AR039345A1 - Derivados de acido amino-1h-indol-2-carboxilico 3-sustituidos y de acido amino-benzo(b)-tiofeno-2-carboxilico 3-sustituidos como inhibidores de la expresion del gen de la inteleuquina-4 - Google Patents

Derivados de acido amino-1h-indol-2-carboxilico 3-sustituidos y de acido amino-benzo(b)-tiofeno-2-carboxilico 3-sustituidos como inhibidores de la expresion del gen de la inteleuquina-4

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Publication number
AR039345A1
AR039345A1 ARP030101394A ARP030101394A AR039345A1 AR 039345 A1 AR039345 A1 AR 039345A1 AR P030101394 A ARP030101394 A AR P030101394A AR P030101394 A ARP030101394 A AR P030101394A AR 039345 A1 AR039345 A1 AR 039345A1
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AR
Argentina
Prior art keywords
6alkyl
alkyl
amino
phenyl
group
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ARP030101394A
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English (en)
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Aventis Pharma Inc
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Publication date
Application filed by Aventis Pharma Inc filed Critical Aventis Pharma Inc
Publication of AR039345A1 publication Critical patent/AR039345A1/es

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    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic 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
    • A61P37/08—Antiallergic agents
    • 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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • C07D409/12—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 chain containing hetero atoms as chain links
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    • 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
    • C07D417/12—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 chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Otolaryngology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

Reivindicación 1: Un método de tratamiento de alergia, asma, rinitis, dermatitis, linfomas de células B, tumores, anti-bacterianos, rinovirus o virus respiratorio sincitial (RSV) que comprende administrar a un paciente que se encuentra en necesidad de dicho tratamiento una cantidad terapéuticamente eficaz de un compuesto de la fórmula (1), en la cual: X e Y son iguales o diferentes y se seleccionan independientemente del grupo constituido por H, halógeno, nitro, amino, hidroxi, C1-6 alquilo, C2-6-alquenilo, C2-6-alquinilo, C1-6-alcoxi, C1-6-perfluoro-alquilo, C1-6-perfluoroalcoxi, fenilo y bencilo, en las cuales fenilo o bencilo está sustituido opcionalmente con uno o dos sustituyentes cada uno de los cuales se selecciona independientemente de C1-6-alquilo, C1-6-perfluoroalquilo, halógeno, hidroxi o C1-6-perfluoroalquilo o C1-6-perfluoroalcoxi; Z es N-R o S, donde R se selecciona del grupo constituido por H, C1-6 alquilo, C1-6alquilcarbonilo, C1-6alcoxicarbonil-C1-6alquilo, C1-6alquilcarbamoil-C1-6alquilo y C1-6-dialquilcarbamoil-C1-6alquilo; R1 se selecciona del grupo constituido por H, C1-6alquilo, C2-6alquenilo, C2-6alquinilo, C1-6perfluoroalquilo, C3-8cicloalquilo, C3-8cicloalquil-C1-6alquilo, C1-6alcoxi-C1-6alquilo, hidroxi-C1-6alquilo, amino-C1-6alquilo, mono- o di-C1-6-alquil-amino-C1-6alquilo, formilo, C1-6alquilcarbonilo, amino-C1-6alquilcarbonilo, C1-6alcoxicarbonilo, fenilo, difenil-C1-6alquilo y fenil C1-6alquilo, fenilcarbonil-C1-6alquilo, fenoxi-C1-6alquilo, donde fenilo está sustituido opcionalmente con uno o dos sustituyentes cada uno de los cuales se selecciona independientemente de C1-6alquilo, C1-6perfluoroalquilo, halógeno, hidroxi o C1-6perfluoroalquilo o C1-6perfluoroalcoxi; R3 es como se muestra en el grupo de fórmulas (2) en cuyas fórmulas R4 se selecciona del grupo constituido por H, halógeno, nitro, amino, hidroxi, C1-6alquilo, C1-6alcoxi, C1-6perfluoroalquilo, C1-6perfluoroalcoxi, fenilo y bencilo, donde fenilo o bencilo está sustituido opcionalmente con uno o dos sustituyentes seleccionados cada uno independientemente de C1-6 alquilo, C1-6 perfluoroalquilo, halógeno, hidroxi o C1-6perfluoroalquilo o C1-6perfluoroalcoxi, y n es un número entero de 0 a 4; y R2 se selecciona del grupo constituido por H, C1-6 alquilo, C1-6 perfluoroalquilo, perfluoroarilo, indanilo, C1-6-alcoxiC1-6alquilo, C2-6aciloxi-C1-6alquilo, C1-6alcoxicarbonil-C1-6alquilo, C1-6alquilo, C3-8cicloalquilo, C3-8cicloalcoxicarbonil-oxi-C1-6alquilo, adamantiloxicarboniloxi-C1-6alquilo, C3-8cicloalcoxicarbonil-C1-6alquilo, mono- o di-C1-6alquilamino-C1-6alquilo, C3-8azacicloalquil-C1-6-alquilo, mono- o di-C1-6alquilcarbamoil-C1-6alquilo, C3-8azacicloalquilcarboniloxi-C1-6 alquilo, bencilC1-6-alquilcarbamoil-C1-6alquilo, mono- o di-C1-6alquil-carbamoiloxi-C1-6alquilo, C3-8azacicloalquilcarboniloxi-C1-6alquilo, bencilC1-6-alquilcarbamoiloxi-C1-6alquilo, bencilcarbamoiloxi-C1-6alquilo, C1-6alcoxicarbonil-amino-oxo-C1-6alquilo, o un resto seleccionado del grupo de fórmulas (3), en donde R5 es H o C1-6 alquilo, R6 es C1-6 alquilo, fenilo o tolilo, y A es CH2, NH u O, o una de sus sales farmacéuticamente aceptables, opcionalmente en combinación con un vehículo farmacéuticamente aceptable.
ARP030101394A 2002-04-23 2003-04-23 Derivados de acido amino-1h-indol-2-carboxilico 3-sustituidos y de acido amino-benzo(b)-tiofeno-2-carboxilico 3-sustituidos como inhibidores de la expresion del gen de la inteleuquina-4 AR039345A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US37530402P 2002-04-23 2002-04-23
GBGB0217920.8A GB0217920D0 (en) 2002-04-23 2002-08-02 Interleukin-4 Gene Expression inhibitors

Publications (1)

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AR039345A1 true AR039345A1 (es) 2005-02-16

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Country Status (6)

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US (3) US20040006123A1 (es)
JP (1) JP4746271B2 (es)
KR (2) KR20040104613A (es)
AR (1) AR039345A1 (es)
GB (1) GB0217920D0 (es)
TW (1) TWI296926B (es)

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KR20040106382A (ko) 2004-12-17
KR100972304B1 (ko) 2010-07-26
US20040010029A1 (en) 2004-01-15
US7169925B2 (en) 2007-01-30
GB0217920D0 (en) 2002-09-11
KR20040104613A (ko) 2004-12-10
JP4746271B2 (ja) 2011-08-10
JP2005529134A (ja) 2005-09-29
US20080132481A1 (en) 2008-06-05
TWI296926B (en) 2008-05-21
US20040006123A1 (en) 2004-01-08
TW200408389A (en) 2004-06-01

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