KR102320753B1 - Sn-38 서방성 컨쥬게이트 - Google Patents

Sn-38 서방성 컨쥬게이트 Download PDF

Info

Publication number
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
Authority
KR
South Korea
Prior art keywords
conjugate
peg
formula
release
linker
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
KR1020167011936A
Other languages
English (en)
Korean (ko)
Other versions
KR20160065203A (ko
Inventor
개리 애쉴리
에릭 엘. 쉬나이더
Original Assignee
프로린크스 엘엘시
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 프로린크스 엘엘시 filed Critical 프로린크스 엘엘시
Publication of KR20160065203A publication Critical patent/KR20160065203A/ko
Application granted granted Critical
Publication of KR102320753B1 publication Critical patent/KR102320753B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

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
    • A61K31/33—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

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)
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

Family

ID=51871275

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020167011936A Active KR102320753B1 (ko) 2013-10-04 2014-10-03 Sn-38 서방성 컨쥬게이트

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

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
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
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
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

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

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
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
CA2925132C (en) 2021-11-30
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

Similar Documents

Publication Publication Date Title
KR102320753B1 (ko) Sn-38 서방성 컨쥬게이트
JP6363125B2 (ja) 巨大分子共役体からの徐放
AU749321B2 (en) Polymeric derivatives of camptothecins
CA3074268A1 (en) Enpp1 inhibitors and their use for the treatment of cancer
US10758626B2 (en) Polymer conjugate comprising a bioactive agent
US12338244B2 (en) Temozolomide compounds, polymers prepared therefrom, and method of treating a disease
CN112957463A (zh) 免疫激活型抗体及其应用
US12472261B2 (en) Conjugated inhibitors of DNA damage response
AU2010265144B2 (en) Acid-labile trigger units
HK1227290B (en) Slow-release conjugates of sn-38
HK1227290A1 (en) Slow-release conjugates of sn-38
KR20170091610A (ko) 신규 peg 유도체

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

P22-X000 Classification modified

St.27 status event code: A-2-2-P10-P22-nap-X000

A201 Request for examination
P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 5

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-OTH-PR1001 (AS PROVIDED BY THE NATIONAL OFFICE)

Year of fee payment: 5