27687-12-3Relevant articles and documents
8-METHYL-1-PHENYL-IMIDAZOL[1,5-A]PYRAZINE COMPOUNDS
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Page/Page column 112, (2011/09/14)
The present invention provides 8-methyl-1 -phenyl-imidazo[1,5-a]pyrazine derivatives according to formula I or pharmaceutically acceptable salts thereof. The compounds of the current invention show inhibitory activity against Lck and can be used for the treatment of Lck-mediated diseases or Lck-mediated conditions such as inflammatory disorders.
Fused bicyclic mTOR inhibitors
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Page/Page column 65, (2008/06/13)
Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
METHOD OF PREPARING DENDRITIC DRUGS
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Page/Page column 28, (2010/11/28)
Synthetic design of drug-incorporated novel dendrimer structures for quantitatively controlled drug delivery. The dendritic drugs have better control and thus a quantitative drug release can be obtained. There are no prior art dendritic drugs that control release both sequentially and quantitatively like the dendritic drugs disclosed herein. The dendritic drugs are formed by incorporating multiple same type drug units or more than two different drug types into a dendritic cascade structure to form a dendrimer drug.
Structure-activity studies of cyclic ketone inhibitors of the serine protease plasmin: Design, synthesis, and biological activity
Xue, Fengtian,Seto, Christopher T.
, p. 8467 - 8487 (2008/02/05)
Three series of cyclic ketone inhibitors were synthesized and evaluated against the serine protease plasmin. Peptide inhibitors that incorporated 3-oxotetrahydrofuran and 3-oxotetrahydrothiophene 1,1-dioxide groups had the highest activities. Alkylamino substituents, which were designed to bind in the S1 subsite of plasmin, were attached to the inhibitors. Compounds 5c and 5g, which incorporated 6-aminohexyl substituents, were found to be optimal and demonstrated IC50 values in the low micromolar range. Incorporating conformationally constrained peptide segments into the inhibitors did not improve their activities.
Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists
Curtin, Michael L.,Davidsen, Steven K.,Heyman, H. Robin,Garland, Robert B.,Sheppard, George S.,Florjancic, Alan S.,Xu, Lianhong,Carrera Jr., George M.,Steinman, Douglas H.,Trautmann, Jeff A.,Albert, Daniel H.,Magoc, Terrance J.,Tapang, Paul,Rhein, David A.,Conway, Richard G.,Luo, Gongjin,Denissen, Jon F.,Marsh, Kennan C.,Morgan, Douglas W.,Summers, James B.
, p. 74 - 95 (2007/10/03)
Studies conducted with the goal of discovering a second-generation platelet-activating factor (PAF) antagonist have identified a novel class of potent and orally active antagonists which have high aqueous solubility and long duration of action in animal m