公开(公告)号：US20130085135A1

公开(公告)日：2013-04-04

申请号：US13678395

申请日：2012-11-15

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Anna Banka ,  Josef R. Bencsik ,  James F. Blake ,  Martin F. Hentemann ,  Nicholas C. Kallan ,  Jun Liang ,  Ian S. Mitchell ,  Stephen T. Schlachter ,  Eli M. Wallace ,  Rui Xu ,  Tony P. Tang

IPC: C07D401/04 ,  C07D401/10 ,  C07D403/10 ,  C07D417/10 ,  C07D487/04 ,  C07D401/12 ,  C07D403/04 ,  C07D409/04 ,  C07D239/70

CPC classification number: C07D401/10 ,  C07D211/08 ,  C07D211/46 ,  C07D239/70 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D409/04 ,  C07D417/04 ,  C07D417/10 ,  C07D487/04

Abstract: Compounds of Formula I are useful for inhibiting AKT protein kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract translation: 式I化合物可用于抑制AKT蛋白激酶。 公开了使用式I化合物及其立体异构体及其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US20130072500A1

公开(公告)日：2013-03-21

申请号：US13676963

申请日：2012-11-14

Applicant: Array BioPharma Inc.

Inventor： Anna Banka ,  Josef R. Bencsik ,  James F. Blake ,  Kin Chiu Fong ,  Martin F. Hentemann ,  Ian S. Mitchell ,  Douglas McCord Sammond ,  Tony P. Tang ,  Eli M. Wallace ,  Rui Xu

IPC: C07D471/10 ,  C07D487/10

CPC classification number: C07D471/10 ,  C07D487/10

Abstract: The present invention provides compounds of Formula I including tautomers, resolved enantiomers, resolved diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as Akt protein kinase inhibitors and for the treatment of Akt-mediated diseases, for example, hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供式I化合物，其包括互变异构体，拆分的对映异构体，拆分的非对映体，溶剂合物，代谢物，盐和药学上可接受的前药。 还提供了使用本发明化合物作为Akt蛋白激酶抑制剂和治疗Akt介导的疾病例如过度增殖性疾病如癌症的方法。

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：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.

公开(公告)号：US11603374B2

公开(公告)日：2023-03-14

申请号：US16962345

申请日：2019-01-18

Applicant: Array BioPharma Inc.

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

IPC: C07D487/04

Abstract: Provided herein are compounds of the Formula I: [INSERT FORMULA I] and tautomers, stereoisomers and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2 and Ry 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：US11524963B2

公开(公告)日：2022-12-13

申请号：US16961973

申请日：2019-01-18

Applicant: Array Biopharma Inc.

Inventor： James F. Blake ,  Donghua Dai ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Andrew T. Metcalf ,  David A. Moreno ,  Brett Prigaro ,  Li Ren

IPC: A61K31/519 ,  C07D487/04

Abstract: Provided herein are compounds of the Formula I: and tautomers and pharmaceutically acceptable salts and solvates thereof, wherein R1 and R2 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：US11453683B1

公开(公告)日：2022-09-27

申请号：US17005004

申请日：2020-08-27

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 F. 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

Abstract: Compounds that inhibit KRas G12D; in particular, compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor, and in particular, methods of treating cancer. The compounds have a general structure represented by Formula (I): or a pharmaceutically acceptable salt thereof.

公开(公告)号：US11267812B2

公开(公告)日：2022-03-08

申请号：US16099398

申请日：2017-05-17

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

Inventor： John P. Fischer ,  Jay Bradford Fell ,  James F. Blake ,  Ronald Jay Hinklin ,  Macedonio J. Mejia ,  Erik James Hicken ,  Mark Joseph Chicarelli ,  John J. Gaudino ,  Guy P. A. Vigers ,  Laurence E. Burgess ,  Matthew Arnold Marx ,  James Gail Christensen ,  Matthew Randolph Lee ,  Pavel Savechenkov ,  Henry J. Zecca ,  Tony P. Tang

IPC: C07D471/04 ,  C07D519/00 ,  A61P35/00

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：US10953005B1

公开(公告)日：2021-03-23

申请号：US16739846

申请日：2020-01-10

Applicant: Array BioPharma, Inc.

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

IPC: C07D401/02 ,  C07D401/10 ,  A61K31/437 ,  A61K31/4353 ,  A61K31/496 ,  C07D471/04 ,  A61P1/12 ,  A61P35/04 ,  C07D519/00 ,  A61P35/02 ,  A61K31/551 ,  A61K31/444 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00

Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X1, X2, X3, X4, Ring D, and E 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：US10441581B2

公开(公告)日：2019-10-15

申请号：US15860894

申请日：2018-01-03

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

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.