公开(公告)号：US20230151003A1

公开(公告)日：2023-05-18

申请号：US17800084

申请日：2021-02-23

申请人： Exelixis, Inc.

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

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

CPC分类号： C07D471/04 ,  C07D401/12 ,  C07D519/00

摘要： 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

申请人： Exelixis, Inc.

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

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

摘要： 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：US20210002228A1

公开(公告)日：2021-01-07

申请号：US17031196

申请日：2020-09-24

申请人： Exelixis, Inc.

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

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

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

公开(公告)号：US20200163954A1

公开(公告)日：2020-05-28

申请号：US16776139

申请日：2020-01-29

申请人： Exelixis, Inc.

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

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

摘要： 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：US10035790B2

公开(公告)日：2018-07-31

申请号：US14436355

申请日：2013-10-17

申请人： BRISTOL-MYERS SQUIBB COMPANY ,  EXELIXIS, INC.

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

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

CPC分类号： C07D403/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

摘要： 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：US20160031818A1

公开(公告)日：2016-02-04

申请号：US14776337

申请日：2014-03-17

申请人： Exelixis, Inc.

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

IPC分类号： C07D215/22 ,  G01N33/487 ,  C07D215/60

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

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

摘要翻译： 本发明涉及卡泊沙坦（I）的代谢物及其用途。

公开(公告)号：US20150376133A1

公开(公告)日：2015-12-31

申请号：US14847801

申请日：2015-09-08

申请人： Exelixis, Inc.

发明人： 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分类号： 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分类号： 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

摘要： 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.

摘要翻译： 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

申请人： BRISTOL-MYERS SQUIBB COMPANY ,  EXELIXIS, INC.

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

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

CPC分类号： C07D403/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

摘要： 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.

摘要翻译： 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。