| 摘要 |
Cyclohexapeptidyl amine compounds are disclosed of the formula:or its acid addition salt,wherein:R1 is H or OH;R2 is H or OH;R3 is QCnH2nNRVRVI, QCnH2nNRVRVIRVII+Y-, or Q(CH2)1-3CRVIIIRIXNHRX.R4 is H or OH;R5 is H, OH or CH3;R6 is H or CH3;RI iswhereinRa is C1-C10 alkyl; or(CH2)qNRbRc wherein Rb and Rc are independently H, C1-C10 alkyl or Rb and Rc taken together arewhereinRd is C1-C16 alkyl, phenyl or benzyl;RII is H, C1-4 alkyl or benzyl;RIII is H, C1-4 alkyl or benzyl;RIV is RII and RIII taken together as -(CH2)4- or -(CH2)5-;RV is H, C1-C4 alkyl or benzyl;RVI is H, C1-C4 alkyl or benzyl or RV and RVI together is -(CH2)4- or -(CH2)5-;RVII is H or C1-C4 alkyl;RVIII is H, (CH2)mH, (CH2)mOH, (CH2)mNH2 or COXwhereinX is NH2, OH or O(CH2)mH;RIX is H, (CH2)mH, or together with RVIII is =O (carbonyl);RX is H (except when RVIII and RIX are H, C(=NH)NH2, C(=NH)CH2)0-3H, CO(CH2)0-3H, CO(CH2)mNH2, (CH2)2-4OH or (CH2)2-4NH2;Q is O or S;Y is an anion of a pharmaceutically acceptable salteach m is independently an integer from 1 to 3, inclusive;n is an integer from 2 to 4, inclusive;p is an integer from 1 to 2, inclusive andq is an integer from 2 to 4, inclusive. |
