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AR070836A1 - Derivados de carbazol inhibidores de hsp90, composiciones que los contie-nen; utilizacion de los compuestos para preparar medicamentos; un proce-dimiento para la preparacion de los compuestos; medicamentos; y compues-tos intermediarios de sintesis - Google Patents

Derivados de carbazol inhibidores de hsp90, composiciones que los contie-nen; utilizacion de los compuestos para preparar medicamentos; un proce-dimiento para la preparacion de los compuestos; medicamentos; y compues-tos intermediarios de sintesis

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Publication number
AR070836A1
AR070836A1 ARP090100879A ARP090100879A AR070836A1 AR 070836 A1 AR070836 A1 AR 070836A1 AR P090100879 A ARP090100879 A AR P090100879A AR P090100879 A ARP090100879 A AR P090100879A AR 070836 A1 AR070836 A1 AR 070836A1
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Argentina
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alkyl
radicals
formula
radical
products
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ARP090100879A
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Perez Maria Mendez
Jean-Marie Ruxer
Victor Certal
Luc Bertin
Patrick Mailliet
Marcel Alasia
Franck Halley
Herve Minoux
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Sanofi Aventis
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Application filed by Sanofi Aventis filed Critical Sanofi Aventis
Publication of AR070836A1 publication Critical patent/AR070836A1/es

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    • 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
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    • 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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    • 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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    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
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Abstract

Reivindicacion 1: Productos de la formula (1) en los que Het representa un heterociclo aromático o parcialmente insaturado de tipo dihidro o tetrahidro mono o bicíclico, de 5 a 11 eslabones, que contiene de 1 a 4 heteroátomos, elegidos entre N, O o S, opcionalmente sustituido por uno o varios radicales R1 o R'1, iguales o diferentes, tal como se describe a continuacion, R si elige del grupo constituido por las formulas (2); R1 y/o R'1, iguales o diferentes, son del grupo constituido por: H, halogeno, CF3, nitro, ciano, alquilo, hidroxi, mercapto, amino, alquilamino, dialquilamino, alcoxi, fenilalcoxi, alquiltio, carboxi libre o esterificado por un radical: alquilo, carboxamida, CO-NH(alquilo), CON(alquilo)2, NH-CO-alquilo, sulfonamida, NH-SO2-alquilo, S(O)2-NHalquilo, S(O2)-N(alquilo)2, estando todos los radicales alquilo, alcoxi y alquiltio opcionalmente sustituidos por uno o varios radicales, iguales o diferentes, elegido(s) entre: halogeno, hidroxi, alcoxi, amino, alquilamino y dialquilamino; W1, W2, W3 representan independientemente CH o N, X representa el átomo de oxigeno o de azufre o un radical: NR2, C(O), S(O) o S(O)2; Z representa un átomo de hidrogeno o un átomo de halogeno o un radical -O-R2 o un radical -NH-R2 en el que R2 representa un átomo de hidrogeno o un radical alquilo C1-6, cicloalquilo C3-8 o heterocicloalquilo C3-10, mono o bicíclico; estando estos radicales alquilo, cicloalquilo y heterocicloalquilo opcionalmente substituidos por uno o varios radicales, iguales o diferentes, elegido(s) entre los radicales: -O-PO3H2, O-PO3Na2, -O-SO3H2, -O-SO3Na2, -O-CH2-PO3H2, -O-CH2-PO3Na2, O-CO-alanina, O-CO-serina, O-CO-lisina, O-CO-arginina, O-CO-glicina-lisina, -O-CO-alanina-lisina, halogeno, hidroxi; mercapto; amino; carboxamida (CONH2); carboxi; heterocicloalquilo tal como: aziridino; azetidino; oxetano; tetrahidrofurano; piperidino; tetrahidropirano; piperazino; alquilpiperazino; pirrolidino; morfolino; homopiperidino; homopiperazino; quinuclidino; cicloalquilo, heteroarilo; carboxi esterificado por un radical alquilo; CO-NH(alquilo); -O-CO-alquilo, -NH-CO-alquilo; alquilo; alcoxi; hidroxialcoxi; alquiltio; alquilamino; dialquilamino; estando todos estos radicales, los radicales alquilos, alcoxi y alquiltio opcionalmente substituidos por un radical: hidroxi, mercapto, amino, alquilamino, dialquilamino, CO2alquilo, NHCO2alquilo; azetidino, oxetano, pirrolidino, tetrahidrofurano, piperidino, tetrahidropirano, piperazino, morfolino, homopiperidino, homopiperazino o quinuclidino; estando todos estos radicales, todos los radicales cíclicos, cicloalquilo, heterocicloalquilo y heteroarilo opcionalmente substituidos por uno o varios radicales, iguales a diferentes, elegido(s) entre los radicales hidroxi, alquilo, alcoxi, CH2OH; amino, alquilamino, dialquilamino, CO2alquilo o NHCO2alquilo; estando dichos productos de formula (1) en todas las formas tautomeras e isomeras posibles, racémicos, enantiomeros y diastereoisomeros, así como sales de adicion con ácidos minerales y orgánicos o con bases minerales y orgánicas de productos de formula (1), así como profármacos de productos de formula (1). Reivindicacion 11: Como nuevos productos industriales, los compuestos intermedios de síntesis de formulas (3), (4), (5), (6), (7), (8), (9) y (10).En formula (4) Z= C(O)-OMe o C(O)-OH u OH u O-CH2-Ph u OTf, en formula (5) Z= C(O)-OMe o C(O)-OH u OH u O-CH2-Ph u OTf; en formula (7) Z= C(O)-OH o C(O)-Ome o C(O)-Oet. Productos de formulas (3), (4), (5), (6), (7), (8), (9) y (10) en los que los sustituyentes Het, R, R2, W1 y W2 tienen los significados indicados para los productos de formula (1) tal como se define en las reivindicaciones precedentes y Z tiene el significado indicado anteriormente en el esquema (1) o en el esquema (42).
ARP090100879A 2008-03-14 2009-03-12 Derivados de carbazol inhibidores de hsp90, composiciones que los contie-nen; utilizacion de los compuestos para preparar medicamentos; un proce-dimiento para la preparacion de los compuestos; medicamentos; y compues-tos intermediarios de sintesis AR070836A1 (es)

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FR0801394A FR2928645A1 (fr) 2008-03-14 2008-03-14 Nouveaux derives de carbazole inhibiteurs d'hsp90, compositions les contenant et utilisation

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US (1) US8309721B2 (es)
EP (1) EP2265598A2 (es)
JP (1) JP5674483B2 (es)
KR (1) KR20100130603A (es)
CN (1) CN102026992A (es)
AR (1) AR070836A1 (es)
AU (1) AU2009232121A1 (es)
BR (1) BRPI0909731A2 (es)
CA (1) CA2718488A1 (es)
CL (1) CL2009000619A1 (es)
CO (1) CO6251295A2 (es)
CR (1) CR11653A (es)
DO (1) DOP2010000272A (es)
EA (1) EA201071078A1 (es)
EC (1) ECSP10010473A (es)
FR (1) FR2928645A1 (es)
IL (1) IL208059A0 (es)
MA (1) MA32206B1 (es)
MX (1) MX2010010018A (es)
NI (1) NI201000150A (es)
PE (1) PE20091673A1 (es)
TW (1) TW200938541A (es)
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