Abstract: 2,3-Dihydro-2-oxo-1H-imidazole-4-carboxylic acid derivatives having a 5-(4-phenyl-1-piperidinyl)methyl substituent, are useful as cardiotonics, antihypertensives and antithrombotic agents. The compounds are obtained by the reaction of an appropriate amine with a substituted 5-bromomethyl-2,3-dihydro-2-oxo-1H-imidazole-4-carboxylic acid derivative.

Abstract: 1,3-Dihydro-2H-imidazol-2-ones having 5-acyl and 4-(4-phenyl-1-piperidinyl)methyl substituents, are useful as cardiotonics, antihypertensives and antithrombotic agents. The compounds are obtained by the reaction of an appropriate substituted piperidine with a substituted 4-bromomethyl-1,3-dihydro-2H-imidazol-2-one.

Abstract: Novel compounds of the following general formula are useful pharmacological agents: ##STR1## wherein Y is FCH.sub.2 - or F.sub.2 CH-; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, -NR.sub.10 R.sub.11 wherein each of R.sub.10 and R.sub.11 is hydrogen or a straight or branched alkyl group of from 1 to 4 carbon atoms or ##STR2## wherein R.sub.12 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.2 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 ##STR3## wherein R.sub.8 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; and n is the integer 2 or 3; pharmaceutically acceptable salts and individual optical isomers thereof.

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 formula ##STR1## wherein R.sub.1 is hydrogen, a straight or branched chain alkyl of 1-5 carbon atoms or a straight or branched chain alkanoyl of 1-5 carbon atoms;R.sub.2 is hydrogen, a straight or branched chain alkyl of 1-5 carbon atoms, phenyl, phenyl substituted with halogen, a straight or branched chain alkoxy of 1-5 carbon atoms, a straight or branched chain alkyl of 1-5 carbon atoms or trifluoromethyl or, when R.sub.1 is hydrogen, R.sub.2 can also be a straight or branched chain alkanoyl of 1-5 carbon atoms; orR.sub.1 and R.sub.2 taken together with the nitrogen atom to which they are attached form a saturated heterocyclic ring of 4-7 total ring atoms and 0 or 1 hetero N or O atom in addition to the connecting N atom; or the corresponding heterocyclic ring substituted by a C.sub.1-5 straight or branched chain alkyl group, aryl or aralkyl;R.sub.

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: Novel halomethyl derivatives of amino acids of the following general structure ##STR1## wherein Y is FCH.sub.2 --, F.sub.2 CH.sub.2 --, F.sub.3 C--, ClCH.sub.2 --or Cl.sub.2 CH--; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.11 R.sub.12 wherein each of R.sub.11 and R.sub.12 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms ##STR2## wherein R.sub.5 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.2 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 ##STR3## wherein R.sub.6 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; each of R.sub.3 and R.sub.

Abstract: Clonidine and lofexidine and the pharmaceutically acceptable salts thereof, which are, inter alia, known antihypertensives, also possess very potent antidiarrheal activity which is non-narcotic and more potent than that of conventional antidiarrheal drugs, such as diphenoxylate.

Abstract: A method of achieving a muscle-relaxing effect in a patient comprises administering to a patient in which a muscle relaxing effect is desired an amount effective to achieve a muscle-relaxing effect of a compound of the formula ##STR1## wherein R is H, or C.sub.1-7 straight or branched chain alkyl;R.sub.1 is H, C.sub.1-7 straight or branched chain alkyl, allyl or phenyl;R.sub.2 is phenyl, phenyl monosubstituted with F, Cl, C.sub.1-4 straight or branched chain alkyl or phenyl disubstituted in the 2- and 4-positions with Cl or C.sub.1-4 straight or branched chain alkyl; andR.sub.3 is H or C.sub.1-4 straight or branched chain alkyl, with the proviso that when R.sub.3 is straight or branched chain alkyl, R.sub.2 is unsubstituted phenyl;or a pharmaceutically acceptable acid addition salt thereof.

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: Compounds of the formula ##STR1## wherein R is H, C.sub.1-5 or 7 -straight or branched chain alkyl or allyl and R.sub.1 is H or Cl andthe pharmacologically acceptable acid addition salts thereof are pharmacologically active as anticonvulsant and anxiolytic agents.

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: Novel compounds of the following formula: ##STR1## wherein R.sub.1 is hydrogen or hydroxy; R.sub.2 is hydrogen; or R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ; n is an integer of from 1 to 5; R.sub.3 is --CH.sub.3, --CH.sub.2 OH, --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; and each of A and B is hydrogen or hydroxy; with the provisos that at least one of A or B is hydrogen and one of A or B is other than hydrogen when R.sub.3 is --CH.sub.3 ; and pharmaceutically acceptable salts thereof.

Abstract: Pharmaceutically useful compounds of the following formula: ##STR1## wherein R.sub.1 represents hydrogen or hydroxy; R.sub.2 represents hydrogen; or R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ; n is a positive whole integer of from 1 to 5; R.sub.3 is --CH.sub.3, --CH.sub.2 OH, --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; and A and B are individually hydrogen or hydroxy; with the provisos that at least one of A or B is hydrogen and one of A or B is other than hydrogen when R.sub.3 is --CH.sub.3 ; and pharmaceutically acceptable acid addition salts thereof.

Abstract: Cinnamoylpiperidinobutyrophenone derivatives and pharmaceutically acceptable salts thereof of the following general structure: ##STR1## wherein R is hydrogen, alkyl, alkoxy, halogen or trifluoromethyl; and R' is hydrogen or halogen; are useful as antipsychotic agents. The novel compounds are produced by aldol condensation of a benzaldehyde with a protected 4-(4-acetyl-1-piperidino)-butyrophenone.

Abstract: 4-Aroylethnyl-1-piperidinobutyrophenone derivatives and pharmaceutically acceptable salts thereof of the following general structure: ##STR1## wherein R is hydrogen, alkyl, alkoxy, halogen or trifluoromethyl; and R' is hydrogen or halogen, are useful as antipsychotic agents. The novel compounds are produced by aldol condensation of an acetophenone with a protected 4-(4-formyl-1-piperidino)-butyrophenone.

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: A method of inducing sedation in a patient comprises administering to a patient in which sedation is desired an amount effective for inducing sedation of a compound of the formula ##STR1## wherein R is H, or C.sub.1-5 or 7 -straight or branched chain alkyl:R.sub.1 is H, C.sub.1-5 or 7 -straight or branched chain alkyl or allyl;R.sub.2 is phenyl or phenyl substituted with F, Cl, Br, NO.sub.2, C.sub.1-5 straight or branched chain alkyl, C.sub.1-5 straight or branched chain alkoxy, 2,4-di-Cl, 2,4-di-F or 2,4-di-Br, with the proviso that when the phenyl group is monosubstituted with F, the F atom is not in the o-position; andR.sub.3 is H or C-1-5 straight or branched chain alkyl, with the proviso that when R.sub.3 is straight or branched chain alkyl, R.sub.2 is unsubstituted phenyl; ora pharmaceutically acceptable acid addition salt thereof.