Abstract: The present invention relates to stilbene and quinone compounds related to combretastatin A-4 and their use as anticancer compounds and prodrugs. The compounds include those with an alkyl group on the double bond of cis or trans-stilbenes, compounds with one or more (and preferably 2 or 3) alkyl group substituents on the stilbene A ring, compounds with an alkoxy group other than methoxy at position 3, 4, and/or 5 of the stilbene A ring, compounds (or prodrugs) in which BOC amino acid esters are formed with the phenolic hydroxyl at the 3-position of the B ring and compounds (or prodrugs) based on a benzoquinone B ring. The present invention further relates to the photochemical reactions of stilbene compounds, either the above compounds disclosed for the first time herein or compounds based on prior art stilbenes.

Abstract: The present invention relates to a fungicide containing a novel benzoylpyridine derivative or its salt. The present invention provides a fungicide containing a benzoylpyridine derivative represented by the formula (I) or its salt: wherein X is a halogen atom, a nitro group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group, a hydroxyl group, a substitutable hydrocarbon group, a substitutable alkylthio group, a cyano group, a carboxyl group which may be esterified or amidated, or a substitutable amino group; n is 1, 2, 3 or 4; R1 is a substitutable alkyl group; R2 is a substitutable alkyl group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group or a hydroxyl group; and m is 1, 2, 3 or 4, provided that when m is at least 2, R2 may contain an oxygen atom to form a condensed ring.

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: The present invention is directed to methods of using pro-NAD agents capable of enhancing the dermal and epidermal skin cell NAD content. These pro-NAD agents may be administered topically, orally, or parenterally to enhance DNA repair and other protective responses to DNA damage. The invention further relates to pharmaceutical compositions comprising pro-NAD agents that effectively elevate intracellular NAD content. Finally, the invention relates to the method of using the pro-NAD agents to treat disorders such as sunburn and other skin deterioration that results from DNA damage in skin cells.

Abstract: The present invention provides a topical composition comprising about 6% to about 15% nifedipine and about 6% to about 15% pentoxifylline for treating severe vascular occlusive wounds. The present invention also provides a method and a kit for treating the vascular occlusive wound by applying the composition to the open wound, and cleaning and dressing the wound at least once daily.

Abstract: Disclosed are compositions and methods for treating hypertension comprising lisinopril and lercanidipine in amounts effective in combination to reduce blood pressure to a patent in need of treatment.

Abstract: The present invention provides compounds of Formula I, compositions and methods that are useful for treating viral infections and associated diseases, particularly HCV infections and associated diseases.

Abstract: 1.

Abstract: The present invention relates to antibacterial agents that are useful for sterilization, sanitation, antisepsis, disinfection, and treatment of antibacterial infections in mammals.

Abstract: The use of compounds of the formula 1

Abstract: The present invention describes compounds of the general formula I 1

Abstract: A device and method is described for providing sustained vasodilation at a site in a patient. The device includes a biocompatible and possibly biodegradable carrier, and a vasodilator incorporated into the carrier. The vasodilator is present in a topically effective amount to achieve sustained vasodilation at a selected site in a patient. The vasodilator may be nitroglycerine or calcium channel blockers. The carrier includes methylcellulose and equine collagen, and may be in the form of a strip. The method includes administering, at a selected site in a patient, a vasodilator incorporated into a carrier. The vasodilator is present in a topically effective amount to achieve sustained vasodilation at the selected site.

Abstract: The present invention relates to compounds according to the general formula (I), wherein R1-R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B, C and D are independently CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description.

Abstract: This invention is directed to methods for treating age-related decline in physical performance which comprises administering a growth hormone secretagogue, a prodrug thereof or a pharmaceutically acceptable salt of said secretagogue or said prodrug.

Abstract: The present invention is directed to nanoparticulate compositions comprising nifedipine. The nifedipine particles of the composition have an effective average particle size of less than about 2 microns.

Abstract: Amlodipine camsylate of the present invention is a crystalline salt of amlodipine suitable for pharmaceutical formulation, which is prepared by using low toxic camphor sulfonic acid to meet required pharmaceutical properties for treating cadiovacular diseases.

Abstract: The invention relates to the use of nicotinic acid and nicotinic acid esters, such as nicotinic acid alkyl esters, to increase the amount of leptin in a subject. As a result, one can treat conditions, such as conditions characterized by wounds, by administering sufficient amounts of nicotinic acid or nicotinic acid ester to increase leptin levels to alleviating amounts. Various conditions and modes of treatment are disclosed.

Abstract: The invention provides antimicrobial agents and methods of using the agents for sterilization, sanitation, antisepsis, disinfection, and treatment of infections in mammals.

Abstract: Compositions, methods and uses are provided for treating or preventing cardiovascular disease, including by decreasing serum cholesterol, triglyceride and lipoprotein cholesterol levels in a host that include administering an effective amount of D-malic acid or its pharmaceutically acceptable salt, prodrug or pharmaceutically acceptable derivative.

Abstract: Compounds which can be represented by the general formula (I) indicated below: 1

Abstract: A novel solid pharmaceutical dispersion that improves the bioavailability of poorly water soluble drugs is produced by combining the drug with a polymer carrier such as polyvinylpyrrolidone. The drug is combined with the carrier without the need for using organic solvents or melting temperatures (fusion) through the use of a transition compound such as polyethylene glycol which partially solubilizes the drug and/or plasticizes the polymer.

Abstract: Heterocyclic dicarboxylic acid diamide derivative represented by the general formula (I): wherein R1, R2 and R3 represent each H, optionally halogenated C3-6 cycloalkyl, etc.; Het represents a 5- or 6-membered heterocycle; X and Y represent each halocyano, nitro, optionally halogenated C3-6, cycloalkyl, optionally substituted phenyl, an optionally substituted heterocycle, etc; n is from 0 to 3; m is from 1 to 5; Z1 and Z2 represent each O or S; and B1 to B4 represent each C or N. Agricultural/horticultural insecticides having an excellent controlling effect on pest insects such as diamond-back moth (Pluntella xylostella) and tobacco cutworm (Spodoptera litura).

Abstract: The present invention relates to a compound formula [I]: 1

Abstract: Nonalcoholic steatohepatitis (NASH) is a disease of the liver characterized by inflammation and damage to the liver cells. Typically, steatohepatitis involves inflammation of the liver related to fat accumulation, and mimics alcoholic hepatitis but is observed in patients who seldom or never consume alcohol. Nonalcoholic steatohepatitis can lead to serious liver damage, and ultimately cirrhosis. The present invention provides methods and compositions useful for the treatment or alleviation of nonalcoholic steatohepatitis and the pharmaceutical formulations for their administration to a human. Specifically, compositions comprised of lecithin, antioxidants and vitamin B complex are administered parenterally, most preferably by oral administration. Specific therapeutic formulations include admixtures of these compounds and specific dosage formulations include daily oral administrations of these compounds in tablet or powder forms.

Abstract: This invention relates to neurotrophic, low molecular weight, small molecule heterocyclic ketone and thioester compounds, compositions containing the same, and the use of such compounds for treating neurological disorders, including physically damaged nerves and neurodegenerative diseases.

Abstract: 1) Fungicidal compositions comprising: a) at least one pyridylmethylbenzamide derivative of Formula (1), in which the various radicals are as defined in the description; and b) at least one compound (11) capable of inhibiting the transport of electrons of the respiratory chain of mitochondrial ubiquinol:ferricytochrome-c oxidoreductase or complex III in phytopathogenic fungal organisms. 2) Process for curatively or preventively controlling the phytopathogenic fungi of crops, characterized in that an effective and nonphytotoxic quantity of one of these fungicidal compositions is applied to the aerial parts of plants.

Abstract: Methods and compositions for the topical or transdermal treatment of neuropathy. More particularly, transdermal or topical compositions including a combination of ingredients that provide a surprising degree of effective relief from the symptoms of peripheral neuropathy and methods for administering the compositions to treat various neuropathies.

Abstract: The present invention relates to novel heteroaryl-carboxamides which modulate the activity of protein tyrosine kinases and therefore are expected to be useful in the treatment of abnormal protein tyrosine kinase activity driven disorders including cancer.

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

Abstract: This invention relates to a composition and method for the treatment of white line disease, including ailments such as onychomycosis, sporotichosis, hoof rot, jungle rot, pseudallecheria boydii, scopulariopsis or athletes foot. The composition of the present invention is useful for the treatment of fungal infections such as onychomycosis in warm blooded animals such as humans and horses. The method of the present invention is directed to the application of a therapeutic amount of the present composition.

Abstract: The present invention provides agents for proliferating pancreatic &bgr;-cells of Langerhans' islets, agents for suppressing apoptosis of the cells, and methods of screening for candidate compounds for these agents. The combined use of an inflammatory mediator IL-6 and glucocorticoid remarkably induces the expression of Reg gene in &bgr; cells and thus promotes proliferation of &bgr; cells. HGF suppresses apoptosis induced by Reg protein and IL-6 and glucocorticoid induce intracellular expression of HGF gene. PARP inhibitors such as nicotinamide and 3-aminobenzamide further enhance the induction of the expression of these genes. Moreover, based on the analysis of the expression induction mechanism using the promoter regions of Reg gene and HGF gene, methods of efficiently screening for candidate compounds for these gene expression inducers have been developed.

Abstract: This invention relates to use of the combined action of a nicotinic acetylcholine receptor agonist and a monoaminergic substance for the treatment of affective disorders, as well as to pharmaceutical compositions comprising these substances and chemical substances for use according to the invention.

Abstract: The present invention relates to methods of treating sexual dysfunction associated with hypertension and another condition by administering a pharmaceutical combination of an angiotensin receptor blocker with either an anti-hypertensive drug or an HMG-CoA reductase inhibitor.

Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes, for making such novel compounds.

Abstract: The invention provides controlled release pharmaceutical formulations having a coated core with the core comprising a drug-containing composition and a water-swellable composition, each occupying essentially separate regions within the core. The drug-containing composition comprises a PDE4D inhibitor, or a pharmaceutically acceptable salt thereof, preferably (R)-2-[4-({[2-(benzo[1,3]dioxol-5-yloxy)-pyridine-3-carbonyl]-amino}-methyl)-3-fluoro-phenoxy]-propionic acid, or a pharmaceutically acceptable salt thereof, or 2-(4-fluorophenoxy)-N-[4-(1-hydroxy-1-methyl-ethyl)-benzyl]-nicotinamide, or a pharmaceutically acceptable salt thereof, and a drug-entraining agent. The coating around the core is water-permeable, water-insoluble, and has at least one delivery port therethrough.

Abstract: The invention is a cosmetic or dermatological formulation comprising one or more substances selected from the group of lipofuscins. The present invention also includes methods of using cosmetic or dermatological formulations comprising lipofuscins, for example, in inducing or intensifying the tanning the skin.

Abstract: The present invention relates to novel crystalline forms of Amlodipine Maleate These crystalline forms are useful as pharmaceutical agents. This invention also relates to pharmaceutical compositions which include these crystalline forms and to methods of treatment using these crystalline forms. The novel crystalline compounds of the present invention are useful as calcium channel blockers and are thus useful as anti-ischaemic and anti-hypertensive agents.

Abstract: A free radical quenching composition is disclosed comprising a liposome containing at least two antioxidants selected from the following group: beta-carotene, vitamin E, vitamin C, glutathione, niacin, and optionally at least one trace metal (Zn, Se, Cr, Cu, Mn). Also disclosed is a method for reducing the undesirable side effects of free radicals in a mammal by administering to a mammal in need of such antioxidants an effective amount of liposomes containing at least two antioxidants.

Abstract: Neuro-metabolic and endocrine-function regulating/modulating compositions, are disclosed. The compositions of the present invention comprise Selegiline Hydrochloride, Procaine Hydrochloride, Vinpocetine, trimethylglycine, and an ingredient selected from a group consisting of N-nicotinoyl-gamma-aminobutyric acid (N-GABA), niacin, niacinamide, gamma-aminobutyric acid (GABA), and combinations thereof. Methods of using the compositions, compositions, and compositions of the present invention are also disclosed.

Abstract: Novel methods and combinations for the treatment and/or prophylaxis of a pathologic condition in a subject, wherein the methods comprise the administration of one or more aldosterone receptor antagonists and one or more, nicotinic acid derivatives and the combinations comprise one or more of said aldosterone receptor antagonists and one or more of said nicotinic acid derivatives.

Abstract: Compounds having the formula 1

Abstract: An aromatic sulfonyl aipha-hydroxy hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies. The kits, devices, and methods employ a termiticidal bait matrix containing a) a termiticide selected such that the termiticide causes death to about 50 to about 100% of termites within about 24 to about 84 days after the termites begin to ingest the termiticide or the bait matrix comprising the termiticide, b) a cellulose containing material, and c) water. The termiticidal bait matrix can be used in a bait station installed in the ground. The kits are suitable to be used by consumers in their homes.

Abstract: The present invention provides carbanilides of formula (I), wherein A, Q, R, X, Z and m are as defined herein. A plurality of processes for preparing these compounds is provided, along with methods of using the compounds to control microorganisms in crops and in the protection of materials. The compounds of the present invention also find use in controlling animal pests.

Abstract: Smooth muscle tone modulator compositions and methods of use thereof are provided for the treatment of oesophageal motility disorders and gastro-oesophageal reflux disease. The smooth muscle tone modulators are applied topically to treat the disorder. Topical treatment reduces the risk of undesirable side effects observed in connection with oral or sublingual administration of the modulators.

Abstract: The invention relates to a pharmaceutical formulation containing at least one compound of formula (1) wherein R1, R2, and X have the same meaning as cited in claim 1, and the physiologically acceptable salts thereof and/or solvates and a) at least one antithrombotic or b) at least one calcium antagonist or c) at least one prostaglandin or prostaglandin derivative for producing a medicament for treating angina, high blood pressure, pulmonary hypertension, congestive heart failure (CHF), chronic obstructive pulmonary disease (COPD), pulmonary heart disease, right ventricular failure, atheriosclerosis, permeability conditions of reduced cardiovascular patency, peripheral vascular illnesses, cerebral apoplexy, bronchitis, allergic asthma, chronic asthma, allergic rhinitis, glaucoma, irritable bowel syndrome, tumours, kidney failure, cirrhosis of the liver and for treating female sexual problems.

Abstract: A novel crystalline organic acid salt of amlodipine having improved physiochemical properties, a preparation method thereof and a pharmaceutical composition comprising the same are provided.

Abstract: Pleuromutilin compounds of the formula: 1

Abstract: The present invention relates to solid pharmaceutical combinations for oral administration comprising nicotinic acid or a nicotinic acid compound or mixtures thereof in an extended release form and an HMG-CoA reductase inhibitor, which are useful for altering lipid levels in subjects suffering from, for example, hyperlipidemia and atherosclerosis, without causing drug-induced hepatotoxicity, myopathy or rhabdomyolysis.

Abstract: This invention pertains to the discovery of a novel family of thiolesters and uses thereof. Also provided for are viricidal compounds and pharmaceutical formulations comprising these novel thiolesters. The invention also provides thiolester-inactivated viruses and thiolester-complexed viral proteins.