KR102787533B1 - 인테그린 표적화 리간드 및 그의 용도 - Google Patents

인테그린 표적화 리간드 및 그의 용도 Download PDF

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KR102787533B1
KR102787533B1 KR1020207033772A KR20207033772A KR102787533B1 KR 102787533 B1 KR102787533 B1 KR 102787533B1 KR 1020207033772 A KR1020207033772 A KR 1020207033772A KR 20207033772 A KR20207033772 A KR 20207033772A KR 102787533 B1 KR102787533 B1 KR 102787533B1
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South Korea
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integrin targeting
integrin
mmol
compound
targeting ligand
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KR20210005145A (ko
Inventor
전 리
제프리 칼슨
앤소니 니콜라스
샤오카이 리
동쉬 수
매튜 파울러-워터스
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애로우헤드 파마슈티컬스 인코포레이티드
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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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • 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
    • A61K48/00—Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
    • 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
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/70546—Integrin superfamily
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/70546—Integrin superfamily
    • C07K14/70557—Integrin beta3-subunit-containing molecules, e.g. CD41, CD51, CD61
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113—Non-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
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/10—Type of nucleic acid
    • C12N2310/14—Type 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)
KR1020207033772A 2018-04-27 2019-04-26 인테그린 표적화 리간드 및 그의 용도 Active KR102787533B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862663763P 2018-04-27 2018-04-27
US62/663,763 2018-04-27
US201962790372P 2019-01-09 2019-01-09
US62/790,372 2019-01-09
PCT/US2019/029393 WO2019210200A1 (en) 2018-04-27 2019-04-26 Integrin targeting ligands and uses thereof

Publications (2)

Publication Number Publication Date
KR20210005145A KR20210005145A (ko) 2021-01-13
KR102787533B1 true KR102787533B1 (ko) 2025-03-31

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KR1020207033772A Active KR102787533B1 (ko) 2018-04-27 2019-04-26 인테그린 표적화 리간드 및 그의 용도

Country Status (20)

Country Link
US (1) US20210093725A1 (enExample)
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)
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
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
WO1999031061A1 (en) 1997-12-17 1999-06-24 Merck & Co., Inc. Integrin receptor antagonists
WO2014114776A1 (en) 2013-01-28 2014-07-31 Janssen R&D Ireland Quinoxalinones and dihydroquinoxalinones as respiratory syncytial virus antiviral agents

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
CA2715034C (en) * 2008-03-14 2016-12-06 Visen Medical, Inc. Integrin targeting agents and in-vivo and in-vitro imaging methods using the same
BR112014016736A8 (pt) 2012-01-27 2017-07-04 Hoffmann La Roche composto, composição farmacêutica, método para tratamento, uso de um composto e invenção
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
WO1999031061A1 (en) 1997-12-17 1999-06-24 Merck & Co., Inc. Integrin receptor antagonists
WO2014114776A1 (en) 2013-01-28 2014-07-31 Janssen R&D Ireland Quinoxalinones and dihydroquinoxalinones as respiratory syncytial virus antiviral agents

Non-Patent Citations (2)

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Title
Bioorg. Med. Chem. Lett., 2004, 14, 1049-1052 (2004.02.23.)
J. Med. Chem., 2003, 46, 4790-4798 (2003.09.27.)

Also Published As

Publication number Publication date
EP3784269B1 (en) 2024-06-05
JP2025060958A (ja) 2025-04-10
DK3784269T3 (da) 2024-07-08
US20210093725A1 (en) 2021-04-01
CN112074290B (zh) 2024-09-10
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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