CN118302197A - 包含磷(v)和药物部分的偶联物 - Google Patents

包含磷(v)和药物部分的偶联物 Download PDF

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Publication number
CN118302197A
CN118302197A CN202280074835.4A CN202280074835A CN118302197A CN 118302197 A CN118302197 A CN 118302197A CN 202280074835 A CN202280074835 A CN 202280074835A CN 118302197 A CN118302197 A CN 118302197A
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CN
China
Prior art keywords
alkyl
unit
optionally substituted
linker
integer
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
CN202280074835.4A
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English (en)
Chinese (zh)
Inventor
C·哈肯伯格
P·奥赫特罗普
J·约泽拉
P·马丘
D·舒马赫
J·赫尔马·斯梅茨
I·迈
M·A·卡斯帕
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.)
Forschungsverbund Berlin FVB eV
Tubulis GmbH
Original Assignee
Forschungsverbund Berlin FVB eV
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 Forschungsverbund Berlin FVB eV, Tubulis GmbH filed Critical Forschungsverbund Berlin FVB eV
Publication of CN118302197A publication Critical patent/CN118302197A/zh
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
    • A61K47/6889—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
    • 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
    • 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
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • 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
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/44—Amides thereof
    • C07F9/4461—Amides thereof the amide moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4476—Amides thereof the amide moiety containing a substituent or a structure which is considered as characteristic of aromatic amines (N-C aromatic linkage)

Landscapes

  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
CN202280074835.4A 2021-11-09 2022-11-09 包含磷(v)和药物部分的偶联物 Pending CN118302197A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP21207195 2021-11-09
EP21207195.5 2021-11-09
PCT/EP2022/081345 WO2023083900A1 (en) 2021-11-09 2022-11-09 Conjugates comprising a phosphorus (v) and a drug moiety

Publications (1)

Publication Number Publication Date
CN118302197A true CN118302197A (zh) 2024-07-05

Family

ID=78592631

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202280074835.4A Pending CN118302197A (zh) 2021-11-09 2022-11-09 包含磷(v)和药物部分的偶联物

Country Status (15)

Country Link
US (2) US20230330258A1 (https=)
EP (1) EP4429708A1 (https=)
JP (1) JP2024540691A (https=)
KR (1) KR20240100413A (https=)
CN (1) CN118302197A (https=)
AU (1) AU2022385379A1 (https=)
CA (1) CA3237371A1 (https=)
CL (1) CL2024001372A1 (https=)
CO (1) CO2024005877A2 (https=)
DE (1) DE22817174T1 (https=)
ES (1) ES2999335T1 (https=)
IL (1) IL312675A (https=)
MX (1) MX2024005546A (https=)
PE (1) PE20242107A1 (https=)
WO (1) WO2023083900A1 (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024133845A1 (en) * 2022-12-22 2024-06-27 Tubulis Gmbh Conjugates comprising a phosphorus(v) moiety and a drug
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

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US633410A (en) 1898-09-22 1899-09-19 George A Ames Ice-cutter.
EP0401384B1 (en) 1988-12-22 1996-03-13 Kirin-Amgen, Inc. Chemically modified granulocyte colony stimulating factor
US5208020A (en) 1989-10-25 1993-05-04 Immunogen Inc. Cytotoxic agents comprising maytansinoids and their therapeutic use
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
KR20200058590A (ko) 2008-04-30 2020-05-27 이뮤노젠 아이엔씨 가교제 및 그 용도
ES2826398T3 (es) 2013-10-15 2021-05-18 Seagen Inc Enlazadores-fármacos pegilados para una mejor farmacocinética de los conjugados ligando-fármaco
AU2017320913B2 (en) 2016-09-01 2024-08-15 Forschungsverbund Berlin E.V. Chemoselective thiol-conjugation with alkene or alkyne-phosphonamidates
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
TWI851577B (zh) 2018-06-07 2024-08-11 美商思進公司 喜樹鹼結合物

Also Published As

Publication number Publication date
PE20242107A1 (es) 2024-10-28
CA3237371A1 (en) 2023-05-19
AU2022385379A1 (en) 2024-06-20
WO2023083900A1 (en) 2023-05-19
MX2024005546A (es) 2024-07-10
CO2024005877A2 (es) 2024-07-08
CL2024001372A1 (es) 2024-10-25
EP4429708A1 (en) 2024-09-18
US20230330258A1 (en) 2023-10-19
ES2999335T1 (en) 2025-02-25
KR20240100413A (ko) 2024-07-01
US20250281634A1 (en) 2025-09-11
IL312675A (en) 2024-07-01
JP2024540691A (ja) 2024-10-31
DE22817174T1 (de) 2024-12-12

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