Abstract: This invention relates to methods of inhibiting a Cav3 calcium channel in a cell using a C2-C10 alkyl alcohol, or mixtures thereof. This invention further relates to methods of treating a thalamocortical dysrhythmia disorder in a mammal and for treating a neurological disorder in a mammal associated with the thalamocortical dysrhythmia using a C2-C10 alkyl alcohol, a lipophilic molecule with a partition coefficient substantially similar to that of a C2-C10 alkyl alcohol, or mixtures thereof, or a pharmaceutical composition comprising the same.

Abstract: This invention relates to a method of imaging amyloid deposits and to styrylpyridine compounds, and methods of making radiolabeled styrylpyridine compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.

Abstract: The present invention provides compositions and methods for maintaining cardiac function by administering dichloroacetate (DCA) in combination with an inotrope.

Abstract: A method of pharmaceutical therapy comprising administering at least one pharmaceutical, complementary medicine, or herbal product, orally at a dose sufficient to provide a clinically effective blood level in the portal vein and less than that required to provide a clinically effective blood level in the peripheral circulation to thereby provide a dose-delivery rate having a selective clinical effect in the liver.

Abstract: Provided are pharmaceutical formulations comprising sustained release particles each having an inner core bead comprising an active pharmaceutical ingredient an intermediate coating substantially surrounding the inner core bead, and an outer coating substantially surrounding the intermediate coating comprising a pH independent polymer. Also provided is a pharmaceutical formulation comprising two bead populations wherein each of the first and second bead populations have a different drug release profile. Also provided is a method of preparing an extended release dosage composition comprising one or more bead populations.

Abstract: The present invention relates to modified release pharmaceutical compositions for oral administration and more particularly to modified release pharmaceutical compositions of a form of at least one selective serotonin re-uptake inhibitor selected from the group consisting of a selective serotonin reuptake inhibitor, racemic mixtures thereof, enantiomers thereof, pharmaceutically-acceptable salts thereof and combinations thereof.

Abstract: The present invention relates to compositions and methods of treating human subjects with a beta-adrenergic receptor blocking agent (“beta-blocker”) provided in a time-sustained-release delivery system. The time-sustained-release drug delivery systems includes at least three populations of beads, where each population of beads includes a beta-blocker. The beads may be selected from immediate-release beads, enteric-release beads, sustained-release beads, and time-sustained-release beads. The beta-blocker may be selected from acebutolol, atenolol, betaxolol, bisoprolol, esmolol, metoprolol, nebivolol, butoxamine, carteolol, carvedilol, labetalol, nadolol, oxprenolol, penbutolol, propranolol, pindolol, sotalol, and timolol. According to presently preferred embodiments, the beta-blocker is propranolol.

Abstract: A method for enhancing absorption of a compound in a medicament that is suitable for administering transmucosally to a subject is conducted in an environment having a suitable pH. The suitable pH is determined based on the ionization constant (dissociation constant) of the compound in water, the solubility of the ionized form of the compound, and the solubility of the non-ionized form of the compound.

Abstract: Ophthalmic compositions suitable for use as artificial tears or as vehicles for ophthalmic drugs are disclosed. The compositions contain a combination of three polymers that have a synergistic effect on viscosity.

Abstract: The present invention relates to novel compounds of formula (I), or a salt, solvate, or physiologically functional derivative thereof, to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.

Abstract: Ophthalmic compositions suitable for use as artificial tears or as vehicles for ophthalmic drugs are disclosed. The compositions contain a combination of three polymers that have a synergistic effect on viscosity.

Abstract: The invention provides sodium channel modulating compounds of formula I: wherein X, Y, Q, R1, w, and R2 have any of the values defined in the specification, and salts thereof, which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of formula (I) or a salt thereof, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).

Abstract: Compounds of formula (Ia) as potent, ?1-specific beta blockers with a short duration of action in the systemic circulation, wherein R is 3?,4?-dimethoxyphenyl, R1 is hydrogen, and R2 is selected from methyl, ethyl, propyl, isobutyl and isopropyl; or R is 3?,4?-dimethoxyphenyl, R1 is selected from fluorine, chlorine and bromine, and R2 is selected from methyl, ethyl, propyl, isopropyl, isobutyl and cyclopropylmethyl; of R is 4?-methoxyphenoxy, R1 is selected from hydrogen, fluorine, chlorine and bromine, and R2 is selected from methyl, ethyl, propyl, isopropyl, isobutyl and cyclopropylmethyl; or R is 3?,4?-dimethoxyphenyl, R1 is cyano, and R2 is cyclopropylmethyl; or R is 4?-methoxyphenoxy, R1 is cyano, and R2 is isobutyl; and physiologically acceptable hydrolysable derivatives thereof having the hydroxy group in the 2-position of the 3-aminopropoxy side chain in esterified form, in their racemic and optically active forms, and their pharmaceutically acceptable acid addition salts.

Abstract: The invention is directed to the use of ?-adrenoceptor antagonists for the manufacture of a medicament for the treatment of disorders of the outer retina.

Abstract: Composition containing at least one aminophenol derivative and a solubilizing compound which is not in the form of vesicles, chosen from: (a) oxyalkylenated fatty acid esters of sorbitan, (b) oxyalkylenated hydrogenated castor oils, and/or (c) oxyalkylenated fatty alcohols. The invention also relates to a process for dissolving at least one aminophenol derivative by mixing it with a solubilizing agent as defined above.

Abstract: A method for treating or preventing retinal pathology or injury. The method locates and secures a retinal stimulating substance in the eye between the internal limiting membrane and the retina, which is the target site for the substance. The substance may be an implant that provides electrical stimulation to adjacent ganglion and neurofiber cells. Alternatively, the substance may be a pharmaceutical substance to stimulate the retina. In addition to providing direct contact of the substance with its target, the method obviates the need for artificial structures such as tacks or adhesives which may cause retinal bleeding or traction.

Abstract: The invention relates to phenoxypropanolamines, to pharmaceutical compositions containing them, to processes for preparing them, and to the method of use thereof in the treatment of diseases that are improved by beta-3 agonist action.

Abstract: Pharmaceutical formulation, its method of preparation, and its use. The pharmaceutical formulation contains peroxidic species or reaction products resulting from oxidation of an alkene, such as geraniol, by an oxygen-containing oxidizing agent, such as ozone; a penetrating solvent, such as dimethyl sulfoxide; a dye containing a chelated metal, such as hematoporphyrin; and an aromatic redox compound, such as benzoquinone. The pharmaceutical formulation is used to treat horses infected with Sarcocystis protozoal infections.

Abstract: Preeclampsia and preterm labor in a pregnant female mammal are treated by administering thereto a combination of a progestin and a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in further combination with one or more of a cyclooxygenase inhibitor, a PGI2-mimetic, a thromboxane (TXA2) inhibitor, a compound possessing TXA2-agonistic and TXA2-inhibiting properties, a compound possessing TXA2-antagonistic and PGI2-memetic activities, and a TXA2 antagonist.

Abstract: Disclosed is method for reducing myocardial cell damage during and/or after percutaneous coronary intervention in a subject's coronary artery. The method includes instilling a beta blocker directly into the subject's coronary artery prior to percutaneous coronary intervention. A kit for carrying out percutaneous coronary intervention is also disclosed. The kit includes a catheter and a beta blocker.

Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule in an amount sufficient to control the aberrant growth state e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. The present invention further makes available methods and reagents for ameliorating to consequences of hedgehog loss-of-function, ptc gain-of-function, or smoothened loss-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule, in an amount sufficient to ameliorate the In certain embodiments, the subject compounds, e.g., a cAMP analog, adenylate cyclase agonist, or cAMP phosphodiesterase inhibitor, regulate cAMP levels, which in turn modulates activity of the hedgehog pathway.

Abstract: (R)-6F-phenylephrine, essentially free of (S)-6F-phenylephrine, and an anesthetic formulation comprising (R)-6F-epinephrin or (R)-6F-phenylephrine and having improved stability compared to formulations containing their non-fluorinated analog, are disclosed. Further disclosed is a method of providing vasoconstriction in a mammal by administering the anesthetic formulation.

Abstract: Effects of MAO-A or MAO-B inhibitors such as L-deprenyl on both cerebral and peripheral vasculature, on non-vascular smooth muscle, on the nervous system, and on platelets, RBC, WBC, mast cells, macrophages, and glial cells are disclosed. The effects are the result of a mode of action for MAO-A or MAO-B inhibitors such as L-deprenyl which is totally unrelated to selective inhibition of MAO-A and/or MAO-B. Therapeutic methods of using MAO-A or MAO-B inhibitors such as L-deprenyl to treat a variety of disorders are disclosed.

Abstract: A method of chemosensitization which comprises administering at least one chemotherapeutic agent and at least one 3-aryloxy-3-phenylpropylamine to a subject in need thereof.

Abstract: Compounds of formula (Ia) as potent, &bgr;1-specific beta blockers with a short duration of action in the systemic circulation, wherein R is 3′,4′-dimethoxyphenyl.

Abstract: Optimal ratios of pharmaceutical compositions of &bgr;-1 and &bgr;-2 agonists with their respective antagonists. Safer, more cost-effective drugs for heart and lung therapies are made by combining specific antagonists with their agonists to prevent desensitization of cellular receptors, reducing some of the unwanted side-effects of the agonist drugs alone. Determining the optimal concentration of an antagonist or inhibitor, which is necessary to prevent desensitization, without causing unnecessary and unwanted inhibition, creates a new class of pharmaceuticals. To derive an optimum ratio for a specific composition, a formulative method is provided to detail how competitive antagonists of the receptor should be combined with agonists, in specific proportions, to maximize and maintain receptor response throughout drug administration.

Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: Ophthalmic compositions having negligible side effects on the heart can be obtained by using as the active ingredient an adrenergic &bgr; receptor agonist having a high selectivity toward adrenergic &bgr;2 receptor. These compositions are usable as preventives or therapeutics for xerophthalmic disorder and keratoconjunctival disorder.

Abstract: A novel oral dosage to be delivered to the stomach comprising a safe and effective amount of an active ingredient selected from the group consisting of emepronium bromidebromide, doxycycline, and other tetracyclines/antibiotics, iron preparations, quinidine, nonsteroidal anti-inflammatory drugs, alprenolol, ascorbic acid, captopril, theophylline, zidovoudine (AZT), bisphosphonates and mixtures thereof and pharmaceutically-acceptable excipients, wherein said oral dosage form is a generally oval form and film coated to facilitate rapid esophageal transit and avoid irritation in the mouth, buccal cavity, pharynx, and esophagus.

Abstract: SGLT2 inhibiting compounds are provided having the formula wherein n is 0, 1 or 2; A is  or heteroaryl which may contain 1 to 4 heteroatoms in the ring which may be selected from N, O, S, SO, and/or SO2, bearing substituents R3 and R4; and R1 to R4 are as defined herein. A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with one, two or more other antidiabetic agents and/or one, two or more hypolipidemic agents.

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 invention disclosed some derivative chemically with Hydroxyphenyl carboxylic acid and Alcohol based phenoxypropanolamine and associated alanyl-proline peptide derivatives.

Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.

Abstract: Compositions and methods for the treatment of anorectal disorders are provided in which certain combinations of NO donors, PDE inhibitors, superoxide (O2−) scavengers, &bgr;-adrenergic agonists, cAMP-dependent protein kinase activators, &agr;1-adrenergic antagonists, L-type Ca2+ channel blockers, estrogens, ATP-sensitive K+ channel activators and smooth muscle relaxants are used.

Abstract: This invention relates to reduced stinging, sustained release ophthalmic formulations and the method of treatment comprising administering such formulations topically to the eye when in need thereof.

Abstract: Controlled cessation of heart beat during coronary bypass surgery and other cardiac surgeries on a beating heart improves surgical technique, and is achieved typically by electrical stimulation of the vagus nerve and administration of a combination of drugs.

Abstract: An aqueous, sterile pharmaceutical composition suitable for parenteral administration for the treatment of cardiac conditions, comprising methyl-3-[4-(2-hydroxy-3-isopropylamino) propoxy] phenylpropionate hydrochloride (esmolol hydrochloride), a buffering agent and an osmotic-adjusting agent, as well as a method for its manufacture, are disclosed.

Abstract: Effects of MAO-A or MAO-B inhibitors such as L-deprenyl on both cerebral and peripheral vasculature, on non-vascular smooth muscle, on the nervous system, and on platelets, RBC, WBC, mast cells, macrophages, and glial cells are disclosed. The effects are the result of a mode of action for MAO-A or MAO-B inhibitors such as L-deprenyl which is totally unrelated to selective inhibition of MAO-A and/or MAO-B. Therapeutic methods of using MAO-A or MAO-B inhibitors such as L-deprenyl to treat a variety of disorders are disclosed.

Abstract: Novel calcilytic compounds are provided.

Abstract: A single dosage medication formulation has a beta-adrenergic blocker and a cholesterol lowering agent that is a statin combined in a single oral formulation for treatment of and reducing the risk of cardiovascular disease to enhance simplicity, cost reduction, convenience, and patient compliance with the use of these agents.

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: The present invention relates to methods and compositions comprising a very low dose of cyclobenzaprine or metabolite thereof for preventing and treating Generalized Anxiety Disorder. The present invention further relates to methods and compositions for treating and preventing symptoms associated with Generalized Anxiety Disorder using a very low dose of cyclobenzaprine.

Abstract: The present invention comprises methods and compositions for the treatment of bronchorestrictive disorders, including asthma, in humans or animals. The methods and compositions are effective in treatment of inflammatory responses, such as those found in asthma and other related pathologies.

Abstract: A method and composition for treating macular disorders. A pharmologically effective amount of a carbonic anhydrase inhibitor is combined with a pharmologically effective amount of an ocular hypotensive agent sufficient to improve visual function.

Abstract: The invention relates to the method of use of compounds with B3-agonist activity for inhibiting uterine contractions, preventing or slowing down premature labor, or for the treatment and/or prophylaxis of dysmenorrhea.

Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule in an amount sufficient to control the aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. The present invention further makes available methods and reagents for ameliorating the consequences of hedgehog loss-of-function, ptc gain-of-function, or smoothened loss-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule, in an amount sufficient to ameliorate the In certain embodiments, the subject compounds, e.g., a cAMP analog, adenylate cyclase agonist, or cAMP phosphodiesterase inhibitor, regulate cAMP levels, which in turn modulates activity of the hedgehog pathway.

Abstract: The present invention comprises methods and compositions for the treatment of bronchorestrictive disorders, including asthma, in humans or animals. The methods and compositions are effective in treatment of inflammatory responses, such as those found in asthma and other related pathologies.

Abstract: A method for the manufacture of metoprolol wherein the process is performed in water as solvent.

Abstract: Optimal ratios of pharmaceutical compositions of &bgr;-1 and &bgr;-2 agonists with their respective antagonists. Safer, more cost-effective drugs for heart and lung therapies are made by combining specific antagonists with their agonists to prevent desensitization of cellular receptors, reducing some of the unwanted side-effects of the agonist drugs alone. Determining the optimal concentration of an antagonist or inhibitor, which is necessary to prevent desensitization, without causing unnecessary and unwanted inhibition, creates a new class of pharmaceuticals. To derive an optimum ratio for a specific composition, a formulative method is provided to detail how competitive antagonists of the receptor should be combined with agonists, in specific proportions, to maximize and maintain receptor response throughout drug administration.

Abstract: Methods are disclosed for increasing the effectiveness of dextromethorphan in treating chronic or intractable pain, for treating tinnitus and for treating sexual dysfunction comprising administering dextromethorphan in combination with a therapeutically effective dosage of a debrisoquin hydroxylase inhibitor. A preferred combination is dextromethorphan and the oxidative inhibitor quinidine.