Patents by Inventor David M. Tschaen

David M. Tschaen 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).

  • Process for making reverse transcriptase inhibitors
    Patent number: 9598397
    Abstract: The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase and HIV replication, and the treatment of human immunodeficiency virus infection in humans.
    Type: Grant
    Filed: December 2, 2014
    Date of Patent: March 21, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Yang Cao, Donald R. Gauthier, Jr., Guy R. Humphrey, Tetsuji Itoh, Michel Journet, Gang Qian, Benjamin D. Sherry, David M. Tschaen
  • PROCESS FOR MAKING REVERSE TRANSCRIPTASE INHIBITORS
    Publication number: 20160297794
    Abstract: The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase and HIV replication, and the treatment of human immunodeficiency virus infection in humans.
    Type: Application
    Filed: December 2, 2014
    Publication date: October 13, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Yang Cao, Donald R. Gauthier, Jr., Guy R. Humphrey, Tetsuji Itoh, Michel Journet, Gang Qian, Benjamin D. Sherry, David M. Tschaen
  • Process for making spirolactone compounds
    Patent number: 7482449
    Abstract: This invention relates to a process for making spirolactone compounds analogous to formula I.
    Type: Grant
    Filed: March 19, 2008
    Date of Patent: January 27, 2009
    Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.
    Inventors: Ralph P. Volante, David M. Tschaen, Steven A. Weissman, Matthew Heileman, Toshiaki Mase, Takehiko Iida, Kenji Maeda, Toshihiro Wada, Hiroki Sato, Kenichi Asakawa
  • Process for making spirolactone compounds
    Publication number: 20080171888
    Abstract: This invention relates to a process for making spirolactone compounds analogous to formula I.
    Type: Application
    Filed: March 19, 2008
    Publication date: July 17, 2008
    Inventors: Ralph P. Volante, David M. Tschaen, Steven A. Weissman, Matthew Heileman, Toshiaki Mase, Takehiko Iida, Kenji Maeda, Toshihiro Wada, Hiroki Sato, Kenichi Asakawa
  • Process for making spirolactone compounds
    Patent number: 7368569
    Abstract: This invention relates to a process for making spirolactone compounds analogous to formula I
    Type: Grant
    Filed: October 14, 2003
    Date of Patent: May 6, 2008
    Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.
    Inventors: Ralph P. Volante, David M. Tschaen, Steven A. Weissman, Matthew Heileman, Toshiaki Mase, Takehiko Iida, Kenji Maeda, Toshihiro Wada, Hiroki Sato, Kenichi Asakawa
  • Process for making spirolactone compounds
    Patent number: 6605720
    Abstract: This invention relates to processes for making spirolactone compounds analogous to formula I:
    Type: Grant
    Filed: January 23, 2003
    Date of Patent: August 12, 2003
    Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.
    Inventors: Kenji Maeda, Shinji Kato, Takehiko Iida, David M. Tschaen
  • PROCESS FOR MAKING SPIROLACTONE COMPOUNDS
    Publication number: 20030144515
    Abstract: This invention relates to processes for making spirolactone compounds analogous to formula I: 1
    Type: Application
    Filed: January 23, 2003
    Publication date: July 31, 2003
    Inventors: Kenji Maeda, Shinji Kato, Takehiko Iida, David M. Tschaen
  • Process for the synthesis of an endothelin receptor antagonist
    Publication number: 20020107391
    Abstract: The present invention relates to a practical and efficient way to synthesize the compound for the endothelin receptor antagonist involving a Grignard addition and a cyclization reaction to give a desired compound of the general formula shown below: 1
    Type: Application
    Filed: October 18, 2001
    Publication date: August 8, 2002
    Inventors: Lisa F. Frey, Cheng Y. Chen, Jing Li, Zhiguo J. Song, Lushi Tan, Richard D. Tillyer, David M. Tschaen, Matthew M. Zhao
  • Asymmetric conjugate addition reaction
    Patent number: 6353110
    Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist the synthesis of this key intermediate via an asymmetric conjugate addition reaction.
    Type: Grant
    Filed: November 24, 1999
    Date of Patent: March 5, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Paul N. Devine, Richard D. Tillyer, Richard M. Heid, Jr., David M. Tschaen
  • Therapeutic polymorphs of a GABA-A alpha-5 inverse agonist and pamoate formulations of the same
    Publication number: 20010049439
    Abstract: There is disclosed 3-(5-methylisoxazol-3-yl)-6-(1-methyl-1,2,3-triazol-4-yl)methyloxy-1,2,4-triazolo[3,4-a]phthalazine in the form of a dihydrate, a dehydrate of the dihydrate and a pentahydrate, pharmaceutical compositions comprising the forms, the use of the forms for enhancing cognition, processes for producing the forms, their incorporation in pharmaceutical compositions comprising pamoate ions and the use of such ions for solubilizing neutral molecules.
    Type: Application
    Filed: November 30, 2000
    Publication date: December 6, 2001
    Applicant: Merck & Co., Inc.
    Inventors: Michael J. Kaufman, James A. McCauley, Daniel J. Rush, David M. Tschaen, Richard J. Varsolona, Guo-Jie Ho
  • Oxidation process using periodic acid
    Patent number: 6172231
    Abstract: The present invention relates to a periodic acid oxidation which converts the penultimate intermediate bearing a primary alcohol to the target endothelin antagonist compound of Formula I having a carboxylic acid.
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: January 9, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Zhiguo Song, Mangzu Zhao, David M. Tschaen
  • Asymmetric conjugate addition reaction
    Patent number: 6172235
    Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist and the synthesis of this key intermediate using an asymmetric conjugate addition reaction.
    Type: Grant
    Filed: April 27, 1999
    Date of Patent: January 9, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen
  • Oxidation process using periodic acid
    Patent number: 6150554
    Abstract: The present invention relates to an oxidation which converts a primary or secondary alcohol of Formula II: ##STR1## to an acid or ketone of Formula I: ##STR2## with periodic acid and a catalytic amount of a chromium reagent.
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: November 21, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Jing Li, David M. Tschaen, Zhiguo Song, Mangzu Zhao
  • Oxidaton of primary alcohols to carboxylic acids with a TEMPO catalyst using NaClO.sub.2 and NaClO
    Patent number: 6127573
    Abstract: The present invention relates to a TEMPO-catalyzed oxidation of primary alcohols, RCH.sub.2 OH to corresponding carboxylic acids, RCOOH in the presence of catalytic in the presence of catalytic amount of NaClO and stoichiometric amount of NaClO.sub.2 as an oxidant.
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: October 3, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Jing Li, Zhiguo Song, David M. Tschaen, Mangzu Zhao
  • Enantioselective bioreduction using yeast
    Patent number: 6121026
    Abstract: The invention relates to a class of enantiomerically pure intermediates represented by Formula I, where X is F, Cl, Br, or I, and a novel enantioselective bioreductive process using yeast to form these intermediates, which are useful in the synthesis of endothelin antagonists, and the like.
    Type: Grant
    Filed: July 23, 1999
    Date of Patent: September 19, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Michel M. Chartrain, Barbara A. Krulewicz, Paul N. Devine, David M. Tschaen
  • Phosphate-mediated cyclization
    Patent number: 6046327
    Abstract: This invention relates to a cyclization process useful in the preparation of a key intermediate in the preparation of an endothelin antagonist of the general formula shown below: ##STR1##
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: April 4, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Richard D. Tillyer, David M. Tschaen, Zhiguo Song, Mangzu Zhao
  • Oxidation process using tempo
    Patent number: 6031101
    Abstract: The present invention relates to an oxidation using sodium chlorite in the presence of a catalytic amount of TEMPO and sodium hypochlorite which converts the penultimate intermediate bearing a primary alcohol to the target endothelin antagonist compound of Formula I having a carboxylic acid ##STR1##
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: February 29, 2000
    Assignees: Merck & Co., Inc., Banyu Pharmaceuticals Co., Ltd
    Inventors: Paul N. Devine, Eiichi Mano, Zhiguo Song, David M. Tschaen, Mangzu Zhao
  • Pyridine propanoic acid derivatives
    Patent number: 6022972
    Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist the synthesis of this key intermediate via an asymmetric conjugate addition reaction.
    Type: Grant
    Filed: July 14, 1998
    Date of Patent: February 8, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Paul N. Devine, Richard D. Tillyer, Richard M. Heid, Jr., David M. Tschaen
  • Asymmetric conjugate addition reaction using a chiral additive
    Patent number: 5998625
    Abstract: This invention relates to a process for the preparation of a key intermediate using an chiral additive to effect an asymmetric conjugate addition.
    Type: Grant
    Filed: January 5, 1998
    Date of Patent: December 7, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Richard D. Tillyer, David M. Tschaen, Feng Xu
  • Stereoselective deoxygenation reaction
    Patent number: 5962688
    Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist, the synthesis of this key intermediate and the synthesis of an endothelin antagonist using this intermediate in a stereoselective deoxygenation reaction.
    Type: Grant
    Filed: August 8, 1997
    Date of Patent: October 5, 1999
    Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.
    Inventors: Paul N. Devine, Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen, Yoshiaki Kato