Acat inhibitors

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 237/28 (2006.01) A61K 31/165 (2006.01) A61K 31/27 (2006.01) A61K 31/33 (2006.01) C07C 233/07 (2006.01) C07C 233/11 (2006.01) C07C 237/04 (2006.01) C07C 237/20 (2006.01) C07C 237/22 (2006.01) C07C 237/24 (2006.01) C07C 271/12 (2006.01) C07C 271/20 (2006.01) C07C 271/22 (2006.01) C07C 271/34 (2006.01) C07C 275/50 (2006.01) C07C 311/19 (2006.01) C07C 323/60 (2006.01) C07C 327/44 (2006.01) C07C 335/12 (2006.01) C07C 335/18 (2006.01) C07C 335/20 (2006.01) C07D 209/20 (2006.01) C07D 213/56 (2006.01) C07D 295

Patent

CA 2024300

ABSTRACT The present invention are novel amino acid amide compounds of the following general formula which inhibit the enzyme acylcoenzyme A:cholesterol acyltransferase: Image wherein R is phenyl or 1- or 2-naphthyl which are unsubstituted or may be substituted; R1 is hydrogen or a straight or branched alkyl group having from 1 to 6 carbon atoms; R2 is hydrogen, an aliphatic group, an aromatic group, an aralkyl or diarylalkyl group or R1 and R2 form a carbocyclic group; R3 is hydrogen, an aliphatic group, an aralkyl group wherein the alkyl moiety may contain a carbocyclic entity; R4 is hydrogen, an aliphatic group, SO2R14 , -C(=S)NHR15, -CO2R15, -COR18, or -C(=O)NHR15 wherein R14 is morpholino, phenyl or substituted phenyl; R15 is an alkyl group, phenyl or phenylalkyl wherein the phenyl group may be substituted; and R18 is the same is R15 or is halo-substituted alkyl, 9-fluorenylmethylene or pyrrolidino.

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