The present invention provides compounds which specifically inhibit FXa, which are effective when orally administered and which are useful as a safe medicine for the prevention or treatment of diseases caused by thrombus or infarction.
Compounds of this invention are piperazinones of the formula:
wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, in addition to being substituted by the group of the formula:
and the group of the formula:
Y is an optionally substituted divalent hydrocarbon group or an optionally substituted divalent heterocyclic group; X is a direct bond or an optionally substituted alkylene chain; Z is (1) an amino group substituted with an optionally substituted hydrocarbon group, (2) an optionally substituted imino group or (3) an optionally substituted nitrogen-containing heterocyclic group; provided that when X is a direct bond and Z is an optionally substituted 6-membered nitrogen-containing aromatic heterocyclic group, Y is an optionally substituted divalent hydrocarbon group or an optionally substituted divalent unsaturated heterocyclic group; or a salt thereof.
The POM-templated MOF of 1 exhibits strong chemical stability that can withstand aqueous solutions of various pH-values (2–10). Particularly, 1 possesses excellent photodegradation activity and recyclability towards the organic dyes of Crystal Violet (CV) and Basic Red 2 in aqueous solutions with different pH values.
以Keggin型多金属氧酸盐(POM)为模板的金属有机框架[Cd(TTPB-4)(DMF)3 ] 4 [PMo 12 O 40 ] 2 [HPMo 12 O 40 ]·6DMF·4H 2 O(1) ,基于新设计的TTPB-4接头[ TTPB-4 = 1,3,5-三(4-(4 H -1,2,4-三唑-4-基)苯基)苯],已经水热使用IR,XRD,TGA,UV-Vis和光致发光光谱合成和表征。单晶X射线晶体学显示1代表唯一的POM模板四重互穿的3-D配位网络。POM模板的MOF1具有很强的化学稳定性,可以承受各种pH值的水溶液(2-10)。特别地,1在具有不同pH值的水溶液中具有极好的光降解活性和对结晶紫(CV)和碱性红2的有机染料的可回收性。
Benzimidazole and pyridylimidazole derivatives
申请人:——
公开号:US20030069257A1
公开(公告)日:2003-04-10
This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I
1
The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABA
A
receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed.
This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABA
A
receptors in tissue sections.
[EN] DIPHENYL SUBSTITUTED CYCLOALKANES<br/>[FR] CYCLOALCANES SUBSTITUÉS PAR DES DIPHÉNYLES
申请人:MERCK & CO INC
公开号:WO2009048547A1
公开(公告)日:2009-04-16
The present invention provides compounds of Formula I which are FLAP inhibitors useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.