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1. WO2021038125 - CONJUGATES AND CONJUGATES FOR USE IN PREVENTING OR TREATING OF BRAIN DAMAGE AND NEURODEGENERATIVE DISEASES

Publication Number WO/2021/038125
Publication Date 04.03.2021
International Application No. PCT/FI2020/050533
International Filing Date 17.08.2020
IPC
A61K 47/54 2017.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
CPC
A61K 47/548
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
548Phosphates or phosphonates, e.g. bone-seeking
A61K 47/549
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
549Sugars, nucleosides, nucleotides or nucleic acids
Applicants
  • MEDICORTEX FINLAND OY [FI]/[FI]
Inventors
  • HAREL, Adrian
Agents
  • FINNPATENT OY
Priority Data
2019571530.08.2019FI
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) CONJUGATES AND CONJUGATES FOR USE IN PREVENTING OR TREATING OF BRAIN DAMAGE AND NEURODEGENERATIVE DISEASES
(FR) CONJUGUÉS ET CONJUGUÉS DESTINÉS À ÊTRE UTILISÉS DANS LA PRÉVENTION OU LE TRAITEMENT DE LÉSIONS CÉRÉBRALES ET DE MALADIES NEURODÉGÉNÉRATIVES
Abstract
(EN)
The present invention relates to conjugates comprising one or more compounds selected from of (i) an anti-inflammatory compound, and/or (ii) an antioxidant compound, and/or (iii) and antibiotic compound and/or, (iv) a metal chelating compound and at least one of (v) a blood-brain barrier compound and (vi) solubility enhancer moiety. The compounds of group (i)-(v) and the solubility enhancer moiety (vi), when present, are covalently bound together with one or more linkers. The blood-brain barrier targeting compound is monosaccharide and the solubility enhancer moiety is a phosphate group. Present invention further provides pharmaceutical compositions including such conjugates and uses of these conjugates and compositions for treating and/or prevention of neurodegenerative diseases and brain damage due to traumatic and/or acquired brain injury.
(FR)
La présente invention concerne des conjugués comprenant un ou plusieurs composés choisis parmi (i) un composé anti-inflammatoire et/ou (ii) un composé antioxydant, et/ou (iii) et un composé antibiotique et/ou, (iv) un composé chélateur métallique et au moins l'un parmi (v) un composé ciblant la barrière hémato-encéphalique et (vi) une fraction d'amélioration de la solubilité. Les composés du groupe (i) à (v) et la fraction d'amélioration de la solubilité (vi), lorsqu'ils sont présents, sont liés de manière covalente à un ou plusieurs lieurs. Le composé ciblant la barrière hémato-encéphalique est un monosaccharide et la fraction d'amélioration de la solubilité est un groupe phosphate. La présente invention concerne en outre des compositions pharmaceutiques comprenant de tels conjugués et des utilisations de ces conjugués et compositions pour le traitement et/ou la prévention de maladies neurodégénératives et de lésions cérébrales dues à une lésion cérébrale traumatique et/ou acquise.
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