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1. WO2020118178 - MONOMETHYL FUMARATE-CARRIER CONJUGATES AND METHODS OF THEIR USE

Publication Number WO/2020/118178
Publication Date 11.06.2020
International Application No. PCT/US2019/064926
International Filing Date 06.12.2019
IPC
A61K 31/225 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
21Esters, e.g. nitroglycerine, selenocyanates
215of carboxylic acids
22of acyclic acids, e.g. pravastatin
225Polycarboxylic acids
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
A61P 25/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 37/02 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
02Immunomodulators
CPC
A61K 31/225
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
21Esters, e.g. nitroglycerine, selenocyanates
215of carboxylic acids
22of acyclic acids, e.g. pravastatin
225Polycarboxylic acids
A61K 47/54
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
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 37/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
02Immunomodulators
Applicants
  • FLAGSHIP PIONEERING INNOVATIONS V, INC. [US]/[US]
Inventors
  • CASEY, John, Patrick, Jr.
  • BERRY, David, Arthur
  • ALEXANDER, Jessica, Elizabeth
  • BRIGGS, Timothy
  • BUCKBINDER, Leonard
  • GUNASEKERA, Dinara, Shashanka
  • KAMALI SARVESTANI, Afrand
  • KIM, Mi-Jeong
  • LANTER, Bernard
  • LIANG, Anna
  • NUDEL, Kathleen
  • PECK, Spencer, Cory
  • ROSS, Cheri
  • TAYLOR, Steven, John
  • YASUDA, Koji
Agents
  • ELBING, Karen, L.
Priority Data
62/776,43006.12.2018US
62/938,61021.11.2019US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) MONOMETHYL FUMARATE-CARRIER CONJUGATES AND METHODS OF THEIR USE
(FR) CONJUGUÉS DE MONOMÉTHYL FUMARATE ET D'UN PORTEUR ET LEURS MÉTHODES D'UTILISATION
Abstract
(EN)
Disclosed are conjugates of monomethyl fumarate and a carrier group or aminocarrier group, or a pharmaceutically acceptable salt thereof. In the conjugates, monomethyl fumarate acyl is covalently bonded to the carrier group or aminocarrier group through a carbon-oxygen bond that is cleavable in vivo. The carrier group may include a core, e.g., a monosaccharide, a sugar acid (e.g., acid monosaccharide), a sugar alcohol, or a catechin polyphenol. The aminocarrier group may include a core, e.g., an aminomonosaccharide. The carrier group or aminocarrier group may include, e.g., at least one short chain fatty acid acyl, at least one tryptophan analogue, at least one ketone body, or at least one preketone body. Also disclosed are pharmaceutical compositions containing the conjugates and methods of their use.
(FR)
L'invention concerne des conjugués de monométhyl fumarate et d'un groupe porteur ou d'un groupe aminoporteur, ou d'un sel pharmaceutiquement acceptable de ceux-ci. Dans les conjugués, l'acyle monofumarate est lié de manière covalente au groupe porteur ou au groupe aminoporteur par l'intermédiaire d'une liaison carbone-oxygène qui peut être clivée in vivo. Le groupe porteur peut comprendre un noyau, par exemple un monosaccharide, un acide de sucre (par exemple, un monosaccharide acide), un alcool de sucre ou un polyphénol de catéchine. Le groupe aminoporteur peut comprendre un noyau, par exemple un aminomonosaccharide. Le groupe porteur ou le groupe aminoporteur peut comprendre, par exemple, au moins un acyle d'acide gras à chaîne courte, au moins un analogue de tryptophane, au moins un corps de cétone, ou au moins un corps de précétone. L'invention concerne également des compositions pharmaceutiques contenant les conjugués et des méthodes d'utilisation de celles-ci.
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