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：US09481690B2

公开(公告)日：2016-11-01

申请号：US14991658

申请日：2016-01-08

Applicant: Genentech, Inc.

Inventor： Jeffrey Stults ,  Travis Remarchuk ,  Frederic St-Jean

IPC: C07D498/04 ,  A61K31/553 ,  C07D498/06 ,  A61K45/06

CPC classification number: C07D498/04 ,  A61K31/553 ,  A61K45/06 ,  C07B2200/13 ,  C07D498/06

Abstract: The present invention relates to crystalline polymorphs of (2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide (GDC-0032, taselisib), methods of use, and processes of preparing thereof.

Abstract translation: 本发明涉及（2-（4-（2-（1-异丙基-3-甲基-1H-1,2,4-三唑-5-基）-5,6-二氢苯并[f]咪唑并[ [1,2-d] [1,4]氧氮杂-9-基）-1H-吡唑-1-基）-2-甲基丙酰胺（GDC-0032，taselisib），使用方法及其制备方法。

公开(公告)号：US20150148559A1

公开(公告)日：2015-05-28

申请号：US14401095

申请日：2013-05-17

Applicant: Genentech, Inc.

Inventor： Travis Remarchuk

IPC: C07C269/06 ,  C07C271/22 ,  C07C229/30 ,  C07C269/04 ,  C07C67/313

CPC classification number: C07C269/06 ,  C07B2200/07 ,  C07C67/313 ,  C07C67/343 ,  C07C229/30 ,  C07C269/04 ,  C07C271/22 ,  C07C69/738

Abstract: The invention provides new processes for making and purifying amino acid compounds, which are useful in the preparation of AKT inhibitors used in the treatment of diseases such as cancer, 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氨基酸化合物的新方法，其可用于制备用于治疗疾病如癌症的AKT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）丙-1-酮 -一。

公开(公告)号：US09416110B2

公开(公告)日：2016-08-16

申请号：US14401087

申请日：2013-05-17

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: C07D239/02 ,  C07D239/42 ,  C07D239/30 ,  C07D403/04 ,  C07D239/70

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: 本发明提供制备式I化合物及其盐的方法，其中R 1在本文中定义，以及所述式的化合物和中间体。

公开(公告)号：US09315471B2

公开(公告)日：2016-04-19

申请号：US14401089

申请日：2013-05-17

Applicant: Genentech, Inc.

Inventor： Srinivasan Babu ,  Francis Gosselin ,  Yingqing Ran ,  Travis Remarchuk ,  Scott J. Savage ,  Jeffrey Stults ,  Herbert Yajima

IPC: C07D239/70 ,  C07D403/04 ,  C12P17/16

CPC classification number: C07D239/70 ,  C07D403/04 ,  C12P17/165

Abstract: The invention provides new processes for making and purifying salts of hydroxylated cyclopentapyrimidine compounds, which are useful as AKT inhibitors used in the treatment of diseases such as cancer, including the monohydrochloride salt of (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并嘧啶化合物的盐的新方法，其可用作用于治疗诸如癌症的疾病的AKT抑制剂，包括（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-one。

公开(公告)号：US09309204B2

公开(公告)日：2016-04-12

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: C07D403/04 ,  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：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：US20170247337A1

公开(公告)日：2017-08-31

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: 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.

公开(公告)号：US20160222027A1

公开(公告)日：2016-08-04

申请号：US14991658

申请日：2016-01-08

Applicant: Genentech, Inc.

Inventor： Jeffrey Stults ,  Travis Remarchuk ,  Frederic St-Jean

IPC: C07D498/04

CPC classification number: C07D498/04 ,  A61K31/553 ,  A61K45/06 ,  C07B2200/13 ,  C07D498/06

Abstract: The present invention relates to crystalline polymorphs of (2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide (GDC-0032, taselisib), methods of use, and processes of preparing thereof.