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1. WO2016080853 - 2-THIOXOTHIAZOLIDIN-4-ONE DERIVATIVES ACTIVE AS TRANSTHYRETIN LIGANDS AND USES THEREOF

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Publication Number WO/2016/080853
Publication Date 26.05.2016
International Application No. PCT/PT2015/050010
International Filing Date 20.11.2015
IPC
C07D 277/34 2006.1
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
C07D 277/36 2006.1
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 2006.1
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
A61P 25/28 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
CPC
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
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
A61P 25/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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
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
Applicants
  • BSIM2 – BIOMOLECULAR SIMULATIONS LDA [PT]/[PT]
Inventors
  • PONTES MEIRELES FERREIRA DE BRITO, Rui Manuel
  • VIEIRA SIMÕES, Carlos Jose
  • VASCONCELOS DIAS DE PINHO E MELO, Teresa Margarida
  • DA SILVA VICTOR, Bruno Lourenço
  • LOURENÇO DE ALMEIDA, Zaida Catarina
  • CABRAL CARDOSO LOPES, Ana Lúcia
  • OLIVEIRA NASCIMENTO, Bruno Filipe
Agents
  • VIEIRA PEREIRA FERREIRA, Maria Silvina
Priority Data
62/083,11821.11.2014US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) 2-THIOXOTHIAZOLIDIN-4-ONE DERIVATIVES ACTIVE AS TRANSTHYRETIN LIGANDS AND USES THEREOF
(FR) DÉRIVÉS DE 2-THIOXOTHIAZOLIDIN-4-ONE ACTIFS EN TANT QUE LIGANDS DE LA TRANSTHYRÉTINE ET UTILISATIONS DE CES DÉRIVÉS
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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).
(FR) L'invention concerne des composés de formule (II) utilisés pour stabiliser la protéine transthyrétine (TTR) et inhiber la formation de fibrilles amyloïdes, notamment la formation de fibrilles amyloïdes à médiation par la transthyrétine, et pour traiter, prévenir ou atténuer un ou plusieurs symptômes de maladies amyloïdes, telles que l'amyloïdose liée à la transthyrétine (ATTR).
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