Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method

US5760246A · kind A · utility

Inventors

• Scott A. Biller · Hopewell, US
• John K. Dickson · Mount Holly, US
• R. Michael Lawrence · Yardley, US
• David R. Magnin · Hillsborough Township, US
• Michael A. Poss · Lawrenceville, US
• Jeffrey A. Robl · Newtown, US
• William A. Slusarchyk · Montgomery, US
• Richard B. Sulsky · Somerville, US
• Joseph A. Tino · Lawrenceville, US

Key dates

• Filing date: Dec 17, 1996
• Grant date: Jun 2, 1998
• Expiry date: Dec 17, 2016

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2603/76
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure ##STR1## including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2; R.sup.x is H, alkyl, aryl or halogen; A is PA1 (1) a bond; PA1 (2) --O--; or PA1 (3) ##STR2## B is: ##STR3## and wherein L.sup.2, L.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.3', R.sup.3a, R.sup.3b, R.sup.4, R.sup.4', R.sup.5, X, ##STR4## are as defined herein.