Abstract: In accordance with the present invention an orally active monosulfactam antibiotics having a crystalline structure and thereby improved stability are disclosed. The antibiotics comprise the dierythromycin (M.sup..sym.=erythromycin.H.sup..sym.) salt or the dicholine (M.sup..sym. =HOCH.sub.2 CH.sub.2 N.sup..sym. (CH.sub.3).sub.3) salt of the acid (M.sup..sym. =H.sup..sym.) having the formula ##STR1## that is, [3S(Z)]-2[[[1-(2-amino-4-thiazolyl)-2-[[2,2-dimethyl-4-oxo-1-(sulfooxy)-3- azetidinyl]-amino]-2-oxoethylidene]amino]oxy]acetic acid.

Abstract: 7-Oxabicycloheptane substituted amino prostaglandin analogs are provided having the structural formula ##STR1## wherein n is 1 to 5; R.sup.1 is CO.sub.2 H, CO.sub.2 lower alkyl or ##STR2## and R.sup.2 is ##STR3## wherein R.sup.3 is lower alkyl, aralkyl, --NHalkyl or --NHaryl, or R.sup.2 is ##STR4## wherein q is 1 to 12, and R.sup.4 is lower alkyl, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aryloxy, arylalkyloxy, amino, alkylamino arylamino, arylalkylamino, lower alkyl-S--, aryl-S--, arylalkyl-S--, ##STR5## (wherein n' is 0, 1 or 2), alkylaminoalkyl, arylaminoalkyl, arylalkylaminoalkyl, alkoxyalkyl, aryloxyalkyl or arylalkoxyalkyl.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease and are useful in the preparation of radiolabelled analogs.

Abstract: Analgesic activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1, R.sub.2 and R.sub.4 are each independently hydrogen, alkyl, carboxyalkyl, halosubstituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl, or heteroaryl, and R.sub.3 is hydroxymethylene or carbonyl.

Abstract: Compounds of the formula ##STR1## are disclosed. These compounds intervene in the conversion of angiotensinogen to angiotensin II by inhibiting renin and thus are useful as antihypertensive agents.

Abstract: A new method is provided for forming crystals of amphotericin B directly in fermentation broth which crystals are easily separable without use of costly solvent extraction techniques which method includes a direct microbial cell autolysis step to induce crystal formation.

Abstract: Vasodilating activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof.

Abstract: A pre-filled syringe is provided with a retractile needle. The needle end of a syringe is enclosed in a sterile chamber within a casing sealed by a cap with a break-off tip. The barrel of the syringe is movable within the casing from a remote pre-injection position to a forward injection position and back again. When the barrel is moved forward a first end of the needle passes through the opening of the cap and then the opposite end comes in contact with the injectant. When the barrel is withdrawn to a pre-injection position, the needle is retracted within the casing and is prevented from re-entering the opening in the cap.

Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is aryl or heterocyclo;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 hydrogen, alkyl, alkenyl, alkynyl, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, halo substituted alkyl, or ##STR2## 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, ##STR3## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR4## Y.sub.3 is hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.m --S--, ##STR5## amino, or substituted amino; Y.sub.4 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.

Abstract: A method is provided for preparing stable liposome precursors in the form of a water-soluble carrier material coated with a predetermined amount of a thin film of liposome components, which method includes the steps of dissolving at least one liposome-forming amphipathic lipid, optionally, at least one biologically active compound, and, optionally, at least one adjuvant in a suitable organic solvent and employing the resulting organic solution to coat a suitable water-soluble carrier material to form thin film of predetermined amount of liposome components thereon. Upon exposing the coated carrier material to water, the thin films of liposome components hydrate and the carrier material dissolves to give liposome preparations.

Abstract: This invention is directed to orally active antihypertensive agents of the formula ##STR1## wherein R.sub.1 is certain alkyl or aralkyl groups.

Abstract: Aerocavin, a novel antibiotic substance having the structure ##STR1## and aerocyanidin, a novel antibiotic substance having the structure ##STR2## can be prepared by cultivation of the microorganism Aerocavin caviae SC 14,030 A.T.C.C. No. 53434.

Abstract: A process is provided for preparing a 7-oxabicycloheptane amino alcohol intermediate of the general structure ##STR1## which is useful in preparing thromboxane A.sub.2 receptor antagonists. This intermediate is prepared by reacting mesonhydride with an aryl amine ##STR2## wherein R is alkyl, CH.sub.2 OH, CO.sub.2 H or CO.sub.2 alkyl, to form the acid ##STR3## which is reduced by treatment with lithium aluminum hydride or diisobutylaluminum hydride or Red-Al to form the alcohol ##STR4## wherein R.sup.1 is CH.sub.2 OH when R is CO.sub.2 H, CO.sub.2 alkyl or CH.sub.2 OH, and R.sup.1 is alkyl when R is alkyl; where in the above alcohol R.sup.1 is CH.sub.2 OH, such alcohol compound is treated with an alkyl chloroformate in the presence of base such as an alkali metal alkoxide to form the alcohol ##STR5## which undergoes cleavage by treatment with alkali metal, ammonia and acid to form the amino alcohol intermediate.Where in the above alcohol R.sup.

Abstract: Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and having an activating group in the 1-position of the formula ##STR1##

Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive 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: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive 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: A process is provided for preparing phosphonous acids of the structure wherein R.sub.1 is lower alkyl or arylalkyl ##STR1## which are useful in preparing phosphinic and phosphonic acid ACE inhibitors, which process includes the steps of treating an olefin of the structure R.sub.1 --CH.dbd.CH.sub.2 wherein R.sub.2 is lower alkyl or arylalkyl with a phosphorus-containing reagent such as sodium hypophosphite or hypophosphorous acid in the presence of an organic alcohol solvent such as ethanol or methanol, and a radical initiator such as azobisisobutyronitrile, under acidic conditions, preferably at the reflux temperature of the organic solvent, to form the phosphonous acid without forming the alkyl ester.

Abstract: In accordance with the present invention, a controlled release formulation is provided from which a drug, selected from the group consisting of angiotensin converting enzyme inhibitors and ascorbic acid, is released at a substantially controlled rate. The controlled release formulation of the invention is comprised of a reactive matrix of from about 5 to about 80 percent by weight of the drug in combination with from about 5 to about 70 percent by weight of poly[(1.fwdarw.4)-2-amino-2-deoxy-.beta.-D-glucose] (also referred to as chitosan herein). Further in accordance with the present invention there is provided a gel-like complex formed of the drug and the chitosan in environments ranging from neutral to acidic.

Abstract: Bisthioamide-7-oxabicycloheptane prostaglandin analogs are provided having the structural formula ##STR1## wherein A is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --; n is 1 to 5; R is CO.sub.2 H, CO.sub.2 lower alkyl or ##STR2## q is 1 to 12; and R.sup.1 is H, lower alkyl, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aryloxy, arylalkyloxy, amino, alkylamino arylamino, arylalkylamino, lower alkyl-S-aryl-S-, arylalkyl-S-, ##STR3## (wherein n' is 0, 1 or 2), alkylaminoalkyl, arylaminoalkyl, arylalkylaminoalkyl, alkoxyalkyl, aryloxyalkyl or arylalkoxyalkyl.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.

Abstract: Intermediates of the formula ##STR1## are disclosed. These compounds are useful in preparing substituted peptide compounds which possess hypotensive and analgesic activity.

Abstract: Candida albicans has been transformed by the insertion of a plasmid comprising a fragment of DNA from Candida albicans containing the intact ADE 2 gene.