CN102083461B - 有效的偶联物和亲水性连接体 - Google Patents

有效的偶联物和亲水性连接体 Download PDF

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Publication number
CN102083461B
CN102083461B CN200980125295.2A CN200980125295A CN102083461B CN 102083461 B CN102083461 B CN 102083461B CN 200980125295 A CN200980125295 A CN 200980125295A CN 102083461 B CN102083461 B CN 102083461B
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cell
antibody
conjugate
binding agent
cancer
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CN102083461A (zh
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R·辛格
Y·科夫通
S·D·威廉
R·V·J·查里
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Immunogen Inc
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Immunogen Inc
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    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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Families Citing this family (185)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7276497B2 (en) * 2003-05-20 2007-10-02 Immunogen Inc. Cytotoxic agents comprising new maytansinoids
JP5149620B2 (ja) 2004-07-23 2013-02-20 エンドサイト,インコーポレイテッド 2価リンカーおよびその結合体
EP3539572A1 (en) 2005-08-24 2019-09-18 ImmunoGen, Inc. Process for preparing maytansinoid antibody conjugates
CN104127878A (zh) 2007-03-14 2014-11-05 恩多塞特公司 结合配体连接的微管溶素递药缀合物
BRPI0809435A2 (pt) 2007-03-27 2014-09-09 Sea Lane Biotechnologies, Llc Constructos e bibliotecas que compreendem sequências de cadeia leve substituida de anticorpos
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
BRPI0812970A2 (pt) 2007-06-25 2019-09-24 Endocyte Inc conjugados contendo espaçadores hidrofílicos
EP2276506A4 (en) 2008-04-30 2014-05-07 Immunogen Inc EFFICIENT CONJUGATES AND HYDROPHILIC BINDER
KR20200058590A (ko) 2008-04-30 2020-05-27 이뮤노젠 아이엔씨 가교제 및 그 용도
CN102482345A (zh) 2009-05-13 2012-05-30 航道生物技术有限责任公司 针对流感病毒的中和分子
AU2015201534B2 (en) * 2009-06-03 2016-11-24 Immunogen, Inc. Conjugation methods
BRPI1010620B8 (pt) * 2009-06-03 2021-05-25 Immunogen Inc métodos de conjugação
FR2947269B1 (fr) 2009-06-29 2013-01-18 Sanofi Aventis Nouveaux composes anticancereux
FR2949469A1 (fr) * 2009-08-25 2011-03-04 Sanofi Aventis Derives anticancereux, leur preparation et leur application en therapeutique
CA2809819A1 (en) * 2009-09-09 2011-03-17 Centrose, Llc Extracellular targeted drug conjugates
AR078471A1 (es) * 2009-10-02 2011-11-09 Sanofi Aventis COMPUESTOS MAITANSINOIDES Y EL USO DE ESTOS PARA PREPARAR CONJUGADOS CON UN ANTICUERPO LOS CUALES SE UTILIZAN COMO AGENTES ANTICANCERIGENOS Y EL PROCEDIMIENTO DE PREPARACIoN DE ESTOS CONJUGADOS
EP2486023A4 (en) * 2009-10-06 2014-05-07 Immunogen Inc EFFICIENT CONJUGATES AND HYDROPHILIC BINDER
CN103037900B (zh) 2010-02-24 2016-04-06 伊缪诺金公司 叶酸受体1抗体与免疫缀合物以及其用途
SG183542A1 (en) 2010-03-12 2012-10-30 Immunogen Inc Cd37-binding molecules and immunoconjugates thereof
FR2963007B1 (fr) 2010-07-26 2013-04-05 Sanofi Aventis Derives anticancereux, leur preparation et leur application therapeutique
WO2012019024A2 (en) 2010-08-04 2012-02-09 Immunogen, Inc. Her3-binding molecules and immunoconjugates thereof
TW201302793A (zh) 2010-09-03 2013-01-16 Glaxo Group Ltd 新穎之抗原結合蛋白
CN105399831A (zh) 2010-10-29 2016-03-16 伊缪诺金公司 非拮抗性egfr结合分子及其免疫偶联物
CN103298489A (zh) 2010-10-29 2013-09-11 伊缪诺金公司 新型egfr结合分子及其免疫偶联物
CN103269712B (zh) * 2010-11-03 2016-09-21 伊缪诺金公司 包含新型安丝菌素衍生物的细胞毒性剂
JP5889912B2 (ja) * 2010-11-17 2016-03-22 ジェネンテック, インコーポレイテッド アラニニルメイタンシノール抗体コンジュゲート
LT3153504T (lt) 2010-12-09 2019-02-11 Immunogen, Inc. Įkrautų skersinių jungčių agentų gavimo būdas
JP6049642B2 (ja) 2011-02-15 2016-12-21 イミュノジェン・インコーポレーテッド 複合体の調製方法
US20140079722A1 (en) * 2011-03-09 2014-03-20 Centrose, Llc Extracellular targeted drug conjugates
WO2012135517A2 (en) 2011-03-29 2012-10-04 Immunogen, Inc. Preparation of maytansinoid antibody conjugates by a one-step process
RS58367B1 (sr) 2011-03-29 2019-03-29 Immunogen Inc Priprema konjugata antitela i majtanzinoida jednostepenim postupkom
IL281714B2 (en) 2011-04-01 2023-11-01 Immunogen Inc Methods for increasing the effectiveness of FOLR1 cancer therapy
US20120282282A1 (en) * 2011-04-04 2012-11-08 Immunogen, Inc. Methods for Decreasing Ocular Toxicity of Antibody Drug Conjugates
BR112013026828A2 (pt) 2011-04-21 2016-11-29 Bristol Myers Squibb Co polipeptídeos de anticorpo que antagonizam cd40
US8815226B2 (en) 2011-06-10 2014-08-26 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
WO2012171020A1 (en) 2011-06-10 2012-12-13 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
WO2013016714A1 (en) 2011-07-28 2013-01-31 Sea Lane Biotechnologies Sur-binding proteins against erbb3
US9233171B2 (en) 2011-11-21 2016-01-12 Immunogen, Inc. Method of treatment of tumors that are resistant to EGFR antibody therapies by EGFR antibody cytotoxic agent conjugate
EP3446707A1 (en) 2011-12-22 2019-02-27 i2 Pharmaceuticals, Inc. Surrogate binding proteins
WO2013110680A1 (en) * 2012-01-27 2013-08-01 F. Hoffmann-La Roche Ag Integrin antagonist conjugates for targeted delivery to cells expressing vla-4
US10080805B2 (en) 2012-02-24 2018-09-25 Purdue Research Foundation Cholecystokinin B receptor targeting for imaging and therapy
US20140080175A1 (en) 2012-03-29 2014-03-20 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
HUE049693T2 (hu) 2012-08-31 2020-10-28 Immunogen Inc Diagnosztikai ASSAY-k és készletek a folát receptor 1 kimutatására
WO2014055842A1 (en) * 2012-10-04 2014-04-10 Immunogen, Inc. Process for preparing stable antibody maytansinoid conjugates
WO2014055877A1 (en) 2012-10-04 2014-04-10 Immunogen, Inc. Use of a pvdf membrane to purify cell-binding agent cytotoxic agent conjugates
EP2908818A4 (en) 2012-10-16 2016-07-13 Endocyte Inc CONJUGATES OF DRUG DELIVERY CONTAINING ARTIFICIAL AMINO ACIDS AND METHODS OF USE
NO2789793T3 (https=) * 2012-10-24 2018-01-27
MX2015005122A (es) * 2012-10-24 2015-10-29 Polytherics Ltd Conjugados de farmaco-proteina novedosos.
US10131682B2 (en) 2012-11-24 2018-11-20 Hangzhou Dac Biotech Co., Ltd. Hydrophilic linkers and their uses for conjugation of drugs to a cell binding molecules
WO2014089177A2 (en) 2012-12-04 2014-06-12 Massachusetts Institute Of Technology Compounds, conjugates and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines
CN104530235A (zh) 2012-12-21 2015-04-22 百奥泰生物科技(广州)有限公司 一种抑制肿瘤生长的抗体药物衍生物及其制备方法和用途
CN104688740A (zh) * 2012-12-21 2015-06-10 百奥泰生物科技(广州)有限公司 类美登素衍生物及其制备方法和用途
FR3002454B1 (fr) * 2013-02-26 2015-04-10 Commissariat Energie Atomique Composition immunogene sous forme d'emulsion
US9968673B2 (en) * 2013-02-26 2018-05-15 Commissariat á l'ènergie atomique et aux ènergies alternatives Immunogenic composition in emulsion form comprising two dispersed phases, one comprising an antigen and the other comprising an immunostimulating agent
JP6494533B2 (ja) * 2013-02-28 2019-04-03 イミュノジェン・インコーポレーテッド 細胞結合剤及び細胞毒性剤としてのマイタンシノイドを含む複合体
PL2968440T3 (pl) 2013-03-15 2019-12-31 Zymeworks Inc. Związki cytotoksyczne i antymitotyczne oraz sposoby ich stosowania
MX379256B (es) 2013-03-15 2025-03-10 Regeneron Pharma Moleculas biologicamente activas, conjugados de las mismas, y usos terapeuticos.
AR096184A1 (es) * 2013-05-02 2015-12-16 Hoffmann La Roche Terapia de combinación de un anticuerpo para cd20 afucosilado con un conjugado de anticuerpos para cd22-fármaco
US10208125B2 (en) 2013-07-15 2019-02-19 University of Pittsburgh—of the Commonwealth System of Higher Education Anti-mucin 1 binding agents and uses thereof
TWI641620B (zh) 2013-08-21 2018-11-21 再生元醫藥公司 抗-prlr抗體及其用途
KR102252925B1 (ko) 2013-08-26 2021-05-18 리제너론 파마슈티칼스 인코포레이티드 마크롤라이드 디아스테레오머를 포함하는 약제학적 조성물, 이의 합성 방법 및 치료학적 용도
AU2014312086B2 (en) 2013-08-30 2020-03-12 Immunogen, Inc. Antibodies and assays for detection of folate receptor 1
EP3299476B1 (en) 2013-09-05 2023-07-19 The Jackson Laboratory Compositions for rna-chromatin interaction analysis and uses thereof
IL298044B2 (en) 2013-10-08 2024-11-01 Immunogen Inc Dosing regimens of anti-FOLR1 immunoconjugate
EA032231B1 (ru) 2013-10-11 2019-04-30 Мерсана Терапьютикс, Инк. Конъюгаты белок-полимер-лекарственное средство
CA2927022C (en) 2013-10-11 2018-08-21 Asana Biosciences, Llc Protein-polymer-drug conjugates
CN103483357B (zh) * 2013-10-12 2015-11-18 齐鲁制药有限公司 一种抗体-美登素偶联物的中间体新晶型及其制备方法
US9562059B2 (en) * 2013-12-02 2017-02-07 Hong Kong Baptist University Anticancer maytansinoids with two fused macrocyclic rings
RU2729194C2 (ru) 2013-12-27 2020-08-05 Займворкс Инк. Сульфонамидсодержащие связывающие системы для лекарственных конъюгатов
JP2017510548A (ja) * 2014-01-29 2017-04-13 シャンハイ ヘンルイ ファーマスーティカル カンパニー リミテッドShanghai Hengrui Pharmaceutical Co., Ltd. リガンド‐細胞傷害性薬物抱合体、その製造方法、およびその用途
AU2015229591B2 (en) 2014-03-11 2020-10-22 Regeneron Pharmaceuticals, Inc. Anti-EGFRvlll antibodies and uses thereof
MA39774A (fr) * 2014-03-24 2021-05-12 Roche Sequencing Solutions Inc Procédés chimiques pour produire des nucléotides étiquetés
AU2015252518B2 (en) * 2014-04-29 2019-11-14 Genequantum Healthcare (Suzhou) Co., Ltd. New stable antibody-drug conjugate, preparation method therefor, and use thereof
EP3160513B1 (en) 2014-06-30 2020-02-12 Glykos Finland Oy Saccharide derivative of a toxic payload and antibody conjugates thereof
CA2953371C (en) 2014-06-30 2021-08-24 Tarveda Therapeutics, Inc. Targeted conjugates and particles and formulations thereof
CN106999604B (zh) 2014-09-02 2021-08-03 伊缪诺金公司 用于配制抗体药物缀合物组合物的方法
ES2815353T3 (es) 2014-09-03 2021-03-29 Immunogen Inc Derivados de benzodiazepina citotóxicos
EP3189057A1 (en) 2014-09-03 2017-07-12 ImmunoGen, Inc. Cytotoxic benzodiazepine derivatives
TW201609152A (zh) 2014-09-03 2016-03-16 免疫原公司 包含細胞結合劑及細胞毒性劑之偶聯物
AU2015318556C1 (en) 2014-09-17 2021-01-07 Zymeworks Bc Inc. Cytotoxic and anti-mitotic compounds, and methods of using the same
EA034950B1 (ru) 2015-03-27 2020-04-09 Регенерон Фармасьютикалз, Инк. Производные майтанзиноида, их конъюгаты и способы использования
CN107849133B (zh) 2015-05-04 2022-08-23 西托姆克斯治疗公司 抗cd166抗体、可活化抗cd166抗体及其使用方法
CN106243127B (zh) * 2015-06-09 2021-01-26 凯惠科技发展(上海)有限公司 抗体药物偶联物、中间体、制备方法、药物组合物及应用
EP3769787A1 (en) 2015-06-29 2021-01-27 ImmunoGen, Inc. Conjugates of cysteine engineered antibodies
CN108811499B (zh) * 2015-07-04 2021-09-24 杭州多禧生物科技有限公司 细胞结合分子的特异性偶联
MY189159A (en) 2015-07-06 2022-01-29 Regeneron Pharma Multispecific antigen-binding molecules and uses thereof
SG10202106529XA (en) 2015-07-21 2021-07-29 Immunogen Inc Methods of preparing cytotoxic benzodiazepine derivatives
EP3331569A1 (en) 2015-08-07 2018-06-13 Gamamabs Pharma Antibodies, antibody drug conjugates and methods of use
AU2016323968B2 (en) 2015-09-17 2023-07-06 Immunogen, Inc. Therapeutic combinations comprising anti-FOLR1 immunoconjugates
JP7057278B2 (ja) 2015-10-28 2022-04-19 ターベダ セラピューティクス インコーポレイテッド Sstr標的化コンジュゲート及び粒子並びにその製剤
SG11201803915UA (en) 2015-11-10 2018-06-28 Childrens Research Institute Childrens National Medical Center Echinomycin formulation, method of making and method of use thereof
PT3380525T (pt) 2015-11-25 2024-02-05 Immunogen Inc Formulações farmacêuticas e métodos que as utilizam
JP2018536682A (ja) 2015-12-11 2018-12-13 リジェネロン・ファーマシューティカルズ・インコーポレイテッドRegeneron Pharmaceuticals, Inc. Egfr及び/またはerbb3遮断に耐性のある腫瘍の成長を低減または防止するための方法
WO2017132173A1 (en) 2016-01-25 2017-08-03 Regeneron Pharmaceuticals, Inc. Maytansinoid derivatives, conjugates thereof, and methods of use
EP3423105B1 (en) * 2016-03-02 2021-05-05 Eisai R&D Management Co., Ltd. Eribulin-based antibody-drug conjugates and methods of use
JP6937773B2 (ja) * 2016-03-07 2021-09-22 ハンミ ファーマシューティカル カンパニー リミテッド ポリエチレングリコール誘導体及びその用途
WO2017190079A1 (en) 2016-04-28 2017-11-02 Regeneron Pharmaceuticals, Inc. Methods of making multispecific antigen-binding molecules
US10918627B2 (en) 2016-05-11 2021-02-16 Massachusetts Institute Of Technology Convergent and enantioselective total synthesis of Communesin analogs
EP3458479B1 (en) 2016-06-08 2020-11-04 AbbVie Inc. Anti-b7-h3 antibodies and antibody drug conjugates
WO2018002902A1 (en) 2016-07-01 2018-01-04 Glaxosmithkline Intellectual Property (No.2) Limited Antibody-drug conjugates and therapeutic methods using the same
RU2653443C2 (ru) * 2016-07-15 2018-05-08 Закрытое Акционерное Общество "Биокад" Биспецифичные анти-her2/анти-her3 антитела
MY194596A (en) 2016-09-23 2022-12-06 Regeneron Pharma Bi Specific Anti-Muc16-CD3 Antibodies And Anti-Muc16 Drug Conjugates
MX2019003325A (es) 2016-09-23 2019-08-05 Regeneron Pharma Anticuerpos anti-steap2, conjugados anticuerpo-farmaco, y moleculas de fijacion al antigeno biespecificas que se fijan a steap2 y cd3, y usos de estos.
KR20250114431A (ko) 2016-11-08 2025-07-29 리제너론 파마슈티칼스 인코포레이티드 스테로이드 및 이의 단백질-접합체
TWI782930B (zh) 2016-11-16 2022-11-11 美商再生元醫藥公司 抗met抗體,結合met之雙特異性抗原結合分子及其使用方法
TWI845890B (zh) 2016-11-23 2024-06-21 美商伊繆諾金公司 苯二氮平衍生物之選擇性磺化
WO2018102304A1 (en) 2016-11-29 2018-06-07 Regeneron Pharmaceuticals, Inc. Methods of treating prlr positive breast cancer
EP3554544A4 (en) 2016-12-16 2020-07-29 Bluefin Biomedicine, Inc. ANTI-PROTEIN 1 ANTIBODY CONTAINING AN ANTI-CUB DOMAIN (CDCP1), ANTIBODY-DRUG CONJUGATES AND THEIR METHODS OF USE
SI3558391T1 (sl) 2016-12-23 2022-06-30 Immunogen, Inc. Imunokonjugati, ciljno usmerjeni na ADAM9, in načini njihove uporabe
WO2018129029A1 (en) 2017-01-04 2018-07-12 Immunogen, Inc. Met antibodies and immunoconjugates and uses thereof
KR20250171447A (ko) 2017-02-28 2025-12-08 이뮤노젠 아이엔씨 자기희생적 펩티드 링커 및 이들의 접합체를 갖는 메이탄시노이드 유도체
KR20240074000A (ko) 2017-02-28 2024-05-27 다이이찌 산쿄 가부시키가이샤 항 her3 항체-약물 콘주게이트 투여에 의한 egfr-tki 저항성의 비소세포 폐암의 치료 방법
EP3381474A1 (en) * 2017-03-27 2018-10-03 Alfasigma S.p.A. Histone deacetylase inhibitors-based antibody drug conjugates (adcs) and use in therapy
EP3604385B1 (en) * 2017-03-30 2024-05-01 NOF Corporation Heterobifunctional monodispersed polyethylene glycol and conjugate using the same
WO2018195243A1 (en) 2017-04-20 2018-10-25 Immunogen, Inc. Cytotoxic benzodiazepine derivatives and conjugates thereof
WO2018209239A1 (en) 2017-05-11 2018-11-15 Massachusetts Institute Of Technology Potent agelastatin derivatives as modulators for cancer invasion and metastasis
KR20250008984A (ko) 2017-05-18 2025-01-16 리제너론 파마슈티칼스 인코포레이티드 사이클로덱스트린 단백질 약물 접합체
WO2018213082A1 (en) 2017-05-18 2018-11-22 Regeneron Pharmaceuticals, Inc. Bis-octahydrophenanthrene carboxamides and protein conjugates thereof
FI3635009T3 (fi) 2017-06-07 2026-04-07 Regeneron Pharma Koostumuksia ja menetelmiä entsyymien internalisoimiseksi
KR102771835B1 (ko) * 2017-06-20 2025-02-26 비바솔, 인코포레이티드. Cd38 항체 약물 접합체
US10640508B2 (en) 2017-10-13 2020-05-05 Massachusetts Institute Of Technology Diazene directed modular synthesis of compounds with quaternary carbon centers
MX2020004691A (es) 2017-11-07 2020-08-20 Regeneron Pharma Enlazadores hidrofilicos para conjugados anticuerpo-farmaco.
CN109771658B (zh) * 2017-11-14 2021-12-10 博瑞生物医药(苏州)股份有限公司 靶向多臂偶联物
TW202413360A (zh) 2017-12-28 2024-04-01 美商伊繆諾金公司 苯二氮平衍生物
CN112004557B (zh) 2018-01-08 2024-07-30 里珍纳龙药品有限公司 类固醇类化合物及其抗体偶联物
MA51629A (fr) * 2018-01-12 2020-11-18 Immunogen Inc Procédés de production, purification et formulation de conjugués anticorps-médicaments
MX2020011487A (es) 2018-04-30 2020-12-07 Regeneron Pharma Anticuerpos y moleculas biespecificas de union al antigeno que se unen a her2 y/o aplp2, conjugados y usos de estos.
CN112533951A (zh) 2018-05-09 2021-03-19 里珍纳龙药品有限公司 抗msr1抗体及其使用方法
EP3793591A1 (en) 2018-05-17 2021-03-24 Regeneron Pharmaceuticals, Inc. Anti-cd63 antibodies, conjugates, and uses thereof
SG11202012257VA (en) 2018-06-26 2021-01-28 Immunogen Inc Immunoconjugates targeting adam9 and methods of use thereof
WO2020014306A1 (en) 2018-07-10 2020-01-16 Immunogen, Inc. Met antibodies and immunoconjugates and uses thereof
KR20210062005A (ko) 2018-09-20 2021-05-28 다이이찌 산쿄 가부시키가이샤 항 her3 항체-약물 콘쥬게이트 투여에 의한 her3 변이암의 치료
CN109350748B (zh) * 2018-10-24 2021-06-11 沈阳药科大学 氧化还原双敏感键桥连小分子前药及其自组装纳米粒
TWI897855B (zh) 2018-10-26 2025-09-21 美商免疫遺傳股份有限公司 E p C A M 抗體、可活化抗體及免疫偶聯物以及其用途
MA53455B1 (fr) 2018-11-20 2022-11-30 Regeneron Pharma Dérivés de bis-octahydrophénanthrène carboxamide et leurs conjugués protéiques destinés à être utilisés en tant qu'agonistes de lxr
MA53765B2 (fr) 2018-12-21 2025-04-30 Regeneron Pharmaceuticals, Inc. Tubulysines et conjugués tubulysines-protéines
JP7591503B2 (ja) 2018-12-21 2024-11-28 リジェネロン ファーマシューティカルズ,インク. リファマイシンアナログおよびその抗体薬物コンジュゲート
EP3908323A2 (en) 2019-01-08 2021-11-17 Regeneron Pharmaceuticals, Inc. Traceless linkers and protein-conjugates thereof
US20220040319A1 (en) 2019-02-21 2022-02-10 Regeneron Pharmaceuticals, Inc. Methods of treating ocular cancer using anti-met antibodies and bispecific antigen binding molecules that bind met
JP7682797B2 (ja) 2019-03-20 2025-05-26 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア クローディン6二重特異性抗体
AU2020241896A1 (en) 2019-03-20 2021-09-23 The Regents Of The University Of California Claudin-6 antibodies and drug conjugates
EP3947395A1 (en) 2019-03-29 2022-02-09 ImmunoGen, Inc. Cytotoxic bis-benzodiazepine derivatives and conjugates thereof with cell-binding agents for inhibiting abnormal cell growth or for treating proliferative diseases
JP7561141B2 (ja) 2019-04-26 2024-10-03 イミュノジェン・インコーポレーテッド カンプトテシン誘導体
US11535634B2 (en) 2019-06-05 2022-12-27 Massachusetts Institute Of Technology Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof
CN114341162B (zh) 2019-07-10 2025-10-17 赛博克萨2公司 作为治疗剂的细胞毒素的肽缀合物
TW202116356A (zh) 2019-07-10 2021-05-01 美商斯布雷克薩三號公司 作為治療劑之微管靶向藥劑之肽結合物
US11896682B2 (en) 2019-09-16 2024-02-13 Regeneron Pharmaceuticals, Inc. Radiolabeled MET binding proteins for immuno-PET imaging and methods of use thereof
US11814428B2 (en) 2019-09-19 2023-11-14 Regeneron Pharmaceuticals, Inc. Anti-PTCRA antibody-drug conjugates and uses thereof
AU2021210987A1 (en) 2020-01-24 2022-08-04 Regeneron Pharmaceuticals, Inc. Protein-antiviral compound conjugates
MX2022010457A (es) 2020-02-25 2022-11-16 Mediboston Ltd Derivados de camptotecina y conjugados de esta.
IL295312A (en) 2020-02-28 2022-10-01 Regeneron Pharma Bispecific antigen binding molecules that bind her2, and methods of use thereof
IL319200A (en) 2020-04-16 2025-04-01 Regeneron Pharma Antibody-drug conjugates prepared using Diels-Alder compression methods
JP2023533218A (ja) 2020-06-24 2023-08-02 レゲネロン ファーマシューティカルス,インコーポレーテッド ツブリシン及びタンパク質-ツブリシンコンジュゲート
EP4178624A2 (en) 2020-07-07 2023-05-17 Bionecure Therapeutics, Inc. Maytansinoids as adc payloads and their use for the treatment of cancer
KR20240038138A (ko) 2020-07-13 2024-03-22 리제너론 파마슈티칼스 인코포레이티드 단백질에서 글루타민 잔기에 접합된 캄토테신 유사체 및 그의 용도
JPWO2022014698A1 (https=) 2020-07-17 2022-01-20
CA3191304A1 (en) 2020-09-14 2022-03-17 Amy Han Antibody-drug conjugates comprising glp1 peptidomimetics and uses thereof
AU2021366691B2 (en) 2020-10-22 2024-06-06 Regeneron Pharmaceuticals, Inc. Anti-FGFR2 antibodies and methods of use thereof
UY39610A (es) 2021-01-20 2022-08-31 Abbvie Inc Conjugados anticuerpo-fármaco anti-egfr
WO2022182415A1 (en) 2021-02-24 2022-09-01 Massachusetts Institute Of Technology Himastatin derivatives, and processes of preparation thereof, and uses thereof
US12521444B2 (en) 2021-02-25 2026-01-13 Fortvita Biologics Limited Anti-HER2 antibody-drug conjugates and uses thereof
AU2022232548A1 (en) 2021-03-08 2023-10-12 Genequantum Healthcare (Suzhou) Co., Ltd. Antibody-immune agonist conjugate and applications thereof
KR20230170769A (ko) 2021-04-14 2023-12-19 진콴텀 헬스케어 (쑤저우) 씨오., 엘티디. 링커, 접합체 및 그 응용
MX2024000897A (es) 2021-07-28 2024-02-06 Regeneron Pharma Conjugados de proteina y compuestos antivirales.
JP2024534101A (ja) * 2021-08-20 2024-09-18 プサン ナショナル ユニバーシティ インダストリー - ユニバーシティ コーポレイション ファンデーション オブジェクトが固定された膨潤性高分子の製造方法
AU2022414083A1 (en) * 2021-12-15 2024-06-20 The Administrators Of The Tulane Educational Fund Conjugates, their compositions, and their related methods
US20230414775A1 (en) 2021-12-29 2023-12-28 Regeneron Pharmaceuticals, Inc. Tubulysins and protein-tubulysin conjugates
CA3241734A1 (en) 2022-01-12 2023-07-20 Amy Han Camptothecin analogs conjugated to a glutamine residue in a protein, and their use
JP2025503700A (ja) 2022-01-14 2025-02-04 レジェネロン ファーマシューティカルズ, インコーポレイテッド ベルカリンa誘導体及びその抗体薬物複合体
AU2023231305A1 (en) 2022-03-11 2024-09-12 Regeneron Pharmaceuticals, Inc. Anti-GLP1r antibody-tethered drug conjugates comprising GLP1 peptidomimetics and uses thereof
CA3261366A1 (en) 2022-07-21 2024-01-25 Firefly Bio, Inc. GLUCOCORTICOID RECEPTOR AGONISTS AND THEIR CONJUGATES
JP2025524986A (ja) 2022-07-27 2025-08-01 メディボストン リミテッド オーリスタチン誘導体およびそのコンジュゲート
CN120659785A (zh) 2022-11-30 2025-09-16 里珍纳龙药品有限公司 Tlr7激动剂及其抗体-药物缀合物
IL321285A (en) 2022-12-21 2025-08-01 Regeneron Pharma Topoisomerase I inhibitor prodrugs for ADC conjugates and a regimen for their use
EP4661914A1 (en) 2023-02-09 2025-12-17 Regeneron Pharmaceuticals, Inc. Antibody-drug conjugates via inverse electron demand diels-alder reactions
WO2024220628A1 (en) * 2023-04-18 2024-10-24 The Regents Of The University Of Colorado, A Body Corporate Target for combatting the foreign body response to implantable biomaterials
EP4705343A1 (en) 2023-05-02 2026-03-11 Regeneron Pharmaceuticals, Inc. Anti-human m-cadherin (cdh15) antibodies, conjugates, and uses thereof for delivery of genetic payloads to muscle cells
WO2024248123A1 (ja) 2023-06-02 2024-12-05 第一三共株式会社 抗her3抗体-薬物コンジュゲートとrasg12c阻害剤の組み合わせ
WO2025014533A1 (en) 2023-07-10 2025-01-16 Regeneron Pharmaceuticals, Inc. Anti-human cacng1 antibody-drug conjugates and uses thereof
WO2025094146A1 (en) 2023-11-02 2025-05-08 Immunogen Switzerland Gmbh Vasconstrictors for reducing ocular toxicity of antibody-maytansinoid conjugates
US20250171516A1 (en) 2023-11-03 2025-05-29 Regeneron Pharmaceuticals, Inc. Peptide acids as a glp1r agonist and antibody-drug conjugates thereof
WO2025117727A1 (en) 2023-11-29 2025-06-05 Regeneron Pharmaceuticals, Inc. Analogs of quinoxaline/quinoline cytotoxins, linker- payloads, protein-drug conjugates, and uses thereof
CN118580194A (zh) * 2024-05-21 2024-09-03 南方科技大学 一种双功能分子探针的制备方法
WO2026020031A2 (en) 2024-07-18 2026-01-22 Novarock Biotherapeutics, Ltd. Cdh17 antibodies and uses thereof
WO2026021443A1 (en) 2024-07-23 2026-01-29 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Antibody-drug conjugates targeting cdh3 and preparation methods and uses thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030220245A1 (en) * 2000-06-02 2003-11-27 Hubbell Jeffrey A Conjugate addition reactions for the controlled delivery of pharmaceutical active compounds
CN101087611A (zh) * 2003-10-10 2007-12-12 伊缪诺金公司 用经不可切割接头连接的细胞结合剂美登木素生物碱偶联物靶向特定细胞群的方法、所述偶联物和制备所述偶联物的方法

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6958212B1 (en) * 1999-02-01 2005-10-25 Eidgenossische Technische Hochschule Zurich Conjugate addition reactions for the controlled delivery of pharmaceutically active compounds
US7157458B2 (en) * 2001-04-17 2007-01-02 Cryolife, Inc. Bifunctional energy-reversible acyl-compositions
WO2002087497A2 (en) * 2001-04-26 2002-11-07 Board Of Regents, The University Of Texas System Therapeutic agent/ligand conjugate compositions, their methods of synthesis and use
US6441163B1 (en) * 2001-05-31 2002-08-27 Immunogen, Inc. Methods for preparation of cytotoxic conjugates of maytansinoids and cell binding agents
US6716821B2 (en) * 2001-12-21 2004-04-06 Immunogen Inc. Cytotoxic agents bearing a reactive polyethylene glycol moiety, cytotoxic conjugates comprising polyethylene glycol linking groups, and methods of making and using the same
US8877901B2 (en) * 2002-12-13 2014-11-04 Immunomedics, Inc. Camptothecin-binding moiety conjugates
US6596757B1 (en) * 2002-05-14 2003-07-22 Immunogen Inc. Cytotoxic agents comprising polyethylene glycol-containing taxanes and their therapeutic use
US8088387B2 (en) * 2003-10-10 2012-01-03 Immunogen Inc. Method of targeting specific cell populations using cell-binding agent maytansinoid conjugates linked via a non-cleavable linker, said conjugates, and methods of making said conjugates
PL3524611T3 (pl) 2003-05-20 2021-06-14 Immunogen, Inc. Udoskonalone czynniki cytotoksyczne zawierające nowe maitansynoidy
US7276497B2 (en) * 2003-05-20 2007-10-02 Immunogen Inc. Cytotoxic agents comprising new maytansinoids
WO2005012484A2 (en) * 2003-07-25 2005-02-10 Neose Technologies, Inc. Antibody-toxin conjugates
KR20120064120A (ko) 2004-06-01 2012-06-18 제넨테크, 인크. 항체 약물 접합체 및 방법
KR101270829B1 (ko) 2004-09-23 2013-06-07 제넨테크, 인크. 시스테인 유전자조작 항체 및 접합체
US20060121042A1 (en) * 2004-10-27 2006-06-08 Medimmune, Inc. Modulation of antibody specificity by tailoring the affinity to cognate antigens
CA2597407C (en) * 2005-02-11 2013-09-10 Immunogen, Inc. Process for preparing stable drug conjugates
EP1942944A2 (en) * 2005-10-31 2008-07-16 Genentech, Inc. Macrocyclic depsipeptide antibody-drug conjugates and methods
ES2567402T3 (es) * 2006-05-30 2016-04-22 Genentech, Inc. Anticuerpos anti CD22, sus inmunoconjugados y usos de los mismos
US20080311040A1 (en) * 2007-03-06 2008-12-18 Flagship Ventures METHODS AND COMPOSITIONS FOR IMPROVED THERAPEUTIC EFFECTS WITH siRNA
NZ583318A (en) * 2007-07-16 2012-07-27 Genentech Inc Humanized anti-cd79b antibodies and immunoconjugates and methods of use
EP2276506A4 (en) 2008-04-30 2014-05-07 Immunogen Inc EFFICIENT CONJUGATES AND HYDROPHILIC BINDER

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030220245A1 (en) * 2000-06-02 2003-11-27 Hubbell Jeffrey A Conjugate addition reactions for the controlled delivery of pharmaceutical active compounds
CN101087611A (zh) * 2003-10-10 2007-12-12 伊缪诺金公司 用经不可切割接头连接的细胞结合剂美登木素生物碱偶联物靶向特定细胞群的方法、所述偶联物和制备所述偶联物的方法

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