CN103648530B - 蛋白质‑活性剂缀合物及其制备方法 - Google Patents

蛋白质‑活性剂缀合物及其制备方法 Download PDF

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Publication number
CN103648530B
CN103648530B CN201280031480.7A CN201280031480A CN103648530B CN 103648530 B CN103648530 B CN 103648530B CN 201280031480 A CN201280031480 A CN 201280031480A CN 103648530 B CN103648530 B CN 103648530B
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active agent
amino acid
compound
monoclonal antibody
mmol
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CN201280031480.7A
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Chinese (zh)
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CN103648530A (zh
Inventor
金容珠
朴泰奎
于成昊
李香淑
金永云
赵宗云
郑斗烷
金善英
权贤珍
吴奎万
郑允瑞
朴允熙
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Shanghai Fosun Pharmaceutical Group Co Ltd
Ligachem Biosciences Inc
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Legochem Biosciences Inc
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Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR122020001787A8 (pt) 2011-05-08 2023-04-25 Legochem Biosciences Inc Conjugado de anticorpo-agente ativo, seus métodos de preparação, sua composição e seu uso
US9796754B2 (en) * 2011-05-27 2017-10-24 Ambrx, Inc. Compositions containing, methods involving, and uses of non-natural amino acid linked dolastatin derivatives
EA027971B1 (ru) * 2011-09-20 2017-09-29 Медимьюн Лимитед Пирролбензодиазепины
AU2013328621B2 (en) * 2012-10-12 2016-12-01 Adc Therapeutics Sa Pyrrolobenzodiazepine-anti-HER2 antibody conjugates
WO2014096551A1 (en) * 2012-12-21 2014-06-26 Glykos Finland Oy Linker-payload molecule conjugates
PT3611180T (pt) 2013-03-15 2022-03-15 Biomolecular Holdings Llc Imunoglobulina híbrida que contém uma ligação não peptídica
WO2014177771A1 (en) 2013-05-02 2014-11-06 Glykos Finland Oy Conjugates of a glycoprotein or a glycan with a toxic payload
FR3008408B1 (fr) 2013-07-11 2018-03-09 Mc Saf Nouveaux conjugues anticorps-medicament et leur utilisation en therapie
US10010624B2 (en) 2013-10-11 2018-07-03 Medimmune Limited Pyrrolobenzodiazepine-antibody conjugates
BR112016014913A8 (pt) * 2013-12-23 2020-06-09 Zymeworks Inc anticorpo, ou um fragmento de ligação ao antígeno do mesmo, conjugado, ácido nucléico, vetor, célula hospedeira, composição farmacêutica, método de preparo de uma cadeia leve de um anticorpo ou fragmento de ligação ao antígeno e método de preparo de um conjugado
AU2015229186B2 (en) 2014-03-14 2021-01-28 Biomolecular Holdings Llc Hybrid immunoglobulin containing non-peptidyl linkage
KR101628872B1 (ko) * 2014-05-28 2016-06-09 주식회사 레고켐 바이오사이언스 자가-희생 기를 포함하는 화합물
JP5924795B2 (ja) 2014-06-13 2016-05-25 テンボロン オイ 複合体
DK3160513T3 (da) 2014-06-30 2020-04-06 Glykos Finland Oy Saccharidderivat af en toksisk payload og antistofkonjugater deraf
WO2016014942A1 (en) * 2014-07-25 2016-01-28 Memorial Sloan Kettering Cancer Center Bispecific her2 and cd3 binding molecules
US11820832B2 (en) 2014-07-25 2023-11-21 Memorial Sloan Kettering Cancer Center Bispecific HER2 and CD3 binding molecules
KR20160080832A (ko) * 2014-12-29 2016-07-08 주식회사 레고켐 바이오사이언스 리피바디 유도체-약물 복합체, 그 제조방법 및 용도
CN104587487B (zh) * 2015-01-06 2018-01-16 华东师范大学 一种应用于靶向给药系统的新的支链连接体
CN104650179A (zh) * 2015-02-06 2015-05-27 东南大学 一种新型的可被溶酶体酶裂解的铂类前药
WO2017051254A1 (en) 2015-09-25 2017-03-30 Legochem Biosciences, Inc. Compositions and methods related to anti-egfr antibody drug conjugates
WO2017051249A1 (en) 2015-09-25 2017-03-30 Legochem Biosciences, Inc. Compositions and methods related to anti-cd19 antibody drug conjugates
KR102847348B1 (ko) * 2015-11-25 2025-08-19 주식회사 리가켐바이오사이언스 펩타이드 그룹을 포함하는 접합체 및 이와 관련된 제조방법
CN113599533A (zh) * 2015-11-25 2021-11-05 乐高化学生物科学股份有限公司 包含分支接头的抗体-药物缀合物及其相关方法
CN107847606A (zh) 2015-11-25 2018-03-27 乐高化学生物科学股份有限公司 包含自降解基团的缀合物及其相关方法
GB201521709D0 (en) * 2015-12-09 2016-01-20 Kings College London And Sec Dep For Health The PBD Antibacterial agents
US20170348429A1 (en) * 2016-05-17 2017-12-07 Abbvie Biotherapeutics Inc. ANTI-cMET ANTIBODY DRUG CONJUGATES AND METHODS FOR THEIR USE
CN109641051A (zh) 2016-06-17 2019-04-16 美真达治疗公司 用于耗尽细胞的组合物和方法
PL3432916T3 (pl) 2016-09-13 2020-04-30 Allergan, Inc. Niebiałkowo stabilzowane kompozycje toksyny clostridium
RS61967B1 (sr) * 2016-11-23 2021-07-30 Lilly Co Eli Konjugati leka i met antitela
KR102085798B1 (ko) 2016-12-28 2020-03-06 주식회사 인투셀 베타-갈락토사이드가 도입된 자가-희생 기를 포함하는 화합물
CN108250055B (zh) * 2016-12-28 2022-08-05 重庆医药工业研究院有限责任公司 一种焦磷酸丙酮基香叶酯中间体的制备方法
SG10202102897PA (en) 2017-01-20 2021-04-29 Magenta Therapeutics Inc Compositions and methods for the depletion of cd137+ cells
IL269535B2 (en) * 2017-03-29 2024-11-01 Ligachem Biosciences Inc Pyrrolobenzodiazepine dimer prodrug and ligand-linker conjugate compound of the same
AU2018288030B2 (en) * 2017-06-20 2022-02-03 Systimmune, Inc. Screening of fixed-point coupling sites of cysteine-modified antibody-toxin conjugate (TDC)
WO2019035649A1 (ko) * 2017-08-14 2019-02-21 주식회사 레고켐 바이오사이언스 EGFRvIII에 대한 항체를 포함하는 항체 약물 접합체
CA3094827A1 (en) 2018-03-28 2019-10-03 Mitsubishi Tanabe Pharma Corporation Drug conjugates of cmet monoclonal binding agents, and uses thereof
KR20210023839A (ko) 2018-05-09 2021-03-04 주식회사 레고켐 바이오사이언스 항-cd19 항체 약물 접합체 관련 조성물 및 방법
KR20200084802A (ko) 2019-01-03 2020-07-13 주식회사 레고켐 바이오사이언스 안전성이 향상된 피롤로벤조디아제핀 이량체 화합물 및 이의 용도
JP7542266B2 (ja) 2019-01-03 2024-08-30 リガケム バイオサイエンシズ， インク． 安定性が向上したピロロベンゾジアゼピン二量体化合物及びその用途
BR112021017303A2 (pt) 2019-03-06 2021-11-16 Legochem Biosciences Inc Conjugado de anticorpo ou um sal ou solvato farmaceuticamente aceitável deste, anticorpo que se liga com especificidade ao dlk1 ou um fragmento de ligação ao antígeno deste, composição farmacêutica para prevenção ou tratamento de doença proliferativa, câncer ou angiogênica, métodos para prevenção e para tratamento de doença proliferativa, câncer ou angiogênica, e, uso do conjugado
KR102501394B1 (ko) * 2019-05-02 2023-02-21 주식회사 레고켐 바이오사이언스 트리스 구조를 가지는 링커를 포함하는 리간드-약물 접합체
WO2020222573A1 (ko) 2019-05-02 2020-11-05 주식회사 레고켐 바이오사이언스 트리스 구조를 가지는 링커를 포함하는 리간드-약물 접합체
KR20210028544A (ko) 2019-09-04 2021-03-12 주식회사 레고켐 바이오사이언스 인간 ror1에 대한 항체를 포함하는 항체 약물 접합체 및 이의 용도
BR112022013008A2 (pt) 2019-12-31 2022-09-06 Legochem Biosciences Inc Composto derivado de pirrolobenzodiazepina, conjugado de derivado-ligante de pirrolobenzodiazepina, e, composição farmacêutica e método para prevenção ou tratamento de doença proliferativa
WO2022187591A1 (en) 2021-03-05 2022-09-09 Go Therapeutics, Inc. Anti-glyco-cd44 antibodies and their uses
KR20220136267A (ko) 2021-03-30 2022-10-07 주식회사 레고켐 바이오사이언스 인간 cldn18.2에 대한 항체를 포함하는 항체 약물 접합체 및 이의 용도
US20250101126A1 (en) 2021-08-05 2025-03-27 Go Therapeutics, Inc. Anti-glyco-muc4 antibodies and their uses
KR20230024845A (ko) * 2021-08-09 2023-02-21 주식회사 레고켐 바이오사이언스 신규 항생제 및 이의 용도
GB202203070D0 (en) 2022-03-04 2022-04-20 Iksuda Therapeutics Ltd Anti-canag antibody conjugate
EP4389152A1 (en) 2022-12-23 2024-06-26 Synaffix B.V. Conjugates of pbd prodrugs
EP4410313A1 (en) 2023-01-31 2024-08-07 Synaffix B.V. Homogeneous antibody-conjugates with high payload loading
EP4450489A1 (en) 2023-04-18 2024-10-23 Synaffix B.V. Stable 4-isoxazoline conjugates
KR20250169628A (ko) 2023-04-17 2025-12-03 시나픽스 비.브이. 절단 가능한 면역 세포 인게이저
GB202313214D0 (en) 2023-08-30 2023-10-11 Iksuda Therapeutics Ltd Co-administration of antibody-drug conjugate
WO2025238253A1 (en) 2024-05-16 2025-11-20 Synaffix B.V. Antibody-oligonucleotide conjugates

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6011175A (en) * 1993-05-18 2000-01-04 University Of Pittsburgh Inhibition of farnesyltransferase
US20090081210A1 (en) * 2003-12-04 2009-03-26 Vaccinex, Inc. Methods of Killing Tumor Cells by Targeting Internal Antigens Exposed on Apoptotic Tumor Cells
US20100063114A1 (en) * 2006-03-22 2010-03-11 The Regents Of The University Of California Inhibitors of protein prenyltransferases

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4816567A (en) 1983-04-08 1989-03-28 Genentech, Inc. Recombinant immunoglobin preparations
US5225539A (en) 1986-03-27 1993-07-06 Medical Research Council Recombinant altered antibodies and methods of making altered antibodies
GB8823869D0 (en) 1988-10-12 1988-11-16 Medical Res Council Production of antibodies
US5175384A (en) 1988-12-05 1992-12-29 Genpharm International Transgenic mice depleted in mature t-cells and methods for making transgenic mice
AU8507191A (en) 1990-08-29 1992-03-30 Genpharm International, Inc. Transgenic non-human animals capable of producing heterologous antibodies
US5545806A (en) 1990-08-29 1996-08-13 Genpharm International, Inc. Ransgenic non-human animals for producing heterologous antibodies
US5635483A (en) 1992-12-03 1997-06-03 Arizona Board Of Regents Acting On Behalf Of Arizona State University Tumor inhibiting tetrapeptide bearing modified phenethyl amides
US20030129191A1 (en) * 1992-12-23 2003-07-10 Neorx Corporation Pretargeting methods and compounds
CA2115811A1 (en) 1993-02-17 1994-08-18 Claus Krebber A method for in vivo selection of ligand-binding proteins
DE19544393A1 (de) 1995-11-15 1997-05-22 Hoechst Schering Agrevo Gmbh Synergistische herbizide Mischungen
US20030017149A1 (en) * 1996-10-10 2003-01-23 Hoeffler James P. Single chain monoclonal antibody fusion reagents that regulate transcription in vivo
US7605238B2 (en) 1999-08-24 2009-10-20 Medarex, Inc. Human CTLA-4 antibodies and their uses
EP1282423A2 (en) * 2000-05-11 2003-02-12 Oklahoma Medical Research Foundation Prevention of insulin-dependent diabetes, complications thereof, or allograft rejection by inhibition of cyclooxygenase-2 activity with ns398 or pdtc
US7256257B2 (en) 2001-04-30 2007-08-14 Seattle Genetics, Inc. Pentapeptide compounds and uses related thereto
US6884869B2 (en) 2001-04-30 2005-04-26 Seattle Genetics, Inc. Pentapeptide compounds and uses related thereto
CN1638800B (zh) 2002-01-09 2014-07-16 梅达雷克斯有限责任公司 抗cd30的人类单克隆抗体
EP1391213A1 (en) 2002-08-21 2004-02-25 Boehringer Ingelheim International GmbH Compositions and methods for treating cancer using maytansinoid CD44 antibody immunoconjugates and chemotherapeutic agents
US8048432B2 (en) * 2003-08-06 2011-11-01 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Polysaccharide-protein conjugate vaccines
KR101438983B1 (ko) 2003-11-06 2014-09-05 시애틀 지네틱스, 인크. 리간드에 접합될 수 있는 모노메틸발린 화합물
CA2552043A1 (en) 2004-01-21 2005-08-04 Novo Nordisk A/S Transglutaminase mediated conjugation of peptides
TW200539855A (en) 2004-03-15 2005-12-16 Wyeth Corp Calicheamicin conjugates
US20050266008A1 (en) 2004-03-29 2005-12-01 Medarex, Inc. Human anti-IRTA-5 antibodies
TW200616662A (en) 2004-09-10 2006-06-01 Wyeth Corp Humanized anti-5t4 antibodies and anti-5t4 antibody/calicheamicin conjugates
WO2006111759A1 (en) 2005-04-21 2006-10-26 Spirogen Limited Pyrrolobenzodiazepines
EP1917020B1 (en) 2005-07-07 2016-05-25 Seattle Genetics, Inc. Monomethylvaline compounds having phenylalanine side-chain modifications at the c-terminus
HUE035853T2 (en) * 2005-07-18 2018-05-28 Seattle Genetics Inc Beta-glucuronide-linker-drug conjugates
WO2007030642A2 (en) * 2005-09-07 2007-03-15 Medimmune, Inc. Toxin conjugated eph receptor antibodies
NZ566395A (en) 2005-09-26 2012-03-30 Medarex Inc Human monoclonal antibodies to CD70
CA2630415A1 (en) * 2005-10-20 2007-04-26 The Scripps Research Institute Fc labeling for immunostaining and immunotargeting
WO2007112007A2 (en) * 2006-03-22 2007-10-04 University Of Utah Research Foundation Immobilized proteins and methods and uses thereof
WO2008074004A2 (en) 2006-12-14 2008-06-19 Medarex, Inc. Human antibodies that bind cd70 and uses thereof
EP2176295B1 (en) * 2007-07-16 2014-11-19 Genentech, Inc. Humanized anti-cd79b antibodies and immunoconjugates and methods of use
WO2009026274A1 (en) * 2007-08-22 2009-02-26 Medarex, Inc. Site-specific attachment of drugs or other agents to engineered antibodies with c-terminal extensions
WO2009038685A1 (en) 2007-09-18 2009-03-26 The Scripps Research Institute Ligands for copper-catalyzed azide-alkyne cycloaddition reactions
EP2881736B1 (en) * 2008-03-31 2017-06-07 Pacific Biosciences of California, Inc. Single polymerase molecule loading methods and compositions
GB0813432D0 (en) 2008-07-22 2008-08-27 Spirogen Ltd Pyrrolobenzodiazepines
GB0819095D0 (en) 2008-10-17 2008-11-26 Spirogen Ltd Pyrrolobenzodiazepines
CN102012425A (zh) * 2010-12-29 2011-04-13 南开大学 一种新的免疫荧光标记方法
BR122020001787A8 (pt) 2011-05-08 2023-04-25 Legochem Biosciences Inc Conjugado de anticorpo-agente ativo, seus métodos de preparação, sua composição e seu uso
KR101628872B1 (ko) * 2014-05-28 2016-06-09 주식회사 레고켐 바이오사이언스 자가-희생 기를 포함하는 화합물

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6011175A (en) * 1993-05-18 2000-01-04 University Of Pittsburgh Inhibition of farnesyltransferase
US20090081210A1 (en) * 2003-12-04 2009-03-26 Vaccinex, Inc. Methods of Killing Tumor Cells by Targeting Internal Antigens Exposed on Apoptotic Tumor Cells
US20100063114A1 (en) * 2006-03-22 2010-03-11 The Regents Of The University Of California Inhibitors of protein prenyltransferases

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