CN106456799B - 肽-药物偶联物 - Google Patents

肽-药物偶联物 Download PDF

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Publication number
CN106456799B
CN106456799B CN201580029854.5A CN201580029854A CN106456799B CN 106456799 B CN106456799 B CN 106456799B CN 201580029854 A CN201580029854 A CN 201580029854A CN 106456799 B CN106456799 B CN 106456799B
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ala
asn
pabc
peptide
mitomycin
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CN106456799A (zh
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储少嵩
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Jiaruide Beijing Pharmaceutical Co ltd
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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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K47/50—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
    • A61K47/55—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 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
    • 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
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201580029854.5A 2014-06-03 2015-06-01 肽-药物偶联物 Active CN106456799B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462007159P 2014-06-03 2014-06-03
US62/007,159 2014-06-03
PCT/US2015/033509 WO2015187540A1 (en) 2014-06-03 2015-06-01 Peptide-drug conjugates

Publications (2)

Publication Number Publication Date
CN106456799A CN106456799A (zh) 2017-02-22
CN106456799B true CN106456799B (zh) 2020-05-22

Family

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Family Applications (1)

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CN201580029854.5A Active CN106456799B (zh) 2014-06-03 2015-06-01 肽-药物偶联物

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US (2) US9579317B2 (enExample)
EP (1) EP3152223B1 (enExample)
JP (2) JP6539729B2 (enExample)
CN (1) CN106456799B (enExample)
AU (1) AU2015270924B2 (enExample)
CA (1) CA2951049C (enExample)
ES (1) ES2857192T3 (enExample)
MA (1) MA40030A (enExample)
WO (1) WO2015187540A1 (enExample)

Families Citing this family (17)

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Publication number Priority date Publication date Assignee Title
CN106715457B (zh) 2014-08-22 2021-09-28 亚飞（上海）生物医药科技有限公司 一种肿瘤微环境特异激活的小分子靶向偶联体及其用途
SG10202008909VA (en) * 2016-03-24 2020-10-29 Bayer Pharma AG Prodrugs of cytotoxic active agents having enzymatically cleavable groups
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
US12059472B2 (en) 2016-12-21 2024-08-13 Bayer Aktiengesellschaft Prodrugs of cytotoxic active agents having enzymatically cleavable groups
CN108314703B (zh) * 2017-01-17 2022-02-01 亚飞（上海）生物医药科技有限公司 分子定点靶向和激活的激酶抑制剂的制备和用途
KR102279429B1 (ko) * 2017-04-21 2021-07-20 브라이트제네 바이오-메디컬 테크놀로지 코., 엘티디. 멀티 암 표적 항암 콘쥬게이트
CN107670048B (zh) * 2017-08-30 2019-04-26 南京明臻医药科技有限公司 具有协同抗癌活性的中间体药物和聚乙二醇偶联协同抗癌药物、及其制备方法和应用
EP3908307A4 (en) * 2019-01-07 2022-10-12 Cenna Biosciences Inc. NOVEL PEPTIDES AND USES THEREOF
MX2021011997A (es) * 2019-04-05 2021-11-04 Prolynx Llc Enlazadores de conjugacion mejorados.
US20220313625A1 (en) * 2019-05-24 2022-10-06 The Jikei University Pharmaceutical agent, medicinal solution for cleaning pulmonary alveoli, and nebulizer
JP2023548310A (ja) * 2020-10-30 2023-11-16 アバクタ・ライフ・サイエンシーズ・リミテッド Ｆａｐ活性化血清半減期延長型治療用コンジュゲート
US20230381330A1 (en) * 2020-10-30 2023-11-30 Avacta Life Sciences Limited Enzyme-activated serum extended half-life therapeutic conjugates
CN115850288B (zh) * 2022-11-25 2025-03-21 中科帅天医药(深圳)有限公司 一种丝裂霉素c前体药物及其制备方法和应用
IL322909A (en) * 2023-03-09 2025-10-01 Bicycletx Ltd Synthesis of bicyclic toxin conjugates and their intermediates
CN117683079B (zh) * 2023-12-12 2025-04-04 九洲药业(杭州)有限公司 一种抗体偶联药物连接子的固相合成方法
TW202613146A (zh) * 2024-06-11 2026-04-01 美商克林提克斯醫藥股份有限公司 生長抑素亞型-2受體(sst2r)非肽藥物偶聯物及其用途
CN121851112A (zh) * 2026-03-17 2026-04-14 内蒙古大学 环肽毒素类drug-linker及其制备方法和应用

Citations (3)

* Cited by examiner, † Cited by third party
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CN1406137A (zh) * 2000-02-24 2003-03-26 杰南技术公司 天冬氨酸特异性半胱氨酸蛋白酶活化的前体药物治疗
CN102725001A (zh) * 2009-08-03 2012-10-10 米德列斯公司 抗增殖化合物、其缀合物、其方法及其用途
CN102803228A (zh) * 2009-06-22 2012-11-28 Ktb肿瘤研究有限责任公司 酸不稳定触发子单元

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US3803223A (en) * 1970-07-20 1974-04-09 Searle & Co 3-amino-n-substituted succinamic acids and intermediates thereto
US6214345B1 (en) 1993-05-14 2001-04-10 Bristol-Myers Squibb Co. Lysosomal enzyme-cleavable antitumor drug conjugates
US8314060B2 (en) 2000-09-05 2012-11-20 Biosight Ltd. Peptide conjugated anti-cancer prodrugs
EP1635858A4 (en) * 2003-05-29 2009-08-26 Scripps Research Inst TARGETED DELIVERY TO LEGUMAIN EXPRESSING CELLS
WO2007064759A2 (en) * 2005-11-29 2007-06-07 The Scripps Research Institute Inhibiting tumour cell invasion, metastasis and angiogenesis through targetting legumain
WO2012075472A2 (en) 2010-12-03 2012-06-07 Regents Of The University Of Colorado, A Body Corporate Chemical entities and therapeutic uses thereof

Patent Citations (3)

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CN1406137A (zh) * 2000-02-24 2003-03-26 杰南技术公司 天冬氨酸特异性半胱氨酸蛋白酶活化的前体药物治疗
CN102803228A (zh) * 2009-06-22 2012-11-28 Ktb肿瘤研究有限责任公司 酸不稳定触发子单元
CN102725001A (zh) * 2009-08-03 2012-10-10 米德列斯公司 抗增殖化合物、其缀合物、其方法及其用途

Non-Patent Citations (1)

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The Legumain Protease-Activated Auristatin Prodrugs Suppress Tumor Growth and Metastasis without Toxicity;Krishna Mohan Bajjuri et al.,;《ChemMedChem》;20110103;第6卷(第1期);第54-59页 *

Also Published As

Publication number Publication date
JP6539729B2 (ja) 2019-07-03
CN106456799A (zh) 2017-02-22
ES2857192T3 (es) 2021-09-28
JP2019189623A (ja) 2019-10-31
MA40030A (fr) 2015-12-10
US20150343083A1 (en) 2015-12-03
US9579317B2 (en) 2017-02-28
EP3152223A4 (en) 2017-12-20
WO2015187540A1 (en) 2015-12-10
EP3152223A1 (en) 2017-04-12
JP2017521486A (ja) 2017-08-03
CA2951049A1 (en) 2015-12-10
AU2015270924A1 (en) 2016-12-15
CA2951049C (en) 2023-01-03
AU2015270924B2 (en) 2019-09-12
EP3152223B1 (en) 2020-11-25
US20170232023A1 (en) 2017-08-17

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Effective date of registration: 20220831

Address after: 2547 Cayman Islands KY1-1104 23 Linden Bay Avenue, Grand Cayman #5-204 Governor's Square Hentai

Patentee after: Cayman Jiarui Pharmaceutical

Address before: Room 918, Innovation R&D Building, No. 14, Wenzhuang Road, Economic Development Zone, Yixing City, Wuxi City, Jiangsu Province, 214213

Patentee before: CHU, Shaosong

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Address after: Room 204, Building 3, No. 68 Xinqing Road, Suzhou Industrial Park, Suzhou Area, China (Jiangsu) Pilot Free Trade Zone, Suzhou City, Jiangsu Province 215000

Patentee after: CHU, Shaosong

Country or region after: China

Address before: KY1-1104 Grand Cayman Island, 23 Lime Bay Avenue, # 5-204 Governor's Square, Hengtai

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Effective date of registration: 20241009

Address after: Room 1510, 1st Floor, Building 5, Courtyard A, Banbidian, Haidian District, Beijing 100039

Patentee after: Jiaruide (Beijing) Pharmaceutical Co.,Ltd.

Country or region after: China

Address before: Room 204, Building 3, No. 68 Xinqing Road, Suzhou Industrial Park, Suzhou Area, China (Jiangsu) Pilot Free Trade Zone, Suzhou City, Jiangsu Province 215000

Patentee before: CHU, Shaosong

Country or region before: China