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1. US20190092737 - 2-thioxothiazolidin-4-one derivatives active as transthyretin ligands and uses thereof

Office
United States of America
Application Number 15528589
Application Date 20.11.2015
Publication Number 20190092737
Publication Date 28.03.2019
Grant Number 11117877
Grant Date 14.09.2021
Publication Kind B2
IPC
C07D 277/36
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
277Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
02not condensed with other rings
20having two or three double bonds between ring members or between ring members and non-ring members
32with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
36Sulfur atoms
A61K 9/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
A61K 31/426
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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425Thiazoles
4261,3-Thiazoles
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 277/34
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
277Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
02not condensed with other rings
20having two or three double bonds between ring members or between ring members and non-ring members
32with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
34Oxygen atoms
CPC
A61K 9/0043
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
0012Galenical forms characterised by the site of application
0043Nose
C07D 277/36
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
277Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
02not condensed with other rings
20having two or three double bonds between ring members or between ring members and non-ring members
32with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
36Sulfur atoms
A61K 31/426
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
425Thiazoles
4261,3-Thiazoles
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 277/34
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
277Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
02not condensed with other rings
20having two or three double bonds between ring members or between ring members and non-ring members
32with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
34Oxygen atoms
Applicants BSIM Therapeutics, S.A.
Inventors Rui Manuel Pontes Meireles Ferreira de Brito
Carlos José Vieira Simões
Teresa Margarida Vasconcelos Dias de Pinho e Melo
Bruno Lourenço da Silva Victor
Zaida Catarina Lourenço de Almeida
Ana Lúcia Cabral Cardoso Lopes
Bruno Filipe Oliveira Nascimento
Agents Wolf, Greenfield & Sacks, P.C.
Title
(EN) 2-thioxothiazolidin-4-one derivatives active as transthyretin ligands and uses thereof
Abstract
(EN)

Compounds of formula (II) are provided for stabilizing protein transthyretin (TTR) and inhibiting amyloid fibril formation, for example, transthyretin-mediated amyloid fibril formation, and for treating, preventing, or ameliorating one or more symptoms of amyloid diseases, for example, transthyretin-related amyloidosis (ATTR).


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