Benzoxazole acetonitriles
AssigneeApplied Research Systems ARS Holding N.V.
InventorsMatthias Schwarz, Pascale Gaillard, Patrick Page, Jean-Pierre Gotteland, Russell Thomas
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AssigneeApplied Research Systems ARS Holding N.V.
InventorsMatthias Schwarz, Pascale Gaillard, Patrick Page, Jean-Pierre Gotteland, Russell Thomas
Estimating the term…
The present invention is related to benzoxazole acetonitriles as well as to pharmaceutical formulations containing such benzoxazole acetonitriles pof formula (I). Said benzoxazole acetonitriles are useful in the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS). The present invention is furthermore related to methods of preparing benzoxazole acetonitriles (I). A is a pyrimidinyl.L is a secondary or tertiary amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatom. selected from N, O, S or L is an acylamino moiety. R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, C1C6-alkYl, C2-C6-alkenYl, C2-C6-alkynyl or C1-C6-alkoxy, aryl, halogen, carboxy, aminocarbonyl, cyano or hydroxy.
A benzoxazole acetonitrile according to formula (I)
(canceled)
A method of forming a compound of formula (Ia), comprising reacting a compound of formula (II) with a compound of formula (III′a) to form the compound of formula (IIa′), and reacting the compound of formula (IIa′) with a compound of formula (IV) to form the compound of formula (Ia), wherein R1 is selected from the group consisting of hydrogen, sulfonyl, amino, C1-C6-alkyl C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, aryl, halogen, carboxy, aminocarbonyl, cyano and hydroxy and
An intermediate compound selected from the group consisting of
Dependencies are inferred from the claim text.