Abstract: A method and composition is described for treating impaired neurological function, CNS disease or condition, including altered state of consciousness disorders in a human subject, comprising parenterally administering a composition comprising aminoadamantane derivatives or salts thereof, alone or in combination with other neuroprotective and/or anti-inflammatory compounds, in a pharmacologically effective amount. In some embodiments, a method for treating traumatic brain injury caused by a stroke or an accident in a human subject is provided comprising intravenously administering a composition comprising amantadine hydrochloride in a pharmacologically effective amount to the subject in need thereof.

Abstract: Provided herein are compounds that are useful in the treatment of pain in a subject.

Abstract: The invention provides (1) processes for making substantially-pure (?) huperzine A and substantially-pure (?) huperzine A derivatives; (2) compositions useful in making substantially-pure (?) huperzine A and substantially-pure (?) huperzine A derivatives; and (3) methods of treating or preventing neurological disorders using substantially-pure (?) huperzine A and substantially-pure (?) huperzine A derivatives.

Abstract: The invention provides (1) processes for making substantially-pure (?) huperzine A and substantially-pure (?) huperzine A derivatives; (2) compositions useful in making substantially-pure (?) huperzine A and substantially-pure (?) huperzine A derivatives; and (3) methods of treating or preventing neurological disorders using substantially-pure (?) huperzine A and substantially-pure (?) huperzine A derivatives.

Abstract: The invention provides (1) processes for making substantially-pure (?) huperzine A and substantially-pure (?) huperzine A derivatives; (2) compositions useful in making substantially-pure (?) huperzine A and substantially-pure (?) huperzine A derivatives; and (3) methods of treating or preventing neurological disorders using substantially-pure (?) huperzine A and substantially-pure (?) huperzine A derivatives.

Abstract: The present invention is directed to Benzomorphan Analog compounds of the Formula I?, Formula IA?, Formula IB?, Formula IC?, or Formula ID? as shown below; and related Formula I?, Formula IA?, Formula IB?, Formula IC?, or Formula ID?; Formula I, Formula IA, Formula IB, Formula IC, or Formula ID; wherein R1, R2a, R2b, R3 and R4 are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.

Abstract: The present application relates to analogues of morphan and morphinan, compositions thereof, and methods for treating a disease or condition comprising administering an effective amount of the compounds or compositions to a subject in need thereof.

Abstract: The present invention relates to compounds defined by formula I wherein the groups A, B, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.

Abstract: A system is described for long-term controlled release delivery of a drug or a therapeutic agent. According to the invention, one or more drugs or therapeutic agents contained in microspheres are mixed with a temperature sensitive hydrogel which is then introduced directly to the desired situs of the drug or therapeutic agent. The temperature sensitive hydrogel may also contain a drug or a therapeutic agent, for example, a pain relieving drug, for a short-term controlled release. The temperature sensitive hydrogel is in liquid state at room temperature, but upon injection, shortly becomes gelatinous. This system is particularly suitable for treatment of diseases, disorders, or conditions, for example, tumors, discogenic back pain, or arthritis, warranting localized administration of a drug or a therapeutic agent. In addition, the specification provides a method for production of a drug- or therapeutic agent-containing microspheres.

Abstract: The disclosure provides methods of treating glioblastoma, methods of screening for compounds that treat glioblastoma, and pharmaceutical compositions useful the treatment of glioblastoma.

Abstract: A compound of formula I is disclosed. Compounds of formula I are useful as analgesics, anti-inflammatory agents, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.

Abstract: The invention relates to drug preparations with controlled active ingredient released in the form of microtablets which contain, as active ingredient, flupirtin or one of its physiologically compatible salts, and to processes for their production.

Abstract: The present application relates methods for treating a depressive symptom comprising administering an effective amount of a ? opioid receptor agonist or a pharmaceutically acceptable salt thereof to a subject in need thereof. Non-limiting examples of such agonist include the compounds of Formulas I, II, III, and IV, as well as the compounds of Table A.

Abstract: A compound of formula I is disclosed. Compounds of formula I are useful as analgesics, anti-inflammatory agents, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.

Abstract: The present application relates to analogues of morphan and morphinan, compositions thereof, and methods for treating a disease or condition comprising administering an effective amount of the compounds or compositions to a subject in need thereof.

Abstract: Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenolic opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the phenolic opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.

Abstract: The present invention relates to co-extruded pharmaceutical compositions and dosage forms including an active agent, such as an opioid agonist, and an adverse agent, such as an opioid antagonist. Such compositions and dosage forms are useful for preventing or discouraging tampering, abuse, misuse or diversion of a dosage form containing an active pharmaceutical agent, such as an opioid. The present invention also relates to methods of treating a patient with such a dosage form, as well as kits containing such a dosage form with instructions for using the dosage form to treat a patient.

Abstract: The present invention relates to compounds defined by formula I wherein the groups R1 to R3, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.

Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.

Abstract: The present invention includes compositions and methods for treating certain conditions, the composition comprising a choline compound; a cholinesterase inhibitor; and Acetyl-L-Carnitine, wherein the composition is used to treat at least one of autonomic dysfunctions or vascular diseases.

Abstract: Methods and compositions containing huperzine are used to prevent and alleviate seizures. The invention is also directed to methods and compositions for using huperzine for the prevention and/or treatment of orthostatic hypotension.

Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.

Abstract: Specific Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein m, X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.

Abstract: The present document describes a composition containing an effective amount of an acetylcholinesterase inhibitor, a solvent, and a permeation enhancer in a pharmaceutically acceptable carrier, and uses thereof.

Abstract: The present invention is directed to Benzomorphan Analog compounds of the Formula I-ID as shown below, wherein R1, R2a, R2b, R3 and R4 are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.

Abstract: A compound of formula I is disclosed. Compounds of formula I are useful as analgesics, anti-inflammatory agents, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.

Abstract: The present invention relates to compounds defined by Formula (I), wherein the groups A, B, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.

Abstract: The present invention relates to compounds defined by formula I wherein the groups A, B, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.

Abstract: The present invention is directed to Benzomorphan Analog compounds of the Formula I?, Formula IA?, Formula IB?, Formula IC?, or Formula ID? as shown below; and related Formula I?, Formula IA?, Formula IB?, Formula IC?, or Formula ID?; Formula I, Formula IA, Formula IB, Formula IC, or Formula ID; wherein R1, R2a, R2b, R3 and R4 are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.

Abstract: Compounds of formulas: are disclosed. The compounds are useful for ameliorating the side effects of therapeutic opiates.

Abstract: Benzomorphan compounds are found to be useful for treating, ameliorating or preventing pruritus, and in particular pruritus associated with (including induced by) the administration of opioids. Antipruritic activity is believed to be mediated through the dual action of the compounds as mu opioid receptor antagonists and kappa opioid receptor agonists. Pharmaceutical compositions contain therapeutically effective amounts of these useful compounds, optionally in combination with second therapeutic agents, such as opioid or non-opioid analgesics or other compounds.

Abstract: The present invention provides pharmaceutical release systems comprising an therapeutically effective amount of flibanserin and at least one pharmaceutically acceptable excipient, characterized in that said pharmaceutical release systems exhibit a pharmacokinetic profile that is characterized by an average maximum flibanserin plasma concentration Cmax lower than 300 ng/mL, preferably lower than 200 ng/mL after administration of a single dose to healthy volunteers in fasted state or directly after a meal.

Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. 8-Carboxamides, thiocarboxamides, hydroxyamidines and formamides are preferred.

Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.

Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.

Abstract: The present invention provides compositions and methods for preventing, treating or reversing neuronal dysfunction in a mammal resulting from exposure to organophosphate nerve agents, organophosphate insecticides and incapacitating agents of the central nervous system (CNS); CNS injury, including traumatic brain injury, neurologic complications of cardiac surgery, perinatal asphyxia, and stroke, spinal cord injury, and peripheral nerve injury; and neuronal disorders associated with the loss of motor function including post-polio syndrome, amyotrophic lateral sclerosis, myasthenia gravis, Parkinson's disease and Rett syndrome; neurodegenerative disorders including Alzheimer's disease, mild cognitive impairment and schizophrenia; and cognitive impairment associated with aging.

Abstract: The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R3, R4 and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.

Abstract: The present invention is concerned with the use of combinations of opioid agonists and antagonists for treating Crohn's disease.

Abstract: The invention relates to compounds that are azaadamantane derivatives, particularly ether- or amine-substituted azaadamantane derivatives and salts and prodrugs thereof, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.

Abstract: Sustained-release formulations comprising huperzine A are disclosed herein. The formulations are for oral administration, and contain a carrier which comprises native albumin. Unit dosage forms of the formulations, and kits comprising such unit dosage forms are also disclosed herein. Methods utilizing the formulations for treating a medical condition treatable by huperzine A are also disclosed herein, as well as processes for preparing the formulations, and uses of huperzine A and albumin in the manufacture of a medicament.

Abstract: Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.

Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. 8-Carboxamides, thiocarboxamides, hydroxyamidines and formamides are preferred.

Abstract: The present invention relates to novel 1,2-dihydro-2-oxoquinoline compounds of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The compounds of the present invention are useful in the treatment/prevention of various disorders that are mediated by 5-HT4 receptor activity.

Abstract: The present invention provides compositions and methods for preventing, treating or reversing neuronal dysfunction in a mammal resulting from exposure to organophosphate nerve agents, organophosphate insecticides and incapacitating agents of the central nervous system (CNS); CNS injury, including traumatic brain injury, neurologic complications of cardiac surgery, perinatal asphyxia, and stroke, spinal cord injury, and peripheral nerve injury; and neuronal disorders associated with the loss of motor function including post-polio syndrome, amyotrophic lateral sclerosis, myasthenia gravis, Parkinson's disease and Rett syndrome; neurodegenerative disorders including Alzheimer's disease, mild cognitive impairment and schizophrenia; and cognitive impairment associated with aging.

Abstract: A pharmaceutical composition for external use which is an organogel containing a fatty acid ester and a glycerolglycerin fatty acid ester, in particular, a novel transdermally absorbable pharmaceutical composition for external use which has a drug such as non-narcotic analgesics as an active ingredient made in organogel form containing a drug such as non-narcotic analgesics as an active ingredient, a fatty acid ester and a glycerolglycerin fatty acid ester, and a method for producing the composition. The pharmaceutical composition significantly improves skin permeability of drugs such as non-narcotic analgesics and allows a sufficient amount of drug to permeate the skin sustainably. Moreover, since the pharmaceutical composition is in organogel form, it can be easily applied to a preparation in practice. In addition, the pharmaceutical composition can provide efficient use and the like of drugs due to a high drug release rate and therefore is highly useful.

Abstract: The invention relates to a process for the synthesis of quaternized compounds of formula:

Abstract: The present invention relates generally to the field of pain management, and in particular, the management of neuropathic or inflammatory pain including a neuropathic or inflammatory component of nociceptive pain. More particularly, the present invention provides methods and compositions which treat, alleviate, prevent, diminish or otherwise ameliorate the symptoms of neuropathic or inflammatory pain. The present invention further contemplates combination therapy involved in the treatment of pain in association with the treatment of a particular disease condition or pathology. The present invention further also provides sustained and slow release formulations, tamper-proof deliver systems and stents, catheters and other mechanical devices coated with formulations which permit sustained or slow release of active ingredients involved in pain management.

Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.