AR070649A1 - Derivados de 1,3- dihidro -isoindol - Google Patents

Derivados de 1,3- dihidro -isoindol

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Publication number
AR070649A1
AR070649A1 ARP080103758A ARP080103758A AR070649A1 AR 070649 A1 AR070649 A1 AR 070649A1 AR P080103758 A ARP080103758 A AR P080103758A AR P080103758 A ARP080103758 A AR P080103758A AR 070649 A1 AR070649 A1 AR 070649A1
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Argentina
Prior art keywords
hal
atoms
replaced
mono
nr6conr6r7
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ARP080103758A
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English (en)
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Hans-Michael Eggenweiler
Christian Sirrenberg
Hans-Peter Buchstaller
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Merck Patent Gmbh
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Publication of AR070649A1 publication Critical patent/AR070649A1/es

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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
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Abstract

Los derivados de 1,3-dihidro-isoindol de la formula (1) en donde R1 es A; R2 es A, (CH2)nAr o (CH2)nHet; R1 y R2 son, junto con el átomo de N al que están unidos, isoindolilo; R3 es H, Hal, OH, CN, NO2, C(O)H, NH2, COOH, COOA, CsCH, CsC-CH2OH, CONH2, CONHA, CONAA', SO2NH2, NHCONH2, X-A, X-(CH2)nAr o X-(CH2)nHet, en donde X es un enlace, -O-, -CO-, -CO2-, -C(O)NH, -C(O)NA', -S-, -SO-, -SO2-, SO2NH-, -SO2NA', -NH-, -NA'-, -NHSO2-, -NA'SO2, -NHCO-, -NA'CO-, -NHCONH- o -NA'CONH-; R3' es H, A, Hal, OA o CN; A, A' son en cada caso, de modo independiente entre sí, alquilo no ramificado o ramificado C1-10, en donde uno, dos o tres grupos CH2 o CH no adyacentes pueden estar reemplazados por O, S, SO, SO2, CO, NH, NR5 y/o por grupos -CH=CH y/o también 1-5 átomos de H pueden estar reemplazados por F, Cl, Br y/o R4, o cicloalquilo C3-7, A y A' son, junto con el átomo de N al que están unidos, también un heterociclo monocíclico saturado no sustituido o mono-, di- o trisustituido con Hal, A, (CH2)nOH, (CH2)nOA y/u =O (oxígeno del carbonilo), que puede contener otros 1 a 3 átomos de N, O y/o S; R4 es COOR6, CN, CONR6R7, NR6R7, NHCOR6, NHCOOR6, NR6CONR6R7 u OR6; R5 es cicloalquilo C3-7, cicloalquilalquileno C4-10, Alk o alquilo no ramificado o ramificado C1-6, en donde uno, dos o tres grupos CH2 o CH no adyacentes pueden estar reemplazados por O, CO, S, SO, SO2, NH y/o también 1-5 átomos de H pueden estar reemplazados por F y/o Cl; R6, R7 son en cada caso, de modo independiente entre sí, H o alquilo C1-5, en donde 1-3 grupos CH2 o CH no adyacentes pueden estar reemplazados por O, CO, S, SO, SO2, NH, NMe o Net y/o también 1-5 átomos de H pueden estar reemplazados por F y/o Cl, R6 y R7 son juntos también una cadena de alquileno con 2, 3, 4, 5 o 6 átomos de C, en donde 1-3 átomos de C no adyacentes pueden estar reemplazados por O, CO, S, SO, SO2, NH, NR5, NCOR5 o NCOOR5; Alk es alquenilo C2-6; Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di-, tri-, tetra o pentasustituido con Hal, A, (CH2)nCN, (CH2)nAr', (CH2)nHet', (CH2)nOA, (CH2)nOH, S(O)mA, NO2, (CH2)NR6R7, NR5R6, CONR6R7 CONR5R6, SO2NR6R7, SO2NR5R6, NR6COR7, NR6CONR6R7 y/o NR6SO2R7; Ar' es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con Hal, A, CN, fenilo, OA, OH, S(O)mA, NO2, NR6R7, NR5R6, CONR6R7, CONR5R6, SO2NR6R7, SO2NR5R6, NR6COR7, NR6CONR6R7 y/o NR6SO2R7; Het es un heterociclo saturado, insaturado o aromático mono- o bicíclico con 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di- o trisustituido con Hal, A, CN, Ar', Het' OA, OH, S(O)mA, NO2, NR6R7, NR5R6, CONR6R7, CONR5R6, SO2NR6R7, SO2NR5R6, NR6COR7, NR6CONR6R7, NR6SO2R7, =S, =NR8, =NR8R4 y/u =O (oxígeno del carbonilo); Het' es un heterociclo saturado, insaturado o aromático mono- o bicíclico con 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di- o trisustituido con Hal, A, CN, Ar', OA, OH, S(O)nA, NO2, NR6R7, NR5R6, CONR6R7, CONR5R6, SO2NR6R7, SO2NR5R6, NR6COR7, NR6CONR6R7, NR6SO2R7, =S, =NR8, =NR8R4 y/u =O (oxígeno del carbonilo); R8 es H o A; Hal es F, Cl, Br o I; m es 0, 1 o 2, n 0, 1, 2, 3 o 4; así como sus derivados, sales, solvatos y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Son inhibidores de la HSP90 y pueden ser 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.
ARP080103758A 2007-08-30 2008-08-29 Derivados de 1,3- dihidro -isoindol AR070649A1 (es)

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EP (1) EP2181092B1 (es)
JP (1) JP5529739B2 (es)
KR (1) KR20100061817A (es)
CN (1) CN101790513A (es)
AR (1) AR070649A1 (es)
AU (1) AU2008295176B2 (es)
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EP2181092A1 (de) 2010-05-05
ZA201002217B (en) 2017-11-29
ES2532853T3 (es) 2015-04-01
IL204126A (en) 2015-07-30
JP2010536893A (ja) 2010-12-02
BRPI0815059A2 (pt) 2015-02-10
DE102007041116A1 (de) 2009-03-05
WO2009030316A1 (de) 2009-03-12
CA2697934C (en) 2016-02-16
EP2181092B1 (de) 2015-01-14
US8183279B2 (en) 2012-05-22
AU2008295176A1 (en) 2009-03-12
JP5529739B2 (ja) 2014-06-25
CN101790513A (zh) 2010-07-28
MX2010002042A (es) 2010-03-15
CA2697934A1 (en) 2009-03-12
US20100311745A1 (en) 2010-12-09
KR20100061817A (ko) 2010-06-09
EA201000362A1 (ru) 2010-08-30

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