Novel sypathomimetic amine prodrugs

Details Novel sypathomimetic amine prodrugs Novel sypathomimetic amine prodrugs

1979-12-28

1982-02-02

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Recombinant or stably-transformed bacterium encoding one or...

560170, 2604105, 560172, 424302, 260455R, 424303, 424304, 560106, 424305, 424307, 560142, 424308, 424310, 560252, 424311, 424312, 560171, 424313, 424314, 560 9, 424320, 424324, 560 20, 424156, 424157, 560 46, 564153, 564154, 560 47, 564162, 564165, 560251, 564159, 564160, 560104, 564168, 564169, 560105, 564166, 564167, 560 49, 564196, 564200, 560 50, 564170, 564185, 560 51, 564212, 564213, 560 53, 564202, 564207, 560 54, 564220, 560 75, 560 85, 560121, 560123, 560124, 560125, 560126, 560127, 560128, 560152

Patent

active

043139566

ABSTRACT:
Novel, transient prodrug forms of the phenolic dihydroxy sympathomimetic amines have (i) the structural formula (I): ##STR1## wherein X is O, S or NR.sup.5 ; n is 1 or 2; R.sup.1 is the monodehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 1, and the didehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 2; R.sup.2 is selected from the group consisting of straight or branched chain alkyl having from 1 to 20 carbon atoms; aryl having from 6 to 10 carbon atoms; cycloalkyl having from 3 to 8 carbon atoms; alkenyl having from 2 to 20 carbon atoms; cycloalkenyl having from 4 to 8 carbon atoms; alkynyl having from 2 to 20 carbon atoms; aralkyl, alkaryl, aralkenyl, aralkynyl, alkenylaryl, alkynylaryl, loweracyloxyalkyl, and carboxyalkyl, wherein alkyl, aryl, alkenyl and alkynyl are as defined above; saturated or unsaturated monoheterocyclic or polyheterocyclic, or fused heterocyclic, containing from 1 to 3 of any one or more of the hetero atoms N, S or O in each heterocyclic ring thereof and each such ring being from 3- to 8-membered; and mono-or poly-substituted derivatives of the above, each of said substituents being selected from the group consisting of lower alkyl, lower alkoxy, lower acyl, lower acyloxy, halo, haloloweralkyl, cyano, carbethoxy, loweralkylthio, amino, nitro, loweralkylamino, diloweralkylamino, carboxyl, carbamyl, loweralkylcarbamyl, diloweralkylcarbamyl and ##STR2## wherein R.sup.4 is hydrogen or alkyl having from 1 to 10 carbons; R.sup.3 is hydrogen, R.sup.2, lower acyl, cyano, haloloweralkyl, carbamyl, loweralkylcarbamyl, diloweralkylcarbamyl, --CH.sub.2 ONO.sub.2 and --CH.sub.2 OCOR.sup.2 ; R.sup.5 is hydrogen or lower alkyl; (ii) the structural formula (II): ##STR3## wherein X, R.sup.2 and R.sup.3 are as defined above and R.sup.1 is the didehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine; (iii) either of the structural formulae (I) or (II) wherein ##STR4## is the residue of any naturally occurring protein amino acid, the residue of any N-substituted naturally occurring amino acid, which N-substituent is lower alkyl or any amino acid protective group cleavable via hydrogenolysis or hydrolysis, or the residue of an N, N-lower dialkyl or C.sub.4 -C.sub.7 cycloalkylamino acid; and (iv) the non-toxic, pharmaceutically acceptable salts thereof.

REFERENCES:
patent: 3164629 (1965-01-01), Zolss et al.
patent: 3809714 (1974-05-01), Hussain et al.

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