Abstract: The present invention provides methods of modulating cell junctions via the Gp140 membrane protein. Gp140 agonists and antagonists are provided, including activating and non-activating antibodies of Gp140, as well as compositions including the same. Methods of treatment including administration of a Gp140 agonist or antagonist are also provided. Finally, implants having a Gp140 modulator coupled thereto are provided.

Abstract: Benzocycloheptyl analogs that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs, which, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: Azo dyes and suramin-related small molecules are effective in inhibiting the CD40/CD154 protein-protein interaction, an important co-stimulatory interaction involved in the activation of immune responses mediated by T- and B-cells. The compounds were found to be active as indicated by their IC50 values both in a cell-free binding assay and in the inhibition of CD154-induced B-cell proliferation assay. The compounds may be used as therapeutic compounds for treatment of diseases and disorders related to immune or inflammatory responses. Methods of inhibiting the CD40/CD154 protein-protein interaction and treating diseases and disorders related to immune or inflammatory responses are described.

Abstract: Disclosed herein are compositions and methods for promoting the repair and regeneration of injured tissues, such as injuries resulting from ischemic damage. Also disclosed are compositions and methods for accelerating wound healing in diabetic and elderly patients and inhibiting allograft failure.

Abstract: Wrinkles are improved by applying an oral preparation, injection preparation or external skin preparation having a substance that controls heparanase as an active ingredient thereof.

Abstract: Dermatological disorders having an inflammatory or proliferative component, notably common acne, are treated with topically applicable pharmaceutical compositions containing about 0.3% by weight of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthanoic acid (adapalene) or salt thereof, formulated into pharmaceutically acceptable media therefor, advantageously formulated into topically applicable gels, preferably aqueous gels, creams, lotions or solutions.

Abstract: The mechanism by which the high bone mass (HBM) mutation (G171V) of the Wnt coreceptor LRP5 regulates the canonical Wnt signaling was investigated. The mutation was previously shown to reduce Dkk protein-1-mediated antagonism, suggesting that the first YWTD repeat domain where G171 is located may be responsible for Dkk protein-mediated antagonism. However, we found that the third YWTD repeat, but not the first repeat domain, is required for DKK1-mediated antagonism. Instead, we found that the G171V mutation disrupted the interaction of LRP5 with Mesd, a chaperon protein for LRP5/6 that is required for the coreceptors' transport to cell surfaces, resulting in less LRP5 molecules on the cell surface. Although the reduction in the level of cell surface LRP5 molecules led to a reduction in Wnt signaling in a paracrine paradigm, the mutation did not appear to affect the activity of coexpressed Wnt in an autocrine paradigm.

Abstract: The present invention relates to the field of therapeutic methods to screen for compounds on the basis of their ability to influence Wnt activity. The screening process is applied to both a physical library of a series of compounds and a virtual library of compounds that affect Wnt activity. In one aspect, the virtual screening process could be carried out where a permutational library of small peptides is substituted for the small organic molecules. The inventive methods may be used to empirically test for effects on Wnt activity and may also be applied to any pair of proteins involved in protein-protein interactions.

Abstract: Dermatological disorders having an inflammatory or proliferative component are treated with pharmaceutical compositions containing on the order of 0.3% by weight of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthanoic acid (adapalene) or salt thereof, formulated into pharmaceutically acceptable media therefor, advantageously topically applicable gels, creams or lotions.

Abstract: Dermatological disorders having an inflammatory or proliferative component are treated with pharmaceutical compositions containing on the order of 0.3% by weight of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthanoic acid (adapalene) or salt thereof, formulated into pharmaceutically acceptable media therefor, advantageously topically applicable gels, creams or lotions.

Abstract: This invention relates to novel benzamide derivatives that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels.

Abstract: Chemically functionalized fullerenes are useful in various applications as radical scavengers. These chemically functionalized fullerenes offer the advantages of preservation of the high innate radical scavenging efficiency of the fullerene cage and ease of synthesis of fullerene derivatives of desirably altered chemical and physical properties and single isomers. Further, they are based on a common intermediate chemistry and intermediates can be easily functionalized and tailored to various requirements.

Abstract: The present invention provides methods for treating neurological diseases and disorders. Compounds that replace or enhance the function of SMN or alleviate or reduce a phenotype of cells with low SMN protein levels are provided. Screening methods and kits for identifying such compounds also are provided.

Abstract: Dermatological disorders having an inflammatory or proliferative component, notably common acne, are treated with topically applicable pharmaceutical compositions containing about 0.3% by weight of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthanoic acid (adapalene) or salt thereof, formulated into pharmaceutically acceptable media therefor, advantageously formulated into topically applicable gels, preferably aqueous gels, creams, lotions or solutions.

Abstract: The use of a substance belonging to the class of atypical retinoids for the topical treatment of acne is described. In particular the effects on an animal model for this skin disease of a pharmaceutical or cosmetic compound for topical use containing adamantyl methoxydiphenyl propenoic acid formulated in a gel are demonstrated.

Abstract: The invention relates to the use of derivatives of sulphonic acid (I) or one of the pharmaceutically-acceptable prodrugs or salts thereof in the preparation of a medicament for the treatment of vasoproliferative ocular diseases, said sulphonic acid having formula (I).

Abstract: Benzocycloheptyl analogs that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs, which, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: The present invention relates to a method of treating and preventing a papillomavirus infection in an individual, comprising administering to the individual a therapeutically effective amount of a condensation polymer of an aromatic sulfonic acid and an aldehyde, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention is directed to methods of inhibiting STDs by topically administering suramin or a derivative thereof to actual or potential sites of infection, and methods of preventing pregnancy by topically applying suramin or a derivative thereof intravaginally. Suramin compositions that include an antimicrobial agent and/or a sperm-function inhibitor are also provided and may advantageously be used in the methods of the invention. A method of simultaneously inhibiting STDs and preventing pregnancy is also provided. Devices impregnated or coated with the topical suramin compositions are further disclosed and may be used to apply the compositions described herein.

Abstract: Dermatological disorders having an inflammatory or proliferative component are treated with pharmaceutical compositions containing on the order of 0.3% by weight of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthanoic acid (adapalene) or salt thereof, formulated into pharmaceutically acceptable media therefore, advantageously topically applicable gels, creams or lotions.

Abstract: The present invention relates to a series of new chemical agents that demonstrate anti-tumor activity. More particularly, the present invention relates to molecules, referred to as “combi-molecules”, that combine two major mechanisms of anti-tumor action. A combi-molecule is capable of degrading to a ligand involved in cell signaling pathways and to an agent capable of damaging DNA. More specifically, the present invention relates to molecules capable of blocking epidermal growth factor receptor (EGFR) mediated signal transduction and capable of damaging DNA. The present invention also relates to a general method of synthesis of these combi-molecules.

Abstract: Epimeredinoside A extracted from Epimeredi indica root, oral pharmaceutics made up with the Epimeredi indica root extract and at least one pharmaceutical adjuvant, and preparatory method for the oral pharmaceutics. The root extract is the extracta sicca prepared by water extraction and concentration of Epimeredi indica root, and contains 0.10% to 1.50% of epimeredinoside A. The inventive pharmaceutics of Epimeredi indica root extract do not contain any hormone and progesterone is not needed to be taken to prevent a side effect after using the drug. The pharmaceutics has doubtless effect in treating female menopause.

Abstract: The present invention is directed to methods of inhibiting STDs by topically administering suramin or a derivative thereof to actual or potential sites of infection, and methods of preventing pregnancy by topically applying suramin or a derivative thereof intravaginally. Suramin compositions that include an antimicrobial agent and/or a sperm-function inhibitor are also provided and may advantageously be used in the methods of the invention. A method of simultaneously inhibiting STDs and preventing pregnancy is also provided. Devices impregnated or coated with the topical suramin compositions are further disclosed and may be used to apply the compositions described herein.

Abstract: Dermatological disorders having an inflammatory or proliferative component are treated with pharmaceutical compositions containing on the order of 0.3% by weight of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthanoic acid (adapalene) or salt thereof, formulated into pharmaceutically acceptable media therefor, advantageously topically applicable gels, creams or lotions.

Abstract: The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful in the treatment, including prevention, of obesity, diabetes and a number of diseases or disorders associated therewith.

Abstract: The present invention provides, inter alia, triphenylethylene derivatives, such as, 3-{4-[6-(3-Methoxy-phenyl)-8,9-dihydro-7H-benzocyclohepten-5-yl]-phenyl}-acrylic acid, as selective estrogen receptor modulators. Also provided are methods for treating estrogen stimulated diseases in mammals including, but not limited to, for example, breast, uterine, ovarian, prostate and colon cancer; osteoporosis; endometriosis; uterine fibroid; Alzheimer's disease; macular degeneration; urinary incontinence; and type II diabetes, as well as, pharmaceutical compositions comprising at least one compound of the present invention.

Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.

Abstract: The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by ghrelin including anorexia, cancer cachexia, eating disorders, age-related decline in body composition, weight gain, obesity, and diabetes mellitus.

Abstract: New thyroid receptor ligands are provided which have the general formula in which: X is —O—, —S—, —CH2—, —CO—, or —NH—; Y is —(CH2)n— where n is an integer from 1 to 5, or cis- or trans-ethylene; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 6 carbons, at least one of R2 and R3 being other than hydrogen; R4 is hydrogen or lower alkyl; R5 is hydrogen or lower alkyl; R6 is carboxylic acid, or esters or prodrugs; R7 is hydrogen or an alkanoyl or an aroyl. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.

Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis or apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.

Abstract: The topical use of ursolic acid compounds to alter the lipid content of mammalian skin is disclosed. The compounds can be encapsulated in liposomes and administered in this form to the skin in, for example, a lotion or a gel. The compounds are effective in, among other things, reducing the effects of aging, photoaging, and skin atrophy, including skin atrophy resulting from the topical use of retinoids and/or steroids. Compositions comprising a ursolic acid compound in combination with another therapeutically active topical compounds, such as, a retinoid or a steroid, are also disclosed.

Abstract: This invention relates to biocidal compositions and methods of using same. Also provided is a process for the manufacturing of a biocidal composition in the form of a tablet and a method of using the biocidal compositions for the disinfection of water that may contain microorganisms and biofilms.

Abstract: We have now discovered that certain 9,10-anthraquinone derivatives we developed possess potent activity against O. perornata while possessing a sufficiently high level of solubility in water to make their activity against O. perornata viable. These compounds possess a high level of activity against O. perornata yet are relatively non-toxic to green algae and fishes. The compounds also possess a relatively short half-life. The compounds represent a new means to providing compounds possessing a high degree of selective activity against blue-green algae while being physiologically tolerated by catfish and green algae. The compounds provide a means for controlling blue-green algae in managed bodies of water that are destined for public use or consumption.

Abstract: A liposome formulation containing about 1% diclofenac is an effective topical anti-inflammatory topical treatment for lameness in horses. More particularly it has been discovered that a formulation containing vitamin E, phospholipid and diclofenac salt such as the sodium or potassium salt is a highly effective topical anti-inflammatory formulation that is particularly effective in treating lameness in horses.

Abstract: The present invention relates to a composition comprising an organic preservative acid and a UV-active indicator substance for preserving wood and for detection of the sufficient preservation of wood.

Abstract: Disclosed herein are novel tricyclic diterpene compounds. These compounds, including their prodrug esters and acid-addition salts, are useful as Interleukin-1 and Tumor Necrosis Factor-? modulators, and thus are useful in the treatment of various diseases. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of the novel compounds that are useful as anti-inflammatory analgesics, in treating immune disorders, as anti-cancer and anti-tumor agents, and in the treatment of cardiovascular disease, skin redness, and viral infection. Completely synthetic and semi-synthetic methods of making the compounds and their analogs are also disclosed, as are methods of using these synthetic and semi-synthetic compounds in the treatment of the above-listed disease states.

Abstract: New thyroid receptor ligands are provided which have the general formula in which: X is —O—, —S—, —CH2—, —CO—, or —NH—; Y is —(CH2)n— where n is an integer from 1 to 5, or cis- or trans-ethylene; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 6 carbons, at least one of R2 and R3 being other than hydrogen; R4 is hydrogen or lower alkyl; R5 is hydrogen or lower alkyl; R6 is carboxylic acid, or esters or prodrugs; R7 is hydrogen or an alkanoyl or an aroyl. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.

Abstract: The compounds of formula I-IV: wherein n is an integer of from 1 to 4, or pharmaceutically acceptable salts thereof are useful to prevent and treat visceral pain and gastrointestinal disorders.

Abstract: Disclosed is a plant-derived flavonol-containing dry composition suitable for human consumption, wherein at least 25% of the plant-derived material in the composition comprises polyphenols, together with uses thereof.

Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.

Abstract: A method of controlling target aquatic microorganism pest populations by exposing the target population to a toxic amount of an aquacidal compound comprising an anthraquinone. The method is particularly effective for treating ballast water of ships or other enclosed volumes of water subject to transport between or among geographic areas to control the relocation of plants, toxic bacteria, and animals contained in the water.

Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.

Abstract: Novel glucocorticoid and thyroid receptor ligands as provided which have the general formula (I): in which R1 is an aliphatic hydrocarbon, an aromatic hydrocarbon, carboxylic acid or ester thereof, alkenyl carboxylic acid or ester thereof, hydroxy, halogen, or cyano, or a pharmaceutically acceptable salt thereof. R2 and R3 are the same or different, and are hydrogen, halogen, alkyl of 1 to 4 carbons, or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen. X is carbonyl or methylene. R4 is an aliphatic, aromatic or heteroaromatic. Y is hydroxyl, methoxy, amino, or alkyl amino. n is an integer from 0 to 4. A method for treating diseases associated with metabolism dysfunction or which are dependent on the expression of a glucocorticoid or thyroid receptor gene such as diabetes, hypercholesterolemia, or obesity using these compounds is also disclosed.

Abstract: The invention is directed to pharmaceutical compositions useful in the treatment of migraine. The compositions contain metoclopramide and one or more NSAIDs in unit dosage form. By selecting NSAIDs that are non-acidic or segregating the metoclopramide and NSAID, the storage life of the compositions has been increased. Also disclosed are coordinated dosage forms for the sequential release of drugs. The invention encompasses methods of treating migraine using any of these dosage forms.

Abstract: The present disclosure relates to novel compositions which provide improved nutritional support for premenopausal and menopausal women and/or relief from symptoms associated with menopause, as well as prophylactic effects, and methods for using same.

Abstract: The present invention is directed to aromatic derivatives of formula (I), wherein: R1 is (a), wherein R3 and R4 are selected from between H and OH, provided that R3 and R4 are not simultaneously H, and R2 is H; or R1 and R2 taken together, are (b), wherein R5 is selected from between CH3 and (CH2)5OH, to the iron complexes thereof, and to their use for the preparation of pharmaceutical compositions for the normalization of iron level.

Abstract: The present invention relates to a novel pharmaceutical formulation for the topical application of drugs, particularly non-steroidal anti-inflammatory drugs (NSAID's), comprising a therapeutically effective amount of a drug, sodium phosphate buffer, and, optionally, an alcoholic solvent. It has been found that by the addition of sodium phosphate buffer to such formulations, the permeation of the NSAID can be significantly improved.

Abstract: Preparations and extracts of valerian, as well as isovaleramide, isovaleric acid, and its pharmaceutically acceptable salts, esters, and substituted amides, and other valerian-related compounds, in combination with NSAIDs exhibit clinically significant pharmacological properties which implicate a treatment for acute muscular aches, strains, and sprains which occur from a localized, external insult to a particular muscle or muscle group outside of, or peripheral to, the CNS. The compositions in question generally are non-cytotoxic and do not elicit weakness or sedative activity at doses that are effective for the symptomatic treatment of such pathological conditions.

Abstract: Uses of topical compositions comprising a 2-hydroxycarboxylic acid or related compound to alleviate or improve signs of skin, nail and hair changes associated with intrinsic or extrinsic aging are disclosed. 2-Hydroxycarboxylic acids and their related compounds include, for example, 2-hydroxyethanoic acid, hydroxypropanoic acid, 2-methyl 2-hydroxypropanoic acid, 2-phenyl 2-hydroxyethanoic acid, 2-phenyl 2-methyl 2-hydroxyethanoic acid, 2-phenyl 3-hydroxypropanoic acid, 2,2-diphenyl 2-hydroxyethanoic acid, 2-hydroxybutane-1,4-dioic acid, 2,3-hihydroxybutane-1,4-dioic acid, 2-carboxy 2-hydroxypentane-1,5-dioic acid, 2-ketopropanoic acid, methyl 2-ketopropanoate, ethyl 2-ketopropanoate, and gluconolactone.

Abstract: Novel compounds are disclosed that have the chemical structure of Formula (IIB), and its prodrug esters and acid-addition salts, and that are useful as Interleukin-1 and Tumor Necrosis Factor-&agr; modulators, and thus are useful in the treatment of various diseases. wherein the R groups include the following: R1 is selected from the group consisting of hydrogen, a halogen, COOH, C1-C12 carboxylic acids, C1-C12 acyl halides, C1-C12 acyl residues, C1-C12 esters, C1-C12 secondary amides, (C1-C12)(C1-C12) tertiary amides, C1-C12 alcohols, (C1-C12)( C1-C12) ethers, C1-C12 alkyls, C1-C12 substituted alkyls, C2-C12 alkenyls, C2-C12 substituted alkenyls; R2 is selected from hydrogen, a halogen, C1-C12 alkyl, C1-C12 substituted alkyls, C2-C12 alkenyl, C2-C12 substituted alkenyl, C2-C12 alkynyl, and C1-C12 acyl, and C5-C12 aryl.