Copper-Mediated Oxidative Cyclization of Heterocyclically Substituted Aldimines
摘要:
Copper-mediated cascade reactions were performed with heterocyclically substituted aldimines. These oxidative heterocyclizations include sequences of oxidations and cycloadditions or nucleophilic additions which take place in the coordination sphere of copper ions. When two heterocyclically substituted aldimines were reacted in the presence of copper (II) salts under air, pyridine derivatives were produced. In one case a 1,4-diazatricyclo-[3.2.1.0(2,7)]oct-3-ene was also formed. The basic structure of this new tetracyclic compound contains five new chirale carbon atoms. This cage-like structure has been revealed by X-ray crystallography. The synthesis of 2H-pyrroles by copper-assisted conversions of the aldimines with dimethylacetylene carboxylate or quinones was also described.
Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting &bgr;-amyloid peptide release and/or its synthesis by use of such compounds
A series of new dyes based on the fluorescent imidazo[1,5-a]pyridine moiety has been designed and synthesized specifically for fluorescence cell imaging application. The obtained molecules contain a carboxylic functional group inserted to increase the water solubility and to provide an effective conjugation site. Their structural and optical properties have been deeply investigated and compared with
已经设计并合成了一系列基于荧光咪唑并[1,5- a ]吡啶部分的新型染料,专门用于荧光细胞成像应用。所获得的分子包含插入的羧基官能团以增加水溶性并提供有效的缀合位点。对它们的结构和光学性质进行了深入研究,并与理论计算进行了比较。已经通过激光扫描共聚焦显微镜在拟南芥幼苗体内和体外研究了该产品作为荧光标记物在细胞成像中的适用性。,在小鼠成纤维细胞上。该化合物对植物细胞壁和质膜具有良好的渗透性,可以有效地内化在植物内部组织中,并在水性介质中保持强荧光。
Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
申请人:——
公开号:US20020045747A1
公开(公告)日:2002-04-18
Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation and their use
申请人:Aventis Pharma Deutschland GmbH
公开号:EP1193248A1
公开(公告)日:2002-04-03
The present invention relates to compounds of the of the formula I,
in which R1, R2, A and B have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
N-Alkyl-N'-cyano-N"-(substituted phenyl-pyridinylmethyl) guanidine derivatives were synthesized and tested for inhibitory activity against gastric secretion in rats. Several of the compounds synthesized showed an inhibiting activity as potent as that of cimetidine against basal gastric secretion but showed less potent activity than cimetidine against histamine-stimulated gastric secretion. Some structure-activity relationships are discussed.
[EN] SUBSTITUTED QUINOLINE COMPOUNDS<br/>[FR] COMPOSES DE QUINOLINE SUBSTITUES
申请人:PFIZER PROD INC
公开号:WO2005080373A1
公开(公告)日:2005-09-01
This invention relates to MTP/Apo-B secretion inhibitors of Formula (I) wherein R1-R7, X1, m and n are as defined in the specification, as well as pharmaceutical compositions comprising the compounds, and methods of use of the compounds and compositions. The compounds of the invention are useful in treating obesity and associated diseases, conditions or disorders.