公开(公告)号：US11807651B2

公开(公告)日：2023-11-07

申请号：US17401892

申请日：2021-08-13

申请人： Loxo Oncology, Inc. ,  Array BioPharma Inc.

发明人： Charles Todd Eary ,  Stacey Spencer ,  Zack Crane ,  Katelyn Chando ,  Sylvie Asselin ,  Weidong Liu ,  Mike Welch ,  Adam Cook ,  Gabrielle R. Kolakowski ,  Andrew T. Metcalf ,  David A. Moreno ,  Tony P. Tang

IPC分类号： C07D519/00 ,  C07D471/04

CPC分类号： C07D519/00 ,  C07D471/04

摘要： In some embodiments, provided herein is a process for preparing a compound of Formula I




or a pharmaceutically acceptable salt thereof, as disclosed herein.

公开(公告)号：US11098064B2

公开(公告)日：2021-08-24

申请号：US16902424

申请日：2020-06-16

申请人： Loxo Oncology, Inc. ,  Array BioPharma Inc.

发明人： Charles Todd Eary ,  Stacey Spencer ,  Zack Crane ,  Katelyn Chando ,  Sylvie Asselin ,  Weidong Liu ,  Mike Welch ,  Adam Cook ,  Gabrielle R. Kolakowski ,  Andrew T. Metcalf ,  David A. Moreno ,  Tony P. Tang

IPC分类号： C07D519/00 ,  C07D471/04

摘要： In some embodiments, provided herein is a process for preparing a compound of Formula I or a pharmaceutically acceptable salt thereof, as disclosed herein.

公开(公告)号：US10907215B2

公开(公告)日：2021-02-02

申请号：US15860789

申请日：2018-01-03

申请人： Loxo Oncology, Inc. ,  Array BioPharma, Inc.

发明人： Nisha Nanda ,  Joshua H. Bilenker ,  James F. Blake ,  Gabrielle R. Kolakowski ,  Barbara J. Brandhuber ,  Steven W. Andrews

IPC分类号： A61K31/519 ,  C12Q1/6886 ,  A61K31/5025 ,  G01N33/574

摘要： Provided herein are methods of treating a subject having a cancer, methods of selecting a treatment for a subject having a cancer, methods of selecting a subject having a cancer for a treatment that does not include a Trk inhibitor, methods of determining the likelihood that a subject having a cancer will have a positive response to a treatment with a Trk inhibitor, methods of predicting the efficacy of a Trk inhibitor in a subject having cancer, methods of determining a subject's risk for developing a Trk inhibitor-resistant cancer, and methods of determining the presence of a Trk inhibitor-resistant cancer in a subject, based on the detection of a cell from a sample from the subject that has at least one of the the point mutations in NTRK1 and/or NTRK2 and/or NTRK3.

公开(公告)号：US10655186B2

公开(公告)日：2020-05-19

申请号：US15785218

申请日：2017-10-16

申请人： Loxo Oncology, Inc. ,  Array BioPharma, Inc.

发明人： Nisha Nanda ,  Joshua H. Bilenker ,  James F. Blake ,  Gabrielle R. Kolakowski ,  Barbara J. Brandhuber ,  Steven W. Andrews

IPC分类号： C12Q1/6886 ,  A61K31/5025 ,  A61K31/519 ,  G01N33/574

摘要： Provided herein are methods of treating a subject having a cancer, methods of selecting a treatment for a subject having a cancer, methods of selecting a subject having a cancer for a treatment that does not include a Trk inhibitor, methods of determining the likelihood that a subject having a cancer will have a positive response to a treatment with a Trk inhibitor, methods of predicting the efficacy of a Trk inhibitor in a subject having cancer, methods of determining a subject's risk for developing a Trk inhibitor-resistant cancer, and methods of determining the presence of a Trk inhibitor-resistant cancer in a subject, based on the detection of a cell from a sample from the subject that has at least one of the point mutations in NTRK1 and/or NTRK2 and/or NTRK3.

公开(公告)号：US20190270749A1

公开(公告)日：2019-09-05

申请号：US16415575

申请日：2019-05-17

申请人： Array BioPharma Inc.

发明人： Shelley Allen ,  Steven Wade Andrews ,  James F. Blake ,  Barbara J. Brandhuber ,  Julia Haas ,  Yutong Jiang ,  Timothy Kercher ,  Gabrielle R. Kolakowski ,  Allen A. Thomas ,  Shannon L. Winski

IPC分类号： C07D491/048 ,  C07D409/14 ,  C07D401/14 ,  C07D231/52 ,  C07D231/56 ,  C07D401/04 ,  C07D453/02 ,  C07D413/12 ,  C07D405/12 ,  C07D403/14 ,  C07D403/04 ,  C07D403/02 ,  C07D401/12 ,  C07D231/54 ,  C07D231/40 ,  C07D405/14 ,  C07D471/08

摘要： Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.

公开(公告)号：US10323022B2

公开(公告)日：2019-06-18

申请号：US15839706

申请日：2017-12-12

申请人： Array BioPharma Inc.

发明人： Shelley Allen ,  Steven W. Andrews ,  James F. Blake ,  Kevin R. Condroski ,  Julia Haas ,  Lily Huang ,  Yutong Jiang ,  Timothy Kercher ,  Gabrielle R. Kolakowski ,  Jeongbeob Seo

IPC分类号： C07D403/12 ,  A61K31/4162 ,  A61K31/4155 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  C07D491/048

摘要： Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Y, B, and Ring C are as defined herein, and wherein the Y—B moiety and the NH—C(═X)—NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

公开(公告)号：US20190076437A1

公开(公告)日：2019-03-14

申请号：US16199875

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 ,  A61K31/675 ,  A61K31/4545 ,  A61K31/496 ,  A61P35/00

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：US20190076436A1

公开(公告)日：2019-03-14

申请号：US16199867

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 ,  A61K31/675 ,  A61K31/4545 ,  A61P35/00

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：US10174027B2

公开(公告)日：2019-01-08

申请号：US15858658

申请日：2017-12-29

申请人： Array BioPharma, Inc.

发明人： Steven W. Andrews ,  James F. Blake ,  Mark J. Chicarelli ,  Adam Golos ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski

IPC分类号： C07D471/04 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/499 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D519/00

摘要： Provided herein are compounds of the General 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：US20180133207A1

公开(公告)日：2018-05-17

申请号：US15860894

申请日：2018-01-03

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： A61K31/4545 ,  A61K45/06 ,  A61P35/00 ,  A61P35/02 ,  A61K31/444 ,  A61K31/506 ,  A61K31/501 ,  A61K31/497 ,  A61K31/5377

CPC分类号： 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

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.