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).
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Patent number: 7834201Abstract: 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: GrantFiled: June 21, 2006Date of Patent: November 16, 2010Assignee: H. Lundbeck A/SInventors: Robert Dancer, Hans Petersen, Ole Nielsen, Michael Harold Rock, Helle Eliasen, Ken Liljegren
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Patent number: 7723533Abstract: 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: GrantFiled: March 12, 2008Date of Patent: May 25, 2010Assignee: H. Lundbeck A/SInventors: Robert Dancer, Hans Petersen, Ole Nielsen, Michael Harold Rock, Helle Eliasen, Ken Liljegren
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Patent number: 7560576Abstract: 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: GrantFiled: March 12, 2008Date of Patent: July 14, 2009Assignee: H. Lundbeck A/SInventors: Robert Dancer, Hans Petersen, Ole Nielsen, Michael Harold Rock, Helle Eliasen, Ken Liljegren
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Publication number: 20090088469Abstract: 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: ApplicationFiled: December 8, 2008Publication date: April 2, 2009Applicant: H. Lundbeck A/SInventors: Hans Petersen, Michael Harold Rock, Henrik Svane
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Publication number: 20080161584Abstract: 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: ApplicationFiled: March 12, 2008Publication date: July 3, 2008Applicant: H. LUNDBECK A/SInventors: Robert Dancer, Hans Petersen, Ole Nielsen, Michael Harold Rock, Helle Eliasen, Ken Liljegren
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Publication number: 20080161388Abstract: 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: ApplicationFiled: March 12, 2008Publication date: July 3, 2008Applicant: H. LUNDBECK A/SInventors: Robert Dancer, Hans Petersen, Ole Nielsen, Michael Harold Rock, Helle Eliasen, Ken Liljegren
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Patent number: 7271273Abstract: 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: GrantFiled: November 23, 2005Date of Patent: September 18, 2007Assignee: H. Lundbeck A/SInventors: Hans Petersen, Michael Harold Rock
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Patent number: 6768011Abstract: 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: GrantFiled: August 29, 2002Date of Patent: July 27, 2004Assignee: H. Lundbeck A/SInventors: Michael Harold Rock, Haleh Ahmadian
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Patent number: 6750358Abstract: 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: GrantFiled: November 6, 2001Date of Patent: June 15, 2004Assignee: H. Lundbeck A/SInventors: Hans Petersen, Michael Harold Rock
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Patent number: 6727279Abstract: 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: GrantFiled: August 21, 2002Date of Patent: April 27, 2004Assignee: Bayer AktiengesellschaftInventors: 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
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Publication number: 20030114692Abstract: A method for the preparation of citalopram wherein the aldehyde of formula 1Type: ApplicationFiled: November 1, 2002Publication date: June 19, 2003Applicant: H. Lundbeck A/SInventors: Hans Petersen, Michael Harold Rock
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Aryl sulfonamides and analogues thereof and their use in the treatment of neurodegenerative diseases
Patent number: 6573278Abstract: 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: GrantFiled: June 11, 2001Date of Patent: June 3, 2003Assignee: Bayer AktiengesellschaftInventors: 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: 6566540Abstract: 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: GrantFiled: May 3, 2002Date of Patent: May 20, 2003Assignee: H. Lundbeck A/SInventors: Michael Harold Rock, Hans Petersen, Peter Ellegaard
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Publication number: 20030092761Abstract: The invention relates to a method for the preparation of citalopram comprising reaction of a compound of formula II 1Type: ApplicationFiled: August 29, 2002Publication date: May 15, 2003Applicant: H. Lundbeck A/SInventors: Michael Harold Rock, Haleh Ahmadian
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Publication number: 20030083508Abstract: A method for the preparation of citalopram wherein the aldehyde of formula 1Type: ApplicationFiled: August 23, 2002Publication date: May 1, 2003Applicant: H. Lundbeck A/SInventors: Hans Petersen, Michael Harold Rock
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Publication number: 20030073727Abstract: 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: ApplicationFiled: August 21, 2002Publication date: April 17, 2003Inventors: 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
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Patent number: 6545050Abstract: 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: GrantFiled: February 16, 2001Date of Patent: April 8, 2003Assignee: Bayer AktiengesellschaftInventors: 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
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Publication number: 20020198391Abstract: 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: ApplicationFiled: June 27, 2002Publication date: December 26, 2002Applicant: H. Lundbeck A/SInventors: Hans Petersen, Michael Harold Rock
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Publication number: 20020177722Abstract: A method for the preparation of escitalopram comprising reaction of a compound of 1Type: ApplicationFiled: May 3, 2002Publication date: November 28, 2002Applicant: H. Lundbeck A/SInventors: Michael Harold Rock, Hans Petersen, Peter Ellegaard
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Patent number: 6469054Abstract: 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: GrantFiled: February 16, 2001Date of Patent: October 22, 2002Assignee: Bayer AktiengesellshaftInventors: 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