Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method

US6472414B1 · kind B1 · utility

Assignee

• Bristol-Myers Squibb Company · US

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: May 18, 1999
• Grant date: Oct 29, 2002
• Expiry date: Nov 13, 2019

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 including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2;Rx is H, alkyl, aryl or halogen;A is(1) a bond;(2) —O—; or(3) B is: and wherein L2, L1, R1, R2, R3, R3′, R3a, R3b, R4, R4′, R5, X,  are as defined herein.