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11.发明授权公开(公告)号：US09695240B2
公开(公告)日：2017-07-04
申请号：US14528142
申请日：2014-10-30
Applicant: Genentech, Inc.
Inventor： Italo Beria , Michele Caruso , John A. Flygare , Vittoria Lupi , Rita Perego , Paul Polakis , Andrew Polson , Matteo Salsa , Susan D. Spencer , Barbara Valsasina , Robert L. Cohen
CPC classification number: C07K16/2863 , A61K47/64 , A61K47/6809 , C07K2317/76
Abstract: The present invention relates to conjugates of therapeutically useful anthracyclines with carriers such as polyclonal and monoclonal antibodies, proteins or peptides of natural or synthetic origin; methods for their preparation, pharmaceutical composition containing them and use thereof in treating certain mammalian tumors.
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12.发明申请公开(公告)号：US20160074528A1
公开(公告)日：2016-03-17
申请号：US14851206
申请日：2015-09-11
Applicant: GENENTECH, INC.
Inventor： John A. Flygare , Thomas H. Pillow
IPC: A61K47/48 , A61K31/704
CPC classification number: A61K31/704 , A61K47/6809 , A61K47/6849 , A61K47/6855
Abstract: The invention provides antibody-drug conjugates comprising an antibody conjugated to an anthracycline drug moiety via a disulfide linker, anthracycline disulfide intermediates, and methods of using the antibody-drug conjugates.
Abstract translation: 本发明提供抗体 - 药物偶联物，其包含通过二硫键接头与蒽环类药物部分缀合的抗体，蒽环类二硫化物中间体以及使用抗体 - 药物偶联物的方法。
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公开(公告)号：US10556895B2
公开(公告)日：2020-02-11
申请号：US15583492
申请日：2017-05-01
Applicant: Genentech, Inc.
Inventor： John A. Flygare , Thomas Pillow , Leanna Staben
IPC: C07D417/14 , C07D403/14 , C07D403/12 , C07D471/02
Abstract: This invention relates to quaternary amine linkers and anti-body drug conjugates thereof, to pharmaceutical compositions containing them, and to their use in therapy for the prevention or treatment of cancer.
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公开(公告)号：US20190224269A1
公开(公告)日：2019-07-25
申请号：US16372940
申请日：2019-04-02
Applicant: GENENTECH, INC.
Inventor： Frederick Cohen , Lewis J. Gazzard , Vickie Hsiao-Wei Tsui , John A. Flygare
Abstract: Novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies and have the general formula I: wherein R1,R2,R3,R4,R5 and R6 are as described herein.
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公开(公告)号：US20190083643A1
公开(公告)日：2019-03-21
申请号：US16150623
申请日：2018-10-03
Applicant: Genentech, Inc.
Inventor： Ho Huat Lee , Moana Tercel , John A. Flygare , Janet Gunzner-Toste , Thomas H. Pillow , Brian Safina , Leanna Staben , Vishal Verma , BinQing Wei , Guiling Zhao
Abstract: This invention relates to peptidomimetic linkers and anti-body drug conjugates thereof, to pharmaceutical compositions containing them, and to their use in therapy for the prevention or treatment of cancer.
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Patent Agency Ranking
公开(公告)号：US09586991B2
公开(公告)日：2017-03-07
申请号：US14974140
申请日：2015-12-18
Applicant: GENENTECH, INC.
Inventor： Frederick Cohen , Lewis J. Gazzard , Vickie Hsiao-Wei Tsui , John A. Flygare
CPC classification number: A61K38/06 , A61K38/00 , A61K45/06 , C07K5/08 , C07K5/0804 , C07K5/0806 , C07K5/0812 , C07K5/0815
Abstract: Novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies and have the general formula I: wherein R1, R2, R3, R4, R5 and R6 are as described herein.
Abstract translation: 可用作治疗恶性肿瘤的治疗剂并具有通式I的IAP的新型抑制剂：其中R 1，R 2，R 3，R 4，R 5和R 6如本文所述。
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17.发明申请ANTHRACYCLINE DERIVATIVE CONJUGATES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS ANTITUMOR COMPOUNDS 审中-公开蒽醌衍生物偶联物，其制备方法及其作为抗微生物化合物的用途公开(公告)号：US20150051380A1
公开(公告)日：2015-02-19
申请号：US14528142
申请日：2014-10-30
Applicant: Genentech, Inc.
Inventor： Italo Beria , Michele Caruso , John A. Flygare , Vittoria Lupi , Rita Perego , Paul Polakis , Andrew Polson , Matteo Salsa , Susan D. Spencer , Barbara Valsasina , Robert L. Cohen
CPC classification number: C07K16/2863 , A61K47/64 , A61K47/6809 , C07K2317/76
Abstract: The present invention relates to conjugates of therapeutically useful anthracyclines with carriers such as polyclonal and monoclonal antibodies, proteins or peptides of natural or synthetic origin; methods for their preparation, pharmaceutical composition containing them and use thereof in treating certain mammalian tumors.
Abstract translation: 本发明涉及治疗有用的蒽环类与载体的缀合物，例如天然或合成来源的多克隆和单克隆抗体，蛋白质或肽; 其制备方法，含有它们的药物组合物及其在治疗某些哺乳动物肿瘤中的用途。
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公开(公告)号：US08716236B2
公开(公告)日：2014-05-06
申请号：US13733244
申请日：2013-01-03
Applicant: Genentech, Inc.
Inventor： Frederick Cohen , Lewis J. Gazzard , Vickie Hsiao-Wei Tsui , John A. Flygare
IPC: A61K38/00 , C07D211/60 , C07D307/14 , C07D307/52 , C07D319/22
CPC classification number: A61K38/06 , A61K38/00 , A61K45/06 , C07K5/08 , C07K5/0804 , C07K5/0806 , C07K5/0812 , C07K5/0815
Abstract: Novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies and have the general formula I: wherein R1, R2, R3, R4, R5 and R6 are as described herein.
Abstract translation: 可用作治疗恶性肿瘤的治疗剂的具有通式I的IAP的新型抑制剂：其中R1，R2，R3，R4，R5和R6如本文所述。
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公开(公告)号：US20130266595A1
公开(公告)日：2013-10-10
申请号：US13650277
申请日：2012-10-12
Applicant: Genentech, Inc. , SPIROGEN DEVELOPMENTS SARL
Inventor： John A. Flygare , Janet L. Gunzner-Toste , Thomas Pillow , Philip Wilson Howard , Luke Masterson
IPC: A61K47/48
CPC classification number: A61K47/6803 , A61K47/6849 , C07D487/04 , C07D519/00
Abstract: A conjugate of formula (A): where Y is selected from a single bond, and a group of formulae A1 or A2: where N shows where the group binds to the N10 of the PBD moiety; RL1 and RL2 are independently selected from H and methyl, or together with the carbon atom to which they are bound form a cyclopropylene group; CBA represents a cell binding agent; Q is independently selected from O, S and NH; R11 is either H, or R or, where Q is O, SO3M, where M is a metal cation.
Abstract translation: 式（A）的缀合物：其中Y选自单键，并且具有式A1或A2的基团：其中N表示该基团与PBD部分的N10结合的位置; RL1和RL2独立地选自H和甲基，或与它们所结合的碳原子一起形成环亚丙基; CBA代表细胞结合剂; Q独立地选自O，S和NH; R 11是H或R，或其中Q是O，SO 3 M，其中M是金属阳离子。
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公开(公告)号：US11104673B2
公开(公告)日：2021-08-31
申请号：US16697706
申请日：2019-11-27
Applicant: Genentech, Inc.
Inventor： John A. Flygare , Thomas Pillow , Leanna Staben
IPC: A61K39/00 , C07D417/14 , C07D403/14 , C07D403/12 , C07D471/02 , A61K47/68
Abstract: This invention relates to quaternary amine linkers and anti-body drug conjugates thereof, to pharmaceutical compositions containing them, and to their use in therapy for the prevention or treatment of cancer.
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