公开(公告)号：US20200253969A1

公开(公告)日：2020-08-13

申请号：US16651733

申请日：2018-09-28

Applicant: Relay Therapeutics, Inc. ,  D.E. Shaw Research, LLC

Inventor： Alexander M. Taylor ,  W. Patrick Walters ,  Mark Andrew Murcko ,  Fabrizio Giordanetto ,  Eric Therrien ,  Sathesh Bhat ,  Markus Kristofer Dahlgren

IPC: A61K31/4985 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00

Abstract: Disclosed herein are novel compounds of formula (I) and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds ad compositions of the disclosure.

公开(公告)号：US12152034B2

公开(公告)日：2024-11-26

申请号：US17455507

申请日：2021-11-18

Applicant: Relay Therapeutics, Inc.

Inventor： André Lescarbeau ,  Jethro Beamish-Cook ,  Zoe Prentice ,  Thomas Kendall ,  Aaron Dumas ,  Elisabeth Isaak ,  Piera Trinchera ,  Oleksandr Zhurakovskyi ,  Osama Suleiman

IPC: C07D487/04

Abstract: The disclosure is in part directed to crystalline forms of N-(4-(4-amino-5-(3-fluoro-4-((4-methylpyrimidin-2-yl)oxy)phenyl)-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl)phenyl)methacrylamide represented by the following structure: its salts, its cocrystals, and variants thereof.

公开(公告)号：US20240122925A1

公开(公告)日：2024-04-18

申请号：US18545478

申请日：2023-12-19

Applicant: Relay Therapeutics, Inc.

Inventor： Alexander M. Taylor ,  André Lescarbeau ,  Jing Wang ,  Yanyan Zhang ,  Gaodeng Lian

IPC: A61K31/4985 ,  A61K45/06 ,  C07D401/14 ,  C07D519/00

CPC classification number: A61K31/4985 ,  A61K45/06 ,  C07D401/14 ,  C07D519/00 ,  C07B2200/13 ,  C07D221/20

Abstract: The disclosure is in part directed to crystalline forms of (R)-1′-(3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl)-3H-spiro[benzofuran-2,4′-piperidin]-3-amine, its salt, and variants thereof.

公开(公告)号：US20230234958A1

公开(公告)日：2023-07-27

申请号：US18066551

申请日：2022-12-15

Applicant: Relay Therapeutics, Inc. ,  D. E. Shaw Research, LLC.

Inventor： Alexander M. Taylor ,  Andre Lescarbbeau ,  Elizabeth H. Kelley ,  Kelley C. Shortsleeves ,  W. Patrick Walters ,  Mark Andrew Murcko ,  Thomas H. McLean ,  Hakan Gunaydin ,  Fabrizio Giordanetto ,  Eric Therrien

IPC: C07D487/04 ,  C07D401/04 ,  C07D401/14 ,  C07D519/00 ,  C07D221/20 ,  C07D401/12 ,  C07D417/04 ,  C07D417/14 ,  C07D491/107 ,  C07D513/04

CPC classification number: C07D487/04 ,  C07D401/04 ,  C07D401/14 ,  C07D519/00 ,  C07D221/20 ,  C07D401/12 ,  C07D417/04 ,  C07D417/14 ,  C07D491/107 ,  C07D513/04

Abstract: The present disclosure relates to novel compounds including formula (X) and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure.

公开(公告)号：US20210085677A1

公开(公告)日：2021-03-25

申请号：US17029376

申请日：2020-09-23

Applicant: Relay Therapeutics, Inc.

Inventor： Alexander M. Taylor ,  André Lescarbeau ,  Jing Wang ,  Yanyan Zhang ,  Gaodeng Lian

IPC: A61K31/4985 ,  C07D519/00 ,  A61K45/06

Abstract: The disclosure is in part directed to crystalline forms of (R)-1′-(3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl)-3H-spiro[benzofuran-2,4′-piperidin]-3-amine, its salt, and variants thereof.

公开(公告)号：US20190307745A1

公开(公告)日：2019-10-10

申请号：US16335933

申请日：2017-09-22

Applicant: Relay Therapeutics, Inc. ,  D.E. Shaw Research, LLC

Inventor： Brian K. Albrecht ,  Fabrizio Giordanetto ,  Jack Benjamin Greisman ,  Paul Maragakis ,  Alexander M. Taylor ,  Patrick W. Walters

IPC: A61K31/4985 ,  C07D519/00 ,  C07D487/04 ,  A61K31/55

Abstract: The present invention relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the invention. The present invention further relates to, but is not limited to, methods for suppressing tumor cell growth, ameliorating the pathogenesis of systemic lupus erythematosus, and the treatment of various other disorders, including Noonan syndrome, diabetes, neutropenia, neuroblastoma, melanoma, juvenile leukemia, juvenile myelomonocytic leukemia, chronic myelomonocytic leukemia, acute myeloid leukemia, and other cancers associated with SHP2 deregulation with the compounds and compositions of the invention, alone or in combination with other treatments. Other cancers associated with SHP2 deregulation include HER2-positive breast cancer, triple-negative breast cancer, ductal carcinoma of the breast, invasive ductal carcinoma of the breast, non-small cell lung cancer, esophageal cancer, gastric cancer, squamous-cell carcinoma of the head and neck (SCCHN), and colon cancer.

公开(公告)号：US12219327B2

公开(公告)日：2025-02-04

申请号：US18208023

申请日：2023-06-09

Applicant: Relay Therapeutics, Inc. ,  D.E. Shaw Research, LLC

Inventor： Lucian V. Dipietro ,  Kelley C. Shortsleeves ,  Thomas H. Mclean ,  Alexandre Larivee ,  Fabrizio Giordanetto ,  André Lescarbeau ,  Alessandro Boezio ,  Hanmo Zhang

IPC: A61K31/4035 ,  A61B5/00 ,  C07D209/46 ,  C07D487/04 ,  H04R25/00

Abstract: The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of PI3K-α enzymes with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with PI3K-α signaling with the compounds and compositions of the disclosure.

公开(公告)号：US12084447B2

公开(公告)日：2024-09-10

申请号：US16950576

申请日：2020-11-17

Applicant: Relay Therapeutics, Inc. ,  D. E. Shaw Research, LLC

Inventor： Alexander M. Taylor ,  André Lescarbeau ,  Elizabeth H. Kelley ,  Kelley C. Shortsleeves ,  W. Patrick Walters ,  Mark Andrew Murcko ,  Thomas H. McLean ,  Hakan Gunaydin ,  Fabrizio Giordanetto ,  Eric Therrien

IPC: C07D487/04 ,  C07D221/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D417/04 ,  C07D417/14 ,  C07D491/107 ,  C07D513/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D221/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D417/04 ,  C07D417/14 ,  C07D491/107 ,  C07D513/04 ,  C07D519/00

Abstract: The present disclosure relates to novel compounds including formula (X) and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure.

公开(公告)号：US20240190855A1

公开(公告)日：2024-06-13

申请号：US18276946

申请日：2022-02-11

Applicant: Relay Therapeutics, Inc.

Inventor： Alexander M. Taylor ,  Timothy F. Briggs ,  Nicolas A. Pabon ,  Jing He ,  Andre Lescarbeau ,  Alessandro Boezio ,  Catherine A. Evans ,  Cary Griffin Fridrich ,  Brian P. Kelley ,  Elaine B. Krueger ,  Ravi Kurukulasuriya ,  Thomas H. McLean

IPC: C07D413/12 ,  C07D231/40 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/052 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

CPC classification number: C07D413/12 ,  C07D231/40 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/052 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

Abstract: The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of CDK enzymes with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with CDK signaling with the compounds and compositions of the disclosure.

公开(公告)号：US20230353959A1

公开(公告)日：2023-11-02

申请号：US18208023

申请日：2023-06-09

Applicant: Relay Therapeutics, Inc. ,  D.E. Shaw Research, LLC

Inventor： Lucian V. DIPIETRO ,  Kelley C. SHORTSLEEVES ,  Thomas H. MCLEAN ,  Alexandre LARIVEE ,  Fabrizio GIORDANETTO

IPC: H04R25/00 ,  A61B5/00

CPC classification number: H04R25/554 ,  A61B5/0026 ,  A61B5/746 ,  H04R2225/55

Abstract: The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of PI3K-α enzymes with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with PI3K-α signaling with the compounds and compositions of the disclosure.