发明名称 Quinazoline derivatives
摘要 Novel quinazolinamide derivatives of the formula (I), in which R1-R4 and X have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
申请公布号 US8906930(B2) 申请公布日期 2014.12.09
申请号 US201013511218 申请日期 2010.10.26
申请人 Merck Patent GmbH 发明人 Eggenweiler Hans Michael;Sirrenberg Christian;Buchstaller Hans Peter
分类号 A01N43/54;A61K31/517;C07D239/72;C07D401/00 主分类号 A01N43/54
代理机构 Millen, White, Zelano & Branigan, P.C. 代理人 Millen, White, Zelano & Branigan, P.C.
主权项 1. A compound of formula I in which R1, R2 each, independently of one another, denote H, A, (CH2)nHet or (CH2)nAr, R1 and R2, together with the N atom to which they are bonded, also denote a saturated, unsaturated or aromatic mono- or bicyclic heterocycle, which may contain a further 1 to 3 N, O and/or S atoms and which is unsubstituted or mono-, di- or trisubstituted by Hal, A, (CH2)nHet, (CH2)nAr, (CH2)nOH, (CH2)nOA, (CH2)nNH2, (CH2)nCOOH, (CH2)nCOOA, NHCOA, NA′COA, CONH2, CONHA, CONAA′, OC(═O)(CH2)pNH2 and/or ═O (carbonyl oxygen), R3 and R4, together with the C atom to which they are bonded, denote a saturated or unsaturated monocyclic C3-C10-carbocycle, which may contain a further 1 to 3 N, O and/or S atoms and which is unsubstituted or mono-, di- or trisubstituted by Hal, A, (CH2)nOH, (CH2)nOA, (CH2)nNH2, (CH2)nCOOH, (CH2)nCOOA, NHCOA, NA′COA, CONH2, CONHA, CONAA′, OC(═O)(CH2)pNH2 and/or ═O (carbonyl oxygen), X denotes NR5R6, CONR5R6, CH2NR5R6, COOR5, —OR5, CH2OR5, COHet, Het, CONH(CH2)pCN or CONH(CH2)pNR5R6, R5, R6 each, independently of one another, denote H, A, (CH2)nHet or (CH2)nAr, Ar denotes phenyl, naphthyl, tetrahydronaphthyl or biphenyl, each of which is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted by 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 and/or (CH2)nCH(NH2)COOH, Het denotes a mono- or bicyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono-, di- or trisubstituted by A, OA, OH, phenyl, SH, S(O)mA, Hal, NO2, CN, COA, COOA, COObenzyl, CONH2, CONHA, CONAA′, SO2NH2, NH2, NHA, NAA′, NHCOA, NHSO2A and/or ═O (carbonyl oxygen), A, A′ each, independently of one another, denote unbranched or branched alkyl having 1-10 C atoms, in which 1-3 non-adjacent CH2 groups may be replaced by O, S, SO, SO2, NH, NMe or Net, and/or, in addition, 1-5 H atoms may be replaced by F and/or Cl, or cyclic alkyl having 3-8 C atoms, Hal denotes F, Cl, Br or I, n denotes 0, 1, 2, 3 or 4, p denotes 1, 2, 3 or 4, or pharmaceutically usable salts, tautomers or stereoisomers thereof, including mixtures thereof in all ratios.
地址 Darmstadt DE