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![Solid forms of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3- fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol and processes for preparing fused tricyclic compounds comprising a substituted phenyl or pyridinyl moiety, including methods of their use](/abs-image/US/2021/03/23/US10954234B2/abs.jpg.150x150.jpg)
公开(公告)号：US10954234B2
公开(公告)日：2021-03-23
申请号：US16443515
申请日：2019-06-17
Applicant: Genentech, Inc. , Hoffman-La Roche, Inc.
Inventor： Cheol Keun Chung , Jie Xu , Hans Iding , Kyle Clagg , Michael Dalziel , Alec Fettes , Francis Gosselin , Ngiap-Kie Lim , Andrew McClory , Haiming Zhang , Paroma Chakravarty , Karthik Nagapudi , Sarah Robinson
IPC: C07D471/04 , C07D403/14 , A61P35/00 , A61P35/04
Abstract: Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.
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2.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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3.发明授权Amorphous form of an AKT inhibiting pyrimidinyl-cyclopentane compound, compositions and methods thereof 有权AKT抑制嘧啶基 - 环戊烷化合物的无定形形式，其组合物和方法公开(公告)号：US09290458B2
公开(公告)日：2016-03-22
申请号：US14401092
申请日：2013-05-17
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 and solid forms of (s)-2-((2-((s)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide, and methods of production](/abs-image/US/2021/06/08/US11028100B2/abs.jpg.150x150.jpg)
公开(公告)号：US11028100B2
公开(公告)日：2021-06-08
申请号：US16875537
申请日：2020-05-15
Applicant: Genentech, Inc.
Inventor： Paroma Chakravarty , Chong Han , Sean M. Kelly , Karthik Nagapudi , Scott Savage
IPC: C07D498/04 , A61P35/00 , A61P35/02 , A61P35/04 , A61K9/20
Abstract: The present invention relates to crystalline polymorph forms of (S)-2-((2-((S)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide (GDC-0077), having the structure, Formula I: or stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, and processes of preparing the polymorph forms.
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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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Patent Agency Ranking
![Solid forms of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3- yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol and processes for preparing fused tricyclic compounds comprising a substituted phenyl or pyridinyl moiety, including methods of their use](/abs-image/US/2023/10/10/US11780834B2/abs.jpg.150x150.jpg)
公开(公告)号：US11780834B2
公开(公告)日：2023-10-10
申请号：US17110607
申请日：2020-12-03
Applicant: Hoffmann-La Roche Inc. , GENENTECH, INC.
Inventor： Cheol Keun Chung , Jie Xu , Hans Iding , Kyle Clagg , Michael Dalziel , Alec Fettes , Francis Gosselin , Ngiap-Kie Lim , Andrew McClory , Haiming Zhang , Paroma Chakravarty , Karthik Nagapudi , Sarah Robinson
IPC: C07D471/04 , C07D403/14
CPC classification number: C07D471/04 , C07D403/14 , C07B2200/13
Abstract: Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.
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7.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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![POLYMORPHS AND SOLID FORMS OF (S)-2-((2-((S)-4-(DIFLUOROMETHYL)-2-OXOOXAZOLIDIN-3-YL)-5,6-DIHYDROBENZO[F]IMIDAZO[1,2-D][1,4]OXAZEPIN-9-YL)AMINO)PROPANAMIDE, AND METHODS OF PRODUCTION](/abs-image/US/2023/06/01/US20230167128A1/abs.jpg.150x150.jpg)
公开(公告)号：US20230167128A1
公开(公告)日：2023-06-01
申请号：US18101951
申请日：2023-01-26
Applicant: Genentech, Inc.
Inventor： Paroma Chakravarty , Chong Han , Sean M. Kelly , Karthik Nagapudi , Scott Savage
IPC: C07D498/04 , A61P35/00 , A61P35/02 , A61P35/04
CPC classification number: C07D498/04 , A61P35/00 , A61P35/02 , A61P35/04 , A61K9/20
Abstract: The present invention relates to crystalline polymorph forms of (S)-2-((2-((S)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[ƒ]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide (GDC-0077), having the structure, Formula I:
or stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, and processes of preparing the polymorph forms.-
![Polymorphs and solid forms of (s)-2-((2-((s)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide, and methods of production](/abs-image/US/2023/02/28/US11591345B2/abs.jpg.150x150.jpg)
公开(公告)号：US11591345B2
公开(公告)日：2023-02-28
申请号：US16875545
申请日：2020-05-15
Applicant: Genentech, Inc.
Inventor： Paroma Chakravarty , Chong Han , Sean M. Kelly , Karthik Nagapudi , Scott Savage
IPC: C07D498/04 , A61P35/00 , A61P35/02 , A61P35/04 , A61K9/20
Abstract: The present invention relates to crystalline polymorph forms of (S)-2-((2-((S)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide (GDC-0077), having the structure, Formula I: or stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, and processes of preparing the polymorph forms.
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![POLYMORPHS AND SOLID FORMS OF (S)-2-((2-((S)-4-(DIFLUOROMETHYL)-2-OXOOXAZOLIDIN-3-YL)-5,6-DIHYDROBENZO[F]IMIDAZO[1,2-D][1,4]OXAZEPIN-9-YL)AMINO)PROPANAMIDE, AND METHODS OF PRODUCTION](/abs-image/US/2021/04/01/US20210094970A1/abs.jpg.150x150.jpg)
公开(公告)号：US20210094970A1
公开(公告)日：2021-04-01
申请号：US16875545
申请日：2020-05-15
Applicant: Genentech, Inc.
Inventor： Paroma Chakravarty , Chong Han , Sean M. Kelly , Karthik Nagapudi , Scott Savage
IPC: C07D498/04 , A61P35/00 , A61P35/02 , A61P35/04
Abstract: The present invention relates to crystalline polymorph forms of (S)-2-((2-((S)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide (GDC-0077), having the structure, Formula I: or stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, and processes of preparing the polymorph forms.
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