公开(公告)号：US09790190B2

公开(公告)日：2017-10-17

申请号：US15593064

申请日：2017-05-11

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： David Askin ,  Chong Han ,  Jonathan W. Lane ,  Travis Remarchuk ,  Sagar Shakya ,  C. Gregory Sowell ,  Keith L. Spencer ,  Peter J. Stengel

IPC: C07D403/00 ,  C07D239/42 ,  C07D403/04

CPC classification number: C07D239/42 ,  C07D239/30 ,  C07D239/70 ,  C07D403/04

Abstract: The invention provides processes for preparing a compound of formula I and salts thereof, wherein R1 is defined herein, and compounds and intermediates of said formula.

公开(公告)号：US20150099881A1

公开(公告)日：2015-04-09

申请号：US14401091

申请日：2013-05-17

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Jonathan W. Lane ,  Travis Remarchuk ,  Sagar Shakya ,  Keith L. Spencer ,  Peter J. Stengel

IPC: C07D239/70 ,  C07D239/42

CPC classification number: C07D239/70 ,  C07D239/42 ,  C07D403/04

Abstract: The invention provides new processes for making and purifying hydroxylated cyclopenta[d]pyrimidine compounds, which are useful for the treatment of diseases such as cancer as AKT protein kinase inhibitors, including the compound (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one.

Abstract translation: 本发明提供了用于制备和纯化羟基化环戊二烯并[d]嘧啶化合物的新方法，其可用于治疗诸如癌症的疾病作为AKT蛋白激酶抑制剂，包括化合物（S）-2-（4-氯苯基）-1 - （4 - （（5R，7R）-7-羟基-5-甲基-6,7-二氢-5H-环戊二烯并[d]嘧啶-4-基）哌嗪-1-基）-3-（异丙基氨基） -1。

公开(公告)号：US20150051217A1

公开(公告)日：2015-02-19

申请号：US14473336

申请日：2014-08-29

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Josef R. Bencsik ,  James F. Blake ,  Nicholas C. Kallan ,  Ian S. Mitchell ,  Keith L. Spencer ,  Dengming Xiao ,  Rui Xu ,  Christine Chabot ,  Steven Do ,  Jun Liang ,  Brian Safina ,  Birong Zhang ,  James Graham

IPC: C07D239/70

CPC classification number: C07D239/70

Abstract: The present invention provides a compound and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compound of this invention as an AKT protein kinase inhibitor and for the treatment of hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供了包含式I的化合物及其药学上可接受的盐：还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。

公开(公告)号：US20140080829A1

公开(公告)日：2014-03-20

申请号：US14086717

申请日：2013-11-21

Applicant: Genentech, Inc. ,  Array BioPharma Inc.

Inventor： Josef Bencsik ,  James F. Blake ,  James M. Graham ,  Martin F. Hentemann ,  Nicholas C. Kallan ,  Ian S. Mitchell ,  Stephen T. Schlachter ,  Keith L. Spencer ,  Dengming Xiao ,  Rui Xu ,  Mike Welch ,  Jun Liang ,  Brian S. Safina

IPC: C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/12 ,  C07D401/12 ,  C07D405/14

CPC classification number: C07D403/12 ,  C07D401/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12

Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

公开(公告)号：US20180258054A1

公开(公告)日：2018-09-13

申请号：US15782620

申请日：2017-10-12

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： David Askin ,  Chong Han ,  Jonathan W. Lane ,  Travis Remarchuk ,  Sagar Shakya ,  C. Gregory Sowell ,  Keith L. Spencer ,  Peter J. Stengel

IPC: C07D239/42 ,  C07D403/04

CPC classification number: C07D239/42 ,  C07D239/30 ,  C07D239/70 ,  C07D403/04

Abstract: The invention provides processes for preparing a compound of formula I and salts thereof, wherein R1 is defined herein, and compounds and intermediates of said formula.

公开(公告)号：US09676730B2

公开(公告)日：2017-06-13

申请号：US15204715

申请日：2016-07-07

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： David Askin ,  Chong Han ,  Jonathan W. Lane ,  Travis Remarchuk ,  Sagar Shakya ,  C. Gregory Sowell ,  Keith L. Spencer ,  Peter J. Stengel

IPC: C07D239/70 ,  C07D239/42 ,  C07D239/30 ,  C07D403/04

CPC classification number: C07D239/42 ,  C07D239/30 ,  C07D239/70 ,  C07D403/04

Abstract: The invention provides processes for preparing a compound of formula I and salts thereof, wherein R1 is defined herein, and compounds and intermediates of said formula.

公开(公告)号：US20160152601A9

公开(公告)日：2016-06-02

申请号：US14086717

申请日：2013-11-21

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Josef Bencsik ,  James F. Blake ,  James M. Graham ,  Martin F. Hentemann ,  Nicholas C. Kallan ,  Ian S. Mitchell ,  Stephen T. Schlachter ,  Keith L. Spencer ,  Dengming Xiao ,  Rui Xu ,  Mike Welch ,  Jun Liang ,  Brian S. Safina

IPC: C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/12 ,  C07D401/12 ,  C07D405/14

CPC classification number: C07D403/12 ,  C07D401/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12

Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

公开(公告)号：US20160318877A1

公开(公告)日：2016-11-03

申请号：US15204715

申请日：2016-07-07

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： David Askin ,  Chong Han ,  Jonathan W. Lane ,  Travis Remarchuk ,  Sagar Shakya ,  C. Gregory Sowell ,  Keith L. Spencer ,  Peter J. Stengel

IPC: C07D239/42

CPC classification number: C07D239/42 ,  C07D239/30 ,  C07D239/70 ,  C07D403/04

Abstract: The invention provides processes for preparing a compound of formula I and salts thereof, wherein R1 is defined herein, and compounds and intermediates of said formula.

Abstract translation: 和其盐，其中R1如本文所定义，以及所述式的化合物和中间体。

公开(公告)号：US20150197496A1

公开(公告)日：2015-07-16

申请号：US14665879

申请日：2015-03-23

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Josef R. Bencsik ,  James F. Blake ,  Nicholas C. Kallan ,  Ian S. Mitchell ,  Keith L. Spencer ,  Dengming Xiao ,  Rui Xu ,  Christine Chabot ,  Jun Liang ,  Brian S. Safina

IPC: C07D239/70 ,  C07D403/12 ,  C07D401/12 ,  C07D409/12

CPC classification number: C07D239/70 ,  A61K31/506 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12

Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供了式I化合物，包括互变异构体，拆分的对映异构体，非对映异构体，溶剂合物，代谢物，盐和药学上可接受的前药。 还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。

公开(公告)号：US08846683B2

公开(公告)日：2014-09-30

申请号：US13753008

申请日：2013-01-29

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Josef R. Bencsik ,  James F. Blake ,  Nicholas C. Kallan ,  Ian S. Mitchell ,  Keith L. Spencer ,  Dengming Xiao ,  Rui Xu ,  Christine Chabot ,  Jun Liang ,  Brian S. Safina

IPC: A61P35/00

CPC classification number: C07D239/70 ,  A61K31/506 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12

Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供了式I化合物，包括互变异构体，拆分的对映异构体，非对映异构体，溶剂合物，代谢物，盐和药学上可接受的前药。 还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。