公开(公告)号：US11504370B2

公开(公告)日：2022-11-22

申请号：US16402068

申请日：2019-05-02

Applicant: Array BioPharma Inc.

Inventor： Patrice A. Lee ,  Shannon L. Winski ,  Kevin Koch

IPC: A61K31/517 ,  A61P35/04 ,  A61P35/00 ,  A61K31/337 ,  A61K31/7068 ,  A61K45/06

Abstract: Compounds for the treatment of brain cancer are provided herein. Pharmaceutical compositions comprised of those compounds for the treatment of brain cancer are also provided herein.

公开(公告)号：US11472802B2

公开(公告)日：2022-10-18

申请号：US16962305

申请日：2019-01-18

Applicant: Array BioPharma Inc.

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

IPC: C07D471/04 ,  A61P35/00 ,  C07F9/6561

Abstract: Provided herein are compounds of the Formula I: and tautomers and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2 and R3 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：US20220087982A1

公开(公告)日：2022-03-24

申请号：US17313312

申请日：2021-05-06

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

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：US11214571B2

公开(公告)日：2022-01-04

申请号：US16302312

申请日：2017-05-18

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

Inventor： Mark Reynolds ,  Charles Todd Eary ,  Stacey Spencer ,  Derrick Juengst ,  Bruno Hache ,  Yutong Jiang ,  Julia Haas ,  Steven W. Andrews

IPC: C07D487/04

Abstract: Process for preparing (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a] pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide (formula I) or a salt thereof by reacting phenyl(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-3,3a-dihydropyrazolo[1,5-a]pyrimidin-3-yl)carbamate or a similar derivative (formula 13) with (S)-pyrrolidin-3-ol (formula 14). Process for preparing phenyl(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-3,3a-dihydropyrazolo[1,5-a]pyrimidin-3-yl)carbamate (formula 13) or a similar derivative by reduction of (R)-5-(2-(2,5-difluorophenyl) pyrrolidin-1-yl)-3-nitropyrazolo[1,5-a]pyrimidine (formula 11) to (R)-5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-amine (formula 12). Process for preparing (R)-2-(2,5-difluorophenyl)pyrrolidine(R)-2-hydroxysuccinate (formula 10) by treating (R)—N—((R)-1-(2,5-difluorophenyl)-3-(1,3-dioxan-2-yl)propyl)-2-methylpropane-2-sulfinamide (formula 19) with an acid and a reducing agent. (S)—N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, is a tyrosin kinase (TRK) inhibitor for trearing e.g. cancer.

公开(公告)号：US20210380609A1

公开(公告)日：2021-12-09

申请号：US17401892

申请日：2021-08-13

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

Inventor： 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: C07D519/00 ,  C07D471/04

Abstract: 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：US20210380582A1

公开(公告)日：2021-12-09

申请号：US17285997

申请日：2019-10-17

Applicant: Array BioPharma Inc.

Inventor： James Francis BLAKE ,  Mark Laurence BOYS ,  Mark Joseph CHICARELLI ,  Adam Wade COOK ,  Mohamed S. A. ELSAYED ,  Jay Bradford FELL ,  John Peter FISCHER ,  Ronald Jay HINKLIN ,  Oren Teague MCNULTY ,  Macedonio J. MEJIA ,  Martha E. RODRIGUEZ ,  Christina Elizabeth WONG

IPC: C07D471/04 ,  C07D519/00

Abstract: Compounds of Formula Ia or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases. Methods of using compounds of Formula Ia or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt 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

公开(公告)号：US11174273B2

公开(公告)日：2021-11-16

申请号：US16264194

申请日：2019-01-31

Applicant: Array BioPharma Inc.

Inventor： Eli Wallace ,  George Topalov ,  Joseph Lyssikatos ,  Alexandre Buckmelter ,  Qian Zhao

IPC: A61K31/517 ,  C07D498/10 ,  C07D239/94 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04 ,  A61P35/00 ,  A61P29/00

Abstract: The invention includes methods of using compounds of Formula I as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

公开(公告)号：US11091486B2

公开(公告)日：2021-08-17

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: A61P25/00 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00 ,  C07D471/22 ,  A61K31/519

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：US20210077493A1

公开(公告)日：2021-03-18

申请号：US16942094

申请日：2020-07-29

Applicant: Array BioPharma Inc.

Inventor： Donald T. Corson ,  Christopher M. Lindemann ,  Daniel J. Watson

IPC: A61K31/517 ,  A61K31/437 ,  A61P35/00 ,  C07D471/04 ,  A61K45/06

Abstract: Polymorphs of N4-(4-([1,2,4]triazolo[1,5 -a]pyridin-7-yloxy)-3 -methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine are provided herein. Processes for preparing the polymorphs and pharmaceutical composition comprising the polymorphs are also disclosed.

公开(公告)号：US10889589B2

公开(公告)日：2021-01-12

申请号：US16415575

申请日：2019-05-17

Applicant: Array BioPharma Inc.

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

Abstract: 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.