1166827-51-5Relevant articles and documents
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
, 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.
CARBAMOYL COMPOUNDS AS DGAT1 INHIBITORS 190
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Page/Page column 55, (2009/07/25)
DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro- drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, Ring A is optionally substituted 2,6-pyrazindiyl; X is =O; Ring B is optionally substituted 1,4-phenylene; Y1 is a direct bond or -O-; Y2 is -(CH 2) r- wherein r is 2 or 3; n is 0 or n is 1 when Y1 is a direct bond between Ring B and Ring C and when Ring B is 1,4-phenylene and Ring C is (4-6C)cycloalkane; Ring C is optionally substituted (4-6C)cycloalkane, (7-10C)bicycloalkane, (8-12C)tricycloalkane, phenylene or pryidindiyl; L is a direct bond or -O-; p is 0, 1 or 2 and when p is 1 or 2 RA1 and RA2 are each independently hydrogen or (1-4C)alkyl; Z is carboxy or a mimic or bioisostere thereof.