Abstract: Compounds having the formula ##STR1## and alkyl esters and salts thereof. R.sub.1 is hydrogen, alkanoyl or ##STR2## R.sub.2 is hydrogen, alkyl, or phenylalkyl; n is 0 or 1; andA.sub.1 and A.sub.2 each is an .alpha.-amino or .alpha.-imino acid residue joined through a peptide bond, have useful hypotensive activity.

Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is oxygen or sulfur;R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR2## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR3## Y.sub.3 is hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.

Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is oxygen or sulfur;R.sub.1 is alkyl, cycloalkyl, alkenyl, alkynyl, aryl --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3 or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl ##STR2## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR3## Y.sub.3 is hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.

Abstract: Antibacterial activity is exhibited by monocyclic .beta.-lactam antibiotics having in the 1-position an --O--SO.sub.3 H activating group and in the 3-position an acylamino group of the formula ##STR1## wherein R.sub.3 and R.sub.4 are each independently hydrogen or alkyl.

Abstract: Antimicrobial activity is exhibited by .beta.-lactams having a ##STR1## substituent in the 1-position and an acylamino substituent in the 3-position, or a pharmaceutically acceptable salt thereof; wherein Y is oxygen or sulfur and R.sub.5 is hydroxyl, alkyl, substituted alkyl, phenyl, substituted phenyl, alkoxy, alkylthio, (substituted alkyl)oxy, (substituted alkyl)thio, phenyloxy, phenylthio, (substituted phenyl)oxy or (substituted phenyl)thio.

Abstract: This invention is directed to substituted 4-phenoxy and 4-phenylthio prolines of the formula ##STR1## which possess useful hypotensive activity.

Abstract: An electromechanical system which may be used in conjunction with spinning catheters, such as those which have differential cutting burrs, includes an electric prime mover which attaches to an advancer assembly. The advancer assembly has an off-axis drive and apparatus for loading a catheter unit, which is driven through a catheter engagement coupling. The catheter assembly can also include one or two lumens with access ports at the advancer assembly, whereby medicines may be injected or pressure readings may be obtained from the vessel.

Abstract: Antibacterial activity is exhibited by compounds having the formula and pharmaceutically acceptable salts thereof.

Abstract: Compounds having the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently hydrogen or alkyl of 1 to 4 carbon atoms, or R.sub.1 and R.sub.2 together with the carbon atom to which they are attached form a cycloalkyl ring;R.sub.3 is hydrogen or alkyl;R.sub.4 is hydrogen or alkyl, and R.sub.5 is hydrogen, alkyl, phenyl, substituted phenyl, a 4,5,6 or 7-membered heterocycle, phenylalkyl, (substituted phenyl)alkyl, (4,5,6 or 7-membered heterocycle)alkyl, ##STR2## or together R.sub.4 and R.sub.5 are .dbd.CH--Y.sub.7 ; wherein Y.sub.1 is hydrogen, alkyl, phenyl, substituted phenyl, methylcarbonyl, trifluoromethylcarbonyl, phenylcarbonyl, (substituted phenyl)carbonyl, carboxymethyl, methylsulfonyl, phenylsulfonyl, (substituted phenyl)sulfonyl, aminocarbonyl, aminocarbonylamino, aminoethyl, hydroxy, alkoxy, amino, alkylamino, dialkylamino, phenylcarbonylamino, (substituted phenyl)carbonylamino, 1-pyrrolidinyl or 1-piperidinyl; Y.sub.

Abstract: The presence of a copper salt during the oximation of a .beta.-lactam containing compound having glyoxylamino substituents of the formula ##STR1## by reaction with an aminooxy compound having the formulaH.sub.2 N--O--R.sub.a,or a salt or ester thereof, results in a product wherein the ratio of syn isomer to anti isomer is increased.

Abstract: Hydroximic acids of 7-oxabicycloheptane substituted ether and thioether prostaglandin analogs are provided having the structural formula ##STR1## wherein Y is O or ##STR2## and including all stereoisomers thereof. The compounds are inhibitors of prostaglandin and biosynthesis and as such are useful, for example, as anti-allergy and antiinflammatory agents and also as antipsoriatic agents.

Abstract: 7-Oxabicyclo(2.2.1)heptane hydroxamic acid derivatives are disclosed having the general formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, aryl, aralkyl or alkenyl; R.sub.2 is hydrogen, lower alkyl, alkanoyl or aroyl; R.sub.3 is lower alkyl, alkenyl or alkynyl; A is --CH.sub.2 --CH.dbd.CH-- or a single bond; and n is an integer from 0 to 9, with the proviso that when A is a single bond, n is an integer from 1 to 9; and including all stereoisomers and pharmaceutically acceptable salts thereof.These new compounds have been found to simultaneously inhibit the arachidonic acid enzymes cyclooxygenase and 5-lipoxygenase and are therefore useful as antiinflammatory, antiasthma and antipsoriatic agents.

Abstract: Antibacterial activity is exhibited by compounds having the formula ##STR1## and salts thereof, wherein R.sub.1 is acyl;R.sub.2 is hydrogen or methoxy;R.sub.3 and R.sub.4 are the same or different and each is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl or a 5,6 or 7-membered heterocycle or one of R.sub.3 and R.sub.4 is hydrogen and the other is azido, halomethyl, dihalomethyl, trihalomethyl, alkoxycarbonyl, 2-phenylethenyl, 2-phenylethynyl, carboxyl, ##STR2## X.sub.1 is azido, amino, hydroxy, alkanoylamino, alkylsulfonyloxy, arylsulfonyloxy, aryl, cyano, --S--X.sub.2 or --O--X.sub.2 ;X.sub.2 is alkyl, substituted alkyl, aryl, arylalkyl, alkanoyl, substituted alkanoyl, arylcarbonyl or heteroarylcarbonyl;one of X.sub.3 and X.sub.4 is hydrogen and the other is hydrogen or alkyl, or X.sub.3 and X.sub.4 when taken together with the carbon atom to which they are attached from a cycloalkyl group;X.sub.

Abstract: Antibacterial activity is exhibited by .beta.-lactams having a 3-acylamino substituent and in the 1-position a substituent having the formula ##STR1## wherein R.sub.5 and R.sub.6 are the same or different and each is hydrogen, alkyl, alkenyl, alkynyl, phenyl, substituted phenyl, cycloalkyl or a 4,5,6 or 7-membered heterocycle, or R.sub.5 and R.sub.6 together with the carbon atom to which they are attached are cycloalkyl or a 4,5,6 or 7-membered heterocycle, or one of R.sub.5 and R.sub.6 is hydrogen and the other is azido, halomethyl, dihalomethyl, trihalomethyl, alkoxycarbonyl, alkenyl, alkynyl, 2-phenylethenyl, 2-phenylethynyl, carboxyl, --CH.sub.2 X.sub.1, --S--X.sub.2, --O--X.sub.2, or ##STR2## R.sub.7 is hydrogen, alkyl, substituted alkyl, phenyl, substituted phenyl, 1-(ethoxycarbonyloxy)ethyl, 1,3-dihydro-3-oxo-1-isobenzofuranyl, ##STR3## wherein R' is hydrogen or alkyl, R" is alkyl or phenyl, R"' is hydrogen, methyl or phenyl, and R.sup.iv is hydrogen or together with R"' is --(CH.sub.2).sub.

Abstract: A process for preparing phosphonic acids of the structure ##STR1## wherein R.sub.1 is lower alkyl, aryl, cycloalkyl or arylalkyl, and R.sub.2 is H, benzyl or ##STR2## by oxidizing the corresponding phosphonous acid ##STR3## employing as the oxidizing agent potassium permanganate or sodium periodate.

Abstract: Compounds of the formula ##STR1## wherein X is various amino or imino acids and esters are disclosed. These compounds are useful as anti-hypertensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.

Abstract: An enkephalin-degrading aminopeptidase enzyme is inhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl, carboxyalkyl, halo substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl, or heteroaryl;R.sub.3 is hydroxy, alkoxy, (substituted alkyl)oxy, arylalkoxy, (heteroaryl)alkoxy or --NY.sub.1 Y.sub.2, wherein Y.sub.1 and Y.sub.2 are each independently hydrogen, alkyl, aryl, or arylalkyl or Y.sub.1 is hydrogen and Y.sub.2 is substituted alkyl or (heteroaryl)alkyl;A.sub.1 is glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, prolyl, norleucyl, norvalyl, or ##STR2## wherein n.sub.6 is an integer of 2 to 15;A.sub.2, A.sub.3, A.sub.4 and A.sub.

Abstract: 7-Oxabicycloheptane substituted amidocarbamoyl prostaglandin analogs are provided having the structural formula ##STR1## wherein m is 0 to 4; A is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --; n is 1 to 5; R.sup.1 is CO.sub.2 H, CO.sub.2 alkyl, CO.sub.2 alkali metal, CO.sub.2 polyhydroxyamine salt, ##STR2## wherein R.sup.4 and R.sup.5 are the same or different and are H, lower alkyl, hydroxy, lower alkoxy or aryl, at least one of R.sup.4 and R.sup.5 being other than hydroxy and lower alkoxy; p is 1 to 4; X is O or S; R.sup.2 is H or lower alkyl; and R.sup.3 is lower alkyl, lower alkenyl, aryl, arylalkyl, cycloalkyl or cycloalkylalkyl.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.

Abstract: A controlled release pharmaceutical formulation which undergoes slow release of active drug is provided, preferably in the form of a tablet containing medicament, such as captopril, is slowly released over a controlled length of time. The tablet also includes an acrylic acid polymer or copolymer and one or more lubricants and is formed by a dry granulation technique.

Abstract: An ostomy device for releasably connecting an ostomy bag to an adhesive backed label including a mounting member for connecting one of two coupling parts to the label. The mounting member comprises an expandable portion for facilitating displacement of the connected coupling part between a normal closed position and an expanded position. The expanded portion comprises a pair of accordion-like folds including an inner fold and a smaller outer fold. The connected coupling part comprises a rib portion having a deflectible sealing strip extending therefrom. The rib portion is connected to the mounting member adjacent the outer folds such that the sealing strip is positioned intermediate the inner and outer folds when the coupling part is in the normal closed position. The inner fold guides discharge from the stoma into the bag and away from the interengaged coupling parts. In an alternate embodiment, the mounting member is affixed to the label.