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公开(公告)号:US11667643B2
公开(公告)日:2023-06-06
申请号:US17358698
申请日:2021-06-25
发明人: Somasekhar Bhamidipati , Simon Shaw , Ihab Darwish , Jiaxin Yu , Rao Kolluri , Vanessa Taylor , Esteban Masuda , Mark Irving
IPC分类号: A61P9/00 , A61P25/00 , A61P29/00 , A61P37/00 , A61K31/55 , A61K31/551 , A61K31/553 , A61K31/554 , C07D471/04 , C07D487/04 , C07D498/04 , C07D498/14 , C07D498/22 , C07D513/04 , C07D513/14 , C07D519/00
CPC分类号: C07D487/04 , C07D471/04 , C07D498/04 , C07D498/22 , C07D513/14 , C07D519/00
摘要: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.
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公开(公告)号:US11649236B2
公开(公告)日:2023-05-16
申请号:US17058251
申请日:2019-05-30
申请人: Shionogi & Co., Ltd.
发明人: Yoshiyuki Taoda , Yuto Unoh
IPC分类号: C07D471/14 , C07D471/18 , C07D491/22 , C07D498/22 , A61P31/18
CPC分类号: C07D471/14 , C07D471/18 , C07D491/22 , C07D498/22 , C07D471/18 , C07B2200/07 , C07D491/22 , C07B2200/07 , C07D498/22 , C07B2200/07 , C07D471/20 , C07B2200/07 , C07D471/22 , C07B2200/07 , C07D498/14 , C07B2200/07
摘要: The present invention provides a compound represented by Formula (I):
wherein ring A is a substituted or unsubstituted heterocycle; ring C is a benzene ring or the like; R1 is halogen or the like; R2a and R2b are each independently hydrogen or the like; R3 is substituted or unsubstituted alkyl or the like; R4 is hydrogen or the like; and n is an integer of 1 to 3.-
公开(公告)号:US20230146535A1
公开(公告)日:2023-05-11
申请号:US17964491
申请日:2022-10-12
申请人: PFIZER INC.
发明人: Thomas Allen Chappie , Nandini Chaturbhai Patel , Patrick Robert Verhoest , Christopher John Helal , Simone Sciabola , Erik Alphie LaChapelle , Travis T. Wager , Ramalakshmi Yegna Chandrasekaran
IPC分类号: C07D471/14 , C07D491/147 , C07D491/22 , C07D513/14 , C07D519/00 , C07D487/04 , C07D487/14 , C07D498/22 , C07D471/22
CPC分类号: C07D471/14 , C07D491/147 , C07D491/22 , C07D513/14 , C07D519/00 , C07D487/04 , C07D487/14 , C07D498/22 , C07D471/22
摘要: The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents A, R1, R2, R3a, R3b, R4a, R4b and n are as defined herein. The inventions also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds and methods of preparing the compounds.
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公开(公告)号:US20230099745A1
公开(公告)日:2023-03-30
申请号:US17528729
申请日:2021-11-17
发明人: Jeremy J. Clemens , William Schulz Bechara , Brett C. Bookser , Thomas Cleveland , Timothy R. Coon , Michel Gallant , Peter Grootenhuis , Sara Sabina Hadida Ruah , Julie Laterreur , Mark Thomas Miller , Prasuna Paraselli , Yeeman K. Ramtohul , Thumkunta Jagadeeswar Reddy , Claudio Sturino , Lino Valdez , Jinglan Zhou
IPC分类号: A61K31/439 , A61K31/404 , A61K31/443 , A61K31/4439 , A61K31/529 , C07D498/22 , C07D498/18 , A61K31/4995
摘要: This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR), pharmaceutical compositions containing at least one such modulator, methods of treatment of cystic fibrosis using such modulators and pharmaceutical compositions, and processes for making such modulators.
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公开(公告)号:US11608346B2
公开(公告)日:2023-03-21
申请号:US17088986
申请日:2020-11-04
发明人: Elena S. Koltun , James Cregg , Adrian L. Gill
IPC分类号: C07D498/18 , C07D401/14 , C07D498/22 , C07D513/22 , C07D519/00 , A61P35/00
摘要: The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.
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公开(公告)号:US20230019032A1
公开(公告)日:2023-01-19
申请号:US17224733
申请日:2021-04-07
发明人: Valerio BERDINI , Ildiko Maria BUCK , James Edward Harvey DAY , Charlotte Mary GRIFFITHS-JONES , Thomas Daniel HEIGHTMAN , Steven HOWARD , Christopher William MURRAY , David NORTON , Marc O'REILLY , Alison Jo-Anne WOOLFORD , Michael Liam COOKE , David COUSIN , Stuart Thomas ONIONS , Jonathan Martin SHANNON , John Paul WATTS
IPC分类号: C07D405/14 , C07D403/14 , C07D409/14 , C07D471/04 , C07D413/14 , C07D471/08 , C07D401/14 , C07D417/14 , A61P35/00 , A61K31/444 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/553 , C07D403/04 , C07D487/04 , C07D497/08 , C07D498/22 , C07D513/04
摘要: The invention provides a compound of formula (0): or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and C—F; Z is selected from C—Rz and N; R1 is selected from: -(Alk1)t-Cyc1; wherein t is 0 or 1; Optionally substituted C1-6 acyclic hydrocarbon groups R2 is selected from hydrogen; halogen; and C1-3 hydrocarbon groups optionally substituted with one or more fluorine atoms; R3 is hydrogen or a group L1-R7; R4 is selected from hydrogen; methoxy; and optionally substituted C1-3 alkyl; and R4a is selected from hydrogen and a C1-3 alkyl group; wherein Rz, Alk1, Cyc1, L1 and R7 are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof. The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.
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公开(公告)号:US11542278B1
公开(公告)日:2023-01-03
申请号:US17514877
申请日:2021-10-29
申请人: Nuvalent, Inc.
发明人: Joshua Courtney Horan , Xinxing Tang , Scot Richard Mente , Henry Efrem Pelish , Matthew D. Shair , Anupong Tangpeerachaikul
IPC分类号: A61K31/4427 , C07D471/22 , C07D498/22 , A61P35/00 , C07D513/22
摘要: Disclosed are heterocyclic heteroaromatic macrocyclic ether compounds of Formula (I): pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof. The disclosure further relates to methods of treating or preventing cancer using the heterocyclic heteroaromatic macrocyclic ether compounds, pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof.
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公开(公告)号:US20220306651A1
公开(公告)日:2022-09-29
申请号:US17617873
申请日:2020-06-12
发明人: Giles Albert Brown , Miles Stuart Congreve , Stephen Paul Watson , Julie Cansfield , Michael Alistair O'Brien , Francesca Deflorian , Gregory R. Ott , Nigel Alan Swain , Andrew David Cansfield , John Andrew Christopher , Andrea Bortolato
IPC分类号: C07D498/22
摘要: The disclosures herein relate to novel compounds of Formula (1): and salts thereof, wherein A1, A2, Q, X, R1, R2 and R3 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with CGRP receptors.
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公开(公告)号:US20220289765A1
公开(公告)日:2022-09-15
申请号:US17638358
申请日:2020-08-27
发明人: Jianfei Wang , Jikui Sun , Guangwen Yang , Yang Zhang
IPC分类号: C07D498/22 , A61P35/00
摘要: Disclosed are a crystal of a carcinogenic fused kinase inhibitor and a preparation method therefor; also disclosed are applications of the crystal in preparing a medicament for treating tumor-related diseases.
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公开(公告)号:US20220235070A1
公开(公告)日:2022-07-28
申请号:US17612315
申请日:2020-05-20
发明人: Youxi CHEN , Liang GONG , Xingwu ZHU , Qing XIANG , Wentao MAO , Cheng YE , Taishan HU , Lei CHEN , Guoping JIANG
IPC分类号: C07D498/22 , C07D487/04 , A61P35/00
摘要: Provided are a macrolide derivative represented by formula (I), a preparation method thereof, and an application of the macrolide derivative as an inhibitor of one or more protein kinases of TRK, ALK and ROS1,
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