公开(公告)号：US09796723B2

公开(公告)日：2017-10-24

申请号：US15401792

申请日：2017-01-09

Applicant: Array BioPharma, Inc.

Inventor： Steven W. Andrews ,  Julia Haas ,  Yutong Jiang ,  Gan Zhang

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/541 ,  C07C51/412 ,  C07C53/18 ,  C07D471/04 ,  C07D519/00

Abstract: Methods for treating a disease or disorder selected from pain, cancer, inflammation, neurodegenerative disease, Typanosoma cruzi infection and osteolytic disease in a mammal, which comprise administering to said mammal a therapeutically effective amount of a compound of Formula I in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification.

公开(公告)号：US09718822B2

公开(公告)日：2017-08-01

申请号：US15401839

申请日：2017-01-09

Applicant: Array BioPharma, Inc.

Inventor： Steven W. Andrews ,  Kevin Ronald Condroski ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Jeongbeob Seo ,  Hong-Woon Yang ,  Qian Zhao

IPC: C07D487/22 ,  A61K31/519 ,  C07D471/22 ,  C07D498/22

CPC classification number: C07D498/22 ,  A61K31/519 ,  C07D471/22 ,  C07D487/04 ,  C07D487/22 ,  C07D519/00

Abstract: 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, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

公开(公告)号：US09682979B2

公开(公告)日：2017-06-20

申请号：US14321246

申请日：2014-07-01

Applicant: Array BioPharma Inc.

Inventor： Shelley Allen ,  Steven Wade Andrews ,  Kevin Ronald Condroski ,  Julia Haas ,  Lily Huang ,  Yutong Jiang ,  Timothy Krecher ,  Jeongbeob Seo

IPC: A01N43/90 ,  A61K31/519 ,  C07D487/04 ,  C07D519/00 ,  C07D453/02 ,  C07D471/22 ,  C07D498/22

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  C07D453/02 ,  C07D471/22 ,  C07D498/22 ,  C07D519/00

Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

公开(公告)号：US20160355521A1

公开(公告)日：2016-12-08

申请号：US14442609

申请日：2013-11-13

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

CPC classification number: C07D491/048 ,  C07D231/40 ,  C07D231/52 ,  C07D231/54 ,  C07D231/56 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/02 ,  C07D403/04 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D453/02 ,  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.

公开(公告)号：US20160297796A1

公开(公告)日：2016-10-13

申请号：US14442522

申请日：2013-11-13

Applicant: ARRAY BIOPHARMA INC.

Inventor： Shelley Allen ,  Steven Wade Andrews ,  James F. Blake ,  Barbara J. Brandhuber ,  Kevin Ronald Condroski ,  Julia Haas ,  Yutong Jiang ,  Timothy Kercher ,  Gabrielle R. Kolakowski ,  Shannon L. Winski

IPC: C07D401/12 ,  C07D417/14 ,  C07D417/12 ,  C07D413/12 ,  C07D401/14 ,  C07D403/12

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: Compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Ring B, and Ring C are as defined herein, and wherein Ring 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/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.

公开(公告)号：US20160228441A1

公开(公告)日：2016-08-11

申请号：US14846166

申请日：2015-09-04

Applicant: Array BioPharma, Inc.

Inventor： Julia Haas ,  Steven W. Andrews ,  Yutong Jiang ,  Gan Zhang

IPC: A61K31/519 ,  A61K45/06 ,  A61K31/5377 ,  A61K9/00

CPC classification number: C07D487/04 ,  A61K9/0053 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  A61P29/00 ,  C07D471/04 ,  C07D519/00

Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.

Abstract translation: 用于合成用于治疗哺乳动物疼痛，癌症，炎症，神经变性疾病或克氏锥虫感染的化合物的化合物。

公开(公告)号：US11851434B2

公开(公告)日：2023-12-26

申请号：US17514684

申请日：2021-10-29

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: A61K31/4985 ,  C07D487/04

CPC classification number: 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：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：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：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.