发明名称 Piperidine and piperazine derivatives
摘要 Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in Claim (1), can and be employed for the treatment of tumors.
申请公布号 US8791111(B2) 申请公布日期 2014.07.29
申请号 US200812681440 申请日期 2008.09.19
申请人 Merck Patent GmbH 发明人 Schiemann Kai;Schultz Melanie;Blaukat Andree;Kober Ingo
分类号 A61K31/535;A61K31/497;C07D403/06;C07D413/06 主分类号 A61K31/535
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 denotes which is optionally mono- or disubstituted by A, Hal, NR2, (CR2)nCN and/or OR5, D denotes C or S, G denotes N, R2 is absent, Q denotes unbranched or branched alkylene having 1, 2, 3 or 4 C atoms, in which 1-5 H atoms may be replaced by A, (CR2)n[X(CR2)n]p—Y, F and/or Cl, R3 denotes H, A, Ar, OR, SR, NR2, Hal, NO2, CN or (CR2)n[X(CR2)n]p—Y, X denotes O, NR or CR2, Y denotes OR or NR2, R5 denotes H or unbranched or branched alkyl having 1, 2, 3, 4, 5 or 6 C atoms, in which 1-7 H atoms may be replaced by F and/or Cl, E denotes COO(CR2)n, COO(CRR4), CO(CR2)mO, CONH(CR2)n, C(═S)NH(CR2)n, S(O)qNH(CR2)n, S(O)q(CR2)n, COCH2CH2, CO(CR2)mO(CR2)n, CO(CR2)mNH(CR2)n, CO(CH2)nCO, COCHR6CHR7, C(═S)O(CR2)n, CO(CRR4)(CR2)n, COO(CRR4), (CRR4)(CR2)n, S(O)qCR═CR, COCR═CR, CONH(CR2)mCRR4 or (CR2)mCONR, R4 denotes COOR5, Ar1, NRCOOR8, (CR2)nNR2 or NRCOOA, R6,R7 together denote (CH2)1-4, R8 denotes phenyl, naphthyl or fluorenyl, R denotes H or unbranched or branched alkyl having 1, 2, 3, 4, 5 or 6 C atoms, W denotes Ar or Het, Ar denotes phenyl, indanyl, naphthyl or biphenyl, each of which is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted by Hal, A, (CR2)nOR, O(CR2)n, Ar1, (CR2)nNR2, SR, NO2, CN, COOR, CONR2, NRCOA, NRSO2A, SO2NR2, S(O)qA, CO-Het, (CR2)nHet, O(CR2)nNR2, O(CR2)nHet, NHCOOA, NHCONR2, NHCOO(CR2)nNR2, NHCOO(CR2)nHet, CR5═CR5Ar1, SO2Het, NHCONH(CR2)nNR2, NHCONH(CR2)nHet, OCONH(CR2)nNR2, OCONH(CR2)nHet, CONR(CR2)nNR2, CONR(CR2)nHet and/or COA, Het denotes a mono-, bi- or tricyclic 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 Hal, A, (CR2)nAr1, O(CR2)nAr1, (CR2)nOR, (CR2)nNR2, SR, NO2, CN, COOR, CONR2, NRCOA, NRSO2A, SO2NR2, S(O)qA, CO-Het1, (CR2)nHet1, O(CR2)nNR2, O(CR2)nHet1, NHCOOA, NHCONR2, NHCOO(CR2)nNR2, NHCOO(CR2)n-Het1, NHCONH(CR2)nNR2, NHCONH(CR2)nHet1, OCONH(CR2)nNR2, OCONH(CR2)nHet1, CO-Het1, CHO, COA, ═S, ═NH, ═NA and/or ═O (carbonyl oxygen), Het1 denotes a monocyclic saturated heterocycle having 1 to 2 N and/or O atoms, which may be mono- or disubstituted by A, OA, OH, Hal and/or ═O (carbonyl oxygen), Ar1 denotes phenyl which is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted by Hal, CN, A and/or (CR2)nOR, A denotes unbranched or branched alkyl having 1-10 C atoms, in which 1-7 H atoms may be replaced by OR, CN, NR2, F and/or Cl and/or in which one or two non-adjacent CH2 groups may be replaced by O, NH, S, SO, SO2 and/or by CH═CH groups, orcyclic alkyl having 3-7 C atoms, m denotes 1, 2, 3, 4, 5 or 6, n denotes 0, 1, 2, 3, 4, 5, 6, 7 or 8, p denotes 1, 2, 3, 4, 5 or 6, q denotes 0, 1 or 2, and Hal denotes F, Cl, Br or I, or a pharmaceutically acceptable tautomer, salt or stereoisomer thereof.
地址 Darmstadt DE