Abstract: The present invention relates to novel imaging probes and methods for using the probes in diagnostic imaging processes and other imaging processes to determine physiological functions.

Abstract: Cathepsin S is a highly active cysteine protease belonging to the papain superfamily. It is found mainly in lymph nodes, spleen, and macrophages and this limited occurrence suggests the potential involvement of this enzyme in the pathogenesis of degenerative disease. The invention relates to novel protease inhibitors, particularly inhibitors of the cysteine proteases of the papain superfamily and more particularly to Cathepsin S. The inhibitors are Furanone derivatives of Formula (II) which have a characteristic non-hydrogen substituent R5. They are selective over other members of the family and in particular show selectivity over other members of the Cathepsin family such as L and K.

Abstract: This invention describes the new, nonsteroidal gestagens of general formula I 1

Abstract: This invention relates to novel heterocyclic derivatives of the formula (VII), (VIII) or (IX) 1

Abstract: Compounds, compositions and methods are provided for the treatment and prophylaxis of infections and associated diseases caused by viruses of the Flaviviridae family by administering certain rhodanine derivatives, and analogs thereof, tri- and tetracyclic rhodanine alkanoic acids and rhodanine benzoic acids being particularly effective.

Abstract: Compounds of general formula (I): 1

Abstract: Compounds having the general structure 1

Abstract: The invention relates to substituted and unsubstituted 3H-benzo[1,2,3]oxathiazole 2,2-dioxides, 1,3-dihydrobenzo[1,2,5]thiadiazole 2,2-dioxides and 1,3-dihydrobenzo[c]isothiazole 2,2-dioxides, to their preparation and to their use in medicaments.

Abstract: An article and method for reducing somnolence in a patient receiving tizanidine therapy. Tizanidine may be administered in the form of an immediate release multiparticulate composition at or around the time food is consumed. The composition may be packaged in a container for distribution.

Abstract: Compounds of formula (I) as defined herein, or a pharmaceutically acceptable salt, or an in-vivo-hydrolysable ester thereof, are useful as antibacterial agents. Processes for their manufacture and pharmaceutical compositions containing them are described.

Abstract: The invention provides compounds of formula (I) wherein n, A, R1, R2 and R3 are as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals.

Abstract: The invention concerns a compound of the formula (I): wherein, for example: T is of the formula (IA), (IB), or (IC); R1 is of the formula —NHC(═O)Rb wherein Rb is (1-4C)alkyl; R2 and R3 are hydrogen or fluoro; >A—B— is >C═CH— (but not when T is (IA)) or >CH—CH2—; wherein when T is of the formula (IA) or (IB); R6 is, for example, (1-4C)alkyl; R5 is hydrogen, R10CO—, R10SO2— or R10CS— wherein R10 is, for example, optionally substituted phenyl, or (1-10C)alkyl, or when T is of the formula (IA), (IB); or (IC): R5 and R6 are linked to give a 5- or 6-membered ring which is fused to the ring shown in (IA), (IB), or (IC) so as to give an optionally substituted bicyclic ring; and pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them, and their use as antibacterial agents.

Abstract: Disclosed are substituted benzimidazole compounds of formula(I): 1

Abstract: Embodiments of the invention relate to methods of reducing weight in mammals and for the prophylaxis or treatment of obesity comprising administration of of C2-substituted indan-1-ol systems and their physiologically acceptable salts and physiologically functional derivatives.

Abstract: A series of compounds of Formula I are disclosed which are useful in treating viral hepatitus C.

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

Abstract: Novel CycloHexenyl-Ethyl-Thiourea (CHET) compounds as inhibitors of reverse transcriptase and effective agents for the treatment of HIV infection, including mutant, drug-sensitive, drug-resistant, and multi-drug resistant strains of HIV.

Abstract: The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.

Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various mammalian cellular receptors, including G-protein coupled receptors. A third aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for mammalian dopamine, muscarinic or serotonin receptors or transporters. Another aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for mammalian dopamine, muscarinic or serotonin receptors.

Abstract: P51084 The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.

Abstract: The present invention is directed to novel inhibitors and methods for inhibiting serine elastases. These compounds and methods achieve a novel approach to enzyme inhibition; namely, balanced inhibition of a plurality of serine elastases. Balanced inhibition of a plurality of elastases offers a novel approach to therapeutic treatment of diseases that involve abnormal activities of a plurality of elastases resulting in pathological changes such as occur in inflammatory and vascular conditions. These pathological changes are not limited to the breakdown of elastin but may include the processing of other proteins by serine elastases which in turn results in adverse effects. The opportunity of targeting a plurality of enzymes using single inhibitor offers therapeutic advantages over administering multiple therapeutic against where each agent has a single specificity for an individual target enzyme.

Abstract: The present invention relates to muscarinic receptor modulators, specifically, 7-oxo-2-azabicyclo[2.2.1]heptanes of formula (I) which are useful for the treatment of various diseases and conditions, for example, Alzheimer's disease, glaucoma, psychosis, particularly schizophrenia or schizophreniform conditions, mania, pain, bipolar disorder, depression, sleeping disorders, epilepsy, gastrointestinal motility disorders, urinary incontinence, and cognition enhancement.

Abstract: Methods of treating exercise-induced asthma using a PDE-4 inhibitor are disclosed.

Abstract: According to the invention there is provided a compound the formula I; 1

Abstract: Disclosed is a pharmaceutical composition, comprising a combination of a dose of rofecoxib or a pharmaceutically acceptable salt thereof and a dose of oxcodone or a pharmaceutically acceptable salt thereof, said combination in an amount sufficient to provide an analgesic effect in a human patient. Also disclosed is a method of effectively treating pain in humans or other mammals, comprising administering to the patient a combination of a dose of rofecoxib or a pharmaceutically acceptable salt thereof and a dose of oxycodone or a pharmaceutically acceptable salt thereof such that the dosing interval of the rofecoxib overlaps with the dosing interval of the oxycodone, said combination in an amount sufficient to provide an analgesic effect in a human patient.

Abstract: A compound of formula (I) or its enantiomers or diastereoisomers thereof: 1

Abstract: The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: 1

Abstract: Heterocyclic aromatic amides having a hydroxy group adjacent to the amide functionality are useful as antifungal agents, particularly for plants.

Abstract: The invention provides compounds of formula (I) wherein R0, R1, R2 and A are as defined in the description, and the preparation thereof. The compounds of formula (I) have high affinity as &agr;2 adrenoceptors and hence are useful as pharmaceuticals.

Abstract: The present application relates to novel guanidine derivatives of the formula (I) in which R1 represents a five- or six-membered heterocyclic group; R2 represents hydrogen or alkyl, R3 represents the groupings —OR4, —OCOR5, —OCOOR6, —OCONR7R8 and —OSO2R9, where R4, R5 and R6 independently of one another represent alkyl, alkoxyalkyl, halogenoalkyl, alkenyl, alkinyl, alkylaminoalkyl, dialkylaminoalkyl, optionally substituted cycloalkyl and in each case optionally substituted phenyl or benzyl, R7 and R8 independently of one another represent hydrogen, alkyl, alkenyl and in each case optionally substituted phenyl or benzyl and R9 represents alkyl or optionally substituted phenyl, A represents the groupings —CH2CH2—, (CH2)3 and —CH═CH— and z represents cyano or nitro, with the proviso that, if Z represents NO2 and A represents —CH2CH2—, the radical R2 represents hydrogen; and the compound of the formula (I) in which

Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract: The invention provides compounds having formula (I), wherein W is OH, or derivatives of the carboxylic acid, and Q is a heterocyclo-condensed ortho-phenylene residue. These compounds are useful as MEK inhibitors, particularly in the treatment of proliferative diseases such as cancer.

Abstract: The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particularly, these compounds are potent and selective inhibitors of tryptase and are therefore effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis.

Abstract: The present invention relates to a method of treating Multiple Sclerosis, other demyelinating disorders and peripheral neuropathy in a mammal by administering to the mammal a neurotransmitter-inducing or precursor agent in combination with an (SRI) antidepressant or an anxiolytic agent with improvement in efficiency. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a neurotransmitter-inducing or precursor agent, and an SRI antidepressant or anxiolytic agent.

Abstract: Compounds with heterocyclic-hydroxyimino-fluorene nuclei that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.

Abstract: The invention proposes the use of a leukotriene antagonist, particularly a montelukast sodium compound such as SINGULAIR, in combination with cystine to combat inflammatory disease and hopefully reduce the necessary use of SINGULAIR. Combination with other anti-inflammatory agents and anti-asthmatic agents is proposed. Selenium to assure glutathione pathway benefit is suggested. The addition of a selective COX-2 inhibitor is suggested.

Abstract: An article and method for reducing somnolence in a patient receiving tizanidine therapy. Tizanidine may be administered in the form of an immediate release multiparticulate composition at or around the time food is consumed. The composition may be packaged in a container for distribution.

Abstract: The present invention relates to novel angiogenic-inhibitory compounds of formula (I) 1

Abstract: Compound represented by the structural formula 1

Abstract: The present invention relates to therapeutically active azabicyclic compounds, a method of preparing the same and to pharmaceutical or veterinary compositions comprising the compounds. The novel compounds are useful in treating a disease in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.

Abstract: This invention relates to a method for the prophylaxis of or reducing the severity of post-viral bacterial infection by administering a PDE 4-specific inhibitor prior to or during the course of a viral infection or thereafter during the course of the bacterial infection.

Abstract: A method for inhibiting the action of TNF for treating neurological conditions in a human by administering a TNF antagonist for reducing the inflammation of neuronal tissue of said human, or for modulating the immune response affecting neuronal tissue of said human, comprising the step of: administering a therapeutically effective dosage level to said human of said TNF antagonist selected from the group consisting of etanercept, infliximab, and D2E7 (a human anti-TNF mAb from Knoll Pharmaceuticals) for reducing the inflammation of neuronal tissue of said human, or for modulating the immune response affecting neuronal tissue of said human. In addition, for the viral-associated neurological disorders, the following additional step is performed: administering a therapeutically effective dosage level to said human of an antiviral agent or anti-retroviral agents for reducing the inflammation of neuronal tissue of said human, or for modulating the immune response affecting neuronal tissue of said human.

Abstract: Substituted derivatives of 1,2,5-thiadiazolidin-3-one 1,1-dioxides, oligomers containing them, and methods of using them.

Abstract: The invention provides fungicidal compounds of formula I and salts thereof: 1

Abstract: This invention provides compounds of Formula I having the structure wherein, R1, R2, and X are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.

Abstract: Trisubstituted pyrroles are useful in the control of coccidiosis in poultry.

Abstract: Compounds with heterocyclic-hydroxyimino-fluorene nuclei that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.

Abstract: Compounds of formula (I) 1

Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.