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：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.

公开(公告)号：US20230374024A1

公开(公告)日：2023-11-23

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

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：US20230192619A1

公开(公告)日：2023-06-22

申请号：US17922208

申请日：2021-04-30

Applicant: Exelixis, Inc.

Inventor： Frenel DeMorin ,  Khalid Shah ,  Sagar Shakya ,  Yong Wang ,  Wei Xu

IPC: C07D215/48

CPC classification number: C07D215/48

Abstract: The present invention relates to processes for the synthetic preparation of c-Met inhibitors of Formula I, or pharmaceutically acceptable salts thereof. The present invention further relates to processes for the synthetic preparation of the c-Met inhibitor, Compound 1, or a pharmaceutically acceptable salt thereof. The present invention also relates to processes for the synthetic preparation of Compound 1.hemifumarate. The invention further relates to large scale processes for the synthetic preparation of the c-Met inhibitor, Compound 1 and Compound 1.hemifumarate.

公开(公告)号：US20230151003A1

公开(公告)日：2023-05-18

申请号：US17800084

申请日：2021-02-23

Applicant: Exelixis, Inc.

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

IPC: C07D471/04 ,  C07D401/12 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D401/12 ,  C07D519/00

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：US11542259B2

公开(公告)日：2023-01-03

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：US10035790B2

公开(公告)日：2018-07-31

申请号：US14436355

申请日：2013-10-17

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  EXELIXIS, INC.

Inventor： Wei Xu ,  Yong Wang ,  Sunghoon Ma ,  Elena S. Koltun ,  Byung Gyu Kim ,  Joon Won Jeong ,  T. G. Murali Dhar ,  Lynne Canne Bannen

IPC: C07D403/04 ,  C07D403/14 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D405/14 ,  C07D417/14

CPC classification number: C07D403/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: Described are RORy modulators of the formula (I), and N-oxides thereof, and pharmaceutically acceptable salts thereof, and solvates and hydrates thereof, wherein R1, R2, R3, R4, R5, R6, Ra, x, y, L, G, Z, the bond denoted by “q”, the ring system denoted by “A” and the ring system denoted by “B” are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORy activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORy activity, for example, autoimmune and/or inflammatory disorders.

公开(公告)号：US20150376133A1

公开(公告)日：2015-12-31

申请号：US14847801

申请日：2015-09-08

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: C07D215/46 ,  A61K31/506 ,  A61K31/47 ,  C07D401/12 ,  A61K31/4709 ,  A61K31/505 ,  C07D239/94 ,  C07D413/12 ,  C07D417/12 ,  A61K31/5377 ,  A61K31/4725 ,  A61K31/501 ,  A61K31/496 ,  C07D401/14 ,  C07D413/14 ,  C07D405/14 ,  C12Q1/48 ,  C07D403/12

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, 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.

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/或调节激酶受体，特别是c-Met，KDR，c-Kit，flt-3和flt-4，与细胞活性变化相关的信号转导途径的喹啉和喹啉 含有这些化合物的组合物，以及使用它们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：US20150266856A1

公开(公告)日：2015-09-24

申请号：US14436355

申请日：2013-10-17

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  EXELIXIS, INC.

Inventor： Wei Xu ,  Yong Wang ,  Sunghoon Ma ,  Elena S. Koltun ,  Byung Gyu Kim ,  Joon Won Jeong ,  T.G. Muralii Dhar ,  Lynn Canne Bannen

IPC: C07D403/04 ,  C07D405/14 ,  C07D413/14 ,  C07D403/14 ,  C07D417/14

CPC classification number: C07D403/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: Described are RORy modulators of the formula (I), and N-oxides thereof, and pharmaceutically acceptable salts thereof, and solvates and hydrates thereof, wherein R1, R2, R3, R4, R5, R6, Ra, x, y, L, G, Z, the bond denoted by “q”, the ring system denoted by “A” and the ring system denoted by “B” are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORy activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORy activity, for example, autoimmune and/or inflammatory disorders.

Abstract translation: 描述了式（I）的RORY调节剂及其N-氧化物及其药学上可接受的盐及其溶剂化物和水合物，其中R1，R2，R3，R4，R5，R6，Ra，x，y，L， G，Z，由“q”表示的键，由“A”表示的环系统和由“B”表示的环系统在此定义。 还提供了包含其的药物组合物。 这样的化合物和组合物可用于调节细胞中的RORY活性的方法和用于治疗受试者治疗受益于RORY活性（例如自身免疫和/或炎症性疾病）的疾病或病症的受试者的方法。