Tomasz Cierpicki from 4496 Lake Forest Dr W, Ann Arbor, MI 48108, age 51

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.

Ash1L Inhibitors And Methods Of Treatment Therewith
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US Patent:

20220288217, Sep 15, 2022
Filed:

Oct 18, 2021
Appl. No.:

17/504159
Inventors:

- Ann Arbor MI, US
Szymon Klossowski - Ann Arbor MI, US
Jing Deng - Ann Arbor MI, US
Tomasz Cierpicki - Ann Arbor MI, US
Hao Li - Ann Arbor MI, US
Hongzhi Miao - Ann Arbor MI, US
Trupta Purohit - Ann Arbor MI, US
EunGi Kim - Ann Arbor MI, US
International Classification:

A61K 47/64
A61K 9/00
A61K 31/454
A61K 38/45
A61P 35/02
A61K 47/54
A61K 31/404
A61K 31/4545
C07D 209/24
C07D 471/04
Abstract:

Provided herein are small molecules that bind to ASH1L and inhibit ASH1L activity, and methods of use thereof for the treatment of disease, including acute leukemia, solid cancers and other diseases dependent on activity of ASH1L.

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.

Ash1L Inhibitors And Methods Of Treatment Therewith
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US Patent:

20200246474, Aug 6, 2020
Filed:

Apr 21, 2020
Appl. No.:

16/854527
Inventors:

- Ann Arbor MI, US
Szymon Klossowski - Ann Arbor MI, US
Jing Deng - Ann Arbor MI, US
Tomasz Cierpicki - Ann Arbor MI, US
Hao Li - Ann Arbor MI, US
Hongzhi Miao - Ann Arbor MI, US
Trupta Purohit - Ann Arbor MI, US
EunGi Kim - Ann Arbor MI, US
International Classification:

A61K 47/64
A61K 38/45
C07D 471/04
C07D 209/24
A61P 35/02
A61K 47/54
A61K 31/4545
A61K 31/454
A61K 31/404
A61K 9/00
Abstract:

Provided herein are small molecules that bind to ASH1L and inhibit ASH1L activity, and methods of use thereof for the treatment of disease, including acute leukemia, solid cancers and other diseases dependent on activity of ASH1L.

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.

Ash1L Inhibitors And Methods Of Treatment Therewith
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US Patent:

20190142799, May 16, 2019
Filed:

May 12, 2017
Appl. No.:

16/300421
Inventors:

- Ann Arbor MI, US
Tomasz Cierpicki - Ann Arbor MI, US
David Rogawski - Ann Arbor MI, US
Dmitry Borkin - Ann Arbor MI, US
Szymon Klossowski - Ann Arbor MI, US
Jin Zhuang - Ann Arbor MI, US
Deanna Montgomery - Ann Arbor MI, US
International Classification:

A61K 31/404
A61P 35/02
Abstract:

Provided herein are small molecule inhibitors of ASH1L activity and small molecules that facilitate ASH1L degradation and methods of use thereof for the treatment of disease, including acute leukemia, solid cancers and other diseases dependent on activity of ASH1L.

Ash1L Degraders And Methods Of Treatment Therewith
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US Patent:

20190142961, May 16, 2019
Filed:

Nov 9, 2018
Appl. No.:

16/186012
Inventors:

- Ann Arbor MI, US
Szymon Klossowski - Ann Arbor MI, US
Jing Deng - Ann Arbor MI, US
Tomasz Cierpicki - Ann Arbor MI, US
Hao Li - Ann Arbor MI, US
Hongzhi Miao - Ann Arbor MI, US
Trupta Purohit - Ann Arbor MI, US
EunGi Kim - Ann Arbor MI, US
Dong Chen - Ann Arbor MI, US
International Classification:

A61K 47/64
A61K 9/00
A61P 35/02
A61K 38/45
A61K 31/454
Abstract:

Provided herein are small molecules comprising a first domain that binds to ASH1L and a second domain that facilitates ASH1L degradation. In particular, ASH1L-targeting proteolysis targeting chimeras (PROTACs) and methods of use thereof for the treatment of disease (e.g., acute leukemia, solid cancers and other diseases dependent on activity of ASH1L) are provided.

Tomasz Cierpicki