Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.

Abstract: The present invention provides a method for protecting against UV radiation-induced skin damage. Specifically, compositions including dapsone are administered to provide UV protection. The dapsone compositions may be administered orally, or by other parenteral routes, such as topically, transdermally, by inhalation, and the like.

Abstract: The invention provides a method of treating comorbid premature ejaculation and erectile dysfunction. In particular, the method comprises administering an effective amount of a tramadol material and an effective amount of a phosphodiesterase inhibitor. The invention also provides a pharmaceutical composition comprising a pharmaceutically-acceptable carrier, a tramadol material and a phosphodiesterase inhibitor. The invention further provides a kit comprising a tramadol material and a phosphodiesterase inhibitor.

Abstract: The invention provides compounds of Formula (I) and pharmaceutical compositions comprising compounds of Formula (I).

Abstract: Stilbene derivatives exhibit killing and suppression of growth activity against a variety of cancer cells, and are effective at suppressing tumor growth in vivo. The stilbene derivatives may be used in the treatment of diseases characterized by cell hyperproliferation including human malignancies and non-malignant diseases such as liver cirrhosis. Stilbenes may also disrupt abnormal vessels in tumor to achieve vascular disrupting effect to suppress tumor growth. Water soluble pro-drug forms of stilbene derivatives are particularly useful in suppressing tumor growth in vivo.

Abstract: Triphenylethylene compounds of formula (I) are provided. The compounds are particularly useful for selective estrogen receptor modulation.

Abstract: Novel calcilytic compounds and methods of using them are provided.

Abstract: Disclosed are multibinding compounds which are ?2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: The present invention relates to a tetrafluorobenzyl derivative and a pharmaceutical composition for prevention and treatment of acute and chronic neurodegenerative disease in central nervous system and ophthalmic diseases containing the same. The tetrafluorobenzyl derivative of the present invention can effectively be used to prevent and treat chronic neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease and Huntington's disease, degenerative brain disease such as epilepsy and ischemic brain disease such as stroke.

Abstract: Compounds are disclosed having the structure of Formula I: where R1, R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. Such compounds may be utilized for the prophylaxis or treatment of various diseases, particularly inflammatory conditions of the GI tract. Methods of treating inflammatory conditions of the GI tract such as inflammatory bowel disease using compounds having the following formula are also disclosed: where R9, R10 and R11 are independently selected from the group consisting of hydrogen and C1 to C4 alkyl, and R12 is selected from the group consisting of hydrogen and —C(O)R13, where R13 is a C1 to C6 alkyl or an aryl group.

Abstract: A method for inhibiting the activity of a natural polyamine transporter comprising the step of contacting the transporter with an inhibitorily effective amount of a compound of formula (I) or (II): wherein L is a linker; R1=H, methyl, ethyl or propyl; R2=H or methyl; 0<x<3; 0<y<3; 2<v<5; and 2<w<8. Such a method is particularly useful for treating disorders involving the control of polyamine transport.

Abstract: The present invention concerns compounds of formula: where R1, R2, R3 and R4 are defined in the specification.

Abstract: Systems and methods for longevity, anti-aging, fatigue management, obesity, weight loss, weight management, delivery of nutraceuticals, and treating hyperglycemia, Alzheimer's disease, sleep disorders, Parkinson's disease, Attention Deficit Disorder and nicotine addiction involve synchronizing and tailoring the administration of nutraceuticals, medications and other substances (for example, stimulants) in accordance with the body's natural circadian rhythms, meal times and other factors. Improved control of blood glucose levels, extended alertness, and weight control, and counteracting of disease symptoms when they are at their worst are possible.

Abstract: Sustained release spherical or non-spherical pellets comprising (a) an active ingredient (b) a wax-like agent, and (c) a spheronizing agent are provided. Oral dosage forms comprising said pellets and methods for preparing and using such pellets and dosage forms are also provided.

Abstract: The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen or lower alkyl; R3, R4, R5 and R6 are each hydrogen, halogen, lower alkyl or lower alkoxy; R7 and R8 are each hydrogen, halogen, lower alkyl, halo-lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, cyano, a hydroxyl group, lower acyl, carboxy or the like; R9 is —C(O)—R10, -A1-C(O)—R10, —O-A2-C(O)—R10 or a tetrazol-5-yl group, which exhibit potent and selective ?3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.

Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S, and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.

Abstract: This invention relates to methods for treating, preventing and/or managing cancer in a subject including enhancing the efficacy of a Vascular Disrupting Agent (e.g., a combretastatin or derivative thereof) by administering to the subject a Chemokine Receptor Antagonist (e.g., a CXCR4 antagonist) or Chemokine Antagonist (e.g., a SDF-1 antagonist) sequentially or simultaneously in combination with said Vascular Disrupting Agent.

Abstract: Chitosan silicon dioxide coprecipitate composition, method of production thereof, pharmaceutical composition comprising the chitosan silicon dioxide coprecipitate composition and use of the chitosan silicon dioxide coprecipitate composition for manufacturing a sustained or immediate release formulation.

Abstract: Disclosed are polar, hydrophilic stimulant prodrug compositions comprising at least one stimulant chemically attached to a polar hydrophilic ligand, a salt thereof, a derivative thereof, or a combination thereof. Methods of making and using the same are also disclosed.

Abstract: An orally disintegrating tablet which can be chewed or disintegrated by contact with saliva and containing weight-loss drugs for weight control in humans, especially in children and adolescents, is disclosed.

Abstract: Pharmaceutical compositions comprising at least one compound of the formulas (Ia) or (Ib) and a pharmaceutically acceptable carrier wherein the symbols have the following meaning —X— is e.g. and Y being e.g. or the pharmaceutically acceptable salts can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.

Abstract: Selective estrogen receptor modulators, as well their related pharmaceutical compositions and methods of use, are provided herein. These estrogen receptor modulators include compounds that primarily exhibit estrogen receptor antagonist activity or primarily exhibit selective estrogen receptor antagonist and agonist activity, i.e., SERM activity, in specific tissue types. Particular embodiments provide compounds that behave as NeuroSERMs promoting neurotrophism and neuroprotection in brain tissue. These NeuroSERMs represent a subset of the modulators compounds provided herein that can cross the blood-brain-barrier and exert estrogen receptor agonist-like effects in the brain. The compounds should be useful for treating a variety of diseases, particularly estrogen receptor-mediated diseases and disorders, such as osteoporosis, breast and endometrial cancers, atherosclerosis and Alzheimer's disease.

Abstract: The present invention relates a method of treating drug addiction in an individual by administering to the addicted individual a therapeutically effective amount of dextro-morphine capable of activating an opioid receptor. It is disclosed here that dextro-morphine is suitable for treating addiction to natural opiates, semi-synthetic opiates, fully synthetic opioids, and endogenous opioid peptides, as well as nicotine.

Abstract: The invention relates to extended release pharmaceutical compositions of venlafaxine or pharmaceutically acceptable salts. More particularly this invention relates to a pharmaceutical composition having a core comprising venlafaxine and a coating thereupon. The coating utilizes at least one water insoluble polymer and at least one polymer having pH dependent solubility to delay and modulate the release of the drug in an extended manner.

Abstract: The present invention relates to a composition comprising sibutramine free base. The present invention provides a solid dispersion wherein sibutramine free base, acid and hydrophilic polymer are uniformly dispersed and a manufacturing method thereof. The composition of the present invention has improved dissolution rate compared to conventional compositions containing sibutramine free base or sibutramine hydrochloride, and is also stable during storage and can be easily mass-produced.

Abstract: The invention provides novel N-benzyl-N-propargyl-amines that are monoamine oxidase inhibitors, but generally exhibit little or no CNS effects.

Abstract: An analgesic composition for external application for increasing the percutaneous permeability of tramadol or a pharmaceutically acceptable salt thereof and for achieving a quick pharmacological effect. The analgesic composition includes tramadol or a pharmaceutically acceptable salt thereof, a menthol substance and a pyrrolidone compound.

Abstract: Chronic pain is alleviated in a mammal suffering there from by administering to the mammal a chronic pain alleviating amount of a nontoxic N-methyl-D-aspartate receptor antagonist such as dextromethorphan, dextrorphan, ketamine or pharmaceutically acceptable salt thereof, in combination with a ?-opiate analgesic such as tramadol or an analogously acting molecular entity, and a methylxanthine such as caffeine, and optionally in sustained release dosage form.

Abstract: The invention relates to radiolabeled compounds and their use in methods of imaging amyloid deposits, as well as to methods of their manufacture. The invention also relates to compounds for inhibiting the aggregation of amyloid proteins that form amyloid deposits, methods for delivering therapeutic agents to amyloid deposits, as well as methods of making compounds that inhibit the aggregation of amyloid proteins.

Abstract: The present invention relates to compounds of formula (AA) (I) and (X): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

Abstract: The invention pertains, at least in part, to a method for treating metabolic syndrome in a subject. The method includes administering to a subject an effective amount of a compound of formula (I). The compound of formula (I) is: wherein R1 and R2 are independently H or methyl, and enantiomers and pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to the use of compounds of the formula (I), with radicals defined in the description, as antioxidants, to corresponding novel compounds and compositions, and to corresponding processes for the preparation of compounds and compositions.

Abstract: A new weight reduction program and method 1 having three phases, an acute weight loss phase 2, a transitional phase 3 and a long-term maintenance phase 4. Appetite suppressants 12 (such as phenylkylamine sympathomimetic amine 13), calcium pyruvate 17, a multiple vitamin-mineral supplement 16, amino acids and cyanocobalomine 10 are taken in conjunction with the new diet program to achieve optimal weight loss and health benefits.

Abstract: Disclosed herein is a pharmaceutical composition comprising a serotonin-norepinephrine reuptake inhibitor and a pan-alpha-2 receptor agonist. The composition is effective for treating chronic pain, and methods of treating pain using the composition and compounds comprising it are also disclosed.

Abstract: Disclosed is the use of sphingosine-1-phosphate (S1P) receptor agonists, preferably 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol, in the treatment of progressive dementia or brain degenerative diseases.

Abstract: The present invention provides novel cycloalkylmethylamine analogs, and methods of preparing cycloalkylmethylamine analogs. The present invention also provides methods of using cycloalkylmethylamine analogs and compositions of cycloalkylmethylamine analogs. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications.

Abstract: The invention provides new inhibitors of protein glycation, identified from compound libraries by a high throughput screening assay. The anti-glycation agents so identified are characterized by a variety of chemical structures and are useful for the prevention or treatment of age-, diabetes-, and smoking-related complications, including neuropathy, nephropathy, ocular pathologies, or the loss of mechanical properties of collagenous tissues. Among compounds identified as having the anti-glycation activity, of special interest are epinephrine and its analogs, in particular D-epinephrine and its analogs, which are particularly useful for the prevention or treatment of age-, diabetes-, and smoking-related ocular pathologies.

Abstract: Antimicrobial compositions having a rapid and persistent antiviral and antibacterial effectiveness are disclosed. The antimicrobial compositions contain (a) a divalent zinc salt, (b) an optional disinfecting alcohol, (c) an optional antimicrobial agent, and (d) an optional organic acid, wherein the composition has a pH of about 5 or less.

Abstract: The present invention provides compounds and methods for the inhibition of monoamine uptake in mammals.

Abstract: This invention is directed to substituted aryl compounds, which are linked to a substituted indole moiety by various linkers, and the kynurenine/kynuramine-like metabolites of these agents, their preparation and pharmaceutical compositions containing these compounds. This invention further is directed to the pharmaceutical use of the compounds for inhibiting GSK3? kinase and/or modulating N-methyl-D-aspartate (NMDA) channel activities for the treatment of neurodegenerative and other disorders.

Abstract: Compounds having anti-androgenic activities are disclosed. Further disclosed are methods of using the compounds to prevent or treat androgen-dependent diseases or to provide nutraceutical benefits. Pharmaceutical and nutraceutical compositions containing the anti-androgenic compounds are also disclosed.

Abstract: The present invention relates to methods of alleviating pain with the administration of norketamine with a narcotic. More particularly, the invention provides a method of alleviating pain through the administration of a dose of norketamine, which, if administered alone would provide sub-optimal analgesic relief, yet provides analgesic relief when combined with a narcotic. In some embodiments, the combination of norketamine with a narcotic, further allows for the administration of a dose narcotic, which would be sub-optimal if used alone, but provides adequate pain relief in combination with norketamine. The invention relates to self-management of pain on an outpatient basis comprising administering via conventional routes, including transdermal, nasal, rectal, oral, transmucosal, intravenous, intramuscular, and other routes, one or more doses of norketamine/opioid compositions effective to alleviate pain to a subject suffering from pain.

Abstract: The invention relates to the cancer antigen PRAME (PReferentially expressed Antigen in MElanoma) and its use in a method of treatment of a tumour which comprises administering to a subject in need of treatment an effective amount of an inhibitor of PRAME, in combination with a second agent selected from the group of an inhibitor of HDAC (an HDACi) and a retinoid.

Abstract: A method for treating the adverse effects of acetyl-cholinesterase inhibitors used in the treatment of cognitive disorders such as acute delirium and cognitive impairment in elderly human patients. The administration of a clinically effective amount of a quaternary ammonium anti-cholinergic muscarinic receptor antagonist having very low lipid solubility substantially eliminates the adverse effects of urinary and/or fecal incontinence, nausea, bradycardia, bronchorrhea or brochospasm caused by the acetyl-cholinesterase inhibitors, without affecting the beneficial activity of the acetyl-cholinesterase inhibitors. This permits the administration of the optimum effective dosing of acetyl-cholinesterase inhibitors to provide maximum benefit to the patient with the added benefit of reducing or eliminating the unwanted side effects of fecal and urinary incontinence.

Abstract: A method for treating increased uninary urgency or urinary incontinence, comprising administering an effective amount of a compound corresponding to formula I It has been surprisingly discovered that the methods of the present invention are effective for treating increased urinary urgency or urinary incontinence. Also disclosed are methods of treatment using related pharmaceutical compositions.

Abstract: The present invention is directed to benzylether and benzylamino derivative compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract: A biodegradable medicament delivery system comprising a multi-layered calcium-sulfate based drug delivery vehicle. The vehicle comprises a calcium sulfate center or core with the medicament or medicaments, encased in one or more layers of chitosan. The chitosan may be cross-linked with a cross-linking agent. The vehicle may comprise any suitable shape, including, but not limited to, a sphere, bead or pellet. Medicaments include, but are not limited to, antibiotics, anesthetics, growth factors, and proteins. A physician can implant the coated vehicles into the desired site to create a beneficial, localized treatment that produces high local concentrations of medication while reducing the overall serum concentration throughout the body.

Abstract: A combination therapy for treating mood disorders, including depressive disorders such as major depression, panic disorder, obsessive compulsive disorder, social anxiety disorder, seasonal affective disorder, and premenstrual dysphoria is provided herein. The combination therapy comprises administering an effettive amount of mecamylamine together with at least one agent for treatment of a mood disorder to a patient in need of treatment of the mood disorder. Pharmaceutical formulations, including packaged pharmaceutical formulations, comprising mecamylamine and an additional agent, such as an SSRI, are also provided herein.

Abstract: The present invention relates to new use of inhibitors of bcl-2/bcl-XI family of anti-apoptotic compounds for the treatment of post-angioplasty restenosis and in-stent restenosis. Small molecules of Bcl inhibitors are incorporated into a stent, typically by a fine polymeric coating over the metal, which would be placed during angioplasty of occluded blood vessels, to act on fibroproliferative in-growth. Hollow organs such as urethras, Fallopian tubes and vascular access grafts could be treated in a similar manner to prevent their closure due to fibrosis. Other iatrogenic fibrosis such as adhesions after surgery could also be blocked by this therapy.