公开(公告)号：US20240150371A1

公开(公告)日：2024-05-09

申请号：US18132124

申请日：2023-04-07

Applicant: Exelixis, Inc.

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

IPC: C07D491/147 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  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：US20210040076A1

公开(公告)日：2021-02-11

申请号：US16964330

申请日：2019-01-25

Applicant: Exelixis, Inc.

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

IPC: C07D413/12 ,  C07D215/22 ,  C07D401/12 ,  C07D405/12 ,  C07D413/10 ,  C07D498/04

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：US20200331860A1

公开(公告)日：2020-10-22

申请号：US16921542

申请日：2020-07-06

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

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：US10273211B2

公开(公告)日：2019-04-30

申请号：US14776337

申请日：2014-03-17

Applicant: Exelixis, Inc.

Inventor： Dana T. Aftab ,  Sriram Naganathan ,  Wei Xu ,  Steven Lacy ,  Linh Nguyen

IPC: C07D215/22 ,  C07C305/24 ,  C07C233/60 ,  C07D215/60 ,  G01N33/487

Abstract: The invention relates to metabolites of cabozantinib (I) as well as uses thereof.

公开(公告)号：US20190076420A1

公开(公告)日：2019-03-14

申请号：US16190869

申请日：2018-11-14

Applicant: Exelixis, Inc.

Inventor： Dana T. Aftab ,  Sriram Naganathan ,  Wei Xu ,  Steven Lacy

IPC: A61K31/47 ,  A61K9/00 ,  A61K9/20

Abstract: The invention relates to administration of various pharmaceutical formulations of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, (cabozantinib) a c-Met inhibitor, and its metabolites, to achieve desirable pharmacokinetic and pharmacodynamic effects.

公开(公告)号：US20160185725A1

公开(公告)日：2016-06-30

申请号：US15066872

申请日：2016-03-10

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 ,  C07D239/88 ,  C12Q1/48 ,  C07D215/36 ,  C07D215/38 ,  C07D401/12 ,  C07D401/14

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.

公开(公告)号：US20130252940A1

公开(公告)日：2013-09-26

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：US12264161B2

公开(公告)日：2025-04-01

申请号：US18323510

申请日：2023-05-25

Applicant: Exelixis, Inc.

Inventor： Sunghoon Ma ,  Yong Wang ,  Wei Xu

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

公开(公告)号：US20240287002A1

公开(公告)日：2024-08-29

申请号：US18641587

申请日：2024-04-22

Applicant: Exelixis, Inc.

Inventor： Dana T. Aftab ,  Sriram Naganathan ,  Wei Xu ,  Steven Lacy ,  Linh Nguyen

IPC: C07D215/22 ,  C07C233/60 ,  C07C305/24 ,  C07D215/60 ,  G01N33/487

CPC classification number: C07D215/22 ,  C07C233/60 ,  C07C305/24 ,  C07D215/60 ,  G01N33/487 ,  C07C2601/02 ,  G01N2570/00

Abstract: The invention relates to metabolites of cabozantinib (I) as well as uses thereof.

公开(公告)号：US20240043414A1

公开(公告)日：2024-02-08

申请号：US17989393

申请日：2022-11-17

Applicant: Exelixis, Inc.

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

IPC: C07D413/12 ,  C07D215/22 ,  C07D401/12 ,  C07D405/12 ,  C07D413/10 ,  C07D498/04

CPC classification number: C07D413/12 ,  C07D215/22 ,  C07D401/12 ,  C07D405/12 ,  C07D413/10 ,  C07D498/04

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.