Patent number: 5312928
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.
Type:
Grant
Filed:
February 11, 1991
Date of Patent:
May 17, 1994
Assignee:
Cambridge Neuroscience
Inventors:
Stanley M. Goldin, Kazumi Kobayashi, Andrew G. Knapp, Lee Margolin, Subbarao Katragadda, Deborah Daly, Lain-Yen Hu, N. Laxma Reddy