JP7509768B2 - インテグリンリガンドを有する新規な細胞増殖抑制コンジュゲート - Google Patents

インテグリンリガンドを有する新規な細胞増殖抑制コンジュゲート Download PDF

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JP7509768B2
JP7509768B2 JP2021523599A JP2021523599A JP7509768B2 JP 7509768 B2 JP7509768 B2 JP 7509768B2 JP 2021523599 A JP2021523599 A JP 2021523599A JP 2021523599 A JP2021523599 A JP 2021523599A JP 7509768 B2 JP7509768 B2 JP 7509768B2
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cancer
acid
solvate
compounds
compound
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JP2022506299A5 (OSRAM
JP2022506299A (ja
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ラーチェン，ハンス－ジョージ
ステルテ－ルートヴィッヒ，ベアトリクス
コーピッツ，シャーロット，クリスティン
ケルデニヒ，イェルク
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バイエル ファーマ アクチェンゲゼルシャフト
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    • 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
    • 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
    • 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
    • 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)
JP2021523599A 2018-11-05 2019-10-30 インテグリンリガンドを有する新規な細胞増殖抑制コンジュゲート Active JP7509768B2 (ja)

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

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JP2022506299A JP2022506299A (ja) 2022-01-17
JP2022506299A5 JP2022506299A5 (OSRAM) 2022-08-17
JP7509768B2 true JP7509768B2 (ja) 2024-07-02

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

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107921288A (zh) 2015-06-23 2018-04-17 拜耳医药股份有限公司 Ksp抑制剂的靶向缀合物
WO2017216028A1 (en) 2016-06-15 2017-12-21 Bayer Pharma Aktiengesellschaft Specific antibody-drug-conjugates (adcs) with ksp inhibitors and anti-cd123-antibodies
WO2018114804A1 (de) 2016-12-21 2018-06-28 Bayer Pharma Aktiengesellschaft Spezifische antikörper-wirkstoff-konjugate (adcs) mit ksp-inhibitoren
CA3047491A1 (en) 2016-12-21 2018-06-28 Bayer Aktiengesellschaft Prodrugs of cytotoxic active agents having enzymatically cleavable groups
KR102556826B1 (ko) 2016-12-21 2023-07-18 바이엘 파마 악티엔게젤샤프트 효소적으로 절단가능한 기를 갖는 항체 약물 접합체 (adc)
EP3876993A1 (en) * 2018-11-05 2021-09-15 Bayer Pharma Aktiengesellschaft Cytostatic conjugates with integrin ligands
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
CN118556062A (zh) 2021-10-04 2024-08-27 文赛克斯制药有限责任公司 用于治疗、预防或管理过度增殖病症的化合物、药物组合物和方法
JP2024536628A (ja) 2021-10-04 2024-10-04 ヴィンセルクス ファーマ ゲーエムベーハー 過剰増殖性障害の処置、予防、または管理のための化合物、医薬組成物、および方法
EP4619044A1 (en) 2022-11-17 2025-09-24 Hans-Georg Lerchen Antibody-drug-conjugates cleavable in a tumor microenvironment
JP2025537882A (ja) 2022-11-17 2025-11-20 ハンス－ゲオルク レルケン 腫瘍微小環境において切断可能な小分子－薬物コンジュゲート
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004529118A (ja) 2001-03-08 2004-09-24 バイエル アクチェンゲゼルシャフト インテグリンリガンドを有する酵素活性化細胞分裂停止接合体
JP2011523415A (ja) 2008-05-20 2011-08-11 シグマ−タウ・インドゥストリエ・ファルマチェウチケ・リウニテ・ソシエタ・ペル・アチオニ 新規な二重標的化抗腫瘍複合体

Family Cites Families (10)

* 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
JP2001501600A (ja) 1996-09-10 2001-02-06 ザ バーナム インスティテュート 腫瘍ホーミング分子、それに由来する結合体、およびその使用方法
MXPA01011502A (es) 1999-05-14 2003-08-20 Boehringer Ingelheim Pharma Compuestos de tipo profarmaco anti-tumorigenos, activados por enzimas.
EP3876993A1 (en) * 2018-11-05 2021-09-15 Bayer Pharma Aktiengesellschaft Cytostatic conjugates with integrin ligands

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004529118A (ja) 2001-03-08 2004-09-24 バイエル アクチェンゲゼルシャフト インテグリンリガンドを有する酵素活性化細胞分裂停止接合体
JP2011523415A (ja) 2008-05-20 2011-08-11 シグマ−タウ・インドゥストリエ・ファルマチェウチケ・リウニテ・ソシエタ・ペル・アチオニ 新規な二重標的化抗腫瘍複合体

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IL282748B1 (en) 2025-03-01
WO2020094471A1 (en) 2020-05-14
SG11202104491SA (en) 2021-05-28
BR112021008232A2 (pt) 2021-08-03
US20210386864A1 (en) 2021-12-16
EA202191244A1 (ru) 2021-10-11
MX2021005134A (es) 2021-07-07
EP3876993A1 (en) 2021-09-15
TW202039005A (zh) 2020-11-01
IL282748A (en) 2021-06-30
CN113260382A (zh) 2021-08-13
AR116999A1 (es) 2021-06-30
IL282748B2 (en) 2025-07-01
CA3118041A1 (en) 2020-05-14
US20240325553A1 (en) 2024-10-03
CN113260382B (zh) 2024-09-13
AU2019376293A1 (en) 2021-06-03
CL2021001142A1 (es) 2021-11-12
JP2022506299A (ja) 2022-01-17
KR20210100607A (ko) 2021-08-17

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