Patents Represented by Attorney, Agent or Law Firm Mark L. Bosse
  • Patent number: 7462608
    Abstract: Phosphorus-substituted imidazole compounds with anti-HIV properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit reverse transcriptase activity and are useful therapeutically for the inhibition of such enzymes, as well as in assays for the detection of such enzymes.
    Type: Grant
    Filed: April 25, 2003
    Date of Patent: December 9, 2008
    Assignee: Gilead Sciences, Inc.
    Inventors: James M. Chen, Xiaowu Chen, Choung U. Kim, William A. Lee, Christopher P. Lee, Peter H. Nelson, James D. Tario, Lianhong Xu
  • Patent number: 7253180
    Abstract: Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. A1 and A2 are moieties forming a five, six, or seven membered ring. L is a bond or a linker connecting a ring atom of Ar to N. X is O, S, or substituted nitrogen. Ar is aryl or heteroaryl. Q is N, +NR, or CR4. The aryl carbons may be independently substituted with substituents other than hydrogen. The compounds may include prodrug moieties covalently attached at any site.
    Type: Grant
    Filed: October 16, 2003
    Date of Patent: August 7, 2007
    Assignee: Gilead Sciences, Inc.
    Inventors: James M. Chen, Xiaowu Chen, Maria Fardis, Haolun Jin, Choung U. Kim, Laura N. Schacherer
  • Patent number: 7115592
    Abstract: Novel compounds are provided having formula (I) where R1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).
    Type: Grant
    Filed: June 16, 2004
    Date of Patent: October 3, 2006
    Assignees: Institute of Organic Chemistry, Biochemistry of the Academy of Sciences of the Czech Republic
    Inventors: Jan M. R. Balzarini, Erik D. A. De Clercq, Antonin Holy, Dana Hockova
  • Patent number: 7071305
    Abstract: This invention is concerned with human organic anion transporter (“hOAT”). Isolated nucleic acid encoding hOAT is provided, along with ioslated hOAT polypeptide. hOAT nucleic acid and/or hOAT polypeptide are employed in transgenic animals, recombinant cells, replicable vectors and analytical procedures for identifying hOAT agonists or antagonists, assays for identifying hOAT alleles and/or isotypes, screening tests for nephrotoxic or neurologically active compounds, and determination of drug-drug interactions within the kidney or brain.
    Type: Grant
    Filed: February 28, 2002
    Date of Patent: July 4, 2006
    Assignee: Gilead Sciences, Inc.
    Inventor: Tomas Cihlar
  • Patent number: 7060484
    Abstract: Novel polypeptides (NPs) are provided which are capable of protein C activation without significant fibrinogen clotting activity, and vice versa. NPs having enhanced protein C activating properties in relation to fibrinogen clotting are useful in particular as anticoagulants and in screening for substances that agonize or antagonize this property and in diagnostic procedures to determine the status of patients' activated protein C-mediated anticoagulant pathway. Procoagulant NPs are useful to promote clotting in the course of therapy of solid tumors, as an impregnate for bandages, or in diagnostic assays. The NPs are produced in recombinant cell culture or by in vitro methods.
    Type: Grant
    Filed: February 16, 2000
    Date of Patent: June 13, 2006
    Assignee: Gilead Sciences, Inc.
    Inventors: Craig S. Gibbs, Lawrence L. K. Leung, Manuel Tsiang
  • Patent number: 6770290
    Abstract: A novel composition and method for solubilizing amphiphilic drugs in a small amount of organic solvent for use in improved liposomes is disclosed. A phosphatidylglycerol is acidified in a small amount of organic solvent. The amphiphilic drug, such as Amphotericin B, suspended in organic solvent is then added to the acidified phosphatidylycerol and a soluble complex is formed between the phosphatidylglycerol and the amphiphilic drug. When the liposome composition incorporating the soluble complex is hydrated, the final pH of the hydrating aqueous buffer is carefully controlled. The Amphotericin B liposomes formed have markedly reduced toxicity.
    Type: Grant
    Filed: October 19, 1990
    Date of Patent: August 3, 2004
    Assignee: Gilead Sciences, Inc.
    Inventors: Richard T. Proffitt, Jill Adler-Moore, Su-Ming Chiang
  • Patent number: 6518438
    Abstract: The present invention provides new synthetic methods and compositions. In particular, new methods of preparing intermediates useful in the synthesis of neuraminidase inhibitors and compositions useful as intermediates that are themselves useful in the synthesis of neuraminidase inhibitors are provided.
    Type: Grant
    Filed: September 27, 2001
    Date of Patent: February 11, 2003
    Assignee: Gilead Sciences, Inc.
    Inventors: Kenneth M. Kent, Choung U. Kim, Lawrence R. McGee, John D. Munger, Ernest J. Prisbe, Michael J. Postich, John C. Rohloff, Daphne E. Kelly, Matthew A. Williams, Lijun Zhang
  • Patent number: 6376674
    Abstract: Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidaseactivity are also described.
    Type: Grant
    Filed: August 18, 1999
    Date of Patent: April 23, 2002
    Assignee: Gilead Sciences, Inc.
    Inventors: Choung U. Kim, Matthew A. Williams
  • Patent number: 6284891
    Abstract: The present invention relates to a process for preparing camptothecin and camptothecin analogs of Formula (I) from compounds of Formula (II) and to novel intermediates useful in their preparation, wherein R1 to R6 represent various substituents.
    Type: Grant
    Filed: August 15, 2000
    Date of Patent: September 4, 2001
    Assignee: Gilead Sciences, Inc.
    Inventors: Francis Gerard Fang, Shiping Xie
  • Patent number: 6274115
    Abstract: Micellular particles such as small unilamellar vesicles of less than 2000 A° loaded with 111In are administered to BALB/c mice in which EMT6 tumors had been induced. Whole body scintographs of the mice to which either neutral or positively or negatively charged vesicles had been administered show a substantial quantity of the vesicle entrapped 111In localized in the tumor. Blocking of macrophages in the liver and spleen by first administering unlabeled, aminomannose substituted vesicles before administration of the labeled vesicles increases uptake of the 111In labeled vesicles in the tumor.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 14, 2001
    Assignee: Gilead Sciences, Inc.
    Inventors: Cary A. Presant, Richard T. Proffitt, Raymond L. Teplitz, Lawrence E. Williams, George W. Tin
  • Patent number: 6225341
    Abstract: Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
    Type: Grant
    Filed: April 8, 1999
    Date of Patent: May 1, 2001
    Assignee: Gilead Sciences, Inc.
    Inventors: Norbert W. Bischofberger, Choung U. Kim, Willard Lew, Hongtao Liu, Matthew A. Williams
  • Patent number: 6221388
    Abstract: A liposomal aminoglycoside formulation comprising a neutral lipid, a negatively charged lipids and a sterol. The formulation contains unilamellar vesicles having an average size below 100 nm. A process of making liposomes containing an aminoglycoside is also provided. A method is also provided for the treatment of drug susceptible and drug resistant bacteria.
    Type: Grant
    Filed: September 28, 1999
    Date of Patent: April 24, 2001
    Assignee: Gilead Sciences, Inc.
    Inventors: Evan M. Hersch, Eskild A. Petersen, Richard T. Proffitt, Kevin R. Bracken, Su-Ming Chiang
  • Patent number: 6204398
    Abstract: The present invention provides new synthetic methods and compositions. In particular, new methods of preparing intermediates such as those having formulas (I)-(IV), useful in the synthesis of neuraminidase inhibitors and compositions useful as intermediates that are themselves useful in the synthesis of neuraminidase inhibitors are provided.
    Type: Grant
    Filed: April 28, 1999
    Date of Patent: March 20, 2001
    Assignee: Gilead Sciences, Inc.
    Inventors: Kenneth M. Kent, Choung U. Kim, Lawrence R. McGee, John D. Munger, Ernest J. Prisbe, Michael J. Postich, John C. Rohloff, Daphne E. Kelly, Matthew A. Williams, Lijun Zhang
  • Patent number: 6111132
    Abstract: Novel compounds of Formula (I) are described. R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are described in this specification.Synthetic intermediates and pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Assay methods for detecting neuraminidase activity are also described.
    Type: Grant
    Filed: December 10, 1998
    Date of Patent: August 29, 2000
    Assignee: Gilead Sciences, Inc.
    Inventors: Choung U. Kim, Willard Lew
  • Patent number: 6090567
    Abstract: Methods for immunoassay of analytes employing mutant glucose-6-phosphate dehydrogenase (G6PDH) enzymes as labels. In particular, the invention relates to the use of conjugates of an analyte or analyte analog and a mutant NAD.sup.+ dependent G6PDH differing from any precursor G6PDH by the deletion, substitution, or insertion, or any combination thereof of at least one amino acid per subunit. The invention also involves the construction of several mutations in precursor glucose-6-phosphate dehydrogenase (G6PDH) enzymes. Typically, the mutations involve deletion or substitution of one or more lysine residues, or introduction of one or more cysteine residues by insertion of cysteine to precursor G6PDH or substitution of precursor G6PDH amino acids residues with cysteine.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: July 18, 2000
    Assignee: Behringwerke AG
    Inventors: Edward Benjamin Jakobovits, Joy L. Silen, Mark J. Levy, Thomas C. Goodman, Martin Becker, Edwin F. Ullman, Robert M. Caldwell, Richard R. Bott, Christopher Charles Barnett
  • Patent number: 6057459
    Abstract: The present invention provides new synthetic methods and compositions. In particular, new methods of preparing intermediates useful in the synthesis of neuraminidase inhibitors and compositions useful as intermediates that are themselves useful in the synthesis of neuraminidase inhibitors are provided.
    Type: Grant
    Filed: October 20, 1998
    Date of Patent: May 2, 2000
    Assignee: Gilead Sciences, Inc.
    Inventors: Kenneth M. Kent, Choung U. Kim, Lawrence R. McGee, John D. Munger, Jr., Ernest J. Prisbe, Michael J. Postich, John C. Rohloff, Daphne E. St. John, Matthew A. Williams, Lijun Zhang
  • Patent number: 6034118
    Abstract: Tri- and tetra substituted thiepane compositions having use as immunogens, therapeutics, diagnostics and for other industrial purposes are disclosed. The compositions inhibit proteolytic activity of viral enzymes and are useful for the inhibition of such enzymes as well as in assays for the detection of such enzymes. Embodiments in which antigenic polypeptides are bonded to the compositions are useful in raising antibodies against the thiepane haptens or the polypeptide. Labeled thiepanes of this invention are useful as diagnostic reagents.
    Type: Grant
    Filed: November 3, 1995
    Date of Patent: March 7, 2000
    Assignee: Gilead Sciences, Inc.
    Inventors: Norbert W. Bischofberger, Choung U. Kim, Steven H. Krawczyk, Lawrence R. McGee, Michael J. Postich, Wenjin Yang
  • Patent number: 5994377
    Abstract: Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
    Type: Grant
    Filed: October 17, 1997
    Date of Patent: November 30, 1999
    Assignee: Gilead Sciences, Inc.
    Inventors: Choung U. Kim, Matthew A. Williams
  • Patent number: 5958973
    Abstract: The present invention is directed to compositions of the formula: ##STR1## wherein: R.sub.2 is H, or an alkyl group having 1 to 3 carbon atoms and 0 to 2 hydroxyls;R.sub.3 is H, or hydroxyl;R.sub.4 is H, or forms a hydrolyzable ester or amide with --CO.sub.2 --;R.sub.5 are H, or are taken together to form .dbd.NH; andR.sub.6 comprises an amine, or a group having 1 to 12 carbon atoms and 1 to 3 amine groups. The invention is also directed to methods of inhibiting the activity of neuraminidase using the compounds of the invention.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 28, 1999
    Assignee: Gilead Sciences, Inc.
    Inventors: Norbert W. Bischofberger, Choung U. Kim, Willard Lew, Hongtao Liu, John C. Martin, Sundaramoorthi Swaminathan, Matthew A. Williams
  • Patent number: 5952375
    Abstract: Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
    Type: Grant
    Filed: February 26, 1996
    Date of Patent: September 14, 1999
    Assignee: Gilead Sciences, Inc.
    Inventors: Norbert W. Bischofberger, Choung U. Kim, Willard Lew, Hongtao Liu, Matthew A. Williams