Patents by Inventor Philip J. Pye

Philip J. Pye 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).

  • HIV integrase inhibitors
    Patent number: 7598264
    Abstract: Hydroxy (tetra- or hexa-)hydronaphthyridine dione compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein a, R1?, R2?, R3?, R4? and R5? are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: March 9, 2005
    Date of Patent: October 6, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Wei Han, Melissa Egbertson, John S. Wai, Linghang Zhuang, Rowena D. Ruzek, Debra S. Perlow, Mark Cameron, Bruce S. Foster, Ulf H. Dolling, R. Scott Hoerrner, Philip J. Pye, Remy Angelaud, Danny E. Mancheno, David Askin
  • Process for preparing integrin antagonist intermediate
    Patent number: 6914144
    Abstract: A process is provided for the preparation of 2,5-di-(3?-aminopropyl)pyridine which is useful in the synthesis of ?v?3 integrin receptor antagonists. Also provided are useful intermediates obtained from the process.
    Type: Grant
    Filed: January 29, 2003
    Date of Patent: July 5, 2005
    Assignee: Merck & Co., Inc.
    Inventor: Philip J. Pye
  • Process for preparing integrin antagonist intermediate
    Publication number: 20030176707
    Abstract: A novel process is provided for the preparation of 2,5-di-(3′-aminopropyl)pyridine which is useful in the synthesis of &agr;v&bgr;3 integrin receptor antagonists. Also provided are useful intermediates obtained from the process.
    Type: Application
    Filed: January 29, 2003
    Publication date: September 18, 2003
    Inventor: Philip J. Pye
  • 4-Benzyl-2-hydroxy-1,4-oxazine-3-one and polymorphic forms thereof
    Patent number: 6538134
    Abstract: The present invention is concerned with 4-benzyl-2-hydroxy-1,4-oxazin-3-one, and novel processes for the preparation therof. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Grant
    Filed: June 8, 2001
    Date of Patent: March 25, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Louis S. Crocker, Karel M. Jos Brands, Todd D. Nelson, Philip J. Pye, Jonathan D. Rosen, Kai Rossen
  • Process for the synthesis of (2R, 2-alpha-R)-4-benzyl-2-[1-(3,5-bis (trifluoromethyl)phenyl)ethoxy]-1,4-oxazine-3-one
    Patent number: 6469164
    Abstract: The present invention is concerned with novel processes for the preparation of (2R, 2-alpha-R)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy-1,4-oxazin-3-one. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Grant
    Filed: June 8, 2001
    Date of Patent: October 22, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Karel M. Jos Brands, Joseph F. Payack, Philip J. Pye
  • Intramolecular glycosidation process for the synthesis of (2R, 2-alpha-R, 3a)-2-[1-(3,5- bis (trifluoromethyl) phenyl)ethoxy]-3-(4-fluorophenyl)-1,4-oxazine
    Patent number: 6403793
    Abstract: The present invention is concerned with novel processes for the preparation of (2R-cis)-2-[[1-[3.5-bis(trifluoromethyl)phenyl]ethenyl]oxy]-3-(4-fluorophenyl)-4-(phenylmethyl) mopholine. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Grant
    Filed: June 8, 2001
    Date of Patent: June 11, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Philip J. Pye, Kai Rossen
  • Process for the synthesis of carbapenem intermidiates, and compounds produced
    Patent number: 6395894
    Abstract: A process of synthesizing a compound of structural formula 6 is disclosed wherein R1 represents H or a suitable protecting group for an alcohol; R2 represents a benzyl, C1-6 alkyl or aryl; Y represents C1-3 alkyl, O, NH or S; X represents O, NH, or S and R5 represents a carboxy protecting group, comprising reacting a compound of formula 5: wherein R1, R2, R5, X and Y are as previously described with a phosphite or phosphonite reagent to produce a compound of formula 6. Further disclosed is an efficient method for the synthesis of a compound of formula 2: which comprises reacting a 4-acyl-2-azetidinone with a titanium, zirconium or hafnium enolate of a 1-hydroxy-2-butanone derivative.
    Type: Grant
    Filed: April 15, 1999
    Date of Patent: May 28, 2002
    Inventors: Philip J. Pye, Paul J. Reider, Kai Rossen, Ralph P. Volante
  • Process for the synthesis of (2R, 2-alpha-R) -4-benzyl-2-[1- (3,5-bis (trifluoromethyl) phenyl) ethoxy] -1,4-oxazine-3-one
    Publication number: 20020052493
    Abstract: The present invention is concerned with novel processes for the preparation of (2R, 2-alpha-R)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy-1,4-oxazin-3-one. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Application
    Filed: June 8, 2001
    Publication date: May 2, 2002
    Inventors: Karel M. Jos Brands, Joseph F. Payack, Philip J. Pye
  • 4-Benzyl-2-hydroxy-1, 4-oxazine-3-one and polymorphic forms thereof
    Publication number: 20020042510
    Abstract: The present invention is concerned with 4-benzyl-2-hydroxy-1,4-oxazin-3-one, and novel processes for the preparation therof. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Application
    Filed: June 8, 2001
    Publication date: April 11, 2002
    Inventors: Louis S. Crocker, Karel M. Jos Brands, Todd D. Nelson, Philip J. Pye, Jonathan D. Rosen, Kai Rossen
  • Process for making diaryl pyridines useful as cox-2 inhibitors
    Patent number: 6369275
    Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: November 17, 2000
    Date of Patent: April 9, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Ian W. Davies, Michel Journet, Linda Gerena, Robert D. Larsen, Philip J. Pye, Kai Rossen
  • Intramolecular glycosidation process for the synthesis of (2R, 2-alpha-R, 3A)-2-[1-(3,5- BIS (trifluoromethyl)phenyl)ethoxy]-3-(4-fluorophenyl)-1,4-oxazine
    Publication number: 20020016458
    Abstract: The present invention is concerned with novel processes for the preparation of (2R-cis)-2-[[1 -[3.5-bis(trifluoromethyl)phenyl]ethenyl] oxy]-3-(4-fluorophenyl)-4-(phenylmethyl)mopholine. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Application
    Filed: June 8, 2001
    Publication date: February 7, 2002
    Inventors: Philip J. Pye, Kai Rossen
  • PROCESS FOR THE SYNTHESIS OF CARBAPENEM INTERMEDIATES, AND COMPOUNDS PRODUCED
    Publication number: 20010025103
    Abstract: An efficient method for the synthesis of a compound of formula 2: 1
    Type: Application
    Filed: April 15, 1999
    Publication date: September 27, 2001
    Inventors: PHILIP J. PYE, PAUL J. REIDER, KAI ROSSEN, RALPH P. VOLANTE
  • Intermediates useful in a process for synthesizing COX-2 inhibitors
    Patent number: 6252116
    Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: January 21, 2000
    Date of Patent: June 26, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Edward G. Corley, Ian W. Davies, Robert D. Larsen, Philip J. Pye, Kai Rossen
  • Process for making diaryl pyridines useful as COX-2 inhibitors
    Patent number: 6204387
    Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: March 23, 2000
    Date of Patent: March 20, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Ian W. Davies, Linda Gerena, Michel Journet, Robert D. Larsen, Philip J. Pye, Kai Rossen
  • Process for preparing 4-tert-butyloxycarbonyl-(S)-piperazine-2-tert-butylcarboxamide
    Patent number: 6156895
    Abstract: An improved process using chiral hydrogenation is described for the synthesis in high yields of a 4-protected-(S)-piperazine-2-tert-butylcarboxamide, an intermediate for an HIV protease inhibitor.
    Type: Grant
    Filed: August 4, 1999
    Date of Patent: December 5, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Kai Rossen, Philip J. Pye, Ralph P. Volante, Paul J. Reider
  • Process for making 2-aryl-3-aryl-5-halo pyridines useful as COX-2 inhibitors
    Patent number: 6130334
    Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: April 15, 1998
    Date of Patent: October 10, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Philip J. Pye, Ashok Maliakal, Kai Rossen, Ralph P. Volante, Jess Sager
  • Process for making 2-aryl-3-aryl-5-halo pyridines useful as COX-2 inhibitors
    Patent number: 6127545
    Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: September 18, 1998
    Date of Patent: October 3, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Philip J. Pye, Kai Rossen, Ashok Maliakal, Ralph P. Volante, Jess Sager, Jean-Francois Marcoux, Ian Davies, Edward G. Corley, Daniel Richard Sidler, Robert D. Larsen
  • Process for making diaryl pyridines useful as cox-2-inhibitors
    Patent number: 6040450
    Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: September 15, 1998
    Date of Patent: March 21, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Ian W. Davies, Michel Journet, Linda Gerena, Robert D. Larsen, Philip J. Pye, Kai Rossen
  • Process for synthesizing COX-2 inhibitors
    Patent number: 6040319
    Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: April 23, 1999
    Date of Patent: March 21, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Edward G. Corley, Ian W. Davies, Robert D. Larsen, Philip J. Pye, Kai Rossen
  • Process for preparing 4-tert-butyloxycarbonyl-(S)-piperazine-2-tert-butylcarboxamide
    Patent number: 5977364
    Abstract: An improved process using chiral hydrogenation is described for the synthesis in high yields of a 4-protected-(S)-piperazine-2-tert-butylcarboxaimide, an intermediate for an HIV protease inhibitor.
    Type: Grant
    Filed: February 2, 1999
    Date of Patent: November 2, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Kai Rossen, Philip J. Pye, Ralph P. Volante, Paul J. Reider