AR052482A1 - Derivados de triazol como inhibidores de hsp90 - Google Patents

Derivados de triazol como inhibidores de hsp90

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Publication number
AR052482A1
AR052482A1 ARP060100568A ARP060100568A AR052482A1 AR 052482 A1 AR052482 A1 AR 052482A1 AR P060100568 A ARP060100568 A AR P060100568A AR P060100568 A ARP060100568 A AR P060100568A AR 052482 A1 AR052482 A1 AR 052482A1
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AR
Argentina
Prior art keywords
replaced
hal
con
atoms
so2n
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Application number
ARP060100568A
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English (en)
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Hans-Michael Eggenweiler
Michael Wolf
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Merck Patent Gmbh
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Publication of AR052482A1 publication Critical patent/AR052482A1/es

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    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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Abstract

Los nuevos derivados de triazol de la formula (1) en donde R1 es OH, OCH3, OCF3, OCHF2, OBz1, OAc, p-metoxibenciloxi, SH, S(O) mCH3, SO2NH2, Hal, CF3 o CH3; R2, R3 son cada uno, de modo independiente entre sí, H, Hal, CN; NO2, A, Alk, (CH2)nAr, (CH2)nHet, COOH, COOA, COOAr, COOHet, CONH2, CONHA, CONAA', CON-HAr, CONAAr, CON(Ar)2, CONHHet, CON(Het)2, NH2, NHA, NHAr, NHHet, NAA', NHCOA, NACOA', NHCOAr, NHCOHet, NHCOOA, NHCOOAr, NHCOOHet, NHCONHA, NHCON-HAr, NHCONHHet, OH, OA, OAr, OHet, SH, S(O)mA, S(O)mAr, S(O)mHet, SO2NH2, SO2NHA, SO2NAA', SO2NHAr, SO2NAAr, SO2NHHet, SO2NAHet, SO2NAbencilo, SO2N(Ar)2 o SO2N(Het)2, R4, R5, R6 son cada uno, de modo independiente entre sí, H, Hal, CN, NO2, A, Alk, (CH2)nAr, (CH2)nHet, COOH, COOA, COOAr, COOHet, CONH2, CONHA, CONAA', CONHAr, CONAAr, CON(Ar)2, CONHHet, CON(Het)2, NH2, NHA, NHAr, NHHet, NAA', NHCOA, NHCONH2, NACOA', NHCO(CH2)nAr, NHCOHet, NHCOOA, NHCOOAr, NHCOOHet, NHCONHA, NHCONHAr, NHCONHHet, OH, OA, O(CH2) oHet, O(CH2)oNH2, O(CH2)oCN, OAr, OHet, SH, S(O)mA, S(O)mAr, S(O)mHet, SO2NH2, SO2NHA, SO2NAA', SO2NHAr, SO2NAAr, SO2NHHet, SO2N(Ar)2 o SO2N(Het)2; R4 y R5 también son juntos OCH2O, OCH2CH2O, -CH=CH-CH=CH-, NH-CH=CH o CH=CH-NH; Y es OH o SH; A, A' son cada uno, de modo independiente entre sí, alquilo no ramificado o ramificado C1-10, en donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NR8 y/o por grupos -CH=CH y/o también 1-5 átomos de H pueden estar reemplazados por F, Cl, Br y/o R7; Alk o alquilo cíclico C3-7; A y A' también son juntos una cadena alquileno con 2, 3, 4, 5 o 6 átomos de C, en donde un grupo CH2 puede estar reemplazado por O, S, SO, SO2, NH, NR8, NCOR8 o NCOOR8; Alk es alquenilo C2-6, R7 es COOR9, CONR9R10, NHCOR9, NHCOOR9 u OR9; R8 es cicloalquilo C3-7, cicloalquilalquileno C4-10, Alk o alquilo no ramificado o ramificado C1-6, en donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH y/o también 1-5 átomos de H pueden estar reemplazados por F y/o Cl; R9, R10 son cada uno, de modo independiente entre sí, H o alquilo C1-5, en donde 1-3 grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NMe o NEt y/o también 1-5 átomos de H pueden estar reemplazados por F y/o Cl; R9 y r10 también son juntos una cadena alquileno con 2, 3, 4, 5 o 6 átomos de C, en donde un grupo CH2 puede estar reemplazado por O, S, SO, SO2, NH, NR8, NCOR8 o NCOOR8; Ar es fenilo, naftilo o bifenilo no sustituido mono-, di- o trisustituido con Hal, A, OR11, N(R11)2, NO2, CN, fenilo, CON(R11)2, NR11COA, NR11CON(R11)2, NR11SO2A, COR11, SO2N(R11)2, S(O)mA, -[C(R11)2]n-COOR11 y/u -O[C(R11)2]o-COOR11; Het es un heterociclo mono- o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar mono-, di- o trisustituido con Hal, A, OR11, N(R11)2, NO2, CN, COOR11, CON(R11)2, NR11COA, NR11SO2A, COR11, SO2NR11, S(O)mA, =S, =NR11 y/u =O (oxígeno del carbonilo), R11 es H o A, Hal es F, Cl, Br o I; m es 0, 1, o 2; n es 0, 1, 2, 3, o 4; o es 1, 2 o 3; así como sus derivados, sales, solvatos, tautomeros y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones, excluyendo los compuestos seleccionados del grupo 5-(2,4-dihidroxifenil)-4-(naft-1-il)-4H-[1,2,4]triazol-3-tiol, 5-(2,4-dihidroxifenil)-4-(2-metilfenil)-4H-[1,2,4]triazol-3-tiol, 5-(2,4-dihidroxifenil)-4-(2,5-dimetoxi)-4H-[1,2,4]triazol-3-tiol. Son inhibidores de la HSP90 y pueden se utilizados para preparar un medicamento para el tratamiento de enfermedades en las que la inhibicion, la regulacion y/o la modulacion de la HSP90 desempena un papel importante.
ARP060100568A 2005-02-17 2006-02-17 Derivados de triazol como inhibidores de hsp90 AR052482A1 (es)

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DE102005007304A DE102005007304A1 (de) 2005-02-17 2005-02-17 Triazolderivate

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AR052482A1 true AR052482A1 (es) 2007-03-21

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EP (1) EP1853570B1 (es)
JP (1) JP5133068B2 (es)
KR (1) KR101273043B1 (es)
CN (1) CN101119978B (es)
AR (1) AR052482A1 (es)
AU (1) AU2006215902B2 (es)
BR (1) BRPI0607191A2 (es)
CA (1) CA2598017C (es)
DE (1) DE102005007304A1 (es)
ES (1) ES2394513T3 (es)
HK (1) HK1114839A1 (es)
MX (1) MX2007009777A (es)
RU (1) RU2416605C2 (es)
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CA2598017A1 (en) 2006-08-24
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