公开(公告)号：US12195475B2

公开(公告)日：2025-01-14

申请号：US18334113

申请日：2023-06-13

Applicant: Exelixis, Inc.

Inventor： Lynne Canne Bannen ,  Minna Bui ,  Faming Jiang ,  Yong Wang ,  Wei Xu

IPC: C07D487/04 ,  C07D239/88 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12

Abstract: Disclosed herein are compounds of Formula (I′). Compounds of Formula (I′) inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

公开(公告)号：US11708367B2

公开(公告)日：2023-07-25

申请号：US16964228

申请日：2019-01-25

Applicant: Exelixis, Inc.

Inventor： Lynne Canne Bannen ,  Minna Bui ,  Faming Jiang ,  Yong Wang ,  Wei Xu

IPC: C07D487/04 ,  C07D239/88 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12

CPC classification number: C07D487/04 ,  C07D239/88 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12

Abstract: Disclosed herein are compounds of Formula (I′). Compounds of Formula (I′) inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

公开(公告)号：US20220315579A1

公开(公告)日：2022-10-06

申请号：US17033475

申请日：2020-09-25

Applicant: Exelixis, Inc.

Inventor： Lynne Bannen ,  Minna Bui ,  Faming Jiang ,  Jack Maung ,  Andrew Raub ,  Justin Salvant ,  Benjamin Spangler ,  Kin Tso ,  Yong Wang ,  Wei Xu

IPC: C07D471/04

Abstract: The present disclosure relates generally to compounds and pharmaceutical compositions suitable as modulators of protein kinases, and methods for their use in treating disorders mediated, at least in part by, protein kinases.

公开(公告)号：US20150202196A1

公开(公告)日：2015-07-23

申请号：US14518733

申请日：2014-10-20

Applicant: Exelixis, Inc.

Inventor： Lynne Canne Bannen ,  Diva Sze-Ming Chan ,  Timothy Patrick Forsyth ,  Richard George Khoury ,  James William Leahy ,  Morrison B. Mac ,  Larry W. Mann ,  John M. Nuss ,  Jason Jevious Parks ,  Yong Wang ,  Wei Xu ,  Diane Simeone

IPC: A61K31/47 ,  A61N5/10 ,  A61K31/7068

CPC classification number: A61K31/47 ,  A61K31/517 ,  A61K31/7068 ,  A61K45/06 ,  A61N5/10 ,  A61K2300/00

Abstract: Disclosed are methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt thereof, in combination with gemcitabine (GEM), or a pharmaceutically acceptable salt thereof, and optionally one or more additional treatments, wherein: R1 is halo; R2 is halo; R3 is (C1-C6)alkyl; R4 is (C1-C6)alkyl; and Q is CH or N.

Abstract translation: 公开了通过给予式I化合物或其药学上可接受的盐与吉西他滨（GEM）或其药学上可接受的盐以及任选的一种或多种另外的治疗组合治疗癌症的方法，其中：R1是卤素; R2是卤素; R3是（C1-C6）烷基; R4是（C1-C6）烷基; Q为CH或N.

公开(公告)号：US20230382917A1

公开(公告)日：2023-11-30

申请号：US18323510

申请日：2023-05-25

Applicant: Exelixis, Inc.

Inventor： Sunghoon Ma ,  Yong Wang ,  Wei Xu

IPC: C07D487/04 ,  C07D513/14 ,  C07D487/14

CPC classification number: C07D487/04 ,  C07D513/14 ,  C07D487/14

Abstract: Heterocyclic compounds useful as antagonists of adenosine receptors, and methods of treatment of diseases using antagonists of adenosine receptors are disclosed herein. Also disclosed herein are pharmaceutical compositions and methods of administration of heterocyclic antagonists of adenosine receptors and processes for producing heterocyclic antagonists of adenosine receptors.

公开(公告)号：US11673897B2

公开(公告)日：2023-06-13

申请号：US16964274

申请日：2019-01-25

Applicant: Exelixis, Inc.

Inventor： Lynne Canne Bannen ,  Minna Bui ,  Faming Jiang ,  Yong Wang ,  Wei Xu

IPC: C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D491/147 ,  C07D471/04

CPC classification number: C07D491/147 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04

Abstract: Disclosed herein are compounds of Formula I′. Compounds of Formula I′ inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

公开(公告)号：US20210032263A1

公开(公告)日：2021-02-04

申请号：US16964274

申请日：2019-01-25

Applicant: Exelixis, Inc.

Inventor： Lynne Canne Bannen ,  Minna Bui ,  Faming Jiang ,  Yong Wang ,  Wei Xu

IPC: C07D491/147 ,  C07D401/12 ,  C07D413/14 ,  C07D401/14 ,  C07D471/04

Abstract: Disclosed herein are compounds of Formula I′. Compounds of Formula I′ inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

公开(公告)号：US20170355678A1

公开(公告)日：2017-12-14

申请号：US15688310

申请日：2017-08-28

Applicant: Exelixis, Inc.

Inventor： Lynne Canne Bannen ,  Diva Sze-Ming Chan ,  Jeff Chen ,  Lisa Esther Dalrymple ,  Timothy Patrick Forsyth ,  Tai Phat Huynh ,  Vasu Jammalamadaka ,  Richard George Khoury ,  James William Leahy ,  Morrison B. Mac ,  Grace Mann ,  Larry W. Mann ,  John M. Nuss ,  Jason Jevious Parks ,  Craig Stacy Takeuchi ,  Yong Wang ,  Wei Xu

IPC: C07D215/233 ,  C07D239/94 ,  A61K31/4725 ,  C07D239/88 ,  C07D405/14 ,  A61K31/5377 ,  A61K31/505 ,  A61K31/517 ,  C07D295/15 ,  C07D413/12 ,  A61K31/506 ,  C07D401/12 ,  A61K31/501 ,  C07D413/14 ,  C07D215/46 ,  A61K31/47 ,  C12Q1/48 ,  A61K31/4709 ,  C07D403/12 ,  C07D215/22 ,  C07D215/36 ,  C07D417/12 ,  C07D215/38 ,  C07D401/14 ,  A61K31/496

CPC classification number: C07D215/233 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  C07D215/22 ,  C07D215/36 ,  C07D215/38 ,  C07D215/46 ,  C07D239/88 ,  C07D239/94 ,  C07D295/15 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C12Q1/485 ,  G01N2500/04 ,  Y02A50/393

Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

公开(公告)号：US20140155378A9

公开(公告)日：2014-06-05

申请号：US13888592

申请日：2013-05-07

Applicant: Exelixis, Inc.

Inventor： Lynne Canne Bannen ,  Diva Sze-ming Chan ,  Jeff Chen ,  Timothy Patrick Forsyth ,  Tai Phat Huynh ,  Vasu Jammalamadaka ,  Richard George Khoury ,  James William Leahy ,  Morrison B. Mac ,  Larry W. Mann ,  John M. Nuss ,  Jason Jevious Parks ,  Craig Stacy Takeuchi ,  Yong Wang ,  Wei Xu

IPC: C07D215/233 ,  C07D413/14 ,  C07D401/14 ,  C07D405/14 ,  C07D295/15 ,  C07D401/12

CPC classification number: C07D215/233 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  C07D215/22 ,  C07D215/36 ,  C07D215/38 ,  C07D215/46 ,  C07D239/88 ,  C07D239/94 ,  C07D295/15 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C12Q1/485 ,  G01N2500/04 ,  Y02A50/393

Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

Abstract translation: 本发明提供调节蛋白激酶酶活性以调节细胞活性如增殖，分化，程序性细胞死亡，迁移和化学侵蚀的化合物。 更具体地，本发明提供抑制，调节和/或调节与细胞活性变化相关的激酶受体，特别是c-Met，KDF，c-Kit，flt-3和flt-4信号转导途径的喹唑啉和喹啉 如上所述，含有这些化合物的组合物，及其用于治疗激酶依赖性疾病和病症的方法。 本发明还提供了制备上述化合物的方法和含有这些化合物的组合物。

公开(公告)号：US11718622B2

公开(公告)日：2023-08-08

申请号：US17201380

申请日：2021-03-15

Applicant: Exelixis, Inc.

Inventor： Sunghoon Ma ,  Yong Wang ,  Wei Xu

IPC: C07D487/04 ,  C07D487/14 ,  C07D513/14 ,  A61K31/4985 ,  A61K31/519 ,  A61P9/00 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00

CPC classification number: C07D487/04 ,  C07D487/14 ,  C07D513/14

Abstract: Heterocyclic compounds useful as antagonists of adenosine receptors, and methods of treatment of diseases using antagonists of adenosine receptors are disclosed herein. Also disclosed herein are pharmaceutical compositions and methods of administration of heterocyclic antagonists of adenosine receptors and processes for producing heterocyclic antagonists of adenosine receptors.