公开(公告)号：US07169926B1

公开(公告)日：2007-01-30

申请号：US10918319

申请日：2004-08-12

Applicant: Laurence E. Burgess ,  Scott D. Cowen ,  Stephen L. Gwaltney, II ,  Jeongboeb Seo ,  Jeffrey A. Stafford

Inventor： Laurence E. Burgess ,  Scott D. Cowen ,  Stephen L. Gwaltney, II ,  Jeongboeb Seo ,  Jeffrey A. Stafford

IPC: C07D471/04 ,  C07D471/14 ,  C07D491/14 ,  C07D491/147

CPC classification number: C07D471/04 ,  C07D471/14 ,  C07D491/14 ,  C07D491/147

Abstract: Compounds are provided which may be used to inhibit DPP-IV comprising the formula: wherein the substituents are as described in the specification and claims.

Abstract translation: 提供可用于抑制DPP-IV的化合物，其包含下式：其中取代基如说明书和权利要求书中所述。

公开(公告)号：US07144907B2

公开(公告)日：2006-12-05

申请号：US10654580

申请日：2003-09-03

Applicant: Eli Wallace ,  Brian Hurley ,  Hon Woon Yang ,  Joseph Lyssikatos ,  Jim Blake

Inventor： Eli Wallace ,  Brian Hurley ,  Hon Woon Yang ,  Joseph Lyssikatos ,  Jim Blake

IPC: C07D261/20 ,  A61K31/423

CPC classification number: C07D471/04 ,  C07D261/20

Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9 and R10, W and Y 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 are methods 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R 1，R 2，R 7，R 4， 8，R 9和R 10，W和Y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和含有这些化合物的药物组合物。

公开(公告)号：US20060189649A1

公开(公告)日：2006-08-24

申请号：US11410343

申请日：2006-04-24

Applicant: Eli Wallace ,  Jim Blake

Inventor： Eli Wallace ,  Jim Blake

IPC: C07D471/02 ,  A61K31/4745

CPC classification number: C07D471/04 ,  C07D261/20

Abstract: Disclosed are compounds of the Formula V and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, R10, R11 and W 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 are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Abstract translation: 公开了式V的化合物及其药学上可接受的盐和前药，其中R 1，R 2，R 7，R 4， 8，R 9，R 10，R 11和W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和含有这些化合物的药物组合物。

公开(公告)号：US20040014643A1

公开(公告)日：2004-01-22

申请号：US10389012

申请日：2003-03-14

Applicant: Array BioPharma Inc.

Inventor： Barbara J. Brandhuber ,  Guy P.A. Vigers

IPC: A61K038/16 ,  G06F019/00 ,  G01N033/48 ,  G01N033/50 ,  C07K014/715

CPC classification number: A61K38/2006 ,  C07K14/7155 ,  C07K2299/00 ,  G01N33/6869 ,  G01N2333/715 ,  G06F19/16

Abstract: Crystals comprising a modified interleukin-1 type 1 receptor (IL-1R1) and one or more modulators of IL-1 activity are described. Methods of identifying potential inhibitors of IL-1 activity are also described. Compositions and methods for the treatment of IL-1 mediated diseases, such as rheumatoid arthritis, osteoarthritis, and other inflammatory conditions, are described.

Abstract translation: 描述了包含修饰的白细胞介素-1型受体（IL-1R1）和一种或多种IL-1活性调节剂的晶体。 还描述了识别IL-1活性的潜在抑制剂的方法。 描述了用于治疗IL-1介导的疾病如类风湿性关节炎，骨关节炎和其它炎性病症的组合物和方法。

公开(公告)号：US11964988B2

公开(公告)日：2024-04-23

申请号：US17274990

申请日：2019-09-06

Applicant: ARRAY BIOPHARMA INC.

Inventor： James F. Blake ,  Donghua Dai ,  Julia Haas ,  Yutong Jiang ,  Dean Kahn ,  Gabrielle R. Kolakowski ,  Elizabeth A. McFaddin ,  Megan L McKenney ,  Andrew T. Metcalf ,  David A. Moreno ,  Brett Prigaro ,  Ginelle A. Ramann ,  Li Ren ,  Shane M. Walls ,  Hailong Zhang

IPC: C07D498/22 ,  A61K31/519 ,  A61K31/55 ,  A61K31/554 ,  A61K45/06 ,  A61P35/00 ,  C07D487/14 ,  C07D498/14 ,  C07D513/22

CPC classification number: C07D498/22 ,  A61K31/519 ,  A61K31/55 ,  A61K31/554 ,  A61K45/06 ,  A61P35/00 ,  C07D487/14 ,  C07D498/14 ,  C07D513/22

Abstract: Provided herein are compounds of the Formula (I): (I) and tautomers, stereoisomers and pharmaceutically acceptable salts and solvates thereof, wherein Rx, Ry, W, X, Y, Z, Ring A and (AA) 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 RET-associated diseases and disorders.

公开(公告)号：US20240124474A1

公开(公告)日：2024-04-18

申请号：US18499669

申请日：2023-11-01

Applicant: Array BioPharma Inc.

Inventor： Mark Laurence BOYS ,  Bryan Daniel ELLIS ,  John Joseph GAUDINO ,  Erik James HICKEN ,  Ellen Ruth LAIRD ,  Nicholas Charles LAZZARA ,  Bradley Jon NEWHOUSE ,  Spencer Phillip PAJK

IPC: C07D487/04 ,  A61K45/06 ,  C07D519/00

CPC classification number: C07D487/04 ,  A61K45/06 ,  C07D519/00

Abstract: This invention relates to compounds of Formula (I):




and enantiomers thereof, and to pharmaceutically acceptable salts of Formula (I) and said enantiomers, wherein L1, L2, R1, R2, R3 and n are as defined herein. The invention further relates to pharmaceutical compositions comprising such compounds and salts, and to methods and uses of such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer, in a subject in need thereof.

公开(公告)号：US20240101553A1

公开(公告)日：2024-03-28

申请号：US18230580

申请日：2023-08-04

Applicant: MIRATI THERAPEUTICS, INC. ,  ARRAY BIOPHARMA INC.

Inventor： Matthew Arnold MARX ,  James Gail CHRISTENSEN ,  Christopher Ronald SMITH ,  James F. BLAKE ,  Laurence E. BURGESS ,  Mark Joseph CHICARELLI ,  Adam COOK ,  Jay Bradford FELL ,  John P. FISCHER ,  Macedonio J. MEJIA ,  Martha E. RODRIGUEZ ,  Pavel SAVECHENKOV ,  Tony P. TANG ,  Guy P.A. VIGERS

IPC: C07D471/04 ,  A61P35/00 ,  C07D491/08

CPC classification number: C07D471/04 ,  A61P35/00 ,  C07D491/08

Abstract: The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

公开(公告)号：US20240041834A1

公开(公告)日：2024-02-08

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 ,  A61K9/14 ,  A61K9/48 ,  C07D235/06 ,  A61K47/36 ,  A61K9/00 ,  A61K47/22

CPC classification number: A61K31/4184 ,  A61K9/145 ,  A61K9/146 ,  A61K9/4858 ,  A61K9/4866 ,  C07D235/06 ,  A61K47/36 ,  A61K9/0053 ,  A61K47/22

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：US20230279025A1

公开(公告)日：2023-09-07

申请号：US18015691

申请日：2021-02-25

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

Inventor： Xiaolun Wang ,  Aaron Craig Burns ,  James Gail Christensen ,  John Michael Ketcham ,  John David Lawson ,  Matthew Arnold Marx ,  Christopher Ronald Smith ,  Shelley Allen ,  James Francis Blake ,  Mark Joseph Chicarelli ,  Joshua Ryan Dahlke ,  Donghua Dai ,  Jay Bradford Fell ,  John Peter Fischer ,  Macedonio J. Mejia ,  Brad Newhouse ,  Phong Nguyen ,  Jacob Matthew O'Leary ,  Spencer Pajk ,  Martha E. Rodriguez ,  Pavel Savechenkov ,  Tony P. Tang ,  Guy P.A. Vigers ,  Qian Zhao ,  Dean Russell Kahn ,  John Gaudino ,  Michael Christopher Hilton

IPC: C07D519/00

CPC classification number: C07D519/00 ,  C07B2200/05

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：US11648243B2

公开(公告)日：2023-05-16

申请号：US17108528

申请日：2020-12-01

Applicant: Array Biopharma Inc.

Inventor： Steven W. Andrews ,  Sean Aronow ,  James F. Blake ,  Barbara J. Brandhuber ,  James Collier ,  Adam Cook ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Elizabeth A. Mcfaddin ,  Megan L. Mckenney ,  Oren T. McNulty ,  Andrew T. Metcalf ,  David A. Moreno ,  Ginelle A. Ramann ,  Tony P. Tang ,  Li Ren ,  Shane M. Walls

IPC: A61K31/4545 ,  A61K31/4162 ,  C07D471/04 ,  A61P1/00 ,  A61P35/00 ,  A61P35/02 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P1/12

CPC classification number: A61K31/4545 ,  A61K31/4162 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P1/00 ,  A61P1/12 ,  A61P35/00 ,  A61P35/02 ,  C07D471/04

Abstract: Provided herein are compounds of the Formula I:




or pharmaceutically acceptable salt or solvate thereof, wherein A, B, X1, X2, X3, X4, Ring D, E, Ra, Rb, n and m 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 RET-associated diseases and disorders.