AR032592A1 - Aminoalcoxicarbazoles y el uso de los mismos para la manufactura de un medicamento para el tratamiento de enfermedades del snc - Google Patents

Aminoalcoxicarbazoles y el uso de los mismos para la manufactura de un medicamento para el tratamiento de enfermedades del snc

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Publication number
AR032592A1
AR032592A1 ARP000104632A ARP000104632A AR032592A1 AR 032592 A1 AR032592 A1 AR 032592A1 AR P000104632 A ARP000104632 A AR P000104632A AR P000104632 A ARP000104632 A AR P000104632A AR 032592 A1 AR032592 A1 AR 032592A1
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Argentina
Prior art keywords
alkyl
substituted
cycloalkyl
independently
optionally substituted
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ARP000104632A
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English (en)
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Upjohn Co
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • 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
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    • A—HUMAN NECESSITIES
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    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • C07D209/88—Carbazoles; Hydrogenated carbazoles 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 carbon atoms of the ring system
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D417/06—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 linked by a carbon chain containing only aliphatic carbon atoms

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  • Health & Medical Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
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  • General Chemical & Material Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Anesthesiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Aminoalcoxicarbazoles, que proporcionan compuestos de la formula (1) o su sal farmacéuticamente aceptable, racemato, solvato, tautomero, isomero optico o su derivado profármaco; en donde R1 es H, halo, o C1-6 alquilo; cada R2 es independientemente H, halo, -OH, -CN, CF3, -O C1-6 alquilo, C1-6 alquilo, C3-6cicloalquilo, -NR5R6, -CONR5R6, -SO2NR5R6, -COOR7, -OCF3,o fenilo opcionalmente sustituido con halo, OH, O C1-4 alquilo, o C1-6 alquilo; cada R3 es independientemente H, C1-6 alquilo, o C3-6 cicloalquilo; R4 es arilo, o heteroarilo; R5 y R6 son independientemente H, C1-6 alquilo, o C3-6 cicloalquilo, R7 es H, C1-6 alquilo, o C1-3 alquil-fenilo en donde el fenilo puede estar sustituido con R3; R8 y R9 son independientemente H, C1-6 alquilo, opcionalmente sustituido con arilo, heteroarilo, o C3-6 cicloalquilo, C2-6 alqueno, C3-6 cicloalquilo, C2-6 alquilo sustituido con R10, -CHO, siempre que solamente uno de R8 y R9 sea CHO, y el otro sea H, arilo, heterociclo, en donde el heterociclo está unido a través de un átomo de carbono al nitrogeno al cual está unido, o R8 y R9 conjuntamente con el nitrogeno al cual están unidos forman un anillo heterocíclico en donde el anillo heterocíclico puede tener uno o dos heteroátomos seleccionados del grupo integrado por oxígeno, azufre y N(Y) y en donde los átomos de carbono del anillo heterocíclico están opcionalmente sustituidos con uno o dos R14; R10 es -OH, -O (C1-4 alquilo, ), opcionalmente el alquilo está sustituido con OH, -O(C1-4 alquil)-NR11R12, heterociclo, o -CO2R5; R11 y R12 son independientemente, H o C1-4 alquilo, arilo es fenilo o naftilo, opcionalmente sustituido con uno o más R13; heteroarilo es un radical que es un anillo aromático monocíclico de 5 o 6 miembros, con uno o dos heteroátomos, cada uno seleccionado del grupo integrado por oxígeno, azufre, y N(X), o un radical que es un anillo aromático bicíclico ortofusionado de 9 o 10 miembros, que tiene uno, dos o tres heteroátomos, cada uno seleccionado del grupo integrado por oxígeno, azufre, y N(X); en donde los átomos de carbono del heteroarilo pueden estar sustituidos con R13; heterociclo es un radical que es un anillo heterocíclico parcialmente saturado o no saturado, de 5, 6 o 7 miembros, con uno, dos o tres heteroátomos seleccionados del grupo integrado por oxígeno, azufre y N(Y), en donde los átomos de carbono del anillo heterocíclico pueden estar sustituidos con R14; X está ausente, o es H o C1-4 alquilo, Y es H, C1-6 alquilo, opcionalmente sustituido con arilo o heteroarilo, C3-6 cicloalquilo, o C2-6 alquilo sustituido con -OH, -O(C1-4 alquilo), -O(C1-4 alquil)-NR11R12, -CO2R5, o NHCHO, o -OH; R13 es halo, -OH, -CN, -CF3, -O C1-6 alquilo, C1-6 alquilo, C3-6 cicloalquilo, -NR5R6, -CONR5R6, -SO2NR5R6, -COOR7, -OCF3, o fenilo, opcionalmente sustituido con halo, OH, O C1-4 alquilo, o C1-6 alquilo; R14 es C1-6 alquilo, C3-6 cicloalquilo, C2-6 alquilo sustituido con -OH, -O (C1-4 alquilo), -O(C1-4 alquil)-NR11R12, o -CO2R5, -OH, u oxo (=O); m es 1, 2, 3 o 4; n es 1, 2, 3 o 4; en el C3-6 cicloalquilo de cada una de las definiciones anteriores, cada uno puede estar sustituido independientemente con -OH, C1-4 alquilo, u oxo (=O), y con las siguientes condiciones: (a) cuando R4 es 4-fluorofenilo, n es 1, m es 1, cada R3 es independientemente hidrogeno, R8 y R9 es independientemente -CH2CH3, entonces R2 no puede ser fluoro o cloro en la posicion C1-6 de la formula (1); (b) cuando n es 1, m es 1, R2, R3, R8 o R9 son hidrogeno, R4 es 4-tiazolilo, entonces dicho 4-tiazolilo no puede estar sustituido con 4-clorofenilo; (c) cuando n es 1, m es 1, R2, R3, R8 o R9 son hidrogeno, entonces R4 no es 4-piridilo; (d) cuando n es 1, m es 1, R2, R3, R8 o R9 son hidrogeno, entonces R4 no es 2-bromofenilo o 4-bromofenilo. Estos compuestos son ligandos de la 5-HT, y son utiles para tratar enfermedades en donde se desee modular la actividad de la 5-HT. Además se describe el uso de los mismos para la manufactura de un medicamento para tratar una enfermedad o condicion tal como ansiedad, depresion, esquizofrenia, una enfermedad relacionada con el estrés, un trastorno por pánico, una fobia, trastorno obsesivo-compulsivo, síndrome de estrés postraumático, depresion del sistema inmunologico, psicosis, parafrenia, manía, trastornos convulsivos, trastornos de la personalidad, cefalea por migrana, drogadiccion, alcoholismo, obesidad, trastornos de la alimentacion, o trastornos del sueno.
ARP000104632A 1999-09-07 2000-09-05 Aminoalcoxicarbazoles y el uso de los mismos para la manufactura de un medicamento para el tratamiento de enfermedades del snc AR032592A1 (es)

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US15263899P 1999-09-07 1999-09-07
US20377100P 2000-05-12 2000-05-12

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AR032592A1 true AR032592A1 (es) 2003-11-19

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ARP000104632A AR032592A1 (es) 1999-09-07 2000-09-05 Aminoalcoxicarbazoles y el uso de los mismos para la manufactura de un medicamento para el tratamiento de enfermedades del snc

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US (1) US6514968B1 (es)
EP (1) EP1210329A2 (es)
JP (1) JP2003508518A (es)
KR (1) KR20020027622A (es)
CN (1) CN1169789C (es)
AR (1) AR032592A1 (es)
AU (1) AU780190B2 (es)
BR (1) BR0013767A (es)
CA (1) CA2380763A1 (es)
CO (1) CO5190697A1 (es)
MX (1) MXPA02002496A (es)
MY (1) MY125942A (es)
NZ (1) NZ517661A (es)
PE (1) PE20010522A1 (es)
WO (1) WO2001017963A2 (es)

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CN109562085A (zh) 2015-06-12 2019-04-02 阿速万科学有限责任公司 用于预防和治疗rem睡眠行为障碍的二芳基和芳基杂芳基脲衍生物
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WO2001017963A3 (en) 2001-11-15
CO5190697A1 (es) 2002-08-29
AU7053200A (en) 2001-04-10
BR0013767A (pt) 2002-06-25
NZ517661A (en) 2004-02-27
MXPA02002496A (es) 2002-07-30
WO2001017963A2 (en) 2001-03-15
CN1169789C (zh) 2004-10-06
JP2003508518A (ja) 2003-03-04
CA2380763A1 (en) 2001-03-15
KR20020027622A (ko) 2002-04-13
EP1210329A2 (en) 2002-06-05
AU780190B2 (en) 2005-03-03
PE20010522A1 (es) 2001-04-28
US6514968B1 (en) 2003-02-04
MY125942A (en) 2006-09-29
CN1372547A (zh) 2002-10-02

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