| 摘要 |
Deoxy and oxygen-substituted sugar-containing 14-aminosteroid compounds and the pharmaceutically acceptable acid salts or esters thereof of general formula (I), wherein a) R1 is (i) COOR5, where R5 is a 1-6 carbon lower alkyl group; a 1-6 carbon lower alkyl group substituted by an amino group; an arylalkyl or heteroarylalkyl group or a carbocyclic ring, or (ii) CHR6OH, where R6 is a hydrogen atom or a 1-6 carbon lower alkyl group, or (iii) COR''', where R''' is hydrogen; 1-6 carbon lower alkyl; 1-6 carbon lower alkyl substituted amino; amino or dialkylamino, and b) R2 is -NR7R8; where R7 and R8, which may be the same or different, are hydrogen atoms or 1-6 carbon lower alkyl group, and c) R3 is (i) a deoxy or oxygen-substituted monosaccharide sugar residue, (II) wherein R9a, R9, R10, and R10a, which may be the same or different, are 1-6 carbon lower alkyl; hydrogen; hydroxy; fluorine; alkoxy; acetoxy; arylalkyloxy; or benzoxy; R11 is 1-6 carbon lower alkyl; hydrogen; hydroxy; fluorine ; benzoxy; arylalkyloxy; heteroarylalkyloxy; acetoxy or alkoxy; wherein further when R5 is 1-6 carbon lower alkyl; either R9, R10, or R11 cannot be hydroxy or acetoxy; further provided that when R9a is hydrogen and R10a is hydrogen and R9 is hydrogen; hydroxy or acetoxy; and R11 is hydroxy; acetoxy or alkoxy; R10 cannot be hydroxy or acetoxy; and R12 is methyl; acetoxymethyl or hydroxymethyl; t can be a single or double bond, or (ii) a deoxy or oxygen-substituted monosaccharide sugar residue, (III) wherein R11 is arylalkyloxy; heteroarylalkyloxy or 1-6 carbon lower alkyl substituted oxosilane and R12 is methyl, and d) R4 is (i) OH, or (ii) H, or (iii) OR13, where R13 is a monosaccharide sugar residue; acetoxy; benzoxy; arylalkyl or heteroarylalkyl, and e) Z is (i) -CH-, where a and b are single bonds, or (ii) =C, where either a or b is a double bond.
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