854267-89-3Relevant articles and documents
THIADIAZOLYL DERIVATIVES AS DNA POLYMERASE THETA INHIBITORS
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Paragraph 0688, (2020/12/11)
Disclosed herein are certain thiadiazolyl derivatives Formula (I): that inhibit DNA Polymerase Theta (Polθ) activity, in particular inhibit Polθ activity by inhibiting ATP dependent helicase domain activity of Polθ. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and/or preventing diseases treatable by inhibition of Polθ such as cancer, including homologous recombination (HR) deficient cancers.
NEW AZIRIDINE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE AS ACETYL-COA CARBOXYLASE INHIBITORS
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Page/Page column 91, (2013/07/05)
The invention relates to new azetidine derivatives of the formula (I) wherein Ar1, Ar2, X, R, T and L are as defined in the description, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
SUBSTITUTED 5-,6- AND 7-MEMBERED HETEROCYCLES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, AND THEIR USE
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Page/Page column 66, (2012/01/06)
The present invention relates to compounds defined by formula I: wherein the variables A1, A2, Cy1 Cy2, Cy3, E, R1a, R1b, R2, R3, n, and Q are as defined herein, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11 β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.