Calcium channel antagonists and methodology for their identification

US5312928A · kind A · utility

Assignee

• Cambridge NeuroScience, Inc. · US

Inventors

• Stanley M. Goldin · Lexington, US
• Kazumi Kobayashi · Arlington, US
• Andrew Gannett Knapp · Salem, US
• Lee David Margolin · Belmont, US
• Subbarao Katragadda · Belmont, US
• Deborah Daly · Melrose, US
• Lain-Yen Hu · Ann Arbor, US
• N. Laxma Reddy · Solon, US

Key dates

• Filing date: Feb 11, 1991
• Grant date: May 17, 1994
• Expiry date: Feb 11, 2011

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D209/18
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

A substantially pure compound of the formula: ##STR1## wherein each of R.sub.1 and R.sub.2, independently, is H, CH.sub.3, CF.sub.3, F, Cl, Br, I, OH, OCH.sub.3, OCF.sub.3, SH, SCH.sub.3, NH.sub.2, N.sub.3, NO.sub.2, CN, COOH, CONH.sub.2, CH.sub.2 CONH.sub.2, or SO.sub.2 NH.sub.2 ; PA0 R.sub.3 is H, CH.sub.3, COOH, CONH.sub.2, or COOR where R is C.sub.1-4 alkyl; PA0 each R.sub.4, independently, is H or C.sub.1-6 alkyl; PA0 X is CH.sub.2, CH.sub.2 CH.sub.2, CH.dbd.CH, or CH.sub.2 CH.sub.2 CH.sub.2 ; ##STR2## each Z, independently, is H, CH.sub.3, or Q where Q is a hydrophobic acyl, benzoyl, phenacetyl, benzyloxycarbonyl, alkoxycarbonyl, or N-methyl-dihydropyridine-3-carbonyl linked to N by an amide bond which is cleavable by an endogenous central nervous system enzyme; PA0 D is H or ##STR3## where R.sub.5 is H or C.sub.1-4 alkyl; m is an integer from 2 to 12, inclusive; and PA0 each n, independently, is an integer from 2 to 12, inclusive; a therapeutic composition including such compound; and a process for identifying calcium channel antagonists.