JP6215194B2 - 生体直交型薬物活性化 - Google Patents

生体直交型薬物活性化 Download PDF

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Publication number
JP6215194B2
JP6215194B2 JP2014510928A JP2014510928A JP6215194B2 JP 6215194 B2 JP6215194 B2 JP 6215194B2 JP 2014510928 A JP2014510928 A JP 2014510928A JP 2014510928 A JP2014510928 A JP 2014510928A JP 6215194 B2 JP6215194 B2 JP 6215194B2
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alkyl
aryl
independently
tetrazine
drug
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JP2014515039A (ja
JP2014515039A5 (enExample
Inventor
ステファン ロビラルト，マルク
ステファン ロビラルト，マルク
マリー ヤンセン，ヘンリキュス
マリー ヤンセン，ヘンリキュス
フーフェ，ウォルテル テン
フーフェ，ウォルテル テン
マティウ フェルステーヘン，ロニー
マティウ フェルステーヘン，ロニー
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Koninklijke Philips NV
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Koninklijke Philips NV
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    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
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    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
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    • A61K47/54—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 organic compound
    • A61K47/555—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 organic compound pre-targeting systems involving an organic compound, other than a peptide, protein or antibody, for targeting specific cells
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    • A61K47/558—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 organic compound the modifying agent being a chemiluminescent acceptor
    • A—HUMAN NECESSITIES
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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
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    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
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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
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C33/00—Unsaturated compounds having hydroxy or O-metal groups bound to acyclic carbon atoms
    • C07C33/05—Alcohols containing rings other than six-membered aromatic rings
    • C07C33/16—Alcohols containing rings other than six-membered aromatic rings containing rings with more than six ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/08—Six-membered rings
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
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  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Nanotechnology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Mycology (AREA)
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  • General Engineering & Computer Science (AREA)
  • Medical Informatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biotechnology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2014510928A 2011-05-16 2012-05-16 生体直交型薬物活性化 Active JP6215194B2 (ja)

Applications Claiming Priority (17)

Application Number Priority Date Filing Date Title
EP11166241 2011-05-16
EP11166241.7 2011-05-16
EP11166942 2011-05-20
EP11166942.0 2011-05-20
US201161515432P 2011-08-05 2011-08-05
US201161515458P 2011-08-05 2011-08-05
US61/515,458 2011-08-05
EP11176741 2011-08-05
EP11176736.4 2011-08-05
US61/515,432 2011-08-05
EP11176741.4 2011-08-05
EP11176736 2011-08-05
EP11192572 2011-12-08
EP11192577.2 2011-12-08
EP11192572.3 2011-12-08
EP11192577 2011-12-08
PCT/IB2012/052445 WO2012156918A1 (en) 2011-05-16 2012-05-16 Bio-orthogonal drug activation

Publications (3)

Publication Number Publication Date
JP2014515039A JP2014515039A (ja) 2014-06-26
JP2014515039A5 JP2014515039A5 (enExample) 2017-03-02
JP6215194B2 true JP6215194B2 (ja) 2017-10-18

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JP2014510928A Active JP6215194B2 (ja) 2011-05-16 2012-05-16 生体直交型薬物活性化
JP2014510930A Active JP6482273B2 (ja) 2011-05-16 2012-05-16 生体直交型薬物活性化
JP2014510929A Active JP5993940B2 (ja) 2011-05-16 2012-05-16 生体直交型薬物活性化
JP2016161617A Ceased JP2017014262A (ja) 2011-05-16 2016-08-22 生体直交型薬物活性化
JP2018000737A Active JP6608467B2 (ja) 2011-05-16 2018-01-05 生体直交型薬物活性化

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JP2014510929A Active JP5993940B2 (ja) 2011-05-16 2012-05-16 生体直交型薬物活性化
JP2016161617A Ceased JP2017014262A (ja) 2011-05-16 2016-08-22 生体直交型薬物活性化
JP2018000737A Active JP6608467B2 (ja) 2011-05-16 2018-01-05 生体直交型薬物活性化

Country Status (9)

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US (8) US9421274B2 (enExample)
EP (4) EP2709668A1 (enExample)
JP (5) JP6215194B2 (enExample)
CN (4) CN103732256A (enExample)
AU (3) AU2012257416B8 (enExample)
CA (3) CA2836338C (enExample)
DK (1) DK2709667T3 (enExample)
ES (1) ES2920373T3 (enExample)
WO (3) WO2012156919A1 (enExample)

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JP6215194B2 (ja) * 2011-05-16 2017-10-18 コーニンクレッカ フィリップス エヌ ヴェＫｏｎｉｎｋｌｉｊｋｅ Ｐｈｉｌｉｐｓ Ｎ．Ｖ． 生体直交型薬物活性化
US9701998B2 (en) 2012-12-14 2017-07-11 10X Genomics, Inc. Methods and systems for processing polynucleotides
US10323279B2 (en) 2012-08-14 2019-06-18 10X Genomics, Inc. Methods and systems for processing polynucleotides
AU2013302756C1 (en) 2012-08-14 2018-05-17 10X Genomics, Inc. Microcapsule compositions and methods
US11591637B2 (en) 2012-08-14 2023-02-28 10X Genomics, Inc. Compositions and methods for sample processing
US10584381B2 (en) 2012-08-14 2020-03-10 10X Genomics, Inc. Methods and systems for processing polynucleotides
US10752949B2 (en) 2012-08-14 2020-08-25 10X Genomics, Inc. Methods and systems for processing polynucleotides
US9902705B2 (en) 2012-10-24 2018-02-27 The General Hospital Corporation Functionalized 1,2,4,5-tetrazine compounds for use in bioorthogonal coupling reactions
WO2014081300A1 (en) * 2012-11-22 2014-05-30 Tagworks Pharmaceuticals B.V. Channel protein activatable liposomes
WO2014081301A1 (en) * 2012-11-22 2014-05-30 Tagworks Pharmaceuticals B.V. Bio-orthogonal drug activation
WO2014081299A1 (en) * 2012-11-22 2014-05-30 Tagworks Pharmaceuticals B.V. Activatable liposomes
DK2922574T3 (da) 2012-11-22 2023-08-21 Tagworks Pharmaceuticals B V Kemisk spaltbar gruppe
WO2014133620A2 (en) * 2012-12-07 2014-09-04 University Of Washington Through Its Center For Commercialization Thermally-activated self-immolative materials
US10533221B2 (en) 2012-12-14 2020-01-14 10X Genomics, Inc. Methods and systems for processing polynucleotides
BR112015019159A2 (pt) 2013-02-08 2017-07-18 10X Genomics Inc geração de código de barras de polinucleotídeos
KR102306490B1 (ko) 2013-03-15 2021-09-28 리제너론 파아마슈티컬스, 인크. 생물학적 활성 분자, 그의 접합체 및 치료 용도
DK2968495T3 (da) 2013-03-15 2019-10-14 Daniel J Capon Hybrid immunoglobulin indeholdende en ikke-peptid-bro
US20150087043A1 (en) * 2013-04-11 2015-03-26 Coferon, Inc Monomers capable of multimerizing in an aqueous solution that employ bioorthogonal chemistries, and methods of using same
ES2966631T3 (es) 2013-06-19 2024-04-23 Univ California Estructuras químicas para el suministro localizado de agentes terapéuticos
SG11201601230RA (en) 2013-08-26 2016-03-30 Regeneron Pharma Pharmaceutical compositions comprising macrolide diastereomers, methods of their synthesis and therapeutic uses
IL291329B1 (en) 2013-09-25 2025-09-01 Cytomx Therapeutics Inc Polypeptides that can be determined in matrix metalloproteinases and uses thereof
CN106459153B (zh) * 2014-01-31 2021-12-21 西托姆克斯治疗公司 蛋白裂解酶和u型纤溶酶原激活物的底物和其它可裂解部分及其使用方法
JP6625550B2 (ja) 2014-03-14 2019-12-25 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 Ｔｃｏ複合体および治療薬の送達のための方法
LT3116486T (lt) * 2014-03-14 2020-04-10 Biomolecular Holdings Llc Hibridinis imunoglobulinas, turintis nepetidilinę jungtį
WO2015154082A1 (en) * 2014-04-04 2015-10-08 President And Fellows Of Harvard College Refillable drug delivery devices and methods of use thereof
US12312640B2 (en) 2014-06-26 2025-05-27 10X Genomics, Inc. Analysis of nucleic acid sequences
CN113249435B (zh) 2014-06-26 2024-09-03 10X基因组学有限公司 分析来自单个细胞或细胞群体的核酸的方法
KR102062025B1 (ko) 2014-06-30 2020-01-03 타베다 세라퓨틱스, 인코포레이티드 표적화된 콘주게이트 및 입자 및 그것의 제형
WO2016025480A1 (en) * 2014-08-11 2016-02-18 The General Hospital Corporation Cyclooctenes for bioorthogonol reactions
CN104356110B (zh) * 2014-11-19 2018-01-23 西北大学 一种硫诱导3,6‑芳香杂环不对称取代‑1,2,4,5‑四嗪化合物及其合成方法
MA41374A (fr) 2015-01-20 2017-11-28 Cytomx Therapeutics Inc Substrats clivables par métalloprotéase matricielle et clivables par sérine protéase et procédés d'utilisation de ceux-ci
CN107995912A (zh) 2015-03-27 2018-05-04 里珍纳龙药品有限公司 美登素类衍生物、其偶联物和使用方法
US20160331852A1 (en) * 2015-05-11 2016-11-17 Memorial Sloan Kettering Cancer Center Radioligands for pretargeted pet imaging and methods of their therapeutic use
EP3319968A1 (en) 2015-07-06 2018-05-16 Rodin Therapeutics, Inc. Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase
ES2899906T3 (es) 2015-07-06 2022-03-15 Alkermes Inc Inhibidores bicíclicos de histona desacetilasa
WO2017044983A1 (en) * 2015-09-10 2017-03-16 Shasqi, Inc. Bioorthogonal compositions
GB201516480D0 (en) 2015-09-17 2015-11-04 Univ Edinburgh Tetrazine as a trigger to release caged cargo
ES2874930T3 (es) * 2015-10-08 2021-11-05 Harvard College Dispositivos recargables de administración de fármacos y procedimientos de uso de los mismos
WO2017075495A1 (en) 2015-10-28 2017-05-04 Tarveda Therapeutics, Inc. Sstr-targeted conjugates and particles and formulations thereof
US10875840B2 (en) * 2015-12-15 2020-12-29 University Of Delaware Methods for inducing bioorthogonal reactivity
MX390630B (es) 2016-01-25 2025-03-21 Regeneron Pharma Derivados de maitansinoide, conjugados de los mismos y metodos de uso.
WO2017156164A1 (en) 2016-03-09 2017-09-14 Board Of Regents, The University Of Texas System 20-hete receptor (gpr75) antagonists and methods of use
WO2017175613A1 (ja) 2016-04-06 2017-10-12 住友化学株式会社 複素環化合物
US11617799B2 (en) * 2016-06-27 2023-04-04 Tagworks Pharmaceuticals B.V. Cleavable tetrazine used in bio-orthogonal drug activation
ES2875562T3 (es) 2017-01-11 2021-11-10 Alkermes Inc Inhibidores bicíclicos de histona desacetilasa
EP3385779A1 (en) * 2017-04-05 2018-10-10 Koninklijke Philips N.V. Multi-view display device and method
ES2983582T3 (es) 2017-04-07 2024-10-23 Tambo Inc Composiciones bioortogonales
US11560384B2 (en) 2017-05-04 2023-01-24 University Of Utah Research Foundation Benzonorbornadiene derivatives and reactions thereof
CN107281204A (zh) * 2017-05-04 2017-10-24 北京大学 一种非对称的1，2，4，5‑四嗪分子的应用
US11559494B2 (en) 2017-07-14 2023-01-24 The Penn State Research Foundation Compositions and methods for targeted delivery of therapeutic and/or diagnostic species
US11225475B2 (en) 2017-08-07 2022-01-18 Alkermes, Inc. Substituted pyridines as inhibitors of histone deacetylase
US10590244B2 (en) 2017-10-04 2020-03-17 10X Genomics, Inc. Compositions, methods, and systems for bead formation using improved polymers
US10837047B2 (en) * 2017-10-04 2020-11-17 10X Genomics, Inc. Compositions, methods, and systems for bead formation using improved polymers
WO2019084323A1 (en) 2017-10-25 2019-05-02 Georgia State University Research Foundation, Inc. CHEMICAL RELEASE SYSTEM DELIVERED BY ENRICHMENT
EP3954782A1 (en) 2017-11-15 2022-02-16 10X Genomics, Inc. Functionalized gel beads
US10829815B2 (en) 2017-11-17 2020-11-10 10X Genomics, Inc. Methods and systems for associating physical and genetic properties of biological particles
EP3774784A4 (en) * 2018-04-11 2021-12-15 Clarity Pharmaceuticals Ltd TARGETING COMPOUNDS AND METHOD FOR CREATING THEREOF
EP3787691A1 (en) 2018-05-04 2021-03-10 Tagworks Pharmaceuticals B.V. Tetrazines for high click conjugation yield in vivo and high click release yield
EP4382167A3 (en) 2018-05-04 2024-08-28 Tagworks Pharmaceuticals B.V. Compounds comprising a linker for increasing transcyclooctene stability
WO2019231016A1 (ko) 2018-05-31 2019-12-05 (주)스파크바이오파마 신규한 형광체-테트라진 화합물 및 이의 용도
KR102011772B1 (ko) * 2018-05-31 2019-08-19 (주)스파크바이오파마 신규한 형광체-테트라진 화합물 및 이의 용도
AU2019344897B2 (en) 2018-09-18 2024-01-18 Nikang Therapeutics, Inc. Tri-substituted heteroaryl derivatives AS SRC homology-2 phosphatase inhibitors
AU2019359398B2 (en) * 2018-10-10 2023-03-30 Tambo, Inc. Processes for preparing functionalized cyclooctenes
CA3120327A1 (en) 2018-12-06 2020-06-11 Cytomx Therapeutics, Inc. Matrix metalloprotease-cleavable and serine or cysteine protease-cleavable substrates and methods of use thereof
US20220062428A1 (en) * 2018-12-12 2022-03-03 The General Hospital Corporation Prodrugs with a tridentate self-immolative linker
CN112010817A (zh) * 2019-05-31 2020-12-01 四川大学华西医院 一种制备四嗪类化合物的方法及其应用
IL289095A (en) 2019-06-17 2022-02-01 Tagworks Pharmaceuticals B V Activating components to cleave labels from biomolecules in vivo
IL289094A (en) 2019-06-17 2022-02-01 Tagworks Pharmaceuticals B V Tetrazines for increasing the speed and yield of the "click release" reaction
EP4382129A3 (en) 2019-06-17 2024-07-03 Tagworks Pharmaceuticals B.V. Compounds for fast and efficient click release
CN113321702B (zh) * 2020-02-28 2022-08-05 国家纳米科学中心 一种单甲基澳瑞他汀f甲酯前药及其制备方法和应用
CN113321698B (zh) * 2020-02-28 2022-08-23 国家纳米科学中心 一种单甲基澳瑞他汀e前药及其制备方法和应用
CN113354657B (zh) * 2020-03-05 2022-10-21 国家纳米科学中心 一种Mytoxin A前药及其制备方法和应用
EP3909944A1 (en) * 2020-05-14 2021-11-17 Rigshospitalet Nuclide labelled h-tetrazines and use thereof for pet and spect pretargeted imaging and radionuclide therapy
WO2022032191A1 (en) * 2020-08-07 2022-02-10 Tambo, Inc. Trans-cyclooctene bioorthogonal agents and uses in cancer and immunotherapy
US20230301988A1 (en) 2020-08-27 2023-09-28 The Texas A&M University System Inhibitors of sars cov-2 infection and uses thereof
US20240058455A1 (en) * 2020-10-02 2024-02-22 The General Hospital Corporation Bioorthogonal linkers and reactions
WO2022197877A1 (en) 2021-03-19 2022-09-22 Genentech, Inc. Methods and compositions for time delayed bio-orthogonal release of cytotoxic agents
WO2023028165A2 (en) * 2021-08-25 2023-03-02 R.P. Scherer Technologies, Llc Tumor-associated calcium signal transducer 2 (tacstd2) antibody-maytansine conjugates and methods of use thereof
WO2023081809A1 (en) * 2021-11-05 2023-05-11 Tambo, Inc. Trans-cyclooctene-modified bispecific antibodies
EP4186529B1 (en) * 2021-11-25 2025-07-09 Veraxa Biotech GmbH Improved antibody-payload conjugates (apcs) prepared by site-specific conjugation utilizing genetic code expansion
CA3244098A1 (en) 2022-02-15 2023-08-24 Tagworks Pharmaceuticals B V Masked il12 protein
CN114652857B (zh) * 2022-03-31 2023-10-20 成都大学 一种用于修复内皮糖萼受损的靶向药物递送系统及其制备方法
CN115974892B (zh) * 2022-12-27 2023-09-08 四川大学华西医院 三氮唑四嗪类化合物及其制备方法、应用
CN116370650B (zh) * 2023-04-14 2024-03-22 四川大学华西医院 基于四嗪连接子的多肽药物偶联物及其制备方法、应用
CN116675664B (zh) * 2023-04-21 2025-06-24 苏州大学 一种生物正交断键反应体系及前药与应用
WO2025043219A1 (en) * 2023-08-24 2025-02-27 The Regents Of The University Of California Methods for uncaging tetrazines
WO2025166289A1 (en) * 2024-01-31 2025-08-07 Oregon State University Tunable tetrazine amino acids for encodable protein labeling
CN117700394B (zh) * 2024-02-06 2024-05-28 南京大学 一类可与非张力烯基硼酸快速环加成反应的四嗪类化合物及其生物医药应用
WO2025174248A1 (en) * 2024-02-16 2025-08-21 Tagworks Pharmaceuticals B.V. Trans-cyclooctenes with "or gate" release
CN117752824A (zh) * 2024-02-21 2024-03-26 中国医学科学院医学实验动物研究所 预靶向肿瘤免疫探针、生物正交制剂、试剂盒及应用

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4826964A (en) 1982-07-20 1989-05-02 Sri International Bridged oxygen analogs of daunorubcin and doxorubicin
US4486414A (en) 1983-03-21 1984-12-04 Arizona Board Of Reagents Dolastatins A and B cell growth inhibitory substances
US4486444A (en) 1983-06-20 1984-12-04 Merck & Co., Inc. (Hydroxybenzoyl)thiophenesulfonamide and acyl derivatives thereof for the topical treatment of elevated intraocular pressure
US4879278A (en) 1989-05-16 1989-11-07 Arizona Board Of Regents Isolation and structural elucidation of the cytostatic linear depsipeptide dolastatin 15
US4986988A (en) 1989-05-18 1991-01-22 Arizona Board Of Regents Isolation and structural elucidation of the cytostatic linear depsipeptides dolastatin 13 and dehydrodolastatin 13
US5138036A (en) 1989-11-13 1992-08-11 Arizona Board Of Regents Acting On Behalf Of Arizona State University Isolation and structural elucidation of the cytostatic cyclodepsipeptide dolastatin 14
US5198560A (en) 1990-04-27 1993-03-30 Bristol-Myers Squibb Company Cytotoxic bicyclo[7.3.1]tridec-4-ene-2,6-diyne compounds and process for the preparation thereof
US6034065A (en) 1992-12-03 2000-03-07 Arizona Board Of Regents Elucidation and synthesis of antineoplastic tetrapeptide phenethylamides of dolastatin 10
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
US5410024A (en) 1993-01-21 1995-04-25 Arizona Board Of Regents Acting On Behalf Of Arizona State University Human cancer inhibitory pentapeptide amides
US5780588A (en) 1993-01-26 1998-07-14 Arizona Board Of Regents Elucidation and synthesis of selected pentapeptides
US5521284A (en) 1994-08-01 1996-05-28 Arizona Board Of Regents Acting On Behalf Of Arizona State University Human cancer inhibitory pentapeptide amides and esters
US5530097A (en) 1994-08-01 1996-06-25 Arizona Board Of Regents Acting On Behalf Of Arizona State University Human cancer inhibitory peptide amides
US5504191A (en) 1994-08-01 1996-04-02 Arizona Board Of Regents Acting On Behalf Of Arizona State University Human cancer inhibitory pentapeptide methyl esters
US5599902A (en) 1994-11-10 1997-02-04 Arizona Board Of Regents Acting On Behalf Of Arizona State University Cancer inhibitory peptides
US5663149A (en) 1994-12-13 1997-09-02 Arizona Board Of Regents Acting On Behalf Of Arizona State University Human cancer inhibitory pentapeptide heterocyclic and halophenyl amides
EP0904066A4 (en) 1996-05-03 2002-04-24 Roger S Cubicciotti DRUG COMPOSITIONS AND METHOD FOR ADMINISTERING DRUGS USING SYNTHETIC RECEPTORS
DE69832158T2 (de) 1997-02-25 2006-08-10 Arizona Board Of Regents, Tempe Isolierung und strukturelle aufklärung der kryostatischen linearen und cyclo-depsipeptide dolastatin 16, dolastatin 17, und dolastatin 18
US6323315B1 (en) 1999-09-10 2001-11-27 Basf Aktiengesellschaft Dolastatin peptides
US8236949B2 (en) * 2007-07-17 2012-08-07 University Of Delaware Tetrazine-based bio-orthogonal coupling reagents and methods
WO2009109998A1 (en) 2008-03-03 2009-09-11 Lupin Limited Novel protein tyrosine phosphatase - ib inhibitors
EP2361098B1 (en) 2008-10-31 2019-08-28 The General Hospital Corporation Compositions and methods for delivering a substance to a biological target
GB0906379D0 (en) * 2009-04-14 2009-05-20 Kencryst Ltd Reduced sodium salt
EP2419141A1 (en) * 2009-04-16 2012-02-22 Koninklijke Philips Electronics N.V. Pretargeting kit, method and agents used therein
US20120034161A1 (en) 2009-04-16 2012-02-09 Koninklijke Philips Electronics N.V. Pretargeting kit, method and agents used therein
EP2595967B1 (en) 2010-07-23 2016-03-23 University Of Delaware Tetrazine-trans-cyclooctene ligation for the rapid construction of radionuclide labeled probes
JP6063384B2 (ja) * 2010-10-14 2017-01-18 コーニンクレッカ フィリップス エヌ ヴェＫｏｎｉｎｋｌｉｊｋｅ Ｐｈｉｌｉｐｓ Ｎ．Ｖ． プレターゲットキット、プレターゲット方法及びその使用試薬
RU2013133813A (ru) * 2010-12-21 2015-01-27 Конинклейке Филипс Электроникс Н.В. Средства для выведения биомолекул из кровотока
EP2522369A1 (en) * 2011-05-09 2012-11-14 Koninklijke Philips Electronics N.V. Pretargeting kit, method and agents used therein
JP6215194B2 (ja) * 2011-05-16 2017-10-18 コーニンクレッカ フィリップス エヌ ヴェＫｏｎｉｎｋｌｉｊｋｅ Ｐｈｉｌｉｐｓ Ｎ．Ｖ． 生体直交型薬物活性化
US9902705B2 (en) 2012-10-24 2018-02-27 The General Hospital Corporation Functionalized 1,2,4,5-tetrazine compounds for use in bioorthogonal coupling reactions
WO2014081301A1 (en) 2012-11-22 2014-05-30 Tagworks Pharmaceuticals B.V. Bio-orthogonal drug activation
DK2922574T3 (da) 2012-11-22 2023-08-21 Tagworks Pharmaceuticals B V Kemisk spaltbar gruppe
WO2016025480A1 (en) 2014-08-11 2016-02-18 The General Hospital Corporation Cyclooctenes for bioorthogonol reactions
US11617799B2 (en) * 2016-06-27 2023-04-04 Tagworks Pharmaceuticals B.V. Cleavable tetrazine used in bio-orthogonal drug activation
EP3787691A1 (en) * 2018-05-04 2021-03-10 Tagworks Pharmaceuticals B.V. Tetrazines for high click conjugation yield in vivo and high click release yield
EP4382167A3 (en) * 2018-05-04 2024-08-28 Tagworks Pharmaceuticals B.V. Compounds comprising a linker for increasing transcyclooctene stability
EP4382129A3 (en) * 2019-06-17 2024-07-03 Tagworks Pharmaceuticals B.V. Compounds for fast and efficient click release
IL289095A (en) * 2019-06-17 2022-02-01 Tagworks Pharmaceuticals B V Activating components to cleave labels from biomolecules in vivo
IL289094A (en) * 2019-06-17 2022-02-01 Tagworks Pharmaceuticals B V Tetrazines for increasing the speed and yield of the "click release" reaction

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