Pentafulvene synthesis
    9.
    发明授权
    Pentafulvene synthesis 失效
    五萜烯合成

    公开(公告)号:US6025512A

    公开(公告)日:2000-02-15

    申请号:US226404

    申请日:1999-01-06

    IPC分类号: C07C13/15 C07F17/00 C07F2/00

    CPC分类号: C07C13/15 C07C2101/10

    摘要: This invention relates to a method to produce pentfulvenes comprising combining a partially substituted cyclopentadiene with a carbonyl containing compound and lithium or an alkyl lithium, wherein the partially substituted cyclopentadiene is represented by the formula: ##STR1## wherein the R.sup.1 to R.sup.5 groups are independently hydrogen or a C.sub.1 to C.sub.100 group, provided at least one R group is hydrogen but not more than three R groups are hydrogen.

    摘要翻译: 本发明涉及一种生产pentfulvenes的方法,包括将部分取代的环戊二烯与含羰基化合物和锂或烷基锂组合,其中部分取代的环戊二烯由下式表示:其中R1至R5基团独立地为氢或C1 至C100基团,提供至少一个R基团为氢,但不超过三个R基团为氢。

    Selective thrombin inhibitors
    10.
    发明授权
    Selective thrombin inhibitors 失效
    选择性凝血酶抑制剂

    公开(公告)号:US5985899A

    公开(公告)日:1999-11-16

    申请号:US967661

    申请日:1997-11-10

    摘要: The present invention relates to a novel selective thrombin inhibitor having the following formula (I), which is also effective by oral administration: ##STR1## in which R.sup.1 represents acetyl substituted with aryl or aryloxy, or represents sulfonyl substituted with substituted or unsubstituted aryl or N-containing heterocyclic group,X represents a group of formula ##STR2## R.sup.2 and R.sup.3 independently of one another represent hydrogen; cycloalkyl substituted or unsubstituted with carboxyl or alkoxycarbonyl; arylalkyloxy; hydroxy; or lower alkyl substituted or unsubstituted with carboxyl, alkoxycarbonyl or hydroxy, orR.sup.2 and R.sup.3 together with nitrogen atom to which they are attached can form a piperidine group substituted with carboxyl or alkoxycarbonyl,R.sup.4 represents hydrogen, lower alkyl or lower alkoxy,R.sup.5 represents alkanesulfonyl; alkoxycarbonyl; alkylcarbonyl; formyl; lower alkyl; aryl substituted or unsubstituted with alkoxy or haloalkyl; or hydroxy-substituted lower alkyl, andR.sup.6 and R.sup.7 independently of one another represent hydrogen, lower alkyl or amino,and to a process for preparation thereof and a pharmaceutical composition for thrombin inhibition which comprises the compound of formula (I) as an active ingredient.

    摘要翻译: 本发明涉及一种新型的具有下列通式(I)的选择性凝血酶抑制剂,其也可通过口服给药有效:其中R1表示被芳基或芳氧基取代的乙酰基,或表示被取代或未取代的芳基或含N 杂环基,X表示式R 2的基团,R 3彼此独立地表示氢; 被羧基或烷氧基羰基取代或未取代的环烷基; 芳基烷氧基; 羟基; 或与羧基,烷氧基羰基或羟基取代或未取代的低级烷基,或R 2和R 3与它们所连接的氮原子一起形成被羧基或烷氧基羰基取代的哌啶基,R 4表示氢,低级烷基或低级烷氧基,R 5表示烷磺酰基 ; 烷氧基羰基 烷基羰基; 甲酰基 低级烷基 被烷氧基或卤代烷基取代或未取代的芳基; 或羟基取代的低级烷基,R 6和R 7彼此独立地表示氢,低级烷基或氨基,以及其制备方法和用于凝血酶抑制的药物组合物,其包含式(I)化合物作为活性成分 。