New 4-(substituted-.alpha., .alpha.-dimethyl-1-piperazine pentanoic acids and derivatives which are useful as anti-arteriosclerotic agents are disclosed. These compounds elevate the high density lipoprotein fraction of cholesterol, and also lower the low density lipoprotein fraction of cholesterol.
The present invention relates to substituted piperazine derivatives of general formula ##STR1## wherein R.sub.a, R.sub.b, R.sub.c, R.sub.f, R.sub.g, X, m and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyceride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.
The present invention provides compounds of the formula (I): ##STR1## or salts, esters or amide derivatives thereof, wherein R.sub.1 is --CO.sub.2 H, --CH.dbd.CH--CO.sub.2 H, --(CH.sub.2).sub.n CO.sub.2 H, or --O--(CH.sub.2).sub.n CO.sub.2 H (n=1 to 4); R.sub.2 is C.sub.1.varies. alkyl or benzyl which is optionally substituted by a C.sub.1-4 alkyl group or groups; R.sub.3 is C.sub.1-4 alkoxy, C.sub.1-4 alkyl or halogen. Also provided are pharmaceutical formulations containing the compounds of the formula (I) and methods for the preparation of the compounds. The above mentioned compounds have antihistaminic activity.
The invention relates to triamide MTP/ApoB inhibitors of the formula 1 ##STR1## wherein R.sup.1 -R.sup.8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.
The invention relates to triamide MTP/ApoB inhibitors of the formula 1 ##STR00001## wherein R.sup.1-R.sup.8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.
The invention relates to triamide MTP/ApoB inhibitors of the formula 1 ##STR1## wherein R.sup.1 -R.sup.8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.
