Claims
- 1. A compound of the formula ##STR223## 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.dbd.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,
- 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.a R.sup.b amino(C.sub.1 -C.sub.4)alkoxy group, wherein R.sup.a R.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.a R.sup.b is (CH.sub.2).sub.m, m=2-6, or (CH.sub.2).sub.2 W(CH.sub.2)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.a R.sup.b aminoxy group, wherein R.sup.a R.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.a R.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2 W(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.n CO-- 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.a R.sup.b - amino(C.sub.1 -C.sub.4)alkoxy group wherein R.sup.a R.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.a R.sup.b is (CH).sub.m m=2-6 or --(CH.sub.2).sub.2 W(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.a R.sup.b aminoxy group, wherein R.sup.a R.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.a R.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2 W(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).sub.n 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.a R.sup.b amino (C.sub.1 -C.sub.4) alkoxy group, wherein R.sup.a R.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.a R.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2 W--(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.a R.sup.b aminoxy group, wherein R.sup.a R.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.a R.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2 W(CH.sub.2).sub.2 -- wherein W is selected from --N(C.sub.1 -C.sub.3) alkyl, O, S, --NY, --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.n SO.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.a R.sup.b amino (C.sub.1 -C.sub.4) alkoxy, wherein R.sup.a R.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.a R.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2 W(CH.sub.2).sub.2 --wherein W is selected from --N(C.sub.1 -C.sub.3)alkyl, O,S, --NY, or NOB and B is selected from hydrogen or (C.sub.1 -C.sub.3)alkyl; or R.sup.a R.sup.b aminoxy group, wherein R.sup.a R.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.a R.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2 W(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.n COOR.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' 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.2 W(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 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.n CO-- or R.sup.4' (CH.sub.2).sub.n SO.sub.2 --;
- and when R=R.sup.4 (CH.sub.2).sub.n CO-- 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, (C.sub.1 -C.sub.4) alkoxycarbonyl, halo-(C.sub.1 -C.sub.3)alkyl group; (C.sub.1 -C.sub.4)alkoxy group; C.sub.6 -aryloxy group selected form 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.a R.sup.b amino(C.sub.1 -C.sub.4)alkoxy group, wherein R.sup.a R.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.a R.sup.b aminoxy group, wherein R.sup.a R.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.n CO-- 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; disubstituted amino selected from dimethylamino, diethylamino, ethyl(1-methylethyl)amino, monomethylbenzylamino, piperidinyl, morpholinyl, 1-imidazolyl, 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.a R.sup.b amino(C.sub.1 -C.sub.4)alkoxy group, wherein R.sup.a R.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.a R.sup.b is (CH.sub.2).sub.m, m=2-6, or --(CH.sub.2).sub.2 W(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.a R.sup.b aminoxy group, wherein R.sup.a R.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.a R.sup.b is (CH.sub.2).sub.m, m=2-6,or --(CH.sub.2).sub.2 W--(CH.sub.2).sub.2 -- wherein W is selected from --N(C.sub.1 -C.sub.3)-alkyl, O,S, --NY, --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 C.sub.4)alkoxycarbonylamino selected from tert-butoxycarbonylamino, allyloxycarbonylamino, methoxycarbonylamino, ethoxycarbonylamino or propoxycarbonylamino;
- and when R.dbd.R.sup.4' (CH.sub.2).sub.n SO.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 and R.sup.6 taken together are --(CH.sub.2).sub.2 W(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-naphthacenecarboxamide.
- 8. A compound according to claim 1, [4S-(4.alpha.,12a.alpha.)]-9-[(4-Bromo-1-oxobutyl)amino]-4,7-bis(dimethylamino)-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 sulfate.
- 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-methoxybenzoyl)amino]-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-naphthacenecarboxamide.
- 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)amino]-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-nitrobenzoyl)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-dimethylamino)-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-[[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.
- 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-naphthacenecaboxamide.
- 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-naphthacenyl]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-naphthacenecarboxamide 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 (2-diethylamino)ethyl 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]-4,7-bis(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-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-naphthacenecarboxamide.
- 45. 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-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(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,10,12, 12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide.
- 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-[(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.
- 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-[(methanesulfonyl)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]-1,4,4a,5,5a,6,11,12a-octahydro-3,10,12, 12a-tetrahydroxy-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-[[(ethylamino)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-octahydro-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,6,6a,7,10,10a,12-octahydro-1,8,10a,11-tetrahydroxy-10,12-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]amino]-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-oxopropyl]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-oxopropyl]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-naphthacenyl]-alphamethyl-1-pyrrolidineacetamide dihydrochloride.
- 87. A compound according to claim 1 [4S-(4alpha,12aalpha)]-4,7-Bis(dimethylamino)-9-[[4-(dimethylamino)-1-oxobutyl]amino]-1,4,4a,5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-1,11-dioxo-2-napthacenecarboxamide 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-octahydro-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-octahydro-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]amino]-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]amino]-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]amino]-1,4,4a,5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-1,11-dioxo-N-(1-piperidinylmethyl)-2-naphthacenecarboxamide.
- 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-napthacenyl]-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.
Parent Case Info
This application is a continuation of application Ser. No. 07/926,091 filed Aug. 13, 1992, now abandoned, which is a continuation-in-part of application Ser. No. 07/771,576 filed Oct. 4, 1991, now abandoned.
US Referenced Citations (11)
Non-Patent Literature Citations (3)
Entry |
Chopra, Handbook of Experimental Parmacology, vol. 78, 317-392, Springer-Verlag (1985). |
Levy, Antimicrobial Agents and Chemotherapy, vol. 33, No. 8, 1373-1374, (Aug. 1989). |
Salyers, Molecular Microbiology 4(1), 151-156 (1990). |
Continuations (1)
|
Number |
Date |
Country |
Parent |
926091 |
Aug 1992 |
|
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
771576 |
Oct 1991 |
|