Method of inhibiting osteoclast-mediated bone resorption by administration of N-heterocyclicalkyl-substituted phenyl derivatives

US5204350A · kind A · utility

Assignee

• MERCK & CO., INC. · US

Inventors

• Melissa Egbertson · Ambler, US
• George D. Hartman · Lansdale, US
• Robert J. Gould · Baltimore, US

Key dates

• Filing date: Aug 9, 1991
• Grant date: Apr 20, 1993
• Expiry date: Aug 9, 2011

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compounds of the general formula ##STR1## Y is an integer of from 0 to 6 is chosen from: O, PA1 SO.sub.2, PA1 --CONH--, PA1 --NHCO--, PA1 --CH2-- or ##STR2## R.sup.1 is substituted or unsubstituted mono- or polycyclic saturated hetero-cyclic ring system having 1, 2 or 3 heteroatoms where said heteroatoms are independently chosen from N, O and S and said substituents are chosen from the group comprising R.sup.2 ; PA0 R.sup.2 is PA1 C.sub.1-6 alkyl, PA1 aryl C.sub.0-6 alkyl, PA1 hydroxy C.sub.0-6 alkyl, PA1 C.sub.1-6 alkoxy C.sub.0-6 alkyl, PA1 carboxy C.sub.0-6 alkyl PA1 oxo, PA1 halogen, PA1 CF.sub.3, PA1 C.sub.0-4 alkylamino-C.sub.0-6 alkyl or PA1 C.sub.0-4 dialkylamino-C.sub.0-6 alkyl; PA0 R.sup.3 is PA1 C.sub.1-8 alkyl or cycloalkyl, PA1 aryl C.sub.0-4 alkyl, PA1 hydroxy C.sub.0-4 alkyl PA1 C.sub.1-4 alkyloxy C.sub.0-4 alkyl, PA1 carboxy C.sub.0-4 alkyl, PA1 halogen, PA1 CF.sub.3 or PA1 hydrogen; PA0 R.sup.4 is PA1 hydrogen, PA1 C.sub.1-6 alkyl, PA1 aryl C.sub.0-4 alkyl or PA1 C.sub.1-6 alkylcarbonyloxymethyl; and PA0 R.sup.5 is PA1 C.sub.1-6 alkyl, PA1 aryl C.sub.0-4 alkyl or PA1 heterocycly C.sub.0-4 alkyl and the pharmaceutically acceptable salts thereof; are used in a method…