CN118994152A - 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
CN118994152A
CN118994152A CN202411099363.5A CN202411099363A CN118994152A CN 118994152 A CN118994152 A CN 118994152A CN 202411099363 A CN202411099363 A CN 202411099363A CN 118994152 A CN118994152 A CN 118994152A
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CN
China
Prior art keywords
optionally substituted
integrin
group
cargo molecule
integrin targeting
Prior art date
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Pending
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CN202411099363.5A
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English (en)
Chinese (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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Publication of CN118994152A publication Critical patent/CN118994152A/zh
Pending legal-status Critical Current

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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)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (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)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN202411099363.5A 2018-04-27 2019-04-26 整联蛋白靶向配体和其用途 Pending CN118994152A (zh)

Applications Claiming Priority (6)

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
CN201980028704.0A CN112074290B (zh) 2018-04-27 2019-04-26 整联蛋白靶向配体和其用途
PCT/US2019/029393 WO2019210200A1 (en) 2018-04-27 2019-04-26 Integrin targeting ligands and uses thereof

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201980028704.0A Division CN112074290B (zh) 2018-04-27 2019-04-26 整联蛋白靶向配体和其用途

Publications (1)

Publication Number Publication Date
CN118994152A true CN118994152A (zh) 2024-11-22

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CN201980028704.0A Active CN112074290B (zh) 2018-04-27 2019-04-26 整联蛋白靶向配体和其用途
CN202411099363.5A Pending CN118994152A (zh) 2018-04-27 2019-04-26 整联蛋白靶向配体和其用途

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US (1) US20210093725A1 (enExample)
EP (2) EP4435000A3 (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)
FI (1) FI3784269T3 (enExample)
HR (1) HRP20240907T1 (enExample)
IL (2) IL309955A (enExample)
JO (1) JOP20200266A1 (enExample)
MX (1) MX2020011290A (enExample)
SA (1) SA520420426B1 (enExample)
SG (1) SG11202009734VA (enExample)
SI (1) SI3784269T1 (enExample)
TW (1) TW202014206A (enExample)
WO (1) WO2019210200A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3120580A1 (en) 2019-01-09 2020-07-16 Arrowhead Pharmaceuticals, Inc. Rnai agents for inhibiting expression of hif-2 alpha (epas1), compositions thereof, and methods of use
WO2022056266A2 (en) * 2020-09-11 2022-03-17 Arrowhead Pharmaceuticals, Inc. Rnai agents for inhibiting expression of dux4, compositions thereof, and methods of use
US20240409927A1 (en) * 2021-07-07 2024-12-12 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

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
IL136495A0 (en) 1997-12-17 2001-06-14 Merck & Co Inc Integrin receptor antagonists
US20040224986A1 (en) * 2002-08-16 2004-11-11 Bart De Corte Piperidinyl targeting compounds that selectively bind integrins
AU2009223235B2 (en) * 2008-03-14 2014-09-11 Merck Sharp & Dohme Corp. Integrin targeting agents and in-vivo and in-vitro imaging methods using the same
MX2014008373A (es) 2012-01-27 2014-09-26 Hoffmann La Roche Conjugados antagonistas de integrina para suministro dirigido a celulas que expresan alfa-v-beta-3.
CA2895430C (en) 2013-01-28 2021-11-23 Janssen Sciences Ireland Uc Quinoxalinones and dihydroquinoxalinones as respiratory syncytial virus antiviral agents
SG11201506805QA (en) 2013-02-28 2015-09-29 Arrowhead Res Corp Organic compositions to treat epas1-related diseases
KR20160035081A (ko) 2013-08-07 2016-03-30 애로우헤드 리서치 코오포레이션 생체 내에서 RNAi 유발제를 종양 세포로 전달하기 위한 폴리콘주게이트
EP3925959A1 (en) * 2015-02-19 2021-12-22 OcuTerra Therapeutics, Inc. Fluorinated derivatives of 3-(2-oxo-3-(3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propyl)imidazolidin-1-yl)propanoic acid and uses thereof
WO2016172710A2 (en) * 2015-04-24 2016-10-27 Cornell University Methods and reagents for determination and treatment of organotropic metastasis
EP3288555A1 (en) * 2015-04-30 2018-03-07 SciFluor Life Sciences, Inc. Tetrahydronaphthyridinyl propionic acid derivatives and uses thereof
TWI761305B (zh) 2015-05-29 2022-04-21 美商愛羅海德製藥公司 抑制Hif2α基因表現之組合物及方法

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IL309955A (en) 2024-03-01
IL278304B1 (en) 2024-02-01
SG11202009734VA (en) 2020-11-27
KR20210005145A (ko) 2021-01-13
KR102787533B1 (ko) 2025-03-31
HRP20240907T1 (hr) 2024-10-25
AU2019260738B2 (en) 2025-01-30
FI3784269T3 (fi) 2024-07-03
CA3097656A1 (en) 2019-10-31
CN112074290B (zh) 2024-09-10
ES2983950T3 (es) 2024-10-28
JP7704529B2 (ja) 2025-07-08
JP2025060958A (ja) 2025-04-10
EP4435000A2 (en) 2024-09-25
BR112020021949A2 (pt) 2021-01-26
DK3784269T3 (da) 2024-07-08
JP2021522269A (ja) 2021-08-30
US20210093725A1 (en) 2021-04-01
TW202014206A (zh) 2020-04-16
SI3784269T1 (sl) 2024-08-30
EP3784269A4 (en) 2022-03-23
CN112074290A (zh) 2020-12-11
SA520420426B1 (ar) 2024-11-19
EP4435000A3 (en) 2025-02-19
EP3784269B1 (en) 2024-06-05
AU2019260738A1 (en) 2020-10-15
JOP20200266A1 (ar) 2020-10-21
WO2019210200A1 (en) 2019-10-31
IL278304A (enExample) 2020-12-31
MX2020011290A (es) 2020-11-13
IL278304B2 (en) 2024-06-01
EP3784269A1 (en) 2021-03-03

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