公开(公告)号：EP3458456B1

公开(公告)日：2020-11-25

申请号：EP17726442.1

申请日：2017-05-18

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

发明人： REYNOLDS, Mark ,  EARY, Charles Todd ,  SPENCER, Stacey ,  JUENGST, Derrick ,  HACHE, Bruno ,  JIANG, Yutong ,  HAAS, Julia ,  ANDREWS, Steven W.

IPC分类号： C07D487/04 ,  A61K31/5025 ,  A61P35/00 ,  A61P43/00

公开(公告)号：EP3322706A1

公开(公告)日：2018-05-23

申请号：EP16741825.0

申请日：2016-07-15

申请人： Array Biopharma, Inc.

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

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

摘要： 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：EP3523302A1

公开(公告)日：2019-08-14

申请号：EP17787844.4

申请日：2017-10-10

申请人： Array Biopharma, Inc. ,  McFaddin, Elizabeth A. ,  McKenney, Megan L. ,  McNulty, Oren T. ,  Metcalf, Andrew T. ,  Moreno, David A. ,  Ramann, Ginelle A. ,  Tang, Tony P. ,  Ren, Li ,  Walls, Shane M.

发明人： ANDREWS, Steven W. ,  ARONOW, Sean ,  BLAKE, James F. ,  BRANDENHUBER, Barbara J. ,  COLLIER, James ,  COOK, Adam ,  HAAS, Julia ,  JIANG, Yutong ,  KOLAKOWSKI, Gabrielle R.

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

公开(公告)号：EP3523301B1

公开(公告)日：2020-05-27

申请号：EP17787843.6

申请日：2017-10-10

申请人： Array Biopharma Inc.

发明人： ANDREWS, Steven W. ,  ARONOW, Sean ,  BLAKE, James F. ,  BRANDHUBER, Barbara J. ,  COOK, Adam ,  HAAS, Julia ,  JIANG, Yutong ,  KOLAKOWSKI, Gabrielle R. ,  MCFADDIN, Elizabeth A. ,  MCKENNEY, Megan L. ,  MCNULTY, Oren T. ,  METCALF, Andrew T. ,  MORENO, David A. ,  TANG, Tony P. ,  REN, Li

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

公开(公告)号：EP3154959B1

公开(公告)日：2019-07-10

申请号：EP15726455.7

申请日：2015-05-14

申请人： Array Biopharma, Inc.

发明人： ALLEN, Shelley ,  ANDREWS, Steven W. ,  BAER, Brian ,  CRANE, Zackary ,  LIU, Weidong ,  WATSON, Daniel John

IPC分类号： A61K45/06 ,  A61K9/00 ,  A61K31/506 ,  C07D207/16 ,  C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  C07D403/14

公开(公告)号：EP3154959A1

公开(公告)日：2017-04-19

申请号：EP15726455.7

申请日：2015-05-14

申请人： Array Biopharma, Inc.

发明人： ALLEN, Shelley ,  ANDREWS, Steven W. ,  BAER, Brian ,  CRANE, Zackary ,  LIU, Weidong ,  WATSON, Daniel John

IPC分类号： C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  C07D403/14 ,  A61K31/4155

CPC分类号： A61K31/506 ,  A61K9/0053 ,  A61K45/06 ,  C07D207/16 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14

摘要： Provided is Compound (I) or a pharmaceutically acceptable salt thereof, which is an inhibitor of TrkA kinase and is useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation and inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis, pelvic pain syndrome, diseases related to an imbalance of the regulation of bone remodeling, and diseases resulting from Connective Tissue Growth Factor aberrant signaling.

摘要翻译： 提供作为TrkA激酶抑制剂的化合物（I）或其药学上可接受的盐，可用于治疗可用TrkA激酶抑制剂如疼痛，癌症，炎症和炎性疾病，神经变性疾病治疗的疾病 ，某些传染病，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，骨盆疼痛综合征，与骨重塑调节失调有关的疾病，以及由结缔组织生长因子异常信号传导引起的疾病。

公开(公告)号：EP2044032A2

公开(公告)日：2009-04-08

申请号：EP07810228.2

申请日：2007-07-05

申请人： Intermune, Inc. ,  Array Biopharma, Inc.

发明人： BLATT, Lawrence M. ,  SEIWERT, Scott ,  BEIGELMAN, Leonid ,  KERCHER, Timothy ,  KENNEDY, April L. ,  ANDREWS, Steven W.

IPC分类号： C07D231/56 ,  C07D403/14 ,  C07D471/04 ,  A61K31/4035 ,  A61K31/416 ,  A61K31/437 ,  A61P31/14

CPC分类号： C07D403/14 ,  C07D231/56 ,  C07D471/04

摘要： The embodiments provide compounds of the general Formula (I), as well as compositions, including pharmaceutical compositions, comprising a, subject compound. The embodiments provide compounds of the general Formula (II), as well as compositions, including pharmaceutical compositions, comprising a subject compound, The embodiments provide compounds of the general Formula (III), 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.

公开(公告)号：EP3800189A1

公开(公告)日：2021-04-07

申请号：EP20208218.6

申请日：2017-05-18

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

发明人： REYNOLDS, Mark ,  EARY, Charles Todd ,  SPENCER, Stacey ,  JUENGST, Derrick ,  HACHE, Bruno ,  JIANG, Yutong ,  HAAS, Julia ,  ANDREWS, Steven W.

IPC分类号： C07D487/04 ,  A61K31/5025 ,  A61P35/00 ,  A61P43/00

摘要： 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-l-yl)-pyrazolo[l,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：EP3322706B1

公开(公告)日：2020-11-11

申请号：EP16741825.0

申请日：2016-07-15

申请人： Array Biopharma, Inc.

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

IPC分类号： A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/499 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  C07D519/00 ,  A61P1/00 ,  A61P35/04 ,  A61P43/00 ,  C07D471/04 ,  A61P29/00 ,  A61P35/00

公开(公告)号：EP3595651A1

公开(公告)日：2020-01-22

申请号：EP18716714.3

申请日：2018-03-16

申请人： Array Biopharma Inc.

发明人： ANDREWS, Steven W. ,  BLAKE, James F. ,  HAAS, Julia ,  LOLAKOWSKI, Gabrielle R.

IPC分类号： A61K31/395 ,  G01N33/574