.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 5,530,117

« Back to Dashboard

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
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc