CY1115885T1 - Αντιστρεπτα πεγκυλιωμενα (pegylated) φαρμακα - Google Patents

Αντιστρεπτα πεγκυλιωμενα (pegylated) φαρμακα

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Publication number
CY1115885T1
CY1115885T1 CY20141100753T CY141100753T CY1115885T1 CY 1115885 T1 CY1115885 T1 CY 1115885T1 CY 20141100753 T CY20141100753 T CY 20141100753T CY 141100753 T CY141100753 T CY 141100753T CY 1115885 T1 CY1115885 T1 CY 1115885T1
Authority
CY
Cyprus
Prior art keywords
drugs
fluorenylmethoxycarbonyl
fms
pegylated
medicines
Prior art date
Application number
CY20141100753T
Other languages
English (en)
Inventor
Yoram Shechter
Matityahu Fridkin
Haim Tsubery
Original Assignee
Yeda Research And Development 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 Yeda Research And Development Co., Ltd. filed Critical Yeda Research And Development Co., Ltd.
Publication of CY1115885T1 publication Critical patent/CY1115885T1/el

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    • 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
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    • C07D207/36—Oxygen or sulfur atoms
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Abstract

Παρέχονται αντιστρεπτά πεγκυλιωμένα (pegylated) φάρμακα με παραγώγιση των ελεύθερων λειτουργικών ομάδων του φαρμάκου που επιλέγονται από amino, υδροξύλιο, mercapto, phosphate και/ ή καρβοξύλιο με ομάδες ευαίσθητες σε ήπιες βασικές συνθήκες όπως 9-fluorenylmethoxycarbonyl (Fmoc) ή 2-sulfo-9-fluorenylmethoxycarbonyl (FMS), στις οποίες ομάδες προσαρτάται μία ρίζα PEG. Σε αυτά τα πεγκυλιωμένα (pegylated) φάρμακα, η ρίζα PEG και το υπόλοιπο φαρμάκου δεν συνδέονται απευθείας μεταξύ τους, αλλά μάλλον και τα δύο υπόλοιπα συνδέονται σε διαφορετικές θέσεις της σκαλωσιάς Fmoc ή της δομής FMS που είναι ευαίσθητη σε υψηλό βαθμό σε βάσεις και μπορεί να απομακρυνθεί υπό φυσιολογικές συνθήκες. Τα φάρμακα είναι κατά προτίμηση φάρμακα που περιέχουν μία ομάδα amino, κατά μέγιστη προτίμηση πεπτίδια και πρωτεΐνες χαμηλού ή μεσαίου μοριακού βάρους.
CY20141100753T 2003-04-08 2014-09-17 Αντιστρεπτα πεγκυλιωμενα (pegylated) φαρμακα CY1115885T1 (el)

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US46081603P 2003-04-08 2003-04-08
EP04726602.8A EP1620118B1 (en) 2003-04-08 2004-04-08 Reversible pegylated drugs

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CY1115885T1 true CY1115885T1 (el) 2017-01-25

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US (7) US7585837B2 (el)
EP (1) EP1620118B1 (el)
JP (1) JP4698579B2 (el)
AU (2) AU2004228793B2 (el)
CA (2) CA2521784C (el)
CY (1) CY1115885T1 (el)
DK (1) DK1620118T3 (el)
ES (1) ES2512499T3 (el)
PL (1) PL1620118T3 (el)
PT (1) PT1620118E (el)
SI (1) SI1620118T1 (el)
WO (1) WO2004089280A2 (el)

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