公开(公告)号：US07235537B2

公开(公告)日：2007-06-26

申请号：US10652733

申请日：2003-08-29

Applicant: Eli M. Wallace ,  Joseph P. Lyssikatos ,  Allison L. Marlow ,  T. Brian Hurley ,  Kevin Koch

Inventor： Eli M. Wallace ,  Joseph P. Lyssikatos ,  Allison L. Marlow ,  T. Brian Hurley ,  Kevin Koch

IPC: A61K31/675 ,  C07F9/06

CPC classification number: C07D235/06 ,  C04B35/632 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D413/04 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12 ,  C07F9/65068 ,  C07F9/65586

Abstract: Disclosed are compounds of the formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.

Abstract translation: 公开了式I化合物及其药学上可接受的盐和前药，其中W，R 1，R 2，R 7，R 7， SUP> 8，R 9和R 10如说明书中所定义。 这些化合物是MEK抑制剂，可用于治疗哺乳动物中的过度增生性疾病，例如癌症和炎症。 还公开了使用这些化合物治疗哺乳动物中过度增殖性疾病的方法，以及含有这些化合物的药物组合物。

公开(公告)号：US20060189668A1

公开(公告)日：2006-08-24

申请号：US11410344

申请日：2006-04-24

Applicant: Eli Wallace ,  Hong Yang ,  Jim Blake

Inventor： Eli Wallace ,  Hong Yang ,  Jim Blake

IPC: A61K31/42

CPC classification number: C07D471/04 ,  C07D261/20

Abstract: Disclosed are methods of inhibiting MEK activity, comprising administering to a mammal an effective amount of a compound of Formula I or IV or a solvate or pharmaceutically acceptable salt thereof, wherein R1, R2, R7, R8, R9, R10, W and Y are as defined in the specification. Also disclosed are methods of treating hyperproliferative diseases, such as cancer and inflammation, in mammals, said method comprising administering to a mammal an effective amount of a compound of Formula I or IV.

Abstract translation: 公开了抑制MEK活性的方法，包括向哺乳动物施用有效量的式I或IV化合物或其溶剂合物或药学上可接受的盐，其中R 1，R 2， R 4，R 8，R 8，R 9，R 10，W和Y定义如上所述。 在规范中。 还公开了在哺乳动物中治疗过度增殖性疾病如癌症和炎症的方法，所述方法包括向哺乳动物施用有效量的式I或IV化合物。

公开(公告)号：US20250152560A1

公开(公告)日：2025-05-15

申请号：US18838130

申请日：2023-02-13

Applicant: OnKure, Inc. ,  Array BioPharma Inc.

Inventor： Anthony D. Piscopio ,  Patrice Anne Lee ,  James Winkler ,  Richard D. Woessner

IPC: A61K31/429 ,  A61K31/4184 ,  A61K31/506 ,  A61P35/00

Abstract: A method of treating cancer in a subject in need thereof, wherein the method comprises administration of therapeutically effective amounts of OKI-179 and binimetinib or a pharmaceutically acceptable salt thereof, or administration of therapeutically effective amounts of OKI-179, binimetinib or a pharmaceutically acceptable salt thereof, and encorafenib or a pharmaceutically acceptable salt thereof according to the dosing schedules described herein.

公开(公告)号：US12220403B2

公开(公告)日：2025-02-11

申请号：US18484334

申请日：2023-10-10

Applicant: ASTRAZENECA AB ,  Array BioPharma, Inc.

Inventor： Nicola Frances Bateman ,  Paul Richard Gellert ,  Kathryn Jane Hill

IPC: A61K31/4184 ,  A61K9/00 ,  A61K9/14 ,  A61K9/48 ,  A61K47/22 ,  A61K47/36 ,  C07D235/06

Abstract: The invention concerns pharmaceutical compositions containing a hydrogen sulphate salt of 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide and solvates, crystalline forms and amorphous forms thereof, to the use of said compositions as a medicament; and to processes for the preparation of said compositions.

公开(公告)号：US20250011304A1

公开(公告)日：2025-01-09

申请号：US18709091

申请日：2022-12-02

Applicant: Array BioPharma Inc.

Inventor： Connor James COWDREY

IPC: C07D403/12 ,  A61K9/20 ,  A61K31/4184 ,  A61K31/517 ,  A61K45/06

Abstract: This invention relates to a crystalline form of N-(2-chloro-3-((5-chloro-3-methyl-4-oxo-3,4-dihydroquinazolin-6-yl)amino)-4-fluorophenyl)-3-fluoroazetidine-1-sulfonamide, pharmaceutical compositions comprising said crystalline form, and methods of using said crystalline form in the treatment of BRAF-associated diseases and disorders, such as BRAF-associated tumors.

公开(公告)号：US20240034733A1

公开(公告)日：2024-02-01

申请号：US18034852

申请日：2021-11-02

Applicant: Mirati Therapeutics, Inc. ,  Array BioPharma Inc.

Inventor： Matthew Arnold Marx ,  John David Lawson ,  Patrick Michael Doerner Barbaur ,  James Francis Blake ,  Jay Bradford Fell ,  John Peter Fischer ,  Bradley J. Newhouse ,  Phong Nguyen ,  Jacob M. O'Leary ,  Spencer Pajk ,  Martha E. Rodriguez ,  Tony Pisal Tang

IPC: C07D471/08 ,  C07D519/00 ,  C07D403/12

CPC classification number: C07D471/08 ,  C07D519/00 ,  C07D403/12

Abstract: The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.

公开(公告)号：US11851434B2

公开(公告)日：2023-12-26

申请号：US17514684

申请日：2021-10-29

Applicant: Array BioPharma Inc.

Inventor： Steven W. Andrews ,  James F. Blake ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  David A. Moreno ,  Li Ren ,  Shane M. Walls

IPC: A61K31/4985 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: Provided herein are compounds of the Formula I:




and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.

公开(公告)号：US20230357277A1

公开(公告)日：2023-11-09

申请号：US18027300

申请日：2021-09-21

Applicant: Mirati Therapeutics, Inc. ,  Array BioPharma Inc.

Inventor： Xiaolun Wang ,  Matthew Arnold Marx ,  Shelley Allen ,  Mark Joseph Chicarelli ,  Joshua Ryan Dahlke ,  Donghua Dai ,  Jay Bradford Fell ,  John Peter Fischer ,  Michael Christopher Hilton ,  Dean Russell Kahn ,  Macedonio Junior Mejia ,  Phong Nguyen ,  Spencer Pajk ,  Martha E. Rodriguez ,  Pavel Yu Savechenkov ,  Tony Pisal Tang

IPC: C07D519/00 ,  A61P35/00

CPC classification number: C07D519/00 ,  A61P35/00

Abstract: The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.

公开(公告)号：US20230339976A1

公开(公告)日：2023-10-26

申请号：US18020013

申请日：2021-08-03

Applicant: Mirati Therapeutics, Inc. ,  Array BioPharma Inc.

Inventor： Xiaolun Wang ,  Matthew Arnold Marx ,  John David Lawson ,  Shelley Allen ,  Patrick Michael Barbour ,  James Francis Blake ,  Joshua Ryan Dahlke ,  Donghua Dai ,  Jay Bradford Fell ,  John Peter Fischer ,  Sherif Hosam Hassanien ,  Michael Christopher Hilton ,  Macedonio Junior Mejia ,  Jacob Matthew O’Leary ,  Tony Pisal Tang

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D519/00 ,  C07D471/04

Abstract: The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.

公开(公告)号：USRE49556E1

公开(公告)日：2023-06-20

申请号：US17376199

申请日：2021-07-15

Applicant: Array BioPharma Inc.

Inventor： Shenlin Huang ,  Xianming Jin ,  Zuosheng Liu ,  Daniel Poon ,  John Tellew ,  Yongqin Wan ,  Xing Wang ,  Yongping Xie

IPC: A61K31/506 ,  A61K9/00 ,  A61K31/4184 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14

CPC classification number: A61K31/506 ,  A61K9/0053 ,  A61K31/4184 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  A61K31/506 ,  A61K2300/00

Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.