Abstract: This invention relates to an abuse deterrent dosage form of opioid analgesics, wherein an analgesically effective amount of opioid analgesic is combined with a polymer to form a matrix.

Abstract: This invention relates to an abuse deterrent dosage form of opioid analgesics, wherein an analgesically effective amount of opioid analgesic is combined with a polymer to form a matrix.

Abstract: Disclosed herein are substituted cyclohexanone-based NMDA receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Compounds of the formula (I), in which W, R, R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.

Abstract: One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor. The present invention also relates to the use of a compound of the invention for treating a mammal suffering from Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism or trichtillomania.

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: Disclosed are (i) compounds of a steroid, a ?-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, ?-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO?), or as the neutral species, nitric oxide (NO.) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.

Abstract: The present invention relates to novel compounds that are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

Abstract: A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to about 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. In another embodiment, a biocompatible polymer incorporates a C-nitroso moiety.

Abstract: The subject invention relates to 3-azabicyclo[3.2.1]octane derivatives, pharmaceutical compositions comprising such derivatives and methods of using such derivatives to treat disease states, disorders and conditions mediated by opioid receptors. The subject invention also particularly relates to using such derivatives to treat certain disorders and conditions, for example irritable bowel syndrome, drug addiction, depression, anxiety, schizophrenia and eating disorders, among others.

Abstract: The present invention is directed to methods of treating patients for pain by administering noribogaine. Noribogaine may also be used to treat patients for the symptoms associated with withdrawal from drug dependency. In the latter case, the noribogaine treatment should be supplemented with the administration of an opioid antagonist such as naloxone.

Abstract: This invention relates to an abuse deterrent dosage form of opioid analgesics, wherein an analgesically effective amount of opioid analgesic is combined with a polymer to form a matrix.

Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is where the variables have the definitions discussed herein. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat a disease or condition in which ?7 is known to be involved.

Abstract: Compounds of formula (I) wherein n is 0, 1, or 2; X is O, S, —NH—, and —N-alkyl-; Ar1 is a 6-membered aromatic ring; and Ar2 is a fused bicycloheterocycle. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formula (I) and methods for using such compounds and compositions.

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: A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. In another embodiment, a biocompatible polymer incorporates a C-nitroso moiety.

Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is W is a six-membered heterocyclic ring system having 1–2 nitrogen atoms or a 10-membered bicyclic-six-six-fused-ring system having up to two nitrogen atoms within either or both rings, provided that no nitrogen is at a bridge of the bicyclic-six-six-fused-ring system, and further having 1–2 substitutents independently selected from R3. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat diseases or conditions in which ?7 is known to be involved.

Abstract: The invention relates to pyridopyranoazepine derivatives, to pharmaceutical compositions containing them, to process for preparing them, and to the method of use thereof in the treatment or prevention of disorders associated with a dysfunction of the nicotine receptors.

Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals to treat diseases or conditions in which ?7 is known to be involved.

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: A method of enhancing lucid dreaming comprising administration to individuals the Acetylcholine Esterase inhibitor class of drugs. Use of therapeutic agents recently developed for Alzheimer”s Disease such as Donepizil (Aricept®), Rivastigmin (Exelon®), Galantamine (Reminyl®, Nivalin®), and Huperzine results in minimal side-effects (e.g., insomnia and gastrointestinal symptoms) while significantly enhancing dreaming cognitive clarity, lucidity, self-reflection, recall, control, bizarreness, and visual vividness.

Abstract: The invention relates to compounds of the formula 1 1

Abstract: New analgesic compounds, which are prepared by the hydrolysis of N-acylated 4-hydroxyphenylamine derivatives, their synthesis and pharmaceutical compositions containing them are disclosed. These compounds surprisingly possess high analgesic activity with little hepatotoxic effect, making them more useful than conventional non-steroidal anti-inflammatory drugs (NSAIDs) in the treatment of chronic pain.

Abstract: Athletic performance may be improved by administering a composition comprising galanthamine as an active ingredient to an athlete before and during sports activities. Also provided is an herbal sports performance composition comprising whole plant extract of Leucojum aestivum.

Abstract: The present invention relates to a new technique formed from polysaccharides of kelp (PK), which has function of anticancer and increasing immunity, and new nanoparticles (NP) and special liposome (SSL), which contained natural anticancer drug their preparation. Also, the present invention is aimed at the overall improvement of therapeutic efficacy of anticancer drugs, including Homoharringtonine (HHT), Curcumol (CUR), Eelemene (ELE) and Camptothecin (CPT) by NP and SSL. NP improves the anticancer therapeutic efficacy of HHT, CUR, ELE and CPT by using PK as polymer. PK can improve the anticancer therapeutic index and decrease side effect of free anticancer drugs. Also, PK has the function of increasing immunity.

Abstract: A method of treatment of a host with a cellular proliferative disease, comprising contacting the host with a cephalotaxine and an antiproliferative agent, each in an amount sufficient to modulate said cellular proliferative disease, is described. In some embodiments, the cephalotaxine comprises homoharringtonine (cephalotaxine, 4-methyl-2-hydroxy-2-(4-hydroxy-4-methyl pentyl)butanediocate ester). Antiproliferative agents of the invention comprise alkylating agents, intercalating agents, metal coordination complexes, pyrimidine nucleosides, purine nucleosides, inhibitors of nucleic acid associated enzymes and proteins, and agents affecting structural proteins and cytoplasmic enzymes.

Abstract: The invention concerns a natural, synthetic or semi-synthetic harringtonines including their tautomeric forms and their salts of the following formula: wherein n=2 (i.e. harringtonine) or n=3(i.e. homoharringtonine), in which the total content of impurities, possibly including enantiomeric forms, is lower than 1%, and/or the content of the major impurity is lower than 0.9%, and/or the chromatographic assay exhibits a harringtonines content higher than 97.5%.

Abstract: The present invention relates to an active ingredient combination composed of at least one modulator of the cholinergic system with at least one substance blocking central opioid receptors for the pharmacological treatment of nicotine dependence.

Abstract: A method for treating an addiction disorder (such as an addiction to or dependency on stimulants, nicotine, morphine, heroin, other opiates, amphetamines, cocaine, and/or alcohol) in a patient is disclosed. The method includes administering to the patient a first &agr;3&bgr;4 nicotinic receptor antagonist and administering to the patient a second &agr;3&bgr;4 nicotinic receptor antagonist. The second &agr;3&bgr;4 nicotinic receptor antagonist is different than the first &agr;3&bgr;4 nicotinic receptor antagonist, and the first &agr;3&bgr;4 nicotinic receptor antagonist and the second &agr;3&bgr;4 nicotinic receptor antagonist are administered simultaneously or non-simultaneously. Compositions which include a first &agr;3&bgr;4 nicotinic receptor antagonist and a second &agr;3&bgr;4 nicotinic receptor antagonist are also described.

Abstract: The invention relates to novel heterocyclic compounds of general formula (I), and their salts with a base or an acid: 1

Abstract: Pharmaceutical compositions incorporate compounds that are capable of affecting nicotinic cholinergic receptors. A wide variety of conditions and disorders, and particularly conditions and disorders associated with dysfunction of the central and autonomic nervous systems can be treated using pharmaceutical compositions incorporating compounds in which an aromatic ring is bridged with an ethylenic or acetylenic unit to an azabicyclic moiety.

Abstract: The invention relates to the use of galanthamine, as free base or as acid addition salt, for the treatment of cerebral, central nervous or psychiatric symptoms, defunctionalization manifestations or disorders occurring through intake of psychotropic substances as a consequence of occasional or chronic abuse of addictive substances, intoxicants or medicines, or as side effects of the use, especially repeated or prolonged, as intended of medicaments, or as an effect of use, in particular repeated or prolonged, not as intended of medicaments, or as a result of acute poisoning by psychotropic toxic substances, or as a result of chronic exposure to toxic substances with a psychotropic effect in humans or other vertebrates.

Abstract: Disclosed are once a day pharmaceutical compositions containing acetylcholinesterase inhibitors, including those with nicotinic receptor modulation such as galantamine or a pharmaceutically acceptable salt thereof Also disclosed is the use of such compositions, for example, for treating or preventing cognitive or other CNS performance impairment in a mammal, such as primary or secondary memory impairment, toxic, secondary to medical or psychiatric, Alzheimer's, vascular and other dementias, mild cognitive impairments, and other cognitive impairments, such as Attention Deficit Disorder, Fibromyalgia, Chronic Fatigue Syndrome, PTSD and Down's Syndrome. This includes behavioral efficacy, as anxiety depression apathy and agitation, in addition to neurophysiological and functional outcomes including a decrease in care givers distress.

Abstract: The present invention is directed to compositions and methods for the treatment of patients with cephalotaxines, for example, homoharringtonine. The invention is also directed to improvements in the purity, manufacturing process, formulation and administration of homoharringtonine for the treatment of cancer and other aberrant cellular diseases. The invention also provides methods and compositions for antiparasitic, antifungal, antiviral and antibacterial treatments.

Abstract: A melanin-concentrating hormone antagonist comprising a compound of the formula (I): 1

Abstract: The invention relates to compositions and methods useful in treating or preventing angiogenic disease. The invention provides for compositions comprising cephalotaxine alkaloids as antiangiogenic agents for treatment of a host with an angiogenic disease or for prophylactic treatment of a host to inhibit the onset or progression of an angiogenic disease.

Abstract: The present invention related to the natural drug of Homoharringtonine (HHT) combined with other ingredients which include Matrine (MAT), Apigenin (APN), Yejuhua lactone (YLE), Lipopolysaccharide of Kelp (LIK), Puerarin (PUN) and Indirubin (IND) for diverting human cancer cells to closely normal cells, inducing apoptosis of cancer cells and inhibiting cancer cells.

Abstract: Galantamine has be used in the treatment of a number of chronic diseases. Galantamine has been found to be safe and effective in the treatment of Alzheimer's disease. Neuropsychiatric disorders are often associated with Alzheimer's disease. It is demonstrated that galantamine is also effective in reducing or stabilizing the incidence of neuropsychiatric behaviour seen in Alzheimer's patients.

Abstract: The present invention relates to pharmaceutical compositions for treatment or prevention of memory impairment which comprise a cholinesterase inhibitor and at least one other pharmacologically active agent selected from HMG-CoA reductase inhibitors, cholesterol absorption inhibitors, gamma or beta secretase inhibitors, NMDA antagonists, muscarinic receptor agonists and nicotinic receptor agonists. Additionally, the present invention relates to the use of these pharmaceutical compositions to treat or prevent memory impairment in a mammal, such as a human.

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: The present invention concerns a method of treating chronic myelogenous leukemia, a related myeloproliferative disorder or a Ph-positive acute lymphocytic leukemia in a subject animal, comprising:

Abstract: There is provided a method of reducing insulin resistance in a mammalian subject comprising administering a suitable acetylcholine esterase antagonist

Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is adminstered to a patient in need of such treatment.

Abstract: The present invention discloses compounds which, are novel receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Abstract: Many males and females experience sexual dysfunction either caused or made worse by medications, other substances, diseases, and other medical conditions. Currently, there is need for additional treatment alternatives for these patients' sexual dysfunction. The subject invention provides a novel treatment for these individuals with sexual dysfunction by inhibiting the enzyme that breaks down acetylcholine (a compound that helps modulate normal sexual function) and elevates acetylcholine levels in the body.

Abstract: The present invention relates to novel aryl and heteroaryl diazabicycloalkane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

Abstract: A method for treating the effects of low LDL-cholesterol values in the brain on cognitive performance or other central nervous system functions by modulating nicotinic receptors by administering an effective amount of a nicotinic allosteric potentiator, an acetylcholinesterase inhibitor, nicotine, a nicotinic agonist or a mixture thereof to a patient in need of such modulation.

Abstract: An essentially pure noribogaine compound having the formula: 1

Abstract: The present invention relates to methods of therapy for substance addiction comprising the administration to a subject in need thereof a combination of: (i) a &mgr;-opioid receptor antagonist; (ii) a calcium channel blocker which is long-acting or in sustained-release form or which is nimodipine in rapid release form; and (iii) an NMDA glutamate receptor modulator; as well as combinations, kits and composition useful therefor.

Abstract: Galantamine has be used in the treatment of a number of chronic diseases. The use of this drug is associated with side effects such as, nausea or vomiting, and headaches. It has been demonstrated that by slowly introducing the patient to the drug these side effects can be reduced. It has also been shown that this slower titration results in the ability to use a lower effective dose of the drug.