KR20240100413A - 인(v) 및 약물 모이어티를 포함하는 접합체 - Google Patents

인(v) 및 약물 모이어티를 포함하는 접합체 Download PDF

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Publication number
KR20240100413A
KR20240100413A KR1020247019065A KR20247019065A KR20240100413A KR 20240100413 A KR20240100413 A KR 20240100413A KR 1020247019065 A KR1020247019065 A KR 1020247019065A KR 20247019065 A KR20247019065 A KR 20247019065A KR 20240100413 A KR20240100413 A KR 20240100413A
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KR
South Korea
Prior art keywords
alkyl
unit
moiety
conjugate
optionally substituted
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Pending
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KR1020247019065A
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English (en)
Korean (ko)
Inventor
크리스티안 하켄베르거
필립 오크트롭
야하질 야체라
파울 마쿠이
도미니크 슈마커
요나스 헬마-스메츠
이자벨 마이
마르크-안드레 카스퍼
Original Assignee
투불리스 게엠베하
포슝스베르분드 베를린 에.베.
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Application filed by 투불리스 게엠베하, 포슝스베르분드 베를린 에.베. filed Critical 투불리스 게엠베하
Publication of KR20240100413A publication Critical patent/KR20240100413A/ko
Pending legal-status Critical Current

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    • 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)

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  • 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)
KR1020247019065A 2021-11-09 2022-11-09 인(v) 및 약물 모이어티를 포함하는 접합체 Pending KR20240100413A (ko)

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
KR20240100413A true KR20240100413A (ko) 2024-07-01

Family

ID=78592631

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020247019065A Pending KR20240100413A (ko) 2021-11-09 2022-11-09 인(v) 및 약물 모이어티를 포함하는 접합체

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

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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
US20250281634A1 (en) 2025-09-11
CN118302197A (zh) 2024-07-05
IL312675A (en) 2024-07-01
JP2024540691A (ja) 2024-10-31
DE22817174T1 (de) 2024-12-12

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PA0105 International application

Patent event date: 20240607

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application