AU2018315154B2 - New targeted cytotoxic ratjadone derivatives and conjugates thereof - Google Patents

New targeted cytotoxic ratjadone derivatives and conjugates thereof Download PDF

Info

Publication number
AU2018315154B2
AU2018315154B2 AU2018315154A AU2018315154A AU2018315154B2 AU 2018315154 B2 AU2018315154 B2 AU 2018315154B2 AU 2018315154 A AU2018315154 A AU 2018315154A AU 2018315154 A AU2018315154 A AU 2018315154A AU 2018315154 B2 AU2018315154 B2 AU 2018315154B2
Authority
AU
Australia
Prior art keywords
amino
esi
methyl
ppm
pmol
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.)
Ceased
Application number
AU2018315154A
Other languages
English (en)
Other versions
AU2018315154A1 (en
Inventor
Mark BRÖNSTRUP
Wera COLLISI
Verena Fetz
Stephan HÜTTEL
Philipp KLAHN
Katrin I. MOHR
Werner Tegge
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.)
Helmholtz Zentrum fuer Infektionsforschung HZI GmbH
Original Assignee
Helmholtz Zentrum fuer Infektionsforschung HZI GmbH
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 Helmholtz Zentrum fuer Infektionsforschung HZI GmbH filed Critical Helmholtz Zentrum fuer Infektionsforschung HZI GmbH
Publication of AU2018315154A1 publication Critical patent/AU2018315154A1/en
Application granted granted Critical
Publication of AU2018315154B2 publication Critical patent/AU2018315154B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/32—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/16—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D309/28—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D309/30—Oxygen atoms, e.g. delta-lactones
    • 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
    • A61K47/551—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 one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic acid
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2018315154A 2017-08-09 2018-08-08 New targeted cytotoxic ratjadone derivatives and conjugates thereof Ceased AU2018315154B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP17185598.4 2017-08-09
EP17185598 2017-08-09
PCT/EP2018/071507 WO2019030284A1 (en) 2017-08-09 2018-08-08 NOVEL TARGETED CYTOTOXIC RATJADONE DERIVATIVES AND CONJUGATES THEREOF

Publications (2)

Publication Number Publication Date
AU2018315154A1 AU2018315154A1 (en) 2020-02-27
AU2018315154B2 true AU2018315154B2 (en) 2022-11-10

Family

ID=59579518

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2018315154A Ceased AU2018315154B2 (en) 2017-08-09 2018-08-08 New targeted cytotoxic ratjadone derivatives and conjugates thereof

Country Status (6)

Country Link
US (1) US11236059B2 (https=)
EP (1) EP3665161B1 (https=)
JP (1) JP7218351B2 (https=)
AU (1) AU2018315154B2 (https=)
CA (1) CA3072399A1 (https=)
WO (1) WO2019030284A1 (https=)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020220085A1 (en) * 2019-05-02 2020-11-05 The University Of Sydney Peptide derivatives and conjugates thereof for treating cancer

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040092581A1 (en) * 2001-02-12 2004-05-13 Arne Burzlaff Ratjadone derivatives for inhibiting cell growth

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1690934A3 (en) 1990-01-12 2008-07-30 Abgenix, Inc. Generation of xenogeneic antibodies
DK0450461T3 (da) * 1990-04-06 1995-10-23 Univ Tulane LHRH-analoger
DE19636721A1 (de) 1996-09-10 1998-03-12 Biotechnolog Forschung Gmbh Antibiotische und antitumorale Verbindung, Herstellungsverfahren, Mittel und DSM 11 071
EP1391213A1 (en) 2002-08-21 2004-02-25 Boehringer Ingelheim International GmbH Compositions and methods for treating cancer using maytansinoid CD44 antibody immunoconjugates and chemotherapeutic agents
US7446196B2 (en) 2004-06-03 2008-11-04 Kosan Biosciences, Incorporated Leptomycin compounds
US7541330B2 (en) 2004-06-15 2009-06-02 Kosan Biosciences Incorporated Conjugates with reduced adverse systemic effects
AU2007254821B2 (en) * 2006-06-01 2013-11-14 Bayer Consumer Care Ag Sustained release pharmaceutical formulation comprising phenylephrine
EP1864682A1 (en) 2006-06-09 2007-12-12 Sanofi-Aventis Leptomycin derivatives
FR2947269B1 (fr) 2009-06-29 2013-01-18 Sanofi Aventis Nouveaux composes anticancereux
DK2528625T3 (da) 2010-04-15 2013-10-14 Spirogen Sarl Pyrrolobenzodiazepiner og konjugater deraf
FI2911699T4 (fi) 2012-10-23 2025-12-09 Synaffix Bv Muokattu vasta-aine, vasta-ainekonjugaatti ja menetelmä niiden valmistamiseksi
WO2015012904A2 (en) 2012-12-13 2015-01-29 Immunomedics, Inc. Antibody-sn-38 immunoconjugates with a cl2a linker
CN105592861A (zh) * 2013-08-02 2016-05-18 赛诺菲 抗Muc1类美登素免疫偶联抗体用于治疗实体瘤的用途

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040092581A1 (en) * 2001-02-12 2004-05-13 Arne Burzlaff Ratjadone derivatives for inhibiting cell growth

Also Published As

Publication number Publication date
WO2019030284A1 (en) 2019-02-14
EP3665161A1 (en) 2020-06-17
US20200239426A1 (en) 2020-07-30
US11236059B2 (en) 2022-02-01
EP3665161B1 (en) 2023-09-27
AU2018315154A1 (en) 2020-02-27
JP7218351B2 (ja) 2023-02-06
JP2020529457A (ja) 2020-10-08
CA3072399A1 (en) 2019-02-14

Similar Documents

Publication Publication Date Title
JP7362714B2 (ja) アマニチンコンジュゲート
AU2021290341B2 (en) Antibody drug conjugates (ADCs) and antibody prodrug conjugates (APDCs) with enzymatically cleavable groups
AU2020200566B2 (en) Novel Hydrophilic Linkers and Ligand-Drug Conjugates Thereof
ES2994375T3 (en) Hydrophilic drug-linker compounds
CN109195631B (zh) 具有鹅膏毒肽的衍生物作为药物的抗体药物缀合物
CN119300867A (zh) 连接子、药物连接子及其偶联物及其使用方法
ES2815353T3 (es) Derivados de benzodiazepina citotóxicos
CA2934617A1 (en) Antibody drug conjugates (adcs) with kinesin spindle protein (ksp)
AU2016360828B2 (en) Derivatives of gamma-amanitin
Klahn et al. The nuclear export inhibitor aminoratjadone is a potent effector in extracellular-targeted drug conjugates
US9486535B2 (en) Methods of making and using nanostructures
AU2018315154B2 (en) New targeted cytotoxic ratjadone derivatives and conjugates thereof
KR20240041969A (ko) 접합 시약 및 이의 접합체
US12377164B2 (en) Linkers and conjugates
US20240376154A1 (en) Bis-intercalating peptides, conjugates and methods of use
Bisbal Lopez Tumor-Targeted Release of Immunostimulatory Agents: Synthesis and Biological Evaluation of Imidazoquinoline-Based Prodrugs and Antibody Conjugates
BR112020004307A2 (pt) análogos de tailanestatina
HK1204473B (en) Methods of making and using nanostructures

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired