76128-71-7Relevant academic research and scientific papers
HETEROCYCLIC COMPOUND, APPLICATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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Paragraph 0808, (2020/12/08)
Disclosed in the present invention are a heterocyclic compound, an application thereof and a pharmaceutical composition comprising the same. Provided by the present invention are a heterocyclic compound represented by formula I or a pharmaceutically acceptable salt thereof. The compound has a novel structure and a good inhibitory activity against autotaxin (ATX).
Preparation of Triazolopyrimidines as Potential Antiasthma Agents
Medwid, Jeffrey B.,Paul, Rolf,Baker, Jannie S.,Brockman, John A.,Du, Mila T.,et al.
, p. 1230 - 1241 (2007/10/02)
With the use of the human basophil histamine release assay, 5-aryl-2-aminotriazolopyrimidines were found to be active as mediator release inhibitors.These compounds were prepared by reacting arylamidines with sodium ethyl formylacetate or with ethyl propiolate to give pyrimidinones.Treatment with phosphorus oxychloride gave a chloropyrimidine, which was converted to a hydrazinopyrimidine with hydrazine.Cyclization, using cyanogen bromide, gave the triazolopyrimidines, after a Dimroth rearrangement.Following a structure-activity evaluation, the5--2-amino (8-10), 5-(3-bromophenyl)-2-amino (8-13), 5--2-amino (8-11), and 5-(4-pyridinyl)-2-amino (6-7) compounds were found to have the best activity.They were chosen for further pharmacological and toxicological study.
