CN112074290B - 整联蛋白靶向配体和其用途 - Google Patents

整联蛋白靶向配体和其用途 Download PDF

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Publication number
CN112074290B
CN112074290B CN201980028704.0A CN201980028704A CN112074290B CN 112074290 B CN112074290 B CN 112074290B CN 201980028704 A CN201980028704 A CN 201980028704A CN 112074290 B CN112074290 B CN 112074290B
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integrin
mmol
compound
group
integrin targeting
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Chinese (zh)
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CN112074290A (zh
Inventor
李珍
J·卡尔森
A·尼古拉斯
X·李
D·舒
M·富勒-沃特斯
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Arrowhead Pharmaceuticals Inc
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Arrowhead Pharmaceuticals Inc
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088Compounds having three or more nucleosides or nucleotides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/545Heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/56Medicinal 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
    • A61K47/59Medicinal 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
    • A61K47/60Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K48/00Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/70546Integrin superfamily
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/70546Integrin superfamily
    • C07K14/70557Integrin beta3-subunit-containing molecules, e.g. CD41, CD51, CD61
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09Recombinant DNA-technology
    • C12N15/11DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00Structure or type of the nucleic acid
    • C12N2310/10Type of nucleic acid
    • C12N2310/14Type of nucleic acid interfering nucleic acids [NA]

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Biotechnology (AREA)
  • Biomedical Technology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Wood Science & Technology (AREA)
  • Toxicology (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Cell Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Physics & Mathematics (AREA)
  • Plant Pathology (AREA)
  • Microbiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
CN201980028704.0A 2018-04-27 2019-04-26 整联蛋白靶向配体和其用途 Active CN112074290B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202411099363.5A CN118994152A (zh) 2018-04-27 2019-04-26 整联蛋白靶向配体和其用途

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862663763P 2018-04-27 2018-04-27
US62/663763 2018-04-27
US201962790372P 2019-01-09 2019-01-09
US62/790372 2019-01-09
PCT/US2019/029393 WO2019210200A1 (en) 2018-04-27 2019-04-26 Integrin targeting ligands and uses thereof

Related Child Applications (1)

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CN112074290A CN112074290A (zh) 2020-12-11
CN112074290B true CN112074290B (zh) 2024-09-10

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EP (2) EP3784269B1 (enExample)
JP (2) JP7704529B2 (enExample)
KR (1) KR102787533B1 (enExample)
CN (2) CN112074290B (enExample)
AU (1) AU2019260738B2 (enExample)
BR (1) BR112020021949A2 (enExample)
CA (1) CA3097656A1 (enExample)
DK (1) DK3784269T3 (enExample)
ES (1) ES2983950T3 (enExample)
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HR (1) HRP20240907T1 (enExample)
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Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2021008261A (es) 2019-01-09 2021-08-16 Arrowhead Pharmaceuticals Inc Agentes de rnai para inhibir la expresion de hif-2 a (epas1), composiciones de estos y metodos de uso.
WO2022056266A2 (en) * 2020-09-11 2022-03-17 Arrowhead Pharmaceuticals, Inc. Rnai agents for inhibiting expression of dux4, compositions thereof, and methods of use
EP4367246A2 (en) * 2021-07-07 2024-05-15 Alnylam Pharmaceuticals, Inc. Integrin targeting ligands for ocular delivery of rnai compounds
WO2024260259A1 (zh) * 2023-06-19 2024-12-26 广东众生睿创生物科技有限公司 一种整合素配体及其用途
WO2025252118A1 (zh) * 2024-06-06 2025-12-11 苏州瑞博生物技术股份有限公司 整联蛋白αvβ6特异性配体化合物、缀合物、药物组合物及其用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1284944A (zh) * 1997-12-17 2001-02-21 麦克公司 整联蛋白受体拮抗剂
CN102026671A (zh) * 2008-03-14 2011-04-20 Visen医药公司 整联蛋白靶向试剂及使用其的体内和体外成像方法

Family Cites Families (12)

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US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US6017926A (en) * 1997-12-17 2000-01-25 Merck & Co., Inc. Integrin receptor antagonists
US6048861A (en) * 1997-12-17 2000-04-11 Merck & Co., Inc. Integrin receptor antagonists
US20040224986A1 (en) * 2002-08-16 2004-11-11 Bart De Corte Piperidinyl targeting compounds that selectively bind integrins
BR112014016736A8 (pt) 2012-01-27 2017-07-04 Hoffmann La Roche composto, composição farmacêutica, método para tratamento, uso de um composto e invenção
EP2948444B1 (en) * 2013-01-28 2016-12-07 Janssen Sciences Ireland UC Quinoxalinones and dihydroquinoxalinones as respiratory syncytial virus antiviral agents
CA2902393C (en) 2013-02-28 2022-11-01 Arrowhead Research Corporation Organic compositions to treat epas1-related diseases
SG11201600379TA (en) 2013-08-07 2016-02-26 Arrowhead Res Corp Polyconjugates for delivery of rnai triggers to tumor cells in vivo
KR102647026B1 (ko) 2015-02-19 2024-03-12 사이플루어 라이프 사이언시즈, 인크 플루오르화 테트라히드로나프티리디닐 노난산 유도체 및 이의 용도
US11971402B2 (en) * 2015-04-24 2024-04-30 Cornell University Methods and reagents for determination and treatment of organotropic metastasis
KR20170141757A (ko) * 2015-04-30 2017-12-26 사이플루어 라이프 사이언시즈, 인크 테트라하이드로나프티리디닐 프로피온산 유도체 및 이의 용도
BR112017025698A2 (pt) 2015-05-29 2018-08-14 Arrowhead Pharmaceuticals Inc composições e métodos para inibir a expressão do gene de hif2alfa

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
CN1284944A (zh) * 1997-12-17 2001-02-21 麦克公司 整联蛋白受体拮抗剂
CN102026671A (zh) * 2008-03-14 2011-04-20 Visen医药公司 整联蛋白靶向试剂及使用其的体内和体外成像方法

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KR102787533B1 (ko) 2025-03-31
EP3784269B1 (en) 2024-06-05
JP2025060958A (ja) 2025-04-10
DK3784269T3 (da) 2024-07-08
US20210093725A1 (en) 2021-04-01
MX2020011290A (es) 2020-11-13
HRP20240907T1 (hr) 2024-10-25
TW202014206A (zh) 2020-04-16
JOP20200266A1 (ar) 2020-10-21
KR20210005145A (ko) 2021-01-13
SA520420426B1 (ar) 2024-11-19
CN118994152A (zh) 2024-11-22
CN112074290A (zh) 2020-12-11
AU2019260738B2 (en) 2025-01-30
JP7704529B2 (ja) 2025-07-08
CA3097656A1 (en) 2019-10-31
EP3784269A4 (en) 2022-03-23
EP4435000A2 (en) 2024-09-25
SI3784269T1 (sl) 2024-08-30
JP2021522269A (ja) 2021-08-30
IL278304B1 (en) 2024-02-01
AU2019260738A1 (en) 2020-10-15
WO2019210200A1 (en) 2019-10-31
IL278304B2 (en) 2024-06-01
SG11202009734VA (en) 2020-11-27
IL278304A (enExample) 2020-12-31
EP3784269A1 (en) 2021-03-03
FI3784269T3 (fi) 2024-07-03
BR112020021949A2 (pt) 2021-01-26
IL309955A (en) 2024-03-01
ES2983950T3 (es) 2024-10-28
EP4435000A3 (en) 2025-02-19

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