Anilide compounds, including use thereof in ACAT inhibitition

Anilide compounds of general formula (II):

• wherein R1, R2 and R3 are the same or different, and each represents a hydrogen atom, a lower alkyl group having from 1 to 8 carbon atoms, a lower alkoxy group having from 1 to 8 carbon atoms, a halogen atom, a hydroxyl group, a phosphoric acid group, a sulfonamido group, or an optionally-substituted amino group;
• or any two of R1, R2 and R3 together form an alkylenedioxy group having from 1 to 8 carbon atoms, or a lower alkoxy group having from 1 to 8 carbon atoms;
• R4 and R5 are the same or different, and each represents a hydrogen atom, a lower alkyl group having from 1 to 8 carbon atoms, or a lower alkoxy group having from 1 to 8 carbon atoms;
• or R4 and R5 may together form a lower alkylene group having from 1 to 8 carbon atoms, or a lower alkoxy group having from 1 to 8 carbon atoms, or a lower alikylene group having from 1 to 8 carbon atoms of which one or more methylene moieties is/are optionally substituted by oxygen and/or sulfur atoms;
• X represents an oxygen atoms;
• Y represents —NH—, a oxygen or sulfur atom or a sulfoxide or sulfone;
• Z represents a single bond;
• n represents an integer of from 0 to 15;
• provided that, when Y is an oxygen atom, sulfur atom or a sulfoxide, then n must not be 0, when Y is a sulfur atom or sulfone, R4 and R5 are hydrogen atoms, then n must not be 0 or 2, and
• when Y is a sulfur atom or an oxygen atom, R4 and R5 are hydrogen atoms
• Z is a single bond and n is 1, then each R1 to R3 must not be hydrogen atoms,
• or a salt or solvate thereof.

A method for treating a mammal suffering from or susceptible to a disorder that can be treated with an ACAT inhibitor, an intracellular cholesterol transferance inhibitor, a blood cholesterol depressant, or an anti-foaming agent for macrophages, which comprises administering to the mammal an effective dosage of a compound of a general formula (III):

• wherein Ar represents an optionally substituted aryl group;
• R4 and R5 are the same or different, and each represents a hydrogen atom, a lower alkyl group having from 1 to 8 carbon atoms, or a lower alkoxy group having from 1 to 8 carbon atoms;
• or R4 and R5 may together form a lower alkylene group having from 1 to 8 carbon atoms of which are one or more methylene moieties is/are optionally substituted by oxygen and/or sulfur atoms;
• X represents an oxygen atom;
• Y represents —NH—, an oxygen atom or a sulfur atom, or a sulfoxide or sulfone;
• Z represents a single bond;
• and
• n represents an integer of from 0 to 15;
• or salt or solvate thereof.

A method for treating a mammal suffering from or susceptible to a disorder that can be treated with an ACAT inhibitor, an intracellular cholesterol transference inhibitor, a blood cholesterol depressant, or an anti-foaming agent for macrophages, which comprises administering to the mammal an effective dosage of a compound of a general formula (IV):

• wherein R1, R2 and R3 are the same or different, and each represents a hydrogen atom, a lower alkyl group having from 1 to 8 carbon atoms, a lower alkoxy group having from 1 to 8 carbon atoms, a halogen, a hydroxyl group, a phosphoric acid group, a sulfonamido group, or an optionally-substituted amino group;
• or any two of R1, R2 and R3 together form an alkylenediosy group having from 1 to 8 carbon atoms;
• R4 and R5 are the same or different, and each represents a hydrogen atom, a lower alkyl group having from 1 to 8 carbon atoms, or a lower alkoxy group having from 1 to 8 carbon atoms;
• or
• R4 and R5 may together form a lower form a lower alkylene group having from 1 to 8 carbon atoms of which one or methylene moieties is/are optionally substituted by oxygen and/or sulfur atoms;
• X represents an oxygen atom;
• Y represents —NH—, an oxygen or a sulfur atom, or a sulfoxide or sulfone;
• Z represents a single bond;
• n represents an integer of from 0 to 15;
• or a salt or solvate thereof.