Patents by Inventor Cristina Gardelli

Cristina Gardelli 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).

  • Patent number: 8314062
    Abstract: The present invention relates to macrocyclic compounds of formula (I): wherein W, n, m, R1, R2, R3, R4, R5, Ra, M, Z and ring B are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
    Type: Grant
    Filed: June 21, 2007
    Date of Patent: November 20, 2012
    Assignee: Instituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A.
    Inventors: Benedetta Crescenzi, Monica Donghi, Marco Ferrara, Cristina Gardelli, Steven Harper, Uwe Koch, Michael Rowley, Vincenzo Summa
  • Patent number: 8148349
    Abstract: The present invention provides nucleoside cyclic phosphoramidates of formula (I), pharmaceutical compositions comprising the compounds of formula (I) and methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection using the compounds of formula (I).
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: April 3, 2012
    Assignees: Istituto di Ricerche di Biologia Molecolare P. Angeletti S.P.A., Merck Sharp & Dohme Corp.
    Inventors: Malte Meppen, Frank Narjes, Barbara Pacini, Cristina Gardelli, Philippe L. Durette
  • Patent number: 8071568
    Abstract: The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside aryl phosphoramidates of the present invention.
    Type: Grant
    Filed: December 28, 2007
    Date of Patent: December 6, 2011
    Assignees: Merck Sharp & Dohme Corp., Instituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A.
    Inventors: Frank Narjes, Cristina Gardelli, Monica Donghi, Barbara Attenni, Philippe L. Durette
  • Publication number: 20110034449
    Abstract: N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Application
    Filed: September 17, 2010
    Publication date: February 10, 2011
    Applicant: Istituto di Ricerche di Biologia Molecolare P. Angeletti SpA
    Inventors: Benedetta Crescenzi, Cristina Gardelli, Ester Muraglia, Emanuela Nizi, Federica Orvieto, Paola Pace, Giovanna Pescatore, Alessia Petrocchi, Marco Poma, Michael Rowley, Rita Scarpelli, Vincenzo Summa
  • Patent number: 7879815
    Abstract: The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside aryl phosphoramidates of the present invention.
    Type: Grant
    Filed: February 12, 2007
    Date of Patent: February 1, 2011
    Assignees: Merck Sharp & Dohme Corp., Istituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A.
    Inventors: Malcolm MacCoss, David B. Olsen, Monica Donghi, Cristina Gardelli, Steven Harper, Malte Meppen, Frank Narjes, Barbara Pacini
  • Patent number: 7820660
    Abstract: N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: October 26, 2010
    Assignee: Instituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A.
    Inventors: Benedetta Crescenzi, Cristina Gardelli, Ester Muraglia, Emanuela Nizi, Federica Orvieto, Paola Pace, Giovanna Pescatore, Alessia Petrocchi, Marco Poma, Michael Rowley, Rita Scarpelli, Vincenzo Summa
  • Publication number: 20100234316
    Abstract: The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside aryl phosphoramidates of the present invention.
    Type: Application
    Filed: February 12, 2007
    Publication date: September 16, 2010
    Inventors: Malcolm MacCoss, David B. Olsen, Monica Donghi, Cristina Gardelli, Steven Harper, Malte Meppen, Frank Narjes, Barbara Pacini
  • Publication number: 20100152128
    Abstract: A compound of formula (I) and pharmaceutically acceptable salts thereof; compositions containing it and its use in medicine, particularly for the treatment or inhibition of HCV infections, and processes for making it are disclosed.
    Type: Application
    Filed: May 19, 2008
    Publication date: June 17, 2010
    Inventors: Barbara Attenni, Monica Donghi, Cristina Gardelli, Malte Meppen, Frank Narjes, Barbara Pacini
  • Publication number: 20100035835
    Abstract: The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside aryl phosphoramidates of the present invention.
    Type: Application
    Filed: December 28, 2007
    Publication date: February 11, 2010
    Inventors: Frank Narjes, Cristina Gardelli, Monica Donghi, Barbara Attenni, Philippe L. Durette
  • Publication number: 20100022468
    Abstract: The present invention provides nucleoside cyclic phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as pre-cursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside cyclic phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside cyclic phosphoramidates of the present invention.
    Type: Application
    Filed: December 14, 2007
    Publication date: January 28, 2010
    Inventors: Malte Meppen, Frank Narjes, Barbara Pacini, Cristina Gardelli, Philippe L. Durette
  • Publication number: 20090312241
    Abstract: The present invention relates to macrocyclic compounds of formula (I): wherein W, n, m, R1, R2, R3, R4, R5, Ra, M, Z and ring B are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
    Type: Application
    Filed: June 21, 2007
    Publication date: December 17, 2009
    Applicant: Istituto di Ricerche di Biologia Molecolare P. Angeletti SPA
    Inventors: Benedetta Crescenzi, Monica Donghi, Marco Ferrara, Cristina Gardelli, Steven Harper, Uwe Koch, Michael Rowley, Vincenzo Summa
  • Publication number: 20090099168
    Abstract: Pyridopyrazine- and pyrimidopyrazine-dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dihydroxypyridine carboxamides are of Formula I: wherein G, Q, bond a, R5, R6 and R7 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: Application
    Filed: December 9, 2008
    Publication date: April 16, 2009
    Inventors: Monica Donghi, Cristina Gardelli
  • Patent number: 7459452
    Abstract: 4,5-Dihydroxypyrimidine-6-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: September 7, 2006
    Date of Patent: December 2, 2008
    Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A.
    Inventors: Maria E. Di Francesco, Cristina Gardelli, Steven Harper, Victor G. Matassa, Ester Murgalia, Emanuela Nizi, Paola Pace, Barbara Pacini, Alessia Petrocchi, Marco Poma, Vincenzo Summa
  • Publication number: 20080275004
    Abstract: N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Application
    Filed: June 20, 2008
    Publication date: November 6, 2008
    Inventors: Benedetta Crescenzi, Cristina Gardelli, Ester Muraglia, Emanuela Nizi, Federica Orvieto, Paola Pace, Giovanna Pescatore, Alessia Petrocchi, Marco Poma, Michael Rowley, Rita Scarpelli, Vincenzo Summa
  • Patent number: 7435734
    Abstract: N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: December 19, 2006
    Date of Patent: October 14, 2008
    Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A.
    Inventors: Benedetta Crescenzi, Cristina Gardelli, Ester Muraglia, Emanuela Nizi, Federica Orvieto, Paola Pace, Giovanna Pescatore, Alessia Petrocchi, Marco Poma, Michael Rowley, Rita Scarpelli, Vincenzo Summa
  • Publication number: 20070161639
    Abstract: Pyridopyrazine- and pyrimidopyrazine-dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dihydroxypyridine carboxamides are of Formula (I); wherein G, Q, bond a, R5, R6 and R7 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: Application
    Filed: March 1, 2005
    Publication date: July 12, 2007
    Inventors: Philip Jones, Vincenzo Summa, Monica Donghi, Cristina Gardelli
  • Patent number: 7232819
    Abstract: 4,5-Dihydroxypyrimidine-6-carboxamides of formula (I); are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These 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: October 21, 2002
    Date of Patent: June 19, 2007
    Assignee: Istituto Di Ricerche Di Biologia P. Angeletti S.p.A.
    Inventors: Maria E. Di Francesco, Cristina Gardelli, Steven Harper, Victor G. Matassa, Ester Murgalia, Emanuela Nizi, Paola Pace, Barbara Pacini, Alessia Petrocchi, Marco Poma, Vincenzo Summa
  • Publication number: 20070123524
    Abstract: N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Application
    Filed: December 19, 2006
    Publication date: May 31, 2007
    Inventors: Benedetta Crescenzi, Cristina Gardelli, Ester Muraglia, Emanuela Nizi, Federica Orvieto, Paola Pace, Giovanna Pescatore, Alessia Petrocchi, Marco Poma, Michael Rowley, Rita Scarpelli, Vincenzo Summa
  • Patent number: 7217713
    Abstract: N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: July 24, 2006
    Date of Patent: May 15, 2007
    Assignee: Istituto Di Richerche Di Biologia Molecolare P. Angeletti S.p.A.
    Inventors: Benedetta Crescenzi, Cristina Gardelli, Ester Muraglia, Emanuela Nizi, Federica Orvieto, Paola Pace, Giovanna Pescatore, Alessia Petrocchi, Marco Poma, Michael Rowley, Rita Scarpelli, Vincenzo Summa
  • Publication number: 20070083045
    Abstract: 4,5-Dihydroxypyrimidine-6-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Application
    Filed: September 7, 2006
    Publication date: April 12, 2007
    Inventors: Maria Di Francesco, Cristina Gardelli, Steven Harper, Victor Matassa, Ester Murgalia, Emanuela Nizi, Paola Pace, Barbara Pacini, Alessia Petrocchi, Marco Poma, Vincenzo Summa