Patents Represented by Attorney, Agent or Law Firm Richard C. Billups
  • Process of producing 8A- and 9A-azalide antibiotics
    Patent number: 5332807
    Abstract: A process of producing 8a- and 9a- azalide compounds is disclosed, comprised of reacting an 8a- aza or 9a- aza azalide eastern fragment or a derivative thereof with a compound of the formula:X--A'--Ywherein X and Y are appropriate reactive groups and A' is a fragment or compound which forms the western portion of the azalide, andcyclizing this intermediate to form the target 8a- or 9a-azalide compound. Compounds of formula I, II and III as well as other azalides can be synthesized according to this process.
    Type: Grant
    Filed: April 14, 1993
    Date of Patent: July 26, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Sherman T. Waddell, Timothy A. Blizzard
  • Lipopeptide compounds
    Patent number: 5310726
    Abstract: Antifungal and antiparasital lipopeptide compounds stable in aqueous media are described. Stability in aqueous media render lipopeptides more useful for compositions for therapeutic applications.
    Type: Grant
    Filed: March 19, 1990
    Date of Patent: May 10, 1994
    Assignee: Merck & Co., Inc.
    Inventor: James M. Balkovec
  • Cyclohexapeptide compound
    Patent number: 5310873
    Abstract: A cyclohexapeptide base which is the nucleus of closely related antibiotics obtained by culturing Zalerion arboricola and its salts are described. They are useful intermediates for the preparation of new semisynthetic compounds having antimicrobial activity.
    Type: Grant
    Filed: March 12, 1990
    Date of Patent: May 10, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Dennis M. Schmatz, Jan S. Tkacz, Robert E. Schwartz, Mervyn Turner
  • Antibiotic producing microorganism
    Patent number: 5304485
    Abstract: An organism of the Sporormiella species produces a compound having the formula ##STR1## which is useful. The compound is useful as an antifungal agent.
    Type: Grant
    Filed: October 19, 1992
    Date of Patent: April 19, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Gerald F. Bills, Fernando Pelaez
  • 2-(aza-9-fluorenonyl)carbapenem antibacterial agents
    Patent number: 5294610
    Abstract: Carbapenems of the formula ##STR1## wherein a suitably substituted aza-9-fluorenone is attached at the 2-position of the carbapenem are useful antibacterial agents.
    Type: Grant
    Filed: October 15, 1992
    Date of Patent: March 15, 1994
    Assignee: Merck & Co. Inc.
    Inventors: Frank P. DiNinno, Ravindra N. Guthikonda
  • Antibiotic agents
    Patent number: 5276055
    Abstract: Compounds having the formula ##STR1## wherein R and R.sup.1 may be H or COCH.sub.3 provided that when R.sup.1 is COCH.sub.3, R is COCH.sub.3 are described.
    Type: Grant
    Filed: October 19, 1992
    Date of Patent: January 4, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Angeles Cabello, Guy Harris, Robert A. Giacobbe, Gregory L. Helms, Otto D. Hensens, Suzanne M. Mandala, E. Tracy T. Jones, Isabel Martin, Walter Rozdilsky
  • 2-(N-imidazoliumphenyl)-carbapenems
    Patent number: 5276149
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: October 17, 1991
    Date of Patent: January 4, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Alan D. Adams, James V. Heck
  • 2-phenyl-carbapenems
    Patent number: 5256777
    Abstract: Carbapenems of the formula ##STR1## are useful intermediates to antibacterial agents.
    Type: Grant
    Filed: October 17, 1991
    Date of Patent: October 26, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Frank DiNinno, Ravindra N. Guthikonda
  • (2-substituted phenyl) carbapenems
    Patent number: 5247074
    Abstract: Carbapenems of the formula: ##STR1## are useful intermediates to antibacterial agents.
    Type: Grant
    Filed: May 20, 1992
    Date of Patent: September 21, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. Dininno, Thomas N. Salzmann, Eugene D. Thorsett
  • Derivatives of virginiamycin M1
    Patent number: 5242938
    Abstract: Dicarbonyloxy, carbonyloxy, carbanilate, and dihydroxy derivatives of Virginiamycin M.sub.1 are useful antibiotics and effectively bind gastrin and brain CCK receptors.
    Type: Grant
    Filed: August 27, 1992
    Date of Patent: September 7, 1993
    Assignee: Merck & Co., Inc.
    Inventor: Yiu-Kuen T. Lam
  • Antimigraine alkyl indole
    Patent number: 5233050
    Abstract: An alkyl indole of the formula: ##STR1## is a useful antimigraine agent.
    Type: Grant
    Filed: February 7, 1992
    Date of Patent: August 3, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Robert P. Borris, Yiu-Kuen T. Lam, Lawrence Koupal
  • 10-AZA-9-deoxo-11-deoxy-erythromycin A and derivatives thereof
    Patent number: 5215980
    Abstract: Compounds of the formula: ##STR1## where R is hydrogen, C.sub.1 -C.sub.10 alkylcarbonyl, or C.sub.1 -C.sub.10 alkyl which can be substituted by amino or cyano, R.sup.1 and R.sup.2 are independently hydrogen, hydroxyl or amino, and the pharmaceutically aceptable salts and esters thereof. Pharmaceutical compositions and methods of their use are also provided for.
    Type: Grant
    Filed: January 17, 1992
    Date of Patent: June 1, 1993
    Assignee: Merck & Co., Inc.
    Inventor: Anthony B. Jones
  • 2-benzocoumarinyl-carbapenems
    Patent number: 5216146
    Abstract: Carbapenems of the formula ##STR1## are useful intermediates to antibacterial agents.
    Type: Grant
    Filed: May 24, 1991
    Date of Patent: June 1, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Frank DiNinno, Mark L. Greenlee, Thomas A. Rano
  • 2-phenanthridonyl-carbapenems
    Patent number: 5214139
    Abstract: Carbapenems of the formula ##STR1## wherein: P' is a removable protecting group for hydroxy; andM is a removable protecting group for carboxy;are useful intermediates for carbapenem antibiotics.
    Type: Grant
    Filed: April 16, 1991
    Date of Patent: May 25, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Frank DiNinno, Thomas A. Rano, Mark L. Greenlee
  • Methods of elaborating erythromycin fragments into amine-containing fragments of azalide antibiotics
    Patent number: 5210235
    Abstract: A method of making compounds of the formulae: ##STR1## wherein X is ##STR2## R.sup.1 is hydrogen, methyl, C.sub.1-10 alkoxycarbonyl or arylsulfonyl when X is CH.sub.3 CH.sub.2 CHNH.sub.2 and is additionally aralkoxycarbonyl when X is NH.sub.2 ; one of R.sup.2 and R.sup.3 is hydrogen and the other is OH, NHR.sup.1 or NMeR.sup.1 where R.sup.1 is as defined above; R.sup.4 is hydrogen or C.sub.1-10 alkyl when X is CH.sub.3 CH.sub.2 CHNH.sub.2 and is additionally aralkyl when X is NH.sub.2 ; R.sup.5 is hydrogen or C.sub.1-3 alkyl when X is CH.sub.3 CH.sub.2 CHNH.sub.2 ; R.sup.5 is hydrogen when X is NH.sub.2 ; one of R6 and R7 is hydrogen and the other is methyl except when X is CH.sub.3 CH.sub.2 CHNH.sub.2 and R.sup.2 is H, in which case R.sup.6 is methyl and R.sup.7 is hydrogen. These compounds are made from erythromycin-derived fragments of the formulae: ##STR3## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined as before for when X is NH.sub.2 ; R.sup.5 is hydrogen or C.sub.1-3 alkyl; if R.sup.
    Type: Grant
    Filed: August 26, 1992
    Date of Patent: May 11, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Sherman T. Waddell, Timothy A. Blizzard
  • 2-biphenyl carbapenem intermediates
    Patent number: 5208329
    Abstract: Carbapenems of the formula ##STR1## are useful intermediates to antibacterial agents.
    Type: Grant
    Filed: February 14, 1992
    Date of Patent: May 4, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. Dininno, Thomas N. Salzmann
  • 2-phenanthridonyl carbapenem intermediates
    Patent number: 5208328
    Abstract: Carbapenems of the formula ##STR1## wherein: P' is a removable protecting group for hydroxy; and M is a removable protecting group for carboxy; are useful intermediates for carbapenem antibiotics.
    Type: Grant
    Filed: April 16, 1991
    Date of Patent: May 4, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Frank DiNinno, Mark L. Greenlee, Thomas A. Rano
  • 2-(1,2,3-triazolylsubstituted)phenyl carbapenem antibacterial agents
    Patent number: 5208229
    Abstract: Carbapenems having the formula: ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: March 23, 1992
    Date of Patent: May 4, 1993
    Assignee: Merck & Co., Inc.
    Inventor: Susan M. Schmitt
  • 2-biphenyl-carbapenem antibacterial agents
    Patent number: 5192758
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: February 28, 1992
    Date of Patent: March 9, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Frank DiNinno, Kevin D. Dykstra, James V. Heck
  • Inhibitors of slow reacting substance of anaphylaxis
    Patent number: 4988716
    Abstract: Novel compounds and compositions which inhibit SRS-A in mammals are disclosed. Methods for preparing said compounds and compositions and methods for their use for treating allergic reactions, inflammation and for reducing the severity of myocardial infarction resulting from heart attack are disclosed.Useful intermediates for preparing said compounds are also disclosed.
    Type: Grant
    Filed: July 28, 1987
    Date of Patent: January 29, 1991
    Assignee: Schering Corporation
    Inventors: Anil K. Saksena, Jesse K. Wong, Pietro Mangiaracina