Patents by Inventor David J. Mathre

David J. Mathre has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20130037977
    Abstract: The present invention provides a process for producing lipid nanoparticles encapsulating therapeutic products, said process comprising: a) providing one or more aqueous solutions in one or more reservoirs; b) providing one or more organic solutions in one or more reservoirs, wherein one or more of the organic solutions contains a lipid and wherein one or more of the aqueous solutions and/or one or more of the organic solutions includes therapeutic products; c) mixing said one or more aqueous solutions with said one or more organic solutions in a first mixing region, wherein said first mixing region is a Multi-Inlet Vortex Mixer (MIVM), wherein said one or more aqueous solutions and said one or more organic solutions are introduced tangentially into a mixing chamber within the MIVM so as to substantially instantaneously produce a lipid nanoparticle solution containing lipid nanoparticles encapsulating therapeutic products.
    Type: Application
    Filed: April 7, 2011
    Publication date: February 14, 2013
    Inventors: Paul A. Burke, Marian E. Gindy, David J. Mathre, Varun Kumar, Robert K. Prud'homme
  • Patent number: 6153787
    Abstract: The invention encompasses a process for making compounds of Formula I or Ia useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: December 4, 1998
    Date of Patent: November 28, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Kai Rossen, Guo-Jie Ho, Ralph P. Volante, Roger N. Farr, David J. Mathre
  • Patent number: 5883267
    Abstract: The invention encompasses a process for making compounds of Formula I or Ia useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: May 6, 1997
    Date of Patent: March 16, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Kai Rossen, Ralph P. Volante, Guo-Jie Ho, Roger N. Farr, David J. Mathre
  • Patent number: 5777105
    Abstract: Imidazolmethyloxy-substituted tricyclo-macrolide immunosuppressants are prepared by reacting a tricyclo-macrolide with an imidazolmethyl trichloroacetimidate in the presence of an acid. The invention further provides a crystalline salt of imidazolmethyloxy-substituted tricyclo-macrolide, as well as novel compounds useful in the process of the present invention.
    Type: Grant
    Filed: July 23, 1996
    Date of Patent: July 7, 1998
    Assignee: Merck & Co., Inc.
    Inventors: David J. Mathre, Richard F. Shuman, Paul Sohar, Zhiguo Song
  • Patent number: 5773575
    Abstract: The present invention is drawn to a process for forming an amide bond linkage comprising reacting a carboxylic acid and an amine in a two-phase mixture of water and an organic solvent selected from an oxygenated organic solvent or an aromatic solvent in the presence of a coupling reagent and an additive. This process is useful for making ubiquitous amides and polypeptides having various biological activities.
    Type: Grant
    Filed: October 1, 1996
    Date of Patent: June 30, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Guo-Jie Ho, David J. Mathre, Zhiguo Song, Khateeta Emerson
  • Patent number: 5760249
    Abstract: This invention is concerned with an improved process for the synthesis of hydroxysulfone, which is a key intermediate in the synthesis of carbonic anhydrase inhibitors, especially dorzolamide. Carbonic anhydrase inhibitors are known to be effective in treating elevated intraocular pressure or glaucoma.
    Type: Grant
    Filed: August 28, 1996
    Date of Patent: June 2, 1998
    Assignees: Merck & Co., Inc., Zeneca Limited
    Inventors: David J. Mathre, Paul Sohar, David Moody, Andrew J. Blacker
  • Patent number: 5693805
    Abstract: A process for the manufacture of oxytocin receptor antagonists of the following formula (I) ##STR1## and their crystalline salts is disclosed.
    Type: Grant
    Filed: September 12, 1995
    Date of Patent: December 2, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Anthony M. DeMarco, Edward J.J. Grabowski, Guo-Jie Ho, David J. Mathre, Khateeta M. Emerson, Richard F. Shuman, Paul Sohar
  • Patent number: 5688968
    Abstract: A key step in the synthesis of 5,6-dihydro-(S)-4-(ethylamino)-(S)-6-methyl-4H-thieno?2,3-b!thiopyran-2-su lfonamide 7,7-dioxide (dorzolamide) and related compounds is a Ritter reaction with an unexpected tendency to proceed with retention of chirality.
    Type: Grant
    Filed: January 6, 1995
    Date of Patent: November 18, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Thomas J. Blacklock, David J. Mathre, Paul Sohar
  • Patent number: 5686607
    Abstract: The invention is a highly efficient synthesis for making compounds of formula (iv) wherein R is C.sub.1-4 alkyl or benzyl; and R.sup.1, when present, is C.sub.1-4 alkyl, OH, O--C.sub.1-4 alkyl, or S--C.sub.1-4 alkyl; which are useful intermediates for making compounds such as those represented in formula (I).
    Type: Grant
    Filed: August 29, 1996
    Date of Patent: November 11, 1997
    Assignee: Merck & Co., Inc.
    Inventors: John Y. L. Chung, Dalian Zhao, David J. Mathre
  • Patent number: 5618934
    Abstract: The present invention is directed to a compound represented by the structural formula: ##STR1## wherein Z-- represents a negatively charged counterion.
    Type: Grant
    Filed: February 27, 1995
    Date of Patent: April 8, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Ann E. DeCamp, Edward J. J. Grabowski, Mark A. Huffman, Lyndon C. Xavier, Nobuyoshi Yasuda, Guo-Jie Ho, David J. Mathre
  • Patent number: 5594134
    Abstract: A process of synthesizing N-acyl auxiliary compounds is disclosed. A compound of the formula: ##STR1## is reacted with an anhydride in the presence of a lithium salt and an amine base to produce the N-acylated auxiliary.
    Type: Grant
    Filed: March 31, 1995
    Date of Patent: January 14, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Guo-Jie Ho, David J. Mathre
  • Patent number: 5574176
    Abstract: This invention is concerned with an improved process for the synthesis of and intermediate en route to 5,6-dihydro-(s)-4-(ethylamino)-(s)-6-methyl-4h-thieno[2,3-b]thiopyran-2-su lfonamide 7,7-dioxide and related compounds. The instant process reduces the reaction time for the synthesis of the key intermediate from 3 to 4 days to from about 2 to about 4 hours while retaining the high enantiomeric purity of the product.
    Type: Grant
    Filed: April 26, 1995
    Date of Patent: November 12, 1996
    Assignee: Merck & Co., Inc.
    Inventors: David J. Mathre, Paul Sohar, Lynn M. Brown
  • Patent number: 5461162
    Abstract: A process of synthesizing N-acyl auxiliary compounds is disclosed. A compound of the formula: ##STR1## is reacted with an anhydride in the presence of a lithium salt and an amine base to produce the N-acylated auxiliary.
    Type: Grant
    Filed: July 27, 1994
    Date of Patent: October 24, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Guo-Jie Ho, David J. Mathre
  • Patent number: 5369093
    Abstract: The present invention is directed to water-soluble derivatives of antibiotic lipopeptides having the formula. ##STR1## wherein R is H or OH and R' is a phosphono, sulfo or acyl radical possessing a charged group at neutral pH.The derivatives are esters but having a charged group, have good solubility properties in aqueous medium, rendering them more useful as therapeutic agents.
    Type: Grant
    Filed: March 15, 1991
    Date of Patent: November 29, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Milton L. Hammond, James M. Balkovec, David J. Mathre
  • Patent number: 5336756
    Abstract: A process for obtaining a compound of the formula ##STR1## in crystalline form by solubilizing the compound in warm aqueous n-propanol and then allowing the solution to stand at ambient temperature until crystal formation is substantially complete is described. The crystalline compound obtained thereby is also described.
    Type: Grant
    Filed: August 27, 1991
    Date of Patent: August 9, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Robert E. Schwartz, August J. Kempf, David J. Mathre
  • Patent number: 5264585
    Abstract: The chiral catalyst of general structure 1, or its enantiomer ##STR1## is prepared by treating the corresponding N-carboxy anhydride of structure 2 ##STR2## with an aryl metal, especially a phenyl metal such as an aryl magnesium halide, aryl lithium, aryl zinc or aryl cesium, to form a 1,1-diaryl- methanol of structure 3 ##STR3## followed by treatment with a compound of structure, 4 ##STR4## The catalyst, wherein R is aromatic, is novel and in some cases superior to the catalyst wherein R is alkyl or aralkyl in directing the chirality of diborane, borane-dimethyl sulfide or borane-tetrahydrofuran reductions of ketones to secondary alcohols.
    Type: Grant
    Filed: October 26, 1992
    Date of Patent: November 23, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Thomas J. Blacklock, Todd K. Jones, David J. Mathre, Lyndon C. Xavier
  • Patent number: 5264574
    Abstract: Oxazaborolidine-borane complexes are prepared by adding a C.sub.5-8 alkane, typically hexane, to an aged solution of oxazaborolidine and a source of borane such as borane-dimethyl sulfide or gaseous diborane to crystallize the oxazaborolidine complex.
    Type: Grant
    Filed: April 3, 1992
    Date of Patent: November 23, 1993
    Assignee: Merck & Co., Inc.
    Inventors: James D. Carroll, David J. Mathre, Edward G. Corley, Andrew S. Thompson
  • Patent number: 5233023
    Abstract: A facile process for preparing a compound of the formula ##STR1## or a salt thereof, wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, X.sup.1 Y and Z are as defined in the specification, by direct phosphorylation of the corresponding phenolic compound with tetrabenzyl pyrophosphate in the presence of lithium hydroxide is described.
    Type: Grant
    Filed: July 30, 1991
    Date of Patent: August 3, 1993
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Mallory F. Loewe, David J. Mathre
  • Patent number: 5198421
    Abstract: There is disclosed a monophosphorylated cyclic lipopeptide compound obtained by biophosphorylating a cyclic lipopeptide related to echinocandins and having a peptide skeleton bearing several hydroxy groups wherein in the phosphorylated cyclic lipopeptide, the phosphate group is attached to the hydroxy group of the 4-hydroxyproline component of the lipopeptide. The compounds are useful for the control of fungi and parasites.
    Type: Grant
    Filed: April 26, 1991
    Date of Patent: March 30, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, David J. Mathre, Brian R. Petuch, Robert A. Reamer
  • Patent number: 5189177
    Abstract: The chiral catalyst of general structure 1, or its enantiomer ##STR1## is prepared by treating the corresponding N-carboxy anhydride of structure 2 ##STR2## with an aryl metal, especially a phenyl metal such as an aryl magnesium halide, aryl lithium, aryl zinc or aryl cesium, to form a 1,1-diaryl- methanol of structure 3 ##STR3## followed by treatment with a compound of structure, 4 ##STR4## The catalyst, wherein R is aromatic, is novel and in some cases superior to the catalyst wherein R is alkyl or aralkyl in directing the chirality of diborane, borane-dimethyl sulfide or borane-tetrahydrofuran reductions of ketones to secondary alcohols.
    Type: Grant
    Filed: July 15, 1991
    Date of Patent: February 23, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Thomas J. Blacklock, Todd K. Jones, David J. Mathre, Lyndon C. Xavier