Spirocycloalkyl-substituted azetidinones useful as hypocholesterolemic agents

US5698548A · kind A · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Sundeep Dugar · Bound Brook, US
• John W. Clader · Cranford, US
• Duane A. Burnett · Wayland, US

Key dates

• Filing date: May 25, 1995
• Grant date: Dec 16, 1997
• Expiry date: May 25, 2015

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D205/12
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Novel compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R.sub.1 is ##STR2## R.sub.2 and R.sub.3 are independently selected from --CH.sub.2 --, --CH(lower alkyl)--, --C(di-lower alkyl)--, --CH.dbd.CH-- and --C(lower alkyl).dbd.CH--; or R.sub.1 with R.sub.2, or R.sub.1 with R.sub.3, form --CH.dbd.CH-- or --CH.dbd.C(lower alkyl)--; PA1 u and v are independently 0-3, provided both are not zero; PA1 R.sub.4 is B--(CH.sub.2).sub.m C(O)--; m is 0-5; PA2 B--(CH.sub.2).sub.q --; q is 0-6; PA2 B--(CH.sub.2).sub.e --Z--(CH.sub.2).sub.r ; Z is --O--, --C(O)--, phenylene, --N(R.sub.8)-- or --S(O).sub.0-2 --, e and r is 0-5; the sum of e and r is 0-6; PA2 B--(C.sub.2 -C.sub.6 alkenylene)--; B'--(C.sub.4 -C.sub.6 alkadienylene)--; PA2 B--(CH.sub.2).sub.t --Z--(C.sub.2 -C.sub.6 alkenylene)--; t is 0-3; the sum of t and the number of carbon atoms in the alkenylene chain is 2-6; PA2 B--(CH.sub.2).sub.f --V--(CH.sub.2).sub.g --; V is cycloalkylene, f is 1-5, g is 0-5; the sum of f and g is 1-6; PA2 B--(CH.sub.2).sub.t --V--(C.sub.2 -C.sub.6 alkenylene)-- or B'--(C.sub.2 -C.sub.6 alkenylene)--V--(CH.sub.2).sub.t --; the sum of t and the number of carbon atoms in…