Abstract: 2-Azasteroids, displaying valuable pharmacological properties, e.g. anti-viral, are manufactured by a total synthesis originating with dihydroresorcinol.

Abstract: The present invention encompasses a compound of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein Y is alkylene having 1-4 carbon atoms; R.sub.1 and R.sub. 2 together with N is a heterocyclic ring system consisting of an azamonocyclic ring of the formula ##STR2## wherein Z is oxygen, methylene, phenylhydroxymethylene, phenylcarboxymethylene or, phenylloweralkoxymethylene, or an azabicycloalkane structure having 6-9 carbon atoms and having at least 5 atoms in each ring of the azabicycloalkane structure; X is hydrogen, halogen, loweralkyl having 1-7 carbon atoms, or loweralkoxy having 1-7 carbon atoms; and Ar is phenyl, pyridyl, or monosubstituted phenyl wherein the substituent is halogen, loweralkyl having 1-7 carbon atoms, or loweralkoxy having 1-7 carbon atoms when R.sub.3 is hydrogen or Ar is 3 or 4 pyridyl when R.sub.3 is lower alkyl having 1-7 carbon atoms.

Abstract: The administration of aldosterone inhibitors of the spirolactone structural type prior to and during treatment with anti-neoplastic agents such as adriamycin results in retention of the desired activity of the latter substances while inhibiting their undesirable cardiotoxic properties.

Abstract: There is provided novel and useful pro-drug forms of theophylline having the formula: ##STR1## wherein R represents a member selected from the group consisting of a straight or branched C.sub.4 -C.sub.20 alkyl group, a straight or branched C.sub.14 -C.sub.20 alkenyl group, a substituted phenyl group or a substituted or unsubstituted naphthyl group whose substituents are selected from the group consisting of a hydroxy group, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.14 acyloxy group, and a halogen atom (Cl, Br, I), and a substituted or unsubstituted heteroaromatic group whose substituents are selected from the group consisting of a hydroxy group, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.4 acyloxy group, and a halogen atom (Cl, Br, I), and wherein A presents a member selected from the group consistng of a --CO-- group, a --CO--(CH.sub.2).sub.

Abstract: There is provided, a method for synthesizing certain selected pro-drug forms of theophylline, having the formula: ##STR1## wherein R represents a member selected from the group consisting of a straight or branched C.sub.4 -C.sub.20 alkyl group, a straight or branched C.sub.4 -C.sub.20 alkenyl group, a substituted phenyl group or a substituted or unsubstituted naphthyl group whose substituents are selected from the group consisting of a hydroxy group, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.4 acyloxy group, and a halogen atom and a substituted or unsubstituted heteroaromatic group whose substituents are selected from the group consisting of a hydroxy group, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.4 acyloxy group, and a halogen atom, and wherein A represents a member selected from the group consisting of a --CO-- group, a --CO--(CH.sub.2).sub.

Abstract: The present invention comprehends a method for treating diarrhea comprising administering to an animal in need of anti-diarrheal treatment an effective antidiarrheal amount of a compound of the formula ##STR1## AND ACID ADDITION SALTS THEREOF WHEREIN Y is alkylene containing 1-4 carbon atoms; R.sub.2 and R.sub.3 together with N is a heterocyclic ring system comprising azamonocyclic ring of the formula ##STR2## wherein Z is phenylhydroxymethylmethylene, phenylhydroxymethylene, phenylcarboxymethylene, phenylcarbalkoxymethylene or azabicycloalkyl or phenyl or hydroxyl substituted azabicycloalkyl containing 6-9 carbon atoms and containing at least 5 atoms in each ring of the azabicycloalkyl or 4-azatricyclo[4.3.1.1.sup.3,8 ]undec-4-yl; Ar.sub.1 and Ar.sub.2 are phenyl, halo-substituted phenyl, (lower alkyl) substituted phenyl, pyridyl, thienyl or furyl, and Ar.sub.

Abstract: 8-Chloro-10,11-dihydrodibenz[b,f][1,4]oxazepine is transformed by various microorganisms into compounds having useful pharmacological properties or useful as intermediates in the synthesis of various pharmaceutical compounds. Among the microorganisms useful for this purpose are Trichoderma lignorum NRRL 8138, Hormodendrum sp. NRRL 8133, Cladosporium lignicolum NRRL 8131, Hormodendrum cladosporioides NRRL 8132, Pullularia pullulans NRRL 8137, Penicillium sp. NRRL 8136, Mucor sp. NRRL 8135, Chaetomium sp. NRRL 8130, and Hormodendrum sp. NRRL 8134.

Abstract: The present invention is concerned with a method for preparing grandisol, the major component of the boll weevil sex pheromone. This method involves the conversion of 4-chloro-2-butanone to 5-chloro-3-methyl-1-penten-3-ol, acid-catalyzed isomerization of the latter compound to E- and Z-5-chloro-3-methyl-2-penten-1-ol, followed by conversion to ethyl 3-[2-chloroethyl]-3-methyl-4-pentenoate by treatment with triethyl orthoacetate, cyclization of ethyl 3-[2-chloroethyl]-3-methyl-4-pentenoate to ethyl Z- and E-2-vinyl-2-methylcyclobutanecarboxylate by reaction with base, conversion of ethyl Z- and E-2-vinyl-2-methylcyclobutanecarboxylate to Z- and E-2-[2-methyl-2-vinylcyclobutyl]-2-propanol by reaction with methyllithium, and the conversion of the latter compound to grandisol by reaction with diborane and basic hydrogen peroxide followed by dehydration.

Abstract: The present invention encompasses compounds of the formula ##SPC1##Wherein R.sub.1 is lower alkyl containing 1-7 carbon atoms, phenyl, halo(substituted)phenyl, phenyl, or lower alkoxy (substituted)phenyl containing 1-7 carbon atoms; R.sub.2 and R.sub.3 are lower alkyl containing 1-7 carbon atoms; and R.sub.4 is hydrogen or lower alkyl containing 1-7 carbon atoms. The compounds of the present invention are prepared by the condensation of alkyl(4-formylphenoxy)-2,2-dialkyl acetate with an appropriate alkyl or aryl methyl/ketone in base. These compounds have antibiotic activity and in particular they are antifungal agents effective against Trichophyton mentagrophytes. Halophenyl members of the present invention are also effective hypolipemic agents.

Abstract: The present invention is concerned with the preparation of 3-oxo-pregna-4,17(20)-dien-21-carboxylic acid and esters thereof by the microbial degradation of fucosterol, cholesterol, stigmasterol, campesterol or sitosterol with Mycobacterium sp. NRRL B-8054. The compounds of the present invention are useful antispasmodic agents and are also active against influenza virus.

Abstract: Derivatives of the dibenzoxazepine N-carboxylic acid hydrazides are acylated to yield N,N'-diacyl hydrazines which are useful pharmacological agents as is evidenced by their anti-arrhythmic, anti-inflammatory, anti-diarrheal, prostaglandin antagonist and 5-hydroxytryptamine antagonist activity.

Abstract: The present invention is concerned with a pharmaceutical delivery device comprising a biologically acceptable silicone polymer matrix having microsealed compartments of 10-200 microns throughout, wherein the microsealed compartments contain a pharmaceutical in a hydrophilic solvent system. The biologically acceptable silicone polymer matrix is formed by in situ cross linking of a liquid, biologically acceptable silicone polymer in an emulsion of pharmaceutical in the hydrophilic solvent system and liquid biologically acceptable silicone polymer. The biologically acceptable silicone polymer matrix is placed in a sealed or unsealed biologically acceptable polymer container.

Abstract: The present invention is concerned with a method for sterilizing psyllium seed husk without substantial swelling of the psyllium seed husk comprising contacting for 5 minutes or more said psyllium seed husk with a 15.degree.-50.degree. C solution of 0.2-10% by weight hydrogen peroxide in a solvent having 2-50 parts by volume water and 50-98 parts by volume isopropanol.

Abstract: The present invention encompasses compounds of the formula ##SPC1##Wherein R represents hydrogen or lower alkyl having 1-7 carbon atoms and wherein one X represents (nitrogen) N and the other X represents methylidyne. The compounds of the present invention are prepared by the methods set out in the following scheme: ##SPC2##Wherein R and X are as defined above. Compounds of the present invention are useful anti-inflammatory agents.

Abstract: Interferon and interferon-like proteins isolated from animal cells are purified by means of zonal density gradient centrifugation.

Abstract: Octapeptide derivatives characterized by an oxygen or sulfur-containing moiety in the C-terminal position are potent inhibitors of the pharmacological effects of Angiotensin and possess the additional advantage of a favorable antagonist/agonist ratio.

Abstract: The present invention is concerned with a vegetable oil emulsion containing from 1-10% water, preferably 1-5% water, and 1-4% emulsifying agent. The emulsifying agent is a particular mixed polyglycerol ester of 12-hydroxy-9 octadecenoic acid or of dimerized fatty acids of soybean oil. These water-in-oil (w/o) emulsions are useful in preparing edible food products, cosmetics and paints containing a minimum amount of water.

Abstract: Vaccines affording protection against the diseases resulting from infection of cats with feline leukemia virus are produced from cells infected with that virus or from the virus alone.

Abstract: Preparation of the subject compounds by reaction of 1-(3-cyano-3,3-diphenylpropyl)-4-phenylpiperidine-4-carboxylic acid with an N-hydroxy compound of the type HO--N Q wherein ##EQU1## represents an optionally substituted monocyclic- or fused polycylic-heterocyclic radical containing at least one carbonyl function adjacent the nitrogen atom, in the presence of a suitable dehydrating agent, and their useful biological properties, including analgesic and especially potent antidiarrheal activity are disclosed.

Abstract: 2-(2-Methyl-5-nitro-1-imidazolyl)ethyl esters of cycloaminocarbodithioates are herein described. These compounds are anti-protozoal and anti-fungal agents. The compounds are prepared in 2 steps. The reaction of the appropriate cycloamine with carbon disulfide in aqueous base forms the aminocarbodithioate salt and the final products are formed by the reaction of this salt with 1-(2-chloroethyl)-2-methyl-5-nitroimidazole.