公开(公告)号：WO2018136663A1

公开(公告)日：2018-07-26

申请号：PCT/US2018/014281

申请日：2018-01-18

Applicant: ARRAY BIOPHARMA, INC.

Inventor： ANDREWS, Steven W. ,  BLAKE, James F. ,  HAAS, Julia ,  JIANG, Yutong

IPC: C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  A61P35/00 ,  A61K31/506

Abstract: Provided herein are compounds of the Formula (I): and pharmaceutically acceptable salts or solvates thereof, where A, B, Y, X 1 , X 2 , X 3 , X 4 , R 1 , R 2 , n and m are as defined 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：WO2012158413A2

公开(公告)日：2012-11-22

申请号：PCT/US2012/037003

申请日：2012-05-09

Applicant: ARRAY BIOPHARMA INC. ,  ALLEN, Shelley ,  ANDREWS, Steven, W. ,  BLAKE, James, F. ,  CONDROSKI, Kevin, R. ,  HAAS, Julia ,  HUANG, Lily ,  JIANG, Yutong ,  KERCHER, Timothy ,  KOLAKOWSKI, Gabrielle R. ,  SEO, Jeongbeob

Inventor： ALLEN, Shelley ,  ANDREWS, Steven, W. ,  BLAKE, James, F. ,  CONDROSKI, Kevin, R. ,  HAAS, Julia ,  HUANG, Lily ,  JIANG, Yutong ,  KERCHER, Timothy ,  KOLAKOWSKI, Gabrielle R. ,  SEO, Jeongbeob

IPC: C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  A61K31/4155 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4375 ,  A61K31/454 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61P25/28 ,  A61P29/02 ,  A61P35/00 ,  A61P33/00

CPC classification number: C07D403/12 ,  A61K31/4155 ,  A61K31/4162 ,  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 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  Y02A50/414

Abstract: Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R 1 , R 2 , R a , R b , R c , R d , 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.

Abstract translation: 其中R1，R2，Ra，Rb，Rc，Rd，X，Y，B和环C如本文所定义的式I化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂合物或前药，其中 YB部分和NH-C（= X）-NH部分是反式构型，是TrkA激酶的抑制剂，可用于治疗可用TrkA激酶抑制剂如疼痛，癌症，炎症治疗的疾病 ，神经变性疾病和某些传染病。

公开(公告)号：WO2020055672A1

公开(公告)日：2020-03-19

申请号：PCT/US2019/049859

申请日：2019-09-06

Applicant: ARRAY BIOPHARMA INC.

Inventor： BLAKE, James F. ,  DAI, Donghua ,  HAAS, Julia ,  JIANG, Yutong ,  KAHN, Dean ,  KOLAKOWSKI, Gabrielle R. ,  MCFADDIN, Elizabeth A. ,  MCKENNEY, Megan L. ,  METCALF, Andrew T. ,  MORENO, David A. ,  PRIGARO, Brett ,  RAMANN, Ginelle A. ,  REN, Li ,  WALLS, Shane M. ,  ZHANG, Hailong

IPC: C07D487/14 ,  C07D487/22 ,  C07D498/14 ,  C07D498/22 ,  A61P35/00 ,  A61K31/551

Abstract: Provided herein are compounds of the Formula (I): (I) and tautomers, stereoisomers and pharmaceutically acceptable salts and solvates thereof, wherein R x , R y , W, X, Y, Z, Ring A and (AA) 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：WO2019143994A1

公开(公告)日：2019-07-25

申请号：PCT/US2019/014277

申请日：2019-01-18

Applicant: ARRAY BIOPHARMA INC.

Inventor： WALLS, Shane M. ,  REN, Li ,  RAMANN, Ginelle A. ,  MORENO, David A. ,  METCALF, Andrew T. ,  MCFADDIN, Elizabeth A. ,  KOLAKOWSKI, Gabrielle R. ,  BLAKE, James F. ,  DAI, Donghua ,  HAAS, Julia ,  JIANG, Yutong ,  KAHN, Dean

IPC: C07D471/04 ,  A61P35/00 ,  A61K31/437

Abstract: Provided herein are compounds of the Formula I: and tautomers and pharmaceutically acceptable salts and solvates thereof, wherein R 1 , R 2 and R 3 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：WO2007047146A2

公开(公告)日：2007-04-26

申请号：PCT/US2006/039044

申请日：2006-10-10

Applicant: INTERMUNE, INC. ,  ARRAY BIOPHARMA, INC. ,  BEIGELMAN, Leonid ,  ANDREWS, Steven, W. ,  CONDROSKI, Kevin, R. ,  GUNAWARADANA, Indrani ,  HAAS, Julia

Inventor： BEIGELMAN, Leonid ,  ANDREWS, Steven, W. ,  CONDROSKI, Kevin, R. ,  GUNAWARADANA, Indrani ,  HAAS, Julia

CPC classification number: C07D409/04 ,  C07C233/11 ,  C07C233/22 ,  C07C323/62 ,  C07D205/04 ,  C07D207/09 ,  C07D207/27 ,  C07D211/58 ,  C07D211/62 ,  C07D231/12 ,  C07D233/56 ,  C07D233/72 ,  C07D233/74 ,  C07D233/76 ,  C07D233/78 ,  C07D235/02 ,  C07D249/08 ,  C07D295/13 ,  C07D295/185 ,  C07D307/68 ,  C07D401/06 ,  C07D403/06 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/06 ,  C07D471/04 ,  C07D487/04

Abstract: The embodiments provide compounds of the general Formulas I-IV, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

Abstract translation: 实施方案提供通式I-IV的化合物，以及包含药物组合物的组合物，其包含主题化合物。 所述实施方案进一步提供治疗方法，包括治疗丙型肝炎病毒感染的方法和治疗肝纤维化的方法，所述方法通常包括向有需要的个体施用有效量的主题化合物或组合物。

公开(公告)号：WO2020101736A1

公开(公告)日：2020-05-22

申请号：PCT/US2019/032249

申请日：2019-05-14

Applicant: MIRATI THERAPEUTICS, INC. ,  ARRAY BIOPHARMA INC.

Inventor： MARX, Matthew, Arnold ,  BOBINSKI, Thomas, P. ,  BURNS, Aaron, Craig ,  GAUDINO, John ,  HAAS, Julia ,  KETCHAM, John, Michael ,  LAWSON, John, David ,  NEWHOUSE, Brad ,  PAJK, Spencer ,  SMITH, Christopher, Ronald ,  TANG, Tony, P.

IPC: A61K31/519 ,  C07D471/04 ,  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：WO2017011776A1

公开(公告)日：2017-01-19

申请号：PCT/US2016/042576

申请日：2016-07-15

Applicant: ARRAY BIOPHARMA, INC.

Inventor： ANDREWS, Steven W. ,  BLAKE, James F. ,  CHICARELLI, Mark J. ,  GOLOS, Adam ,  HAAS, Julia ,  JIANG, Yutong ,  KOLAKOWSKI, Gabrielle R.

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00 ,  A61P29/00

CPC classification number: C07D471/04 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/499 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D519/00

Abstract: Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X 1 , X 2 , X 3 and X 4 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.

Abstract translation: 本文提供了通式I的化合物及其立体异构体及其药学上可接受的盐或溶剂化物，其中A，B，D，E，X 1，X 2，X 3和X 4具有说明书中给出的含义，其为RET的抑制剂 激酶，并且可用于治疗和预防可用RET激酶抑制剂治疗的疾病，包括由RET激酶介导的疾病或病症。

公开(公告)号：WO2014078454A1

公开(公告)日：2014-05-22

申请号：PCT/US2013/069951

申请日：2013-11-13

Applicant: ARRAY BIOPHARMA INC. ,  ALLEN, Shelley ,  ANDREWS, Steven, Wade ,  BLAKE, James, F. ,  BRANDHUBER, Barbara, J. ,  HAAS, Julia ,  JIANG, Yutong ,  KERCHER, Timothy ,  KOLAKOWSKI, Gabrielle, R. ,  THOMAS, Allen, A. ,  WINSKI, Shannon, L.

Inventor： ALLEN, Shelley ,  ANDREWS, Steven, Wade ,  BLAKE, James, F. ,  BRANDHUBER, Barbara, J. ,  HAAS, Julia ,  JIANG, Yutong ,  KERCHER, Timothy ,  KOLAKOWSKI, Gabrielle, R. ,  THOMAS, Allen, A. ,  WINSKI, Shannon, L.

IPC: C07D401/14 ,  C07D405/14 ,  C07D231/40 ,  C07D231/54 ,  C07D401/12 ,  C07D403/02 ,  C07D403/04 ,  C07D403/14 ,  C07D405/12 ,  C07D413/12 ,  C07D453/02 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/4162 ,  A61P25/00

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.

Abstract translation: 式I化合物或其立体异构体，互变异构体或其药学上可接受的盐，溶剂合物或前药，其中环A，环C和X如本文所定义，是TrkA激酶的抑制剂，并且可用于治疗可治疗的疾病 具有TrkA激酶抑制剂如疼痛，癌症，炎症/炎性疾病，神经变性疾病，某些感染性疾病，干燥综合征，子宫内膜异位症，糖尿病性周围神经病变，前列腺炎和骨盆疼痛综合征。

公开(公告)号：WO2014078331A1

公开(公告)日：2014-05-22

申请号：PCT/US2013/069750

申请日：2013-11-12

Applicant: ARRAY BIOPHARMA INC. ,  BLAKE, James F. ,  BRANDHUBER, Barbara J. ,  HAAS, Julia ,  NEWHOUSE, Brad ,  THOMAS, Allen A. ,  WINSKI, Shannon L.

Inventor： BLAKE, James F. ,  BRANDHUBER, Barbara J. ,  HAAS, Julia ,  NEWHOUSE, Brad ,  THOMAS, Allen A. ,  WINSKI, Shannon L.

IPC: C07D403/12 ,  C07D401/14 ,  C07D231/40 ,  C07D231/52 ,  C07D231/54 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D413/12 ,  C07D495/04 ,  A61K31/4155 ,  A61P35/00 ,  A61P29/00

CPC classification number: C07D231/52 ,  C07D231/38 ,  C07D231/40 ,  C07D231/54 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D453/02 ,  C07D495/04

Abstract: Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C, X, Ra, Rb, Rc, Rd and n 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 or pelvic pain syndrome.

Abstract translation: 式I或其立体异构体，互变异构体或其药学上可接受的盐，溶剂合物或前药的化合物，其中环A，环C，X，R a，R b，R c，R d和n如本文所定义，是TrkA激酶的抑制剂，并且是有用的 治疗可用TrkA激酶抑制剂如疼痛，癌症，炎症/炎性疾病，神经变性疾病，某些感染性疾病，干燥综合征，子宫内膜异位症，糖尿病性周围神经病变，前列腺炎或骨盆疼痛综合征治疗的疾病。

公开(公告)号：WO2011006074A1

公开(公告)日：2011-01-13

申请号：PCT/US2010/041538

申请日：2010-07-09

Applicant: ARRAY BIOPHARMA INC. ,  ALLEN, Shelley ,  ANDREWS, Steven S. ,  CONDROSKI, Kevin Ronald ,  HAAS, Julia ,  HUANG, Lily ,  JIANG, Yutong ,  KERCHER, Timothy ,  SEO, Jeongbeob

Inventor： ALLEN, Shelley ,  ANDREWS, Steven S. ,  CONDROSKI, Kevin Ronald ,  HAAS, Julia ,  HUANG, Lily ,  JIANG, Yutong ,  KERCHER, Timothy ,  SEO, Jeongbeob

IPC: C07D487/04 ,  A61K31/519 ,  C07D519/00

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 R 1 , R 2 , R 3 , R 4 , 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.

Abstract translation: 其中R1，R2，R3，R4，X，Y和n具有本说明书中给出的含义的式（I）化合物及其盐是Trk激酶的抑制剂，可用于治疗可用 一种Trk激酶抑制剂，如疼痛，癌症，炎症，神经变性疾病和某些传染病。