Abstract: Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have at a group having a guanidino moiety or derivative thereof. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.

Abstract: The invention provides methods for treating HIV infection in a subject in need thereof comprising lipid analogs of phosphonoformate-containing pharmaceutically active compounds. Lipid analogs contemplated for use in the practice of the present invention comprise phosphonoformates covalently linked (directly or indirectly through a linker molecule) to a substituted or unsubstituted alkylglycerol, alkylpropanediol, alkylethanediol, or related moiety. In particular, the invention provides methods for treating viral infections caused by viruses which have developed resistance to currently available antiviral agents, as well as methods comprising the use of invention compounds in combination with azidodeoxythymidine to minimize the selection of drug-resistant HIV variants during therapy.

Abstract: Methods, compositions, and kits, are provided for the use of nitric oxide synthase inhibitors to prevent and reduce wrinkles.

Abstract: This invention relates to treating an inflammatory disease by administering a phosphodiesterase 4 inhibitor in combiantion with an inhibitor of prostaglandin synthesis, NSAIDs being exemplary.

Abstract: A method for the prevention, treatment, or amelioration of pain, inflammation, or inflammation-related disorder in a subject that is in need of such prevention, treatment or amelioration, involves the administration to the subject of a cyclooxygenase-2 selective inhibitor or prodrug thereof and enteric coated aspirin. A method can also involve the administration of a cyclooxygenase-2 selective inhibitor and aspirin in an amount lower than 75 mg/day. A method can also involve the administration of a cyclooxygenase-2 selective inhibitor and aspirin where the cycloxygenase-2 selective inhibitor is BMS-347070, S-33516, CS-502, darbufelone, LAS 34475, LAS 34556, L-745337, SD-8381, RWJ-63556, L-784512, COX-189, ABT-963, or valdecoxib, or any pharmaceutical salt or prodrug thereof. Compositions, pharmaceutical compositions and kits that can be used with the methods are also described.

Abstract: A method of and composition for diminishing multiple sclerosis symptoms are disclosed. In one embodiment, the method comprises the step of administrating an amount of calcium and a vitamin D compound effect to diminish multiple sclerosis symptoms. In another embodiment, the invention is a pharmaceutical composition comprising an amount of calcium and vitamin D compound effective to diminish multiple sclerosis symptoms.

Abstract: A composition is described comprising a vitamin D analog and a retinoid wherein: (a) the vitamin D analog is capable of binding a vitamin D receptor or being converted in vivo into a compound capable of binding a vitamin D receptor; and (b) the retinoid is selected from the group consisting of retinol in a concentration of at least about 1.0%, a compound in a concentration of at least about 1.0% capable of being converted in vivo into retinol, and a retinoid characterized by having a substitution at the 4-position. Further, methods of treating disorders characterized by abnormal cell-proliferation and/or cell-differentiation are also described.

Abstract: The present invention demonstrates that p38MAPK inhibitor induces low density lipoprotein receptor expression 6-8 fold, and further provides the application of such inhibitor in the treatment of hypercholesterolemia.

Abstract: This invention relates to methods and pharmaceutical compositions for providing hormone replacement therapy in perimenopausal, menopausal, and postmenopausal women through the continuous administration of combinations of conjugated estrogens and trimegestone.

Abstract: A therapeutic composition is provided that comprises a 1-R1-phenyl, 4-R2-phenyl substituted 1,2,3,6-tetrahydropyrimidine-2-one cold receptor agonist in a therapeutically effective amount and preferably further comprises one or more pharmaceutically active drugs such as an anti-inflammatory glucocorticosteroid, a sympathomimetic amine decongestant, an anti-histamine, a local anesthetic, menthol or a menthol analog, and mixtures thereof. The cold receptor agonist may be represented by the general formula 1-[1R-phenyl]-4-[R2-phenyl]-1,2,3,6-tetrahydropyrimidine-2-one wherein: R1 is -hydroxy, -chloro, -fluoro, -alkyl, -acetoxy, -trifluoromethyl; and R2 is -nitro, -chloro, -fluoro, -alkyl, -trifluoromethyl. Therapeutic compositions of the invention elicit long-lasting cooling or soothing, particularly when formulated for delivery to suppress the sensations of itch and pain, such as for delivery to inflamed skin, to the mucous membranes of the anogenital areas, and to the enteric mucosa.

Abstract: Methods and formulations for treating female sexual dysfunction are provided. A pharmaceutical composition formulated so as to contain a selected vasoactive agent is administered to the vagina, vulvar area or urethra of the individual undergoing treatment. Suitable vasoactive agents are vasodilators, including naturally occurring prostaglandins, synthetic prostaglandin derivatives, endothelial-derived relaxation factors, vasoactive intestinal polypeptide agonists, smooth muscle relaxants, leukotriene inhibitors, and others. The formulations are also useful for preventing the occurrence of yeast infections, improving vaginal muscle tone and tissue health, enhancing vaginal lubrication, and minimizing excess collagen deposition. A clitoral drug delivery device is also provided.

Abstract: The present invention sterol-modified hedgehog polypeptides and functional fragments thereof. Methods of identifying compositions which affect hedgehog activity based on inhibition of cholesterol modification of hedgehog protein are described. In one aspect of the invention, the method provides a means for affecting cholesterol biosynthesis or transport in a cell comprising contacting a cell with an effective amount of a compound that affects hedgehog, thereby affecting cholesterol biosynthesis or transport. The effect may be inhibition or stimulation of cholesterol biosynthesis or transport.

Abstract: The present invention features methods of inhibiting progestin activity in a cell or in a subject in need of such inhibition, and methods of treating or preventing progestin-dependent conditions in a subject in need of such treatment or prevention. The methods include administering an effective amount of a C-17-derivatized dexamethasone antiprogestin to the cell or the subject. The invention also provides methods of screening substances for progestin or antiprogestin activity, and methods of detecting progestins, progestin agonists, or antiprogestins in a sample, using the C-17-derivatized dexamethasone antiprogestins of the invention.

Abstract: Novel estrogenic compounds of Formula I are provided.

Abstract: Methods, compositions and devices for inhibiting restenosis are provided. Specifically, molecular chaperone inhibitor compositions and medical devices useful for the site specific delivery of molecular chaperones are disclosed. In one embodiment the medical device is a vascular stent coated with a molecular chaperone inhibitor selected from the group consisting of geldanamycin, herbimycin, macbecin and derivatives and analogues thereof. In another embodiment an injection catheter for delivery an anti-restenotic effective amount of geldanamycin to the adventitia is provided.

Abstract: The invention relates to compounds of formula I 1

Abstract: The present invention provides compounds of the formula: 1

Abstract: This invention relates to novel substituted succinic acid metallo-&bgr;-lactamase inhibitors which are useful potentiators of &bgr;-lactam antibiotics.

Abstract: The present invention discloses compounds which, are novel receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Abstract: Compounds having the general structure: 1

Abstract: A prophylactic or therapeutic agent for central nervous system diseases based on amyloid &bgr;40 secretion inhibitory activity of a compound having urotensin II receptor antagonistic activity or a salt thereof.

Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

Abstract: This invention relates to 2-arylimino heterocycles, including 2-arylimino-1,3-thiazolidines, 2-arylimino-2,3,4,5-tetrahydro-1,3-thiazines, 2-arylimino-1,3-thiazolidin-4-ones, 2-arylimino-1,3-thiazolidin-5-ones, and 2-arylimino-1,3-oxazolidines, and their use in modulating progesterone receptor mediated processes, and pharmaceutical compositions for use in such therapies.

Abstract: The present invention provides pharmaceutically active compounds useful for the treatment of diseases or disorders of the central nervous system.

Abstract: Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.

Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.

Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) 1

Abstract: This invention relates to methods of using aryl ureas to treat diseases mediated by the VEGF induced signal transduction pathway characterized by abnormal angiogenesis or hyperpermeability processes.

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: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.

Abstract: The present invention provides compounds of formula I: 1

Abstract: Compounds of formula (I), (IIa) or (IIb) wherein R1-R6, Z, Q and n are as defined in claim 1 and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. Compositions comprising a compound of formula (I), (IIa) or (IIb) are also described.

Abstract: This invention provides compounds of the formula (I) and (II): 1

Abstract: Compounds of formula I, 1

Abstract: The present invention provides a compound of formula I 1

Abstract: The invention relates to compounds of the formula (I): wherein: ring C is 9 or 10-membered bicyclic heteroaromatic group containing at least one nitrogen atom in the ring attached to Z and optionally containing a further 1-3 heteroatoms, selected independently from O, S, and N, with the proviso that ring C is not a quinazoline, quinoline or cinnoline group; either any one of G1, G2, G3, G4 and G5 is nitrogen and the other four are —CH—; or G1, G2, G3, G4 and G5 are all —CH—; Z is —O—, NH—, —S—, CH2— or a direct substituents R1 may be attached at any free carbon atom of the indole, azaindole or indazole group; m is an integer from 0 to 2; Rb represents hydrogen or another value as defined herein; R1 represents hydrogen, hydroxy, halogeno, C1-4alkyl, or any other value as defined herein; R2 represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3alkylsulphanyl, —NR3R4 (wherein R3 and R4, which may be the

Abstract: The present invention relates generally to compounds of formula (IA): (IA) 1

Abstract: The present invention provides a compound of formula I 1

Abstract: The use of a compound of formula (I): wherein R1, R2, R3, R4, R5 and R6 are independently selected from hydrogen, alkyl, aryl and non-aromatic heterocyclic groups, or each of one or more pair(s) of the substituent groups R1 to R6 may together form a 3, 4, 5, 6, 7 or 8-membered ring containing 0, 1 or 2 heteroatom(s); R7 is selected from alkyl, aryl and non-aromatic heterocyclic groups, and R8 is selected from hydrogen, halogen, alkyl, aryl and non-aromatic heterocyclic groups; and pharmaceutically acceptable salts and prodrugs thereof, in the manufacture of a medicament for use in the treatment of a condition generally associated with abnormalities in glutamatergic transmission; novel compounds of formula (1) per se and for use in therapy.

Abstract: Compounds of formula (I), wherein G1 is CH or N; G2 is CH or N; R1 is a variety of optional substituents, L1 is (1-4C)alkylene; T1 is CH or N; R2 and R3 are independently hydrogen or (1-4C)alkyl or are joined to form a ring; X1 and X2 represent various linking groups; Ar is phenylene or certain heteroaryl rings and Q represents a variety of aromatic or heterocyclic rings systems, and pharmaceutically acceptable salts thereof are described as useful antithrombotic and anticoagulant agents, and are selective Factor Xa inhibitors. Processes for their preparation and pharmaceutical compositions containing them are also described.

Abstract: Organic compounds having the structure I are provided where the variables have the values described herein.

Abstract: The use of compounds of formula (1) is described, in which compounds R1, R2 and R3 are each independently of the others hydrogen; C1-C20alkyl; C3-C7cycloalkyl; C2-C20alkenyl; C4-C7cycloalkenyl; C2-C20alkynyl, C4-C7cycloalkynyl; or unsubstituted or C1-C5alkyl-, C3-C7cylcoalkyl-, C1-C5alkoxyl-, C3-C7cycloakoxy-, halo-, oxo-, carboxy-, carboxy-C1-C7alkyl ester-, carboxy-C3-C7cylcloalkyl ester-, cyano-, trifluoromethyl-, pentafluoroethyl-, amino-, N,N-mono- or di-C1-C20alkylamino- or nitro-substituted phenyl-C1-C5alkyl, naphthyl-C1-C5alkyl, phenylcarbonyl-C1-C5alkyl, naphthylcarbonyl-C1-C5alkyl, pyrrolylalkyl, furanylalkyl, thiophenylalkyl, pyrazolylalkyl, imidazolylalkyl, oxazolylalkyl, thiazolylalkyl, isoxazolylalkyl, isothiazolylalkyl, 1,2,3-triazolylalkyl, 1,2,4-triazolylalkyl, 1,2,3-oxadiazolylalkyl, 1,3,4-oxadiazolylalkyl, 1,2,3-thiadiazolylalkyl, 1,3,4-thiadiazolylalkyl, indolylalkyl, pyridylalkyl, pyridazinylalkyl, pyrimidinylalkyl, pyridazinylalkyl, quinolinylalkyl, isoquinolinylalkyl, pyrrolyl, furanyl,

Abstract: This invention relates to heteroaryl substituted fused bicyclic heteroaryl compounds, such as heteroaryl substituted imidazopyridines, imidazopyrazines, imidazopyridizines, imidazopyrimidines, and imidazothiazoles, which may be described by Formula I or Formula II: 1

Abstract: The invention relates to the use of quinoxaline derivatives as photostable UV filters in cosmetic and pharmaceutical preparations for protecting the human epidermis or human hair against UV radiation, especially in the 280-400 nm range.

Abstract: This invention comprises the novel compounds of formula (I) 1

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

Abstract: Hydroxamic and carboxylic acid derivatives having MMP and TNF inhibitory activity.

Abstract: Compositions and methods for treating disorders of the outer retina with compounds with 5-HT1A against activity are disclosed.

Abstract: The invention is directed to compositions and methods for modulating the human sexual response. The compositions comprise two or more pharmaceutically active agents which preferably include an alpha-adrenergic antagonist and a phosphodiesterase inhibitor.