular, immunogenic, non-pyrogenic complex is obtained from isolates of N. gonorrhoeae by cultivating N. gonorrhoeae on a suitable nutrient medium; harvesting and centrifuging the cells; extracting the cell pellet with TRITON X-100 at alkaline pH; suspending the solids remaining after extraction in aqueous medium and precipitating in the cold with ethanol.
    Type: Grant
    Filed: August 20, 1981
    Date of Patent: May 31, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Edward C. O'Rourke, W. Wardle Fullerton
  • Patent number: 4358447
    Abstract: Disclosed are antibiotic cephalosporins (I) of the formula: ##STR1## Wherein the stylized radical attached to the 7-amino nitrogen of the cephalosporin moiety represents a nitrogen-containing heterocyclic group (mono- or polycyclic); R is, inter alia, hydrogen, alkyl, heterocyclylalkyl, aryl, alkenyl, aralkyl, --NR.sub.2, --OR, COOR, CONR.sub.2 or CN; A is conventionally known in the cephalosporin art; and R.sup.2 is H, or lower alkoxyl. Also disclosed are the pharmaceutically acceptable salt and ester derivatives of I; processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
    Type: Grant
    Filed: April 27, 1979
    Date of Patent: November 9, 1982
    Assignee: Merck & Co., Inc.
    Inventor: John Hannah
  • Patent number: 4349687
    Abstract: Disclosed is a process for the stereocontrolled total synthesis of thienamycin via intermediates II and IIa: ##STR1## wherein R is a readily removable carboxyl protecting group.
    Type: Grant
    Filed: April 8, 1981
    Date of Patent: September 14, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Thomas M. H. Liu, David G. Melillo, Kenneth M. Ryan, Ichiro Shinkai, Meyer Sletzinger
  • Patent number: 4348325
    Abstract: Disclosed is methyl 3-azido-4-C-cyano-2,3,4,6-tetradeoxy-.alpha.-D-arabino-hexopyranoside and processes for its preparation from methyl 3-azido-2,3,6-trideoxy-.alpha.-D-arabino-hexopyranoside via the 4-bromo-4-deoxy intermediate; wherein the two inversions of configuration at C-4 result in a net retention of the .alpha.-D-arabino stereochemistry.
    Type: Grant
    Filed: March 30, 1981
    Date of Patent: September 7, 1982
    Assignee: Merck & Co., Inc.
    Inventor: Philippe L. Durette
  • Patent number: 4344885
    Abstract: Disclosed is a process for the stereocontrolled total synthesis of thienamycin from acetone dicarboxylate via intermediate II: ##STR1## wherein R is a readily removable carboxyl protecting group.
    Type: Grant
    Filed: April 17, 1981
    Date of Patent: August 17, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Thomas M. H. Liu, David G. Melillo, Kenneth M. Ryan, Ichiro Shinkai, Meyer Sletzinger
  • Patent number: 4343937
    Abstract: Process and intermediate products useful in the preparation of cephalosporin compounds having a substituent at the 7-position in place of hydrogen are provided. The new cephalosporin compounds are active against various gram-negative and gram-positive organisms.
    Type: Grant
    Filed: April 30, 1980
    Date of Patent: August 10, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, Sandor Karady, Lovji D. Cama, Meyer Sletzinger
  • Patent number: 4342869
    Abstract: Process and intermediate products useful in the preparation of cephalosporin compounds having a substituent at the 7-position in place of hydrogen are provided. The new cephalosporin compounds are active against various gram-negative and gram-positive organisms.
    Type: Grant
    Filed: April 30, 1980
    Date of Patent: August 3, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, Sandor Karady, Lovji D. Cama, Meyer Sletzinger
  • Patent number: 4342757
    Abstract: Process and intermediate products useful in the preparation of cephalosporin compounds having a substituent at the 7-position in place of hydrogen are provided. The new cephalosporin compounds are active against various gram-negative and gram-positive organisms.
    Type: Grant
    Filed: April 30, 1980
    Date of Patent: August 3, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, Sandor Karady, Lovji D. Cama, Meyer Sletzinger
  • Patent number: 4341706
    Abstract: Disclosed is a process for the synthesis of carbapenem antibiotics I and their pharmaceutically acceptable salts and esters from 1: ##STR1## wherein: R.sup.7, R.sup.6, R.sup.1, R.sup.2 and R.sup.8 are selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, spirocycloalkyl, cycloalkylalkyl, alkylcycloalkyl, aryl, aralkyl, aralkenyl, aralkynyl, heteroalkyl, heteroaralkyl, heterocyclyl and heterocyclyalkyl.
    Type: Grant
    Filed: October 10, 1980
    Date of Patent: July 27, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, David H. Shih
  • Patent number: 4341791
    Abstract: Disclosed are S-oxides of 6-, 2- and 1,1-disubstituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein: n is 1 or 2; and R.sup.1, R.sup.2, R.sup.6, R.sup.7 and R.sup.8 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl. Such compounds as well as their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
    Type: Grant
    Filed: October 10, 1980
    Date of Patent: July 27, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, David H. Shih
  • Patent number: 4340673
    Abstract: Certain glucans modify the biosynthetic route of extracellular polysaccharides involved in dental plaque development causing critical loss of adhesiveness. They interfere with the biosynthesis of cell-bound polysaccharides reducing and preventing agglutination of cells. They thus aid in the prevention of dental plaque formation or concomitant dental caries and periodontal disease.
    Type: Grant
    Filed: November 7, 1980
    Date of Patent: July 20, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Thomas H. Stoudt, Karl H. Nollstadt
  • Patent number: 4338438
    Abstract: Process and intermediate products useful in the preparation of cephalosporin compounds having a substituent at the 7-position in place of hydrogen are provided. The new cephalosporin compounds are active against various gram-negative and gram-positive organisms.
    Type: Grant
    Filed: April 30, 1980
    Date of Patent: July 6, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, Sandor Karady, Lovji D. Cama, Meyer Sletzinger
  • Patent number: 4338437
    Abstract: Process and intermediate products useful in the preparation of cephalosporin compounds having a substituent at the 7-position in place of hydrogen are provided. The new cephalosporin compounds are active against various gram-negative and gram-positive organisms.
    Type: Grant
    Filed: April 30, 1980
    Date of Patent: July 6, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, Sandor Karady, Lovji D. Cama, Meyer Sletzinger
  • Patent number: 4335212
    Abstract: Disclosed is a fermentation process for preparing and isolating the antibiotic, (5R,6S,8S)-3-(2-aminoethylthio)-6-(1-hydroxyethyl)-7-oxo-1-azabicyclo[3.2. 0]hept-2-ene-2-carboxylic acid in substantially pure form.
    Type: Grant
    Filed: June 17, 1981
    Date of Patent: June 15, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth E. Wilson, August J. Kempf
  • Patent number: 4335101
    Abstract: Enzymes called cariogenanases, elaborated by microorganisms are isolated and characterized as polysaccharases capable of degrading cariogenan, a newly discovered glucan of dental plaque composed of .alpha.-(1.fwdarw.3) and .alpha.-(1.fwdarw.2) linkages. The enzymes are isolable from culture broths of various organisms by protein precipitation methods, and have utility as an anti-dental plaque agent, either as the sole enzymatic agent or in combination with dextranases and/or plaque dispersing proteases.
    Type: Grant
    Filed: June 21, 1973
    Date of Patent: June 15, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Thomas H. Stoudt, Karl H. Nollstadt
  • Patent number: 4330624
    Abstract: The antibiotic Tunicamycin is produced by fermenting a Tunicamycin-producing strain of Streptomyces (Streptomyces griseus ATCC 31591) under controlled conditions in a suitable nutrient medium and isolating the antibiotic so produced from the fermentation medium.
    Type: Grant
    Filed: December 3, 1980
    Date of Patent: May 18, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Enrique Tejera, Sara A. Currie, James E. Flor, Richard L. Monaghan
  • Patent number: 4324890
    Abstract: Process and intermediate products useful in the preparation of cephalosporin compounds having a substituent at the 7-position in place of hydrogen are provided. The new cephalosporin compounds are active against various gram-negative and gram-positive organisms.
    Type: Grant
    Filed: April 30, 1980
    Date of Patent: April 13, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, Sandor Karady, Lovji D. Cama, Meyer Sletzinger
  • Patent number: 4324900
    Abstract: Disclosed is a chiral, total synthesis of thienamycin from D-glucose, which proceeds via intermediates I, II, and III and joins aldehyde IV or acid V, which are known to be useful in the total synthesis of thienamycin (VI): ##STR1## wherein R.sup.1 is hydrogen or a removable protecting group;R is lower alkyl having 1-6 carbon atoms or bi-valent alkyl having 2-6 carbon atoms which joins the two sulfur atoms.
    Type: Grant
    Filed: March 30, 1981
    Date of Patent: April 13, 1982
    Assignee: Merck & Co., Inc.
    Inventor: Philippe L. Durette
  • Patent number: 4321197
    Abstract: Antibiotic 1-carba-6-(1-hydroxyethyl-2-carbonyl-penem-3-carboxylic acid is prepared by total chemical synthesis from 4-iodomethyl-1-(t-butyldimethylsilyl)-2-azetidinone.
    Type: Grant
    Filed: December 24, 1980
    Date of Patent: March 23, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Lovji D. Cama, Ravindra Guthikonda, Burton G. Christensen