Entries |
Document | Title | Date |
20080207600 | Pharmaceutical Combination for the Treatment of Cns Functional Disorders - The invention relates to a method and a pharmaceutical combination for the treatment of CNS disorders, which includes at least a first compound having therapeutic effect on the CNS, and a second compound which facilitates penetration through the hematoencephalic barrier of the former. The second compound is administered endonasally, and has refectory (mainly neuro- and vasoactive) effects over structures and receptors of nasal mucous membrane, mainly receptors of vomeronasal systems and trifacial nerve. | 08-28-2008 |
20080207601 | Methods of and Compositions For the Prevention of Anxiety, Substance Abuse, and Dependence - Compositions for reducing dependency and addiction to substances of abuse are provided. Chloride channels such as the GABA | 08-28-2008 |
20080207602 | SUCCINOYLAMINO BENZODIAZEPINES AS INHIBITORS OF ABETA PROTEIN PRODUCTION - This invention relates to novel lactams having the formula (I): | 08-28-2008 |
20080214526 | Macrocyclic Compounds and Compositions Useful as Bace Inhibitors - The invention relates to novel macrocyclic compounds of the formula in which R | 09-04-2008 |
20080221087 | Substituted lactams as inhibitors of abeta protein production - This invention relates to novel lactams of Formula (I): | 09-11-2008 |
20080227772 | Diazabicyclic Aryl Derivatives as Nicotinic Acetylcholine Receptor Ligands - This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 09-18-2008 |
20080227773 | Diazabicyclic Aryl Derivatives as Cholinergic Receptor Modulators - This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemicals substances. | 09-18-2008 |
20080234255 | SUBSTITUTED PYRIMIDODIAZEPINES - The present invention provides PLK1 inhibitor compounds of formula I: | 09-25-2008 |
20080255098 | Compositions and Methods for Treatment of Psychiatric Disorders - Compositions and methods for the treatment of a unipolar depression containing betaine, and folate. Formulations for oral administration optionally also contain L-methionine. | 10-16-2008 |
20080261957 | DIHYDRO-BENZO[B][1,4]DIAZEPIN-2-ONE SULFONAMIDE DERIVATIVES - The present invention relates to compounds of formula (I), a process for the manufacture thereof, their use for the preparation of medicaments for treating CNS disorders and pharmaceutical compositions containing them. Compounds of formula (I) are represented by general formula (I) | 10-23-2008 |
20080269202 | Novel 2,3-benzodiazepine derivatives and their use as antipsychotic agents - Disclosed are novel 2,3-benzodiazepine derivatives and methods of making the same. | 10-30-2008 |
20080269203 | COMPOSITIONS AND METHODS RELATING TO NOVEL COMPOUNDS AND TARGETS THEREOF - The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, and hyperproliferation, and the like. | 10-30-2008 |
20080280887 | Selected Cgrp-Antagonists, Processes for Preparing Them and Their Use as Pharmaceutical Compositions - The invention relates to CGRP-antagonists of general formula (I), wherein R | 11-13-2008 |
20080293700 | Compositions and Methods Relating to Novel Compounds and Targets Thereof - The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, and hyperproliferation, and the like. | 11-27-2008 |
20080306050 | Aminodiazepines as Toll-Like Receptor Modulators - Provided are compositions and methods useful for modulation signaling through the Toll-like receptor TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency. | 12-11-2008 |
20080318935 | SUBSTITUTED IMIDAZOHETEROCYCLES - The present invention provides substituted imidazoheterocyclic compounds having the structure of formula I | 12-25-2008 |
20090012065 | Therapeutic applications of pro-apoptotic benzodiazepines - Benzodiazepine compounds, and methods for using those compounds are provided. Some of the benzodiazepine compounds include 1,4-benzodiazepine-2-one and 1,4-benzodiazepine-2,5-dione compounds of the following structures: | 01-08-2009 |
20090012066 | Method of Use of Deacetylase Inhibitors - The present invention provides methods of treating and/or preventing pathologic cardiac hypertrophy and heart failure comprising administering hydroxamate compounds which are deacetylase inhibitors. | 01-08-2009 |
20090054413 | Novel 5,6-Dihydropyrazolo[3,4-E] [L,4]Diazepin-4 (IH) -One Derivatives for the Treatment of Asthma and Chronic Obstructive Pulmonary Disease - The present invention provides a compound of a formula (I): | 02-26-2009 |
20090054414 | Rufinamide for the Treatment of Post-Traumatic Stress Disorder - Provided are methods of treating post-traumatic stress disorder with rufinamide. Also provided are methods of treating kindling and improving resilience with rufinamide. Also provided are methods of diagnosing post-traumatic stress disorder in a patient by administering to the patient a therapeutically effective amount of rufinamide and assessing at least one of sign, symptom, or symptom cluster of post-traumatic stress disorder; and diagnosing post-traumatic stress disorder in the patient if the rufinamide reduces at least one of sign, symptom, and symptom cluster of post-traumatic stress disorder. | 02-26-2009 |
20090054415 | COMBINATIONS, METHODS AND COMPOSITIONS FOR TREATING CANCER - The invention relates to a combination of BCR-ABL inhibitor, exemplified by ‘N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide and/or other BCR/ABL inhibitors, and a stem cell selective cytotoxic, exemplified by (R)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine-7-carbonitrile, hydrochloride salt, and or other stem cell cytotoxic agents, pharmaceutical compositions of the combination and to methods of using the pharmaceutical compositions in the treatment of oncological disorders. | 02-26-2009 |
20090054416 | 1,4-Diazabicyclo[3.2.2]nonanecarboxamide Derivatives, Preparation and Therapeutic Use Thereof - The present invention discloses and claims compounds of general formula | 02-26-2009 |
20090075983 | Novel Diazabicycloalkane Derivatives and Their Medical Use - This invention relates to novel diaza-bicyclo-alkane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 03-19-2009 |
20090082341 | 4-hydroxy-4-methyl-piperidine-1-carboxylic acid (4-methoxy-7-morpholin-4-yl-benzothiazol-2-yl)-amide FOR THE TREATMENT OF POST-TRAUMATIC STRESS DISORDER - Provided are methods of treating post-traumatic stress disorder with 4-hydroxy-4-methyl-piperidine-1-carboxylic acid (4-methoxy-7-morpholin-4-yl-benzothiazol-2-yl)-amide. Also provided are methods of improving resilience with 4-hydroxy-4-methyl-piperidine-1-carboxylic acid (4-methoxy-7-morpholin-4-yl-benzothiazol-2-yl)-amide. Also provided are methods of diagnosing post-traumatic stress disorder in a patient. | 03-26-2009 |
20090082342 | N-SUBSTITUTED PIPERIDINE DERIVATIVES AS SEROTONIN RECEPTOR AGENTS - Disclosed herein are isolated forms of the compounds of Formula (I), (II), (III), (IV) and (V), or a pharmaceutically acceptable salt, prodrug, hydrate, solvate, polymorph, or ester thereof. Also disclosed are methods of inhibiting an activity of a serotonin receptor, methods inhibiting an activation of a serotonin receptor, and methods of alleviating or treating various disease conditions and side effects. | 03-26-2009 |
20090088421 | Intranasal Anti-Convulsive Compositions And Methods - Contemplated pharmaceutical compositions comprise a benzodiazepine anti-convulsive compound for intranasal administration in a single phase, multi-component solvent system with water content of at least 15 vol % and a benzodiazepine concentration of at least 30 mg/ml. It is noted that contrary to common expectation, the concentration of the anti-convulsive compound was increased by increasing water content in the multi-component solvent. Moreover, the anti-convulsive compound remained chemically stable and substantially completely dissolved over large periods of time. Thus, stable and highly concentrated spray formulations for intranasal administration could be prepared having sufficiently high concentrations of the anti-convulsive compounds that now allow single spray administration to achieve clinically relevant dosages. | 04-02-2009 |
20090093467 | THERAPEUTIC COMPOSITIONS AND METHODS - The invention includes methods, compositions, and kits useful for treating a viral infection by administering 6-(3-chloro-2-fluorobenzyl)-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable salt thereof, with atazanavir or a pharmaceutically acceptable salt thereof, and optionally with a compound that inhibits cytochrome P-450, or a pharmaceutically acceptable salt thereof. | 04-09-2009 |
20090111796 | 7-membered ring compound and method of production and pharmaceutical application thereof - A 7-membered heterocyclic compound having the formula (I), or its salt, or a solvate thereof with a chymase inhibitory action and useful for the prevention or treatment of various diseases, in which chymase is involved: | 04-30-2009 |
20090111797 | Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions - The present invention relates to the CGRP antagonists of general formula | 04-30-2009 |
20090118265 | NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONANE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 05-07-2009 |
20090118266 | NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL OXADIAZOLYL DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. | 05-07-2009 |
20090137565 | Method for treatment of movement disorders - The invention is directed to methods of treating movement disorders by administering an effective amount of the compound of formula (I) to patients in need thereof. More particularly, the invention is directed to a method for treating myoclonus including administering to a patient a compound of formula (I), wherein the myoclonus is not alcohol responsive essential myoclonus with dystonia. In some embodiments, the myoclonus is posthypoxic myoclonus. The invention is also directed to a method for treating dystonia, essential tremor cerebellar tremor, a tic, or chorea, including administering to a patient a compound of formula (I). | 05-28-2009 |
20090143366 | CHEMICAL COMPOUNDS - The present invention relates to dihydrobenzodiazepine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such dihydrobenzodiazepine derivatives are useful in the treatment of diseases associated with inappropriate ROCK kinase. | 06-04-2009 |
20090143367 | ARYL AND HETEROARYL FUSED IMIDAZO[1,5-a]PYRAZINES AS INHIBITORS OF PHOSPHODIESTERASE 10 - The invention relates to imidazo[1,5-a]pyrazine derivatives, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10 (PDE10), as active compounds for treating central nervous system diseases of mammals, including humans. | 06-04-2009 |
20090149450 | SUBSTITUTED IMIDAZOHETEROCYCLES - The present invention provides substituted imidazoheterocyclic compounds having the structure of formula I | 06-11-2009 |
20090163478 | Salts and Crystal Modifications Thereof - The invention relates to salts of 1-(2-Fluoro-phenyl)-3-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-urea and crystalline forms thereof, their production and usage, and pharmaceutical preparations containing such salts and crystalline forms. | 06-25-2009 |
20090176769 | CGRP RECEPTOR ANTAGONISTS - The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions. | 07-09-2009 |
20090176770 | Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions - The present invention relates to the CGRP antagonists of general formula | 07-09-2009 |
20090176771 | GYRASE INHIBITORS AND USES THEREOF - The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals. | 07-09-2009 |
20090186880 | NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONANE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 07-23-2009 |
20090186881 | CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions - The present invention relates to the CGRP-antagonists of general formula I | 07-23-2009 |
20090192143 | Substituted diazepan orexin receptor antagonists - The present invention is directed to substituted 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. | 07-30-2009 |
20090197872 | NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINYL DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. | 08-06-2009 |
20090197873 | COMPOSITIONS COMPRISING ALPRAZOLAM FOR TREATING PRIMARY INSOMNIA AND INSOMNIA ASSOCIATE WITH ANXIETY STATES AND PROCESS FOR PREPARING THEM - Disclosed is a composition comprising alprazolam for treating primary insomnia and insomnia associated with anxiety states and the corresponding use and method comprising the administration of alprazolam sublingual tablets having a disintegration time lower than 30 seconds and having the alprazolam preferably in non-crystalline or partially crystalline form according to the X-ray diffraction crystallography expanded for the position delta 9-12.5 (2 theta), to a patient suffering from said disorder. There is also disclosed a method for preparing a composition according to the invention, where the alprazolam is solved in a pharmaceutical acceptable solvent and a binder, preferably polyvinylpyrrolidone, is incorporated to the solution. A pre-made mixture of part of the cross-linked carboxymethyl-cellulose and the rest of the ingredients of the composition is impregnated with the solution and is dried and grinded, and is added to the rest of the cross-linked carboxymethyl-cellulose and the flavoring additives, being then mixed and compressed. | 08-06-2009 |
20090215752 | Compounds, preparation and therapeutic use thereof - The invention relates to benzodiazepine derivatives having PDE2 inhibitory activities, as well as therapeutic methods of administering said compounds, in particular for treating various diseases of the central or peripheral nervous system. The invention further includes methods of preparing the subject compounds and pharmaceutical compositions containing them. | 08-27-2009 |
20090215753 | Topical Compositions for Paediatric Use - The present invention provides pharmaceutical compositions for treating a paediatric mammal, the compositions comprising a therapeutic agent and a pharmaceutically acceptable carrier, the composition being suitable for topical application resulting in transdermal administration of the therapeutic agent and a systemic therapeutic effect. The invention also provides relates uses of the compositions, applicators and kits. | 08-27-2009 |
20090221561 | Cell Migration Modulating Compounds - The described invention relates to compounds which modulate cell migration, and find use in, for example, wound healing, cancer progression and angiogenesis. | 09-03-2009 |
20090233913 | OPTICAL ISOMERS OF DIHYDRO-2,3-BENZODIAZEPINES AND THEIR STEREOSELECTIVE SYNTHESIS - The present invention relates to dihydro-2,3-benzodiazepine compounds of high enantiomeric purity according to the general formula (I), which contain an asymmetric centre at the position 4 of the dihydro-2,3-benzodiazepine compound, and the preparation thereof and the used intermediates as well. These compounds have anti-convulsiveA muscle relaxant and neuroprotective effect due their non-competitive AMPA antagonistic properties. | 09-17-2009 |
20090253685 | Product comprising at least one Cdc25 phosphatase inhibitor in combination with at least one other anti-cancer agent - A subject of the invention is a product comprising at least one Cdc25 phosphatase inhibitor in combination with at least one other anti-cancer agent for a therapeutic use which is simultaneous, separate or spread over time in the treatment of cancer. | 10-08-2009 |
20090253686 | UNSOLVATED BENZODIAZEPINE COMPOSITIONS AND METHODS - The present invention relates to systems and methods for generating new forms of benzodiazepine and benzodiazepine related compounds as well as new compounds and formulations generated by such methods. In particular, the present invention provides high throughput systems and methods for generating and identifying new crystalline benzodiazepine and benzodiazepine related polymorphs and new unsolvated, solvated, and other forms of the compounds that find use as improved drugs and drug formations. | 10-08-2009 |
20090258864 | PYRIMIDINE-2-AMINE COMPOUNDS AND THEIR USE AS INHIBITORS OF JAK KINASES - This invention is directed to compounds of formula (I): | 10-15-2009 |
20090258865 | ADMINISTRATION OF BENZODIAZEPINE COMPOSITIONS - The invention relates to pharmaceutical compositions comprising one or more benzodiazepine drugs for nasal administration, methods for producing and for using such compositions. | 10-15-2009 |
20090258866 | CGRP Receptor Antagonists - The disclosure generally relates to the novel compounds of formula I, including their salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD). | 10-15-2009 |
20090264419 | CYCLIC MALONAMIDES AS INHIBITORS OF Abeta PROTEIN PRODUCTION - This invention relates to novel cyclic malonamides having the formula (I): | 10-22-2009 |
20090264420 | ORGANIC COMPOUNDS - The present invention provides a compound of formula I: | 10-22-2009 |
20090281092 | POLO-LIKE KINASE INHIBITORS - Compounds of the following formula are provided for use with kinases: | 11-12-2009 |
20090318427 | BENZODIAZEPINE DERIVATIVES FOR TREATING HEPATITIS C INFECTION - Use of a benzodiazepine of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or preventing a hepatitis C infection, wherein: —R | 12-24-2009 |
20090325939 | 1H-INDAZOLES, BENZOTHIAZOLES, 1,2-BENZOISOXAZOLES, 1,2-BENZOISOTHIAZOLES, AND CHROMONES AND PREPARATION AND USES THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof. | 12-31-2009 |
20100004227 | COMPOSITIONS AND METHODS RELATING TO NOVEL COMPOUNDS AND TARGETS THEREOF - The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and related compounds and methods of using benzodiazepine derivatives and related compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like. | 01-07-2010 |
20100004228 | SELECTED CGRP ANTAGONISTS, PROCESSES FOR PREPARING THEM AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - The present invention relates to the CGRP antagonists of general formula I | 01-07-2010 |
20100016294 | METHODS FOR REDUCING THE RISK OF AN ADVERSE DRUG INTERACTION IN A PATIENT SUFFERING FROM INSOMNIA - Disclosed herein is a method for treating a patient with Quazepam that reduces the risk of an adverse interaction between the Quazepam and drug that is a substrate of the cytochrome P450 enzyme isoform 2B6 (CYP2B6 substrate drug), e.g., Bupropion. The method includes determining if the patient to be treated with Quazepam is being treated with a CYP2B6 substrate drug, and prescribing or treating the patient with Quazepam based on the determination. | 01-21-2010 |
20100022519 | HETEROCYCLIC-SUBSTITUTED PIPERIDINE COMPOUNDS AND THE USES THEREOF - The invention relates to Heterocyclic-Substituted Piperidine Compounds, compositions comprising an effective amount of a Heterocyclic-Substituted Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Heterocyclic-Substituted Piperidine Compound. | 01-28-2010 |
20100029622 | MICROEMULSIONS - Pharmaceutical compositions in the form of microemulsions comprising the following components, in amounts expressed as % by weight, the sum of the components being 100%:
| 02-04-2010 |
20100048541 | SUBSTITUTED LACTAMS AS INHIBITORS OF ABETA PROTEIN PRODUCTION - This invention relates to novel lactams of Formula (I): | 02-25-2010 |
20100056500 | Stable Parenteral Formulation - The present invention relates to pharmaceutical formulations of benzodiazepine compounds which are active against Respiratory Syncytial Virus (RSV) suitable for parenteral administration. | 03-04-2010 |
20100056501 | SUBSTITUTED LACTAMS AS INHIBITORS OF ABETA PROTEIN PRODUCTION - This invention relates to novel lactams of Formula (I): | 03-04-2010 |
20100069373 | SUBSTITUTED LACTAMS AS INHIBITORS OF A BETA PROTEIN PRODUCTION - This invention relates to novel lactams of Formula (I): | 03-18-2010 |
20100081648 | Methods for Characterizing and Treating Cognitive Impairment In Aging and Disease - This invention provides methods for identifying genes associated with cognitive impairment and for identifying compounds useful in the treatment of cognitive impairment. The methods can in particular be used to identify genes associated with, and compounds useful in treating, cognitive impairment in aging. | 04-01-2010 |
20100093705 | Therapeutic agents, and methods of making and using the same - In part, the present invention is directed to antibacterial compounds. | 04-15-2010 |
20100093706 | MULTIMEDIATOR TRANSPORTER INHIBITORS FOR USE IN TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS - The invention provides a class of inhibitors, packaged pharmaceuticals comprising such inhibitors, and uses of the inhibitors in treating, or the manufacturing medicaments for treating central nervous system disorders, including depression, anxiety, sleep disorders, obesity, attention deficit disorder (ADD), attention deficit hyperactivity disorder (ADHD), sexual dysfunction, substance abuse, and movement disorders. Related business methods, such as methods for conducting a pharmaceutical business and methods for conducting a medical assistance reimbursement program, are also provided. | 04-15-2010 |
20100113428 | DIAZABICYCLIC ARYL DERIVATIVES AS CHOLINERGIC RECEPTOR MODULATORS - This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 05-06-2010 |
20100113429 | INHIBITORS OF FTSZ AND USES THEREOF - The invention relates to inhibitors of FtsZ polymerization and uses thereof. | 05-06-2010 |
20100130482 | DIAZABICYCLIC ARYL DERIVATIVES AS NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 05-27-2010 |
20100130483 | NOVEL DIAZABICYCLIC ARYL DERIVATIVES - This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 05-27-2010 |
20100137287 | ARYL-AND HETEROARYL-SUBSTITUTED TETRAHYDROBENZO-1,4-DIAZEPINES AND USE THEREOF TO BLOCK REUPTAKE OF NOREPINEPHRINE, DOPAMINE, AND SEROTONIN - The aryl- and heteroaryl-substituted tetrahydrobenzo-1,4-diazepine derivative compounds of the present invention are represented by formulae 1(A-D) having the following structure: where the substituents X and R | 06-03-2010 |
20100137288 | INDAZOLES, BENZOTHIAZOLES, BENZOISOTHIAZOLES, BENZISOXAZOLES, PYRAZOLOPYRIDINES, ISOTHIAZOLOPYRIDINES, AND PREPARATION AND USES THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof. | 06-03-2010 |
20100144715 | Substituted Benzodiazepinones, Benzoxazepinones and Benzothiazepinones as Sodium Channel Blockers - The present invention is directed to substituted benzodiazepinones, benzoxazepinones and benzothiazepinones compounds that are sodium channel blockers useful for the treatment of chronic and neuropathic pain. The compounds of the present invention are also useful for the treatment of other conditions, including disorders of the CNS such as anxiety, depression, epilepsy, manic depression and bipolar disorder. This invention also provides pharmaceutical compositions comprising a compound of the present invention, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. This invention further comprises methods for the treatment of acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain and disorders of the CNS including, but not limited to, epilepsy, manic depression, depression, anxiety and bipolar disorder comprising administering the compounds and pharmaceutical compositions of the present invention. | 06-10-2010 |
20100144716 | New CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions - The present invention relates to the CGRP-antagonists of general formula I | 06-10-2010 |
20100152171 | CGRP Antagonists - CGRP antagonists of the formula | 06-17-2010 |
20100160299 | DENDRIMER CONJUGATES - The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. | 06-24-2010 |
20100173897 | SUBSTITUTED N-PHENYL-BIPYRROLIDINE CARBOXAMIDES AND THERAPEUTIC USE THEREOF - The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). | 07-08-2010 |
20100173898 | SUBSTITUTED N-PHENYL-PYRROLIDINYLMETHYLPYRROLIDINE AMIDES AND THERAPEUTIC USE THEREOF - The present invention discloses and claims a series of substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides of formula (I). | 07-08-2010 |
20100179133 | COMPOSITIONS, ARTICLES AND METHODS COMRISING TSPO LIGANDS FOR PREVENTING OR REDUCING TOBACCO-ASSOCIATED DAMAGE - Articles of manufacturing (such as tobacco products), methods, devices and compositions for preventing or reducing tobacco-associated damage and/or disorders associated with oxidative stress in a subject, and which utilize a TSPO receptor ligand (such as diazepam), are disclosed. | 07-15-2010 |
20100197668 | 1,2,3,4-TETRAHYDROPYRROLO[1,2-A]PYRAZINE-6-CARBOXAMIDE AND 2,3,4,5-TETRAHYDROPYRROLO[1,2-a][1,4]-DIAZEPINE-7-CARBOXAMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - The present invention relates to derivatives of 1,2,3,4-tetrahydropyrrolo-[1,2-a]pyrazine-6-carboxamides and of 2,3,4,5-tetrahydropyrrolo[1,2-a][1,4]diazepine-7-carboxamides, to the preparation thereof and to the therapeutic use thereof. | 08-05-2010 |
20100210632 | NOVEL PYRROLINONE DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - The present invention provides a compound represented by the formula (I): | 08-19-2010 |
20100216780 | NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL OXADIAZOLYL DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. | 08-26-2010 |
20100222331 | NEW COMPOUNDS - The present invention encompasses compounds of general Formula (1) wherein R | 09-02-2010 |
20100222332 | PYRAZOLO-PYRAZINES DERIVATIVES USED AS G PROTEIN INHIBITORS - The invention relates to pyrazolo-pyrazines derivatives of the general formula (I) in which the radicals Z, R | 09-02-2010 |
20100234361 | SELECTED CGRP-ANTAGONISTS, PROCESS FOR PREPARING THEM AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - The present invention relates to the CGRP antagonists of general formula | 09-16-2010 |
20100240641 | Aldosterone Synthase and/or 11B-hydroxylase Inhibitors - The present invention provides a compound of formula I: | 09-23-2010 |
20100249114 | Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions - The present invention relates to the CGRP antagonists of general formula | 09-30-2010 |
20100249115 | SUBSTITUTED HETEROCYCLIC COMPOUNDS - The present invention relates to substituted heterocyclic compounds and substituted tetrahydroisoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzodiazepine compounds and substituted tetrahydroisoquinoline 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 |
20100273783 | Compositions and Methods for Treating and Preventing Overactive Bladder and Conditions Associated Therewith - Compositions and methods for the treatment and prevention of overactive bladder are provided. Such compositions and methods provide locally effective amounts of diazepam sufficient to treat or prevent overactive bladder and conditions associated therewith. | 10-28-2010 |
20100280015 | NOVAL 1,4-DIAZA-BICLO[3.2.2]NONYL OXADIAZOLYL DERIVATIVES USEFUL AS NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. | 11-04-2010 |
20100286128 | 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINYL DERIVATIVES USEFUL AS NICOTINIC ACETYLCHOLINE-RECEPTOR LIGANDS - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. | 11-11-2010 |
20100298305 | TIZANIDINE FOR THE TREATMENT OF POST-TRAUMATIC STRESS DISORDER AND NIGHTMARES - Disclosed herein are methods of treating a psychiatric disorder, such as a sleep disorder, an anxiety disorder, a mood disorder or a perceptual disturbance. In one example, a method of treating a sleep disorder or anxiety disorder includes selecting a subject with a sleep disturbance or anxiety disorder in the absence of an underlying physical disorder and administering a therapeutically effective amount of tizanidine, thereby reducing or inhibiting a symptom of the sleep disorder or anxiety disorder. In another example, a method of treating a mood disorder or a perceptual disturbance is disclosed. This method includes selecting a subject with a mood disorder or perceptual disturbance and administering a therapeutically effective amount of tizanidine, thereby reducing or inhibiting a symptom of the mood disorder or perceptual disturbance. | 11-25-2010 |
20100298306 | (1,4-Diaza-bicyclo[3.2.2]non-6-en-4-yl)-heterocyclyl-methanone Ligands for Nicotinic Acetylcholine Receptors, Useful for the Treatment of Disease - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds, which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof. The novel compounds include compounds of formula I: | 11-25-2010 |
20100298307 | NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidine derivatives of formula (I) and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 11-25-2010 |
20100305108 | NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidine derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 12-02-2010 |
20100317654 | 1,4-DIAZA-BICYCLO[3.2.2]NONYL OXADIAZOLYL DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. | 12-16-2010 |
20100324028 | NOVEL COMPOUNDS - The present invention relates to new CGRP-antagonists of general formulae Ia and Ib | 12-23-2010 |
20100331316 | 5-PHENYL-LH-BENZ0 [E] [1,4] DIAZEPINE COMPOUNDS SUBSTITUTED WITH AN HYDROXAMIC ACID GROUP AS HISTONE DEACETYLASE INHIBITORS - Novel hydroxamate histone deacetylase inhibitors of formula (I) wherein X is C═O or CH | 12-30-2010 |
20100331317 | BENZODIAZEPINE COMPOUND AND PHARMACEUTICAL COMPOSITION - The present invention provides a novel benzodiazepine compound that blocks the I | 12-30-2010 |
20110009392 | GAMMA SECRETASE MODULATORS - In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions. | 01-13-2011 |
20110009393 | Novel Soluble 1,4 Benzodiazepine Compounds and Stable Salts Thereof - The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and related compounds and methods of using benzodiazepine derivatives and related compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like. | 01-13-2011 |
20110015187 | SUBSTITUTED HETEROARYLAMIDE DIAZEPINOPYRIMIDONE DERIVATIVES - The disclosure relates to a series pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: | 01-20-2011 |
20110021508 | Methods for Alzheimer's Disease Treatment and Cognitive Enhancement - The present invention relates to compositions comprising a combination of PKC activators and PKC inhibitors and methods to modulate α-secretase activity; improve or enhance cognitive ability; and or reduce neurodegeneration in individuals suffering from diseases that impair cognitive ability, particularly Alzheimer's Disease. The invention also relates to methods for improving or enhancing cognitive ability. The present invention also provides methods for increasing the generation of non-amyloidogenic soluble APP (sAPP) comprising the activation of protein kinase C (PKC) in the brain and inhibiting PKC in peripheral tissues. Macrocyclic lactones (i.e. bryostatin class and neristatin class) are preferred PKC activators and Vitamin E is a preferred PKC inhibitor for use in the inventive composition. | 01-27-2011 |
20110034443 | USES OF SUBSTITUTED IMIDAZOHETEROCYCLES - The present invention provides methods of prevention and treatment of cannabinoid receptor-associated diseases and conditions, wherein the method includes administering a substituted imidazoheterocyclic compounds having the structure of formula I or a pharmaceutically acceptable salt, acid salt, hydrate, solvate or stereoisomer of a compound having the structure of formula I. | 02-10-2011 |
20110034444 | SELECTED CGRP ANTAGONISTS, PROCESSES FOR PREPARING THEM AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - The present invention relates to the CGRP antagonists of general formula I | 02-10-2011 |
20110039835 | SUBSTITUTED ARYLAMIDE DIAZEPINOPYRIMIDONE DERIVATIVES - The disclosure relates to a series pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: | 02-17-2011 |
20110046118 | NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 1,4-diaza-bicyclo [3.2.2]nonyl pyrimidine derivatives of formula (I) and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 02-24-2011 |
20110059954 | CGRP ANTAGONISTS - The present invention relates to new CGRP-antagonists of general formula I | 03-10-2011 |
20110059955 | NOVEL 3-AMINOALKYL-1,3-DIHYDRO-2H-INDOL-2-ONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The present invention relates to novel 3-aminoalkyl-1,3-dihydro-2H-indol-2-one derivatives, to their preparation and to their therapeutic application. | 03-10-2011 |
20110059956 | THERAPEUTIC AGENT FOR PAIN - To provide a cancer pain therapeutic and/or prophylactic agent which can be administered to a patient for a long period of time from the early stage to the final stage of the cancer pain therapy, instead of conventional non-opioid analgesic agents or opioid analgesic agents. | 03-10-2011 |
20110077239 | GLYCINE RECEPTOR AGONISTS FOR THE TREATMENT OF PHANTOM PHENOMENA - A medicament for the treatment of the phantom phenomena of acute tinnitus and/or phantom pain, a method for the production of such a medicament, and a method for the treatment of such phantom phenomena | 03-31-2011 |
20110105476 | SUBSTITUTED 7,8-DIHYDRO-1HPYRIMIDO[4,5-B]DIAZEPIN-4-AMINES ARE NOVEL KINASE INHIBITORS - Compounds having the Formula (I) | 05-05-2011 |
20110105477 | COMPOSITIONS AND METHODS RELATING TO HIV PROTEASE INHIBITION - The present invention relates to HIV protease, and methods for inhibiting the function of HIV protease. In particular, present invention provides compounds that inhibit or block the biological activity of HIVp, thereby causing the replication of the HIV virus to be inhibited or to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS. The compounds and formulations also find use in diagnostic and research settings. | 05-05-2011 |
20110105478 | NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL OXADIAZOLYL DERIVATIVES USEFUL AS MODULATOR OF NICOTINIC ACETYLCHOLINE RECEPTORS - This invention relates to novel N-oxides of a 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivative and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 05-05-2011 |
20110112078 | NOVEL OXADIAZOLYL-DIAZABICYCLONONANE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholin receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 05-12-2011 |
20110118238 | 2-ANILINOPURIN-8-ONES AS INHIBITORS OF TTK/MPS1 FOR THE TREATMENT OF PROLIFERATIVE DISORDERS - This invention relates to chemical compounds of the formula (I), or a pharmaceutically acceptable salt thereof, which possess inhibitory activity against the spindle checkpoint kinase: Tyrosine Threonine Kinase (TTK)/monopolar spindle 1 (Mps1) and are accordingly useful for their anti-cancer effect in a warm-blooded animal such as man. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them, and to their use in the manufacture of a medicament for the treatment of conditions mediated by TTK/Mps1, for use either alone or in combination with other anti-pro liferative agents. | 05-19-2011 |
20110118239 | PREPARATION AND ENANTIOMERIC SEPARATION OF 7-(3-PYRIDINYL)-1,7-DIAZASPIRO[4.4]NONANE AND NOVEL SALT FORMS OF THE RACEMATE AND ENANTIOMERS - A novel scalable synthesis for the preparation of 7-(3-pyridinyI)-1,7-diazaspiro[4.4)nonane has been developed, and 7-(3-pyridinyl)-1,7-diazaspiro[4.4]nonane salts have been formed with succinic acid and oxalic acid. Additionally, 7-(3-pyridinyl)-1,7-diaza-spiro[4.4]nonane has been separated into its stereoisomers via resolution with L and D di-p-toluoyltartaric acids, giving (R)- and (S)-7-(3-pyridinyl)-1,7-diazaspiro[4.4]nonane of high enantiomeric purity. Numerous solid salts of the resulting (R)- and (S)-7-(3-pyridinyl)-1,7-diazaspiro[4.4}nonane have been prepared. Methods for the preparation of the racemic and enantiomeric salts, pharmaceutical compositions comprising such salts, and uses thereof are disclosed. The salts can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders. | 05-19-2011 |
20110130389 | FUMARATE SALT OF 4-BROMOPHENYL 1,4-DIAZABICYCLO[3.2.2]NONANE-4-CARBOXYLATE, CRYSTALLINE FORMS THEREOF, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - Fumarate salt of 4-bromophenyl 1,4-diazabicyclo[3.2.2]nonane-4-carboxylate, crystalline forms thereof, methods of preparation thereof, and therapeutic use thereof. | 06-02-2011 |
20110130390 | Use of COX-2 Inhibitors for the Treatment of Schizophrenia, Delusional Disorders, Affective Disorders, Autism or Tic Disorders - The invention concerns the use of a COX-2 inhibitor for the treatment of psychiatric disorders such as schizophrenia, delusional disorders, affective disorders, autism or tic disorders, in particular chronic schizophrenic psychoses and schizoaffective psychoses, temporary acute psychotic disorders, depressive episodes, recurring depressive episodes, manic episodes and bipolar affective disorders. Moreover, the invention is concerned with the use of a COX-2 inhibitor, in particular celecoxib, in combination with a neuroleptic drug, in particular risperidone, or an antidepressant, for the treatment of psychiatric disorders such as schizophrenia, delusional disorders, affective disorders, autism or tic disorders. | 06-02-2011 |
20110136791 | COMBINATION OF A NICOTINIC RECEPTOR PARTIAL AGONIST AND OF AN ACETYLCHOLINESTERASE INHIBITOR, PHARMACEUTICAL COMPOSITION CONTAINING SAME AND USE THEREOF IN THE TREATMENT OF COGNITIVE DISORDERS - The combination of an alpha-7 nicotinic receptor agonist and of an acetylcholinesterase inhibitor, pharmaceutical composition comprising the combination and the use thereof in the treatment of cognitive disorders. | 06-09-2011 |
20110152252 | SHIGA TOXIN B-SUBUNIT/CHEMOTHERAPEUTICS CONJUGATES - The present invention relates to the use of a Shiga toxin B-subunit moiety as carrier for therapeutic agents, for example, anti-cancer agents such as anti-cancer agents that require intracellular uptake to exert their anti-cancer effects. In particular, the present invention provides conjugates comprising a Shiga toxin moiety covalently linked to an anti-cancer agent through a self-immolative spacer, and methods of using such conjugates to increase cellular uptake and/or specificity for cancer cells of the anti-cancer drug. Also provided are methods of treatment involving administration of such conjugates, and pharmaceutical compositions and kits useful for carrying out such methods of treatment. | 06-23-2011 |
20110172211 | Transnasal Anticonvulsive Pharmaceutical Composition Comprising Poorly Soluble Anticonvulsant - There is provided a transnasal anticonvulsive pharmaceutical composition including a poorly soluble anti-convulsant. The anticonvulsive pharmaceutical composition comprising a poorly soluble anticonvulsant as an active component, which is transnasally spray-administered, comprises diethylene glycol monoethyl ether and fatty acid ester, wherein the fatty acid ester is selected from the group consisting of caprylocaproyl polyoxylglyceride, isopropyl palmitate, oleoyl polyoxylglyceride, sorbitan monolaurate 20, methyl laurate, ethyl laurate, and polysorbate 20. Also, the anticonvulsive pharmaceutical composition comprising a poorly soluble anticonvulsant as an active component, which is transnasally spray-administered, comprises diethylene glycol monoethyl ether, fatty acid ester, methylpyrrolidone, water and alcohol. Therefore, the transnasal anticonvulsive pharmaceutical composition may be useful to highly enhance the bioavailability of the poorly soluble anticonvulsant. Also, the transnasal anticonvulsive pharmaceutical composition may be useful to allow the poorly soluble anticonvulsant to show the improved viscosity and/or enhanced solubility in order to effectively deliver the poorly soluble anticonvulsant at a therapeutic dose. | 07-14-2011 |
20110172212 | AMINE-BASED COMPOUND AND USE THEREOF - Novel amine compounds which are represented by the following formula (1) and efficacious against diseases such as a viral infectious disease with HIV, rheumatism, and cancer metastasis; | 07-14-2011 |
20110178069 | INHIBITORS OF INTERLEUKIN-1 BETA CONVERTING ENZYME - The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-γ-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-γ-mediated diseases and decreasing IGIF and IFN-γ production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds. | 07-21-2011 |
20110178070 | PI3K/mTOR INHIBITORS - The invention relates to PI3K/mTOR inhibiting compounds consisting of the formula: | 07-21-2011 |
20110190276 | Pyridine Derivatives And Their Use In The Treatment Of Psychotic Disorders - A method of treatment of anxiety disorders which comprises administering to a host in need thereof an effective amount of a compound of formula (I): | 08-04-2011 |
20110195959 | Compositions And Methods Relating To Novel Compounds And Targets Thereof - The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine compounds, and structurally and functionally related compounds, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, vascular abnormalities, and the like. | 08-11-2011 |
20110201601 | INHIBITORS OF THE SHIGA TOXINS TRAFFICKING THROUGH THE RETROGRADE PATHWAY - The present invention relates to the use of compounds of general formula (I) and (II) for the preparation of a drug for preventing and/or treating disorders caused by Shiga toxins and related toxins. | 08-18-2011 |
20110207722 | TREATMENT OF ANXIETY DISORDERS - This invention relates to the treatment of anxiety disorders. The invention furthermore relates to novel pharmaceutical compositions comprising a therapeutically effective amount of the compound exo-7-(8-H-8-aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one, or a therapeutically effective amount of the compound exo- 7-(8-H-8- aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one and a benzodiazepine drug. | 08-25-2011 |
20110230472 | RING-FUSED AZOLE DERIVATIVE HAVING PI3K-INHIBITING ACTIVITY - It is an object of the present invention to provide a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a ring-fused azole compound shown in the present specification, or a pharmaceutically acceptable salt thereof. | 09-22-2011 |
20110230473 | Methods and Compositions for Treating Status Epilepticus and Seizures Causing Status Epilepticus - Disclosed herein are methods, kits and compositions for treating, preventing, inhibiting, or reducing a seizure, status epilepticus, neuropathogenesis or a neuropathology caused by overstimulation of the NMDA receptor pathway and/or exposure to an OP compound. | 09-22-2011 |
20110245238 | Novel Soluble 1,4 Benzodiazepine Compounds and Stable Salts Thereof - The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and related compounds and methods of using benzodiazepine derivatives and related compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like. | 10-06-2011 |
20110251184 | SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I): | 10-13-2011 |
20110257161 | NOVEL DIAZA-BICYCLONONYL-PHENYL DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel diazabicyclononyl-phenyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 10-20-2011 |
20110257162 | HIV INTEGRASE INHIBITORS - Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: | 10-20-2011 |
20110263575 | Compounds Useful as Protein Kinase Inhibitors - The present invention relates to compounds useful as inhibitors of protein kinase. 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. | 10-27-2011 |
20110263576 | PHARMACEUTICAL COMPOSITION CONTAINING BENZODIAZEPINE AND/OR BENZODIAZEPINE DERIVATIVES - The invention relates to a pharmaceutical composition characterized in that it comprises a benzodiazapine and/or benzodiazapine derivative, and a non-ionic solubilizer, and induces in said combination an analogous effect to an opiate, described as a Straub phenomenon. | 10-27-2011 |
20110263577 | NOVEL OXADIAZOLYL-DIAZABICYCLONONANE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 10-27-2011 |
20110269748 | 2-ANILINE-4-ARYL SUBSTITUTED THIAZOLE DERIVATIVES - This invention concerns the use of a compound of formula (I) | 11-03-2011 |
20110288078 | PYRAZINOPYRAZINES AND DERIVATIVES AS KINASE INHIBITORS - This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use. | 11-24-2011 |
20110288079 | Tannate Compositions, Methods of Making and Methods of Use - Tannate compositions containing active pharmaceutical ingredients to be used for treating nausea, vomiting, pain, convulsions, and insomnia and manufacturing processes for preparing the tannate compositions. | 11-24-2011 |
20110294793 | HYDROXYPHENYL SULFONAMIDES AS ANTIAPOPTOTIC BCL INHIBITORS - The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compounds and methods of treating diseases using the compounds. | 12-01-2011 |
20110294794 | TREATMENT OF PROTEINOPATHIES USING A FARNESYL TRANSFERASE INHIBITOR - Methods and pharmaceutical compositions comprising a low dose of a farnesyl transferase inhibitor useful in the treatment of proteinopathies are provided. These low doses are below the doses used in oncological treatments for which these compounds were initially designed. The treatment includes administering to a subject in need thereof a therapeutically effective amount of a farnesyl transferase inhibitor, wherein the amount is effective to inhibit the farnesylation of a non-Ras FTase substrate involved in the autophagy pathway without substantially affecting the farnesylation of Ras or other oncology related substrates. Treatments in accordance with the present invention may also include an acetylcholinesterase inhibitor, an activator of neurotrophic receptors, an NMDA anatagonist, an amyloid deposit inhibitor, an antipsychotic agent, an antidepressant, an anxiolytic, or an antioxidant. | 12-01-2011 |
20110306604 | 3- AND 6-QUINOLINES WITH N-ATTACHED HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS - Compounds of Formula (I): (where variables R | 12-15-2011 |
20110306605 | COUMARIN-BASED COMPOUNDS FOR THE TREATMENT OF ALZHEIMER'S DISEASE AND CANCER - Compounds including those of the Formula I | 12-15-2011 |
20110319396 | BENZODIAZEPIN-2-ON DERIVATIVES - The present invention relates to a compound represented by the formula (I): wherein R | 12-29-2011 |
20110319397 | NOVEL N-OXIDES OF FURANYL-OXADIAZOLYL-DIAZABICYCLONONANE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel N-oxides of certain furanyl-oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. | 12-29-2011 |
20120004214 | N-OXIDES OF 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINYL DERIVATIVES USEFUL AS NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. Formula (I) a stereoisomer or a mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein Ar represents an indolyl group, which indolyl may optionally be substituted one or more times with substituents selected from halo, trifluoromethyl, trifluoromethoxy, cyano, nitro, amino, alkyl, hydroxy and alkoxy. | 01-05-2012 |
20120004215 | N-OXIDES OF DIAZABICYCLONONYL PYRIMIDINE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel N-oxides of certain diazabicyclononyl pyrimidine derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 01-05-2012 |
20120010197 | PROTEIN KINASE INHIBITORS - In one aspect, the invention provides compounds of Formula I | 01-12-2012 |
20120010198 | Methods for Treating Sleep Disorders by Cholecystokinin (CCK) Receptor B Antagonists - The present invention relates to a method for preventing or ameliorating a sleep-related breathing disorder. The method involves the use of one or a combination of cholecystokinin (CCK) receptor antagonists. | 01-12-2012 |
20120010199 | NOVEL PYRROLINONE DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - The present invention provides a compound represented by the formula (I): | 01-12-2012 |
20120015938 | 1,4-BENZODIAZEPIN-2-ON DERIVATIVES - The present invention relates to a compound represented by a formula (I): wherein R | 01-19-2012 |
20120028965 | COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. 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. The invention also provides processes for preparing compounds of the inventions. | 02-02-2012 |
20120028966 | PROTEIN KINASE INHIBITORS - In one aspect, the invention provides compounds of Formula I | 02-02-2012 |
20120028967 | NOVEL DIAZA-BICYCLONONYL-PYRIMIDINYL DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidine derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 02-02-2012 |
20120028968 | NOVEL DIBENZOFURANYL-OXADIAZOLYL-DIAZABICYCLONONANE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel dibenzofuranyl-oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 02-02-2012 |
20120040970 | INTRANASAL DELIVERY SYSTEM FOR DANTROLENE - The present invention provides a method for rapidly and reliably delivering dantrolene, or derivatives thereof, alone or in combination with other compounds, to the systemic circulation by administration via the nasal route to produce rapid onset of beneficial effects in the treatment or prevention of malignant hyperthermia (MH), spasticity, and Ecstasy intoxication. The present invention further provides intranasal pharmaceutical compositions comprising dantrolene sodium or any pharmaceutically acceptable salts thereof in a variety of pharmaceutical dosage forms, with and without other compounds. | 02-16-2012 |
20120040971 | BENZODIAZEPINONE COMPOUNDS USEFUL IN THE TREATMENT OF SKIN CONDITIONS - The present invention provides a family of benzodiazepinone compounds and pharmaceutical compositions thereof. The present invention also provides methods of treating certain skin conditions, e.g., atopic dermatitis, rosacea, or psoriasis, by administering a benzodiazepinone and methods of reducing the proliferation of keratinocyte cells by exposing such cells to a benzodiazepinone. | 02-16-2012 |
20120058994 | NOVEL COMPOUNDS - The invention relates to the novel salts AB of the base A with a physiologically acceptable acid B which is selected from the group consisting of hydrochloric acid, hydrobromic acid, sulfuric acid, fumaric acid and silcylic acid and the polymorphic compounds, the corresponding solvates and hydrates thereof. | 03-08-2012 |
20120065194 | USE OF CYPROHEPTADINE TO TREAT ORGANOPHOSPHATE EXPOSURE - A method of treating exposure to an organophosphate compound by administering a cyproheptadine compound to a subject in need thereof. | 03-15-2012 |
20120071468 | METHODS OF TREATING MILD COGNITIVE IMPAIRMENT (MCI) AND RELATED DISORDERS - The invention provides compositions and methods for the treatment of mild cognitive impairment (MCI), and for inhibiting, reducing, delaying and/or preventing the progression of MCI to Alzheimer's disease. The methods entail administering an effective amount of one or more compounds selected from the group consisting of tropisetron, disulfuram, honokiol and nimetazepam. The methods also are useful for prophylactic and therapeutic treatment of amyloidogenic diseases, including Alzheimer's disease. | 03-22-2012 |
20120071469 | NOVEL 1,4-DIAZA-BICYCLO[3.2.1]OCTANE DERIVATIVES USEFUL AS NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS - This invention relates to novel 1,4-diaza-bicyclo[3.2.1]octane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 03-22-2012 |
20120077805 | UNSOLVATED BENZODIAZEPINE COMPOSITIONS AND METHODS - The present invention relates to systems and methods for generating new forms of benzodiazepine and benzodiazepine related compounds as well as new compounds and formulations generated by such methods. In particular, the present invention provides high throughput systems and methods for generating and identifying new crystalline benzodiazepine and benzodiazepine related polymorphs and new unsolvated, solvated, and other forms of the compounds that find use as improved drugs and drug formations. | 03-29-2012 |
20120088755 | Novel Compounds - The present invention relates to the new compounds of general formula I | 04-12-2012 |
20120088756 | Methods for Regulating Neurotransmitter Systems by Inducing Counteradaptations - The present invention relates to methods for regulating neurotransmitter systems by inducing a counteradaptation response. According to one embodiment of the invention, a method for regulating a neurotransmitter includes the step of repeatedly administering a ligand for a receptor in the neurotransmitter system, with a ratio of administration half-life to period between administrations of no greater than ½. The methods of the present invention may be used to address a whole host of undesirable mental and neurological conditions. | 04-12-2012 |
20120088757 | NOVEL 1,4-BENZODIAZEPINE-2,5-DIONES WITH THERAPEUTIC PROPERTIES - The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides novel 1,4-benzodiazepine-2,5-dione compounds, and methods of using novel 1,4-benzodiazepine-2,5-dione compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like. | 04-12-2012 |
20120088758 | FIVE-MEMBERED HETEROCYCLES USEFUL AS SERINE PROTEASE INHIBITORS - The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): | 04-12-2012 |
20120094982 | 1,4-BENZODIAZEPINONE COMPOUNDS AND THEIR USE IN TREATING CANCER - The invention provides a family of 1,4-benzodiazepinone compounds and methods for their use as therapeutic agents in treating cancer. Pharmaceutical compositions and methods of making the 1,4-benzodiazepinone compounds are provided. | 04-19-2012 |
20120101088 | Transmembrane Penetration Enhancer - A transmembrane penetration enhancer includes a thermotropic liquid crystal suitably prepared for use in a therapeutic system to improve delivery of at least one active ingredient across a biomembrane and/or skin. The thermotropic liquid crystal comprises at least one cholesteryl ester and is effective in a mesomorphic state at a temperature of the biomembrane and/or skin. A therapeutic system includes the prepared thermotropic liquid crystal for enahanced transmembrane penetration and at least one active ingredient for delivery by the thermotropic liquid crystal. A method for making and using the transmembrane penetration enhancer is presented. | 04-26-2012 |
20120108575 | HETEROCYCLIC-SUBSTITUTED PIPERIDINE COMPOUNDS AND THE USES THEREOF - The invention relates to Heterocyclic-Substituted Piperidine Compounds, compositions comprising an effective amount of a Heterocyclic-Substituted Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Heterocyclic-Substituted Piperidine Compound. | 05-03-2012 |
20120122853 | ANNELATED N-HETEROCYCLIC SULFONAMIDES WITH OXADIAZOLONE HEADGROUP, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS - Annelated N-heterocyclic sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals The invention relates to annelated N-heterocyclic sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system. | 05-17-2012 |
20120165319 | INHIBITORS OF INTERLEUKIN-1 BETA CONVERTING ENZYME - The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-γ-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-γ-mediated diseases and decreasing IGIF and IFN-γ production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds. | 06-28-2012 |
20120165320 | NOVEL AZABICYCLOHEXANES - The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. | 06-28-2012 |
20120172353 | 1,4-DIAZA-BICYCLO[3.2.2]NONYL OXADIAZOLYL COMPOUNDS AND THEIR MEDICAL USE - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. | 07-05-2012 |
20120172354 | Substituted N-Phenyl-1-(4-Pyridinyl)-1H-Pyrazol-3-Amines - The present invention relates to N-phenyl-1-(4-pyridinyl)-1H-pyrazol-3-amine derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to formula (I) | 07-05-2012 |
20120190670 | Transnasal Anticonvulsive Pharmaceutical Composition Comprising Poorly Soluble Anticonvulsant - There is provided a transnasal anticonvulsive pharmaceutical composition including a poorly soluble anti-convulsant. The anticonvulsive pharmaceutical composition comprising a poorly soluble anticonvulsant as an active component, which is transnasally spray-administered, comprises diethylene glycol monoethyl ether and fatty acid ester, wherein the fatty acid ester is selected from the group consisting of caprylocaproyl polyoxylglyceride, isopropyl palmitate, oleoyl polyoxylglyceride, sorbitan monolaurate 20, methyl laurate, ethyl laurate, and polysorbate 20. Also, the anticonvulsive pharmaceutical composition comprising a poorly soluble anticonvulsant as an active component, which is transnasally spray-administered, comprises diethylene glycol monoethyl ether, fatty acid ester, methylpyrrolidone, water and alcohol. Therefore, the transnasal anticonvulsive pharmaceutical composition may be useful to highly enhance the bioavailability of the poorly soluble anticonvulsant. Also, the transnasal anticonvulsive pharmaceutical composition may be useful to allow the poorly soluble anticonvulsant to show the improved viscosity and/or enhanced solubility in order to effectively deliver the poorly soluble anticonvulsant at a therapeutic dose. | 07-26-2012 |
20120190671 | Controlled-Release CNS Modulating Compositions and Methods for the Treatment of Otic Disorders - Disclosed herein are compositions and methods for the treatment of otic disorders with CNS modulating agent compositions and compositions administered locally to an individual afflicted with an otic disorder, through direct application of these compositions and compositions onto or via perfusion into the targeted auris structure(s). | 07-26-2012 |
20120196851 | WNT PATHWAY ANTAGONISTS - The present invention relates to known and novel compounds of formula (I) as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer. | 08-02-2012 |
20120202800 | DUAL SMALL MOLECULE INHIBITORS OF CANCER AND ANGIOGENESIS - The present invention provides analogs and derivatives of thalidomide which inhibit cancer and angiogenesis. The present invention further provides compounds which disrupt microtubule polymerization. The present further provides methods of treating cancers comprising mutant p53. | 08-09-2012 |
20120208801 | Aminodiazepines as Toll-Like Receptor Modulators - Provided are compositions and methods useful for modulation signaling through the Toll-like receptor TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency. | 08-16-2012 |
20120214801 | COMPOSITIONS AND METHODS RELATING TO NOVEL COMPOUNDS AND TARGETS THEREOF - The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and related compounds and methods of using benzodiazepine derivatives and related compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like. | 08-23-2012 |
20120225866 | NITROGEN-CONTAINING COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF ATRIAL FIBRILLATION - The present invention provides a novel diazepine compound that blocks the I | 09-06-2012 |
20120232067 | BENZODIAZEPINONE COMPOUNDS AND METHODS OF TREATMENT USING SAME - The invention provides 1,4-benzodiazepinone compounds, pharmaceutical compositions, and methods of treating autoimmune disorders, chronic inflammatory disorders, and hyperproliferative disorders. For example, the 1,4-benzodiazepinone compounds and pharmaceutical compositions are contemplated to be useful for treating rheumatoid arthritis, graft-versus-host disease, inflammatory bowel disease, and the like. | 09-13-2012 |
20120238553 | NOVEL BENZODIOXOLYL-OXADIAZOLYL-DIAZABICYCLONONANE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel benzodioxolyl-oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances (I). | 09-20-2012 |
20120245151 | BISFLUOROALKYL-1,4-BENZODIAZEPINONE COMPOUNDS - Disclosed are compounds of Formula (I) or prodrugs thereof; | 09-27-2012 |
20120252793 | INTRANASAL BENZODIAZEPINE PHARMACEUTICAL COMPOSITIONS - The present invention generally relates to intranasal pharmaceutical compositions comprising a benzodiazepine and methods of use thereof that can provide a therapeutic effect without a decrease in blood pressure and/or pulse after administration of the pharmaceutical composition. | 10-04-2012 |
20120264746 | CELL MIGRATION MODULATING COMPOUNDS - The described invention relates to compounds (I) which modulate cell migration, and find use in, for example, wound healing, cancer progression and angiogenesis. All definitions as in claim | 10-18-2012 |
20120270860 | METHODS FOR TREATING OR PREVENTING ALCOHOL-RELATED DISORDERS OR CRAVING-RELATED DISORDERS - The invention provides methods for treating or preventing alcohol-related disorders or craving-related disorders comprising administering an effective amount of N-acetylcysteine or a pharmaceutically acceptable salt thereof to a patient to treat or prevent the alcohol or craving disorders. Methods for enhancing drug delivery and improving treatment outcomes are also described. | 10-25-2012 |
20120270861 | Primary Amines And Derivatives Thereof As Modulators Of The 5-HT2A Serotonin Receptor Useful For The Treatment Of Disorders Related Thereto - The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT | 10-25-2012 |
20120270862 | 1,4-BENZODIAZEPINE-2,5-DIONES AND RELATED COMPOUNDS WITH THERAPEUTIC PROPERTIES - The present invention provides novel chemical compounds characterized as Rho kinase (ROCK) inhibitors, methods for their discovery, and their therapeutic, research, and diagnostic use. In particular, the present invention provides 1,4-benzo-diazepine-2,5-dione compounds and related compounds having ROCK inhibitory activity, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with ROCK activity. | 10-25-2012 |
20120289498 | Compositions And Methods Relating To Novel Compounds And Targets Thereof - The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine compounds, and structurally and functionally related compounds, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, vascular abnormalities, and the like. | 11-15-2012 |
20120309747 | PROTEIN KINASE INHIBITORS - In one aspect, the invention provides compounds of Formula I | 12-06-2012 |
20120322794 | TREATMENT TOOL AND METHOD OF GRADUAL WITHDRAWAL FROM BENZODIAZEPINE DEPENDENCY - A treatment tool and method is disclosed for gradual withdrawal from benzodiazepine dependency while reducing or even minimizing withdrawal symptom intensity. An example method includes reducing emotional stress to maintain current neurotransmitter levels, stabilizing a condition with a pre-taper plan, establishing a maximum daily dosage reduction amount of benzodiazepine, based on historical data to prevent symptom escalation, reducing a current dosage of the benzodiazepine by the maximum daily dosage amount on a daily basis for up to about two weeks, and repeating establishing the maximum daily dosage reduction amount and reducing the current dosage until the daily dosage of benzodiazepine reaches zero. | 12-20-2012 |
20120329785 | Novel kinase inhibitors - The present invention relates to novel compounds of formula (I) | 12-27-2012 |
20130023525 | GYRASE INHIBITORS AND USES THEREOF - The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals. | 01-24-2013 |
20130029975 | CGRP ANTAGONISTS - The present invention relates to new CGRP-antagonists of general formula I | 01-31-2013 |
20130040941 | BENZODIAZEPINE COMPOUND AND PHARMACEUTICAL COMPOSITION - The present invention provides a novel benzodiazepine compound that blocks the I | 02-14-2013 |
20130045966 | Method of Lowering Serum Uric Acid Levels With (S)-Tofisopam - Enantiomerically-pure (S)-tofisopam is administered to lower serum uric acid levels in a mammal. | 02-21-2013 |
20130065886 | ADMINISTRATION OF BENZODIAZEPINE COMPOSITIONS - The invention relates to pharmaceutical compositions comprising one or more benzodiazepine drugs for nasal administration, methods for producing and for using such compositions. | 03-14-2013 |
20130079336 | Treatment of Prolonged Status Epilepticus - Methods for terminating, preventing, and/or treating status epilepticus are generally provided. The method can include administering a prophylactically or therapeutically effective amount of stiripentol or a related compound thereof to an individual in need of treatment of status epilepticus. The individual can be in need of treatment of prolonged status epilepticus, refractory status epilepticus, and/or benzodiazepine-resistant status epilepticus. | 03-28-2013 |
20130116243 | INHIBITORS OF AKT ACTIVITY - The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer. | 05-09-2013 |
20130116244 | PHARMACEUTICAL POWDER COMPOSITIONS - The present invention provides a powder composition for the buccal delivery comprising a drug compound, a muco-adhesive agent and a dispersing agent Suitable compounds drugs include benzodiazepine compounds. Suitable muco-adhesive agents include those selected from (t) esters and salts of alginic acid and (it) hydroxyethyl cellulose. Suitable dispersing agents include those selected from ethylene oxide-propylene oxide copolymers. | 05-09-2013 |
20130158017 | METHODS FOR TREATING OR PREVENTING CANCER AND NEURODEGENERATIVE DISEASES - Provided are methods of treating or preventing a neurodegenerative disease comprising administering to a subject having a neurodegenerative disease an effective amount of a compound of Formula I: | 06-20-2013 |
20130178465 | INTRANASAL DEXMEDETOMIDINE COMPOSITIONS AND METHODS OF USE THEREOF - The present invention provides intranasal formulations comprising dexmedetomidine, or a pharmaceutically acceptable salt thereof, and uses thereof. | 07-11-2013 |
20130190300 | COMPOSITIONS AND METHODS FOR INHIBITING THE PROLIFERATION OF CELLS - The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, and hyperproliferation, and the like. | 07-25-2013 |
20130196980 | DIAGNOSTIC AGENT, DIAGNOSTIC METHOD AND THERAPEUTIC AGENT FOR FIBROMYALGIA - A diagnostic agent and a diagnostic method for appropriately diagnosing fibromyalgia of a specific type, and a therapeutic agent for the aforesaid type include a diagnostic agent for fibromyalgia relating to an anti-voltage-gated potassium channel complex antibody (anti-VGKC complex antibody), said diagnostic agent containing a reagent for detecting the anti-VGKC complex antibody; a diagnostic method using the diagnostic agent; and a therapeutic agent for fibromyalgia relating to the anti-VGKC complex antibody. A diagnostic agent for fibromyalgia relating to an antibody against a voltage-gated potassium channel complex includes a reagent for detecting the antibody against the voltage-gated potassium channel complex; and a therapeutic agent for fibromyalgia relating to an antibody against voltage-gated potassium channel contains an effective amount of an anticonvulsant drug (gabapentine or clonazepam) as the active ingredient. | 08-01-2013 |
20130261110 | NOVEL 1,4-BENZODIAZEPINE-2,5-DIONES WITH THERAPEUTIC PROPERTIES - The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides novel 1,4-benzodiazepine-2,5-dione compounds, and methods of using novel 1,4-benzodiazepine-2,5-dione compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like. | 10-03-2013 |
20130281442 | Compounds for Treatment of Bovine Mastitis - Described herein are methods of treating mastitis in female mammals, e.g., cows, wherein the methods may include administering to mammals in need thereof compounds disclosed herein. | 10-24-2013 |
20130289021 | PHARMACEUTICAL 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. | 10-31-2013 |
20130289022 | TETRAMERIC ALPHA-SYNUCLEIN AND USE THEREOF - Disclosed herein are methods and related compositions for identifying compounds that stabilize natively folded tetrameric α-synuclein. These methods and compositions are useful for the treatment and diagnosis of α-synuclein-associated diseases and disorders. | 10-31-2013 |
20130303523 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF ADDICTION, PSYCHIATRIC DISORDERS, AND NEURODEGENERATIVE DISEASE - The present invention features, inter alia, pharmaceutically acceptable compositions that include metyrapol as the sole pharmaceutically active agent; compositions that include metyrapol and at least one additional pharmaceutically active agent; compositions in which the agent targeting the HPA axis is, itself, new or modified (e.g., a bi-specific antibody designed to traverse the blood-brain barrier or a known compound redesigned by, for example, conjugation to a substance that traverses the blood-brain barrier); and compositions in which the agent targeting the HPA axis is newly formulated in such a way that it fails to significantly inhibit cortisol production in the adrenal gland. For example, the composition can be formulated to include a dosage that is too low to reduce plasma cortisol levels or formulated to preferentially affect the skin. | 11-14-2013 |
20130324521 | IMPLANT FOR TREATING OR PREVENTING AN ANEURYSM - A medical product ( | 12-05-2013 |
20130345203 | SUBSTITUTED BICYCLIC ALKOXY PYRAZOLE ANALOGS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS - In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 12-26-2013 |
20130345204 | SUBSTITUTED BICYCLIC CYCLOALKYL PYRAZOLE LACTAM ANALOGS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS - In one aspect, the invention relates to substituted bicyclic cycloalkyl pyrazole lactam analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 12-26-2013 |
20130345205 | SUBSTITUTED BICYCLIC ARALKYL PYRAZOLE LACTAM ANALOGS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS - In one aspect, the invention relates to substituted bicyclic aralkyl pyrazole lactam analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 12-26-2013 |
20130345206 | SUBSTITUTED BICYCLIC ALKOXY PYRAZOLE ANALOGS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS - In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 12-26-2013 |
20140024641 | TREATMENT OF ORGANOPHOSPHATE EXPOSURE WITH TRIPTANS - A method of treating exposure to organophosphate agents and preventing morbidity due to such exposure through the administration of a triptan compound to a subject. | 01-23-2014 |
20140038947 | THERAPEUTIC APPLICATIONS OF PRO-APOPTOTIC BENZODIAZEPINES - Benzodiazepine compounds, and methods for using those compounds are provided. Some of the benzodiazepine compounds include 1,4-benzodiazepine-2-one and 1,4-benzodiazepine-2,5-dione compounds of structures: | 02-06-2014 |
20140051690 | Transnasal Anticonvulsive Pharmaceutical Composition Comprising Poorly Soluble Anticonvulsant - There is provided a transnasal anticonvulsive pharmaceutical composition including a poorly soluble anticonvulsant. The anticonvulsive pharmaceutical composition comprising a poorly soluble anticonvulsant as an active component, which is transnasally spray-administered, comprises diethylene glycol monoethyl ether and fatty acid ester, wherein the fatty acid ester is selected from the group consisting of caprylocaproyl polyoxylglyceride, isopropyl palmitate, oleoyl polyoxylglyceride, sorbitan monolaurate 20, methyl laurate, ethyl laurate, and polysorbate 20. Also, the anticonvulsive pharmaceutical composition comprising a poorly soluble anticonvulsant as an active component, which is transnasally spray-administered, comprises diethylene glycol monoethyl ether, fatty acid ester, methylpyrrolidone, water and alcohol. Therefore, the transnasal anticonvulsive pharmaceutical composition may be useful to highly enhance the bioavailability of the poorly soluble anticonvulsant. Also, the transnasal anticonvulsive pharmaceutical composition may be useful to allow the poorly soluble anticonvulsant to show the improved viscosity and/or enhanced solubility in order to effectively deliver the poorly soluble anticonvulsant at a therapeutic dose. | 02-20-2014 |
20140057903 | METHODS FOR CHARACTERIZING AND TREATING COGNITIVE IMPAIRMENT IN AGING AND DISEASE - This invention provides methods for identifying genes associated with cognitive impairment and for identifying compounds useful in the treatment of cognitive impairment. The methods can in particular be used to identify genes associated with, and compounds useful in treating, cognitive impairment in aging. | 02-27-2014 |
20140066436 | PYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS - The present invention relates to a compound of formula (VII)I, or pharmaceutically acceptable salt or ester thereof, wherein: X is NR | 03-06-2014 |
20140088090 | 6,7-DIHYDRO-[1,3,4]THIADIAZOLO-[3,2-a][1,3]DIAZEPIN DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS HYPNOTIC OR ANESTHETIC AGENT AND METHOD FOR THEIR PREPARATION - The present invention relates to a compound of formula 1, a pharmaceutical composition containing the compound, a method for its preparation as well as the use of the compound as hypnotic agent or anesthetic agent. | 03-27-2014 |
20140088091 | 6,7-DIHYDRO-[1,3,4]THIADIAZOLO-[3,2-a][1,3]DIAZEPIN DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME AS NEUROMUSCULAR BLOCKER OR SKELETAL MUSCLE RELAXANT, AND METHOD FOR THE PREPARATION - The present invention relates to a compound of formula 1, a pharmaceutical composition containing the compound, a method for its preparation as well as the use of the compound as neuromuscular blocker or skeletal muscle relaxant. | 03-27-2014 |
20140128379 | NASAL FORMULATIONS OF BENZODIAZEPINE - The present invention provides pharmaceutical compositions for intranasal delivery of a benzodiazepine. The composition may contain a therapeutically effective amount of a benzodiazepine or a pharmaceutically acceptable salt thereof, and a permeation enhancer. The permeation enhancer may be propylene glycol or a Hsieh permeation enhancer. The present compositions have excellent bioavailability. After administration of the present compositions, therapeutically effective plasma levels of the benzodiazepine may be achieved rapidly. The present pharmaceutical composition may be used to treat a patient suffering from anxiety, epilepsy, insomnia, agitation, seizures, muscular disorders, alcohol dependence, and drug withdrawal. | 05-08-2014 |
20140128380 | METHODS OF MODULATING THE ACTIVITY OF THE MC1 RECEPTOR AND TREATMENT OF CONDITIONS RELATED TO THIS RECEPTOR - The present invention provides compounds of Formula (I) that are useful for binding and/or modulating the biological activity of the melanocortin-1 receptor (MC1R). Compounds of this invention can be used to treat diseases and/or conditions in which modulation of MC1R is beneficial. Such diseases and/or conditions include, but are not limited to, hyperpigmentation (including melasma), hypopigmentation (including vitiligo), melanoma, basal cell carcinoma, squamous cell carcinoma, erythropoietic protoporphyria, polymorphous light eruption, solar urticaria, photosensitivity, sunburn, inflammatory diseases, aberrant fibroblast activity and pain. | 05-08-2014 |
20140128381 | Intranasal Benzodiazepine Pharmaceutical Compositions - The present invention generally relates to intranasal pharmaceutical compositions comprising a benzodiazepine and methods of use thereof that can provide a therapeutic effect without a decrease in blood pressure and/or pulse after administration of the pharmaceutical composition. | 05-08-2014 |
20140135317 | FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS - The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: | 05-15-2014 |
20140135318 | SUBSTITUTED SULFONAMIDES USEFUL AS ANTIAPOPTOTIC BCL INHIBITORS - Disclosed are compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein: W and Q and G are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bcl-2 family antiapoptotic proteins for the treatment of cancer; and pharmaceutical compositions comprising such compounds. | 05-15-2014 |
20140148445 | Methods of Detecting Amyotrophic Lateral Sclerosis (ALS) - In one aspect, the invention is directed to a method of identifying an individual that has amyotrophic lateral sclerosis (ALS) or is at risk of developing ALS comprising detecting one or more alterations in a profilin 1 (PFN1) sequence of an individual in need thereof compared to a wild type profilin sequence. In another aspect, the invention is directed to a method of identifying an individual that has amyotrophic lateral sclerosis (ALS) or is at risk of developing ALS comprising selectively sequencing a profilin 1 (PFN1) sequence of an individual in need thereof; and detecting one or more alterations in the PFN1 sequence of the individual. If the one or more alterations are detected then the individual has ALS. | 05-29-2014 |
20140155389 | BICYCLIC INHIBITORS OF ALK - The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, wherein R | 06-05-2014 |
20140171423 | AGENTS FOR TREATING PAIN AND USES THEREOF - This invention relates to: (a) compounds and salts thereof that, inter alia, treat pain; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions. | 06-19-2014 |
20140221357 | PYRROLINONE CARBOXAMIDE COMPOUNDS USEFUL AS ENDOTHELIAL LIPASE INHIBITORS - The present invention provides compounds of Formula (I) or Formula (III): [INSERT CHEMICAL STRUCTURE HERE] (I) [INSERT CHEMICAL STRUCTURE HERE] (III) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments. | 08-07-2014 |
20140235622 | PRIMARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT | 08-21-2014 |
20140249140 | Nerve Agent Antidotes - The present invention includes compositions that are useful in treating, ameliorating, or preventing nerve agent poisoning. The present invention also includes methods of preventing, treating or ameliorating nerve agent poisoning in a subject in need thereof, the method comprising administering to the subject an effective amount of a composition of the invention. The present invention also includes methods of preventing, treating or ameliorating a seizure induced by a disease or disorder in a subject in need thereof, the method comprising administering to the subject an effective amount of a composition of the invention. The present invention also comprises a kit comprising compositions of the invention. | 09-04-2014 |
20140249141 | 1,4-DIAZABICYCLO[3.2.2]NONANES AS NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including inflammatory diseases and diseases associated with dysfunction of the central nervous system (CNS). | 09-04-2014 |
20140288059 | THERAPEUTIC COMPOSITIONS AND METHODS - PAD4 inhibitory compositions and methods for their use in treatment of cancer and autoimmune disease are provided according to embodiments of the present invention. | 09-25-2014 |
20140296220 | PYRIDAZINO[4,5-D]PYRIMIDIN-5(6H)-ONE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 10-02-2014 |
20140309217 | Controlled-Release CNS Modulating Compositions and Methods for the Treatment of Otic Disorders - Disclosed herein are compositions and methods for the treatment of otic disorders with CNS modulating agent compositions and compositions administered locally to an individual afflicted with an otic disorder, through direct application of these compositions and compositions onto or via perfusion into the targeted auris structure(s). | 10-16-2014 |
20140323473 | COMPOUNDS AND METHODS TO TREAT ORGANOPHOSPHORUS POISONING - Organophosphate (OP) nerve agents and pesticides are potent inhibitors of acetylcholinesterase (AChE). Though oxime nucleophiles can reactivate an AChE-phosphyl adduct, the adduct can undergo a reaction called aging, leading to an aged-AChE adduct. The invention provides compounds and methods that can be used to reactivate an aged-AChE adduct. Such compounds and methods are useful to counteract organophosphorus poisoning. | 10-30-2014 |
20140329805 | DUAL SMALL MOLECULE INHIBITORS OF CANCER AND ANGIOGENESIS - The present invention provides analogs and derivatives of thalidomide which inhibit cancer and angiogenesis. The present invention further provides compounds which disrupt microtubule polymerization. The present further provides methods of treating cancers comprising mutant p53. | 11-06-2014 |
20140364423 | Pyrazinopyrazines and Derivatives as Kinase Inhibitors - This invention relates to compounds of the general formula: | 12-11-2014 |
20150011537 | Benzodiazepine compounds with anti-flavivirus activity - The present invention describes a unique antiviral screen system. The assay is based on quantitatively monitoring viral activation of host cell beta-interferon (IFN-β) gene expression in a HEK293-derived reporter cell line expressing a firefly luciferase gene under the control of a human IFN-β promoter. Unlike the traditional high throughput antiviral assays that measure either the reduction of viral components/yields or cytopathic effect, the readout of the reporter assay in the present invention is the virus-induced host cellular innate immune response. Hence, the assay allows for identification of compounds that inhibit virus infection. In addition, because induction of IFN is one of the most common attributes of viruses, the assay is applicable to all the viruses that are able to infect the reporter cell line and induce IFN-β expression. Compounds that interfere with viral mediated activation of the interferon pathway in a primary screen, can be further screened with virus-specific assay to confirm their antiviral activity. | 01-08-2015 |
20150018345 | NOVEL NEUROKININ 1 RECEPTOR ANTAGONIST COMPOUNDS - The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, C | 01-15-2015 |
20150025064 | NOVEL BENZODIAZEPINONES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR FUNCTIONS AND NEUROLOGICAL USES THEREOF - The present invention relates to novel benzodiazepinone compounds of Formulae (I) | 01-22-2015 |
20150038495 | THERAPEUTIC AGENT FOR PAIN - To provide a cancer pain therapeutic and/or prophylactic agent which can be administered to a patient for a long period of time from the early stage to the final stage of the cancer pain therapy, instead of conventional non-opioid analgesic agents or opioid analgesic agents. | 02-05-2015 |
20150065491 | ADMINISTRATION OF BENZODIAZEPINE COMPOSITIONS - The invention relates to pharmaceutical compositions comprising one or more benzodiazepine drugs for nasal administration, methods for producing and for using such compositions. | 03-05-2015 |
20150072974 | HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF - Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and neurological disorders, including, but not limited to, e.g., psychosis, schizophrenia, depression, movement disorders, and Parkinson's disease. | 03-12-2015 |
20150105378 | PYRROLINONE CARBOXAMIDE COMPOUNDS USEFUL AS ENDOTHELIAL LIPASE INHIBITORS - The present invention provides compounds of Formula (I) or Formula (III): | 04-16-2015 |
20150133437 | Tetrahydro[1,8]naphthyridine Sulfonamide and Related Compounds for Use as Agonists of RORy and the Treatment of Disease - The invention provides tetrahydro[1,8]naphthyridine and related compounds, methods of promoting RORy activity and/or increasing the amount of iL-17 in a subject, and therapeutic uses of the tetrahydro[1,8]naphthyridine and related compounds. In particular, the invention provides sulfonamide-tetrahydro[1,8]naphthyridine and related compounds, methods of using such compounds to promote RORy activity and/or increase the amount of iL-17 in a subject, and treat medical conditions in which activation of immune response would be beneficial such as in cancer and infections. | 05-14-2015 |
20150141410 | GPR17 Receptor Modulators - Chemical compounds are provided which act on GPR17 receptors and are useful in the treatment or amelioration of chronic and/or acute neurodegenerative diseases, such as multiple sclerosis, inflammatory diseases, pathologies involving the immune system, cardiovascular diseases, and renal diseases. | 05-21-2015 |
20150141411 | SUBSTITUTED 3,4-DIHYDRO-2H-PYRIDO[1,2-A]PYRAZINE-1,6-DIONE DERIVATIVES USEFUL FOR THE TREATMENT OF (INTER ALIA) ALZHEIMER'S DISEASE - The present invention is concerned with novel substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione derivatives of Formula (I) wherein R | 05-21-2015 |
20150148339 | GASTRIN ANTAGONISTS FOR TREATMENT AND PREVENTION OF OSTEOPOROSIS - The provided embodiments are based in some aspects on the demonstration herein of a role for gastrin in regulating the aging gut-ovary axis and effects of targeting gastrin activity in reversing gastrin-mediated bone loss. Provided are methods, compositions and agents, including gastrin antagonists, for treatment, amelioration, and prevention of bone diseases and conditions. Methods for treating a bone disease or condition associated with hypergastrinemia in a subject in need thereof may comprise administering to the subject at least one dose of a therapeutically effective amount of a gastrin receptor-targeting agent, thereby treating the bone disease or condition associated with hypergastrinemia. | 05-28-2015 |
20150313868 | USE OF CANNABINOIDS AND TERPENES FOR TREATMENT OF ORGANOPHOSPHATE AND CARBAMATE TOXICITY - Pharmaceutical compositions in which isolated cannabinoid receptor modulators are optionally combined with terpene blends in a pharmaceutically acceptable carrier. Methods for treating or preventing a disease, disorder, dysfunction or condition caused by exposure to an organophosphate or carbamate acetylcholineesterase inhibitor with the inventive compositions are also disclosed. | 11-05-2015 |
20150320742 | COMBINATIONS COMPRISING 3-PHENYLSULFONYL-8-PIPERAZINYL-1YL-QUINOLINE - The combination of 3-phenylsulfonyl-8-piperazinyl-1yl-quinoline or a pharmaceutically acceptable salt thereof with a second therapeutic agent, wherein the second therapeutic agent is selected from:
| 11-12-2015 |
20150320762 | TREATMENT OF PROLIFERATIVE DISEASES WITH PYRIMIDODIAZEPINONES - A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, for use in treating a proliferative disorder, wherein: X is NR | 11-12-2015 |
20150336904 | RUFINAMIDE AND DERIVATIVES AND THEIR USE IN MODULATING THE GATING PROCESS OF HUMAN VOLTAGE-GATED SODIUM CHANNELS - The present invention provides compounds of formula I which are capable of inhibition of the activation of hNav1.1 or hNav1.6 sodium channels in neurons. Pharmaceutical compositions comprising these compounds are also provided. Methods for prevention and treatment of neurological disorders, including, for example, seizures and seizure disorders, including Lennox-Gastaut Syndrome, Dravet syndrome, epileptic encephalopathies, autism, Familial hemiplegic migraine (FHM), anxiety disorders, including Post-traumatic stress disorder (PTSD), panic disorder and obsessive-compulsive disorder, neuropathic pain, and Rett syndrome by administration of these compounds are also provided. | 11-26-2015 |
20150344486 | PYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS - The present invention relates to pyrimidine derivatives capable of inhibiting one or more protein kinases. Further aspects relate to pharmaceutical compositions comprising the pyrimidine derivatives and the use thereof in the treatment of proliferative disorders. | 12-03-2015 |
20150368211 | RUFINAMIDE AND DERIVATIVES AND THEIR USE IN MODULATING THE GATING PROCESS OF HUMAN VOLTAGE-GATED SODIUM CHANNELS - The present invention provides compounds of formula I or a salt, solvate, or stereoisomer thereof, wherein X is H, or an electron withdrawing group such as a halogen, NH | 12-24-2015 |
20160000702 | PHARMACEUTICAL COMPOSITION FOR ENHANCED TRANSMUCOSAL ADMINSTRATION OF BENZODIAZEPINES - The current application relates to a liquid pharmaceutical composition for intiaoral transmucosal administration of a benzodiazepine drag to a mammal The composition comprises a physiologically acceptable hydrophobic phase, a eutectic mixture of benzodiazepine compound providing high solubility of the benzodiazepine in said hydrophobic phase, at least one physiologically acceptable organic solvent and at least one physiologically acceptable surfactant. | 01-07-2016 |
20160000803 | PHARMACEUTICAL COMPOSITION FOR TRANSMUCOSAL ADMINISTRATION OF BENZODIAZEPINES - The current application relates to a liquid pharmaceutical composition for intraoral transmucosal administration of a benzodiazepine drug to a mammal. The composition comprises a physiologically acceptable hydrophobic phase, an eutectic mixture of benzodiazepine compound providing high solubility of the benzodiazepine in said hydrophobic phase, at least one physiologically acceptable organic solvent and at least one physiologically acceptable surfactant. | 01-07-2016 |
20160015685 | FURO [3, 2-B] PYRR0L-3-0NES AS CATHESPIN S INHIBITORS - A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, | 01-21-2016 |
20160024055 | DIMERIC COMPOUNDS - Disclosed are compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein Z, X, Q and R | 01-28-2016 |
20160038509 | Compositions and Methods for the Treatment of Addiction, Psychiatric Disorders, and Neurodegenerative Disease - The present invention features, inter alia, pharmaceutically acceptable compositions that include metyrapol as the sole pharmaceutically active agent; compositions that include metyrapol and at least one additional pharmaceutically active agent; compositions in which the agent targeting the HPA axis is, itself, new or modified (e.g., a bi-specific antibody designed to traverse the blood-brain barrier or a known compound redesigned by, for example, conjugation to a substance that traverses the blood-brain barrier); and compositions in which the agent targeting the HPA axis is newly formulated in such a way that it fails to significantly inhibit cortisol production in the adrenal gland. For example, the composition can be formulated to include a dosage that is too low to reduce plasma cortisol levels or formulated to preferentially affect the skin. | 02-11-2016 |
20160083355 | COMPOUNDS WHICH HAVE A PROTECTIVE ACTIVITY WITH RESPECT TO THE ACTION OF TOXINS AND OF VIRUSES WITH AN INTRACELLULAR MODE OF ACTION - The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells. | 03-24-2016 |
20160095866 | 1,4-Benzodiazepone-2,5-Diones And Related Compounds With Therapeutic Properties - The present invention provides novel chemical compounds characterized as Rho kinase (ROCK) inhibitors, methods for their discovery, and their therapeutic, research, and diagnostic use. In particular, the present invention provides 1,4-benzodiazepine-2,5-dione compounds and related compounds having ROCK inhibitory activity, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with ROCK activity. | 04-07-2016 |
20160136114 | METHOD FOR THE TREATMENT OF DRAVET SYNDROME - A method of treating and/or preventing Dravet Syndrome in a patient such as a patient previously diagnosed with Dravet Syndrome, by administering an effective dose of fenfluramine or its pharmaceutically acceptable salt to that patient. Dravet Syndrome patients are typically children under the age of 18 and are treated at a preferred dose of less than about 0.5 to about 0.01 mg/kg/day. | 05-19-2016 |
20160151385 | STABLE FORMULATIONS FOR PARENTERAL INJECTION OF SMALL MOLECULE DRUGS | 06-02-2016 |
20160199296 | NASAL FORMULATIONS OF BENZODIAZEPINE | 07-14-2016 |
20170233386 | Compounds Which Have a Protective Activity with Respect to the Action of Toxins and of Viruses with an Intracellular Mode of Action | 08-17-2017 |
20220135575 | Substituted Fused Pyrrolo-Diazepinones and Uses Thereof - Disclosed are compounds, pharmaceutical compositions, and methods of treatment. The disclosed compounds are based on fused 1,4-diazepine and pyrrolidinedione scaffolds. The compounds may be utilized in pharmaceutical compositions and methods for treating diseases and disorders associated with cell proliferation such as cancer and may have a formula illustrated as follows: | 05-05-2022 |