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1.发明授权Process of making hydroxylated cyclopentapyrimidine compounds and salts thereof 有权制备羟基化环戊并嘧啶化合物及其盐的方法公开(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。
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公开(公告)号：US08431694B1
公开(公告)日：2013-04-30
申请号：US13712114
申请日：2012-12-12
Applicant: Genentech, Inc.
Inventor： Srinivasan Babu , Zhigang Cheng , Mark E. Reynolds , Scott J. Savage , Qingping Tian , Herbert Yajima
IPC: C07D413/14
CPC classification number: C07D513/04 , C07D405/04 , C07D495/04 , C07F5/025
Abstract: The invention provides processes of preparing, separating, and purifying PI3K inhibitor, Formula I and II compounds, and novel intermediates for preparing Formula I and II compounds.
Abstract translation: 本发明提供制备，分离和纯化PI3K抑制剂，式I和II化合物的方法，以及制备式I和II化合物的新型中间体。
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公开(公告)号：US20160311817A1
公开(公告)日：2016-10-27
申请号：US15202911
申请日：2016-07-06
Applicant: Genentech, Inc.
Inventor： Benjamin Fauber , Olivier Rene , Sushant Malhotra , Herbert Yajima
IPC: C07D417/14 , C07D417/04
CPC classification number: C07D417/14 , C07D417/04 , C07D417/10
Abstract: Compounds of the formula I or a pharmaceutical salt thereof, wherein m, n, q, r, A, W, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
Abstract translation: 或其药物盐，其中m，n，q，r，A，W，X1，X2，X3，X4，Y，Z，R1，R2，R3，R4，R5，R6，R7，R8，R9，R10 和R 11如本文所定义。 还公开了制备化合物和使用该化合物治疗炎性疾病如关节炎的方法。
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4.发明申请PROCESS OF MAKING HYDROXYLATED CYCLOPENTAPYRIMIDINE COMPOUNDS AND SALTS THEREOF 有权制备羟肟酸环己基嘧啶化合物及其制备方法公开(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。
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5.发明公开公开(公告)号：US20230242550A1
公开(公告)日：2023-08-03
申请号：US18189623
申请日：2023-03-24
Applicant: Genentech, Inc.
Inventor： Andreas Stumpf , Remy Angelaud , Andrew McClory , Herbert Yajima , Chudi Ndubaku , Alan Olivero
IPC: C07D498/14 , C07D487/04 , C07D498/22 , A61P35/00 , A61K9/00 , A61K31/495 , A61K31/5383 , A61K39/395 , A61K45/06
CPC classification number: C07D498/14 , C07D487/04 , C07D498/22 , A61P35/00 , A61K9/0053 , A61K31/495 , A61K31/5383 , A61K39/3955 , A61K45/06
Abstract: The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.
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Patent Agency Ranking
6.发明申请公开(公告)号：US20180354970A1
公开(公告)日：2018-12-13
申请号：US15780328
申请日：2016-12-16
Applicant: GENENTECH, INC.
Inventor： Andreas Stumpf , Remy Angelaud , Andrew McClory , Herbert Yajima , Chudi Ndubaku , Alan Olivero
IPC: C07D498/14 , A61P35/00 , A61K9/00 , A61K45/06 , A61K39/395 , A61K31/495 , A61K31/5383
CPC classification number: C07D498/14 , A61K9/0053 , A61K31/495 , A61K31/5383 , A61K39/3955 , A61K45/06 , A61P35/00 , C07D487/04 , C07D498/22
Abstract: The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.
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公开(公告)号：US20130109852A1
公开(公告)日：2013-05-02
申请号：US13712114
申请日：2012-12-12
Applicant: Genentech, Inc.
Inventor： Srinivasan Babu , Zhigang Cheng , Mark E. Reynolds , Scott J. Savage , Qingping Tian , Herbert Yajima
IPC: C07D513/04
CPC classification number: C07D513/04 , C07D405/04 , C07D495/04 , C07F5/025
Abstract: The invention provides processes of preparing, separating, and purifying PI3K inhibitor, Formula I and II compounds, and novel intermediates for preparing Formula I and II compounds.
Abstract translation: 本发明提供制备，分离和纯化PI3K抑制剂，式I和II化合物的方法，以及制备式I和II化合物的新型中间体。
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公开(公告)号：US11643421B2
公开(公告)日：2023-05-09
申请号：US17115095
申请日：2020-12-08
Applicant: Genentech, Inc.
Inventor： Andreas Stumpf , Remy Angelaud , Andrew McClory , Herbert Yajima , Chudi Ndubaku , Alan Olivero
IPC: C07D498/14 , C07D487/04 , C07D498/22 , A61P35/00 , A61K9/00 , A61K31/495 , A61K31/5383 , A61K39/395 , A61K45/06
CPC classification number: C07D498/14 , A61K9/0053 , A61K31/495 , A61K31/5383 , A61K39/3955 , A61K45/06 , A61P35/00 , C07D487/04 , C07D498/22
Abstract: The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.
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公开(公告)号：US20210253599A1
公开(公告)日：2021-08-19
申请号：US17115095
申请日：2020-12-08
Applicant: Genentech, Inc.
Inventor： Andreas Stumpf , Remy Angelaud , Andrew McClory , Herbert Yajima , Chudi Ndubaku , Alan Olivero
IPC: C07D498/14 , C07D487/04 , C07D498/22 , A61P35/00 , A61K9/00 , A61K31/495 , A61K31/5383 , A61K39/395 , A61K45/06
Abstract: The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.
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公开(公告)号：US10906918B2
公开(公告)日：2021-02-02
申请号：US15780328
申请日：2016-12-16
Applicant: GENENTECH, INC.
Inventor： Andreas Stumpf , Remy Angelaud , Andrew McClory , Herbert Yajima , Chudi Ndubaku , Alan Olivero
IPC: C07D498/14 , C07D487/04 , C07D498/22 , A61P35/00 , A61K9/00 , A61K31/495 , A61K31/5383 , A61K39/395 , A61K45/06
Abstract: The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.
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