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AR047160A1 - Compuestos moduladores de cb1 - Google Patents

Compuestos moduladores de cb1

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Publication number
AR047160A1
AR047160A1 ARP040104819A ARP040104819A AR047160A1 AR 047160 A1 AR047160 A1 AR 047160A1 AR P040104819 A ARP040104819 A AR P040104819A AR P040104819 A ARP040104819 A AR P040104819A AR 047160 A1 AR047160 A1 AR 047160A1
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AR
Argentina
Prior art keywords
alkyl
hydrogen
group
compounds
formulas
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Application number
ARP040104819A
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English (en)
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Lilly Co Eli
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Publication of AR047160A1 publication Critical patent/AR047160A1/es

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    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
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    • 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
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    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
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    • 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
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
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    • 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
    • C07D209/40—Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
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    • 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
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    • C07D209/56—Ring systems containing three or more rings
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    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
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    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
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    • 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
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    • 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
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    • C07D405/02—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 two hetero rings
    • C07D405/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D405/02—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 two hetero rings
    • C07D405/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
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    • 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
    • C07D409/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
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    • 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
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems

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  • Diabetes (AREA)
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  • Obesity (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Indole Compounds (AREA)

Abstract

Se describen compuestos como moduladores del receptor de cannabinoides-1 (CB1), estos compuestos son utiles en el tratamiento, prevencion y supresion de enfermedades mediadas por el receptor CB1. Como tales, los compuestos del presente son utiles para el tratamiento, prevencion y supresion de psicosis, pérdidas de memoria, trastornos cognitivos, migrana, neuropatía, trastornos neuroinflamatorios (por ejemplo, esclerosis multiple, síndrome de Guillain-Barre y las secuelas inflamatorias de la encefalitis viral), accidentes cerebrovasculares, y traumatismo craneal, trastornos de ansiedad, estrés, epilepsias, enfermedad de Parkinson, y esquizofrenia. Los compuestos también son utiles para el tratamiento de trastornos de abuso de sustancias, particularmente de opiáceos, alcohol, y nicotina. Los compuestos también son utiles para el tratamiento de la obesidad o trastornos alimenticios asociados con una ingesta excesiva de alimentos y las complicaciones asociadas que conllevan. Reivindicacion 1: Un compuesto de formula (1), en la que el resto de formula (2) es un anillo 6,5-bicíclico seleccionado de entre el grupo de formulas (3); R1 se selecciona entre el grupo compuesto por: a) hidrogeno; b) alquilcarbonilo opcionalmente sustituido con heterociclilo; c) heterociclilcarbonilo opcionalmente sustituido con alquilo o acetilo; d) alquilo o haloalquilo; e) cicloalquilo opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre el grupo compuesto por alquilo, halo, oxo, hidroxi, alcoxi, amino, alquilamino y dialquilamino; f) heterociclilo seleccionado entre los compuestos del grupo de formulas (4); g) arilo opcionalmente sustituido con halo, alquilo, alcoxi ciano, amino, alquilamino o dialquilamino; y h) heteroarilo seleccionado entre los compuestos del grupo de formulas (5); R2 es hidrogeno, alquilo, heterociclilo o, junto con R1 y el carbono a los que están unidos, forma un sustituyente de anillo saturado seleccionado entre el grupo compuesto por: a) cicloalquilo; y b) heterociclilo seleccionado entre el grupo compuesto por tetrahidrofuranilo, tetrahidropiranilo y piperidinilo opcionalmente N-sustituido con alquilo, acetilo o arilo, X es -NR13R3 o un compuesto de formula (6); R3 se selecciona entre el grupo compuesto por: a) hidrogeno; b) alquilo opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre el grupo compuesto por hidroxi, alcoxi, halogeno, amino, alquilamino y dialquilamino; c) cicloalquilo opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre el grupo compuesto por hidroxi, alcoxi, halo, amino, alquilamino y dialquilamino; d) heterociclilo seleccionado entre los compuestos del grupo de formulas (7); e) cicloalquilalquilo seleccionado entre los compuestos del grupo de formulas (8); f) heterociclilalquilo seleccionado entre los compuestos del grupo de formulas (9); g) arilalquilo seleccionado entre los compuestos del grupo de formulas (10); h) heteroarilalquilo seleccionado entre los compuestos del grupo de formulas (11); y el compuesto de formula (6) es un anillo heterocíclico seleccionado entre los compuestos del grupo de formulas (12); R4 es hidrogeno, fenilo, halofenilo, acilo o alcoxicarbonilo; R5 es hidrogeno, hidroxi o alcoxi; cada uno de R6 y R7 se selecciona independientemente entre hidrogeno, halo, ciano, alquilo, alcoxi, haloalquilo, haloalcoxi, amino, alquilamino, dialquilamino, alcoxicarbonilo, dialquilaminocarbonilo, arilo y ariloxi; R8 es hidrogeno, hidroxialquilo, acilo, oxo, arilo, piridinilo, alquil-SO2-O-, Rb-NH-CH2-, arilalquilo o Rc2N-CO-O-; R9 es hidrogeno, hidroxi, hidroxialquilo, acilo, halo, dihalo, oxo, arilo, haloaril-CH2-, piridinilo, alquil-SO2-O-, Ra-NH-, Rb-NH-CH2, arilalquilo, el compuesto de formula (13) o Rc2N-CO-O-; R10 es hidrogeno, alquilo, alcoxicarbonilo, arilo o haloarilo; R11 es hidrogeno, alquilo o arilo; R12 es hidrogeno o arilo; R13 es hidrogeno o alquilo; R14 es hidrogeno, alquilo, arilo o acilo; Ra es hidrogeno, alcoxicarbonilo o halofenilo; Rb es hidrogeno, alcoxi, fenilo, halofenilo, halofenilalquilo, halopiridinilo, pirimidinilo, alcoxicarbonilo, dialquilaminocarbonilo o dialquilaminotiocarbonilo; y Rc es hidrogeno o alquilo; y todas las sales, solvatos, isomeros opticos y geométricos y formas cristalinas de los mismos con la condicion de que el compuesto de formula (1) es diferente de [4- (2,3-dihidro-indol-1-sulfonil)-fenil]-(4-fenil-piperazin-1-il)-metanona, [4-(2,3-dihidro-indol-1-sulfonil)-fenil]-morfolin-4-il-metanona y [4-(2,3-dihidro-indol-1-sulfonil)-fenil]-piperidin-1-il-metanona.
ARP040104819A 2003-12-23 2004-12-21 Compuestos moduladores de cb1 AR047160A1 (es)

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AR047160A1 true AR047160A1 (es) 2006-01-11

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US (2) US7276516B2 (es)
EP (1) EP1699761B1 (es)
JP (1) JP2007519631A (es)
AR (1) AR047160A1 (es)
AT (1) ATE502009T1 (es)
AU (1) AU2004312311A1 (es)
BR (1) BRPI0418079A (es)
CA (1) CA2549396A1 (es)
DE (1) DE602004031875D1 (es)
ES (1) ES2360112T3 (es)
IL (1) IL176069A0 (es)
NO (1) NO20063381L (es)
PE (1) PE20050598A1 (es)
SV (1) SV2005001984A (es)
TW (1) TW200522944A (es)
WO (1) WO2005066126A1 (es)
ZA (1) ZA200605159B (es)

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SE521512C2 (sv) 2001-06-25 2003-11-11 Niconovum Ab Anordning för administrering av en substans till främre delen av en individs munhåla
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