Patents by Inventor Michael-Harold Rock

Michael-Harold Rock 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: 7834201
    Abstract: The present invention relates to the crystalline base of the well known antidepressant drug escitalopram, S-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile, formulations of said base, a process for the preparation of purified salts of escitalopram, such as the oxalate, using the base, the salts obtained by said process and formulations containing such salts, and a process for the preparation of purified escitalopram free base or salts of escitalopram, such as the oxalate, using the hydrobromide, the salts obtained by said process and formulations containing such salts. Finally the present invention relates to an orodispersible tablet having a hardness of at least 22 N and an oral-disintegration time of less than 120 s and comprising an active pharmaceutical ingredient adsorbed onto a water soluble filler wherein the active pharmaceutical ingredient has a melting point in the range of 40-100° C., as well as a method for making such an orodispersible tablet.
    Type: Grant
    Filed: June 21, 2006
    Date of Patent: November 16, 2010
    Assignee: H. Lundbeck A/S
    Inventors: Robert Dancer, Hans Petersen, Ole Nielsen, Michael Harold Rock, Helle Eliasen, Ken Liljegren
  • Patent number: 7723533
    Abstract: The present invention relates to the crystalline base of the well known antidepressant drug escitalopram, S-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzo-furancarbonitrile, formulations of said base, a process for the preparation of purified salts of escitalopram, such as the oxalate, using the base, the salts obtained by said process and formulations containing such salts, and a process for the preparation of purified escitalopram free base or salts of escitalopram, such as the oxalate, using the hydrobromide, the salts obtained by said process and formulations containing such salts. Finally the present invention relates to an orodispersible tablet having a hardness of at least 22 N and an oral-disintegration time of less than 120 s and comprising an active pharmaceutical ingredient adsorbed onto a water soluble filler wherein the active pharmaceutical ingredient has a melting point in the range of 40-100° C., as well as a method for making such an orodispersible tablet.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: May 25, 2010
    Assignee: H. Lundbeck A/S
    Inventors: Robert Dancer, Hans Petersen, Ole Nielsen, Michael Harold Rock, Helle Eliasen, Ken Liljegren
  • Patent number: 7560576
    Abstract: The present invention relates to the crystalline base of the well known antidepressant drug escitalopram, S-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzo-furancarbonitrile, formulations of said base, a process for the preparation of purified salts of escitalopram, such as the oxalate, using the base, the salts obtained by said process and formulations containing such salts, and a process for the preparation of purified escitalopram free base or salts of escitalopram, such as the oxalate, using the hydrobromide, the salts obtained by said process and formulations containing such salts. Finally the present invention relates to an orodispersible tablet having a hardness of at least 22 N and an oral-disintegration time of less than 120 s and comprising an active pharmaceutical ingredient adsorbed onto a water soluble filler wherein the active pharmaceutical ingredient has a melting point in the range of 40-100° C., as well as a method for making such an orodispersible tablet.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: July 14, 2009
    Assignee: H. Lundbeck A/S
    Inventors: Robert Dancer, Hans Petersen, Ole Nielsen, Michael Harold Rock, Helle Eliasen, Ken Liljegren
  • Publication number: 20090088469
    Abstract: Method for the preparation of citalopram comprising reaction of a compound of Formula (IV) wherein R is halogen, or CF3—(CF2)n—SO2—, n being 0 to 8, with a cyanide source in the presence of a palladium catalyst and a catalytic amount of Cu+ or Zn2+, or with Zn(CN)2 in the presence of a palladium catalyst.
    Type: Application
    Filed: December 8, 2008
    Publication date: April 2, 2009
    Applicant: H. Lundbeck A/S
    Inventors: Hans Petersen, Michael Harold Rock, Henrik Svane
  • Publication number: 20080161584
    Abstract: The present invention relates to the crystalline base of the well known antidepressant drug escitalopram, S-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzo-furancarbonitrile, formulations of said base, a process for the preparation of purified salts of escitalopram, such as the oxalate, using the base, the salts obtained by said process and formulations containing such salts, and a process for the preparation of purified escitalopram free base or salts of escitalopram, such as the oxalate, using the hydrobromide, the salts obtained by said process and formulations containing such salts. Finally the present invention relates to an orodispersible tablet having a hardness of at least 22 N and an oral-disintegration time of less than 120 s and comprising an active pharmaceutical ingredient adsorbed onto a water soluble filler wherein the active pharmaceutical ingredient has a melting point in the range of 40-100° C., as well as a method for making such an orodispersible tablet.
    Type: Application
    Filed: March 12, 2008
    Publication date: July 3, 2008
    Applicant: H. LUNDBECK A/S
    Inventors: Robert Dancer, Hans Petersen, Ole Nielsen, Michael Harold Rock, Helle Eliasen, Ken Liljegren
  • Publication number: 20080161388
    Abstract: The present invention relates to the crystalline base of the well known antidepressant drug escitalopram, S-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzo-furancarbonitrile, formulations of said base, a process for the preparation of purified salts of escitalopram, such as the oxalate, using the base, the salts obtained by said process and formulations containing such salts, and a process for the preparation of purified escitalopram free base or salts of escitalopram, such as the oxalate, using the hydrobromide, the salts obtained by said process and formulations containing such salts. Finally the present invention relates to an orodispersible tablet having a hardness of at least 22 N and an oral-disintegration time of less than 120 s and comprising an active pharmaceutical ingredient adsorbed onto a water soluble filler wherein the active pharmaceutical ingredient has a melting point in the range of 40-100° C., as well as a method for making such an orodispersible tablet.
    Type: Application
    Filed: March 12, 2008
    Publication date: July 3, 2008
    Applicant: H. LUNDBECK A/S
    Inventors: Robert Dancer, Hans Petersen, Ole Nielsen, Michael Harold Rock, Helle Eliasen, Ken Liljegren
  • Patent number: 7271273
    Abstract: The invention provides a new and improved method for the preparation of 5-cyano-phtalid, which is a key intermediate in the preparation of the antidepressant compound citalopram.
    Type: Grant
    Filed: November 23, 2005
    Date of Patent: September 18, 2007
    Assignee: H. Lundbeck A/S
    Inventors: Hans Petersen, Michael Harold Rock
  • Patent number: 6768011
    Abstract: The invention relates to a method for the preparation of citalopram comprising reaction of a compound of formula II with a compound having the formula wherein R is halogen or —O—SO2—X, wherein X is alkyl, alkenyl, alkynyl or optionally alkyl substituted aryl or aralkyl, and R1 is dimethylamino, halogen, —O—SO2—X wherein X is as defined above, provided that R is not halogen when R1 is dimethylamino; and if R1 is dimethylamino followed by isolation of citalopram base or a pharmaceutically acceptable acid addition salt thereof, and if R1 is halogen or —O—SO2—X, wherein X is as defined above, followed by conversion of the resulting compound of formula wherein R2 is halogen or a group of formula —O—SO2—X wherein X is as defined above to citalopram, followed by isolation of citalopram base or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: August 29, 2002
    Date of Patent: July 27, 2004
    Assignee: H. Lundbeck A/S
    Inventors: Michael Harold Rock, Haleh Ahmadian
  • Patent number: 6750358
    Abstract: Method for the preparation of citalopram comprising reaction of a compound of Formula (IV) wherein R is Cl or Br with a cyanide source in the presence of a nickel catalyst and isolation of the corresponding 5-cyano compound, i.e. citalopram.
    Type: Grant
    Filed: November 6, 2001
    Date of Patent: June 15, 2004
    Assignee: H. Lundbeck A/S
    Inventors: Hans Petersen, Michael Harold Rock
  • Patent number: 6727279
    Abstract: The present invention relates to novel arylsulphonamides and analogues, to processes for their preparation and to their use for the prophylaxis and treatment of neurodegenerative disorders, in particular for the treatment of cerebral apoplexy, craniocerebral trauma, pain and spasticity.
    Type: Grant
    Filed: August 21, 2002
    Date of Patent: April 27, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Joachim Mittendorf, Jürgen Dressel, Michael Matzke, Jörg Keldenich, Frank Mauler, Jean-Marie-Victor de Vry, Jürgen Franz, Peter Spreyer, Verena Vöhringer, Joachim Schumacher, Michael-Harold Rock, Ervin Horvàth, Arno Friedl, Klaus-Helmut Mohrs, Siegfried Raddatz, Reinhard Jork
  • Publication number: 20030114692
    Abstract: A method for the preparation of citalopram wherein the aldehyde of formula 1
    Type: Application
    Filed: November 1, 2002
    Publication date: June 19, 2003
    Applicant: H. Lundbeck A/S
    Inventors: Hans Petersen, Michael Harold Rock
  • Patent number: 6573278
    Abstract: The present invention relates to new aryl ether sulphonamides and analogues, processes for their preparation and their use for the treatment of neurodegenerative disorders, in particular for the prophylaxis and treatment of neurodegenerative disorders, in particular for the treatment of cerebral apoplexy and craniocerebral trauma.
    Type: Grant
    Filed: June 11, 2001
    Date of Patent: June 3, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Joachim Mittendorf, Jürgen Dressel, Michael Matzke, Jörg Keldenich, Klaus-Helmut Mohrs, Siegfried Raddatz, Jürgen Franz, Peter Spreyer, Verena Vöhringer, Joachim Schuhmacher, Michael-Harold Rock, Ervin Horváth, Arno Friedl, Frank Mauler, Jean Marie Viktor de Vry, Reinhard Jork
  • Patent number: 6566540
    Abstract: A method for the preparation of S-citalopram comprising reaction of a compound of Formula (IV), wherein R is C1-6 alkyl, acyl, C1-6 alkylsulfonyl or arylsulfonyl, with 3-(N,N-dimethylamino)-propyl magnesium halide, to prepare citalopram.
    Type: Grant
    Filed: May 3, 2002
    Date of Patent: May 20, 2003
    Assignee: H. Lundbeck A/S
    Inventors: Michael Harold Rock, Hans Petersen, Peter Ellegaard
  • Publication number: 20030092761
    Abstract: The invention relates to a method for the preparation of citalopram comprising reaction of a compound of formula II 1
    Type: Application
    Filed: August 29, 2002
    Publication date: May 15, 2003
    Applicant: H. Lundbeck A/S
    Inventors: Michael Harold Rock, Haleh Ahmadian
  • Publication number: 20030083508
    Abstract: A method for the preparation of citalopram wherein the aldehyde of formula 1
    Type: Application
    Filed: August 23, 2002
    Publication date: May 1, 2003
    Applicant: H. Lundbeck A/S
    Inventors: Hans Petersen, Michael Harold Rock
  • Publication number: 20030073727
    Abstract: The present invention relates to novel arylsulphonamides and analogues, to processes for their preparation and to their use for the prophylaxis and treatment of neurodegenerative disorders, in particular for the treatment of cerebral apoplexy, craniocerebral trauma, pain and spasticity.
    Type: Application
    Filed: August 21, 2002
    Publication date: April 17, 2003
    Inventors: Joachim Mittendorf, Jurgen Dressel, Michael Matzke, Jorg Keldenich, Frank Mauler, Jean-Marie-Victor de Vry, Jurgen Franz, Peter Spreyer, Verena Vohringer, Joachim Schumacher, Michael-Harold Rock, Ervin Horvath, Arno Friedl, Klaus-Helmut Mohrs, Siegfried Raddatz, Reinhard Jork
  • Patent number: 6545050
    Abstract: The present invention relates to novel amino acid esters of arylsulphonamides and analogues, to processes for their preparation and to their use for the prophylaxis and treatment of neurodegenerative disorders, in particular for the treatment of cerebral apoplexy, craniocerebral trauma, pain and spasticity.
    Type: Grant
    Filed: February 16, 2001
    Date of Patent: April 8, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Joachim Mittendorf, Jürgen Dressel, Michael Matzke, Jörg Keldenich, Frank Mauler, Jean-Marie-Viktor de Vry, Jürgen Franz, Peter Spreyer, Verena Vöhringer, Joachim Schumacher, Michael-Harold Rock, Ervin Horvàth, Arno Friedl
  • Publication number: 20020198391
    Abstract: The invention provides a new and improved method for the preparation of 5-cyano-phtalid, which is a key intermediate in the preparation of the antidepressant compound citalopram.
    Type: Application
    Filed: June 27, 2002
    Publication date: December 26, 2002
    Applicant: H. Lundbeck A/S
    Inventors: Hans Petersen, Michael Harold Rock
  • Publication number: 20020177722
    Abstract: A method for the preparation of escitalopram comprising reaction of a compound of 1
    Type: Application
    Filed: May 3, 2002
    Publication date: November 28, 2002
    Applicant: H. Lundbeck A/S
    Inventors: Michael Harold Rock, Hans Petersen, Peter Ellegaard
  • Patent number: 6469054
    Abstract: The present invention relates to novel arylsulphonamides and analogues, to processes for their preparation and to their use for the prophylaxis and treatment of neurodegenerative disorders, in particular for the treatment of cerebral apoplexy, craniocerebral trauma, pain and spasticity.
    Type: Grant
    Filed: February 16, 2001
    Date of Patent: October 22, 2002
    Assignee: Bayer Aktiengesellshaft
    Inventors: Joachim Mittendorf, Jürgen Dressel, Michael Matzke, Jörg Keldenich, Frank Mauler, Jean-Marie-Victor de Vry, Jürgen Franz, Peter Spreyer, Verena Vöhringer, Joachim Schumacher, Michael-Harold Rock, Ervin Horvàth, Arno Friedl, Klaus-Helmut Mohrs, Siegfried Raddatz, Reinhard Jork