KR102320753B1 - Sn-38 서방성 컨쥬게이트 - Google Patents

Sn-38 서방성 컨쥬게이트 Download PDF

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KR102320753B1
KR102320753B1 KR1020167011936A KR20167011936A KR102320753B1 KR 102320753 B1 KR102320753 B1 KR 102320753B1 KR 1020167011936 A KR1020167011936 A KR 1020167011936A KR 20167011936 A KR20167011936 A KR 20167011936A KR 102320753 B1 KR102320753 B1 KR 102320753B1
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conjugate
peg
formula
release
linker
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KR20160065203A (ko
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개리 애쉴리
에릭 엘. 쉬나이더
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프로린크스 엘엘시
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    • 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
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (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)
KR1020167011936A 2013-10-04 2014-10-03 Sn-38 서방성 컨쥬게이트 Active KR102320753B1 (ko)

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
KR20160065203A KR20160065203A (ko) 2016-06-08
KR102320753B1 true KR102320753B1 (ko) 2021-11-02

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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) SG11201602258WA (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
MX371201B (es) * 2013-10-04 2020-01-22 Prolynx Llc Conjugados de liberación lenta de sn-38.
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
KR102279429B1 (ko) 2017-04-21 2021-07-20 브라이트제네 바이오-메디컬 테크놀로지 코., 엘티디. 멀티 암 표적 항암 콘쥬게이트
MX2020007442A (es) * 2018-01-12 2020-09-14 Prolynx Llc Protocolo para minimizar la toxicidad de dosificaciones de combinacion y agente formador de imagen para verificacion.
CA3112778A1 (en) 2018-09-17 2020-03-26 The Children's Hospital Of Philadelphia Polymer-based macromolecular prodrugs
CN119970617A (zh) * 2019-04-05 2025-05-13 普罗林科斯有限责任公司 改良偶联接头
CA3151529A1 (en) * 2019-08-28 2021-03-04 Prolynx Llc Conjugated inhibitors of dna damage response
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
WO2023186822A1 (en) 2022-03-28 2023-10-05 Hospital Sant Joan De Deu Peptidic water-soluble delivery system of anticancer drugs

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005007136A1 (en) 2003-06-05 2005-01-27 Imarx Therapeutics, Inc. Methods of making pharmaceutical formulations for the delivery of drugs having low aqueous solubility
WO2012029076A2 (en) 2010-08-30 2012-03-08 Sun Pharma Advanced Research Company Ltd. Stable pharmaceutical composition

Family Cites Families (16)

* 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
JP2005537266A (ja) * 2002-07-12 2005-12-08 バイオマリン ファーマシューティカル インコーポレイテッド 加水分解性活性物質であるバイオポリマーコンジュゲートを作製するためのイソシアネートリンカーの使用
AU2003280592B2 (en) 2002-10-31 2008-12-18 Nippon Kayaku Kabushiki Kaisha High-molecular weight derivatives of camptothecins
CA2537336C (en) 2003-09-17 2013-02-26 Nektar Therapeutics Al, Corporation 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
JP2010503708A (ja) * 2006-09-15 2010-02-04 エンゾン ファーマスーティカルズ インコーポレイテッド 多官能性リンカーを含む標的化ポリマープロドラッグ
KR20110075029A (ko) * 2008-10-21 2011-07-05 엔즌 파마슈티칼스, 인코포레이티드 7-에틸-10-하이드록시캄토테신의 다중-암 고분자 컨쥬게이트로 신경모세포종의 치료
AU2009316749A1 (en) 2008-11-18 2011-06-30 Baxter Healthcare S.A. Methods of determining polydispersity and/or molecular weight distribution of a polyethylene glycol sample
AU2010254013A1 (en) 2009-05-28 2011-11-24 Mersana Therapeutics, Inc. Polyal drug conjugates comprising variable rate-releasing linkers
PT2501413T (pt) * 2009-11-18 2019-07-10 Nektar Therapeutics Formas de sal de ácido de conjugados de polímero-fármaco
US8703907B2 (en) * 2010-05-05 2014-04-22 Prolynx Llc Controlled drug release from dendrimers
ES2584381T3 (es) * 2010-05-05 2016-09-27 Prolynx Llc Liberación controlada de compuestos activos desde conjugados macromoleculares
JP2012000072A (ja) * 2010-06-18 2012-01-05 Japan Health Science Foundation 新規な抗フィブリン抗体
EP2654795B1 (en) * 2010-12-21 2018-03-07 Nektar Therapeutics Multi-arm polymeric prodrug conjugates of pemetrexed-based compounds
WO2013036857A1 (en) * 2011-09-07 2013-03-14 Prolynx Llc Sulfone linkers
MX371201B (es) * 2013-10-04 2020-01-22 Prolynx Llc Conjugados de liberación lenta de sn-38.

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005007136A1 (en) 2003-06-05 2005-01-27 Imarx Therapeutics, Inc. Methods of making pharmaceutical formulations for the delivery of drugs having low aqueous solubility
WO2012029076A2 (en) 2010-08-30 2012-03-08 Sun Pharma Advanced Research Company Ltd. Stable pharmaceutical composition

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WO2015051307A1 (en) 2015-04-09
AU2014331591A1 (en) 2016-05-19
KR20160065203A (ko) 2016-06-08
JP6473145B2 (ja) 2019-02-20
JP2019104739A (ja) 2019-06-27
AU2018256608A1 (en) 2018-11-22
TWI716342B (zh) 2021-01-21
JP2016531895A (ja) 2016-10-13
TW201601759A (zh) 2016-01-16
CN106061483A (zh) 2016-10-26
US20160243106A1 (en) 2016-08-25
EP3052101B1 (en) 2019-11-20
CA2925132A1 (en) 2015-04-09
BR112016007410A2 (pt) 2017-08-01
CN106061483B (zh) 2021-01-08
US20180289695A1 (en) 2018-10-11
ES2759905T3 (es) 2020-05-12
DK3052101T3 (da) 2019-12-16
JP6842479B2 (ja) 2021-03-17
BR112016007410B1 (pt) 2022-07-19
SG10201811365RA (en) 2019-02-27
CA2925132C (en) 2021-11-30
AU2014331591B2 (en) 2018-08-16
MX2016004299A (es) 2016-10-04
US10016411B2 (en) 2018-07-10
SG11201602258WA (en) 2016-04-28
US10342792B2 (en) 2019-07-09
EP3052101A1 (en) 2016-08-10
BR112016007410A8 (pt) 2020-02-27
MX371201B (es) 2020-01-22

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