| 摘要 |
Modified aminoacids of formula RC(=O)ZC(R11)((C=O)m(CH2)nR2)C(=X)ANR3R4 (I), their tautomers, diastereomers, enantiomers, mixtures and salts are new. R = 1-7C n-alkyl (optionally w-substituted), 1-6C n-alkylamino (optionally N-substituted) etc.; X = O or H; Z = CH2 or NR1; R1 = H, alkyl or phenylalkyl; R11 = H, 1-3C alkyl, 2-4C alkoxycarbonyl or benzyl; n = 1 or 2, or may be 0 if m = 1; m = 0 or 1; R2 = Ph, 1- or 2- naphthyl, 1,2,3,4-tetrahydro-1-naphthyl, 1H-indol-3-yl, 1-(methyl, formyl or t-butoxycarbonyl)-1H-indol-3-yl, 4-imidazolyl etc. (all optionally C-substituted); A = a direct bond or NR8CHR9CO; R8+R9 = (CH2)3; or R8 = H, alkyl or phenylalkyl; R9 = H or 1-5C alkyl, optionally w substituted if unbranched; R3 = H, 1-7C alkyl (optionally w-substituted) or phenyl or pyridinyl (optionally C-substituted); R4 = H or 1-3C alkyl (optionally substituted by Ph or pyridinyl).
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| 申请人 |
BOEHRINGER INGELHEIM PHARMA KG, 55218 INGELHEIM, DE |
发明人 |
RUDOLF, KLAUS, DIPL.-CHEM. DR., 88400 BIBERACH, DE;EBERLEIN, WOLFGANG, DIPL.-CHEM. DR., 88400 BIBERACH, DE;ENGEL, WOLFHARD, DIPL.-CHEM. DR., 88400 BIBERACH, DE;PIEPER, HELMUT, DIPL.-CHEM. DR., 88400 BIBERACH, DE;DOODS, HENRI, DR., 88447 WARTHAUSEN, DE;HALLERMAYER, GERHARD, DR., 88437 MASELHEIM, DE;ENTZEROTH, MICHAEL, DIPL.-CHEM. DR., 88447 WARTHAUSEN, DE;WIENEN, WOLFGANG, DIPL.-BIOL. DR., 88400 BIBERACH, DE |
