Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by clear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: The invention relates to oxazine derivatives by means of which a broad spectrum of material to be examined can be marked and identified using fluorescence techniques.

Abstract: The invention features sulfhydryl rifamycin compositions, methods of making these compositions, and methods for treating disease using these compositions.

Abstract: The present invention provides a compound of the formula (I) and pharmaceutically acceptable salts having useful antiviral activity against viruses of the herpes family. In said formula, X=O, (CH2)m, S, SO, SO2, NH, NR8 or a chemical bond; Y=O, (CH2)m, S, SO, SO2, NH, NR8; Z=NH, O, NR8, S, SO, SO2. The remaining substituents are described in the specification.

Abstract: Inhibition of RNA function, and treatment or control of diseases or conditions, e.g. infectious diseases such as viruses and viral infections (including HIV) and microbial infections, by the contacting of the RNA with a compound having a central or core structure comprising three fused rings containing from 12 to 15 ring atoms, the central ring including at least one heteroatom selected from nitrogen, oxygen and sulfur, the atoms of the three-ring core structure being optionally substituted with substituents such as halogens, cyano, and/or various substituted or unsubstituted aliphatic and/or heteroaliphatic moieties, or contacting the RNA with yohimbine, usnic acid or N-{4-[2,5-Dioxo-1-(4-trifluoromethoxy-phenyl)-pyrrolidin-3-yl]-phenyl}-2,2,2-trifluoro-acetamide. Preferred compounds are various phenothiazines, including both known and novel compounds.

Abstract: A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, 1

Abstract: The present invention is concerned with combinations of a farnesyl transferase inhibitor and two or more further anti-cancer agents for inhibiting the growth of tumor cells and useful in the treatment of cancer.

Abstract: The invention provides methods and use of heterocyclic amines, and phenylazacycloalkane compounds, and their pharmacologically acceptable salts for the treatment of Restless Legs Syndrome (RLS).

Abstract: The present invention relates to a group of aza-thioxanthenone compounds having antitumor activity, and processes for their preparation. Compositions containing the aza-thioxanthenone compounds and methods of treating tumors and cancer in mammals with the compounds of the present invention are also disclosed.

Abstract: A method for treatment of bacterial infections with rifalazil administered once-weekly, or twice-weekly. A method for treatment of tuberculosis caused by Mycobacterium tuberculosis, infections caused by Mycobacterium avium complex, infections caused by Chlamydia pneumoniae and infections caused by Helicobacter pylori by administering to a patient suffering from the bacterial infection 1-100 mg of rifalazil once or twice a week. In this dose regimen, the treatment is fast, efficacious and eliminates undesirable secondary symptoms observed with daily doses of 1-50 mg of rifalazil.

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

Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist and an arylpyrrole insecticide. Also provided are methods for synergistic insect control and crop protection.

Abstract: Compounds, pharmaceutical compositions, and methods for modulating processes mediated by steroid receptors. In particular, preparation and methods of use of non-steroidal compounds and compositions that are agonists, partial agonists, and antagonists for the androgen receptor (AR) are described. Further, described are the methods of making and use of critical intermediates including a stereoselective synthetic route to intermediates for the AR modulators.

Abstract: A phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative represented by formula (I) 1

Abstract: The present invention relates to new derivatives of amino acids and their use as medicaments.

Abstract: The present invention relates to novel &bgr;-carboline derivatives of the general formula 1

Abstract: The present invention relates to water-containing formulations for the dermal control of parasitic insects on animals, having the following composition

Abstract: Pirenoxine or 1-hydroxy-5-oxo-5H-pyrido-[3,2a]-phenoxazin-3-carboxylic acid, also called pirfenossone and already used as anti-cataract agent, in the form of a pharmaceutically acceptable salt thereof, if desired, is used for the protection of the corneal tissue in photokeratectomy interventions, as cornea photoablation using excimer laser, for both refractive and therapeutic purpose. In fact pirenoxine is able to inhibit, in the cornea, the oxidative phenomena determined by reactive oxygen species (ROS) which are produced within the tissues following the laser irradiation.

Abstract: The invention relates to crystalline anhydrous (1&agr;,2&bgr;,4&bgr;,5&agr;,7&bgr;)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.022,4]nonane-bromide, processes for preparing it and its use for preparing a pharmaceutical composition, particularly for preparing a pharmaceutical composition with an anticholinergic activity.

Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animal, such as stroke.

Abstract: The present invention is directed to a procedure for making an enantiomerically enriched compound containing a hydronaphthalene ring structure. The process involves reacting oxabenzonorbornadienes with nucleophiles using rhodium as a catalyst and in the presence of a phosphine ligand. The compounds synthesized may be used in pharmaceutical preparations for the treatment of a variety of diseases and conditions.

Abstract: The present invention is concerned with combinations of two or more farnesyl transferase inhibitors for inhibiting the growth of tumour cells and useful in the treatment of cancer.

Abstract: The present invention is drawn to methods and compounds for photodynamic therapy (PDT) of a target tissue or compositions in a mammalian subject, using a light source that preferably transmits light to a treatment site transcutaneously. The method provides for administering to the subject a therapeutically effective amount of a photosensitizing agent. This photosensitizing agent preferentially associates with the target tissue. Light at a wavelength or waveband corresponding to that which is absorbed by the photosensitizing agent is then administered. The light intensity is relatively low, but a high total fluence is employed to ensure the activation of the photosensitizing agent.

Abstract: The invention provides compounds of Formula I: 1

Abstract: The present invention is concerned with combinations of a farnesyl transferase inhibitor and a camptothecin compound for inhibiting the growth of tumor cells and useful in the treatment of cancer.

Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke.

Abstract: Tablets and capsules wherein the content of active ingredient in the tablet or capsule is not more than about 3% (weight/weight) can be prepared if microcrystalline cellulose and silicon dioxide are used as some of the starting materials.

Abstract: This invention relates to novel polymorphic/pseudopolymorphic forms of arginine salt of 3-[4-[2-(phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid, having the formula I shown below. The invention also relates to a pharmaceutical composition comprising the novel polymorphic form or their mixture and a pharmaceutically acceptable carrier. The polymorphic forms of the present invention are more active, as antidiabetic and hypolipidemic agent, than the novel 3-[4-[2-(phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid.

Abstract: The invention relates to hydroxamic and carboxylic acid derivatives.

Abstract: Disclosed are compounds which are conjugates of (a) a moiety capable of localizing in the cells of a tumor or atheroma and (b) a moiety capable of catalyzing the production of reactive oxygen species from a cellular metabolite. The disclosed compounds which are useful for treating atheroma, tumors and other neoplastic tissue.

Abstract: A method is disclosed for the prevention and treatment of Alzheimer's disease by administering to a human in need thereof an effective amount of a substituted tricyclic sPLA2 inhibitor.

Abstract: The present invention provides methods and compositions for treatment and/or prevention of type 1 and type 2 diabetes, dyslipdemia, impaired glucose tolerance, insulin resistance, obesity, and beta-cell apoptosis, as well as methods for increasing the size and number of beta-cells in a subject and/or stimulating beta-cell proliferation, which comprise administering both a stable GLP-1 analogue and a non-thiazolidinedione PPAR ligand.

Abstract: The invention provides compounds which are PDE7inhibitors, having the following formula (I), (II) and (III) 1

Abstract: Novel non-steroidal tricyclic quinolinone and tricyclic quinoline compounds and compositions that are agonists, partial agonists and/or antagonists for androgen receptors (AR), their preparation and their uses are described.

Abstract: The present invention relates to pharmaceutically acceptable salts of compound of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.

Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: Compounds, pharmaceutical compositions, and methods for modulating processes mediated by steroid receptors. In particular, preparation and methods of use of non-steroidal compounds and compositions that are agonists, partial agonists, and antagonists for the androgen receptor (AR) are described. Further, described are the methods of making and use of critical intermediates including a stereoselective synthetic route to intermediates for the AR modulators.

Abstract: Disclosed are compounds of the Formula I 1

Abstract: Described are compounds and a method of inhibiting epidermal growth factor receptor tyrosine kinase by treating, with an effective inhibiting amount, a mammal, in need thereof, a compound of Formula II: where: one of A or E is nitrogen, with remaining atoms carbon; X=O, S, NH or NR7, such that R7=lower alkyl (1-4 carbon atoms), OH, NH2, lower alkoxy (1-4 carbon atoms) or lower monoalkylamino (1-4 carbon atoms). Other terms are described in the specification.

Abstract: A compound of formula (1) it derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts, or its pharmaceutically acceptable solvates, processes for its preparation and methods of use thereof.

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

Abstract: A phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative represented by formula (I) 1

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

Abstract: The present invention relates generally to the non-enzymatic glycosylation of amyloidogenic proteins and the consequent formation of advanced glycosylation endproducts (AGEs). It has been found that formation of AGE-amyloidogenic proteins can enhance amyloidosis. The invention further relates to compositions and methods for the prevention and treatment of amyloidosis associated with amyloid diseases, particularly neurodegenerative disease and Type II diabetes, and more particularly Alzheimer's disease. In a specific example, aggregation of an amyloidogenic peptide, &bgr;AP, is enhanced by the glycosylation reaction of &bgr;AP to form AGE-&bgr;AP as defined herein. Accordingly, the invention extends to a method for modulating the in vivo aggregation of amyloid polypeptides and associated amyloidosis by controlling the formation and presence of AGE-amyloid polypeptide.

Abstract: Disclosed are novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula 1 are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) including PTP1B, T cell PTP, wherein n, m, X, R1, R2, R3, R4, R5, R6, and R7 are defined more fully in the description. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.

Abstract: Novel &bgr;-aryl-&agr;-oxysubstituted alkylcarboxylic acids of the formula (I) and compositions containing them.

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

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

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

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