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: Disclosed are naphthalinamidinimide of formula (I), wherein R1, R2, R3, R4, R5 and R6 independently from each other are hydrogen; or C1-C37alkyl; wherein—one to 10 of the CH2 units of C1-C37alkyl independently from each may be substituted by carbonyl groups; oxygen atoms; sulphur atoms; selenium atoms; tellurium atoms; cis- or trans-CH?CH— groups; acetylenic C?C— groups; 1,2-, 1,3- or 1,4-substituted phenyl radicals; 2,3-, 2,4-, 2,5-, 2,6-, 3,4- or 3,5-disubstituted pyridine radicals; 2,3-, 2,4-, 2,5- or 3,4-disubstituted thiophene radicals; 1,2-, 1,3-, 1,4-, 1,5-, 1,6-, 1,7-, 1,8-, 2,3-, 2,6- or 2,7-disubstituted 1,2-, 1,3-, 1,4-, 1,5-, 1,6-, 1,7-, 1,8-, 1,9-, 1,10-, 2,3-, 2,6-, 2,7-, 2,9-, 2,10- or 9,10-disubstituted anthracene radicals; wherein one or 2 CH— groups of the CH?CH— groups, the naphthalene radicals and the anthracene radicals may be substituted by nitrogen atoms; —up to 12 single hydrogen atoms of the CH2— groups independently from each other may be substituted at the same carbon atoms by fluor

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

Abstract: Methods of preventing and/or treating at least one symptom of Restless Leg Syndrome (RLS) and its related disorders, including disorders such as periodic limb movements in sleep (PLMS) and periodic limb movement disorder (PLMD), are disclosed. The methods comprise identifying a host, afflicted with Restless Leg Syndrome (RLS) and its related disorders; and administering to the host a pharmaceutically effective amount of a 4-hydroxyphenylpyruvate dioxygenase. Also provided are methods and compositions for treating/preventing sleep disorders, and methods and compositions for improving sleep quantity and adequacy.

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 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 a cabergoline crystal form L, its preparation from halogenated aromatic solvents and aliphatic hydrocarbons and to pharmaceutical compositions containing the new form.

Abstract: Described are compounds having a thiazolhydrazide scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said thiazolhydrazide compounds can be used for prophylaxis and/or treatment of neurodegenerative diseases and conditions.

Abstract: The present invention relates to a stable pharmaceutical composition of a poorly water-soluble drug with a view to increasing its solubility and bioavailability. The present invention relates to a solid dispersion of a poorly water-soluble drug.

Abstract: The present invention relates to a transdermal therapeutic system (TTS) consisting of an impermeable coating, a matrix containing an ergoline compound having the formula (I) or a physiologically compatible salt or derivative thereof, wherein R1 denotes an H atom or a halogen atom and R2 is an alkyl group having 1 to 4 carbon atoms and denotes a single or double bond, and a removable protective layer, wherein the ergoline compound or a physiologically compatible salt or derivative thereof is stabilised by an antioxidant and a basic polymer.

Abstract: The present invention provides IA derivative compounds of the formula: where the variables are described herein.

Abstract: Disclosed are pharmaceutical compositions comprising mirtazapine and an anticonvulsant drug. Also disclosed are methods of preventing weight gain associated with the administration of mirtazapine comprising identifying a patient to whom mirtazapine is to be administered and administering to said patient a pharmaceutical composition comprising mirtazapine and an anticonvulsant drug. Further disclosed are methods of increasing the efficacy of mirtazapine comprising identifying a patient to whom mirtazapine is to be administered and administering to said patient a pharmaceutical composition comprising mirtazapine and an anticonvulsant drug.

Abstract: The use of a dopamine agonist in the manufacture of a medicament for the treatment or prevention of endometriosis.

Abstract: A method of treating trypanosomiasis in a mammal, which entails administering to a mammal in need thereof an effective amount of medicinal producting comprising a plant extract comprising one or more compounds of formula (I).

Abstract: The invention provides a class of inhibitors, packaged pharmaceuticals comprising such inhibitors, and uses of the inhibitors in treating, or the manufacturing medicaments for treating central nervous system disorders, including depression, anxiety, sleep disorders, obesity, attention deficit disorder (ADD), attention deficit hyperactivity disorder (ADHD), sexual dysfunction, substance abuse, and movement disorders. Related business methods, such as methods for conducting a pharmaceutical business and methods for conducting a medical assistance reimbursement program, are also provided.

Abstract: Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for screening and identifying compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase. In particular, provided herein are assays for the identification of compounds that inhibit or reduce the activity of a bacterial peptidyl tRNA hydrolase. The methods provided herein provide a simple, sensitive assay for high-throughput screening of libraries of compounds to identify pharmaceutical leads useful for preventing, treating, and managing a bacterial infection or one or more symptoms thereof. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.

Abstract: Disclosed are ergoline derivatives, Formula (I), wherein either each of R1 and R2, independently, is H; optionally R10 and/or R11-substituted-phenyl or -phenyl-C1-4alkyl; optionally R10 and/or R11-substituted-heteroaryl or -heteroaryl-C1-4alkyl; optionally R10 and/or R11-substituted heteroaryl N-oxide; optionally R10-substituted C1-C8 alkyl; optionally R10-substituted C2-C8 alkenyl, optionally R10-substituted C2-C8 alkynyl; optionally R10-substituted C3-C8 cycloalkyl, or optionally R10-substituted C4-C8 cycloalkenyl; or R1 and R2 form together with the nitrogen atom to which they are attached an optionally R10-substituted 3-8 membered ring containing in addition to the nitrogen atom up to 2 heteroatoms selected independently from N, O and S; R3 is H; OR1; CH2R1R2; (CH2)1-2NR1R2; CH2—CH2—OR1; CH2—CO—NR1R2; or CO—CH2R1R2; R4 is F; Cl; Br; I; OR1; NR1R2 or has one of the significances given for R1; and R5 has one of the significances given for R1, in free form or in salt form for preventing or treating disorders

Abstract: Methods for treating a patient having neurological, psychotic, and psychiatric disorders are described comprising the steps of administering to the patient an effective amount of a partial and/or full dopamine D1 receptor agonist, and administering to the patient an effective amount of a dopamine D2 receptor antagonist, Pharmaceutical compositions comprising a dopamine D1 receptor agonist and a dopamine D2 receptor antagonist are also described. The D1 dopamine receptor agonist and the D2 dopamine receptor antagonist can be administered to the patient in the same or in a different composition or compositions.

Abstract: The present invention provides novel methods and compositions for the treatment and prevention of headaches, vascular headaches, migraine headaches, cluster headaches, and migraine. One of the headaches, vascular headaches, migraine headaches, cluster headaches, and migraine treated by the methods and compositions of the invention is migraine.

Abstract: Activation of 5-HT2A receptors using agonists at surprisingly low concentrations was shown to potently inhibit TNF-?-induced inflammation in multiple cell types. Significantly, proinflammatory markers were also inhibited by the agonist, (R)-DOI, even many hours after treatment with TNF-?. With the exception of a few natural toxins, no current drugs or small molecule therapeutics demonstrate a comparable potency for any physiological effect. TNF-? and TNF-? receptor mediated inflammatory pathways have been strongly implicated in a number of diseases, including atherosclerosis, asthma, rheumatoid arthritis, psoriasis, type II diabetes, depression, schizophrenia, and Alzheimer's disease. Importantly, because (R)-DOI can significantly inhibit the effects of TNF-? many hours after the administration of TNF-?, potential therapies could be aimed not only at preventing inflammation, but also treating inflammatory injury that has already occurred or is ongoing.

Abstract: The present invention belongs to the field of pharmaceutical industry and relates to a new method for the treatment of psychostimulant addiction, in particular cocaine addiction, or pharmaceutically acceptable acid addition salts thereof, with a therapeutically effective amount of 9,10-didehydro-N-methyl-N-(2-propy-nyl)-6-methyl-8?-aminomethylergo-line in the form of free base or in the form of pharmaceutically acceptable addition salt, in particular the bimaleate salt, as well as pharmaceutical compositions containing said compound. In literature, the compound is also known under code LEK-8829. More particularly, present invention relates to a novel method of treatment for reduction of abstinence symptoms after cocaine withdrawal and for suppression the symptoms of craving for cocaine withdrawal and for suppression the symptoms of craving for cocaine reinforcement, and to the use of said active substance for the preparation of the pharmaceutical composition for the treatment of cocaine addiction.

Abstract: A method of treating Restless Legs Syndrome (RLS) comprises the joint administration of an agent selected from dopamine turnover increasing agent and dopaminergic receptor exciting agent, in particular pramipexole, and iron in a biologically usable form, in pharmacologically effective combined amounts. Also disclosed is a corresponding use; a pharmaceutical composition comprising an agent selected from dopamine turnover increasing agent and dopaminergic receptor exciting agent, in particular pramipexole, and iron in a biologically usable form, and a pharmaceutically acceptable carrier; a package comprising a pharmaceutical composition for per-oral administration comprising an agent selected from dopamine turnover increasing agent and dopaminergic receptor exciting agent and a pharmaceutically acceptable carrier and a pharmaceutical composition for per-oral administration comprising iron in a biologically usable form and a pharmaceutical acceptable carrier.

Abstract: This invention relates to 1-allyl ergot alkaloids and their derivatives with selective antagonistic properties to 5-HT2 receptors for the prevention of, and relief from, migraine-related headache, Parkinson's disease, disorders of the thrombocyte function, etc.

Abstract: The invention provides a method for diagnosing a disorder or disease associated with an imbalance of monoamines in a subject, or of diagnosing susceptibility of the subject to the same, wherein the method comprising (a) providing a sample from a subject to be tested, (b) measuring the levels of dopamine, melatonin and/or serotonin in the sample; and (c) comparing the levels measured in step (b) with levels of dopamine, melatonin and/or serotonin associated with a reference population of subjects, wherein a difference in one or more of the levels measured in step (b) with the levels of dopamine, melatonin and serotonin associated with the reference population of subjects is indicative of a positive diagnosis. The invention further provides a method of prevention or treatment of a disorder or disease associated with an imbalance of monoamines, and kits for the same.

Abstract: Disclosed is a series of somatostatin-dopamine chimeric analogs which retain both somatostatin and dopamine activity in vivo.

Abstract: Compounds, e.g., of formula (I) and (Ia), pharmaceutical compositions comprising the compounds and methods of using the compounds and pharmaceutical compositions for treating pain disorders, e.g., disorders associated with cephalic pain, are provided.

Abstract: There is provided pharmaceutical compositions for the treatment of migraine comprising a pharmacologically-effective amount of a triptan or an ergot, or a pharmaceutically-acceptable salt thereof; a pharmacologically-effective amount of an antiemetic compound, or a pharmaceutically-acceptable salt thereof; a bioadhesion and/or a mucoadhesion promoting agent; and carrier particles, wherein the active ingredients are presented in particulate form upon the surfaces of the carrier particles, which carrier particles are larger in size than the particles of the active ingredients; and the bioadhesion and/or mucoadhesion promoting agent is, at least in part, presented on the surfaces of the carrier particles.

Abstract: A transdermal therapeutic system for administering lipophilic, poorly water-soluble and/or sparingly skin-permeable pharmaceutical active substances. The active substance is present in a multi-component enhancer system consisting of 4 components and each component of the multi-component enhancer system is selected from a different one of the substance groups: a) terpenes, b) cyclic glucitol ethers, c) medium-chain triglycerides of capric and caprylic acid and/or of linoleic acid; and d) longer-chain alcohols having a chain length of 8 or more carbon atoms.

Abstract: Provided are new crystalline Forms VIII, IX, XI, XII, XIV, XV, XVI, XVII, and XVIII of cabergoline. Also provided are novel processes for preparation of cabergoline Form I, Form II, Form VII, and amorphous cabergoline.

Abstract: An electrotransport system for delivery of lisuride or a pharmaceutically acceptable salt thereof. The system has a donor electrode assembly, a counter electrode assembly, and a controller electrically connected to the donor electrode assembly and the counter electrode assembly. The donor electrode assembly has a donor reservoir that contains a lisuride salt. The controller is electrically connected to the donor and counter electrode assemblies and is operatable for controlling current for the electrotransport.

Abstract: Disclosed are ergoline derivatives, Formula (I), wherein either each of R1 and R2, independently, is H; optionally R10 and/or R11-substituted-phenyl or -phenyl-C1-4alkyl; optionally R10 and/or R11-substituted-heteroaryl or -heteroaryl-C1-4alkyl; optionally R10 and/or R11-substituted heteroaryl N-oxide; optionally R10-substituted C1-C8 alkyl; optionally R10-substituted C2-C8 alkenyl, optionally R10-substituted C2-C8 alkynyl; optionally R10-substituted C3-C8 cycloalkyl, or optionally R10-substituted C4-C8 cycloalkenyl; or R1 and R2 form together with the nitrogen atom to which they are attached an optionally R10-substituted 3-8 membered ring containing in addition to the nitrogen atom up to 2 heteroatoms selected independently from N, O and S; R3 is H; OR1; CH2R1R2; (CH2)1-2NR1R2; CH2—CH2—OR1; CH2—CO—NR1R2; or CO—CH2R1R2; R4 is F; Cl; Br; I; OR1; NR1R2 or has one of the significances given for R1; and R5 has one of the significances given for R1, in free form or in salt form for preventing or treating disorders

Abstract: The present invention provides compositions, methods, and kits for treatment of Parkinson's disease and other conditions for which treatment with a dopamine agonist is therapeutically beneficial. The invention provides a biocompatible nonerodible polymeric device which releases dopamine agonist continuously with generally linear release kinetics for extended periods of time. Dopamine agonist is released through pores that open to the surface of the polymeric matrix in which it is encapsulated. The device may be administered subcutaneously to an individual in need of continuous treatment with dopamine agonist.

Abstract: The present invention is directed to a method of simultaneously treating hypertension, hypertriglyceridemia, a pro-inflammatory state, a pro-coagulative state, and insulin resistance (with or without treating obesity or endothelial dysfunction), associated with or independent from Metabolic Syndrome, as well as vascular disease such as cardiovascular, cerebrovascular, or peripheral vascular disease comprising the step of administering to a patient suffering from such disorders a therapeutically effective amount of a central acting dopamine agonist. In one embodiment, the central acting dopamine agonist is bromocriptine, optionally combined with a pharmaceutically acceptable carrier.

Abstract: The present invention relates to compounds useful for detecting the activity of monoamine oxidases, compounds useful for competitively inhibiting monoamine oxidases, for determining inhibitors of monoamine oxidases and compounds useful for treating monoamine oxidase-related nervous system pathologies, as well as pharmaceutical compositions and methods of manufacture thereof.

Abstract: The present invention relates to usefulness of zonisamide as a pharmaceutical composition for treating dementia or cognitive impairment.

Abstract: The present invention provides an antiallergic latex or PVC product, which includes one or more natural antiallergic medicines selected from baicalin, matrine, liquorice saponin, tea polyphenol, arctigenin, oleanolic acid, tetrandrine, sodium ferulate, total alkaloid of asiatic moonseed rhizome, extraction of cortex dictamni radics, ginkgo bilobal A, total glycoside of Rhizoma Anemones flaccidae, extraction of engelhardtia chryolepis, magnolin, osthole, catechin. The latex or PVC products of the present invention are generally in the forms of glove or condom. The present invention solves the problem of hypersensitivity to condom or glove in prior arts by adding the natural antiallergic medicine into the matrix of latex or PVC.

Abstract: The present invention relates to the use of terguride and proterguride for the prophylaxis and/or the treatment of chronic pain conditions as well as to pharmaceutical compositions comprising terguride and/or proterguride optionally together with an opiate analgesic.

Abstract: Disclosed are new pharmaceutical formulations for aerosols with at least two or more active substances together with at least one surfactant for inhalative or nasal application.

Abstract: An objective of the present invention is to provide a harmful organism control agent that possesses excellent control effect against harmful organisms and can be safely used. The present invention provides a compound of formula (1) or a salt thereof. The present invention also provides a harmful organism control agent comprising the compound of formula (1). wherein R1, n, R2, and R3 are as defined in the specification.

Abstract: Method for enhancing in a mammalian cell the activity of an enzyme associated with Gaucher Disease by administering a competitive inhibitor of glucocerebrosidase in an amount effective to enhance the activity of the enzyme. Preferred compounds for use in the method are imino sugars and related compounds. In particular, C8–12-alkyl derivatives of N-alkyl-deoxynojirimycin, isofagomine compounds, and calystegine compounds are effective to enhance glucocerebrosidase activity.

Abstract: The present invention is directed to methods of treating addictive behavior and sleep disorders by administering compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The compounds used in the method of treatment of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including addictive behavior and sleep disorders.

Abstract: Methods are disclosed for the treatment and prevention of disorders and conditions including, but are not limited to, erectile dysfunction, affective disorders, weight gain, cerebral functional disorders, pain, obsessive-compulsive disorder, substance abuse, chronic disorders, anxiety, eating disorders, migraines, and incontinence. The methods comprise the administration of a dopamine reuptake inhibitor and optionally an additional pharmacologically active compound. Pharmaceutical compositions and dosage forms are also disclosed that comprise a dopamine reuptake inhibitor and optionally an additional pharmacologically active compound. Preferred dopamine reuptake inhibitors are racemic or optically pure sibutramine metabolites and pharmaceutically acceptable salts, solvates, and clathrates thereof. Preferred additional pharmacologically active compounds include drugs that affect the central nervous system, such as 5-HT3 antagonists.

Abstract: The invention provides methods for preparing amorphous physical form of cabergoline, and solvate form A of cabergoline useful in the preparation of the first mentioned physical form. A method for treating a prolactin disorder with medicaments prepared from amorphous physical form of cabergoline and solvate form A of cabergoline is also disclosed.

Abstract: A process for producing crystalline form I of cabergoline, which process comprises crystallization of the desired form from a toluene/diethyl ether mixture comprising raw cabergoline, followed by recovery and drying of the resulting crystals. A new solvate form V of cabergoline, useful as an intermediate, is also provided.

Abstract: Method for enhancing in a mammalian cell the activity of an enzyme associated with Gaucher Disease by administering a competitive inhibitor of glucocerebrosidase in an amount effective to enhance the activity of the enzyme. Preferred compounds for use in the method are imino sugars and related compounds. In particular, C8-12-alkyl derivatives of N-alkyl-deoxynojirimycin, isofagomine compounds, and calystegine compoiunds are effective to enhance glucocerebrosidase activity.

Abstract: Compositions and methods are provided for use in the treatment of cancer.

Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, R8, R9, X, b, k, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Abstract: It has been found that sampangine and related analogs such as benzo[4,5]sampangine, 4-bromosampangine and 4-methoxysampangine may be used as effective fungicidal agents for plants. Fungicidal plant compositions and methods of using the materials for such a purpose are also provided.