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    Cyclohexapeptidyl amine compounds
    4.
    发明授权
    Cyclohexapeptidyl amine compounds 失效
    环己酰胺胺化合物

    公开(公告)号：US06268338B1

    公开(公告)日：2001-07-31

    申请号：US08055996

    申请日：1993-04-30

    申请人： James M. Balkovec ,  Frances Aileen Bouffard ,  James F. Dropinski ,  Robert A. Zambias

    发明人： James M. Balkovec ,  Frances Aileen Bouffard ,  James F. Dropinski ,  Robert A. Zambias

    IPC分类号： A61K3800

    CPC分类号： C07K7/56 ,  A61K38/00

    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 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.

    摘要翻译： 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。