KR20210100607A - 인테그린 리간드를 갖는 세포증식억제 콘쥬게이트 - Google Patents

인테그린 리간드를 갖는 세포증식억제 콘쥬게이트 Download PDF

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Publication number
KR20210100607A
KR20210100607A KR1020217015569A KR20217015569A KR20210100607A KR 20210100607 A KR20210100607 A KR 20210100607A KR 1020217015569 A KR1020217015569 A KR 1020217015569A KR 20217015569 A KR20217015569 A KR 20217015569A KR 20210100607 A KR20210100607 A KR 20210100607A
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South Korea
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acid
compounds
salts
compound
treatment
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KR1020217015569A
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Korean (ko)
Inventor
한스-게오르그 러헨
베아트릭스 슈텔테-루트빅
샤를로테 크리스티네 코피츠
외르그 켈데니히
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바이엘 파마 악티엔게젤샤프트
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Publication of KR20210100607A publication Critical patent/KR20210100607A/ko
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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
    • A61K47/54—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
    • 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
    • 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
    • A61K47/56—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
KR1020217015569A 2018-11-05 2019-10-30 인테그린 리간드를 갖는 세포증식억제 콘쥬게이트 Ceased KR20210100607A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP18204423 2018-11-05
EP18204423.0 2018-11-05
PCT/EP2019/079601 WO2020094471A1 (en) 2018-11-05 2019-10-30 Cytostatic conjugates with integrin ligands

Publications (1)

Publication Number Publication Date
KR20210100607A true KR20210100607A (ko) 2021-08-17

Family

ID=64453279

Family Applications (1)

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KR1020217015569A Ceased KR20210100607A (ko) 2018-11-05 2019-10-30 인테그린 리간드를 갖는 세포증식억제 콘쥬게이트

Country Status (16)

Country Link
US (2) US20210386864A1 (enExample)
EP (1) EP3876993A1 (enExample)
JP (1) JP7509768B2 (enExample)
KR (1) KR20210100607A (enExample)
CN (1) CN113260382B (enExample)
AR (1) AR116999A1 (enExample)
AU (1) AU2019376293A1 (enExample)
BR (1) BR112021008232A2 (enExample)
CA (1) CA3118041A1 (enExample)
CL (1) CL2021001142A1 (enExample)
EA (1) EA202191244A1 (enExample)
IL (1) IL282748B2 (enExample)
MX (1) MX2021005134A (enExample)
SG (1) SG11202104491SA (enExample)
TW (1) TW202039005A (enExample)
WO (1) WO2020094471A1 (enExample)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2017017138A (es) 2015-06-23 2018-04-30 Bayer Pharma AG Conjugados homogeneos especificos de sitio con inhibidores de ksp.
WO2017216028A1 (en) 2016-06-15 2017-12-21 Bayer Pharma Aktiengesellschaft Specific antibody-drug-conjugates (adcs) with ksp inhibitors and anti-cd123-antibodies
AU2017380871C1 (en) 2016-12-21 2025-05-15 Bayer Aktiengesellschaft Antibody drug conjugates (ADCs) having enzymatically cleavable groups
US12059472B2 (en) 2016-12-21 2024-08-13 Bayer Aktiengesellschaft Prodrugs of cytotoxic active agents having enzymatically cleavable groups
US11433140B2 (en) 2016-12-21 2022-09-06 Bayer Pharma Aktiengesellschaft Specific antibody drug conjugates (ADCs) having KSP inhibitors
MX2021005134A (es) * 2018-11-05 2021-07-07 Bayer Pharma AG Nuevos conjugados citostaticos con ligandos de integrina.
EP4413006A1 (en) 2021-10-04 2024-08-14 Vincerx Pharma GmbH Compounds, pharmaceutical compositions, and methods for the treatment, prevention, or management of hyperproliferative disorders
EP4412656A1 (en) 2021-10-04 2024-08-14 Vincerx Pharma GmbH Compounds, pharmaceutical compositions, and methods for the treatment, prevention, or management of hyperproliferative disorders
US20240408222A1 (en) 2021-10-04 2024-12-12 Vincerx Pharma Gmbh Compounds, pharmaceutical compositions, and methods for the treatment, prevention, or management of hyperproliferative disorder
WO2024105206A1 (en) 2022-11-17 2024-05-23 Vincerx Pharma Gmbh Antibody-drug-conjugates cleavable in a tumor microenvironment
TW202430150A (zh) 2022-11-17 2024-08-01 德商溫瑟克斯製藥公司 在腫瘤微環境中可裂解之小分子藥物結合物
US12624109B2 (en) * 2023-04-25 2026-05-12 Targetthera Llc αv-integrin targeted small molecule drug conjugates
CN119143798B (zh) * 2024-08-01 2025-09-30 河北医科大学 一种骨靶向阿仑膦酸-普萘洛尔及其制备方法与应用

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8705477D0 (en) 1987-03-09 1987-04-15 Carlton Med Prod Drug delivery systems
US4975278A (en) 1988-02-26 1990-12-04 Bristol-Myers Company Antibody-enzyme conjugates in combination with prodrugs for the delivery of cytotoxic agents to tumor cells
US4943579A (en) 1987-10-06 1990-07-24 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Water soluble prodrugs of camptothecin
FR2676058B1 (fr) 1991-04-30 1994-02-25 Hoechst Lab Prodrogues glycosylees, leur procede de preparation et leur utilisation dans le traitement des cancers.
DE4229903A1 (de) 1992-09-08 1994-03-10 Bayer Ag Neue Acetale von Ketophosphamid und Alkylglycosiden
DE4236237A1 (de) 1992-10-27 1994-04-28 Behringwerke Ag Prodrugs, ihre Herstellung und Verwendung als Arzneimittel
US5646159A (en) 1994-07-20 1997-07-08 Research Triangle Institute Water-soluble esters of camptothecin compounds
WO1998010795A2 (en) 1996-09-10 1998-03-19 The Burnham Institute Tumor homing molecules, conjugates derived therefrom, and methods of using same
MXPA01011502A (es) 1999-05-14 2003-08-20 Boehringer Ingelheim Pharma Compuestos de tipo profarmaco anti-tumorigenos, activados por enzimas.
EP1238678A1 (en) 2001-03-08 2002-09-11 Bayer Aktiengesellschaft Enzyme-activated cytostatic conjugates with integrin ligands
TW201004647A (en) 2008-05-20 2010-02-01 Sigma Tau Ind Farmaceuti Novel dual targeting antitumoural conjugates
MX2021005134A (es) * 2018-11-05 2021-07-07 Bayer Pharma AG Nuevos conjugados citostaticos con ligandos de integrina.

Also Published As

Publication number Publication date
IL282748B2 (en) 2025-07-01
WO2020094471A1 (en) 2020-05-14
CN113260382B (zh) 2024-09-13
BR112021008232A2 (pt) 2021-08-03
TW202039005A (zh) 2020-11-01
EP3876993A1 (en) 2021-09-15
EA202191244A1 (ru) 2021-10-11
AU2019376293A1 (en) 2021-06-03
US20210386864A1 (en) 2021-12-16
IL282748A (en) 2021-06-30
IL282748B1 (en) 2025-03-01
SG11202104491SA (en) 2021-05-28
JP7509768B2 (ja) 2024-07-02
MX2021005134A (es) 2021-07-07
JP2022506299A (ja) 2022-01-17
AR116999A1 (es) 2021-06-30
CA3118041A1 (en) 2020-05-14
CN113260382A (zh) 2021-08-13
US20240325553A1 (en) 2024-10-03
CL2021001142A1 (es) 2021-11-12

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