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AR056891A1 - Derivados policiclicos de indazol que son inhibidores de erk - Google Patents

Derivados policiclicos de indazol que son inhibidores de erk

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Publication number
AR056891A1
AR056891A1 ARP060105474A ARP060105474A AR056891A1 AR 056891 A1 AR056891 A1 AR 056891A1 AR P060105474 A ARP060105474 A AR P060105474A AR P060105474 A ARP060105474 A AR P060105474A AR 056891 A1 AR056891 A1 AR 056891A1
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Argentina
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substituted
alkyl
group
independently selected
cycloalkyl
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ARP060105474A
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Schering Corp
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • 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
    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
    • C07D413/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/12—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
    • 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
    • C07D417/14—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 three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Se describen métodos para el tratamiento de cáncer donde se usan los compuestos de formula (1). Reivindicacion 1: Un compuesto de formula [1], o las sales farmacéuticamente aceptables de éste, donde Y1, Y2, e Y3 están cada uno independientemente seleccionado del grupo que consiste en: -CH=, -N= y -CR9=; z es 1 a 3; Q es un sustituyente seleccionado del grupo de formulas [2]; cada Q1 representa un anillo seleccionado independientemente del grupo que consiste en: cicloalquilo, cicloalquilo sustituido, heterocicloalquilo, heterocicloalquilo sustituido, arilo, arilo sustituido, heteroarilo, y heteroarilo sustituido, donde dichos anillos sustituidos están sustituidos con 1 a 3 sustituyentes independientemente seleccionados del grupo que consiste en los restos R10; con la condicion de que cuando Q1 es arilo, heteroarilo, arilo sustituido o heteroarilo sustituido entonces los átomos de carbono en la union del anillo no están sustituidos; Q2 representa un anillo seleccionado del grupo que consiste en cicloalquilo, cicloalquilo sustituido, heterocicloalquilo, y heterocicloalquilo sustituido, donde dichos anillos sustituidos están sustituidos con 1 a 3 sustituyentes independientemente seleccionados del grupo que consiste en restos R10; Z1 representa -(C(R24)2)w- donde cada R24 está independientemente seleccionado del grupo que consiste en: H, alquilo y F, y donde w es 1, 2 o 3; Z2 está seleccionado del grupo que consiste en: -N(R44)-, -O- y -C(R46)2-; m es 1 a 6; n es 1 a 6; p es 0 a 6; t es 0, 1 o 2; R1 está seleccionado del grupo que consiste en (1) -CN, (2) -NO2, (3) -OR10, (4) -SR10, (5) -N(R10)2, (6) R10, (7) -C(O)R10, (8) -(C(R30)2)n-NR32-C(O)-R10, (9) -(C(R30)2)n-NR32-S(O)t-R10, (10) -(C(R30)2)n-NR32-C(O)-N(R32)- R10, (11) un resto de formula [3], (12) -CF3, (13) -C(O)OR10, (14) -(C(R30)2)nR13 (por ejemplo, -(CH2)nR13), (15) alquenilo, (16) -NR32-C(O)-R14, (17) -N(R10)-C(:O)-N(R10)2, donde cada R10 está seleccionado independientemente, (18) -N(R10)-S(O)t- R10, donde cada R10 está seleccionado independientemente, (19) -C(=NH)-N(R32)-R15, (20) -C(O)-NR32-(C(R30)2)p-OR10, (21) -C(O)N(R10)2 donde cada R10 está seleccionado independientemente, (22) -C(O)-NR32-C(R18)3, (23) -C(O)-NR32-(C(R30)2)n-C(O)- N(R10)2, (24) heterocicloalquenilo, (25) un resto formula [4], y (26) arilalquenil-; R2 está seleccionado del grupo que consiste en (1) H, (2) -CN, (3) halo, (4) alquilo, (5) alquilo sustituido donde cada alquilo sustituido está sustituido con 1 a 3 sustituyentes seleccionados del grupo que consiste en: (a) -OH, (b) -O-alquilo (por ejemplo, -O-(alquilo C1-3), (c) -O-alquilo sustituido con 1 a 3 átomos de F, y (d) -N(R40)2 donde cada R40 está independientemente seleccionado del grupo que consiste en: (i) H, (ii) C1-3 alquilo, (iii) -CF3, y (e) halo, (6) alquinilo, (7) alquenilo, (8) -(CH2)mR11, (9) -N(R26)2, (10) -OR23, (11) -N(R26)C(O)R42, (12) cicloalquilo, (13) cicloalquilalquilo, (14) un resto de formula [5], (15) -O-(alquilo sustituido) donde cada alquilo sustituido está sustituido con 1 a 3 átomos de F, (16) -S(O)talquilo, (17) -C(O)-alquilo, (18) -C(=N-O-H)-alquilo, (19) -C(=N-O-alquilo)alquilo, donde cada alquilo está seleccionado independientemente, (20) un resto de formula [6] donde cada alquilo está seleccionado independientemente, (21) un resto de formula [7] donde cada alquilo está seleccionado independientemente, (22) -N(R48)-C(O)-R48 donde cada R48 está independientemente seleccionado del grupo que consiste en H y alquilo, y (23) -C(O)-alquilo, tal como, por ejemplo, -C(O)-(alquilo C1-6), tal como, por ejemplo, -C(O)CH3; donde cada R3, R4, R5, R6 y R7 está independientemente seleccionado del grupo que consiste en (1) H, (2) alquenilo, (3) alquenilo sustituido, (4) alquilo, (5) alquilo sustituido, (6) cicloalquilo, (7) cicloalquilo sustituido, (8) cicloalquilalquil-, (9) cicloalquilalquil- sustituido, (10) heterocicloalquilo, (11) heterocicloalquilo sustituido, (12) heterocicloalquilalquil-, (13) heterocicloalquilalquil- sustituido, (14) -C(O)R10, (15) arilheteroaril-, (16) arilheteroaril- sustituido, (17) heteroarilaril-, (18) heteroarilaril- sustituido, (19) arilo, (20) arilo sustituido, (21) heteroarilo, (22) heteroarilo sustituido, (23) heteroarilheteroaril-, (24) heteroarilheteroaril- sustituido, (25) arilaminoheteroaril-, (26) arilaminoheteroaril- sustituido, (27) arilalquinil-, (28) arilalquinil- sustituido, (29) heteroarilalquinil-, (30) heteroarilalquinil- sustituido, donde dichos grupos R3, R4, R5, R6 y R7 sustituidos (7), (9), (11), (13), (16), (18), (20), (22), (24), (26), (28) y (30) están sustituidos con 1 a 3 sustituyentes seleccionados independientemente del grupo que consiste en: -NH2, alquilo, alquenilo, halo, -C(O)-NH-R28, -C(O)OR28, y -C(O)R28, y donde dichos grupos R3, R4, R5, R6 y R7 sustituidos (3) y (5) están sustituidos con 1 a 3 sustituyentes seleccionados independientemente del grupo que consiste en: - NH2, halo (por ejemplo, F, CI y Br, y en otro ejemplo F), -C(O)NH-R28 (por ejemplo, -C(O)-NH-CH3), -C(O)OR28 (por ejemplo, -C(O)OC2H5), y -C(O)R28 (por ejemplo, -C(O)CH3); R5A está seleccionado del grupo que consiste en: halo, -OH, y -O-alquilo; R8 está seleccionado del grupo que consiste en: H, -OH, -N(R10)2, -NR10C(O)R12, y alquilo; cada R9 está independientemente seleccionado del grupo que consiste en halogeno, -CN, -NO2, -OR10, -SR10, -N(R10)2, y R10, cada R10 está independientemente seleccionado del grupo que consiste en H, alquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, alquilheteroaril-, alquilaril-, alquilo sustituido, arilo sustituido, arilalquilo sustituido, heteroarilo sustituido, heteroarilalquilo sustituido, cicloalquilo sustituido, cicloalquilalquilo sustituido, heterocicloalquilo sustituido, heterocicloalquilalquilo sustituido, alquilheteroaril- sustituido, alquilaril- sustituido, heterocicloalquenilo, y heterocicloalquenilo sustituido, y donde dicho alquilo sustituido R10 está sustituido con 1 a 3 sustituyentes seleccionados independientemente del grupo que consiste en: -NH2, -NHR20, -NO2, -CN, -OR26, halo, -C(O)-NH-R26, -C(O)OR26, y -C(O)R26, y dicho arilo sustituido, arilalquilo sustituido, heteroarilo sustituido, heteroarilalquilo sustituido, cicloalquilo sustituido, cicloalquilalquilo sustituido, heterocicloalquilo sustituido, heterocicloalquilalquilo sustituido, alquilheteroarilsustituido y alquilaril- sustituido R10 están sustituidos con 1 a 3 sustituyentes seleccionados independientemente del grupo que consiste en: (1) -NH2, (2) -NO2, (3) -CN, (4) -OH, (5) -OR20, (6) - OCF3, (7) alquilo sustituido con 1 a 3 átomos de halo seleccionados independientemente, (8) -C(O)R38, (9) alquilo, (10) alquenilo, (11) halo, (12) -C(O)-NH-R26, (13) -C(O)OR38, (14) -C(O)-NR32-(C(R30)2)n-N(R38)2, (15) -S(O)tR38, (16) -C(O)-NR32-R38, (17) -NR32-C(O)-R38, (18) -C(=N)-NR32R38, (19) -NHR20, y (20) cicloalquilo; R11 está seleccionado del grupo que consiste en: F, -OH, -CN, -OR10, -NHNR1R10, -SR10 y heteroarilo; R12 está seleccionado del grupo que consiste en: alquilo, arilo, heteroarilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo y heterocicloalquilalquilo; R14 está seleccionado del grupo que consiste en: alquilo, arilo, heteroarilo, cicloalquilo, cicloalquilalquil-, heterocicloalquilo, alquilheterocicloalquilo, heterocicloalquilalquil-, alquilheteroaril- y alquilaril-; R15 está seleccionado del grupo que consiste en: H, -OH, alquilo, arilo, heteroarilo, cicloalquilo, cicloalquilalquil-, heterocicloalquilo y heterocicloalquilalquil- , alquilheteroaril- y alquilaril-; R20 representa alquilo; R23 está seleccionado del grupo que consiste en H, alquilo, arilo, cicloalquilo, y cicloalquilalquil-; cada R26 está independientemente seleccionado del grupo que consiste en H y alquilo; R28 es alquilo; cada R30 está independientemente seleccionado del grupo que consiste en H, alquilo, y F; cada R32 está independientemente seleccionado del grupo que consiste en H y alquilo, y donde cada R32 es general H; cada R35 está independientemente seleccionado del grupo que consiste en H y alquilo C1-6; R36 está seleccionado del grupo que consiste en: H, alquilo, y -O-alquilo; cada R38 está independientemente seleccionado del grupo que consiste en H, alquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, alquilheteroaril-, alquilaril, alquilo sustituido, arilo sustituido, arilalquilo sustituido, heteroarilo sustituido, heteroarilalquilo sustituido, cicloalquilo sustituido, cicloalquilalquilo sustituido, heterocicloalquilo sustituido, heterocicloalquilalquilo sustituido, alquilheteroaril- sustituido y alquilaril- sustituido, y donde dicho alquilo sustituido R38 está sustituido con 1 a 3 sustituyentes seleccionados independientemente del grupo que consiste en: -NH2, -NO2, -CN, -OR26, halo, -C(O)-NH-R28, -C(O)OR28, y -C(O)R28, y dichos arilo sustituido, arilalquilo sustituido, heteroarilo sustituido, heteroarilalquilo sustituido, cicloalquilo sustituido, cicloalquilalquilo sustituido, heterocicloalquilo sustituido, heterocicloalquilalquilo sustituido, alquilheteroarilsustituido y alquilaril- sustituido R38 están sustituidos con 1 a 3 sustituyentes seleccionados independientemente del grupo que consiste en: (1) -NH2, (2) -NO2, (3) -CN, (4) -OH, (5) -OR20, (6) -OCF3, (7) -CF3, (8) -C(O)R26, (9) alquilo, (10) alquenilo, (11) halo, (12) -C(O)-NH-R26, (13) -C(O)OR26, (14) -C(O)-NR32- (C(R30)2)n-N(R26)2, (15) -S(O)R26, (16) -C(O)N(R32)(R26), (17) -NR32C(O)R26, (18) -C(=N)-NR32R26, (19) -NHR20; R42 está seleccionado del grupo que consiste en: alquilo, arilo, heteroarilo, y cicloalquilo; R44 está seleccionado del grupo que consiste en: H, alquilo, cicloalquilo, y cicloalquilalquilo; y cada uno de R46 está independientemente seleccionado del grupo que consiste en: H, alquilo, cicloalquilo, y cicloalquilalquilo.
ARP060105474A 2005-12-13 2006-12-12 Derivados policiclicos de indazol que son inhibidores de erk AR056891A1 (es)

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