Patents by Inventor Henricus Jacobus Maria Gijsen

Henricus Jacobus Maria Gijsen 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).

  • Publication number: 20170362198
    Abstract: The present invention relates to 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2H-pyrrol-5-amine compound inhibitors of beta-secretase having the structure shown in Formula (I) wherein the radicals are as defined in the specification. 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 associated with beta-amyloid, age-related macular degeneration, type 2 diabetes or metabolic disorders.
    Type: Application
    Filed: December 16, 2015
    Publication date: December 21, 2017
    Applicant: Janssen Pharmaceutica NV
    Inventors: Andrés Avelino Trabanco-Suárez, Óscar Delgado-González, Henricus Jacobus Maria Gijsen, Michiel Luc Maria Van Gool, Sven Franciscus Anna Van Brandt, Michel Anna Jozef De Cleyn, Santos Fustero Lardiés, Natalia Mateu Sanchís
  • Patent number: 9840507
    Abstract: The present invention relates to novel 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine inhibitors of beta-secretase, having the structure shown in Formula (I) wherein R1, R2, R3, R4, X1, X2, X3, X4, L and Ar are defined in the specification. 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, cerebrovascular amyloid angiopathy, multi-infarct dementia, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: December 12, 2017
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Andrés Avelino Trabanco-Suárez, Francisca Delgado-Jiménez, Juan Antonio Vega Ramiro, Gary John Tresadern, Henricus Jacobus Maria Gijsen, Daniel Oehlrich
  • Patent number: 9834559
    Abstract: The present invention relates to novel 5,6-dihydroimidazo[1,5-a]pyrazin-3(2H)-one 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: December 5, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Daniel Oehlrich, Henricus Jacobus Maria Gijsen
  • Patent number: 9828350
    Abstract: The present invention relates to novel 5,6-dihydro-2H-[1,4]oxazin-3-ylamine 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, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta-amyloid.
    Type: Grant
    Filed: February 5, 2016
    Date of Patent: November 28, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Andrés Avelino Trabanco-Suárez, Frederik Jan Rita Rombouts, Gary John Tresadern, Michiel Luc Maria Van Gool, Gregor James Macdonald, Carolina Martinez Lamenca, Henricus Jacobus Maria Gijsen
  • Patent number: 9751886
    Abstract: The present invention relates to novel 6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazin-6-yl 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: September 5, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Daniel Oehlrich, Henricus Jacobus Maria Gijsen
  • 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: 20160310468
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, and G are defined herein.
    Type: Application
    Filed: July 6, 2016
    Publication date: October 27, 2016
    Inventors: Ishtiyaque Ahmad, Rajagopal Bakthavatchalam, Sivaramakrishna Battula, Henricus Jacobus Maria Gijsen, Saravanan Vadivelu, Mark Wall
  • Patent number: 9453002
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, and G are defined herein.
    Type: Grant
    Filed: August 16, 2013
    Date of Patent: September 27, 2016
    Assignee: Janssen Pharmaceutica NV
    Inventors: Ishtiyaque Ahmad, Rajagopal Bakthavatchalam, Sivaramakrishna Battula, Henricus Jacobus Maria Gijsen, Saravanan Vadivelu, Mark Wall
  • Publication number: 20160152581
    Abstract: The present invention relates to novel 5,6-dihydro-2H-[1,4]oxazin-3-ylamine 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, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta-amyloid.
    Type: Application
    Filed: February 5, 2016
    Publication date: June 2, 2016
    Inventors: Andrés Avelino Trabanco-Suárez, Frederik Jan Rita Rombouts, Gary John Tresadern, Michiel Luc Maria Van Gool, Gregor James MacDonald, Carolina Martinez Lamenca, Henricus Jacobus Maria Gijsen
  • Patent number: 9346811
    Abstract: The present invention relates to novel 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-yl-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, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid.
    Type: Grant
    Filed: February 29, 2012
    Date of Patent: May 24, 2016
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Andrés Avelino Trabanco-Suárez, Henricus Jacobus Maria Gijsen, Michiel Luc Maria Van Gool, Juan Antonio Vega Ramiro, Francisca Delgado-Jiménez
  • Publication number: 20160130274
    Abstract: The present invention relates to novel 6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazin-6-yl 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: May 12, 2016
    Inventors: Daniel Oehlrich, Henricus Jacobus, Maria Gijsen
  • Publication number: 20160115171
    Abstract: The present invention relates to novel 5,6-dihydroimidazo[1,5-a]pyrazin-3(2H)-one 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
  • 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
  • Publication number: 20150353544
    Abstract: The present invention is concerned with novel substituted pyrido-piperazinone derivatives of Formula (I) wherein R1, R2, R3, R4, R5, L, Z and X 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 16, 2014
    Publication date: December 10, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: François Paul Bischoff, Adriana Ingrid Velter, Frederik Jan, Rita Rombouts, Michel Anna, Jozef De Cleyn, Sven Franciscus, Anna Van Brandt, Henricus Jacobus, Maria Gijsen, Chiara Zavattaro, Frans Alfons, Maria Van den Keybus
  • Patent number: 9181245
    Abstract: The present invention is concerned with novel substituted 3,4-dihydro-2H-pyrido[1,2- a]pyrazine-1,6-dione derivatives of Formula (I) wherein R1, R2, R3, R4, R5, Z and X 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: May 16, 2013
    Date of Patent: November 10, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Frederik Jan Rita Rombouts, Andrés Avelino Trabanco-Suarez, Henricus Jacobus Maria Gijsen, Gregor James MacDonald, François Paul Bischoff, Sergio-Alvar Alonso-de-Diego, Adriana Ingrid Velter, Yves Emiel Maria Van Roosbroeck
  • Publication number: 20150307496
    Abstract: The present invention is concerned with novel tricyclic 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione derivatives of Formula (I) wherein R1, R2, R3, R4, L, Y, Z and X 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 19, 2013
    Publication date: October 29, 2015
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: François Paul Bischoff, Henricus Jacobus Maria Gijsen, Frans Alfons Maria Van den Keybus, Frederik Jan Rita Rombouts
  • Patent number: 9145399
    Abstract: The present invention is concerned with novel substituted bicyclic 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: September 29, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Michel Anna Jozef De Cleyn, Sven Franciscus Anna Van Brandt, Henricus Jacobus Maria Gijsen, Didier Jean-Claude Berthelot, Daniel Oehlrich
  • Patent number: 9115143
    Abstract: The present invention is concerned with novel substituted indole derivatives of Formula (I) wherein R1, R2, R3, A1, A2, A3, Y and X 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 12, 2012
    Date of Patent: August 25, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Garrett Berlond Minne, François Paul Bischoff, Henricus Jacobus Maria Gijsen, Adriana Ingrid Velter, Serge Maria Aloysius Pieters, Didier Jean-Claude Berthelot
  • 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