Abstract: O-Aryl, O-alkyl, O-alkenyl and O-alkynyl-macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-3" and/or C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses.

Abstract: Novel cytochalasins are the biotransformed products after incubation with a substrate in a culture of the microorganism Kibdelosporangium sp. (Merck Culture Collection MA 6559), ATCC No. 53771. The compounds of the present invention inhibit HIV protease and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as a compound, pharmaceutically acceptable salt, pharmaceutical composition ingredient, whether or not as a prodrug or as a combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines.

Abstract: Imidazolidyl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-3" and/or C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.

Abstract: There is disclosed a child resistant medication container assemblage comprising a container base having a plurality of medication compartments formed therein to house unit doses of medication. The container base is provided with means to receive a slidably removable lid, means to prevent the lid from being returned to its normally closed position until a unit dose of medication has been removed and means coacting with catch means in the lid to resist efforts of children to access the medication.

Abstract: A method for flow injection analysis of total inorganic phosphate contained in an aqueous system such as a cooling tower or boiler is described which uses a reducing agent and preservative composition therefore as the carrier for the sample to be analyzed, thereby creating a facile process which permits conversion of the various polyphosphates to orthophosphate and development of the molybdenum blue complex color reaction at 60.degree.-95.degree. C. and under 2-10 psi. This method has less stringent pressure and temperature requirements than those employed heretofore, thus permitting the use of more reliable and economic devices for measuring total inorganic phosphate in the field.

Abstract: A child resistant drug assemblage is disclosed comprising a container having rows of spaced drug cell cavities each of which receives a unit drug dose of medication. The container is provided with a lock means that enables it to be readily opened by an adult but difficult to be opened by a child.

Abstract: A wound dressing comprises a backing layer, which is preferably a semi-permeable material, and a wound contact pad. The wound contact pad comprises a mixed salt alginate, preferably in the form of fibres, which have first and second cations. The first cation (which may be calcium) is capable of forming an insoluble alginate salt and the second cation (which may be sodium) is capable of forming a soluble alginate salt. The equivalent ratio of the first to second cations is from 40:60 to 90:10, and is preferably about 80:20. Such dressings are useful in wound management, as the mixed salt alginate is particularly efficacious in combination with a backing layer.

Abstract: Proteins which specifically inhibit coagulation Factor Xa. The inhibitors, which do not inhibit Factor VIIa, kallikrein, trypsin, chymotrypsin, thrombin, urokinase, tissue plasminogen activator, plasmin, elastase, Factor XIa or S. aureus V8 protease, are polypeptides of 60 amino acid residues. The inhibitors may be purified from Ornithodoros moubata extract, synthesized, or produced using a recombinant DNA yeast expression system.

Abstract: A process for preparing compounds of the formula ##STR1## which comprises reacting an imidazolide of the formula ##STR2## with an amine of the formula NHR.sub.4 R.sub.5 in the presence of a Grignard reagent to form a compound of formula I or reacting an imidazolide of formula II with a compound of the formula R.sub.6 Mgx to form a compound of formula I.

Abstract: Described is a new process for producing 7.beta.-substituted-4-aza-5.alpha.-androstan-3-ones and related compounds which are 5.alpha.-reductase inhibitors.

Abstract: An intermediate, useful in the conversion of FK-506 to FK-525 and analogous 23-membered ring macrolides, of the structure: ##STR1##

Abstract: An orthophosphate salt and sodium silicate, when used in a 3:1 ratio by weight, and in a concentration of 0.1 to 100 mg/L, are found to have a synergistic effect in controlling the corrosion of carbon steel in an aqueous system, e.g., a municipal water supply system. The synergistic combination is also useful in reducing lead solubility and leaching, and in stabilizing soluble iron and manganese and their reaction products.

Abstract: Polysaccharide fibers are produced by hot extrusion of a gelling polysaccharide into air or a gelling salt bath. Optionally, other polysaccharides, including non-gelling types, may be co-extruded with the gelling polysaccharide. The fibers are useful for the production of wound dressings and catamenial devices, and many other devices.

Abstract: A process for the one-step conversion of cephalosporin C and derivatives thereof to the corresponding 7-aminocephalosporanic acid and derivatives comprising treating said cephalosporin C and derivatives with a cephalosporin C amidase enzyme of a recited sequence, the DNA encoding said enzyme, and expression thereof in a suitable host, e.g., Bacillus species under the control of a suitable promoter.

Abstract: Novel fibrinogen receptor antagonists of the formula ##STR1## are provided in which the claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating thrombus formation.

Abstract: There is disclosed an automated system for testing the sterility of products intended for human health administration or for human consumption. The system permits a plurality of samples of a product to be concurrently tested. To accomplish this, the system includes a novel apparatus for thoroughly mixing therein a plurality of product samples to assure that a statistically meaningful representation of product samples are subjected to sterility testing. The system is arranged so that multiple samples of a product to be tested are deposited in the mixing apparatus after which the mixed samples are conveyed to testing canisters along with appropriate growth media to determine that the product is sterile or that the product is free from microbial contamination.

Abstract: Described is a process for producing a new FK-506 antagonist agent, a C-21 hydroxylated analog of FR-900520 under novel fermentation conditions utilizing the novel microorganism, Streptomyces hygroscopicus (Merck Culture Collection MA 6832) ATCC No. 55166. The macrolide antagonist is useful in preventing and/or counteracting accidental or inadvertent FK-506 overdosage in an FK-506 therapeutic program designed to prevent autoimmune diseases or human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.

Abstract: Biosynthetic production of 7-[1',2',6',-7',8',8a'(R)-hexahydro-2'(S),6'(R)-dimethyl-8'(S)-hydroxy-1'( S)-naphthyl]-3(R),5(R)-dihydroxyheptanoic acid, "triol acid", is accomplished by enzymatic hydrolysis of lovastatin acid or a salt thereof, by treating it with Clonostachys compactiuscula ATCC 38009 or ATCC 74178, or mutants thereof, or a cell-free extract derived therefrom, or a hydrolase derived therefrom. The triol acid and its lactone form are both inhibitors of HMG-CoA reductase and thus useful as anti-hypercholesterolemic agents, and may also serve as intermediates for preparation of other HMG-CoA reductase inhibitors. Also, in the synthesis of simvastatin by direct methylation of lovastatin, selective hydrolysis of residual lovastatin salt by treatment with Clonostachys compactiuscula ATCC 38009 or ATCC 74178 or mutants thereof or a cell-free extract derived therefrom, or a hydrolase derived therefrom yields the "triol" salt which can be easily separated from simvastatin.

Abstract: Described is a process for producing a new immunosuppressant, a C-19/C-22 cyclic hemiketal (Compound I) biotransformation analog of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces sp. (Merck Culture Collection MA6963) ATCC No. 55230. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.