Abstract: This invention is concerned with a novel process for the preparation of N.sup.6 -alkyl-arprinocid (6-alkyl-amino-9-substituted benzyl purines). Such compounds are active anticoccidial agents. The process involves the preparation of a Schiff base from an acetal of dialkylformamide and reduction with a metal hydride.

Abstract: This invention involves spaced, horizontally extending corrugations, spaced, vertically oriented film surface sheets. The surface of the fill is enhanced by molded-in angular grooves to define discrete water passageways and air turbulation ridges.

Abstract: Highly active and long lasting cyclic hexapeptide analogs of somatostatin are prepared. A single amino acid of D-configuration, functioning as a spacer for the remaining amino acids, replaces seven of the ring amino acids of somatostatin. The amino acid adjacent to this spacer amino acid is methylated on the nitrogen and is of the D-configuration. The two amino acids on either side of this dipeptide are also of D-configuration. The remaining two amino acids, Trp and Lys are either D- or L-. The order of the amino acids is reversed relative to the sequence found in somatostatin. The structures therefore represent a modified form of D-retro peptide analogs. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions.

Abstract: The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoi c and cycloalkanoic acids, and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.

Abstract: The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoi c and cycloalkanoic acids and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.

Abstract: 5(Halophenyl)Salicylic acids are prepared in the presence of a palladium catalyst system of high selectivity and turnover number.

Abstract: Mercaptoalkylpyridines carrying an ethenyl or ethynyl substituent are prepared from known pyridine compounds, principally pyridoxine, by known chemical procedures, and are useful in the treatment of rheumatoid arthritis and related inflammatory diseases.

Abstract: Hydrogenation of the natural fermentation product, mevinolin, MK-803, results in the production of dihydro- and tetra-hydro derivatives and hydrogenation of the naturally occurring dihydromevinolin results in the formation of a tetrahydro derivative. These several products with the exception of cis-(4.alpha..beta., 8.alpha..beta.-)-tetrahydromevinolin are potent inhibitors of cholesterol biosynthesis.

Abstract: 4-Substituted-2,3,4,4a,5,6,7,11b-octahydrobenzo[6,7]cyclohept[1,2-b]-1,4-ox azines are prepared from the corresponding 6-(substituted amino)-6,7,8,9-tetrahydro-5H-benzocycloheptene-5-ol. The trans-4-substituted-2,3,4,4a,5,6,7,11b-octahydrobenzo[6,7]cyclohept[1,2-b] -1,4-oxazines have .alpha.-adrenergic agonist and tetrabenazine antagonist activity.

Abstract: Substances isolated after cultivation of a microorganism belonging to the genus Penicillium in a culture medium comprises compounds which have structures: ##STR1## Together with salts and esters of the carboxylic acid, these compounds form a class of highly active hypocholesterolemic and hypolipemic medicaments.

Abstract: Water soluble solid ophthalmic inserts for the treatment of dry eye in patients (human and animal), comprising a water soluble solid polymer of appropriate size.

Abstract: Substances isolated after cultivation of a microorganism belonging to the genus Aspergillus in a culture medium comprise compounds which have structures: ##STR1## Together with salts and esters of the carboxylic acid, these compounds form a class of highly active hypocholesteremic and hypolipemic medicaments.

Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.

Abstract: Novel amino derivatives of 2-hydroxy-6,9-methano-11-amino-5,6,7,8,9,10-hexahydro-benzocyclooctenes, methods for their preparation, and their use as effective analgesic agents is described.

Abstract: Novel halophenyl and loweralkyl substituted halophenyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful because of their low toxicity, and as such are advantageously included as the active agent in surgical scrubs, antibacterial soaps, as preservatives in cosmetic preparations, and the like.

Abstract: The invention relates to 1-[4-(4-sulfanilyl)phenyl] urea and derivatives thereof in pharmaceutical compositions and in methods of treating rheumatoid arthritis and immune complex diseases such as dermatitis herpetiformis.

Abstract: The invention relates to a novel process and novel intermediates useful in the preparation of sympathomimetic amines. The pharmacologically useful final products, which are acyl derivatives of mono- and dihydroxy aromatic amines (e.g., catechol amines) can be prepared in optically active or racemic form by reacting the corresponding mono- or dihydroxy aromatic amine with a reagent capable of forming the N-tert-butoxycarbonyl derivative thereof; reacting the novel intermediate thus obtained with an acyloxymethyl chloride to afford the corresponding novel mono- or diacylated N-protected aromatic amine; and removing the N-protecting group therefrom.

Abstract: The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoi c and cycloalkanoic acid and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.

Abstract: 2-Substituted-aminopropene and propanenitriles of the formula: ##STR1## are effective antimicrobial agents (compounds of Formula II.), and potent anti-inflammatory agents of decreased acute toxicity (compounds of Formula I.).

Abstract: There are disclosed certain new derivatives of C-076 compounds which have been isolated from the livers of animals that had been administered ivermectin and the in vitro incubation of such compounds with animal liver preparations. The compounds retain the basic ivermectin structure, however, 24-methyl group has been oxidized to a hydroxy methyl group and, in some of the new compounds the disaccharide substituent of the starting materials has been cleaved to a monosaccharide moiety. The new compounds have been found to retain the biological activity of the parent C-076 compounds. The compounds are thus potent antiparasitic agents and compositions and methods for such uses are also disclosed.