制备了一系列的单取代的嘧啶鎓和吡嗪鎓三氟甲磺酸酯和3,5-二取代的吡啶鎓三氟甲磺酸酯,并使用硫氧化作为模型反应,对过氧化氢的简单氧化催化剂进行了测试。它们的催化效率在很大程度上取决于取代基的类型,并且对于具有吸电子基团的衍生物而言是显着的,其反应性与黄酮盐相当,后者是氧合作用的主要有机催化剂。由于它们的高稳定性和良好的可及性,4-(三氟甲基)嘧啶鎓和3,5-二硝基吡啶鎓三氟甲磺酸盐是选择的催化剂,并显示出催化脂肪族和芳香族硫化物氧化为亚砜的作用,定量转化率高,制备产率高,并且具有优异的性能。化学选择性。K R +值(p K R + <5)和较小的负还原电位(E red > -0.5 V)。在催化氧化过程中原位形成的过氧化氢加合物充当底物氧化剂。通过在B3LYP / 6-311 ++ g(d,p)水平上的计算获得的从这些杂环氢过氧化物到硫代苯甲醚的转移的吉布斯自由能表明,它们是比烷基氢过氧化
[EN] TETRAHYDROBENZAZEPINES AS ANTAGONISTS AND/OR REVERSE AGONISTS OF THE HISTAMINE H 3 RECEPTOR<br/>[FR] TETRAHYDROBENZAZEPINES UTILISEES COMME ANTAGONISTES ET/OU AGONISTES INVERSES DU RECEPTEUR H3 DE L'HISTAMINE
申请人:GLAXO GROUP LTD
公开号:WO2006018260A1
公开(公告)日:2006-02-23
The present invention relates to novel benzazepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.
Heterobicyclic thiophene compounds and methods of use
申请人:Blake F. James
公开号:US20070197537A1
公开(公告)日:2007-08-23
Compounds of Formula I and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula I and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
This invention provides compositions of matter, pharmaceutical compounds, methods of synthesizing such compounds and methods for using such compounds to treat animals infected with a pathogenic mycobacterium. The invention specifically provides compositions and pharmaceutical compositions thereof for the treatment of tuberculosis and other Mycobacterium-caused diseases.
This invention provides compositions of matter, pharmaceutical compounds, methods of synthesizing such compounds and methods for using such compounds to treat animals infected with a pathogenic mycobacterium. The invention specifically provides compositions and pharmaceutical compositions thereof for the treatment of tuberculosis and other Mycobacterium-caused diseases.