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    • 5. 发明授权
    • Cyclohexapeptidyl amine compounds
    • 环己酰胺胺化合物
    • US06268338B1
    • 2001-07-31
    • US08055996
    • 1993-04-30
    • James M. BalkovecFrances Aileen BouffardJames F. DropinskiRobert A. Zambias
    • James M. BalkovecFrances Aileen BouffardJames F. DropinskiRobert A. Zambias
    • A61K3800
    • C07K7/56A61K38/00
    • 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 is wherein Ra is C1-C10 alkyl; or (CH2)qNRbRc wherein Rb and Rc are independently H, C1-C10 alkyl or Rb and Rc taken together are wherein Rd 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 COX wherein X 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 salt each 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 and q is an integer from 2 to 4, inclusive.
    • 公开了下式:或其酸加成盐的环己酰胺化合物,其中:R1是H或OH; R2是H或OH; R3是QCnH2nNRVRVI,QCnH2nNRVRVIRVII + Y-或Q(CH2)1-3CRVIIIRIXNHRX.R4是H 或OH; R 5是H,OH或CH 3; R 6是H或CH 3; R 1是其中R a是C 1 -C 10烷基; 或(CH 2)q NR b R c其中R b和R c独立地为H,C 1 -C 10烷基或R b和R c在一起,其中R 1为C 1 -C 16烷基,苯基或苄基; R II为H,C 1-4烷基或苄基; R III为H,Cl -4-烷基或苄基; RIV是RII和RIII,一起作为 - (CH 2)4 - 或 - (CH 2)5 - ; RV是H,C 1 -C 4烷基或苄基; R VI是H,C 1 -C 4烷基或苄基或 RV和RVI一起是 - (CH 2)4 - 或 - (CH 2)5; RVII是H或C 1 -C 4烷基; RVIII是H,(CH 2)m H,(CH 2)m OH,(CH 2)m NH 2或COX,其中X是NH 2 ,OH或O(CH 2)m H; RIX为H,(CH 2)m H或与RVIII一起为=((羰基)); RX为H(除非当RVIII和RIX为H时,C(= NH)NH 2,C( = NH)CH 2)0-3H,CO(CH 2)0-3H,CO(CH 2)m NH 2,(CH 2)2-4 OH或(CH 2)2-4 NH 2; Q为O或S; Y为药学上阴离子 可接受的salteach m独立地为1〜3的整数,包括0和n; n为2〜4的整数,p为2〜4的整数,q为2〜4的整数。