公开(公告)号：US20240287058A1

公开(公告)日：2024-08-29

申请号：US17921580

申请日：2021-04-29

申请人： Relay Therapeutics, Inc. ,  D. E. Shaw Research, LLC

发明人： Alessandro BOEZIO ,  Lucian V. DIPIETRO ,  Cary Griffin FRIDRICH ,  Hakan GUNAYDIN ,  Ravi KURUKULASURIYA ,  André LESCARBEAU ,  Mary M. MADER ,  Thomas H. MCLEAN ,  Levi CharlesThomas PIERCE ,  Kevin David RAYNOR ,  Kelley C. SHORTSLEEVES ,  Yong TANG ,  Alexander M. TAYLOR ,  W. Patrick WALTERS ,  Hanmo ZHANG ,  Fabrizio GIORDANETTO ,  Yakov PECHERSKY ,  Qi WANG ,  Bren-Jordan ATIENZA ,  Megan BERTRAND-LAPERLE ,  Andrew J. BURNIE ,  Fei CHEN ,  Sampada CHITALE ,  Shorena GELOZIA ,  Jean-Benoit GIGUERE ,  Elodie LANDAGARAY ,  Alexandre LARIVEE ,  Thomas LEPITRE ,  Gaetan MAERTENS ,  Johanne OUTIN ,  Mohan PAL ,  Claudio STURINO ,  Kashif TANVEER ,  Rakesh THORAT ,  Naresh VEMULA ,  Elaine B. KRUEGER ,  Yue PAN ,  Michael Paul DENINNO ,  Yves BOUSQUET ,  Antoine JOBIN-DES LAURIERS ,  Jessica LEE ,  Tarek MOHAMED

IPC分类号： C07D471/04 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4545 ,  A61K31/472 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/536 ,  A61K31/69 ,  C07D209/46 ,  C07D209/48 ,  C07D217/24 ,  C07D231/56 ,  C07D239/82 ,  C07D265/18 ,  C07D275/06 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D405/06 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D487/04 ,  C07D519/00 ,  C07F5/02

CPC分类号： C07D471/04 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4545 ,  A61K31/472 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/536 ,  A61K31/69 ,  C07D209/46 ,  C07D209/48 ,  C07D217/24 ,  C07D231/56 ,  C07D239/82 ,  C07D265/18 ,  C07D275/06 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D405/06 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D487/04 ,  C07D519/00 ,  C07F5/025

摘要： 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：US20230023559A1

公开(公告)日：2023-01-26

申请号：US17766885

申请日：2020-10-06

申请人： D. E. Shaw Research, LLC

发明人： Fabrizio GIORDANETTO ,  Morten Østergaard JENSEN ,  Vishwanath JOGINI ,  Roger John SNOW

IPC分类号： C07D211/12 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D413/06 ,  C07D401/04 ,  C07D413/04 ,  C07D409/06 ,  C07D401/14 ,  C07D205/04 ,  C07D207/06 ,  C07D223/04 ,  C07D453/02 ,  C07D417/04

摘要： A compound of Formula (I) or a pharmaceutically acceptable salt thereof is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.

公开(公告)号：US11529347B2

公开(公告)日：2022-12-20

申请号：US16335933

申请日：2017-09-22

申请人： Relay Therapeutics, Inc. ,  D. E. Shaw Research, LLC

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

IPC分类号： A61K31/4985 ,  A61K31/55 ,  C07D487/04 ,  C07D519/00 ,  C07D498/10

摘要： The present invention relates to novel compounds having the general formula: 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：US20220340576A1

公开(公告)日：2022-10-27

申请号：US16950576

申请日：2020-11-17

申请人： Relay Therapeutics, Inc. ,  D. E. Shaw Research, LLC

发明人： 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分类号： C07D487/04 ,  C07D401/04 ,  C07D401/14 ,  C07D519/00

摘要： 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：US12084447B2

公开(公告)日：2024-09-10

申请号：US16950576

申请日：2020-11-17

申请人： Relay Therapeutics, Inc. ,  D. E. Shaw Research, LLC

发明人： 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分类号： C07D487/04 ,  C07D221/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D417/04 ,  C07D417/14 ,  C07D491/107 ,  C07D513/04 ,  C07D519/00

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

摘要： 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：US20240169124A1

公开(公告)日：2024-05-23

申请号：US18282818

申请日：2022-03-18

申请人： D. E. Shaw Research, LLC

发明人： Brannon Batson ,  Brian Lee Greskamp ,  Bruce Edwards ,  Jeffrey Adam Butts ,  Christopher Howard Fenton ,  Jeffrey Paul Grossman ,  Douglas John Ierardi ,  Adam Lerer ,  Brian Patrick Towles ,  Michael Edmund Bergdorf ,  Cristian Predescu ,  John K. Salmon ,  Andrew Garvin Taube

IPC分类号： G06F30/25

CPC分类号： G06F30/25

摘要： Improvements in a molecular-dynamic simulator provide ways to save energy during computation and reduce die area consumed on an integrated circuit. Examples of such improvements include different interaction modules for different ranges, the use of streaming along rows while multicasting along columns in an array of interaction modules, the selection of computation units based on balancing computational costs and communication costs, the use of fences in networks that connect computation units, and the use of bond calculators to carry out specialized bond calculations.

公开(公告)号：US11701354B2

公开(公告)日：2023-07-18

申请号：US16651733

申请日：2018-09-28

申请人： Relay Therapeutics, Inc. ,  D. E. Shaw Research, LLC

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

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

CPC分类号： A61K31/4985 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00

摘要： Cellular biological activities are tightly controlled by intracellular signaling processes initiated by extracellular signals. Protein tyrosine phosphatases, which remove phosphate groups from tyrosine phosphorylated signaling molecules, play equally important tyrosine roles as protein kinases in signal transduction. SHP-2, a cytoplasmic SH2 domain containing protein tyrosine phosphatase, is involved in the signaling pathways of a variety of growth factors and cytokines. Recent studies have clearly demonstrated that this phosphatase plays an important role in transducing signal relay from the cell surface to the nucleus, and is a critical intracellular regulator in mediating cell proliferation and differentiation.

公开(公告)号：US11591336B2

公开(公告)日：2023-02-28

申请号：US16616361

申请日：2018-05-25

申请人： Relay Therapeutics, Inc. ,  D. E. Shaw Research, LLC

发明人： Alexander M. Taylor ,  André Lescarbeau ,  Elizabeth H. Kelley ,  Kelley C. Shortsleeves ,  Lucian V. DiPietro ,  W. Patrick Walters ,  Mark Andrew Murcko ,  Levi Charles Thomas Pierce ,  Yong Tang ,  Fabrizio Giordanetto ,  Jack Benjamin Greisman ,  Paul Maragakis ,  Sathesh Bhat ,  Markus Kristofer Dahlgren ,  Eric Therrien

IPC分类号： A61K31/4985 ,  C07D487/04 ,  C07D519/00

摘要： The present disclosure relates to 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 and compositions of the disclosure.

公开(公告)号：US20230049231A1

公开(公告)日：2023-02-16

申请号：US17766834

申请日：2020-10-06

申请人： D. E. Shaw Research, LLC

发明人： Fabrizio GIORDANETTO ,  Morten Østergaard JENSEN ,  Vishwanath JOGINI ,  Roger John SNOW

IPC分类号： C07D471/04 ,  C07D401/02 ,  C07D405/02 ,  C07D413/02 ,  C07D487/04

摘要： A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is described, where the substituents are as defined herein. Pharmaceutical compositions including the same and method of using the same are also described.

公开(公告)号：US20230040182A1

公开(公告)日：2023-02-09

申请号：US17766837

申请日：2020-10-06

申请人： D. E. Shaw Research, LLC

发明人： Fabrizio GIORDANETTO ,  Morten Østergaard JENSEN ,  Vishwanath JOGINI ,  Roger John SNOW

IPC分类号： C07D471/04 ,  C07D471/14 ,  C07D487/04

摘要： A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is described, where the substituents are as defined herein. Pharmaceutical compositions including the same and method of using the same are also described.