Patents Represented by Attorney, Agent or Law Firm Mark R. Daniel
  • Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
    Patent number: 6277843
    Abstract: The present invention relates to carbapenem antibacterial agents of the formula I: as well as salts and hydrates thereof. Pharmaceutical compositions and methods of treatment are also included wherein X is present or absent, when present, represents a members selected from the group consisting of: CH2, C(R)2, C═CR2, O, S(O)x, with x equal to 0, 1 or 2; C(O), C(O)O, OC(O) and NR—.
    Type: Grant
    Filed: October 19, 1999
    Date of Patent: August 21, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. Dininno, Helen Chen
  • Penem antibacterial compounds, compositions and methods of treatment
    Patent number: 6271222
    Abstract: The present invention relates to penem antibacterial agents in which the releaseable liphophilic aromatic side-chain, tethered to the carbapenem nucleus via a methylene linker, necessary for anti-MRSA activity replaces the non-releaseable liphophilic side-chains found in 2-aryl and 2-benzothiazolylthio carbapenem compounds. The compound is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula I: Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: April 23, 1999
    Date of Patent: August 7, 2001
    Assignee: Merck & Co., Inc.
    Inventor: Frank P. Dininno
  • Method for quantitating an inflammatory response
    Patent number: 6268155
    Abstract: A method for objectively quantitating the cellular infiltration in a tissue biopsy of a warm-blooded animal using a capture ELISA method. This method also allows one to quantitate the cellular infiltration of a tissue biopsy corresponding to an inflammatory response. As such this invention has both research and clinical applications in the analysis of an inflammatory response, and the effectiveness of immunosuppresants in addressing the inflammation.
    Type: Grant
    Filed: September 10, 1996
    Date of Patent: July 31, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Gloria C. Koo, Mai P. Nguyen, Althea D. Talento
  • Cyclohexapeptidyl amine compounds
    Patent number: 6268338
    Abstract: Cyclohexapeptidyl amine compounds are disclosed of the formula: or its acid addition salt, wherein: R1 is H or OH; R2 is H or OH; R3 is QCnH2nNRVRVI, QCnH2nNRVRVIRVII+Y−, or Q(CH2)1-3CRVIIIRIXNHRX.
    Type: Grant
    Filed: April 30, 1993
    Date of Patent: July 31, 2001
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Frances Aileen Bouffard, James F. Dropinski, Robert A. Zambias
  • Rearrangement process and tricyclic and tetracyclic compounds
    Patent number: 6268510
    Abstract: A rearrangement process for the preparation of a 6,5,5-tricyclic, a 6,6,5-tricyclic and 6,5,5,7-tetracyclic ring system is disclosed.
    Type: Grant
    Filed: July 6, 2000
    Date of Patent: July 31, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Lisa F. Frey, Edward J. J. Grabowski, Stephane G. Ouellet, Robert A. Reamer, Richard D. Tillyer
  • Ophthalmic composition containing a carbonic anhydrase inhibitor and xanthan gum
    Patent number: 6264935
    Abstract: The present invention relates to ophthalmic compositions for the treatment of ocular hypertension and glaucoma, comprising a hypotonic solution of 0.1 to 0.2% (w/w) of xanthan gum and 0.5 to 5% (w/w) of a topical carbonic anhydrase inhibitor or an ophthalmologically acceptable salt thereof.
    Type: Grant
    Filed: June 14, 1999
    Date of Patent: July 24, 2001
    Assignee: Laboratoires MSD - Chibret
    Inventors: Gilles Chastaing, Bernard Plazonnet, Annouk Rozier
  • Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
    Patent number: 6265395
    Abstract: Compounds of formula I: as well as pharmaceutically acceptable salts thereof useful as carbapenem antibacterial agents are disclosed.
    Type: Grant
    Filed: June 23, 1999
    Date of Patent: July 24, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Timothy A. Blizzard, Ronald W. Ratcliffe
  • Angiogenesis inhibitors
    Patent number: 6265403
    Abstract: The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tyrosine kinase-dependent diseases and conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy, and the like in mammals.
    Type: Grant
    Filed: January 7, 2000
    Date of Patent: July 24, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Fraley, Randall W. Hungate, Andrew J. Tebben
  • Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
    Patent number: 6255300
    Abstract: The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with an iodo-substituted phenyl linked through a CH2—O— group. The compounds of the invention are represented by formula I: wherein A represent O, S or —CH2— attached at position 3, 4 or 6; Q is selected from the group consisting of: &agr; represents O, S or NRs; &bgr;, &dgr;, &ggr;, &mgr; and &sgr; represent CRt, N or N+Rs, provided that no more than one of &bgr;, &dgr;, &ggr;, &mgr; and &sgr; is N+Rs, balanced by L− or a carboxylate anion. Salts and hydrates thereof are included. The iodo-substituted phenyl ring is further substituted with various substituent groups including at least one cationic group. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: December 7, 1999
    Date of Patent: July 3, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. Dininno, Kevin D. Dykstra
  • Crystalline salts of a carbapenem antibiotic
    Patent number: 6252063
    Abstract: Crystalline salts of an amorphous, unstable carbapenem antibiotic having the formula: are disclosed, wherein R− represents beyslate, tosylate, napsylate, saccharate or alizarate.
    Type: Grant
    Filed: November 2, 1999
    Date of Patent: June 26, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Ross A. Miller, Scott S. Ceglia
  • Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
    Patent number: 6251890
    Abstract: The present invention relates to carbapenem antibacterial agents of formula I: or a pharmaceutically acceptable salt thereof, wherein: R2 represents: in formula I, in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a CH2 group. The naphthosultam is further substituted with various substituent groups including at least one cationic group.
    Type: Grant
    Filed: March 13, 2000
    Date of Patent: June 26, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Timothy A. Blizzard, Ronald W. Ratcliffe, Jerry D. Morgan, II, Robert R. Wilkening
  • Method of improved mixing of a varicella-infected cell culture in roller bottles
    Patent number: 6251653
    Abstract: A method for enhancing the mixing of a varicella-infected cell culture in a roller bottle by the introduction of controlled cross-sectional flow perturbations in roller bottle rotation is disclosed. The effectiveness of the method is demonstrated by achieving higher efficiency in cell culturing and virus propagation in roller bottles by introducing controlled cross-sectional flow perturbations during the process.
    Type: Grant
    Filed: October 26, 1998
    Date of Patent: June 26, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Joye L. Bramble, Fernando J. Muzzio, James A. Searles
  • Inhibitors of farnesyl-protein transferase
    Patent number: 6248756
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferas (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: February 11, 1999
    Date of Patent: June 19, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Christopher Dinsmore, Robert P. Gomez, John H. Hutchinson, John S. Wai, Theresa M. Williams, Ian M. Bell, Mark W. Embrey, Thorsten E. Fisher
  • Ophthalmic compositions comprising combinations of a carbonic anhydrase inhibitor and a &bgr;-adrenergic antagonist
    Patent number: 6248735
    Abstract: Combinations of a &bgr;-adrenergic antagonist and a topical carbonic anhydrase inhibitor are particularly useful in the treatment of ocular hypertension, especially in patients insufficiently responsive to treatment with &bgr;-adrenergic antagonists.
    Type: Grant
    Filed: April 3, 1997
    Date of Patent: June 19, 2001
    Assignee: Merck & Co., Inc.
    Inventor: John J. Baldwin
  • Tyrosine kinase inhibitors
    Patent number: 6245759
    Abstract: The present invention relates to pyrazolo-pyrimidinyl compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
    Type: Grant
    Filed: March 7, 2000
    Date of Patent: June 12, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Mark T. Bilodeau, Mark E. Fraley, Randall W. Hungate
  • Sterile inflation system for a sealed bag with flexible wall
    Patent number: 6244023
    Abstract: This system comprises a compacted bag, in particular under vacuum, having an appendage into which a spacer device is inserted (2) which forms a pocket (140) separating two facing flexible partition sections from each other (120,121) of which one (121) is adapted to be applied when placed under vacuum against a set of heatable blades with closed outline linked to each other (51, 61) the interior blade (61) being carried by a mobile part (6) of which the end is able to penetrate into the cut pocket (140) with a view to the inflation of the bag with air brought by a channel (600′) through a sterilizing filter (8).
    Type: Grant
    Filed: November 8, 1999
    Date of Patent: June 12, 2001
    Assignee: Laboratoires Merck Sharp & Dohme-Chibret SNC
    Inventor: Gilbert Lataix
  • Preparation of betamethyl carbapenem intermediates
    Patent number: 6242596
    Abstract: A process for making a beta methyl carbapenem intermediate is disclosed. A compound of formula I: is contacted in a non-reactive solvent with methyl Meldrum's acid and a base to produce a compound of formula III: Compound III is treated in an aprotic solvent with a scavenging base, an alkali metal halide and a tri-organo silyl protecting compound for nitrogen to produce a compound of formula IV: Compound IV may be reacted with a nucleophile Nu—X in a non-reactive solvent and base, and the mixture acidified to produce a compound of formula V. Compound V may be reacted with mild acid to produce a compound of formula VI.
    Type: Grant
    Filed: May 12, 1994
    Date of Patent: June 5, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Woo-Baeg Choi, Guy R. Humphrey, Paul J. Reider, Ichiro Shinkai, Andrew S. Thompson, Ralph P. Volante
  • Process for synthesizing biaryl inhibitors of farnesyl-protein transferase
    Patent number: 6239280
    Abstract: The present invention is directed to a process for synthesizing 1,5 disubstituted imidazoles with biaryl components of the formula (I): which are usefull as Farnesyl-Protein Transferase inhibitors.
    Type: Grant
    Filed: June 30, 1999
    Date of Patent: May 29, 2001
    Assignee: Merck & Co., Inc.
    Inventors: David Askin, Jennifer A. Cowen, Peter E. Maligres, J. Christopher McWilliams, Marjorie S. Waters
  • Process for the synthesis of carbapenem intermediated and compounds produced
    Patent number: 6235898
    Abstract: A process of synthesizing a carbapenem compound of formula 6: is disclosed using a compound of formula 4′: The intermediate compounds that are described herein are also included in the present invention.
    Type: Grant
    Filed: February 23, 2000
    Date of Patent: May 22, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Mark S. Jensen, Chunhua Yang, Nobuyoshi Yasuda
  • Angiogenesis inhibitors
    Patent number: 6235741
    Abstract: The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tyrosine kinase-dependent diseases/conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.
    Type: Grant
    Filed: May 28, 1998
    Date of Patent: May 22, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Mark T. Bilodeau, Randall W. Hungate, Richard L. Kendall, Ruth Rutledge, Kenneth A. Thomas, Jr., Robert Rubino, Mark E. Fraley