N-PHENYLATED AMIDE AND UREA DERIVATIVES

摘要

Novel N-phenylated amide and urea derivatives represented by general formula (I) and salts thereof, which have excellent ACAT inhibitory activity and peroral absorbability and are useful as a remedy and/or a preventive for arteriosclerosis, wherein R<1a> represents C1-C12 alkyl or cycloalkyl-alkyl; R<16> represents H or any of the groups defined above with respect to R<1a>; R<2a>, R<2b> and R<2c> represent each independently H, optionally protected OH, nitro, C1-C12 alkyl, optionally mono- to pentafluorinated C1-C4 alkyl, alkoxy, halogeno, optionally C1-C4-alkylated mono- or dialkylamino, or five- or six-membered nitrogenous saturated heterocycle, or alternatively adjacent groups R<2a> and R<2b> are combined together to form -O-(CH2)m-O- (m being an integer of 1 to 3); R<3> represents C1-C6 alkyl; R<4> represents A<1>-R<5> (A<1> being C1-C6 alkylene or C3-C5 alkenylene; and R<5> being a heterocyclic group selected from among those belonging to the following group alpha and optionally substituted by halogeno, C1-C4 alkyl or C1-C4 hydroxyalkyl) or A<2>-X-A<3>-R<5> (A<2> being C1-C6 alkylene or C3-C5 alkenylene; X being O, S, NH, C1-C4 alkylimino, sulfinyl or sulfonyl; A<3> being a single bond, C1-C6 alkylene or C3-C5 alkenylene; and R<5> being as defined above, provided that the total number of the carbon atoms of A<2> and A<3> is 1 to 8 and that when A<3> represents a single bond, the heterocyclic group R<5> is bonded to X at the ring carbon atom); and n represents 0 or 1. Group alpha : imidazolyl, pyrazolyl, pyrazolidinyl, 1,2,4-triazolyl, tetrazolyl, morpholino, piperazinyl,2-pyridon-1-yl, 2-pyrimidinyl, pyridyl, pyrazinyl, 1,3,5-triazin-2-yl, benzimidazolyl, piperidinyl, pyrrolidinyl and azetidinyl groups.