BR112017012588B8 - Compostos heteroaril-heteroarila bicíclicos de ácido benzoico, seus usos, composições farmacêuticas, métodos de preparação destas e métodos para provocar ou promover o desenvolvimento de neuritos, o crescimento de neuritos e/ou a regeneração de neuritos e para ativar o receptor beta do ácido retinoico - Google Patents

Compostos heteroaril-heteroarila bicíclicos de ácido benzoico, seus usos, composições farmacêuticas, métodos de preparação destas e métodos para provocar ou promover o desenvolvimento de neuritos, o crescimento de neuritos e/ou a regeneração de neuritos e para ativar o receptor beta do ácido retinoico

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Publication number
BR112017012588B8
BR112017012588B8 BR112017012588A BR112017012588A BR112017012588B8 BR 112017012588 B8 BR112017012588 B8 BR 112017012588B8 BR 112017012588 A BR112017012588 A BR 112017012588A BR 112017012588 A BR112017012588 A BR 112017012588A BR 112017012588 B8 BR112017012588 B8 BR 112017012588B8
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Brazil
Prior art keywords
neurite outgrowth
compounds
methods
heteroaryl
neurite
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BR112017012588A
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English (en)
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BR112017012588B1 (pt
BR112017012588A2 (pt
Inventor
David Borthwick Alan
Theresa Brown Jane
Patrick Thomas Corcoran Jonathan
Beatriz De Castro Vasconcelos Gonçalves Maria
trevor mills Mark
Barret Kalindjian Sarkis
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King S College London
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Publication of BR112017012588A2 publication Critical patent/BR112017012588A2/pt
Publication of BR112017012588B1 publication Critical patent/BR112017012588B1/pt
Publication of BR112017012588B8 publication Critical patent/BR112017012588B8/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4245Oxadiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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

Abstract

compostos heteroaril-heteroarila bicíclicos de ácido benzoico como agonistas de receptores beta do ácido retinoico (rarbeta). a presente invenção refere-se em geral ao campo dos compostos terapêuticos e, mais especificamente, a certos compostos heteroaril-heteroarila bicíclicos de ácido benzoico da fórmula seguinte (por conveniência, aqui referidos como "compostos bhba"), os quais, inter alia, são agonistas (seletivos) de receptores beta do ácido retinoico (rarbeta) (p. ex., rarbeta2). a presente invenção também diz respeito a composições farmacêuticas que compreendem tais compostos e ao uso de tais compostos e composições, in vitro e in vivo, para ativar (seletivamente) rarbeta (p. ex., rarbeta2), causar ou promover o desenvolvimento de neuritos, causar ou promover o desenvolvimento de neuritos, o crescimento de neuritos e/ou a regeneração de neuritos e no tratamento de doenças e condições que são mediadas por rarbeta (p. ex., rarbeta2), que melhoram com a ativação de rarbeta (p. ex., rarbeta2), etc., incluindo, p. ex., lesões neurológicas como lesões na medula espinhal.
BR112017012588A 2014-12-17 2015-12-16 Compostos heteroaril-heteroarila bicíclicos de ácido benzoico, seus usos, composições farmacêuticas, métodos de preparação destas e métodos para provocar ou promover o desenvolvimento de neuritos, o crescimento de neuritos e/ou a regeneração de neuritos e para ativar o receptor beta do ácido retinoico BR112017012588B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB201422472 2014-12-17
GB1422472.9 2014-12-17
PCT/EP2015/080029 WO2016097004A1 (en) 2014-12-17 2015-12-16 BICYCLOHETEROARYL-HETEROARYL-BENZOIC ACID COMPOUNDS AS RETINOIC ACID RECEPTOR BETA (RARβ) AGONISTS

Publications (3)

Publication Number Publication Date
BR112017012588A2 BR112017012588A2 (pt) 2018-11-13
BR112017012588B1 BR112017012588B1 (pt) 2023-11-07
BR112017012588B8 true BR112017012588B8 (pt) 2024-03-05

Family

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BR112017012588A BR112017012588B8 (pt) 2014-12-17 2015-12-16 Compostos heteroaril-heteroarila bicíclicos de ácido benzoico, seus usos, composições farmacêuticas, métodos de preparação destas e métodos para provocar ou promover o desenvolvimento de neuritos, o crescimento de neuritos e/ou a regeneração de neuritos e para ativar o receptor beta do ácido retinoico

Country Status (10)

Country Link
US (4) US9994559B2 (pt)
EP (1) EP3233842A1 (pt)
JP (1) JP6596090B2 (pt)
KR (1) KR102526625B1 (pt)
CN (1) CN107207488B (pt)
AU (1) AU2015367531B2 (pt)
BR (1) BR112017012588B8 (pt)
CA (1) CA2970574C (pt)
IL (1) IL252882B (pt)
WO (1) WO2016097004A1 (pt)

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AU2015367531B2 (en) 2014-12-17 2020-04-30 King's College London Bicycloheteroaryl-heteroaryl-benzoic acid compounds as retinoic acid receptor beta (RARbeta) agonists
GB201610867D0 (en) * 2016-06-22 2016-08-03 King's College London Crystalline forms of a therapeutic compound and processes for their preparation
CN111892591A (zh) * 2019-05-06 2020-11-06 南京科技职业学院 一种维奈托克关键中间体的合成方法
GB201907647D0 (en) 2019-05-30 2019-07-17 King S College London Therapeutic methods
CN115427401A (zh) * 2020-05-29 2022-12-02 巴斯夫欧洲公司 取代4-(n′-羟基甲脒基)苯甲酸的制备
CN112552252B (zh) * 2020-09-30 2024-01-02 浙江美诺华药物化学有限公司 一种氟雷拉纳中间体的制备方法
CN113264832A (zh) * 2021-05-13 2021-08-17 南京爱可德夫科技开发有限公司 一种合成高纯度2-氟-4-溴苯甲酸叔丁酯的方法
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KR102526625B1 (ko) 2023-04-27
US20170327489A1 (en) 2017-11-16
CN107207488A (zh) 2017-09-26
EP3233842A1 (en) 2017-10-25
BR112017012588B1 (pt) 2023-11-07
IL252882B (en) 2020-04-30
US20190010146A1 (en) 2019-01-10
AU2015367531A1 (en) 2017-07-06
AU2015367531B2 (en) 2020-04-30
KR20170097125A (ko) 2017-08-25
CN107207488B (zh) 2020-11-17
JP6596090B2 (ja) 2019-10-23
JP2017537967A (ja) 2017-12-21
US11401265B2 (en) 2022-08-02
CA2970574A1 (en) 2016-06-23
US10385044B2 (en) 2019-08-20
BR112017012588A2 (pt) 2018-11-13
US10752616B2 (en) 2020-08-25
IL252882A0 (en) 2017-08-31
WO2016097004A1 (en) 2016-06-23
US20210130337A1 (en) 2021-05-06
CA2970574C (en) 2023-09-19
US20200131165A1 (en) 2020-04-30
US9994559B2 (en) 2018-06-12

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