Abstract: An apomorphine pharmaceutical dosage security system embodied in multiple dosage forms including oral dosage forms, transdermal delivery patches, nasal delivery forms, and transdermal dosage forms. Within the present invention is an amount of apomorphine adapted to be bioavailable to a degree sufficient to cause emesis or severe nausea when an overdose amount of a therapeutic agent enters systemic circulation.

Abstract: Use of ascorbic acid in the manufacture of a powdered medicament for nasal delivery, said medicament comprising an active agent such as apomorphine that exhibits toxicity to ciliated tissue, for ameliorating said toxicity.

Abstract: The present invention includes a group of chemical compounds useful as modulators of calcium ion (Ca2+) channels, especially for T-type, N-Type and L-type channels. The present invention also includes pharmaceutical compositions comprising these calcium ion channel modulating agents and methods of using these calcium ion channel modulating agents for the treatment diseases and conditions associated with the calcium ion channels.

Abstract: The invention relates to a compound of general formula I, II, III, IV, V, VI, VII, VIII, IX, X or a tautomer and the stereochemically isomeric forms thereof or pharmaceutically acceptable salts thereof, a N-oxide form thereof or a pro-drug thereof. The compound is usable as a medicament for the treatment of mycobacterial disease.

Abstract: Compounds of the disclosure provide compositions, which are effective for prophylaxis and treatment of diseases or disorders, such as cell-proliferation, angiogenesis, or apoptosis mediated diseases. The disclosure encompasses compounds, analogs, prodrugs, metabolites, and pharmaceutically acceptable salts thereof, pharmaceutical compositions, and methods for prophylaxis and treatment of diseases and other maladies or conditions involving cancer, tumors, and like conditions. The disclosure also provides therapeutic methods including the administration of an effective amount of a compound of the disclosure.

Abstract: The invention features derivatives of R(?)-2-methoxy-11-hydroxyaporphines and methods of treating Parkinson's disease, sexual dysfunction, and depressive disorders therewith.

Abstract: Compounds of Formula I that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.

Abstract: A method of safely and specifically treating the combined metabolic disturbances of insulin resistance and visceral adiposity in male subject with visceral adiposity, metabolic syndrome (also known as the ‘insulin resistance syndrome’, and ‘syndrome X’), type II diabetes, or insulin resistance by administering a 5-alpha reductase inhibiting compound of structural formula I, II, III, or IV is disclosed. The method is also concerned with the use of the 5alpha reductase inhibiting compound together with antidiabetic agents, lipid lowering agents, antihypertensive agents, antiobesity agents, testosterone, testosterone precursors, testosterone prodrugs, testosterone analogs, and other androgen receptor agonists for treating visceral adiposity, metabolic syndrome, type II diabetes and insulin resistance in men.

Abstract: 13-substituted 5,6-dihydrodibenzo[a,g]quinolizinium salt compounds of the general formula (I): processes for the preparation of said compounds, pharmaceutical compositions containing said compounds and the use of said compounds for the manufacture of medicaments suitable for the treatment of cancerous diseases.

Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

Abstract: The present invention relates to pharmaceutical compositions for intranasal administration to a mammal that contain an effective amount of an opioid, a liquid nasal carrier for the opioid, and optionally a sweetener, flavoring agent or masking agent. In some embodiments of the present invention, the pharmaceutical compositions have improved bioavailability. In other embodiments of the present invention, the opioid compositions improve patient compliance.

Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Abstract: The invention provides compounds of formula I or formula II: wherein: the bond represented by is a single bond or a double bond, and R1—R5, X, and Y have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I or II, processes for preparing compounds of formula I or II, intermediates useful for preparing compounds of formula I or II, and therapeutic methods for treating cancer and other topoisomerase related conditions using compounds of formula I or II.

Abstract: A medicament effective for inhibiting onset of Alzheimer disease via intracellular aggregation mechanism is provided. A medicament for prophylaxis and treatment of Alzheimer disease comprising as an active ingredient apomorphine hydrochloride wherein cell death dependent upon intracellularly accumulated amyloid ? proteins and/or p53 is inhibited; and/or wherein a level of intracellularly accumulated amyloid ? proteins and/or phosphorylated tau proteins is lowered to improve energy production, protein metabolism and synaptic function of neurons so as to ameliorate the recognition capacity such as defects of memory.

Abstract: A composition comprising a benzodiazepine agonist, a benzodiazepine antagonist, and a pharmaceutical acceptable carrier in an effective ratio so as to preserve the therapeutic effects of the benzodiazepine agonist while modulating the side effects of the benzodiazepine agonist.

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.

Abstract: The present invention relates to improved treatment of diseases and disorders of the central nervous system by administration of apomorphine. In particular, the administration is via pulmonary inhalation. The invention provides the means for improving the treatment of a number of conditions, including Parkinson's Disease.

Abstract: The present invention relates to new prop-2-yn-1-amine inhibitors of monoamine oxidase type B activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Disclosed herein are novel imino-indeno[1,2-c]quinoline derivatives of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein each of the substituents is given the definition as set forth in the Specification and Claims. Also disclosed are the preparation processes of these derivatives, their synthetic precursors and their uses in the manufacture of pharmaceutical compositions for use in the treatment of cancers.

Abstract: The present invention relates to compounds for the inhibition of poly(ADP-ribose) polymerase (PARP). In some embodiments, the compounds have the Formula: wherein the constituent variables are as defined herein. The invention further provides methods for the use of the compounds disclosed herein.

Abstract: Methods and compositions for the treatment of alpha-adrenoceptor mediated conditions.

Abstract: A method of treating or inhibiting non-digestive tract derived abdominal disorders associated with pain, in particular interstitial cystitis, chronic pelvic pain syndrome and/or abdominal pain associated with endometriosis, in a patient in need thereof, by administering to the patient a pharmaceutically effective amount of a 5-HT3 receptor antagonist, in particular cilansetron, or a pharmacologically compatible derivative thereof, such as a salt and/or a solvates.

Abstract: Provided herein are tetracyclic 1H-indeno[1,2-b]pyridine-2(5H)-one analogs and derivatives, compositions comprising an effective amount of a tetracyclic 1H-indeno[1,2-b]pyridine-2(5H)-one analog and/or derivative and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes mellitus, a diabetic complication, a reoxygenation injury resulting from organ transplantation, an ischemic condition, a neurodegenerative disease, renal failure, a vascular disease, a cardiovascular disease, an ocular or opthalmologic disease, cancer, a complication of prematurity, cardiomyopathy, retinopathy, nephropathy, contrast induced nephropathy, neuropathy, erectile dysfunction or urinary incontinence, comprising administering to a subject in need thereof an effective amount of a tetracyclic 1H-indeno[1,2-b]pyridine-2(5H)-one analog or derivative.

Abstract: Pseudobase benzo[c]phenanthridines and the pharmaceutically acceptable salts thereof of Formula I are provided herein. The variables R, R1, R2, R3, and R4 are defined herein. Certain pseudobase benzo[c]phenanthridines provided herein act as prodrugs, targeting the parent benzo[c]phenanthridinium alkaloid to hydrophilic or hydrophobic regions in the body. Pharmaceutical compositions comprising a pseudobase benzo[c]phenanthridine and a carrier, excipient, or diluent are provided herein. Methods of treating or preventing microbial, fungal and or viral infections and methods of treating diseases and disorders responsive to protein kinase C modulation, topoisomerase I, and/or topoisomerase II modulation are also provided.

Abstract: The present invention is in the field of oral, abuse resistant pharmaceutical compositions of opioid agonists, extended release pharmaceutical compositions of opioid agonists and extended release abuse resistant pharmaceutical compositions of opioid agonists and the use thereof. The present invention is also directed to extended release pharmaceutical compositions and the use thereof for preventing or minimizing the risk of abuse and/or toxicity from either intentional or unintentional tampering. The present invention is further directed at a method of preventing or minimizing the risk of abuse and/or toxicity from either intentional or unintentional tampering.

Abstract: A liquid aqueous formulation for the intranasal administration of apomorphine includes: (a) at least about 15 mg/ml of apomorphine; and (b) a solubilising agent selected from (i) at least one polyoxyethylene-polyoxypropylene copolymer (poloxamer); (ii) at least one cyclodextrin; and (iii) at least one cyclodextrin together with chitosan. The formulations of the invention can be used in the treatment or management of Parkinson's disease and erectile dysfunction.

Abstract: An adjunctive accessory article (25) for controlled release of at least a single physiologically active agent form an indwelling medical device so equipped is provided. The article is configurable as a tubular element upon a portion of the indwelling medical device, with barriers or facilitating coverings overlaying the carrier in furtherance of the controlled release of the active agent. To the extent that requires, affixation means for stable placement upon an indwelling device are further contemplated. Finally, a variety of application systems are described in connection to deployment of sleeve articles upon a portion of an indwelling device.

Abstract: The process includes the steps of (i) dissolving finasteride in a substantially anhydrous organic solvent selected among n-butyl acetate, iso-butyl acetate, sec-butyl acetate, tert-butyl acetate, C5 alkyl acetate and mixtures thereof, at a temperature equal to or lower than the boiling point of said organic solvent; (ii) slowly cooling said finasteride solution to a cooling temperature determined on the basis of the chosen solvent; (iii) maintaining the resulting suspension at the cooling temperature for a period of time equal to or less than 16 hours; and (iv) recovering the resulting solid phase containing Form I of finasteride, for example by means of filtration, and removing the solvent, for example by means of drying said crystals. The process allows for obtaining the Form I of finasteride only and in a pure form.

Abstract: The invention provides a class of dopamine transporter inhibitors of formula (I) (DAT inhibitors), packaged pharmaceuticals comprising such inhibitors, and their uses in treating, or manufacturing medicaments for treating disease conditions including Parkinson's disease, when assessed by one or more of Hoehn and Yahr Staging of Parkinson's Disease, Unified Parkinson Disease Rating Scale (UPDRS), and Schwab and England Activities of Daily Living Scale. Related business methods such as marketing the inhibitors to healthcare providers are also provided.

Abstract: Substituted indenoisoquinolinium compounds, and pharmaceutical formulations of substituted indenoisoquinolinium compounds are described. Also described are processes for preparing substituted indenoisoquinolinium compounds. Also described are methods for treating cancer in mammals using the described substituted indenoisoquinolinium compounds or pharmaceutical formulations thereof.

Abstract: Apparatus and methods deliver physiologically active agents in the presence of adjuvant gases. The adjuvant gases can enhance the effectiveness of the drug, lower the dosage of drug or concentration of drug necessary to achieve a therapeutic result, or both. Exemplary adjuvant gases include carbon dioxide, nitric oxide, nitrous oxide, and dilute acid gases.

Abstract: Methods are provided for the synthesis of 1-[4-(substituted phenyl)-piperazin-1-yl ] -2- [3-(1H-imidazol-2-yl)-pyrazolo [3,4-b]pyridin-1-yl]-ethanone compounds via construction of the imidazole portion onto the corresponding aldehyde or nitrile compounds.

Abstract: Aromatized A-ring derivatives of tetracycline compounds are described.

Abstract: A method for the treatment and/or prophylaxis of a neurological and/or neuropsychiatric disorder associated with altered dopamine function comprising administering to the eye of a patient in need thereof an effective amount of an agent that modulates neurotransmitter production or function.

Abstract: The present invention is concerned with the use of PDE5 inhibitors in medicine.

Abstract: The present invention relates to Indenoisoquinolinone Analogs, compositions comprising an effective amount of an Indenoisoquinolinone Analog and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes mellitus, a diabetic complication, reoxygenation injury resulting from organ transplantation, an ischemic condition, a neurodegenerative disease, renal failure, a vascular disease, a cardiovascular disease, cancer, a complication of prematurity, cardiomyopathy, retinopathy, nephropathy, neuropathy, erectile dysfunction or urinary incontinence, comprising administering to a subject in need thereof an effective amount of an Indenoisoquinolinone Analog.

Abstract: The invention relates to the use of a compound antagonist to the NK2 receptors of A neurokinine for the preparation of drugs useful for preventing and treating sexual dysfunction.

Abstract: The present invention relates to new substituted hydroxyphenylamine based modulators of hormone and/or pigment levels, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: A dermal or transdermal therapeutic system comprising a reservoir that contains at least one active substance, an active substance-permeable membrane which delimits the active-substance reservoir, and a closing layer. The closing layer is impermeable to the active substance at a temperature lying below the skin temperature while being permeable at skin temperature and above.

Abstract: A reduction in the side effects of treating with an agent having combined 5HT2/5HT3 and alpha-2 antagonistic activity is obtained by administering an agent having selective norepinephrine reuptake inhibitory or histamine H1 agonist activity. A combined dosage form comprising an agent having 5HT2/5HT3 and alpha-2 antagonistic activity and an agent having selective norepinephrine reuptake inhibitory or histamine H1 agonist activity is presented. Some embodiments of the combined dosage form comprise an immediate release component comprising an agent having 5HT2/5HT3 and alpha-2 antagonistic activity and a delayed release component comprising an agent having selective norepinephrine reuptake inhibitor or histamine H1 agonist activity.

Abstract: The invention provides compositions and methods utilizing a nicotinic receptor modulator, e.g., to reduce or eliminate a side effect associated with dopaminergic agent treatment. In some embodiments, the invention provides compositions and methods utilizing a combination of a dopaminergic agent and a nicotinic receptor modulator that reduces or eliminates a side effect associated with dopaminergic agent treatment.

Abstract: The present invention relates to new benzenesulfonamide modulators of alpha-1A adrenergic receptors, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention is directed to azonafide derivatives obtained by reacting azonafide with aldehydes, acyl halides, thioacyl halides, monoisocyanates, isothiocyanates, sulfonyl halides, monohalogenoalkanes, monohalogenoalkenes or monohalogenoalkynes, and are useful as active ingredients of pharmaceutical compositions for the prevention and treatment of cell proliferative disorders, in particular several forms of cancer.

Abstract: The invention features methods, kits, and compositions for generating new hair follicles and growing hair on a subject.

Abstract: An azonafide-based compound of Formula I, a composition comprising the compound, and a method of using the compound to deliver a cytotoxic azonafide derivative to a cell, as well as related compounds and methods for the use thereof to pre-pare an azonafide-based compound of Formula I.

Abstract: This invention concerns compositions for the treatment of Lower Urinary Tract Symptoms (LUTS), and especially LUTS which results from benign prostatic hypertrophy. The compositions of the invention comprise a Beta-3 agonist described below, optionally in combination with a 5-alpha reductase inhibitor, or an NK-1 antagonist or an alpha-1 adrenergic antagonist or an anti-muscarinic agent. The invention also includes compositions comprising a beta-3 agonist and two additional active agents selected from a 5-alpha reductase inhibitor, an NK-1 antagonist, an alpha-1 adrenergic antagonist or an anti-muscarinic agent.

Abstract: A solid pharmaceutical dosage form that is safeguarded against abuse, comprising at least one active substance that is susceptible to abuse and at least one emetic that is spatially separate from the at least one active substance. The active substance or substances are present in the form of at least one sub-unit (a), and the at least one emetic is present in the form of at least one sub-unit (b), and the emetic from sub-unit (b) is not activated in the body if the dosage form has been correctly administered as prescribed.

Abstract: The invention describes a pharmaceutical composition comprising at least compound selected from the group of demethylating agents and HDAC inhibitors and at least one somatostatin analog or dopamine agonist for the treatment of a tumor which expresses a somatostatin and/or dopamine receptor.

Abstract: The invention relates to the film products and methods of their preparation that demonstrate a non-self-aggregating uniform heterogeneity. Desirably, the films disintegrate in water and may be formed by a controlled drying process, or other process that maintains the required uniformity of the film. The films contain a polymer component, which includes polyethylene oxide optionally blended with hydrophilic cellulosic polymers. Desirably, the films also contain a pharmaceutical and/or cosmetic active agent with no more than a 10% variance of the active agent pharmaceutical and/or cosmetic active agent per unit area of the film.

Abstract: The present invention provides a method of promoting bone growth in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I. The present invention also provides methods for the treatment of renal disease and cancer.