Abstract: Embodiments of the present invention include the use of heterocyclic trialkyl ammonium-containing compounds alone or in combination with alkaline phosphatase or other weight loss-inducing drugs or methods to reduce or reverse excess weight gain and obesity as well as reduce the risk of development and help treatment of diseases and unhealthy conditions related to overweight and obesity.

Abstract: Provided are methods of determining whether a compound is an inhibitor of an S100 protein. The methods utilize a biosensor that comprises the S100 protein that has a covalently bound fluorescent dye at an amino acid residue of the S100 protein that becomes less exposed to the aqueous solution upon activation of the S100 protein, where the fluorescent dye has decreased fluorescence when exposed to the aqueous solution than when protected from exposure to the aqueous solution. Also provided are methods of treating a subject having metastatic cancer.

Abstract: Embodiments of the present invention include the use of heterocyclic trialkyl ammonium-containing compounds to promote regeneration of bone marrow from endogenous or exogenous stem/progenitor cells and to normalize blood cell and platelet counts.

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

Abstract: The present invention provides methods for treating neurological diseases and disorders. Compounds that replace or enhance the function of SMN or alleviate or reduce a phenotype of cells with low SMN protein levels are provided. Screening methods and kits for identifying such compounds also are provided.

Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.

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: Provided herein are methods of decreasing glial fibrillary acidic protein (GFAP) levels in a cell. Such methods include administering an effective amount of a GFAP lowering compound to the cell. Also provided are compounds useful for the treatment of Alexander disease in subjects at risk of or diagnosed with Alexander disease and methods for the identification of such compounds.

Abstract: The present invention relates to new pyrrolidinone inhibitors of PDE-4 activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The invention provides novel compounds of formula I: that are opioid receptor ligands. The invention also provides pharmaceutical compositions comprising such compounds as well as methods for treating diseases associated with opioid receptor function by administering such compounds to a mammal in need of treatment. The invention also provides an improved method for isolating intermediate materials useful for obtaining compounds of formula I.

Abstract: The present invention provides a compound represented by Formula (II): wherein R1, R2, R3, and R4 are each independently selected from a hydrogen atom, an optionally substituted C1-C6 alkyl group, an optionally substituted C7-C14 aralkyl group and —C(?O)Rx; Rx is an optionally substituted C1-C6 alkyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted C1-C6 alkoxy group or —NReRf; Ar1 is an optionally substituted aromatic carbocyclic ring, or an optionally substituted aromatic heterocyclic ring which may form a condensed ring; Q is —(CH2)m-(L)p- or -(L)p-(CH2)m—; m is an integer selected from 0 to 2, n is an integer selected from 1 and 2, and p is an integer selected from 0 and 1; L is —O—, —S— or —NR5—; A is an optionally substituted aryl group or an optionally substituted heteroaryl group; and a prodrug thereof and a pharmaceutically acceptable salt thereof, and a pharmaceutical agent or a pharmaceutical composition, which comprises the co

Abstract: Provided is an oral pharmaceutical composition with improved bioavailability and pharmacokinetic properties of a drug, by increasing a bioabsorption rate and an in vivo retention time of an active ingredient via intestine-targeted formulation of a particular naphthoquinone-based compound, or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as an active ingredient.

Abstract: Methods of treating headache with antipsychotics are provided. A kit for treating headache is also provided, comprising an antipsychotic and a device for rapid delivery of the antipsychotic.

Abstract: A class of compounds commonly containing a trialkylammonium group have been synthesized and characterized as anticancer compounds. They can be used alone or in combination with other therapies to treat cancer and other cell proliferative diseases. Representative compounds of this class, N,N-diethyl-N-methyl-2-[(9-oxo-9H-thioxanthen-2-yl)methoxy]ethanaminium iodide and N,N-diethyl-N-allyl-3-(2-methyl-9H-thioxanthen-9-ylidene)-propane-1-aminium bromide, were shown in various tumor models to decrease tumor volume, enhance the effects of other chemotherapeutic agents including cisplatin, reduce chemotherapy-induced loss of body weight, and increase survival of animals co-treated with toxic amounts of cisplatin. These compounds had even greater effects on tumor volume, body weight, and survival when administered together with the human protein placental alkaline phosphatase.

Abstract: A method of treatment for the prevention or therapy of a protein aggregation disease includes the administration in combination of a first active medicament and a second active medicament, wherein the first active medicament is active to impede aggregation of amyloid protein and the second active medicament is active to disaggregate previously formed aggregates of amyloid protein.

Abstract: A class of compounds commonly containing a trialkylammonium group have been synthesized and characterized as anticancer compounds. A representative of this class, N,N-diethyl-N-methyl-2-[(9-oxo-9H-thioxanthen-2-yl)methoxy]ethanaminium iodide (CCDTHT) was shown in various tumor models to decrease tumor volume, enhance the effects of other chemotherapeutic agents including cisplatin, reduce chemotherapy-induced loss of body weight, and increase survival of animals co-treated with toxic amounts of cisplatin. CCDTHT had even greater effects on tumor volume, body weight, and survival when administered to animals together with the human protein placental alkaline phosphatase. These trialkylammonium group-containing compounds and alkaline phosphatases, particularly in combination with each other and other therapies, may be used to treat cancer and other cell proliferative diseases.

Abstract: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 together form, along with the nitrogen atom to which they are attached, an optionally substituted nitrogen containing heterocyclic ring having from 4 to 8 ring atoms; and R3 is selected from hydroxy and —NRN1RN2, where RN1 and RN2 are independently selected from hydrogen, optionally substituted C1-7 alkyl groups, optionally substituted C3-20 heterocyclyl groups and optionally substituted C5-20 aryl groups, or together form, along with the nitrogen atom to which they are attached, an optionally substituted nitrogen containing heterocyclic ring having from 4 to 8 ring atoms, and its use in inhibiting ATM.

Abstract: Embodiments of the present invention include the in vivo use of a family of heterocyclic compounds containing a quaternary ammonium group as exemplified by the thioxanthone and thioxanthene compounds [3-(3,4-dimethyl-9-oxo-9H-thioxanthen-2-yloxy)-2-hydroxypropyl]trimethylammonium chloride, or CCcompound1, N,N,-diethyl-N-methyl-2-[9-oxo-9H-thioxanthen-2-yl)methoxy]ethanaminium iodide, or CCcompound3, and N,N,N-trimethyl-3-(9H-thioxanthen-9-ylidene)-propane-1-aminium iodide, or CCcompound19 to reduce higher than normal blood glucose level within or close to the normal range in subjects with insulin resistance, hyperglycemia, and diabetes thereby also reducing or preventing associated diseases, complications, and pathological states.

Abstract: The present invention relates to certain tricyclic derivatives which are capable of inhibiting histone deacetylases. The compounds of this invention are therefore useful in treating diseases associated with abnormal histone deacetylase activities. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing these compounds are also disclosed.

Abstract: A class of compounds commonly containing a trialkylammonium group have been synthesized and characterized as anticancer compounds. A representative of this class, N,N-diethyl-N-methyl-2-[(9-oxo-9H-thioxanthen-2-yl)methoxy]ethanaminium iodide (CCDTHT) was shown in various tumor models to decrease tumor volume, enhance the effects of other chemotherapeutic agents including cisplatin, reduce chemotherapy-induced loss of body weight, and increase survival of animals co-treated with toxic amounts of cisplatin. CCDTHT had even greater effects on tumor volume, body weight, and survival when administered to animals together with the human protein placental alkaline phosphatase. These trialkylammonium group-containing compounds and alkaline phosphatases, particularly in combination with each other and other therapies, may be used to treat cancer and other cell proliferative diseases.

Abstract: The present disclosure relates to methods of treating cancer in mammals by administration of Lucanthone and at least one anti-metabolite. Pharmaceutical compositions and kits comprising Lucanthone and at least one anti-metabolite also are disclosed.

Abstract: The present invention is concerned with certain novel spiro substituted heterocylic ring derivatives. These compounds may be useful in the manufacture of pharmaceutical compositions for treating disorders mediated by lipoxygenases. They may also be useful in the manufacture of pharmaceutical formulations for the treatment of lipoxygenase-mediated disorders.

Abstract: Embodiments of the present invention include the in vivo and in vitro use of a family of anticancer heterocyclic compounds containing a quaternary ammonium group as exemplified by the thioxanthone and thioxanthene compounds [3-(3,4-dimethyl-9-oxo-9H-thioxanthen-2-yloxy)-2-hydroxypropyl]trimethylammonium chloride, or CCompound1, N,N,-diethyl-N-methyl-2-[9-oxo-9H-thioxanthen-2-yl)methoxy]ethanaminium iodide, or CCompound3, and N,N,N-trimethyl-3-(9H-thioxanthen-9-ylidene)-propane-1-aminium iodide, or CCompound19 to maintain and increase viability of normal endocrine and exocrine pancreatic cells under pathological conditions, such as type 1 and type 2 diabetes, pancreatitis, pancreatic cancer, or during and after islet transplant, or in preparation for transplant of isolated islet cells via (i) direct contact with these cells, and/or via (ii) enhancing survival and proliferation of endogenous or transplanted adult stem cells, and/or via (iii) reducing viability of pancreatic cancer cells.

Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly congestive heart disease, hypertension, rheumatoid arthritis or inflammation, comprising administering to a patient in thereof an effective amount of a compound of Formula (I).

Abstract: Embodiments of the present invention include the use of heterocyclic trialkyl ammonium-containing compounds to promote regeneration of bone marrow from endogenous or exogenous stem/progenitor cells and to normalize blood cell and platelet counts.

Abstract: The present invention is directed to the use of chemosensitising compounds, in particular thioxanthene derivatives and phenothiazine derivatives, for treatment of infectious diseases in combination with an anti-infective agent. The invention furthermore relates to compositions comprising said chemosensitising compounds and anti-infective agents.

Abstract: The present invention relates to novel crystalline forms of 3-(2R-tetrahydrofuryl-methyl)-2-thioxanthine. Further the present invention also relates to compositions comprising them and their use in therapy.

Abstract: The present invention relates to methods for treating or preventing podocyte-related diseases and disorders using compounds that modulate the calcium sensing receptor or pharmaceutical compositions comprising thereof.

Abstract: Histamine H3 inverse agonists or histamine H3 antagonists are useful, alone or in combination with a neuroleptic agent, for treating or preventing movement disorders, including tremor, such as essential tremor, and tremor associated with Parkinson's disease, cranofacial trauma, multiple sclerosis, stroke, dystonia, and neuropathic, toxic or drug induced tremor.

Abstract: Embodiments of the present invention include the use of heterocyclic trialkyl ammonium-containing compounds to promote regeneration of bone marrow from endogenous or exogenous stem/progenitor cells and to normalize blood cell and platelet counts.

Abstract: Embodiments of the present invention include the use of heterocyclic trialkyl ammonium-containing compounds to promote regeneration of bone marrow from endogenous or exogenous stem/progenitor cells and to normalize blood cell and platelet counts.

Abstract: Embodiments of the invention provide a method and composition for treating or reducing multiple drug resistance in cancers. Embodiments of the invention also provide for a xanthene compound to inhibit multidrug resistance protein 1.

Abstract: A method of mono-therapeutically treating a patient suffering from a condition selected from naïve schizophrenia, therapy resistant schizophrenia, therapy refractory schizophrenia, therapy resistant depression, chronic depression, recurrent depression, and resistant bipolar disorder comprises the administration of a pharmacologically effective amount of a thioxanthene, such as chlorprothixene, flupenthixol, thiotixene, zuclopenthixol, zuclopenthixol acetate and zuclopenthixol decanoate, including a pharmaceutically acceptable salt thereof. Also disclosed is a corresponding use and the manufacture of a corresponding medicament.

Abstract: One embodiment of the invention uses thioxanthone compounds containing a choline or choline analogue moiety, such as CCcompound1 or [3-(3,4-Dimethyl-9-oxo-9H-thioxanthen-2-yloxy)-2-hydroxypropyl]trimethyl-ammonium chloride, to reduce or reverse body weight loss in various mouse models of human tumors. Another embodiment of the invention discloses a method for reducing or reversing cachexia or disease-induced body weight loss in human and other mammals using thioxanthone compounds containing a choline analogue moiety.

Abstract: Spirocyclic cyclohexane compounds, methods for their production, pharmaceutical compositions containing these compounds, and the use of these spirocyclic cyclohexane compounds for treating conditions associated with the nociceptin/ORL1 receptor system, e.g. pain, drug withdrawal, anxiety, etc.

Abstract: The present invention relates to spirocyclic cyclohexane compounds, to methods for their production, to pharmaceutical compositions containing these compounds, to methods of treatment using such compounds and to the use of such spirocyclic cyclohexarie compounds for producing pharmaceutical compositions.

Abstract: Acne-affected skin has been found to be accompanied by the presence of matrix-degrading enzymes such as MMPs and neutrophil elastase, induction of neutrophils, and a reduction in procollagen biosynthesis. This invention treats scarring and inflammation accompanying acne by administering, topically or systemically, at least one of (i) an inhibitor of the matrix degrading enzymes and (ii) a cytokine inhibitor that alleviates inflammation and thus also alleviate neutrophil infiltration. Alleviating the matrix degradation and renormalizing procollagen biosynthesis allows for reduced inflammation and better natural repair of acne-affected skin. Inhibiting cytokines alleviates induction of MMPs in resident skin cells, and also alleviates inflammation with its concommitant induction of neutrophils from the blood stream bringing MMPs and elastase into the acne lesion.

Abstract: The present invention relates to novel tricyclic compounds useful for the treatment of inflammatory conditions, diseases of the central nervous and insulin resistant diabetes.

Abstract: The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the Formula (1), their analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxide, pharmaceutically acceptable solvates and the pharmaceutical compositions containing them.

Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are also useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

Abstract: PDF inhibitors and novel methods for their use are provided.

Abstract: New active compound combinations of valinamide derivatives of the formula (I) in which R1 and R2 has the meaning given in the description, with known fungicidal active substances, and their use for combating phytopathogenic fungi are described.

Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.

Abstract: The invention provides lapachone analogs and derivatives as well as methods of use thereof. These compounds can be used in pharmaceutical compositions for the treatment or prevention of cell proliferation disorders. These compounds can also be used in the treatment or prevention of psoriasis or cancer or precancerous conditions.

Abstract: The invention relates to the discovery that specific adamantyl or adamantyl group derivatives containing retinoid-related compounds induce apoptosis of cancer cells and therefore may be used for the treatment of cancer, including advanced cancer. Also, the present invention relates to novel adamantyl or adamantyl group derivatives containing retinoid compounds and their usage for treatment and/or prevention of cancer, keratinization disorders, dermatological conditions, and other therapies More specifically, it has been shown that such adamantyl compounds, e.g., 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoicacid, 2-[3-(1-adamantyl)-4-methoxyphenyl]-5-benzimidazole carboxylic acid, and 6-[3-(1-adamantyl)-4,5-methylenedioxyphenyl]-2-naphthoic acid, can be used to treat or prevent cervical cancers and precancers such as cervical dysplasias, including high grade and low grade dysplasias.

Abstract: The present invention relates to compounds of formula (I) 1

Abstract: This invention relates to compounds that alter PPAR activity. The invention also relates to pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing dyslipidemia, hypercholesterolemia, obesity, hyperglycemia, atherosclerosis, hypertriglyceridemia and hyperinsulinemia in a mammal. The present invention also relates to methods for making the disclosed compounds.

Abstract: Spiro[9,10-dihydroanthracene]-9,3′-pyrrolidine (SPAN) and derivatives thereof are provided as selective serotonin receptor antagonists. The compounds are selective, high affinity antagonists of 5-HT2 serotonin receptors. The compounds are useful as antidepressant and antianxiety agents.

Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).

Abstract: The present invention relates to therapeutically active cubane compounds, a method of preparing the same, and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases of the central nervous system related to the metabotropic glutamate receptor system.