利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

8 条记录 (耗时 0.023 秒)

    ANTIVIRAL PROTEASE INHIBITORS
    5.
    发明授权
    ANTIVIRAL PROTEASE INHIBITORS 失效
    抗病毒蛋白酶抑制剂

    公开(公告)号：EP1005493B1

    公开(公告)日：2005-11-02

    申请号：EP98915095.8

    申请日：1998-04-03

    申请人： MEDIVIR AB

    发明人： CLASSON, Björn ,  KVARNSTRÖM, Ingemar, Sven-Anders ,  SAMUELSSON, Bengt, Bertil

    IPC分类号： C07K14/81 ,  A61K38/55

    CPC分类号： C07D213/30 ,  C07C235/14 ,  C07C237/22 ,  C07C2601/02 ,  C07C2601/16 ,  C07C2602/08 ,  C07D213/40 ,  C07D277/24 ,  C07D309/10 ,  C07D333/16 ,  C07D405/12 ,  C07D407/12 ,  C07D493/04

    摘要： Compounds of formula (I), wherein A' and A'' are independently the same or different group of formula (II) wherein: R' is H, CH3, C(CH3)2, -OR?a, -N(Ra)¿2, -N(Ra)ORa or -DP; R''' is H or CH¿3; R?a is H, C¿1?-C3 alkyl; D is a bond, alkylene, -C(=O)-, -S(O)- or -S(O)2-; P is an optionally substituted, mono or bicyclic carbo- or heterocycle; R'' is H, any of the sidechains found in the natural amino acids, carboxacetamide, or a group (CH2)nDP; M is a bond or -C(=O)N(R''')-; Q is absent, a bond, -CH(OH)- or -CH2-; or R'' together with Q, M and R' define an optionally substituted 5 or 6 membered carbo- or heterocyclic ring which is optionally fused with a further 5 or 6 membered carbo- or heterocyclic ring; with the proviso that R' is -OR?a, -N(Ra)¿2, -N(Ra)ORa or -DP, if M is a bond and Q is absent; X is H, OH, OCH¿3?; Y is H, OH, OCH3, but X and Y are not both H; Z' and Z'' are independently -(CH2)mP where P is as defined above; n and m are independently 0, 1 or 2; and pharmaceutically acceptable salts and prodrugs thereof have utility as aspartyl protease inhibitors of HIV. They can be prepared in a facile two step synthesis from novel 2,5-di-O-benzyl-L-mannaro-1,4:6,3-dilactone intermediates.

    ANTIVIRAL PROTEASE INHIBITORS
    8.
    发明公开
    ANTIVIRAL PROTEASE INHIBITORS 失效
    抗病毒蛋白酶

    公开(公告)号：EP1005493A1

    公开(公告)日：2000-06-07

    申请号：EP98915095.8

    申请日：1998-04-03

    申请人： MEDIVIR AB

    发明人： CLASSON, Björn ,  KVARNSTRÖM, Ingemar, Sven-Anders ,  SAMUELSSON, Bengt, Bertil

    IPC分类号： C07K14/81 ,  A61K38/55

    CPC分类号： C07D213/30 ,  C07C235/14 ,  C07C237/22 ,  C07C2601/02 ,  C07C2601/16 ,  C07C2602/08 ,  C07D213/40 ,  C07D277/24 ,  C07D309/10 ,  C07D333/16 ,  C07D405/12 ,  C07D407/12 ,  C07D493/04

    摘要： Compounds of formula (I), wherein A' and A'' are independently the same or different group of formula (II) wherein: R' is H, CH3, C(CH3)2, -OR?a, -N(Ra)¿2, -N(Ra)ORa or -DP; R''' is H or CH¿3; R?a is H, C¿1?-C3 alkyl; D is a bond, alkylene, -C(=O)-, -S(O)- or -S(O)2-; P is an optionally substituted, mono or bicyclic carbo- or heterocycle; R'' is H, any of the sidechains found in the natural amino acids, carboxacetamide, or a group (CH2)nDP; M is a bond or -C(=O)N(R''')-; Q is absent, a bond, -CH(OH)- or -CH2-; or R'' together with Q, M and R' define an optionally substituted 5 or 6 membered carbo- or heterocyclic ring which is optionally fused with a further 5 or 6 membered carbo- or heterocyclic ring; with the proviso that R' is -OR?a, -N(Ra)¿2, -N(Ra)ORa or -DP, if M is a bond and Q is absent; X is H, OH, OCH¿3?; Y is H, OH, OCH3, but X and Y are not both H; Z' and Z'' are independently -(CH2)mP where P is as defined above; n and m are independently 0, 1 or 2; and pharmaceutically acceptable salts and prodrugs thereof have utility as aspartyl protease inhibitors of HIV. They can be prepared in a facile two step synthesis from novel 2,5-di-O-benzyl-L-mannaro-1,4:6,3-dilactone intermediates.

    摘要翻译： 式I的化合物：其中：A'和A“独立地是相同或不同的式II的基团：其中：R'是H，CH 3，C（CH 3）2，-OR a，-N（R a）2，-N（R a）OR a或-DP R“'是H或CH 3; R a是H，C 1 -C 3烷基; D是键，亚烷基，-C（= O） - ， - （O） - 或-S（O）2 - ; P是任选取代的单或双环碳 - 或杂环; R“是H，在天然氨基酸中发现的任何侧链，羧基乙酰胺或 一组（CH 2）n DP; M是键或-C（= O）N（R“'） - ; Q不存在，键，-CH（OH） - 或-CH 2 - ; 或R“连同Q，M和R'定义任选取代的5或6元碳环或杂环，其任选地与另外的5或6元碳 - 或杂环稠合;条件是R'为-OR a，-N（R a）2，-N（R a）OR a或-DP，如果M是键且Q不存在; X是H，OH，OCH 3; Y是H，OH，OCH 3， 但X和Y不同时为H; Z'和Z“独立地为 - （CH 2）m P，其中P如上定义; n和m独立地为0,1或2; 其药学上可接受的盐和前药具有作为HIV的天冬氨酰蛋白酶抑制剂的效用。 它们可以通过新的2,5-di-O-苄基-L-肉豆蔻-4,4：6,3-二酮中间体的容易的两步合成来制备。