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
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Argentina
Prior art keywords
noa
noh
nnha
nnh2
mono
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ARP080102977A
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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 AR067506A1 publication Critical patent/AR067506A1/es

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    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
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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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AR077405A1 (es) 2009-07-10 2011-08-24 Sanofi Aventis Derivados del indol inhibidores de hsp90, composiciones que los contienen y utilizacion de los mismos para el tratamiento del cancer
FR2949467B1 (fr) 2009-09-03 2011-11-25 Sanofi Aventis Nouveaux derives de 5,6,7,8-tetrahydroindolizine inhibiteurs d'hsp90, compositions les contenant et utilisation
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GB2486631A (en) * 2010-12-01 2012-06-27 Univ Sheffield Phenol/quinone boronic acids/esters and method of preparation thereof
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CA2905417A1 (en) 2013-03-15 2014-09-18 Rexahn Pharmaceuticals, Inc. Tetrahydroisoquinolin-2-yl-(quinazolin-4-yl) methanone compounds as cancer cell growth inhibitors
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KR20180086187A (ko) 2015-10-05 2018-07-30 더 트러스티이스 오브 콜롬비아 유니버시티 인 더 시티 오브 뉴욕 자가포식 유동의 활성체 및 포스포리파제 d 및 타우를 포함하는 단백질 응집물의 클리어런스 및 단백질질환의 치료
TWI734806B (zh) * 2016-07-19 2021-08-01 日商日本化藥股份有限公司 攝像元件用光電變換元件用材料及含有該材料之光電變換元件
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KR20100044846A (ko) 2010-04-30
CN101743229A (zh) 2010-06-16
AU2008278032B2 (en) 2013-03-28
CA2694475A1 (en) 2009-01-22
EA201000098A1 (ru) 2010-06-30
JP2010533132A (ja) 2010-10-21
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EP2164833A2 (de) 2010-03-24
BRPI0814236A2 (pt) 2015-01-06
US20100234324A1 (en) 2010-09-16
ES2538218T3 (es) 2015-06-18
CN101743229B (zh) 2013-08-14
CA2694475C (en) 2015-07-28
WO2009010139A3 (de) 2009-03-12
AU2008278032A1 (en) 2009-01-22
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EA017585B1 (ru) 2013-01-30
IL203206A (en) 2015-03-31

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