AR035493A1 - Derivados de azepino (4,5b) indolina sustituidos, composicion farmaceutica y el uso de dichos derivados para preparar un medicamento - Google Patents

Derivados de azepino (4,5b) indolina sustituidos, composicion farmaceutica y el uso de dichos derivados para preparar un medicamento

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Publication number
AR035493A1
AR035493A1 ARP010104449A ARP010104449A AR035493A1 AR 035493 A1 AR035493 A1 AR 035493A1 AR P010104449 A ARP010104449 A AR P010104449A AR P010104449 A ARP010104449 A AR P010104449A AR 035493 A1 AR035493 A1 AR 035493A1
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AR
Argentina
Prior art keywords
alkyl
hydrocarbylene
hydrogen
independently
het
Prior art date
Application number
ARP010104449A
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English (en)
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Upjohn Co
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Publication date
Application filed by Upjohn Co filed Critical Upjohn Co
Publication of AR035493A1 publication Critical patent/AR035493A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • 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
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurosurgery (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Child & Adolescent Psychology (AREA)
  • Addiction (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Indole Compounds (AREA)

Abstract

Derivados de azepino[4,5b]indolina sustituidos, que comprenden un compuesto de Fórmula (1) en la cual R1 está seleccionado del grupo que consiste en hidrógeno, alquilo C1-8 y hidrocarbileno C1-8 Ar, cada R2 independientemente está seleccionado del grupo que consiste en alquilo C1-8, y OH; R3 es hidrógeno, alquilo C1-8, Ar, Het, R7C(=O)-, R7OC(=O)-, R5R6NC(=O)-, R7C(=S)-, R7SC(=O)-, R5R6NC(=S)-, R7SO2-, R5R6NSO2, R7S(=O)-, R5R6NS(=O)-, Rc hidrocarbileno C1-8, o Rc hidrocarbileno C1-8 C(=O)-; cada R4, independientemente , esta seleccionado del grupo que consiste en Ar, alquilo C1-8, ArO-, alcoxi C1-8, Het, halo, OH, CN, NO2, CF3, CF3O, NRaRb, N=CRaRb, R7S, hidrocarbileno C1-8 Ar, e hidrocarbileno C1-8 ORa; cada R5 y R6 es independientemente hidrógeno, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, haloalquilo C1-8, cicloalquenilo C3-8, Ar, o hidrocarbileno C1-8 Ar; o R5 y R6 conjuntamente con el nitrógeno al cual están unidos forman un anillo pirrolidino, piperidino, morfolino, o tiomorfolino, cada R7 es independientemente hidrógeno, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, haloalquilo C1-8, cicloalquenilo C3-8, Ar, o hidrocarbileno C1-8 Ar, Ra y Rb, independientemente, están seleccionados del grupo que consiste en hidrógeno, alquilo C1-8, Ar, hidrocarbileno C1-3 Ar, SO2Ar, SO2 alquilo C1-4, (cicloalquilo C3-8) alquilo C1-8, y Het; Rc es Ar, Het, R7CO2-, R7C(=O)-, R7OC(=O)-, R7O-, R7 alquileno C1-8 O-, R7S-, R7C(=S)-, R7S(=O)-, R7S(=O)2-, R7SC(=O)-, R7C(=O)N(R7)-, R7C(=S)N(R7)-, R5R6N-, R5R6NC(=O)-, R5R6NC(=S)-, R5R6NS(=O)-, R5R6NSO2-, R7S(=O)N(R7)-, R7SO2N(R7)-, o R7N(R7)C(=O)N(R7)-; cada Ar es independientemente arilo o heteroarilo; p es 0, 1, 2, 3, o 4; y q es 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 o 10; donde Ar de R1, R3- R7, Ra, Rb y Rc está opcionalmente sustituido con uno o más (por ejemplo 1, 2, 3, 4 o 5) sustituyentes independientemente seleccionados de halo, CN, NO2, ORe, metilendioxi, etilendioxi, CF3, OCF3, SRe, SO2Re, NRfRg, CONRfRg, CORe, Re e hidrocarbileno Rd C1-8, cada Rd es independientemente hidroxi, alcoxi C1-8, ciano, SRh o C(=O)Rh, cada Re está independientemente seleccionado del grupo que consiste en hidrógeno, alquilo C1-8, Ar, hidrocarbileno Ar C1-3, SO2Ar, SO2alquilo C1-4, (cicloalquilo C3-8) alquilo C1-8 y Het; donde cualquier Ar de Re está opcionalmente sustituido con uno o más (por ejemplo 1, 2, 3, 4 o 5) sustituyentes independientemente seleccionados de halo, CN, NO2, ORd, metilendioxi, etilendioxi, CF3, OCF3, SRf, SO2Rf, NRfRg, CONRfRg, CORf, Rf e hidrocarbileno Rd C1-8; cada Rf y Rg está independientemente seleccionado del grupo que consiste en hidrógeno, alquilo C1-8, Ar, hidrocarbileno Ar C1-3, SO2Ar, SO2 alquilo C1-4, (cicloalquilo C3-8) alquilo C1-8 y Het; y cada Rh es independientemente hidrógeno, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, halolaquilo C1-8, cicloalquenilo C3-8, fenilo o hidrocarbileno (fenilo) C1-8; o una sal farmacéuticamente aceptable del mismo; con la condición de que cuando (a) R1 es metilo; y (b) R3 hidrógeno o -(CH2)3NR5R6, donde, R5 y R6 son cada uno metilo; entonces p y q no son cada uno 0, y composiciones farmacéuticas que contienen dichos compuestos o sales. Los compuestos y sales son ligandos 5-HT y son útiles para tratar enfermedades, desórdenes, y/o condiciones de un mamífero en el cual está implicada la actividad de un receptor 5-HT. Los compuestos y sales son particularmente útiles para tratar enfermedades del sistema nervioso central. También se refiere al uso de dichos derivados para preparar medicamentos útiles para tratar una enfermedad del sistema nervioso central.
ARP010104449A 2000-09-20 2001-09-20 Derivados de azepino (4,5b) indolina sustituidos, composicion farmaceutica y el uso de dichos derivados para preparar un medicamento AR035493A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US23437600P 2000-09-20 2000-09-20
US26604701P 2001-02-01 2001-02-01
US30196401P 2001-06-29 2001-06-29

Publications (1)

Publication Number Publication Date
AR035493A1 true AR035493A1 (es) 2004-06-02

Family

ID=27398561

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP010104450A AR034264A1 (es) 2000-09-20 2001-09-20 Derivados azepino(4,5-b)indol sustituidos y composiciones farmaceuticas
ARP010104449A AR035493A1 (es) 2000-09-20 2001-09-20 Derivados de azepino (4,5b) indolina sustituidos, composicion farmaceutica y el uso de dichos derivados para preparar un medicamento

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP010104450A AR034264A1 (es) 2000-09-20 2001-09-20 Derivados azepino(4,5-b)indol sustituidos y composiciones farmaceuticas

Country Status (7)

Country Link
US (4) US6583135B2 (es)
EP (2) EP1319005A2 (es)
JP (2) JP2004509893A (es)
AR (2) AR034264A1 (es)
AU (2) AU2001292898A1 (es)
PE (2) PE20020510A1 (es)
WO (2) WO2002024700A2 (es)

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DE19929076A1 (de) 1999-06-25 2000-12-28 Aventis Pharma Gmbh Indanylsubstituierte Benzolcarbonamide, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament sowie sie enthaltende pharmazeutische Zubereitungen
MY122278A (en) 1999-07-19 2006-04-29 Upjohn Co 1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles containing arylsulfones at the 9-position
WO2002004456A1 (en) * 2000-07-06 2002-01-17 Pharmacia & Upjohn Company SUBSTITUTED 2,3,7,8,9,10,11,12-OCTAHYDROAZEPINO[4,5-b]PYRANO[3,2-e]INDOLES

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US6828314B2 (en) 2004-12-07
US20020107278A1 (en) 2002-08-08
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WO2002024701A2 (en) 2002-03-28
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JP2004509893A (ja) 2004-04-02
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EP1319004A2 (en) 2003-06-18
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