JP6239598B2 - 薬物複合体、複合体形成方法、およびその使用 - Google Patents

薬物複合体、複合体形成方法、およびその使用 Download PDF

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JP6239598B2
JP6239598B2 JP2015512770A JP2015512770A JP6239598B2 JP 6239598 B2 JP6239598 B2 JP 6239598B2 JP 2015512770 A JP2015512770 A JP 2015512770A JP 2015512770 A JP2015512770 A JP 2015512770A JP 6239598 B2 JP6239598 B2 JP 6239598B2
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lys
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JP2015518832A (ja
JP2015518832A5 (cg-RX-API-DMAC7.html
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ジェンウェイ・ミャオ
ユーフォン・ホン
トン・ジュウ
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Sorrento Therapeutics Inc
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    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
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    • A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
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    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
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  • Health & Medical Sciences (AREA)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
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  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Cell Biology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
JP2015512770A 2012-05-15 2013-05-14 薬物複合体、複合体形成方法、およびその使用 Active JP6239598B2 (ja)

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US201261647300P 2012-05-15 2012-05-15
US61/647,300 2012-05-15
US201261648532P 2012-05-17 2012-05-17
US201261648406P 2012-05-17 2012-05-17
US61/648,532 2012-05-17
US61/648,406 2012-05-17
US201261652512P 2012-05-29 2012-05-29
US61/652,512 2012-05-29
PCT/US2013/041027 WO2013173392A1 (en) 2012-05-15 2013-05-14 Drug-conjugates, conjugation methods, and uses thereof

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Families Citing this family (142)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1789391B1 (en) 2004-07-23 2017-06-28 Endocyte, Inc. Bivalent linkers and conjugates thereof
CA2680535C (en) 2007-03-14 2016-09-20 Endocyte, Inc. Binding ligand linked drug delivery conjugates of tubulysins
CA2690943A1 (en) 2007-06-25 2008-12-31 Endocyte, Inc. Conjugates containing hydrophilic spacer linkers
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
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
US20140079636A1 (en) 2012-04-16 2014-03-20 Dinesh U. Chimmanamada Targeted therapeutics
ES2887208T3 (es) 2012-05-15 2021-12-22 Concortis Biosystems Corp Conjugados de fármacos y usos de los mismos
IN2015DN04147A (cg-RX-API-DMAC7.html) 2012-10-16 2015-10-16 Endocyte Inc
RU2015129800A (ru) 2012-12-21 2017-01-30 Биоэллаенс К. В. Гидрофильные саморазрушающиеся линкеры и их конъюгаты
CN110143999B (zh) 2013-03-15 2023-12-05 酵活英属哥伦比亚省公司 具细胞毒性和抗有丝分裂的化合物以及其使用方法
CA2914448A1 (en) 2013-06-12 2014-12-18 Muhammad Naveed Yousaf Compounds for promoting liposomal and cellular adhesion and compositions and methods of use thereof
WO2015038649A1 (en) 2013-09-10 2015-03-19 Synta Pharmaceuticals Corp. Targeted therapeutics
CA3187392A1 (en) 2013-10-15 2015-04-23 Seagen Inc. Pegylated drug-linkers for improved ligand-drug conjugate pharmacokinetics
RU2016134258A (ru) 2013-10-15 2018-02-28 Сорренто Терапьютикс Инк. Конъюгат лекарственного средства с направляющей молекулой и двумя различными лекарственными средствами
WO2015066053A2 (en) 2013-10-28 2015-05-07 Synta Pharmaceuticals Corp. Targeted therapeutics
KR20160125361A (ko) 2013-12-27 2016-10-31 자임워크스 인코포레이티드 Ｖａｒ２ｃｓａ－약물 접합체
JP6560681B2 (ja) 2013-12-27 2019-08-14 ザイムワークス インコーポレイティド 薬物結合体のためのスルホンアミド含有連結系
AU2015213106B2 (en) * 2014-01-28 2019-07-25 Tube Pharmaceuticals Gmbh Cytotoxic tubulysin compounds for conjugation
JP2017505777A (ja) 2014-01-29 2017-02-23 シンタ ファーマスーティカルズ コーポレーション 標的化治療薬
GB201402006D0 (en) * 2014-02-06 2014-03-26 Oncomatryx Biopharma S L Antibody-drug conjugates and immunotoxins
EP3129064B1 (en) 2014-03-03 2020-01-01 Madrigal Pharmaceuticals, Inc. Targeted therapeutics
EP3131586A4 (en) 2014-03-18 2017-10-25 Madrigal Pharmaceuticals, Inc. Targeted therapeutics
ES2883023T3 (es) * 2014-05-28 2021-12-03 Agensys Inc Derivados de péptidos de dolaproína-dolaisoleuina citotóxicos para el tratamiento del cáncer
US9950077B2 (en) 2014-06-20 2018-04-24 Bioalliance C.V. Anti-folate receptor alpha (FRA) antibody-drug conjugates and methods of using thereof
PL3169706T3 (pl) 2014-07-11 2020-05-18 Genmab A/S Przeciwciała wiążące axl
CN107108694B (zh) * 2014-09-11 2022-05-03 西雅图基因公司 含叔胺药物物质的靶向递送
KR102494557B1 (ko) 2014-09-17 2023-02-02 자임워크스 비씨 인코포레이티드 세포독성 및 항유사분열성 화합물, 그리고 이를 이용하는 방법
KR20230158134A (ko) 2014-10-14 2023-11-17 폴리테릭스 리미티드 Peg의 일부를 포함하는 이탈기를 포함하는 시약을 사용한, 펩티드 또는 단백질의 접합방법
US10077287B2 (en) 2014-11-10 2018-09-18 Bristol-Myers Squibb Company Tubulysin analogs and methods of making and use
SG11201704458SA (en) * 2014-12-08 2017-06-29 Sorrento Therapeutics Inc C-met antibody drug conjugate
US9968683B2 (en) 2014-12-17 2018-05-15 Organolinx Corp. Method for conjugating molecules
CN107849090A (zh) * 2015-01-28 2018-03-27 索伦托医疗有限公司 抗体药物偶联物
WO2016127081A1 (en) * 2015-02-06 2016-08-11 Sorrento Therapeutics, Inc. Antibody drug conjugates
BR112017016503A2 (pt) * 2015-02-15 2018-04-10 Jiangsu Hengrui Medicine Co., Ltd. conjugado de fármaco de citotoxicidade-ligante, método de preparação para o mesmo, e aplicação para o mesmo
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
US10449258B2 (en) 2015-06-09 2019-10-22 Xdcexplorer (Shanghai) Co., Ltd. Antibody drug conjugate, intermediate, preparation method, pharmaceutical composition and uses thereof
CN108368171A (zh) 2015-07-10 2018-08-03 根马布股份公司 用于癌症治疗的axl特异性抗体-药物缀合物
CA2991973C (en) 2015-07-12 2021-12-07 Suzhou M-Conj Biotech Co., Ltd. Bridge linkers for conjugation of a cell-binding molecule
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
CA3006000A1 (en) 2015-12-04 2017-06-08 Seattle Genetics, Inc. Conjugates of quaternized tubulysin compounds
MX395252B (es) 2016-01-08 2025-03-25 Altrubio Inc Anticuerpos tetravalentes anti ligando-1 de glicoproteina p-selectina (psgl-1) y usos de estos.
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
RS62108B1 (sr) 2016-03-02 2021-08-31 Eisai R&D Man Co Ltd Antitelo-lek konjugati na bazi eribulina i postupci primene
JP7073266B2 (ja) 2016-03-25 2022-05-23 シージェン インコーポレイテッド Ｐｅｇ化薬物リンカー及びその中間体を調製するためのプロセス
EP3438118B1 (en) * 2016-03-29 2023-03-29 Toray Industries, Inc. Peptide derivative and use thereof
US20170281758A1 (en) * 2016-03-29 2017-10-05 Sorrento Therapeutics, Inc. Calicheamicin antibody drug conjugates linking an amidoacetyl group to a sugar moiety on calicheamicin
MA45328A (fr) 2016-04-01 2019-02-06 Avidity Biosciences Llc Compositions acide nucléique-polypeptide et utilisations de celles-ci
CA3025931A1 (en) * 2016-05-31 2017-12-07 Sorrento Therapeutics, Inc. Antibody drug conjugates having derivatives of amatoxin as the drug
US10111966B2 (en) 2016-06-17 2018-10-30 Magenta Therapeutics, Inc. Methods for the depletion of CD117+ cells
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
CN110088086B (zh) * 2016-11-25 2022-12-16 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
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
JP7573966B2 (ja) 2017-01-06 2024-10-28 アビディティー バイオサイエンシーズ，インク． エクソンスキッピングを誘導する核酸ポリペプチド組成物および方法
SG10202102897PA (en) 2017-01-20 2021-04-29 Magenta Therapeutics Inc Compositions and methods for the depletion of cd137+ cells
US11730822B2 (en) 2017-03-24 2023-08-22 Seagen Inc. Process for the preparation of glucuronide drug-linkers and intermediates thereof
US20200069814A1 (en) * 2017-04-06 2020-03-05 Hangzhou Dac Biotech Co., Ltd. Conjugation of a cytotoxic drug with bis-linkage
WO2018192407A1 (zh) 2017-04-19 2018-10-25 四川科伦博泰生物医药股份有限公司 细胞毒素和偶联物、其用途和制备方法
CA3067311A1 (en) * 2017-06-20 2018-12-27 Sorrento Therapeutics, Inc. Cd38 antibody drug conjugate
KR20200016875A (ko) 2017-06-20 2020-02-17 마드리갈 파마슈티칼스 인코포레이티드 표적화 치료제
IL299892A (en) 2017-06-20 2023-03-01 Madrigal Pharmaceuticals Inc Combination therapies that include prescribed medications
GB201711809D0 (en) 2017-07-21 2017-09-06 Governors Of The Univ Of Alberta Antisense oligonucleotide
CN111201030B (zh) 2017-07-25 2024-11-01 真和制药有限公司 通过阻断tim-3和其配体的相互作用治疗癌症
US10799598B2 (en) 2017-08-01 2020-10-13 Sorrento Therapeutics, Inc. Disulfide bridging conjugates
TWI799438B (zh) 2017-08-10 2023-04-21 日商住友製藥股份有限公司 半星芒體衍生物及此等之抗體藥物複合體
MA50124A (fr) 2017-09-08 2020-07-15 Seattle Genetics Inc Procédé de préparation de tubulysines et d'intermédiaires de celles-ci
CN118267396A (zh) 2017-10-04 2024-07-02 艾维迪提生物科学公司 核酸-多肽组合物及其用途
KR102762352B1 (ko) * 2017-11-30 2025-02-05 씨젠 인크. 약물 링커 화합물의 제조방법
IL319835A (en) 2017-12-06 2025-05-01 Avidity Biosciences Inc Compositions and methods for treating muscular dystrophy and myotonic dystrophy
CN120248020B (zh) 2017-12-15 2025-10-03 四川科伦博泰生物医药股份有限公司 生物活性物偶联物及其制备方法和用途
WO2019149116A1 (zh) * 2018-01-30 2019-08-08 四川科伦博泰生物医药股份有限公司 制备偶联物的方法
CN111989339A (zh) * 2018-02-20 2020-11-24 西雅图基因公司 疏水性奥瑞他汀f化合物及其缀合物
CN112367996B (zh) 2018-06-01 2024-05-24 卫材R&D管理有限公司 使用剪接调节剂的方法
JP7390315B2 (ja) 2018-06-01 2023-12-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 スプライシング調節薬抗体－薬物コンジュゲート及びその使用方法
WO2019246445A1 (en) 2018-06-20 2019-12-26 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
SG11202103424UA (en) * 2018-10-12 2021-05-28 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
IL319265A (en) 2018-12-21 2025-04-01 Avidity Biosciences Inc Anti-transferrin receptor antibodies and their uses
US20220040320A1 (en) * 2018-12-21 2022-02-10 Seagen Inc. Adcs with thiol multiplex linkers
CA3127113A1 (en) 2019-01-30 2020-08-06 Dongxu Sun Anti-gal3 antibodies and uses thereof
WO2020166600A1 (ja) 2019-02-13 2020-08-20 大日本住友製薬株式会社 システイン残基を有するヘミアスタリン誘導体
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
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
CA3137715A1 (en) 2019-04-25 2020-10-29 Avidity Biosciences, Inc. Nucleic acid compositions and methods of multi-exon skipping
AU2020289464B2 (en) 2019-06-06 2025-12-04 Avidity Biosciences, Inc. Nucleic acid-polypeptide compositions and uses thereof
CN114375297A (zh) 2019-06-06 2022-04-19 艾维迪提生物科学公司 Una亚酰胺及其用途
US11918649B2 (en) 2019-09-18 2024-03-05 Molecular Templates, Inc. PD-L1-binding molecules comprising Shiga toxin a subunit scaffolds
WO2021144315A1 (en) 2020-01-13 2021-07-22 Synaffix B.V. Conjugates of antibodies an immune cell engagers
WO2021144314A1 (en) 2020-01-13 2021-07-22 Synaffix B.V. Via cycloaddition bilaterally functionalized antibodies
WO2021144313A1 (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
CA3170633A1 (en) * 2020-03-09 2021-09-16 David Goeddel Efficient preparation of dolastatin and auristatin analogs through a common intermediate
KR20220156867A (ko) 2020-03-19 2022-11-28 어비디티 바이오사이언시스 인크. 안면견갑상완 근이영양증의 치료용 조성물 및 방법
EP4126066B1 (en) 2020-03-27 2025-11-19 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
JP2023528797A (ja) 2020-05-26 2023-07-06 トゥルーバインディング，インコーポレイテッド ガレクチン－３を遮断することにより炎症性疾患を処置する方法
MX2022015374A (es) 2020-06-05 2023-01-16 Eisai R&D Man Co Ltd Conjugados de anticuerpo anti antigeno de maduracion de linfocitos b (bcma)-farmaco y metodos de uso.
WO2021260232A1 (en) 2020-06-26 2021-12-30 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
CA3193584A1 (en) 2020-09-04 2022-03-10 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
MX2023007126A (es) 2020-12-23 2023-09-04 Univ Muenchen Ludwig Maximilians Conjugados anticuerpo-droga mejorados dirigidos contra cd30 y usos de los mismos.
WO2022161452A1 (zh) * 2021-01-28 2022-08-04 南京桦冠生物技术有限公司 缀合物及其用途
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
US20250026838A1 (en) 2021-07-13 2025-01-23 Truebinding, Inc. Methods of preventing protein aggregation
EP4401792A4 (en) 2021-09-16 2025-12-03 Avidity Biosciences Inc COMPOSITIONS AND METHODS OF TREATMENT OF FACIO-SCAPULO-HUMERAL MUSCULAR DYSTROPHY
CN118524852A (zh) 2021-11-09 2024-08-20 真和制药有限公司 治疗或抑制心血管疾病的方法
AU2022422149A1 (en) 2021-12-23 2024-08-01 Mirecule, Inc. Compositions for delivery of polynucleotides
EP4489790A1 (en) 2022-03-10 2025-01-15 Vivasor, 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
IL318625A (en) 2022-07-29 2025-03-01 Regeneron Pharma Compositions and methods for transferrin receptor (TFR)-mediated delivery to brain and muscle
CN119997985A (zh) 2022-08-15 2025-05-13 西纳福克斯股份有限公司 蒽环类药物及其缀合物
CN117801107A (zh) 2022-09-30 2024-04-02 上海迪诺医药科技有限公司 苯并氮杂卓衍生物、含其的偶联物及其应用
US20240173426A1 (en) 2022-11-14 2024-05-30 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
EP4674840A1 (en) 2023-02-28 2026-01-07 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Chemical coupling linker and use thereof
WO2024211235A1 (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
WO2024211236A2 (en) 2023-04-05 2024-10-10 Sorrento Therapeutics, Inc. Antibody-drug conjugates and uses thereof
EP4450093A1 (en) 2023-04-17 2024-10-23 Synaffix B.V. Cleavable immune cell engagers
KR20250169628A (ko) 2023-04-17 2025-12-03 시나픽스 비.브이. 절단 가능한 면역 세포 인게이저
WO2025006639A2 (en) 2023-06-27 2025-01-02 Avidity Biosciences, Inc. Compositions and methods of using prkag2-targeting antibody-oligonucleotide conjugates abstract
WO2025007063A1 (en) 2023-06-30 2025-01-02 Avidity Biosciences, Inc. Compositions and methods of using pln-targeting antibody-oligonucleotide conjugates
WO2025027529A1 (en) 2023-07-31 2025-02-06 Advesya Anti-il-1rap antibody drug conjugates and methods of use thereof
TW202530255A (zh) 2023-12-15 2025-08-01 法商亞維西亞有限公司 抗ｉｌ－１ｒａｐ結合結構域及其抗體－藥物偶聯物
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

Family Cites Families (54)

* 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
CA2173150C (en) 1993-10-01 2004-11-30 Kyoichi Sakakibara Novel peptide derivatives
US5525474A (en) * 1994-01-31 1996-06-11 Boehringer Mannheim Corporation Piperidine analogs and conjugates of procainamide and NAPA
US20020151525A1 (en) 2000-10-25 2002-10-17 Collins Douglas A. Transcobalamin receptor binding conjugates useful for treating abnormal cellular proliferation
EP1487493B1 (en) * 2002-03-01 2010-01-20 The Administrators of The Tulane Educational Fund Conjugates of cytotoxic agents and biologically active peptides
US20090068178A1 (en) 2002-05-08 2009-03-12 Genentech, Inc. Compositions and Methods for the Treatment of Tumor of Hematopoietic Origin
DK1523493T3 (da) 2002-07-09 2013-12-02 Alexander Doemling Nye tubulysinanaloge
SI1545613T1 (sl) 2002-07-31 2011-11-30 Seattle Genetics Inc Avristatinski konjugati in njihova uporaba za zdravljenje raka avtoimunske bolezni ali infekcijskebolezni
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
KR101438983B1 (ko) 2003-11-06 2014-09-05 시애틀 지네틱스, 인크. 리간드에 접합될 수 있는 모노메틸발린 화합물
CN104447992A (zh) * 2004-09-23 2015-03-25 健泰科生物技术公司 半胱氨酸改造的抗体和偶联物
JP4993645B2 (ja) * 2004-12-01 2012-08-08 ジェネンテック， インコーポレイテッド 抗体薬剤結合体および方法
US20070134243A1 (en) * 2004-12-01 2007-06-14 Gazzard Lewis J Antibody drug conjugates and methods
WO2006083936A2 (en) * 2005-01-31 2006-08-10 Genentech, Inc. Anti-ephb2 antibodies and methods using same
HUE035853T2 (en) * 2005-07-18 2018-05-28 Seattle Genetics Inc Beta-glucuronide-linker-drug conjugates
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
WO2007146695A1 (en) 2006-06-06 2007-12-21 Enanta Pharmaceuticals, Inc. Acyclic oximyl hepatitis c protease inhibitors
AU2007281709B2 (en) * 2006-08-11 2013-04-18 Rutgers, The State University Of New Jersey Dual-sensitizer-containing luminescent compounds, conjugates, and uses thereof
KR101133799B1 (ko) * 2006-08-18 2012-04-24 에프. 호프만-라 로슈 아게 폴리뉴클레오타이드의 생체내 전달을 위한 다가접합체
CA2680535C (en) 2007-03-14 2016-09-20 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
CA2690943A1 (en) * 2007-06-25 2008-12-31 Endocyte, Inc. Conjugates containing hydrophilic spacer linkers
US20110263650A1 (en) 2007-07-20 2011-10-27 Helmholtz-Zentrum Für Infektions-Forschung Gmbh Tubulysin D Analogues
CN102159248B (zh) 2008-07-15 2013-09-11 健泰科生物技术公司 蒽环类衍生物缀合物、它们的制备方法以及它们作为抗肿瘤化合物的用途
PL2349274T3 (pl) * 2008-09-17 2025-09-22 Endocyte, Inc. Koniugaty antyfolianów wiążące się z receptorem folianów
EP2174947A1 (en) 2008-09-25 2010-04-14 Universität des Saarlandes Bioactive pre-tubulysins and use thereof
US9211319B2 (en) * 2009-01-09 2015-12-15 Seattle Genetics, Inc. Weekly dosing regimens for anti-CD30 VC-PAB-MMAE antibody drug-conjugates
US9005598B2 (en) 2009-03-04 2015-04-14 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
JP6046494B2 (ja) 2010-02-08 2016-12-14 アジェンシス，インコーポレイテッド １６１ｐ２ｆ１０ｂタンパク質に結合する抗体薬物コンジュゲート（ａｄｃ）
KR20130098165A (ko) * 2010-06-03 2013-09-04 제넨테크, 인크. 항체 및 면역접합체의 이뮤노-ｐｅｔ 영상화 및 그의 용도
KR101839163B1 (ko) 2010-06-08 2018-03-15 제넨테크, 인크. 시스테인 조작된 항체 및 접합체
EP2409983A1 (en) 2010-07-19 2012-01-25 Leibniz-Institut für Pflanzenbiochemie (IPB) Tubulysin analogues
ES2553874T3 (es) 2010-09-29 2015-12-14 Seattle Genetics, Inc. N-Carboxialquil-auristatinas y su uso
WO2012073217A1 (en) 2010-12-02 2012-06-07 Nerviano Medical Sciences S.R.L. Process for the preparation of morpholinyl anthracycline 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
US9796754B2 (en) 2011-05-27 2017-10-24 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
WO2012177837A2 (en) 2011-06-21 2012-12-27 Immunogen, Inc. Novel maytansinoid derivatives with peptide linker and conjugates thereof
US20130224228A1 (en) 2011-12-05 2013-08-29 Igenica, Inc. Antibody-Drug Conjugates and Related Compounds, Compositions, and Methods
ES2887208T3 (es) 2012-05-15 2021-12-22 Concortis Biosystems Corp Conjugados de fármacos y usos de los mismos
DK2858676T3 (da) 2012-06-07 2019-05-13 Ambrx Inc Prostata-specifikke membran-antigen-antistof-lægemiddelkonjugater
JP6343609B2 (ja) * 2012-06-19 2018-06-13 アンブルックス, インコーポレイテッドAmbrx, Inc. 抗ｃｄ７０抗体薬物複合体
MX2015000314A (es) 2012-07-09 2015-04-10 Genentech Inc Anticuerpos anti-cd79b e inmunoconjugados.
RU2016134258A (ru) 2013-10-15 2018-02-28 Сорренто Терапьютикс Инк. Конъюгат лекарственного средства с направляющей молекулой и двумя различными лекарственными средствами
CN107849090A (zh) 2015-01-28 2018-03-27 索伦托医疗有限公司 抗体药物偶联物
WO2016127081A1 (en) 2015-02-06 2016-08-11 Sorrento Therapeutics, Inc. Antibody drug conjugates

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