BR112016007410B1 - Conjugados de sn-38 de liberação lenta, formulações farmacêuticas, métodos de preparo do referido conjugado e usos relacionados - Google Patents

Conjugados de sn-38 de liberação lenta, formulações farmacêuticas, métodos de preparo do referido conjugado e usos relacionados Download PDF

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Publication number
BR112016007410B1
BR112016007410B1 BR112016007410-6A BR112016007410A BR112016007410B1 BR 112016007410 B1 BR112016007410 B1 BR 112016007410B1 BR 112016007410 A BR112016007410 A BR 112016007410A BR 112016007410 B1 BR112016007410 B1 BR 112016007410B1
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BR
Brazil
Prior art keywords
conjugate
peg
conjugates
release
fact
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BR112016007410-6A
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English (en)
Portuguese (pt)
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BR112016007410A8 (pt
BR112016007410A2 (pt
Inventor
Gary Ashley
Eric L. Schneider
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Prolynx Llc
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Publication of BR112016007410A2 publication Critical patent/BR112016007410A2/pt
Publication of BR112016007410A8 publication Critical patent/BR112016007410A8/pt
Publication of BR112016007410B1 publication Critical patent/BR112016007410B1/pt

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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)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (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)
BR112016007410-6A 2013-10-04 2014-10-03 Conjugados de sn-38 de liberação lenta, formulações farmacêuticas, métodos de preparo do referido conjugado e usos relacionados BR112016007410B1 (pt)

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 (3)

Publication Number Publication Date
BR112016007410A2 BR112016007410A2 (pt) 2017-08-01
BR112016007410A8 BR112016007410A8 (pt) 2020-02-27
BR112016007410B1 true BR112016007410B1 (pt) 2022-07-19

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BR112016007410-6A BR112016007410B1 (pt) 2013-10-04 2014-10-03 Conjugados de sn-38 de liberação lenta, formulações farmacêuticas, métodos de preparo do referido conjugado e usos relacionados

Country Status (14)

Country Link
US (2) US10016411B2 (enExample)
EP (1) EP3052101B1 (enExample)
JP (2) JP6473145B2 (enExample)
KR (1) KR102320753B1 (enExample)
CN (1) CN106061483B (enExample)
AU (2) AU2014331591B2 (enExample)
BR (1) BR112016007410B1 (enExample)
CA (1) CA2925132C (enExample)
DK (1) DK3052101T3 (enExample)
ES (1) ES2759905T3 (enExample)
MX (1) MX371201B (enExample)
SG (2) SG11201602258WA (enExample)
TW (1) TWI716342B (enExample)
WO (1) WO2015051307A1 (enExample)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201602258WA (en) * 2013-10-04 2016-04-28 Prolynx Llc Slow-release conjugates of 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
US11730836B2 (en) * 2018-01-12 2023-08-22 Prolynx Llc Synergistic cancer treatment
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
EP3946460A4 (en) 2019-04-05 2023-03-29 Prolynx LLC IMPROVED CONJUGATIONAL LINKERS
MX2022002340A (es) * 2019-08-28 2022-04-06 Prolynx Llc Inhibidores conjugados de la respuesta al daño de adn.
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
JP2025512809A (ja) 2022-03-28 2025-04-22 ホスピタル サン ジョアン デ デウ 抗がん剤のペプチド性水溶性送達システム

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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
AU2003280592B2 (en) 2002-10-31 2008-12-18 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
LT1675622T (lt) * 2003-09-17 2017-09-11 Nektar Therapeutics Daugiašakio polimero provaistai
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
WO2008034124A2 (en) * 2006-09-15 2008-03-20 Enzon Pharmaceuticals, Inc. Targeted polymeric prodrugs containing multifunctional linkers
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WO2010059661A1 (en) 2008-11-18 2010-05-27 Baxter International Inc. Methods of determining polydispersity and/or molecular weight distribution of a polyethylene glycol sample
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AU2010321882B2 (en) * 2009-11-18 2016-01-14 Nektar Therapeutics Salt form of a multi-arm polymer-drug conjugate
EP2571496A4 (en) * 2010-05-05 2016-03-30 Prolynx Llc CONTROLLED RELEASE OF MEDICINE FROM DENIMERS
DK2566335T3 (en) * 2010-05-05 2016-10-03 Prolynx Llc Controlled release of active ingredients from macromolecular CONJUGATES
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SG11201602258WA (en) * 2013-10-04 2016-04-28 Prolynx Llc Slow-release conjugates of sn-38

Also Published As

Publication number Publication date
BR112016007410A8 (pt) 2020-02-27
AU2014331591A1 (en) 2016-05-19
US10016411B2 (en) 2018-07-10
US10342792B2 (en) 2019-07-09
SG10201811365RA (en) 2019-02-27
CN106061483B (zh) 2021-01-08
DK3052101T3 (da) 2019-12-16
ES2759905T3 (es) 2020-05-12
AU2018256608A1 (en) 2018-11-22
BR112016007410A2 (pt) 2017-08-01
KR20160065203A (ko) 2016-06-08
MX2016004299A (es) 2016-10-04
CN106061483A (zh) 2016-10-26
EP3052101A1 (en) 2016-08-10
WO2015051307A1 (en) 2015-04-09
TWI716342B (zh) 2021-01-21
CA2925132A1 (en) 2015-04-09
JP6842479B2 (ja) 2021-03-17
JP6473145B2 (ja) 2019-02-20
KR102320753B1 (ko) 2021-11-02
MX371201B (es) 2020-01-22
US20160243106A1 (en) 2016-08-25
CA2925132C (en) 2021-11-30
JP2016531895A (ja) 2016-10-13
EP3052101B1 (en) 2019-11-20
US20180289695A1 (en) 2018-10-11
SG11201602258WA (en) 2016-04-28
TW201601759A (zh) 2016-01-16
JP2019104739A (ja) 2019-06-27
AU2014331591B2 (en) 2018-08-16

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Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B15K Others concerning applications: alteration of classification

Ipc: A61K 31/4745 (2006.01), A61K 9/00 (2006.01), A61K

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 03/10/2014, OBSERVADAS AS CONDICOES LEGAIS