CY1118072T1 - Συζευγματα cc-1065 αναλογων και διλειτουργικων αρθρωτων - Google Patents

Συζευγματα cc-1065 αναλογων και διλειτουργικων αρθρωτων

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Publication number
CY1118072T1
CY1118072T1 CY20161100997T CY161100997T CY1118072T1 CY 1118072 T1 CY1118072 T1 CY 1118072T1 CY 20161100997 T CY20161100997 T CY 20161100997T CY 161100997 T CY161100997 T CY 161100997T CY 1118072 T1 CY1118072 T1 CY 1118072T1
Authority
CY
Cyprus
Prior art keywords
conjugates
agents
analogs
intermediates
release
Prior art date
Application number
CY20161100997T
Other languages
English (en)
Inventor
Patrick Henry Beusker
Rudy Gerardus Elisabeth Coumans
Ronald Christiaan Elgersma
Wiro Michaël Petrus Bernardus Menge
Johannes Albertus Frederikus Joosten
Henri Johannes Spijker
Groot Franciscus Marinus Hendrikus De
Original Assignee
Syntarga B.V.
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 Syntarga B.V. filed Critical Syntarga B.V.
Publication of CY1118072T1 publication Critical patent/CY1118072T1/el

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    • 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
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    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
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    • A61K47/545—Heterocyclic compounds
    • A61K47/546—Porphyrines; Porphyrine with an expanded ring system, e.g. texaphyrine
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    • 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
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    • 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
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    • 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
    • A61K47/646—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 entire peptide or protein drug conjugate elicits an immune response, e.g. conjugate vaccines
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    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
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    • A61K47/6851—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Virology (AREA)
  • Cell Biology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

Η παρούσα εφεύρεση σχετίζεται με νέα ανάλογα του DNA-αλκυλιωτικού παράγοντα CC-1065 και με τα συζεύγματα αυτών. Περαιτέρω, η εφεύρεση σχετίζεται με ενδιάμεσα για την παρασκευή των εν λόγω παραγόντων και συζευγμάτων. Τα συζεύγματα είναι σχεδιασμένα να απελευθερώνουν το (πολλαπλό) φορτίο τους μετά από ένα ή περισσότερα στάδια ενεργοποίησης με ρυθμό και σε χρονικό διάστημα ελεγχόμενα από το σύζευγμα ώστε να διανεμηθούν εκλεκτικά και/ή να απελευθερωθούν με ελεγχόμενο τρόπο ένας ή περισσότεροι των εν λόγω DNA αλκυλιωτικών παραγόντων. Οι παράγοντες, συζεύγματα, και ενδιάμεσα μπορούν να χρησιμοποιηθούν για τη θεραπευτική αγωγή ασθένειας η οποία χαρακτηρίζεται από ανεπιθύμητο πολλαπλασιασμό (κυττάρων). Ως παράδειγμα, οι παράγοντες και τα συζεύγματα της παρούσας εφεύρεσης μπορούν να χρησιμοποιηθούν για τη θεραπεία νεοπλάσματος.
CY20161100997T 2010-04-21 2016-10-06 Συζευγματα cc-1065 αναλογων και διλειτουργικων αρθρωτων CY1118072T1 (el)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US32643710P 2010-04-21 2010-04-21
US42182410P 2010-12-10 2010-12-10
PCT/NL2011/050278 WO2011133039A2 (en) 2010-04-21 2011-04-21 Novel conjugates of cc-1065 analogs and bifunctional linkers

Publications (1)

Publication Number Publication Date
CY1118072T1 true CY1118072T1 (el) 2017-06-28

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CY20161100997T CY1118072T1 (el) 2010-04-21 2016-10-06 Συζευγματα cc-1065 αναλογων και διλειτουργικων αρθρωτων
CY20181100146T CY1119893T1 (el) 2010-04-21 2018-02-06 Προϊοντα συζευξης cc-1065 αναλογων και διλειτουργικων συνδετων
CY20201100778T CY1124632T1 (el) 2010-04-21 2020-08-20 Προϊοντα συζευξης αναλογων cc-1065 και διλειτουργικοι συνδετες

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CY20181100146T CY1119893T1 (el) 2010-04-21 2018-02-06 Προϊοντα συζευξης cc-1065 αναλογων και διλειτουργικων συνδετων
CY20201100778T CY1124632T1 (el) 2010-04-21 2020-08-20 Προϊοντα συζευξης αναλογων cc-1065 και διλειτουργικοι συνδετες

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US (3) US9629924B2 (el)
EP (3) EP3108886B1 (el)
JP (2) JP6009434B2 (el)
KR (3) KR101747478B1 (el)
CN (1) CN106749665B (el)
AU (2) AU2011243294C1 (el)
BR (1) BR112012026953A8 (el)
CA (2) CA2956934C (el)
CY (3) CY1118072T1 (el)
DK (3) DK3108886T3 (el)
ES (3) ES2660428T3 (el)
HR (3) HRP20161339T1 (el)
HU (3) HUE036912T2 (el)
LT (3) LT2560645T (el)
MX (1) MX336853B (el)
NO (1) NO3056203T3 (el)
PL (3) PL3056203T3 (el)
PT (3) PT2560645T (el)
RU (2) RU2730502C2 (el)
TR (1) TR201802539T4 (el)
UA (1) UA112291C2 (el)
WO (1) WO2011133039A2 (el)
ZA (1) ZA201208282B (el)

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