AR058403A1 - PIRIMIDINILOXI Y PIRIDINILOXI UREAS SUSTITUíDAS COMO INHIBIDORES DE PROTEíNA QUINASAS, COMPOSICIONES FARMACÉUTICAS QUE LAS CONTIENEN Y SU USO EN LA PREPARACIoN DE UN MEDICAMENTO PARA EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR LA ACTIVIDAD BASAL DE B-RAF. - Google Patents

PIRIMIDINILOXI Y PIRIDINILOXI UREAS SUSTITUíDAS COMO INHIBIDORES DE PROTEíNA QUINASAS, COMPOSICIONES FARMACÉUTICAS QUE LAS CONTIENEN Y SU USO EN LA PREPARACIoN DE UN MEDICAMENTO PARA EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR LA ACTIVIDAD BASAL DE B-RAF.

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Publication number
AR058403A1
AR058403A1 ARP060105791A ARP060105791A AR058403A1 AR 058403 A1 AR058403 A1 AR 058403A1 AR P060105791 A ARP060105791 A AR P060105791A AR P060105791 A ARP060105791 A AR P060105791A AR 058403 A1 AR058403 A1 AR 058403A1
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AR
Argentina
Prior art keywords
group
cycloalkyl
arylalkyl
heterocycloalkyl
optionally substituted
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ARP060105791A
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English (en)
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Kalypsys Inc
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Publication of AR058403A1 publication Critical patent/AR058403A1/es

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    • 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
    • C07D403/04—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
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P37/02—Immunomodulators
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • 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
    • C07D401/04—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
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/04—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Compuestos como inhibidores de proteína quinasas incluyendo B-Raf y diverso receptor de tirosina y tirosina citoplasmática quinasa. Derivados de pirimidiniloxi y piridiniloxi urea sustituida de formulas (1), (2) y (3), y composiciones y sus aplicaciones como fármacos para el tratamiento de enfermedades. Su uso en la preparacion de medicamentos para la modulacion de la actividad de proteína quinasas en un sujeto humano o animal para el tratamiento de enfermedades como el cáncer. Reivindicacion (1): Un compuesto caracterizado porque tiene una formula estructural (4), o una sal, éster o prodroga de lo mismo, en lo cual X1-X4 son seleccionados cada uno independientemente de un grupo formado por C(R2) y N; X5 es seleccionado de un grupo formado por C(R3)(R4), N(R3), O y S(O)m; m es 0, 1 o 2; A y C son seleccionados cada uno en forma independiente de un grupo formado por arilo y heteroarilo, cada uno de los cuales puede ser opcionalmente sustituido; B es seleccionado del grupo formado por -N(R8)C(O)N(R8)- y -N(R8)C(O)N(R8)CH2-; R1 es seleccionado de un grupo formado por heteroarilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido y un resto de formula (5); I, J, K, L y M son seleccionados cada uno en forma independiente de un grupo formado por C(R5)(R6), S(O)n, O y N(R7); n es 0, 1 o 2; R2 es seleccionado de un grupo formado por alquenilo, alcoxi, alcoxialquilo, alquilo, alquinilo, amido, amino, aminoalquilo, ciano, cianoalquenilo, éster, éter, halo, haloalquilo, haloalcoxi, hidrogeno, hidroxido, hidroxialquilo y nitro, cada uno de los cuales puede ser opcionalmente sustituido; R3 y R4 son seleccionados cada uno independientemente del grupo formado por hidrogeno y alquilo inferior; R5 y R6 son seleccionados en forma independiente del grupo formado por alquenilo, alcoxi, alcoxialquilo, alquilo, alquinilo, amido, amidoalquilo, amino, aminoalquilo, aminoalquilamino, arilo, arilalquenilo, arilalquilo, arilalquinilo, ciano, cianoalquilo, cianoalquenilo, cicloalquilo, éster, ésteralquilo, halo, haloalquilo, haloalcoxi, heteroarilo, heteroarilalquenilo, heteroarilalquilo, heterocicloalquenilo, heterocicloalquilo, heterocicloalquilalquilo, heterocicloalquilalcoxi, heterocicloalquilalquiltio, hidrogeno, hidroxi, hidroxialquilo, nitro y nulo cualquiera de los cuales puede ser opcionalmente sustituido; R7 es seleccionado de un grupo formado por alquenilo, alcoxialquilo, alcoxicarbonilo, alquilo, alquilamino, alquileno, alquinilo, amidoalquilo, arilo, arilalcoxi, arilalquilo, arilalquenilo, arilalquinilo, arilcarbonilo, arilsulfonilo, cianoalquenilo, cianoalquilo, cicloalquilo, éster, ésteralquilo, haloalquilo, haloalcoxi, haloalquilcarbonilo, heteroarilo, heteroarilalquenilo, heteroarilalquilo, heleroarilsulfonilo, heterocicloalquenilo, heterocicloalquilo, heterocicloalquilalquilo, heterocicloalquilalcoxi, heterocicloalquilalquiltio, hidrogeno, hidroxialquilo y nulo, cualquiera de los cuales puede ser opcionalmente sustituido; y R8 es seleccionado de un grupo formado por alquilo inferior, cicloalquilo y heterocicloalquilo, cualquiera de los cuales puede ser opcionalmente sustituido; y con las siguientes condiciones: cuando X1 es nitrogeno, X2-X4 son C(R2), X5 es O o S y B es -NHC(O)NH-; A no puede ser fenil a menos que C sea fenil sustituido con -Oj(CH2)kX6, en el cual X6 es heterocicloalquilo; y donde B es -NHC(O)NH- y X5 es O entonces A no puede ser naftaleno.
ARP060105791A 2005-12-23 2006-12-26 PIRIMIDINILOXI Y PIRIDINILOXI UREAS SUSTITUíDAS COMO INHIBIDORES DE PROTEíNA QUINASAS, COMPOSICIONES FARMACÉUTICAS QUE LAS CONTIENEN Y SU USO EN LA PREPARACIoN DE UN MEDICAMENTO PARA EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR LA ACTIVIDAD BASAL DE B-RAF. AR058403A1 (es)

Applications Claiming Priority (2)

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US75399905P 2005-12-23 2005-12-23
US85173406P 2006-10-13 2006-10-13

Publications (1)

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AR058403A1 true AR058403A1 (es) 2008-01-30

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US (1) US20070155764A1 (es)
AR (1) AR058403A1 (es)
TW (1) TW200804349A (es)
WO (1) WO2007076473A2 (es)

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