Abstract: The present invention relates to novel compounds, in particular novel imidazo[1,2-a]piridine derivatives according to Formula (I). The compounds according to the invention are positive allosteric modulators of metabotropic receptors-sub-type 2 (‘mGluR2’) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

Abstract: The present invention relates to crystalline forms of 11?-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17?-pregna-4,9-dien-3-one. The invention relates in particular to two crystalline ansolvate/anhydrate forms of this compound, polymorphs I and II. However, the present invention also relates to crystalline solvates, for example methanol and ethanol solvates of 11?-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17?-pregna-4,9-dien-3-one as precursors for preparing these two polymorphs I and II. Processes for preparing polymorph I by displacement crystallization or by trituration are described. Selection of the last solvent before formation of the ansolvate can be based on the differences in the purification behaviour of the individual solvates of 11?-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17?-pregna-4,9-dien-3-one. Polymorph I according to the invention is particularly suitable for the manufacture of medicinal products.

Abstract: Materials and methods for treating certain cancers are described, preferably cancers that result from the up-regulation of the RAF-MEK-ERK pathway, and more preferably chronic myelogenous leukemia, and which cancer is preferably resistant to the inhibition of the Bcr-Abl tyrosine kinase, imatinib.

Abstract: The present invention relates to stilbene and quinone compounds related to combretastatin A-4 and their use as anticancer compounds and prodrugs. The compounds include those with an alkyl group on the double bond of cis or trans-stilbenes, compounds with one or more (and preferably 2 or 3) alkyl group substituents on the stilbene A ring, compounds with an alkoxy group other than methoxy at position 3, 4, and/or 5 of the stilbene A ring, compounds (or prodrugs) in which BOC amino acid esters are formed with the phenolic hydroxyl at the 3-position of the B ring and compounds (or prodrugs) based on a benzoquinone B ring. The present invention further relates to the photochemical reactions of stilbene compounds, either the above compounds disclosed for the first time herein or compounds based on prior art stilbenes.

Abstract: The invention relates to the utilization of a highly fluorinated oligomeric alkane as a therapeutic agent in ophthalmology, the alkane having the general formula [—RF(CH2)nCR1—CR2—]x, wherein RF is a linear or branched perfluorinated alkyl chain C2F5 to C12F23, R1 and R2 are independently selected from the group consisting of H, CH3, C2H5 and C3H7, n is selected from the numbers 0, 1 and 2, and x is a number between 2 and 6, with a molar mass of at least 750. According to the invention, a pharmacological agent is provided that is used in ophthalmology and that causes little or no damage to the retina even when used over a long period.

Abstract: Perfluorocarbons are used to control nitric oxide metabolism, either to inhibit nitric oxide activity or to potentiate the effects of nitric oxide. Perfluorocarbons can be used, for example, to treat hypotension and vasoplegia in septic shock, to protect against myocardial ischemia-reperfusion injury, to treat hypertension, and to provide antiplatelet effects.

Abstract: A stable FC emulsion is described. The FC emulsion of the present invention comprises a continuous FC immiscible hydrophilic liquid phase and a dispersed phase comprising FC suspended as droplets within the continuous phase. The emulsion further comprises an emulsifying agent and a stabilizing agent. The stabilizing agent of the present invention reduces the ability of the FC droplets to move within the continuous phase. The present invention also provides a method of making a FC emulsion. The method comprises mixing an FC immiscible hydrophilic liquid and a solid emulsifying agent by agitation at a temperature elevated above the phase transition temperature of the emulsifying agent and below the boiling temperature of the FC immiscible hydrophilic liquid, and adding FC to the mixture of step (a) and agitating at the elevated temperature to disperse droplets of FC in the FC immiscible hydrophilic liquid to form the FC emulsion.

Abstract: Cosmetic or personal care compositions comprise: a hair styling polymer having one or more groups selected from acidic functional groups, anionic groups derived from the acidic functional groups or a mixture of said groups; a partially or fully fluorinated compound having one or more groups selected from amino groups, acid salts of the amino groups or a mixture of said groups, wherein the partially or fully fluorinated compound comprises an aromatic ring; and a cosmetically acceptable diluent or carrier. The compositions are particularly effective under high humidity conditions.

Abstract: This invention relates to a method for the inhibition of the growth of undesirable microorganisms on fruit, vegetable, turfgrass and other plant systems by the application of specific enzymes either alone or in combination with fungicidally active agents.

Abstract: The present invention relates to a chemical composition useful in the chemical management of plant disease. The pesticides of the present invention incorporate benzophenanthridine alkaloids into formulations that are (1) residual and active for a period of time, (2) are adhesive to plant surfaces, (3) have good spreading properties, (4) are stable against photodeactivation, (5) have low phytoxicity, and (6) are capable of penetrating plant tissues.

Abstract: A method is disclosed for the treatment of right to left shunt. The method comprises introducing, into the blood circulation of an individual, to be treated, a therapeutically effective amount of the stabilized microbubbles. In a preferred embodiment, oxygen is additionally administered to the individual.

Abstract: Disclosed are methods of using stabilized microbubbles, such as those formulated from slowly permeating gas, to deliver or remove from tissue at least one gas selected from a respiratory gas, anesthetic gas, inert gas, or toxic gas. The methods comprise introducing, into the blood circulation of an individual to be treated, a therapeutically effective amount of the stabilized microbubbles. The methods are based on using the inherent physical properties of the blood circulation, of the microbubbles, and of the gases. The methods are especially useful for enhancing transport of oxygen in applications or conditions such as blood loss, anemia, organ perfusion, coronary Angioplasty, venous to arterial shunting of blood, oxygenation of ischemic tissues resulting from vascular obstructions, and oxygenation of solid tumor tissues in anticancer therapy.

Abstract: Novel hydrocarbon oil/fluorochemical preparations and methods for their use are provided. The preparations, which preferably comprise a fluorophilic dispersing agent, may be in the form of hydrocarbon oil-in-fluorochemical dispersions or in the form of a multiple emulsion comprising a polar liquid continuous phase and are particularly useful for administering bioactive agents. In particular the preparations of the present invention may be used to control the bioavailability and improve the efficacy of lipophilic bioactive agents having limited solubility in an aqueous physiological environment.

Abstract: The present invention concerns the use of hydrofluorocarbon compounds with formula (I):R.sub.F -(CH.sub.2).sub.n -X-?C.sub.3 H.sub.5 (OH)!-Y-(CH.sub.2).sub.m -R'.sub.F (I')whereC.sub.3 H.sub.5 (OH) represents the structures: ##STR1## R.sub.F and R.sub.F', which may be identical or different, represent a perfluorinated linear or branched C.sub.4 -C.sub.20 alkyl radical or a mixture of perfluorinated linear or branched C.sub.4 -C.sub.20 alkyl radicals;m and n, which may be identical or different, are 0, 1, 2, 3 or 4;X and Y, which may be identical or different, represent O or S. It also concerns certain of these compounds and cosmetic compositions containing these compounds.

Abstract: Stable emulsions of highly fluorinated organic compounds for use as oxygen transport agents, "artificial bloods" or red blood cell substitutes and as contrast agents for biological imaging. The emulsions comprise a highly fluorinated organic compound, an oil that is not substantially surface active and not significantly soluble in water, a surfactant and water.

Abstract: Stable emulsions of highly fluorinated organic compounds for use as oxygen transport agents, "artificial bloods" or red blood cell substitutes and as contrast agents for biological imaging. The emulsions comprise a highly fluorinated organic compound, an oil that is not substantially surface active and not significantly soluble in water, a surfactant and water.

Abstract: Perfluoroindane is used as a gas transport agent in animals without causing gas or vapor pulmonary embolism. Emulsions containing perfluoroindane as the oxygen carrying component are made and infused into an animal and the perfluoroindane escapes at a very rapid rate from the animal body. The perfluoroindane-containing liquids or emulsions are considered valuable for angioplasty and as a blood substitute.

Abstract: Stable emulsions of highly fluorinated organic compounds for use as oxygen transport agents, "artificial bloods" or red blood cell substitutes and as contrast agents for biological imaging. The emulsions comprise a highly fluorinated organic compound, an oil that is not substantially surface active and not significantly soluble in water, a surfactant and water.

Abstract: Nonaqueous thixotropic drug delivery vehicles for use in aqueous physiological systems are disclosed comprising a substantially homogeneous dispersion of at least one suspending aid in a nonaqueous perfluorocarbon or fluorinated silicone liquid carrier. Pharmaceutical compounds may be incorporated to provide thixotropic pharmaceutical compositions having improved delivery profiles and high drug localization. The thixotropic compositions act as free-flowing, drop-instillable liquids upon the application of stress yet behave as a visco-elastic material when at rest. Due to these thixotropic properties the pharmaceutical compositions have improved bioavailability, are capable of low dose volume delivery, and do not degrade the incorporated therapeutic or diagnostic compounds making them well suited for multidose packaging and administration.

Abstract: Oil and water emulsions containing alkylphosphoryl choline or alkylglycerophosphoryl choline surfactants are disclosed. The surfactants have the following general structures: ##STR1## In the above general structures, R.sub.1, R.sub.2 or R.sub.3 is alkyl, alkenyl, fluoroalkyl and alkenyl; and PC is the phosphoryl choline. The emulsions are useful as oxygen transport agents, artificial bloods or red blood cell substitutes.

Abstract: The present invention relates to fluorochemical blood substitutes used for preserving mammalian tissue having lysophosphatidyl compounds in non-toxic concentrations. More specifically, the invention relates to aqueous fluorochemical emulsions of a fluorochemical and an emulsifier useful as oxygen delivery agents and methods of preserving tissue in investigational and clinical settings, particularly those settings involving in in vivo transfusion, cardiac and other organ preservation, and in vitro organ perfusion.

Abstract: Improved emulsions of highly fluorinated organic compounds. The emulsions comprise a highly fluorinated organic compound, an oil, that is not substantially surface active and not significantly water soluble, and a surfactant. They are characterized by a well-defined relationship in the relative amounts of the three components.

Abstract: A stable concentrated aqueous emulsion of perfluorochemical, a phospholipid and a triglyceride of fatty acids has been demonstrated which has enhanced stability, diminished particle size and heightened tolerance by biological systems. The emulsion has utility as an oxygen transport medium, such as artificial blood. The emulsion can optionally include additional emulsifiers of SURFYNOL.RTM.SE surfactant and PLURONIC.RTM. P-105 surfactant. The emulsion is produced using an improved emulsification technique. The invention includes methods of oxygen transport in vascular systems wherein the oxygen carrying capacity of the vascular systems is improved with the emulsions of the present invention. Methods are also described for organ preservation extra-vivo by perfusing, suffusing, flushing and filling organs outside the body with the oxygen carrying emulsions of the present invention.

Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.

Abstract: A compound of formula: ##STR1## wherein W represents one or more substituents selected from halo, alkyl, alkoxy, alkoxyalkyl, haloalkyl and haloalkoxy or W represents a bidentate group linking adjacent carbon atoms selected from alkylene and alkylenedioxy; Y is a group of formula ##STR2## wherein X is a group of formula --(CF.sub.2).sub.n R.sup.3, where R.sup.3 is selected from hydrogen, chloro and fluoro, and n is one or two, R.sup.1 is selected from hydrogen, chloro, fluoro and hydroxy and R.sup.2 is selected from methyl, cyano, ethynyl and hydrogen; Q is selected from carbon bearing a hydrogen atom and nitrogen; and Z represents one or more substituents selected from fluoro, benzyl, phenoxy, chlorophenoxy, fluorophenoxy and bromophenoxy, or any isomer thereof. Processes for preparing these compounds and intermediates for use therein, insecticidal compositions containing these compounds and the use thereof are also disclosed.

Abstract: This invention relates to a novel compound represented by the following general formula (I), its production, and an insecticidal and acaricidal composition containing it as an active ingredient: ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, are a hydrogen atom, a halogen atom, a lower alkyl group, a trifluoromethyl group, a lower alkoxyl group, a lower alkenyloxy group or a halogenated lower alkoxyl group or are, taken together, a methylenedioxy group; R.sub.3 is a vinyl group or a ethynyl group; R.sub.4 is a hydrogen atom or a lower alkyl group; R.sub.5 is a hydrogen atom or a fluorine atom; R.sub.6 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxyl group or a trifluoromethyl group; Z is a nitrogen atom or a group represented by the formula --CH.dbd.; when Z is a nitrogen atom, Y is an oxygen atom; and when Z is a group of the formula --CH.dbd., Y is an oxygen atom, a sulfur atom, a methylene group or a group represented by the formula --NH--.

Abstract: A method of inhibiting the absorption of nutritional elements, principally food, from the gastrointesinal tract is disclosed which comprises ingesting perfluorodecalin in an amount sufficient to form a nutritional element-impermeable film thereof on at least a substantial part of the inner wall of the upper intestine and maintaining the film for a time long enough to inhibit the absorption from the gastrointestinal tract of a significant proportion of the ingested nutritional elements. An emulsion dosage form is preferred for carrying out this method, which emulsion contains perfluorodecalin, water, and a non-toxic emulsifier, preferably Pluronic F-68, and optionally flavoring and/or coloring agents.

Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.