CA2837979C - Dendrimers comprising terminal pharmaceutically active agents and terminal pharmacokinetic modifying agents - Google Patents

Dendrimers comprising terminal pharmaceutically active agents and terminal pharmacokinetic modifying agents Download PDF

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Publication number
CA2837979C
CA2837979C CA2837979A CA2837979A CA2837979C CA 2837979 C CA2837979 C CA 2837979C CA 2837979 A CA2837979 A CA 2837979A CA 2837979 A CA2837979 A CA 2837979A CA 2837979 C CA2837979 C CA 2837979C
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Canada
Prior art keywords
macromolecule
pharmaceutically active
active agent
terminal group
dendrimer
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CA2837979A
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English (en)
French (fr)
Other versions
CA2837979A1 (en
Inventor
David Owen
Brian Devlin Kelly
Peter Karellas
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Starpharma Pty Ltd
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Starpharma Pty Ltd
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Publication of CA2837979A1 publication Critical patent/CA2837979A1/en
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    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G73/00—Macromolecular compounds obtained by reactions forming a linkage containing nitrogen with or without oxygen or carbon in the main chain of the macromolecule, not provided for in groups C08G12/00 - C08G71/00
    • C08G73/02—Polyamines
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • 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
    • 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
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26—Androgens
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G69/00—Macromolecular compounds obtained by reactions forming a carboxylic amide link in the main chain of the macromolecule
    • C08G69/02—Polyamides derived from amino-carboxylic acids or from polyamines and polycarboxylic acids
    • C08G69/08—Polyamides derived from amino-carboxylic acids or from polyamines and polycarboxylic acids derived from amino-carboxylic acids
    • C08G69/10—Alpha-amino-carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G69/00—Macromolecular compounds obtained by reactions forming a carboxylic amide link in the main chain of the macromolecule
    • C08G69/40—Polyamides containing oxygen in the form of ether groups
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G83/00—Macromolecular compounds not provided for in groups C08G2/00 - C08G81/00
    • C08G83/002—Dendritic macromolecules
    • C08G83/003—Dendrimers

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Polymers & Plastics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Inorganic Chemistry (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Bipolar Transistors (AREA)
CA2837979A 2011-06-06 2012-06-06 Dendrimers comprising terminal pharmaceutically active agents and terminal pharmacokinetic modifying agents Active CA2837979C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161493886P 2011-06-06 2011-06-06
US61/493,886 2011-06-06
PCT/AU2012/000647 WO2012167309A1 (en) 2011-06-06 2012-06-06 Macromolecules

Publications (2)

Publication Number Publication Date
CA2837979A1 CA2837979A1 (en) 2012-12-13
CA2837979C true CA2837979C (en) 2021-03-30

Family

ID=47295262

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2837979A Active CA2837979C (en) 2011-06-06 2012-06-06 Dendrimers comprising terminal pharmaceutically active agents and terminal pharmacokinetic modifying agents

Country Status (18)

Country Link
US (2) US9744246B2 (enExample)
EP (1) EP2729179B1 (enExample)
JP (1) JP6158177B2 (enExample)
KR (1) KR101941318B1 (enExample)
CN (2) CN110124051B (enExample)
AU (1) AU2012267200B2 (enExample)
BR (1) BR112013031556B1 (enExample)
CA (1) CA2837979C (enExample)
DK (1) DK2729179T3 (enExample)
ES (1) ES2834992T3 (enExample)
HR (1) HRP20201998T1 (enExample)
HU (1) HUE052285T2 (enExample)
IN (1) IN2014DN00101A (enExample)
LT (1) LT2729179T (enExample)
PL (1) PL2729179T3 (enExample)
PT (1) PT2729179T (enExample)
SI (1) SI2729179T1 (enExample)
WO (1) WO2012167309A1 (enExample)

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US20180326081A1 (en) * 2011-06-06 2018-11-15 Starpharma Pty Ltd Macromolecules
EP2996726A1 (fr) * 2013-05-16 2016-03-23 Université de Strasbourg Composés dendritiques comprenant un agent chélatant, fluorochrome ou agent de reconnaissance, compositions les comprenant et leurs utilisations
WO2015035446A1 (en) * 2013-09-10 2015-03-19 Starpharma Pty Ltd Macromolecules of dendrimer-platinum conjugates
EP3152248B1 (en) 2014-06-06 2019-10-09 Starpharma Pty Ltd Dendrimer-drug conjugates
CA2987322C (en) 2015-08-11 2020-02-11 Coherent Biopharma Multi-ligand drug conjugates and uses thereof
CN106554330B (zh) * 2015-09-26 2019-07-05 南京友怡医药科技有限公司 水溶性多西他赛抗癌药物化合物及其制备方法和应用
CN106554329B (zh) * 2015-09-26 2019-07-05 南京友怡医药科技有限公司 水溶性紫杉醇抗癌药物化合物及其制备方法和应用
WO2017068051A1 (en) * 2015-10-21 2017-04-27 Lek Pharmaceuticals D.D. Peg-based dendron and process for producing the same
WO2017135893A1 (en) * 2016-02-05 2017-08-10 Nipsea Technologies Pte Ltd Aqueous dendritic amine coatings
US20190142953A1 (en) * 2016-05-10 2019-05-16 Massachusetts Institute Of Technology Dendrimer-Drug Conjugates, Hydrogel Compositions, and Methods
TWI773730B (zh) * 2017-02-22 2022-08-11 瑞典商阿斯特捷利康公司 治療性樹枝狀聚合物
EP3778628A4 (en) * 2018-03-29 2021-11-24 NOF Corporation DEGRADABLE POLYETHYLENE GLYCOL CONJUGATE
US12071517B2 (en) * 2018-07-19 2024-08-27 Starpharma Pty Ltd. Therapeutic dendrimer
EP3823961A4 (en) * 2018-07-19 2022-06-08 Starpharma Pty Limited THERAPEUTIC DENDRIMER
TWI831817B (zh) * 2018-08-17 2024-02-11 瑞典商阿斯特捷利康公司 治療癌症之方法
TWI856967B (zh) 2018-08-17 2024-10-01 瑞典商阿斯特捷利康公司 樹枝狀體配製物
CN113056469B (zh) 2018-11-20 2025-05-23 星法马私人有限公司 治疗性树状聚体
AU2019390489B2 (en) * 2018-11-29 2023-08-17 Starpharma Pty Ltd Dendrimer for therapy and imaging
EP4021511A4 (en) * 2019-08-28 2023-10-04 Starpharma Pty Ltd TARGETED DENDRIMER CONJUGATES
CN114585389A (zh) * 2019-09-26 2022-06-03 星法马私人有限公司 治疗性树枝状大分子
WO2021213492A1 (zh) * 2020-04-24 2021-10-28 上海森辉医药有限公司 一类载药的大分子及其制备方法
AU2021284918A1 (en) * 2020-06-03 2023-01-05 Starpharma Pty Ltd Therapeutic conjugates
JP7880863B2 (ja) * 2020-08-25 2026-06-26 上海森輝医薬有限公司 薬剤を担持する高分子及びその調製方法
US20230263900A1 (en) * 2020-08-31 2023-08-24 Starpharma Pty Ltd. Dendrimer-drug conjugate
EP3973952B1 (en) * 2020-09-24 2024-02-14 Ocular Therapeutix, Inc. Sustained release biodegradable intracanalicular inserts comprising a hydrogel and cyclosporine
EP4216929A1 (en) * 2020-09-24 2023-08-02 Ocular Therapeutix, Inc. Sustained release biodegradable intracanalicular inserts comprising a hydrogel and an active agent
CN117164357B (zh) * 2023-01-03 2024-07-19 广东捷成科创电子股份有限公司 一种五元系大功率型压电陶瓷材料及其制备方法
TW202448514A (zh) * 2023-05-08 2024-12-16 大陸商上海森輝醫藥有限公司 抗真菌藥的載藥大分子及其製備方法
CN118063414B (zh) * 2024-02-29 2026-04-28 常州大学 一种半胱氨酸-多西他赛偶联物及其制备方法和应用
WO2026046228A1 (zh) * 2024-08-27 2026-03-05 苏州拓界医药有限公司 树枝状聚合物偶联物及其制备方法

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Also Published As

Publication number Publication date
JP2014520105A (ja) 2014-08-21
JP6158177B2 (ja) 2017-07-05
CN110124051A (zh) 2019-08-16
HUE052285T2 (hu) 2021-04-28
ES2834992T3 (es) 2021-06-21
AU2012267200B2 (en) 2016-02-25
WO2012167309A1 (en) 2012-12-13
CN103796684A (zh) 2014-05-14
CN110124051B (zh) 2022-10-21
HK1198356A1 (en) 2015-04-10
HRP20201998T1 (hr) 2021-02-05
AU2012267200A1 (en) 2013-05-09
KR20140041678A (ko) 2014-04-04
PL2729179T3 (pl) 2021-07-19
US10265409B2 (en) 2019-04-23
KR101941318B1 (ko) 2019-01-22
IN2014DN00101A (enExample) 2015-05-15
CA2837979A1 (en) 2012-12-13
BR112013031556B1 (pt) 2022-03-29
EP2729179A4 (en) 2015-01-28
EP2729179A1 (en) 2014-05-14
SI2729179T1 (sl) 2021-01-29
EP2729179B1 (en) 2020-09-23
CN103796684B (zh) 2019-06-25
US9744246B2 (en) 2017-08-29
LT2729179T (lt) 2020-12-28
BR112013031556A2 (enExample) 2017-08-29
PT2729179T (pt) 2020-11-25
DK2729179T3 (da) 2020-12-21
US20170354739A1 (en) 2017-12-14
US20140171375A1 (en) 2014-06-19

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