Abstract: Described is a novel process for the preparation of penems and carbapenems useful as antibacterial agents which comprises the reaction of an appropriate 4-substituted-azetidine-2-one with an acid halide in the presence of a tertiary amine and an alkaline earth metal carbonate, followed by reaction of the thereby formed 1-imido-4-substituted-azetidine-2-one with a trialkyl phosphite.Also described are novel penems useful as antibacterials which are prepared by the described process.This is a division; of application Ser. No. 230,774, filed Feb. 2, 1981 now U.S. Pat. No. 4,347,183.

Abstract: Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2 and R.sup.4 are independently selected from hydrogen and lower alkyl; R.sup.3 is hydrogen, lower alkyl or amino lower alkyl; A and B taken together with the carbons to which they are attached form an alkylene ring having six carbon atoms or A and B are hydrogen; and Z is ##STR2## are disclosed. The compounds are useful as anti-hypertensive agents.

Abstract: Disclosed herein are (5R,6S,8R)-6-(1-hydroxyethyl)-2-(2-fluoroethylthio)-penem-3-carboxylic acid and the metabolisable esters thereof and alkali metal salts thereof, which are potent antibacterial agents.

Abstract: Compounds of the formula ##STR1## and their pharmaceutically acceptable salts are disclosed. The compounds are useful as anthelmintics.

Abstract: In the fermentation production of gentamicin C a plurality of additional antibiotic compounds are obtained. Four of these compounds, gentamicin A, gentamicin B, gentamicin B.sub.1 and gentamicin X exhibit significant anti-protozoal and anthelmintic activity while gentamicin B and B.sub.1 have significant antibacterial properties with markedly reduced side affects.

Abstract: This invention relates to 5-(2-alkylamino-1-hydroxyethyl)salicylamides and 4-(2-alkylamino-1-hydroxyethyl)-2-(methylsulfinyl)phenols wherein the alkyl group is substituted by arylmethoxy, arylmethylthio, heteroarylmethoxy, or heteroarylmethylthio, pharmaceutical compositions thereof, and their use as cardiovascular agents.

Abstract: Antihistamines of the formula ##STR1## wherein ##STR2## is a 5 or 6 membered ring which is phenyl or heterocyclic; ##STR3## is a six membered ring which is 2,3 or 4 pyridyl or is phenyl or substituted phenyl, with the proviso that is ##STR4## is a nitrogen containing ring, ##STR5## must be phenyl; Z is an alkylene chain having 0 to 2 carbon atoms in the chain, said 2 carbon chain optionally having one double bond, said chain optionally having either a carbonyl oxygen, or a hydroxy group as a substituent; W is ##STR6## wherein p is 1 or 2 and n is 1 or 2, R.sup.1 is C.sub.1 to C.sub.6 alkyl, R.sup.2 is hydrogen or C.sub.1 to C.sub.6 alkyl, and the dotted line represents an optical double bond, R.sup.2 being absent if the double bond is present, and Y is substituted carboxylate or substituted sulfonyl. Said antihistamines have little or no sedative effects.

Abstract: 3-Aralkyloxy-2,3-dihydro-2-(imidazolylmethyl(benzo(b)thiophenes and related derivatives having antifungal, antibacterial, and antiprotozoal activity are prepared by the reaction of the corresponding 2,3-dihydro-3-hydroxy-2-(imidazolylmethyl)benzo(b)thiophene or related derivative and an aralkyl halide.Preferred compounds are those where the aralkyl function is a hetercyclic aromatic, particularly 2-chloro-3-thenyl, and where the benzene nucleus is substituted by chlorine or fluorine.Pharmaceutical formulations comprising compounds of this invention are described, as well as the method for their use in treating microbial infections.

Abstract: Alkoxyalkanoate esters of vidarabine of the formula ##STR1## wherein R.sub.x, R.sub.y and R.sub.z are ##STR2## or hydrogen and wherein R.sub.1 is lower alkyl and R.sub.2 is lower alkylene, which compounds are useful in treating susceptible viral infections, are disclosed.

Abstract: 17-Arylcarboxylate esters of 9,11-unsubstituted 4-pregnene-17.alpha.,21-diol-3,20-diones are prepared by reaction of the corresponding 17.alpha.-hydroxy derivative with alkyl lithium and an anhydride or acyl halide reagent in the presence of 4-(di-lower alkyl)aminopyridine at low temperatures. A preferred mode of the process is the preparation of 16.beta.-methyl-1,4-pregnadiene-17.alpha.,21-diol3,20-dione 17.alpha.-m-iodobenzoate 21-benzoate, a valuable intermediate in the manufacture of betamethasone.

Abstract: An improved synthetic process for the removal of an allyl group in an allylic ester or an allyloxycarbonyl group in an allylic carbonate or carbamate by reaction with 2-ethylhexanoic acid or an alkali metal salt thereof and a catalytic amount of an organic-soluble palladium complex is disclosed herein.

Abstract: 2-(Alkylthio, alkylsulfinyl or alkylsulfonyl)-4-[2-(anilinoalkylamino)-1-hydroxyalkyl]phenols and derivatives thereof, particularly useful as agents for the treatment of hypertension, are disclosed herein.

Abstract: This invention describes a novel process whereby D-glucose and D-mannose are converted to S-3-amino-2-hydroxypropionic acid and R-3-amino-2-hydroxypropionic acid, respectively, and their N-blocked derivatives.

Abstract: A novel process whereby 4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols are reacted with a dialkylaminosulfur trifluoride to produce novel 5-fluoro-5-deoxy and 5-epi-fluoro-5-deoxy-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitol antibacterial agents.

Abstract: This invention relates to derivatives of polyene macrolide antibiotics containing an amino sugar moiety, the process for their preparation and pharmaceutical compositions containing them useful in the treatment of fungal infections.