117086-91-6Relevant articles and documents
QUATERNARY LACTAM COMPOUND AND PHARMACEUTICAL USE THEREOF
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Paragraph 0143-0145, (2021/02/05)
A quaternary lactam compound of formula (I). The compound is used in the manufacture of a medicament for the treatment and/or prevention of thrombotic or thromboembolic disorders.
Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?
Adkison, Kim K.,Barrett, David G.,Deaton, David N.,Gampe, Robert T.,Hassell, Anne M.,Long, Stacey T.,McFadyen, Robert B.,Miller, Aaron B.,Miller, Larry R.,Payne, J. Alan,Shewchuk, Lisa M.,Wells-Knecht, Kevin J.,Willard Jr., Derril H.,Wright, Lois L.
, p. 978 - 983 (2007/10/03)
Starting from potent aldehyde inhibitors with poor drug properties, derivatization to semicarbazones led to the identification of a series of semicarbazone-based cathepsin K inhibitors with greater solubility and better pharmacokinetic profiles than their parent aldehydes. Furthermore, a representative semicarbazone inhibitor attenuated bone resorption in an ex vivo rat calvarial bone resorption model. However, based on enzyme inhibition comparisons at neutral pH, semicarbazone hydrolysis rates, and 13C NMR experiments, these semicarbazones probably function as prodrugs of aldehydes.
Mesolimbic selective antipsychotic arylcarbamates
Hansen, John Bondo,Fink-Jensen, Anders,Christensen, Birgitte V.,Gronvald, Frederick C.,Jeppesen, Lone,Mogensen, John P.,Nielsen, Erik B.,Scheideler, Mark A.,White, Francis J.,Zhang, Xu-Feng
, p. 839 - 858 (2007/10/03)
4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidine has been linked to various arylcarbamates to obtain compounds having affinity for dopamine-D1 and -D2, serotonin 5HT(2A) and α1-adrenoceptors. When linkers with restricted flexibility are used, the biological activity is reduced indicating that a bended conformation is needed in this series of bioactive molecules. Compounds with a relatively low D2/5HT(2A) affinity ratio in receptor binding experiments and high affinity for the α1-adrenoceptors exhibit a pharmacological profile which suggests a preferential effect on the mesocorticolimbic dopaminergic system and an 'atypical' antipsychotic activity.