Patents by Inventor Marcelis van der Stelt

Marcelis van der Stelt 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: 20230121721
    Abstract: Provided are compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof: Also provided are compositions comprising compounds of formula (I). The compounds and compositions are also provided for use as medicaments, for example as medicaments useful in the treatment of a condition modulated by monoacylglycerol lipase (MAGL). Also provided are the use of compounds and compositions for the inhibition of monoacylglycerol lipase (MAGL).
    Type: Application
    Filed: March 3, 2021
    Publication date: April 20, 2023
    Inventors: Marcelis VAN DER STELT, Ming JIANG, Florian David MOHR, Constant Adriaan Anton VAN BOECKEL, Mirjam Cornelia Wellemina HUIZENGA, Avand AMEDI
  • Patent number: 10583137
    Abstract: Provided herein are triazole compounds and pharmaceutical compositions comprising said compounds useful as modulators of DAGL(?) and DAGL(?). In some embodiments, the compounds described herein are selective DAGL(?) inhibitors. Furthermore, the subject compounds and compositions are useful for the treatment of neurodegenerative or neuroinflammatory disease.
    Type: Grant
    Filed: December 2, 2016
    Date of Patent: March 10, 2020
    Assignees: THE SCRIPPS RESEARCH INSTITUTE, LEIDEN UNIVERSITY
    Inventors: Benjamin F. Cravatt, Daisuke Ogasawara, Andreu Viader, Hui Deng, Tom Van Der Wel, Marcelis Van Der Stelt
  • Publication number: 20180344729
    Abstract: Provided herein are triazole compounds and pharmaceutical compositions comprising said compounds useful as modulators of DAGL(?) and DAGL(?). In some embodiments, the compounds described herein are selective DAGL(?) inhibitors. Furthermore, the subject compounds and compositions are useful for the treatment of neurodegenerative or neuroinflammatory disease.
    Type: Application
    Filed: December 2, 2016
    Publication date: December 6, 2018
    Inventors: Benjamin F. CRAVATT, Daisuke OGASAWARA, Andreu VIADER, Hui DENG, Tom VAN DER WEL, Marcelis VAN DER STELT
  • Patent number: 8993757
    Abstract: The invention relates to a N-piperidin-4-yl derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same and to the use of said N-piperidin-4-yl derivatives for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, or for the treatment of uterine fibroids or other menstrual-related disorders.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: March 31, 2015
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Ines Huisman, Marcelis Van Der Stelt, Wouter Wiedenhof, Charles Anthony Graham Baker-Glenn, Wesley Peter Blackaby, Naimisha Trivedi
  • Publication number: 20140329822
    Abstract: The invention relates to a N-piperidin-4-yl derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same and to the use of said N-piperidin-4-yl derivatives for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, or for the treatment of uterine fibroids or other menstrual-related disorders.
    Type: Application
    Filed: September 14, 2012
    Publication date: November 6, 2014
    Inventors: Ines Huisman, Marcelis Van Der Stelt, Wouter Wiedenhof, Charles Anthony Graham Baker-Glenn, Wesley Peter Blackaby, Naimisha Trivedi
  • Patent number: 8143246
    Abstract: The invention relates to 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, (C1-3)alkyloxy, (C1-3)alkyloxycarbonyl, halogen or CN), (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl, each cycloalkyl ring optionally comprising a heteroatom selected from O and S; R2 and R3 are independently H or (C1-3)alkyl; or R2 and R3 form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R4 is H or 1 to 3 F substituents; R5 is H or 1 to 4 F substituents; R6 and R7 are independently H or F; X represents R8, OR8, NR8R9, R8 is (C5-7)cycloalkyl optionally comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; R10 represents 1-3 substituents independently selected from H, (C1-3)alkyl, halogen, oxo, CN and CF3; Y is CF2, O, S, SO or SO2; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said 1-(4
    Type: Grant
    Filed: February 15, 2010
    Date of Patent: March 27, 2012
    Assignee: MSD OSS B.V.
    Inventors: Marcelis van der Stelt, Joseph Maria Gerardus Barbara Cals, Johannes Petrus Gerardus Klomp
  • Patent number: 7960560
    Abstract: The invention relates to A 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, OR4, COOR5, halogen or CN), (C2-6)alkenyl, (C2-6)alkynyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl; R2 and R2? are independently H or (C1-3)alkyl; or R2 and R2? form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R3 represents H or 1 to 4 F substituents; Y represents or NR8R9; X represents CHR6, CF2, O, S, SO or SO2; R4 and R5 are (C1-6)alkyl; R6 is H, OR7 or CN; R7 is (C1-3)alkyl; R8 is (C5-7)cycloalkyl comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; o and m represent the ortho or meta position of the substituent Y—CH2; or a pharmaceutically acceptable salt thereof; as well as to the use of said 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivatives in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cance
    Type: Grant
    Filed: December 1, 2009
    Date of Patent: June 14, 2011
    Assignee: N.V. Organon
    Inventors: Marcelis van der Stelt, Joseph Maria Gerardus Barbara Cals
  • Publication number: 20100144723
    Abstract: The invention relates to A 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, OR4, COOR5, halogen or CN), (C2-6)alkenyl, (C2-6)alkynyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl; R2 and R2? are independently H or (C1-3)alkyl; or R2 and R2? form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R3 represents H or 1 to 4 F substituents; Y represents or NR8R9; X represents CHR6, CF2, O, S, SO or SO2; R4 and R5 are (C1-6)alkyl; R6 is H, OR7 or CN; R7 is (C1-3)alkyl; R8 is (C5-7)cycloalkyl comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; o and m represent the ortho or meta position of the substituent Y—CH2; or a pharmaceutically acceptable salt thereof; as well as to the use of said 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivatives in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer
    Type: Application
    Filed: December 1, 2009
    Publication date: June 10, 2010
    Inventors: Marcelis van der Stelt, Joseph Maria Gerardus Barbara Cals
  • Publication number: 20100144724
    Abstract: The invention relates to 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, (C1-3)alkyloxy, (C1-3)alkyloxycarbonyl, halogen or CN), (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl, each cycloalkyl ring optionally comprising a heteroatom selected from O and S; R2 and R3 are independently H or (C1-3)alkyl; or R2 and R3 form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R4 is H or 1 to 3 F substituents; R5 is H or 1 to 4 F substituents; R6 and R7 are independently H or F; X represents R8, OR8, NR8R9, R8 is (C5-7)cycloalkyl optionally comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; R10 represents 1-3 substituents independently selected from H, (C1-3)alkyl, halogen, oxo, CN and CF3; Y is CF2, O, S, SO or SO2; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said 1-(4-
    Type: Application
    Filed: February 15, 2010
    Publication date: June 10, 2010
    Inventors: Marcelis van der Stelt, Joseph Maria Gerardus Barbara Cals, Johannes Petrus Gerardus Klomp