Abstract: A method of treating a subject with a cytokine-mediated inflammatory disorder comprising administering to the subject an effective amount of a pharmaceutically acceptable cholinesterase inhibitor, provided that the inhibitor is not galantamine.

Abstract: Suggested are agrochemical compositions, comprising (a) biocides, and (b) alkoxylation products of di- and/or oligosaccharide esters.

Abstract: Aqueous gel-free two-phase coacervate compositions including a coacervate phase and an equilibrium water phase, comprising a mixture of: (a) a poorly water-soluble bio-active agent, (b) a tensio-active system consisting of non-ionic tensio-active agents, (c) one or more water-soluble carriers for said poorly water-soluble bio-active agent, said carriers being selected from the group consisting of maltodextrins and polyols, and (d) water. Such coacervate compositions may be dried into solid dosage forms from which rapid release of the bio-active agent can be obtained.

Abstract: The present invention relates to the novel use of Propineb as bird repellent.

Abstract: The invention relates to the compounds suitable for radiolabeling with a chelator free radioisotope and radiolabeled compounds of the general Formula I. Said compounds are ornithine or lysine derivatives.

Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.

Abstract: The invention relates to propionic acids, propionic acid esters, and related compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds for the treatment of various diseases or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).

Abstract: Disclosed are drug delivery systems for the delivery of small molecule and macromolecular drugs. More particularly, disclosed are substituted analogs of 3,6-di(alkyl-4 aminobutyl)-2,5-diketopiperazine (which may also be referred to DKP), their use in the formulation of both small molecule and macromolecular drugs including therapeutic, prophylactic and diagnostic agents, stabilizing agents and systems for their delivery.

Abstract: This invention is directed to methods for preventing, treating, reversing, inhibiting or arresting epilepsy and epileptogenesis in a subject comprising administering to the subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of Formula (I) and Formula (II), or a pharmaceutically acceptable salt or ester thereof: wherein phenyl is substituted at X with one to five halogen atoms selected from the group consisting of fluorine, chlorine, bromine and iodine; and, R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).

Abstract: A synthesis and purification of felbamate, an anticonvulsant, are provided. The product of the synthesis and purification is with high untapped and tapped bulk densities, which increase ease of handling and suitability for use in pharmaceutical formulations. The felbamate may be incorporated into pharmaceutical compositions that can be administered orally for treatment of epilepsy.

Abstract: The present invention relates to the use of a beta-adrenergic receptor agonist as active ingredient for the production of a medicament for use in the treatment of neuropathic pain, in particular neuropathic allodynia, in particular chronic neuropathic allodynia, and more generally for the production of medicaments for relieving pain. The principal field of application of the present invention is the biomedical field, and more specifically the therapeutics field. The present invention aims in particular to provide a medicament which can be used as a substitute for the antidepressants currently used to treat pain. It finds a use in the human and veterinary clinical field.

Abstract: The invention provides methods and compositions for treatment of tumors comprising administering to subject bearing a tumor an effective amount of at least one agent that decreases the [GSH]2/[GSSG] ratio in the malignant cells of said tumor, wherein said at least one agent is administered continuously to said patient for a period of time within the range of from about 15 to about 75 hours.

Abstract: There is provided a method for inhibiting ATF/CREB and cancer cell growth using disulfiram, administered in combination with heavy metals. It was found that disulfiram disrupts transcription factor DNA binding by forming mixed disulfides with thiols within the DNA-binding region, and that this process is facilitated by metal ions. Disulfiram administered to melanoma cells in combination with copper (II) or zinc(II) decreased expression of cyclin A, reduced proliferation in vitro, and inhibited growth of melanoma cells. The combination of oral zinc gluconate and disulfiram at currently approved doses for alcoholism stabilized tumor growth in two of three patients with Stage IV metastatic melanoma, with 12 and 17 month survivals, respectively, to date, and produced a >50% reduction in hepatic metastases in one individual.

Abstract: The invention relates to application of 4,4?-diphenylmethane-bis(methyl)carbamates (DPMC) extracted and isolated from Cortex Mori and preparation of medicine for diabetic nephropathy. The pharmaceutical composition is made up of DPMC as active ingredient and the normal drug carriers, and the weight percentage of active ingredient is 0.1-99.5%. For the remarkable effect of prevention and cure for diabetic nephropathy and convenience for use, it will be a new facultative drug for patients.

Abstract: Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse; and an effective amount of an irritant to impart an irritating sensation to an abuser upon administration of said dosage form after tampering.

Abstract: The present invention provides a pesticide composition comprising a pesticidal active ingredient and a compound represented by chemical formula (I) or chemical formula (II) R—O-(EO)w-(PO)x-(EO)y-(PO)z-H??(I) R—O—(PO)w-(EO)x-(PO)y-(EO)z-H??(II) (wherein, BO represents an ethyleneoxy group, PO represents a propyleneoxy group, R represents an alkyl or alkenyl group having 8 to 20 carbons, w represents on average an integer in the range of 1 to 25, x represents on average an integer in the range of 1 to 25, y represents on average an integer in the range of 1 to 25, and z represents on average an integer in the range of 1 to 25). Further the present invention provides a method for potentiating the efficacy of the pesticidal active ingredient comprising using a compound represented by chemical formula (I) or chemical formula (II) in combination with a pesticidal active ingredient.

Abstract: The present invention provides compositions comprising carisoprodol or pharmaceutically acceptable salts, esters or derivatives thereof. In certain embodiments, the invention provides pharmaceutical compositions comprising the skeletal muscle relaxant carisoprodol and one or more additional active agents, such as one or more nonsteroidal antiinflammatory drugs (NSAIDs). The invention further provides methods of use of such compositions in preventing, alleviating and/or treating musculoskeletal pain, muscle spasms, or other non-malignant painful conditions including methods in which the circulating levels of the active pharmaceutical form of carisoprodol are controlled by use of extended- or controlled-release formulations or by strict control of dosage regimen, so as to reduce the level of somnolence observed with other muscle relaxant compositions.

Abstract: Treatment of mitochondrial related conditions in mammals with antagonists or chelating agents of copper (II), preferably tetramines or penicillamines. These agents affect TGF-beta, Smad 4, collagen IV, cytochrome C oxidase and erectile dysfunction.

Abstract: A novel use of conjugates of psychotropic drugs (e.g., antidepressants or anti-epileptic drugs) and organic acids such as GABA in the treatment of pain is disclosed. A novel GABA conjugate and uses thereof is also disclosed.

Abstract: Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes.

Abstract: Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes.

Abstract: Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes.

Abstract: Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes.

Abstract: Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes.

Abstract: Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes.

Abstract: Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes.

Abstract: Disclosed are pharmaceutical compositions comprising mirtazapine and an anticonvulsant drug. Also disclosed are methods of preventing weight gain associated with the administration of mirtazapine comprising identifying a patient to whom mirtazapine is to be administered and administering to said patient a pharmaceutical composition comprising mirtazapine and an anticonvulsant drug. Further disclosed are methods of increasing the efficacy of mirtazapine comprising identifying a patient to whom mirtazapine is to be administered and administering to said patient a pharmaceutical composition comprising mirtazapine and an anticonvulsant drug.

Abstract: This invention concerns multiple release spacers and spacer systems, which release multiple leaving groups following a single activation. It concerns compounds comprising a specifier linked to two or more of the same or different leaving groups (L in the figure) via a self-eliminating multiple release spacer or spacer system, which compounds upon a single activation step, in particular removal or transformation of the specifier, release at least two leaving groups.

Abstract: A pharmaceutical composition is provided. The pharmaceutical composition includes an amount of disulfuram in unit dosage form which results in a peak serum concentration level which is therapeutically effective in treating an angiogenesis-dependent disorder and can also exhibit minimal or no disulfuram related side effects.

Abstract: Compounds having a general formula X-(A)n-Y, wherein: n varies between 6 and 20; X denotes a hydrogen atom, an RaCO, RaOCO, RaNHCO or RaSO2 group, Ra being an alkyl, alkenyl, alkynyl, aryl, aralkyl, heteroaryl group, the groups being substituted or not, on condition that X is different from H when n is equal to 6; A denotes either a group having formula (I) or (II), wherein Ri is a hydrogen atom, an amino acid side chain, an alkyl, alkenyl, alkynyl, aryl, aralkyl or heteroaryl group, said groups being substituted or not, i being an integer of between 1 and n; Y is an NRbRc, Rb and Rc group having the same meaning as given earlier for Ra. The compounds are used for the preparation of medicaments that are intended to treat bacterial, fungal or cytotoxic diseases and, in particular, fungal infections, such as aspergillosis and candidiasis, and resistant bacterial infections.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: The present invention relates to a novel crystal of (S)-(+)-2-(2-chlorophenyl)-2-hydroxy-ethyl carbamate, pharmaceutical compositions comprising this crystal and, and methods of making and using this crystal.

Abstract: This invention is directed to a method for preventing or treating anxiety disorders comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of Formula (I) and Formula (II): wherein phenyl is substituted at X with one to five halogen atoms selected from the group consisting of fluorine, chlorine, bromine and iodine; and, R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).

Abstract: The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

Abstract: A method of using carisoprodol comprises informing a user that administration of carisoprodol in the presence of food decreases the Cmax for carisoprodol compared to administration in the absence of food. In one embodiment, informing comprises providing printed labeling instructions. Also included are articles comprising a carisoprodol formulation and prescribing information, and methods of manufacturing carisoprodol dosage forms. Included are measures intended to increase the safe use of narrow therapeutic medications with carisoprodol.

Abstract: Pro-drug forms of linear polyamine-bridged platinum compounds and methods for their production and use are provided. The polyamine-bridge portion of the compounds is based on spermine or spermidine, and the central amines of the polyamine-bridge are chemically bonded to labile blocking groups. The presence of the blocking groups serves to minimize the toxicity of the Pt compounds upon administration. Selective removal of the blocking groups and release of the active, unblocked species occurs upon exposure to suitable environmental conditions.

Abstract: The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-active agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS.

Abstract: The present invention provides polymeric conjugates containing positively charged moieties. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.

Abstract: 2-amino-2-phenyl-alkanol ester derivatives of general formula (I) in which: R1 is H, straight or branched 1 to 4C alkyl, straight or branched 2 to 4C alkyl substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino, alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, R2 is a —CO—R radical in which R is H, alkyl, aryl, heterocyclyl, benzyl or heterocyclylmethyl, or R2 is a —CO—Y—R4 radical for which Y is —O—, —S—, —NH—, -Nalk- for which alk is straight or branched (1 to 4C) alkyl, and R4 is alkyl, aryl, aralkyl or heterocyclylalkyl, capable of being substituted by one or more halogen atoms or OH radicals, straight or branched (1 to 4C) alkyl, alkoxy, alkylthio, acylaminoalkylthio, alkoxycarbonyl or acylamino (1 to 4C) straight or branched, or oxo, or capable of being substituted by R5COO— in which R5 is alkyl optionally substituted by benzyloxycarbonylamino, acylamino or by an amino acid residue, or represents an heterocyclyl radical, or R2 is alkyl (2 to 4C) substituted by OH, alk

Abstract: The presently described embodiments are directed to compositions that include one or more carotenoid analogs or derivatives for use in the treatment of a disorder associated with platelet aggregation. Certain embodiments provide for the use of said carotenoid analogs or derivatives in preparing compositions suitable for use in such treatments. Further embodiments provide for pharmaceutical compositions that include one or more carotenoid analogs or derivatives in combination with one or more additional compositions or medicaments suitable for the treatment of a disorder associated with platelet aggregation.

Abstract: A synthesis and purification of felbamate, an anticonvulsant, are provided. The product of the synthesis and purification is with high untapped and tapped bulk densities, which increase ease of handling and suitability for use in pharmaceutical formulations. The felbamate may be incorporated into pharmaceutical compositions that can be administered orally for treatment of epilepsy.

Abstract: This invention is directed to a method for preventing or treating neuropathic pain and cluster and migraine headache-associated pain comprising administering to a subject in need thereof a therapeutically effective amount of a compound of Formula (I): wherein phenyl is substituted at X with one to five halogen atoms independently selected from the group consisting of fluorine, chlorine, bromine and iodine; and; R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).

Abstract: R-enantiomer of Bambuterol, its preparation and therapeutic uses are disclosed. A composition includes R-Bambuterol or its therapeutically acceptable salt. A composition of R-Bambuterol includes at least 80% by weight of the R-enantiomer and not more than 20% by weight of the S-enantiomer based on a total weight of the Bmbuterol. A process includes: (a) asymmetrically reducing a suitably substituted and suitably protected bromoacetophenone compound to a chiral phenyl-bromoethanol comprising a primary bromo group and a secondary hydroxyl group; (b) displacing the bromo group by a suitably substituted and optionally protected primary amine to produce a protected chiral phenylethanolamine, and (c) removing the protecting groups to convert the protected chiral phenylethanolamine to a chiral phenylethanolamine.

Abstract: An alcohol based hand surgical scrub, which includes cationic anti-microbial agent preservatives, cationic polymer film-forming agents and a skin emollient, and provides a long term residual, anti-microbial “invisible glove” on the skin. The composition provides an immediate reduction in bacterial microbes. The polymer system creates an invisible film on the skin following solvent evaporation. This invisible film provides a lasting anti-microbial barrier on the skin which acts to prevent microbial growth.

Abstract: Described herein are cannabidiol prodrugs, methods of making cannabidiol prodrugs, formulations comprising cannabidiol prodrugs and methods of using cannabidiols. One embodiment described herein relates to the transdermal or topical administration of a cannabidiol prodrug for treating and preventing diseases and/or disorders.

Abstract: The present invention provides propofol prodrugs, methods of making propofol prodrugs, pharmaceutical compositions of propofol prodrugs and methods of using propofol prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting.

Abstract: This invention is directed to a method for preventing or treating neurodegenerative disorders comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of Formula (I) and Formula (II): wherein phenyl is substituted at X with one to five halogen atoms selected from the group consisting of fluorine, chlorine, bromine and iodine; and, R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).

Abstract: The present invention is a method for the treatment of depression comprising administering to a subject in need thereof a therapeutically effective amount of one or more carbamate compounds of Formula 1 and/or Formula 2 as herein defined and shown below for the treatment of depression. The present invention is directed to a method for the treatment of depression, which includes mono-therapy and alternatively, co-therapy with at least one additional antidepressant.

Abstract: The present invention relates to benzoyl-substituted serineamides of the formula I in which the variables R1 to R11 are as defined in the description, and to their agriculturally useful salts, to processes and intermediates for their preparation, and to the use of these compounds or of compositions comprising these compounds for controlling unwanted plants.

Abstract: Angiogenesis, tumor growth, and metalloproteinase 2 (MMP2) interaction with integrin-?v?3 are inhibited by an inhibitor compound of formula: wherein G1 and G2 are each independently —NH—C(O)—O—(CH2)v—(C6H4)—X3 ; Y1 and Y2 are each independently —OH or C1-C4 alkoxy; X1 and X2 are each independently halo or C1-C4 alkoxy; X3 is fluoro, nitro, C1-C4 alkyl, C1-C4 alkoxy, or C1-C4 perfluoroalkyl; Z is —C?C—, —C6H4—, cis-CH?CH—, trans-CH?CH—, cis-CH2—CH?CH—CH2—, trans-CH2—CH?CH—CH2—, 1,4-naphthyl, cis-1,3-cyclohexyl, trans-1,3-cyclohexyl, cis-1,4-cyclohexyl, or trans-1,4-cyclohexyl; A is H or a covalent bond; m and n are each 1; t is an integer having a value of 0 or 1; p and r are each 2, and v is 1; with the proviso that when A is H, t is 0, and when A is a covalent bond, t is 1.