Abstract: Diarylmethyl piperazine compounds having utility as exogenous receptor combinant species for binding with receptors such as delta, mu, sigma, and/or kappa receptors are disclosed. Compounds of the invention may be employed as conjugates in agonist/antagonist pairs for transductional monitoring and assays of neurotransmitter function, and also variously exhibit therapeutic utility, including mediating analgesia, and possessing utility for the treatment of diarrhea, urinary incontinence, mental illness, drug and alcohol addiction/overdose, lung edema, depression, asthma, emphysema, cough, and apnea, respiratory depression, cognitive disorders, emesis and gastrointestinal disorders.

Abstract: The prevention and treatment of exercise-induced pulmonary hemorrhaging in non-human mammals is accomplished by the timely administration of effective amounts of vasodilators, including angiotensin converting enzyme inhibitors such as lisinopril, enalapril and captopril, and angiotensin II blocking vasodilators such as losartan potassium.

Abstract: An antimicrobial lipid-containing oil-in-water emulsion comprising an agent selected from the group consisting of glycerol monooleate, glycerol trioleate, glycerol monolaurate, and glycerol dilaurate as the primary lipid and a cationic halogen-containing compound having a C.sub.12 -C.sub.16 chain as a positive charge producing agent is disclosed. The antimicrobial emulsion can be used in the form of a pharmaceutical preparation to inhibit the growth of a wide variety of infectious pathogens.

Abstract: An antimicrobial lipid-containing oil-in-water emulsion comprising an agent selected from the group consisting of glycerol monooleate, glycerol trioleate, glycerol monolaurate, and glycerol dilaurate as the primary lipid and a cationic halogen-containing compound having a C.sub.12 -C.sub.16 chain as a positive charge producing agent is disclosed. The antimicrobial emulsion can be used in the form of a pharmaceutical preparation to inhibit the growth of a wide variety of infectious pathogens.

Abstract: A method of inhibiting a physiological condition associated with an excess of bradykinin comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.

Abstract: A method is provided for avoiding premature labor in a pregnant mammal comprising administering to said mammal, during labor, but before an infant is to be delivered, an effective amount of an activin antagonist. In one embodiment, the antagonist is follistatin. In another aspect a method is provided for assaying whether a pregnant mammal is in imminent delivery of its fetus in preterm labor comprising contacting a maternal serum sample or amniotic fluid sample of the mammal with a reagent that detects activin A and measuring the level of activin A in the serum or amniotic fluid. In addition, a kit for the assay is provided.

Abstract: The present invention relates to a hydrazinecarboxamide derivative of the general formula (I) shown below: ##STR1## wherein the substituents are as defined in the specification, which has a wide insecticidal spectrum at a low dosage, a process for producing said derivative, and utilization of said derivative as an insecticide.

Abstract: Nabumetone which is spray-chilled and formulated into unit dose forms which have a smaller volume than was previously possible.

Abstract: A pharmaceutical composition for oral use comprising an effective amount of a compound of the formula (I) having antagonistic action to angiotensin II ##STR1## (wherein the ring W is an optionally substituted N-containing heterocyclic residue; R.sup.3 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; and n is an integer of 1 or 2) and an oily substance having a lower melting point, and a method for preparing a pharmaceutical composition for oral use comprising an effective amount of a compound of the formula (I) and an oily substance having a lower melting point, which comprises admixing the compound of the formula (I) with an oily substance having a lower melting point and then subjecting the mixture to molding.

Abstract: This invention provides a method of inducing cognition enhancement in a mammal by administering to the mammal experiencing a cognition impairment an effective amount of a hydroxycycloalkanephenethyl amine compound of the following structural formula: ##STR1## in which A is a moiety of the formula ##STR2## wherein the dotted line represents optional unsaturation;R.sub.1 is hydrogen or alkyl;R.sub.2 is alkyl;R.sub.4 is hydrogen, alkyl, formyl, or alkanol;R.sub.5 and R.sub.6 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, cyano, nitro, alkylmercapto, amino, alkylamino, dialkylamino, alkanamido, halo, trifluoromethyl, or taken together, methylene dioxy;R.sub.7 is hydrogen or alkyl; andn is 0, 1, 2, 3, or 4;or a pharmaceutically acceptable salt thereof.

Abstract: o-Iminooxymethylbenozic acids of the general formula I ##STR1## are disclosed where, m, X, R.sup.1 and R.sup.2 are defined herein.

Abstract: The present invention relates to compounds of the formula ##STR1## wherein B.sub.1 and B.sub.2 are each independently hydrogen; hydroxy; --OR.sub.2 wherein R.sub.2 is a C.sub.1 -C.sub.4 alkyl or an Ar-Y group wherein Ar is aryl and Y is a hydrogen or C.sub.1 -C.sub.4 alkyl; or, where B.sub.1 and B.sub.2 are attached to adjacent carbon atoms, B.sub.1 and B.sub.2 can be taken together with said adjacent carbons to form a benzene ring or methylenedioxy;A is a bond, methylene or oxygen, sulfur or NR.sub.4 or NCOR.sub.5 wherein R.sub.4 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar-Y- group and R.sub.5 is --CF.sub.3, a C.sub.1 -C.sub.10 alkyl or an Ar-Y- group;R.sub.3 is hydrogen or --CH.sub.2 OC(O)C(CH.sub.3).sub.3 ;R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or --CH.sub.2 OC(O)--C(CH.sub.3).sub.3 ; andn is an integer 1 to 3,which are useful as inhibitors of enkephalinase and ACE.

Abstract: Disclosed are novel compositions comprising mixtures useful to treat the metabolically impaired and to improve patient compliance. Included are non-racemic mixtures of certain chiral spirofluorenehydantoins. Methods of use to treat glucose toxicity and complications arising from diabetes mellitus are also disclosed.

Abstract: Administration of protein kinase C inhibitors protect neuronal cells from death from cerebral ischemia. Model for screening compounds for potential for protecting neuronal cells from death from cerebral ischemia comprises adding the compounds to medium containing neuronal cells before, at the same time as, and/or after nitric oxide administration.

Abstract: The present invention relates to the use in the treatment of cognitive disorders associated with the aging processes of the brain and perinatal brain disorders of compounds which act as inhibitors of the enzyme kynurenine aminotransferase (KAT).The present invention also provides, as novel compounds, a selected class of KAT inhibitors which are the compounds of formula (IA) ##STR1## wherein R is halogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.6 -C.sub.10 aryloxy, phenyl-C.sub.1 -C.sub.4 alkoxy or trifluoromethyl, andR.sub.1 is hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, mono-C.sub.1 -C.sub.6 alkylamino, di-C.sub.1 -C.sub.6 alkylamino, hydroxylamino, C.sub.1 -C.sub.4 alkoxyamino or benzyloxyamino; with the provisos that(i) when R.sub.1 is hydroxy and, at the same time, R is halogen, then this halogen is not fluorine; and(ii) when R.sub.1 is hydroxy and, at the same time, R is C.sub.1 -C.sub.6 alkyl, then this C.sub.1 -C.sub.

Abstract: A method for inhibiting smooth muscle cell proliferation in an injured blood vessel includes the steps of administering a photoactivatable psoralen to a patient in an amount to achieve local arterial tissue levels of psoralen suitable for light-dependent inhibition of smooth muscle cell growth, and delivering radiation in the visible wavelength range to the injured region of the blood vessel at a level sufficient for photoactivation of the psoralen. The psoralen is preferably 8-methoxypsoralen and can be delivered systemically or locally. The method of the invention can be used for preventing restenosis in a blood vessel following transluminal angioplasty. Both the psoralen and the visible light can be delivered with a laser balloon catheter having a porous balloon. The method of the invention may also be used for inhibiting proliferation of other undesired cell types in a patient's body.

Abstract: A new composition and method of treating depression includes administering to a depressed patient a pharmacologically effective dose of naloxone or naltrexone or their pharmacologically effective salts and esters in combination with at least one nontricyclic serotonin reuptake inhibitor antidepressant or their pharmacologically effective salts and esters. The patient may while undergoing antidepressant therapy be undergoing treatment with a benzodiazepine for anxiety.

Abstract: An antimicrobial and interferon-inducing composition containing the crystalline gamma-modification of para-amino benzenesulfanilamide and a method for inducing interferon by administering a composition containing crystalline gamma-modification of para-amino benzenesulfanilamide.

Abstract: The present invention provides three optical resolution methods. The first aspect comprises the steps of adding an optically active bifunctional resolving reagent to a bifunctional compound to form a liquid material, precipitating crystals therefrom, and treating the crystals and the liquid material separately with an acidic material, a basic material, or a basic material and an acidic material, to obtain a pair of enantiomers of an optically active bifunctional compound. The second aspect comprises an optical resolution method by which one necessary enantiomer of a pair of enantiomers in an optically active bifunctional compound is exclusively obtained. The third aspect comprises a method for racemizing one unnecessary enantiomer of a pair of enantiomers in an optically active bifunctional compound which is formed by the optical resolution method of the present invention.

Abstract: Compositions containing PBN, or active derivatives thereof, in a suitable pharmaceutical carrier for administration to a patient, are disclosed for treating or preventing gastric ulceration caused by ingestion of non-steroidal anti-inflammatories. Based on animal studies, the dosage is in the range of 3 to 300 mg/kg and is administered prior to, simultaneously, or shortly after ingestion of the NSAID compounds(s). In the preferred embodiment, the range is between 10 and 30 mg/kg, depending on the dosage unit required to protect the mucosa. The preferred method of administration is orally, alone or in combination with the non-steroidal anti-inflammatory. It is believed that the PBN is also useful alone for treatment or prevention of ulcers, aspects of diarrhea, gastritis, esophagitis, ileitis, and as an analgesic.