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1. WO2021080846 - NOVEL CONJUGATION CHEMISTRY FOR CATALYTIC ANTTIBODY 38C2

Publication Number WO/2021/080846
Publication Date 29.04.2021
International Application No. PCT/US2020/055768
International Filing Date 15.10.2020
IPC
A61K 39/395 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
39Medicinal preparations containing antigens or antibodies
395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
A61K 47/48 2006.01
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
48the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
A61K 47/51 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
A61K 47/68 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
68the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07K 16/46 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
16Immunoglobulins, e.g. monoclonal or polyclonal antibodies
46Hybrid immunoglobulins
Applicants
  • THE SCRIPPS RESEARCH INSTITUTE [US]/[US]
Inventors
  • RADER, Christoph
  • HWANG, Dobeen
Agents
  • FITTING, Thomas
  • WANG, Hugh
Priority Data
62/925,05123.10.2019US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) NOVEL CONJUGATION CHEMISTRY FOR CATALYTIC ANTTIBODY 38C2
(FR) NOUVELLE CHIMIE DE CONJUGAISON POUR ANTICORPS CATALYTIQUE 38C2
Abstract
(EN)
The present invention provides modified catalytic antibody 38C2 with arylation of the reactive lysine residue (Lys99). The Lys99 residue is arylated with a heteroaryl methyl sulfonyl compound such as methylsulfone phenyl oxadi azole (MS- PODA). The invention also provides antibody conjugated agents (e.g., antibody drug conjugates) that contain an agent moiety that is site-specifically conjugated to 38C2 via a methyl sulfonyl compound. Further provided in the invention are methods of making the antibody conjugated agents and therapeutic applications of the antibody conjugated agents.
(FR)
La présente invention concerne un anticorps catalytique modifié 38C2 avec arylation du résidu lysine réactif (Lys99). Le résidu Lys99 est arylé avec un composé méthylsulfonyle hétéroaryle tel que le méthylsulfone phényl-oxadiazole (MS-PODA). L'invention concerne également des agents conjugués d'anticorps (par exemple, des conjugués anticorps-médicament) qui contiennent une fraction d'agent qui est spécifiquement conjuguée à 38C2 par l'intermédiaire d'un composé méthylsulfonyle. L'invention concerne en outre des procédés de préparation des agents conjugués d'anticorps et des applications thérapeutiques des agents conjugués d'anticorps.
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