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1. US20220096652 - ACETAL-BASED CLEAVABLE LINKERS

Office
États-Unis d'Amérique
Numéro de la demande 17539929
Date de la demande 01.12.2021
Numéro de publication 20220096652
Date de publication 31.03.2022
Type de publication A1
CIB
A61K 47/68
ANÉCESSITÉS COURANTES DE LA VIE
61SCIENCES MÉDICALE OU VÉTÉRINAIRE; HYGIÈNE
KPRÉPARATIONS À USAGE MÉDICAL, DENTAIRE OU POUR LA TOILETTE
47Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p.ex. les supports ou les additifs inertes; Agents de ciblage ou de modification chimiquement liés à l’ingrédient actif
50l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p.ex. conjugués polymère-médicament
51l’ingrédient non actif étant un agent de modification
68l’agent de modification étant un anticorps, une immunoglobuline ou son fragment, p.ex. un fragment Fc
A61K 31/4995
ANÉCESSITÉS COURANTES DE LA VIE
61SCIENCES MÉDICALE OU VÉTÉRINAIRE; HYGIÈNE
KPRÉPARATIONS À USAGE MÉDICAL, DENTAIRE OU POUR LA TOILETTE
31Préparations médicinales contenant des ingrédients actifs organiques 
33Composés hétérocycliques
395ayant l'azote comme hétéro-atome d'un cycle, p.ex. guanéthidine ou rifamycines
495ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p.ex. pipérazine
4995Pyrazines ou pipérazines formant une partie de systèmes cycliques pontés
CPC
A61K 47/6803
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
68the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
A61K 47/6851
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
68the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
6835the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
6851the antibody targeting a determinant of a tumour cell
A61K 31/4995
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
4995Pyrazines or piperazines forming part of bridged ring systems
Déposants Synaffix B.V.
Inventeurs Jorge Merijn Mathieu VERKADE
Arnoldus Jacobus VAN SCHAIK
Remon VAN GEEL
Maria Antonia WIJDEVEN
Sander Sebastiaan VAN BERKEL
Floris Louis VAN DELFT
Données relatives à la priorité 19177933.9 03.06.2019 EP
Titre
(EN) ACETAL-BASED CLEAVABLE LINKERS
Abrégé
(EN)

The current invention concerns compounds, such as antibody-conjugates, with an enhanced selectivity of payload release inside a tumour or in the tumour microenvironment versus payload release in circulation or in healthy cells. The enhanced selectivity is achieved by incorporation of a cleavable linker that requires two consecutive mechanisms for release of the payload. The compounds according to the invention have structure (1):

or a salt thereof, wherein AB is an antibody or a reactive moiety capable of reacting with a functional group on an antibody, L1 and L2 are linkers, moiety I contains an activating group and an aromatic ring, X is O or N and D is the payload. The invention further concerns application of these compounds in for example a method of targeting a cell and a method for enhancing the bystander effect of an amino-containing payload. The invention also concerns the payloads that may be released from the compounds according to the invention.


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