BR112017027205A2 - derivados de bis-furano como estabilizadores de transtirretina (ttr) e inibidores da amilóide para o tratamento de polineuropatia amiloidótica familiar (fap). - Google Patents

derivados de bis-furano como estabilizadores de transtirretina (ttr) e inibidores da amilóide para o tratamento de polineuropatia amiloidótica familiar (fap).

Info

Publication number
BR112017027205A2
BR112017027205A2 BR112017027205A BR112017027205A BR112017027205A2 BR 112017027205 A2 BR112017027205 A2 BR 112017027205A2 BR 112017027205 A BR112017027205 A BR 112017027205A BR 112017027205 A BR112017027205 A BR 112017027205A BR 112017027205 A2 BR112017027205 A2 BR 112017027205A2
Authority
BR
Brazil
Prior art keywords
transthyretin
amyloid
fap
treatment
bis
Prior art date
Application number
BR112017027205A
Other languages
English (en)
Inventor
Lúcia Cabral Cardoso Lopes Ana
José Vieira Simões Carlos
Cristina Silva Costa Dora
Manuel Pontes Meireles Ferreira De Brito Rui
Margarida Vasconcelos Dias De Pinho E Melo Teresa
Catarina Lourenço De Almeida Zaida
Original Assignee
Bsim2 Biomolecular Simulations S A
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bsim2 Biomolecular Simulations S A filed Critical Bsim2 Biomolecular Simulations S A
Publication of BR112017027205A2 publication Critical patent/BR112017027205A2/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with 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
    • C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545—Heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

derivados de bis-furano como estabilizadores de transtirretina (ttr) e inibidores da amilóide para o tratamento de polineuropatia amiloidótica familiar (fap). o projeto e a síntese de um novo andaime de bis-furano adaptado para alta eficiência na inibição da formação de transtirretina amilóide são relatados. os resultados in vitro mostram que os compostos descobertos são inibidores mais eficientes da formação de amilóides do que o tafamidis, um fármaco atualmente utilizado no tratamento da polineuropatia amiloidótica familiar (fap), apesar do menor peso molecular e lipofilicidade. além disso, experimentos ex vivo com o inibidor mais forte da série, conduzidos em plasma sanguíneo humano de transportadores normais e fap val30met-transtirretina, revelam perfis notáveis de afinidade e seletividade. as promessas e os desafios enfrentados pelo desenvolvimento deste composto são discutidos à luz de evidências crescentes que implicam a estabilidade da transtirretina como fator-chave não apenas nas amiloidoses da transtirretina e várias co-morbidades associadas, mas também na doença de alzheimer.
BR112017027205A 2015-06-15 2016-06-15 derivados de bis-furano como estabilizadores de transtirretina (ttr) e inibidores da amilóide para o tratamento de polineuropatia amiloidótica familiar (fap). BR112017027205A2 (pt)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201562180036P 2015-06-15 2015-06-15
US201562204346P 2015-08-12 2015-08-12
PT10944216 2016-06-09
PCT/IB2016/053546 WO2016203402A1 (en) 2015-06-15 2016-06-15 Bis-furan derivatives as transthyretin (ttr) stabilizers and amyloid inhibitors for the treatment of familial amyloid polyneuropathy (fap)

Publications (1)

Publication Number Publication Date
BR112017027205A2 true BR112017027205A2 (pt) 2019-06-18

Family

ID=57545309

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112017027205A BR112017027205A2 (pt) 2015-06-15 2016-06-15 derivados de bis-furano como estabilizadores de transtirretina (ttr) e inibidores da amilóide para o tratamento de polineuropatia amiloidótica familiar (fap).

Country Status (4)

Country Link
US (1) US10377729B2 (pt)
EP (1) EP3307723B1 (pt)
BR (1) BR112017027205A2 (pt)
WO (1) WO2016203402A1 (pt)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3221299A1 (en) 2014-11-21 2017-09-27 BSIM2 Biomolecular Simulations Lda. 2-thioxothiazolidin-4-one derivatives active as transthyretin ligands and uses thereof
WO2020205683A1 (en) * 2019-03-29 2020-10-08 The Scripps Research Institute Benzopyrane and imidazole derivatives useful for the stabilization of amyloidogenic immunoglobulin light chains

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US303065A (en) * 1884-08-05 John a
US325970A (en) * 1885-09-08 William h
US1156379A (en) * 1914-06-11 1915-10-12 Thomas Spillane Apparatus for removing glass.
NZ241954A (en) 1991-03-15 1994-01-26 Amgen Inc Compositions of g-csf for pulmonary administration.
US5451569A (en) 1994-04-19 1995-09-19 Hong Kong University Of Science And Technology R & D Corporation Limited Pulmonary drug delivery system
US6673814B2 (en) 1997-08-19 2004-01-06 Emory University Delivery systems and methods for noscapine and noscapine derivatives, useful as anticancer agents
US5981496A (en) 1997-09-19 1999-11-09 Millennium Pharmaceutical, Inc. α-pyrones for treating α-pyrone responsive states
US6635677B2 (en) 1999-08-13 2003-10-21 Case Western Reserve University Methoxyamine combinations in the treatment of cancer
ITRM20030194A1 (it) 2003-04-24 2004-10-25 Univ Roma Uso di derivati del 7-nitro-2, 1, 3-benzossadiazolo per
EP1768968A1 (en) 2004-05-20 2007-04-04 Foldrx Pharmaceuticals, Inc. 2-((hetero) aryl)-benzoxazole compounds and derivatives, compositions and methods for stabilizing transthyretin and inhibiting transthyretin misfolding
WO2006002284A1 (en) 2004-06-22 2006-01-05 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
WO2008124838A1 (en) * 2007-04-10 2008-10-16 University Of Maryland, Baltimore Compounds that inhibit human dna ligases and methods of treating cancer
EP3221299A1 (en) * 2014-11-21 2017-09-27 BSIM2 Biomolecular Simulations Lda. 2-thioxothiazolidin-4-one derivatives active as transthyretin ligands and uses thereof

Also Published As

Publication number Publication date
US20180208570A1 (en) 2018-07-26
EP3307723A1 (en) 2018-04-18
US10377729B2 (en) 2019-08-13
EP3307723B1 (en) 2020-11-11
WO2016203402A1 (en) 2016-12-22

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Legal Events

Date Code Title Description
B15I Others concerning applications: loss of priority

Free format text: VIDE PARECER

B11A Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing
B11N Dismissal: publication cancelled [chapter 11.14 patent gazette]

Free format text: ANULADA A PUBLICACAO CODIGO 11.1 NA RPI NO 2530 DE 02/07/2019 POR TER SIDO INDEVIDA.

B25G Requested change of headquarter approved

Owner name: BSIM2 - BIOMOLECULAR SIMULATIONS, S.A. (PT)

B12F Other appeals [chapter 12.6 patent gazette]
B25D Requested change of name of applicant approved

Owner name: BSIM THERAPEUTICS, S.A. (PT)

B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B350 Update of information on the portal [chapter 15.35 patent gazette]
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]