CA3237379A1 - Conjugates comprising a phosphorus (v) and a camptothecin moiety - Google Patents

Conjugates comprising a phosphorus (v) and a camptothecin moiety Download PDF

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Publication number
CA3237379A1
CA3237379A1 CA3237379A CA3237379A CA3237379A1 CA 3237379 A1 CA3237379 A1 CA 3237379A1 CA 3237379 A CA3237379 A CA 3237379A CA 3237379 A CA3237379 A CA 3237379A CA 3237379 A1 CA3237379 A1 CA 3237379A1
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CA
Canada
Prior art keywords
optionally substituted
unit
conjugate
alkyl
group
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.)
Pending
Application number
CA3237379A
Other languages
English (en)
French (fr)
Inventor
Marc-Andre Kasper
Paul MACHUI
Isabelle MAI
Annette VOGL
Saskia SCHMITT
Dominik SCHUMACHER
Jonas HELMA-SMETS
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.)
Tubulis GmbH
Original Assignee
Tubulis GmbH
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 Tubulis GmbH filed Critical Tubulis GmbH
Publication of CA3237379A1 publication Critical patent/CA3237379A1/en
Pending legal-status Critical Current

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Classifications

    • 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
    • A61K47/68037—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a camptothecin [CPT] or derivatives
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K47/68—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
    • A61K47/6807—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug or compound being a sugar, nucleoside, nucleotide, nucleic acid, e.g. RNA antisense
    • A61K47/6809—Antibiotics, e.g. antitumor antibiotics anthracyclins, adriamycin, doxorubicin or daunomycin
    • 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
    • A61K47/6889—Conjugates 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
CA3237379A 2021-11-09 2022-11-09 Conjugates comprising a phosphorus (v) and a camptothecin moiety Pending CA3237379A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP21207284.7 2021-11-09
EP21207284 2021-11-09
PCT/EP2022/081371 WO2023083919A1 (en) 2021-11-09 2022-11-09 Conjugates comprising a phosphorus (v) and a camptothecin moiety

Publications (1)

Publication Number Publication Date
CA3237379A1 true CA3237379A1 (en) 2023-05-19

Family

ID=78592674

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3237379A Pending CA3237379A1 (en) 2021-11-09 2022-11-09 Conjugates comprising a phosphorus (v) and a camptothecin moiety

Country Status (16)

Country Link
US (1) US20230158154A1 (https=)
EP (1) EP4429709A1 (https=)
JP (1) JP2024540692A (https=)
KR (1) KR20240100415A (https=)
CN (1) CN118302198A (https=)
AU (1) AU2022386680A1 (https=)
CA (1) CA3237379A1 (https=)
CL (1) CL2024001373A1 (https=)
CO (1) CO2024005880A2 (https=)
DE (1) DE22817180T1 (https=)
ES (1) ES3001145T1 (https=)
IL (1) IL312677A (https=)
MX (1) MX2024005545A (https=)
PE (1) PE20242114A1 (https=)
TW (1) TW202339803A (https=)
WO (1) WO2023083919A1 (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025027529A1 (en) 2023-07-31 2025-02-06 Advesya Anti-il-1rap antibody drug conjugates and methods of use thereof
WO2025046090A1 (en) 2023-09-01 2025-03-06 Tubulis Gmbh Methods of preparing phosphonamidate compounds
TW202530255A (zh) 2023-12-15 2025-08-01 法商亞維西亞有限公司 抗ｉｌ－１ｒａｐ結合結構域及其抗體－藥物偶聯物
WO2025149667A1 (en) 2024-01-12 2025-07-17 Pheon Therapeutics Ltd Antibody drug conjugates and uses thereof
EP4658320A1 (en) * 2024-02-27 2025-12-10 Bristol-Myers Squibb Company Anti-ceacam5 antibody drug conjugates
WO2025262641A1 (en) 2024-06-19 2025-12-26 Pheon Therapeutics Ltd Antibody drug conjugates that bind cdcp1 and uses thereof
WO2026016639A1 (zh) * 2024-07-19 2026-01-22 昆山新蕴达生物科技有限公司 一种靶向adam-9的抗体-药物偶联物及其制备方法和用途

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EP0401384B1 (en) 1988-12-22 1996-03-13 Kirin-Amgen, Inc. Chemically modified granulocyte colony stimulating factor
JP3008226B2 (ja) 1991-01-16 2000-02-14 第一製薬株式会社 六環性化合物
AP9300587A0 (en) * 1992-11-12 1995-05-05 Glaxo Inc Water soluble camptothecin derivatives.
JP2763020B2 (ja) 1995-04-27 1998-06-11 日本電気株式会社 半導体パッケージ及び半導体装置
US5672662A (en) 1995-07-07 1997-09-30 Shearwater Polymers, Inc. Poly(ethylene glycol) and related polymers monosubstituted with propionic or butanoic acids and functional derivatives thereof for biotechnical applications
AU725609C (en) 1995-08-18 2002-01-03 Morphosys Ag Protein/(poly)peptide libraries
EP1731174A3 (en) 1996-08-02 2007-01-17 Ortho-McNeil Pharmaceutical, Inc. Polypeptides having a covalently bound N-terminal polyethylene glycol via hydrazone or oxime bond
SI1545613T1 (sl) 2002-07-31 2011-11-30 Seattle Genetics Inc Avristatinski konjugati in njihova uporaba za zdravljenje raka avtoimunske bolezni ali infekcijskebolezni
PE20100251A1 (es) 2004-09-10 2010-04-10 Wyeth Corp Anticuerpos anti-5t4 humanizados y conjugados anticuerpo anti-5t4/calicheamicina
US7687496B2 (en) * 2007-10-16 2010-03-30 Bionumerik Pharmaceuticals, Inc. C7-substituted camptothecin analogs
KR20200058590A (ko) 2008-04-30 2020-05-27 이뮤노젠 아이엔씨 가교제 및 그 용도
AU2009293140A1 (en) * 2008-09-17 2010-03-25 Endocyte, Inc. Folate receptor binding conjugates of antifolates
ES2826398T3 (es) 2013-10-15 2021-05-18 Seagen Inc Enlazadores-fármacos pegilados para una mejor farmacocinética de los conjugados ligando-fármaco
CN109310885B (zh) 2016-03-15 2022-05-31 梅尔莎纳医疗公司 NaPi2b靶向抗体-药物缀合物及其使用方法
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JP7429191B2 (ja) 2018-03-07 2024-02-07 フォルシュングスフェアバント ベルリン エー．ベー． アルケンホスホノチオレートまたはアルキンホスホノチオレートおよびアルケンホスホネートまたはアルキンホスホネートとの化学選択的チオールコンジュゲーション
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Also Published As

Publication number Publication date
WO2023083919A1 (en) 2023-05-19
TW202339803A (zh) 2023-10-16
CO2024005880A2 (es) 2024-07-08
KR20240100415A (ko) 2024-07-01
CN118302198A (zh) 2024-07-05
AU2022386680A1 (en) 2024-06-20
IL312677A (en) 2024-07-01
US20230158154A1 (en) 2023-05-25
JP2024540692A (ja) 2024-10-31
CL2024001373A1 (es) 2024-10-25
DE22817180T1 (de) 2024-12-12
EP4429709A1 (en) 2024-09-18
PE20242114A1 (es) 2024-10-28
ES3001145T1 (es) 2025-03-04
MX2024005545A (es) 2024-07-19

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