Abstract: The present invention relates to new derivatives of imidazo, pyrimido and diazepine-pyrimidine-dione of the general formula (I) in which R1, R2, L1, L2, Y, Z and A are various and varying groups. These products exhibit a good affinity for certain sub-types of cannabinoid receptors, in particular the CB2 receptors. They are particularly useful for treating pathological conditions and diseases in which one or more cannabinoid receptors are involved. The invention also relates to pharmaceutical compositions containing said products, and to the use thereof for preparing a drug.

Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: (A) and (B) wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disase pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.

Abstract: A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Abstract: This invention relates to a pharmaceutical kit containing a lyophilized preparation of a pyrimidine compound described in the specification. Also disclosed is a lyophilization process for making this preparation.

Abstract: The present invention relates to the use of a 2-cyanopyrimidine compound of the formula wherein R1, R2, R3 and X are as defined in the specification and in the claims, in free form or in salt form, and, where possible, in tautomeric form, as an inhibitor of the activity of cathepsin S.

Abstract: The present invention relates to new phenylpropanone modulators of dopamine receptors, serotonin receptors, and/or nicotinic acetylcholine receptors, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention is directed to the provision of pharmaceutical compositions such as multi-dose, ophthalmic compositions. The compositions possess sufficient antimicrobial activity to satisfy preservative efficacy requirements in the United States and/or Europe. The compositions include sorbate or a non-polymeric diquaternary ammonium compound for enhancing preservation efficacy. Further, the compositions typically have relatively low ionic strengths to assist in maintaining such efficacy.

Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a 5HTR agent, in combination with one or more other neurogenic agents, or anti-astrogenic agent, to stimulate or activate the formation of new nerve cells.

Abstract: The present invention concerns a method of administering at least one active pharmaceutical agent to a patient in need thereof, which method comprises the intranasal administration of a composition comprising a therapeutically effective amount of this agent, phospholipids, one or more C2-C4 alcohols and water, wherein the concentrations of the phospholipids and the one or more alcohols in the composition are in the ranges of 0.2 to 10% and 12 to 30% by weight, respectively, with the water content of said composition being not less than 30% by weight, the phospholipids forming vesicles in said composition. Further are disclosed pharmaceutical compositions and combinations suitable for intranasal delivery.

Abstract: The present invention provides a prophylactic or therapeutic agent for depression or anxiety disorders, comprising (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide.

Abstract: The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced.

Abstract: A combination therapy for treating depressive disorders is provided herein. The combination therapy comprises administering an effective amount of bupropion or its metabolites together with at least one serotonin 5-HT1A partial agonist or its metabolites to a patient in need of treatment of the depressive disorder. Pharmaceutical formulations, including packaged pharmaceutical formulations, comprising this combination are also provided herein.

Abstract: The invention provides compounds of Formula I or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors.

Abstract: The present invention relates to novel compounds, the preparation and use, particularly therapeutic, thereof. More specifically, it relates to compounds derived from aryl carbamates, the preparation and use thereof, particularly in the field of human and animal health. The compounds according to the invention are preferably 5-HT4 serotoninergic receptor ligands and can therefore be used in the therapeutic or prophylactic treatment of any disorder involving a 5-HT4 receptor. The invention also relates to pharmaceutical compositions comprising such compounds, the preparation and use thereof and treatment methods using said compounds.

Abstract: The invention provides compounds which are PDE7 inhibitors, having the following formula (I), (II) and (III) in which X1, X2, X3, X4, X, Y, Z, A and Z1 are as defined in the description, methods for preparing them and their use for the treatment of disorders for which therapy by a PDE7 inhibitor is relevant.

Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Abstract: The present invention provides a method for improving respiratory function and inhibiting muscular degeneration (e.g., dystrophy and atrophy). Alternative embodiments of the invention provide a method of inhibiting motor neuron apoptosis and the subsequent muscular degeneration associated with the denervation of muscular tissue resulting from neuron death.

Abstract: The S-stereoisomer of 6-hydroxy-buspirone is an effective treatment for anxiety, depression, and other psychogenic disorders. The S-isomer may provide reduced potential for adverse effects and a longer duration of action compared to the racemic mixture and with buspirone.

Abstract: Compounds of the formula useful for treatment of disorders of the dopaminergic system, such as schizophrenia, schizoaffective disorder, bipolar disorder, Parkinson's disease, L-DOPA induced pychoses and dyskinesias, Tourette's syndrome and hyperprolactinemia and in the treatment of drug addiction such as the addiction to ethanol, nicotine or cocaine and related illnesses.

Abstract: A liquid aerosol formulation comprising at least one thermally stable active ingredient selected from the group consisting of buspirone, buprenorphine, triazolam, cyclobenzaprine, zolpidem, pharmaceutically acceptable salts and esters thereof and derivatives thereof. The liquid formulation can include an organic solvent such as propylene glycol and one or more optional excipients. The active ingredient can be present in an amount of 0.01 to 5 wt. % and the formulation can be heated to provide a vapor which forms an aerosol having a mass median aerodynamic diameter of less than 3 &mgr;m.

Abstract: This invention is directed towards a method of inhibiting activation of a human &agr;1d adrenergic receptor which comprises contacting the receptor with a compound so as to inhibit activation of the receptor, wherein the compound binds selectively to a human &agr;1d adrenergic receptor. This invention provides for a compound which binds selectively to a human &agr;1d adrenergic receptor. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier. This invention further provides for a method of treating a subject afflicted with a disease which is susceptible to treatment by antagonism of the human &agr;1d adrenergic receptor which comprises administering to the subject an amount of the above defined compounds effective to treat the disease.

Abstract: The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which R1, R2, R3 and A are each as defined, and to processes for their preparation and to their use as medicaments, in particular as medicaments for the treatment of cardiovascular disorders.

Abstract: The invention relates to the use of compounds that enhance 5-hydroxytryptamine 1a receptor activity, or activation (e.g. a selective 5-hydroxytryptamine 1a receptor agonists) for preventing or reducing motor fluctuations associated with dopamine replacement therapy.

Abstract: This invention relates to a pharmaceutical composition for oral administration comprising a carrier and, as an active ingredient, a 5-HT1 agonist, characterized in that the composition is formulated to reduce pre-systemic metabolism of said 5-HT1 agonist. A process for preparing such a composition and the use of such a composition for the treatment of anxiety, depression, attention deficit disorder and/or panic disorders and/or as a memory enhancer are also provided.

Abstract: The R-stereoisomer of 6-hydroxy-buspirone is an effective treatment for anxiety, depression, and other psychogenic disorders. The R-isomer exhibits greater receptor specificity than the S-isomer and should have reduced potential for the adverse effects associated with the racemic mixture and with buspirone.

Abstract: The present invention relates to a method for treatment of attention deficit disorder by administering certain 5-HT1A receptor agonists

Abstract: The present invention relates to the treatment of depression and/or anxiety by the administration of a combination of a specific class of NK-1 receptor antagonists and an antidepressant or anti-anxiety agent.

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

Abstract: Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and air-ways, and the preparation thereof.

Abstract: This invention relates to a method of treating depression and anxiety-related disorders comprising administering to a mammal in need of such treatment an effective amount of a combination of an adenosine A2A antagonist and an antidepressant or an anxiolytic; another aspect of the invention is a pharmaceutical composition comprising a therapeutically effective amount of a combination of an adenosine A2A antagonist and an antidepressant or anxiolytic in a pharmaceutically acceptable carrier.

Abstract: The present invention provides a method for improving respiratory function and inhibiting muscular degeneration (e.g., dystrophy and atrophy). Alternative embodiments of the invention provide a method of inhibiting motor neuron apoptosis and the subsequent muscular degeneration associated with the denervation of muscular tissue resulting from neuron death.

Abstract: Compounds with 5-HT1A agonist activity which are useful for controlling the visual field loss associated with glaucoma are disclosed.

Abstract: A method of treating stress in a patient showing stress related symptoms is disclosed, where the method comprises administering to the patient an effective amount of a serotoninergic drug or prodrug. Specific examples of such drugs are described, and include, among others, tryptophan or 5-hydroxytryptophan, or their salts.

Abstract: A method of treating pain with acetaminophen comprises the concurrent administration of an azapirone such as buspirone. This combination of agents surprisingly results in a strengthened analgesic response characterized by rapid onset, greater pain relief, and a longer duration of action.

Abstract: An improved method of treating anxious patients involves direct administration of 6-hydroxy-8-[4-[4-(2-pyrimidinyl)-piperazinyl]-butyl]-8-azaspiro[4.5]-7,9-dione (BMY 28674) or a pharmaceutically acceptable salt or hydrate formulated in appropriate pharmaceutical compositions to patients in need of such treatment. Syntheses of BMY 28674 are also provided.

Abstract: Nicotine dependency is treated by administration of an opioid antagonist. In some embodiments, rapid or ultra rapid detoxification techniques include using a combination of an effective amount of an opioid antagonist such as nalmefene, naloxone or naltrexone or a mixture of any one of these, and either clonidine or related compounds either while awake, or while under sedation or anesthesia, followed by continued administration of an effective amount of an opioid antagonist with or without agents that enhance nicotine dependency treatment.

Abstract: The S-stereoisomer of 6-hydroxy-buspirone is an effective treatment for anxiety, depression, and other psychogenic disorders. The S-isomer may provide reduced potential for adverse effects and a longer duration of action compared to the racemic mixture and with buspirone.

Abstract: A method of treating pain with acetaminophen comprises the concurrent administration of buspirone. This combination of agents surprisingly results in a morphine-like analgesic response characterized by rapid onset, greater pain relief, and a longer duration of action.

Abstract: A method of treating pain with acetaminophen comprises the concurrent administration of a hydroxyazapirone selected from 6-hydroxybuspirone or 3-hydroxygepirone. This combination of agents results in a more morphine-like analgesic response characterized by rapid onset and greater pain relief.

Abstract: The products and methods of the present invention provide a means for increasing the solubility and bioavailability of active agents. More particularly the invention provides compositions containing active agents as water-soluble complexes with glycyrrhizin, and methods of preparing such complexes. The invention further provides methods for the preparation of highly water soluble complex dosage forms.

Abstract: Compounds having heterocyclic groups containing two nitrogen atoms are disclosed. The compounds are useful for treating multidrug resistance. The compounds can be formulated in compositions with a carrier and, optionally, a therapeutic agent.

Abstract: Compounds, compositions, and methods for treating multidrug resistance are disclosed. Suitable compounds are 2-substituted heterocyclic compounds.

Abstract: A method of treating pain with acetaminophen comprises the concurrent administration of an azapirone such as buspirone. This combination of agents surprisingly results in a strengthened analgesic response characterized by rapid onset, greater pain relief, and a longer duration of action.

Abstract: A method of reducing cravings in a mammal to food or an addictive substance is disclosed. The method comprises administering to the mammal an effective amount of a D1/D5 antagonist or a D1/D5 partial agonist alone or in combination with other specified CNS compounds.

Abstract: A method of treating pain with acetaminophen comprises the concurrent administration of buspirone. This combination of agents surprisingly results in a morphine-like analgesic response characterized by rapid onset, greater pain relief, and a longer duration of action.

Abstract: The present invention encompasses methods of treating patients for tobacco addiction and nicotine addiction, for palliating the effects of nicotine withdrawal, for providing or facilitating the effects of smoking cessation therapies and as long-term smoking cessation maintenance therapy. The invention also includes related pharmaceutical compositions comprising nicotine receptor antagonists and either an anti-depressant or an anti-anxiety drug. Specific combinations of drugs (mecamylamine HCl and bupropion HCl) as well as mecamylamine in combination with certain drug classes (e.g., anti-anxiety drugs and anti-depressants) comprise the pharmaceutical compositions disclosed. These compositions are also contemplated for use in the treatment of cocaine addiction and the treatment of alcohol dependence.

Abstract: A controlled release form of buspirone medicament is described. This medicament comprises a buspirone in intimate admixture with an anionic exchange polymer complexing agent. These components form a complex upon the addition of water and thereby permit improved dosing of buspirone to achieve a more targeted therapeutic effect in patients.

Abstract: An improved method of orally dosing buspirone in a manner favoring production of the active metabolite 6-hydroxy-8-[4-[4-(2-pyrimidinyl)-piperazinyl]-butyl]-8-azaspiro[.5]-7,9-dione should enhance the alleviation of anxiety in anxious patients.

Abstract: A combination of medicines are administered daily for the relief of the symptoms of an Anxiety Disorder or an Adjustment Disorder With Anxiety. The combination comprises a centrally-acting beta-blocker which passes the brain blood barrier, preferably the beta-blocker betaxolol, and a serotonin-enhancer, for example, the serotonin agonist buspirone or the serotonin reuptake inhibitor sertraline.