Patents by Inventor Richard D. Tillyer

Richard D. Tillyer 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: 20030211151
    Abstract: The instant invention provides methods and pharmaceutical compositions for inhibiting HMG-CoA reductase, as well as for treating and/or reducing the risk for diseases and conditions affected by inhibition of HMG-CoA reductase, comprising orally administering a therapeutically effective amount of a compound selected from a dihydroxy open acid statin and a pharmaceutically acceptable salt or ester thereof in a delayed-release pharmaceutical dosage form to a patient in need of such treatment wherein substantial release of the compound from the dosage form is delayed until after passage of the dosage form through the stomach.
    Type: Application
    Filed: April 29, 2003
    Publication date: November 13, 2003
    Applicant: Merck & Co., Inc.
    Inventors: Richard D. Tillyer, Paul J. Reider, Edward J. J. Grabowski, Feng Xu, Jose M. Vega, Mandana Asgharnejad
  • Publication number: 20030176501
    Abstract: The instant invention provides methods and pharmaceutical compositions for inhibiting HMG-CoA reductase, as well as for treating and/or reducing the risk for diseases and conditions affected by inhibition of HMG-CoA reductase, comprising orally administering a therapeutically effective amount of a crystalline hydrated form of the calcium salt of dihydroxy open acid simvastatin to a patient in need of such treatment. Methods for making the calcium salt of dihydroxy open acid simvastatin are also provided.
    Type: Application
    Filed: November 13, 2002
    Publication date: September 18, 2003
    Inventors: Richard D. Tillyer, Paul J. Reider, Edward J. J. Grabowski, Feng Xu, Robert M. Wenslow, Jose M. Vega, Richard J. Varsolona
  • Patent number: 6569461
    Abstract: The instant invention provides methods and pharmaceutical compositions for inhibiting HMG-CoA reductase, as well as for treating and/or reducing the risk for diseases and conditions affected by inhibition of HMG-CoA reductase, comprising orally administering a therapeutically effective amount of a compound selected from a dihydroxy open acid statin and a pharmaceutically acceptable salt or ester thereof in a delayed-release pharmaceutical dosage form to a patient in need of such treatment wherein substantial release of the compound from the dosage form is delayed until after passage of the dosage form through the stomach.
    Type: Grant
    Filed: April 26, 2000
    Date of Patent: May 27, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Richard D. Tillyer, Paul J. Reider, Edward J. J. Grabowski, Feng Xu, Jose M. Vega, Mandana Asgharnejad
  • 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
  • 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
  • Patent number: 6281391
    Abstract: This invention encompasses a novel process for synthesizing compounds represented by formula A: These compounds are intermediates useful in the preparation of certain agents that are selective COX-2 inhibitors.
    Type: Grant
    Filed: October 27, 1999
    Date of Patent: August 28, 2001
    Assignees: Merck & Co., Inc., Merck Frosst Canada & Co.
    Inventors: Richard D. Tillyer, Ian W. Davies, Robert D. Larsen, Xin Wang, Paul O'Shea, Anthony On-Ping King, Dalian Zhao, Cheng Y. Chen, Edward J. J. Grabowski
  • 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
  • Patent number: 6232472
    Abstract: This invention encompasses a novel process for synthesizing the compound represented by formula I: These compounds are useful as non-steroidal anti-inflammatory agents.
    Type: Grant
    Filed: September 13, 2000
    Date of Patent: May 15, 2001
    Assignee: Merck Frosst Canada & Co.
    Inventors: Paul O'Shea, Xin Wang, Richard D. Tillyer, Sophie-Dorothee Clas, Chad Dalton
  • 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
  • Patent number: 6150534
    Abstract: This invention encompasses a novel process for synthesizing the compound represented by formula I: ##STR1## These compounds are useful as non-steroidal anti-inflammatory agents.
    Type: Grant
    Filed: January 14, 2000
    Date of Patent: November 21, 2000
    Assignee: Merck Frosst Canada & Co.
    Inventors: Paul O'Shea, Richard D. Tillyer, Xin Wang, Sophie-Dorothee Clas, Chad Dalton
  • Patent number: 6114569
    Abstract: An efficient method for the preparation of a compound of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-ben zoxazin-2-one, also known as DMP-266, a reverse transcriptase inhibitor is achieved using a cyclization reaction of the amino alcohol intermediate with an alkyl or aryl chloroformate and a base.
    Type: Grant
    Filed: January 4, 1999
    Date of Patent: September 5, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Lisa F. Frey, Edward J. J. Grabowski, Richard D. Tillyer
  • 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
  • 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
  • Patent number: 6015926
    Abstract: An efficient method for the preparation of key intermediate, in the synthesis of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-ben zoxazin-2-one, a reverse transcriptase inhibitor is achieved using a chiral addition reaction to the 4-chloro-2-trifluoromethylketoaniline with an organozinc complex to give the desired alcohol. This instant method has broad applicability in the chiral addition to any prochiral ketone.
    Type: Grant
    Filed: May 11, 1998
    Date of Patent: January 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Cheng Yi Chen, Lushi Tan, Richard D. Tillyer
  • 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
  • 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
  • Patent number: 5952528
    Abstract: A process for enhancing the purity of 2R-?1-hydroxy-1-trifluoromethyl-3-cyclopropylpropyn-2-yl!-4-chloroaniline comprising the formation of an acid addition salt which is capable of rejecting the racemate in the selected organic solvent.
    Type: Grant
    Filed: September 2, 1998
    Date of Patent: September 14, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Cheng Yi Chen, Edward J. J. Grabowski, Paul J. Reider, Lushi Tan, Richard D. Tillyer
  • Patent number: 5922864
    Abstract: An efficient method for the preparation of a compound of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl- 1,4-dihydro-2H-3, 1-benzoxazin-2-one, also known as DMP-266, a reverse transcriptase inhibitor is achieved using a cyclization reaction of the amino alcohol intermediate with an alkyl or aryl chloroformate and a base.
    Type: Grant
    Filed: February 3, 1998
    Date of Patent: July 13, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Lisa F. Frey, Richard D. Tillyer, Edward J. J. Grabowski
  • Patent number: 5856492
    Abstract: An efficient method for the quantitative preparation and isolation of a compound of formula I ##STR1## or its enantiomer, a chiral mediator used in enantioselective synthesis.
    Type: Grant
    Filed: January 5, 1998
    Date of Patent: January 5, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Cheng Yi Chen, Feng Xu, Richard D. Tillyer, Dalian Zhao
  • Patent number: 5849914
    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: August 4, 1997
    Date of Patent: December 15, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen