361337-08-8Relevant articles and documents
Identification of a novel class of autotaxin inhibitors through cross-screening
Castagna, Diana,Duffy, Emma L.,Semaan, Dima,Young, Louise C.,Pritchard, John M.,Macdonald, Simon J. F.,Budd, David C.,Jamieson, Craig,Watson, Allan J. B.
supporting information, p. 1149 - 1155 (2015/06/25)
Three novel series were generated in order to mimic the pharmacophoric features displayed by lead compound AM095, a lysophosphatidic acid (LPA1) receptor antagonist. Biological evaluation of this array of putative LPA1 antagonists le
Purinenucleoside derivative modified in 8-position and medical use thereof
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Page/Page column 19, (2010/11/28)
The present invention provides an 8-modified purinenucleoside derivative which is useful for diseases associated with an abnormality of plasma uric acid level. An 8-modified purinenucleoside derivative represented by the following formula (I), a prodrug thereof or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, is useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; RA is a hydrogen atom or a hydroxyl group; R1 is a hydrogen atom, a hydroxyl group, a thiol group, an amino group or a chlorine atom; ring J represents an optionally substituted 2-naphthyl group, or a group represented by the following general formula (II) wherein Y represents a single bond or a connecting group; ring Z represents an optionally substituted aryl group or heteroaryl group or the like; and R2 to R4, P1 and Q represents a halogen atom, a cyano group or the like.
Synthesis and crystal structures of substituted benzenes and benzoquinones as tissue factor VIIa inhibitors
Parlow, John J.,Stevens, Anna M.,Stegeman, Roderick A.,Stallings, William C.,Kurumbail, Ravi G.,South, Michael S.
, p. 4297 - 4312 (2007/10/03)
Several multistep syntheses of substituted benzenes are reported. The benzene analogues were designed such that their substitution pattern would occupy and interact with the S1, S2, and S3 pockets of the tissue Factor VIIa enzyme. A variety of chemical transformations including nucleophilic additions, reductive aminations, Stille couplings, and polymer-assisted solution-phase (PASP) techniques were used to prepare key intermediates and final products. The initial analogues identified some weakly active compounds which ultimately led to a 340 nM (IC50) tissue Factor VIIa inhibitor with selectivity over other related enzymes. The structure-activity relationship of these inhibitors and the synthetic progression from the discovery of the lead compound to the development of potent analogues will be discussed. The X-ray crystal structures of fluorobenzene 50c and benzoquinone 54 inhibitors complexed with the TF/VIIa enzyme will also be described.
