AR073924A1 - Azepino[4, 5-b]indoles, una composicion farmaceutica y kits que los comprenden y su uso en la modulacion de un receptor de histamina. - Google Patents

Azepino[4, 5-b]indoles, una composicion farmaceutica y kits que los comprenden y su uso en la modulacion de un receptor de histamina.

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Publication number
AR073924A1
AR073924A1 ARP090104221A ARP090104221A AR073924A1 AR 073924 A1 AR073924 A1 AR 073924A1 AR P090104221 A ARP090104221 A AR P090104221A AR P090104221 A ARP090104221 A AR P090104221A AR 073924 A1 AR073924 A1 AR 073924A1
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AR
Argentina
Prior art keywords
substituted
unsubstituted
taken together
alkoxy
carbonylalkoxy
Prior art date
Application number
ARP090104221A
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English (en)
Inventor
Rajendra Parasmal Jain
Sarvajit Chakravarty
Andrew Ahser Protter
David T Hung
Andrew Asher Protter
Marco Giorgetti
Original Assignee
Medivation Technologies 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 Medivation Technologies Inc filed Critical Medivation Technologies Inc
Publication of AR073924A1 publication Critical patent/AR073924A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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

Abstract

Compuesto de azepino[4,5-b]indoles que se pueden usar para modular un receptor de histamina en un individuo. Se describen compuestos, incluyendo 1,2,3,4,5,6-tetrahidroazepino[4,5-b]indoles. También se provee composiciones farmacéuticas y kit que comprenden estos compuestos. Reivindicacion 1: Un compuesto de la formula (1) en donde R1 es H, hidroxilo, nitro, ciano, halo, alquilo C1-8 sustituido o no sustituido alquenilo C2-8 sustituido o no sustituido, alquinilo C2-8 sustituido o no sustituido, perhaloalquilo, acilo, aciloxi, carbonilalcoxi, heterociclilo sustituido o no sustituido, arilo sustituido no sustituido, heteroarilo sustituido o no sustituido, aralquilo sustituido o no sustituido, perhaloalcoxi C1-8, alcoxi, ariloxi, carboxilo, tiol, tioalquilo. amino sustituido o no sustituido, acilamino, aminoacilo, aminocarbonilamino, aminocarboniloxi, aminosulfonilo, sulfonilamino, sulfonilo, alquilsulfonilamino o carbonilalquilenalcoxi; cada R2a, R2b, R3a y R3b es, de modo independiente, H, hidroxilo, nitro, ciano, halo, alquilo C1-8 sustituido o no sustituido, alquenilo C2-8 sustituido o no sustituido, alquinilo C2-8 sustituido o no sustituido, perhaloalquilo, acilo, aciloxi, carbonilalcoxi, heterociclilo sustituido o no sustituido, arilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, aralquilo sustituido o no sustituido, perhaloalcoxi C1-8, alcoxi, ariloxi, carboxiIo, tiol, tioalquilo, amino sustituido o no sustituido, acilamino, aminoacilo, aminocarbonilamino, aminocarboniloxi, aminosulfonilo, sulfonilamino, sulfonilo, alquilsulfonilamino o carbonilalquilenalcoxi o se toma junto con el carbono al que está unido y un R2 o R3 geminal para formar un resto de carbonilo; cada R10a, R10b, R11a y R11b es, de modo independiente, H, hidroxilo, nitro, ciano, halo, alquilo C1-8 sustituido o no sustituido, alquenilo C2-8 sustituido o no sustituido, alquinilo C2-8 sustituido o no sustituido, perhaloalquilo, acilo, aciloxi, carbonilalcoxi, heterociclilo sustituido o no sustituido, arilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, aralquilo sustituido o no sustituido, perhaloalcoxi C1-8, alcoxi, ariloxi, carboxilo, tiol, tioalquilo, amino sustituido, acilamino, aminoacilo, aminocarbonilamino, aminocarboniloxi, aminosulfonilo, sulfonilamino, sulfonilo, alquilsulfonilamino o carbonilalquilenalcoxi o se toma junto con el carbono al que está unido y un geminal R10 o R11 para formar un resto de cicloalquilo o un resto de carbonilo; cada X7, X8, X9 y X10 es, de modo independiente N o CR4; cada R4 es, de modo independiente, H, hidroxilo, nitro, ciano, halo, perhaloalquilo C1-8, alquilo C1-8 sustituido o no sustituido, alquenilo C2-8 sustituido o no sustituido, alquinilo C2-8 sustituido o no sustituido, arilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, perhaloalcoxi C1-8, alcoxi C1-8, ariloxi, carboxilo, carbonilalcoxi, tiol, heterociclilo sustituido o no sustituido, aralquilo sustituido o no sustituido, tioalquilo, amino sustituido o no sustituido, acilamino, aminoacilo, aminocarbonilamino, aminocarboniloxi, aminosulfonilo, sulfonilamino, sulfonilo, carbonilalquilenalcoxi, alquilsulfonilamino o acilo; cada m y q es, de modo independiente, 0 o 1; cada R8a, R8b, R8c, R8d, R8e y R8f es, de modo independiente, H, hidroxilo, alcoxi, halo, perhaloalquilo C1-8, carboxi, carbonilalcoxi, arilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, alquilo C1-8 sustituido o no sustituido, cicloalquilo C3-6 sustituido o no sustituido, alquenilo C2-8 sustituido o no sustituido o se toma junto con un R8 geminal para formar un resto de la formula -OCH2CH2O-, se toma junto con el carbono al que está unido y un R8 geminal para formar un resto de cicloalquilo o un resto de carbonilo, se toma junto con un R8 geminal para formar un metileno o un metileno sustituido, se toma junto con un R8 vecinal y los átomos de carbono a los que están unidos para formar un cicloalquilo C3-8 sustituido o no sustituido, cicloalquenilo C3-8 sustituido o no sustituido o resto de heterociclilo sustituido o no sustituido o se toma junto con un R8 vecinal para formar un enlace, siempre que: (i) a lo sumo un par de grupos vecinales R8 se toman juntos para formar un enlace; y (ii) cuando un R8 se toma junto con un R8 vecinal para formar un enlace, el R8 geminal sea distinto de hidroxilo; Q es un arilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, cicloalquenilo sustituido o no sustituido o heterociclilo sustituido o no sustituido, amino sustituido o no sustituido, alcoxi, aminoacilo, aciloxi, carbonilalcoxi, aminocarbonilalcoxi o acilamino; o una de sus sales o solvatos.
ARP090104221A 2008-10-31 2009-10-30 Azepino[4, 5-b]indoles, una composicion farmaceutica y kits que los comprenden y su uso en la modulacion de un receptor de histamina. AR073924A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US11052708P 2008-10-31 2008-10-31
US17396509P 2009-04-29 2009-04-29
US24525709P 2009-09-23 2009-09-23

Publications (1)

Publication Number Publication Date
AR073924A1 true AR073924A1 (es) 2010-12-09

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ARP090104221A AR073924A1 (es) 2008-10-31 2009-10-30 Azepino[4, 5-b]indoles, una composicion farmaceutica y kits que los comprenden y su uso en la modulacion de un receptor de histamina.

Country Status (11)

Country Link
US (4) US8569287B2 (es)
EP (1) EP2348847A4 (es)
JP (1) JP5551708B2 (es)
CN (1) CN102316732B (es)
AR (1) AR073924A1 (es)
AU (1) AU2009308708B2 (es)
BR (1) BRPI0921798A2 (es)
CA (1) CA2742322A1 (es)
HK (1) HK1164641A1 (es)
TW (1) TWI482773B (es)
WO (1) WO2010051503A1 (es)

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