Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5.alpha.-reductase. Also invented are intermediates used in preparing these compounds.

Abstract: Invented are phosphinic acid substituted analogues of steroidal synthetic compounds, pharamaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size.

Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are intermediates used in preparing these compounds.

Abstract: Invented are 4-aza-5-alpha-8(14)-17 substituted-androsten-3-ones having an 8(14), 7(8), or 16(17) double bond, optionally also having a 1(2) double bond, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-alpha-reductase.

Abstract: Invented are phosphonic acid substituted analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size. Also invented are intermediates used in preparing these compounds.

Abstract: This application relates to 4-amino-4,5-dihydro-2-furancarboxylic acid, and esters thereof, useful as .gamma.-aminobutyric acid transaminase inhibitors.

Abstract: This application relates to 4-amino-4,5-dihydro-2-thiophenecarboxylic acid, the C.sub.1-6 alkyl esters thereof and to their use in the treatment of epilepsy.

Abstract: 5-Amino-4-oxo-pentanoic acids of the formula ##STR1## wherein R is CF.sub.3, CHF.sub.2 or CH.sub.2 F; R.sub.1 is H or akyl of 1-4 carbon atoms; and R.sub.2 is H or alkyl or 1-4 carbon atoms or benzyl, which are intermediates to ACE inhibitors or elastase inhibitors, are produced by reacting a 1-(methylthio)-1-methylsulfinyl)-2-R.sub.1 -ethylmetal with an ester of a 3-R-acrylic acid; optionally R.sub.2 -alkylating the thus-produced ester enolate anion of 4-(methylsulfinyl)-4-(methylthio)-5-R.sub.1 R-pentanoic acid followed by splitting off of methylsulfinic acid; reacting the thus-produced 2-R.sub.2 -5-R.sub.1 -4-(methylthio)-3-R-4-pentenoic acid ester with a source of Br.sup.+ to produce a 5-bromo-substituted acid or ester thereof otherwise corresponding to the desired 5-amino-4-oxo-pentanoic acid; and replacing the bromine atom with an amino group, e.g., via the corresponding 5-azido- and 5-N-acylamino- compounds, with hydrolysis of the ester group, if still remaining.

Abstract: Novel compounds of the formula ##STR1## wherein A is methylene, ethylene or ethylidene; R.sub.1 is --C.tbd.CH or --CH.dbd.CH.sub.2 ; R.sub.2 is hydrogen or COR wherein R is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.5 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms or ##STR2## wherein R.sub.6 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.a is hydrogen, ##STR3## alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched or ##STR4## wherein R.sub.7 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl; and R.sub.b has the same meaning as defined for R.sub.a except R.sub.b is not ##STR5## and R.sub.a and R.sub.

Abstract: Aromatase inhibitors are provided having the formula ##STR1## wherein represents a single or double bond; R is hydrogen or C.sub.1-4 alkyl; R.sup.1 is methyl or ethyl; R.sup.2 is (H) (OR.sup.8) or .dbd.O; R.sup.3 is H or C.sub.1-3 alkyl; R.sup.4 is H or OR.sup.8 ; R.sup.5 is H, C.sub.1-3 alkyl or, when the 5,6-bond is saturated, R.sup.5 is divalent .dbd.O; R.sup.6 and R.sup.7 are each H or C.sub.1-3 alkyl; and R.sup.8 is H or C.sub.2-4 alkanoyl. Intermediates useful in preparing the foregoing aromatase inhibitors, and methods of using the aromatase inhibitors of the invention are also provided.

Abstract: Compounds of the following general formula are testosterone 5.alpha.-reductase inhibitors rendering the compounds useful in the treatment of acne and oily skin and benign prostatic hypertrophy: ##STR1## wherein R is: .dbd.O, --OH, --OCO--alkyl C.sub.1-5, --COOH, --CH.sub.2 OH, --COO--alkyl C.sub.1-6, --COCH.sub.

Abstract: Progesterone derivatives having a vinylidene or a 1-alkynyl substituent at the 18-position and further optionally hydroxylated at the 11-position and the 21-position are described herein. Compounds having both an ethynyl substituent and a hydroxy substituent at the 18-position are also described herein. The compounds are useful as aldosterone inhibitors.

Abstract: Irreversible aromatase inhibitors are provided having the formulae ##STR1## wherein represents a single or a double bond; R.sup.1 is CH.sub.3 or C.sub.2 H.sub.5 ; R.sup.2 is (H) (OR.sup.8) or O; R.sup.3 is H or C.sub.1-3 alkyl; R.sup.4 is H or OR.sup.8 ; R.sup.5 is H.sub.2, O or (H) (C.sub.1-3 alkyl); R.sup.6 and R.sup.7 are each independently H or C.sub.1-3 alkyl; and R.sup.8 is H or C.sub.1-4 alkanoyl. Intermediates useful in preparing the foregoing aromatase inhibitors, methods of using them and a pharmaceutical composition containing them are also provided.

Abstract: Compounds of the following general formula are irreversible inhibitors of pancreatic elastase: ##STR1## wherein M is hydroxy, lower alkoxy, benzyloxy or --NY.sub.1 Y.sub.2 wherein each of R.sub.4 and R.sub.5 is hydrogen or lower alkyl; R is CF.sub.3, CHF.sub.2 or CH.sub.2 F; R.sub.1 is straight or branched lower alkyl; R.sub.2 is defined the same as R.sub.1 or is benzyl; R.sub.30 is CHO, carbobenzoxy, tert-butoxycarbonyl, benzoyl or lower alkanoyl; X is pro, ala or leu and Y and Z together form a single bond; or Y-X is ala-pro, ala-ala or ala-leu and Z forms a single bond; and Z-Y-X is ala-ala-pro, ala-ala-ala or pro-ala-leu.

Abstract: Novel compounds of the formula ##STR1## wherein A is methylene, ethylene or ethylidene; R.sub.1 is --C.tbd.CH or --CH.dbd.CH.sub.2 ; R.sub.2 is hydrogen or COR wherein R is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.5 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms or ##STR2## wherein R.sub.6 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.a is hydrogen, ##STR3## alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched or ##STR4## wherein R.sub.7 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl; and R.sub.b has the same meaning as defined for R.sub.a except R.sub.b is not ##STR5## and R.sub.a and R.sub.

Abstract: Novel acetylenic derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein R is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## is hydrogen, a straight or branched lower alkyl group of 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; each R.sub.1 is the same and is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.3 R.sub.4 wherein each of R.sub.3 and R.sub.4 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms and can be the same or different, or ##STR3## wherein R.sub.5 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; and pharmaceutically acceptable salts and individual optical isomers thereof.

Abstract: Novel acetylenic derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein n is an integer of from 1 to 3; R is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; each R.sub.1 is the same and is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.3 R.sub.4 wherein each of R.sub.3 and R.sub.4 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms and can be the same or different, or ##STR3## wherein R.sub.5 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; and the lactams thereof when n is 2 or 3; and pharmaceutically acceptable salts and individual optical isomers thereof.

Abstract: Compounds of the following general formula and salts thereof are irreversible inhibitors of .gamma.-aminobutyric acid transaminase: ##STR1## wherein R.sub.1 is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, the radical ##STR2## wherein R.sub.4 is hydrogen, a straight or branched alkyl group having from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.2 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, the group-NR.sub.5 R.sub.6wherein each of R.sub.5 and R.sub.6 is hydrogen or a straight or branched alkyl group having from 1 to 4 carbon atoms, or ##STR3## wherein R.sub.7 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; and R.sub.3 is hydrogen or bromine.

Abstract: Novel compounds of the following general formula ##STR1## and pharmaceutically acceptable salts and individual optical isomers thereof. The compounds are useful as aromatic amine decarboxylase inhibitors.

Abstract: Novel compounds of the following general formula are useful pharmacologic agents: ##STR1## R is .[.selected from.]. hydrogen.[., alkylcarbonyl wherein the alkyl moiety contains from 1 to 4 carbon atoms, alkoxycarbonyl wherein the alkoxy moiety contains from 1 to 4 carbon atoms and may be straight or branched, and ##STR2## wherein R.sub.10 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl.].; R.sub.2 is .[.selected from.]. hydroxy.[., a straight or branched alkoxy group of from 1 to 8 carbon atoms, a lower alkylamino group wherein the alkyl moiety contains from 1 to 4 carbon atoms, and ##STR3## wherein R.sub.4 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl, and p-hydroxybenzyl.].; R.sub.3 is .[.selected from.]. hydrogen.[., chlorine, bromine, and iodine.].; [A] is .[.selected from.]. ##STR4## .[.and --CH.dbd.CH--.]. wherein R.sub.1 is .[.selected from.]. hydrogen.[.