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Claims for Patent: RE40183

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Claims for Patent: RE40183

Title:7-Substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines
Abstract:The invention is drawn to 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds of the formula ##STR00001## wherein R, X, R.sup.5 and R.sup.6 are defined in the specification. The compounds of the invention are useful as broad spectrum antibiotics.
Inventor(s): Hlavka; Joseph J. (Tuxedo Park, NY), Sum; Phaik-Eng (Pomona, NY), Gluzman; Yakov (Upper Saddle River, NJ), Lee; Ving J. (Los Altos, CA), Ross; Adma A. (Airmont, NY)
Assignee: Wyeth Holdings Corporation (Madison, NJ)
Application Number:11/145,508
Patent Claims: 1. A compound of the formula ##STR00223## wherein: X is selected from amino, NR.sup.1 R.sup.2, or halogen; the halogen is selected from bromine, chlorine, fluorine or iodine; R.sup.1 is selected from hydrogen, methyl, ethyl, n-propyl, 1-methylethyl, n-butyl and 1-methylpropyl; R.sup.2 is selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl, and 1,1-dimethylethyl such that when X=NR.sup.1 R.sup.2 and R.sup.1=hydrogen, R.sup.2=methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl or 1,1-dimethylethyl; and when R.sup.1=methyl or ethyl; R.sup.2=methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl or 2-methylpropyl; and when R.sup.1=n-propyl, R.sup.2=n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl or 2-methylpropyl; and when R.sup.1=1-methylethyl, R.sup.2=n-butyl, 1-methylpropyl or 2-methylpropyl; and when R.sup.1=n-butyl, R.sup.2=n-butyl, 1-methylpropyl or 2-methylpropyl; and when R.sup.1=1-methylpropyl, R.sup.2=2-methylpropyl; R is selected from R.sup.4 (CH.sub.2).sub.n CO-- or R.sup.4' (CH.sub.2).sub.n SO.sub.2--; and n=0-4; and when R=R.sup.4(CH.sub.2).sub.n CO-- and .[.n-0.]. .Iadd.n=0.Iaddend., R.sup.4 is selected from amino; monosubstituted amino selected from straight or branched (C.sub.1-C.sub.6)alkylamino, cyclopropylamino, cyclobutylamino, benzylamino or phenylamino; disubstituted amino selected from dimethylamino, diethylamino, ethyl(1-methylethyl)amino, monomethylbenzylamino, piperidinyl, morpholinyl, 1-imidazolyl, 1-pyrrolyl, 1-(1,2,3-triazolyl) or 4-(1,2,4-triazolyl); a substituted (C.sub.3-C.sub.6)cycloalkyl group with substitution selected from cyano, amino or (C.sub.1-C.sub.3)acyl; a substituted (C.sub.6-C.sub.10)aryl group with substitution selected from halo, (C.sub.1-C.sub.4)alkoxy, trihalo (C.sub.1-C.sub.3)-alkyl, nitro, amino, cyano, (C.sub.1-C.sub.4)alkoxycarbonyl (C.sub.1-C.sub.3)alkylamino or carboxy; .alpha.-amino-(C.sub.1-C.sub.4)alkyl selected from aminomethyl, .alpha.-aminoethyl, .alpha.-aminopropyl or .alpha.-amino-butyl; carboxy (C.sub.2-C.sub.4)-alkylamino selected from aminoacetic acid, .alpha.-aminobutyric acid or .alpha.-aminopropionic acid and the optical isomers thereof; (C.sub.7-C.sub.9)aralkylamino; (C.sub.1-C.sub.4)alkoxycarbonylamino substituted (C.sub.1-C.sub.4) alkyl group; .alpha.-hydroxy(C.sub.1-C.sub.3)alkyl selected from hydroxymethyl, .alpha.-hydroxyethyl or .alpha.-hydroxy-1-methylethyl or .alpha.-hydroxypropyl; .alpha.-mercapto (C.sub.1-C.sub.3)alkyl selected from mercaptomethyl, .alpha.-mercaptoethyl, .alpha.-mercapto-1-methylethyl or .alpha.-mercaptopropyl; halo-(C.sub.1-C.sub.3)alkyl group; a heterocycle selected from the group consisting of a five membered aromatic or saturated ring with one N, O, S or Se heteroatom optionally having a benzo or pyrido ring fused thereto, a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto, a six membered aromatic ring with one to three N, O, S or Se heteroatoms, or a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; acyl or haloacyl group selected from acetyl, propionyl, chloroacetyl, trifluoroacetyl; (C.sub.3-C.sub.6)cycloalcylcarbonyl, (C.sub.6-C.sub.10)aroyl selected from benzoyl or naphthoyl; halo substituted (C.sub.6-C.sub.10)aroyl; (C.sub.1-C.sub.4) alkylbenzoyl, or (heterocycle)-carbonyl, the heterocycle as defined hereinabove; (C.sub.1-C.sub.4)alkoxycarbonyl selected from methoxycarbonyl, ethoxycarbonyl, straight or branched propoxylcarbonyl, straight or branched butoxycarbonyl or allyloxycarbonyl; a substituted vinyl group with substitution selected from halogen, halo(C.sub.1-C.sub.3)alkyl, or a substituted (C.sub.6-C.sub.10)aryl group with substitution selected from halo, (C.sub.1-C.sub.4)-alkoxy, trihalo(C.sub.1-C.sub.3)alkyl, nitro, amino, cyano, (C.sub.1-C.sub.4)alkoxycarbonyl, (C.sub.1-C.sub.3)alkylamino or carboxy; (C.sub.1-C.sub.4)alkoxy group; C.sub.6-aryloxy selected from phenoxy or substituted phenoxy with substitution selected from halo, (C.sub.1-C.sub.4) alkyl, nitro, cyano, thiol, amino, carboxy, di(C.sub.1-C.sub.3)alkylamino; (C.sub.7-C.sub.10)aralkyloxy; vinyloxy or a substituted vinyloxy group with substitution selected from (C.sub.1-C.sub.4)alkyl, cyano, carboxy, or (C.sub.6-C.sub.10)aryl selected from phenyl, .alpha.-naphthyl, or .beta.-naphthyl; R.sup.aR.sup.b amino(C.sub.1-C.sub.4)alkoxy group, wherein R.sup.aR.sup.b is a straight or branched (C.sub.1-C.sub.4)alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, or 2-methylpropyl or R.sup.aR.sup.b is (CH.sub.2).sub.m, m=2-6, or .[.(CH.sub.2).sub.2W(CH.sub.2)2--.]. (.Iadd.CH.sub.2).sub.2W(CH.sub.2).sub.2--.Iaddend. wherein W is selected from --N(C.sub.1-C.sub.3)alkyl, O, S, --NH, --NOB and B is selected from hydrogen or (C.sub.1-C.sub.3)alkyl; or R.sup.aR.sup.b aminoxy group, wherein R.sup.aR.sup.b is straight or branched (C.sub.1-C.sub.4)alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl, or 1,1-dimethylethyl or R.sup.aR.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2W(CH.sub.2).sub.2-- wherein W is selected from --N(C.sub.1-C.sub.3)alkyl, O, S, --NH, --NOB and B is selected from hydrogen or (C.sub.1-C.sub.3)alkyl; and when R=R.sup.4 (CH.sub.2).sub.nCO-- and n=1-4, R.sup.4 is selected from amino; a substituted (C.sub.3-C.sub.6)cycloalkyl group with substitution selected from cyano, amino or (C.sub.1-C.sub.3)acyl; a substituted(C.sub.6-C.sub.10)-aryl group with substitution selected from halo, (C.sub.1-C.sub.4)-alkoxy, trihalo(C.sub.1-C.sub.3)alkyl, nitro, amino, cyano, (C.sub.1-C.sub.4)alkoxycarbonyl, (C.sub.1-C.sub.3)alkylamino or carboxy; acyloxy or haloacyloxy group selected from acetyl, propionyl, chloroacetyl, trichlorocetyl, (C.sub.3-C.sub.6)cycloalkylcarbonyl, (C.sub.6-C.sub.10)aroyl selected from benzoyl or naphthoyl, halo substituted (C.sub.6-C.sub.10)aroyl, (C.sub.1-C.sub.4)alkylbenzoyl, or (heterocycle)-carbonyl, the heterocycle as defined hereinabove; (C.sub.1-C.sub.4)alkoxy; C.sub.6-aryloxy selected from phenoxy or substituted phenoxy with substitution selected from halo, (C.sub.1-C.sub.4)-alkyl, nitro, cyano, thiol, amino, carboxy, di(C.sub.1-C.sub.3)-alkylamino; (C.sub.7-C.sub.10)aralkyloxy; (C.sub.1-C.sub.3)alkylthio group selected from methylthio, ethylthio, propylthio or allythio; C.sub.6-arylthio group selected from phenylthio or substituted phenylthio with substitution selected from halo, (C.sub.1-C.sub.4)alkyl, nitro, cyano, thiol, amino, carboxy, di(C.sub.1-C.sub.3)alkylamino; C.sub.6-arylsulfonyl group selected from phenylsulfonyl or substituted phenylsulfonyl with substitution selected from halo, (C.sub.1-C.sub.4)alkoxy, trihalo(C.sub.1-C.sub.3)alkyl, nitro, amino, cyano, (C.sub.1-C.sub.4)alkoxycarbonyl, (C.sub.1-C.sub.3)alkylamino or carboxy; (C.sub.7-C.sub.8)aralkylthio group; a heterocycle as defined hereinabove; hydroxy; mercapto; mono- or di-straight or branched chain (C.sub.1-C.sub.6)-alkylamino with the alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl, 1,1-dimethylethyl, 2-methylbutyl, 1,1-dimethylpropyl, 2,2-dimethylpropyl, 3-methylbutyl, n-hexyl, 1-methylpentyl, 1,1-methylbutyl, 2,2-dimethylbutyl, 2-methylpentyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl or 1-methyl-1-ethylpropyl; (C.sub.2-C.sub.5)azacycloalkyl group; a carboxy(C.sub.2-C.sub.4) alkylamino group with the carboxy alkyl selected from aminoacetic acid, .alpha.-aminopropionic acid, .alpha.-aminobutyric acid and the optical isomers thereof; .alpha.-hydroxy(C.sub.1-C.sub.3)alkyl selected from hydroxymethyl, .alpha.-hydroethyl or .alpha.-hydroxy-1-methylethyl or .alpha.-hydropropyl; halo(C.sub.1-C.sub.3)alkyl group; acyl or haloacyl selected from acetyl, propionyl, chloroacetyl, trifluoroacetyl; (C.sub.3-C.sub.6)cycloalkylcarbonyl; (C.sub.6-C.sub.10)aroyl selected from benzoyl or naphthoyl; halo substituted (C.sub.6-C.sub.10)aroyl; (C.sub.1-C.sub.4)alkylbenzoyl, or (heterocycle)carbonyl, the heterocycle as defined hereinabove; (C.sub.1-C.sub.4)alkoxycarbonylamino.[.,.]. group selected from tert-butoxycarbonylamino, allyloxycarbonylamino, methoxycarbonylamino, ethoxycarbonylamino or propoxycarbonylamino; (C.sub.1-C.sub.4)alkoxycarbonyl group selected from methoxycarbonyl, ethoxycarbonyl, straight or branched propoxycarbonyl, allyloxycarbonyl or straight or branched butoxycarbonyl; R.sub.aR.sup.b-amino(C.sub.1-C.sub.4)alkoxy group wherein R.sup.aR.sup.b is straight or branched (C.sub.1-C.sub.4)alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, or 2-methylpropyl or R.sup.aR.sup.b is .[.(CH).sub.m.]. (.Iadd.CH.sub.2).sub.m .Iaddend.m=2-6 or --(CH.sub.2).sub.2W(CH.sub.2).sub.2-- wherein W is selected from --N(C.sub.1-C.sub.3)-alkyl, O, S, --NH, --NOB, and B is selected from hydrogen or (C.sub.1-C.sub.3)alkyl; or R.sup.aR.sup.b aminoxy group, wherein R.sup.aR.sup.b is straight or branched (C.sub.1-C.sub.4)-alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl or R.sup.aR.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2W(CH.sub.2).sub.2-- wherein W is selected from --N(C.sub.1-C.sub.3)-alkyl, O, S, --NH, --NOB and B is selected from hydrogen or (C.sub.1-C.sub.3)alkyl, and when .[.R.dbd.R.sup.4' (CH.sub.2)SO.sub.2--.]. .Iadd.R.dbd.R.sup.4' (CH.sub.2).sub.nSO.sub.2--.Iaddend. and n=0 R.sup.4' is selected from amino; monosubstituted amino selected from straight or branched (C.sub.1-C.sub.6)alkylamino, cyclopropylamino, cyclobutylamino, benzylamino or phenylamino; disubstituted amino selected from dimethylamino, diethylamino, ethyl(1-methylethyl)amino, monomethylbenzlamino, piperidinyl, morpholinyl, 1-imidazoyl, 1-pyrrolyl, 1-(1,2,3-triazolyl) or 4-(1,2,4-triazolyl); a substituted (C.sub.3-C.sub.6)cycloalkyl group with substitution selected from cyano, amino or (C.sub.1-C.sub.3)acyl; halo(C.sub.1-C.sub.3)alkyl group; a heterocycle as defined hereinabove; R.sup.aR.sup.b amino (C.sub.1-C.sub.4)alkoxy group, wherein R.sup.aR.sup.b is a straight or branched (C.sub.1-C.sub.4)-alkyl selected from methyl, ethyl, n-propyl, 1-methyl-ethyl, n-butyl, 1-methylpropyl, or 2-methylpropyl or R.sup.aR.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2W--(CH.sub.2).sub.2-- wherein W is selected from --N(C.sub.1-C.sub.3) alkyl, O, S, --NH, --NOB and B is selected from hydrogen or (C.sub.1-C.sub.3)-alkyl; or R.sup.aR.sup.b aminoxy group, wherein R.sup.aR.sup.b is a straight or branched (C.sub.1-C.sup.4)alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methyl-propyl, or 2-methyl-propyl or R.sup.aR.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2W(CH.sub.2).sub.2-- wherein W is selected from --N(C.sub.1-C.sub.3)alkyl, O, S, .[.--NY.]. .Iadd.--NH.Iaddend., --NOB and B is selected from hydrogen or (C.sub.1-C.sub.3) alkyl; and when R.dbd.R.sup.4' (CH.sub.2).sub.nSO.sub.2-- and n=1-4, R.sup.4' is selected from (C.sub.1-C.sub.4)carboxyalkyl; a substituted (C.sub.3-C.sub.6)cyclalkyl group with substitution selected from cyano, amino or (C.sub.1-C.sub.3)-acyl; (C.sub.1-C.sub.4)alkoxy; C.sub.6-aryloxy selected from phenoxy or substituted phenoxy with substitution selected from halo, (C.sub.1-C.sub.3)alkyl, nitro, cyano, thiol, amino, carboxy, di(C.sub.1-C.sub.3) alkylamino; (C.sub.7-C.sub.10)aralkyoxy; R.sup.aR.sup.b amino (C.sub.1-C.sub.4) alkoxy, wherein R.sup.aR.sup.b is a straight or branched (C.sub.1-C.sub.4)-alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, or 2-methylpropyl or R.sup.aR.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2W(CH.sub.2).sub.2-- wherein W is selected from --N(C.sub.1-C.sub.3)alkyl, O, S, .[.--NY.]. .Iadd.--NH .Iaddend.or --NOB and B is selected from hydrogen or (C.sub.1-C.sub.3)alkyl; or R.sup.aR.sup.b aminoxy group, wherein R.sup.aR.sup.b is straight or branched (C.sub.1-C.sub.4)alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, or 2-methylpropyl or R.sup.aR.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2W(CH.sub.2).sub.2-- wherein W is selected from --N(C.sub.1-C.sub.3)alkyl, O, S, --NH, --NOB and B is selected from hydrogen or (C.sub.1-C.sub.3)alkyl; (C.sub.1-C.sub.3) alkylthio selected from methylthio, ethylthio or n-propylthio; C.sub.6-arylthio selected from phenylthio or substituted phenylthio with substitution selected from halo, (C.sub.1-C.sub.3)alkyl, nitro, cyano, thiol, amino, carboxy, di(C.sub.1-C.sub.3)alkylamino; (C.sub.7-C.sub.8) aralkylthio; a heterocycle as defined hereinabove; hydroxy; mercapto; mono- or di-straight or branched (C.sub.1-C.sub.6)alkyl- amino group the alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl, 1,1-dimethylethyl, 2-methylbutyl, 1,1-dimethylpropyl, 2,2-dimethylpropyl, 3-methylbutyl, n-hexyl, 1-methylpentyl, 1,1-dimethylbutyl, 2,2-dimethylbutyl, 2-methylpentyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl or 1-methyl-1-ethylpropyl; halo (C.sub.1-C.sub.3) alkyl; acyl or haloacyl selected from acetyl, propionyl, chloro-acetyl, trifluoroacetyl; (C.sub.3-C.sub.6) cycloalkylcarbonyl; (C.sub.6-C.sub.10) aroyl selected from benzoyl or naphthoyl; halo substituted (C.sub.6-C.sub.10)aroyl, (C.sub.1-C.sub.4) alkylbenzoyl, or (heterocycle) carbonyl, the heterocycle as defined hereinabove; (C.sub.1-C.sub.4)alkoxycarbonyl selected from methoxycarbonyl, ethoxycarbonyl, straight or branched propoxycarbonyl, allyloxycarbonyl or straight or branched butoxycarbonyl; R.sup.5 is selected from hydrogen; straight or branched (C.sub.1-C.sub.3) alkyl selected from methyl, ethyl n-propyl or 1-methylethyl; (C.sub.6-C.sub.10)aryl selected from phenyl, .alpha.-naphthyl or .beta.-naphthyl; (C.sub.7-C.sub.9) aralkyl group; a heterocycle as defined hereinabove; or --(CH.sub.2).sub.nCOOR.sup.7 where n=0-4 and R.sup.7 is selected from hydrogen; straight or branched (C.sub.1-C.sub.3)alkyl group selected from methyl, ethyl, n-propyl or 1-methylethyl; or (C.sub.6-C.sub.10)aryl group selected from phenyl, .alpha.-naphthyl or .beta.-naphthyl; R.sup.6 is selected from hydrogen, straight or branched (C.sub.1-C.sub.3)alkyl group selected form methyl, ethyl, n-propyl or 1-methylethyl; (C.sub.6-C.sub.10)aryl group selected from phenyl, .alpha.-naphthyl or .beta.-naphthyl; (C.sub.7-C.sub.9)-aralkyl group; a heterocycle as defined hereinabove; or .[.--CH.sub.2).sub.n(COOR.sup.7'.]. .Iadd.--(CH.sub.2).sub.nCOOR.sup.7'.Iaddend. where n=0-4 and R.sup.7' is selected from hydrogen; straight or branched (C.sub.1-C.sub.3)alkyl selected from methyl, ethyl, n-propyl or 1-methylethyl; or (C.sub.6-C.sub.10)aryl selected from phenyl, .alpha.-naphthyl or .beta.-naphthyl; with the proviso that R.sup.5 and R.sup.6 cannot both be hydrogen ; or R.sup.5 and R.sup.6 taken together are --(CH.sub.2).sub.2W(CH.sub.2).sub.2--, wherein W is selected from (CH.sub.2).sub.q and q=0-1, --NH, --N(C.sub.1-C.sub.3)-alkyl, --N(C.sub.1-C.sub.4) alkoxy, oxygen, sulfur or substituted congeners selected from (L or D) proline, ethyl (L or D) prolinate, morpholine, pyrrolidine or piperidine; and the pharmacologically acceptable organic and inorganic salts or metal complexes.

2. The compound according to claim 1, wherein: X is selected .[.form.]. .Iadd.from .Iaddend.amino, NR.sup.1 R.sup.2, or halogen; the halogen is selected from bromine, chlorine, fluorine or iodine; and when X=NR.sup.1 R.sup.2 and R.sup.1=methyl or ethyl, R.sup.2=methyl or ethyl R is selected from R.sup.4 (CH.sub.2).sub.nCO-- or R.sup.4' (CH.sub.2).sub.nSO.sub.2--; and when R=R.sup.4 (CH.sub.2).sub.nCO-- and n=0, R.sup.4 is selected from .[.substituted (C.sub.6-C.sub.10)aryl group with substitution selected from halo, (C.sub.1-C.sub.4)alkoxy, nitro, amino, or (C.sub.1-C.sub.2)alkoxycarbonyl;.]. (C.sub.1-C.sub.4)alkoxycarbonyl group selected from methoxycarbonyl, ethoxycarbonyl, straight or branched propoxyl-carbonyl, straight or branched butoxycarbonyl or allyl-oxycarbonyl; a substituted (C.sub.6-C.sub.10)aryl group with substitution selected from halo, (C.sub.1-C.sub.4)alkoxy, .Iadd.nitro, amino, .Iaddend.(C.sub.1-C.sub.4) alkoxycarbonyl, .Iadd.tri.Iaddend.halo-(C.sub.1-C.sub.3)alkyl group; (C.sub.1-C.sub.4)alkoxy group; C.sub.6-aryloxy group selected from phenoxy or substituted phenoxy with substitution selected from halo, (C.sub.1-C.sub.4)alkyl; (C.sub.7-C.sub.10)aralkyloxy group; vinyloxy or substituted vinyloxy group with substitution selected from (C.sub.1-C.sub.2)-alkyl; R.sup.aR.sup.b amino(C.sub.1-C.sub.4)alkoxy group, wherein R.sup.aR.sup.b is a straight or branched (C.sub.1-C.sub.4)alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl; or R.sup.aR.sup.b aminoxy group, wherein R.sup.aR.sup.b is a straight or branched (C.sub.1-C.sub.4)-alkyl selected from methyl, ethyl, n-propyl, 1-methyl-ethyl, n-butyl, 1-methylpropyl, or 2-methylpropyl; and when R=R.sup.4 (CH.sub.2).sub.nCO-- and n=1-4, R.sup.4 is selected from amino; monosubstituted amino selected from straight or branched (C.sub.1-C.sub.6)alkyl-amino, cyclopropylamino, cyclobutylamino, benzylamino or phenylamino.Iadd., said (C.sub.1-C.sub.6)-alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl, 1,1-dimethylethyl, 2-methylbutyl, 1,1-dimethylpropyl, 2,2-dimethylpropyl, 3-methylbutyl, n-hexyl, 1-methylpentyl, 1,1-dimethylbutyl, 2,2-dimethylbutyl, 2-methylpentyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl or 1-methyl-1-ethylpropyl.Iaddend.; disubstituted amino selected from dimethylamino, diethylamino, ethyl(1-methylethyl)amino, .[.monomethylbenzylamino, piperidinyl, morpholinyl.]. , 1-imidazolyl, .Iadd.or .Iaddend.1-pyrrolyl .[.or 1-(1,2,3-triazolyl).]. ; a substituted (C.sub.6-C.sub.10)aryl group with substitution selected from halo, (C.sub.1-C.sub.4)alkoxy, nitro, amino, (C.sub.1-C.sub.4)alkoxycarbonyl; acyloxy or haloacyloxy group selected from acetyl, propionyl or chloroacetyl; (C.sub.1-C.sub.4)alkoxy group; R.sup.aR.sup.b amino(C.sub.1-C.sub.4)alkoxy group, wherein R.sup.aR.sup.b is a straight or branched (C.sub.1-C.sub.4)alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, or 2-methylpropyl or R.sup.aR.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2W(CH.sub.2).sub.2-- wherein W is selected from --N(C.sub.1-C.sub.3)alkyl, O, S, --NH, --NOB and B is selected from hydrogen or (C.sub.1-C.sub.3)alkyl; or R.sup.aR.sup.b aminoxy group, wherein R.sup.aR.sup.b is a straight or branched (C.sub.1-C.sub.4)alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, or 2-methylpropyl or R.sup.aR.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2W--(CH.sub.2).sub.2-- wherein W is selected from --N(C.sub.1-C.sub.3)-alkyl, O, S, .[.--NY.]. .Iadd.--NH.Iaddend., --NOB and B is selected from hydrogen or (C.sub.1-C.sub.3)-alkyl; halo (C.sub.1-C.sub.3)-alkyl group; (C.sub.1.Iadd.-.Iaddend.C.sub.4)alkoxycarbonylamino selected from tert-butoxycarbonylamino, allyloxycarbonylamino, methoxycarbonylamino, ethoxycarbonylamino or propoxycarbonylamino; .[.and when R.dbd.R.sup.4' (CH.sub.2).sub.nSO.sub.2-- and n=0, R.sup.4' is selected from a substituted (C.sub.6-C.sub.10)aryl group with substitution selected from halo, (C.sub.1-C.sub.4)alkoxy, nitro, (C.sub.1-C.sub.4) alkoxycarbonyl;.]. R.sup.5 is selected from hydrogen; straight or branched (C.sub.1-C.sub.3)alkyl selected from methyl, ethyl, n-propyl or 1-methylethyl; R.sup.6 is selected from hydrogen; straight or branched (C.sub.1-C.sub.3)alkyl selected from methyl, ethyl, n-propyl or 1-methylethyl; with the proviso that R.sup.5 and R.sup.6 cannot both be hydrogen; or R.sup.5 or R.sup.6 taken together are --(CH.sub.2).sub.2W(CH.sub.2).sub.2--, wherein W is selected from (CH.sub.2).sub.q and q=0-1, --NH, --N(C.sub.1-C.sub.3)-alkyl, --N(C.sub.1-C.sub.4)alkoxy, oxygen, sulfur or substituted congeners selected from (L or D)proline, ethyl(L or D)prolinate, morpholine, pyrrolidine or piperidine; and the pharmacologically acceptable organic and inorganic salts or metal complexes.

3. The compound according to claim 1 wherein said inorganic salts comprise hydrochloric, hydrobromic, hydroiodic, phosphoric, nitric or sulfate.

4. The compound according to claim 1 wherein said organic salts comprise acetate, benzoate, citrate, cysteine or other amino acids, fumarate, glycolate, maleate, succinate, tartrate, alkylsulfonate or arylsulfonate.

5. The compound according to claim 1 wherein said metal complexes comprise aluminium, calcium, iron, magnesium, manganese and complex salts.

6. A compound according to claim 1 [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-1,4,4a,5,5a,6,11, 12a-octahydro-3, 10,12,12a-tetrahydroxy-1,11-dioxo- 9-[(trifluoroacetyl)amino]-2-naphthacenecarboxamide sulfate.

7. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-1,4,4a,5,5a,6, 11,12a-octahydro-3, 10,12,12a-tetrahydroxy-9-[(methoxyacetyl)amino]-1,11-dioxo-2-naphthacenec- arboxamide.

8. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-9-[(4-Bromo-1-oxobutyl)amino]-4,7-bis(dimethyl- amino)-1,4, 4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide.

9. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-1,4,4a,5,5a,6, 11,12a-octahydro-3, 10,12,12a-tetrahydroxy-1,11-dioxo- 9-[(1-oxo-2-propenyl)amino]-2-naphthacenecarboxamide.

10. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-9-[[(Acetyloxy)acetyl]amino]-4,7-bis (dimethylamino)-1,4, 4a,5,5a,6,11,12a-octahydro-3,10, 12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide sulfide.

11. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-9-(Benzoylamino)-4,7-bis(dimethylamino)- 1,4,4a,5,5a,6,11, 12a-octahydro-3,10,12,12a-tetrahydroxy- 1,11-dioxo-2-naphthacenecarboxamide.

12. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-1,4,4a,5 5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-9-[(4-methyoxybenzoyl)amin- o]-1,11-dioxo-2-naphthacenecarboxamide.

13. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-1,4,4a,5 5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-9-[(2-methylbenzoyl)amino]- -1,11-dioxo-2-naphthacenecarboxamide.

14. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-9-[(2-fluorobenzoyl)amino]-- 1,4,4a,5,5a,6,11,12a-octahydro-3, 10,12,12a-tetrahydroxy-1,11-dioxo-2-naphathacenecarboxamide.

15. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-1,4,4a, 5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-9-[(pentafluorobenzoyl)a- mino]-1,11 -dioxo-2-naphthacenecarboxamide hydrochloride.

16. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-1,4,4a,5 , 5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-1,11-dioxo- 9-[[3-(trifluoromethyl)benzoyl]amino]-2-naphthacenecarboxamide.

17. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-9-[(2-furanylcarbonyl)amino- ]- 1,4,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide.

18. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-1,4,4a, 5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy- 1,11-dioxo-9-[(2-thienylcarbonyl)amino]-2-naphthacenecarboxamide.

19. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-1,4,4a, 5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-9-[ (4-nitrobenzonyl)amino]-1, 11-dioxo-2-naphthacenecarboxamide.

20. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-9-[(4-Aminobenzoyl)amino]-4,7-bis-dimethylamin- o)- 1,4, 4a,5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy- 1,11-dioxo-2-naphthacenecarboxamidesulfate.

21. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-9-[[(4-dimethylamino)benzoyl]amino]-1,4,4a,5,5a,6,11- ,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide.

22. A compound according to claim 1, [7S-(7.alpha.,10a.alpha.)]-[2-[[(Aminocarbonyl)-4,7-bis(dimethylamino)- 5,5a,6,6a, 7,10,10a,12-octahydro-1,8,10a, 11-tetrahydroxy-10,12-dioxo-2-naphthacenyl]amino]- 2-oxoethyl]carbamic acid 1,1-dimethylethyl ester.

23. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-9-[(Aminoacetyl)amino]-4,7-bis(dimethylamino)- 1,4,4a,5, 5a,6,11,12a-octahydro-3,10,12, 12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide mono(trifluoroacetate).

24. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-1,4,4a,5,5a,6, 11,12a-octahydro-3, 10,12,12a-tetrahydroxy-1,11-dioxo- 9-[(phenylsulfonyl)amino]-2-naphthacenecarboxamide.

25. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-9-[[(4-Chlorophenyl)sulfonyl]amino]- 4,7-bis(dimethylamino)-1,4,4a,5,5a,6,11,12a-tetrahydroxy- 1,11-dioxo-2-naphthacenecarboxamide.

26. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4,7-Bis(dimethylamino)-1,4,4a,5, 5a,6,11,12a-octahydro-3, 10,12,12a-tetrahydroxy-9-[(3-nitrophenyl)sulfonyl]amino-1,11-dioxo-2-naph- thacenecarboxamide.

27. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-1,4,4a,- 5a,6,11,12a-octahydro-3,10, 12,12a-tetrahydroxy-9-[ [(4-nitrophenyl)sulfonyl]amino]-1, 11-dioxo-2-naphthacenecarboxamide.

28. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-1,4,4a,5, 5a,6,11,12a-octahydro-3, 10,12,12a-tetrahydroxy-1,11-dioxo- 9-[(2-thienylsulfonyl)amino]-2-naphthacenecarboxamide.

29. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-9-[[(2-(Acetylamino)-4-methyl- 5-thiazolylsulfonyl]amino]-4,7-bis(dimethylamino)-1,4, 4a,5,5a,6,11,12a-octahydro-3, 10,12,12a-tetrahydroxy- 1,11-dioxo-2-naphthacenecarboxamide.

30. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-9-[ (ethylsulfonyl)amino]-1, 4,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1, 11-dioxo-2-naphthacenecarboxamide.

31. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-9-(formylamino)- 1,4,4a,5a,6,11, 12a-octahydro-3,10,12,12a-tetrahydroxy- 1,11-dioxo-N-(1-pyrrolidinylmethyl)-2-naphthacenecarboxamide.

32. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-1,4,4a,5,5a,6, 11,12a-octahydro-3, 10,12,12a-tetrahydroxy-9-[ (methanesulfonyl)amino]-1,11-dioxo-2-naphthacenecarboxamide.

33. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-1,4,4a,5,5a,6, 11,12a-octahydro-3, 10,12,12a-tetrahydroxy-1,11-dioxo- 9-[[(phenylmethoxy-)acetyl]amino]-2-naphthacenecarboxamide.

34. A compound according to claim 1, [7S-(7.alpha.,10a.alpha.)]-[[9-(Aminocarbonyl)-4,7-bis(dimethylamino)- 5,5a,6,6a,7, 10,10a,12-octahydro-1,8,10a,11-tetrahydroxy- 10,12-dioxo-2-naphathacenyl]amino] oxoacetic acid ethyl ester.

35. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-1,4,4a,5,5a, 6,11,12a-octahydro-3, 10,12,12a-tetrahydroxy-9-[ (hydroxyacetyl)amino]-1,11-dioxo-2-naphthacenecarboxamide.

36. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-9-[[(methylamino)acetyl] amino]-1, 4,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1, 11-dioxo-2-napthacenecarboxamide hydrochloride.

37. A compound according to claim 1, [7S-(7.alpha.,10a.alpha.)]-[9-(Aminocarbonyl)-4,7-bis(dimethylamino)- 5,5a,6,6a,7, 10,10a,12-octahydro-1,8,10a,11-tetrahydroxy- 10,12-dioxo-2-naphthacenyl]carbamic acid methyl ester.

38. A compound according to claim 1, [7S-(7.alpha.,10a.alpha.)]-[9-(Aminocarbonyl)-4,7-bis(dimethylamino)- 5,5a,6,6a,7, 10,10a,12-octahydro-1,8,10a,11-tetrahydroxy- 10,12-dioxo-2-naphthacenyl]carbamic acid ethenyl ester.

39. A compound according to claim 1, [7S-(7.alpha.,10a.alpha.)]-[9-(Aminocarbonyl)-4,7-bis(dimethyl-amino)- 5,5a,6,6a,7, 10,10a,12-octahydro-1,8,10a,11-tetrahydroxy- 10,12-dioxo-2-naphthacenyl]carbamic acid ethenyl ester.

40. A compound according to claim 1, [7S-(7.alpha.,10a.alpha.)]-[9-(Aminocarbonyl)-4,7-bis(dimethyl-amino)- 5,5a,6,6a,7, 10,10a,12-octahydro-1,8,10a,11-tetrahydroxy- 10,12-dioxo-2-naphthacenyl]carbamic acid 2-propenyl ester.

41. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-9-[[(dimethylamino)acetyl] amino]-1,4,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide sulfate.

42. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-1,4,4a,5,5a,6, 11,12a-octahydro-3, 10,12,12a-tetrahydroxy-9-[ (methoxyacetyl)amino]-1,11-dioxo-2-naphthacenecarboxamide hydrochloride.

43. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-9-[[(4-Bromo-1-oxobutyl)amino]-4,7bis(dimethyl- amino)-1,4,4a,5,5a,6,11,12a-octahydroxy- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide sulfate.

44. A compound according to claim 1 [4S-(4.alpha.,12a.alpha.)]-9-[[(Acetyloxy)acetyl]amino]-4,7-bis (dimethylamino)-1,4, 4a,5,5a,6,11,12a-octahydro-3,10, 12,12a-tetrahydroxy-1,11-dioxo-2-napthacenecarboxamide.

45. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-9-(Benzolyamino)-4,7-bis(dimethylamino)- 1,4,4a,5,5a,6, 11,12a-octahydro-3,10,12,12a-tetra-hydroxy- 1,11 -dioxo-2-naphthacenecarboxamide sulfate.

46. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-1,4,4a,5, 5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-1,11 -dioxo- 9-[[3-(trifluoromethyl)benzoyl]amino]-2-naphthacenecarboxamide hydrochloride.

47. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-9-[(4-Aminobenzoyl)amino]-4,7-bis(dimethylamin- o)- 1,4, 4a,5,5a,6,11,12a-octahydro-3,10,12, 12a-tetrahydroxy-1,11-dioxo-2-napthacenecarboxamide.

48. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-9-[[(4-dimethylamino)benzoyl]amino]-1,4,4a,5,5a,6,11- ,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide hydrochloride.

49. A compound according to claim 1, [7S-(7.alpha.,10a.alpha.)]-[2-[[9-(Aminocarbonyl)-4,7-bis(dimethylamino)- 5,5a,6,6a, 7,10,10a,12-octahydro-1,8,10a, 11-tetrahydroxy-10,12-dioxo-2-naphthacenyl]amino]- 2-oxoethyl]carbamic acid 1,1-dimethylethyl ester hydrochloride.

50. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-9-[(Aminocarbonyl)-amino]-4,7-bis(dimethylamin- o)- 1,4,4a,5, 5a,6,11,12a-octahydro-3,10,12, 12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide.

51. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-9-[ (ethylsulfonyl)amino]-1, 4,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1, 11-dioxo-2-naphthacenecarboxamide hydrochloride.

52. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-1,4,4a,5,5a,6, 11,12a-octahydro-3, 10,12,12a-tetrahydroxy-9-[ (methansulfonyl)amino]-1,11-dioxo-2-naphthacenecarboxamide sulfate.

53. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-1,4,4a,5,5a,6, 11,12a-octahydro-3, 10,12,12a-tetrahydroxy-1,11-dioxo- 9-[[(phenylmethoxy-)acetyl]amino]-2-naphthacenecarboxamide hydrochloride.

54. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-1,4,4a,5,5a, 6 11,12a-octahydro-3, 10,12,12a-tetrahydroxy-9-[ (hydroxyacetyl)amino]-1,11-dioxo-2-naphthacenecarboxamide sulfate.

55. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-9-[[(dimethylamino)acetyl] amino]-1,4,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide.

56. A compound according to claim 1, [7S-(7.alpha.,10a.alpha.)]-[9-(Aminocarbonyl)-4,7-bis(dimethylamino)- 5,5a,6,6a,7, 10,10a,12-octahydro-1,8,10a,11-tetrahydroxy- 10,12-dioxo-2-naphthacenyl]carbamic acid methyl ester sulfate.

57. A compound according to claim 1, [7S-(7.alpha.,10a.alpha.)]-[9-(Aminocarbonyl)-4,7-bis(dimethylamino)- 5,5a,6,6a,7, 10,10a,12-octahydro-1,8,10a,11-tetrahydroxy- 10,12-dioxo-2-naphthacenyl]carbamic acid (2-diethylamino)ethyl ester hydrochloride.

58. A compound according to claim 1, [7S-(7.alpha.,10a.alpha.)]-[9-(Aminocarbonyl)-4,7-bis(dimethylamino)- 5,5a,6,6a,7, 10,10a,12-octahydro-1,8,10a,11-tetrahydroxy- 10,12-dioxo-2-naphthacenyl]carbamic acid ethenyl ester sulfate.

59. A compound according to claim 1, [7S-(7.alpha.,10a.alpha.)]-[9-(Aminocarbonyl)-4,7-bis(dimethylamino)- 5,5a,6,6a,7, 10,10a,12-octahydro-1,8,10a,11-tetrahydroxy- 10,12-dioxo-2-naphthacenyl]carbamic acid 2-propenyl ester hydrochloride.

60. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-9-[[(diethylamino) acetyl]amino]-1, 4,4a,5,5a,6,11,12a-octahydro-3,10,12, 12a-tetrahydroxy-1, 11-dioxo-2-naphthacenecarboxamide sulfate.

61. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-9-[[(diethylamino) acetyl]amino]-1, 4,4a,5,5a,6,11,12a-octahydro-3,10,12, 12a-tetrahydroxy-1, 11-dioxo-2-naphthacenecarboxamide hydrochloride.

62. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-9-[[(diethylamino) acetyl]amino]-1, 11-dioxo-2-naphthacenecarboxamide.

63. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-9-[[(dimethylamino)acetyl] amino]-1,4,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide dihydrochloride.

64. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-4, 7-Bis(dimethylamino)-9-(chloroacetylamino)- 1,4,4a,5,5a, 6,11,12a-octahydro-3,10,12,12a-tetrahydroxy- 1,11-dioxo-2-naphthacenecarboxamide.

65. A compound according to claim 1, [4S-(4alpha,12aalpha)]-9-[(Chloroacetyl)amino]-4,7-bis(dimethylamino)-1,4- ,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide dihydrochloride.

66. A compound according to claim 1, [4S-(4alpha,12aalpha)]-9-[(Bromoacetyl)amino]-4,7-bis(dimethylamino)-1,4,- 4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide dihydrochloride.

67. A compound according to claim 1, [4S-(4alpha,12aalpha)]-9-[(Bromoacetyl)amino]-4,7-bis(dimethylamino)-1,4,- 4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide (free base).

68. A compound according to claim 1, [4S-(4alpha,12aalpha)]-9-[(Bromoacetyl)amino]-4,7-bis(dimethylamino)-1,4,- 4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide monohydrobromide.

69. A compound according to claim 1, [4S-(4alpha,12aalpha)]-9-[(2-Bromo-1-oxopropyl)amino]- 4,7-bis(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide hydrobromide.

70. A compound according to claim 1, [4S-(4alpha,12aalpha)]-9-[(2-Bromo-1-oxopropyl)amino]- 4,7-bis(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide hydrobromide.

71. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)- 1,4,4a,5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy- 9-[[(methylamino)acetyl]amino]-1,11-dioxo-2-naphthacenecarboxamide dihydrochloride.

72. A compound according to claim 1, [7S-(7alpha,10aalpha)]-N-[9-(Aminocarbonyl)-4,7-bis(dimethylamino)- 5,5a, 6,6a,7,10,10a,12-octahydro- 1,8,10a,11-tetrahydroxy-10, 12-dioxo-2-naphthacenyl]-4-morpholineacetamide dihydrochloride.

73. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-9-[ [(ethyamino)acetyl]amino]-1,4,4a,5,5a,6,11,12a,-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide dihydrochloride.

74. A compound according to claim 1, [4S-(4alpha,12aalpha)]-9-[[(Cyclopropylamino)acetyl]amino]- 4,7-bis(dimethylamino)-1,4,4a,5,5a,6,11,12a,-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide dihydrochloride.

75. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-9-[ [(butylamino)acetyl]amino]-1,4,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide dihydrochloride.

76. A compound according to claim 1, [4S-(4alpha,12aalpha)]-9-[[(Diethylamino)acetyl]amino]- 4,7-bis(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide dihydrochloride.

77. A compound according to claim 1, [7S-(7alpha,10aalpha)]-N-[9-(Aminocarbonyl)-4,7-bis(dimethylamino)- 5,5a, 6,6a,7,10,10a,12-octahydro- 1,8,10a,11-tetrahydroxy-10, 12-dioxo-2-naphthacenyl]-1-pyrrolidineacetamide dihydrochloride.

78. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahy- dro-3,10,12,12a-tetrahydroxy-9-[ [[(2-methylpropyl)amino]acetyl]amino]-1,11-dioxo-2-naphthacenecarboxamide dihydrochloride.

79. A compound according to claim 1, [7S-(7alpha,10aalpha)]-N-[9-(Aminocarbonyl)-4,7-bis(dimethylamino)- 5,5a, 6,6a,7,10,10a,12-octahydro-1,8,10a, 11-tetrahydroxy-10, 12-dioxo-2-naphthacenyl]-1-piperidineacetamide dihydrochloride.

80. A compound according to claim 1, [7S-(7alpha,10aalpha)]-N-[9-(Aminocarbonyl)-4,7-bis(dimethylamino)- 5,5a, 12-dioxo-2-naphthacenyl]-1H-imidazole- 1-acetamide dihydrochloride.

81. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-1,4,4a, 5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-1,11-dioxo- 9-[[(propylamino)acetyl]amino]-2-naphthacenecarboxamide dihydrochloride.

82. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-9-[[(dimethylamino)acetyl]a- mino]-1,4,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide.

83. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-9-[ [(hexylamino)acetyl]amino]-1,4,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide dihydrochloride.

84. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-9-[[2-(dimethylamino)-1-oxo- propyl]amino]-1,4,4a,5,5a,6,11, 12a-octahydro-3,10, 12,12a-tetrahydroxy-1,11-dioxo-2-napthacenecarboxamide dihydrochloride.

85. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-1,4,4a, 5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-9-[[2-(methylamino)- 1-oxo-propyl]amino]-1,11-dioxo-2-naphthacenecarboxamide dihydrochloride.

86. A compound according to claim 1, [7S-(7alpha,10aalpha)]-N-[9-(Aminocarbonyl)-4,7-bis(dimethylamino)- 5,5a, 6,6a,7,10,10a,12-octahydro-1,8,10a, 11-tetrahydroxy-10, 12-dioxo-2-naphthacencyl]-alphamethyl-1-pyrrolidineacetamide dihydrochloride.

87. A compound according to claim 1 [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-9-[[4-(dimethylamino)-1-oxo- butyl]amino]-1,4,4a,5,5a,6,11,12a-octahydro- 3,10, 12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide dihydrochloride.

88. A compound according to claim 1, [4S-(4alpha,12aalpha)]-9-[[(Butylmethylamino)acetyl]amino]- 4,7-bis(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecenecarboxamide dihydrochloride.

89. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahy- dro-3,10,12,12a-tetrahydroxy-1,11-dioxo- 9-[[(pentylamino)acetyl]amino]-2-naphthacenecarboxamide dihydrochloride.

90. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahy- dro-3,10,12,12a-tetrahydroxy-1,11-dioxo- 9-[[(phenylmethyl)amino]acetyl]amino]-2-naphthacenecarboxamide dihydrochloride.

91. A compound according to claim 1, [7S-(7alpha,10aalpha) ]-N-[2-[ [9-(Aminocarbonyl) -4,7-bis(dimethylamino)-5,5a,6,6a,7,10a,12-octahydro-1,8, 10a,11-tetrahydroxy-10, 12-dioxo-2-naphthacenyl]amino]- 2-oxoethyl]glycine.

92. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-9-[[(dimethylamino)acetyl]a- mino]-1,4,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-N-(1-pyrrolidinylmethyl)- 2-naphthacenecarboxamide.

93. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-9-[[(dimethylamino)acetyl]a- mino]-1,4,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-N-(4-morpholinylmethyl)- 2-naphthacenecarboxamide.

94. A compound according to claim 1, [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-9-[[(dimethylamino)acetyl]a- mino]-1,4,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-N-(1-piperidinylmethyl)-2-naphthacene- cearboxamide.

95. A compound according to claim 1, [7S-(7alpha,10aalpha)]-N-[9-(Aminocarbonyl-4,7-bis(dimethylamino)- 5,5a, 6,6a,7,10,10a,12-octahydro-1,8, 10a,11-tetrahydroxy-10, 12-dioxo-2-naphthacenyl]-1-azetidineacetamide.

96. A compound according to claim 1, [4S-(4alpha,12aalpha)]-9-[[(Cyclobutylamino)acetyl]amino]- 4,7-bis(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro- 3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide hydrochloride.

97. A pharmaceutical composition of matter comprising a compound according to claim 1 in association with a pharmaceutically acceptable carrier.

98. A veterinary composition which comprises a pharmacologically effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.

.Iadd.99. A compound of the formula ##STR00224## wherein: X is selected from amino, NR.sup.1 R.sup.2, or halogen; the halogen is selected from bromine, chlorine, fluorine or iodine; R.sup.1 is selected from hydrogen, methyl, ethyl, n-propyl, 1-methylethyl, n-butyl and 1-methylpropyl; R.sup.2 is selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl, and 1,1-dimethylethyl such that when X=NR.sup.1 R.sup.2 and R.sup.1=hydrogen, R.sup.2=methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl or 1,1-dimethylethyl; and when R.sup.1=methyl or ethyl, R.sup.2=methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl or 2-methylpropyl; and when R.sup.1=n-propyl, R.sup.2=n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl or 2-methylpropyl; and when R.sup.1=1-methylethyl, R.sup.2=n-butyl, 1-methylpropyl or 2-methylpropyl; and when R.sup.1=n-butyl, R.sup.2=n-butyl, 1-methylpropyl or 2-methypropyl; and when R.sup.1=1-methylpropyl, R.sup.2=2-methylpropyl; R is selected from R.sup.4 (CH.sub.2).sub.nCO-- or R.sup.4' (CH.sub.2).sub.nSO.sub.2--; and n=0-4; and when R=R.sup.4 (CH.sub.2).sub.nCO-- and n=0, R.sup.4 is selected from amino; monosubstituted amino selected from straight or branched (C.sub.1-C.sub.6)alkylamino, cyclopropylamino, cyclobutylamino, benzylamino or phenylamino; disubstituted amino selected from dimethylamino, diethylamino, ethyl(1-methylethyl)amino, monomethylbenzylamino, piperidinyl, morpholinyl, 1-imidazolyl, 1-pyrrolyl, 1-(1,2,3-triazolyl) or 4-(1,2,4-triazolyl); a substituted (C.sub.3-C.sub.6)cycloalkyl group with substitution selected from cyano, amino or (C.sub.1-C.sub.3)acyl; a substituted (C.sub.6-C.sub.10)aryl group with substitution selected from halo, (C.sub.1-C.sub.4)alkoxy, trihalo (C.sub.1-C.sub.3)-alkyl, nitro, amino, cyano, (C.sub.1-C.sub.4)alkoxycarbonyl (C.sub.1-C.sub.3)alkylamino or carboxy; .alpha.-amino-(C.sub.1-C.sub.4)alkyl selected from aminomethyl, .alpha.-aminoethyl, .alpha.-aminopropyl or .alpha.-amino-butyl; carboxy (C.sub.2-C.sub.4)-alkylamino selected from aminoacetic acid, .alpha.-aminobutyric acid or .alpha.-aminopropionic acid and the optical isomers thereof; (C.sub.7-C.sub.9)aralkylamino; (C.sub.1-C.sub.4)alkoxycarbonylamino substituted (C.sub.1-C.sub.4) alkyl group; .alpha.-hydroxy(C.sub.1-C.sub.3)alkyl selected from hydroxymethyl, .alpha.-hydroxyethyl or .alpha.-hydroxy-1-methylethyl or .alpha.-hydroxypropyl; .alpha.-mercapto (C.sub.1-C.sub.3)alkyl selected from mercaptomethyl, .alpha.-mercaptoethyl, .alpha.-mercapto-1-methylethyl or .alpha.-mercaptopropyl; halo-(C.sub.1-C.sub.3)alkyl group; a heterocycle selected from the group consisting of a five membered aromatic or saturated ring with one N, O, S or Se heteroatom optionally having a benzo or pyrido ring fused thereto, a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto, a six membered aromatic ring with one to three N, O, S or Se heteroatoms, or a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; acyl or haloacyl group selected from acetyl, propionyl, chloroacetyl, trifluoroacetyl; (C.sub.3-C.sub.6)cycloalcylcarbonyl, (C.sub.6-C.sub.10)aroyl selected from benzoyl or naphthoyl; halo substituted (C.sub.6-C.sub.10)aroyl; (C.sub.1-C.sub.4) alkylbenzoyl, or (heterocycle)-carbonyl, the heterocycle as defined hereinabove; (C.sub.1-C.sub.4)alkoxycarbonyl selected from methoxycarbonyl, ethoxycarbonyl, straight or branched propoxylcarbonyl, straight or branched butoxycarbonyl or allyloxycarbonyl; a substituted vinyl group with substitution selected from halogen, halo(C.sub.1-C.sub.3)alkyl, or a substituted (C.sub.6-C.sub.10)aryl group with substitution selected from halo, (C.sub.1-C.sub.4)-alkoxy, trihalo(C.sub.1-C.sub.3)alkyl, nitro, amino, cyano, (C.sub.1-C.sub.4)alkoxycarbonyl, (C.sub.1-C.sub.3)alkylamino or carboxy; (C.sub.1-C.sub.4)alkoxy group; C.sub.6-aryloxy selected from phenoxy or substituted phenoxy with substitution selected from halo, (C.sub.1-C.sub.4) alkyl, nitro, cyano, thiol, amino, carboxy, di(C.sub.1-C.sub.3)alkylamino; (C.sub.7-C.sub.10)aralkyloxy; vinyloxy or a substituted vinyloxy group with substitution selected from (C.sub.1-C.sub.4)alkyl, cyano, carboxy, or (C.sub.6-C.sub.10)aryl selected from phenyl, .alpha.-naphthyl or .beta.-naphthyl; R.sup.aR.sup.b amino(C.sub.1-C.sub.4)alkoxy group, wherein R.sup.aR.sup.b is a straight or branched (C.sub.1-C.sub.4)alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, or 2-methylpropyl or R.sup.aR.sup.b is (CH.sub.2).sub.m, m=2-6, or (CH.sub.2).sub.2W(CH.sub.2).sub.2-- wherein W is selected from --N(C.sub.1-C.sub.3)alkyl, O, S, --NH, --NOB and B is selected from hydrogen or (C.sub.1-C.sub.3)alkyl; or R.sup.aR.sup.b aminoxy group, wherein R.sup.aR.sup.b is a straight or branched (C.sub.1-C.sub.4)alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl, or 1,1-dimethylethyl or R.sup.aR.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2W(CH.sub.2).sub.2-- wherein W is selected from --N(C.sub.1-C.sub.3)alkyl, O, S, --NH, --NOB and B is selected from hydrogen or (C.sub.1-C.sub.3)alkyl; and when R=R.sup.4 (CH.sub.2).sub.nCO-- and n=1-4, R.sup.4 is selected from amino; a substituted (C.sub.3-C.sub.6)cycloalkyl group with substitution selected from cyano, amino or (C.sub.1-C.sub.3)acyl; a substituted(C.sub.6-C.sub.10)-aryl group with substitution selected from halo, (C.sub.1-C.sub.4)-alkoxy, trihalo(C.sub.1-C.sub.3)alkyl, nitro, amino, cyano, (C.sub.1-C.sub.4)alkoxycarbonyl, (C.sub.1-C.sub.3)alkylamino or carboxy; acyloxy or haloacyloxy group selected from acetyl, propionyl, chloroacetyl, trichlorocetyl, (C.sub.3-C.sub.6)cycloalkylcarbonyl, (C.sub.6-C.sub.10)aroyl selected from benzoyl or naphthoyl, halo substituted (C.sub.6-C.sub.10)aroyl, (C.sub.1-C.sub.4)alkylbenzoyl, or (heterocycle)-carbonyl, the heterocycle as defined hereinabove; (C.sub.1-C.sub.4)alkoxy; C.sub.6-aryloxy selected from phenoxy or substituted phenoxy with substitution selected from halo, (C.sub.1-C.sub.4)-alkyl, nitro, cyano, thiol, amino, carboxy, di(C.sub.1-C.sub.3)-alkylamino; (C.sub.7-C.sub.10)aralkyloxy; (C.sub.1-C.sub.3)alkylthio group selected from methylthio, ethylthio, propylthio or allythio; C.sub.6-arylthio group selected from phenylthio or substituted phenylthio with substitution selected from halo, (C.sub.1-C.sub.4)alkyl, nitro, cyano, thiol, amino, carboxy, di(C.sub.1-C.sub.3)alkylamino; C.sub.6-arylsulfonyl group selected from phenylsulfonyl or substituted phenylsulfonyl with substitution selected from halo, (C.sub.1-C.sub.4)alkoxy, trihalo(C.sub.1-C.sub.3)alkyl, nitro, amino, cyano, (C.sub.1-C.sub.4)alkoxycarbonyl, (C.sub.1-C.sub.3)alkylamino or carboxy; (C.sub.7-C.sub.8)aralkylthio group; a heterocycle as defined hereinabove; hydroxy; mercapto; mono- or di-straight or branched chain (C.sub.1-C.sub.6)-alkylamino with the alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl, 1,1-dimethylethyl, 2-methylbutyl, 1,1-dimethylpropyl, 2,2-dimethylpropyl, 3-methylbutyl, n-hexyl, 1-methylpentyl, 1,1-dimethylbutyl, 2,2-dimethylbutyl, 2-methylpentyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl or 1-methyl-1-ethylpropyl; (C.sub.2-C.sub.5)azacycloalkyl group; a carboxy(C.sub.2-C.sub.4) alkylamino group with the carboxy alkyl selected from aminoacetic acid, .alpha.-aminopropionic acid, .alpha.-aminobutyric acid and the optical isomers thereof; .alpha.-hydroxy(C.sub.1-C.sub.3)alkyl selected from hydroxymethyl, .alpha.-hydroxyethyl or .alpha.-hydroxy-1-methylethyl or .alpha.-hydroxypropyl; halo(C.sub.1-C.sub.3)alkyl group; acyl or haloacyl selected from acetyl, propionyl, chloroacetyl, trifluoroacetyl; (C.sub.3-C.sub.6)cycloalkylcarbonyl; (C.sub.6-C.sub.10)aroyl selected from benzoyl or naphthoyl; halo substituted (C.sub.6-C.sub.10)aroyl; (C.sub.1-C.sub.4)alkylbenzoyl, or (heterocycle)carbonyl, the heterocycle as defined hereinabove; (C.sub.1-C.sub.4)alkoxycarbonylamino group selected from tert-butoxycarbonylamino, allyloxycarbonylamino, methoxycarbonylamino, ethoxycarbonylamino or propoxycarbonylamino; (C.sub.1-C.sub.4)alkoxycarbonyl group selected from methoxycarbonyl, ethoxycarbonyl, straight or branched propoxycarbonyl, allyloxycarbonyl or straight or branched butoxycarbonyl; R.sup.aR.sup.b-amino(C.sub.1-C.sub.4)alkoxy group wherein R.sup.aR.sup.b is a straight or branched (C.sub.1-C.sub.4)alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, or 2-methylpropyl or R.sup.aR.sup.b is (CH.sub.2).sub.m m=2-6 or --(CH.sub.2).sub.2W(CH.sub.2).sub.2-- wherein W is selected from --N(C.sub.1-C.sub.3)-alkyl, O, S, --NH, --NOB, and B is selected from hydrogen or (C.sub.1-C.sub.3)alkyl; or R.sup.aR.sup.b aminoxy group, wherein R.sup.aR.sup.b is a straight or branched (C.sub.1-C.sub.4)-alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl or R.sup.aR.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2W(CH.sub.2).sub.2-- wherein W is selected from --N(C.sub.1-C.sub.3)-alkyl, O, S, --NH, --NOB and B is selected from hydrogen or (C.sub.1-C.sub.3)alkyl, and when R=R.sup.4, (CH.sub.2)SO.sub.2-- and n=0 R.sup.4' is selected from amino; monosubstituted amino selected from straight or branched (C.sub.1-C.sub.6)alkylamino, cyclopropylamino, cyclobutylamino, benzylamino or phenylamino; disubstituted amino selected from dimethylamino, diethylamino, ethyl(1-methylethyl)amino, monomethylbenzylamino, piperidinyl, morpholinyl, 1-imidazoyl, 1-pyrrolyl, 1-(1,2,3-triazolyl) or 4-(1,2,4-triazolyl); a substituted (C.sub.3-C.sub.6)cycloalkyl group with substitution selected from cyano, amino or (C.sub.1-C.sub.3)acyl; halo(C.sub.1-C.sub.3)alkyl group; a heterocycle as defined hereinabove; R.sup.aR.sup.b amino (C.sub.1-C.sub.4) alkoxy group, wherein R.sup.aR.sup.b is a straight or branched (C.sub.1-C.sub.4)-alkyl selected from methyl, ethyl, n-propyl, 1-methyl-ethyl, n-butyl, 1-methylpropyl, or 2-methylpropyl or R.sup.aR.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2W--(CH.sub.2).sub.2-- wherein W is selected from --N(C.sub.1-C.sub.3) alkyl, O, S, --NH, --NOB and B is selected from hydrogen or (C.sub.1-C.sub.3)-alkyl; or R.sup.aR.sup.b aminoxy group, wherein R.sup.aR.sup.b is a straight or branched (C.sub.1-C.sub.4)alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methyl-propyl, or 2-methyl-propyl or R.sup.aR.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2W(CH.sub.2).sub.2-- wherein W is selected from --N(C.sub.1-C.sub.3) alkyl, O, S, --NH, --NOB and B is selected from hydrogen or (C.sub.1-C.sub.3) alkyl; and when R=R.sup.4' (CH.sub.2).sub.nSO.sub.2-- and n=1-4, R.sup.4' is selected from (C.sub.1-C.sub.4)carboxyalkyl; a substituted (C.sub.3-C.sub.6)cyclalkyl group with substitution selected from cyano, amino or (C.sub.1-C.sub.3)-acyl; (C.sub.1-C.sub.4)alkoxy; C.sub.6-aryloxy selected from phenoxy or substituted phenoxy with substitution selected from halo, (C.sub.1-C.sub.3)alkyl, nitro, cyano, thiol, amino, carboxy, di(C.sub.1-C.sub.3) alkylamino; (C.sub.7-C.sub.10)aralkyloxy; R.sup.aR.sup.b amino (C.sub.1-C.sub.4) alkoxy, wherein R.sup.aR.sup.b is a straight or branched (C.sub.1-C.sub.4)-alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, or 2-methylpropyl or R.sup.aR.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2W(CH.sub.2).sub.2-- wherein W is selected from --N(C.sub.1-C.sub.3)alkyl, O, S, --NH or --NOB and B is selected from hydrogen or (C.sub.1-C.sub.3)alkyl; or R.sup.aR.sup.b aminoxy group, wherein R.sup.aR.sup.b is a straight or branched (C.sub.1-C.sub.4)alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, or 2-methylpropyl or R.sup.aR.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2W(CH.sub.2).sub.2-- wherein W is selected from --N(C.sub.1-C.sub.3)alkyl, O, S, --NH, --NOB and B is selected from hydrogen or (C.sub.1-C.sub.3)alkyl; (C.sub.1-C.sub.3) alkylthio selected from methylthio, ethylthio or n-propylthio; C.sub.6-arylthio selected from phenylthio or substituted phenylthio with substitution selected from halo, (C.sub.1-C.sub.3)alkyl, nitro, cyano, thiol, amino, carboxy, di(C.sub.1-C.sub.3)alkylamino; (C.sub.7-C.sub.8) aralkylthio; a heterocycle as defined hereinabove; hydroxy; mercapto; mono- or di-straight or branched (C.sub.1-C.sub.6)alkyl- amino group the alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl, 1,1-dimethylethyl, 2-methylbutyl, 1,1-dimethylpropyl, 2,2-dimethylpropyl, 3-methylbutyl, n-hexyl, 1-methylpentyl, 1,1-dimethylbutyl, 2,2-dimethylbutyl, 2-methylpentyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl or 1-methyl-1-ethylpropyl; halo (C.sub.1-C.sub.3) alkyl; acyl or haloacyl selected from acetyl, propionyl, chloro-acetyl, trifluoroacetyl; (C.sub.3-C.sub.6) cycloalkylcarbonyl; (C.sub.6-C.sub.10) aroyl selected from benzoyl or naphthoyl; halo substituted (C.sub.6-C.sub.10)aroyl, (C.sub.1-C.sub.4) alkylbenzoyl, or (heterocycle) carbonyl, the heterocycle as defined hereinabove; (C.sub.1-C.sub.4)alkoxycarbonyl selected from methoxycarbonyl, ethoxycarbonyl, straight or branched propoxycarbonyl, allyloxycarbonyl or straight or branched butoxycarbonyl; and the pharmacologically acceptable organic and inorganic salts or metal complexes..Iaddend.

.Iadd.100. A compound of formula I ##STR00225## wherein X is selected from amino, NR.sup.1R.sup.2, or halogen, the halogen is selected from bromine, chlorine, fluorine or iodine, and when X is NR.sup.1R.sup.2, R.sup.1 is methyl or ethyl and R.sup.2 is methyl or ethyl; R is R.sup.4(CH.sub.2).sub.nCO--; n=1-4; and R.sup.4 is monosubstituted or disubstituted amino selected from straight or branched (C.sub.1-C.sub.6)alkylamino, with the alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl, 1,1-dimethylethyl, 2-methylbutyl, 1,1-dimethylpropyl, 2,2-dimethylpropyl, 3-methylbutyl, n-hexyl, 1-methylpentyl, 1,1-dimethylbutyl, 2,2-dimethylbutyl, 2-methylpentyl, 1,2-dimethylbutyl, 1,3-dimethybutyl or 1-methyl-1-ethylpropyl and pharmacologically acceptable organic and inorganic salts or metal complexes..Iaddend.

.Iadd.101. A compound of formula I ##STR00226## wherein X is N(CH.sub.3).sub.2 and R is R.sup.4(CH.sub.2).sub.nCO-- where n=1-4 and R.sup.4 is monosubstituted or disubstituted amino selected from straight or branched (C.sub.1-C.sub.6)alkylamino, with the alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl, 1,1-dimethylethyl, 2-methylbutyl, 1,1-dimethylpropyl, 2,2-dimethylpropyl, 3-methylbutyl, n-hexyl, 1-methylpentyl, 1,1-dimethylbutyl, 2,2-dimethylbutyl, 2-methylpentyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl or 1-methyl-1-ethylpropyl and pharmacologically acceptable organic and inorganic salts or metal complexes..Iaddend.

.Iadd.102. A compound of formula I ##STR00227## wherein X is N(CH.sub.3).sub.2 and R is R.sup.4(CH.sub.2).sub.nCO-- where n=1 and R.sup.4 is monosubstituted or disubstituted amino selected from straight or branched (C.sub.1-C.sub.6)alkylamino, with the alkyl selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl, 1,1-dimethylethyl, 2-methylbutyl, 1,1-dimethylpropyl, 2,2-dimethylpropyl, 3-methylbutyl, n-hexyl, 1-methylpentyl, 1,1-dimethylbutyl, 2,2-dimethylbutyl, 2-methylpentyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl or 1-methyl-1-ethylpropyl and pharmacologically acceptable organic and inorganic salts or metal complexes..Iaddend.

.Iadd.103. A compound of the following structure: ##STR00228## wherein R.sup.4 is a monsubstituted straight or branched C.sub.4-alkylamino, and pharmacologically acceptable organic and inorganic salts or metal complexes..Iaddend.
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