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

Info

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
Authority
CN
China
Prior art keywords
integrin
mmol
compound
group
integrin targeting
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CN201980028704.0A
Other languages
English (en)
Chinese (zh)
Other versions
CN112074290A (zh
Inventor
李珍
J·卡尔森
A·尼古拉斯
X·李
D·舒
M·富勒-沃特斯
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Arrowhead Pharmaceuticals Inc
Original Assignee
Arrowhead Pharmaceuticals Inc
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.)
Filing date
Publication date
Application filed by Arrowhead Pharmaceuticals Inc filed Critical Arrowhead Pharmaceuticals Inc
Priority to CN202411099363.5A priority Critical patent/CN118994152A/zh
Publication of CN112074290A publication Critical patent/CN112074290A/zh
Application granted granted Critical
Publication of CN112074290B publication Critical patent/CN112074290B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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]

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)
  • Biomedical Technology (AREA)
  • Biotechnology (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)

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

Publications (2)

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

Family

ID=68294255

Family Applications (2)

Application Number Title Priority Date Filing Date
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

Family Applications After (1)

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

Country Status (20)

Country Link
US (1) US12667619B2 (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 (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL309955A (en) 2018-04-27 2024-03-01 Arrowhead Pharmaceuticals Inc Integrin-targeting ligands and their uses
KR20210113273A (ko) 2019-01-09 2021-09-15 애로우헤드 파마슈티컬스 인코포레이티드 HIF-2 알파 (EPAS1)의 발현을 억제하기 위한 RNAi 작용제, 그의 조성물, 및 사용 방법
AU2021342155A1 (en) * 2020-09-11 2023-04-13 Arrowhead Pharmaceuticals, Inc. RNAi agents for inhibiting expression of DUX4, compositions thereof, and methods of use
EP4367246A4 (en) * 2021-07-07 2026-07-29 Alnylam Pharmaceuticals Inc Integrin-targeting ligands for the ocular administration of arni 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

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 (18)

* 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
US6048861A (en) * 1997-12-17 2000-04-11 Merck & Co., Inc. Integrin receptor antagonists
US6017926A (en) * 1997-12-17 2000-01-25 Merck & Co., Inc. Integrin receptor antagonists
AU2002337954C1 (en) 2001-10-22 2008-10-23 The Scripps Research Institute Integrin targeting compounds
US20040224986A1 (en) * 2002-08-16 2004-11-11 Bart De Corte Piperidinyl targeting compounds that selectively bind integrins
EP2990410A1 (en) 2004-08-10 2016-03-02 Alnylam Pharmaceuticals Inc. Chemically modified oligonucleotides
JP2012517447A (ja) 2009-02-10 2012-08-02 ザ スクリプス リサーチ インスティチュート 化学的にプログラムされたワクチン接種法
US9586916B2 (en) * 2012-01-27 2017-03-07 Hoffmann-La Roche Inc. Integrin antagonist conjugates for targeted delivery to cells expressing alpha-V-beta-3
JP6383735B2 (ja) 2013-01-28 2018-08-29 ヤンセン・サイエンシズ・アイルランド・ユーシー Ｒｓウイルスの抗ウイルス剤としてのキノキサリノンおよびジヒドロキノキサリノン
HK1214301A1 (zh) * 2013-02-28 2016-07-22 箭头研究公司 治療epas1相關疾病的有機組合物
WO2015021092A1 (en) 2013-08-07 2015-02-12 Arrowhead Research Corporation Polyconjugates for delivery of rnai triggers to tumor cells in vivo
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
EP3273965A4 (en) 2015-03-26 2018-12-05 Merck Sharp & Dohme Corp. Composition and methods for treating chronic kidney disease
US11971402B2 (en) 2015-04-24 2024-04-30 Cornell University Methods and reagents for determination and treatment of organotropic metastasis
JP2018514568A (ja) * 2015-04-30 2018-06-07 サイフルーア ライフ サイエンシズ インコーポレイテッド テトラヒドロナフチリジニルプロピオン酸誘導体およびその使用法
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
CN120247964A (zh) 2018-02-17 2025-07-04 箭头药业股份有限公司 三炔连接剂和使用方法
IL309955A (en) * 2018-04-27 2024-03-01 Arrowhead Pharmaceuticals Inc Integrin-targeting ligands and their uses

Patent 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

Also Published As

Publication number Publication date
IL278304A (enExample) 2020-12-31
TW202014206A (zh) 2020-04-16
AU2019260738B2 (en) 2025-01-30
FI3784269T3 (fi) 2024-07-03
CN118994152A (zh) 2024-11-22
JOP20200266A1 (ar) 2020-10-21
EP4435000A3 (en) 2025-02-19
HRP20240907T1 (hr) 2024-10-25
JP7704529B2 (ja) 2025-07-08
KR20210005145A (ko) 2021-01-13
IL309955A (en) 2024-03-01
US12667619B2 (en) 2026-06-30
MX2020011290A (es) 2020-11-13
IL278304B1 (en) 2024-02-01
ES2983950T3 (es) 2024-10-28
SA520420426B1 (ar) 2024-11-19
IL278304B2 (en) 2024-06-01
JP2025060958A (ja) 2025-04-10
CN112074290A (zh) 2020-12-11
CA3097656A1 (en) 2019-10-31
SI3784269T1 (sl) 2024-08-30
KR102787533B1 (ko) 2025-03-31
DK3784269T3 (da) 2024-07-08
WO2019210200A1 (en) 2019-10-31
AU2019260738A1 (en) 2020-10-15
EP3784269A1 (en) 2021-03-03
US20210093725A1 (en) 2021-04-01
BR112020021949A2 (pt) 2021-01-26
JP2021522269A (ja) 2021-08-30
EP4435000A2 (en) 2024-09-25
EP3784269A4 (en) 2022-03-23
EP3784269B1 (en) 2024-06-05
SG11202009734VA (en) 2020-11-27

Similar Documents

Publication Publication Date Title
JP7843302B2 (ja) トリアルキン結合剤及び使用方法
KR102787533B1 (ko) 인테그린 표적화 리간드 및 그의 용도
KR102762143B1 (ko) 인테그린 리간드 및 그의 용도
TWI842117B (zh) 治療性化合物之標靶性配體
WO2022056286A1 (en) Integrin targeting ligands and uses thereof
CN113613661B (zh) 用于抑制HIF-2α(EPAS1)的表达的RNAi试剂、其组合物和使用方法
EP3535397A1 (en) Alpha-v beta-6 integrin ligands and uses thereof
US12582718B2 (en) Integrin targeting ligands and uses thereof
HK40047192A (en) Integrin targeting ligands and uses thereof
HK40047192B (en) Integrin targeting ligands and uses thereof
EA048950B1 (ru) Нацеленные на интегрин лиганды и их применение
OA20532A (en) Integrin ligands and uses thereof.

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant