Abstract: Novel naphthyridines having a 3-amino-2-OR-propoxy substituent are disclosed. The compounds have .beta.-adrenergic blocking and immediate onset antihypertensive activities.

Abstract: Novel interphenylene derivatives of 11,12-secoprostaglandins are prepared by the stepwise alkylation of the ethyl ester or the t-butyl ester of acetoacetic acid. One such method involves treatment of the t-butyl ester of acetoacetic acid with a strong base to form the anion followed by treatment with ethyl p-(3-bromopropyl)benzoate to produce ethyl 4-(4-tert-butoxycarbonyl-5-oxo-hexyl)benzoate, subsequently reacting the anion of the thus-formed benzoate with 1-chloro-4-acetoxynonane to produce ethyl 4-(4-acetyl-4-tert-butoxycarbonyl-8-acetoxytridecyl)benzoate followed by decarboxylation and alkaline hydrolysis to produce the desired product 4-(4-acetyl-8-hydroxytridecyl)benzoic acid which is useful as a pharmaceutical in the treatment of patients with renal failure and in the prevention of transplant rejection.

Abstract: The novel compound 7-methyl-8-methylamino-10-(1'-D-ribityl)isoalloxazine is prepared. This compound has anticoccidial, antiprotozoal and antiparasitic activity. It is particularly 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: Tricyclicdicarboximides representatively prepared by the Diels-Alder condensation of a cyclic diene such as cycloheptatriene, cyclooctatetraene and the like with a dienophile such as substituted N-phenylmaleimide and the like are disclosed having pharmaceutical utility as minor tranquilizers and anti-convulsants. Also disclosed are processes for the preparation of such tricyclicdicarboximides; pharmaceutical compositions comprising such compounds and their salt; ester and amide or derivatives; and methods of treatment comprising administering such compounds and compositions.

Abstract: An efficient method has been found for the removal of the 3-isomer present in crude 9-(2-chloro-6-fluorobenzyl)adenine. Crude 9-(2-chloro-6-fluorobenzyl)adenine is transalkylated in sulfuric acid-toluene to reduce the 3-isomer to undetectable levels (<100 ppm). Alternately, crude 9-(3-chloro-6-fluorobenzyl)adenine is first treated with dilute nitric acid to remove the bulk of the 3-isomer followed by transalkylation to sulfuric acid-toluene to reduce the 3-isomer to undetectable levels (<100 ppm). The overall yield for this purification is about 95% based on the 9-(2-chloro-6-fluorobenzyl)adenine content of the crude material. The resulting pure 9-(2-chloro-6-fluorobenzyl)adenine has anticoccidial activity and is useful in controlling cecal and/or intestinal coccidiosis when administered in minor quantities to animals, in particular to poultry usually in admixture with animal sustenance.

Abstract: Novel pharmaceutical compositions are disclosed. The compositions comprise an aryl substituted alanine and a substituted phenyl hydrazino propionic acid. The compositions are useful for treating hypertension.

Abstract: A process for preparing methyl vanillyl ketone from guaiacol is disclosed.

Abstract: Novel isothiazoles having a 3-amino-2-OR-propoxy or - propyl substituent are disclosed. The isothiazoles have pharmaceutical activity.

Abstract: A novel peptide designated anthopleurin-B, hereinafter also referred to as AP-B, obtained from the sea anemone Anthopleura xanthogrammica is found to possess cardiotonic activity.

Abstract: The case involves novel 3-amino-N-[(phosphonoamino)iminomethyl]-6-halopyrazinecarboxamides, derivatives thereof and processes for preparing same. 3-Amino-N-(phosphonoaminoiminomethyl)-6-halopyrazinecarboxamides of the instant case are eukalemic agents possessing diuretic and natriuretic properties.

Abstract: Somatostatin analogs having the structural formula:Cyclo[(X).sub.j -(A).sub.k -(B).sub.1 -Phe-Phe-(D- or L-)Trp-Lys-Thr-Phe-Thr-(C).sub.m ]WhereinX is ##STR1## and n=0 to 4; A is Lys, (.epsilon.-INOC) Lysine;B is Asn, Ala, .alpha.-aminobutyric acid;C is Ser, Gly;J, k, l and m are 0 to 1; with the proviso that j, k, l, and m are not all 1 and not all 0,Wherein the ring formed by the peptide backbone contains 24 to 33 atoms and the pharmaceutically acceptable non-toxic acid addition salts thereof are prepared by the solid phase method. These peptides have the property of inhibiting release of insulin, decreasing gastric secretion, inhibiting growth hormone release and inhibiting glucagon release in humans and animals.

Abstract: Somatostatin analogs having the structural formula: ##STR1## are prepared by controlled stepwise procedures starting with individual amino acid components. These peptides have the property of lowering blood glucose, inhibiting gastric secretion, inhibiting growth hormone release and inhibiting glucagon release in humans and animals.

Abstract: Novel polymers having a linear backbone which is free from both branching and cross-linking, comprising either tertiary or quaternized nitrogen atoms linked to each other through ethylene groups. These polymers are useful as antimicrobials, flocculating agents, antistatic agents, electroconductive agents for coating paper, chelating agents and bile acid binding agents, as well as in similar applications where their high charge to weight ratio and fully accessible nitrogen atoms can be employed. The polymers are obtained by the polymerization of an oxazoline, hydrolysis or direct reduction, nitrogen substitution, and optional quaternization of the resulting polymer.

Abstract: N-carboxyanhydrides of hydroxyphenylalanines are disclosed. The compounds have antihypertensive activity.

Abstract: Novel pharmaceutical compositions are disclosed. The compositions comprise an aryl substituted alanine and a substituted phenyl hydrazino propionic acid. The compositions are useful for treating hypertension.

Abstract: This case relates to a novel process which aids in the isolation and purification of novel compounds which are produced by the microorganism, Streptomyces avermitilis. The process described herein utilizes a hydroxypropyl Sephadex column chromatographic step in the isolation of the compounds from broth. The compounds which are isolated and purified are described generically s C-076 and have significant parasiticidal activity.

Abstract: 10,11-Dihydro-3-carboxycyproheptadine is disclosed to have pharmaceutical utility as an appetite stimulant and as an antihistaminic agent. Also disclosed are processes for the preparation of such compound; pharmaceutical compositions comprising such compound; and methods of treatment comprising administering such compound and compositions.

Abstract: Nuclear substituted 2-hydroxyphenylmethanesulfamic acids and their pharmaceutically acceptable salts wherein the phenyl nucleus is substituted with 2 to 4 nuclear substituents and which are useful saluretic-diuretics and anti-inflammatories are disclosed. The products may be prepared by reacting nuclear substituted salicylaldehydes with ammonium sulfamate to generate intermediate imines which are reduced to afford the compounds of this invention.

Abstract: Novel linear, unbranched, non-cross-linked polymers particularly poly-[{methyl-(3-trimethylammoniopropyl)iminio}trimethylene dihalide] are prepared by the polymerization of the novel monomer, 3-[N'-(3-halopropyl)-N'-methylamino]-N,N,N-trimethyl-1-propanaminium halide, or an acid addition salt thereof preferably in an oxygen excluded environment, e.g., under nitrogen or argon. The polymer, especially after modification of terminal groups, is an excellent oral anticholesterolemic.

Abstract: This invention relates to 9-thia- , 9-oxothia, and 9-dioxothia-11,12-seco-prostaglandins and processes for their manufacture. These compounds have prostaglandin-like biological activity and are particularly useful for the treatment of skin diseases such as psoriasis, for the prevention of thrombus formation, in stimulating the production of growth hormone in intact animals, and as regulators of the immune response.