CN114630818A - 蛋白-大分子偶联物及其使用方法 - Google Patents

蛋白-大分子偶联物及其使用方法 Download PDF

Info

Publication number
CN114630818A
CN114630818A CN202080068415.6A CN202080068415A CN114630818A CN 114630818 A CN114630818 A CN 114630818A CN 202080068415 A CN202080068415 A CN 202080068415A CN 114630818 A CN114630818 A CN 114630818A
Authority
CN
China
Prior art keywords
substituted
alkyl
alkynyl
aryl
conjugate
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.)
Pending
Application number
CN202080068415.6A
Other languages
English (en)
Chinese (zh)
Inventor
宋运涛
李慧
周海平
廖川
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Aojin Life Sciences Yixing Co ltd
Original Assignee
Beijing Xuan Yi Medical Science And Technology Co ltd
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 Beijing Xuan Yi Medical Science And Technology Co ltd filed Critical Beijing Xuan Yi Medical Science And Technology Co ltd
Publication of CN114630818A publication Critical patent/CN114630818A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • 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
    • A61K47/54—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 compound
    • A61K47/545—Heterocyclic compounds
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • 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
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/642—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent the peptide or protein in the drug conjugate being a cytokine, e.g. IL2, chemokine, growth factors or interferons being the inactive part of the conjugate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/36—Oxygen or sulfur atoms
    • C07D207/40—2,5-Pyrrolidine-diones

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Inorganic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN202080068415.6A 2019-09-30 2020-09-30 蛋白-大分子偶联物及其使用方法 Pending CN114630818A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962908435P 2019-09-30 2019-09-30
US62/908,435 2019-09-30
PCT/US2020/053572 WO2021067458A1 (en) 2019-09-30 2020-09-30 Protein-macromolecule conjugates and methods of use thereof

Publications (1)

Publication Number Publication Date
CN114630818A true CN114630818A (zh) 2022-06-14

Family

ID=75337536

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080068415.6A Pending CN114630818A (zh) 2019-09-30 2020-09-30 蛋白-大分子偶联物及其使用方法

Country Status (13)

Country Link
US (1) US20220401561A1 (https=)
EP (1) EP4037715A4 (https=)
JP (1) JP7784993B2 (https=)
KR (1) KR20220074897A (https=)
CN (1) CN114630818A (https=)
AU (1) AU2020360397A1 (https=)
BR (1) BR112022005465A2 (https=)
CA (1) CA3153644A1 (https=)
IL (1) IL291730B2 (https=)
MX (1) MX2022003065A (https=)
TW (1) TW202126332A (https=)
WO (1) WO2021067458A1 (https=)
ZA (1) ZA202204162B (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115947745A (zh) * 2022-12-26 2023-04-11 中山大学 一种基于白蛋白的光热转换纳米材料及其制备方法和应用
CN120737012A (zh) * 2025-08-29 2025-10-03 苏州金顶生物有限公司 一种新型保护氨基酸、制备方法及其应用

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220109436A (ko) 2019-12-03 2022-08-04 에보텍 인터내셔널 게엠베하 인터페론-결합된 항원 결합 단백질 및 이의 용도
WO2022103983A2 (en) * 2020-11-11 2022-05-19 Sutro Biopharma, Inc. Fluorenylmethyloxycarbonyl and fluorenylmethylaminocarbonyl compounds, protein conjugates thereof, and methods for their use
AU2022249281B2 (en) * 2021-03-29 2025-08-14 Aj Sciences (Yixing) Co., Ltd Protein-macromolecule conjugates and methods of use thereof
CN113929731B (zh) * 2021-12-16 2022-05-10 北京春雷杰创生物科技有限公司 一种促进低分子量蛋白体外复性和提高免疫原性的方法
EP4539887A1 (en) * 2022-06-16 2025-04-23 Merck Sharp & Dohme LLC Interleukin-2 prodrugs

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013036857A1 (en) * 2011-09-07 2013-03-14 Prolynx Llc Sulfone linkers
CN103025164A (zh) * 2010-05-05 2013-04-03 普罗林科斯有限责任公司 从固体支撑物中药物的控制释放
CN103025165A (zh) * 2010-05-05 2013-04-03 普罗林科斯有限责任公司 自大分子共轭物的控释
US20130123461A1 (en) * 2010-05-05 2013-05-16 Prolynx Llc Controlled drug release from dendrimers
US20140256626A1 (en) * 2011-10-18 2014-09-11 Prolynx Llc Peg conjugates of exenatide
CN106232131A (zh) * 2013-10-22 2016-12-14 普洛林克斯有限责任公司 生长抑素和其类似物的结合物

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5116943A (en) 1985-01-18 1992-05-26 Cetus Corporation Oxidation-resistant muteins of Il-2 and other protein
US4766106A (en) 1985-06-26 1988-08-23 Cetus Corporation Solubilization of proteins for pharmaceutical compositions using polymer conjugation
US5206344A (en) 1985-06-26 1993-04-27 Cetus Oncology Corporation Interleukin-2 muteins and polymer conjugation thereof
US5089261A (en) 1989-01-23 1992-02-18 Cetus Corporation Preparation of a polymer/interleukin-2 conjugate
US4902502A (en) 1989-01-23 1990-02-20 Cetus Corporation Preparation of a polymer/interleukin-2 conjugate
US5153310A (en) 1989-02-28 1992-10-06 Du Pont Merck Pharmaceutical Company Il-2 analogs containing n-linked glycosylation sites
US5635597A (en) 1994-05-27 1997-06-03 Affymax Technologies, N.V. Peptides that bind IL-2 receptors
US5932462A (en) 1995-01-10 1999-08-03 Shearwater Polymers, Inc. Multiarmed, monofunctional, polymer for coupling to molecules and surfaces
IL119029A0 (en) 1996-08-07 1996-11-14 Yeda Res & Dev Long-acting drugs and pharamaceutical compositions comprising them
DK1411075T3 (da) 1998-03-12 2008-10-27 Nektar Therapeutics Al Corp Fremgangsmåde til fremstilling af polymerkonjugater
US6168785B1 (en) 1998-07-16 2001-01-02 Institut Pasteur Biological applications of new peptides of IL-2 and derivatives and use as therapeutic agents
FR2826365B1 (fr) 2001-06-20 2003-09-26 Oreal Compositions cosmetiques photoprotectrices contenant des derives amides, sulfonamides ou carbamates aromatiques d'acrylonitrile et nouveaux derives amides, sulfonamides ou carbamates d'acrylonitrile
US20070027073A1 (en) 2003-04-08 2007-02-01 Menachem Rubinstein Long-acting derivatives of pyy agonists
WO2005007121A2 (en) 2003-07-18 2005-01-27 Massachusetts Institute Of Technology Mutant interleukin-2(il-2) polypeptides
BRPI0611872B8 (pt) 2005-06-16 2021-05-25 Nektar Therapeutics reagente polimérico, conjugado, método para preparação de um conjugado e composição farmacêutica
KR101508621B1 (ko) 2007-02-28 2015-04-07 세리나 쎄라퓨틱스, 인코포레이티드 활성화된 폴리옥사졸린 및 이를 포함하는 조성물
US7567215B1 (en) 2007-10-23 2009-07-28 The United States Of America As Represented By The Secretary Of The Navy Portable and inflatable antenna device
CN104529711B (zh) 2007-11-21 2020-02-07 乔治亚大学研究基金公司 炔烃以及炔烃与1,3-偶极-官能化合物反应的方法
WO2009158668A1 (en) 2008-06-26 2009-12-30 Prolynx Llc Prodrugs and drug-macromolecule conjugates having controlled drug release rates
US20100240773A1 (en) * 2009-03-23 2010-09-23 Kenneth Korzekwa Multifunctional linkers
ES2866674T3 (es) 2010-11-12 2021-10-19 Nektar Therapeutics Conjugados de una fracción de IL-2 y un polímero
KR102109067B1 (ko) * 2011-09-07 2020-05-13 프로린크스 엘엘시 생분해성 교차결합을 가지는 하이드로젤
WO2016053107A1 (en) * 2014-10-03 2016-04-07 Synaffix B.V. Sulfamide linker, conjugates thereof, and methods of preparation
WO2019028419A1 (en) 2017-08-03 2019-02-07 Synthorx, Inc. CYTOKINE CONJUGATES FOR THE TREATMENT OF PROLIFERATIVE AND INFECTIOUS DISEASES
KR20220004134A (ko) 2019-04-26 2022-01-11 프로린크스 엘엘시 서방형 사이토카인 컨쥬게이트

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103025164A (zh) * 2010-05-05 2013-04-03 普罗林科斯有限责任公司 从固体支撑物中药物的控制释放
CN103025165A (zh) * 2010-05-05 2013-04-03 普罗林科斯有限责任公司 自大分子共轭物的控释
US20130116407A1 (en) * 2010-05-05 2013-05-09 Gary Ashley Controlled release from macromolecular conjugates
US20130123461A1 (en) * 2010-05-05 2013-05-16 Prolynx Llc Controlled drug release from dendrimers
WO2013036857A1 (en) * 2011-09-07 2013-03-14 Prolynx Llc Sulfone linkers
US20140256626A1 (en) * 2011-10-18 2014-09-11 Prolynx Llc Peg conjugates of exenatide
CN106232131A (zh) * 2013-10-22 2016-12-14 普洛林克斯有限责任公司 生长抑素和其类似物的结合物

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
DANIEL V. SANTI, ET AL.: ""Predictable and tunable half-life extension of therapeutic agents by controlled chemical release from macromolecular conjugates"", 《PNAS》, vol. 109, no. 16, pages 6211, XP055251910, DOI: 10.1073/pnas.1117147109 *
GARY W. ASHLEY, ET AL.: ""Hydrogel drug delivery system with predictable and tunable drug release and degradation rates"", 《PNAS》, vol. 110, no. 6, pages 2318, XP055222102, DOI: 10.1073/pnas.1215498110 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115947745A (zh) * 2022-12-26 2023-04-11 中山大学 一种基于白蛋白的光热转换纳米材料及其制备方法和应用
CN115947745B (zh) * 2022-12-26 2024-02-27 中山大学 一种基于白蛋白的光热转换纳米材料及其制备方法和应用
CN120737012A (zh) * 2025-08-29 2025-10-03 苏州金顶生物有限公司 一种新型保护氨基酸、制备方法及其应用

Also Published As

Publication number Publication date
IL291730B2 (en) 2026-02-01
AU2020360397A1 (en) 2022-03-31
CA3153644A1 (en) 2021-04-08
IL291730B1 (en) 2025-10-01
WO2021067458A1 (en) 2021-04-08
MX2022003065A (es) 2022-06-09
EP4037715A4 (en) 2023-12-13
TW202126332A (zh) 2021-07-16
JP2022549295A (ja) 2022-11-24
JP7784993B2 (ja) 2025-12-12
ZA202204162B (en) 2024-11-27
KR20220074897A (ko) 2022-06-03
BR112022005465A2 (pt) 2022-06-14
EP4037715A1 (en) 2022-08-10
IL291730A (en) 2022-05-01
US20220401561A1 (en) 2022-12-22

Similar Documents

Publication Publication Date Title
CN114630818A (zh) 蛋白-大分子偶联物及其使用方法
US12274737B2 (en) PEGylated recombinant human growth hormone compounds
AU2024227552A1 (en) Conjugates of an IL-2 moiety and a polymer
JP2021091708A (ja) Ｉｌ−７部分とポリマーとのコンジュゲート
KR20100014215A (ko) 신규 단백질 접합체 및 그것의 제조 방법
US20240269293A1 (en) Protein-macromolecule conjugates and methods of use thereof
HK40067205A (en) Protein-macromolecule conjugates and methods of use thereof
RU2845911C1 (ru) Конъюгаты белок-макромолекула и способы их применения
HK40098591A (zh) 蛋白-大分子缀合物及其使用方法
RU2530714C9 (ru) Пэгилированные соединения рекомбинантного гормона роста человека
HK40053166A (en) Conjugates of an il-2 moiety and a polymer
WO2005085283A1 (ja) 修飾インターロイキン−１１及びそれを含有する医薬組成物

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40067205

Country of ref document: HK

TA01 Transfer of patent application right
TA01 Transfer of patent application right

Effective date of registration: 20231010

Address after: Room 2102, 21st Floor, Fengsheng Creation Building, 39 Queen's Road Central, Hong Kong, China

Applicant after: Audiman Pharmaceutical Technology Co.,Ltd.

Address before: 101113 2F, B2 building, No. 13, Guangyuan West Street, Zhangjiawan Town, Tongzhou District, Beijing

Applicant before: Beijing Xuan Yi medical science and Technology Co.,Ltd.

TA01 Transfer of patent application right
TA01 Transfer of patent application right

Effective date of registration: 20241213

Address after: No. 10, Chaquan Road, Nanyue Village, Xinjie Street, Yixing City, Wuxi City, Jiangsu Province, 214205

Applicant after: Aojin Life Sciences (Yixing) Co.,Ltd.

Country or region after: China

Address before: Room 2102, 21st Floor, Fung Shing Building, 39 Queen's Road Central, Hong Kong, China

Applicant before: Audiman Pharmaceutical Technology Co.,Ltd.

Country or region before: Hong-Kong