New aminoacid derivs. with N-terminal aza-cyclic substit.

    公开(公告)号:DE4028741A1

    公开(公告)日:1991-03-28

    申请号:DE4028741

    申请日:1990-09-10

    Applicant: HOECHST AG

    Abstract: N-azacyclic-amino-diol derivs. of formula (I) and their physiologically acceptable salts are new: R1 = gp. of formula (II), (III) or (IV) R6 and R7 = H or (all opt. substd.) 1-21C aliphatic, 3-20C alicyclic, 4-20C alicyclic-aliphatic, 6-12C aromatic, 7-32C araliphatic etc. R7 can also be NH2, OH or (all opt. substd.) mono- or di(1-4C) alkylamino, 6-12C arylsulphonyl or carbamoyl etc. R8 is as for R6 or R7; R9 = H, 1-8C alkyl, 3-8C cycloalkyl (1-4C) alkyl 7-13C aralkyl, etc. R10, R11 and R12 = H or 1-6C alkyl, or R10 + R11 = 2-4C alkandiyl; m and n = 0-3; n and p = 1-4; X = CO, CS, SO2 or SO; Y = (CH2)q-(CR13R14)r, O or S; q = 0-3; r = 0-2; Z = 1-6C opt. branched aliphatic; R13 and R14 = H or 1-6C alkyl; R2 = H, 6-12C aryl, 3-8C cycloalkyl, heteroaryl or heteroaryl (1-4C)alkyl; (hetero)aryl gps. can be substd. by 1 or 2 of halo, OH, 1-4C alkoxy, NH2 (opt. substd. by 1 or 2 1-4C alkyl), CF3 or 1-4C alkyl; R3 = 3-8C cycloalkyl (1-4C) alkyl, or 6-12C aryl (1-4C) alkyl, etc. R4 = 6-12C aryl, 6-12C aryl (1-4C) alkyl, OH or NH2; R5 (CH2)5-CHR15-Het; R15 = H, 1-7C alkyl, OH, N3 or halo; Het = 5-7 membered heterocycle which can be benzo-fused, aromatic or (partly) hydrogenated, contg. 1 or 2 of N, O, S, NO, SO or SO2 as heteroatoms and opt. substd. by 1 or 2 of 1-4C alkyl or alkoxy, allyl, OH, halo, NH2 (opt. substd. by 1 or 2 1-4C alkyl) or CF3; S = 0-4; B = residue of the amino acid H-B-OH, most esp. His or norvaline.

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