Inventors:
Stanley M. Goldin - Lexington MA
Kazumi Kobayashi - Arlington MA
Andrew G. Knapp - Salem MA
Lee Margolin - Belmont MA
Subbarao Katragadda - Belmont MA
Deborah Daly - Melrose MA
N. Laxma Reddy - Malden MA
Assignee:
Cambridge Neuroscience - Cambridge MA
International Classification:
C07D20920
A61K 31405
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 ; R. sub. 3 is H, CH. sub. 3, COOH, CONH. sub. 2, or COOR where R is C. sub. 1-4 alkyl; each R. sub. 4, independently, is H or C. sub. 1-6 alkyl; 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; 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 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.