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Additional hetero atom in the polycyclo ring system

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514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514183000 - Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI

514212010 - Hetero ring is seven-membered consisting of one nitrogen and six carbons

514213010 - Polycyclo ring system having the seven-membered hetero ring as one of the cyclos

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DocumentTitleDate
20120172349THERAPEUTIC COMPOUNDS AND COMPOSITIONS - Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.07-05-2012
20120184532GALANTAMINE AMINO ACID AND PEPTIDE PRODRUGS AND USES THEREOF - Prodrugs of galantamine or its 3-hydroxy metabolite with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and methods for treating a memory or cognition disorder with the galantamine prodrugs are provided herein. Prodrugs having side chains of valine, phenylalanine, tyrosine or para amino benzoic acid and mono-, di- and tripeptides thereof are preferred. Additionally, methods for avoiding or minimizing the adverse gastrointestinal side effects associated with galantamine administration, as well as improving the pharmacokinetics of galantamine are provided herein.07-19-2012
20120184531BENZOFURO[3,2-c] PYRIDINES AND RELATED ANALOGS AS SEROTONIN SUB-TYPE 6 (5-HT6) MODULATORS FOR THE TREATMENT OF OBESITY, METABOLIC SYNDROME, COGNITION AND SCHIZOPHRENIA - The present invention relates to benzofuro[3,2-c]pyridine and azepine analogs as serotonin sub-type 6 (5-HT07-19-2012
20100152163AZEPINO[4,5-B]INDOLES AND METHODS OF USE - This disclosure relates to new azepino[4,5-b]indole compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new 1,2,3,4,5,6-tetrahydroazepino[4,5-b]indoles. Pharmaceutical compositions are also provided.06-17-2010
20110195954NOVEL COMPOUNDS - The present invention relates to new CGRP-antagonists of general formula I08-11-2011
20130040938COMPOSITIIONS FOR TREATING COGNITIVE DISORDERS - Disclosed herein is a pharmaceutical composition comprising a cholinesterase inhibitor and compound of the following formula:02-14-2013
20090042862NOVEL COMPOUNDS - The present invention relates to novel bicyclic benzamide derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.02-12-2009
20090325931USE OF CDK INHIBITORS FOR THE TREATMENT OF GRANULOCYTE MEDIATED DISORDERS - Described herein is the use of CDK inhibitors such as roscovitine for inducing apoptosis of granulocytes, for example neutrophils. Their use for treating inflammatory diseases is also provided.12-31-2009
20130090331TRICYCLIC HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF JANUS KINASE - The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.04-11-2013
20090306047HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS - Disclosed are compounds of the formula I12-10-2009
20130072474TREATMENT OF DEMENTIA OF ALZHEIMER'S TYPE WITH MASITINIB - The present invention relates to the use of masitinib or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment of dementia of Alzheimer's type, at appropriate dosage regimen.03-21-2013
20130072473COMPOUNDS FOR TREATING PROTEIN FOLDING DISORDERS - The present invention is directed to compounds of Formulae (I), (IIa-IIh), (IIIa-IIIe), (IVa-IVc), (Va-V1), (VIa-VII), (VII), (VIII) and (IX), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis.03-21-2013
20110059948QUINOLINE, NAPHTHALENE AND CONFORMATIONALLY CONSTRAINED QUINOLINE OR NAPHTHALENE DERIVATIVES AS ANTI-MYCOBACTERIAL AGENTS - The invention relates to a compound of general formula I, II, III, IV, V, VI, VII, VIII, IX, X or a tautomer and the stereochemically isomeric forms thereof or pharmaceutically acceptable salts thereof, a N-oxide form thereof or a pro-drug thereof. The compound is usable as a medicament for the treatment of mycobacterial disease.03-10-2011
20130059837BENZAZEPINE COMPOUND - Provided is a compound which is useful as an agent for treating or preventing 5-HT03-07-2013
20110015179COMPOSITIONS FOR TREATING COGNITIVE DISORDERS - Disclosed herein is a pharmaceutical composition comprising a cholinesterase inhibitor and compound of the following formula:01-20-2011
20080275026Benzamide derivatives as oxytocin agonists and vasopressin antagonists - Novel compounds according to general formula 1, wherein G11-06-2008
20090270370FUSED HETEROCYCLIC COMPOUNDS - Certain fused pyrrole- and pyrazole-containing heterocyclic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.10-29-2009
20080318929Pyrimidine Derivatives Useful as Inhibitors of Pkc-Theta - Disclosed are novel compounds of formula (I) wherein R12-25-2008
20080293694New compounds - The present invention relates to novel compounds of formula (I):11-27-2008
20080293693Treatment or Prevention of Ovarian Hyperstimulation Syndrome (Ohss) Using a Dopamine Agonist - Disclosed herein is a method for preventing ovarian hyperstimulation syndrome in a subject by administering an effective amount of a dopamine agonist in a pharmaceutically acceptable carrier. Also disclosed herein is a method for treating ovarian hyperstimulation syndrome by administering an effective amount of a dopamine agonist in a pharmaceutically acceptable carrier.11-27-2008
20110144094HETEROCYCLIC TETRACYCLIC TETRAHYDROFURAN DERIVATIVES - This invention concerns novel substituted heterocyclic tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonin receptors, in particular 5-HT06-16-2011
20090023706Method of Treating Organophosphorous Poisoning - The present invention is directed to various methods for treating organophosphorus poisoning in an animal that is at risk of exposure to an organophosphorus compound or preventing organophosphorus poisoning in an animal that has been exposed to an organophosphorus compound, by administering a therapeutically effective amount of galantamine or a salt thereof, or a biologically active analog, derivative, fragment or variant thereof.01-22-2009
20100234351FUSED NITROGEN-COMPRISING HETEROCYCLIC COMPOUND - A compound of the formula:09-16-2010
20100331311GALANTAMINE AS A NEUROPROTECTIVE DRUG FOR RETINAL GANGLION CELLS - The present invention relates to the use of galantamine for neuroprotection of retinal ganglion cells.12-30-2010
20100113421NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS - Compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein X, R05-06-2010
20100113422Pyrimido [4,5-D] Azepine Derivatives As 5-HT2C Agonists - The present invention provides a compound of formula (I):05-06-2010
20110269744Benzazepine Compound - [Problem] Provided is a compound which is useful as an agent for treating or preventing 5-HT11-03-2011
20110201597METHOD AND COMPOSITION FOR TREATING ALZHEIMER-TYPE DEMENTIA - There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetylcholinesterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-anticholinergic antiemetic agent, whereby an enhanced acetylcholinesterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-anticholinergic antiemetic agent for the preparation of a pharmaceutical composition for the treatment of Alzheimer type dementia in combination with an acetylcholinesterase inhibitor (AChEI) and pharmaceutical compositions comprising (a) a 5HT08-18-2011
20100286123INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL - This invention relates to compounds having structural Formula I:11-11-2010
20110195953COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS - The invention generally relates to thienopyridinone 5-HT08-11-2011
20100227852Combination therapy using 1-aminocyclohexane derivatives and acetylcholinesterase inhibitors - The invention relates to a novel drug combination therapy useful in the treatment of dementia comprising administering an 1-aminocyclohexane derivative such as memantine or neramexane and an acetylcholinesterase inhibitor (AChEI) such as galantamine, tacrine, donepezil, or rivastigmine.09-09-2010
200900884184-SUBSTITUTED QUINUCLIDINE DERIVATIVES, METHODS OF PRODUCTION, AND PHARMACEUTICAL USES THEREOF - The present invention relates to compounds and formulations capable of affecting nicotinic acetylcholine receptors (nAChRs), for example, as modulators of specific nicotinic receptor subtypes (specifically, the alpha7 nAChR subtype). The present invention also relates to methods for treating a wide variety of conditions and disorders, particularly those associated with dysfunction of the central and autonomic nervous systems.04-02-2009
20100249110SUBSTITUTED PYRAZOLO-PYRIMIDINE COMPOUNDS - The present invention relates to substituted pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.09-30-2010
20100249109SUBSTITUTED TETRAHYDROPYRAZOLO-PYRIDO-AZEPINE COMPOUNDS - The present invention relates to substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.09-30-2010
20100249108SUBSTITUTED DIPYRIDO-PYRIMIDO-DIAZEPINE AND BENZO-PYRIDO-PYRIMIDO COMPOUNDS - The present invention relates to substituted dipyrido-pyrimido-diazepine compounds, substituted benzo-pyrido-pyrimido-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted dipyrido-pyrimido-diazepine compounds, substituted benzo-pyrido-pyrimido-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.09-30-2010
20100249107Biomarkers for Alzheimer's Disease Progression - This invention relates generally to the analytical testing of tissue samples in vitro, and more particularly to aspects of genetic polymorphisms associated with the conversion from Mile Cognitive Impairment to dementia, e.g., Alzheimer's Disease (AD). The invention provides AD-associated mutations which are useful in the diagnosis, prognosis or therapeutic treatment of dementia, e.g., Alzheimer's Disease.09-30-2010
20080207594Use of Gsk-3 Inhibitors for Preventing and Treating Pancreatic Autoimmune Disorders - This invention relates to the use of Pax4 stimulating compounds, e.g. Glycogen synthase kinase-3 (GSK-3) inhibitors, particularly in combination with immunomodulating agents, in the prevention, and/or treatment of pancreatic autoimmune disorders, e.g. type I diabetes or LADA. More particularly, this invention relates to the use of compounds selected from paullones, indirubines, substituted ureas, maleimide derivatives and pyrimidine thiones. Further, the present invention relates to a method of identifying and/or characterizing pancreatic beta-cell mitogens by using cells expressing a pancreatic gene or a gene whose function is controlled by a pancreatic gene, particularly the Pax4 gene, and which are transfected with a reporter gene.08-28-2008
20080269195Compounds Having Affinity For the Dopamine D3 Receptor and Uses Thereof in Medicine - Compounds of formula (I) or a salt thereof are disclosed:10-30-2008
20090298810IL-8 Receptor Antagonists - This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (II-8).12-03-2009
201102077172-AMINOPYRIMIDINE COMPOUNDS AS SEROTONIN RECEPTOR MODULATORS - Certain 2-aminopyrimidine compounds are serotonin receptor modulators useful in the treatment of diseases mediated by serotonin receptors.08-25-2011
20090181947BICYCLIC ENAMINO(THIO)CARBONYL COMPOUNDS - The present invention relates to novel bicyclic enamino(thio)carbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.07-16-2009
20090131408Organic Compounds - The present invention relates to novel aza-thia-benzoazulene derivatives of formula I as defined in the claims, their preparation, the use of these novel compounds for the preparation of pharmaceutical compositions, the use of these novel compounds and compositions for managing arthritis and arthritis-related conditions as well as in the treatment of pain in animals and humans. More particularly, the present invention relates to pharmaceutical, preferably veterinary compositions and methods for reducing inflammation and pain associated with acute inflammation of body parts, particularly joints, due to injury or due to arthritic conditions or other disease conditions.05-21-2009
20110144093METHOD OF TREATING ORGANOPHOSPHOROUS POISONING - A method for treating organophosphorous poisoning (OP) comprising administering to a mammal at risk for OP poisoning an OP poisoning-inhibiting amount of galantamine.06-16-2011
20080261954Cholinergic Enhancers with Improved Blood-Brain Barrier permeability for the Treatment of Diseases Accompanied by Cognitive Impairment - The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g. Galanthamine, narwedine and lycoramine, or from metabolites of said compounds.10-23-2008
20080261953Compounds, Compositions and Methods of Inhibiting Alpha-Synuclein Toxicity - Compounds and compositions are provided for treatment or amelioration of one or more symptoms of α-synuclein toxicity, α-synuclein mediated diseases or diseases in which α-synuclein fibrils are a symptom or cause of the disease. In one embodiment, the compounds for use in the compositions and methods are heteroaryl acylguanidines, heteroarylhydrazones, dihy-dropyridones, heteroaryl and aryl styryl ketones, and heteroarylpyrazoles.10-23-2008
200901978685ht2c receptor modulator compositions and methods of use - The present invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist. In addition, the invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist having Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof. These compositions are useful in pharmaceutical compositions whose use includes the treatment of obesity.08-06-2009
20090197869AZEPINE INHIBITORS OF JANUS KINASES - The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.08-06-2009
20090239844ACE INHIBITOR-VASOPRESSIN ANTAGONIST COMBINATIONS - Combinations of ACE inhibitors and vasopressin antagonists are useful to slow and reverse the process of ventricular dilation, and CHF in mammals.09-24-2009
20090239843Bridged diazepan orexin receptor antagonists - The present invention is directed to bridged diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.09-24-2009
20090048234Pharmaceutical compositions and methods for preventing, treating, or reversing neuronal dysfunction - 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. The compositions of the invention preferably comprise in effective amounts (a) at least one acetylcholinesterase inhibitor, (b) at least one compound with anticholinergic properties or both anticholinergic and antiglutamatergic properties, (c) optionally an anticonvulsive compound, and a pharmaceutically acceptable carrier.02-19-2009
20100216775Adamantanamines and Neramexane Salts of Thiomolybdic and Thiotungstic Acids - This invention concerns adamantanamines (e.g. memantine, amantadine, and rimantadine) and neramexane salts of thiomolybdic and thiotungstic acids, including their preparation and pharmaceutical compositions, as dual acting drugs. These salts are used to treat or potentially arrest the neurodegenerative pathophysiology, clinical signs and symptoms of dementia of the Alzheimer's type, Parkinson's, Huntington's, AIDS-related dementia and Schizophrenia and its cognitive deficits. Additional uses of these derivatives include antiviral activity. The novel compositions of the present invention appear particularly useful in enhancing the therapeutic benefits of copper-sequestering tetrathiomolybdates in treating elevated copper-induced toxicities in neurologically presenting Wilson's disease, and in treating diseases of the inflammatory etiology and abnormal copper biochemistry, such as tumor angiogenesis, liver cirrhosis, hepatitis, pulmonary fibrosis and other fibrotic diseases, cardiovascular disease, cerebral ischemia, renal anemia, rheumatoid arthritis, diabetes, obesity, gastrointestinal disorders, and eye diseases such as glaucoma, proliferative diabetic retinopathy, and age related macular degeneration. These compounds have excellent stability and aqueous solubility for good oral bioavailability.08-26-2010
20100152164Method For Stabilizing Anti-Dementia Drug - The present invention provides a method for stabilizing an anti-dementia drug in a pharmaceutical composition containing the anti-dementia drug and a high molecular weight basic substance by adding a high molecular weight acidic substance to said pharmaceutical composition. Further, the present invention provides a pharmaceutical composition containing an anti-dementia drug and a high molecular basic substance in which a high molecular weight acidic substance is contained for stabilizing the anti-dementia drug. Furthermore, the present invention provides a method for manufacturing a pharmaceutical composition which comprises steps wherein a solution or suspension containing a high molecular weight acidic substance is added to a mixture of an anti-dementia drug and a high molecular weight basic substance for the sake of stabilizing the anti-dementia drug.06-17-2010
20100240637Inhibitors of the Interaction Between MDM2 and P53 - The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds:09-23-2010
20110112072THIOPHENYL AND PYRROLYL AZEPINES AS SEROTONIN 5-HT2C RECEPTOR LIGANDS AND USES THEREOF - The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are thiophenyl and pyrrolyl azepine compounds. These compounds are serotonin receptor (5-HT05-12-2011
20130217675PYRIDO [4,3-B] INDOLE AND PYRIDO [3,4-B] INDOLE DERIVATIVES AND METHODS OF USE - This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.08-22-2013
20080287423Use of Azapaullones For Preventing and Treating Pancreatic Autoimmune Disorders - This invention relates to the use of azapaullones, particularly in combination with immunomodulating agents, in the prevention, and/or treatment of pancreatic autoimmune disorders, e.g. type I diabetes or LADA and neurodegenerative disorders.11-20-2008
20100311726REDUCTION OF BETA-AMYLOID LEVELS BY TREATMENT WITH THE SMALL MOLECULE DIFFERENTIATION-INDUCING FACTOR - The present invention relates to novel uses for a family of small molecules, Differentiation-Inducing Factors (DIFs). It has been discovered that DIFs surprisingly can alter the metabolic processing of amyloid precursor protein (APP) and in turn reduce the level of secreted Aβ. The metabolic processing of other γ-secretase substrates normally present in cells (Notch and APLP1) is not affected when treated with DIF. The invention provides methods for reducing Aβ production in mammalian cells that express APP by administering DIF-I, DIF-2, DIF-3, a functionally equivalent analog and or any combination thereof. The invention also provides methods for treating and/or preventing Alzheimer's disease by preferentially reducing Aβ production.12-09-2010
20110021503USE AND COMPOSITION FOR TREATING DEMENTIA - There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-selective, peripheral anticholinergic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-selective, peripheral anticholinergic agent (nsPAChA) for the preparation of a pharmaceutical composition for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia and pharmaceutical compositions comprising a non-selective peripheral anticholinergic agent of formula II as illustrated in the description and an acetylcholine esterase inhibitor are also described.01-27-2011
20110039826PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF CANCER AND OTHER DISEASES OR DISORDERS - This invention provides novel pharmaceutical compositions of the compound of formula (I):02-17-2011
20100144704Method of reducing amyloid-beta peptide levels using a bisdioxopiperazine - Disclosed are methods of reducing amyloid-β peptide levels in a subject. The method involves administering to the subject a therapeutically effective amount of a bisdioxopiperazine or a pharmaceutically acceptable salt thereof to reduce β-amyloid peptide levels.06-10-2010
20130190295AZEPINO[4,5-B]INDOLES AND METHODS OF USE - This disclosure relates to new azepino[4,5-b]indole compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new 1,2,3,4,5,6-tetrahydroazepino[4,5-b]indoles. Pharmaceutical compositions are also provided.07-25-2013
20090221554METHOD OF TREATING COGNITIVE IMPAIRMENT - Disclosed is an method of treating cognitive impairment, including administering to a subject in need thereof a combination of a therapeutic agent for neurodegenerative disease and a therapeutically effective amount of a heterocyclic compound represented by the following general formula (I):09-03-2009
20090312306TETRAHYDRO-5H-PYRIDO[2,3-D]AZEPINES AS 5-HT2C LIGANDS - A compound of Formula I:12-17-2009
20090215748FXR agonists for treating vitamin D associated diseases - Provided are certain methods of treating at least one condition that can be treated by elevating the vitamin D receptor (VDR) activity level in a patient with at least one farnesoid X receptor (FXR) agonist. Also provided are certain methods of modulating levels of Cytochrome P450, family 27, subfamily B, polypeptide 1 (CYP27B1) and 1α,25-dihydroxyvitamin D08-27-2009
20100069361Fused Thiazole Derivatives as Kinase Inhibitors - A series of 5,5-dimethyl-5,6-dihydro-1,3-benzothiazol-7(4H)-one and 7,7-dimethyl-5,6,7,8-tetrahydro-4H-[1,3]thiazolo[5,4-c]azepin-4-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted benzofused morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. Formula (I).03-18-2010
20110098277Fab I Inhibitors - Compounds are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections.04-28-2011
20110098278GALANTAMINE AMINO ACID AND PEPTIDE PRODRUGS AND USES THEREOF - Prodrugs of galantamine or its 3-hydroxy metabolite with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and methods for treating a memory or cognition disorder with the galantamine prodrugs are provided herein. Prodrugs having side chains of valine, phenylalanine, tyrosine or para amino benzoic acid and mono-, di- and tripeptides thereof are preferred. Additionally, methods for avoiding or minimizing the adverse gastrointestinal side effects associated with galantamine administration, as well as improving the pharmacokinetics of galantamine are provided herein.04-28-2011
20100099664SUBSTITUTED PYRROLIDINE AMIDES, THE PRODUCTION THEREOF, AND THE USE THEREOF AS MEDICATIONS - The object of the present invention is novel substituted pyrrolidine amides of the general formula (I) in which D, L. E, G, J, M, L04-22-2010
20120202791Tricyclic and Tetracyclic Systems with Activity on the Central Nervous and Vascular Systems - The present invention relates to chemistry and pharmacy and, in particular, to the production of novel molecular entities, tricyclic and tetracyclic derivatives of benzodiazepine, pyridodiazepine and pyrimidodiazepine type fused with 1,4-dihydropyridine derivatives, having an effect on the central-nervous and vascular systems. Derivatives containing a dihydropyridine ring are used, by means of reactions with compounds of the ortho-phenylenediamine, ortho-diaminopyridine and ortho-diaminopyrimidine type, and also subsequent conversions to some thereof, to obtain tricyclic and tetracyclic derivatives of general formula I-XII that contain a diazepine or diazepinone nucleus fused to a 1,4-dihydropyridine nucleus, in which the A ring is a substituted or unsubstituted benzene, pyridine or pyrimidine ring. These molecular entities exhibit GABAergica and modulating action in the case of calcium channels which can be used in the treatment of cardiovascular, cerebrovascular, neurodegenerative, neuropsychiatric and neurological disorders.08-09-2012
20080221084METHOD FOR REDUCING INFARCTION USING VASOPRESSIN ANTAGONIST COMPOUNDS, AND COMPOSITIONS AND COMBINATIONS THEREFOR - The present invention relates to a method for reducing infarction comprising administering to a patient ion need thereof a therapeutically effective amount of a composition comprising as an active ingredient a vasopressin antagonist compound and to a composition useful therefor. The present invention also relates to a method for reducing infarction comprising administering to a patient in need thereof a therapeutically effective amount of a combination of a vasopressin antagonist compound and a beta-blocker and to combinations useful therefor. The methods, compositions and combinations of the present invention can be used for reducing infarction in the heart (myocardial infarction) and the brain (stroke). The methods, compositions and combinations of the present invention can also be used for the treatment and/or prevention of hypertension, edema, ascites, heart failure, renal function disorder, vasopressin inappropriate secretion syndrome (SIADH), hepatocirrhosis, hyponatremia, hypokalemia, polycystic kidney disease, diabetes, or circulation disorder.09-11-2008
20110136789C-MET PROTEIN KINASE INHIBITORS - The present invention relates to compounds of formula I useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative disorders.06-09-2011
20090137557Calcilytic Compounds - Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.05-28-2009
20100305102HETEROCYCLE-SUBSTITUTED PIPERAZINO-DIHYDROTHIENOPYRIMIDINES - The invention relates to new dihydrothienopyrimidinesulphoxides of formula 1, as well as pharmacologically acceptable salts thereof,12-02-2010
20100324024Quinolizidinone M1 Receptor Positive Allosteric Modulators - The present invention is directed to compounds of formula (I) (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.12-23-2010
201100398241,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylate nuclear receptor inhibitors - Provided are certain 1,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylate compounds which are useful for modulating the activity of nuclear receptors, such as farnesoid X receptors, and/or for the treatment, prevention, or amelioration diseases or disorders related to the activity of these receptors.02-17-2011
201000296171,4,5,6,7,8-HEXAHYDRO-1,2,5-TRIAZA-AZULENE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS - The invention relates to 1,4,5,6,7,8-hexahydro-1,2,5-triaza-azulene derivatives and their use as orexin receptor antagonists.02-04-2010
20100016287COMPOUNDS HAVING AFFINITY FOR DOPAMINE D3 RECEPTOR AND USES THEREOF" - Compounds of formula (I)01-21-2010
20100081645TRICYCLIC HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF JANUS KINASE - The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.04-01-2010
20110082130PIPERAZINYL OXOALKYL TETRAHYDROISOQUINOLINES AND RELATED ANALOGUES - Piperazinyl oxoalkyl tetrahydroisoquinolines and related analogues of the Formula:04-07-2011
20090062258FUSED PYRIMIDINE DERIVATIVE AND USE THEREOF - The present invention provides a compound represented by the formula (I) and a salt thereof03-05-2009
20120178740HETEROCYCLIC COMPOUNDS AS JAK RECEPTOR AND PROTEIN TYROSINE KINASE INHIBITORS - The invention relates to compounds of general formula (I) wherein A, R07-12-2012
20120040966ANTI-VIRAL COMPOUNDS, TREATMENT, AND ASSAY - The compounds provided herein are suitable for inhibiting a virus in a patient and for treating a patient suffering from a viral infection such as an influenza virus. Also provided is a method for screening of compounds for use in treating and preventing viral infections. The assay screens compounds for activity against an influenza virus by measuring the cytopathogenic effect (CPE) of the compound on influenza infected-cells using percent cell viability as the end point.02-16-2012
20120040965SUBSTITUTED AZEPINO[4,3-B]INDOLES, PHARMACOLOGICAL COMPOSITION AND A METHOD FOR THE PRODUCTION AND USE THEREOF - The invention relates to novel chemical compounds, searching for novel physiologically active substances, leader compounds, “molecular tools”, and drug candidates obtained on the basis of screening of combinatorial and focused libraries of the said compounds, and also to pharmaceutical composition, methods for preparation and use thereof.02-16-2012
20110071136NOVEL TRICYCLIC PROTEIN KINASE MODULATORS - The invention provides compounds that inhibit CK2 and/or Pim kinases and compositions containing such compounds. These tricyclic compounds and compositions containing them are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, pathogenic infections, and certain immunological disorders.03-24-2011
20110071135METHOD AND COMPOSITION FOR TREATING ALZHEIMER-TYPE DEMENTIA - There is described a method for increasing the maximal tolerated close and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-anticholinergic antiemetic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-anticholinergic antiemetic agent for the preparation of a pharmaceutical composition for the treatment of Alzheimer type dementia in combination with an acetyl choline esterase inhibitor (AChEI) and pharmaceutical compositions comprising (a) a 5HT03-24-2011
20090069295DEUTERIUM-ENRICHED CONIVAPTAN - The present application describes deuterium-enriched conivaptan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-12-2009
20120046272Novel Therapeutic Compounds - The present invention describes a series of therapeutically active compounds of formula I,02-23-2012
20090156580ANTI-FOOT-AND-MOUTH DISEASE VIRUS AGENT FOR ANIMAL BELONGING TO FAMILY SUIDAE OR SHEEP, AND METHOD FOR PREVENTION OR TREATMENT OF FOOT-AND-MOUTH DISEASE IN ANIMAL BELONGING TO FAMILY SUIDAE OR SHEEP - Disclosed is an anti-foot-and-mouth disease virus agent for an animal belonging to the Family Suidae, which comprises 3-oxo-3,4-dihyro-2-pyrazincarboxamide or a salt thereof. The agent is extremely useful for the prevention or treatment of food-and-mouth disease in an animal belonging to the Family Suidae. Also disclosed is an anti-foot-and-mouth disease virus agent for sheep, which comprises 3-oxo-3,4-dihyro-2-pyrazincarboxamide or a salt thereof. The agent is extremely useful for the prevention, therapy or the like of food-and-mouth disease in sheep.06-18-2009
20090275563Combination of 5-HT7 Receptor Antagonist and Serotonin Reuptake Inhibitor Therapy - Patients suffering from serotonin-mediated diseases or conditions, such as depression, may be treated by administering an effective combined amount of a 5-HT7 receptor antagonist and a serotonin reuptake inhibitor.11-05-2009
20120015935Substituted Tetrahydropyrazolo-Pyrido-Azepine Compounds - The present invention relates to substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.01-19-2012
20110092487NOVEL 3,8-DIAZA-BICYCLO[3.2.1]OCTANE-AND 3,9-DIAZA-BICYCLO[3.3.1]-NONANE-3-CARBOXYLIC ACID ESTER DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - This invention relates to novel 3,8-diaza-bicyclo[3.2.1]octane-and 3,9-diaza-bicyclo[3.3.1]nonane-3-carboxylic acid ester derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention. Formula (I).04-21-2011
200901314091,4,5,6,7,8-HEXAHYDRO -PYRROLO[2,3-d]AZEPINES AND -IMIDAZO[4,5-d]AZEPINES AS MODULATORS OF NUCLEAR RECEPTOR ACTIVITY - Disclosed are chemical entities including compounds of Formula I05-21-2009
20090131407TETRACYCLIC KINASE INHIBITORS - The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula (I): I wherein X, Y, Z, R05-21-2009
20120258956USE OF A SPIROLIDE, ANALOGUES AND DERIVATIVES FOR TREATING AND/OR PREVENTING PATHOLOGICAL CONDITIONS LINKED TO THE TAU AND BETA-AMYLOID PROTEINS - The present invention is in the field of biomedicine. Specifically, it relates to the use of a spirolide compound with the chemical structure:10-11-2012
20120129838Composition for Preventing and Treating Alopecia Disorder Containing Morgalanthamine Compounds as an Active Ingredient - Provided are a pharmaceutical composition, a cosmetic composition and health foods for preventing and treating alopecia disorder, which include a norgalanthamine compound as an active ingredient. Since the norgalanthamine compound has an effect on growth and proliferation of dermal papilla cells that play an important role in hair growth, the norgalanthamine compound may be used for the pharmaceutical composition, the cosmetic composition and health foods, which are useful in preventing and treating alopecia disorder.05-24-2012
20100048537HETEROARYL DERIVATIVES - The present invention relates to a compound represented by formula [1] or a pharmaceutically acceptable salt thereof:02-25-2010
20100273776INHIBITION OF ALPHA-SYNUCLEIN TOXICITY - Compounds and compositions are provided for treatment or amelioration of one or more symptoms of α-synuclein toxicity, α-synuclein mediated diseases or diseases in which α-synuclein fibrils are a symptom or cause of the disease.10-28-2010
20100009969Fused Oxazoles & Thiazoles As Histamine H3- Receptor Ligands - The present invention relates to compounds comprising fused oxazole or thiazole derivatives of formula (I), processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as H01-14-2010
20090203671METHOD OF TREATING CANCER - Methods of treating cancer in patients comprising administering thereto aurora kinase inhibitors and TRAIL (tumor necrosis factor (TNF)-related apoptosis inducing ligand) inhibitors is disclosed.08-13-2009
20120220572TRICYCLIC INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts,08-30-2012
20120083486KIT, COMPOSITION, PRODUCT OR MEDICAMENT FOR TREATING COGNITIVE IMPAIRMENT - A kit, composition, product or medicament for treating cognitive impairment is provided, which includes a therapeutic agent for neurodegenerative disease and a heterocyclic compound represented by the following General Formula (I): 04-05-2012
20110124631TREATMENT OF COGNITIVE DISORDERS WITH CERTAIN ALPHA-7 NICOTINIC ACID RECEPTORS IN COMBINATION WITH ACETYLCHOLINESTERASE INHIBITORS - A method for improving cognition comprising administering to a patient (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide or a pharmaceutically acceptable salt thereof and an acetylcholinesterase inhibitor is described together with related compositions.05-26-2011
20120264741PHARMACEUTICAL COMPOSITIONS AND METHODS FOR PREVENTING, TREATING, OR REVERSING NEURONAL DYSFUNCTION - 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. The compositions of the invention preferably comprise in effective amounts (a) at least one acetylcholinesterase inhibitor, (b) at least one compound with anticholinergic properties or both anticholinergic and antiglutamatergic properties, (c) optionally an anticonvulsive compound, and a pharmaceutically acceptable carrier.10-18-2012
20110039825LIGANDS OF ALPHA-ADRENOCEPTORS, DOPAMINE, HISTAMINE, IMIDAZOLINE AND SEROTONIN RECEPTORS AND THEIR USE - The invention relates to novel ligands the broad spectrum of biological activity of which includes simultaneously α-adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors and serotonin receptors, among them serotonin 5-HT02-17-2011
20120322791PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS - The present invention provides Pyrazolopyrimidine Compounds of Formula (I):12-20-2012
20120322790Pyrazolopiperidine Compounds As CCR1 Receptor Antagonists - Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis.12-20-2012
201202772161,2-DIHYDRO-2-OXOQUINOLINE COMPOUNDS AS 5-HT4 RECEPTOR LIGANDS - 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.11-01-2012
20120329782AZEPINE INHIBITORS OF JANUS KINASES - The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.12-27-2012
20100204207Compounds and Methods for Treating Dyslipidemia - Compounds of Formula (I): wherein n, m, p, q, Y, R1, R2, R3a, R3b, R4, R5, and R6 are as defined herein and their pharmaceutical compositions and methods of use are disclosed.08-12-2010
20110319387INDOLE DERIVATIVES FOR TREATING NEURODEGENERATIVE DISEASES - The invention relates to a compound of the following formula (I),12-29-2011
20110319386NEUROGENESIS BY MUSCARINIC RECEPTOR MODULATION - The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on muscarinic receptor modulation, such as via inhibition of acetylcholine esterase (AChE) activity, alone or in combination with another neurogenic agent to stimulate or activate the formation of new nerve cells.12-29-2011
20120101086THIADIAZOLE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF DISORDERS MEDIATED BY S1P1 RECEPTORS - The present invention relates to novel compounds having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.04-26-2012
20100168082Heterobicyclic Carboxamides as inhibitors for kinases - The invention relates to novel organic compounds of formula (I)07-01-2010
20100168081GALANTAMINE AS A NEUROPROTECTIVE DRUG FOR RETINAL GANGLION CELLS - The present invention relates to the use of galantamine for neuroprotection of retinal ganglion cells.07-01-2010
20130012496BENZAZEPINE COMPOUND - Provided is a compound which is useful as an agent for treating or preventing 5-HT01-10-2013
20130172320PYRIDO [4,3-B] INDOLE AND PYRIDO [3,4-B] INDOLE DERIVATIVES AND METHODS OF USE - This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.07-04-2013
20130172321Compositions Comprising Nicotinic Agonists and Methods of Using Same - The disclosure is directed at least in part to compositions and methods comprising nicotinic agonists for treating e.g., nervous system disorders, in particular, to combination therapies that include a nicotinic agonist (for example, nicotine) and a nicotinic acetylcholine receptor desensitization inhibitor (for example, opipramol).07-04-2013
20130102590PYRIDOPYRIMIDINONE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts,04-25-2013
20130123239COMPOUNDS HAVING TRPV1 ANTAGONISTIC ACTIVITY AND USES THEREOF - The invention relates to compounds of Formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof.05-16-2013
20130158011NOVEL COMPOUNDS - This invention relates to compounds of formula I06-20-2013
20130158012USE AND COMPOSITION FOR TREATING DEMENTIA - There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-selective, peripheral anticholinergic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-selective, peripheral anticholinergic agent (nsPAChA) for the preparation of a pharmaceutical composition for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia and pharmaceutical compositions comprising a non-selective peripheral anticholinergic agent of formula II as illustrated in the description and an acetylcholine esterase inhibitor are also described.06-20-2013
20080200453Methods of treating metabolic syndrome using dopamine receptor agonists - The present invention is directed to a method of simultaneously treating hypertension, hypertriglyceridemia, a pro-inflammatory state, a pro-coagulative state, and insulin resistance (with or without treating obesity or endothelial dysfunction), associated with or independent from Metabolic Syndrome, as well as vascular disease such as cardiovascular, cerebrovascular, or peripheral vascular disease comprising the step of administering to a patient suffering from such disorders a therapeutically effective amount of a central acting dopamine agonist. In one embodiment, the central acting dopamine agonist is bromocriptine, optionally combined with a pharmaceutically acceptable carrier.08-21-2008
20080200452Oral, Rapidly Disintegrating Film, Which Cannot be Spat Out, for a Neuroleptic - Film-form, single-layered, cavity-free preparation free of surfactants, effervescent additive and taste masker and comprising one or more film former(s), one or more gel former(s) and one or more active ingredient(s) from the group of neuroleptics.08-21-2008
20110245234CRYSTALLINE FORMS OF SODIUM 4--2-METHOXYBENZOATE - The present invention is directed to a compound of formula (I):10-06-2011
20130150346Use of FAAH Inhibitors for Treating Parkinson's Disease and Restless Legs Syndrome - The present disclosure relates to methods of using fatty acid amide hydrolase (FAAH) inhibitors to treat aspects of Parkinson's disease (PD), restless legs syndrome (RLS) and periodic limb movement disorder (PLMD), the use of FAAH inhibitors for the manufacture of medicaments for use in the treatment of PD, RLS and PLMD, as well as pharmaceutically acceptable compositions comprising FAAH inhibitors for use in the treatment of PD, RLS and PLMD.06-13-2013
20130150347NOVEL COMPOUNDS - This invention relates to compounds of formula I06-13-2013
20120283245AZABICYCLO[3.1.0]HEX-2-YL COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - Compounds of formula:11-08-2012
20120283244ASSOCIATION BETWEEN 4-BENZAMIDE AND AN ACETYLCHOLINESTERASE INHIBITOR, AND PHARMACEUTICAL COMPOSITIONS CONTAINING IT - Association between 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy}benzamide of formula (I):11-08-2012
20130123238Use of (+)-1-(3,4-Dichlorophenyl)-3-Azabicyclo[3.1.0]Hexane to treat addictive and alcohol-related disorders - The present invention relates to (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane and pharmaceutically acceptable salts thereof, compositions comprising (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and methods for treating or preventing an alcohol-related or addictive disorder. The (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or pharmaceutically acceptable salt thereof is preferably substantially free of its corresponding (−)-enantiomer05-16-2013
20110306600NOVEL THERAPEUTIC COMPOUNDS - The invention discloses a number of therapeutic compounds and a method of treating a disorder in mammal.12-15-2011
20110312943AURORA KINASE INHIBITORS FOR INHIBITING MITOTIC PROGRESSION - The present invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides potent inhibitors of Aurora A kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.12-22-2011
20110312942AURORA KINASE INHIBITORS FOR INHIBITING MITOTIC PROGRESSION - The present invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides potent inhibitors of Aurora A kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.12-22-2011
201103129411,4-DISUBSTITUTED PIPERIDINES AS VASOPRESSIN RECEPTOR VIA ANTAGONISTS - The present invention provides compounds of formula (1) compositions comprising such compounds; the use of such compounds in therapy (such as in the treatment of dysmenorrhoea); and methods of treating patients with such compounds; wherein A and G are as defined herein.12-22-2011
20130190293PYRIDO [4,3-B] INDOLE AND PYRIDO [3,4-B] INDOLE DERIVATIVES AND METHODS OF USE - This disclosure is directed to tetracyclic pyrido[4,3-b]indole and pyrido[3,4-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.07-25-2013
20130190294COMPOUNDS AND METHODS FOR TREATING DIABETES - Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor α07-25-2013
20120022046Thienopyridine Derivatives for the Treatment and Prevention of Dengue Virus Infections - Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.01-26-2012
20130203737FUSED HETEROCYCLIC DERIVATIVES AS S1P MODULATORS - The present invention relates to a fused heterocyclic derivative of the formula (I)08-08-2013
20130210808CHOLINERGIC ENHANCERS WITH IMPROVED BLOOD-BRAIN BARRIER PERMEABILITY FOR THE TREATMENT OF DISEASES ACCOMPANIED BY COGNITIVE IMPAIRMENT - The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g., galantamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as “pro-drugs”, in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. The compounds of this invention may be used as medicaments.08-15-2013
20130210807Tricyclic Compounds as Allosteric Modulators of Metabotropic Glutamate Receptors. - The present invention describes and claims compounds of the Structural Formula I, Structural Formula II, or Structural Formula III: wherein R08-15-2013

Patent applications in class Additional hetero atom in the polycyclo ring system