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
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JP2022506299A (ja
JP2022506299A5 (https=
JPWO2020094471A5 (https=
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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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)

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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 (https=) 2022-08-17
JPWO2020094471A5 JPWO2020094471A5 (https=) 2022-08-17
JP7509768B2 true JP7509768B2 (ja) 2024-07-02

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

Families Citing this family (13)

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RU2018102358A (ru) 2015-06-23 2019-07-25 Байер Фарма Акциенгезельшафт Нацеленные конъюгаты ksp ингибиторов
WO2017216028A1 (en) 2016-06-15 2017-12-21 Bayer Pharma Aktiengesellschaft Specific antibody-drug-conjugates (adcs) with ksp inhibitors and anti-cd123-antibodies
JP7030811B2 (ja) 2016-12-21 2022-03-07 バイエル・ファルマ・アクティエンゲゼルシャフト Ｋｓｐ阻害剤を有する特異的抗体－薬物コンジュゲート（ａｄｃ）
CA3047491A1 (en) 2016-12-21 2018-06-28 Bayer Aktiengesellschaft Prodrugs of cytotoxic active agents having enzymatically cleavable groups
JP7066714B2 (ja) 2016-12-21 2022-05-13 バイエル・ファルマ・アクティエンゲゼルシャフト 酵素的に切断可能な基を有する抗体薬物コンジュゲート（ａｄｃ）
KR20210100607A (ko) * 2018-11-05 2021-08-17 바이엘 파마 악티엔게젤샤프트 인테그린 리간드를 갖는 세포증식억제 콘쥬게이트
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
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
CN118354796A (zh) 2021-10-04 2024-07-16 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
TW202434305A (zh) 2022-11-17 2024-09-01 德商溫瑟克斯製藥公司 於腫瘤微環境中可裂解之抗體-藥物結合物
EP4619037A1 (en) 2022-11-17 2025-09-24 Hans-Georg Lerchen Small molecule-drug-conjugates cleavable in a tumor microenvironment
US20240376212A1 (en) * 2023-04-25 2024-11-14 Targetthera Llc Alpha v-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

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

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