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20 条记录 (耗时 0.093 秒)

    Amino-substituted compounds useful as inhibitors of IMPDH enzyme
    9.
    发明授权
    Amino-substituted compounds useful as inhibitors of IMPDH enzyme 有权
    可用作IMPDH酶抑制剂的氨基取代的化合物

    公开(公告)号：US06617323B2

    公开(公告)日：2003-09-09

    申请号：US10155274

    申请日：2002-05-23

    申请人： Edwin J. Iwanowicz ,  Katerina Leftheris ,  Chunjian Liu ,  Toomas Mitt ,  Scott H. Watterson

    发明人： Edwin J. Iwanowicz ,  Katerina Leftheris ,  Chunjian Liu ,  Toomas Mitt ,  Scott H. Watterson

    IPC分类号： A61K31535

    CPC分类号： C07D413/12 ,  C07D263/32

    摘要： The present invention discloses compounds useful in treating or preventing IMPDH-associated disorders, such as transplant rejection and autoimmune diseases, having the formula (I), wherein X is —C(O)—, —C(S)—, or —S(O)2—; A is an optionally-substituted saturated or unsaturated monocyclic or bicyclic ring; B is a saturated or unsaturated monocyclic or bicyclic ring system having at least one substituent Q which is selected from R7 and R8; R7 is selected from (C0-C6)alkyl, (C2-C6)alkenyl and (C2-C6)alkynyl and R7 is substituted with R8 is selected from (C0-C6)alkyl, (C2-C6)alkenyl and (C2-C6)alkynyl and R8 is substituted with and Z1 through Z5 are as defined in the specification.

    摘要翻译： 本发明公开了可用于治疗或预防具有式（I）的IMPDH相关疾病如移植排斥反应和自身免疫性疾病的化合物，其中X是-C（O） - ， - C（S） - 或-S （O）2 - ; A是任选取代的饱和或不饱和单环或双环; B是具有至少一个选自R7和R8的取代基Q的饱和或不饱和单环或双环体系; R 7选自（C 0 -C 6）烷基，（C 2 -C 6）烯基和（C 2 -C 6）炔基，R 7被R 8取代为（C 0 -C 6）烷基，（C 2 -C 6）烯基和（C 2 -C 6 ）炔基和R8被Z取代，Z 1至Z 5如说明书中所定义。

    Inhibitors of farnesyl protein transferase
    10.
    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