JP7218351B2 - 新たな標的化された細胞傷害性ラトジャドン誘導体及びそのコンジュゲート - Google Patents

新たな標的化された細胞傷害性ラトジャドン誘導体及びそのコンジュゲート Download PDF

Info

Publication number
JP7218351B2
JP7218351B2 JP2020506940A JP2020506940A JP7218351B2 JP 7218351 B2 JP7218351 B2 JP 7218351B2 JP 2020506940 A JP2020506940 A JP 2020506940A JP 2020506940 A JP2020506940 A JP 2020506940A JP 7218351 B2 JP7218351 B2 JP 7218351B2
Authority
JP
Japan
Prior art keywords
amino
methyl
esi
μmol
ppm
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
JP2020506940A
Other languages
English (en)
Japanese (ja)
Other versions
JP2020529457A (ja
JP2020529457A5 (enExample
Inventor
クラーン フィリップ
ブレンストループ マルク
フェッツ ベレナ
コリッシ ベーラ
イー．モーア カトリン
ヒュッテル シュテファン
テッゲ ベルナー
Original Assignee
ヘルムホルツ－ツェントルン フュル インフェクティオンスフォルシュング ゲゼルシャフト ミット ベシュレンクテル ハフツング
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 ヘルムホルツ－ツェントルン フュル インフェクティオンスフォルシュング ゲゼルシャフト ミット ベシュレンクテル ハフツング filed Critical ヘルムホルツ－ツェントルン フュル インフェクティオンスフォルシュング ゲゼルシャフト ミット ベシュレンクテル ハフツング
Publication of JP2020529457A publication Critical patent/JP2020529457A/ja
Publication of JP2020529457A5 publication Critical patent/JP2020529457A5/ja
Application granted granted Critical
Publication of JP7218351B2 publication Critical patent/JP7218351B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/16—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D309/28—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D309/30—Oxygen atoms, e.g. delta-lactones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/32—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • 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
    • A61K47/55—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 also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • A61K47/551—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 also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic acid
    • 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
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2020506940A 2017-08-09 2018-08-08 新たな標的化された細胞傷害性ラトジャドン誘導体及びそのコンジュゲート Active JP7218351B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP17185598 2017-08-09
EP17185598.4 2017-08-09
PCT/EP2018/071507 WO2019030284A1 (en) 2017-08-09 2018-08-08 NOVEL TARGETED CYTOTOXIC RATJADONE DERIVATIVES AND CONJUGATES THEREOF

Publications (3)

Publication Number Publication Date
JP2020529457A JP2020529457A (ja) 2020-10-08
JP2020529457A5 JP2020529457A5 (enExample) 2021-09-24
JP7218351B2 true JP7218351B2 (ja) 2023-02-06

Family

ID=59579518

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2020506940A Active JP7218351B2 (ja) 2017-08-09 2018-08-08 新たな標的化された細胞傷害性ラトジャドン誘導体及びそのコンジュゲート

Country Status (6)

Country Link
US (1) US11236059B2 (enExample)
EP (1) EP3665161B1 (enExample)
JP (1) JP7218351B2 (enExample)
AU (1) AU2018315154B2 (enExample)
CA (1) CA3072399A1 (enExample)
WO (1) WO2019030284A1 (enExample)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022530823A (ja) * 2019-05-02 2022-07-01 ザ・ユニバーシティ・オブ・シドニー がん治療のためのペプチド誘導体とそのコンジュゲート

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040092581A1 (en) 2001-02-12 2004-05-13 Arne Burzlaff Ratjadone derivatives for inhibiting cell growth
JP2009538920A (ja) 2006-06-01 2009-11-12 シェーリング−プラウ ヘルスケア プロダクツ，インコーポレイテッド 結腸吸収のためのフェニレフリン薬学的製剤および組成物
JP2009539820A (ja) 2006-06-09 2009-11-19 サノフイ−アベンテイス レプトマイシン誘導体
JP2016525560A (ja) 2013-08-02 2016-08-25 サノフイ 固形腫瘍を処置するための抗−Ｍｕｃ１メイタンシノイドイムノコンジュゲート抗体の使用

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69133566T2 (de) 1990-01-12 2007-12-06 Amgen Fremont Inc. Bildung von xenogenen Antikörpern
DE69112684T2 (de) * 1990-04-06 1996-02-01 Univ Tulane LHRH-Analoge.
DE19636721A1 (de) 1996-09-10 1998-03-12 Biotechnolog Forschung Gmbh Antibiotische und antitumorale Verbindung, Herstellungsverfahren, Mittel und DSM 11 071
EP1391213A1 (en) 2002-08-21 2004-02-25 Boehringer Ingelheim International GmbH Compositions and methods for treating cancer using maytansinoid CD44 antibody immunoconjugates and chemotherapeutic agents
US7446196B2 (en) 2004-06-03 2008-11-04 Kosan Biosciences, Incorporated Leptomycin compounds
US7541330B2 (en) 2004-06-15 2009-06-02 Kosan Biosciences Incorporated Conjugates with reduced adverse systemic effects
FR2947269B1 (fr) 2009-06-29 2013-01-18 Sanofi Aventis Nouveaux composes anticancereux
US20110256157A1 (en) 2010-04-15 2011-10-20 Spirogen Limited Pyrrolobenzodiazepines and conjugates thereof
JP6855661B2 (ja) 2012-10-23 2021-04-07 シンアフィックス ビー．ブイ． 修飾抗体、抗体コンジュゲート及びそれらを調製する方法
ES2819573T3 (es) 2012-12-13 2021-04-16 Immunomedics Inc Método para producir inmunoconjugados de anticuerpo-SN-38 con un enlazador CL2A

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040092581A1 (en) 2001-02-12 2004-05-13 Arne Burzlaff Ratjadone derivatives for inhibiting cell growth
JP2009538920A (ja) 2006-06-01 2009-11-12 シェーリング−プラウ ヘルスケア プロダクツ，インコーポレイテッド 結腸吸収のためのフェニレフリン薬学的製剤および組成物
JP2009539820A (ja) 2006-06-09 2009-11-19 サノフイ−アベンテイス レプトマイシン誘導体
JP2016525560A (ja) 2013-08-02 2016-08-25 サノフイ 固形腫瘍を処置するための抗−Ｍｕｃ１メイタンシノイドイムノコンジュゲート抗体の使用

Also Published As

Publication number Publication date
EP3665161A1 (en) 2020-06-17
US11236059B2 (en) 2022-02-01
AU2018315154A1 (en) 2020-02-27
CA3072399A1 (en) 2019-02-14
EP3665161B1 (en) 2023-09-27
US20200239426A1 (en) 2020-07-30
JP2020529457A (ja) 2020-10-08
AU2018315154B2 (en) 2022-11-10
WO2019030284A1 (en) 2019-02-14

Similar Documents

Publication Publication Date Title
JP7362714B2 (ja) アマニチンコンジュゲート
JP7482191B2 (ja) γ－アマニチンの誘導体
CN114728073B (zh) 药物从生物活性化合物的内化缀合物的选择性释放
JP2022105640A (ja) 四級化チューブリシン化合物の複合体
JP2019142870A (ja) ヒドラジニル−ピロロ化合物及び複合体を生成するための方法
CN120665147A (zh) 具有针对抗体的亲和性物质和生物正交性官能团的化合物或其盐
JP2018506509A (ja) 細胞透過性Ｂｃｌ−ｘＬ阻害剤との抗体薬物コンジュゲート
EP4213884A1 (en) Molecules with solubility tag and related methods
JP2024506300A (ja) 免疫刺激化合物及びコンジュゲート体
BR112020004307A2 (pt) análogos de tailanestatina
CN117551032A (zh) 包含喹啉衍生物的药物偶联物
US9486535B2 (en) Methods of making and using nanostructures
JP7218351B2 (ja) 新たな標的化された細胞傷害性ラトジャドン誘導体及びそのコンジュゲート
US20250082768A1 (en) Conjugating reagents and conjugates thereof
US12377164B2 (en) Linkers and conjugates
US20250152723A1 (en) Antibody-drug conjugates involving erianin and the fabrication methods and applications thereof
TWI900494B (zh) 從生物活性化合物的內化共軛物選擇性釋出藥物
HK40076663B (zh) 药物从生物活性化合物的内化缀合物的选择性释放
BISBAL LOPEZ Tumor-Targeted Release of Immunostimulatory Agents: Synthesis and Biological Evaluation of Imidazoquinoline-Based Prodrugs and Antibody Conjugates
HK40076663A (en) Selective drug release from internalized conjugates of biologically active compounds

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20210806

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20210806

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20220728

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20220802

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20221102

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20230110

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20230125

R150 Certificate of patent or registration of utility model

Ref document number: 7218351

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150