Entries |
Document | Title | Date |
20080200508 | Pharmaceutical Compositions For Sleep Disorders - Pharmaceutical compositions are provided for the pharmacological treatment of breathing disorders and, more specifically, to compositions containing agents having serotonin receptor modulating activity for the alleviation of sleep apnea (central and obstructive) and other sleep-related breathing disorders wherein the active ingredients are released such as to extend effective blood plasma concentrations across the period of sleep. | 08-21-2008 |
20080207690 | Benzisoxazole Derivatives - This invention relates to compounds of the formula (I): wherein A, B, R | 08-28-2008 |
20080255194 | 1,2-Benzisoxazol-3-yl Compounds - This invention relates to novel 1,2-benzisoxazol-3-yl compounds, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an antagonist of both dopamine and serotonin receptors. | 10-16-2008 |
20080287495 | Novel benzo[d][1,3]-dioxol derivatives - The present invention relates to an isotopologue of Compound 1 substituted with deuterium at the methylene carbon of the benzodioxol ring. The isotopologues of this invention selective serotonin reuptake inhibitors (SSRIs) and possess unique biopharmaceutical and metabolic properties compared to Compound 1. They may also be used to accurately determine the concentration of Compound 1 in biological fluids and to determine metabolic patterns of Compound 1 and its isotopologues. The invention further provides compositions comprising these deuterated isotopologues and methods of treating diseases and conditions that are responsive to increased neuronal serotonin transmission, alone and in combination with additional agents. | 11-20-2008 |
20080300275 | Novel Benzothiazolone Derivatives - The present invention provides compounds of formula (I) wherein e, R | 12-04-2008 |
20090023779 | Indazoles, benzisoxazoles and benzisothiazoles and their use as estrogenic agents - The present invention relates to compounds of formula (I): | 01-22-2009 |
20090036488 | RECURRENCE PREVENTIVE THERAPEUTIC AGENT FOR PSYCHOSTIMULANT-INDUCED PSYCHOSIS AND SCHIZOPHRENIA - The present invention provides a therapeutic agent for preventing recurrence of psychostimulant-induced psychosis and schizophrenia. This therapeutic agent for preventing recurrence of psychostimulant-induced psychosis and schizophrenia includes a drug that amplifies serotonin signals as an active component. This therapeutic agent for preventing recurrence of psychostimulant-induced psychosis and schizophrenia includes a drug that amplifies serotonin signals as an active component. This therapeutic agent for preventing recurrence of psychostimulant-induced psychosis and schizophrenia includes a drug that amplifies serotonin signals as an active component. | 02-05-2009 |
20090099232 | INJECTABLE DEPOT FORMULATION COMPRISING CRYSTALS OF ILOPERIDONE - An injectable depot formulation comprising crystals having structure (I) wherein R is (FII) and the X50 value of the crystals is from 1 to 200 microns. Depot formulations containing crystals of iloperidone or its metabolites have the following advantages: (i) release of the crystals in plasma can be correlated with the size of the crystals; (ii) absorption of the crystals in plasma can be correlated with the size of the crystals; (iii) the particle size of the crystals can be controlled by crystal engineering and/or milling; and (iv) the crystals are stable upon storage, and stable to sterilization procedures, such as gamma irradiation. | 04-16-2009 |
20090124660 | Piperidine Compounds Useful as Malonyl-CoA Decarboxylase Inhibitors - The present invention provides methods for the use of compounds as depicted by structure I, pharmaceutical compositions containing the same, and methods for the prophylaxis, management and treatment of metabolic diseases and diseases modulated by MCD inhibition. The compounds disclosed in this invention are useful for the prophylaxis, management and treatment of diseases involving in malonyl-CoA regulated glucose/fatty acid metabolism pathway. In particular, these compounds and pharmaceutical composition containing the same are indicated in the prophylaxis, management and treatment of cardiovascular diseases, diabetes, cancer and obesity. | 05-14-2009 |
20090131477 | NEW USE OF ILOPERIDONE - The invention relates to the use of iloperidone in the treatment of affective disorders, including bipolar mood disorders. | 05-21-2009 |
20090143432 | Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof - The present invention provides a convenient and efficient process for the synthesis of d | 06-04-2009 |
20090143433 | COCKTAIL FOR MODULATION OF ALZHEIMER'S DISEASE - Formulations for the prevention and treatment of neurological diseases and cognitive deficiencies, i.e., Alzheimer's Disease (AD), Parkinson's Disease, amyotrophic lateral sclerosis, mild cognitive impairment and other types of dementia, comprise therapeutically effective amounts of curcumin, piperine, epigallocatechin-3-gallate (EGCG) and n-acetylcysteine. The combination addresses some or all of the pathways which can result in neurological deficiencies, degeneration and diseases. | 06-04-2009 |
20090156640 | NOCICEPTIN ANALOGS - A compound of the formula (I), (II), (III) or (IV) | 06-18-2009 |
20090170899 | Stimulators of 5-HT4 receptors and uses thereof - The present invention relates to a novel combination of a serotonin selective re-uptake inhibitor (SSRI) and an agonist of the serotonin 4 (5-HT | 07-02-2009 |
20090192194 | Cyclic Amine Derivatives, Processes For Their Preparation, And Pharmaceutical Compositions Containing Them - A compound of formula (I) | 07-30-2009 |
20090209583 | 2-(SUBSTITUTED-AMINO)-BENZOTHIAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS - The present invention relates to 2-(substituted-amino)-benzothiazole sulfonamide compounds and derivatives, their use as protease inhibitors, in particular as broad-spectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present 2-(substituted-amino)-benzothiazole sulfonamide compounds and derivatives with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents. | 08-20-2009 |
20090239908 | METHODS OF TREATING PSYCHOSIS AND SCHIZOPHRENIA BASED ON POLYMORPHISMS IN THE CNTF GENE - This invention relates to the use of the association between the 103 G>A polymorphism in the CNTF gene to determine antipsychotic treatment strategies in patients with psychotic disorders. | 09-24-2009 |
20090247583 | PHARMACEUTICAL COMPOSITION COMPRISING, IN COMBINATION, SAREDUTANT AND PAROXETINE - A subject-matter of the present invention is pharmaceutical compositions comprising, in combination, at least one active ingredient chosen from (S)-(−)-N-[4-(4-acetamido-4-phenylpiperidin-1-yl)-2-(3,4-dichlorophenyl)butyl]-N-methylbenzamide and pharmaceutically acceptable salts thereof and at least one second active ingredient chosen from trans-(−)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)piperidine and pharmaceutically acceptable salts thereof. | 10-01-2009 |
20090258901 | LIGANDS FOR MONOAMINE RECEPTORS AND TRANSPORTERS, AND METHODS OF USE THEREOF - One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters. | 10-15-2009 |
20090275615 | Method of treating thermoregulatory disfunction with paroxetine - The present invention relates to a method for treating a patient suffering from a thermoregulatory dysfunction, especially hot flashes and flushes associated with hormonal changes due to naturally occurring menopause (whether male or female) or due to chemically or surgically induced menopause. The method is also applicable to treating the hot flashes, hot flushes, or night sweats associated with disease states that disrupt normal hormonal regulation of body temperature. | 11-05-2009 |
20090298880 | METHODS FOR THE ADMINISTRATION OF ILOPERIDONE - The present invention relates to methods for the identification of genetic polymorphisms that may be associated with a risk for QT prolongation after treatment with iloperidone and related methods of administering iloperidone to patients with such polymorphisms. | 12-03-2009 |
20090298881 | Water-Soluble Artemisinin Derivatives, Their Preparation Methods, the Pharmaceutical Compositions and the Use Thereof - Water-soluble artemisinin derivatives, their preparation methods, the pharmaceutical compositions containing the same derivatives and the use thereof are disclosed. The artemisinin derivatives have following formula I. It has been proved by pharmacological tests that these compounds and compositions have evident immuno-suppressive activities, and may be used in the preparation of novel immuno-suppressants for treating the diseases caused by hyperfunction of human immunity (e.g. the auto-immune diseases such as lupus erythematosus, rheumatoid arthritis, multiple sclerosis and the like), and for inhibiting the graft rejection after cell or organ transplantation. | 12-03-2009 |
20090306137 | TREATMENT FOR DEPRESSIVE DISORDERS - A method of treating depression comprising administering a melatonin agonist. | 12-10-2009 |
20100010044 | NOVEL CRYSTALLINE FORM OF 2-[4-(4-FLUORO-BENZYL)-PIPERIDINE-1-YL]-2-OXO-N-(2-OXO-2,3-DIHYDRO-BENZOX- AZOL-6-YL)-ACETAMIDE - The present invention relates to a novel crystalline form of 2-[4-(4-fluoro-benzyl)-piperidine-1-yl]-2-oxo-N-(2-oxo-2,3-dihydro-benzoxazol-6-yl)-acetamide. Processes for the preparation of this form, compositions containing the form, and methods of use thereof are also described. | 01-14-2010 |
20100048629 | METHODS FOR TREATING NEUROPATHIC PAIN - The present invention relates to methods of treating diabetic neuropathic pain comprising administering piperidine derivatives, such as 2-[4-(4-fluoro-benzyl)-piperidine-1-yl]-2-oxo-N-(2-oxo-2,3-dihydro-benzoxazol-6-yl)acetamide, and pharmaceutically acceptable salts thereof. Methods of treating post-herpetic neuralgia, chronic lower back pain, osteoarthritis and acute inflammatory pain are described. | 02-25-2010 |
20100048630 | METHODS FOR TREATING CNS DISORDERS - The present invention relates to methods for treating central nervous system disorders, such as Alzheimer's disease, anxiety and major depressive disorder, by administering piperidine derivatives, e.g., 2-[4-(4-fluoro-benzyl)-piperidine-1-yl]-2-oxo-N-(2-oxo-2,3-dihydro-benzoxazol-6-yl)acetamide, and pharmaceutically acceptable salts thereof. | 02-25-2010 |
20100063093 | METHODS FOR THE ADMINISTRATION OF ILOPERIDONE - The present invention relates to methods for the identification of genetic polymorphisms that may be associated with a risk for QT prolongation after treatment with iloperidone and related methods of administering iloperidone to patients with such polymorphisms. | 03-11-2010 |
20100087483 | Aminosulfonyl Substituted 4-(Aminomethyl)-Piperidine Benzamides As 5HT 4-Antagonists - The present invention is concerned with novel compounds of formula (I) having 5HT | 04-08-2010 |
20100130549 | PSYCHOTROPIC COMPOUNDS, COMPOSITIONS AND METHODS OF USE - The present invention provides a method for treating or preventing a disease or disorder treatable by the inhibition of serotonin reuptake in a patient, and/or norepinephrine reuptake and/or dopamine reuptake in a patient, the method comprising administering to the patient a neurotransmitter reuptake inhibiting-effective amount of at least one compound of the formula A-L-B (I) or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein A is a psychotropic derivative; L is a linking group comprising two carbon atoms; and B is an alkyl, alkenyl, alkynyl or aralkyl comprising at least one substituent of the formula Q, wherein: the alkyl, alkenyl, alkynyl or aralkyl is optionally substituted with one or more halogean halogens, hydroxyl, cyano, nitro, amino or thiol; and Q is OR | 05-27-2010 |
20100152240 | PYRROLINE-2-ONE DERIVATIVES AGAINST CELL RELEASING TUMOR NECROSIS FACTOR, PREPARATION METHODS AND USES THEREOF - Compounds represented by Formula (I) or Formula (II), their pharmaceutically acceptable salts or hydrates | 06-17-2010 |
20100179189 | PYRROLINE DERIVATIVES AGAINST CELL RELEASING TUMOR NECROSIS FACTOR, PREPARATION METHODS AND USES THEREOF - Compounds represented by Formula (I) or Formula (II) against cell releasing TNFα, their pharmaceutically acceptable salts or hydrates and preparation methods and uses thereof, in which A and B represent CH | 07-15-2010 |
20100210687 | Compounds which have activity at M1 receptor and their uses in medicine - Compounds of formula (I) or a salt thereof are provided: | 08-19-2010 |
20100210688 | Novel Benzothiazolone Derivatives - The present invention provides compounds of formula (I) wherein e, R | 08-19-2010 |
20100216840 | BENZIMIDAZOLIDINONE DERIVATIVES AS MUSCARINIC AGENTS - Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M | 08-26-2010 |
20100249188 | PREDICTION OF QT PROLONGATION BASED ON SNP GENOTYPE - The present invention relates to the prediction of QT prolongation following administration of a compound capable of increasing an individual's QT interval based on the individual's genotype at one or more single nucleotide polymorphism (SNP) loci and to the treatment of a patient based on such prediction. | 09-30-2010 |
20100249189 | NITRIC OXIDE DONOR COMPOUNDS - The invention relates to nitric oxide donors of the formula (I) and pharmaceutically acceptable salts or stereoisomers thereof: | 09-30-2010 |
20100267771 | AUTOMATED IMMUNOSSAY APPARATUS WITH FLEXIBLE PICK-UP ARM - An automated sample handling apparatus is disclosed having a pipette mechanism ( | 10-21-2010 |
20100267772 | Combination of a Serotonin Reuptake Inhibitor and Agomelatine - The present invention relates to the use of a combination of agomelatine and a serotonin reuptake inhibitor (SRIs), or any other compound, which causes an elevation in the level of extracellular serotonin, for the treatment of depression and other affective disorders. | 10-21-2010 |
20100298379 | PHARMACEUTICAL COMPOSITIONS OF 5-HYDROXYTRYPTOPHAN AND SEROTONIN-ENHANCING COMPOUND - This invention relates to novel pharmaceutical compositions comprising a therapeutically effective amount of a slow-release formulation of 5-hydroxytryptophan (5-HTP) and a serotonin-enhancing compound. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for combating CNS disorders, including depressive disorders, bipolar disorders, anxiety disorders, obesity and pain. | 11-25-2010 |
20110015227 | WARMING SENSATE COMPOSITION - The invention relates to a warming sensate composition of (i) a hot component, (ii) a cooling component, and (iii) optionally a bitter component. The weight ratio of (i):(ii) is from 1:3 to 1:100. If a solvent is provided in the composition, the solvent is present in an amount of less than 10 wt % ethanol, based on the total weight of the composition. Also, the bitter component, when used, is present in an amount of less than 0.15% by weight based on the total weight of the composition. | 01-20-2011 |
20110021566 | GENETIC MARKERS FOR EFFICACY OF ILOPERIDONE IN THE TREATMENT OF PSYCHOTIC SYMPTOMS - Methods for predicting whether iloperidone will be efficacious in treating a psychotic symptom in an individual, based on the individual's genotype at one or more single nucleotide polymorphism (SNP) loci are described, as are methods for treating an individual based on such prediction. | 01-27-2011 |
20110130423 | Compounds Which Have Activity At M1 Receptor And Their Uses In Medicine - Compounds of formula (I) and salts thereof are provided: | 06-02-2011 |
20110130424 | SUBSTITUTED PHENYLPIPERIDINES WITH SEROTONINERGIC ACTIVITY AND ENHANCED THERAPEUTIC PROPERTIES - Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and/or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, and/or premature ejaculation are described. | 06-02-2011 |
20110144159 | ETHER BENZYLIDENE PIPERIDINE ARYL CARBOXAMIDE COMPOUNDS USEFUL AS FAAH INHIBITORS - The present invention relates to compounds of Formula (I) wherein Ar is optionally substituted phenyl or 6-membered heteroaryl moiety, or a benzisoxazole, pyrrolopyridine, or benzotriazole group; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, including pain, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease. | 06-16-2011 |
20110172272 | BENZISOXAZOLES - The present invention relates to novel fatty acid esters of the reversible Iloperidone metabolite P-88-8991, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them. | 07-14-2011 |
20110178126 | PYRAZOLYLBENZOTHIAZOLE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS - Pharmaceutical compositions and compounds are provided. The compounds of the invention have use as therapeutic agents, e.g., they demonstrate anti-proliferative, anti-inflammatory, anti-angiogenic, anti-migration activities. In one embodiment of the invention, formulations of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical formulations are useful in the treatment of, e.g., anti-inflammatory, renal, and hyperproliferative disorders. The compounds of the invention are pyrazolylbenzothiazole derivatives of the following formula (1) | 07-21-2011 |
20110178127 | AMINE COMPOUNDS AND MEDICAL USES THEREOF - The present invention relates to a new amine compound or a pharmaceutically acceptable salt thereof, wherein the definitions of X, R | 07-21-2011 |
20110184021 | 2-Acylaminopropoanol-Type Glucosylceramide Synthase Inhibitors - A compound for use in treating polycystic kidney disease is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating polycystic kidney disease in a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Methods of treating in polycystic kidney disease in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. | 07-28-2011 |
20110190347 | METHODS FOR TREATING NEUROPATHIC PAIN - The present invention relates to methods of treating diabetic neuropathic pain comprising administering piperidine derivatives, such as 2-[4-(4-fluoro-benzyl)-piperidine-1-yl]-2-oxo-N-(2-oxo-2,3-dihydro-benzoxazol-6-yl)acetamide, and pharmaceutically acceptable salts thereof. Methods of treating post-herpetic neuralgia, chronic lower back pain, osteoarthritis and acute inflammatory pain are described. | 08-04-2011 |
20110190348 | METHODS FOR TREATING CNS DISORDERS - The present invention relates to methods for treating central nervous system disorders, such as Alzheimer's disease, anxiety and major depressive disorder, by administering piperidine derivatives, e.g., 2-[4-(4-fluoro-benzyl)-piperidine-1-yl]-2-oxo-N-(2-oxo-2,3-dihydro-benzoxazol-6-yl)acetamide, and pharmaceutically acceptable salts thereof. | 08-04-2011 |
20110201646 | OPTICAL ISOMERS OF AN ILOPERIDONE METABOLITE - The present invention relates to novel isomers of a metabolite of Iloperidone, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them. | 08-18-2011 |
20110251241 | GREASE-LIKE GEL FOR REPELLING RODENTS - Grease-like compositions are provided for repelling rodents. The compositions utilize nontoxic mineral, synthetic, or vegetable oil based gels containing silica, clay, urea, polytetrafluoroethylene, or metallic soap thickeners and capsaicin. | 10-13-2011 |
20110288125 | NOVEL USE OF PIPERINE - The present invention is related to novel use of piperine, and more specifically, it is related to a pharmaceutical or food composition for preventing and treating obesity comprising piperine or a salt thereof as an active ingredient. The present invention is related to novel use of piperine, and it provides a pharmaceutical or food composition for preventing and treating obesity comprising piperine or a salt thereof as an active ingredient. The composition comprising piperine of the present disclosure is effective on suppression of abdominal fat accumulation and body weight loss. Therefore, the composition can be effectively used to prevent and treat obesity. | 11-24-2011 |
20110306637 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 12-15-2011 |
20120022105 | GREASE-LIKE GEL FOR REPELLING RODENTS - Grease-like compositions are provided for repelling rodents. The compositions utilize nontoxic mineral, synthetic, or vegetable oil based gels containing silica, clay, urea, polytetrafluoroethylene, or metallic soap thickeners and capsaicin. | 01-26-2012 |
20120029018 | 9-SUBSTITUTED PHENANTHRENE BASED TYLOPHORINE DERIVATIVES - The present invention provides compounds of Formula I: compositions containing the same, and methods of use thereof such as for the treatment of cancer. | 02-02-2012 |
20120035215 | METHOD OF PREDICTING A PREDISPOSITION TO QT PROLONGATION - The present invention describes an association between genetic polymorphisms in the ABCC2 gene and a predisposition to prolongation of the QT interval, and provides related methods for the prediction of such a predisposition, the administration of QT interval-prolonging compounds to individuals having such a predisposition, and determining whether a compound is capable of inducing QT prolongation. | 02-09-2012 |
20120041026 | (R)-4-((4-((4-(TETRAHYDROFURAN-3-YLOXY)BENZO[D]ISOXAZOL-3-YLOXY)METHYL)PIP- ERIDIN-1-YL)METHYL)TETRAHYDRO-2H-PYRAN-4-OL, A PARTIAL AGONIST OF 5-HT4 RECEPTORS - (R)-4-((4-((4-(tetrahydrofuran-3-yloxy)benzo[d]isoxazol-3-yloxy)methyl)piperidin-1-yl)methyl)tetrahydro-2H-pyran-4-ol and its use in treating neurodegenerative disorders, is described herein. | 02-16-2012 |
20120059034 | NOVEL CRYSTALLINE HYDRATE, AMORPHOUS AND POLYMORPHIC FORMS OF DIHYDRO-BENZOXAZOLE-6-YL-ACETAMIDE DERIVATIVE AND PROCESSES FOR THEIR PREPARATION - The invention relates to novel crystalline hydrate, amorphous and crystalline polymorphic forms of 2-[4-(4-Fluoro-benzyl)-piperidine-1-yl]-2-oxo-N-(2-oxo-2,3-dihydro-benzoxazole-6-yl)-acetamide (I) (radiprodil). Processes for the preparation of these forms, compositions containing these forms, and methods of use thereof are also described. | 03-08-2012 |
20120059035 | METHOD OF PREDICTING A PREDISPOSITION TO QT PROLONGATION - The present invention describes an association between genetic polymorphisms in the BAI3 gene and a predisposition to prolongation of the QT interval, and provides related methods for the prediction of such a predisposition, the administration of QT interval-prolonging compounds to individuals having such a predisposition, and determining whether a compound is capable of inducing QT prolongation. | 03-08-2012 |
20120095048 | ALLOSTERIC BINDING COMPOUNDS - The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds. | 04-19-2012 |
20120220631 | USE OF 5H-THIOENO(3,4-c)PYRROLE-4,6-DIONE DERIVATIVES AS TUMOR NECROSIS FACTOR INHIBITOR - A method of treating or curing a disease caused by or associated with elevated levels of TNF in a patient including administering to the patient 5H-thioeno(3,4-c)pyrrole-4,6-dione derivatives. | 08-30-2012 |
20120258984 | 5-HTP COMBINATION THERAPY - The present invention relates to combination therapies and pharmaceutical compositions comprising a combination of 5-hydroxytryptophan and a serotonin reuptake inhibitor. The present invention provides a pharmaceutical composition comprising (i) a serotonin reuptake inhibitor and (ii) 5-hydroxytrytophan. The present invention further provides a pharmaceutical composition comprising (i) 5-hydroxytryptophan in an amount ranging from about 1 mg to about 75 mg; and (ii) a serotonin reuptake inhibitor. The present invention also provides a pharmaceutical composition comprising (i) a subclinical dose of a serotonin reuptake inhibitor; and (ii) 5-hydroxytryptophan. | 10-11-2012 |
20130012542 | INJECTABLE DEPOT FORMULATION COMPRISING CRYSTALS OF ILOPERIDONE - An injectable depot formulation comprising crystals having structure (I) wherein R is (FII) and the X50 value of the crystals is from 1 to 200 microns. Depot formulations containing crystals of iloperidone or its metabolites have the following advantages: (i) release of the crystals in plasma can be correlated with the size of the crystals; (ii) absorption of the crystals in plasma can be correlated with the size of the crystals; (iii) the particle size of the crystals can be controlled by crystal engineering and/or milling; and (iv) the crystals are stable upon storage, and stable to sterilization procedures, such as gamma irradiation. | 01-10-2013 |
20130065924 | COMPOSITION AND METHOD FOR THE TREATMENT OF NEURODEGENERATION - A composition and method for the treatment of neurodegeneration and brain-derived neurotrophic factor. The composition and method comprising providing fluoxetine, simvastatin, and optionally, an antioxidant. | 03-14-2013 |
20130085162 | AMIDO COMPOUNDS AS RORyT MODULATORS AND USES THEREOF - Amido compounds are disclosed that have a formula represented by the following: | 04-04-2013 |
20130261154 | FUNGICIDAL AZOCYCLIC AMIDES - Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, | 10-03-2013 |
20130289067 | COMPOUNDS AND METHODS FOR TREATING HIV - Inhibitors of HIV-1 protease and compositions containing them are described. Use of the inhibitors and compositions containing them to treat HIV, AIDS, and AIDS-related diseases is described. | 10-31-2013 |
20130296366 | OPTICAL ISOMERS OF AN ILOPERIDONE METABOLITE - The present invention relates to novel isomers of a metabolite of Iloperidone, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them. | 11-07-2013 |
20130338192 | METHOD FOR AUGMENTING THE EFFECTS OF SEROTONIN REUPTAKE INHIBITORS - A method of treating a subject for a serotonergic neurotransmission dysregulation disorder, comprises administering the subject a serotonin enhancer (e.g., a serotonin reuptake inhibitor) in an amount effective to treat the disorder; and concurrently administering the subject 5-hydroxytryptophan in an amount effective to enhance the activity of the serotonin enhancer, (e.g., serotonin reuptake inhibitor). In preferred embodiments the disorder is depression, anxiety, or substance abuse. | 12-19-2013 |
20140018390 | DEUTERATED BENZO[D][1,3]-DIOXOL DERIVATIVES - The present invention relates to an isotopologue of Compound 1 substituted with deuterium at the methylene carbon of the benzodioxol ring. The isotopologues of this invention selective serotonin reuptake inhibitors (SSRIs) and possess unique biopharmaceutical and metabolic properties compared to Compound 1. They may also be used to accurately determine the concentration of Compound 1 in biological fluids and to determine metabolic patterns of Compound 1 and its isotopologues. The invention further provides compositions comprising these deuterated isotopologues and methods of treating diseases and conditions that are responsive to increased neuronal serotonin transmission, alone and in combination with additional agents. | 01-16-2014 |
20140039008 | METHODS FOR THE ADMINISTRATION OF ILOPERIDONE - The present invention relates to methods for the identification of genetic polymorphisms that may be associated with a risk for QT prolongation after treatment with iloperidone and related methods of administering iloperidone to patients with such polymorphisms. | 02-06-2014 |
20140045893 | METHODS FOR THE ADMINISTRATION OF ILOPERIDONE - The present invention relates to methods for the identification of genetic polymorphisms that may be associated with a risk for QT prolongation after treatment with iloperidone and related methods of administering iloperidone to patients with such polymorphisms. | 02-13-2014 |
20140051726 | 5-HT4 Receptor Agonist as a Prokinetic Agent - This invention relates to Compound A or a pharmaceutically acceptable salt thereof with 5-HT4 agonistic activities, which is useful in the treatment of gastrointestinal diseases. This invention also relates to a pharmaceutical composition for the treatment of gastrointestinal diseases which comprises a therapeutically effective amount of Compound A or a pharmaceutically acceptable salt thereof. Further this invention relates to a method for the treatment of gastrointestinal diseases in an animal subject including a mammalian subject, which comprises administering to the animal subject including a mammalian subject Compound A or a pharmaceutically acceptable salt thereof. | 02-20-2014 |
20140094493 | Novel Ether Linked Compounds and Improved Treatments for Cardiac and Cardiovascular Disease - A compound of Formula (I), and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: | 04-03-2014 |
20140100248 | Novel Heterocyclic Compounds as Modulators of Sphingolipid Signaling and Uses Thereof - The present invention relates to new heterocyclic compounds as modulators of sphingolipid signaling and uses thereof of as pharmaceutically active agents, suitable for treating proliferative, degenerative, infectious, and other diseases. | 04-10-2014 |
20140121242 | SUBSTITUTED CINNAMAMIDE DERIVATIVE, PREPARATION METHOD AND USE THEREOF - The present invention relates to substituted cinnamamide derivatives, the method for preparing thereof and the use thereof. Each of said derivatives has a structure of formula (I). The method for preparing the substituted cinnamamides and their derivatives of the present invention is also disclosed. Substituted piperonal derivatives are selected as starting materials to prepare the substituted cinnamamide derivatives of the present invention by Wittig reaction and acid-amine condensation reaction. Further, a use of the present compounds in preventing and treating depressive-type mental diseases is disclosed. | 05-01-2014 |
20140128433 | METHODS FOR THE ADMINISTRATION OF ILOPERIDONE - The present invention relates to methods for the identification of genetic polymorphisms that may be associated with a risk for QT prolongation after treatment with iloperidone and related methods of administering iloperidone to patients with such polymorphisms. | 05-08-2014 |
20140187582 | SOLID DISPERSIONS OF AMORPHOUS PAROXETINE MESYLATE - The invention relates to solid dispersions containing paroxetine mesylate. One solid dispersion contains amorphous paroxetine mesylate and a methacrylic acid-methyl methacrylate copolymer, where the weight ratio of paroxetine mesylate to polymer ranges from about 30:70 to about 90:10. Another solid dispersion contains amorphous paroxetine mesylate and a -vinylpyrrolidone/vinylacetate copolymer (PVP-VA), where the weight ratio of paroxetine mesylate to copolymer ranges from about 30:70 to about 50:50. An amorphous solid dispersion of the invention may have a single glass transition temperature. An amorphous solid dispersion is stable for at least 48 hours at 60° C. and 75% relative humidity. A further embodiment of the invention relates to pharmaceutical compositions of paroxetine mesylate comprising a solid dispersion of the invention and at least one pharmaceutically acceptable excipient. Methods for the treatment using paroxetine mesylate in the form of a solid dispersion according to the invention are also disclosed. | 07-03-2014 |
20140187583 | Polymorph Form of 4-methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid - The present invention relates to novel crystal forms of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid. More particularly, the invention relates to polymorph forms (Polymorph Form I or Polymorph Form II), and to processes for the preparation of, compositions containing and to uses of, such polymorph forms. | 07-03-2014 |
20140221426 | SELECTIVE METABOLIC APPROACH TO INCREASING ORAL BIOAVAILABILITY OF PHENYLEPHRINE AND OTHER PHENOLIC BIOACTIVITIES - Presystemic metabolism in intestine of bioactives such as phenylephrine is avoided by administering a subject (human or animal) the bioactive (e.g., phenylephrine) in combination with one or more inhibitors of sulfation (e.g., sulfotransferase enzymes aka SULTs). This can also be enhanced be co-administering inhibitors of monoamine oxidases aka, MAOs, and uridine diphosphate glucoronysl transferases, aka UGTs. Preferably the inhibitors are GRAS compounds. The one or more inhibitor compounds inhibit the enzymes responsible for rapid presystemic metabolism, thus allowing the bioactives (e.g., phenylephrine) to be more readily absorbed intact into the circulatory system. | 08-07-2014 |
20140235674 | METHOD OF TREATING THERMOREGULATORY DISFUNCTION WITH PAROXETINE - The present invention relates to a method for treating a patient suffering from a thermoregulatory dysfunction, especially hot flashes and flushes associated with hormonal changes due to naturally occurring menopause (whether male or female) or due to chemically or surgically induced menopause. The method is also applicable to treating the hot flashes, hot flushes, or night sweats associated with disease states that disrupt normal hormonal regulation of body temperature. | 08-21-2014 |
20140243370 | Pyrano[3,2-D][1,3]thiazole as glycosidase inhibitors - Novel compounds of formula (I) | 08-28-2014 |
20140249182 | METHOD OF TREATING THERMOREGULATORY DYSFUNCTION WITH PAROXETINE - The present invention relates to a method for treating a patient suffering from a thermoregulatory dysfunction, especially hot flashes and flushes associated with hormonal changes due to naturally occurring menopause (whether male or female) or due to chemically or surgically induced menopause. The method is also applicable to treating the hot flashes, hot flushes, or night sweats associated with disease states that disrupt normal hormonal regulation of body temperature. | 09-04-2014 |
20140350051 | Dual Modulators Of 5HT2A and D3 Receptors - The present invention relates to compounds of the formula (I) | 11-27-2014 |
20150031725 | COMPOSITIONS AND METHODS FOR TREATING CANCER - Provided herein, inter alia, are compositions and methods useful for treating hyperproliferative diseases, including cancer and non-malignant hyperproliferative diseases. | 01-29-2015 |
20150045390 | ILOPERIDONE METABOLITE FOR USE IN THE TREATMENT OF PSYCHIATRIC DISORDERS - R-P88 is used for the treatment of disorders amenable to treatment with an atypical antipsychotic. | 02-12-2015 |
20150051247 | COMPOUNDS AND METHODS FOR TREATING CANCER BY INHIBITING THE UROKINASE RECEPTOR - Compounds and methods for treating or preventing cancer associated with binding to the urokinase receptor are provided. Biological processes affected by the compounds include cell migration, cell growth, cell adhesion, angiogenesis, cancer cell invasion, apoptosis, tumor formation, tumor progression, metastasis, degradation of the extracellular matrix, pericellular proteolysis, activation of plasminogen, changes in the levels of an extracellular protease, and changes in the levels of a VEGF receptor. | 02-19-2015 |
20150073019 | AMINOMETHYLENE PYRAZOLONES WITH THERAPEUTIC ACTIVITY - A compound having the structure according to formula III wherein: X is NH or S; R | 03-12-2015 |
20150133499 | PHARMACEUTICAL COMPOSITIONS OF 5-HYDROXYTRYPTOPHAN AND SEROTONIN-ENHANCING COMPOUND - This invention relates to novel pharmaceutical compositions comprising a therapeutically effective amount of a slow-release formulation of 5-hydroxytryptophan (5-HTP) and a serotonin-enhancing compound. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for combating CNS disorders, including depressive disorders, bipolar disorders, anxiety disorders, obesity and pain. | 05-14-2015 |
20150315648 | ANTIPSYCHOTIC TREATMENT BASED ON DRD2 OR ANKK1 SNP GENOTYPE - The present invention relates to the treatment of an individual with an antipsychotic based on individual's genotype at one or more single nucleotide polymorphism (SNP) associated with the dopamine receptor D2 (DRD2) and/or ankyrin repeat and kinase domain containing 1 (ANKK1) genes. | 11-05-2015 |
20150322055 | POLYMORPH FORMS - The present invention relates to novel crystal forms of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid. More particularly, the invention relates to polymorph forms (Polymorph Form I, Polymorph Form II, Polymorph Form III, Polymorph Form IV, Polymorph Form V, and Polymorph Form VI), and to processes for the preparation of compositions containing and to uses of such polymorph forms. | 11-12-2015 |
20160053324 | METHODS FOR THE ADMINISTRATION OF ILOPERIDONE - The present invention relates to methods for the identification of genetic polymorphisms that may be associated with a risk for QT prolongation after treatment with iloperidone and related methods of administering iloperidone to patients with such polymorphisms. | 02-25-2016 |
20160082065 | PROPHYLACTIC USE OF NEUROPROTECTANTS IN SPORTS-RELATED TRAUMATIC BRAIN INJURY - Dietary supplements for reducing damage to brain cells characterized by loss of brain cells or loss of brain cell function in patients that have suffered from traumatic brain injury (“TBI”) while participating in sports and/or other athletic events are disclosed herein. The Nutraceutical compositions offer possible ameliorating effects for the secondary phase of TBI. Creatine, vitamin E, zinc, magnesium, DHA, and lipoic acid, taken together, offer a prophylactic measure to ameliorate brain damage that occurs during the secondary phase of SRTBI. | 03-24-2016 |
20160106727 | COMPOSITION AND METHOD FOR THE TREATMENT OF NEURODEGENERATION - A composition and method for the treatment of neurodegeneration and brain-derived neurotrophic factor. The composition and method comprising providing paroxetine, simvastatin, and optionally, an antioxidant. | 04-21-2016 |
20160107996 | Mitochondrial Aldehyde Dehyrogenase-2 Modulators and Methods of Use Thereof - The present disclosure provides compounds of formula (I) that function as modulators of mitochondrial aldehyde dehydrogenase-2 (ALDH2) activity, and methods of preparing these compounds. | 04-21-2016 |
20160136148 | SOLID DISPERSIONS OF AMORPHOUS PAROXETINE MESYLATE - The invention relates to solid dispersions containing paroxetine mesylate. One solid dispersion contains amorphous paroxetine mesylate and a methacrylic acid-methyl methacrylate copolymer, where the weight ratio of paroxetine mesylate to polymer ranges from about 30:70 to about 90:10. Another solid dispersion contains amorphous paroxetine mesylate and a-vinylpyrrolidone/vinylacetate copolymer (PVP-VA), where the weight ratio of paroxetine mesylate to copolymer ranges from about 30:70 to about 50:50. An amorphous solid dispersion of the invention may have a single glass transition temperature. An amorphous solid dispersion is stable for at least 48 hours at 60° C. and 75% relative humidity. A further embodiment of the invention relates to pharmaceutical compositions of paroxetine mesylate comprising a solid dispersion of the invention and at least one pharmaceutically acceptable excipient. Methods for the treatment using paroxetine mesylate in the form of a solid dispersion according to the invention are also disclosed. | 05-19-2016 |
20160137662 | COMPOSITIONS AND METHODS FOR TREATING CANCER - Provided herein, inter alia, are compositions and methods useful for treating hyperproliferative diseases, including cancer and non-malignant hyperproliferative diseases. | 05-19-2016 |
20160166560 | Urea Compounds and Their Use as FAAH Enzyme Inhibitors | 06-16-2016 |
20160166561 | ANTIPSYCHOTIC TREATMENT BASED ON DRD2 OR ANKK1 SNP GENOTYPE | 06-16-2016 |
20160251324 | MACROCYCLIC UREA AND SULFAMIDE DERIVATIVES AS INHIBITORS OF TAFIA | 09-01-2016 |
20170233810 | METHOD AND SYSTEM TO PREDICT SSRI RESPONSE | 08-17-2017 |