Patents Represented by Attorney Frank M. Mahon
  • Patent number: 4312871
    Abstract: Disclosed are 6-, 1- and 2-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein: 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: December 3, 1979
    Date of Patent: January 26, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, David H. Shih
  • Patent number: 4311704
    Abstract: Disclosed are substituted N-methylene derivatives of thienamycin having the formula: ##STR1## wherein: (1.) X.dbd.--NR.sup.1 R.sup.2, and Y.dbd.--R'--N.dbd.CRNR.sup.1 R.sup.2, and(2.) X.dbd.R, and Y.dbd.--NR.sup.1 R'N.dbd.CRNR.sup.1 R.sup.2 ; andwherein: R is, inter alia, hydrogen, NH.sub.2, --NHR.sup.1, --NR.sup.1 R.sup.2, R.sup.1 and R.sup.2 ; R.sup.1 and R.sup.2 are independently selected from: hydrogen, substituted, or unsubstituted: alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, and heterocyclylalkyl; R' is --(CH.sub.2).sub.n.sup.-, n is 1-6, or --(CH.sub.2).sub.m --Q--(CH.sub.2).sub.p.sup.-, m, n.dbd.1-3 and Q is O, S or R' is a carbocyclic or heterocyclic ring. Such compounds and their pharmaceutically acceptable salt, ether, ester and amide derivatives are useful as antibiotics.
    Type: Grant
    Filed: June 16, 1980
    Date of Patent: January 19, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, William J. Leanza, David H. Shih, Kenneth J. Wildonger
  • Patent number: 4311693
    Abstract: The antibiotic MSD A63A, having antibacterial and growth-permittant activity, is produced by fermentation of Streptoverticillum hiroshimense MA4845 (ATCC 31586), in a suitable nutrient media.
    Type: Grant
    Filed: November 17, 1980
    Date of Patent: January 19, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Sebastian Hernandez, Sheldon B. Zimmerman, Vincent P. Gullo, Ray S. Dewey
  • Patent number: 4309438
    Abstract: Disclosed are N-alkyl-N-iminomethyl derivatives of thienamycin which may be represented by the following structural formula: ##STR1## wherein R.sup.5 is, inter alia, alkyl, alkenyl, aryl, or aralkyl, R.sup.6 is selected from R, OR, SR and NR.sup.1 R.sup.2 wherein R is, inter alia, hydrogen and substituted or unsubstituted: alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, and heterocyclylalkyl; and R.sup.1 and R.sup.2 are hydrogen or R. Such compounds, including their O-- and carboxyl derivatives are useful as antibiotics. Also dislosed 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: March 31, 1980
    Date of Patent: January 5, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, William J. Leanza, Kenneth J. Wildonger
  • Patent number: 4304867
    Abstract: The antibiotic thienamycin is active against both gram-positive and gram-negative bacteria. The antibiotic is produced by growing a newly-found and hitherto undescribed species of Streptomyces on suitable fermentation media.
    Type: Grant
    Filed: January 3, 1978
    Date of Patent: December 8, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Jean S. Kahan, Frederick M. Kahan, Edward O. Stapley, Robert T. Goegelman, Sebastian Hernandez
  • Patent number: 4304859
    Abstract: There is disclosed a new antibiotic agent, A73A, produced by Streptomyces viridifaciens MA-4864 (ATCC 31495) under suitable conditions. Said antibiotic shows antibacterial and growth-permittant activity.
    Type: Grant
    Filed: October 27, 1980
    Date of Patent: December 8, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Ray S. Dewey, James E. Flor, Sheldon B. Zimmerman, Patrick J. Cassidy, Satoshi Omura, Ruiko Oiwa
  • Patent number: 4296111
    Abstract: Disclosed are antibiotic 7-(substituted methyl) cephalosporins, derivatives and nuclear analogues thereof; wherein the methyl substituent is, inter alia, hydroxyl, ketonic oxygen, imino nitrogen, amino or thio. Also disclosed are processes for the preparation of such compounds and their pharmaceutically acceptable salt, ester and amide derivatives; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
    Type: Grant
    Filed: June 14, 1979
    Date of Patent: October 20, 1981
    Assignee: Merck & Co. Inc.
    Inventors: Thomas R. Beattie, Burton G. Christensen, Frank P. Dininno
  • Patent number: 4290966
    Abstract: Traumatin, 12-oxo-trans (E) -10-docecenoic acid, is prepared from 10-oxomethyldecanoate by reaction with (triphenylphosphoranylene)acetaldehyde to form 12-oxomethyldodecenoate; blocking the 12-oxo group; hydrolyzing the ester group; and deblocking the 12-oxo group.
    Type: Grant
    Filed: October 3, 1980
    Date of Patent: September 22, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Jeannette E. Brown, Edward F. Rogers, Donald W. Graham
  • Patent number: 4283397
    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 H or is conventionally known in the cephalosporin art; R.sup.2 is H, or loweralkoxyl; p is 1 or 2; and R.degree. is H or CH.sub.3. 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: August 1, 1979
    Date of Patent: August 11, 1981
    Assignee: Merck & Co., Inc.
    Inventor: John Hannah
  • Patent number: 4283402
    Abstract: This invention relates to a new class of penicillins (I) and their pharmaceutically acceptable salts which are useful as antibiotics: ##STR1## wherein the stylized radical (hereafter referred to as R'): ##STR2## attached to the 6-amino nitrogen moiety of the penicillin nucleus represents a mono- or polycyclic N-containing heterocyclic group; and R is, inter alia, hydrogen, substituted and unsubstituted: alkyl, aryl, alkenyl, heterocyclylalkyl, heterocyclylalkenyl, aralkenyl, aralkyl, --NR.sub.2, COOR, CONR.sub.2,--OR, or CN.
    Type: Grant
    Filed: August 1, 1979
    Date of Patent: August 11, 1981
    Assignee: Merck & Co., Inc.
    Inventor: John Hannah
  • Patent number: 4282365
    Abstract: Novel dibenz[b,e]oxepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma.
    Type: Grant
    Filed: November 24, 1978
    Date of Patent: August 4, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Joshua Rokach, Edward J. Cragoe, Jr., Clarence S. Rooney
  • Patent number: 4282322
    Abstract: This invention relates to two new antibiotics, desacetyl 890A.sub.1 and desacetyl 890A.sub.3, active against both gram-positive and gram-negative bacteria, which are produced by treating 890A.sub.1 and 890A.sub.3, respectively, with an N-acetylthienamycin amidohydrolase produced by a soil microorganism isolated by enrichment techniques. This invention also relates to the process whereby N-acetylated structures of the thienamycin class of antibiotics such as N-acetyl thienamycin can be enzymatically deacetylated.
    Type: Grant
    Filed: August 27, 1979
    Date of Patent: August 4, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Jean S. Kahan, Frederick M. Kahan
  • Patent number: 4282219
    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; R.degree. is hydrogen or methyl; and R.sup.2 is H, or loweralkoxyl. 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: August 1, 1979
    Date of Patent: August 4, 1981
    Assignee: Merck & Co., Inc.
    Inventor: John Hannah
  • Patent number: 4271159
    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; R.sup.o is H or CH.sub.3 ; and R.sup.2 is H, or loweralkoxyl: 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: August 1, 1979
    Date of Patent: June 2, 1981
    Assignee: Merck & Co., Inc.
    Inventor: John Hannah
  • Patent number: 4269873
    Abstract: Disclosed are 2-, 5- and 6-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are, inter alia, independently selected from the group consisting of hydrogen, (R.sup.9 is not 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 and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
    Type: Grant
    Filed: July 25, 1979
    Date of Patent: May 26, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, David B. R. Johnston, Susan M. Schmitt
  • Patent number: 4267188
    Abstract: Disclosed are 1-carba-pen-2-em-3-carboxylic acids of the following structure: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are, inter alia, independently selected from the group consisting of hydrogen (R.sup.4 is not hydrogen), alkyl, 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: August 9, 1979
    Date of Patent: May 12, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Lovji D. Cama, Burton G. Christensen
  • Patent number: 4264736
    Abstract: The antibiotic MSD 890A.sub.10 and pharmaceutically acceptable salts thereof (hereinafter referred to as antibiotic 890A.sub.10) is active against both gram-positive and gram-negative bacteria. The antibiotic is produced by growing species of Streptomyces on suitable fermentation media.
    Type: Grant
    Filed: September 26, 1979
    Date of Patent: April 28, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Patrick J. Cassidy, Sheldon B. Zimmerman, Josefino B. Tunac, Sebastian Hernandez
  • Patent number: 4264621
    Abstract: Antibiotic 5-substituted-3-(2-aminoethylthio)-6-(1-hydroxyethyl)-7-oxo-1-azabicyclo[3 .2.0]hept-2-ene-2-carboxylic acids (I) are disclosed: ##STR1## wherein R is alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or heteroaryl.
    Type: Grant
    Filed: July 25, 1979
    Date of Patent: April 28, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, David B. R. Johnston, Susan M. Schmitt
  • Patent number: 4264734
    Abstract: This invention relates to the new antibiotic, desacetyl 890A.sub.10, active against both gram-positive and gram-negative bacteria, which is produced by treating 890A.sub.10 with an N-acetyl-890A.sub.10 amidohydrolase produced by a soil microorganism isolated by enrichment techniques. This invention also relates to the process by which 890A.sub.10 is enzymatically deacetylated.
    Type: Grant
    Filed: September 11, 1979
    Date of Patent: April 28, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Jean S. Kahan, Frederick M. Kahan
  • Patent number: 4264607
    Abstract: There is disclosed a new antibiotic agent, A40A, produced by Streptomyces lavedulae MA-4758 (ATCC 31312) under suitable conditions. Said antibiotic shows antibacterial and growth-permittant activity.
    Type: Grant
    Filed: September 13, 1979
    Date of Patent: April 28, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Ray S. Dewey, Vincent P. Gulla, Sheldon B. Zimmerman, Satoshi Omura, Ruiko Oiwa