AU2019260738B2 - Integrin targeting ligands and uses thereof - Google Patents

Integrin targeting ligands and uses thereof Download PDF

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Publication number
AU2019260738B2
AU2019260738B2 AU2019260738A AU2019260738A AU2019260738B2 AU 2019260738 B2 AU2019260738 B2 AU 2019260738B2 AU 2019260738 A AU2019260738 A AU 2019260738A AU 2019260738 A AU2019260738 A AU 2019260738A AU 2019260738 B2 AU2019260738 B2 AU 2019260738B2
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Australia
Prior art keywords
integrin
integrin targeting
group
compound
mmol
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AU2019260738A
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AU2019260738A1 (en
Inventor
Jeffrey Carlson
Matthew FOWLER-WATTERS
Xiaokai Li
Zhen Li
Anthony Nicholas
Dongxu Shu
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Arrowhead Pharmaceuticals Inc
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Arrowhead Pharmaceuticals Inc
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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)
  • 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)
AU2019260738A 2018-04-27 2019-04-26 Integrin targeting ligands and uses thereof Active AU2019260738B2 (en)

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
AU2019260738A1 AU2019260738A1 (en) 2020-10-15
AU2019260738B2 true AU2019260738B2 (en) 2025-01-30

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AU2019260738A Active AU2019260738B2 (en) 2018-04-27 2019-04-26 Integrin targeting ligands and uses thereof

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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

Citations (3)

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JP2011519348A (ja) * 2008-03-14 2011-07-07 ビセン メディカル， インコーポレイテッド インテグリン標的化剤およびそれらを用いるｉｎｖｉｖｏおよびｉｎｖｉｔｒｏでの画像化方法
WO2016134223A2 (en) * 2015-02-19 2016-08-25 Scifluor Life Sciences, Inc. Fluorinated tetrahydronaphthyridinyl nonanoic acid derivatives and uses thereof
WO2016176532A1 (en) * 2015-04-30 2016-11-03 Scifluor Life Sciences, Inc. Tetrahydronaphthyridinyl propionic acid derivatives and uses thereof

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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
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
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
WO2016172710A2 (en) * 2015-04-24 2016-10-27 Cornell University Methods and reagents for determination and treatment of organotropic metastasis
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

Patent Citations (3)

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JP2011519348A (ja) * 2008-03-14 2011-07-07 ビセン メディカル， インコーポレイテッド インテグリン標的化剤およびそれらを用いるｉｎｖｉｖｏおよびｉｎｖｉｔｒｏでの画像化方法
WO2016134223A2 (en) * 2015-02-19 2016-08-25 Scifluor Life Sciences, Inc. Fluorinated tetrahydronaphthyridinyl nonanoic acid derivatives and uses thereof
WO2016176532A1 (en) * 2015-04-30 2016-11-03 Scifluor Life Sciences, Inc. Tetrahydronaphthyridinyl propionic acid derivatives and uses thereof

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Also Published As

Publication number Publication date
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
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
CN118994152A (zh) 2024-11-22
IL278304B2 (en) 2024-06-01
EP3784269A1 (en) 2021-03-03

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