Abstract: Disclosed herein are a method of inhibiting hair growth, which comprises administering an inhibitor of elastase-like enzymes or a neutral endopeptidase inhibitor, and use of an inhibitor of elastase-like enzymes or a neutral endopeptidase inhibitor for the preparation of a hair-growth inhibitor.

Abstract: The present invention is related to new substituted pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of neurodegenerative disorders, diseases associated with polygultamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders renal hypoxia, hepatitis and AIDS. Said pyrrolidine derivatives display a modulatory and most notably a down-regulating-up to an inhibitory-activity with respect to the cellular death agonist Bax and/or the activation pathways leading to Bax and allows therefore to block the release of cytochrome (c).

Abstract: Pharmaceutical compositions for treating bone lesions in multiple myeloma or pharmaceutical compositions for treating multiple myeloma which contain as an active ingredient a compound having both of an effect of suppressing bone resorption accompanying multiple myeloma and an effect of inhibiting multiple myeloma, more particularly, 1-hydroxy-2-(imidazo[1,2-a]pyridin-3-yl)ethane-1,1-bisphosphonic acid or its salt.

Abstract: The present invention provides novel phosphate derivatives having the general Formula I wherein the wavy bond () represents the racemate, the (R)-enantiomer or the (S)-enantiomer and A, B, R1, R2, R3, R4, m and n are as defined herein, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of potassium channels.

Abstract: The invention is directed to 4h-benzo[1,4]oxazin-3-ones useful as peroxisome proliferator activated receptor gamma (PPAR?) agonists or antagonists. Pharmaceutical compositions comprising compounds of the present invention and methods of treating conditions such as NIDDM and obesity are also disclosed.

Abstract: The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a partially unsaturated bicyclic heterocyclic ring structure, and B represents an aryl or a heteroaryl group. Preferred compounds of the present invention comprise a benzimidazole or indole nucleus. The compounds of this invention are inhibitors of serine proteases, Urokinase (uPA), Factor Xa (FXa), and/or Factor VIIa (FVIIa), and have utility as anti cancer agents and/or as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals.

Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.

Abstract: Novel pyridinones and their derivatives which are effective in treating or preventing Gram-negative bacterial infections are provided. The pyridinones are stable and easily derivatized; the methods by which these derivatizations occur is described. Two regioselective and functional group tolerant methods for the synthesis of the novel pyridinones are also provided. One such synthetic method involves reacting an imine and a Meldrum's acid derivative in solution. The other synthetic method is a solid phase synthesis of the pyridinones in which an imine is prepared bound to a solid support and a Meldrum's acid derivative is reacted with the imine. Novel imine intermediates useful in the solid phase and solution methods of synthesizing the pyridionones are also described.

Abstract: This invention provides PAI-1 inhibiting compounds of Formula I: 1

Abstract: Methods and compositions utilizing compounds represented by Formula III, 1

Abstract: The present invention relates to the use of nucleoside derivatives of formula I 1

Abstract: Composition and methods are disclosed that include a synergistic combination of an inhibitor of Herpes simplex virus thymidine kinase, and an antiherpes substance.

Abstract: The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and methods for their use.

Abstract: Chiral ligands and metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The metal complexes according to the present invention are useful as catalysts in asymmetric reactions, such as, hydrogenation, hydride transfer, allylic alkylation, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, olefin metathesis, hydrocarboxylation, isomerization, cyclopropanation, Diels-Alder reaction, Heck reaction, isomerization, Aldol reaction, Michael addition; epoxidation, kinetic resolution and [m+n] cycloaddition. Processes for the preparation of the ligands are also described.

Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.

Abstract: This invention relates to the prevention and treatment of obesity.

Abstract: The present invention describes a method for programming a specific course and rate of metabolism for a parent drug compound that leads to an inactive or very weakly active and nontoxic metabolite when the modified drug compound is administered.

Abstract: Compounds of the formula I 1

Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.

Abstract: Glutamate antagonists (NMDA, AMPA and kainate receptor antagonists) and their physiologically compatible salts can be used for the preparation of drugs for treatment of cancer.

Abstract: The present invention is directed to a class indolinone compounds, hexahydro-cyclohepta-pyrrole oxindoles, which are useful as protein kinase inhibitors.

Abstract: A method for preventing loss of bone mineral in mammals which method comprises administering to a mammal an amount of an aminoalkylenephosphonate which is effective to prevent or minimize loss of bone material density. The aminoalkylenephophonates of the present invention should have at least one R-N(Alk-PO3H2)2 group or at least two RRN-Alk-PO3H2 groups wherein R and R can be, same or different, aliphatic or cyclic moiety, and Alk is an alkylene group having from 1 to 4 carbon atoms.

Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.

Abstract: Compounds of the following formula are disclosed: 1

Abstract: The invention relates to compounds of the general formula (and pharmaceutically acceptable derivatives thereof): 1

Abstract: The present invention relates to a method for treating a disease, comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a fullerene. The diseases treated comprise bacterial and viral diseases such as those cause by Gram positive and Gram negative bacteria, Dengue 2 virus and viral encephalitis. The fullerene is administered in vivo in an amount of about 0.001 to about 100 mg/kg of body weight of the subject.

Abstract: This invention relates to compounds of the general formula: 1

Abstract: Compounds useful as HCV anti-infectives having the formula: wherein the formula variables are as defined herein, are disclosed. Also disclosed are methods of making and using the same.

Abstract: This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subcllinical hyperthyrodism and liver diseases.

Abstract: The present invention is directed to particular bisphosphonate compounds, and in particular, to bisphosphonate conjugates that are useful in the treatment of soft tissues surrounding bone and bone-related diseases, such as bone cancer and osteoporosis.

Abstract: Compounds of formula (I) 1

Abstract: The present invention provides compositions and methods to treat or prevent neuropathic pain in a subject using a combination of a COX-2 selective inhibitor and a NMDA receptor antagonist.

Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.

Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.

Abstract: Pharmaceutical compositions for treating bone lesions in multiple myeloma or pharmaceutical compositions for treating multiple myeloma which contain as an active ingredient a compound having both of an effect of suppressing bone resorption accompanying multiple myeloma and an effect of inhibiting multiple myeloma, more particularly, 1-hydroxy-2-(imidazo[1,2-a]pyridin-3-yl)ethane-1,1-bisphosphonic acid or its salt.

Abstract: An isoquinuclidine derivative represented by the following general formula (I): (I) [wherein A1 is methylene or carbonyl]: R1 is hydrogen or methyl: R2 is —(CH2)n-A2-Ph (n is an integer of 0 to 3 and A2 is a single bond or —O—): and R3 is —COOH, —COOR4, —COSR4 (R4 is lower alkyl, unsubstituted phenyl, or phenyl substituted by a lower alkyl, lower alkoxy, hydroxyl, methoxycarbonyl, ethoxycarbonyl, or trifluoromethanesulfonamide group or by a halogen atom), etc.] or a pharmaceutically acceptable salt of the compound. Also provided is an oral remedy for diabetes, which contains the compound and has hypoglycemic activity.

Abstract: The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.

Abstract: This invention relates to compounds, pharmaceutical compositions, and methods for the treatment or prevention of neural or cardiovascular tissue damage related to cerebral ischemia and reperfusion injury in an animal by administering Poly(ADP-ribose) polymerase (“PARP”) inhibitors.

Abstract: Vascular damaging agents composed of substituted 5(6)-substituted benzimidazole-2-carbamates are provided. These agents are useful in the preparation of medicaments for the treatment of diseases involving neovascularisation, particularly for the treatment of solid tumors, macular degeneration, diabetic retinopathy, rheumatoid arthritis, psoriasis, and atherosclerosis.

Abstract: Novel FBPase inhibitors of the formula I and X 1

Abstract: The present invention relates to novel &agr;-substituted-&bgr;-aminoethylphosphonate and &agr;-substituted-&bgr;-aminovinylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and very low density lipoproteins) and for lowering plasma levels of total cholesterol.

Abstract: A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, phosphoramidates, and other prodrugs capable of demonstrating selective targeting and destruction of tumor cell vasculature.

Abstract: Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer.

Abstract: This invention provides compounds having the structure wherein A is OR5, or R1 is alkyl, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, pyridyl, R2 is H, alkyl, or aryl; R3 and R4 are halo, H, alkyl, aryl, trifluoromethyl, alkoxyaryl, nitro, amino, carboalkoxy, carbamide, carbamate, urea, alkylsulfonamide, —NR7(CH2)mCO2H, arylsulfonamide, cycloalkyl, or a heterocycle; R5 is H, alkyl, —CH(R8)R9, —CH2(CH2)nCO2R10, —C(CH3)2CO2R10, —CH(R8)(CH2)nCO2R10, —CH(R8)C6H4CO2R10, or —CH2-tetrazole; R6 is H, alkyl, halo, alkoxy, trifluoroalkyl or trifluoroalkoxy; R7 is H or alkyl; R8 is H, alkyl, aryl, arylalkyl, cycloalkyl, phthalic acid, R9 is CO2R12, CONHR12, tetrazole, or PO3R12; R10 is H, alkyl, aryl, or aralkyl; R11 is alkyl; R12 is H, alkyl, aryl, or aralkyl; X is O, or S; Y is O, N, or S; Z is C, or N; Q is O, N, or S; m=1-3; n=1-6, or a pharmaceutically acceptable salt thereof, which

Abstract: The present invention relates to compounds of Formula (I): wherein A1 is methylene, ethylene or propylene group and A2 is N or CR5, or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HCV NS3 protease, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.

Abstract: This invention provides indole and benzimidazole 15-lipoxygenase (15-LO) inhibitors of the formula where one of Y1 and Y2 is CH, N, or NH, and the other is R3 includes H, halo. HN2, COOH, alkyl; R4 includes halo, alkyl, and alkoxy; Z is C, CH, or NR5; R5 is H or oxycabonyl; and each X is independently H, alkyl, alkoxy, or halo.

Abstract: The present invention relates to compositions and methods of preventing or reducing the risk or incidence of skeletal injuries in horses. The present invention further relates to compositions and methods for alleviating pain associated with skeletal injuries in horses and to treating skeletal injuries in horses.

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 intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not require a &bgr;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: A novel bicyclic imidazo-5-yl-amine derivative of Formula I, 1