AR035626A1 - Compuestos de indol inhibidores de tirosina quinasa, composicion farmaceutica, procedimiento para prepararla,y, uso de los compuestos en la preparación de medicamentos - Google Patents

Compuestos de indol inhibidores de tirosina quinasa, composicion farmaceutica, procedimiento para prepararla,y, uso de los compuestos en la preparación de medicamentos

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Publication number
AR035626A1
AR035626A1 ARP000105472A ARP000105472A AR035626A1 AR 035626 A1 AR035626 A1 AR 035626A1 AR P000105472 A ARP000105472 A AR P000105472A AR P000105472 A ARP000105472 A AR P000105472A AR 035626 A1 AR035626 A1 AR 035626A1
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Argentina
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alkyl
aob
aryl
cycloalkyl
heterocyclyl
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ARP000105472A
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English (en)
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Merck & Co Inc
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Publication of AR035626A1 publication Critical patent/AR035626A1/es

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    • 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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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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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    • C07D—HETEROCYCLIC COMPOUNDS
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    • 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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    • 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
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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
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  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
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Abstract

Se refieren compuestos de indol de fórmula (1) que inhiben, regulan y/o modulan la transducción de senales de tirosina quinasa, las composiciones que contienen estos compuestos, y los métodos de uso de los mismos para tratar enfermedades y condiciones que dependen de tirosina quinasa, tales como angiogénesis, cáncer, desarrollo de tumores, arteriosclerosis, degeneración macular relacionada con la edad, retinopatía diabética, enfermedades inflamatorias, y similares en mamíferos. Reivindicación 1: Un compuesto de indol caracterizado porque es de fórmula (1) o una sal farmacéuticamente aceptable o un estereoisómero del mismo, donde Z es fórmulas (2) o (3) o (4); W1 es S, O o N-R; V1 es N o C; W2 es N o C; V2 es S, O o N-R; a es 0 o 1; b es 0 o 1; m es 0, 1 o 2; s es 1 o 2; t es 1, 2 o 3; X=Y es C=N, N=C, o C=C; R es H o alquilo C1-6; R1 y R5 están independientemente seleccionados de: H, (C=O)aOb alquilo C1-10, (C=O)aOb arilo, (C=O)aOb alquenilo C2-10, (C=O)aOb alquinilo C2-10, CO2H, halo, OH, Ob perfluoroalquilo C1-6, (C=O)a NR7R8, CN, (C=O)aOb cicloalquilo C3-8, y (C=O)aOb heterociclilo, dicho alquilo, arilo, alquenilo, alquinilo cicloalquilo y heterociclilo está opcionalmente sustituido con uno o más sustituyentes seleccionados de R6; R2 y R3 están independientemente seleccionados de: H, (C=O)Oa alquilo C1-6, (C=O)Oa arilo, alquilo C1-6, SO2Ra, y arilo; R4 está seleccionado de: (C=O)aOb alquilo C1-10, (C=O)aOb arilo, (C=O)aOb alquenilo C2-10, (C=O)aOb alquinilo C2-10, CO2H, halo, OH, Ob perfluoralquilo C1-6, (C=O)a NR7R8, CN, (C=O)aOb cicloalquilo C3-8, y (C=O)aOb heterociclilo, dicho alquilo, arilo, alquenilo, alquinilo, cicloalquilo y heterociclilo está opcionalmente sustituido con uno o más sustituyentes seleccionados de R6; R6 es(C=O)aOb alquilo C1-6, (C=O)aOb arilo, alquenilo C2-10, alquinilo C2-10, (C=O)aOb heterociclilo, CO2H, halo, CN, OH, Ob perfluoralquilo C1-3, Oa(C=O)b NR7R8, oxo, CHO, (N=O)R7R8, o (C=O)aOb cicloalquilo C3-8, dicho alquilo, arilo, alquenilo, alquinilo, heterociclilo y cicloalquilo está opcionalmente sustituido con uno o más sustituyentes seleccionados de R6a; R6a está seleccionado de: C=O)rOs alquilo C1-10, donde r y s son independientemente 0 o 1, Or perfluoralquilo C1-3, donde r es 0 o 1, alquileno C0-6-S(O)mRa, donde m es 0, 1 o 2, oxo, OH, halo, CN, alquenilo C2-10, alquinilo C2-10, cicloalquilo C3-6, alquileno C0-6-arilo, alquileno C0-6-heterociclilo, alquileno C0-6-N(Rb)2, C(O)Ra, alquileno C0-6-CO2Ra, C(O)H, y alquileno C0-6-CO2H, dicho alquilo, alquenilo, alquinilo, cicloalquilo, arilo y heterociclilo está opcionalmente sustituido con hasta tres sustituyentes seleccionados de Rb, OH, alcoxi C1-6, halógeno, CO2H, CN, O(C=O) alquilo C1-6, oxo, y N(Rb)2; R7 y R8 están independientemente seleccionados de: H, (C=O)Ob alquilo C1-10, (C=O)Ob cicloalquilo C3-8, (C=O)Ob arilo, (C=O)Ob heterociclilo, alquilo C1-10, arilo, alquenilo C2-10, alquinilo C2-10, heterociclilo, cicloalquilo C3-8, SO2Ra, y (C=O)NRb 2, dicho alquilo, cicloalquilo, arilo, heterociclilo, alquenilo y alquinilo están opcionalmente sustituidos con uno o más sustituyentes seleccionados de R6a, o R7 y R8 pueden estar tomados conjuntamente al nitrógeno al cual están unidos para formar un heterociclo monocíclico o bicíclico con 5-7 miembros en cada anillo y que contiene opcionalmente además del nitrógeno uno o dos heteroátomos adicionales seleccionados de N, O y S, estando dicho heterociclo monocíclico o bicíclico opcionalmente sustituido con uno o más sustituyentes seleccionados de R6a; Ra es alquilo C1-6, cicloalquilo C3-6, arilo, o heterociclilo; y Rb es H, alquilo C1-6, arilo, heterociclilo, cicloalquilo C3-6, (C=O)O alquilo c1-6, (C=O) alquilo C1-6 o S(O)2Ra.
ARP000105472A 1999-10-19 2000-10-18 Compuestos de indol inhibidores de tirosina quinasa, composicion farmaceutica, procedimiento para prepararla,y, uso de los compuestos en la preparación de medicamentos AR035626A1 (es)

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US16035699P 1999-10-19 1999-10-19

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AR035626A1 true AR035626A1 (es) 2004-06-23

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ARP000105472A AR035626A1 (es) 1999-10-19 2000-10-18 Compuestos de indol inhibidores de tirosina quinasa, composicion farmaceutica, procedimiento para prepararla,y, uso de los compuestos en la preparación de medicamentos

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US (1) US6306874B1 (es)
EP (1) EP1226136B1 (es)
JP (2) JP3822494B2 (es)
KR (1) KR100681724B1 (es)
CN (1) CN1213045C (es)
AR (1) AR035626A1 (es)
AT (1) ATE286045T1 (es)
AU (1) AU778588B2 (es)
BG (1) BG65585B1 (es)
BR (1) BR0014843A (es)
CA (1) CA2387351C (es)
CO (1) CO5261601A1 (es)
CZ (1) CZ20021390A3 (es)
DE (1) DE60017179T2 (es)
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EA (1) EA005812B1 (es)
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GE (1) GEP20053530B (es)
HK (1) HK1054931A1 (es)
HR (1) HRP20020349A2 (es)
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