Abstract: A pharmaceutical composition and method for modifying levels of cholesterol is described. Implementations of a pharmaceutical composition may comprise milk thistle and one of niacin, policosanol, and both niacin and policosanol. Implementations of a pharmaceutical composition may be administered using a method for reducing total cholesterol, LDL cholesterol, and triglycerides and increasing HDL cholesterol levels in a human or animal. The method may include the step of administering a pharmaceutically effective amount of a pharmaceutical composition that includes milk thistle and one of niacin, policosanol, and both niacin and policosanol to a human or animal.

Abstract: Disclosed relates to a novel chalcone derivative, pharmaceutically acceptable salt thereof, a method for preparing the same and uses thereof, the chalcone derivative being readily obtained through the steps of: reacting aminoacetophenone with sulfonylchloride under the presence of an appropriate salt; and reacting the compound prepared in the above step with hydroxybenzaldehide under the presence of an appropriate catalyst. The chalcone derivative of formula 1 in accordance with the present invention having strong enzyme inhibitory activities for glycosidase can be effectively used in preventing and treating various diseases induced by glycosidase, and the chalcone derivative of the invention having tyrosinase and melanin synthesis inhibitory activities can be effectively used as a skin-whitening compound.

Abstract: The use of benzophenones of the formula I in which R is hydrogen or C1-C4-alkyl and Hal is fluorine, chlorine or bromine for controlling Pseudocercosporella herpotrichoides in crop plants is described.

Abstract: The present invention relates to, inter alia, the use of a compound capable of inhibiting 4-hydroxyphenylpyruvate dioxygenase (HPPD) in an animal in the manufacture of a medicament for use in the treatment and/or prevention of depression. The invention also provides for the use of a compound capable of inhibiting HPPD in an animal in the manufacture of a medicament for use in the treatment of the withdrawal symptoms associated with an addictive drug which causes dopamine dependant associative learning disorders in said animal. In a particular embodiment said HPPD inhibitor is selected from the group consisting of the compound depicted as compound 1; 2; and 3.22.

Abstract: A bacterial autoinducer, CAI-1, was purified and its structure identified. Methods for synthesis of the autoinducer and its analogues were elucidated. Methods of using the autoinducer or its analogues for treating bacterial pathogenicity and bio film formation are described. Methods for prevention and treatment of cholera are described. Synthetic (S)-3-hydroxytridecan-4-one functions as well as natural CAI-1 in repressing production of the virulence factor toxin co-regulated pilus (TCP). Strategies are described to manipulate bacterial quorum sensing in the clinical arena.

Abstract: This invention relates to ?-hydroxyketones and ?-alkoxyketones of formula (I), to their use as estrogen receptor modulators, and to methods for their preparation.

Abstract: Methods of inhibiting phagolysosomal fusion in patients infected with a microorganism involve the administration of a 4-hydroxyphenylpyruvate dioxygenase (HPPD)-inhibiting compound, such as 2-(2-nitro-4-trifluoromethylbenzoyl)-1,3-cyclohexanedione (NTBC) to the patient. A HPPD-inhibiting compound administered in an amount effective to enhance phagolysosomal fusion in the macrophages or neutrophils of the patient reduces or treats the infection. Methods for treating bacterial infections by administering a HPPD-inhibiting compound and reducing the production of pyomelanin or melanin in microorganisms are disclosed.

Abstract: The invention relates to pharmaceutical formulations, and more particularly to formulations containing cannabinoids for administration via a pump action spray. In particular, the invention relates to pharmaceutical formulations, for use in administration of lipophilic medicaments via mucosal surfaces, comprising: at least one lipophilic medicament, a solvent and a co-solvent, wherein the total amount of solvent and co-solvent present in the formulation is greater than 55% wt/wt of the formulation and the formulation is absent of a self emulsifying agent and/or a fluorinated propellant.

Abstract: The present invention provides methods of treating chronic pain in a mammal by administering to the mammal an effective amount of a selective persistent sodium channel antagonist that has at least 20-fold selectivity for persistent sodium current relative to transient sodium current.

Abstract: The invention relates to compounds of formula (I) wherein A1 is C(R1R2)p; A2 is C(R6R7)q; p is 1 or 2; q is 1 or 2; each of R1, R2, R3, R4, R5, R6, R7 and R8 which may be the same or different, represents hydrogen, methyl or ethyl and R9 is C1-C4alkyl; R10 is hydrogen, halogen, C1-C3alkyl or C1-C3-haloalkyl, and agronomically acceptable salts/isomers/enantiomers/tautomers/N-oxides of those compounds.

Abstract: Methods of preventing and/or treating at least one symptom of Restless Leg Syndrome (RLS) and its related disorders, including disorders such as periodic limb movements in sleep (PLMS) and periodic limb movement disorder (PLMD), are disclosed. The methods comprise identifying a host, afflicted with Restless Leg Syndrome (RLS) and its related disorders; and administering to the host a pharmaceutically effective amount of a 4-hydroxyphenylpyruvate dioxygenase. Also provided are methods and compositions for treating/preventing sleep disorders, and methods and compositions for improving sleep quantity and adequacy.

Abstract: Antimitotic agents comprising a modified chalcone or modified chalcone derivative are disclosed. The modified chalcone or modified chalcone derivative compounds are of the general formula CHAL-LIN—COV, wherein CHAL is a chalcone or chalcone derivative portion, LIN is an optional linker portion, and COV is a covalent bonding portion (e.g., an ?,?-unsaturated thiol ester group). The modified chalcone or modified chalcone derivative compounds provide an improved method of interference with tubulin polymerization, for example by covalent (and essentially irreversible) bonding between tubulin and the covalent bonding portion, potentially resulting in a decrease in tumor size and/or disappearance of the cancer, to the benefit of cancer patients.

Abstract: The present invention relates to a controlled release granule technology, methods of preparing such a granule and methods for using the granule in the control of pests.

Abstract: ?-Aminoamide derivatives useful as antimigraine agents, particularly for the treatment of head pain conditions such as migraine, cluster headache or other severe headache, are disclosed. The antimigraine agents of the invention are able to reduce or even stop the pain deriving from such conditions without, virtually, any side effects.

Abstract: The present invention provides methods of treating neurological disorders in a mammal by administering to the mammal an effective amount of a selective persistent sodium channel antagonist that has at least 20-fold selectivity for persistent sodium current relative to transient sodium current.

Abstract: The present invention relates to, inter alia, the use of 2-(2-Nitro-4-Trifluoromethylbenzoyl)-1,3-Cyclohexanedione (compound 2) in the treatment of a neurodegenerative disease, such as Parkinson's disease. The invention also relates to the use of the compound depicted as compound 2 or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in the treatment of a neurodegenerative disease such as Parkinson's disease.

Abstract: Termite bait matrix containing cellulose, calco oil blue V (solvent blue 58 or 9,10-anthracenedione, 1,4-bis[(2-ethylhexyl)amino]), and optionally a termite toxicant (e.g., chitin synthesis inhibitor). Methods of monitoring termite activity in a region involving placing a termite bait matrix in the region and assessing the presence of termites at the site of the termite matrix, the termite bait matrix contains cellulose and 9,10-anthracenedione, 1,4-bis[(2-ethylhexyl)amino]. Methods of killing termites, involving placing a termite bait matrix in a termite habitat and allowing termites to feed on the bait matrix, the termite bait matrix contains cellulose, 9,10-anthracenedione, 1,4-bis[(2-ethylhexyl)amino], and a termite toxicant (e.g., chitin synthesis inhibitor).

Abstract: The present invention relates to a pharmaceutical composition of practically water insoluble or low water soluble compounds containing catechol moiety by enhancing the solubility of such compounds using one or more alkalising agent and optionally adding one or more pharmaceutically acceptable excipient.

Abstract: Disclosed herein is a method for treating a patient with Quazepam that reduces the risk of an adverse interaction between the Quazepam and drug that is a substrate of the cytochrome P450 enzyme isoform 2B6 (CYP2B6 substrate drug), e.g., Bupropion. The method includes determining if the patient to be treated with Quazepam is being treated with a CYP2B6 substrate drug, and prescribing or treating the patient with Quazepam based on the determination.

Abstract: Disclosed relates to a novel chalcone derivative, pharmaceutically acceptable salt thereof, a method for preparing the same and uses thereof, the chalcone derivative being readily obtained through the steps of: reacting aminoacetophenone with sulfonylchloride under the presence of an appropriate salt; and reacting the compound prepared in the above step with hydroxybenzaldehide under the presence of an appropriate catalyst. The chalcone derivative of formula 1 in accordance with the present invention having strong enzyme inhibitory activities for glycosidase can be effectively used in preventing and treating various diseases induced by glycosidase, and the chalcone derivative of the invention having tyrosinase and melanin synthesis inhibitory activities can be effectively used as a skin-whitening compound.

Abstract: A method for treating skin, reducing oxidative damage to a skin cell, reducing lipoxygenase (LO) activity in a skin cell, reducing cyclooxygenase (COX) activity in a skin cell, reducing tumor necrosis factor alpha (TNF-?) in a skin cell, or reduction matrix metalloproteinase enzyme activity in a skin cell comprising contacting skin or a skin cell with an aromatic skin-active ingredient.

Abstract: The present invention provides pharmaceutical compositions comprising droxidopa alone, or in combination with one or more further active ingredients, for the treatment of conditions, such as mood disorders, sleep disorders, or attention deficit disorders. In certain embodiments, the compositions useful in the methods of the invention comprise droxidopa and a compound selected from the group consisting of DOPA decarboxylase inhibiting compounds, catechol-O-methyltransferase inhibiting compounds, cholinesterase inhibiting compounds, monoamine oxidase inhibiting compounds, norepinephrine reuptake inhibiting compounds, selective serotonin reuptake inhibiting compounds, tricyclic antidepressant compounds, serotonin norepinephrine reuptake inhibiting compounds, norepinephrine dopamine reuptake inhibiting compound, noradrenergic and specific serotonergic antidepressants, and combinations thereof.

Abstract: The invention provides a method for the treatment of certain psychiatric disorders using entacapone, tolcapone and other COMT inhibitor drugs or MB-COMT inhibitor compounds. The method is effective in particular for improving positive and negative symptoms of Schizophrenia (SCZ), major depression, the depressive phase of Bipolar Disorder (BD) and substance dependency. The method can also be used as a treatment to combat cravings associated with abuse of alcohol, opiates, cocaine, marijuana, amphetamines and Tobacco addiction. In addition to these diseases it is useful for the treatment of ADD/ADHD, cognitive enhancement in head injuries and dementias.

Abstract: Provided herein is a method of protecting a neuron from dysfunction induced by an HIV neurotoxin, comprising contacting the cell with a therapeutically effective dose of a dopamine D1 receptor agonist. Also provided is a method of treating or preventing HIV-1 associated dementia (HAD) in a subject in need of such treatment or prevention, comprising administering to the subject a therapeutically effective dose of a dopamine D1 receptor agonist and estrogenic compound.

Abstract: The invention provides para substituted dialkylphenol derivatives of propofol. The invention further provides pharmaceutical compositions comprising such analogs, methods for preparing such analogs, and methods of using such analogs to induce general anesthesia, sedation, and/or hypnotic or sleep effects in a patient.

Abstract: By disrupting a natural process used by developing mammalian brains to prune and delete surplus neurons, surgical anesthetics and other drugs that suppress brain activity in fetuses and infants can trigger permanent pathological brain damage. That type of damage can be prevented by drug interventions that block one or more “upstream” events that otherwise would lead to the release of “Cytochrome C”, a messenger molecule that triggers apoptosis (programmed cell death) among immature neurons. Lithium is a potent protective agent that can be coadministered along with ketamine or other NMDA-acting or GABA-acting anesthetics and anticonvulsants. Xenon gas triggers only mild damage, and can enable improved anesthesia when combined with other drugs. Other protective drugs (also called safener drugs), and treatments that can prevent or minimize fetal alcohol syndrome, also are disclosed.

Abstract: The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.

Abstract: The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.

Abstract: This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.

Abstract: The present invention relates to the use of compounds and composition of compounds that modulate norepinephrine levels for the prevention and treatment of vasomotor symptoms, such as hot flush, caused by, inter alia, thermoregulatory dysfunctions.

Abstract: N-(Sulfonyloxybiarylmethyl) aminocyclopropanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.

Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.

Abstract: The present invention provides methods of treating or preventing vascular diseases caused by nitric oxide (NO) insufficiency. The methods encompass administering a composition comprising an antioxidant, a compound to treat cardiovascular diseases, a nitrosated compound, a compound that donates, transfers or relases NO, or is a NO synthase substrate, or endogenously stimulates NO synthesis, or stimulates levels of endothelium derived relaxing factor. In the said composition, a hydralazine compound may be an antioxidant, isosorbide mono-or dinitrate may be the compound to donate, transfer, release, or stimulate endogenous NO synthesis. The isorsorbide may also elevate endogenous levels of endotherlium-derived relaxing factor, or be a NO synthase substrate and angiotensin enzyme inhibitor may be nitrosated compound.

Abstract: The present invention provides 4-substituted-2-azetidinone compounds, bicyclic 2-5-diketopiperazine compounds, and pharmaceutical compositions thereof that are potent, safe and effective neuroprotective agents. Due to their strong central nervous system (CNS) activity, the compounds can be used to enhance memory and to treat a variety of neurological disorders. The compounds are particularly useful for treating neurological disorders caused by, or associated with, CNS trauma.

Abstract: The present invention relates to novel hydroxyethylene compounds having Asp2 (?-secretase. BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated ?-amyloid levels or ?-amyloid deposits, particularly Alzheimer's disease.

Abstract: The use of benzazepin-N-acetic acid derivatives which contain an oxo group in the a position to the nitrogen atom and are substituted in the 3 position by a 1-(carboxyalkyl)-cyclopentyl-carbonyl-amino radical, and of their salts and biolabile esters, for the prophylaxis and/or treatment of heart damage caused by cardiotoxic doses of medicaments or chemicals, in larger mammals and in particular humans. The invention is particularly applicable to the prophylaxis and/or treatment of heart damage, in particular to the myocardium, which may occur during cytostatic chemotherapy. The invention also includes the use of the afore-mentioned benzazepin-N-acetic acid derivatives for adjuvant treatment in therapies in which medicaments having oxidative-toxic side-effects are used, and the preparation of medicaments suitable for this prophylaxis and/or treatment or adjuvant treatment.

Abstract: A method for applying a topical anesthetic to an area of skin comprising the steps of a) incorporating an anesthetic in a lipophilic base into a volatile solvent, to form a homogeneous solution; b) applying the homogeneous solution into the area of skin to be treated; and c) evaporating the volatile solvent from the homogeneous solution; wherein the volatile solvent is present in the formulation in amounts between 40-80%; and wherein said topical anesthetic rapidly penetrates the skin surface at said skin, leaving a cooling sensation on the skin. The topical anesthetic formulation contains a penetrating enhancer carrier that markedly enhances the delivery of the anesthetic across human skin without altering the acceptable delivery rate of the anesthetic that needs to be delivered through the skin and leaves a cooling sensation on the skin.

Abstract: The present invention concerns novel mediators of the activity of picornavirus 3C protease and the modulation of the activity of other similar proteins. The modulators may be used in pharmaceutical compositions either for inhibition of 3C protease (for example in viral infections) or for the enhancement of the activity of proteins similar to the 3C protease such as Apopain (for induction of apoptosis).

Abstract: The two carbohydrate mixture of this invention utilizes a source of fructose in combination with at least one readily digestible glucose polymer source. The addition of the fructose significantly decreases the glycemic response when compared to the digestible glucose polymer alone. Additional components may be added to the simple two component carbohydrate mixture to form a carbohydrate system suitable for incorporation into an enteral nutritional. This carbohydrate system optionally incorporates nonabsorbent carbohydrates, dietary fiber and indigestible oligosaccharides. The present invention is also directed to an enteral nutritional which incorporates the two component carbohydrate mixture and less than 37% of calories from fat. Additionally, the invention is directed to a method of delivering nutrients to a person with diabetes by feeding the enteral nutritional.

Abstract: The invention relates to a novel fungicidal composition comprising a fungicidally acceptable carrier and/or surface active agent together with, and synergistically effective amounts of (a) at least one benzophenone of formula I wherein R1, R2, R3, R4, R5, R6, R7, m and n have the meaning given; at least one fungicidal active ingredient selected from the following groups (A), (B), (C), (D) and (E): (A) an ergosterol biosynthesis inhibitor; (B) a strobilurine derivative, (C) a melanin biosynthesis inhibitor; (D) a compound selected from the group consisting of acibenzolar, benomyl, captan, carboxin, chlorothalonil, copper, cyprodinil, dinocap, dithianon, dimethomorph, dodine, ethirimol, famoxadone, fenpiclonil, fluazinam, mancozeb, metalaxyl, pyrifenox, sulfur, vinclozolin and (E) an azolopyrimidine of formula II in which R8, R9, R10, R11, A, L and p have the meaning given; and to a method of controlling the growth of phytopathogenic fungi at a locus which comprises a

Abstract: This invention relates to the use of a conjugate comprising an active substance and a native protein which is not recognized as foreign protein for the production of a pharmaceutical preparation for treating and/or diagnosing inflammatory, infectious and/or skin diseases.

Abstract: The invention relates to a method of combating phytopathogenic diseases on crop plants which comprises applying to the crop plants or the locus thereof being infested with said phytopathogenic disease an effective amount of a combination of a) a benzophenone of formula I  wherein R1 is methoxy or methyl, R2 is C1-C4alkoxy or 2-halogenbenzyloxy, R3 is C1-C4alkoxy, R4 is C1-C4alkyl, halogen or trifluoromethyl, and R5 is hydrogen, halogen, C1-C4alkoxy, trifluoromethyl or nitro; in association with b) a compound selected from the group comprising compounds of formulae II, III, IV, V, VI, VII, VIII, IX, X and XI as described herein.

Abstract: Disclosed are methods to lower blood cholesterol levels or inhibit ileal apical sodium co-dependent bile acid transport (ASBT) protein using coumarin and anthracene dione derivatives. Pharmaceutical compositions are also disclosed.

Abstract: The present invention is directed to a new class of serotonin 5HT2 antagonists and thier use in the treatment of a variety of diseases.

Abstract: The present invention relates to the compounds of formula: 1

Abstract: The invention comprises a method of combating phytopathogenic diseases on crop plants which comprises applying to the crop plants or the locus thereof being infested with said phytopathogenic disease an effective amount of a combination of

Abstract: The present invention relates to an oral compacted composition comprising entacapone, nitecapone, or a pharmaceutically acceptable salt thereof and croscarmellose sodium. The composition is premised on the discovery that croscarmellose sodium increases the release rate of entacapone or nitecapone from an oral compacted composition. Preferably the amount of croscarmellose sodium in the composition is at least 6% by weight, preferably from about 8% to about 16% by weight, especially from about 10% to about 14% by weight.

Abstract: A use of tetralin derivatives as biocidal and antifouling agents for preventing and slowing the growth of algae, molds and microorganisms. In particular, the vitamin derivatives are constituted by salts of menadione bisulfite with the heterocyclic bases triazine and piperazine.

Abstract: The present invention is the synthesis of a series of 1,5-dichloro-9(10H)-anthracenones bearing O-linked and N-linked substituents in the 10-position. These compounds were evaluated for their ability to inhibit the growth of the human oral epidermoid carcinoma cells (KB cell line), human cervical carcinoma cells of ME 180 (GBM 8401) and Chinese hamster ovary cells (CHO), respectively. In addition, redox property of the compounds for inhibition of lipid peroxidation in model membranes was determined.

Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.