公开(公告)号：US11597699B2

公开(公告)日：2023-03-07

申请号：US16853043

申请日：2020-04-20

Applicant: Exelixis, Inc.

Inventor： Naing Aay ,  Neel Kumar Anand ,  Charles M. Blazey ,  Owen Joseph Bowles ,  Joerg Bussenius ,  Simona Costanzo ,  Jeffry Kimo Curtis ,  Steven Charles DeFina ,  Larisa Dubenko ,  Anagha Abhijit Joshi ,  Abigail R. Kennedy ,  Angie Inyoung Kim ,  Elena S. Koltun ,  Jean-Claire Limun Manalo ,  Csaba J. Peto ,  Kenneth D. Rice ,  Tsze H. Tsang

IPC: C07D205/04 ,  C07D205/06 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D401/04 ,  C07D409/12

Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.

公开(公告)号：US20170166523A9

公开(公告)日：2017-06-15

申请号：US14615079

申请日：2015-02-05

Applicant: Exelixis, Inc.

Inventor： Naing Aay ,  Neel Kumar Anand ,  Charles M. Blazey ,  Owen Joseph Bowles ,  Joerg Bussenius ,  Simona Costanzo ,  Jeffry Kimo Curtis ,  Steven Charles DeFina ,  Larisa Dubenko ,  Anagha Abhijit Joshi ,  Abigail R. Kennedy ,  Angie Inyoung Kim ,  Elena S. Koltun ,  Jean-Claire Limun Manalo ,  Csaba J. Peto ,  Kenneth D. Rice ,  Tsze H. Tsang

IPC: C07D205/04 ,  C07D403/06 ,  C07D401/14 ,  C07D471/04 ,  C07D401/04 ,  C07D403/04 ,  C07D409/06

CPC classification number: C07D205/04 ,  C07D205/06 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

Abstract: Disclosed are compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.

公开(公告)号：US20250100966A1

公开(公告)日：2025-03-27

申请号：US18672226

申请日：2024-05-23

Applicant: Exelixis, Inc.

Inventor： Naing Aay ,  Neel Kumar Anand ,  Charles M. Blazey ,  Owen Joseph Bowles ,  Joerg Bussenius ,  Simona Costanzo ,  Jeffry Kimo Curtis ,  Steven Charles DeFina ,  Larisa Dubenko ,  Anagha Abhijit Joshi ,  Abigail R Kennedy ,  Angie Inyoung Kim ,  Elena S. Koltun ,  Jean-Claire Limun Manalo ,  Csaba J. Peto ,  Kenneth D. Rice ,  Tsze H. Tsang

IPC: C07D205/04 ,  C07D205/06 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

Abstract: Disclosed am compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and am useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.

公开(公告)号：US20200283383A1

公开(公告)日：2020-09-10

申请号：US16853043

申请日：2020-04-20

Applicant: Exelixis, Inc.

Inventor： Naing Aay ,  Neel Kumar Anand ,  Charles M. Blazey ,  Owen Joseph Bowles ,  Joerg Bussenius ,  Simona Costanzo ,  Jeffry Kimo Curtis ,  Steven Charles DeFina ,  Larisa Dubenko ,  Anagha Abhijit Joshi ,  Abigail R. Kennedy ,  Angie Inyoung Kim ,  Elena S. Koltun ,  Jean-Claire Limun Manalo ,  Csaba J. Peto ,  Kenneth D. Rice ,  Tsze H. Tsang

IPC: C07D205/04 ,  C07D205/06 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D401/04

Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.

公开(公告)号：US20190144382A1

公开(公告)日：2019-05-16

申请号：US15952923

申请日：2018-04-13

Applicant: Exelixis, Inc.

Inventor： Naing Aay ,  Neel Kumar Anand ,  Charles M. Blazey ,  Owen Joseph Bowles ,  Joerg Bussenius ,  Simona Costanzo ,  Jeffry Kimo Curtis ,  Steven Charles DeFina ,  Larisa Dubenko ,  Anagha Abhijit Joshi ,  Abigail R. Kennedy ,  Angie Inyoung Kim ,  Elena S. Koltun ,  Jean-Claire Limun Manalo ,  Csaba J. Peto ,  Kenneth D. Rice ,  Tsza H. Tsang

IPC: C07D205/04 ,  C07D401/04 ,  C07D471/04 ,  C07D413/14 ,  C07D413/12 ,  C07D409/12 ,  C07D409/06 ,  C07D405/12 ,  C07D403/12 ,  C07D403/06 ,  C07D403/04 ,  C07D401/14 ,  C07D401/12 ,  C07D401/06 ,  C07D205/06 ,  C07D417/12

Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.

公开(公告)号：US20140275527A1

公开(公告)日：2014-09-18

申请号：US13929062

申请日：2013-06-27

Applicant: Exelixis, Inc.

Inventor： Naing Aay ,  Neel Kumar Anand ,  Charles M. Blazey ,  Owen Joseph Bowles ,  Joerg Bussenius ,  Simona Costanzo ,  Jeffry Kimo Curtis ,  Steven Charles DeFina ,  Larisa Dubenko ,  Anagha Abhijit Joshi ,  Abigail R. Kennedy ,  Angie Inyoung Kim ,  Elena S. Koltun ,  Jean-Claire Limun Manalo ,  Csaba J. Peto ,  Kenneth D. Rice ,  Tsze H. Tsang

IPC: C07D471/04 ,  C07D409/06 ,  C07D403/04 ,  C07D401/04 ,  C07D205/04 ,  C07D205/06

CPC classification number: C07D205/04 ,  C07D205/06 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.

Abstract translation: 公开了式（I）的化合物及其药学上可接受的盐和溶剂化物。 这些化合物是MEK抑制剂，可用于治疗增殖性疾病如癌症。 还公开了含有这些化合物的药物组合物以及使用本发明化合物和组合物治疗癌症的方法。

公开(公告)号：US20200031770A1

公开(公告)日：2020-01-30

申请号：US16597607

申请日：2019-10-09

Applicant: Exelixis, Inc.

Inventor： Naing Aay ,  Neel Kumar Anand ,  Charles M. Blazey ,  Owen Joseph Bowles ,  Joerg Bussenlus ,  Simona Costanzo ,  Jeffry Kimo Curtis ,  Steven Charles DeFina ,  Larisa Dubenko ,  Anagha Abhijit Joshi ,  Abigall R. Kennedy ,  Angle Inyoung Kim ,  Elena S. Koltun ,  Jean-Claire Limun Manalo ,  Csaba J. Peto ,  Kenneth D. Rice ,  Tsze H. Tsang

IPC: C07D205/04 ,  C07D205/06 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D401/04

Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.

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：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。

公开(公告)号：US20150141399A1

公开(公告)日：2015-05-21

申请号：US14615079

申请日：2015-02-05

Applicant: Exelixis, Inc.

Inventor： Naing Aay ,  Neel Kumar Anand ,  Charles M. Blazey ,  Owen Joseph Bowles ,  Joerg Bussenius ,  Simona Costanzo ,  Jeffry Kimo Curtis ,  Steven Charles DeFina ,  Larisa Dubenko ,  Anagha Abhijit Joshi ,  Abigail R. Kennedy ,  Angie Inyoung Kim ,  Elena S. Koltun ,  Jean-Claire Limun Manalo ,  Csaba J. Peto ,  Kenneth D. Rice ,  Tsze H. Tsang

IPC: C07D205/04 ,  C07D403/06 ,  C07D401/14 ,  C07D471/04 ,  C07D401/04 ,  C07D403/04 ,  C07D409/06

CPC classification number: C07D205/04 ,  C07D205/06 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

Abstract: Disclosed are compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.

Abstract translation: 公开了式I的化合物及其药学上可接受的盐和溶剂化物。 这些化合物是MEK抑制剂，可用于治疗增殖性疾病如癌症。 还公开了含有这些化合物的药物组合物以及使用本发明化合物和组合物治疗癌症的方法。