Pecazine – Knowledge and References

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Anesthesia and analgesia and the curse of Eve

Published in Michael J. O’Dowd, The History of Medications for Women, 2020

Atarexic (Greek ataraxia, peace of mind) drugs were combined with pethidine by Hayward-Butt (1957 p. 972) and he coined the term ‘ataralgesia’. He used pecazine (pectal), a phenodiiazine derivative, with the intention of combining very effective pain relief while retaining normal physical and mental functions. This appeared to be an ideal situation, especially for obstetric cases, and was in vogue for about 20 years. Promazine (sparine) was another much used ataractic drug. Ataralgesia was overtaken by conduction analgesia and also by the increasing safety of general anesthesia.

A patent review of MALT1 inhibitors (2013-present)

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Journal Information

Published in Expert Opinion on Therapeutic Patents, 2021

Isabel Hamp, Thomas J. O’Neill, Oliver Plettenburg, Daniel Krappmann

In another approach, Toray described a series of diphenyl pyrazole guanidine derivatives (Figure 9, compounds 43 and 44) (WO2017/057695) [97]. The initial application is complemented by the two other patent applications WO2018/021520 and WO2018/159650 [98,99], utilizing pyridine or phenyl groups as central scaffolds. One recent publication by Toray scientists describes the MALT1 inhibitory properties of a series of basic diphenyl pyrazoles, and the most potent compound displays potency in the range of thioridazine and mepazine (Figure 9, compound 45) [70,100]. Of note, the Toray compounds share some structural similarities to MI-2 (Figure 4, compound 1), but they are not reactive. The publication suggested that these substances inhibit MALT1 through binding to the allosteric pocket, which may question if the MI-2 mode of action on MALT1 is exclusively mediated via the active site [62].