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    Inhibitors of farnesyl protein transferase
    1.
    发明授权
    Inhibitors of farnesyl protein transferase 失效

    公开(公告)号：US06455523B1

    公开(公告)日：2002-09-24

    申请号：US09374210

    申请日：1999-08-13

    申请人： Charles Z. Ding ,  Soong-Hoon Kim ,  John T. Hunt ,  Toomas Mitt ,  Rajeev Bhide ,  Katerina Leftheris

    发明人： Charles Z. Ding ,  Soong-Hoon Kim ,  John T. Hunt ,  Toomas Mitt ,  Rajeev Bhide ,  Katerina Leftheris

    IPC分类号： A61K3155

    CPC分类号： C07D243/14 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00 ,  C07D487/04 ,  C07D495/04

    摘要： Inhibition of farnesyl transferase, which is an enzyme involved in ras ocogene expression, is effected by compounds of the formulas their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs and solvates thereof inhibit farnesyl protein transferase which is an enzyme involved in ras oncogene expression. In formulas I-IV and throughout their specification, the above symbols are defined as follows: m, n, r, s and t are 0 or 1; p is 0, 1 or 2; V, W and X are selected from the group consisting of oxygen, hydrogen, R1, R2 or R3; Z and Y are selected from the group consisting of CHR9, SO2, SO3, CO, CO2, O, NR10, So2NR11, CONR12, or Z may be absent; R6, R7, R9, R10, R11, R12 R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R24, R25, R26, R27, R28, R29, R30, R31, R32,R33, R34, R35, R36, R37, and R38 are selected from the group consisting of hydrogen, lower alkyl, substituted alkyl, aryl or substituted aryl; R4, R5 are selected from the group consisting of hydrogen, halo, nitro, cyano and U-R23; U is selected from the group consisting of sulfur, oxygen, NR24, CO, SO, SO2, CO2, NR25CO2, NR26CONR27, NR28SO2, NR29SO2NR30, SO2NR31, NR32CO, CONR33, PO2R34 and PO3R35 or U is absent; R1, R2, and R3 are selected from the group consisting of hydrogen, alkyl, alkoxycarbonyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aralkyl, cycloalkyl, aryl, substituted aryl, heterocyclo, substituted heterocyclo, cyano, carboxy, carbamyl (e.g. CONH2) or substituted carbamyl further selected from CONH alkyl, CONH aryl, CONH aralkyl or cases where there are two substituents on the nitrogen selected from alkyl, aryl or aralkyl; R8 and R23 are selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aralkyl, cycloalkyl, aryl, substituted aryl, heterocyclo, substituted heterocyclo; Any two of R1, R2, and R3 can be joined to form a cycloalkyl group; R, S and T are selected from the group consisting of CH2, CO and CH(CH2)pQ wherein Q is NR36R37, OR38, or CN; and A, B, C and D are carbon, oxygen, sulfur or nitrogen. with the provisos that 1. When m is zero then V and W are not both oxygen or 2 W and X together can be oxygen only if Z is either absent, O, NR10, in formulas I and II, and V and X together can be oxygen only if Y is O, NR10, in formulas III and IV or 3. R23 may be hydrogen except when U is SO, SO2, NR25CO2 or NR28SO2, or 4. R8 may be hydrogen except when Z is SO2, CO2, or

    1,2,5-benzothiadiazepine-1,1-dioxides with n-2 imidazolylalkyl substituents
    5.
    发明授权
    1,2,5-benzothiadiazepine-1,1-dioxides with n-2 imidazolylalkyl substituents 有权
    具有n-2个咪唑基烷基取代基的1,2,5-苯并噻二氮杂-1,1-二氧化物

    公开(公告)号：US6156746A

    公开(公告)日：2000-12-05

    申请号：US354038

    申请日：1999-07-15

    申请人： Katerina Leftheris ,  John T. Hunt ,  Charles Z. Ding

    发明人： Katerina Leftheris ,  John T. Hunt ,  Charles Z. Ding

    IPC分类号： C07D417/06 ,  A61K31/551 ,  C07D419/14

    CPC分类号： C07D417/06

    摘要： Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formula ##STR1## and their enantiomers, diastereomers, and their pharmaceutically acceptable salts, including prodrugs and solvates thereof.The compounds of formula I are useful in the treatment of a variety of cancers. In addition, the formula I compounds may also be useful in the treatment of diseases other than cancer.

    摘要翻译： 抑制参与ras癌基因表达的酶的法呢基转移酶由下式的化合物及其对映异构体，非对映异构体及其药学上可接受的盐包括其前体药物和溶剂化物来实现。 式I化合物可用于治疗各种癌症。 此外，式I化合物还可用于治疗除癌症以外的疾病。