Abstract: The present invention is directed to novel compounds of Formula (I), pharmaceutically acceptable salts or solvates thereof, and their use.

Abstract: The present invention concerns a method for treating and/or preventing a disease in a subject comprising the step of administrating an effective amount of a compound of formula I to a subject in need thereof.

Abstract: Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.

Abstract: This invention relates to pharmaceutical compositions for veterinary use in form of aqueous injectable suspensions comprising Florfenicol or Florfenicol in form of a substantially water-insoluble complex, co-crystal or salt, sterile and micronised, in a concentration up to 500 mg/ml. The suspensions enable parenteral antimicrobial therapies in animals, with limited numbers of injections and showing good general- and local tolerances. They also possess a limited sedimentation on standing as well as after shipping, are easily resuspendable and have good syringablity.

Abstract: Gamma-amino-butyric acid derivatives that are GABAB receptor ligands, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives and pharmaceutical compositions thereof for treating diseases are disclosed.

Abstract: The invention relates to using neurotoxic substances which in particular are toxic to the axons and to the nociceptive nerve endings in the preparations of agents treating joint pains.

Abstract: Intraorally rapidly disintegrating tablets which, when ingested, disintegrates in the oral cavity rapidly without presenting unpleasant taste, can be quickly absorbed in the digestive tract and express efficacy are provided. The intraorally rapidly disintegrating tablets contain a drug being hardly water-soluble under neutral or alkaline conditions and being highly water-soluble under acidic conditions yet presenting unpleasant taste, which tablets can be prepared by combining the medicinal substance with a water-soluble acidic substance, coating either or both of the substances with a water-soluble coating agent being insoluble in alcoholic solvent, further adding a water-soluble binding agent being soluble in alcoholic solvent and a water-soluble saccharide, subjecting the resultant mixture to compression, and treating the products with an alcoholic solvent.

Abstract: This invention is directed to compounds of formula (I), wherein m, formula (II), R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment of iron disorders. This invention is also directed to pharmaceutical compositions comprising the compounds and methods of using the compounds to treat iron disorders.

Abstract: This application provides a method for the use of select quaternary ammonium antagonists to alpha-7 nAChR for the treatment of cancer and HIV and AIDS.

Abstract: Provided are methods of modulating, treating, reversing and/or preventing pain using tetrakis quaternary ammonium compounds, especially regarding pain of central and/or peripheral origin and/or pain which is nociceptive, neuropathic, somatic, visceral, and/or inflammatory in nature.

Abstract: The present invention provides a method of treating glaucoma or ocular hypertension which comprises applying to the eye of a person in need thereof an amount sufficient to treat glaucoma or ocular hypertension of a compound of formula I wherein Y, Q, Z, R, R1 and R2 are as defined in the specification. The present invention further comprises pharmaceutical compositions, e.g. ophthalmic compositions, including said compound of formula I.

Abstract: Methods for treating an individual having cancer are provided. The method may include administering a cell migration inhibitor and a chemotherapeutic agent to the individual to inhibit migration of cancer cell. Inhibiting cell migration may increase cell division. In this manner, the cell migration inhibitor and the chemotherapeutic agent in combination may have increased efficacy compared to the chemotherapeutic agent alone due to the increased cell division. The cell migration inhibitor may include any of the inhibitors described herein. For example, the cell migration inhibitor may be an organic molecule having a molecular weight of less than about 700, a monoclonal antibody, or a natural product.

Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.

Abstract: Compounds of formula I in which R has a meaning as indicated in claim 1, or one of their optical isomers or pharmaceutically acceptable salts, used for the treatment of extrapyramidal movement disorders and/or adverse effects in extrapyramidal movement disorders and/or for the treatment of extrapyramidal symptoms (EPS) induced by neuroleptics.

Abstract: The present invention generally relates to a novel therapeutical use of liver X receptor (LXR) agonsits. More specifically, the present invention relates to the use of LXR agonist for the preparation of a medicament useful for the treatment and/or the prevention of a disease associated with beta cells degeneration, such as diabetes, and a method for increasing ex vivo viability of pancreatic islet cells, comprising contacting said islet cells with a LXR agonist.

Abstract: An additive mixture useful as a flame retardant is described. The mixture is comprised of (i) a poly(bromophenyl)alkane having in the molecule in the range of 13 to 60 carbon atoms and in the range of two to four aryl groups and (ii) a poly(bromophenyl)bromoalkane having in the molecule in the range of 13 to 60 carbon atoms and in the range of two to four aryl groups, said poly(bromophenyl)bromoalkane being in an amount which is greater than 25 wt %, based on the total weight of the additive mixture. A facile process for making the poly(bromophenyl)bromoalkane is also described.

Abstract: The invention relates to bactericidal formulations that come into contact with human body, particularly wash formulations including liquid soaps, comprising perfume ingredients active against gram-negative bacteria. Such compositions contact the target site, for example the skin surface, only for a short time, usually not longer than 30 seconds. Therefore the antibacterial action has to be of the bactericidal type and rapid. Furthermore, the bactericidal activity has to be sufficiently high to ensure an effect even when applied to wet substrates that will dilute the bactericidal formulation.

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: Methods for treating an individual having cancer are provided. The method may include administering a cell migration inhibitor and a chemotherapeutic agent to the individual to inhibit migration of cancer cell. Inhibiting cell migration may increase cell division. In this manner, the cell migration inhibitor and the chemotherapeutic agent in combination may have increased efficacy compared to the chemotherapeutic agent alone due to the increased cell division. The cell migration inhibitor may include any of the inhibitors described herein. For example, the cell migration inhibitor may be an organic molecule having a molecular weight of less than about 700, a monoclonal antibody, or a natural product.

Abstract: A new use for chemicals paradichlorobenzene (10) and naphthalene (20), colorless or white, volatile crystals with a strong coal tar odor, that when positioned in areas where birds gather or roost, such as rooftops, eaves or ledges, diffuses into the surrounding air resulting in birds being deterred from affected area.

Abstract: An additive mixture useful as a flame retardant is described. The mixture is comprised of (i) a poly(bromophenyl)alkane having in the molecule in the range of 13 to 60 carbon atoms and in the range of two to four aryl groups and (ii) a poly(bromophenyl)bromoalkane having in the molecule in the range of 13 to 60 carbon atoms and in the range of two to four aryl groups, said poly(bromophenyl)bromoalkane being in an amount which is greater than 25 wt %, based on the total weight of the additive mixture. A facile process for making the poly(bromophenyl)bromoalkane is also described.

Abstract: Methods of inhibiting angiogenesis, endothelial cell migration or endothelial cell proliferation, by inhibiting NADPH oxidase inhibitors, production of reactive oxygen species, or by inhibition of mRNA induction of superoxide dismutase (e.g., mitochondrial SOD), are described herein.

Abstract: This invention relates to compositions, compounds, and methods for lightening skin, using active compounds having the general structure: wherein each X is halo; m is 1 to 4; each R′ and R″ is independently selected from hydrogen, halo, C1-C10 alkyl, substituted C1-C10 alkyl, substituted or unsubstituted phenyl, substituted or unsubstituted naphthyl, OR, OCOR, OCRROR, COR, CR(OR)OR, CONRR, COOR, CRROR, CN, SR, and NRR; each R is selected from hydrogen, C1-C10 alkyl, substituted C1-C10 alkyl, substituted or unsubstituted phenyl, and substituted or unsubstituted naphthyl; n is 1 to 5; Z is O; in an amount effective to lighten skin; and a pharmaceutically-acceptable carrier therefor.

Abstract: The invention provides low viscosity iodinated aryl compounds, useful as X-ray contrast agents of formula I wherein n is 0 or 1, and where n is 1 each C6R5 moiety may be the same or different; X denotes a bond or a group providing a 1 to 7 atom chain linking two C6R5 moieties or, where n is 0, X denotes a group R; each group R is a hydrogen atom, an iodine atom or a hydrophilic moiety M or M1, two or three non-adjacent R groups in each C6R5 moiety being iodine and at least one R group in each C6R5 moiety being an M or M1 moiety; each M which may be the same or different, is a non-ionic hydrophilic moiety; and each M1 independently represents a —CHOHCON(R1)2 group wherein each R1, which may be the same or different, is a hydrogen atom, an OH group or a C1-6 alkoxy or optionally hydroxylated C1-5 alkyl group; at least one R group in the molecule being an M1 moiety; and isomers thereof.

Abstract: The present invention provides improved dialysis compositions and methods for dialysis comprising utilizing the disclosed AGE inhibitors, together with methods to reduce dialysis-related complications and disorders.

Abstract: A projectile which can be a paint ball, capsule or the like can be used to administer pesticides such as one or more from the group consisting of 4-allylanisole, anisole, allylbenzene, 4-isopropylanisole, p-anisaldehyde, ethylbenzene, cumene, 4-methoxyacetophenone, 4-methylstyrene, 2-propylphenol, phenetole, and toluene, for scolytid infestation or a pheromone or a mixture of the foregroup. Conifers, which are a target for scolytids, are protected by the application of the pesticides and attractants by use of a projectile containing the compounds which explodes or sufficiently disintegrates upon contact with the conifer thereby emitting the compounds.

Abstract: The invention provides low viscosity iodinated aryl compounds, useful as X-ray contrast agents, of formula C6R6 wherein three non-adjacent R groups are iodine and the remaining R groups are non-ionic, hydrophilic moieties, said compound being water soluble at 20° C. to a concentration of at least 350 mgl/ml and which in aqueous solution at 20° C. at a concentration of 350 mgl/ml has a viscosity no greater than 13.8 mPas.

Abstract: The invention provides low viscosity iodinated aryl compounds, useful as X-ray contrast agents, of formula I ##STR1## (wherein n is 0 or 1, and where n is 1 each C.sub.6 R.sub.5 moeity may be the same or different; each group R is a hydrogen atom, an iodine atom or a hydrophilic moiety M or M.sub.1, two or three non-adjacent R groups in each C.sub.6 R.sub.5 moiety being iodine and at least one, and preferably two or three, R groups in each C.sub.6 R.sub.5 moiety being M or M.sub.1 moieties; X denotes a bond or a group providing a 1 to 7 atom chain linking two C.sub.6 R.sub.5 moieties or, where n is 0, X denotes a group R; each M independently is a non-ionic hydrophilic moiety; and each M.sub.1 independently represents a C.sub.1-4 alkyl group substituted by at least one hydroxyl group and optionally linked to the phenyl ring via a carbonyl, sulphone or sulphoxide group, at least one R group being an M.sub.1 moiety; with the proviso that where n is zero either at least one M.sub.

Abstract: The invention provides low viscosity iodinated aryl compounds, useful as X-ray contrast agents, of formula I ##STR1## (wherein n is 0 or 1, and where n is 1 each C.sub.6 R.sub.5 moeity may be the same or different; each group R is a hydrogen atom, an iodine atom or a hydrophilic moiety M or M.sub.1, two or three non-adjacent R groups in each C.sub.6 R.sub.5 moiety being iodine and at least one, and preferably two or three, R groups in each C.sub.6 R.sub.5 moiety being M or M.sub.1 moieties; X denotes a bond or a group providing a 1 to 7 atom chain linking two C.sub.6 R.sub.5 moieties or, where n is 0, X denotes a group R; each M independently is a non-ionic hydrophilic moiety; and each M.sub.1 independently represents a C.sub.1-4 alkyl group substituted by at least one hydroxyl group and optionally linked to the phenyl ring via a carbonyl, sulphone or sulphoxide group, at least one R group being an M.sub.1 moiety; with the proviso that where n is zero either at least one M.sub.

Abstract: The invention relates to hair protective formulations which can be administered to a subject in a manner so as to protect hair follicles against oxidative stress. Additionally, the instant invention relates to a test model for assessing oxidative damage to hair follicles and to determine protection from same.

Abstract: A method for the acceleration of tissue growth using continuous fluorocarbon liquid-based positive pressure is disclosed, whereby significant increase in tissue growth is achieved.

Abstract: This invention provides a nitric oxide synthesis inhibitor composition comprising, as an active ingredient, at least one member of the group consisting of various phenanthrene derivatives, typically represented by the following general formula (1), and salts thereof. ##STR1## The nitric oxide synthesis inhibitor composition of this invention is useful for the prophylaxis and therapy of nitric oxide-associated diseases such as endotoxin shock.

Abstract: Organoselenones of the formulaR.sub.1 --Se(O.sub.2)--(CH.sub.2).sub.n --Xwherein R.sub.1 is selected from the group consisting of aryl, vinyl, acetylenyl, and aralkyl, n is an integer equal to 2 to 6 and X is a leaving group selected from the group consisting of halides, sulfonates and selenones; were surprisingly found to be useful as alkylating agents which possessed a high degree of selectivity for nitrogen nucleophiles without the usual increased preference for sulfur nucleophiles. This property allows the effective use of these compounds as anti-cancer alkylating agents suitable for use in drug-resistant cell lines which display either thiol mediated drug resistance or MER(+)-mediated drug resistance. Two methods of synthesizing these compounds are also provided.

Abstract: A sterilizing agent comprising:(A) a dichlorobenzene; and(B) a dialkyldimethylammonium halide represented by the formula ##STR1## wherein X is bromine or chlorine, and,R.sub.1 and R.sub.2 each independently represent an alkyl group.

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: The invention is directed to synergistic biocidal compositions that combine a copper salt and an organic biocide selected from the group of tribromophenol, its salts and chelates, and sodium-omadine, its salts and chelates. Wood treated with the preservative compositions have improved fungi resistance.

Abstract: Organic compounds for diagnostic imaging which contain at least one aryl group which has been derivatized to contain at least one perfluoro-1H,1H-neopentyl moiety are provided. The perfluoro-1H,1H-neopentyl groups produce a single magnetic resonance to insure a maximum signal to noise ratio. One compound disclosed is 2-O-oleoylglycerol 1,3-bis(7'-{3",5"-di[2"',2"'-di(trifluoromethyl)3"', 3"',3"'-trifluoropropyl]phenyl}heptanoate). In the preferred embodiment, a lipid emulsion is provided as a carrier vehicle to deliver the derivitized analog to a mammalian recipient. Methods to use these compounds in MRI and computerized tomography are provided.

Abstract: This invention relates to structurally novel acyclic tocotrienol analogs, which are useful for cholesterol/lipid lowering in cases of hypercholesterolemia and hyperlipidemia, and for atherosclerosis. Also provided are pharmaceutical compositions and a method of use employing those compositions.

Abstract: The present invention provides a cordless thermal vaporizer of the liquid type wherein the body of the vaporizer has a heater for heating a wick for drawing up a chemical solution from a bottle, and a socket disposed under the heater and removably fittable in the form of a cap to the bottle for attachment thereto. The body is reduced in weight and thereby made attachable to an electric outlet with stability. The solution bottle can be attached directly to the socket of the body and is therefore easy to replace.

Abstract: A composition suitable for topical application to mammalian skin or hair for inducing, maintaining or increasing hair growth comprises:(i) a special protein tyrosine kinase inhibitor; and(ii) a cosmetically acceptable vehicle for the inhibitor.

Abstract: A new use for naphthalene comprising a snake repellant in the form of granules comprising 8% naphthalene, 32% sulfur and 60% montmorillonite. The compound is spread in a strip across an area where snakes are to be repelled and is effective against venomous and non-venomous varieties.

Abstract: Novel 1,3-diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediate by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.

Abstract: An agricultural granule capable of carrying and releasing incorporated biocidal or nutritional agricultural chemicals. The granule is formed by the agitative agglomeration of a plant fiber slurry and resembles a clay granule in all respects except for its chemical inertness.

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: A method of inhibiting cell proliferation in a patient suffering from such disorder comprising administering to said patient an effective amount of a composition comprising, in admixture with a pharmaceutically acceptable carrier, a compound, or a pharmaceutically acceptable salt thereof, which is a substituted styrene compound which can also be a naphthalene, an indane or a benzoxazine; including nitrile and molononitrile compounds, and pharmaceutical compositions comprising, in admixture with a pharmaceutically acceptable carrier, a pharmaceutically-effective amount of such compound.