公开(公告)号：US11007194B2

公开(公告)日：2021-05-18

申请号：US14355903

申请日：2012-11-09

Applicant: Array BioPharma Inc.

Inventor： Darrin Stuart ,  Meghna Das Thakur

IPC: A61K31/506

Abstract: The present invention relates to a method of treating a patient with a serine/threonine kinase inhibitor wherein resistance to the treatment with a serine/threonine kinase inhibitor is suppressed by administering the serine/threonine kinase inhibitor on an intermittent dosing schedule.

公开(公告)号：US20200331911A1

公开(公告)日：2020-10-22

申请号：US16917128

申请日：2020-06-30

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

Inventor： Matthew Arnold Marx ,  James Gail Christensen ,  Christopher Ronald Smith ,  John P. Fischer ,  Aaron Craig Burns

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

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：US20200246338A1

公开(公告)日：2020-08-06

申请号：US16722384

申请日：2019-12-20

Applicant: Array BioPharma Inc.

Inventor： Giordano Caponigro ,  Darrin Stuart ,  Laure De Parseval

IPC: A61K31/506 ,  A61K45/06 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K9/00 ,  A61K9/20 ,  A61K9/48 ,  C12Q1/6886

Abstract: Reversing resistance to a B-Raf inhibitor for the treatment of a proliferative disease by obtaining a tumor sample from the patient and testing it for genetic alterations in a panel of genes comprising BRAF, CRAF, CCND1, CDK4, HER2, IGF-1R, cMET, FGFR1, FGFR2, FGFR3, EGFR, MAP2K1, MAP2K2, NRAS, KRAS, HRAS, PTEN, PIK3CA, and P16 and administering a drug combination therapy comprising the B-Raf inhibitor and a second inhibitor which overcomes resistance to the B-Raf inhibitor, which second inhibitor is selected based on genetic alterations discovered in the tumor sample.

公开(公告)号：US20200230108A1

公开(公告)日：2020-07-23

申请号：US16580505

申请日：2019-09-24

Applicant: Array BioPharma Inc.

Inventor： Giordano Caponigro ,  Zhu Alexander Cao

IPC: A61K31/4184 ,  A61K31/506 ,  A61K39/395 ,  A61P35/04 ,  A61K45/06 ,  A61K31/573 ,  A61P35/00 ,  C07K16/28 ,  A61K9/00

Abstract: Provided herein are pharmaceutical combinations comprising (a) a B-Raf inhibitor, or a pharmaceutically acceptable salt thereof, (b) at least one mitogen activated protein kinase (MEK) inhibitor, or a pharmaceutically acceptable salt thereof, and (c) an epidermal growth factor receptor (EGFR) inhibitor or a pharmaceutically acceptable salt thereof; and optionally at least one pharmaceutically acceptable carrier; methods for preparing the pharmaceutical combinations, and the uses of the pharmaceutical combinations in the treatment of proliferative diseases, such as cancer.

公开(公告)号：US20200216451A1

公开(公告)日：2020-07-09

申请号：US16345571

申请日：2017-10-26

Applicant: Array BioPharma Inc. ,  Loxo Oncology, Inc.

Inventor： Qian Zhao ,  Stacey Spencer ,  Yutong Jiang ,  Julia Haas ,  Charles Todd Eary

IPC: C07D471/22

Abstract: In some embodiments, provided herein are processes for preparing a compound of Formula C or a salt thereof, as disclosed herein. In some embodiments, provided herein is a compound of Formula I or a pharmaceutically acceptable salt, solvate or hydrate thereof. In some embodiments, provided herein is a solid form of the compound, such as a crystalline form of the compound crystalline Form I.

公开(公告)号：US20200179344A1

公开(公告)日：2020-06-11

申请号：US16597237

申请日：2019-10-09

Applicant: AstraZeneca AB ,  Array BioPharma, Inc.

Inventor： Nicola Frances BATEMAN ,  Paul Richard GELLERT ,  Kathryn Jane HILL

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

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：US20200055860A1

公开(公告)日：2020-02-20

申请号：US16478071

申请日：2018-01-18

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: 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：US10548894B2

公开(公告)日：2020-02-04

申请号：US15875031

申请日：2018-01-19

Applicant: Array BioPharma Inc.

Inventor： Giordano Caponigro ,  Darrin Stuart ,  Laure De Parseval

IPC: A61K31/506 ,  A61K45/06 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K9/00 ,  A61K9/20 ,  A61K9/48 ,  C12Q1/6886

Abstract: Reversing resistance to a B-Raf inhibitor for the treatment of a proliferative disease by obtaining a tumor sample from the patient and testing it for genetic alterations in a panel of genes comprising BRAF, CRAF, CCND1, CDK4, HER2, IGF-1R, cMET, FGFR1, FGFR2, FGFR3 EGFR, MAP2K1, MAP2K2, NRAS, KRAS HRAS, PTEN, PIK3CA, and P16 and administering a drug combination therapy comprising the B-Raf inhibitor and a second inhibitor which overcomes resistance to the B-Raf inhibitor, which second inhibitor is selected based on genetic alterations discovered in the tumor sample.

公开(公告)号：US20200030311A1

公开(公告)日：2020-01-30

申请号：US16579150

申请日：2019-09-23

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

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：US20200000807A1

公开(公告)日：2020-01-02

申请号：US16366368

申请日：2019-03-27

Applicant: Array BioPharma, Inc.

Inventor： Alisha B. Arrigo ,  Derrick Juengst ,  Khalid Shah

IPC: A61K31/519 ,  C07D487/04 ,  C12Q1/48

Abstract: A novel crystalline form of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.