AR035721A1 - Indolinonas 4-aril sustituidas; sus composiciones farmaceuticas y metodo para modular la actividad catalitica de una proteina quinasa - Google Patents

Indolinonas 4-aril sustituidas; sus composiciones farmaceuticas y metodo para modular la actividad catalitica de una proteina quinasa

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Publication number
AR035721A1
AR035721A1 ARP010105973A ARP010105973A AR035721A1 AR 035721 A1 AR035721 A1 AR 035721A1 AR P010105973 A ARP010105973 A AR P010105973A AR P010105973 A ARP010105973 A AR P010105973A AR 035721 A1 AR035721 A1 AR 035721A1
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Argentina
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aryl
heterocycle
lower alkyl
group
cycloalkyl
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ARP010105973A
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English (en)
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Sugen Inc
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
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    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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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    • 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
    • C07D209/32—Oxygen atoms
    • C07D209/34—Oxygen atoms in position 2
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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

Abstract

4-Arilindolinonas, capaces de modular la senal de transducción de proteína quinasas a fin de regular, modular y/o inhibir la proliferación celular anormal, de fórmula (1) donde: R1 es un sustituyente arilo o heteroarilo, opcionalmente sustituido por uno o más sustituyentes seleccionados entre el grupo que consiste en halógeno, -OR6, -COR6, -COOR6, -OCOR6, -CONR6R7, -R6NCOR7, -NR6R7, -CN, -NO2, -CX3, -SR6, -SOR6, -SO2R6, -SO2OR6, -SO2NR6R7, -R6NSO2R7, perfluoroalquilo, alquilo inferior, alquilo inferior sustituido adicionalmente por uno o más de R2, alquenilo inferior, alquenilo inferior sustituido adicionalmente por uno o más de R2, alquinilo inferior, alquinilo inferior sustituido adicionalmente por uno o más de R2, cicloalquilo, cicloalquilo sustituido adicionalmente por uno o más de R2, anillo heterociclilo, anillo heterociclilo sustituido adicionalmente por uno o más de R2, arilo, arilo heterociclilo sustituido adicionalmente por uno o más de R2; R2 se selecciona entre el grupo que consiste en hidrógeno, halógeno, OR6, -COR6, -COOR6, OCOR6, -CONR6R7, -R6NCOR7, -NR6R7, -CN, -NO2, -CX3, -SR6, -SOR6, -SO2R6, -SO2OR6, -SO2NR6R7, -R6NSO2R7, perfluoroalquilo, alquilo inferior, alquenilo inferior, alquinilo inferior, cicloalquilo, heterociclo y arilo; R3 se selecciona entre el grupo que consiste en hidrógeno, halógeno, OR6, -COR6, -COOR6, -OCOR6, -CONR6R7, -R6NCOR7, -NR6R7, -CN, NO2, -CX3, -SR6, -SOR6, SO2R6, -SO2OR6, -SO2NR6R7, R6NSO2R7, perfluoroalquilo, alquilo inferior, alquenilo inferior, alquinilo inferior, cicloalquilo, anillo heterociclo, un anillo heterociclo adicionalmente sustituido por uno o más de R2, y arilo; donde dicho alquilo inferior es adicionalmente sustituido por -CONR6R7, NR6R7, -SO2R6, R6NSO2R7 o -SO2NR6R7; R4 se selecciona entre el grupo que consiste en hidrógeno, halógeno, -OR6, -COR6, -COOR6, -OCOR6, -CONR6R7, -R6NCOR7, -NR6R7, -CN, -NO2, -CX3, -SR6, -SOR6, -SO2R6, -SO2OR6, -SO2NR6R7, -R6NSO2R7, perfluoroalquilo, alquilo inferior, alquenilo inferior, alquinilo inferior, cicloalquilo, heterociclo y arilo, donde dicho alquilo inferior es adicionalmente sustituido por -CONR6R7, NR6R7, -SO2R6, R6NSO2R7 o -SO2NR6R7; R5 se selecciona entre el grupo que consiste en hidrógeno, halógeno, -OR6, -COR6, -COOR6, OCOR6, -CONR6R7, -R6NCOR7, -NR6R7, -CN, -NO2, -CX3, -SR6, -SOR6, -SO2R6, -SO2OR6, -SO2NR6R7, -R6NSO2R7, perfluoroalquilo, alquilo inferior, alquenilo inferior, alquinilo inferior, cicloalquilo, heterociclo y arilo, con la salvedad de que uno o más de uno entre R3, R4 y R5 sea hidrógeno, R3 y R4 ó R4 y R5 pueden estar ligados para formar un anillo de 4-, 5-, 6- ó 7- miembros que opcionalmente contiene uno o más heteroátomos seleccionados del grupo que consiste en O, N, S, SO y SO2, que puede contener uno o dos enlaces dobles y puede estar adicionalmente sustituido por uno o más entre -(CH2)n-NR6R7, -(CH2)n-CR6R7, -(CH2)n-C(O)-(CH2)n-NR6R7, -(CH2)n-NSO2R6R7 ó -(CH2)n-C(O)-R6 donde n es 0-4; R6 y R7 se seleccionan independientemente entre el grupo que consiste en hidrógeno, halógeno, -OR2, -CX3, perfluoroalquilo, alquilo inferior, alquenilo inferior, alquinilo inferior, cicloalquilo, heterociclo y arilo; donde alquilo inferior, alquenilo inferior, alquinilo inferior, cicloalquilo, heterociclo y arilo pueden ser adicionalmente sustituidos por uno o más entre (i) NR12R13, (ii) hidroxilo, (iii) halo, (iv) un anillo heterociclo, (v) alquilo inferior, (vi) -C(O)-NR12R13, (vii) -OR12, (viii) -SO2R12R13, o (ix) -COR6, donde dicho anillo heterociclo (iv) puede ser adicionalmente sustituido por uno o más entre alquilo inferior, -COR12, -NR12COR13, halógeno, -OR12, CX3, -C(O)NR12R13, SO2R12R13, ó -SO2NR12R13, o R6 y R7 pueden estar unidos para formar un anillo de 4-, 5- o 6- miembros opcionalmente conteniendo un heteroátomo seleccionado entre el grupo que consiste en N, O, S y SO2 que pueden ser adicionalmente sustituidos por -CONR12R13, alquilo inferior, hidroxi, -(CH2)n-NR12R13-(CH2)n-heterociclo, -(CH2)n-C(O)-NR12R13, -(CH2)nSO2R12R13, o -(CH2)nNSO2R12R13, donde dicho heterociclo puede ser adicionalmente sustituido por halo, alquilo inferior, -COR12, hidroxi, -C(O)-N-R12R13, -OR12, -SO2R12R13, o -SO2NR12R13, X es flúor, cloro, bromo o yodo; R12 se selecciona entre el grupo que consiste en hidrógeno, -CX3, perfluoroalquilo, alquilo inferior, alquenilo inferior, alquinilo inferior, -(CH2)n-cicloalquilo, -(CH2)n-heterociclo y arilo; R13 se selecciona entre el grupo que consiste en hidrógeno, -CX3, perfluoroalquilo, alquilo inferior, alquenilo inferior, alquinilo inferior, -(CH2)n-cicloalquilo, -(CH2)n-heterociclo y arilo; R12 y R13 pueden estar unidos para formar un anillo de 4-, 5- o 6- miembros que opcionalmente contiene uno o más heteroátomos seleccionados del grupo que consiste en O, N, S, SO y SO2 que puede contener uno o dos enlaces dobles; o una sal del mismo aceptable para uso farmacéutico. Las 4-aril indolinonas exhiben modulación de la actividad catalítica de PKs y tienen un efecto saludable contra desórdenes relacionados con la actividad anormal de PK. Esta familia de compuestos modulan la actividad catalítica de tirosina quinasa de receptor (RTKs), tirosina quinasas celulares (no receptor) (CTKs) y serina -treonina proteína quinasas (STKs). También se describen métodos para modular la actividad catalítica de proteína quinasas y para el tratamiento de afecciones relacionadas con proteína quinasa, como así también las composiciones farmacéuticas que comprende 4-aril indolinonas.
ARP010105973A 2000-12-20 2001-12-20 Indolinonas 4-aril sustituidas; sus composiciones farmaceuticas y metodo para modular la actividad catalitica de una proteina quinasa AR035721A1 (es)

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US (2) US6677368B2 (es)
EP (1) EP1349852A2 (es)
JP (1) JP2004518669A (es)
AR (1) AR035721A1 (es)
CA (1) CA2432114A1 (es)
PE (1) PE20020776A1 (es)
WO (1) WO2002055517A2 (es)

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US6677368B2 (en) 2004-01-13
PE20020776A1 (es) 2002-08-22
WO2002055517A3 (en) 2002-09-26
CA2432114A1 (en) 2002-07-18
WO2002055517A2 (en) 2002-07-18
US20040157909A1 (en) 2004-08-12

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