AR049540A1 - Derivados de quinazolindiona como inhibidores del parp; metodos para su preparacion; composiciones farmaceuticas que los contienen como ingrediente activo y su uso en medicamentos para el tratamiento o prevencion del cancer. - Google Patents

Derivados de quinazolindiona como inhibidores del parp; metodos para su preparacion; composiciones farmaceuticas que los contienen como ingrediente activo y su uso en medicamentos para el tratamiento o prevencion del cancer.

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Publication number
AR049540A1
AR049540A1 ARP050102689A ARP050102689A AR049540A1 AR 049540 A1 AR049540 A1 AR 049540A1 AR P050102689 A ARP050102689 A AR P050102689A AR P050102689 A ARP050102689 A AR P050102689A AR 049540 A1 AR049540 A1 AR 049540A1
Authority
AR
Argentina
Prior art keywords
formula
quinazolindione
alkanediyl
piperidinyl
compound
Prior art date
Application number
ARP050102689A
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English (en)
Original Assignee
Janssen Pharmaceutica Nv
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Filing date
Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR049540A1 publication Critical patent/AR049540A1/es

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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
    • C07D401/04Heterocyclic 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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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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Abstract

Derivados de quinazolindiona como inhibidores de PARP así como también composiciones farmacéuticas que los contengan y su uso en medicamentos para la profilaxis o el tratamiento del cáncer. Reivindicacion 1: Un compuesto de la formula (1), las formas N-oxidos, las sales de adicion farmacéuticamente aceptables y las formas estereoquímicamente isoméricas de las mismas, donde cada X es independientemente >N-, o >CH-; y cuando X es >CH- entonces Y es >N-; cada Y es independientemente >N-, o >CH-; excepto cuando X es >CH- entonces Y es >N-; L1 es un enlace directo o un radical bivalente seleccionado de alcanodiilo C1-6; L2 es un enlace directo o un radical bivalente seleccionado de carbonilo, alcanodiilo C1-6, -(hidroxi)alcanodiilo C1- 6, -C(O)-alcanodiilo C1-6 o alcanodiilo C1-6-C(O)-; R1 es H o hidroxi; y Z es H o un radical seleccionado del grupo de formulas (2) donde R2 se selecciona independientemente de H, halo o alquilo C1-6 con la condicion de que 1-[1-[(2S)-2-[(2R)-3,4- dihidro-2H-1-benzopiran-2-il]-2-hidroxietil]-4-piperidinil]-2,4-(1H,3H)-quinazolindiona, 1-[2-[4-(4-fluorbenzoil)-1-piperidinil]etil]-2,4-(1H,3H)-quinazolindiona, 1-[3-[4-(4-fluorbenzoil)-1-piperidinil]propil]-2,4-(1H,3H)-quinazolindiona, 3-[2-[4-(4- clorobenzoil)-1-piperidinil]etil]-2,4-(1H,3H)-quinazolindiona y 3-[2-[4-[(4-fluorfenil)hidroximetil]-1-piperidinil]etil]-2,4-(1H,3H)-quinazolindiona no están incluidos. Reivindicacion 13: Un proceso para la preparacion de un compuesto como se reivindico en la reivindicacion 1, caracterizado por a) la reaccion de un producto intermedio de la formula (3) con un producto intermedio de la formula (4), donde W es un grupo saliente apropiado, con la formacion de un compuesto de la formula (5), donde X es >N-, en un solvente inerte de reaccion y con el agregado de una base adecuada, o b) la reaccion de un producto intermedio de la formula (6) con un producto intermedio de la formula (7), donde W es un grupo saliente apropiado, con la formacion de un compuesto de la formula (8), donde Y es >N-, en un solvente inerte de reaccion y con el agregado de una base apropiada.
ARP050102689A 2004-06-30 2005-06-29 Derivados de quinazolindiona como inhibidores del parp; metodos para su preparacion; composiciones farmaceuticas que los contienen como ingrediente activo y su uso en medicamentos para el tratamiento o prevencion del cancer. AR049540A1 (es)

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EP04076885 2004-06-30

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AR049540A1 true AR049540A1 (es) 2006-08-09

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US (4) US8080557B2 (es)
EP (1) EP1763523B1 (es)
JP (1) JP5100376B2 (es)
CN (1) CN1980913B (es)
AR (1) AR049540A1 (es)
AU (1) AU2005259190B2 (es)
BR (1) BRPI0512938A (es)
CA (1) CA2569827C (es)
EA (1) EA011552B1 (es)
EG (1) EG25942A (es)
ES (1) ES2415771T3 (es)
HK (1) HK1105957A1 (es)
IL (1) IL180409A0 (es)
MX (1) MXPA06014541A (es)
NO (2) NO20070529L (es)
NZ (1) NZ551801A (es)
SG (1) SG154432A1 (es)
TW (1) TWI359142B (es)
UA (1) UA88012C2 (es)
WO (1) WO2006003148A1 (es)
ZA (1) ZA200610771B (es)

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