Rudolf, Klaus; Eberlein, Wolfgang; Engel, Wolfhard; Pieper, Helmut; Entzeroth, Michael; Hallermayer, Gerhard; Doods, Henri published the artcile< Development of Human Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonists. Potent and Selective Small Molecule CGRP Antagonists. 1-[N2-[3,5-Dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1- piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)piperazine: The First CGRP Antagonist for Clinical Trials in Acute Migraine>, Computed Properties of 76535-74-5, the main research area is oxoquinazolinpiperazine derivative preparation CGRP receptor antagonist antimigraine migraine.
Although the triptans have greatly improved the acute treatment of migraine headache, there are yet many shortcomings. Therefore, new strategies for the treatment of migraine are needed which offer advantages over current therapy, e.g. triptans. Our novel approach was based on the hypothesis that the release of calcitonin gene-related peptide (CGRP) could play a causative role in migraine headache. Thus the authors initiated a program aimed at the design and synthesis of small mol. CGRP receptor antagonists. High throughput screening led to the identification of (R)-Tyr-(S)-Lys dipeptide-like compounds that showed weak but unequivocal binding to the human CGRP receptor. Lead optimization afforded highly potent CGRP antagonists, the prototype being compound (I) (BIBN4096). This compound exhibiting a favorable biol. profile was selected for initial clin. trials. A proof of concept study indicated that i.v. application of I was effective in the treatment of acute migraine headache. This finding strongly supports our initial working hypothesis that CGRP plays an important role in the pathophysiol. of migraine.
Journal of Medicinal Chemistry published new progress about Antimigraine agents. 76535-74-5 belongs to class piperazines, and the molecular formula is C9H19ClN2O2, Computed Properties of 76535-74-5.
Referemce:
Piperazine – Wikipedia,
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