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AR055212A1 - Compuestos heterociclicos como bloqueantes del canal ionico p2x7 - Google Patents

Compuestos heterociclicos como bloqueantes del canal ionico p2x7

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Publication number
AR055212A1
AR055212A1 ARP040102578A ARP040102578A AR055212A1 AR 055212 A1 AR055212 A1 AR 055212A1 AR P040102578 A ARP040102578 A AR P040102578A AR P040102578 A ARP040102578 A AR P040102578A AR 055212 A1 AR055212 A1 AR 055212A1
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Argentina
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integer
alkyl
aryl
alkoxy
hydrogen
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ARP040102578A
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Aventis Pharma Inc
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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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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D233/22—Radicals substituted by oxygen atoms
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    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D233/24—Radicals substituted by nitrogen atoms not forming part of a nitro radical
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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 ring carbon atoms
    • C07D233/30—Oxygen or sulfur atoms
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    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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 ring carbon atoms
    • C07D233/44—Nitrogen atoms not forming part of a nitro radical
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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 ring carbon atoms
    • C07D233/44—Nitrogen atoms not forming part of a nitro radical
    • C07D233/48—Nitrogen atoms not forming part of a nitro radical with acyclic hydrocarbon or substituted acyclic hydrocarbon radicals, attached to said nitrogen atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
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    • 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
    • C07D401/06—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 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
    • C07D405/06—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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    • 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
    • C07D405/02—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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    • 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
    • C07D409/10—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 aromatic rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
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  • Medicinal Chemistry (AREA)
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  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
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  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Métodos para preparar estos compuestos. Dichos compuestos son bloqueadores del canal ionico P2X7 y por lo tanto son utiles como agentes farmacéuticos, especialmente en el tratamiento y/o prevencion de una variedad de enfermedades que tienen un componente inflamatorio, incluyendo la enfermedad intestinal inflamatoria, artritis reumatoidea, y afecciones asociadas con el sistema nervioso central, tales como apoplejía, enfermedad de Alzheimer, etc. Reivindicacion 1: Un compuesto que incluye enantiomeros, estereoisomeros, rotomeros y tautomeros de dicho compuesto y sus sales, solvatos o derivados aceptables desde el punto de vista farmacéutico, caracterizado porque dicho compuesto tiene la estructura general que se muestra en la formula (1), en la cual: R is hidrogeno, alquilo C1-6, acilo C2-6, alcoxicarbonilo C1-6, o ariloxicarbonilo C6-12; Rl y R3 son iguales o diferentes y cada uno de se selecciona independientemente de: cicloalquilo C5-8, heterociclo, seleccionado de morfolinilo, piperidinilo, piperazinilo, pirrolidinilo, tetrahidrofuranilo, tetrahidropiranilo, tetrahidrotiofenilo o tiazolinilo, arilo, seleccionado de fenilo, bifenilo o naftilo, heteroarilo, seleccionado de benzoimidazolilo, benzofuranilo, benzoxazolilo, furanilo, imidazolilo, indolilo, isoxazolilo, isoquinolilo, isotiazolilo, oxadiazolilo, oxazolilo, pirazinilo, pirazolilo, piridilo, pirimidilo, pirrolilo, quinolilo, tetrazolilo, tiazidazolilo, tiazolilo, tienilo o triazolilo, arilalquilo C1-4, cicloalquilC5-8-alquiloC1-4, heteroarilalquilo Cl-4, donde arilo y heteroarilo son como se definieron anteriormente, y donde cicloalquilo C5-8, arilo o heteroarilo está opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo integrado por halogeno, alquilo C1-4, fluoroalquilo o fluoroalcoxi formula CnHxFy o OCnHxFy, donde n es un entero de 1 a 4, x es un entero de 0 a 8, y es un entero de 1 a 9 y suma de x e y es 2n + 1, , alcoxi C1-4, tioalquilo C1-4, hidroxi, aciloxi C1-4, nitro, amino, alquilamino C1-4, dialquilamino C1-4, aminoalquilo Cl-4, alquilaminoCl-4-alquiloCl-4, dialquilaminoCl-4-alquiloCl-4, -CN, -CO2H, -CO2-alquiloCl-4, fenilo, fenoxi y benciloxi; o R1 y R3 tomados juntos con los átomos de carbono a los cuales están unidos forman un ciclopentano, ciclohexano, cicloheptano o ciclooctano; R2 y R4 son iguales o diferentes y cada uno se selecciona independientemente de: hidrogeno, alquilo C1-6 o fluoroalquilo de formula CnHXFy, donde n es un entero de 1 a 4, x es un entero de 0 a 8, y es un entero de 1 a 9 y la suma de x e y es 2n + l; R5 es hidrogeno, cicloalquilo C3-8, alquinilo C2-4, heterociclo, seleccionado de morfolinilo, piperidinilo, piperazinilo, pirrolidinilo, piridinonilo, tetrahidrofuranilo, tetrahidropiranilo, dioxanilo, benzopiranilo, dihidrobenzodioxanilo, tetrahidrotiofenilo o tiazolinilo, arilo, seleccionado de fenilo, bifenilo, naftilo o antracenilo, heteroarilo, seleccionado de benzoimidazolilo, benzofuranilo, benzoxazolilo, furanilo, imidazolilo, indolilo, isoxazolilo, isoquinolilo, isotiazolilo, oxadiazolilo, oxazolilo, pirazinilo, pirazolilo, piridilo, pirimidilo, pirrolilo, quinolilo, tetrazolilo, tiazidazolilo, tiazolilo, tienilo o triazolilo, donde cicloalquilo C5-8, heterociclilo, arilo o heteroarilo está opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo integrado por halogeno, alquilo C1-4, fluoroalquilo fluoroalcoxi de formula CnHXFy o OCnHXFy, donde n es un entero de 1 a 4, x es un entero de 0 a 8, y es un entero de 1 a 9 y la suma de x e y es 2n + 1, alcoxi C1-4, tioalquilo C1-4, hidroxi, aciloxi C1-4, nitro, amino, alquilamino C1-4, dialquilamino Cl-4, aminoalquilo C1-4, alquilaminoC1-4-alquiloC1-4, dialquilaminoC1-4-alquiloC1-4, -CN,-CO2H, y-CO2alquiloC1-4, fenilo, fenoxi y benciloxi; X-Y es -(CH2)-Z-(CH2)b-, -(CH2)a-Z-(CH2)b-Z1- o -NHCO-, donde (CH2) está opcionalmente sustituido con uno o más grupos seleccionados independientemente de: hidroxi, alcoxi C1-6, arilaminocarboniloxi, cicloalquilo C3-8, alquilo C1-4 o fluoroalquilo de formula CnHxFy, donde n es un entero de 1 a 4, x, es un entero de 0 a 8, y es un entero de 1 a9 y la suma de x e y es 2n + 1, donde dicho alcoxi o alquilo o fluoroalquilo está opcionalmente sustituido con al menos un sustituyente seleccionado del grupo integrado por hidroxi, -SH, alcoxi C1-4, tioalquilo C1-4, aciloxi C1-4, nitro, amino, alquilamino C1-4, dialquilamino C1-4, -CN, -CO2H, y -CO2-alquiloC1-4, arilo; Z y Z1 son iguales o diferentes y cada uno se selecciona independientemente de: O, S, NR6, NR6-NR6, -OCONH-, -NH-CO-NH, -SO2-NH-, -(NR6)SO2-, o un enlace; donde R6 se selecciona de: hidrogeno, alcoxi C1-6, alquilo C1-6, o fluoroalquilo de formula CnHxFy, donde n es un entero de 1 a 4, x es un entero de 0 a 8, y es un entero de 1 a 9 y la suma de x e y es 2n + 1, donde dicho alcoxi o alquilo o fluoroalquilo está opcionalmente sustituido con al menos un sustituyente seleccionado del grupo integrado por: hidroxi, -SH, alcoxi c1-4, tioalquilo C1-4, aciloxi c1-4, nitro, amino, alquilamino C1-4, dialquilamino C1-4, -CN, -CO2H, y -CO2-alquiloC1-4, arilo; a es un entero de 0 a 2 y b es un entero de 0 a 4 siempre que la suma de a y b sea al menos 1; y con la salvedad de que: cuando X-y sea -(CH2)aZ-(CH2)b-, cuando Z sea S, R, R2, y R4 sean hidrogeno, R1 y R3 sean fenilo o p-Cl-fenilo, a sea 0 y b sea 1, R5 no sea hidrogeno o fenilo; y cuando X-Y sea -(CH2)a-Z-(CH2)b-, cuando Z sea un enlace, R, R2, y R4 sean hidrogeno, R1 y R3 sean fenilo, a sea 0 y b sea 1, R5 no sea hidrogeno.
ARP040102578A 2003-07-21 2004-07-21 Compuestos heterociclicos como bloqueantes del canal ionico p2x7 AR055212A1 (es)

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EP (1) EP1651613B1 (es)
JP (1) JP2006528178A (es)
KR (1) KR20060041255A (es)
CN (1) CN1826325A (es)
AR (1) AR055212A1 (es)
AT (1) ATE469130T1 (es)
AU (1) AU2004263491A1 (es)
BR (1) BRPI0412897A (es)
CA (1) CA2532910A1 (es)
DE (1) DE602004027382D1 (es)
GB (1) GB0324498D0 (es)
IL (1) IL173146A0 (es)
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WO (1) WO2005014555A1 (es)

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