BR112022007503A2 - Derivados de ácido 3-(4-(11h-dibenzo[b,e][1,4]azepin-6-il)piperazin-1-il)- e 3-(4-(11h-dibenzo[b,f][1,4]oxazepin/tiazepin/diazepin-11-il)piperazin-1-il)-propanoico como moduladores de receptor de h1 e 5-ht2a para o tratamento de distúrbios do sono - Google Patents

Derivados de ácido 3-(4-(11h-dibenzo[b,e][1,4]azepin-6-il)piperazin-1-il)- e 3-(4-(11h-dibenzo[b,f][1,4]oxazepin/tiazepin/diazepin-11-il)piperazin-1-il)-propanoico como moduladores de receptor de h1 e 5-ht2a para o tratamento de distúrbios do sono

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Publication number
BR112022007503A2
BR112022007503A2 BR112022007503A BR112022007503A BR112022007503A2 BR 112022007503 A2 BR112022007503 A2 BR 112022007503A2 BR 112022007503 A BR112022007503 A BR 112022007503A BR 112022007503 A BR112022007503 A BR 112022007503A BR 112022007503 A2 BR112022007503 A2 BR 112022007503A2
Authority
BR
Brazil
Prior art keywords
piperazin
dibenzo
oxazepin
diazepin
azepin
Prior art date
Application number
BR112022007503A
Other languages
English (en)
Inventor
E Duggan Mark
M Edgar Dale
Original Assignee
Alairion Inc
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 Alairion Inc filed Critical Alairion Inc
Publication of BR112022007503A2 publication Critical patent/BR112022007503A2/pt

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/18—Dibenzazepines; Hydrogenated dibenzazepines
    • C07D223/20—Dibenz [b, e] azepines; Hydrogenated dibenz [b, e] azepines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D267/16—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with two six-membered rings
    • C07D267/18—[b, e]-condensed
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/04—Heterocyclic 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

Landscapes

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

Abstract

DERIVADOS DE ÁCIDO 3-(4-(11H- DIBENZO[B,E][1,4]AZEPIN-6-IL)PIPERAZIN-1-IL)- E 3-(4-(11H- DIBENZO[B,F][1,4]OXAZEPIN/TIAZEPIN/DIAZEPIN-11-IL)PIPER- AZIN-1-IL)-PROPANOICO COMO MODULADORES DE RECEPTOR DE H1 E 5-HT2A PARA O TRATAMENTO DE DISTÚRBIOS DO SONO. A presente invenção refere-se aos derivados de ácido 3-(4-(11H-dibenzo[b,e][1,4]azepin-6-il)piperazin-1-il)-, 3-(4-(dibenzo[b,f] [l,4]oxazepin-11-il)piperazin-1-il)-, 3-(4-(dibenzo[b,f][1,4]tiazepin-11-il)piperazin-1-il)- e 3-(4-(dibenzo[b,f][1,4]diazepin-11-il)piperazin-1-il)-propanoico das fórmulas (I), (II1) e (II): em que X é CR7R8, O, S ou NR7, e aos seus sais farmaceuticamente aceitáveis, composições farmacêuticas, métodos para sua preparação, bem como aos compostos para uso em métodos de tratamento médico. Os compostos descritos aqui são úteis para modular os receptores de H1 e 5-HT2A e devem ser usados no tratamento de distúrbios do sono, tais como fragmentação do sono, sono/despertar perturbado e limiar de despertar. A presente descrição descreve a síntese e caracterização de compostos exemplares, bem como os dados farmacológicos dos mesmos (por exemplo, páginas 143 a 224; exemplos 1 a 33; compostos 1 a 39; tabelas A a R). Um com-posto exemplar é, por exemplo, o ácido 3-(4-(7-cloro-3-metildibenzo[b,f][1,4]oxazepin-ll-il)piperazin-1-il)-2,2-dimetilpropanoico (exemplo 1, composto 1): (I), (II) ou (II').
BR112022007503A 2019-10-21 2020-10-20 Derivados de ácido 3-(4-(11h-dibenzo[b,e][1,4]azepin-6-il)piperazin-1-il)- e 3-(4-(11h-dibenzo[b,f][1,4]oxazepin/tiazepin/diazepin-11-il)piperazin-1-il)-propanoico como moduladores de receptor de h1 e 5-ht2a para o tratamento de distúrbios do sono BR112022007503A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962923762P 2019-10-21 2019-10-21
US202063002096P 2020-03-30 2020-03-30
PCT/US2020/056520 WO2021080997A1 (en) 2019-10-21 2020-10-20 3-(4-(11h-dibenzo[b,e][1,4]azepin-6-yl)piperazin-1-yl)- and 3-(4-(dibenzo[b,f][1,4]oxazepin/thiazepin/diazepin-11-yl)piperazin-1-yl)-propano ic acid derivatives as h1 and 5-ht2a-receptor modulators for the treatment of sleep disorders

Publications (1)

Publication Number Publication Date
BR112022007503A2 true BR112022007503A2 (pt) 2022-07-12

Family

ID=73543319

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112022007503A BR112022007503A2 (pt) 2019-10-21 2020-10-20 Derivados de ácido 3-(4-(11h-dibenzo[b,e][1,4]azepin-6-il)piperazin-1-il)- e 3-(4-(11h-dibenzo[b,f][1,4]oxazepin/tiazepin/diazepin-11-il)piperazin-1-il)-propanoico como moduladores de receptor de h1 e 5-ht2a para o tratamento de distúrbios do sono

Country Status (11)

Country Link
US (1) US11046651B2 (pt)
EP (1) EP4048667B1 (pt)
JP (1) JP2023501000A (pt)
KR (1) KR20220084369A (pt)
CN (1) CN114929688A (pt)
AU (1) AU2020370063A1 (pt)
BR (1) BR112022007503A2 (pt)
CA (1) CA3154630A1 (pt)
IL (1) IL292370A (pt)
MX (1) MX2022004736A (pt)
WO (1) WO2021080997A1 (pt)

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Also Published As

Publication number Publication date
EP4048667A1 (en) 2022-08-31
JP2023501000A (ja) 2023-01-17
IL292370A (en) 2022-06-01
CA3154630A1 (en) 2021-04-29
US20210114989A1 (en) 2021-04-22
CN114929688A (zh) 2022-08-19
AU2020370063A1 (en) 2022-06-02
WO2021080997A1 (en) 2021-04-29
US11046651B2 (en) 2021-06-29
EP4048667B1 (en) 2024-07-03
KR20220084369A (ko) 2022-06-21
MX2022004736A (es) 2022-07-27

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