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1.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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公开(公告)号：US09321761B2
公开(公告)日：2016-04-26
申请号：US14575018
申请日：2014-12-18
Applicant: GENENTECH, INC. , CURIS, INC.
Inventor： Janet L. Gunzner-Toste , Daniel Sutherlin , Mark S. Stanley , Liang Bao , Georgette M. Castanedo , Rebecca L. LaLonde , Shumei Wang , Mark E. Reynolds , Scott J. Savage , Kimberly Malesky , Michael S. Dina , Michael F. T. Koehler
IPC: C07D413/12 , C07D417/04 , C07D417/12 , C07D213/38 , C07D213/40 , C07D213/56 , C07D213/70 , C07D213/75 , C07D213/81 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07F9/58
CPC classification number: C07D213/16 , C07D213/38 , C07D213/40 , C07D213/56 , C07D213/70 , C07D213/75 , C07D213/81 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07F9/58
Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
Abstract translation: 本发明提供了可用作治疗恶性肿瘤的治疗剂的刺猬蛋白信号传导的新型抑制剂，其中化合物具有通式I：其中A，X，Y R1，R2，R3，R4，m和n如本文所述。
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3.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：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
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：US09790183B2
公开(公告)日：2017-10-17
申请号：US15015586
申请日：2016-02-04
Applicant: GENENTECH, INC. , CURIS, INC.
Inventor： Janet L. Gunzner-Toste , Daniel Sutherlin , Mark S. Stanley , Liang Bao , Georgette M. Castanedo , Rebecca L. Lalonde , Shumei Wang , Mark E. Reynolds , Scott J. Savage , Kimberly Malesky , Michael S. Dina , Michael F. T. Koehler
IPC: C07D213/16 , C07D401/12 , A61K31/44 , C07D213/38 , C07D213/40 , C07D213/56 , C07D213/70 , C07D213/75 , C07D213/81 , C07D213/82 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07F9/58
CPC classification number: C07D213/16 , C07D213/38 , C07D213/40 , C07D213/56 , C07D213/70 , C07D213/75 , C07D213/81 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07F9/58
Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
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8.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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9.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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10.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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