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

Info

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
Authority
JP
Japan
Prior art keywords
alkyl
antibody
mmol
cancer
methyl
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.)
Withdrawn
Application number
JP2017147506A
Other languages
English (en)
Japanese (ja)
Other versions
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 Inc
Original Assignee
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.)
Filing date
Publication date
Application filed by Pfizer Inc filed Critical Pfizer Inc
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Withdrawn legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • 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
    • A61K47/54Medicinal 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
    • 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
    • A61K47/6801Drug-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
    • 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
    • A61K47/6867Medicinal 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
    • 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
    • A61K47/6889Conjugates 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K4/00Peptides having up to 20 amino acids in an undefined or only partially defined sequence; Derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Cell Biology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • 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)

Application Number Priority Date Filing Date Title
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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
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

Publications (2)

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

Family

ID=59677272

Family Applications (3)

Application Number Title Priority Date Filing Date
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

Family Applications After (2)

Application Number Title Priority Date Filing Date
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

Country Status (5)

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPWO2023068325A1 (enExample) * 2021-10-20 2023-04-27

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015502397A (ja) 2011-12-23 2015-01-22 ファイザー・インク 部位特異的コンジュゲーションのための操作された抗体定常領域、ならびにそのための方法および使用
US11364303B2 (en) 2017-09-29 2022-06-21 Pfizer Inc. Cysteine engineered antibody drug conjugates
CN119241554A (zh) * 2017-12-15 2025-01-03 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
KR20240109256A (ko) * 2021-11-03 2024-07-10 애드센트릭스 테라퓨틱스 잉크. 약물 접합체 및 이의 제조 및 사용 방법
GEAP202516798A (en) 2022-12-14 2025-10-27 Merck Sharp & Dohme Llc Auristatin linker-payloads, pharmaceutical compositions, and uses thereof
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
AR133125A1 (es) * 2023-06-29 2025-08-27 Beigene Switzerland Gmbh Conjugados bioactivos, método de preparación y uso de estos
CN121568721A (zh) * 2023-06-29 2026-02-24 广州百济神州生物制药有限公司 生物活性缀合物、其制备方法和其用途
WO2025261478A1 (en) * 2024-06-21 2025-12-26 Biotheus Inc. Antibody drug conjugates and applications thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014144878A2 (en) * 2013-03-15 2014-09-18 The Scripps Research Institute Novel thiol & amino modifying reagents for protein chemistry and methods of use thereof

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2036891B (en) 1978-12-05 1983-05-05 Windsor Smith C Change speed gear
GB8308235D0 (en) 1983-03-25 1983-05-05 Celltech Ltd Polypeptides
US4816567A (en) 1983-04-08 1989-03-28 Genentech, Inc. Recombinant immunoglobin preparations
JPS6147500A (ja) 1984-08-15 1986-03-07 Res Dev Corp Of Japan キメラモノクロ−ナル抗体及びその製造法
EP0173494A3 (en) 1984-08-27 1987-11-25 The Board Of Trustees Of The Leland Stanford Junior University Chimeric receptors by dna splicing and expression
GB8422238D0 (en) 1984-09-03 1984-10-10 Neuberger M S Chimeric proteins
JPS61134325A (ja) 1984-12-04 1986-06-21 Teijin Ltd ハイブリツド抗体遺伝子の発現方法
DE3689123T2 (de) 1985-11-01 1994-03-03 Xoma Corp Modulare einheit von antikörpergenen, daraus hergestellte antikörper und verwendung.
US5225539A (en) 1986-03-27 1993-07-06 Medical Research Council Recombinant altered antibodies and methods of making altered antibodies
US5225530A (en) 1986-07-16 1993-07-06 Eniricerche S.P.A. Polypeptide useful for the preparation of antimalarial vaccines and of diagnostic kits for the detection of malarial affections
US5530101A (en) 1988-12-28 1996-06-25 Protein Design Labs, Inc. Humanized immunoglobulins
DE3920358A1 (de) 1989-06-22 1991-01-17 Behringwerke Ag Bispezifische und oligospezifische, mono- und oligovalente antikoerperkonstrukte, ihre herstellung und verwendung
US5545806A (en) 1990-08-29 1996-08-13 Genpharm International, Inc. Ransgenic non-human animals for producing heterologous antibodies
US5625126A (en) 1990-08-29 1997-04-29 Genpharm International, Inc. Transgenic non-human animals for producing heterologous antibodies
US5633425A (en) 1990-08-29 1997-05-27 Genpharm International, Inc. Transgenic non-human animals capable of producing heterologous antibodies
US5661016A (en) 1990-08-29 1997-08-26 Genpharm International Inc. Transgenic non-human animals capable of producing heterologous antibodies of various isotypes
ATE158021T1 (de) 1990-08-29 1997-09-15 Genpharm Int Produktion und nützung nicht-menschliche transgentiere zur produktion heterologe antikörper
ATE207080T1 (de) 1991-11-25 2001-11-15 Enzon Inc Multivalente antigen-bindende proteine
US6214345B1 (en) 1993-05-14 2001-04-10 Bristol-Myers Squibb Co. Lysosomal enzyme-cleavable antitumor drug conjugates
US5773001A (en) 1994-06-03 1998-06-30 American Cyanamid Company Conjugates of methyltrithio antitumor agents and intermediates for their synthesis
JP4046354B2 (ja) 1996-03-18 2008-02-13 ボード オブ リージェンツ,ザ ユニバーシティ オブ テキサス システム 増大した半減期を有する免疫グロブリン様ドメイン
US20050287596A9 (en) * 1998-06-26 2005-12-29 Braisted Andrew C Novel ligands and libraries of ligands
US7691962B2 (en) 2004-05-19 2010-04-06 Medarex, Inc. Chemical linkers and conjugates thereof
JP2005330229A (ja) * 2004-05-20 2005-12-02 Ube Ind Ltd 4−トリフルオロメトキシフェニル(オキシ)エチルアミン誘導体及び抗菌剤
DK3248613T3 (da) 2005-07-18 2022-03-14 Seagen Inc Beta-glucuronid-lægemiddel-linkerkonjugater
US8748623B2 (en) 2009-02-17 2014-06-10 Syntrix Biosystems, Inc. Pyridinecarboxamides as CXCR2 modulators
CA2813411C (en) 2010-11-05 2016-08-02 Rinat Neuroscience Corporation Engineered polypeptide conjugates and methods for making thereof using transglutaminase
AU2012322095B2 (en) 2011-10-14 2017-06-29 Ambit Biosciences Corporation Heterocyclic compounds and use thereof as modulators of type III receptor tyrosine kinases
TWI495644B (zh) 2011-11-11 2015-08-11 Rinat Neuroscience Corp 營養層細胞表面抗原(Trop-2)之專一性抗體類及彼等之用途
CN104185477B (zh) 2011-11-17 2017-05-24 辉瑞公司 细胞毒性肽及其抗体‑药物缀合物
JP2015502397A (ja) 2011-12-23 2015-01-22 ファイザー・インク 部位特異的コンジュゲーションのための操作された抗体定常領域、ならびにそのための方法および使用
CN105121421B (zh) 2012-11-05 2020-10-02 辉瑞公司 司普力西欧他汀类似物
WO2015015448A2 (en) 2013-07-31 2015-02-05 Rinat Neuroscience Corp. Engineered polypeptide conjugates
SG11201605437YA (en) 2014-01-27 2016-08-30 Pfizer Bifunctional cytotoxic agents
PT3134127T (pt) 2014-04-25 2020-04-09 Rinat Neuroscience Corp Conjugados de anticorpo-fármaco com alta carga de fármaco
PL3185908T3 (pl) * 2014-08-28 2020-09-07 Pfizer Inc. Łączniki modulujące stabilność do stosowania z koniugatami przeciwciało-lek
US10870706B2 (en) 2015-03-20 2020-12-22 Pfizer Inc. Bifunctional cytotoxic agents containing the CTI pharmacophore

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014144878A2 (en) * 2013-03-15 2014-09-18 The Scripps Research Institute Novel thiol & amino modifying reagents for protein chemistry and methods of use thereof

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
ANGEWANDTE CHEMIE INTERNATIONAL EDITION, vol. 52, no. 48, JPN6021027080, 2013, pages 12592 - 12596, ISSN: 0004560497 *
BIOCONJUGATE CHEMISTRY, vol. 25, JPN6021027081, 2014, pages 1402 - 1407, ISSN: 0004560498 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPWO2023068325A1 (enExample) * 2021-10-20 2023-04-27
WO2023068325A1 (ja) * 2021-10-20 2023-04-27 国立研究開発法人産業技術総合研究所 抗ガン剤、抗ガン剤のプロドラッグ、体外でガン細胞を死滅させる方法、ガンの治療方法、及びガンの治療装置
JP7455316B2 (ja) 2021-10-20 2024-03-26 国立研究開発法人産業技術総合研究所 抗ガン剤、抗ガン剤のプロドラッグ、体外でガン細胞を死滅させる方法、ガンの治療方法、及びガンの治療装置

Also Published As

Publication number Publication date
JP7555998B2 (ja) 2024-09-25
US11712480B2 (en) 2023-08-01
WO2018025168A1 (en) 2018-02-08
CA3032559A1 (en) 2018-02-08
JP2022126826A (ja) 2022-08-30
JP2024174998A (ja) 2024-12-17
US20210308276A1 (en) 2021-10-07
CA3032559C (en) 2022-04-19
EP3493853A1 (en) 2019-06-12

Similar Documents

Publication Publication Date Title
JP7555998B2 (ja) 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
RU2669807C2 (ru) Бифункциональные цитотоксические агенты
US11365263B2 (en) Bifunctional cytotoxic agents containing the CTI pharmacophore
JP2019507126A (ja) ツブリシン類似体およびこれらの調製のための方法
EP3271365B1 (en) Bifunctional cytotoxic agents containing the cti pharmacophore
HK1233252B (zh) 双功能细胞毒类药剂
HK1245252B (zh) 包含cti药效团的双功能细胞毒性剂

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20200702

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20200702

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20210803

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20211013

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20220309

A761 Written withdrawal of application

Free format text: JAPANESE INTERMEDIATE CODE: A761

Effective date: 20220627