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1. WO2021091881 - HIGH CONCENTRATION CELL PENETRATING CASPASE INHIBITOR CONJUGATES COMPOSITIONS AND METHODS THEREOF

Publication Number WO/2021/091881
Publication Date 14.05.2021
International Application No. PCT/US2020/058683
International Filing Date 03.11.2020
IPC
A61K 31/4458 2006.01
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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
445Non-condensed piperidines, e.g. piperocaine
4458only substituted in position 2, e.g. methylphenidate
A61K 38/55 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
55Protease inhibitors
A61K 47/64 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
62the modifying agent being a protein, peptide or polyamino acid
64Drug-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
Applicants
  • THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK [US]/[US]
Inventors
  • TROY, Carol, M.
  • POTENTSKI, Anna, M.
  • AVRUTSKY, Maria, I.
Agents
  • LECOINTE, Michelle M.
Priority Data
62/930,37104.11.2019US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) HIGH CONCENTRATION CELL PENETRATING CASPASE INHIBITOR CONJUGATES COMPOSITIONS AND METHODS THEREOF
(FR) COMPOSITIONS DE CONJUGUÉS D'INHIBITEURS DE CASPASE DE PÉNÉTRATION CELLULAIRE À CONCENTRATION ÉLEVÉE ET PROCÉDÉS ASSOCIÉS
Abstract
(EN)
A method of providing a high concentration disulfide-linked caspase inhibitor-cell penetrating peptide conjugate is described. The method includes incubating a caspase inhibitor having one or more thiol groups with a reducing agent selected from dithiothreitol (DTT), 2-mercaptoethanol (2-ME) and tris(2-carboxyethyl)phosphine (TCEP) to provide a reduced caspase inhibitor, removing the reducing agent from the reduced caspase inhibitor, and conjugating the reduced caspase inhibitor with a cell-penetrating peptide by a disulfide linkage.
(FR)
L'invention concerne un procédé de fourniture d'un conjugué de peptide de pénétration cellulaire-inhibiteur de caspase à liaison disulfure à concentration élevée. Le procédé consiste à incuber un inhibiteur de caspase comportant un ou plusieurs groupes thiol avec un agent réducteur choisi parmi le dithiothréitol (DTT), le 2-mercaptoéthanol (2-ME) et la tris(2-carboxyéthyl)phosphine (TCEP) pour fournir un inhibiteur de caspase réduit, à éliminer l'agent réducteur de l'inhibiteur de caspase réduit et à conjuguer l'inhibiteur de caspase réduit avec un peptide de pénétration cellulaire au moyen d'une liaison disulfure.
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