公开(公告)号：US12168668B2

公开(公告)日：2024-12-17

申请号：US17976267

申请日：2022-10-28

Applicant: SHY Therapeutics LLC

Inventor： Yaron R. Hadari ,  Luca Carta ,  Michael Schmertzler ,  Theresa M. Williams ,  Charles H. Reynolds

IPC: C07D495/04 ,  A61K31/52 ,  A61P29/00 ,  A61P35/00 ,  C07D221/04 ,  C07D239/94 ,  C07D265/30 ,  C07D271/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/30 ,  C07D487/04 ,  C07D495/14 ,  C07D513/04

Abstract: Provided herein are compounds that inhibit the phosphorylation of MAPK and thus are useful in compositions and methods for treating cancer and inflammatory disease.

公开(公告)号：US20230286997A1

公开(公告)日：2023-09-14

申请号：US17976267

申请日：2022-10-28

Applicant: SHY Therapeutics LLC

Inventor： Yaron R. Hadari ,  Luca Carta ,  Michael Schmertzler ,  Theresa M. Williams ,  Charles H. Reynolds

IPC: C07D495/04 ,  C07D473/30 ,  C07D401/04 ,  C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D221/04 ,  C07D401/12 ,  C07D407/14 ,  C07D409/14 ,  C07D239/94 ,  C07D417/14 ,  C07D487/04 ,  C07D265/30 ,  C07D271/06 ,  C07D495/14

CPC classification number: C07D495/04 ,  C07D473/30 ,  C07D401/04 ,  C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D221/04 ,  C07D401/12 ,  C07D407/14 ,  C07D409/14 ,  C07D239/94 ,  C07D417/14 ,  C07D487/04 ,  C07D265/30 ,  C07D271/06 ,  C07D495/14

Abstract: Provided herein are compounds that inhibit the phosphorylation of MAPK and thus are useful in compositions and methods for treating cancer and inflammatory disease.

公开(公告)号：US20230149369A1

公开(公告)日：2023-05-18

申请号：US17851684

申请日：2022-06-28

Applicant: Shy Therapeutics LLC

Inventor： Yaron R. Hadari ,  Luca Carta ,  Michael Schmertzler ,  Theresa M. Williams ,  Charles H. Reynolds ,  Rebecca Hutcheson

IPC: A61K31/4365 ,  A61P29/00 ,  A61P35/00 ,  A61P25/28 ,  C07D495/04 ,  C07K14/435 ,  A61K31/505 ,  C12N15/10

CPC classification number: A61K31/4365 ,  A61P29/00 ,  A61P35/00 ,  A61P25/28 ,  C07D495/04 ,  C07K14/435 ,  A61K31/505 ,  C12N15/1037 ,  C12N15/1065

Abstract: Provided herein are methods and compositions for treating cancers, inflammatory diseases, rasopathies, and fibrotic disease involving aberrant Ras superfamily signaling through the binding of compounds to the GTP binding domain of Ras superfamily proteins including, in certain cases, K-Ras and mutants thereof, and a novel method for assaying such compositions.

公开(公告)号：US20230078755A1

公开(公告)日：2023-03-16

申请号：US17414565

申请日：2019-12-18

Applicant: SHY Therapeutics, LLC

Inventor： Yaron R. Hadari ,  Michael Schmertzler ,  Theresa M. Williams ,  Luca Carta ,  Rebecca Hutcheson ,  Charles H. Reynolds

IPC: C07D495/04 ,  C07D519/00 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  A61P35/00

Abstract: Provided herein are methods and compositions for treating cancers, inflammatory diseases, rasopathies, and fibrotic disease involving aberrant Ras superfamily signaling through the binding of compounds to the GTP binding domain of Ras superfamily proteins including, in certain cases, K-Ras and mutants thereof, and a method for assaying such compositions.

公开(公告)号：US11213515B1

公开(公告)日：2022-01-04

申请号：US17143077

申请日：2021-01-06

Applicant: Shy Therapeutics LLC

Inventor： Yaron R. Hadari ,  Luca Carta ,  Michael Schmertzler ,  Theresa M. Williams ,  Charles H. Reynolds ,  Rebecca Hutcheson

IPC: A61K31/4365 ,  A61K31/505 ,  C07D495/04 ,  C12N15/10 ,  A61P25/28 ,  A61P35/00 ,  A61P29/00 ,  C07K14/435

Abstract: Provided herein are methods and compositions for treating cancers, inflammatory diseases, rasopathies, and fibrotic disease involving aberrant Ras superfamily signaling through the binding of compounds to the GTP binding domain of Ras superfamily proteins including, in certain cases, K-Ras and mutants thereof, and a novel method for assaying such compositions.

公开(公告)号：US20240309015A1

公开(公告)日：2024-09-19

申请号：US18273646

申请日：2022-01-27

Applicant: SHY Therapeutics, LLC

Inventor： Yaron R. Hadari ,  Michael Schmertzler ,  Theresa M. Williams ,  Luca Carta ,  Rebecca Hutcheson

IPC: C07D495/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61P21/00 ,  G01N33/573

CPC classification number: C07D495/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61P21/00 ,  G01N33/573 ,  G01N2333/914 ,  G01N2470/10 ,  G01N2500/20

Abstract: Provided herein are methods and corresponding compounds for treating fibrotic disease by administering to a subject a compound of Formula I or pharmaceutically acceptable salt thereof, which inhibits phosphorylation of Smad2/3, according to Phospho-Smad2/3 Inhibition Assay, and is inactive according to MAPK p38 Activation Assay; or a compound of Formula II or III. Also provided are methods and corresponding compounds for treating cancers, inflammatory diseases, rasopathies and autoimmune leukoproliferative disorders.

公开(公告)号：US20230227466A1

公开(公告)日：2023-07-20

申请号：US18010697

申请日：2021-06-17

Applicant: SHY Therapeutics, LLC

Inventor： Yaron R. Hadari ,  Michael Schmertzler ,  Theresa M. Williams ,  Luca Carta ,  Rebecca Hutcheson

IPC: C07D495/04 ,  C07D519/00 ,  A61P35/00

CPC classification number: C07D495/04 ,  C07D519/00 ,  A61P35/00

Abstract: Provided herein are methods and compositions for treating cancers, inflammatory diseases, rasopathies, and fibrotic disease involving aberrant Ras superfamily signaling through the binding of compounds to the GTP binding domain of Ras superfamily proteins including, in certain cases, K-Ras and mutants thereof, and a method for assaying such compositions.

公开(公告)号：US20220332725A1

公开(公告)日：2022-10-20

申请号：US17023266

申请日：2020-09-16

Applicant: SHY Therapeutics LLC

Inventor： Yaron R. Hadari ,  Luca Carta ,  Michael Schmertzler ,  Theresa M. Williams ,  Charles H. Reynolds

IPC: C07D495/04 ,  C07D473/30 ,  C07D413/14 ,  C07D239/94 ,  C07D401/14 ,  C07D495/14 ,  C07D401/12 ,  C07D401/04 ,  C07D271/06 ,  C07D487/04 ,  C07D265/30 ,  C07D417/14 ,  C07D221/04 ,  C07D407/14 ,  C07D409/14 ,  C07D471/04

Abstract: Provided herein are compounds that inhibit the phosphorylation of MAPK and thus are useful in compositions and methods for treating cancer and inflammatory disease.

公开(公告)号：US10588894B2

公开(公告)日：2020-03-17

申请号：US16013872

申请日：2018-06-20

Applicant: SHY Therapeutics LLC

Inventor： Yaron R. Hadari ,  Luca Carta ,  Michael Schmertzler ,  Theresa M. Williams ,  Charles H. Reynolds ,  Rebecca Hutcheson

IPC: A61K31/4365 ,  C07D495/04 ,  A61P29/00 ,  A61P35/00 ,  A61P25/28 ,  A61K31/505 ,  C12N15/10

Abstract: Provided herein are methods and compositions for treating cancers, inflammatory diseases, rasopathies, and fibrotic disease involving aberrant Ras superfamily signaling through the binding of compounds to the GTP binding domain of Ras superfamily proteins including, in certain cases, K-Ras and mutants thereof, and a novel method for assaying such compositions.

公开(公告)号：US20240124483A1

公开(公告)日：2024-04-18

申请号：US18273644

申请日：2022-01-27

Applicant: SHY Therapeutics, LLC

Inventor： Yaron R. Hadari ,  Michael Schmertzler ,  Theresa M. Williams ,  Luca Carta ,  Rebecca Hutcheson

IPC: C07D495/04 ,  A61P35/00

CPC classification number: C07D495/04 ,  A61P35/00

Abstract: Provided herein are methods and corresponding compounds for treating fibrotic disease by administering to a subject a compound of Formula I or pharmaceutically acceptable salt thereof, which inhibits phosphorylation of Smad2/3, according to Phospho-Smad2/3 Inhibition Assay, including compounds that are active according to MAPK p38 Activation Assay; or a compound of Formula II or III. Also provided are methods and corresponding compounds for treating cancers, inflammatory diseases, rasopathies and autoimmune leukoproliferative disorders.