Patents by Inventor Herman Steven Overkleeft

Herman Steven Overkleeft 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: 10590082
    Abstract: Deoxynojirimycin and deoxygalactonojirimycin derivatives according to the present invention are N-alkylated D-galacto, D-gluco- or L-ido-deoxynojirimycin with a linear methyloxypentyl group bearing various sidegroups and a non-fused bicyclic aromatic group (“X”) on the methyloxy-carbon. Formula (I), Formula (Ia). These compounds display an increased inhibitory potency towards GCS, and/or an increased inhibitory potency towards GBA2, and/or a decreased inhibitory potency towards GBA1, relative to known deoxynojirimycin derivatives of the same (D-gluco, L-ido or D-galacto) configuration.
    Type: Grant
    Filed: January 7, 2019
    Date of Patent: March 17, 2020
    Assignees: Academisch Medisch Centrum, Universiteit Leiden
    Inventors: Herman Steven Overkleeft, Stan Van Boeckel, Johannes Maria Franciscus Gerardus Aerts, Amar Ghisaidoobe, Richard Van Den Berg
  • Publication number: 20190144388
    Abstract: Deoxynojirimycin and deoxygalactonojirimycin derivatives according to the present invention are N-alkylated D-galacto, D-gluco- or L-ido-deoxynojirimycin with a linear methyloxypentyl group bearing various sidegroups and a non-fused bicyclic aromatic group (“X”) on the methyloxy-carbon. Formula (I), Formula (Ia). These compounds display an increased inhibitory potency towards GCS, and/or an increased inhibitory potency towards GBA2, and/or a decreased inhibitory potency towards GBA1, relative to known deoxynojirimycin derivatives of the same (D-gluco, L-ido or D-galacto) configuration.
    Type: Application
    Filed: January 7, 2019
    Publication date: May 16, 2019
    Inventors: Herman Steven OVERKLEEFT, Stan VAN BOECKEL, Johannes Maria Franciscus Gerardus AERTS, Amar GHISAIDOOBE, Richard VAN DEN BERG
  • Patent number: 10189784
    Abstract: Deoxynojirimycin and deoxygalactonojirimycin derivatives according to the present invention are N-alkylated D-galacto, D-gluco- or L-ido-deoxynojirimycin with a linear methyloxypentyl group bearing various sidegroups and a non-fused bicyclic aromatic group (“X”) on the methyloxy-carbon. These compounds display an increased inhibitory potency towards GCS, and/or an increased inhibitory potency towards GBA2, and/or a decreased inhibitory potency towards GBA1, relative to known deoxynojirimycin derivatives of the same (D-gluco, L-ido or D-galacto) configuration.
    Type: Grant
    Filed: March 23, 2015
    Date of Patent: January 29, 2019
    Assignees: ACADEMISCH MEDISCH CENTRUM, UNIVERSITEIT LEIDEN
    Inventors: Herman Steven Overkleeft, Stan Van Boeckel, Johannes Maria Franciscus Gerardus Aerts, Amar Ghisaidoobe, Richard Van Den Berg
  • Publication number: 20170226058
    Abstract: Deoxynojirimycin and deoxygalactonojirimycin derivatives according to the present invention are N-alkylated D-galacto, D-gluco- or L-ido-deoxynojirimycin with a linear methyloxypentyl group bearing various sidegroups and a non-fused bicyclic aromatic group (“X”) on the methyloxy-carbon. These compounds display an increased inhibitory potency towards GCS, and/or an increased inhibitory potency towards GBA2, and/or a decreased inhibitory potency towards GBA1, relative to known deoxynojirimycin derivatives of the same (D-gluco, L-ido or D-galacto) configuration.
    Type: Application
    Filed: March 23, 2015
    Publication date: August 10, 2017
    Inventors: Herman Steven OVERKLEEFT, Stan VAN BOECKEL, Johannes Maria Franciscus Gerardus AERTS, Amar GHISAIDOOBE, Richard VAN DEN BERG
  • Patent number: 9056847
    Abstract: An activity based probe (ABP) comprising a glycosidase inhibitor, and a detection-group. The ABPs of the inventions are used for diagnosing storage disorder for screening of compounds suitable for preventing and/or treating a storage disorder, for monitoring of therapeutic enzymes for lysosomal storage disorders, and for ultra-sensitive visualization of glycosidase-fusion proteins in molecular imaging.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: June 16, 2015
    Assignee: ACADEMISCH MEDISCH CENTRUM BIJ UNIVERSITEIT VAN AMSTERDAM
    Inventors: Johannes Maria Franciscus Gerardus Aerts, Herman Steven Overkleeft
  • Publication number: 20130143228
    Abstract: An activity based probe (ABP) comprising a glycosidase inhibitor, and a detection-group. The ABPs of the inventions are used for diagnosing storage disorder for screening of compounds suitable for preventing and/or treating a storage disorder, for monitoring of therapeutic enzymes for lysosomal storage disorders, and for ultra-sensitive visualization of glycosidase-fusion proteins in molecular imaging.
    Type: Application
    Filed: March 10, 2011
    Publication date: June 6, 2013
    Inventors: Johannes Maria Franciscus Gerardus Aerts, Herman Steven Overkleeft
  • Publication number: 20090312521
    Abstract: The invention concerns derivatives of drosocin which have an increased half-life in mammalian serum by substituting one or more of the amino acid residues of wild type drosocin with another amino acid or a peptidomimetic moiety capable of replacing said amino acid. These derivatives can be used for antibiotic therapy or in a bacteriocidal composition.
    Type: Application
    Filed: November 10, 2005
    Publication date: December 17, 2009
    Inventors: Petrus Albertus Venantia Van Hooft, Daniel Noort, Peter Christian De Visser, Herman Steven Overkleeft, Jacobus Hubertus Van Boom, Elisabeth M.H.C. van Boon-Husken, Floris Jacob Bikker
  • Patent number: 6376468
    Abstract: The invention pertains to novel peptide analogs suitable for inhibiting protein:prenyl transferases. As such they are therapeutically useful in e.g. inhibiting oncogenesis and other unwanted cell proliferation, and in supressing aberrant high signal transduction. The analogs comply with the following formula: in which: R1 is hydrogen or a thiol-protecting group; R2 and R3 are independently hydrogen or C1-C4 alkyl; R4 is hydrogen, C1-C4 alkyl, C1-C4 acyl or peptidyl; R5 is hydrogen or C1-C4 alkyl; R6 is hydrogen or optionally substituted C1-C6 alkyl; A is a direct bond or an optionally substituted C1-C4 alkylene chain; Y represents an oxo group or two hydrogen atoms; Z is oxygen, sulphur, imino or C1-C5 alkyl-, aryl- or acylimino; M is 0, 1 or 2; N is 0 or 1.
    Type: Grant
    Filed: February 3, 2000
    Date of Patent: April 23, 2002
    Assignees: Nederlandse Organisatie Voor Toegepast-Natuurwetenschappelijk Onderzoek TNO, Rijksuniversiteit Leiden
    Inventors: Herman Steven Overkleeft, Steven Hendrik Leonard Verhelst, Nicolaas Johannes Meeuwenoord, Elsbet Jantine Pieterman, Louis Hartog Cohen, Mark Overhand, Gijsbert Arie Van der Marel, Jacobus Hubertus Van Boom
  • Patent number: 6177447
    Abstract: Deoxynojirimycin derivatives containing a large hydrophobic moiety, such as cholesterol or adamantame-methanol, linked through a spacer, such as pentamethylene, to the nitrogen atom of deoxynojirimycin, and salts thereof, inhibit glucosylceramidase and may be useful in the treatment of diseases involving a ceramide-mediated signaling process, such as Gaucher disease.
    Type: Grant
    Filed: April 30, 1999
    Date of Patent: January 23, 2001
    Assignee: Universiteit van Amsterdam
    Inventors: Johannes Maria F. G. Aerts, Upendra Kumar Pandit, Gerrit-Jan Koomen, Herman Steven Overkleeft, Paola Vianello