Abstract: The invention relates to novel 1,2-disubstituted-4-nitroimidazole compounds that are useful as potent antiprotozoal agents and simultaneously possess non-mutagenicity as compared to known 4- or 5-nitroimidazole compounds. Also, compositions and methods for antiprotozoal uses of said novel 1,2-disubstituted-4-nitroimidazole compounds are disclosed herein.

Abstract: Benzo(f)isoquinoline compounds, particularly, penta- and tetrahydrobenzo(f)isoquinoline dicarboxylic acid compounds, their preparation and their use as calcium entry blockers are disclosed.

Abstract: There is disclosed a macrolide isolated from the fermentation broth, with 22,23-dihydro avermectin Bla aglycone as a substrate, of a known microorganism identified as MA-5853. The structure of the novel compound isolated from the microorganism is presented based upon analytical studies. The compound is a highly potent antiparasitic, insecticidal, and anthelmintic agent. Compositions for such uses are also disclosed.

Abstract: Substituted lactams and related compounds and methods for their preparation are disclosed. These compounds are useful as angiotensin converting enzyme inhibitors and as antihypertensives.

Abstract: There are disclosed novel compounds which are derived from 22,23-dihydro avermectin Bla aglycone, 13-deoxy-22,23 dihydro overmectin Bla aglycone and 13-deoxy-22,23-dihydro overmectin Blb aglycone. The six compounds are hydroxy adducts of the substrate avermectin compound at the 12a, 24, 24a, 26, 26a and 27 positions. The hydroxy adducts are prepared by incubating the substrate with the microorganism Cunninghamella blakesleeana and isolating the hydroxy adducts from the fermentation broth. The compounds are highly potent antiparasitic, insecticidal and anthelmintic agents.

Abstract: The invention relates to compositions and methods of enhancing rectal absorption of L-dopa via the formation of an ester prodrug and optionally with a decarboxylase inhibitor.

Abstract: The present invention is directed to a synergistic antimicrobial admixture comprising 2-bromo-2-bromomethylglutaronitrile and a formaldehyde donor.

Abstract: The instant invention is directed to an admixture, and its use in inhibiting scale and corrosion in aqueous systems, comprising:(a) a water-soluble polymer having a weight average molecular weight of less than 25,000, as determined by low angle laser light scattering, comprising an unsaturated carboxylic acid and an unsaturated sulfonic acid, or their salts, having a ratio of 1:20 to 20:1, and(b) at least one compound selected from the group consisting of water-soluble polycarboxylates, phosphonates, phosphates, polyphosphates, metal salts and sulfonates.The instant invention is also directed to a method of inhibiting the formation of insoluble alluvial, metal oxide and metal hydroxide deposits in an aqueous system, comprising adding to the system at least 0.

Abstract: The instant invention is directed to a polymer with at least one labile backbone bond per repeat unit and at least one pendant acid functionality per thousand repeat units.The instant invention is also directed to a controlled release device which comprises:(A) a polymer with at least one labile backbone bond per repeat unit and at least one pendant acid functionality per thousand repeat units; and(B) a beneficial substance incorporated within or surrounded by the matrix of said polymer.

Abstract: Novel 3-amino or substituted amino pyrazoles are disclosed as having antiprotozoal and antiparasitic activity in particular anticoccidial activity and are useful for controlling cecal and or intestinal coccidiosis when administered in minor quantities to animals, in particular to poultry usually in admixture with animal sustenance.

Abstract: There are disclosed novel O-sulfate derivatives of avermectin and milbemycin. The avermectin and milbemycin O-sulfate derivatives have improved water solubility compared to the parent avermectin and milbemycin compounds and have utility as anti-parasitic agents and as potent insecticides against agricultural pests.

Abstract: A novel process for the preparation of intermediates in the totally synthetic antihypercholesterolemic agents, 6-[2-[1,1'-biphenyl]-2-yl-ethenyl] pyranones, involving a highly efficient nickel catalyzed aryl cross-coupling reaction is disclosed.

Abstract: The instant invention is directed to a process for inhibiting corrosion and the formation and deposition of scale and iron oxide in aqueous systems, comprising adding to the system at least 0.1 ppm of a water-soluble polymer having an intrinsic viscosity of 0.05 to 2.5 dl/g, prepared from:(a) 35 to 90%, by weight, of an unsaturated carboxylic acid, or its salt;(b) 5 to 40%, by weight of an unsaturated sulfonic acid, or its salt; and(c) 5 to 40%, by weight, of an unsaturated, polyalkylene oxide compound, the total of (a), (b) and (c) being 100% weight of the polymer.

Abstract: The present invention is directed to a composition useful for inhibiting the corrosion of copper and copper alloy metals in an aqueous system comprising mercaptothiazoline and ferrous ions.The present invention is also directed to a method of inhibiting the corrosion of copper and copper alloy metals in an aqueous system comprising maintaining in the aqueous system at least about 1 ppm (parts per million) of mercaptothiazoline, preferably in combination with ferrous ions.

Abstract: The instant invention is directed to synergistic antimicrobial admixtures comprising 2-bromo-2-bromomethylglutaronitrile and methylene bis(thiocyanate) and its use in inhibiting microbial growth.

Abstract: Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven of the ring amino acids of somatostatin. 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. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method and/or solution synthesis.

Abstract: Cyclic hexapeptide somatostatin analogs are prepared wherein a peptide surrogate replaces eight of the ring amino acids of somatostatin. 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. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method.

Abstract: Pharmaceutical compositions and methods useful in the treatment of cardiac arrhythmias are described.

Abstract: The instant invention is directed to a process for inhibiting corrosion and the formation and deposition of scale in aqueous systems comprising adding to the system at least 0.1 ppm. of a water soluble polymer, having an intrinsic viscosity of 0.05 to 2.5 dl/g, prepared from:(A) 50 to 95%, by weight, of an unsaturated carboxylic acid, or its salt, and(B) 5 to 50%, by weight, of a betaine-containing monomer selected from the group consisting of: ##STR1## wherein R, which may be the same or different, is hydrogen, a straight or branched, alkyl or an aryl or alkylaryl group of from 1 to 20 carbon atoms;R.sup.

Abstract: The instant invention is directed to synergistic antimicrobial admixtures comprising 2-bromo-2-bromomethylglutaronitrile and 2,2-dibromo-3-nitrilopropionamide and its use in inhibiting microbial growth.