JP2019507126A - ツブリシン類似体およびこれらの調製のための方法 - Google Patents

ツブリシン類似体およびこれらの調製のための方法 Download PDF

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JP2019507126A
JP2019507126A JP2018539095A JP2018539095A JP2019507126A JP 2019507126 A JP2019507126 A JP 2019507126A JP 2018539095 A JP2018539095 A JP 2018539095A JP 2018539095 A JP2018539095 A JP 2018539095A JP 2019507126 A JP2019507126 A JP 2019507126A
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alkyl
hydrogen
heterocyclyl
aryl
methyl
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JP2019507126A5 (enExample
Inventor
サブラマンヤム チャクラパニー
サブラマンヤム チャクラパニー
エヌ．トゥミー ローレンス
エヌ．トゥミー ローレンス
シエ ロングフェイ
シエ ロングフェイ
エー．レヴァレット キャロリン
エー．レヴァレット キャロリン
シー． ヴェテリノ ベス
シー． ヴェテリノ ベス
トゥータン ケー．シュクール サイ
トゥータン ケー．シュクール サイ
ハドソン サラ
ハドソン サラ
ラマナ ドッパラプディ ヴェンカタ
ラマナ ドッパラプディ ヴェンカタ
エス．ブハット アブヒジット
エス．ブハット アブヒジット
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ファイザー・インク
コヴェックス・テクノロジーズ・アイルランド・リミテッド
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Publication of JP2019507126A publication Critical patent/JP2019507126A/ja
Publication of JP2019507126A5 publication Critical patent/JP2019507126A5/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
JP2018539095A 2016-02-01 2017-01-27 ツブリシン類似体およびこれらの調製のための方法 Pending JP2019507126A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662289485P 2016-02-01 2016-02-01
US62/289,485 2016-02-01
US201662322328P 2016-04-14 2016-04-14
US62/322,328 2016-04-14
PCT/IB2017/050462 WO2017134547A1 (en) 2016-02-01 2017-01-27 Tubulysin analogs and methods for their preparation

Publications (2)

Publication Number Publication Date
JP2019507126A true JP2019507126A (ja) 2019-03-14
JP2019507126A5 JP2019507126A5 (enExample) 2020-02-20

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JP2018539095A Pending JP2019507126A (ja) 2016-02-01 2017-01-27 ツブリシン類似体およびこれらの調製のための方法

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Country Link
US (1) US10723727B2 (enExample)
EP (1) EP3411371A1 (enExample)
JP (1) JP2019507126A (enExample)
CA (1) CA3012960A1 (enExample)
WO (1) WO2017134547A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11274124B2 (en) 2017-11-29 2022-03-15 William Marsh Rice University Tubulysin analogues as anticancer agents and payloads for antibody-drug conjugates and methods of treatment therewith
WO2020132658A2 (en) 2018-12-21 2020-06-25 Regeneron Pharmaceuticals, Inc. Tubulysins and protein-tubulysin conjugates
CN115867563B (zh) * 2020-06-24 2025-06-27 里珍纳龙药品有限公司 微管溶素及蛋白质-微管溶素偶联物
WO2023129518A1 (en) * 2021-12-29 2023-07-06 Regeneron Pharmaceuticals, Inc. Tubulysins and protein-tubulysin conjugates
CN114920749B (zh) * 2022-06-02 2024-08-16 山东鲁抗医药股份有限公司 7-氮杂双环[2.2.1]庚烷衍生物溴化物中间体的制备方法
WO2025078841A2 (en) 2023-10-11 2025-04-17 Antikor Biopharma Limited Antibodies, conjugates, and uses thereof

Citations (3)

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US20120129779A1 (en) * 2007-05-10 2012-05-24 R&D-Biopharmaceuticals Gmbh Tubulysine derivatives
WO2015113760A1 (en) * 2014-01-28 2015-08-06 Tube Pharmaceuticals Gmbh Cytotoxic tubulysin compounds for conjugation
WO2015157594A1 (en) * 2014-04-11 2015-10-15 Medimmune Llc Tubulysin derivatives

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US20120129779A1 (en) * 2007-05-10 2012-05-24 R&D-Biopharmaceuticals Gmbh Tubulysine derivatives
WO2015113760A1 (en) * 2014-01-28 2015-08-06 Tube Pharmaceuticals Gmbh Cytotoxic tubulysin compounds for conjugation
WO2015157594A1 (en) * 2014-04-11 2015-10-15 Medimmune Llc Tubulysin derivatives

Also Published As

Publication number Publication date
WO2017134547A1 (en) 2017-08-10
EP3411371A1 (en) 2018-12-12
US20180362519A1 (en) 2018-12-20
US10723727B2 (en) 2020-07-28
CA3012960A1 (en) 2017-08-10

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