Patents by Inventor Michel Surkyn

Michel Surkyn 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: 9580433
    Abstract: The present invention relates to novel 5,6-dihydroimidazo[1,5-a]pyrazinyl derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, in particular BACE1 and/or BACE2 (wherein BACE1, is also known as Asp2, or memapsin2 and BACE2 is also known as Asp1, Memapsin 1 or DRAP). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease, dementia of the Alzheimer's type, dementia associated with beta-amyloid, age-related macular degeneration, type 2 diabetes and other metabolic disorders.
    Type: Grant
    Filed: June 12, 2014
    Date of Patent: February 28, 2017
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Daniel Oehlrich, Henricus Jacobus Maria Gijsen, Michel Surkyn
  • Publication number: 20160115170
    Abstract: The present invention relates to novel 5,6-dihydroimidazo[1,5-a]pyrazinyl derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, in particular BACE1 and/or BACE2 (wherein BACE1, is also known as Asp2, or memapsin2 and BACE2 is also known as Asp1, Memapsin 1 or DRAP). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease, dementia of the Alzheimer's type, dementia associated with beta-amyloid, age-related macular degeneration, type 2 diabetes and other metabolic disorders.
    Type: Application
    Filed: June 12, 2014
    Publication date: April 28, 2016
    Inventors: Daniel Oehlrich, Henricus Jacobus, Maria Gijsen, Michel Surkyn
  • Patent number: 9284303
    Abstract: The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.
    Type: Grant
    Filed: August 6, 2013
    Date of Patent: March 15, 2016
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Henricus Jacobus Maria Gijsen, Michel Anna Jozef De Cleyn, Michel Surkyn, Bie Maria Pieter Verbist
  • Patent number: 9079886
    Abstract: The present invention is concerned with novel substituted triazole derivatives of Formula (I) wherein Het1, R1, R2, A1, A2, A3, A4, L1, and L2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: January 12, 2011
    Date of Patent: July 14, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Sven Franciscus Anna Van Brandt, Michel Anna Jozef De Cleyn, Henricus Jacobus Maria Gijsen, Didier Jean-Claude Berthelot, Michel Surkyn
  • Publication number: 20150094311
    Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Application
    Filed: December 1, 2014
    Publication date: April 2, 2015
    Inventors: HENRICUS JACOBUS MARIA GIJSEN, ADRIANA INGRID VELTER, GREGOR JAMES MACDONALD, FRANCOIS PAUL BISCHOFF, TONGFEI WU, SVEN FRANCISCUS ANNA VAN BRANDT, MICHEL SURKYN, MIRKO ZAJA, SERGE MARIA ALOYSIUS PIETERS, DIDIER JEAN-CLAUDE BERTHELOT, MICHEL ANNA JOZEF DE CLEYN, DANIEL OEHLRICH
  • Patent number: 8946426
    Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: February 2, 2010
    Date of Patent: February 3, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Henricus Jacobus Maria Gijsen, Adriana Ingrid Velter, Gregor James MacDonald, François Paul Bischoff, Tongfei Wu, Sven Franciscus Anna Van Brandt, Michel Surkyn, Mirko Zaja, Serge Maria Aloysius Pieters, Didier Jean-Claude Berthelot, Michel Anna Jozef De Cleyn, Daniel Oehlrich
  • Patent number: 8946266
    Abstract: The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: July 13, 2010
    Date of Patent: February 3, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Tongfei Wu, Henricus Jacobus Maria Gijsen, Frederik Jan Rita Rombouts, François Paul Bischoff, Didier Jean-Claude Berthelot, Daniel Oehlrich, Michel Anna Jozef De Cleyn, Serge Maria Aloysius Pieters, Garrett Berlond Minne, Adriana Ingrid Velter′, Sven Franciscus Anna Van Brandt, Michel Surkyn
  • Publication number: 20140343048
    Abstract: The invention relates to novel 6-difluoromethyl-5,6-dihydro-2H-[1,4]oxazin-3-amine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, cerebral amyloid angiopathy, multi-infarct dementia, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta-amyloid.
    Type: Application
    Filed: December 4, 2012
    Publication date: November 20, 2014
    Inventors: Andrés Avelino Trabanco-Suárez, Henricus Jacobus Maria Gijsen, Michel Surkyn, Hana Prokopcová
  • Patent number: 8772504
    Abstract: The present invention is concerned with novel substituted benzoxazole, benzimidazole, oxazolopyridine and imidazopyridine derivatives of Formula (I) wherein R1, R2, R3, R4, X, A1, A2, A3, A4, Y1, Y2, Y3 and Z have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: February 15, 2010
    Date of Patent: July 8, 2014
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Henricus Jacobus Maria Gijsen, François Paul Bischoff, Wei Zhuang, Sven Franciscus Anna Van Brandt, Michel Surkyn, Mirko Zaja, Didier Jean-Claude Berthelot, Michel Anna Jozef De Cleyn, Gregor James MacDonald, Daniel Oehlrich
  • Publication number: 20130324529
    Abstract: The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.
    Type: Application
    Filed: August 6, 2013
    Publication date: December 5, 2013
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Henricus Jacobus Maria Gijsen, Michel Anna Jozef De Cleyn, Michel Surkyn, Bie Maria Pieter Verbist
  • Patent number: 8524757
    Abstract: The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.
    Type: Grant
    Filed: July 2, 2007
    Date of Patent: September 3, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Henricus Jacobus Maria Gijsen, Michel Anna Jozef De Cleyn, Michel Surkyn, Bie Maria Pieter Verbist
  • Patent number: 8318742
    Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
    Type: Grant
    Filed: September 20, 2011
    Date of Patent: November 27, 2012
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef DeCleyn, Michel Surkyn
  • Publication number: 20120295891
    Abstract: The present invention is concerned with novel substituted triazole derivatives of Formula (I) wherein Het1, R1, R2, A1, A2, A3, A4, L1, and L2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Application
    Filed: January 12, 2011
    Publication date: November 22, 2012
    Inventors: Sven Franciscus Anna Van Brandt, Michel Anna Jozef De Cleyn, Henricus Jacobus Maria Gijsen, Didier Jean-Claude Berthelot, Michel Surkyn
  • Patent number: 8193369
    Abstract: The present invention is related to novel benzimidazole compounds of Formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.
    Type: Grant
    Filed: March 25, 2008
    Date of Patent: June 5, 2012
    Assignee: Janssen Pharmaceutica NV
    Inventors: Henricus Jacobus Maria Gijsen, Michel Anna Jozef De Cleyn, Michel Surkyn
  • Publication number: 20120135981
    Abstract: The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Application
    Filed: July 13, 2010
    Publication date: May 31, 2012
    Inventors: Tongfei Wu, Henricus Jacobus Maria Gijsen, Frederik Jan Rita Rombouts, François Paul Bischoff, Didier Jean-Claude Berthelot, Daniel Oehlrich, Michel Anna Jozef De Cleyn, Serge Maria Aloysius Pieters, Garrett Berlond Minne, Adriana Ingrid Velter', Sven Franciscus Anna Van Brandt, Michel Surkyn
  • Publication number: 20120028987
    Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
    Type: Application
    Filed: September 20, 2011
    Publication date: February 2, 2012
    Applicant: JANSSEN PHARMACEUTICA N.V.
    Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef DeCleyn, Michel Surkyn
  • Publication number: 20120022090
    Abstract: The present invention is concerned with novel substituted benzoxazole, benzimidazole, oxazolopyridine and imidazopyridine derivatives of Formula (I) wherein R1, R2, R3, R4, X, A1, A2, A3, A4, Y1, Y2, Y3 and Z have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Application
    Filed: February 15, 2010
    Publication date: January 26, 2012
    Inventors: Henricu Jacobus Maria Gijsen, Francois Paul Bischoff, Wei Zhuang, Sven Franciscus Anna Van Brandt, Michel Surkyn, Mirko Zaja, Didier Jean-Claude Berthelot, Michel Anna Jozef Cleyn, Gregor James Macdonald, Daniel Oehlrich
  • Patent number: 8063070
    Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
    Type: Grant
    Filed: May 4, 2010
    Date of Patent: November 22, 2011
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn
  • Publication number: 20110281881
    Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Application
    Filed: February 2, 2010
    Publication date: November 17, 2011
    Inventors: Henricus, Jacobus, Maria Gijsen, Adriana Ingrid Velter, Gregor James MacDonald, Francois Paul Bischoff, Tongfei Wu, Sven, Franciscus, Anna Van Brandt, Michel Surkyn, Mirko Zaja, Serge, Maria, Aloysius Pieters, Didier Jean-Claude Berthelot, Michel, Anna, Josef De Cleyn, Daniel Oehlrich
  • Publication number: 20100273831
    Abstract: The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.
    Type: Application
    Filed: December 16, 2008
    Publication date: October 28, 2010
    Inventors: Henricus Jacobus Maria Gijsen, Bie Maria Pieter Verbist, Michel Surkyn