TW202014206A - 整合素靶向配體及其用途 - Google Patents

整合素靶向配體及其用途 Download PDF

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Publication number
TW202014206A
TW202014206A TW108114935A TW108114935A TW202014206A TW 202014206 A TW202014206 A TW 202014206A TW 108114935 A TW108114935 A TW 108114935A TW 108114935 A TW108114935 A TW 108114935A TW 202014206 A TW202014206 A TW 202014206A
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TW
Taiwan
Prior art keywords
integrin
optionally substituted
group
mmol
integrin targeting
Prior art date
Application number
TW108114935A
Other languages
English (en)
Chinese (zh)
Inventor
李
傑佛瑞 卡爾森
安東尼 尼可拉斯
李曉愷
舒東旭
沃特斯 馬修 佛勒
Original Assignee
美商愛羅海德製藥公司
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by 美商愛羅海德製藥公司 filed Critical 美商愛羅海德製藥公司
Publication of TW202014206A publication Critical patent/TW202014206A/zh

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    • 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
    • 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
    • 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
    • A61K47/56—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
    • 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]

Landscapes

  • 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)
TW108114935A 2018-04-27 2019-04-29 整合素靶向配體及其用途 TW202014206A (zh)

Applications Claiming Priority (4)

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

Publications (1)

Publication Number Publication Date
TW202014206A true TW202014206A (zh) 2020-04-16

Family

ID=68294255

Family Applications (1)

Application Number Title Priority Date Filing Date
TW108114935A TW202014206A (zh) 2018-04-27 2019-04-29 整合素靶向配體及其用途

Country Status (20)

Country Link
US (1) US20210093725A1 (https=)
EP (2) EP4435000A3 (https=)
JP (2) JP7704529B2 (https=)
KR (1) KR102787533B1 (https=)
CN (2) CN118994152A (https=)
AU (1) AU2019260738B2 (https=)
BR (1) BR112020021949A2 (https=)
CA (1) CA3097656A1 (https=)
DK (1) DK3784269T3 (https=)
ES (1) ES2983950T3 (https=)
FI (1) FI3784269T3 (https=)
HR (1) HRP20240907T1 (https=)
IL (2) IL309955A (https=)
JO (1) JOP20200266A1 (https=)
MX (1) MX2020011290A (https=)
SA (1) SA520420426B1 (https=)
SG (1) SG11202009734VA (https=)
SI (1) SI3784269T1 (https=)
TW (1) TW202014206A (https=)
WO (1) WO2019210200A1 (https=)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20210093725A1 (en) * 2018-04-27 2021-04-01 Arrowhead Pharmaceuticals, Inc. Integrin targeting ligands and uses thereof
SG11202105577TA (en) 2019-01-09 2021-06-29 Arrowhead Pharmaceuticals Inc Rnai agents for inhibiting expression of hif-2 alpha (epas1), compositions thereof, and methods of use
IL301187A (en) * 2020-09-11 2023-05-01 Arrowhead Pharmaceuticals Inc RNAi agents for suppressing DUX4 expression, preparations containing them and uses thereof
EP4367246A2 (en) * 2021-07-07 2024-05-15 Alnylam Pharmaceuticals, Inc. Integrin targeting ligands for ocular delivery of rnai compounds
CN121399119A (zh) * 2023-06-19 2026-01-23 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
WO2025261536A1 (zh) * 2024-06-21 2025-12-26 长春金赛药业有限责任公司 一种整联蛋白配体关键中间体及其制备方法
WO2026034639A1 (ja) * 2024-08-09 2026-02-12 株式会社Spin Wave ペプチド合成用可溶性担体およびこれを用いた合成方法

Family Cites Families (15)

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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
ES2241192T3 (es) * 1997-12-17 2005-10-16 MERCK & CO., INC. (A NEW JERSEY CORP.) Antagonistas del receptor de integrina.
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
CN102026671B (zh) * 2008-03-14 2014-09-03 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
BR112014016736A8 (pt) * 2012-01-27 2017-07-04 Hoffmann La Roche composto, composição farmacêutica, método para tratamento, uso de um composto e invenção
CA2895430C (en) 2013-01-28 2021-11-23 Janssen Sciences Ireland Uc Quinoxalinones and dihydroquinoxalinones as respiratory syncytial virus antiviral agents
SG10201706960TA (en) * 2013-02-28 2017-10-30 Arrowhead Res Corp Organic compositions to treat epas1-related diseases
WO2015021092A1 (en) 2013-08-07 2015-02-12 Arrowhead Research Corporation 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
HK1252852A1 (zh) 2015-05-29 2019-06-06 Arrowhead Pharmaceuticals, Inc. 阻止HIF2α基因表达的组合物及方法
US20210093725A1 (en) * 2018-04-27 2021-04-01 Arrowhead Pharmaceuticals, Inc. Integrin targeting ligands and uses thereof

Also Published As

Publication number Publication date
JOP20200266A1 (ar) 2020-10-21
CA3097656A1 (en) 2019-10-31
SA520420426B1 (ar) 2024-11-19
IL309955A (en) 2024-03-01
FI3784269T3 (fi) 2024-07-03
KR102787533B1 (ko) 2025-03-31
AU2019260738B2 (en) 2025-01-30
ES2983950T3 (es) 2024-10-28
IL278304B1 (en) 2024-02-01
JP2021522269A (ja) 2021-08-30
DK3784269T3 (da) 2024-07-08
HRP20240907T1 (hr) 2024-10-25
WO2019210200A1 (en) 2019-10-31
JP7704529B2 (ja) 2025-07-08
CN118994152A (zh) 2024-11-22
JP2025060958A (ja) 2025-04-10
KR20210005145A (ko) 2021-01-13
US20210093725A1 (en) 2021-04-01
AU2019260738A1 (en) 2020-10-15
IL278304A (https=) 2020-12-31
EP3784269A4 (en) 2022-03-23
CN112074290B (zh) 2024-09-10
CN112074290A (zh) 2020-12-11
BR112020021949A2 (pt) 2021-01-26
EP3784269A1 (en) 2021-03-03
IL278304B2 (en) 2024-06-01
EP3784269B1 (en) 2024-06-05
MX2020011290A (es) 2020-11-13
SG11202009734VA (en) 2020-11-27
SI3784269T1 (sl) 2024-08-30
EP4435000A2 (en) 2024-09-25
EP4435000A3 (en) 2025-02-19

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