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Jolanta Ewa Grembecka

age ~54

from Ann Arbor, MI

Also known as:
  • Jolanta A
Phone and address:
5518 Gallery Park Dr, Ann Arbor, MI 48103

Jolanta Grembecka Phones & Addresses

  • 5518 Gallery Park Dr, Ann Arbor, MI 48103
  • Charlottesville, VA

Us Patents

  • Inhibitors Of Inv(16) Leukemia

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  • US Patent:
    20120059003, Mar 8, 2012
  • Filed:
    May 13, 2010
  • Appl. No.:
    13/320123
  • Inventors:
    John H. Bushweller - Charlottesville VA, US
    Jolanta Grembecka - Ann Arbor MI, US
    Anuradha Illendula - Charlottesville VA, US
    Lauren Dixon - Ann Arbor MI, US
  • Assignee:
    UNIVERSITY OF VIRGINIA PATENT FOUNDATION - Charlottesville VA
  • International Classification:
    A61K 31/5377
    A61K 31/4439
    A61P 35/02
    C07D 211/14
    A61K 31/4545
    C07D 401/04
    C07D 413/14
  • US Classification:
    5142345, 5462734, 514338, 544124, 546194, 514318
  • Abstract:
    This invention describes the development of targeted small molecule inhibitors of the inv(16) fusion, the causative agent in 12% of acute myeloid leukemia (AML). The inv(16) fusion results in expression of the CBFβ-SMMHC fusion protein in the blood cells of afflicted patients. The present invention provides compounds which inhibit the function of both CBFβ and the CBFβ-SMMHC fusion. These compounds block the growth of an inv(16) leukemia cell line as well as increase its apoptosis, while showing minimal effects against non inv(16) cell lines. As a mechanism to develop inhibitors with selectivity for the CBFβ-SMMHC fusion protein, the present invention further provides dimeric derivatives of these compounds which show both increased potency as well selectivity for CBFβ-SMMHC. These compounds show potent inhibition of an inv(16) leukemia cell line with minimal effects on non inv(16) cell lines. Analysis of the pharmacokinetics of the developed compounds has made it possible to improve the lifetime of the compound in the plasma of mice to a level commensurate with long-term treatment.
  • Compositions And Methods For Treatment Of Leukemia

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  • US Patent:
    20110065690, Mar 17, 2011
  • Filed:
    Sep 3, 2010
  • Appl. No.:
    12/875968
  • Inventors:
    Jolanta Grembecka - Charlottesville VA, US
    Tomasz Cierpicki - Charlottesville VA, US
    Jay Hess - Ann Arbor MI, US
  • Assignee:
    THE REGENTS OF THE UNIVERSITY OF MICHIGAN - Ann Arbor MI
    UNIVERSITY OF VIRGINIA PATENT FOUNDATION - Charlottesville VA
  • International Classification:
    A61K 31/519
    C07D 495/04
    C07D 491/048
    A61K 31/5377
    A61K 31/551
    C07D 401/04
    C07D 405/10
    C07D 243/38
    A61P 35/04
    C12N 5/02
  • US Classification:
    514218, 544250, 51425216, 544278, 544117, 5142342, 540575, 51425211, 540557, 435375
  • Abstract:
    The invention relates generally to effective treatment leukemia. In particular, the present invention provides compositions and methods to inhibit the interaction of menin with MLL and MLL-fusion oncoproteins, and well as systems and methods to screen for such compositions.
  • Nsd Family Inhibitors And Methods Of Treatment Therewith

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  • US Patent:
    20230046569, Feb 16, 2023
  • Filed:
    Apr 26, 2022
  • Appl. No.:
    17/729836
  • Inventors:
    - Ann Arbor MI, US
    Jolanta Grembecka - Ann Arbor MI, US
    Huang Huang - Ann Arbor MI, US
    Sergei Zari - Ann Arbor MI, US
    Hyo Je Cho - Ann Arbor MI, US
    Mykhaylo Potopnyk - Ann Arbor MI, US
    Sergii Dudkin - Ann Arbor MI, US
    Wenbing Chen - Ann Arbor MI, US
    Yassir Adam - Ann Arbor MI, US
    Christina Howard - Ann Arbor MI, US
    EunGi Kim - Ann Arbor MI, US
  • International Classification:
    A61K 31/428
    A61P 35/00
  • Abstract:
    Provided herein are small molecule inhibitors of NSD1, NSD2 and/or NSD3 activity, and methods of use thereof for the treatment of disease, including leukemia, breast cancer, osteosarcoma, lung and prostate cancers and other solid tumors as well as other diseases dependent on the activity of NSD1, NSD2 and/or NSD3.
  • Bridged Bicyclic Inhibitors Of Menin-Mll And Methods Of Use

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  • US Patent:
    20210107917, Apr 15, 2021
  • Filed:
    Jul 13, 2020
  • Appl. No.:
    16/927844
  • Inventors:
    - San Diego CA, US
    - Ann Arbor MI, US
    Yi WANG - San Diego CA, US
    Pingda REN - San Diego CA, US
    Jolanta GREMBECKA - Ann Arbor MI, US
    Tomasz CIERPICKI - Ann Arbor MI, US
    Szymon KLOSSOWSKI - Ann Arbor MI, US
    Jonathan POLLOCK - Ann Arbor MI, US
    Dmitry BORKIN - Ann Arbor MI, US
  • International Classification:
    C07D 495/04
    A61K 31/445
    A61P 35/02
  • Abstract:
    The present disclosure provides methods of inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The methods are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin. Compositions for use in these methods are also provided.
  • Substituted Inhibitors Of Menin-Mll And Methods Of Use

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  • US Patent:
    20210101908, Apr 8, 2021
  • Filed:
    Jul 30, 2020
  • Appl. No.:
    16/944040
  • Inventors:
    - San Diego CA, US
    - Ann Arbor MI, US
    Yi WANG - San Diego CA, US
    Pingda REN - San Diego CA, US
    Jolanta GREMBECKA - Ann Arbor MI, US
    Tomasz CIERPICKI - Ann Arbor MI, US
    Szymon KLOSSOWSKI - Ann Arbor MI, US
    Jonathan POLLOCK - Ann Arbor MI, US
    Dmitry BORKIN - Ann Arbor MI, US
  • International Classification:
    C07D 495/04
    A61P 35/00
  • Abstract:
    The present disclosure provides methods of inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The methods are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin. Compositions for use in these methods are also provided.
  • Methods And Compositions For Inhibiting The Interaction Of Menin With Mll Proteins

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  • US Patent:
    20200165224, May 28, 2020
  • Filed:
    Jun 7, 2018
  • Appl. No.:
    16/619423
  • Inventors:
    - San Diego CA, US
    - Ann Arbor MI, US
    Jun FENG - San Diego CA, US
    Pingda REN - San Diego CA, US
    Yi LIU - San Diego CA, US
    Jolanta GREMBECKA - Ann Arbor MI, US
    Tomasz CIERPICKI - Ann Arbor MI, US
    Dmitry BORKIN - Feasterville PA, US
    Jonathan POLLOCK - Ann Arbor MI, US
  • International Classification:
    C07D 401/14
    C07K 14/47
    C07D 207/32
    C07D 417/14
    C07D 413/14
    A61P 35/00
  • Abstract:
    The present disclosure provides compositions and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The compositions and methods of use are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin.
  • Prc1 Inhibitors And Methods Of Treatment Therewith

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  • US Patent:
    20200039963, Feb 6, 2020
  • Filed:
    Jun 7, 2019
  • Appl. No.:
    16/434508
  • Inventors:
    - Avin Arbor MI, US
    Jolanta Grembecka - Ann Arbor MI, US
    Weijiang Ying - Ann Arbor MI, US
    Yiwu Yao - Ann Arbor MI, US
    Felicia Gray - Ann Arbor MI, US
    Qingjie Zhao - Ann Arbor MI, US
  • International Classification:
    C07D 403/14
    C07D 403/04
    C07D 405/14
    C07D 417/14
    C07D 493/10
    C07D 471/04
    C07D 513/16
    C07D 498/06
    C07D 413/14
    C07D 471/16
    C07D 498/16
  • Abstract:
    Provided herein are small molecule inhibitors of Polycomb Repressive Complex 1 (PRC1) activity, and methods of use thereof for the treatment of disease, including leukemia and other cancers, as well as other diseases dependent on the activity of PRC1.
  • Nsd Family Inhibitors And Methods Of Treatment Therewith

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  • US Patent:
    20190183865, Jun 20, 2019
  • Filed:
    Dec 7, 2018
  • Appl. No.:
    16/213564
  • Inventors:
    - Ann Arbor MI, US
    Jolanta Grembecka - Ann Arbor MI, US
    Huang Huang - Ann Arbor MI, US
    Sergi Zari - Ann Arbor MI, US
    Hyo Je Cho - Ann Arbor MI, US
    Mykhaylo Potopnyk - Ann Arbor MI, US
    Sergeii Dudkin - Ann Arbor MI, US
    Wenbing Chen - Ann Arbor MI, US
    Yassir Adam - Ann Arbor MI, US
    Christina Howard - Ann Arbor MI, US
    EunGi Kim - Ann Arbor MI, US
  • International Classification:
    A61K 31/428
    A61P 35/00
  • Abstract:
    Provided herein are small molecule inhibitors of NSD1, NSD2 and/or NSD3 activity, and methods of use thereof for the treatment of disease, including leukemia, breast cancer, osteosarcoma, lung and prostate cancers and other solid tumors as well as other diseases dependent on the activity of NSD1, NSD2 and/or NSD3.

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