Abstract: The present disclosure encompasses crystalline polymorphs of Rigosertib Sodium, processes for preparation thereof, and pharmaceutical compositions thereof.

Abstract: Pharmaceutical compositions of (E)-2,4,6-trimethoxystyryl-3-[(carboxymethyl)amino]-4-methoxybenzylsulphone and pharmaceutically acceptable salts thereof are described as well as methods of their use.

Abstract: An aqueous pharmaceutical solution composition comprising between about 20 mg/ml to about 100 mg/ml of a radioprotective ?,?-unsaturated aryl sulfone, a cosolvent comprising polyethylene glycol (PEG), polypropylene glycol, polyglycerol, DMA, propylene glycol, glycerol, ethanol, sorbitol, isopropyl alcohol, or a combination thereof in an amount between about 25% and about 90% w/v, and a water soluble Vitamin E derivative, wherein the composition has a pH within the range of about 7.0 to about 9.5.

Abstract: The invention relates to compositions including a charged oligo-phenylene ethynylene singlet-oxygen sensitizer and an oppositely-charged surfactant, which show an enhanced biocidal activity relative to a comparable concentration of the oligo-phenylene ethynylene without the oppositely-charged surfactant. The enhancement of biocidal activity is observed with an anionic oligo-phenylene ethynylene in the presence of a cationic surfactant such as TTAB, and with a cationic oligo-phenylene ethynylene in the presence of an anionic surfactant such as SDS.

Abstract: Compounds useful as antiproliferative agents according to formula (I): wherein Ar1, Ar2, Ar3, m and n are as defined herein, salts, antibody conjugates, pharmaceutical compositions, methods of treatment, and synthetic methods are provided.

Abstract: The present invention relates to lipid compounds of the general formula (I): wherein R1 is selected from a C10-C22 alkyl, a C10-C22 alkenyl having 1-6 double bonds, and a C10-C22alkynyl having 1-6 triple bonds; R2 and R3 are the same or different and may be selected from a group of different substituents; Y is selected from sulphur, sulfoxide, and sulfone; and X represents a carboxylic acid or a derivative thereof, a carboxylic ester, a carboxylic anhydride or a carboxamide; or a pharmaceutically acceptable salt, complex or solvate thereof. The invention also relates to pharmaceutical compositions and lipid compositions comprising such compounds, and to such compounds for use as medicaments or for use in therapy, in particular for the treatment of diseases related to the cardiovascular, metabolic and inflammatory disease area.

Abstract: A pharmaceutical composition comprising a docusate; an osmotic laxative; and a benzoate.

Abstract: Broad spectrum disinfecting and microbicidal compositions of biodegradable and environmentally friendly compositions containing esters formed from fatty organic alcohols and fatty carboxylic acids. These compositions display activities against the most resistant microbial forms including bacterial spores. The preparations can be used in health care, food processing, personal care and other industries where the use of harsh oxidizing chemicals is undesirable.

Abstract: Formulations are provided for parenteral administration of (amino substituted (e)-2,6-dialkoxystyryl 4-substituted benzylsulfones and the sodium and potassium salts thereof for the prevention and/or treatment of conditions mediated by abnormal cell proliferation. Composition for parenteral administration are provided which comprise an effective amount of a compound of formula I or a compound of formula IIa and at least about 50% by weight of at least one water soluble polymer selected from the group consisting essentially of polyethylene glycol (PEG), poly-oxyethylene, poly-oxyethylene-poly-oxypropylene copolymers, polyglycerol, polyvinylalcohol, polyvinylpyrrolidone (PVP), polyvinylpyridine N-oxide, copolymer of vinylpyridine N-oxide and vinylpyridine.

Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

Abstract: An aqueous pharmaceutical solution composition comprising between about 20 mg/ml to about 100 mg/ml of a radioprotective ?,?-unsaturated aryl sulfone, a cosolvent comprising polyethylene glycol (PEG), polypropylene glycol, polyglycerol, DMA, propylene glycol, glycerol, ethanol, sorbitol, isopropyl alcohol, or a combination thereof in an amount between about 25% and about 90% w/v, and a water soluble Vitamin E derivative, wherein the composition has a pH within the range of about 7.0 to about 9.5.

Abstract: The present invention is directed to the identification of predictive markers that can be used to determine whether patients with cancer are clinically responsive or non-responsive to a therapeutic regimen prior to treatment. In particular, the present invention is directed to the use of certain individual and/or combinations of predictive markers, wherein the expression of the predictive markers correlates with responsiveness or non-responsiveness to a therapeutic regimen. Thus, by examining the expression levels of individual predictive markers and/or predictive markers comprising a marker set, it is possible to determine whether a therapeutic agent, or combination of agents, will be most likely to reduce the growth rate of tumors in a clinical setting.

Abstract: The invention relates to a new process for the synthesis of high purity 17?-cyanomethyl-17?-hydroxy-estra-4,9-diene-3-one (further on dienogest) of formula (I) from 3-methoxy-17-hydroxy-estra-2,5(10)-diene of formula (V). The invention relates also to the high purity 17?-cyanomethyl-17?-hydroxy-estra-4,9-diene-3-one and pharmaceutical compositions containing that as active ingredient. The pharmaceutical compositions according to this invention contain high purity dienogest of formula (I) in which the total amount of impurities is less than 0.1%, while the amount of 4-bromo-dienogest is under the detection limit (0.02%) as active ingredient or at least one of the active ingredients and auxiliary materials, which are commonly used in practice, such as carriers, excipients or diluents.

Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

Abstract: There is provided a halogen-containing organosulfur compound having an excellent controlling effect on arthropod pests represented by the formula (I): wherein, m represents 0, 1 or 2, n represents 0, 1 or 2, A represents optionally substituted C3-C7 cycloalkyl or optionally substituted C5-C7 cycloalkenyl group, Q represents a C1-C5 haloalkyl group containing at least one fluorine atom, or a fluorine atom, R1 and R3 independently represent optionally substituted C1-C4 chain hydrocarbon, halogen or hydrogen, R2 and R4 independently represent optionally substituted C1-C4 chain hydrocarbon, —C(?G)R5, cyano, halogen or hydrogen, G represents oxygen or sulfur, and R5 represents optionally substituted C1-C4 alkyl, hydroxyl, optionally substituted C1-C4 alkoxy, optionally substituted C3-C6 alkenyloxy, optionally substituted C3-C6 alkynyloxy, amino, optionally substituted C1-C4 alkylamino, optionally substituted di(C1-C4 alkyl)amino, C2-C5 cyclic amino or hydrogen.

Abstract: Methods and compositions are provided for treating proliferative disorders, wherein the composition comprises at least one compound according to Formula I: wherein R1 is selected from the group consisting of —OH, —NH2, —NH—CH2—CO2H, —NH—CH(CH3)—CO2H, and —NH—C(CH3)2—CO2H, or a pharmaceutically acceptable salt of such a compound; and an anthracycline, e.g. doxorubicin, or a pharmaceutically acceptable salt thereof, or a platin, e.g. oxaliplatin, or a pharmaceutically acceptable salt thereof.

Abstract: Formulations are provided for parenteral administration of (amino substituted (e)-2,6-dialkoxystyryl 4-substituted benzylsulfones and the sodium and potassium salts thereof for the prevention and/or treatment of conditions mediated by abnormal cell proliferation. Composition for parenteral administration are provided which comprise an effective amount of compound of formula I or a compound of formula IIa and at least about 50% by weight of at least one water soluble polymer selected from the group consisting essentially of polyethylene glycol (PEG), poly-oxyethylene, poly-oxyethylene-poly-oxypropylene copolymers, polyglycerol, polyvinylalcohol, polyvinylpyrrolidone (PVP), polyvinylpyridine N-oxide, copolymer of vinylpyridine N-oxide and vinylpyridine.

Abstract: Modafinil is selectively delivered to the brain, minimizing delivery to the blood, of a person in need thereof by administering to the person a therapeutically-effective dosage of modafinil, wherein the dosage is less than 1 mg, formulated in a lipid microemulsion (LME) and selectively delivered to the upper third of the nasal cavity. The method may be implemented with an intranasal pharmaceutical delivery device loaded with a modafinil composition and adapted to deliver the dosage to the upper third of the nasal cavity.

Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that upregulate the expression of Apolipoprotein A-I (ApoA-I). The disclosed compositions and methods can be used for treatment and prevention of cardiovascular disease and related disease states, including cholesterol or lipid related disorders, such as, e.g., atherosclerosis.

Abstract: A pharmaceutical composition is provided for administration prior to or after exposure to ionizing radiation for reducing toxic effects of the radiation in a subject. An effective amount of the pharmaceutical composition provided comprising an effective amount of at least one radioprotective ?, ? unsaturated aryl sulfone, and at least one component selected from the group consisting of a) at least one water soluble polymer in an amount between about 0.5% and about 90% w/v, b) at least one chemically modified cyclodextrin in an amount between about 20% and about 60% w/v, and c) DMA in an amount between about 10% and about 50% w/v.

Abstract: Embodiments of the invention relate to methods of reducing weight in mammals and for the prophylaxis or treatment of obesity comprising administration of C2-substituted indan-1-ol systems and their physiologically acceptable salts and physiologically functional derivatives. Compounds for use in the methods of the embodiments of the invention include compounds of the formula (I) in which the radicals are as defined, and their physiologically acceptable salts.

Abstract: Inhibitors of the enzyme prenylated methylated protein methyl esterase (PMPMEase), the last step in the prenylation process for many eukaryotic proteins, having the general structure R1—X-A-B(R2)—Y or R1—X-A(R2)—B—Y, where R1 is preferably a polyisoprenyl group, X is a linking group, Y is a group that promotes affinity interactions to the active site of PMPMEase and imparts hydrolysis resistance to the inhibitor, A and B are bridge atoms, and R2 is a characteristic-providing substituent.

Abstract: Compounds useful as antiproliferative agents according to formula (I): wherein Ar1, Ar2, Ar3, m and n are as defined herein, salts, antibody conjugates, pharmaceutical compositions, methods of treatment, and synthetic methods are provided.

Abstract: ?,?-Unsaturated sulfones, sulfoxides and sulfonamides according to Formula I: wherein Ar1, Ar2, X, n, * and R are as defined herein are useful for the treatment of proliferative disorders which are resistant to treatment by ATP-competitive kinase inhibitors.

Abstract: Solution and suspension formulations are provided for administration prior to or after exposure to ionizing radiation for reducing toxic effects of the radiation in a subject which comprises an effective amount of at least one radioprotective ?,? unsaturated aryl sulfone wherein the composition has a pH within the range of about 8 to about 9.

Abstract: Pre-treatment with ?,? unsaturated aryl sulfones protects normal cells from the cytotoxic side effects of two classes of anticancer chemotherapeutics. Administration of a cytoprotective sulfone compound to a patient prior to anticancer chemotherapy with a mitotic phase cell cycle inhibitor or topoisomerase inhibitor reduces or eliminates the cytotoxic side effects of the anticancer agent on normal cells. The cytoprotective effect of the ?,? unsaturated aryl sulfone allows the clinician to safely increasing the dosage of the anticancer chemotherapeutic.

Abstract: A method of treating a poison-caused pathology in an individual subject is described which includes administering a pharmaceutical composition including a therapeutically effective amount of a chloride current modulator, a therapeutically effective amount of an exogenous oxygen carrier, or a combination of a therapeutically effective amount of a chloride current modulator and a therapeutically effective amount of an exogenous oxygen carrier, to an individual subject exposed to a poison. Optionally, an inventive method further includes administering a therapeutic agent to inhibit poison-caused pathology. A composition according to the invention is described which includes a therapeutically effective amount of a chloride current modulator, a therapeutically effective amount of an exogenous oxygen carrier, or a combination of a therapeutically effective amount of a chloride current modulator and a therapeutically effective amount of an exogenous oxygen carrier.

Abstract: A method using quinazoline derivatives, celastrol, cape, BAY 11-7082, rocaglamide, and 7-Methoxy-5,11,12-trihydroxy-coumestan is administered to a mammal for the treatment and prevention of viral diseases and cancers. The chemical compounds are targeted to inhibit NF-?B transcriptional activity. These treatments for viral diseases, especially for infection caused by HIV, and cancers may be accomplished utilizing quinazoline derivatives, celastrol, cape, BAY 11-7082, rocaglamide, 7-Methoxy-5,11,12-trihydroxy-coumestan, and compounds similar to them alone or in combination with prior art other therapy.

Abstract: One aspect of the present invention is directed to a composition. The composition includes a dispersion inducer comprising: H3C—(CH2)n—CHmCHmR, where is a single or double carbon-carbon bond, m is 1 or 2, n is 2 to 15, and R is a carboxylic acid, a salt, an ester, or an amide, where the ester or amide is an isostere or biostere of the carboxylic acid. The composition additionally contains an additive component selected from one or more of the group consisting of biocides, surfactants, antibiotics, antiseptics, detergents, chelating agents, virulence factor inhibitors, gels, polymers, pastes, edible products, and chewable products. The composition is formulated so that when it is contacted with a biofilm produced by a microorganism, where the biofilm comprises a matrix and microorganism on a surface, the dispersion inducer selectively acts on the microorganism and has a suitable biological response without a required direct effect on the matrix to disperse the biofilm.

Abstract: Compounds of formula I: are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.

Abstract: The present invention relates to compounds for the inhibition of pyruvate kinase and ATP production which are capable of inhibiting cancer cells proliferation.

Abstract: The use is described of merocyanine derivatives of formula (1), wherein R1 and R2 are each independently of the other hydrogen; C1-C22alkyl; cyclo-C3C8alkyl; or unsubstituted or C1-C5alkyl- or C1-C5alkoxy-substituted C6-C20aryl; orl; or R1 and R2 together with the nitrogen atom linking them form a —(CH2)m— ring which is uninterrupted or, interrupted by —O— or by —NH—; R3 is a cyano group; —COOR5; —CONHR5; —COR5; or —SO2R5; R4 is a cyano group; —COOR6; —CONHR6; —COR6; or —SO2R6; R5 and R6 are each independently of the other C1-C22alkyl; or unsubstituted or C1-C5alkyl substituted C6-C20aryl; or R3 and R4 together or R5 and R6 together form in a 5- to 7-membered, monocyclic, carbocyclic or heterocyclic ring; Z1, and Z2 are each independently of the other a —(CH2)n— group which is uninterrupted or interrupted by —O—, —S—, or by —NR7—, and/or is unsubstituted or substituted by C1-C5alkyl; R7 is (ClC5alkyl; 1 is from 1 to 4; m is from 1 to 7; n is from 1 to 4; when n=2, R1, R5 or R6 is a bivalent alkyl group; or R1

Abstract: Method and article for providing a rapid, broad spectrum bacterial control, and a rapid and persistent antiviral control on an inanimate surface is disclosed. In the method, a compound or composition capable of lowering surface pH to less than about 4 is applied to the surface, and preferably is allowed to remain on the surface, and the nonvolatile components of the composition can form a barrier film or layer on a treated surface.

Abstract: Biodegradable compositions for cleaning and disinfecting nasal tract and sinus cavity using food additive ingredients or ingredients that are safe.

Abstract: Compounds of formula I: are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.

Abstract: A wood treatment composition having a synergistic combination of fungicides which may include two or more compounds. These combinations are shown to be especially effective in providing resistance to decay, mold and mildew when wood is treated with these combinations. Also provided is wood treated by these combinations, and a method of treatment for composite wood.

Abstract: (E)-styryl benzylsulfones of formula I are useful as anticancer agents: wherein R1, R2, R3, and R4 are as defined herein.

Abstract: (E)-Styryl benzylsulfones useful as antiproliferative agents, including, for example, anticancer agents, are provided according to formula I: wherein: R1 is selected from the group consisting of halogen, C1–C6 alkoxy, nitro, phosphonato, amino, sulfamyl, carboxy, acetoxy and dimethylamino (C2–C6 alkoxy); and R2 and R3 are independently selected from the group consisting of halogen, C1–C6 alkoxy, C1–C6 alkyl, nitro, cyano, hydroxyl, phosphonato, amino, sulfamyl, carboxy, acetoxy, and dimethylamino (C2–C6 alkoxy); provided: R1 may not be halogen when R2 and R3 are both halogen; R2 may not be 2-halogen when R3 is 4-halogen; or a pharmaceutically acceptable salt thereof; or formula II: wherein: R4 is selected from the group consisting of C1–C6 alkoxy, phosphonato, amino, sulfamyl, carboxy, acetoxy and dimethylamino (C2–C6 alkoxy); R6 is selected from the group consisting of nitro, hydrogen, phosphonato, amino, sulfamyl, carboxy, acetoxy and dimethylamino (C2–C6 alkoxy); and R7 is selected from the group consistin

Abstract: A method for reducing bacterial and fungal soil pathogens which comprises applying to a soil a chemically effective amount of a lignosulfonate, the amount preferably being between 0.05% and about 5% on a volume/weight basis. The method is effective in controlling a number of soil pathogens and can be used to treat the soil for diseases such as potato scab disease.

Abstract: (E)-styryl benzylsulfones of formula I are useful as anticancer agents: 1

Abstract: Pre-treatment with &agr;,&bgr; unsaturated aryl sulfones protects normal cells from the cytotoxic side effects of two classes of anticancer chemotherapeutics. Administration of a cytoprotective sulfone compound to a patient prior to anticancer chemotherapy with a mitotic phase cell cycle inhibitor or topoisomerase inhibitor reduces or eliminates the cytotoxic side effects of the anticancer agent on normal cells. The cytoprotective effect of the &agr;,&bgr; unsaturated aryl sulfone allows the clinician to safely increasing the dosage of the anticancer chemotherapeutic.

Abstract: Pre-treatment with &agr;,&bgr; unsaturated aryl sulfones protects normal cells from the cytotoxic side effects of two classes of anticancer chemotherapeutics. Administration of a cytoprotective sulfone compound to a patient prior to anticancer chemotherapy with a mitotic phase cell cycle inhibitor or topoisomerase inhibitor reduces or eliminates the cytotoxic side effects of the anticancer agent on normal cells. The cytoprotective effect of the &agr;,&bgr; unsaturated aryl sulfone allows the clinician to safely increasing the dosage of the anticancer chemotherapeutic.

Abstract: (E)-styryl benzylsulfones of formula I are useful as anticancer agents: wherein R1, R2, R3, and R4 are independently selected from the group consisting of hydrogen, fluoro, chloro, iodo, bromo, C1-C6 alkyl, C1-C4 alkoxy, nitro, cyano and trifluoromethyl, with the proviso that (a) R1, R2, and R3 not all hydrogen when R4 is 2-chloro or 4-chloro; (b) when R1 and R3 are hydrogen and R2 is 4-bromo or 4-chloro, then R4 may not be 4-chloro, 4-fluoro or 4-bromo; (c) when R1 and R3 are hydrogen and R2 is 4-fluoro, then R4 may not be 4-fluoro or 4-bromo; (d) when R1 is hydrogen, and R4 is 2-fluoro, the R2 and R3 may not be 4-fluoro; and (e) when R1 is hydrogen and R3 is 4-hydrogen, 4-chloro, 4-bromo, 4-methyl or 4-methoxy, and R4 is 2-hydrogen, 2-chloro, or 2-fluoro; then R2 may not be 4-hydrogen, 4-chloro, 4-fluoro, or 4-bromo.

Abstract: The invention relates to novel phenoxyphenyl alkanesulphonates, processes for their preparation, their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment of states of pain and neurodegenerative disorders.

Abstract: The mastitis control teat dip composition of the invention provides rapid initial kill, a useful highly pseudoplastic rheology, a barrier/film-forming capacity, a unique antimicrobial composition that is stable over an extended period of time, and unexpected long term microbial control when compared to the prior art materials disclosed in patents and used in the marketplace. The compositions of the invention are made by combining an aqueous thickened liquid composition containing the organic components which can be combined with a simple aqueous solution of a salt of chlorous acid, preferably an alkali metal chlorite. The materials can be combined, blended into a smooth viscous material and can be immediately contacted with the target animals. The compositions of the invention provide rapid initial kill, consistent long term kill and chemical and rheological stability.

Abstract: The mastitis control teat dip composition having a visible indicator aspect of the invention provides a softening, soothing, smoothing, relaxing property, a rapid initial kill, a useful highly pseudoplastic rheology, a barrier/film-forming capacity, a unique antimicrobial composition that is stable over an extended period of time, and unexpected long term microbial control when compared to the prior art materials disclosed in patents and used in the marketplace. The indicator aspect provides ease of visually detecting the material on the animal skin and can indicate efficacy of the material. The compositions of the invention are made by combining an aqueous liquid composition containing the visual indicator combined with the organic components which can be combined with a simple aqueous solution of a salt of chlorous acid, preferably an alkali metal chlorite.

Abstract: Pre-treatment with &agr;,&bgr; unsaturated aryl sulfones protects normal cells from the toxic side effects of ionizing radiation. Administration of a radioprotective &agr;,&bgr; unsaturated aryl sulfone compound to a patient prior to anticancer radiotherapy reduces the cytotoxic side effects of the radiation on normal cells. The radioprotective effect of the &agr;,&bgr; unsaturated aryl sulfone allows the clinician to safely increase the dosage of anticancer radiation. In some instances, amelioration of toxicity following inadvertent radiation exposure may be mitigated with administration of &agr;,&bgr; unsaturated arylsulfone.

Abstract: Provided are the compound (E)-4-carboxystyryl-4-chlorobenzyl sulfone, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof.

Abstract: This invention relates to novel compounds, capable of potentiating the efficacy of therapeutically active compounds, for example cytotoxic compounds used in the treatment of cancer. The novel compounds have been shown to increase the pharmacological activity of a conventional paclitaxel formulation and to make it possible to manufacture a new formulation of paclitaxel, exhibiting improved solubility, improved storage properties, and increased therapeutic efficacy as shown in the enclosed examples.

Abstract: The mastitis control teat dip composition having a visible indicator aspect of the invention provides a softening, soothing, smoothing, relaxing property, a rapid initial kill, a useful highly pseudoplastic rheology, a barrier/film-forming capacity, a unique antimicrobial composition that is stable over an extended period of time, and unexpected long term microbial control when compared to the prior art materials disclosed in patents and used in the marketplace. The indicator aspect provides ease of visually detecting the material on the animal skin and can indicate efficacy of the material. The compositions of the invention are made by combining an aqueous liquid composition containing the visual indicator combined with the organic components which can be combined with a simple aqueous solution of a salt of chlorous acid, preferably an alkali metal chlorite.