Patents Represented by Attorney, Agent or Law Firm Richard C. Billups
  • Process for synthesizing carbapenem intermediates using a rhodium catalyst and lewis acid
    Patent number: 5493018
    Abstract: This invention relates to the synthesis of a bicyclic ketoester compound of the formula 1 obtained by cyclizing a diazo compound of formula 2: in the presence of a rhodium catalyst. ##STR1## By adding an effective amount of a Lewis acid to the cyclization reaction, the reaction selectively produces the 1-beta methyl isomer, and epimerization of the 1-beta methyl compound to the 1-alpha isomer is minimized.
    Type: Grant
    Filed: January 25, 1994
    Date of Patent: February 20, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Thomas Meng-Han Liu, Joseph E. Lynch, Ralph P. Volante
  • Anti-fungal agents
    Patent number: 5461071
    Abstract: A compound having the formula ##STR1## which is an anti-fungal agent is described. The producing organism Colletotricum accutatum is also described, along with a method of production.
    Type: Grant
    Filed: October 21, 1994
    Date of Patent: October 24, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Evon A. Bolessa, Robert E. Schwartz, Gerald F. Bills, Robert A. Giacobbe, Fernando Pelaez Perez, Angeles Cabello Arroyo, Teresa Diez Matas, Isabel Martin Fernandez, Francisca Vincente Perez, Suzanne M. Mandala, Deborah L. Zink, Rosemary Thornton, John R. Thompson, James E. Curotto
  • 3-aryl of heteroaryl-7-heteroaralkylamido cephalosporin compounds, compositions and methods of use
    Patent number: 5455239
    Abstract: A compound of the formula I is disclosed. ##STR1## R.sup.13 represents hydrogen, NH.sub.2, C1-4 alkyl, C1-4 alkylamino or di(C1-4) alkylamino-;Y represents CH or N;Y" represents (a) CR.sup.y' R.sup.z' with R.sup.y' and R.sup.z' hydrogen, C1-6 alkyl, C.sub.3-8 cycloalkyl or C.sub.1-6 alkyl substituted with C.sub.3-8 cycloalkyl, or (b) N substituted with OR.sup.14 with R.sup.14 representing H, C.sub.1-4 alkyl or C.sub.1-4 alkyl substituted with COOH.Ar represents: ##STR2## One of R.sup.1 and R.sup.2 independently represent H, W as defined below or one of the groups (a) through (d) below, and the other represents H or W. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: August 5, 1993
    Date of Patent: October 3, 1995
    Assignee: Merck & Co. Inc.
    Inventors: Lovji D. Cama, James V. Heck
  • 1-.beta.-methyl-carbapenem, compositions containing same and methods of use
    Patent number: 5451579
    Abstract: A carbapenem antibiotic of the formula I ##STR1## is disclosed. The variable X.sup..crclbar. represents a counterion. Pharmaceutical compositions and methods of use are also disclosed.
    Type: Grant
    Filed: February 15, 1994
    Date of Patent: September 19, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Mark L. Greenlee, Frank P. DiNinno, Milton L. Hammond
  • Preparation of 2-aryl carbapenems via a boronic acid coupling reaction
    Patent number: 5442057
    Abstract: The present invention is directed to a process of making 2-Aryl Carbapenems of Formula 1 from a compound of formula 2.
    Type: Grant
    Filed: April 12, 1994
    Date of Patent: August 15, 1995
    Inventors: Ann Decamp, Ulf H. Dolling, Yulan Li, Dale L. Rieger, Nobuyoshi Yasuda, Lyndon C. Xavier
  • Preparation of 2-aryl carbapenems
    Patent number: 5442056
    Abstract: The present invention is directed to a process of making 2-aryl carbapenems of formula 1 from a compound of formula A.
    Type: Grant
    Filed: May 17, 1994
    Date of Patent: August 15, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Ann E. DeCamp, Edward J. J. Grabowski, Mark A. Huffman, Lyndon C. Xavier, Nobuyoshi Yasuda
  • 2-(3-pyridyl)-carbapenem antibacterial agents
    Patent number: 5409920
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: October 5, 1990
    Date of Patent: April 25, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Ravindra N. Guthikonda, Frank P. DiNinno
  • Bridged biphenyl carbapenem antibacterial compounds
    Patent number: 5401735
    Abstract: Carbapenems of the formula: ##STR1## are disclosed as useful antibacterial agents.
    Type: Grant
    Filed: August 2, 1993
    Date of Patent: March 28, 1995
    Assignee: Merck & Co., Inc.
    Inventor: Frank P. Dininno
  • Process of synthesizing binaphthyl derivatives
    Patent number: 5399771
    Abstract: A process of synthesizing a compound of the formula 1: ##STR1## is disclosed, which comprises reacting a compound of the formula 2: ##STR2## with diphenylphosphine in the presence of an amine base and a nickel catalyst to produce a compound of formula 1.
    Type: Grant
    Filed: June 1, 1994
    Date of Patent: March 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Dongwei Cai, Joseph F. Payack, Thomas R. Verhoeven
  • 6-amido-1-methyl-2-(substituted-thio)carbapenems
    Patent number: 5395931
    Abstract: New antibacterial 6-amido-1-methyl-2-(substituted-thio)-carbapenems and process for their synthesis involving new azetidinone intermediates.
    Type: Grant
    Filed: May 20, 1992
    Date of Patent: March 7, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Mark L. Greenlee, Frank P. DiNinno, Thomas N. Salzmann
  • Bridged biphenyl carbapenem compounds, compositions containing such compounds and methods of use
    Patent number: 5384317
    Type: Grant
    Filed: August 2, 1993
    Date of Patent: January 24, 1995
    Assignee: Merck & Co., Inc.
    Inventor: Frank P. DiNinno
  • (N-pyridiniumphenyl)-carbapenems
    Patent number: 5382575
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: October 7, 1992
    Date of Patent: January 17, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Alan D. Adams, Frank DiNinno, James V. Heck
  • Bridged carbapenem antibacterial compounds
    Patent number: 5374630
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: June 10, 1993
    Date of Patent: December 20, 1994
    Assignee: Merck & Co., Inc.
    Inventor: Frank P. DiNinno
  • Bridged carbapenem compounds, compositions containing such compounds and methods of use
    Patent number: 5372993
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents. Compositions containing such compounds and methods of use are also disclosed.
    Type: Grant
    Filed: June 10, 1993
    Date of Patent: December 13, 1994
    Assignee: Merck & Co., Inc.
    Inventor: Frank P. DiNinno
  • 2-(heterocyclylheteroaryliumalkyl) phenyl carbapenem antibacterial agents
    Patent number: 5362723
    Abstract: Carbapenems having the formula: ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: May 20, 1992
    Date of Patent: November 8, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. DiNinno, Thomas N. Salzmann, David A. Muthard
  • 2-(9-fluorenonyl)-carbapenem intermediates
    Patent number: 5356889
    Abstract: Disclosed are carbapenems of the formula ##STR1## which are 2-(9-fluorenonyl)-carbapenems useful as antibacterial agents. Intermediates for preparation of these compounds is also disclosed.
    Type: Grant
    Filed: October 26, 1992
    Date of Patent: October 18, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Mark L. Greenlee, Frank P. DiNinno, Lovji D. Cama, James V. Heck
  • Triazolyl and tetrazolyl phenyl substituted carbapenems, compositions containing such compounds and methods of use
    Patent number: 5350746
    Abstract: Triazolyl and tetrazolyl phenyl substituted carbapenems of the formula I are disclosed. ##STR1## One or two of the variables X, Y and Z represent nitrogen atoms. The heteroaryl ting may be charged or uncharged.Pharmaceutical compositions and methods of treatment are also disclosed.
    Type: Grant
    Filed: April 14, 1993
    Date of Patent: September 27, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Alan D. Adams, James V. Heck
  • 2-biphenyl-carbapenems
    Patent number: 5350846
    Abstract: Carbapenems of the formula: ##STR1## are useful intermediates to antibacterial agents.
    Type: Grant
    Filed: January 25, 1993
    Date of Patent: September 27, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. DiNinno, Thomas N. Salzmann
  • Boron containing intermediates useful in the preparation of carbapenems
    Patent number: 5338875
    Abstract: The present invention is directed to intermediates of the following formula which are useful in the preparation of Carbapenem-antibiotics ##STR1##
    Type: Grant
    Filed: November 19, 1992
    Date of Patent: August 16, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Ann DeCamp, Ulf H. Dolling, Yulan Li, Dale L. Rieger, Nobuyoshi Yasuda, Lyndon C. Xavier
  • MRSA active 2-phenyl-carbapenems
    Patent number: 5334590
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: July 16, 1993
    Date of Patent: August 2, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Frank DiNinno, Ravindra N. Guthikonda