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Pochodne piperydynowe i piperazynowe do leczenia nowotworów
专利权人:
Merck Patent GmbH
发明人:
SCHIEMANN, KAI,SCHULTZ, MELANIE,BLAUKAT, ANDREE,KOBER, INGO
申请号:
PL11007349
公开号:
PL2426106T3
申请日:
2008.09.19
申请国别(地区):
PL
年份:
2013
代理人:
摘要:
Substituted piperidine- and piperazine compounds (I), and their tautomers, salts or stereoisomers, including their mixtures in all ratios, are new. Substituted piperidine- and piperazine compounds of formula (I), and their tautomers, salts or stereoisomers, including their mixtures in all ratios, are new. R 1>; : binuclear unsaturated or aromatic heterocycle with 1-4 N-, O- and/or S atoms (unsubstituted or 1-3 times substituted by A, hal, NR 2, (CR 2) nCN, OR 5>;and/or =O); D 1>; : C or S; G : N or C; either R 2>; : absent (when G is N) or H or Ar 2>;(when G is C); or CR 2>;+R 2>;, (E-W 1>;)R 2>;+R 2>; : spirocyclic ring of 3H-isobenzofuran-1-one-3,3-diyl, chroman-3-one-2,2-diyl, substituted oxazolidin-2-one moiety of formula (a) or imidazolidine-2,4-dione-5,5-diyl; Q : optionally branched 1-4C alkylene, where 1-5 H atoms are substituted by A, (CR 2) n[X(CR 2) n] p-Y 1>;, F and/or Cl; R 3>; : H, A, Ar 1>;, OR, SR, NR 2, hal, NO 2, CN or (CR 2) n[X(CR 2) n] p-Y 1>;; X : O, NR or CR 2; Y 1>; : OR or NR 2; R 5>; : H or optionally branched 1-6C alkyl, where 1-7 H atoms are substituted by F and/or Cl; E : COO(CR 2) n, COO(CRR 4>;), CO(CR 2) mO, CONH(CR 2) n, C(=S)NH(CR 2) n, S(O) qNH(CR 2) n, S(O) q(CR 2) n, CO(CR 2) n, (CR 2) n, CO(CR 2) mO(CR 2) n, CO(CR 2) mNH(CR 2) n, CO(CH 2) nCO, COCHR 6>;CHR 7>;, C(=S)O(CR 2) n, CO(CRR 4>;)(CR 2) n, COO(CRR 4>;), (CRR 4>;)(CR 2) n, S(O) qCR=CR, COCR=CR, (CR 2) mCO, CONH(CR 2) mCRR 4>;or (CR 2) mCONR; R 4>; : COOR 5>;, Ar 2>;, (CR 2) nNR 2, OH, NRCOOR 8>;or NRCOOA; R 6>;R 7>; : (CH 2) 1 - 4; R 8>; : phenyl, naphthyl or fluorenyl; R : H or optionally branched 1-6C alkyl; W 1>; : Ar 1>;or Het; Ar 1>; : phenyl, indanyl, naphthyl or biphenyl (unsubstituted or 1-3 times substituted by hal, A, (CR 2) nOR, O(CR 2) n, Ar 2>;, (CR 2) nNR 2, SR, NO 2, CN, COOR, CONR 2, NRCOA, NRSO 2A, SO 2NR 2, S(O) qA, CO-Het, (CR 2) nHet, O(CR 2) nNR 2, O(CR 2) nHet, NHCOOA, NHCONR 2, NHCO
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