CN107982545B - 药物偶联物，偶联方法，及其用途 - Google Patents

药物偶联物，偶联方法，及其用途 Download PDF

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CN107982545B
CN107982545B CN201710584374.6A CN201710584374A CN107982545B CN 107982545 B CN107982545 B CN 107982545B CN 201710584374 A CN201710584374 A CN 201710584374A CN 107982545 B CN107982545 B CN 107982545B
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group
compound
antibody
pab
acid
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CN107982545A (zh
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苗振伟
洪予丰
朱同
A·W·楚佐罗斯基
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Lian Ning (Suzhou) biopharmaceutical Co., Ltd.
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Levena Suzhou Biopharma Co ltd
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CN201710584374.6A 2012-05-15 2013-05-14 药物偶联物，偶联方法，及其用途 Active CN107982545B (zh)

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US201261652512P 2012-05-29 2012-05-29
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Families Citing this family (142)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101098854B (zh) 2004-07-23 2012-12-05 恩多塞特公司 二价连接体及其轭合物
NZ599239A (en) 2007-03-14 2013-10-25 Endocyte Inc Binding ligand linked drug delivery conjugates of tubulysins
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
US9138484B2 (en) 2007-06-25 2015-09-22 Endocyte, Inc. Conjugates containing hydrophilic spacer linkers
WO2013126797A1 (en) 2012-02-24 2013-08-29 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
US20140079636A1 (en) 2012-04-16 2014-03-20 Dinesh U. Chimmanamada Targeted therapeutics
WO2013173391A1 (en) 2012-05-15 2013-11-21 Concortis Biosystems, Corp Drug-conjugates, conjugation methods, and uses thereof
US9662402B2 (en) 2012-10-16 2017-05-30 Endocyte, Inc. Drug delivery conjugates containing unnatural amino acids and methods for using
MX379355B (es) 2012-12-21 2025-03-11 Altrubio Inc Enlazadores autodestructivos hidrofilos y conjugados de los mismos.
AU2014228489B2 (en) 2013-03-15 2018-11-15 Zymeworks Bc Inc. Cytotoxic and anti-mitotic compounds, and methods of using the same
WO2014197991A1 (en) 2013-06-12 2014-12-18 Muhammad Yousaf Compounds for promoting liposomal and cellular adhesion and compositions and methods of use thereof
CA2923829A1 (en) 2013-09-10 2015-03-19 Synta Pharmaceuticals Corp. Targeted therapeutics
CN106132431A (zh) 2013-10-15 2016-11-16 索伦托治疗有限公司 具有靶向分子和两种不同药物的药物偶联物
AU2014337555C1 (en) 2013-10-15 2021-01-28 Seagen Inc. PEGylated drug-linkers for improved Ligand-Drug Conjugate pharmacokinetics
WO2015066053A2 (en) 2013-10-28 2015-05-07 Synta Pharmaceuticals Corp. Targeted therapeutics
BR112016015105A8 (pt) * 2013-12-27 2018-04-24 Var2 Pharmaceuticals Aps conjugados var2csa-droga
KR102384740B1 (ko) * 2013-12-27 2022-04-07 자임워크스 인코포레이티드 약물 접합체를 위한 설폰아마이드-함유 연결 시스템
JP6664329B2 (ja) * 2014-01-28 2020-03-13 トゥーベ・ファルマシューティカルズ・ゲー・エム・ベー・ハー コンジュゲーションのための新規な細胞毒性チューブリシン化合物
WO2015116774A1 (en) 2014-01-29 2015-08-06 Synta Pharmaceuticals Corp. Targeted therapeutics
GB201402006D0 (en) 2014-02-06 2014-03-26 Oncomatryx Biopharma S L Antibody-drug conjugates and immunotoxins
JP6576942B6 (ja) 2014-03-03 2019-11-27 マドリガル ファーマシューティカルズ インコーポレイテッド 標的治療薬
WO2015143004A1 (en) 2014-03-18 2015-09-24 Synta Pharmaceuticals Corp. Targeted therapeutics
KR102413079B1 (ko) 2014-05-28 2022-06-24 어젠시스 인코포레이티드 돌라프로인-돌라이소류인 펩타이드의 유도체
SG11201610620UA (en) 2014-06-20 2017-01-27 Bioalliance Cv Anti-folate receptor aplha (fra) antibody-drug conjugates and methods of using thereof
ME03665B (me) 2014-07-11 2020-10-20 Genmab As Antitela koja vezuju axl
EP3900742B1 (en) * 2014-09-11 2024-05-15 Seagen Inc. Targeted delivery of tertiary amine-containing drug substances
RS62860B1 (sr) 2014-09-17 2022-02-28 Zymeworks Inc Citotoksična i antimitotička jedinjenja, i postupci upotrebe istih
JP2017534612A (ja) 2014-10-14 2017-11-24 ポリセリックス・リミテッド Ｐｅｇの部分を含めた脱離基を含む試薬を用いるペプチド又はタンパク質のコンジュゲーションのための方法
US10077287B2 (en) 2014-11-10 2018-09-18 Bristol-Myers Squibb Company Tubulysin analogs and methods of making and use
WO2016094455A1 (en) * 2014-12-08 2016-06-16 Sorrento Therapeutics, Inc. C-met antibody drug conjugate
US9968683B2 (en) 2014-12-17 2018-05-15 Organolinx Corp. Method for conjugating molecules
EP3250238B1 (en) * 2015-01-28 2022-06-01 Sorrento Therapeutics, Inc. Antibody drug conjugates
CN107635405A (zh) * 2015-02-06 2018-01-26 索伦托医疗有限公司 抗体药物缀合物
KR20170117473A (ko) * 2015-02-15 2017-10-23 지앙수 헨그루이 메디슨 컴퍼니 리미티드 리간드-세포독성 약물 접합체, 이의 제조 방법 및 이의 적용
CN106279352B (zh) * 2015-05-29 2020-05-22 上海新理念生物医药科技有限公司 海兔毒素10的衍生物及其应用
EP3308801A4 (en) 2015-06-09 2019-02-27 XDCExplorer (Shanghai) Co., Ltd. ANTIBODY-ACTIVE CONJUGATE, INTERMEDIATE PRODUCT, METHOD OF MANUFACTURE, PHARMACEUTICAL COMPOSITION AND USE THEREOF
ME03772B (me) 2015-07-10 2021-04-20 Genmab As Konjugati antitijela specifičnog za axl i lijeka za liječenje kancera
JP6759326B2 (ja) 2015-07-12 2020-09-23 ハンジョウ ディーエーシー バイオテック シーオー．，エルティディ．Ｈａｎｇｚｈｏｕ Ｄａｃ Ｂｉｏｔｅｃｈ Ｃｏ．，Ｌｔｄ． 細胞結合分子の共役のための架橋連結体
US9839687B2 (en) 2015-07-15 2017-12-12 Suzhou M-Conj Biotech Co., Ltd. Acetylenedicarboxyl linkers and their uses in specific conjugation of a cell-binding molecule
WO2017054080A1 (en) * 2015-09-29 2017-04-06 Zymeworks Inc. Cytotoxic and anti-mitotic compounds, and methods of using the same
WO2017058808A1 (en) * 2015-10-02 2017-04-06 Sirenas Llc Anti-cancer compounds and conjugates thereof
EP3165237B1 (en) 2015-11-03 2018-12-19 Industrial Technology Research Institute Antibody-drug conjugate (adc) and method for forming the same
CN106729743B (zh) * 2015-11-23 2021-09-21 四川科伦博泰生物医药股份有限公司 抗ErbB2抗体-药物偶联物及其组合物、制备方法和应用
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds
US11229708B2 (en) 2015-12-04 2022-01-25 Seagen Inc. Conjugates of quaternized tubulysin compounds
AU2017206074B2 (en) 2016-01-08 2023-09-07 Altrubio Inc. Tetravalent anti-PSGL-1 antibodies and uses thereof
CN107029244B (zh) * 2016-02-04 2021-04-27 浙江昭华生物医药有限公司 抗her2抗体-药物偶联物及其应用
PE20181953A1 (es) 2016-03-02 2018-12-17 Eisai Randd Man Co Ltd Conjugados de anticuerpo y farmaco basados en eribulina y metodos para su uso
KR102626498B1 (ko) 2016-03-25 2024-01-19 씨젠 인크. 페길화된 약물-링커 및 그의 중간체의 제조를 위한 공정
WO2017172907A1 (en) * 2016-03-29 2017-10-05 Sorrento Therapeutics, Inc. Calicheamicin antibody drug conjugates linking an amidoacetyl group to a sugar moiety on calicheamicin
HUE062120T2 (hu) * 2016-03-29 2023-09-28 Toray Industries Peptid-származék és alkalmazása
MA45328A (fr) 2016-04-01 2019-02-06 Avidity Biosciences Llc Compositions acide nucléique-polypeptide et utilisations de celles-ci
WO2017210288A1 (en) * 2016-05-31 2017-12-07 Sorrento Therapeutics, Inc. Antibody drug conjugates having derivatives of amatoxin as the drug
CN109661400A (zh) 2016-06-17 2019-04-19 美真达治疗公司 用于耗尽cd117+细胞的组合物和方法
CN108697809A (zh) * 2016-08-23 2018-10-23 四川科伦博泰生物医药股份有限公司 一种抗体-药物偶联物及其制备方法和应用
US10517958B2 (en) 2016-10-04 2019-12-31 Zymeworks Inc. Compositions and methods for the treatment of platinum-drug resistant cancer
KR102562760B1 (ko) * 2016-11-25 2023-08-04 맵웰 (상하이) 바이오사이언스 컴퍼니, 리미티드 항체-약물 접합을 위한 이-치환된 말레익 아미드 링커 및 이의 제조 방법 및 용도
CN108101825B (zh) * 2016-11-25 2022-02-22 迈威(上海)生物科技股份有限公司 用于抗体-药物偶联的双取代马来酰胺类连接子及其制备方法和用途
CN109810039B (zh) * 2017-11-22 2021-11-12 迈威(上海)生物科技股份有限公司 一种用于抗体-药物偶联的双取代马来酰胺类连接子及其制备方法和用途
US10864279B2 (en) 2016-12-16 2020-12-15 Industrial Technology Research Institute Linker-drug and antibody-drug conjugate (ADC) employing the same
MX2019008199A (es) 2017-01-06 2019-11-25 Avidity Biosciences Llc Composiciones de acido nucleico polipeptido y metodos de induccion de la omision de exon.
CN110461876B (zh) 2017-01-20 2024-05-17 海德堡医药研究有限责任公司 用于耗尽cd137+细胞的组合物和方法
WO2018175994A1 (en) 2017-03-24 2018-09-27 Seattle Genetics, Inc. Process for the preparation of glucuronide drug-linkers and intermediates thereof
BR112019020049A2 (pt) * 2017-04-06 2020-05-12 Hangzhou Dac Biotech Co., Ltd Composto conjungado, célula tumoral, composição farmacêutica, e, agentes sinérgicos.
US11207420B2 (en) 2017-04-19 2021-12-28 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Cytotoxin and conjugate, uses of same and preparation method therefor
US11491145B2 (en) 2017-06-20 2022-11-08 Madrigal Pharmaceuticals, Inc. Combination therapies comprising targeted therapeutics
CA3067572A1 (en) 2017-06-20 2018-12-27 Madrigal Pharmaceuticals, Inc. Targeted therapeutics
WO2018235024A1 (en) * 2017-06-20 2018-12-27 Sorrento Therapeutics, Inc. Cd38 antibody drug conjugate
GB201711809D0 (en) 2017-07-21 2017-09-06 Governors Of The Univ Of Alberta Antisense oligonucleotide
WO2019023247A1 (en) 2017-07-25 2019-01-31 Immutics, Inc. TREATMENT OF CANCER BY BLOCKING THE INTERACTION OF TIM-3 AND ITS LIGAND
US10799598B2 (en) 2017-08-01 2020-10-13 Sorrento Therapeutics, Inc. Disulfide bridging conjugates
CN111051329B (zh) 2017-08-10 2024-07-30 住友制药株式会社 哈米特林衍生物及它们的抗体药物复合物
BR112020004495A2 (pt) 2017-09-08 2020-09-08 Seattle Genetics, Inc. composto, composição, e, método para preparar uma composição.
WO2019071028A1 (en) 2017-10-04 2019-04-11 Avidity Biosciences Llc NUCLEIC ACID-POLYPEPTIDE COMPOSITIONS AND USES THEREOF
US11612666B2 (en) * 2017-11-30 2023-03-28 Seagen Inc. Process for the preparation of drug linker compounds
WO2019113393A1 (en) 2017-12-06 2019-06-13 Avidity Biosciences Llc Compositions and methods of treating muscle atrophy and myotonic dystrophy
CA3080236A1 (en) 2017-12-15 2019-06-20 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Bioactive molecule conjugate, preparation method and use thereof
CN111447939B (zh) * 2018-01-30 2024-07-12 四川科伦博泰生物医药股份有限公司 制备偶联物的方法
AU2019225845B2 (en) * 2018-02-20 2024-06-20 Seagen Inc. Hydrophobic Auristatin F compounds and conjugates thereof
US12172986B2 (en) 2018-06-01 2024-12-24 Eisai R&D Management Co., Ltd Splicing modulator antibody-drug conjugates and methods of use
US11998544B2 (en) 2018-06-01 2024-06-04 Eisai R&D Management Co., Ltd. Methods of using splicing modulators
US20210276971A1 (en) 2018-06-20 2021-09-09 The Research Foundation For The State University Of New York Triazamacrocycle-derived chelator compositions for coordination of imaging and therapy metal ions and methods of using same
AU2018445278B2 (en) * 2018-10-12 2022-07-28 Hangzhou Dac Biotech Co., Ltd Conjugation linkers containing 2,3-diaminosuccinyl group
WO2020081493A1 (en) 2018-10-16 2020-04-23 Molecular Templates, Inc. Pd-l1 binding proteins
CA3114931A1 (en) 2018-12-13 2020-06-18 Eisai R&D Management Co., Ltd. Herboxidiene antibody-drug conjugates and methods of use
EP3897734A4 (en) * 2018-12-21 2022-12-07 Seagen Inc. ADC COMPRISING MULTIPLEX THIOL LINKERS
IL319265A (en) 2018-12-21 2025-04-01 Avidity Biosciences Inc Anti-transferrin receptor antibodies and their uses
EP3918323A4 (en) 2019-01-30 2022-12-28 TrueBinding, Inc. ANTI-GAL3 ANTIBODIES AND USES THEREOF
JP7479302B2 (ja) 2019-02-13 2024-05-08 住友ファーマ株式会社 ヘミアスタリン誘導体とその抗体薬物複合体
EP3925668A4 (en) 2019-02-13 2022-11-09 Sumitomo Pharma Co., Ltd. HEMIASTERLINE DERIVATIVE WITH CYSTEINE RESIDUES
CN109824759A (zh) * 2019-03-08 2019-05-31 联宁（苏州）生物制药有限公司 一种用于抗体药物偶联物的药物-连接子mc-mmaf的制备方法及其中间体
AU2020263487A1 (en) 2019-04-25 2021-12-16 Avidity Biosciences, Inc. Nucleic acid compositions and methods of multi-exon skipping
JP7581252B2 (ja) 2019-06-06 2024-11-12 アビディティー バイオサイエンシーズ，インク． Ｕｎａアミダイトおよびその使用
US11578090B2 (en) 2019-06-06 2023-02-14 Avidity Biosciences, Inc. Nucleic acid-polypeptide compositions and uses thereof
WO2021055816A1 (en) 2019-09-18 2021-03-25 Molecular Templates, Inc. Pd-l1 binding molecules comprising shiga toxin a subunit scaffolds
CN115768483A (zh) 2020-01-13 2023-03-07 西纳福克斯股份有限公司 抗体与免疫细胞衔接器的缀合物
JP2023511857A (ja) 2020-01-13 2023-03-23 シンアフィックス ビー．ブイ． 付加環化を介して両側官能化された抗体
WO2021144314A1 (en) 2020-01-13 2021-07-22 Synaffix B.V. Via cycloaddition bilaterally functionalized antibodies
EP4110817A1 (en) 2020-02-26 2023-01-04 Sorrento Therapeutics, Inc. Activatable antigen binding proteins with universal masking moieties
BR112022018002A2 (pt) * 2020-03-09 2022-11-08 Sigma Aldrich Co Llc Preparação eficiente de análogos de dolastatina e auristatina por meio de um intermediário comum
TW202144572A (zh) 2020-03-19 2021-12-01 美商亞維代堤生物科學公司 治療臉肩胛肱骨肌肉失養症之組合物及方法
WO2021195469A1 (en) 2020-03-27 2021-09-30 Avidity Biosciences, Inc. Compositions and methods of treating muscle dystrophy
US10987487B1 (en) 2020-04-29 2021-04-27 Cure Medical Llc Gripper sleeve for urinary catheter
WO2021242776A2 (en) 2020-05-26 2021-12-02 Truebinding, Inc. Methods of treating inflammatory diseases by blocking galectin-3
BR112022024833A2 (pt) 2020-06-05 2023-02-14 Eisai R&D Man Co Ltd Conjugados anticorpo anti-bcma-fármaco e métodos de uso
EP4172141A1 (en) 2020-06-26 2023-05-03 Synaffix B.V. Methods for the preparation of linker payload constructs
NL2026400B1 (en) 2020-09-02 2022-05-04 Synaffix Bv Methods for the preparation of bioconjugates
EP4208259A2 (en) 2020-09-04 2023-07-12 NovaRock Biotherapeutics, Ltd. Nectin-4 antibodies and uses thereof
WO2022058395A1 (en) 2020-09-15 2022-03-24 Synaffix B.V. Antibody-exatecan conjugates
NL2026947B1 (en) 2020-11-20 2022-07-01 Synaffix Bv Tyrosine-based antibody conjugates
UY39587A (es) 2020-12-23 2022-07-29 Univ Muenchen Ludwig Maximilians Conjugados anticuerpo-droga mejorados dirigidos contra cd30 y usos de los mismos
US20230390411A1 (en) * 2021-01-28 2023-12-07 Nanjing Chempion Biotechnology Co., Ltd. Conjugate and use thereof
US20250262314A1 (en) 2021-02-08 2025-08-21 Synaffix B.V. Multifunctional antibodies
EP4301418A1 (en) 2021-03-03 2024-01-10 Sorrento Therapeutics, Inc. Antibody-drug conjugates comprising an anti-bcma antibody
CA3213295A1 (en) 2021-03-17 2022-09-22 Molecular Templates, Inc. Pd-l1 binding proteins comprising shiga toxin a subunit scaffolds and cd8+ t cell antigens
CN116897149A (zh) * 2021-03-30 2023-10-17 上海复旦张江生物医药股份有限公司 一种连接基药物偶联物的制备方法及其中间体
JP2024526764A (ja) 2021-07-13 2024-07-19 トゥルーバインディング，インコーポレイテッド タンパク質凝集を防止する方法
CN118265544A (zh) 2021-09-16 2024-06-28 艾维迪提生物科学公司 治疗面肩肱型肌营养不良的组合物和方法
WO2023086768A1 (en) 2021-11-09 2023-05-19 Truebinding, Inc. Methods of treating or inhibiting cardiovascular diseases
WO2023122347A2 (en) 2021-12-23 2023-06-29 Mirecule, Inc. Compositions for delivery of polynucleotides
WO2023173026A1 (en) 2022-03-10 2023-09-14 Sorrento Therapeutics, Inc. Antibody-drug conjugates and uses thereof
US12071621B2 (en) 2022-04-05 2024-08-27 Avidity Biosciences, Inc. Anti-transferrin receptor antibody-PMO conjugates for inducing DMD exon 44 skipping
KR20250054842A (ko) 2022-07-29 2025-04-23 리제너론 파마슈티칼스 인코포레이티드 뇌 및 근육으로의 트랜스페린 수용체(tfr)-매개 전달을 위한 조성물 및 방법
JP2025526869A (ja) 2022-08-15 2025-08-15 シンアフィックス ビー．ブイ． アントラサイクリン及びそのコンジュゲート
AU2023350248A1 (en) 2022-09-30 2025-04-17 Shanghai De Novo Pharmatech Co., Ltd. Benzazepine derivative, conjugate containing same, and use thereof
WO2024107765A2 (en) 2022-11-14 2024-05-23 Regeneron Pharmaceuticals, Inc. Compositions and methods for fibroblast growth factor receptor 3-mediated delivery to astrocytes
EP4389152A1 (en) 2022-12-23 2024-06-26 Synaffix B.V. Conjugates of pbd prodrugs
CN116621927B (zh) * 2023-01-09 2024-03-26 联宁（苏州）生物制药有限公司 带有伊喜替康和C-lock定点偶联基团的抗体偶联中间体、偶联方法及抗体偶联药物
EP4410313A1 (en) 2023-01-31 2024-08-07 Synaffix B.V. Homogeneous antibody-conjugates with high payload loading
AU2024229817A1 (en) 2023-02-28 2025-08-14 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Chemical coupling linker and use thereof
WO2024211236A2 (en) 2023-04-05 2024-10-10 Sorrento Therapeutics, Inc. Antibody-drug conjugates and uses thereof
WO2024211234A1 (en) 2023-04-05 2024-10-10 Sorrento Therapeutics, Inc. Antibody-drug conjugates and uses thereof
WO2024211235A1 (en) 2023-04-05 2024-10-10 Sorrento Therapeutics, Inc. Antibody-drug conjugates and uses thereof
WO2024218164A1 (en) 2023-04-17 2024-10-24 Synaffix B.V. Stable 4-isoxazoline conjugates
EP4450093A1 (en) 2023-04-17 2024-10-23 Synaffix B.V. Cleavable immune cell engagers
US12491257B2 (en) 2023-06-27 2025-12-09 Avidity Biosciences, Inc. Compositions and methods of using PRKAG2-targeting antibody-oligonucleotide conjugates
US12409230B2 (en) 2023-06-30 2025-09-09 Avidity Biosciences, Inc. Compositions comprising PLN-targeting anti-transferrin receptor antibody-polynucleotides and methods of use thereof to treat cardiomyopathy
WO2025027529A1 (en) 2023-07-31 2025-02-06 Advesya Anti-il-1rap antibody drug conjugates and methods of use thereof
WO2025126157A1 (en) 2023-12-15 2025-06-19 Advesya Anti-il-1rap binding domains and antibody-drug conjugates thereof
CN117964682A (zh) * 2024-01-12 2024-05-03 杭州爱科瑞思生物医药有限公司 Dolastatin衍生物及其制备方法和应用
WO2025238253A1 (en) 2024-05-16 2025-11-20 Synaffix B.V. Antibody-oligonucleotide conjugates

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008521920A (ja) * 2004-12-01 2008-06-26 ジェネンテック・インコーポレーテッド 抗体薬剤結合体および方法
US7767205B2 (en) * 2005-01-31 2010-08-03 Genentech, Inc. Anti-EphB2 antibodies and methods using same
CN102133407A (zh) * 2002-03-01 2011-07-27 图兰恩教育基金管理人 治疗剂或细胞毒性剂与生物活性肽的偶联物
US7994135B2 (en) * 2003-11-06 2011-08-09 Seattle Genetics, Inc. Monomethylvaline compounds capable of conjugation to ligands
EP2376110A1 (en) * 2009-01-09 2011-10-19 Seattle Genetics, Inc. Weekly dosing regimens for anti-cd30 vc-pab-mmae antibody drug-conjugates

Family Cites Families (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4783443A (en) 1986-03-03 1988-11-08 The University Of Chicago Amino acyl cephalosporin derivatives
US6569834B1 (en) * 1992-12-03 2003-05-27 George R. Pettit Elucidation and synthesis of antineoplastic tetrapeptide w-aminoalkyl-amides
US5780588A (en) 1993-01-26 1998-07-14 Arizona Board Of Regents Elucidation and synthesis of selected pentapeptides
US6214345B1 (en) 1993-05-14 2001-04-10 Bristol-Myers Squibb Co. Lysosomal enzyme-cleavable antitumor drug conjugates
ES2233928T3 (es) * 1993-10-01 2005-06-16 Teikoku Hormone Mfg. Co., Ltd. Derivados de dolastatina.
US5525474A (en) * 1994-01-31 1996-06-11 Boehringer Mannheim Corporation Piperidine analogs and conjugates of procainamide and NAPA
CA2427146A1 (en) 2000-10-25 2002-07-18 Mayo Foundation For Medical Education And Research Transcobalamin binding conjugates useful for treating abnormal cellular proliferation
US20090068178A1 (en) * 2002-05-08 2009-03-12 Genentech, Inc. Compositions and Methods for the Treatment of Tumor of Hematopoietic Origin
AU2003266233A1 (en) 2002-07-09 2004-01-23 Morphochem Aktiengesellschaft Fur Kombinatorische Chemie Novel tubulysin analogues
JP4741838B2 (ja) 2002-07-31 2011-08-10 シアトル ジェネティクス，インコーポレーテッド 癌、自己免疫疾患または感染症を治療するための薬物結合体およびその使用
DE10254439A1 (de) * 2002-11-21 2004-06-03 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) Tubulysine, Herstellungsverfahren und Tubulysin-Mittel
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
US7276497B2 (en) 2003-05-20 2007-10-02 Immunogen Inc. Cytotoxic agents comprising new maytansinoids
ZA200601182B (en) * 2003-10-10 2007-04-25 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
EP3088004B1 (en) * 2004-09-23 2018-03-28 Genentech, Inc. Cysteine engineered antibodies and conjugates
US20070134243A1 (en) 2004-12-01 2007-06-14 Gazzard Lewis J Antibody drug conjugates and methods
PL1912671T3 (pl) * 2005-07-18 2018-02-28 Seattle Genetics, Inc. Koniugaty beta-glukuronid-linker-lek
CN101312748A (zh) * 2005-09-26 2008-11-26 梅达莱克斯公司 抗体-药物轭合物和使用方法
AR059900A1 (es) * 2006-03-17 2008-05-07 Genentech Inc Anticuerpos anti-tat226 e inmunoconjugados
UY30391A1 (es) 2006-06-06 2008-01-31 Enanta Pharm Inc Compuesto de oximilo aciclico inhibidores de proteasa de hepatitis c
WO2008019403A1 (en) * 2006-08-11 2008-02-14 University Of Medicine And Dentistry Of New Jersey Dual-sensitizer-containing luminescent compounds, conjugates, and uses thereof
JP5274461B2 (ja) * 2006-08-18 2013-08-28 アローヘッド リサーチ コーポレイション ポリヌクレオチドのインビボ送達のためのポリ結合体
NZ599239A (en) * 2007-03-14 2013-10-25 Endocyte Inc Binding ligand linked drug delivery conjugates of tubulysins
WO2008128164A1 (en) 2007-04-12 2008-10-23 The Penn State Research Foundation Accumulation field effect microelectronic device and process for the formation thereof
US9138484B2 (en) * 2007-06-25 2015-09-22 Endocyte, Inc. Conjugates containing hydrophilic spacer linkers
WO2009012958A2 (en) 2007-07-20 2009-01-29 Helmholtz-Zentrum für Infektionsforschung GmbH Tubulysin d analogues
US8900589B2 (en) 2008-07-15 2014-12-02 Genetech, Inc. Anthracycline derivative conjugates, process for their preparation and their use as antitumor compounds
AU2009293140A1 (en) * 2008-09-17 2010-03-25 Endocyte, Inc. Folate receptor binding conjugates of antifolates
EP2174947A1 (en) 2008-09-25 2010-04-14 Universität des Saarlandes Bioactive pre-tubulysins and use thereof
EP2403538B1 (en) 2009-03-04 2017-10-04 Polytherics Limited Conjugated proteins and peptides
US8394922B2 (en) * 2009-08-03 2013-03-12 Medarex, Inc. Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
ES2668645T3 (es) 2010-02-08 2018-05-21 Agensys, Inc. Conjugados de fármaco y anticuerpo (ADC) que se unen a proteínas 161P2F10B
AU2011261362B2 (en) * 2010-06-03 2016-06-09 Genentech, Inc. Immuno-pet imaging of antibodies and immunoconjugates and uses therefor
CA2799540A1 (en) * 2010-06-08 2011-12-15 Genentech, Inc. Cysteine engineered antibodies and conjugates
EP2409983A1 (en) 2010-07-19 2012-01-25 Leibniz-Institut für Pflanzenbiochemie (IPB) Tubulysin analogues
WO2012041805A1 (de) 2010-09-29 2012-04-05 Bayer Pharma Aktiengesellschaft N-carboxyalkyl-auristatine und ihre verwendung
WO2012073217A1 (en) 2010-12-02 2012-06-07 Nerviano Medical Sciences S.R.L. Process for the preparation of morpholinyl anthracycline derivatives
US9796754B2 (en) 2011-05-27 2017-10-24 Ambrx, Inc. Compositions containing, methods involving, and uses of non-natural amino acid linked dolastatin derivatives
SG10201605293PA (en) 2011-05-27 2016-08-30 Ambrx Inc Compositions containing, methods involving, and uses of non-natural amino acid linked dolastatin derivatives
US8815226B2 (en) 2011-06-10 2014-08-26 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
BR112013032928A2 (pt) 2011-06-21 2017-01-24 Immunogen Inc "derivados de maitansinoide com ligante de peptídeo e conjugados dos mesmos, composição farmacêutica que os compreende e uso dos mesmos"
CA2857398A1 (en) 2011-12-05 2013-06-13 Igenica Biotherapeutics, Inc. Antibody-drug conjugates and related compounds, compositions, and methods
WO2013173391A1 (en) 2012-05-15 2013-11-21 Concortis Biosystems, Corp Drug-conjugates, conjugation methods, and uses thereof
EP3536700A1 (en) * 2012-06-07 2019-09-11 Ambrx, Inc. Prostate-specific membrane antigen antibody drug conjugates
IL278638B1 (en) * 2012-06-19 2025-09-01 Ambrx Inc Anti-CD70 antibody drug conjugates
EP2869847B1 (en) 2012-07-09 2017-12-06 Genentech, Inc. Immunoconjugates comprising anti-cd79b antibodies
CN106132431A (zh) * 2013-10-15 2016-11-16 索伦托治疗有限公司 具有靶向分子和两种不同药物的药物偶联物
EP3250238B1 (en) 2015-01-28 2022-06-01 Sorrento Therapeutics, Inc. Antibody drug conjugates
CN107635405A (zh) 2015-02-06 2018-01-26 索伦托医疗有限公司 抗体药物缀合物

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102133407A (zh) * 2002-03-01 2011-07-27 图兰恩教育基金管理人 治疗剂或细胞毒性剂与生物活性肽的偶联物
US7994135B2 (en) * 2003-11-06 2011-08-09 Seattle Genetics, Inc. Monomethylvaline compounds capable of conjugation to ligands
JP2008521920A (ja) * 2004-12-01 2008-06-26 ジェネンテック・インコーポレーテッド 抗体薬剤結合体および方法
US7767205B2 (en) * 2005-01-31 2010-08-03 Genentech, Inc. Anti-EphB2 antibodies and methods using same
EP2376110A1 (en) * 2009-01-09 2011-10-19 Seattle Genetics, Inc. Weekly dosing regimens for anti-cd30 vc-pab-mmae antibody drug-conjugates

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