Abstract: A pharmaceutical preparation comprising flutamide, useful in the treatment of prostatic carcinoma, is disclosed.

Abstract: 6-Substituted-hydrocarbon-2-(substituted-thio)penem-3-carboxylic acids and congeners having useful antibacterial activity are disclosed. The compounds are prepared in a reaction sequence starting with a 4-acyloxy-2-azetidinone.

Abstract: Sodium and Potassium (5R,6S,8R)-6-(1-hydroxyethyl)-2-ethylthiopenem-3-carboxylic acid exhibit potent, broad-spectrum antibacterial activity, are orally effective and chemically stable.

Abstract: Described are D-(threo)-1-aryl-2-acylamido-3-fluoro-1-propanol esters and salts thereof, methods for their preparation, and methods for their use as antibacterial agents.

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: 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.

Abstract: Described are transition metal salt complexes of available neighboring amino and hydroxyl group pairs in polyamino organic compounds, their preparation, and use as intermediates in the preparation of selectively N-blocked polyamino organic compounds.

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: N-substituted-4-(polyfluoro-2-hydroxy-2-propyl)anilines and compounds related thereto, useful as antihypertensive agents, are prepared by reaction of an N-substituted aniline with a polyfluoroacetone.

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: Ophthalmic compositions containing (-)-5-{(R)-1-Hydroxy- 2[(R)-1-methyl-3-phenylpropyl)amino]ethyl}salicylamide and a method of using them in the treatment of glaucoma are disclosed.

Abstract: Described are D-(threo)-1-aryl-2-acylamido-3-fluoro-1-propanol esters and salts thereof, methods for their preparation, and methods for their use as antibacterial agents.

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: 6-(Heterocyclic)hydroxymethylpenicillanic acids and compounds related thereto are prepared by reaction of a 6,6-dihalopenicillanic acid with a Grignard reagent and a heterocyclic aldehyde in an anhydrous aprotic solvent. The compounds possess useful antibacterial activity.

Abstract: The present invention relates to topical compositions and methods of use utilizing compounds of the formula ##STR1## wherein X is oxygen or sulfur;W is a bridge group of the formulae ##STR2## wherein R is hydrogen alkyl of 1 to 7 carbon atoms, cycloalkyl of 4-8 carbon atoms, cycloalkenyl of 5-8 carbon atoms, polyfluoroalkyl of 1-4 carbon atoms, phenyl, benzyl or alkoxycarbonylmethyl; R.sub.1 is hydrogen or alkyl of 1-7 carbon atoms; m is 0-2; n is 1-4; with the proviso that m+n is 3-5; andA.sub.1, A.sub.2, A.sub.3, A.sub.4, B.sub.1, B.sub.2, B.sub.3, and B.sub.4 are independently selected from the group consisting of hydrogen, methyl, cyano, nitro, polyfluoroalkyl of 1-3 carbon atoms, chloro, bromo, fluoro and alkylthio, with the proviso that 2-5 of there are hydrogen of which at least one of A.sub.1, A.sub.2, A.sub.3 and A.sub.4 and at least one of B.sub.1, B.sub.2, B.sub.3 and B.sub.4 is hydrogen.

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: This application relates to phenyl-substituted 1,2,3,4-tetrahydrocarbazoles and to their use as anti-depressant agents useful in the treatment of mental depression of either endogenous or reactive nature.

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: 1-N-(R-.beta.-amino-.alpha.-hydroxypropionyl) gentamicin B, 1-N-(R-.gamma.-amino-.alpha.-hydroxybutyryl) gentamicin B, 1-N-(R-.delta.-amino-.alpha.-hydroxyvaleryl) gentamicin B and the corresponding diastereoisomers derived from the respective S-aminohydroxy acids and the acid addition salts thereof exhibit substantial antibacterial activity, especially against strains of bacteria which are resistant to gentamicin B and acid addition salts thereof.

Abstract: .beta.-Lactams having a substituted hydroxymethylene group at the position .alpha. to the lactam carbonyl group are prepared by reaction of an .alpha.-halo-.beta.-lactam with zinc or zinc amalgam in an anhydrous aprotic medium to produce an intermediate which in situ reacts with an appropriate aldehyde or ketone.Also described are novel penicillins and cephalosporins having useful antibacterial activity.