CA2951049C - Peptide-drug conjugates - Google Patents

Peptide-drug conjugates Download PDF

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Publication number
CA2951049C
CA2951049C CA2951049A CA2951049A CA2951049C CA 2951049 C CA2951049 C CA 2951049C CA 2951049 A CA2951049 A CA 2951049A CA 2951049 A CA2951049 A CA 2951049A CA 2951049 C CA2951049 C CA 2951049C
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CA
Canada
Prior art keywords
ala
cancer
peptide
asn
pabc
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
CA2951049A
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English (en)
French (fr)
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CA2951049A1 (en
Inventor
Shaosong Chu
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.)
Jiaray Pharmaceuticals Inc
Original Assignee
Jiaray Pharmaceuticals Inc
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 Jiaray Pharmaceuticals Inc filed Critical Jiaray Pharmaceuticals Inc
Publication of CA2951049A1 publication Critical patent/CA2951049A1/en
Application granted granted Critical
Publication of CA2951049C publication Critical patent/CA2951049C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/407Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/55Medicinal 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, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/62Medicinal 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
    • A61K47/65Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (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)
CA2951049A 2014-06-03 2015-06-01 Peptide-drug conjugates Active CA2951049C (en)

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
CA2951049A1 CA2951049A1 (en) 2015-12-10
CA2951049C true CA2951049C (en) 2023-01-03

Family

ID=54700553

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2951049A Active CA2951049C (en) 2014-06-03 2015-06-01 Peptide-drug conjugates

Country Status (9)

Country Link
US (2) US9579317B2 (en:Method)
EP (1) EP3152223B1 (en:Method)
JP (2) JP6539729B2 (en:Method)
CN (1) CN106456799B (en:Method)
AU (1) AU2015270924B2 (en:Method)
CA (1) CA2951049C (en:Method)
ES (1) ES2857192T3 (en:Method)
MA (1) MA40030A (en:Method)
WO (1) WO2015187540A1 (en:Method)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016026458A1 (zh) 2014-08-22 2016-02-25 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
WO2017162663A1 (de) * 2016-03-24 2017-09-28 Bayer Pharma Aktiengesellschaft Prodrugs von cytotoxischen wirkstoffen mit enzymatisch spaltbaren gruppen
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
CN110312533B (zh) 2016-12-21 2023-11-03 拜耳公司 具有酶促可裂解的基团的细胞毒性活性剂的前药
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
WO2018192550A1 (zh) * 2017-04-21 2018-10-25 博瑞生物医药(苏州)股份有限公司 多臂靶向抗癌偶联物
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
US20220064214A1 (en) * 2019-01-07 2022-03-03 Cenna Biosciences Inc. Novel peptides and uses thereof
MX2021011997A (es) * 2019-04-05 2021-11-04 Prolynx Llc Enlazadores de conjugacion mejorados.
JP7475065B2 (ja) * 2019-05-24 2024-04-26 真喜子 大城戸 薬剤、肺胞の洗浄用の薬液、及び、ネブライザー
EP4237012A1 (en) * 2020-10-30 2023-09-06 Avacta Life Sciences Limited Fap-activated serum extended half-life therapeutic conjugates
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
EP4676539A1 (en) * 2023-03-09 2026-01-14 BicycleTx Limited Synthesis of bicycle toxin conjugates, and intermediates thereof
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

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
AU783679B2 (en) * 2000-02-24 2005-11-24 Genentech Inc. Caspase activated prodrugs therapy
US8314060B2 (en) 2000-09-05 2012-11-20 Biosight Ltd. Peptide conjugated anti-cancer prodrugs
CA2536357A1 (en) * 2003-05-29 2004-12-23 The Scripps Research Institute 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
EP2266964B1 (en) * 2009-06-22 2013-01-09 KTB Tumorforschungsgesellschaft mbH Acid-labile trigger units
US8394922B2 (en) * 2009-08-03 2013-03-12 Medarex, Inc. Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
WO2012075472A2 (en) 2010-12-03 2012-06-07 Regents Of The University Of Colorado, A Body Corporate Chemical entities and therapeutic uses thereof

Also Published As

Publication number Publication date
US20170232023A1 (en) 2017-08-17
AU2015270924A1 (en) 2016-12-15
CA2951049A1 (en) 2015-12-10
CN106456799A (zh) 2017-02-22
AU2015270924B2 (en) 2019-09-12
CN106456799B (zh) 2020-05-22
JP2019189623A (ja) 2019-10-31
EP3152223B1 (en) 2020-11-25
JP6539729B2 (ja) 2019-07-03
EP3152223A4 (en) 2017-12-20
US9579317B2 (en) 2017-02-28
US20150343083A1 (en) 2015-12-03
JP2017521486A (ja) 2017-08-03
MA40030A (fr) 2015-12-10
WO2015187540A1 (en) 2015-12-10
ES2857192T3 (es) 2021-09-28
EP3152223A1 (en) 2017-04-12

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