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1.发明授权Crystalline and mesomorphous forms of an AKT inhibiting pyrimidinyl-cyclopentane compound, compositions and methods thereof 有权AKT抑制嘧啶基 - 环戊烷化合物的结晶和介晶形式，其组合物和方法公开(公告)号：US09505725B2
公开(公告)日：2016-11-29
申请号：US15018636
申请日：2016-02-08
Applicant: Genentech, Inc.
Inventor： Paroma Chakravarty , Sanjeev Kothari , Francis Gosselin , Scott J. Savage , Jeffrey Stults
IPC: C07D239/70 , A61K31/496 , C07D403/04 , A61K31/517
CPC classification number: C07D239/70 , A61K31/517 , C07D403/04
Abstract: Disclosed is (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 monohydrochloride, forms, formulations, pharmaceutical compositions, processes of manufacturing and methods of use thereof.
Abstract translation: 公开了（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] 哌啶-1-基）-3-（异丙基氨基）丙-1-酮单盐酸盐，形式，制剂，药物组合物，制备方法及其使用方法。
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![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, methods of production, and pharmaceutical uses thereof](/abs-image/US/2016/11/01/US09481690B2/abs.jpg.150x150.jpg)
2.发明授权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, methods of production, and pharmaceutical uses thereof 有权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，其制备方法及其药学用途公开(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。
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公开(公告)号：US20160152575A1
公开(公告)日：2016-06-02
申请号：US15018636
申请日：2016-02-08
Applicant: Genentech, Inc.
Inventor： Paroma Chakravarty , Sanjeev Kothari , Francis Gosselin , Scott J. Savage , Jeffrey Stults
IPC: C07D239/70
CPC classification number: C07D239/70 , A61K31/517 , C07D403/04
Abstract: Disclosed is (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 monohydrochloride, forms, formulations, pharmaceutical compositions, processes of manufacturing and methods of use thereof.
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公开(公告)号：US11066389B2
公开(公告)日：2021-07-20
申请号：US16718602
申请日：2019-12-18
Applicant: Genentech, Inc.
Inventor： Jinguang Lin , Alexandra Chestakova , Wei Gu , Hans Iding , Jing Li , Xin Linghu , Patrik Meier , Chunbo Sha , Jeffrey Stults , Youchu Wang , Haiming Zhang , Jianqian Zhang , Tao Zhang
IPC: C07D401/14 , C07D401/04 , A61P35/00 , A61P25/00 , A61P29/00 , C12P17/16
Abstract: The present invention provides a process for the manufacture of a compound of formula VIIIa and salts forms of VIIIa where Rc is an aryl sulfonic acid
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公开(公告)号：US20180282324A1
公开(公告)日：2018-10-04
申请号：US15806650
申请日：2017-11-08
Applicant: Genentech, Inc. , Array Biopharma Inc.
Inventor： Jeffrey Stults , Christopher M. Lindemann , Keith L. Spencer , Weidong Liu , Joseph Lubach
IPC: C07D471/04 , A61K31/437 , A61K45/06
Abstract: Disclosed are crystalline forms of (R)—N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide, and salts, solvates, and hydrates thereof, and pharmaceutical compositions, formulations and a process of manufacturing thereof.
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Patent Agency Ranking
6.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：US20160251350A1
公开(公告)日：2016-09-01
申请号：US15054611
申请日：2016-02-26
Applicant: Genentech, Inc. , Array Biopharma Inc.
Inventor： Jeffrey Stults , Christopher M. Lindemann , Keith L. Spencer , Weidong Liu , Joseph Lubach
IPC: C07D471/04 , A61K45/06 , A61K31/437
CPC classification number: C07D471/04 , A61K31/437 , A61K45/06
Abstract: Disclosed are crystalline forms of (R)—N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide, and salts, solvates, and hydrates thereof, and pharmaceutical compositions, formulations and a process of manufacturing thereof.
Abstract translation: 公开了（R）-N-（4-（3-氨基哌啶-1-基）-5-溴-1H-吡咯并[2,3-b]吡啶-3-基）环丙烷甲酰胺和盐，溶剂化物的结晶形式 及其水合物，以及药物组合物，制剂及其制造方法。
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![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, METHODS OF PRODUCTION, AND PHARMACEUTICAL USES THEREOF](/abs-image/US/2016/08/04/US20160222027A1/abs.jpg.150x150.jpg)
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.
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![Polymorphs of 2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazole-5-yl)-5,6-dihydrobenzo[F]imidazo [1,2-D][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide, methods of production, and pharmaceutical uses thereof](/abs-image/US/2016/02/23/US09266903B2/abs.jpg.150x150.jpg)
9.发明授权Polymorphs of 2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazole-5-yl)-5,6-dihydrobenzo[F]imidazo [1,2-D][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide, methods of production, and pharmaceutical uses thereof 有权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，其制备方法及其药物用途公开(公告)号：US09266903B2
公开(公告)日：2016-02-23
申请号：US14570019
申请日：2014-12-15
Applicant: Genentech, Inc.
Inventor： Jeffrey Stults
IPC: A61K31/553 , C07D498/06 , A61K45/06 , 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.
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。
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10.发明申请AMORPHOUS FORM OF AN AKT INHIBITING PYRIMIDINYL-CYCLOPENTANE COMPOUND, COMPOSITIONS AND METHODS THEREOF 有权AKT抑制吡咯烷基环丙烷化合物的非晶形式，其组合物及其方法公开(公告)号：US20150274677A1
公开(公告)日：2015-10-01
申请号：US14401092
申请日：2012-05-17
Applicant: Genentech, Inc.
Inventor： Paroma Chakravarty , Sanjeev Kothari , Francis Gosselin , Scott J. Savage , Jeffrey Stults
IPC: C07D239/70
CPC classification number: C07D239/70 , A61K31/517 , C07D403/04
Abstract: Disclosed is (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 monohydrochloride, forms, formulations, pharmaceutical compositions, processes of manufacturing and methods of use thereof.
Abstract translation: 公开了（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] 哌啶-1-基）-3-（异丙基氨基）丙-1-酮单盐酸盐，形式，制剂，药物组合物，制备方法及其使用方法。
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