SG10201811365RA - Slow-release conjugates of sn-38 - Google Patents

Slow-release conjugates of sn-38

Info

Publication number
SG10201811365RA
SG10201811365RA SG10201811365RA SG10201811365RA SG10201811365RA SG 10201811365R A SG10201811365R A SG 10201811365RA SG 10201811365R A SG10201811365R A SG 10201811365RA SG 10201811365R A SG10201811365R A SG 10201811365RA SG 10201811365R A SG10201811365R A SG 10201811365RA
Authority
SG
Singapore
Prior art keywords
slow
conjugates
release
release conjugates
glucuronate
Prior art date
Application number
SG10201811365RA
Inventor
Gary Ashley
Eric L Schneider
Original Assignee
Prolynx Llc
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 Prolynx Llc filed Critical Prolynx Llc
Publication of SG10201811365RA publication Critical patent/SG10201811365RA/en

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    • 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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20—Organic 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
    • 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
    • C07D457/00—Heterocyclic compounds containing indolo [4, 3-f, g] quinoline ring systems, e.g. derivatives of ergoline, of the formula:, e.g. lysergic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/22—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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
    • 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
    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32—Polymers modified by chemical after-treatment
    • C08G65/329—Polymers modified by chemical after-treatment with organic compounds
    • 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
    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32—Polymers modified by chemical after-treatment
    • C08G65/329—Polymers modified by chemical after-treatment with organic compounds
    • C08G65/333—Polymers modified by chemical after-treatment with organic compounds containing nitrogen
    • C08G65/33396—Polymers modified by chemical after-treatment with organic compounds containing nitrogen having oxygen in addition to nitrogen
    • 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
    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/34—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from hydroxy compounds or their metallic derivatives
    • C08G65/48—Polymers modified by chemical after-treatment
    • 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

Landscapes

  • 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)

Abstract

SLOW-RELEASE CONJUGATES OF SN- Conjugates of SN-38 that provide optimal drug release rates and minimize the formation of the corresponding glucuronate are described. The conjugates release SN- 38 from a polyethylene glycol through a (3-elimination mechanism. Figure 5 29
SG10201811365RA 2013-10-04 2014-10-03 Slow-release conjugates of sn-38 SG10201811365RA (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361887111P 2013-10-04 2013-10-04

Publications (1)

Publication Number Publication Date
SG10201811365RA true SG10201811365RA (en) 2019-02-27

Family

ID=51871275

Family Applications (2)

Application Number Title Priority Date Filing Date
SG10201811365RA SG10201811365RA (en) 2013-10-04 2014-10-03 Slow-release conjugates of sn-38
SG11201602258WA SG11201602258WA (en) 2013-10-04 2014-10-03 Slow-release conjugates of sn-38

Family Applications After (1)

Application Number Title Priority Date Filing Date
SG11201602258WA SG11201602258WA (en) 2013-10-04 2014-10-03 Slow-release conjugates of sn-38

Country Status (14)

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

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6473145B2 (en) * 2013-10-04 2019-02-20 プロリンクス エルエルシー SN-38 sustained release conjugate
CN107375288B (en) * 2016-05-16 2019-08-23 博瑞生物医药（苏州）股份有限公司 The polymerization target anticancer conjugate of multi-arm
CA3058029A1 (en) * 2017-04-21 2018-10-25 Brightgene Bio-Medical Technology Co., Ltd. Multi-arm targeted anti-cancer conjugate
CA3087628A1 (en) * 2018-01-12 2019-07-18 Prolynx Llc Synergistic cancer treatment
EP3852793A4 (en) * 2018-09-17 2022-07-13 The Children's Hospital Of Philadelphia Polymer-based macromolecular prodrugs
KR20210150496A (en) * 2019-04-05 2021-12-10 프로린크스 엘엘시 Improved conjugation linker
MX2022002340A (en) * 2019-08-28 2022-04-06 Prolynx Llc Conjugated inhibitors of dna damage response.
WO2022064052A1 (en) 2020-09-28 2022-03-31 Fundació Institut De Recerca Biomèdica (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
WO2023186822A1 (en) 2022-03-28 2023-10-05 Hospital Sant Joan De Deu Peptidic water-soluble delivery system of anticancer drugs

Family Cites Families (18)

* Cited by examiner, † Cited by third party
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
CA2491661A1 (en) * 2002-07-12 2004-01-22 Biomarin Pharmaceutical Inc. The use of isocyanate linkers to make hydrolyzable active agent biopolymer conjugates
JP4745664B2 (en) 2002-10-31 2011-08-10 日本化薬株式会社 Polymer 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
PT1675622T (en) * 2003-09-17 2017-09-19 Nektar Therapeutics Multi-arm polymer prodrugs
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
CN101541332A (en) * 2006-09-15 2009-09-23 安佐制药股份有限公司 Targeted polymeric prodrugs containing multifunctional linkers
EP2341774B1 (en) * 2008-10-21 2013-12-04 Belrose Pharma Inc. Treatment of neuroblastoma with multi-arm polymeric conjugates of 7-ethyl-10-hydroxycamptothecin
US20100126866A1 (en) 2008-11-18 2010-05-27 Baxter Healthcare S.A. Methods of determining polydispersity and/or molecular weight distribution of a polyethylene glycol sample
CN102448469A (en) 2009-05-28 2012-05-09 摩萨纳医疗有限公司 Polyal (ketone) drug conjugates comprising variable rate-releasing linkers
MX338134B (en) * 2009-11-18 2016-04-01 Nektar Therapeutics Acid salt forms of polymer-drug conjugates and alkoxylation methods.
WO2011140376A1 (en) * 2010-05-05 2011-11-10 Prolynx Llc Controlled drug release from dendrimers
US8754190B2 (en) 2010-05-05 2014-06-17 Prolynx Llc Controlled release from macromolecular conjugates
JP2012000072A (en) * 2010-06-18 2012-01-05 Japan Health Science Foundation Novel antifibrin antibody
WO2012029076A2 (en) * 2010-08-30 2012-03-08 Sun Pharma Advanced Research Company 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
JP6473145B2 (en) * 2013-10-04 2019-02-20 プロリンクス エルエルシー SN-38 sustained release conjugate

Also Published As

Publication number Publication date
EP3052101A1 (en) 2016-08-10
AU2018256608A1 (en) 2018-11-22
MX371201B (en) 2020-01-22
US10342792B2 (en) 2019-07-09
DK3052101T3 (en) 2019-12-16
KR102320753B1 (en) 2021-11-02
US20160243106A1 (en) 2016-08-25
BR112016007410A2 (en) 2017-08-01
AU2014331591A1 (en) 2016-05-19
SG11201602258WA (en) 2016-04-28
BR112016007410B1 (en) 2022-07-19
ES2759905T3 (en) 2020-05-12
CN106061483A (en) 2016-10-26
WO2015051307A1 (en) 2015-04-09
TW201601759A (en) 2016-01-16
EP3052101B1 (en) 2019-11-20
US20180289695A1 (en) 2018-10-11
BR112016007410A8 (en) 2020-02-27
AU2014331591B2 (en) 2018-08-16
JP6473145B2 (en) 2019-02-20
US10016411B2 (en) 2018-07-10
MX2016004299A (en) 2016-10-04
JP6842479B2 (en) 2021-03-17
CN106061483B (en) 2021-01-08
KR20160065203A (en) 2016-06-08
CA2925132A1 (en) 2015-04-09
JP2016531895A (en) 2016-10-13
CA2925132C (en) 2021-11-30
TWI716342B (en) 2021-01-21
JP2019104739A (en) 2019-06-27

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