1166827-91-3Relevant articles and documents
INHIBITORS OF CBL-B AND METHODS OF USE THEREOF
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Paragraph 1642, (2019/08/12)
Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo.
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 ((DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687)
Barlind, Jonas G.,Bauer, Udo A.,Birch, Alan M.,Birtles, Susan,Buckett, Linda K.,Butlin, Roger J.,Davies, Robert D.M.,Eriksson, Jan W.,Hammond, Clare D.,Hovland, Ragnar,Johannesson, Petra,Johansson, Magnus J.,Kemmitt, Paul D.,Lindmark, Bo T.,Morentin Gutierrez, Pablo,Noeske, Tobias A.,Nordin, Andreas,O'Donnell, Charles J.,Petersson, Annika U.,Redzic, Alma,Turnbull, Andrew V.,Vinblad, Johanna
supporting information, p. 10610 - 10629 (2013/02/23)
A new series of pyrazinecarboxamide DGAT1 inhibitors was designed to address the need for a candidate drug with good potency, selectivity, and physical and DMPK properties combined with a low predicted dose in man. Rational design and optimization of this series led to the discovery of compound 30 (AZD7687), which met the project objectives for potency, selectivity, in particular over ACAT1, solubility, and preclinical PK profiles. This compound showed the anticipated excellent pharmacokinetic properties in human volunteers.
