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501 条记录 (耗时 0.024 秒)

    Process for the preparation of 3-amino-pyrrolidine derivatives
    79.
    发明公开
    Process for the preparation of 3-amino-pyrrolidine derivatives 审中-公开
    Verfahren zur Herstellung von 3-Aminopyrrolidinderivaten

    公开(公告)号：EP1138672A1

    公开(公告)日：2001-10-04

    申请号：EP01114294.0

    申请日：1999-01-08

    申请人： Basilea Pharmaceutica AG

    发明人： Spurr, Paul ,  Wang, Shaoning ,  Klinkhammer, Uwe

    IPC分类号： C07D207/14

    CPC分类号： C07D501/00 ,  C07D207/14 ,  Y02P20/55

    摘要： The invention is concerned with a process for the manufacture of 3-amino-pyrrolidine derivatives of the formula
       wherein

    R 1 signifies hydrogen, alkyl, cyclo-alkyl, alkenyl, aryl or an amino protecting group; and
    R 2 , R 3 each independently signify hydrogen, alkyl, cyclo-alkyl, alkenyl or aryl;
    by converting a compound of the formula
    wherein

    X signifies a protected hydroxy group;
    in the presence of a primary amine of the formula R 1 NH 2 into the pyrrolidine derivative of the formula
       wherein X and R 1 have the aforementioned significances;
    which is subsequently reacted in the presence of R 2 R 3 NH under pressure.

    摘要翻译： 本发明涉及制备式CHEM的3-氨基 - 吡咯烷衍生物的方法，其中R 1表示氢，烷基，环烷基，烯基，芳基或氨基保护基; R 2，R 3各自独立地表示氢，烷基，环烷基，烯基或芳基; 通过转化式的化合物，其中X表示被保护的羟基; 在式R 1 NH 2的伯胺存在下进入式CHEM的吡咯烷衍生物，其中X和R 1具有上述含义; 其随后在R 2 R 3 NH的存在下在压力下反应。

    ACETAMIDE AND SUBSTITUTED ACETAMIDE-CONTAINING THIOUREA INHIBITORS OF HERPES VIRUSES
    80.
    发明公开
    ACETAMIDE AND SUBSTITUTED ACETAMIDE-CONTAINING THIOUREA INHIBITORS OF HERPES VIRUSES 审中-公开
    乙酰胺和取代的乙酰胺含硫脲ALS抑制剂疱疹病毒

    公开(公告)号：EP1137633A2

    公开(公告)日：2001-10-04

    申请号：EP99965132.6

    申请日：1999-12-06

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： BLOOM, Jonathan, David ,  DIGRANDI, Martin, Joseph ,  DUSHIN, Russell, George ,  LANG, Stanley, Albert ,  O'HARA, Bryan, Mark

    IPC分类号： C07C335/20 ,  C07D207/14 ,  C07D207/09 ,  C07D211/58 ,  C07D261/08 ,  A61K31/17 ,  A61K31/40 ,  A61K31/445 ,  A61K31/42

    CPC分类号： C07D261/10 ,  C07C335/20 ,  C07C335/22 ,  C07D207/09 ,  C07D207/14 ,  C07D211/58

    摘要： Compounds of formula (I) wherein R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, -CN, -NO2, -CO2R6, -COR6, -OR6, -SR6, -SOR6, -SO2R6, -CONR7R8, -NR6N(R7R8), -N(R7R8) or W-Y-(CH2)n-Z provided that at least one of R1-R5 is not hydrogen; or R2 and R3 or R3 and R4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl; R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or R7 and R8, taken together may form a 3 to 7 membered heterocycloalkyl; R9-R12 are independently hydrogen, alkyl of 1 to 4 carbon atoms, perhaloalkyl of 1 to 4 carbon atoms, halogen, alkoxy of 1 to 4 carbon atoms, or cyano, or R9 and R10 or R11 and R12 may be taken together to form aryl of 5 to 7 carbon atoms; G is alkyl of 1 to 6 carbon atoms; X is a bond, -NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 carbon atoms, or (CH)J; J is alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or benzyl; and n is an integer from 1 to 6; or pharmaceutical salts thereof, are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.