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公开(公告)号：US20210115159A1
公开(公告)日：2021-04-22
申请号：US16951003
申请日：2020-11-18
Applicant: PFIZER INC. , RINAT NEUROSCIENCE CORP.
Inventor： Pavel STROP , Magdalena Grazyna DORYWALSKA , Arvind RAJPAL , David SHELTON , Shu-Hui LIU , Jaume PONS , Russell DUSHIN
Abstract: The present invention provides engineered polypeptide conjugates (e.g., antibody-drug-conjugates, toxin-(biocompatible polymer) conjugates, antibody-(biocompatible polymer) conjugates, and bispecific antibodies) comprising acyl donor glutamine-containing tags and amine donor agents. In one aspect, the invention provides an engineered Fc-containing polypeptide conjugate comprising the formula (Fc-containing polypeptide)-T-A, wherein T is an acyl donor glutamine-containing tag engineered at a specific site or comprises an endogenous glutamine made reactive by the Fc-containing polypeptide engineering, wherein A is an amine donor agent, and wherein the amine donor agent is site-specifically conjugated to the acyl donor glutamine-containing tag or the endogenous glutamine. The invention also provides methods of making engineered polypeptide conjugates using transglutaminase.
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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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5.发明申请公开(公告)号：US20170313787A1
公开(公告)日：2017-11-02
申请号：US15593259
申请日：2017-05-11
Applicant: PFIZER INC. , RINAT NEUROSCIENCE CORP.
Inventor： Pavel STROP , Magdalena Grazyna DORYWALSKA , Arvind RAJPAL , David SHELTON , Shu-Hui LIU , Jaume PONS , Russell DUSHIN
CPC classification number: C07K17/02 , A61K47/68 , A61K47/6803 , A61K47/6851 , A61K47/6889 , C07K16/30 , C07K2317/31 , C07K2317/73
Abstract: The present invention provides engineered polypeptide conjugates (e.g., antibody-drug-conjugates, toxin-(biocompatible polymer) conjugates, antibody-(biocompatible polymer) conjugates, and bispecific antibodies) comprising acyl donor glutamine-containing tags and amine donor agents. In one aspect, the invention provides an engineered Fc-containing polypeptide conjugate comprising the formula (Fc-containing polypeptide)-T-A, wherein T is an acyl donor glutamine-containing tag engineered at a specific site or comprises an endogenous glutamine made reactive by the Fc-containing polypeptide engineering, wherein A is an amine donor agent, and wherein the amine donor agent is site-specifically conjugated to the acyl donor glutamine-containing tag or the endogenous glutamine. The invention also provides methods of making engineered polypeptide conjugates using transglutaminase.
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Patent Agency Ranking
公开(公告)号：US20160096898A1
公开(公告)日：2016-04-07
申请号：US14864750
申请日：2015-09-24
Applicant: RINAT NEUROSCIENCE CORP. , Pfizer Inc.
Inventor： Hong LIANG , Yasmina Noubia ABDICHE , Javier Fernando CHAPARRO RIGGERS , Bruce Charles GOMES , Julie Jia Li HAWKINS , Jaume PONS , Xiayang QIU , Pavel STROP , Yuli WANG
IPC: C07K16/40
CPC classification number: C07K16/40 , A61K39/3955 , A61K45/06 , A61K2039/505 , C07K2299/00 , C07K2317/24 , C07K2317/33 , C07K2317/76 , C07K2317/92
Abstract: The present invention provides antagonizing antibodies, antigen-binding portions thereof, and aptamers that bind to proprotein convertase subtilisin kexin type 9 (PCSK9). Also provided are antibodies directed to peptides, in which the antibodies bind to PCSK9. The invention further provides a method of obtaining such antibodies and antibody-encoding nucleic acid. The invention further relates to therapeutic methods for use of these antibodies and antigen-binding portions thereof to reduce LDL-cholesterol levels and/or for the treatment and/or prevention of cardiovascular disease, including treatment of hypercholesterolemia.
Abstract translation: 本发明提供了与抗蛋白转化酶枯草杆菌蛋白酶Kexin 9型（PCSK9）结合的拮抗抗体，其抗原结合部分和适体。 还提供了针对肽的抗体，其中抗体结合PCSK9。 本发明还提供了获得这样的抗体和抗体编码核酸的方法。 本发明还涉及使用这些抗体及其抗原结合部分来降低LDL-胆固醇水平和/或用于治疗和/或预防心血管疾病（包括治疗高胆固醇血症）的治疗方法。
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公开(公告)号：US20130273069A1
公开(公告)日：2013-10-17
申请号：US13857063
申请日：2013-04-04
Applicant: Pfizer Inc. , Rinat Neuroscience Corp.
Inventor： Hong LIANG , Yasmina Noubia ABDICHE , Javier Fernando CHAPARRO RIGGERS , Bruce Charles GOMES , Julie Jia Li HAWKINS , Jaume PONS , Xiayang QIU , Pavel STROP , Yuli WANG
IPC: C07K16/40 , A61K45/06 , A61K39/395
CPC classification number: C07K16/40 , A61K39/3955 , A61K45/06 , A61K2039/505 , C07K2299/00 , C07K2317/24 , C07K2317/33 , C07K2317/76 , C07K2317/92
Abstract: The present invention provides antagonizing antibodies, antigen-binding portions thereof, and aptamers that bind to proprotein convertase subtilisin kexin type 9 (PCSK9). Also provided are antibodies directed to peptides, in which the antibodies bind to PCSK9. The invention further provides a method of obtaining such antibodies and antibody-encoding nucleic acid. The invention further relates to therapeutic methods for use of these antibodies and antigen-binding portions thereof to reduce LDL-cholesterol levels and/or for the treatment and/or prevention of cardiovascular disease, including treatment of hypercholesterolemia.
Abstract translation: 本发明提供了与抗蛋白转化酶枯草杆菌蛋白酶Kexin 9型（PCSK9）结合的拮抗抗体，其抗原结合部分和适体。 还提供了针对肽的抗体，其中抗体结合PCSK9。 本发明还提供了获得这样的抗体和抗体编码核酸的方法。 本发明还涉及使用这些抗体及其抗原结合部分来降低LDL-胆固醇水平和/或用于治疗和/或预防心血管疾病（包括治疗高胆固醇血症）的治疗方法。
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公开(公告)号：US20240009319A1
公开(公告)日：2024-01-11
申请号：US18347280
申请日：2023-07-05
Applicant: RINAT NEUROSCIENCE CORP.
Inventor： Santiago Esteban FARIAS , Meritxell GALINDO CASAS , Pavel STROP
IPC: A61K47/68
CPC classification number: A61K47/6803 , A61K47/68 , A61K47/6817 , A61K47/6809 , A61K47/6805
Abstract: The present invention provides engineered polypeptide conjugates (e.g., antibody-drug-conjugates) comprising specific acyl donor glutamine-containing tags and amine donor agents. The invention also provides methods of making such engineered polypeptide conjugates using transglutaminase and methods of using thereof.
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公开(公告)号：US20160193356A1
公开(公告)日：2016-07-07
申请号：US14908492
申请日：2014-07-30
Applicant: RINAT NEUROSCIENCE CORP.
Inventor： Santiago Esteban FARIAS , Meritxell GALINDO CASAS , Pavel STROP
IPC: A61K47/48
CPC classification number: A61K47/6803 , A61K47/68 , A61K47/6805 , A61K47/6809 , A61K47/6817
Abstract: The present invention provides engineered polypeptide conjugates (e.g., antibody-drug-conjugates) comprising specific acyl donor glutamine-containing tags and amine donor agents. The invention also provides methods of making such engineered polypeptide conjugates using transglutaminase and methods of using thereof.
Abstract translation: 本发明提供包含特定酰基供体谷氨酰胺标签和胺供体试剂的工程改造的多肽缀合物（例如抗体 - 药物偶联物）。 本发明还提供了使用转谷氨酰胺酶制备这种工程化多肽缀合物的方法及其使用方法。
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公开(公告)号：US20210162058A1
公开(公告)日：2021-06-03
申请号：US17069969
申请日：2020-10-14
Applicant: RINAT NEUROSCIENCE CORP.
Inventor： Santiago Esteban FARIAS , Meritxell GALINDO CASAS , Pavel STROP
IPC: A61K47/68
Abstract: The present invention provides engineered polypeptide conjugates (e.g., antibody-drug-conjugates) comprising specific acyl donor glutamine-containing tags and amine donor agents. The invention also provides methods of making such engineered polypeptide conjugates using transglutaminase and methods of using thereof.
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