Abstract: An improved process for the preparation of 2' and 3'-(halo-substituted)-2',3'-dideoxy nucleosides by reacting a protected anhydrothymidine compound with a halogenating composition containing a substituted organoaluminum compound which exhibits greater solubility in conventional solvents than AlF.sub.3.

Abstract: A process for making acrylmaleic acid and arylmaleic anhydride derivative useful as intermediates for the preparation of arylmaleimides in the synthesis of compounds having activity in the central nervous system. The process involves reacting arylacetonitriles with glyoxylic acid to provide novel intermediate 3-aryl-3-cyanopropeneoates which may be converted to the arylmaleic acid and arylmaleic anhydride derivatives.

Abstract: New 4-substituted azetidinones having the formulea I and II: ##STR1## with R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and X defined hereafter, which are intermediates for the preparation of carbapenem and carbacephem antibacterials and processes for producing such antibacterials through the utilization of an acid mediated ring closure reaction.

Abstract: Renin inhibiting compounds of the formula: ##STR1## containing two .alpha.-amino acids or a single .alpha.-amino acid wherein R.sub.1 is a phosphorus containing moiety, W is oxygen or NR.sub.3 and A is a moiety selected from those of the formula: ##STR2## wherein Z is O, S, SO, SO.sub.2 and p is an integer from 1 to 2; and, when W is oxygen, A may also be a moiety of the formula ##STR3## and analogs thereof which compounds inhibit the substrate-cleaving action of renin, pharmaceutical compositions containing these compounds, processes for producing the compounds and methods of treating hypertension which employ the novel renin inhibitors.

Abstract: An improved process for producing the antibiotic compound clindamycin phosphate through the use of novel intermediate, 7(S)-chloro-7-deoxylincomycin-2-bis(2,2,2-trichloroethyl)phosphochloridate and similar compounds.

Abstract: The present invention relates to an improved method for producing oligosaccharide conjugate vaccines. In an additional aspect of the invention, oligosaccharide vaccines are produced which elicit a monospecific and homogeneous immune response to capsular polysaccharide. A specific embodiment of the invention provides for vaccines which induce immunity to prevalent serotypes of Streptococcus pneumoniae.

Abstract: Novel processes and intermediates for the preparation of tetrahydro-5-hydroxy-3-methylene-2-furan-methanol and of tetrahydro-5-[lower alkoxy (C.sub.1 -C.sub.3)]-3-methylene-2-furanmethanol useful as intermediates in the synthesis of various modified nucleosides having antiviral and other biological activity.

Abstract: Compounds of the formula: ##STR1## wherein A is t-butoxy carbonyl, which compounds are useful as intermediates for preparing 1-Substituted-2-(3-amino-1-propynyl)pyrrolidine derivatives having cholinergic agonist activity.

Abstract: Bis-aryl amide and urea compounds of the general formula: ##STR1## wherein X is a divalent amide or urea substituent and Y is a nitrogen containing heterocycle, which compounds are inhibitors of platelet activating factor. Pharmaceutical compositions containing the compounds and methods of treating platelet activating factor associated conditions are also included.

Abstract: Stable, cosmetically acceptable gel formulations of the tetracycline antibiotics for the topical treatment of acne in humans. Minocycline hydrochloride is the preferred antibiotic and the pharmaceutical vehicle is a volatile silicone solvent in combination with an emollient ester cosolvent and a polyethylene gelling agent.

Abstract: Renin inhibiting compounds containing a single .alpha.-amino acid of the formula: ##STR1## and analogs thereof which inhibit the substrate-cleaving acting or renin, pharmaceutical compositions containing these compounds, processes for producing the compounds and methods of treating hypertension which employ the novel renin inhibitors.

Abstract: This disclosure describes novel antibacterial agents designated LL-E10985.alpha., LL-E19085.beta., LL-E19085.gamma., LL-E19085.gamma. and LL-E19085.zeta., having the structure: ##STR1## their production by aerobic fermentation of a new subspecies of Micromonospora citrea NRRL 18351 and mutants thereof, and the isolation and purification thereof.

Abstract: This disclosure describes novel 3 or 4 substituted oxotremorine derivatives having polar substituted oxygen or sulfur groups. The compounds have cholinergic activity. Also disclosed are methods for treating diseases of the central nervous system in mammals employing the compounds, pharmaceutical preparations containing the compounds and processes for the production of the compounds.

Abstract: Methods of preparing bis-aryl amide and urea compounds of the general formula: ##STR1## wherein x is a divalent amide or urea substituent and Y is a nitrogen containing heterocycle, which compounds are inhibitors of platelet activating factor.

Abstract: Derivatives of antibiotics derived from the microorganism Streptomyces lydicus subspecies tanzanius, referred to as antibiotics LL-E19020 alpha and beta, are produced by chemical reaction. The derivatives are also active antibiotics useful in the treatment of bacterial infections.

Abstract: This invention relates to a method and apparatus for filling a powder, lipid or granule into a soft shell capsule employing a flat linked track of cavity blocks to prevent spillage.

Abstract: A pharmaceutical composition comprising a freeze-dried preparation of polyhematoporphyrin ether/esters wherein said freeze dried preparation does not contain sodium chloride. Upon reconstitution, the pharmaceutical composition is a photosensitizer preparation useful in photodynamic therapy.

Abstract: Pharmaceutical compounds and compositions which may be represented by the following structural formula: ##STR1## wherein NR'" is selected from amino, (C.sub.1 -C.sub.6) alkylamino, dialkylamino or trialkylamino, pyrrolidino or piperidino. The compounds and compositions are useful in treating central cholinergic dysfunction in mammals.

Abstract: This invention is concerned with ureas and thioureas which may be represented by the formula: ##STR1## wherein X represents at least one substituent selected from the group consisting of (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkenyl, (C.sub.1 -C.sub.4)alkynyl, phenoxy, mercapto, amino, (C.sub.1 -C.sub.4)alkylamino, di-(C.sub.1 -C.sub.4)alkylamino, halo, trihalomethyl, (C.sub.1 -C.sub.4)alkanoyl, benzoyl, (C.sub.1 -C.sub.4)alkanamido, haloacetamido, nitro, cyano, carboxy, (C.sub.1 -C.sub.4)carboalkoxy, carbamoyl, sulfamyl, methylenedioxy, phenyl, orthophenylene, tolyl, benzyl, halobenzyl, methylbenzyl; Y is selected from the group consisting of oxygen and sulfur; R.sub.1 and R.sub.2 are different and are independently selected from the group consisting of (C.sub.4 -C.sub.12)alkyl, (C.sub.4 -C.sub.12)alkenyl, (C.sub.4 -C.sub.12)alkynyl, (C.sub.4 -C.sub.12)cycloalkyalkyl, (C.sub.7 -C.sub.14)aralkyl, and (C.sub.7 -C.sub.

Abstract: Compounds of the formula: ##STR1## pharmaceutical compositions containing the compounds and methods of using the compounds in the treatment of central cholinergic disfunction in a mammal are disclosed.