Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.

Abstract: Selective PDE4 inhibition is achieved by novel compounds, e.g., 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds of the present invention are of formula I: wherein R1, R2, and R3 are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

Abstract: The present invention generally relates to the transdermal delivery of substances and, in some embodiments, to the transdermal delivery of beneficial substances by a hostile biophysical environment. In one aspect, various methods for the transdermal delivery of beneficial substances are disclosed. By creating a hostile biophysical environment, beneficial substances may be delivered, according to certain embodiments, through the stratum corneum of the skin into the body. Beneficial substances include, but are not limited to, pharmaceutical agents, drugs, vitamins, co-factors, peptides, dietary supplements, and others. The beneficial effects disclosed include, for instance, relief of pain and inflammation, prevention and healing of ulcers of the skin, relief of headache, improved sexual function and enjoyment, growth of hair on the scalp, improving muscle size and/or function, removing body fat and/or cellulite, treating cancer, treating viral infections and others.

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: Disclosed herein are compounds useful in treating glaucoma, inflammatory bowel disease, the stimulation of hair growth, and the stimulation of the conversion of vellus hair to terminal hair. The compounds themselves are herein.

Abstract: A crude extract composition derived from the plant family Annonaceae and the method for producing the crude extract composition. Medicinal benefits of the extract include tumor regression and the reduction of tumor antigen levels.

Abstract: An antimicrobial coating is provided for use on textiles, medical devices, packaging materials, and the like. The antimicrobial coating includes a halogenated furanone.

Abstract: The present invention relates to a novel class of compounds mainly, substituted leucinamide-carboxylate derivatives of formula (I) wherein X is O or NR9, Y is CR1R2, —SO2, C?O or NR9; Z is CR1R2, O, S, —SO2 or NR9 and each G is independently a CR1CR2 and pharmaceutical compositions thereof. Said compounds are cathepsin cysteine protease inhibitors, including but not limited to, inhibitors of cathepsin K, L, S and B. These compounds are useful for treating and preventing cathepsin dependent conditions in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract: The present invention relates to a novel class of compounds mainly, leucinamide-amino-carboxylate derivatives of formula (I) wherein Y is CR1R2, O, S, —SO2, C=0 or NR9; Z is CR1R2, O, S, —SO2, C?O or NR9 and each G is independently a CR1CR2. Said compounds are cathepsin cysteine protease inhibitors, including but not limited to, inhibitors of cathepsin K, L, S and B and to pharmaceutical compositions thereof. These compounds are useful for treating and preventing cathepsin dependent conditions in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract: The present invention provides methods for identifying genes, expression regulators, receptors, protein product receptors, and proteins that may regulate rhinovirus infections. The genes identified may be used as markers for disease onset and progression and to measure efficacy of a therapeutic. The present invention also provides methods to screen agents that are capable of regulating rhinovirus infection. The present invention also provides methods of identifying therapeutic compounds that may treat various disorders by regulating the expression and activity of genes, expression regulators, receptors, protein product receptors, and proteins identified.

Abstract: This invention provides new compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, prostate cancer, muscle wasting diseases and/or disorders or a bone-related diseases and/or disorders.

Abstract: This invention relates to crystals comprising apo-LsrB and holo-LsrB. The structure of holo-LsrB identifies a tetrahydroxytetrahydrofuran derived from 4,5-dihydroxy-2,3-pentanedione (DPD) as the active autoinducer-2 (AI-2) molecule in Salmonella typhimurium. The X-ray crystallographic data can be used in a drug discovery method. Additionally the invention provides AI-2 analogs based on this discovery as well as pharmaceutical compositions containing those analogs.

Abstract: Pyrocatechin derivatives of formula I wherein R illustrates a group of formulae Ia, Ib, Ic or Id R1 is 4-halogen-but-2-enyl, R2 is lower alkyl or cycloalkyl, R3 is lower alkoxy and R4 is lower alkoxy lower alkoxy, or, where R is a group of formula (Ia), it is hydroxy, hydroxy lower alkoxy or a group of formula Ie R5 is reactive esterified hydroxy, R6 is azido and R7 is lower alkyl, lower alkenyl, cycloalkyl or aryl lower alkyl, and their salts, are valuable intermediates in the production of active ingredients for medicaments.

Abstract: A method of neuroprotection which comprises administration of an AMPK inhibitor to a patient who is experiencing or has experienced a stroke, the compound being an AMPK inhibitor. Treatments with these agents significantly reduce the size of infarcts, and therefore minimize the loss of brain tissue and neurons. Thus, function can be preserved after stroke or ischemic injury in the brain. Similarly, neuronal loss can be minimized in degenerative diseases that cause neuronal compromise by perturbing energy utilization and availability in neurons.

Abstract: A method for controlling pests, the method comprising applying an effective amount to pests or their locus of one or more compounds of general formula (I) wherein R1 and R2 represent, independently from each other, hydrogen, halogen, alkoxy, substituted alkoxy or an ester group; R1 and R2, together with the carbon atoms to which they are attached, represent an oxirane ring; R1 and R2, taken together, represent an akylidenedioxy or substituted alkylidenedioxy group; and R3 represents —CH2R6, wherein R6 represents an ester group, oxiranyl, or a group of formula wherein R7 represents hydrogen or alkyl, R8 represents phenylsulfanyl, phenylselenyl, phenylsulfoxy or phenylselenoxy, and R9 represents hydrogen, ethoxycarbonyl or carbamoyl; and R4 represents, independently, hydrogen, alkoxy or substituted alkoxy, or R1 and R4, taken together, represent an alkylidenedioxy or a substituted alkylidenedioxy group; wherein the pest dies as a result of contact with the compound.

Abstract: An adjuvant for transdermal or transmucosal administration which comprises at least one substance selected from an aliphatic alcohol, a free fatty acid and a fatty acid derivative but does not contain a substance represented by the following formula: wherein R3 and R4 may together form a cyclic ring, and R1 and R2 independently represent an alkyl side chain having 1 to 16 carbon atoms.

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

Abstract: The present invention relates to selected (R)-arylalkylamino derivatives of formula (I), in which R, R1 and Ar are as defined in the claims. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.

Abstract: This invention provides methods and compositions for inducing weight loss and maintaining optimum weight comprising administering an agent that stimulates carnitine palmitoyl transferase-1 (CPT-1) activity to the patient in need, including human patients. These methods do not require inhibition of fatty acid synthesis. In particular, this invention provides methods for development of therapeutics that selectively enhance fatty acid oxidation, increase energy production, and reduce adiposity while preserving lean mass, through the pharmacological stimulation of CPT-1 activity. In a preferred mode, the agent is administered in an amount sufficient to increase fatty acid oxidation. In another preferred mode, the agent is administered in an amount sufficient to antagonize malonyl CoA inhibition of CPT-1. In yet another preferred mode, the agent is administered in an amount sufficient to increase malonyl CoA level.

Abstract: The present invention relates to novel diterpene compounds isolated from the fruiting body of Antrodia camphorate, especially to the new compounds of following structural formula: and pharmaceutically acceptable salt, solvate, hydrate or biologically active equivalent thereof. The present invention also relates to a pharmaceutical composition containing at least one of the novel diterpene compounds, and a use of the diterpene compound as a neuroprotective agent.

Abstract: The present invention provides methods of identifying agents that reduce a level of active APOBEC3C in a cell. The present invention provides agents that reduce a level of active APOBEC3C in a cell; and compositions comprising the agents. The present invention further provides methods of reducing the mutation rate of a lentivirus in a cell; and methods of reducing the emergence of drug-resistant strains of lentivirus. The present invention further provides methods for treating lentivirus infections.

Abstract: The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: wherein Ring A is aryl or heteroaryl; Q is cycloalkyl, heterocycle, alkyl or alkenyl; Ring T is heteroaryl or heterocycle; R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl or the like; R3 and R4 are independently hydrogen atom, hydroxy, oxo, halogen atom or the like; R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl or the like; or a pharmaceutically acceptable salt thereof.

Abstract: Aryl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed.

Abstract: The present invention relates to novel compounds from Antrodia camphorata and the use thereof.

Abstract: A method for inhibiting formation of adhesions following abdominal surgery which involves application of an anti-static fatty acid ethoxylated amide (Cocamide DEA) in a matrix that is placed in the peritoneal cavity at the conclusion of an abdominal surgery and which releases this anti-adhesive chemical over a predetermined time in a range from about five to seven days. Tests conducted on laboratory rats established that the method reduced the incidences of adhesions from 100 percent (100%) in a test model to near zero percent (0%) in the treated animals. In an alternative embodiment, Andrographalide was delivered through a drug pump with similar results. In still another embodiment, an effective amount of Rapamune was delivered, via a pump, into the abdominal cavity, again with similar results.

Abstract: Disclosed are neuroblastoma tumor-initiating cell inhibiting compositions comprising chemical entities capable of affecting neuroblastoma tumor-initiating cells. Pharmaceutical preparations that include these chemical entities are also provided for the treatment of neuroblastoma. These pharmaceutical preparations are suitable for the treatment of humans, and are particularly suited for the treatment of children of 12 years of age or younger having neuroblastoma. The compositions and pharmaceutical preparations posses reduced normal cell cytotoxicity. The compositions and pharmaceutical preparations may be used alone or together with other conventional neuroblastoma preparations as part of a clinical regimen in the treatment and management of neuroblastoma.

Abstract: The present invention provides a compound of formula I and the use thereof for the inhibition of bacterial cell wall biosynthesis and for the therapeutic treatment of bacterial infection or disease in a patient in need thereof. The present invention also provides the use of the formula I compound for the control of ecto- or endoparasites in homeothermic animals.

Abstract: An object of the present invention is to provide a composition for preventing harmful organisms exerting an excellent control effect against plant diseases and/or insecticidal effect.

Abstract: A method of treating weight loss due to underlying disease in a patient, the method comprising administering to the patient an effective amount of an agent which reduces sympathetic nervous system activity. A method of treating weight loss due to underlying disease in a patient the method comprising administering to the patient an effective amount of any one or more of the following: a compound which inhibits the effect of aldosterone such as an aldosterone antagonist; a chymase inhibitor; a cathepsin B inhibitor; a ? receptor blocker; an imidazoline receptor antagonist; a centrally acting ? receptor antagonist; a peripherally acting ? receptor antagonist; a ganglion blocking agent; a drug that has an effect on cardiovascular reflexes and thereby reduces SNS activity such as an opiate; scopolamine; an endothelin receptor antagonist; and a xanthine oxidase inhibitor. The methods are particularly useful in treating cardiac cachexia.

Abstract: The present invention relates to a pharmaceutical composition and health food comprising Phellinus sp. PL3 extract or phellinsin A isolated from the same as an effective component. More particularly, the present invention relates to a pharmaceutical composition and health food comprising Phellinus sp. PL3 extract or phellinsin A isolated from the same as an effective component, wherein the Phellinus sp. PL3 extract and its phellinsin A inhibit the oxidation of low density lipoprotein (LDL), and further, they can be used as a component for medicine and food to effectively prevent and treat cardiovascular diseases such as hyperlipemia and arteriosclerosis.

Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed, wherein n is 1 or 2; m is 0, 1, 2, 3 or 4; q is 0 or 1; t is 0 or 1; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, hydroxy, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula (

Abstract: The present invention pertains to the discovery that B. anthracis possesses a luxS gene that encodes a functional LuxS polypeptide, and that B. anthracis synthesizes a functional AI-2 quorum-sensing molecule. The invention provides mutant B. anthracis bacteria lacking the function of the luxS gene, which do not produce a functional AI-2 molecule and have growth defects compared to wild-type B. anthracis. The invention also concerns methods for inhibiting the growth of B. anthracis, or for preventing or treating B. anthracis infection, by inhibiting the activity of the B. anthracis LuxS polypeptide, or by exposure of the B. anthracis to furanone. In particular, the invention concerns the use of furanone, a compound that inhibits AI-2-mediated quorum-sensing, to inhibit the growth of B. anthracis, to inhibit B. anthracis toxin production, particularly that of protective antigen, and to prevent or treat B. anthracis infection. The invention also provides methods to prevent B.

Abstract: This invention provides methods and compositions for inducing weight loss and maintaining optimum weight comprising administering an agent that stimulates carnitine palmitoyl transferase-1 (CPT-1) activity to the patient in need, including human patients. These methods do not require inhibition of fatty acid synthesis. In particular, this invention provides methods for development of therapeutics that selectively enhance fatty acid oxidation, increase energy production, and reduce adiposity while preserving lean mass, through the pharmacological stimulation of CPT-1 activity. In a preferred mode, the agent is administered in an amount sufficient to increase fatty acid oxidation. In another preferred mode, the agent is administered in an amount sufficient to antagonize malonyl CoA inhibition of CPT-1. In yet another preferred mode, the agent is administered in an amount sufficient to increase malonyl CoA level.

Abstract: The present invention relates to oxacyclopentene-2 derivatives as compounds possessing antiinflammatory, neuroprotective, immunomodulatory and cardiovascular activities in mammals.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, B, D, Z, R1, R2a, R2b, and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.

Abstract: The present invention provides S-(?)-tulipalin B, acetylated-S-(?)-tulipalin B and an antibacterial composition comprising the same. The active compound tulipalin B and composition of the present invention exhibit superior and stable antibacterial activity over a broad range of temperature and pH, as compared to conventional natural antibacterial agents used in related industries. Therefore, the composition and active compound of the present invention can be widely used as a natural food preservative and/or an antibacterial agent in a variety of fields such as foods, pharmaceuticals, cosmetics, fibers, livingwares, and the like.

Abstract: The invention is directed to a method for treating a cyclooxygenase-2 mediated disease or condition in a mammalian patient at risk of a thrombotic cardiovascular event, wherein the patient is on aspirin therapy to reduce the risk of the thrombotic cardiovascular event, comprising orally concomitantly or sequentially administering to the patient a cyclooxygenase-2 selective inhibitor in an amount effective to treat the cyclooxygenase-2 mediate disease or condition, and a nitric oxide donating compound in accordance with Formula I or a pharmaceutically acceptable salt thereof, wherein the nitric oxide donating compound is administered in an amount effective to reduce the gastrointestinal toxicity caused by the combination of the cyclooxygenase-2 selective inhibitor and aspirin. Pharmaceutical compositions are also encompassed.

Abstract: This invention relates to compositions and methods for the treatment of neurodegenerative, pulmonary and inflammatory diseases described herein with glutathione peroxidase and its mimetics.

Abstract: The present invention relates to methods, compositions and their constituents for inhibiting 5-Lipoxygenase (5-LO), 15-Lipoxygenase (15-LO), cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), in living organisms. More particularly, the present invention relates to methods and compositions involving the inhibition of 5-Lipoxygenase (5-LO), 15-Lipoxygenase (15-LO), cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), using processed Morinda citrifolia L. plant products.

Abstract: The present invention generally relates to refreshing, soothing, and cooling compounds that affect sensory processes. More particularly, the present invention pertains to certain N-alkylcarbonyl-amino acid ester and N-alkylcarbonyl-amino lactone compounds as described herein; compositions and articles comprising such compounds; and methods of treatment, for example, methods of alleviating the discomforts of irritation, itch, and pain in the skin and in the linings of the oral cavity and upper respiratory tract, for example, in methods of treatment of cough and/or asthma.

Abstract: This invention provides methods for detecting or inferring the presence of malignant or premalignant cells in a human wherein the malignant or premalignant cells express COX-2. The methods of the invention detect extracellular COX-2 RNA in blood, plasma, serum, and other bodily fluids. The inventive methods are useful for aiding detection, diagnosis, monitoring, treatment, or evaluation of neoplastic disease, and for identifying individuals for whom COX-2 directed therapies would be beneficial.

Abstract: Compounds of the Formula I, wherein A1 is O or NH; A2 is O or S; each of R1 and R2 is independently hydrogen, a methyl or C2-C8-saturated or mono- or doubly unsaturated, branched or linear hydrocarbon group; and R3 is a C1-C18-saturated or mono- or doubly unsaturated, branched or linear hydrocarbon group wherein, each of R1, R2 and R3 comprises a heteroatom selected from the group consisting of O and S in the chain and/or is mono- or multiply-substituted by a substituent selected from the group consisting of halogen, hydroxy, C1-C6-alkyl, trifluoromethyl, C1-C6-alkoxy, C6-C10-aryl, and C1-C6-alkyl-C6-C10-aryl are useful for controlling the interaction process between microorganisms such as in the development and/or maturation of biofilms; multicellular swarm behavior; the concerted development of antibiotic resistances; the concerted synthesis of antibiotics; the concerted synthesis of pigments; the concerted production of extracellular enzymes; or the concerted production of virulence factors.

Abstract: The present invention relates to the use of selective insecticidal and/or acaricidal compositions, characterized in that they comprise an effective amount of an active compound combination comprising (a) at least one substituted cyclic dicarbonyl compound of the formula (I) in which W, X, Y and Z are as defined in the description and CDC is one of the dicarbonyl radicals mentioned in the description, and (b) at least one crop plant compatibility-improving compound from the group of compounds given in the description. for controlling insects and/or arachnids, and also to a method for controlling insects and/or arachnids using the compositions.

Abstract: The present invention provides a cosmetic mineral foundation, which is a pressed powder, comprising unfermented green rooibos extract (aspalathus linearis leaf), which functions as an antioxidant, and helps reduce the appearance of fine lines and wrinkles, and diminish signs of aging caused by free-radical damage. The foundation is gentle for all skin types, can be used daily, and provides effective anti-aging treatment as well as quality skin coverage.

Abstract: The invention relates to a method for selecting COX-2 selective NSAIDs which have a salutary therapeutic profile. The invention further relates to the use of these selected COX-2 selective NSAIDs in the treatment of certain diseases. The invention yet further relates to combinations comprising COX-2 selective NSAIDs and the use of these combinations.

Abstract: The present invention relates to the side chain functionalization of fimbrolides (halogenated 3-alkyl-5-methylene-2(5H)-furanones) and their synthetic analogues, that yields fimbrolides substituted with a halogen, an oxygen or a nitrogen functionality in the alkyl chain, especially fimbrolide alcohols, caboxylate and sulfinate and sulfonate esters, ethers, aldehydes, ketones, acids, amides, nitro derivatives, hydrophobic, hydrophilic and fluorophilic alkyl derivatives and polymers.

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 invention pertains to a method and compositions for treatment or prevention of chronic pulmonary dysfunction in a patient.

Abstract: The present invention is directed to a novel pharmaceutical composition suitable for ophthalmic use comprising nanoparticles dispersed in a liquid dispersion medium, wherein said nanoparticles comprise a cyclooxygenase-2 selective inhibitor having adsorbed on the surface thereof at least one surface stabilizer. The ophthalmic formulation of the present invention is stable, non-irritating and sufficiently bioavailable. The invention also encompasses a process for making as well as a kit for preparing the novel ophthalmic formulation.

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.