80845-58-5Relevant articles and documents
Novel Compounds as Autotaxin Inhibitors and Pharmaceutical Compositions Comprising the Same
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Paragraph 0962-0963; 0968-09769, (2018/05/17)
The present invention relates to a novel autotaxin inhibitor compound for preventing and treating disease or symptoms due to an increase in concentration of lysophosphatidic acid or activation of autotaxin. The present invention further relates to a pharmaceutical composition containing the same. The novel compound of the present invention is an autotaxin inhibitor which inhibits production of lysophosphatidic acid, and thus is useful for treating or preventing cardiovascular disease, cancer, metabolic disease, kidney disease, liver disease, inflammatory diseases, nervous disease, respiratory disease, desmoid disease, eye disease, cholestatic symptoms, other types of chronic pruritus or acute, or chronic rejection of transplanted organs.COPYRIGHT KIPO 2017
Synthetic Applications of 2-Cyano-1,2,3,6-tetrahydropyridines. 2. Synthesis of Isodasycarpidone and Related Systems, the Ervitsine Skeleton, and Its Benzo Analogue
Bosch, Joan,Rubiralta, Mario,Domingo, Antonio,Bolos, Jordi,Linares, Ana,et al.
, p. 1516 - 1522 (2007/10/02)
The synthesis of isodasycarpidone (8a), N-demethylisodasycarpidone (9a), and their epi derivatives 8b and 9b is described.The condensation of an appropriate 2-cyano-1,2,3,6-tetrahydropyridine with indole and the conjugate addition of diethylcopper(I)-magnesium bromide to the resulting α,β-unsaturated esters constitute the key steps of this synthesis.A similar condensation from methyl 2-cyano-1-methyl-1,2,3,6-tetrahydropyridine-4-acetate (11) and indolylmagnesium iodide or (m-methoxyphenyl)magnesium bromide, followed by catalytic hydrogenation, hydrolysis, and PPA cyclization establishes synthetic routes to the tetracyclic framework (16) of the indole alkaloid ervitsine and its benzo analogue 19.