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：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：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.

公开(公告)号：US09303043B2

公开(公告)日：2016-04-05

申请号：US14205634

申请日：2014-03-12

Applicant: Genentech, Inc.

Inventor： Remy Angelaud ,  Danial R. Beaudry ,  Diane E. Carrera ,  Sushant Malhotra ,  Travis Remarchuk ,  Frederic St-Jean

IPC: C07D233/54 ,  C07D249/08 ,  C07D267/14 ,  C07D498/04

CPC classification number: C07D498/04

Abstract: Processes are described for the preparation of PI3K inhibitor, GDC-0032, Formula I, having the structure: and intermediates useful for the preparation of I.

Abstract translation: 描述了制备具有以下结构的PI3K抑制剂GDC-0032，式I的方法：和用于制备I的中间体。

公开(公告)号：US09278917B2

公开(公告)日：2016-03-08

申请号：US14401095

申请日：2013-05-17

Applicant: Genentech, Inc.

Inventor： Travis Remarchuk

IPC: C07C229/30 ,  C07C269/06 ,  C07C271/22 ,  C07C67/343 ,  C07C67/313 ,  C07C269/04

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：US20140275523A1

公开(公告)日：2014-09-18

申请号：US14205634

申请日：2014-03-12

Applicant: Genentech, Inc.

Inventor： Remy Angelaud ,  Danial R. Beaudry ,  Diane E. Carrera ,  Sushant Malhotra ,  Travis Remarchuk ,  Frederic St-Jean

IPC: C07D498/04

CPC classification number: C07D498/04

Abstract: Processes are described for the preparation of PI3K inhibitor, GDC-0032, Formula I, having the structure: and intermediates useful for the preparation of I.

Abstract translation: 描述了制备具有以下结构的PI3K抑制剂GDC-0032，式I的方法：和用于制备I的中间体。

公开(公告)号：US20150099880A1

公开(公告)日：2015-04-09

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 ,  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。