Details for Patent: 5,530,117

Title:	7-substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines
Abstract:	The disclosure is drawn to novel 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds. These compounds are useful to treat infections caused by a wide spectrum of bacterial organisms, including those which are resistant to tetracycline.
Inventor(s):	Hlavka; Joseph J. (Tuxedo Park, NY), Sum; Phaik-Eng (Pomona, NY), Gluzman; Yakov (Upper Saddle River, NJ), Lee; Ving J. (Monsey, NY), Ross; Adma A. (Airmont, NY)
Assignee:	American Cyanamid Company (Wayne, NJ)
Filing Date:	May 31, 1995
Application Number:	08/455,923
Claims:	1. A compound of the formula: ##STR221## wherein Y is NO.sub.2 ; 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 --; n is an integer between 0 and 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, and phenylamino; disubstituted amino selected from dimethylamino, diethylamino, ethyl(1-methylethyl)amino, monomethylbenzylamino, piperidinyl, morpholinyl, 1-imidazolyl, 1-pyrrolyl, 1-(1,2,3-triazolyl) and 4-(1,2,4-triazolyl); (C.sub.3 -C.sub.6)cycloalkyl group selected from cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl; substituted (C.sub.3 -C.sub.6)cycloalkyl group wherein the substitution is selected from (C.sub.1 -C.sub.3)alkyl, cyano, amino and (C.sub.1 -C.sub.3)acyl; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl or .beta.-napthyl; substituted (C.sub.6 -C.sub.10)aryl wherein the substitution is 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 and carboxy; (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; .alpha.-amino(C.sub.1 -C.sub.4)alkyl group selected from .alpha.-aminomethyl, .alpha.-aminoethyl, .alpha.-aminopropyl and .alpha.-aminobutyl; carboxy(C.sub.2 -C.sub.4)alkylamino group selected from aminoacetic acid, .alpha.-aminobutyric acide, .alpha.-aminoproprionic acid, and their optical isomers; (C.sub.7 -C.sub.9)aralkylamino group; substituted (C.sub.1 -C.sub.4)alkoxycarbonylamino group wherein the substitution is selected from phenyl or p-hydroxyphenyl; .alpha.-hydroxy(C.sub.1 -C.sub.3)alkyl group selected from hydroxymethyl, .alpha.-hydroxyethyl, .alpha.-hydroxy-1-methylethyl and .alpha.-hydroxypropyl; .alpha.-mercapto(C.sub.1 -C.sub.3)alkyl group selected from mercaptomethyl, .alpha.-mercaptoethyl, .alpha.-mercapto-1-methylethyl and .alpha.-mercaptopropyl; halo (C.sub.1 -C.sub.3)alkyl group; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR222## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR223## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR224## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; 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)cycloalkylcarbonyl, (C.sub.6 -C.sub.10)aroyl selected from benzoyl or napthoyl, halo-substituted (C.sub.6 -C.sub.10)aroyl, (C.sub.1 -C.sub.4)alkylbenzoyl, and (heterocycle)carbonyl wherein the heterocycle is selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR225## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR226## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR227## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; (C.sub.1 -C.sub.4)alkoxycarbonyl group selected from methoxycarbonyl, ethoxycarbonyl, straght or branched propoxycarbonyl, straight or branched butoxycarbonyl and allyloxycarbonyl; vinyl or substituted vinyl wherein the substitution is selected from (C.sub.1 -C.sub.3)alkyl group; halogen; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl, .beta.-napthyl; substituted (C.sub.6 -C.sub.10)aryl group wherein the substitution is 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 and carboxy; halo(C.sub.1 -C.sub.3)alkyl group; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optionally having a benzo or pyrido ring fused thereto selected from ##STR228## wherein Z is N, O, S, or Se; (C.sub.1 -C.sub.4)alkoxy group; C.sub.6 -aryloxy group selected from phenoxy or substituted phenoxy where the substitution is selected from halo, (C.sub.1 -C.sub.4)alkyl, nitro, cyano, thiol, amino, carboxy, and di(C.sub.1 -C.sub.3)alkylamino; (C.sub.7 -C.sub.10)aralkoxy group; vinyloxy or substituted vinyloxy group wherein the substitution is selected from (C.sub.1 -C.sub.4)alkyl, cyano, carboxy, and (C.sub.6 -C.sub.10)aryl selected from phenyl, .alpha.-napthyl, and .beta.-napthyl; R.sup.a R.sup.b amino(C.sub.1 -C.sub.4)alkoxy or R.sup.a R.sup.b aminoxy group wherein R.sup.a R.sup.b is selected from 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, 1,1-dimethylethyl, (CH.sub.2).sub.n where n is from 2 to 6, and --(CH.sub.2).sub.2 W(CH.sub.2).sub.2 -- wherein W is selected from --N(C.sub.1 -C.sub.3)alkyl wherein alkyl is straight or branched, --NH, NOB where B is selected from hydrogen or (C.sub.1 -C.sub.4)alkyl, O, and S; and when R=R.sup.4 (CH.sub.2).sub.n CO-- and n=1-4, R.sup.4 is selected from amino; (C.sub.3 -C.sub.6)cycloalkyl group selected from cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl; substituted (C.sub.3 -C.sub.6)cycloalkyl group wherein the substitution is selected from (C.sub.1 -C.sub.3)alkyl, cyano, amino and (C.sub.1 -C.sub.3)acyl; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl or .beta.-napthyl; substituted (C.sub.6 -C.sub.10)aryl wherein the substitution is 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 and carboxy; (C.sub.7 -C.sub. 9)aralkyl group; acyloxy or haloacyloxy group wherein the acyl or haloacyl is selected from acetyl, propionyl, chloroacetyl, trifluoroacetyl, (C.sub.3 -C.sub.6)cycloalkylcarbonyl,(C.sub.6 -C.sub.10)aroyl selected from benzoyl or napthoyl, halo-substituted(C.sub.6 -C.sub.10)aroyl, (C.sub.1 -C.sub.4)alkylbenzoyl, and (heterocycle)carbonyl wherein the heterocycle is selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR229## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR230## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR231## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; (C.sub.1 -C.sub.4)alkoxy group; C.sub.6 -aryloxy group selected from phenoxy or substituted phenoxy where the substitution is selected from halo, (C.sub.1 -C.sub.4)alkyl, nitro, cyano, thiol, amino, carboxy, and di(C.sub.1 -C.sub.3)alkylamino; (C.sub.7 -C.sub.10)aralkoxy group; (C.sub.1 -C.sub.3)alkylthio group selected from methylthio, ethylthio, propylthio or allylthio; C.sub.6 -arylthio group selected from phenylthio or substituted phenylthio wherein the substitution is selected from halo, (C.sub.1 -C.sub.4)alkyl, nitro, cyano, thiol, amino, carboxy, and di(C.sub.1 -C.sub.3)alkylamino; C.sub.6 -arylsulfonyl group selected from phenylsulfonyl or substituted phenylsulfonyl wherein the substitution is 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, and carboxy; (C.sub.7 -C.sub.8)aralkylthio group; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR232## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR233## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR234## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; hydroxy group; mercapto group; mono- or di-straight or branched chain (C.sub.1 -C.sub.6)alkylamino group wherein alkyl is 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, and 1-methyl-1-ethylpropyl; (C.sub.2 -C.sub.5)azacycloalkyl group; carboxy(C.sub.2 -C.sub.4)alkylamino group selected from aminoacetic acid, .alpha.-aminopropionic acid, .alpha.-aminobutyric acid and their optical isomers; .alpha.-hydroxy(C.sub.1 -C.sub.3)alkyl group selected from hydroxymethyl, .alpha.-hydroxyethyl, .alpha.-hydroxy-1-methylethyl, and .alpha.-hydroxypropyl; halo(C.sub.1 -C.sub.3)alkyl group; acyl or haloacyl group selected from acetyl, propionyl, chloroacetyl, trifluoroacetyl, (C.sub.3 -C.sub.6)cycloalkylcarbonyl, (C.sub.6 -C.sub.10)aroyl selected from benzoyl or napthoyl, halo-substituted(C.sub.6 -C.sub.10)aroyl, (C.sub.1 -C.sub.4)alkylbenzoyl, and (heterocycle)carbonyl wherein the heterocycle is selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR235## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR236## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR237## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; (C.sub.1 -C.sub.4)alkoxycarbonylamino group selected from tert-butoxycarbonylamino, allyloxycarbonylamino, methoxycarbonylamino, ethoxycarbonylamino, and propoxycarbonylamino; (C.sub.1 -C.sub.4)alkoxycarbonyl group selected from methoxycarbonyl, ethoxycarbonyl, straight or branched propoxycarbonyl, allyloxycarbonyl, and straight or branched butoxycarbonyl; R.sup.a R.sup.b amino(C.sub.1 -C.sub.4)alkoxy or R.sup.a R.sup.b aminoxy group wherein R.sup.a R.sup.b is selected from 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, 1,1-dimethylethyl, (CH.sub.2).sub.n where n is from 2 to 6, and --(CH.sub.2).sub.2 W(CH.sub.2).sub.2 -- wherein W is selected from --N(C.sub.1 -C.sub.3)alkyl wherein alkyl is straight or branched, --NH, NOB where B is selected from hydrogen or (C.sub.1 -C.sub.4)alkyl, O, and S; and when R=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, and phenylamino; disubstituted amino selected from dimethylamino, diethylamino, ethyl(1-methylethyl)amino, monomethylbenzylamino, piperidinyl, morpholinyl, 1-imidazolyl, 1-pyrrolyl, 1-(1,2,3-triazolyl) and 4-(1,2,4-triazolyl); straight or branched (C.sub.1 -C.sub.4)alkyl group selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl, and 1,1-dimethylethyl; (C.sub.3 -C.sub.6)cycloalkyl group selected from cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl; substituted (C.sub.3 -C.sub.6)cycloalkyl group wherein the substitution is selected from (C.sub.1 -C.sub.3)alkyl, cyano, amino and (C.sub.1 -C.sub.3)acyl; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl or .beta.-napthyl; substituted (C.sub.6 -C.sub.10)aryl wherein the substitution is 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 and carboxy; (C.sub.7 -C.sub.9)aralkyl group; halo (C.sub.1 -C.sub.3)alkyl group; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR238## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR239## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR240## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; R.sup.a R.sup.b amino(C.sub.1 -C.sub.4)alkoxy or R.sup.a R.sup.b aminoxy group wherein R.sup.a R.sup.b is selected from 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, 1,1-dimethylethyl, (CH.sub.2).sub.n where n is from 2 to 6, and --(CH.sub.2).sub.2 W(CH.sub.2).sub.2 -- wherein W is selected from --N(C.sub.1 -C.sub.3)alkyl wherein alkyl is straight or branched, --NH, NOB where B is selected from hydrogen or (C.sub.1 -C.sub.4)alkyl, O, and S; and when R=R.sup.4' (CH.sub.2).sub.n SO.sub.2 -- and n=1-4, R.sup.4 is selected from hydrogen; amino; straight or branched (C.sub.1 -C.sub.4)alkyl group selected from methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl, and 1,1-dimethylethyl; (C.sub.1 -C.sub.4)carboxyalkyl group; (C.sub.3 -C.sub.6)cycloalkyl group selected from cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl; substituted (C.sub.3 -C.sub.6)cycloalkyl group wherein the substitution is selected from (C.sub.1 -C.sub.3)alkyl, cyano, amino and (C.sub.1 -C.sub.3)acyl; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl or .beta.-napthyl; substituted (C.sub.6 -C.sub.10)aryl wherein the substitution is 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 and carboxy; (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; (C.sub.1 -C.sub.4)alkoxy group; C.sub.6 -aryloxy group selected from phenoxy or substituted phenoxy where the substitution is selected from halo, (C.sub.1 -C.sub.4)alkyl, nitro, cyano, thiol, amino, carboxy, and di(C.sub.1 -C.sub.3)alkylamino; (C.sub.7 -C.sub.10)aralkoxy group; R.sup.a R.sup.b amino(C.sub.1 -C.sub.4)alkoxy or R.sup.a R.sup.b aminoxy group wherein R.sup.a R.sup.b is selected from 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, 1,1-dimethylethyl, (CH.sub.2).sub.n where n is from 2 to 6, and --(CH.sub.2).sub.2 W(CH.sub.2).sub.2 -- wherein W is selected from --N(C.sub.1 -C.sub.3)alkyl wherein alkyl is straight or branched, --NH, NOB where B is selected from hydrogen or (C.sub.1 -C.sub.4)alkyl, O, and S; (C.sub.1 -C.sub.3)alkylthio group selected from methylthio, ethylthio, propylthio or allylthio; C.sub.6 -arylthio group selected from phenylthio or substituted phenylthio wherein the substitution is selected from halo, (C.sub.1 -C.sub.4)alkyl, nitro, cyano, thiol, amino, carboxy, and di(C.sub.1 -C.sub.3)alkylamino; (C.sub.7 -C.sub.8)aralkylthio group; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR241## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR242## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR243## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; hydroxy group; mercapto group; mono- or di-straight or branched chain (C.sub.1 -C.sub.6)alkylamino group wherein alkyl is 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, and 1-methyl-1-ethylpropyl; acyl or haloacyl group selected from acetyl, propionyl, chloroacetyl, trifluoroacetyl, (C.sub.3 -C.sub.6)cycloalkylcarbonyl, (C.sub.6 -C.sub.10)aroyl selected from benzoyl or napthoyl, halo-substituted(C.sub.6 -C.sub.10)aroyl, (C.sub.1 -C.sub.4)alkylbenzoyl, and (heterocycle)carbonyl wherein the heterocycle is selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR244## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR245## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR246## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; (C.sub.1 -C.sub.4)alkoxycarbonyl group selected from methoxycarbonyl, ethoxycarbonyl, straght or branched propoxycarbonyl, straight or branched butoxycarbonyl and allyloxycarbonyl; R.sup.5 is selected from hydrogen; straight or branched (C.sub.1 -C.sub.3)alkyl group selected from methyl, ethyl, n-propyl, or 1-methylethyl; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl, or .beta.-napthyl; (C.sub.7 -C.sub.9)aralkyl group; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR247## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR248## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR249## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; --(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; and (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 from methyl, ethyl, n-propyl, or 1-methylethyl; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl, or .beta.-napthyl; (C.sub.7 -C.sub.9)aralkyl group; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR250## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR251## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR252## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; --(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; and (C.sub.6 -C.sub.10)aryl group 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.n where n=0-1; --NH; --N(C.sub.1 -C.sub.3)alkyl where alkyl is straight or branched; --N(C.sub.1 -C.sub.4)alkoxy; O; S; and congeners selected from (L or D)proline, ethyl(L or D)prolinate, morphiline, pyrrolidine and piperidine; or a pharmacologically acceptable organic or inorganic salt or metal complex thereof. 2. The compound according to claim 1, wherein Y is NO.sub.2 ; 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 --; n is an integer between 0 and 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, and phenylamino; disubstituted amino selected from dimethylamino, diethylamino, ethyl(1-methylethyl)amino, monomethylbenzylamino, piperidinyl, morpholinyl, 1-imidazolyl, 1-pyrrolyl, 1-(1,2,3-triazolyl) and 4-(1,2,4-triazolyl); (C.sub.3 -C.sub.6)cycloalkyl group selected from cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl; substituted (C.sub.3 -C.sub.6)cycloalkyl group wherein the substitution is selected from (C.sub.1 -C.sub.3)alkyl, cyano, amino and (C.sub.1 -C.sub.3)acyl; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl or .beta.-napthyl; substituted (C.sub.6 -C.sub.10)aryl wherein the substitution is 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 and carboxy; .alpha.-amino(C.sub.1 -C.sub.4)alkyl group selected from .alpha.-aminomethyl, .alpha.-aminoethyl, .alpha.-aminopropyl and .alpha.-aminobutyl; carboxy(C.sub.2 -C.sub.4)alkylamino group selected from aminoacetic acid, .alpha.-aminobutyric acide, .alpha.-aminoproprionic acid, and their optical isomers; (C.sub.7 -C.sub.9)aralkylamino group; substituted (C.sub.1 - C.sub.4)alkoxycarbonylamino group wherein the substitution is selected from phenyl or p-hydroxyphenyl; .alpha.-hydroxy(C.sub.1 -C.sub.3)alkyl group selected from hydroxymethyl, .alpha.-hydroxyethyl, .alpha.-hydroxy-1-methylethyl and .alpha.-hydroxypropyl; halo C.sub.1 -C.sub.3)alkyl group; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR253## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR254## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR255## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; 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)cycloalkylcarbonyl, (C.sub.6 -C.sub.10)aroyl selected from benzoyl or napthoyl, halo-substituted(C.sub.6 -C.sub.10)aroyl, (C.sub.1 -C.sub.4)alkylbenzoyl, and (heterocycle)carbonyl wherein the heterocycle is selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR256## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR257## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR258## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; (C.sub.1 -C.sub.4)alkoxycarbonyl group selected from methoxycarbonyl, ethoxycarbonyl, straght or branched propoxycarbonyl, straight or branched butoxycarbonyl and allyloxycarbonyl; vinyl or substituted vinyl wherein the substitution is selected 649 from (C.sub.1 -C.sub.3)alkyl group; halogen; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl, .beta.-napthyl; substituted (C.sub.6 -C.sub.10)aryl group wherein the substitution is 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 and carboxy; halo(C.sub.1 -C.sub.3)alkyl group; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optionally having a benzo or pyrido ring fused thereto selected from ##STR259## wherein Z is N, O, S, or Se; (C.sub.1 -C.sub.4)alkoxy group; C.sub.6 -aryloxy group selected from phenoxy or substituted phenoxy where the substitution is selected from halo, (C.sub.1 -C.sub.4)alkyl, nitro, cyano, thiol, amino, carboxy, and di(C.sub.1 -C.sub.3)alkylamino; (C.sub.7 -C.sub.10)aralkoxy group; vinyloxy or substituted vinyloxy group wherein the substitution is selected from (C.sub.1 -C.sub.4)alkyl, cyano, carboxy, and (C.sub.6 -C.sub.10)aryl selected from phenyl, .alpha.-napthyl, and .beta.-napthyl; R.sup.a R.sup.b amino(C.sub.1 -C.sub.4)alkoxy or R.sup.a R.sup.b aminoxy group wherein R.sup.a R.sup.b is selected from 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, 1,1-dimethylethyl, (CH.sub.2).sub.n where n is from 2 to 6, and --(CH.sub.2).sub.2 W(CH.sub.2).sub.2 -- wherein W is selected from --N(C.sub.1 -C.sub.3)alkyl wherein alkyl is straight or branched, --NH, NOB where B is selected from hydrogen or (C.sub.1 -C.sub.4)alkyl, O, and S; and when R=R.sup.4 (CH.sub.2).sub.n CO-- and n=1-4, R.sup.4 is selected from amino; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl or .beta.-napthyl; substituted (C.sub.6 -C.sub.10)aryl wherein the substitution is 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 and carboxy; acyloxy or haloacyloxy group wherein the acyl or haloacyl is selected from acetyl, propionyl, chloroacetyl, trifluoroacetyl, (C.sub.3 -C.sub.6)cycloalkylcarbonyl,(C.sub.6 -C.sub.10)aroyl selected from benzoyl or napthoyl, halo-substituted(C.sub.6 -C.sub.10)aroyl, (C.sub.1 -C.sub.4)alkylbenzoyl, and (heterocycle)carbonyl wherein the heterocycle is selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR260## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR261## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR262## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; (C.sub.1 -C.sub.4)alkoxy group; C.sub.6 -aryloxy group selected from phenoxy or substituted phenoxy where the substitution is selected from halo, (C.sub.1 -C.sub.4)alkyl, nitro, cyano, thiol, amino, carboxy, and di(C.sub.1 -C.sub.3)alkylamino; (C.sub.1 -C.sub.3)alkylthio group selected from methylthio, ethylthio, propylthio or allylthio; C.sub.6 -arylthio group selected from phenylthio or substituted phenylthio wherein the substitution is selected from halo, (C.sub.1 -C.sub.4)alkyl, nitro, cyano, thiol, amino, carboxy, and di(C.sub.1 -C.sub.3)alkylamino; C.sub.6 -arylsulfonyl group selected from phenylsulfonyl or substituted phenylsulfonyl wherein the substitution is 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, and carboxy; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR263## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR264## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR265## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; hydroxy group; .alpha.-hydroxy(C.sub.1 -C.sub.3)alkyl group selected from hydroxymethyl, .alpha.-hydroxyethyl, .alpha.-hydroxy-1-methylethyl, and .alpha.-hydroxypropyl; halo (C.sub.1 -C.sub.3)alkyl group; acyl or haloacyl group selected from acetyl, propionyl, chloroacetyl, trifluoroacetyl, (C.sub.3 -C.sub.6)cycloalkylcarbonyl, (C.sub.6 -C.sub.10)aroyl selected from benzoyl or napthoyl, halo-substituted(C.sub.6 -C.sub.10)aroyl, (C.sub.1 -C.sub.4)alkylbenzoyl, and (heterocycle)carbonyl wherein the heterocycle is selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR266## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR267## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR268## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; (C.sub.1 -C.sub.4)alkoxycarbonylamino group selected from tert-butoxycarbonylamino, allyloxycarbonylamino, methoxycarbonylamino, ethoxycarbonylamino, and propoxycarbonylamino; R.sup.a R.sup.b amino(C.sub.1 -C.sub.4)alkoxy or R.sup.a R.sup.b aminoxy group wherein R.sup.a R.sup.b is selected from 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, 1,1-dimethylethyl, (CH.sub.2).sub.n where n is from 2 to 6, and --(CH.sub.2).sub.2 W(CH.sub.2).sub.2 -- wherein W is selected from --N(C.sub.1 -C.sub.3)alkyl wherein alkyl is straight or branched, --NH, NOB where B is selected from hydrogen or (C.sub.1 -C.sub.4)alkyl, O, and S; and when R=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, and phenylamino; disubstituted amino selected from dimethylamino, diethylamino, ethyl(1-methylethyl)amino, monomethylbenzylamino, piperidinyl, morpholinyl, 1-imidazolyl, 1-pyrrolyl, 1-(1,2,3-triazolyl) and 4-(1,2,4-triazolyl); straight or branched (C.sub.1 -C.sub.4)alkyl group selected from methyl, ethyl, n-propyl, and 1-methylethyl; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl or .beta.-napthyl; substituted (C.sub.6 -C.sub.10)aryl wherein the substitution is 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 and carboxy; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR269## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR270## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR271## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; and when R=R.sup.4' (CH.sub.2).sub.n SO.sub.2 -- and n=1-4, R.sup.4 is selected from hydrogen; amino; straight or branched (C.sub.1 -C.sub.4)alkyl group selected from methyl, ethyl, n-propyl, and 1-methylethyl; (C.sub.1 -C.sub.4)carboxyalkyl group; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl or .beta.-napthyl; substituted (C.sub.6 -C.sub.10)aryl wherein the substitution is 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 and carboxy; (C.sub.1 -C.sub.4)alkoxy group; C.sub.6 -aryloxy group selected from phenoxy or substituted phenoxy where the substitution is selected from halo, (C.sub.1 -C.sub.4)alkyl, nitro, cyano, thiol, amino, carboxy, and di(C.sub.1 -C.sub.3)alkylamino; (C.sub.7 -C.sub.10)aralkoxy group; R.sup.5 is selected from hydrogen; straight or branched (C.sub.1 -C.sub.3)alkyl group selected from methyl, ethyl, n-propyl, or 1-methylethyl; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl, or .beta.-napthyl; (C.sub.7 -C.sub.9)aralkyl group; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR272## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR273## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR274## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; --(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; and (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 from methyl, ethyl, n-propyl, or 1-methylethyl; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl, or .beta.-napthyl; (C.sub.7 -C.sub.9)aralkyl group; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR275## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR276## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR277## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; --(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; and (C.sub.6 -C.sub.10)aryl group 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.n where n=0-1; --NH; --N(C.sub.1 -C.sub.3)alkyl where alkyl is straight or branched; --N(C.sub.1 -C.sub.4)alkoxy; O; S; and congeners selected from (L or D)proline, ethyl(L or D)prolinate, morphiline, pyrrolidine and piperidine; or a pharmacologically acceptable organic or inorganic salt or metal complex thereof. 3. The compound of claim 1 wherein Y is NO.sub.2 ; 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 --; n is an integer between 0 and 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, and phenylamino; disubstituted amino selected from dimethylamino, diethylamino, ethyl(1-methylethyl)amino, monomethylbenzylamino, piperidinyl, morpholinyl, 1-imidazolyl, 1-pyrrolyl, 1-(1,2,3-triazolyl) and 4-(1,2,4-triazolyl); (C.sub.3 -C.sub.6)cycloalkyl group selected from cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl; substituted (C.sub.3 -C.sub.6)cycloalkyl group wherein the substitution is selected from (C.sub.1 -C.sub.3)alkyl, cyano, amino and C.sub.1 -C.sub.3)acyl; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl or .beta.-napthyl; substituted (C.sub.6 -C.sub.10)aryl wherein the substitution is 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 and carboxy; .alpha.-amino(C.sub.1 -C.sub.4)alkyl group selected from .alpha.-aminomethyl, .alpha.-aminoethyl, .alpha.-aminopropyl and .alpha.-aminobutyl; carboxy(C.sub.2 -C.sub.4)alkylamino group selected from aminoacetic acid, .alpha.-aminobutyric acide, .alpha.-aminoproprionic acid, and their optical isomers; (C.sub.7 -C.sub.9)aralkylamino group; substituted (C.sub.1 -C.sub.4)alkoxycarbonylamino group wherein the substitution is selected from phenyl or p-hydroxyphenyl; .alpha.-hydroxy(C.sub.1 -C.sub.3)alkyl group selected from hydroxymethyl, .alpha.-hydroxyethyl, .alpha.-hydroxy-1-methylethyl and .alpha.-hydroxypropyl; halo C.sub.1 -C.sub.3)alkyl group; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR278## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR279## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR280## wherein A is selected from hydrogen; straight or branched C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; 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)cycloalkylcarbonyl, (C.sub.6 -C.sub.10)aroyl selected from benzoyl or napthoyl, halo-substituted(C.sub.6 -C.sub.10)aroyl, (C.sub.1 -C.sub.4)alkylbenzoyl, and (heterocycle)carbonyl wherein the heterocycle is selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR281## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR282## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR283## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; (C.sub.1 -C.sub.4)alkoxycarbonyl group selected from methoxycarbonyl, ethoxycarbonyl, straght or branched propoxycarbonyl, straight or branched butoxycarbonyl and allyloxycarbonyl; vinyl or substituted vinyl wherein the substitution is selected from (C.sub.1 -C.sub.3)alkyl group; halogen; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl, .beta.-napthyl; substituted (C.sub.6 -C.sub.10)aryl group wherein the substitution is 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 and carboxy; halo(C.sub.1 -C.sub.3)alkyl group; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optionally having a benzo or pyrido ring fused thereto selected from ##STR284## wherein Z is N, O, S, or Se; (C.sub.1 -C.sub.4)alkoxy group; C.sub.6 -aryloxy group selected from phenoxy or substituted phenoxy where the substitution is selected from halo, (C.sub.1 -C.sub.4)alkyl, nitro, cyano, thiol, amino, carboxy, and di(C.sub.1 -C.sub.3)alkylamino; (C.sub.7 -C.sub.10)aralkoxy group; vinyloxy or substituted vinyloxy group wherein the substitution is selected from (C.sub.1 -C.sub.4)alkyl, cyano, carboxy, and (C.sub.6 -C.sub.10)aryl selected from phenyl, .alpha.-napthyl, and .beta.-napthyl; R.sup.a R.sup.b amino(C.sub.1 -C.sub.4)alkoxy or R.sup.a R.sup.b aminoxy group wherein R.sup.a R.sup.b is selected from 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, 1,1-dimethylethyl, (CH.sub.2).sub.n where n is from 2 to 6, and --(CH.sub.2).sub.2 W(CH.sub.2).sub.2 -- wherein W is selected from --N(C.sub.1 -C.sub.3)alkyl wherein alkyl is straight or branched, --NH, NOB where B is selected from hydrogen or (C.sub.1 -C.sub.4)alkyl, O, and S; and when R=R.sup.4 (CH.sub.2).sub.n CO-- and n=1-4, R.sup.4 is selected from amino; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl or .beta.-napthyl; substituted (C.sub.6 -C.sub.10)aryl wherein the substitution is 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 and carboxy; acyloxy or haloacyloxy group wherein the acyl or haloacyl is selected from acetyl, propionyl, chloroacetyl, trifluoroacetyl, (C.sub.3 -C.sub.6)cycloalkylcarbonyl,(C.sub.6 -C.sub.10)aroyl selected from benzoyl or napthoyl, halo-substituted(C.sub.6 -C.sub.10)aroyl, (C.sub.1 -C.sub.4)alkylbenzoyl, and (heterocycle)carbonyl wherein the heterocycle is selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR285## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR286## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR287## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; (C.sub.1 -C.sub.4)alkoxy group; C.sub.6 -aryloxy group selected from phenoxy or substituted phenoxy where the substitution is selected from halo, (C.sub.1 -C.sub.4)alkyl, nitro, cyano, thiol, amino, carboxy, and di(C.sub.1 -C.sub.3)alkylamino; (C.sub.1 -C.sub.3)alkylthio group selected from methylthio, ethylthio, propylthio or allylthio; C.sub.6 -arylthio group selected from phenylthio or substituted phenylthio wherein the substitution is selected from halo, (C.sub.1 -C.sub.4)alkyl, nitro, cyano, thiol, amino, carboxy, and di(C.sub.1 -C.sub.3)alkylamino; C.sub.6 -arylsulfonyl group selected from phenylsulfonyl or substituted phenylsulfonyl wherein the substitution is 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, and carboxy; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR288## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR289## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR290## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; hydroxy group; .alpha.-hydroxy(C.sub.1 -C.sub.3)alkyl group selected from hydroxymethyl, .alpha.-hydroxyethyl, .alpha.-hydroxy-1-methylethyl, and .alpha.-hydroxypropyl; halo(C.sub.1 -C.sub.3)alkyl group; acyl or haloacyl group selected from acetyl, propionyl, chloroacetyl, trifluoroacetyl, (C.sub.3 -C.sub.6)cycloalkylcarbonyl, (C.sub.6 -C.sub.10)aroyl selected from benzoyl or napthoyl, halo-substituted(C.sub.6 -C.sub.10)aroyl, (C.sub.1 -C.sub.4)alkylbenzoyl, and (heterocycle)carbonyl wherein the heterocycle is selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR291## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR292## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR293## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; (C.sub.1 -C.sub.4)alkoxycarbonylamino group selected from tert-butoxycarbonylamino, allyloxycarbonylamino, methoxycarbonylamino, ethoxycarbonylamino, and propoxycarbonylamino; R.sup.a R.sup.b amino(C.sub.1 -C.sub.4)alkoxy or R.sup.a R.sup.b aminoxy group wherein R.sup.a R.sup.b is selected from 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, 1,1-dimethylethyl, (CH.sub.2).sub.n where n is from 2 to 6, and --(CH.sub.2).sub.2 W(CH.sub.2).sub.2 -- wherein W is selected from --N(C.sub.1 -C.sub.3)alkyl wherein alkyl is straight or branched, --NH, NOB where B is selected from hydrogen or (C.sub.1 -C.sub.4)alkyl, O, and S; and when R=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, and phenylamino; disubstituted amino selected from dimethylamino, diethylamino, ethyl(1-methylethyl)amino, monomethylbenzylamino, piperidinyl, morpholinyl, 1-imidazolyl, 1-pyrrolyl, 1-(1,2,3-triazolyl) and 4-(1,2,4-triazolyl); straight or branched (C.sub.1 -C.sub.4)alkyl group selected from methyl, ethyl, n-propyl, and 1-methylethyl; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl or .beta.-napthyl; substituted (C.sub.6 -C.sub.10)aryl wherein the substitution is 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 and carboxy; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR294## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR295## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR296## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; and when R=R.sup.4' (CH.sub.2).sub.n SO.sub.2 -- and n=1-4, R.sup.4 is selected from hydrogen; amino; straight or branched (C.sub.1 -C.sub.4)alkyl group selected from methyl, ethyl, n-propyl, and 1-methylethyl; R.sup.a R.sup.b amino(C.sub.1 -C.sub.4)alkoxy or R.sup.a R.sup.b aminoxy group wherein R.sup.a R.sup.b is selected from 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, 1,1-dimethylethyl, (CH.sub.2).sub.n where n is from 2 to 6, and --(CH.sub.2).sub.2 W(CH.sub.2).sub.2 -- wherein W is selected from --N(C.sub.1 -C.sub.3)alkyl wherein alkyl is straight or branched, --NH, NOB where B is selected from hydrogen or (C.sub.1 -C.sub.4)alkyl, O, and S; R.sup.5 is selected from hydrogen; straight or branched (C.sub.1 -C.sub.3)alkyl group selected from methyl, ethyl, n-propyl, or 1-methylethyl; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl, or .beta.-napthyl; (C.sub.7 -C.sub.9)aralkyl group; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR297## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR298## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR299## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substituted C.sub.6 -aryl wherein the substitution is 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 and carboxy; and (C.sub.7 -C.sub.9)aralkyl group selected from benzyl, 1-phenylethyl, 2-phenylethyl and phenylpropyl; a six membered aromatic ring with one to three N, O, S, or Se heteroatoms; a six membered saturated ring with one or two N, O, S or Se heteroatoms and an adjacent appended O heteroatom; --(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; and (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 from methyl, ethyl, n-propyl, or 1-methylethyl; (C.sub.6 -C.sub.10)aryl group selected from phenyl, .alpha.-napthyl, or .beta.-napthyl; (C.sub.7 -C.sub.9)aralkyl group; a heterocycle group selected from a five membered aromatic or saturated ring with one N, O, S, or Se heteroatom optinally having a benzo or pyrido ring fused thereto selected from ##STR300## wherein Z is N, O, S, or Se; a five membered aromatic ring with two N, O, S, or Se heteroatoms optionally having a benzo or pyrido ring fused thereto selected from ##STR301## wherein Z and Z.sub.1 are independently selected from N, O, S, and Se; a five membered saturated ring with one or two N, O, S, or Se heteroatoms and an adjacent appended O heteroatom selected from ##STR302## wherein A is selected from hydrogen; straight or branched (C.sub.1 -C.sub.4)alkyl; C.sub.6 -aryl; substitu