CA2925132C - Slow-release conjugates of sn-38 - Google Patents

Slow-release conjugates of sn-38 Download PDF

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Publication number
CA2925132C
CA2925132C CA2925132A CA2925132A CA2925132C CA 2925132 C CA2925132 C CA 2925132C CA 2925132 A CA2925132 A CA 2925132A CA 2925132 A CA2925132 A CA 2925132A CA 2925132 C CA2925132 C CA 2925132C
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Prior art keywords
conjugate
peg
molecular weight
release
linker
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CA2925132A
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English (en)
French (fr)
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CA2925132A1 (en
Inventor
Gary Ashley
Eric L. Schneider
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Prolynx LLC
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Prolynx LLC
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Publication of CA2925132A1 publication Critical patent/CA2925132A1/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/56Medicinal 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
    • A61K47/59Medicinal 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
    • A61K47/60Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D457/00Heterocyclic compounds containing indolo [4, 3-f, g] quinoline ring systems, e.g. derivatives of ergoline, of the formula:, e.g. lysergic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32Polymers modified by chemical after-treatment
    • C08G65/329Polymers modified by chemical after-treatment with organic compounds
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32Polymers modified by chemical after-treatment
    • C08G65/329Polymers modified by chemical after-treatment with organic compounds
    • C08G65/333Polymers modified by chemical after-treatment with organic compounds containing nitrogen
    • C08G65/33396Polymers modified by chemical after-treatment with organic compounds containing nitrogen having oxygen in addition to nitrogen
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/34Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from hydroxy compounds or their metallic derivatives
    • C08G65/48Polymers modified by chemical after-treatment
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G83/00Macromolecular compounds not provided for in groups C08G2/00 - C08G81/00
    • C08G83/002Dendritic macromolecules

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Polymers & Plastics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA2925132A 2013-10-04 2014-10-03 Slow-release conjugates of sn-38 Active CA2925132C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361887111P 2013-10-04 2013-10-04
US61/887,111 2013-10-04
PCT/US2014/059146 WO2015051307A1 (en) 2013-10-04 2014-10-03 Slow-release conjugates of sn-38

Publications (2)

Publication Number Publication Date
CA2925132A1 CA2925132A1 (en) 2015-04-09
CA2925132C true CA2925132C (en) 2021-11-30

Family

ID=51871275

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2925132A Active CA2925132C (en) 2013-10-04 2014-10-03 Slow-release conjugates of sn-38

Country Status (14)

Country Link
US (2) US10016411B2 (https=)
EP (1) EP3052101B1 (https=)
JP (2) JP6473145B2 (https=)
KR (1) KR102320753B1 (https=)
CN (1) CN106061483B (https=)
AU (2) AU2014331591B2 (https=)
BR (1) BR112016007410B1 (https=)
CA (1) CA2925132C (https=)
DK (1) DK3052101T3 (https=)
ES (1) ES2759905T3 (https=)
MX (1) MX371201B (https=)
SG (2) SG10201811365RA (https=)
TW (1) TWI716342B (https=)
WO (1) WO2015051307A1 (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK3052101T3 (da) * 2013-10-04 2019-12-16 Prolynx Llc Konjugater af sn-38 med langsom frigivelse
CN107375288B (zh) * 2016-05-16 2019-08-23 博瑞生物医药(苏州)股份有限公司 多臂的聚合靶向抗癌偶联物
EP3613792B1 (en) 2017-04-21 2021-02-24 Bright Gene Bio-Medical Technology Co., Ltd. Multi-arm targeted anti-cancer conjugate
MX2020007306A (es) * 2018-01-12 2020-09-25 Prolynx Llc Tratamiento sinergico de cancer.
JP7546552B2 (ja) 2018-09-17 2024-09-06 ザ・チルドレンズ・ホスピタル・オブ・フィラデルフィア ポリマーベースの高分子プロドラッグ
WO2020206358A1 (en) 2019-04-05 2020-10-08 Prolynx Llc Improved conjugation linkers
CN114615978A (zh) * 2019-08-28 2022-06-10 普罗林科斯有限责任公司 Dna损伤响应的偶联抑制剂
IL301558A (en) 2020-09-28 2023-05-01 Fundacio Inst De Recerca Biomedica Irb Barcelona Peptidic conjugates of sn38 useful in the treatment of cancer
US11976196B2 (en) * 2021-04-14 2024-05-07 Cambridge Crops, Inc. Silk packaging applications
IL315988A (en) 2022-03-28 2024-11-01 Sant Joan De Deu Hospital Peptidic water-soluble delivery system of anticancer drugs

Family Cites Families (18)

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Publication number Priority date Publication date Assignee Title
US6011042A (en) * 1997-10-10 2000-01-04 Enzon, Inc. Acyl polymeric derivatives of aromatic hydroxyl-containing compounds
US20040176270A1 (en) * 2002-07-12 2004-09-09 Biomarin Pharmaceutical Inc. Use of isocyanate linkers to make hydrolyzable active agent biopolymer conjugates
EP1580216B1 (en) 2002-10-31 2014-05-14 Nippon Kayaku Kabushiki Kaisha High-molecular weight derivatives of camptothecins
US20040247624A1 (en) * 2003-06-05 2004-12-09 Unger Evan Charles Methods of making pharmaceutical formulations for the delivery of drugs having low aqueous solubility
ES2629696T3 (es) * 2003-09-17 2017-08-14 Nektar Therapeutics Profármacos poliméricos multibrazo
US7462627B2 (en) 2006-02-09 2008-12-09 Enzon Pharmaceuticals, Inc. Multi-arm polymeric conjugates of 7-ethyl-10-hydroxycamptothecin for treatment of breast, colorectal, pancreatic, ovarian and lung cancers
MX2009002855A (es) * 2006-09-15 2009-03-30 Enzon Pharmaceuticals Inc Profarmacos polimericos dirigidos que contienen enlazadores multifuncionales.
CA2738807A1 (en) * 2008-10-21 2010-04-29 Enzon Pharmaceuticals, Inc. Treatment of neuroblastoma with multi-arm polymeric conjugates of 7-ethyl-10-hydroxycamptothecin
JP2012509469A (ja) 2008-11-18 2012-04-19 バクスター・インターナショナル・インコーポレイテッド ポリエチレングリコールサンプルの多分散度および/または分子量分布を決定する方法
WO2010138719A1 (en) 2009-05-28 2010-12-02 Mersana Therapeutics, Inc. Polyal drug conjugates comprising variable rate-releasing linkers
ME03396B (me) * 2009-11-18 2020-01-20 Nektar Therapeutics Oblici kisele soli konjugata polimer-lek
US8703907B2 (en) * 2010-05-05 2014-04-22 Prolynx Llc Controlled drug release from dendrimers
EP2566335B1 (en) 2010-05-05 2016-06-29 Prolynx Llc Controlled release of active compounds from macromolecular conjugates
JP2012000072A (ja) * 2010-06-18 2012-01-05 Japan Health Science Foundation 新規な抗フィブリン抗体
TW201215412A (en) * 2010-08-30 2012-04-16 Sun Pharma Advanced Res Co Ltd Stable pharmaceutical composition
WO2012088282A1 (en) * 2010-12-21 2012-06-28 Nektar Therapeutics Multi-arm polymeric prodrug conjugates of pemetrexed-based compounds
WO2013036857A1 (en) * 2011-09-07 2013-03-14 Prolynx Llc Sulfone linkers
DK3052101T3 (da) * 2013-10-04 2019-12-16 Prolynx Llc Konjugater af sn-38 med langsom frigivelse

Also Published As

Publication number Publication date
JP6473145B2 (ja) 2019-02-20
JP2016531895A (ja) 2016-10-13
JP2019104739A (ja) 2019-06-27
ES2759905T3 (es) 2020-05-12
AU2014331591A1 (en) 2016-05-19
JP6842479B2 (ja) 2021-03-17
CN106061483B (zh) 2021-01-08
SG10201811365RA (en) 2019-02-27
MX371201B (es) 2020-01-22
SG11201602258WA (en) 2016-04-28
BR112016007410A2 (pt) 2017-08-01
TWI716342B (zh) 2021-01-21
MX2016004299A (es) 2016-10-04
KR102320753B1 (ko) 2021-11-02
BR112016007410A8 (pt) 2020-02-27
US10016411B2 (en) 2018-07-10
EP3052101A1 (en) 2016-08-10
AU2018256608A1 (en) 2018-11-22
EP3052101B1 (en) 2019-11-20
US20160243106A1 (en) 2016-08-25
KR20160065203A (ko) 2016-06-08
WO2015051307A1 (en) 2015-04-09
TW201601759A (zh) 2016-01-16
US10342792B2 (en) 2019-07-09
CN106061483A (zh) 2016-10-26
CA2925132A1 (en) 2015-04-09
AU2014331591B2 (en) 2018-08-16
BR112016007410B1 (pt) 2022-07-19
US20180289695A1 (en) 2018-10-11
DK3052101T3 (da) 2019-12-16

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