&bgr;-amyloid inhibitors, processes for preparing them, and their use in pharmaceutical compositions

US6514969B2 · kind B2 · utility

Assignee

• BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG · DE

Inventors

• Hans Briem · Bremen, DE
• Klaus Mendla · Ingelheim am Rhein, DE
• Helmut Michael Romig · Gau-Algesheim, DE
• Katja Fechteler · Wiesbaden, DE
• Klaus Fuchs · Ingelheim am Rhein, DE

Key dates

• Filing date: Jul 24, 2001
• Grant date: Feb 4, 2003
• Expiry date: Jul 24, 2021

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P25/00
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Compounds of general formula (I) wherein:A is —CH2—, —CH2—CH2—, —CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—, —CH2—CO—, —CH2—CH2—CO—, or —CH═CH—CO—;Het is piperidinyl, piperazinyl, or dihydrobenzimidazolonyl;R1 is hydrogen or halogen;R2 is hydrogen, C1-C4-alkyl, CF3, or a phenyl group optionally substituted by halogen, C1-C4-alkyl, or C1-C4-alkyloxy; andR3 is hydrogen, C1-C4-alkyl, HO—C1-C4-alkyl, or C2-C4-alkenyl; or a group selected from phenyl, benzyl, and phenylethyl, each optionally substituted by halogen, CF3, C1-C4-alkyl, or C1-C4-alkyloxy; or a heterocycle selected from among morpholine, piperidine, piperazine, and dihydrobenzimidazolone, the heterocycle either linked directly or via a C1-C4-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 …