JP6482273B2 - 生体直交型薬物活性化 - Google Patents

生体直交型薬物活性化 Download PDF

Info

Publication number
JP6482273B2
JP6482273B2 JP2014510930A JP2014510930A JP6482273B2 JP 6482273 B2 JP6482273 B2 JP 6482273B2 JP 2014510930 A JP2014510930 A JP 2014510930A JP 2014510930 A JP2014510930 A JP 2014510930A JP 6482273 B2 JP6482273 B2 JP 6482273B2
Authority
JP
Japan
Prior art keywords
drug
group
prodrug
alkyl
antibody
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
JP2014510930A
Other languages
English (en)
Japanese (ja)
Other versions
JP2014513717A (ja
JP2014513717A5 (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
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
ロッシン，ラファエッラ
ヨハネス マリア フーベン，フレーク
ヨハネス マリア フーベン，フレーク
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Koninklijke Philips NV
Original Assignee
Koninklijke Philips NV
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Koninklijke Philips NV filed Critical Koninklijke Philips NV
Publication of JP2014513717A publication Critical patent/JP2014513717A/ja
Publication of JP2014513717A5 publication Critical patent/JP2014513717A5/ja
Application granted granted Critical
Publication of JP6482273B2 publication Critical patent/JP6482273B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K38/05—Dipeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/39558—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • 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
    • A61K47/54—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • 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
    • A61K47/54—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
    • A61K47/545—Heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • 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
    • A61K47/54—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • 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
    • A61K47/54—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
    • A61K47/558—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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • 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
    • 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
    • A61K47/68031—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being an auristatin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • 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
    • 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
    • A61K47/68033—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a maytansine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • 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
    • A61K47/6891—Pre-targeting systems involving an antibody for targeting specific cells
    • A61K47/6897—Pre-targeting systems with two or three steps using antibody conjugates; Ligand-antiligand therapies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Nanotechnology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Biotechnology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Medical Informatics (AREA)
  • Biophysics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (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)
  • Saccharide Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2014510930A 2011-05-16 2012-05-16 生体直交型薬物活性化 Active JP6482273B2 (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
EP11176741.4 2011-08-05
EP11176736 2011-08-05
EP11176736.4 2011-08-05
US61/515,432 2011-08-05
EP11192577.2 2011-12-08
EP11192572 2011-12-08
EP11192572.3 2011-12-08
EP11192577 2011-12-08
PCT/IB2012/052447 WO2012156920A1 (en) 2011-05-16 2012-05-16 Bio-orthogonal drug activation

Publications (3)

Publication Number Publication Date
JP2014513717A JP2014513717A (ja) 2014-06-05
JP2014513717A5 JP2014513717A5 (enExample) 2018-09-27
JP6482273B2 true JP6482273B2 (ja) 2019-03-13

Family

ID=47176369

Family Applications (5)

Application Number Title Priority Date Filing Date
JP2014510930A Active JP6482273B2 (ja) 2011-05-16 2012-05-16 生体直交型薬物活性化
JP2014510928A Active JP6215194B2 (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

Family Applications After (4)

Application Number Title Priority Date Filing Date
JP2014510928A Active JP6215194B2 (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

Country Status (9)

Country Link
US (8) US20160151505A1 (enExample)
EP (4) EP2709666B1 (enExample)
JP (5) JP6482273B2 (enExample)
CN (4) CN103732256A (enExample)
AU (3) AU2012257417B2 (enExample)
CA (3) CA2836361C (enExample)
DK (1) DK2709667T3 (enExample)
ES (1) ES2920373T3 (enExample)
WO (3) WO2012156920A1 (enExample)

Families Citing this family (93)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2709666B1 (en) 2011-05-16 2021-07-14 Koninklijke Philips N.V. Bio-orthogonal drug activation
JP6367196B2 (ja) 2012-08-14 2018-08-01 テンエックス・ジェノミクス・インコーポレイテッド マイクロカプセル組成物および方法
US10584381B2 (en) 2012-08-14 2020-03-10 10X Genomics, Inc. Methods and systems for processing polynucleotides
US11591637B2 (en) 2012-08-14 2023-02-28 10X Genomics, Inc. Compositions and methods for sample processing
US10752949B2 (en) 2012-08-14 2020-08-25 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
US9701998B2 (en) 2012-12-14 2017-07-11 10X Genomics, Inc. Methods and systems for processing polynucleotides
WO2014065860A1 (en) * 2012-10-24 2014-05-01 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
EP2922574B1 (en) 2012-11-22 2023-05-17 Tagworks Pharmaceuticals B.V. Chemically cleavable group
WO2014081299A1 (en) * 2012-11-22 2014-05-30 Tagworks Pharmaceuticals B.V. Activatable liposomes
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
KR102190198B1 (ko) 2013-02-08 2020-12-14 10엑스 제노믹스, 인크. 폴리뉴클레오티드 바코드 생성
DK2968495T3 (da) 2013-03-15 2019-10-14 Daniel J Capon Hybrid immunoglobulin indeholdende en ikke-peptid-bro
EP3964237B1 (en) 2013-03-15 2026-02-18 Regeneron Pharmaceuticals, Inc. Biologically active molecules, conjugates thereof, and therapeutic uses
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
WO2014205126A1 (en) 2013-06-19 2014-12-24 The Regents Of The University Of California Chemical structures for localized delivery of therapeutic agents
KR102252925B1 (ko) 2013-08-26 2021-05-18 리제너론 파마슈티칼스 인코포레이티드 마크롤라이드 디아스테레오머를 포함하는 약제학적 조성물, 이의 합성 방법 및 치료학적 용도
KR102488220B1 (ko) 2013-09-25 2023-01-12 싸이톰스 테라퓨틱스, 인크. 매트릭스 메탈로프로테이나제 기질 및 다른 절단성 모이어티 및 이의 사용 방법
KR102466591B1 (ko) * 2014-01-31 2022-11-14 싸이톰스 테라퓨틱스, 인크. 마트립타제 및 ｕ-플라스미노겐 활성화인자 기질 및 다른 절단성 모이어티 및 이의 사용 방법
SI3116486T1 (sl) * 2014-03-14 2020-07-31 Biomolecular Holdings Llc Hibridni imunoglobulin, ki vsebuje nepeptidilno vezavo
CN106659796B (zh) 2014-03-14 2021-04-30 加利福尼亚大学董事会 Tco缀合物和治疗剂递送方法
ES2871029T3 (es) * 2014-04-04 2021-10-28 Harvard College Dispositivos de liberación de fármacos recargables y procedimientos de uso de los mismos
US12312640B2 (en) 2014-06-26 2025-05-27 10X Genomics, Inc. Analysis of nucleic acid sequences
EP4574974A3 (en) 2014-06-26 2025-10-08 10x Genomics, Inc. Methods of analyzing nucleic acids from individual cells or cell populations
WO2016004048A2 (en) 2014-06-30 2016-01-07 Blend Therapeutics, Inc. Targeted conjugates and particles and formulations thereof
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
KR20240142591A (ko) 2015-03-27 2024-09-30 리제너론 파아마슈티컬스, 인크. 메이탄시노이드 유도체, 이의 컨주게이트, 및 사용 방법
US20160331852A1 (en) * 2015-05-11 2016-11-17 Memorial Sloan Kettering Cancer Center Radioligands for pretargeted pet imaging and methods of their therapeutic use
US10421756B2 (en) 2015-07-06 2019-09-24 Rodin Therapeutics, Inc. Heterobicyclic N-aminophenyl-amides as inhibitors of histone deacetylase
LT3319959T (lt) 2015-07-06 2021-12-27 Alkermes, Inc. Histono deacetilazės hetero-halogeno inhibitoriai
JP6823067B2 (ja) * 2015-09-10 2021-01-27 タンボ・インコーポレイテッド 生体直交型組成物
GB201516480D0 (en) 2015-09-17 2015-11-04 Univ Edinburgh Tetrazine as a trigger to release caged cargo
EP3153155B1 (en) * 2015-10-08 2021-03-03 President and Fellows of Harvard College Refillable drug delivery devices and methods of use thereof
HK1259311A1 (zh) 2015-10-28 2019-11-29 Tva (Abc), Llc Sstr靶向綴合物及其顆粒和製劑
US10875840B2 (en) * 2015-12-15 2020-12-29 University Of Delaware Methods for inducing bioorthogonal reactivity
MY198605A (en) 2016-01-25 2023-09-08 Regeneron Pharma Maytansinoid derivatives conjugates thereof, and methods of use
US11690825B2 (en) 2016-03-09 2023-07-04 Board Of Regents, The University Of Texas System 20-HETE receptor (GPR75) antagonists and methods of use
EP3444239B1 (en) 2016-04-06 2020-11-04 Sumitomo Chemical Company, Limited Heterocyclic compounds useful for controlling arthropods
WO2018004338A1 (en) 2016-06-27 2018-01-04 Tagworks Pharmaceuticals B.V. Cleavable tetrazine used in bio-orthogonal drug activation
ES2909086T3 (es) 2017-01-11 2022-05-05 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
SG11202000970WA (en) 2017-08-07 2020-02-27 Rodin Therapeutics Inc Bicyclic 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
US11607458B2 (en) 2017-10-25 2023-03-21 Georgia State University Research Foundation, Inc. Enrichment-triggered chemical delivery system
CN111051523B (zh) 2017-11-15 2024-03-19 10X基因组学有限公司 功能化凝胶珠
US10829815B2 (en) 2017-11-17 2020-11-10 10X Genomics, Inc. Methods and systems for associating physical and genetic properties of biological particles
CN111989324A (zh) * 2018-04-11 2020-11-24 墨尔本大学 靶向化合物及其生产方法
WO2019213570A1 (en) 2018-05-04 2019-11-07 Remedy Plan, Inc. Cancer treatments targeting cancer stem cells
WO2019212356A1 (en) 2018-05-04 2019-11-07 Tagworks Pharmaceuticals B .V. Tetrazines for high click conjugation yield in vivo and high click release yield
CA3099421C (en) * 2018-05-04 2025-05-06 Tagworks Pharmaceuticals B.V. COMPOUNDS INCLUDING A BINDER TO INCREASE TRANSCYCLOOCTENE STABILITY
US11584749B2 (en) 2018-05-31 2023-02-21 Spark Biopharma, Inc. Phosphor-tetrazine compound and use thereof
KR102011772B1 (ko) * 2018-05-31 2019-08-19 (주)스파크바이오파마 신규한 형광체-테트라진 화합물 및 이의 용도
WO2020061103A1 (en) 2018-09-18 2020-03-26 Nikang Therapeutics, Inc. Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors
IL282114B2 (en) 2018-10-10 2025-05-01 Tambo Inc Processes for preparing functional cyclooctanes
SG11202105476XA (en) 2018-12-06 2021-06-29 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
CN114599645A (zh) 2019-06-17 2022-06-07 泰克沃尔科斯制药有限公司 用于在体内从生物分子中裂解标记的试剂
IL289094A (en) * 2019-06-17 2022-02-01 Tagworks Pharmaceuticals B V Tetrazines for increasing the speed and yield of the "click release" reaction
CN115135628A (zh) * 2019-06-17 2022-09-30 泰克沃尔科斯制药有限公司 快速高效点击释放的化合物
KR20220110744A (ko) 2019-11-06 2022-08-09 레미디 플랜, 인크. 암 줄기 세포를 표적화하는 암 치료
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
US12589162B2 (en) 2020-08-07 2026-03-31 Tambo, Inc. Trans-cyclooctene prodrug of monomethyl auristatin E
EP4203957A2 (en) 2020-08-27 2023-07-05 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
JP2024532302A (ja) * 2021-08-25 2024-09-05 アール．ピー．シェーラー テクノロジーズ，エルエルシー 腫瘍関連カルシウムシグナルトランスデューサー２（ｔａｃｓｔｄ２）抗体－メイタンシンコンジュゲート及びその使用方法
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
US20250114489A1 (en) 2022-02-15 2025-04-10 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
AU2024220523B2 (en) * 2023-02-15 2025-12-11 Tagworks Pharmaceuticals B.V. Tetrazines with improved properties
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
WO2025166142A1 (en) * 2024-01-31 2025-08-07 Oregon State University Protein labeling in living cells via control of redox state of encoded tetrazines
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
CA2253204A1 (en) 1996-05-03 1997-11-13 Roger S. Cubicciotti Prodrug compositions and drug delivery methods using synthetic receptors
EP0973540B1 (en) 1997-02-25 2005-11-02 Arizona Board Of Regents Isolation and structural elucidation of the cytostatic linear and cyclo-depsipeptides dolastatin 16, dolastatin 17, and 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
WO2010051530A2 (en) 2008-10-31 2010-05-06 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
US20120039803A1 (en) * 2009-04-16 2012-02-16 Koninklijke Philips Electronics N.V. Pretargeting kit, method and agents used therein
BRPI1006246A2 (pt) * 2009-04-16 2020-02-04 Koninl Philips Electronics Nv "kit para imagem médica marcada e/ou terapias, sonda efetora e método"
WO2012012612A2 (en) 2010-07-23 2012-01-26 University Of Delaware Tetrazine-trans-cyclooctene ligation for the rapid construction of radionuclide labeled probes
RU2013121799A (ru) * 2010-10-14 2014-11-20 Конинклейке Филипс Электроникс Н.В. Набор для претаргетинга, способ и агенты, применяемые в нем
EP2654796A1 (en) 2010-12-21 2013-10-30 Koninklijke Philips N.V. Agents for clearing biomolecules from circulation
EP2522369A1 (en) * 2011-05-09 2012-11-14 Koninklijke Philips Electronics N.V. Pretargeting kit, method and agents used therein
EP2709666B1 (en) * 2011-05-16 2021-07-14 Koninklijke Philips N.V. Bio-orthogonal drug activation
WO2014065860A1 (en) 2012-10-24 2014-05-01 The General Hospital Corporation Functionalized 1,2,4,5-tetrazine compounds for use in bioorthogonal coupling reactions
EP2922574B1 (en) 2012-11-22 2023-05-17 Tagworks Pharmaceuticals B.V. Chemically cleavable group
WO2014081301A1 (en) 2012-11-22 2014-05-30 Tagworks Pharmaceuticals B.V. Bio-orthogonal drug activation
WO2016025480A1 (en) 2014-08-11 2016-02-18 The General Hospital Corporation Cyclooctenes for bioorthogonol reactions
WO2018004338A1 (en) 2016-06-27 2018-01-04 Tagworks Pharmaceuticals B.V. Cleavable tetrazine used in bio-orthogonal drug activation
WO2019212356A1 (en) * 2018-05-04 2019-11-07 Tagworks Pharmaceuticals B .V. Tetrazines for high click conjugation yield in vivo and high click release yield
CA3099421C (en) * 2018-05-04 2025-05-06 Tagworks Pharmaceuticals B.V. COMPOUNDS INCLUDING A BINDER TO INCREASE TRANSCYCLOOCTENE STABILITY
CN115135628A (zh) * 2019-06-17 2022-09-30 泰克沃尔科斯制药有限公司 快速高效点击释放的化合物
IL289094A (en) * 2019-06-17 2022-02-01 Tagworks Pharmaceuticals B V Tetrazines for increasing the speed and yield of the "click release" reaction
CN114599645A (zh) * 2019-06-17 2022-06-07 泰克沃尔科斯制药有限公司 用于在体内从生物分子中裂解标记的试剂

Also Published As

Publication number Publication date
US20170143840A1 (en) 2017-05-25
JP2014513717A (ja) 2014-06-05
US9931408B2 (en) 2018-04-03
JP2017014262A (ja) 2017-01-19
AU2012257417B2 (en) 2017-09-14
JP2014515039A (ja) 2014-06-26
AU2012257416B2 (en) 2017-06-22
JP2014515040A (ja) 2014-06-26
WO2012156920A1 (en) 2012-11-22
CA2836338C (en) 2022-05-03
EP2709666A1 (en) 2014-03-26
US20210162060A1 (en) 2021-06-03
AU2012257416B8 (en) 2017-10-19
CA2836365C (en) 2021-07-27
US10967069B2 (en) 2021-04-06
US20140199331A1 (en) 2014-07-17
US20190336612A1 (en) 2019-11-07
US20240091371A1 (en) 2024-03-21
AU2012257418A1 (en) 2014-01-16
EP2709668A1 (en) 2014-03-26
US9421274B2 (en) 2016-08-23
EP2709666B1 (en) 2021-07-14
JP6608467B2 (ja) 2019-11-20
AU2012257416A8 (en) 2017-10-19
JP5993940B2 (ja) 2016-09-21
US20140093522A1 (en) 2014-04-03
WO2012156919A1 (en) 2012-11-22
EP2709667B1 (en) 2022-04-13
WO2012156918A1 (en) 2012-11-22
DK2709667T3 (da) 2022-07-04
JP6215194B2 (ja) 2017-10-18
US11857636B2 (en) 2024-01-02
CN103732256A (zh) 2014-04-16
AU2012257418B2 (en) 2017-08-03
CA2836361C (en) 2020-11-10
EP3973993A1 (en) 2022-03-30
ES2920373T3 (es) 2022-08-03
AU2012257416A1 (en) 2014-01-16
CA2836365A1 (en) 2012-11-22
CA2836338A1 (en) 2012-11-22
CN103732257A (zh) 2014-04-16
US20160106859A1 (en) 2016-04-21
CA2836361A1 (en) 2012-11-22
US20160151505A1 (en) 2016-06-02
CN103889459A (zh) 2014-06-25
US10376594B2 (en) 2019-08-13
AU2012257417A1 (en) 2014-01-16
CN108524510A (zh) 2018-09-14
US10004810B2 (en) 2018-06-26
JP2018058902A (ja) 2018-04-12
EP2709667A1 (en) 2014-03-26
CN103889459B (zh) 2018-04-24

Similar Documents

Publication Publication Date Title
US11857636B2 (en) Bio-orthogonal drug activation
US20150297741A1 (en) Bio-orthogonal drug activation
JP2014515040A5 (enExample)

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20131119

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20150513

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20160329

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20160623

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160926

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20170221

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20170614

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20170621

A912 Re-examination (zenchi) completed and case transferred to appeal board

Free format text: JAPANESE INTERMEDIATE CODE: A912

Effective date: 20170721

A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20180810

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20181113

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20190212

R150 Certificate of patent or registration of utility model

Ref document number: 6482273

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313113

S531 Written request for registration of change of domicile

Free format text: JAPANESE INTERMEDIATE CODE: R313531

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250