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AR067506A1 - Derivados de quinazolinamida - Google Patents

Derivados de quinazolinamida

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Publication number
AR067506A1
AR067506A1 ARP080102977A ARP080102977A AR067506A1 AR 067506 A1 AR067506 A1 AR 067506A1 AR P080102977 A ARP080102977 A AR P080102977A AR P080102977 A ARP080102977 A AR P080102977A AR 067506 A1 AR067506 A1 AR 067506A1
Authority
AR
Argentina
Prior art keywords
noa
noh
nnha
nnh2
mono
Prior art date
Application number
ARP080102977A
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English (en)
Inventor
Hans-Michael Eggenweiler
Christian Sirrenberg
Hans-Peter Buchstaller
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Merck Patent Gmbh
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Publication of AR067506A1 publication Critical patent/AR067506A1/es

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    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/78Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84Nitrogen atoms
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Abstract

Los nuevos derivados de quinazolinamida de la formula (1) en donde R1 es H, A, (CH2)nCONH2, (CH2)nCONHA, (CH2)nCONAA', Hal, (CH2)nNH2, (CH2)nNHA, (CH2)nNAA', CN, NO2, (CH2)nAr, OAr, (CH2)nCOOH, (CH2)nCOOA, (CH2)nOH, (CH2)nOA, (CH2)nHet, COHet, C:::C-CH2SiA2A', C:::CH, C:::C-A, CH=CH-Ar1, CH=CH-COOA, CH2CH(OH)CH2OH, O(CH2)nOH, NH(CH2)nOH, O(CH2)nOA, NH(CH2)nOA, O(CH2)nNHA, NH(CH2)nNHA, NR4R5, (CH2)nCOOA, (CH2)nCONH(CH2)2CN, NH(CH2)nAr o CH=CH-COOH, R2 es H, A, (CH2)nAr, (CH2)nHet, (CH2)nOH, (CH2)nOA, (CH2)nNHHet, (CH2)nSA o (CH2)nCH(OH)Ar, R3 es A, (CH2)nAr, (CH2)nHet, (CH2)nCN, (CH2)nNH2, (CH2)nNHA, (CH2)nNAA', (CH2)nOH, (CH2)nOA o (CH2)nNHHet, R2 y R3 también son, junto con el átomo de N al que están unidos, un heterociclo mono- o bicíclico saturado, insaturado o aromático 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, R5 son, de modo independiente entre sí, (CH2)nOH, (CH2)nOA, (CH2)nNH2, (CH2)nNHA o (CH2)nNAA', Ar es fenilo, naftilo, tetrahidronaftilo o bifenilo no sustituido o mono-, di-, tri-, tetra- o pentasustituido con A, Hal, (CH2)nOA, (CH2)nOH, (CH2)nCN, SA, SOA, SO2A, NO2, C:::CH, (CH2)nCOOH, CHO, (CH2)nCOOA, CONH2, CONHA, CONAA', NHCOA, CH(OH)A, (CH2)nNH2, (CH2)nNHA, (CH2)nNAA', (CH2)nNAAr1, O(CH2)nHet1, (CH2)nHet1, COO(CH2)nAr1, (CH2)nNHSO2A, (CH2)nOAr1, O(CH2)nAr1, SO2NH(CH2)nNH2, SO2NH2, SO2NHA, SO2NAA', CONHAr1, CONH(CH2)nCOOA, CONH(CH2)nCOOH, NHCO(CH2)nCOOA, NHCO(CH2)nCOOH, CONH(CH2)nNH2, CONH(CH2)nNHA, CONH(CH2)nNAA', CONH(CH2)nCN, NHCOHet, SO2Het, COHet y/o (CH2)nCH(NH2)COOH, Ar1 es fenilo no sustituido o mono-, di-, tri-, tetra- o pentasustituido con A, Hal y/u OA, Het es un heterociclo mono- o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que no está sustituido o que puede estar mono-, di- o trisustituido con A, (CH2)nOA, (CH2)nOH, Ar1, SH, S(O)mA, Hal, NO2, CN, COA, CHO, COOA, COObencilo, CONH2, CONHA, CONAA', SO2NH2, (CH2)nNH2, (CH2)nNHA, (CH2)nNAA', NHSO2A y/u =O (oxígeno del carbonilo), Het1 es un heterociclo mono- o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que no está sustituido o que está mono- o disustituido con A, OA, OH, Hal, CN y/u =O (oxígeno del carbonilo), A, A' son, de modo independiente entre sí, alquilo no ramificado o ramificado C1-10, en donde 1-3 grupos CH2 no adyacentes pueden estar reemplazados por O, S, SO, SO2, NH, NNe o Net y/o también 1-5 átomos de H también pueden estar reemplazados por F, OH y/o Cl, Alk1 es alquilo cíclico C3-8 o cicloalquilalquileno, en donde 1-5 átomos de H pueden estar reemplazados por F, OH y/o Cl, Alk1 es alquenilo o alquinilo C2-6, m es 0, 1 o 2, n es 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.
ARP080102977A 2007-07-13 2008-07-11 Derivados de quinazolinamida AR067506A1 (es)

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DE102007032739A DE102007032739A1 (de) 2007-07-13 2007-07-13 Chinazolinamidderivate

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AR067506A1 true AR067506A1 (es) 2009-10-14

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US (1) US8501754B2 (es)
EP (1) EP2164833B1 (es)
JP (1) JP5457343B2 (es)
KR (1) KR20100044846A (es)
CN (1) CN101743229B (es)
AR (1) AR067506A1 (es)
AU (1) AU2008278032B2 (es)
BR (1) BRPI0814236A2 (es)
CA (1) CA2694475C (es)
DE (1) DE102007032739A1 (es)
EA (1) EA017585B1 (es)
ES (1) ES2538218T3 (es)
IL (1) IL203206A (es)
WO (1) WO2009010139A2 (es)
ZA (1) ZA201001058B (es)

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CA2694475A1 (en) 2009-01-22
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AU2008278032B2 (en) 2013-03-28
AU2008278032A1 (en) 2009-01-22
ES2538218T3 (es) 2015-06-18
EP2164833B1 (de) 2015-04-15
CN101743229B (zh) 2013-08-14
US8501754B2 (en) 2013-08-06
ZA201001058B (en) 2010-11-24
EP2164833A2 (de) 2010-03-24
KR20100044846A (ko) 2010-04-30
WO2009010139A2 (de) 2009-01-22
CN101743229A (zh) 2010-06-16
DE102007032739A1 (de) 2009-01-15
WO2009010139A3 (de) 2009-03-12
BRPI0814236A2 (pt) 2015-01-06
EA017585B1 (ru) 2013-01-30
IL203206A (en) 2015-03-31
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CA2694475C (en) 2015-07-28
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