AR074199A1 - Compuesto de 6-(4-pirimidinil)-1h-indazol, composiciones farmaceuticas que lo comprenden y su uso para preparar un medicamento util para el tratamiento o disminucion de la gravedad del cancer. - Google Patents

Compuesto de 6-(4-pirimidinil)-1h-indazol, composiciones farmaceuticas que lo comprenden y su uso para preparar un medicamento util para el tratamiento o disminucion de la gravedad del cancer.

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Publication number
AR074199A1
AR074199A1 ARP090104456A ARP090104456A AR074199A1 AR 074199 A1 AR074199 A1 AR 074199A1 AR P090104456 A ARP090104456 A AR P090104456A AR P090104456 A ARP090104456 A AR P090104456A AR 074199 A1 AR074199 A1 AR 074199A1
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Argentina
Prior art keywords
substituted
alkyl
cycloalkyl
heteroaryl
aryl
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ARP090104456A
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English (en)
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Glaxosmithkline Llc
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Publication of AR074199A1 publication Critical patent/AR074199A1/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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D401/02—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
    • 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
    • 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Compuesto de 6-(4-pirimidinil)-1H-indazol, inhibidor de PDK1 de la formula (1) en la que: R1 se selecciona entre H, alquilo C1-6, cicloalquilo C3-7, cicloalquilo C3-7 sustituido con uno a tres R8, alcoxi C1-6, mercapto C1-6, -N(R5)(R6), arilo, arilo sustituido con uno a tres R8, heteroarilo, heteroarilo sustituido con uno a tres R8, heterocicloalquilo y heterocicloalquilo sustituido con uno a tres R8, donde, R5 es H o alquilo C1-3; R6 se selecciona entre: H, arilo, arilo sustituido con uno a tres R7 , cicloalquilo C3-7, cicloalquilo C3-7 sustituido con uno a tres R8, alquilo C1-6, y alquilo C1-6 sustituido con un R9, donde, R9 se selecciona entre: fenilo, fenilo sustituido con uno a tres R7, heteroarilo, heteroarilo sustituido con uno a tres R7, cicloalquilo C3-7, cicloalquilo C3-7 sustituido con uno a tres R8; R2 se selecciona entre: hidrogeno, halo, -N(R10)-(CH2)n-R11, -O-(CH2)n-R11, -S-(CH2)n-R11; arilo, arilo sustituido con uno a tres R7, heteroarilo, heteroarilo sustituido con uno a tres R7, cicloalquilo C3-7, cicloalquilo C3-7 sustituido con uno a tres R7, heterocicloalquilo y heterocicloalquilo sustituido con uno a tres R7; donde, R10 es hidrogeno o alquilo C1-3, R11 se selecciona entre: hidrogeno, alquilo C1-3, alquilo C1-3 sustituido con uno a tres R7, cicloalquilo C3-7, cicloalquilo C3-7 sustituido con uno a tres R7, arilo, arilo sustituido con uno a tres R7, heteroarilo, heteroarilo sustituido con uno a tres R7, -O-cicloalquilo C3-7, -O-cicloalquilo C3-7 sustituido con uno a tres R7, -O-arilo, -O-arilo sustituido con uno a tres R7, -O-heteroarilo y -O-heteroarilo sustituido con uno a tres R7, y n es 0, 1, 2 o 3, con la condicion de que cuando R11 es -O-cicloalquilo C3-7, -O-arilo o -O-heteroarilo, n no sea 0; R3 se selecciona entre: H, -NH2, alquilo C1-3 y cicloalquilo C3-7, y R4 se selecciona entre: H, NH2 y NH-alquilo C1-3, donde, cada R8 se selecciona independientemente entre: hidroxi, alquilo C1-6, alquilo C1-6 sustituido con uno a tres R7, -C(O)alquilo C1-6, cicloalquilo C3-7, alcoxi C1-6, amino, alquilamino C1-4, dialquilamino C1-4, -alquil C1-4-NR200R201, arilo, arilo sustituido con uno a tres R7, -alquilarilo C1-4, -alquilarilo C1-4 sustituido con uno a tres R7; fenilheteroarilo, fenilheteroarilo sustituido con uno a tres R7, heterocicloalquilo, heterocicloalquilo sustituido con uno a tres R7, heteroarilo, heteroarilo sustituido con uno a tres R7, nitro, ciano, oxo, halo, -CO2R120, -C(O)NR200R201, -alquil C1-4-OC(O)NR200R201, -OC(O)NR200R201, -OC(O)R200, -NR200C(C)OR301, -alquil C1-4-NR200C(O)OR301, -NR200C(O)R302, -NR200S(O)2R302, -alquil C1-4-NR200C(O)R302 y -alquil C1-4-NR200S(O)2R302; R120 se selecciona entre: H, alquilo C1-4 y cicloalquilo C3-7, R200 es hidrogeno o alquilo C1-3, R201 se selecciona entre: hidrogeno, alquilo C1-6, alquilo C1-6 sustituido con uno a tres R7, cicloalquilo C3-7, cicloalquilo C3-7 sustituido con uno a tres R7, -alquil C1-4-cicloalquilo C3-7, -alquil C1-4-cicloalquilo C3-7 sustituido con uno a tres R7, arilo, arilo sustituido con uno a tres R7, -alquilarilo C1-4, -alquilarilo C1-4 sustituido con uno a tres R7, heteroarilo, heteroarilo sustituido con uno a tres R7, -alquilheteroarilo C1-4, -alquilheteroarilo C1-4 sustituido con uno a tres R7, heterocicloalquilo, heterocicloalquilo sustituido con uno a tres R7, -alquil C1-4-heterocicloalquilo, -alquil C1-4-heterocicloalquilo sustituido con uno a tres R7, R301 se selecciona entre alquilo C1-6, alquilo C1-6 sustituido con uno a tres R7, cicloalquilo C3-7, cicloalquilo C3-7 sustituido con uno a tres R7, -alquilarilo C1-4, -alquilarilo C1-4 sustituido con uno a tres R7, -alquil C1-4-cicloalquilo C3-7, -alquil C1-4-cicloalquilo C3-7 sustituido con uno a tres R7, y R302 se selecciona entre: H, alquilo C1-6, alquilo C1-6 sustituido con uno a tres R7, cicloalquilo C3-7, cicloalquilo C3-7 sustituido con uno a tres R7, -alquil C1-4-cicloalquilo C3-7, -alquil C1-4-cicloalquilo C3-7 sustituido con uno a tres R7, arilo, arilo sustituido con uno a tres R7, -alquilarilo C1-4, -alquilarilo C1-4 sustituido con uno a tres R7, heteroarilo, heteroarilo sustituido con uno a tres R7, -alquilheteroarilo C1-4, -alquilheteroarilo C1-4 sustituido con uno a tres R7, heterocicloalquilo, heterocicloalquilo sustituido con uno a tres R7, -alquil C1-4-heterocicloalquilo, -alquil C1-4 heterocicloalquilo sustituido con uno a tres R7; y cada R7 se selecciona independientemente entre: halo, ciano, hidroxi, amino, alquilamino C1-4, dialquilamino C1-4, alquilo C1-3 y alcoxi C1-3, o una sal del mismo, incluyendo una sal farmacéuticamente aceptable del mismo. Composiciones farmacéuticas que lo comprenden. Su uso, opcionalmente combinado con al menos un agente antineoplásico, para preparar un medicamento util para el tratamiento o disminucion de la gravedad del cáncer, diabetes, rechazo de trasplante/injerto, psoriasis y colitis.
ARP090104456A 2008-11-20 2009-11-18 Compuesto de 6-(4-pirimidinil)-1h-indazol, composiciones farmaceuticas que lo comprenden y su uso para preparar un medicamento util para el tratamiento o disminucion de la gravedad del cancer. AR074199A1 (es)

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EP (1) EP2362775B1 (es)
JP (1) JP5743897B2 (es)
AR (1) AR074199A1 (es)
ES (1) ES2548141T3 (es)
TW (1) TW201031648A (es)
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