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AR074493A1 - Derivados de quinazolinamida - Google Patents

Derivados de quinazolinamida

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Publication number
AR074493A1
AR074493A1 ARP090104724A ARP090104724A AR074493A1 AR 074493 A1 AR074493 A1 AR 074493A1 AR P090104724 A ARP090104724 A AR P090104724A AR P090104724 A ARP090104724 A AR P090104724A AR 074493 A1 AR074493 A1 AR 074493A1
Authority
AR
Argentina
Prior art keywords
conh
hal
mono
ncooa
ncooh
Prior art date
Application number
ARP090104724A
Other languages
English (en)
Inventor
Hans-Michael Eggenweiler
Christian Sirrenberg
Hans-Peter Buchstaller
Original Assignee
Merck Patent Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR074493A1 publication Critical patent/AR074493A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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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
    • C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D403/14—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 three or more hetero rings

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Abstract

Los nuevos derivados de quinazolinamida de la fórmula (1) en donde R1 es H, (CH2)nHet, (CH2)nAr, Hal o A, R2, R3 son en cada caso, de modo independiente entre sí, H, (CH2)nHet, (CH2)nAr, Hal OH u OA, R4, R5 son en cada caso, de modo independiente entre sí, H, A, (CH2)nHet, (CH2)nAr, o (CH2)pOC(=O)(CH2)pNH2, R4 y R5 junto con el átomo de N al que están unidos también son un heterociclo mono- o bicíclico saturado, insaturado o aromático no sustituido o mono-, di- o trisustituido con Hal, A, (CH2)nOH, (CH2)nOA, (CH2)nNH2, (CH2)nCOOH, (CH2)nCOOA, NHCOA, NA'COA, CONH2, CONHA CONAA', OC(=O)(CH2)pNH2 y/u =O (oxigeno del carbonilo), que puede contener otros 1 a 3 átomos de N, O y/o S y en donde también un átomo de N puede estar oxidado, X es CO o SO2, 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)nNHSO2A, SO2NH(CH2)nNH2, SO2NH2, SO2NHA, SO2NAA', CONH(CH2)nCOOA, CONH(CH2)nCOOH, NHCO(CH2)nCOOA, NHCO(CH2)nCOOH, CONH(CH2)nNH2, CONH(CH2)nNHA, CONH(CH2)nNAA', CONH(CH2)nCN y/o (CH2)nCH(NH2)COOH, 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 A, OA, OH, fenilo, SH, S(O)mA, Hal, NO2, CN, COA, COOA, COObencilo, CONH2, CONHA, CONAA', SO2NH2, NH2, NHA, NAA', NHCOA, NHSO2A y/u =O (oxigeno del carbonilo), A, A' son en cada caso, 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, NMe o NEt y/o también 1-5 átomos de H pueden estar reemplazados por F y/o CI, o alquilo cíclico C3-8, n es 0, 1, 2, 3 o 4, p es 1, 2, 3 o 4, así como sus sales y estereoisómeros farmacéuticamente aceptables, 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 inhibición, la regulación y/o la modulación de la HSP90 desempena, un papel importante.
ARP090104724A 2008-12-09 2009-12-07 Derivados de quinazolinamida AR074493A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102008061214A DE102008061214A1 (de) 2008-12-09 2008-12-09 Chinazolinamidderivate

Publications (1)

Publication Number Publication Date
AR074493A1 true AR074493A1 (es) 2011-01-19

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US (1) US8546565B2 (es)
EP (1) EP2356110B1 (es)
JP (1) JP5749653B2 (es)
KR (1) KR20110098772A (es)
CN (1) CN102245596A (es)
AR (1) AR074493A1 (es)
AU (1) AU2009326602B2 (es)
BR (1) BRPI0922652A2 (es)
CA (1) CA2745988C (es)
DE (1) DE102008061214A1 (es)
EA (1) EA201100872A1 (es)
ES (1) ES2564815T3 (es)
IL (1) IL213424A (es)
MX (1) MX2011005986A (es)
SG (1) SG171902A1 (es)
WO (1) WO2010066324A1 (es)
ZA (1) ZA201105050B (es)

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AU2009326602A1 (en) 2011-07-28
CA2745988C (en) 2017-02-28
DE102008061214A1 (de) 2010-06-10
CA2745988A1 (en) 2010-06-17
IL213424A (en) 2014-03-31
KR20110098772A (ko) 2011-09-01
AU2009326602B2 (en) 2015-12-17
EA201100872A1 (ru) 2012-01-30
SG171902A1 (en) 2011-07-28
ZA201105050B (en) 2012-03-28
MX2011005986A (es) 2011-06-27
WO2010066324A1 (de) 2010-06-17
US8546565B2 (en) 2013-10-01
IL213424A0 (en) 2011-07-31
US20110245225A1 (en) 2011-10-06
EP2356110B1 (de) 2016-01-06
CN102245596A (zh) 2011-11-16
JP2012511520A (ja) 2012-05-24
JP5749653B2 (ja) 2015-07-15

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