Patents Represented by Attorney, Agent or Law Firm Curtis C. Panzer
  • .beta.-lactams useful in determining the amount of elastase in a clinical sample
    Patent number: 5229510
    Abstract: Disclosed are .beta.-lactams of formula I ##STR1## wherein X is a chromogenic or fluorogenic substituted aryl or heteroaryl, which are specific inhibitors of Human leukocyte elastase (HLE). Upon contact with HLE these compounds are cleaved to form a chromogenic or fluorogenic species which may be readily measured by the assay disclosed herein. The assay thus provides a means for direct measurement of the amount of active HLE in a body fluid or other sample.
    Type: Grant
    Filed: January 3, 1992
    Date of Patent: July 20, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Wilson B. Knight, William K. Hagmann, Alan L. Maycock
  • Substituted azetidinones as anti-inflammatory and antidegenerative agents
    Patent number: 5229381
    Abstract: New substituted azetidinones of the general formula (A') which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described.
    Type: Grant
    Filed: September 20, 1991
    Date of Patent: July 20, 1993
    Assignee: Merck & Co., Inc.
    Inventors: James B. Doherty, Conrad P. Dorn, Paul E. Finke, William K. Hagmann, Malcolm MacCoss, Shrenik K. Shah
  • Immunosuppressive fluorinated cyclosporin analogs
    Patent number: 5227467
    Abstract: New immunosuppressive cyclosporin analogs are disclosed having one or more fluorinated amino acids. These analogs may also have a "C-9 amino acid" wherein the double bond is replaced by a heteroatom such as sulfur or oxygen.
    Type: Grant
    Filed: April 29, 1991
    Date of Patent: July 13, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, Arsenio A. Pessolano, Janos Kollonitsch
  • Synthesis of novel immunosuppressive cyclosporin analogs with modified amino acids at position-8
    Patent number: 5214130
    Abstract: New immunosuppressive cyclosporin analogs are disclosed consisting of [dehydro-Ala].sup.8 cyclosporins and derived therefrom cyclosporins having a sulfur containing amino acid at position-8.
    Type: Grant
    Filed: August 12, 1991
    Date of Patent: May 25, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Arthur A. Patchett, David Taub, Robert T. Goegelman
  • 2-phenanthrenyl carbapenem intermediates
    Patent number: 5196529
    Abstract: Carbapenems of the formula ##STR1## are useful as intermediates to antibacterial agents.
    Type: Grant
    Filed: October 9, 1990
    Date of Patent: March 23, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. Dininno, Thomas N. Salzmann, Mark L. Greenlee
  • Spirocyclic 6-amido-carbapenems and azetidinones
    Patent number: 5183887
    Abstract: New antibacterial spirocyclic 6-amido carbapenems of the structural formulas: ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-8 substituted or unsubstituted alkyl, or C.sub.6-10 substituted or unsubstituted aryl; R.sup.5 is hydrogen or a protecting group for alcohol; R.sup.6 is hydrogen or a protecting group for amido nitrogen; R.sup.7 is hydrogen or a protecting group for amido nitrogen; and R.sup.8 is hydroxy, hydrogen, C.sub.1-8 substituted or unsubstituted thioalkyl, C.sub.6-10 substituted or unsubstituted thioaryl, 5 or 6 membered, substituted or unsubstituted thioheteroaryl; and a process for their synthesis through novel spirocyclic 4-amido azetidinones are disclosed.
    Type: Grant
    Filed: July 9, 1991
    Date of Patent: February 2, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Mark L. Greenlee, Thomas N. Salzmann, Frank P. DiNinno
  • 2-biphenyl-carbapenems intermediates
    Patent number: 5182385
    Abstract: Carbapenems of the formula: ##STR1## are useful intermediates to antibacterial agents.
    Type: Grant
    Filed: October 9, 1990
    Date of Patent: January 26, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. Dininno, Thomas N. Salzmann
  • 2-benzocoumarinyl carbapenems
    Patent number: 5182384
    Abstract: Carbapenems of the formula ##STR1## are useful intermediates to antibacterial agents.
    Type: Grant
    Filed: May 24, 1991
    Date of Patent: January 26, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Frank DiNinno, Thomas A. Rano, Mark L. Greenlee
  • 2-phenanthrenyl-carbapenems
    Patent number: 5177202
    Abstract: Carbapenems of the formula ##STR1## are useful intermediates to antibacterial agents.
    Type: Grant
    Filed: October 9, 1990
    Date of Patent: January 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. Dininno, Mark L. Greenlee, Thomas N. Salzmann
  • Nitrogen deprotected 4-acyloxyazetidin-2-ones
    Patent number: 5177201
    Abstract: The 4-acyloxyazetidin-2-ones, which are intermediates in the production of carbapenems and penems, are produced from nitrogen deprotected 4-furanylazetidin-2-ones.
    Type: Grant
    Filed: June 21, 1990
    Date of Patent: January 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Joseph E. Lynch, William L. Laswell, Ralph P. Volante, Ichiro Shinkai
  • Purified C5a receptor from human polymorphonuclear leukocytes
    Patent number: 5177190
    Abstract: A method is disclosed for isolating and purifying C5a receptor from human polymorphonuclear leukocytes. C5a is a complement-derived protein which is important as a mediator of inflammatory responses. C5a receptor may be used to screen create and quantify C5a antagonists useful as anti-inflammatory agents and immunoregulants and to generate monoclonal and polyclonal anti-C5a receptor antibodies useful as anti-inflammatory agents and immunoregulants.
    Type: Grant
    Filed: January 22, 1992
    Date of Patent: January 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Thomas E. Rollins, Martin S. Springer
  • 2-benzocoumarinyl carbapenems
    Patent number: 5162314
    Abstract: Carbapenems of the formula ##STR1## with E as ##STR2## are useful antibacterial agents.
    Type: Grant
    Filed: May 24, 1991
    Date of Patent: November 10, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Frank DiNinno, Mark L. Greenlee, Thomas A. Rano
  • 2-phenanthridonyl carbapenems having cationizeable substituents
    Patent number: 5157033
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: April 16, 1991
    Date of Patent: October 20, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Frank DiNinno, Mark L. Greenlee, Thomas A. Rano
  • 2-phenanthridonyl carbapenems
    Patent number: 5153185
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: April 16, 1991
    Date of Patent: October 6, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Frank DiNinno, Mark L. Greenlee, Thomas A. Rano
  • 2-benzocoumarinyl-carbapenems
    Patent number: 5153186
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: May 24, 1991
    Date of Patent: October 6, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Frank DiNinno, Thomas A. Rano, Mark L. Greenlee
  • Intermediates for substituted azetidinones useful as anti-inflammatory and antidegenerative agents
    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
  • Stereoselective synthesis of a chiral cis 3-beta hydrogen (3R) 4-aroyloxy azetidinone
    Patent number: 5145957
    Abstract: A process is described for the stereocontrolled synthesis of (3R,4R)-3-[(1R)-1-hydroxyethyl]-4-benzoyloxyazetidin-2-ones and their derivatives by cycloaddition involving an imine and a ketone, generated from 3(S)-hydroxybutyrate which are useful intermediates in the synthesis of carbapenem antibiotics.
    Type: Grant
    Filed: January 9, 1992
    Date of Patent: September 8, 1992
    Assignee: Merck & Co., Inc.
    Inventors: David M. Tschaen, Joseph E. Lynch, William L. Laswell, Ralph P. Volante, Ichiro Shinkai
  • Substituted cephalosporin sulfones as anti-inflammatory and anti-degenerative agents
    Patent number: 5132301
    Abstract: New substituted cephalosporin sulfones are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.
    Type: Grant
    Filed: January 29, 1990
    Date of Patent: July 21, 1992
    Assignee: Merck & Co., Inc.
    Inventors: James B. Doherty, Raymond A. Firestone, Paul E. Finke, William K. Hagmann, Shrenik K. Shah, Kevan R. Thompson
  • 1,3-diaryl cyclopentanes and derivatives thereof as PAF antagonists
    Patent number: 5132463
    Abstract: Novel 1,3-Diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediated by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.
    Type: Grant
    Filed: June 12, 1991
    Date of Patent: July 21, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Donald W. Graham, John C. Chabala, Tesfaye Biftu, Michael N. Chang, Yuan-Ching P. Chiang, Shu S. Yang, Kathryn L. Thompson
  • Immunosuppressive cyclosporin analogs with modified amino acids at position-8
    Patent number: 5122511
    Abstract: New immunosuppressive cyclosporin analogs are disclosed consisting of [dehydro-Ala].sup.8 cyclosporins and derived therefrom cyclosporins having a sulfur containing amino acid at position-8.
    Type: Grant
    Filed: February 27, 1990
    Date of Patent: June 16, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Arthur A. Patchett, David Taub, Robert T. Goegelman