AR067599A1 - Derivados de indazol sustituido activos como inhibidores de quinasa - Google Patents

Derivados de indazol sustituido activos como inhibidores de quinasa

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Publication number
AR067599A1
AR067599A1 ARP080103104A ARP080103104A AR067599A1 AR 067599 A1 AR067599 A1 AR 067599A1 AR P080103104 A ARP080103104 A AR P080103104A AR P080103104 A ARP080103104 A AR P080103104A AR 067599 A1 AR067599 A1 AR 067599A1
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AR
Argentina
Prior art keywords
alkyl
heterocyclyl
aryl
substituted
heteroaryl
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ARP080103104A
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English (en)
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Nerviano Medical Sciences Srl
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Application filed by Nerviano Medical Sciences Srl filed Critical Nerviano Medical Sciences Srl
Publication of AR067599A1 publication Critical patent/AR067599A1/es

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    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
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    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P3/00Drugs for disorders of the metabolism
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    • A61P3/04Anorexiants; Antiobesity agents
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/00Antineoplastic agents
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • A61P39/06Free radical scavengers or antioxidants
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    • A61P41/00Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
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    • A61P9/00Drugs for disorders of the cardiovascular system
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    • A61P9/10Drugs 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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    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
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    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond

Abstract

Se describen derivados de indazol sustituido de la formula (1) y sales farmacéuticamente aceptables de estos, como se define en la especificacion, procesos para su preparacion y composiciones farmacéuticas que los comprenden. Los compuestos de la presente pueden ser utiles en terapia, en el tratamiento de enfermedades asociadas con una actividad desregulada de la proteína quinasa, como el cáncer. Reivindicacion 1: Un compuesto de la formula (1), caracterizado porque X es -CH2-, -CH(OH)-, -CH(OR')- o -C(R'Rö)-, en donde: R' es alquilo C1-6 y Rö es H o alquilo C1-6; Ar es arilo o heteroarilo opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halogeno, alquenilo C2-6, alquinilo C2-6, ciano, nitro, NHCOR4, COR4, NR5R6, NR5COR4, OR7, SR7, SOR10, SO2R10, NHSOR10, NHSO2R10, R8R9N-alquilo C1-6, R8O-alquilo C1-6, alquilo C1-6, cicloalquilo C3-6, heterociclilo, arilo y heteroarilo de cadena recta o ramificada opcionalmente más sustituido en donde: R4 es hidrogeno, alquenilo C2-6, alquinilo C2-6, NR5R6, OR7, SR7, R8R9N-alquilo C1-6, R8O-alquilo C1-6, alquilo C1-6, cicloalquilo C3-6, heterociclilo, arilo o heteroarilo de cadena recta o ramificada opcionalmente más sustituido; R5 y R6 son independientemente hidrogeno, alquenilo C2-6, alquinilo C2-6, R8R9N-alquilo C2-6, R8O-alquilo C2-6, alquilo C1-6, cicloalquilo C3-6, heterociclilo, arilo o heteroarilo de cadena recta o ramificada, opcionalmente más sustituido, o R5 y R6, tomados juntos con el átomo de nitrogeno al cual están unidos pueden forman un grupo heterociclilo opcionalmente sustituido; R7 es hidrogeno, alquenilo C2-6, alquinilo C2-6, COR4, SOR10, SO2R10, R8R9N-alquilo C2-6, R8O-alquilo C2-6, alquilo C1-6, cicloalquilo C3-6, heterociclilo, arilo o heteroarilo de cadena recta o ramificada, opcionalmente más sustituido, en donde R4 es como se definiera anteriormente; R8 y R9 son independientemente hidrogeno, alquenilo C2-6, alquinilo C2-6, COR4, alquilo C1-6, cicloalquilo C3-6, heterociclilo, arilo o heteroarilo de cadena recta o ramificada opcionalmente más sustituido, o R8 y R9, tomados juntos con el átomo de nitrogeno al cual están unidos, pueden formar un grupo heterociclilo opcionalmente sustituido, en donde R4 es como se definiera anteriormente; R10 es hidrogeno, alquenilo C2-6, alquinilo C2-6, NR5R6, OR7, R8R9N-alquilo C1-6, R8O-alquilo C1-6, alquilo C1-6de cadena recta o ramificado, opcionalmente más sustituido, cicloalquilo C3-6, heterociclilo, arilo o heteroarilo, en donde R5, R6, R7, R8 y R9 son como se definiera anteriormente; Res un alquilo C1-6, cicloalquilo C3-6, heterociclilo, arilo o heteroarilo de cadena recta o ramificada, opcionalmente sustituido, R1, R2 y R3 son independientemente hidrogeno, halogeno, nitro, alquilo C1-6 de cadena recta o ramificada, opcionalmente sustituido, NR5R6, u OR7, en donde R5, R6 y R7 son como se definiera anteriormente; o isomeros, tautomeros, prodrogas o sales de estos farmacéuticamente aceptables.
ARP080103104A 2007-07-20 2008-07-18 Derivados de indazol sustituido activos como inhibidores de quinasa AR067599A1 (es)

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AR067599A1 true AR067599A1 (es) 2009-10-14

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US (11) US8299057B2 (es)
EP (1) EP2176231B1 (es)
JP (1) JP5506674B2 (es)
KR (2) KR101567763B1 (es)
CN (2) CN101754956B (es)
AR (1) AR067599A1 (es)
AU (1) AU2008280283B2 (es)
BR (1) BRPI0814628B1 (es)
CA (1) CA2693901C (es)
CL (1) CL2008002129A1 (es)
DK (1) DK2176231T3 (es)
EA (1) EA018503B1 (es)
ES (1) ES2605230T3 (es)
FR (1) FR20C1064I2 (es)
HK (2) HK1141278A1 (es)
HU (2) HUE030929T2 (es)
IL (1) IL203292A (es)
NL (1) NL301090I2 (es)
NO (1) NO2020042I1 (es)
NZ (1) NZ583450A (es)
PL (1) PL2176231T3 (es)
PT (1) PT2176231T (es)
SG (1) SG183049A1 (es)
SI (1) SI2176231T1 (es)
TW (1) TWI421073B (es)
UA (1) UA99141C2 (es)
WO (1) WO2009013126A1 (es)
ZA (1) ZA201001086B (es)

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