公开(公告)号：US20240309020A1

公开(公告)日：2024-09-19

申请号：US18644056

申请日：2024-04-23

申请人： Mirati Therapeutics, Inc. ,  Array BioPharma Inc.

发明人： 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分类号： C07D519/00

CPC分类号： C07D519/00

摘要： 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：US11998545B2

公开(公告)日：2024-06-04

申请号：US18342314

申请日：2023-06-27

申请人： Array BioPharma, Inc.

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

CPC分类号： A61K31/496 ,  A61K31/444 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  A61P1/12 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  C07D471/04 ,  C07D519/00

摘要： 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：US11964989B2

公开(公告)日：2024-04-23

申请号：US17869575

申请日：2022-07-20

申请人： Mirati Therapeutics, Inc. ,  Array BioPharma Inc.

发明人： 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分类号： C07D519/00

CPC分类号： C07D519/00

摘要： 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：US20220081438A1

公开(公告)日：2022-03-17

申请号：US17416117

申请日：2019-12-13

申请人： ARRAY BIOPHARMA INC.

发明人： James F. Blake ,  David A. MORENO ,  Li REN ,  Tony P. TANG ,  Shane M. WALLS

IPC分类号： C07D471/04 ,  C07D519/00

摘要： Provided herein are compounds of the general Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which Ring A, Ring B, Ring C, R1, R2, L, Y, and W have the meanings given in the specification, which are inhibitors of FGFR1, FGFR2, FGFR3 and/or FGFR4 and are useful in the treatment and prevention of diseases which can be treated with an FGFR inhibitor, including diseases or disorders mediated by FGFR1, FGFR2, FGFR3 and/or FGFR4.

公开(公告)号：US20210186959A1

公开(公告)日：2021-06-24

申请号：US17165168

申请日：2021-02-02

申请人： Array BioPharma, Inc.

发明人： 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分类号： A61K31/496 ,  A61K31/506 ,  A61K31/4995 ,  C07D519/00 ,  A61P35/00 ,  A61K31/5377 ,  A61P1/12 ,  A61P35/04 ,  A61P35/02 ,  A61K31/4985 ,  C07D471/04 ,  A61K45/06 ,  A61K31/551 ,  A61K31/444

摘要： 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：US10966985B2

公开(公告)日：2021-04-06

申请号：US16199818

申请日：2018-11-26

申请人： Array BioPharma Inc.

发明人： Steven W. Andrews ,  James F. Blake ,  Julia Haas ,  Gabrielle R. Kolakowski

IPC分类号： A61K31/529 ,  G01N33/574 ,  A61K31/519 ,  A61K45/06 ,  A61P35/00 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/675

摘要： Methods for inhibiting a ROS1 kinase with compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein. The compounds and methods provided herein are useful in the treatment of cancer (e.g., ROS1-associated cancers as defined herein).

公开(公告)号：US10881652B2

公开(公告)日：2021-01-05

申请号：US16579150

申请日：2019-09-23

申请人： Array Biopharma Inc.

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

摘要： 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：US20200345735A1

公开(公告)日：2020-11-05

申请号：US16736078

申请日：2020-01-07

申请人： Array BioPharma Inc. ,  Genentech, Inc.

发明人： Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik ,  Eli M. Wallace ,  Stephen T. Schlachter ,  Anna L. Leivers ,  Jun Liang ,  Brian Safina ,  Birong Zhang ,  Christine Chabot ,  Steven Do

IPC分类号： A61K31/517 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D239/70 ,  C07D413/12 ,  C07D407/12

摘要： The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

公开(公告)号：US10689377B2

公开(公告)日：2020-06-23

申请号：US16191190

申请日：2018-11-14

申请人： Mirati Therapeutics, Inc. ,  Array BioPharma Inc.

发明人： James F. Blake ,  Laurence E. Burgess ,  Mark Joseph Chicarelli ,  James Gail Christensen ,  Adam Cook ,  Jay Bradford Fell ,  John P. Fischer ,  Matthew Arnold Marx ,  Macedonio J. Mejia ,  Pavel Savechenkov ,  Guy P. A. Vigers ,  Christopher Ronald Smith ,  Martha E. Rodriguez

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

摘要： 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：US10555944B2

公开(公告)日：2020-02-11

申请号：US16173100

申请日：2018-10-29

申请人： Array BioPharma, Inc.

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

摘要： 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.