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公开(公告)号：US20130129753A1
公开(公告)日：2013-05-23
申请号：US13670612
申请日：2012-11-07
Applicant: PFIZER INC.
Inventor： Matthew David DOROSKI , Andreas MADERNA , Christopher John O'DONNELL , Chakrapani SUBRAMANYAM , Beth VETELINO , Russell George DUSHIN , Pavel STROP , Edmund Idris GRAZIANI
CPC classification number: C07K7/06 , A61K38/06 , A61K38/07 , A61K38/08 , A61K47/6803 , A61K47/6811 , A61K47/6851 , A61K47/6855 , A61K47/6863 , A61K47/6889 , C07K5/0205 , C07K5/0808 , C07K7/02 , C07K16/00 , C07K2319/30
Abstract: The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.
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公开(公告)号：US20210308276A1
公开(公告)日：2021-10-07
申请号：US16321695
申请日：2017-07-31
Applicant: PFIZER INC.
Inventor： Russell George DUSHIN , Daniel P. UCCELLO , Jeremy STARR , Ye CHE , Mark FLANAGAN , Jeffrey M. CASAVANT , Christopher John O'DONNELL , Gary Frederick FILZEN , Jennifer YOUNG , Joseph A. ABRAMITE , Lawrence N. TUMEY , Ludivine MOINE , Adam Matthew GILBERT , Lee R. ROBERTS
IPC: A61K47/68
Abstract: The present invention is directed to novel heteroaryl sulfone-based conjugation handles of the formula: (wherein R1, R2, Het, D, E, X, Y, Z, m, n, p, q, r, s and t are as defined herein), methods for their preparation, their use in synthesizing antibody drig conjugates, and the resulting antibody drig conjugates made with components having heteroaryl sulfone-based conjugation handles.
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Patent Agency Ranking
公开(公告)号：US20170043033A1
公开(公告)日：2017-02-16
申请号：US15306481
申请日：2015-04-21
Applicant: Rinat Neuroscience Corp. , Pfizer Inc.
Inventor： Pavel STROP , Katherine Anne DELARIA , Magdalena DORYWALSKA , Davide Luciano FOLETTI , Russell George DUSHIN , David Louis SHELTON , Arvind RAJPAL
IPC: A61K47/48 , G01N33/574 , C07K16/30 , A61K31/427
CPC classification number: A61K31/427 , A61K47/65 , A61K47/6803 , A61K47/6849 , A61K47/6851 , A61K47/6889 , A61K2039/505 , C07K16/3076 , G01N33/57492 , G01N2333/705
Abstract: The present invention provides transglutaminase-mediated antibody-drug conjugates with high anti-body-drug ratio (DAR) comprising 1) glutamine-containing tags, endogenous glutamines, and/or endogenous glutamines made reactive by antibody engineering or an engineered transglutaminase (e.g., with altered substrate specifity); and 2) amine donor agents comprising amine donor units, linkers, and agent moieties, wherein the DAR is at least about 5. The invention also provides methods of making and methods of using such higher drug loaded antibody-drug conjugates.
Abstract translation: 本发明提供了具有高抗体药物比例（DAR）的转谷氨酰胺酶介导的抗体 - 药物偶联物，其包含1）含有抗体工程或工程化转谷氨酰胺酶（例如，谷氨酰胺）的反应产生的含谷氨酰胺的标签，内源性谷氨酰胺和/或内源性谷氨酰胺， 改变底物特异性）; 和2）包含胺供体单元，接头和试剂部分的胺供体试剂，其中DAR为至少约5.本发明还提供了制备方法和使用这种高加载药物的抗体 - 药物共轭物的方法。
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公开(公告)号：US20210205463A1
公开(公告)日：2021-07-08
申请号：US17183265
申请日：2021-02-23
Applicant: PFIZER INC. , RINAT NEUROSCIENCE CORP.
Inventor： Russell George DUSHIN , Pavel STROP , Magdalena Grazyna DORYWALSKA , Ludivine MOINE
Abstract: The present invention provides stability-modulated antibody-drug conjugates, stability-modulating linker components used to make these stability-modulated antibody-drug conjugates, therapeutic methods using stability-modulated antibody-drug conjugates, and methods of making stability modulating linkers and stability-modulated antibody-drug conjugates.
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公开(公告)号：US20180140714A1
公开(公告)日：2018-05-24
申请号：US15504801
申请日：2015-08-14
Applicant: PFIZER INC. , RINAT NEUROSCIENCE CORP.
Inventor： Russell George DUSHIN , Pavel STROP , Magdalena Grazyna DORYWALSKA , Ludivine MOINE
CPC classification number: A61K47/65 , A61K47/64 , A61K47/6803 , A61K2039/505 , C07K2317/94 , C07K2319/01 , C07K2319/35
Abstract: The present invention provides stability-modulated antibody-drug conjugates, stability-modulating linker components used to make these stability-modulated antibody-drug conjugates, therapeutic methods using stability-modulated antibody-drug conjugates, and methods of making stability modulating linkers and stability-modulated antibody-drug conjugates.
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公开(公告)号：US20150307551A1
公开(公告)日：2015-10-29
申请号：US14793942
申请日：2015-07-08
Applicant: PFIZER INC.
Inventor： Matthew David DOROSKI , Andreas MADERNA , Christopher John O'DONNELL , Chakrapani SUBRAMANYAM , Beth VETELINO , Russell George DUSHIN , Pavel STROP , Edmund Idris GRAZIANI
IPC: C07K7/06
CPC classification number: C07K7/06 , A61K38/06 , A61K38/07 , A61K38/08 , A61K47/6803 , A61K47/6811 , A61K47/6851 , A61K47/6855 , A61K47/6863 , A61K47/6889 , C07K5/0205 , C07K5/0808 , C07K7/02 , C07K16/00 , C07K2319/30
Abstract: The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.
Abstract translation: 本发明涉及细胞毒性五肽，其抗体药物偶联物及其用于治疗癌症的方法。
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公开(公告)号：US20140363452A1
公开(公告)日：2014-12-11
申请号：US14322262
申请日：2014-07-02
Applicant: PFIZER INC.
Inventor： Matthew David DOROSKI , Andreas MADERNA , Christopher John O'DONNELL , Chakrapani SUBRAMANYAM , Beth VETELINO , Russell George DUSHIN , Pavel STROP , Edmund Idris GRAZIANI
CPC classification number: C07K7/06 , A61K38/06 , A61K38/07 , A61K38/08 , A61K47/6803 , A61K47/6811 , A61K47/6851 , A61K47/6855 , A61K47/6863 , A61K47/6889 , C07K5/0205 , C07K5/0808 , C07K7/02 , C07K16/00 , C07K2319/30
Abstract: The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.
Abstract translation: 本发明涉及细胞毒性五肽，其抗体药物偶联物及其用于治疗癌症的方法。
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