Abstract: Aminocrotonyl derivatives of 4-nitropyridine N-oxides are disclosed to have activity in increasing the sensitivity of tumor cells to radiation. Also disclosed are methods of preparing such compounds and pharmaceutical compositions including such compounds.

Abstract: Novel, transient prodrug forms of biologically active agents containing mercapto groups have (i) the structural formula (I): ##STR1## wherein X is O, S, or NR.sup.5 ;R.sup.1 S is the residue of any biologically active agent R.sup.1 SH;R.sup.

Abstract: Aminocrotonyl derivatives of 3,5-dinitropyridines are disclosed to have activity in increasing the sensitivity of tumor cells to radiation. Also disclosed are methods of preparing such compounds and pharmaceutical compositions including such compounds.

Abstract: 1-(3-Substituted-2-pyridinyl)piperazines and their acid addition salts are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressant agents and for treating sedation caused by antihypertensive therapy.

Abstract: A process is disclosed for preparing carboxyalkyl dipeptides of the formula: ##STR1##

Abstract: A method and drug form enhancing the absorption of a rectally or orally administered drug from the rectal compartment into the blood stream of a warm blooded animal. The method includes the steps of preparing a drug form capable of being rectally and orally administered. The drug form comprises a therapeutically effective unit dosage amount of a selected drug of the type which is capable of being absorbed into the blood stream from the gastrointestinal area and an .alpha.-keto aldehyde or salts thereof being present in the drug form in a sufficient amount to be effective in enhancing the drug absorption rate, when administering the drug form to warm blooded animals.

Abstract: Totally synthetic analogs of the known inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase, compactin and mevinolin, are prepared from a chiral synthon derived from D-glucose which has the same chirality as the natural products.

Abstract: Tricyclic derivatives of substituted pyrrole acids, e.g., substituted 4,10-dihydro-10-oxo-1H-[1]benzoxepino[4,3-b]pyrrole-2-acetic acids or the 5-thia analogs thereof have been prepared via hydrolysis of a precursor or decarboxylation of a precursor-diacid. These tricyclic compounds are found to have high analgesic and anti-inflammatory activities but low ulcerogenic side effects.

Abstract: Greatly enhanced delivery of a wide variety of bio-affecting agents is provided by formulations for topical application comprising at least one bio-affecting agent and eucalyptol. Optionally, the formulation can further comprise a non-toxic topical carrier and/or an additional penetration enhancer. The eucalyptol acts as a unique transport agent which readily delivers the active bio-affecting agent across the stratum corneum to the target area. Cosmetic and therapeutic dermatological agents as well as systemically effective therapeutic agents can be easily formulated with eucalyptol and effectively delivered through the skin to the desired site, i.e., to the underlying tissues of the epidermis and dermis or to the general circulation.

Abstract: A new strain of Escherichia coli which is enteropathogenic to both calves and piglets is produced by bacterial conjugation of two parents, one enteropathogenic solely to calves and one enteropathogenic solely to piglets. The new strain is useful in the preparation of a vaccine for use in both calves and piglets to prevent colibacillosis.

Abstract: A drug delivery system designed to deliver water and drug to the site of administration is composed of a core of an aqueous solubulizing system in a wax housing, which melts at body temperature, surrounded by a matrix of drug and water-dispersible excipients. The entire unit may also be coated with a semi-permeable membrane to modulate drug release.

Abstract: There is disclosed an improved process for the preparation of monochloroacetone by reacting acetone and chlorine in a vapor-liquid phase reactor and passing the reactor effluent through a fractionator to remove the liquid phase consisting mainly of monochloroacetone (MCA). The fractionator vapor phase effluent is consisting of acetone, hydrogen chloride, some monochloroacetone, and some reaction by-products sequentially fractionated in a series of condensers of varying temperatures such that the hydrogen chloride is isolated free of impurities and the remaining reaction materials, consisting mainly of acetone with some dissolved hydrogen chloride are available for recycling back into the reactor. The hydrogen chloride, isolated in the vapor phase, may be quenched with water to produce concentrated aqueous hydrochloric acid which may be used in other chemical procedures or it may be compressed into anhydrous hydrogen chloride.

Abstract: An osmotic drug (or other beneficial substance) delivery system comprises a multi-chamber compartment formed by an external shell and one or more chamber-dividing walls each with a small orifice, of a microporous material and overlayers of semipermeable membranes completely covering the outer shell of all but one chamber and substantially covering the outer shell of the remaining chamber. Osmotic agents, adjuvants, enzymes, drugs, pro-drugs, pesticides and the like are incorporated in the chambers covered by the semipermeable membrane, and external fluids that diffuse into those chambers form solutions and by osmotic pressure are forced through the orifice to the drug chamber to form a solution thereof and then through the exposed microporous shell to the exterior of the device at a rate controlled by the permeability of the semipermeable overlay and the osmotic pressure gradient across the shell.

Abstract: Although dibasic carbonic anhydrase inhibitors (C.A.I.) can be administered systemically by oral or intravenous routes, attempts to administer them topically were inadvisable because of their elevated pH. The mono-alkali metal salts in the treatment of intraocular hypertension especially the sodium and potassium salts, of dibasic salt-forming C.A.I. are as effective in lowering intraocular pressure as dialkali metal salts of dibasic C.A.I. while having a pH more in harmony with ocular pH. They are found particularly useful when administered in conjunction with an ophthalmologically acceptable water-soluble polymer such as hydroxypropylcellulose in an aqueous carrier.

Abstract: 8-Halo-6-nitro-1,2,4-triazolo[4,3-a]pyrazine and its corresponding 3-alkyl derivatives are prepared by converting amino-5,6-dichloropyrazinecarboxylic acid to 5-chloro-6-hydrazino-3-nitropyrazinamine and treating said hydrazino compound with a lower alkyl ortho ester of a loweraliphatic carboxylic acid to produce an 8-chloro-6-nitro-1,2,4-triazolo[4,3-a]pyrazine-5-amine or the corresponding 3-loweralkyl derivatives thereof.

Abstract: The present invention relates to aminoalkenoate ester derivatives of 2-amino-5-chloro-3-nitropyrazine useful as sensitizers of hypoxic tumor cells to therapeutic radiation. It also relates to the process of preparing such compounds by reaction of 2-amino-5,6-dichloro-3-nitro-pyrazine with an amino or alkylamino substituted .alpha.,.beta.-unsaturated alkenoate ester. In addition the application relates to pharmaceutical compositions containing such compounds and to methods of treatment comprising administering such compounds to patients undergoing radiation treatment to enhance the effectiveness of such treatment by sensitizing hypoxic tumor cells to therapeutic radiation.

Abstract: 5-Aroyl-4-RO-, 5-aroyl-4-RS-, 5-aroyl-4-RSO-, 5-aroyl-4-RSO.sub.2 -, or 5-pyrrylcarbonyl-pyrrole alkanoic acid have been prepared via hydrolysis of a precursor-ester after high temperature decarboxylation or from direct acidic decarboxylation of a precursor diacid. The compounds are analgesic and anti-inflammatory agents of high activities but low ulcerogenic side effects.

Abstract: This disclosure relates to an improved, new convertible child-resistant 2-piece closure comprising an inner cap comprising a circular top panel and integrally attached depending skirt having internal threads for engagement with corresponding external threads surrounding a conventionally threaded container exit neck. A plurality of spaced apart depressions extend downwardly from the top panel of said inner cap. Projecting upwardly and arranged in the same concentric circle of the top panel of said inner cap are a plurality of ratchet lugs, shaped in ramp form. An outer cap is also formed of a circular top panel and integrally attached depending skirt. Integrally formed on the inner side of the outer cap top panel are a plurality of downwardly extending drive lugs positioned in a circle of equal radius as the depression and ratchet lugs on the inner cap top panel.

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

Abstract: The (R,R)-enantiomers of trans-indeno[1,2-b]-1,4-oxazines demonstrate dopaminergic activity, whereas the (S,S)-enantiomers demonstrate .alpha.-adrenergic antagonist activity. They are prepared by cyclization of the appropriate chiral 2-amino-1-hydroxyindane.