Patent Number: 6,514,969

Title: .beta.-amyloid inhibitors, processes for preparing them, and their use in pharmaceutical compositions

Abstract: Compounds of general formula (I) ##STR1## wherein: A is --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CO--, --CH.sub.2 --CH.sub.2 --CO--, or --CH.dbd.CH--CO--; Het is piperidinyl, piperazinyl, or dihydrobenzimidazolonyl; R.sup.1 is hydrogen or halogen; R.sup.2 is hydrogen, C.sub.1 -C.sub.4 -alkyl, CF.sub.3, or a phenyl group optionally substituted by halogen, C.sub.1 -C.sub.4 -alkyl, or C.sub.1 -C.sub.4 -alkyloxy; and R.sup.3 is hydrogen, C.sub.1 -C.sub.4 -alkyl, HO--C.sub.1 -C.sub.4 -alkyl, or C.sub.2 -C.sub.4 -alkenyl; or a group selected from phenyl, benzyl, and phenylethyl, each optionally substituted by halogen, CF.sub.3, C.sub.1 -C.sub.4 -alkyl, or C.sub.1 -C.sub.4 -alkyloxy; or a heterocycle selected from among morpholine, piperidine, piperazine, and dihydrobenzimidazolone, the heterocycle either linked directly or via a C.sub.1 -C.sub.4 -alkylene bridge, or an optical isomer, enantiomer, tautomer, free base, or pharmacologically acceptable acid addition salt thereof; methods of making such compounds; pharmaceutical compositions thereof, and their use in treating or preventing diseases in which a therapeutic benefit can be obtained by interfering in the process of the formation of A.beta. or its release from cells, by inhibiting the A.beta. activity, such as Alzheimer's disease, Parkinson's disease, and Huntington's Chorea.

Inventors: Briem; Hans (Bremen, DE), Mendla; Klaus (Ingelheim, DE), Romig; Helmut Michael (Gau-Algesheim, DE), Fechteler; Katja (Wiesbaden, DE), Fuchs; Klaus (Gau-Algesheim, DE)

Assignee: Boehringer Ingelheim Pharma KG

International Classification: C07D 471/04 (20060101); C07D 471/00 (20060101); C07D 401/14 (); C07D 403/00 (); C07D 413/00 (); A61K 031/445 (); A61P 025/00 ()

Expiration Date: 02/04/2020