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

IPC: A61K47/48 ,  A61K38/06 ,  A61K38/08 ,  A61K38/07 ,  C07K7/02 ,  C07K5/083 ,  C07K5/02

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。

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

IPC: A61K47/65 ,  A61K47/64 ,  A61K47/68

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.

公开(公告)号：US20210188991A1

公开(公告)日：2021-06-24

申请号：US17129833

申请日：2020-12-21

Applicant: PFIZER INC.

Inventor： Tracy Chia-Chien KUO ,  Javier Fernando CHAPARRO RIGGERS ,  Wei CHEN ,  Amy Shaw-Ru CHEN ,  Edward Derrick PASCUA ,  Thomas John VAN BLARCOM ,  Leila Marie BOUSTANY ,  Weihsien HO ,  Yik Andy YEUNG ,  Pavel STROP ,  Arvind RAJPAL

IPC: C07K16/28 ,  A61K39/395 ,  A61K31/454 ,  A61K31/704 ,  A61K31/69 ,  A61K47/68

Abstract: The present invention relates bispecific antibodies that specific binds to BCMA (B-Cell Maturation Antigen) and CD3 (Cluster of Differentiation 3). Method of making the bispecific antibodies and method of using the bispecific antibodies for the treatment of multiple myeloma are also provided.

公开(公告)号：US20200377615A1

公开(公告)日：2020-12-03

申请号：US16891460

申请日：2020-06-03

Applicant: Pfizer Inc.

Inventor： Dangshe MA ,  Frank LOGANZO, Jr. ,  Kimberly Ann MARQUETTE ,  Edmund Idris GRAZIANI ,  Puja SAPRA ,  Pavel STROP

IPC: C07K16/32 ,  A61K47/68 ,  C07K16/30

Abstract: The present invention provides site specific HER2 antibody drug conjugates and methods for preparing and using the same.

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

IPC: A61K47/65 ,  A61K47/68 ,  A61K47/64

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.

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

IPC: C07K17/02 ,  C07K16/30

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.

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。

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。