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Brain-specific analogues of centrally acting amines

  • US 4,771,059 A
  • Filed: 08/29/1985
  • Issued: 09/13/1988
  • Est. Priority Date: 02/29/1984
  • Status: Expired due to Fees
First Claim
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1. A compound having the formula ##STR748## or a non-toxic pharmaceutically acceptable salt thereof, wherein Am is the residue of a centrally acting primary amine which is a non-heterocyclic natural amino acid neurotransmitter, said residue optionally containing, in place of at least one --COOH functional group in the amino acid neurotransmitter from which Am can be considered to be derived, at least one COOY'"'"' group wherein Y'"'"' is a hydrolytically or metabolically cleavable carboxyl protective group;

  • and ##STR749## is a radical of the formula ##STR750## wherein the dotted line in formula (a) indicates the presence of a double bond in either the 4 or 5 position of the dihydropyridine ring;

    the dotted line in formula (b) indicates the presence of a double bond in either the 2 or 3 position of the dihydroquinoline ring system;

    m is zero or one;

    n is zero, one or two;

    p is zero, one or two, provided that when p is one or two, each R in formula (b) can be located on either of the two fused rings;

    q is zero, one or two, provided that when q is one or two, each R in formula (c) can be located on either of the two fused rings; and

    each R is independently selected from the group consisting of halo, C1 -C7 alkyl, C1 -C7 alkoxy, C2 -C8 alkoxycarbonyl, C2 -C8 alkanoyloxy, C1 -C7 haloalkyl, C1 -C7 alkylthio, C1 -C7 alkylsulfinyl, C1 -C7 alkylsulfonyl, --CH═

    NOR'"'"'" wherein R'"'"'" is H or C1 -C7 alkyl, and --CONR'"'"'R" wherein R'"'"' and R", which can be the same or different, are each H or C1 -C7 alkyl.

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