JP2018058822A - ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用 - Google Patents

ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用 Download PDF

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Publication number
JP2018058822A
JP2018058822A JP2017147506A JP2017147506A JP2018058822A JP 2018058822 A JP2018058822 A JP 2018058822A JP 2017147506 A JP2017147506 A JP 2017147506A JP 2017147506 A JP2017147506 A JP 2017147506A JP 2018058822 A JP2018058822 A JP 2018058822A
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Japan
Prior art keywords
alkyl
antibody
mmol
cancer
methyl
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Withdrawn
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JP2017147506A
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Japanese (ja)
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JP2018058822A5 (enExample
Inventor
ジョージ ダッシン ラッセル
George Dushin Russell
ジョージ ダッシン ラッセル
エー. アブラミテ ジョゼフ
A Abramite Joseph
エー. アブラミテ ジョゼフ
エム, カサヴァント ジェフリー
M Casavant Jeffrey
エム, カサヴァント ジェフリー
チェ イエ
Ye Che
チェ イエ
フレデリック フィルツェン ゲイリー
Frederick Filzen Gary
フレデリック フィルツェン ゲイリー
フラナガン マーク
Edward Flanagan Mark
フラナガン マーク
マシュー ギルバート アダム
Matthew Gilbert Adam
マシュー ギルバート アダム
モイネ ルディヴィン
Moine Ludivine
モイネ ルディヴィン
ジョン オドネル クリストファー
Christopher John O'donnell
ジョン オドネル クリストファー
アール. ロバーツ リー
R Roberts Lee
アール. ロバーツ リー
スター ジェレミー
Starr Jeremy
スター ジェレミー
エヌ.トゥミー ローレンス
N Tumey Lawrence
エヌ.トゥミー ローレンス
ピー. ウッチェロ ダニエル
P Uccello Daniel
ピー. ウッチェロ ダニエル
ヤング ジェニファー
Young Jennifer
ヤング ジェニファー
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.)
Pfizer Corp Belgium
Pfizer Inc
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Pfizer Corp Belgium
Pfizer Inc
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.)
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Publication date
Application filed by Pfizer Corp Belgium, Pfizer Inc filed Critical Pfizer Corp Belgium
Publication of JP2018058822A publication Critical patent/JP2018058822A/ja
Publication of JP2018058822A5 publication Critical patent/JP2018058822A5/ja
Priority to JP2022102984A priority Critical patent/JP7555998B2/ja
Priority to JP2024157625A priority patent/JP2024174998A/ja
Withdrawn legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6835Medicinal 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
    • A61K47/6851Medicinal 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 the antibody targeting a determinant of a tumour cell
    • A61K47/6855Medicinal 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 the antibody targeting a determinant of a tumour cell the tumour determinant being from breast cancer cell
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    • A61K47/50Medicinal 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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    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/545Heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
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    • A61K47/51Medicinal 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
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    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/68031Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being an auristatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6835Medicinal 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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    • A61K47/6867Medicinal 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 the antibody targeting a determinant of a tumour cell the tumour determinant being from a cell of a blood cancer
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6889Conjugates 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
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • AHUMAN NECESSITIES
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    • A61P13/12Drugs for disorders of the urinary system of the kidneys
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • AHUMAN NECESSITIES
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    • A61P31/12Antivirals
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    • C07K5/0205Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof
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    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052Val-amino acid
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    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02Linear peptides containing at least one abnormal peptide link

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  • Proteomics, Peptides & Aminoacids (AREA)
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  • Reproductive Health (AREA)
  • Diabetes (AREA)
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  • 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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2017147506A 2016-08-03 2017-07-31 ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用 Withdrawn JP2018058822A (ja)

Priority Applications (2)

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JP2022102984A JP7555998B2 (ja) 2016-08-03 2022-06-27 ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用
JP2024157625A JP2024174998A (ja) 2016-08-03 2024-09-11 ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201662370270P 2016-08-03 2016-08-03
US62/370,270 2016-08-03
US201762530554P 2017-07-10 2017-07-10
US62/530,554 2017-07-10

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JP2022102984A Division JP7555998B2 (ja) 2016-08-03 2022-06-27 ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用

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JP2018058822A true JP2018058822A (ja) 2018-04-12
JP2018058822A5 JP2018058822A5 (enExample) 2020-08-13

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JP2017147506A Withdrawn JP2018058822A (ja) 2016-08-03 2017-07-31 ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用
JP2022102984A Active JP7555998B2 (ja) 2016-08-03 2022-06-27 ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用
JP2024157625A Withdrawn JP2024174998A (ja) 2016-08-03 2024-09-11 ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用

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JP2024157625A Withdrawn JP2024174998A (ja) 2016-08-03 2024-09-11 ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用

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US (1) US11712480B2 (enExample)
EP (1) EP3493853A1 (enExample)
JP (3) JP2018058822A (enExample)
CA (1) CA3032559C (enExample)
WO (1) WO2018025168A1 (enExample)

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JPWO2023068325A1 (enExample) * 2021-10-20 2023-04-27

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ES2721882T3 (es) 2011-12-23 2019-08-06 Pfizer Regiones constantes de anticuerpo modificadas por ingeniería genética para conjugación específica de sitio y procedimientos y usos de las mismas
US11364303B2 (en) 2017-09-29 2022-06-21 Pfizer Inc. Cysteine engineered antibody drug conjugates
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
TW202317205A (zh) * 2021-06-29 2023-05-01 美國公爵大學 用於癌症治療之經放射性標記之parp抑制劑結合物
AU2022380909A1 (en) * 2021-11-03 2024-06-06 Adcentrx Therapeutics Inc. Drug conjugates and methods of preparing and using the same
JP2025522671A (ja) 2022-12-14 2025-07-17 メルク・シャープ・アンド・ドーム・エルエルシー アウリスタチンリンカー-ペイロード、医薬組成物及びその使用
CN120957753A (zh) * 2023-03-23 2025-11-14 广州百济神州生物制药有限公司 生物活性结合物、其制备方法和其用途
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