×

Novel, transient pro-drug forms of L-DOPA

  • US 3,998,799 A
  • Filed: 04/17/1975
  • Issued: 12/21/1976
  • Est. Priority Date: 11/02/1973
  • Status: Expired due to Term
First Claim
Patent Images

1. A pro-drug compound of the formula:

  • ##STR19## wherein R represents a hydrogen atom, an acyl group and a -CO-R3 group, wherein R3 represents the residue of any N,N-C1 -C2 dialkylamino acid or a C4 -C6 cycloalkylamino acid;

    wherein R1 represents a member selected from the group consisting of a hydroxyl group and a -OM group, wherein M is a member selected from the group consisting of an alkali metal and an ammonium ion; and

    wherein R2 represents a -CO-R3 group, wherein R3 represents the residue of any N,N-(C1 -C2)-dialkylamino acid or a C4 -C6 -cycloalkylamino acid;

    ##STR20## wherein R represents an acyl group;

    wherein R2 represents a hydrogen atom; and

    wherein R1 represents a -NHCH(R4)COOR5 group, wherein R4 represents the residue of any naturally occurring protein amino acid, and wherein R5 represents a member selected from the group consisting of a hydrogen atom, a C1 -C5 alkyl group, and a C1 -C5 alkylaryl group, and the HX salts thereof, wherein X is a conventional pharmaceutically acceptable acid addition salt anion;

    ##STR21## wherein R represents an acyl group;

    wherein R1 represents a member selected from the group consisting of a hydroxyl group, a -OCH3 group, a -OC2 H5 group, a -OC3 H7 group, a -OC4 H9 group, and a -OCH2 C6 H5 group; and

    wherein R2 represents an NH2 CH(R6)CO- group, wherein R6 represents the residue of any naturally occurring protein amino acid, and the HX salts thereof, wherein X is defined as above;

    ##STR22## wherein R represents an acyl group;

    wherein R1 represents a member selected from the group consisting of a hydroxyl group, a -OCH3 group, a -OC2 H5 group, a -OC3 H7 group, a -OC4 H9 group, and a -OCH2 -C6 H5 group; and

    wherein R2 represents an NH2 -CH(R7)-CO- group, wherein R7 represents the residue of a 3,4-diacylphenylalanine group having the formula;

    ##STR23## wherein R is defined as above, and the HX salts thereof, wherein X is as defined above; and

    ##STR24## wherein n represents an integer of from 2 to 50 with respect to formula (V-A), and wherein n represents an integer of from 1 to 50 with respect to formula (V-B).

View all claims
  • 0 Assignments
Timeline View
Assignment View
    ×
    ×