2-OXO-BENZIMIDAZOLYL SUBSTITUTED ETHANOLAMINE DERIVATIVES AND THEIR USE AS BETA3 AGONISTS

摘要

The present invention relates to a beta3 adrenergic receptor agonist of formula (I), wherein R is C3-C8 alkyl or (C3-C7 cycloalkyl)C1-C5 alk-di-yl; R1 is H, CN, halo; C1-C6 alkyl, C1-C4 haloalkyl, C02 R6, CONR6R6, NR6COR7, NR6R6, OR6, SR6, SOR7, S02R7 or S02NR6R6; R1a is H, halo or C1-C6 aLkyl; R2 is H or C1-C6 alkyl; R3 and R4 are independently H or C1-C6 alkyl R5 is hydrogen, optionally substituted phenyl or optionally substituted heterocycle; X is absent or is OCH2 or SCH2; X1 is absent or C1-C5 alk-di-yl; and X2 is absent or is O, S, NH, NHS02, S02NH or CH2; or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity. ,