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

Subclass of:

514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

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

514218000 - Hetero ring is seven-membered consisting of two nitrogens and five carbon atoms

514219000 - Polycyclo ring system having the seven-membered hetero ring as one of the cyclos

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DocumentTitleDate
20120202797SUBSTITUTED [(5H-PYRROLO[2,1-c][1,4]BENZODIAZEPIN-11-YL)PIPERAZIN-1-YL]-2,2-DIMETHYLP- ROPANOIC ACID COMPOUNDS AS DUAL ACTIVITY H1 INVERSE AGONISTS/5-HT2A ANTAGONISTS - A dual H1/5-HT08-09-2012
20120202796METHOD FOR COMBATING ADVERSE EFFECTS ARISING FROM ANTIPSYCHOTIC TREATMENT - This invention relates to a method for combating adverse effects arising from antipsychotic treatment. The invention furthermore relates to novel pharmaceutical compositions comprising a therapeutically effective combination of a compound of formula I and an antipsychotic drug.08-09-2012
20120184537[1,4]-BENZODIAZEPINES AS VASOPRESSIN V2 RECEPTOR ANTAGONISTS - The invention relates to a novel class of [1,4]-benzodiazepine derivatives, processes for their preparation, intermediates usable in these processes, and pharmaceutical compositions containing the compounds. Other aspects of the invention are directed to the use of said [1,4]-benzodiazepine derivatives in therapy based on the capability of said compounds to interfere with the binding of the peptide hormone, vasopressin, to its receptors. In particular as vasopressin V2 receptor antagonists and therefore useful for treating involving increased vascular resistance, cardiac insufficiency, and water retention.07-19-2012
20120184536COMPOSITIONS COMPRISING SPECIFIC UGT INHIBITORS AND METHODS OF USE THEREOF - The present invention encompasses compositions comprising UGT inhibitors. Additionally, the invention encompasses methods of reducing the glucuronidation of a compound using a UGT inhibitor.07-19-2012
20100152170Benzazole Derivatives, Compositions, And Methods Of Use As Aurora Kinase Inhibitors - The present invention relates to compounds and methods from the treatment of cancer. The invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising compounds that inhibit Aurora kinase, and methods for the treatment of cancer using the compounds of the presentation invention or pharmaceutical compositions comprising compounds of the present invention.06-17-2010
20130085136NOVEL ANTIFUNGAL 5,6-DIHYDRO-4-[(DIFLUOROETHYL)PHENYL]-4H-PYRROLO[1,2-a][1,4]BENZODIAZEPIN- E AND 4-(DIFLUOROETHYL)PHENYL-6H-PYRROLO[1,2-a][1,4]BENZODIAZEPINE DERIVATIVES - The present invention concerns novel compounds of Formula (I):04-04-2013
20130079335Benzotriazolodiazepine Compounds Inhibitors Of Bromodomains - Benzodiazepine compounds, pharmaceutical compositions containing such compounds and to their use in therapy.03-28-2013
20130079334Compositions for Delivery of Insoluble Agents - Compositions and methods of making the same for in vivo delivery of lixivaptan to a subject in need thereof are described. The composition includes a substantially water-insoluble pharmacologically active agent (e.g., lixivaptan) and a substantially water-insoluble matrix forming material (e.g., a Vitamin E semi-ester), wherein the pharmacologically active agent is dispersed in said matrix forming material, and wherein the composition delivers said substantially water-insoluble pharmacologically active agent upon exposure to physiological medium.03-28-2013
20130040940MERCAPTOAMIDINE DERIVATIVES AND METHODS OF USE - Compounds of formula (I)02-14-2013
20100075955SHORT-ACTING BENZODIAZEPINE SALTS AND THEIR POLYMORPHIC FORMS - The invention relates to esylate salts of the compound of formula (I):03-25-2010
20090186879TRICYCLIC COMPOUNDS AND USE THEREOF - There is provided a compound of the formula (I′):07-23-2009
20100324027DIAZAHOMOADAMANTANE DERIVATIVES AND METHODS OF USE THEREOF - The invention relates to compounds that are diazahomoadamantane derivatives, compositions comprising such compounds, and methods of using such compounds and compositions.12-23-2010
20100041643THIENOTRIAZOLODIAZEPINE COMPOUND AND MEDICINAL USE THEREOF - [Solving means] A thienotriazolodiazepine compound of the following formula (I)02-18-2010
20090156583Tricyclic Amide Derivatives - The present invention relates to compounds of formula I06-18-2009
20090149449PYRROLOBENZODIAZEPINE DERIVATIVES, COMPOSITIONS COMPRISING THE SAME AND METHODS RELATED THERETO - Disclosed are compounds of Formula I06-11-2009
20090124607Novel Bicyclic Sulfonamides for Use as Glucocorticoid Receptor Modulators in the Treatment of Inflammatory Diseases - Compounds of formula (I): or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).05-14-2009
20090124606Composition for Treatment of Psychosis - New pharmaceutical combination providing to decrease or eliminate the extrapyramidal side effects of antipsychotic active ingredients by combination of deramciclane with a classic antipsychotic agent (e.g. haloperidol, chloroprozamine or levoprozamin) or an atypical antipsychotic agent (e.g. risperidone, iloperidone or olanzapine).05-14-2009
20100081647SHORT-ACTING BENZODIAZEPINE SALTS AND THEIR POLYMORPHIC FORMS - The invention relates to besylate salts of the compound of formula (I):04-01-2010
20090318426USE OF FLUMAZENIL IN THE MANUFACTURE OF A MEDICAMENT FOR THE TREATMENT OF DEPRESSIVE DISORDERS - The invention relates to the use of flumazenil in the manufacture of a medicament for the treatment of depressive disorders, for example disorders including depressive symptoms, without psychotic alteration. The flumazenil can be administered sequentially in small quantities at short intervals until a quantity that is therapeutically effective for the treatment of the depressive disorder has been administered.12-24-2009
20090093466Carboxamide GABAa ALPHA2 Modulators - The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.04-09-2009
20130072477TREATMENT OF PARKINSON'S DISEASE AND ENHANCEMENT OF DOPAMINE SIGNAL USING PDE 10 INHIBITOR - The present invention relates to a therapeutic or prophylactic method for treating Parkinson's disease by administering an effective amount of a compound having a phosphodiesterase 10 inhibitory activity; and also relates to a pharmaceutical composition for treatment or prophylaxis of Parkinson's disease comprising as an active ingredient a compound having a phosphodiesterase 10 inhibitory activity. Moreover, the present invention relates to a method for enhancing dopamine signal in the brain, which comprises administering an effective amount of a compound having a phosphodiesterase 10 inhibitory activity; and also relates to pharmaceutical composition for enhancing dopamine signal in brain comprising as an active ingredient a compound having a phosphodiesterase 10 inhibitory activity.03-21-2013
20110015186METHODS AND COMPOSITIONS FOR PROTECTING AND TREATING NEUROINJURY - A method and composition for protecting and/or treating neuroinjury are disclosed. In one aspect, the present application discloses a method for protecting and/or treating a subject from organophosphate-induced neuronal injury. The method comprises administering to a subject an effective amount of 4R cembranoid, 4S cembranoid or a cembranoid analogue. In another aspect, the application discloses neuroprotective pharmaceutical compositions for protecting and/or treating a subject from organophosphate-induced neuronal injury. A kit for protecting and treating a subject from organophosphate-induced neurodamage is also disclosed.01-20-2011
20090270373TREATMENT OF DOWN SYNDROM WITH BENZODIAZEPINE RECEPTOR ANTAGONISTS - Pharmaceutical compositions and methods of treating Down Syndrome, mental retardation or both are provided. The pharmaceutical compositions comprise one or more benzodiazepine receptor antagonists, such as flumazenil.10-29-2009
20090069306PROCESS FOR PRODUCING HIGHLY PURE MIDAZOLAM AND SALTS THEREOF - Provided is a process for producing highly pure midazolam and salts thereof, and a pharmaceutical composition containing the highly pure midazolam and/or a salt thereof.03-12-2009
20090036431Cytotoxic Agents Comprising New Tomaymycin Derivatives - The present invention is related to new tomaymycin derivatives, their process of preparation and their therapeutic uses.02-05-2009
20120225865ARYLCYCLOHEXYLETHERS OF DIHYDROTETRAAZABENZOAZULENES - The present invention is concerned with arylcyclohexylethers of dihydro-tetraazabenzoazulenes, i.e. arylcyclohexylethers of 5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I09-06-2012
20130065885ORAL THERAPEUTIC COMPOUND DELIVERY SYSTEM - The present invention relates generally to therapeutic formulations. More particularly, this present invention provides an oral delivery system for a therapeutic compound that is a base, a salt of a base or an amphoteric compound or a salt of a amphoteric compound with pharmacological, physiological or biochemical activity or a proactive form thereof. The present invention even more particularly provides a swallow formulation comprising a therapeutic compound that is a base, a salt of a base, an amphoteric compound or a salt of an amphoteric compound which facilitates the rapid delivery of the therapeutic compound to the circulatory system.03-14-2013
20110021507INHIBITING ANTIPSYCHOTIC-INDUCED WEIGHT GAIN - The present invention provides methods, compositions and kits for preventing, inhibiting, reducing and reversing weight gain induced by antipsychotic medications, for example olanzapine and clozapine, by co-administration of an M01-27-2011
20090012064Compositions controlling pH range of release and/or release rate - The present invention provides a composition controlling a pH range of release and/or a release rate, which contains (i) a thienotriazolodiazepine compound of the formula (I)01-08-2009
20120238552PHARMACEUTICAL COMPOSITIONS COMPRISING SORBITAN ESTERS - The present invention relates to a pharmaceutical composition comprising sorbitan esters of carboxylic acids that are useful for the delivery of anti-psychotic drugs.09-20-2012
20080293699Inhibitors of thapsigargin-induced cell death - Methods for screening for inhibitors of endoplasmic reticulum (ER) stress are provided. These methods involve the addition of thapsigargin, which induces ER stress, and a test agent to mammalian cells in multi-well plates. Cell survival can be readily monitored by measuring intracellular ATP content using a bioluminescent reagent. Screening a commercially available library of 50,000 compounds led to the identification of 93 hit compounds that were subjected to secondary assays to confirm their ability to rescue cells from thapsigargin-induced cell death.11-27-2008
20110034442Use and Methods of Use for an Antagonist of the Serotin3 Receptor (5-HT3) and a Selective Modulator of Chloride Channels for the Treatment of Addiction to or Dependence on Medicines/Drugs or Nervous System Disorders - The present invention relates to the composition and methods of using a combination of a serotonin02-10-2011
20100210631SUBSTITUTED 2-[2-(PHENYL) ETHYLAMINO] ALKANEAMIDE DERIVATIVES AND THEIR USE AS SODIUM AND/OR CALCIUM CHANNEL MODULATORS - Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them are useful as sodium and/or calcium channel modulators for preventing, alleviating and curing pathologies wherein the above mechanisms play a pathological role. The compounds may be particularly used for the prevention, alleviation, and curing of, for example, neurological, cognitive, psychiatric, inflammatory, urogenital, and gastrointestinal diseases.08-19-2010
20110281853COMPOSITIONS AND METHODS FOR TREATING OR PREVENTING ATRIAL FIBRILLATION - The present invention provides compositions and methods for treating or preventing atrial fibrillation (AF). In particular, the present invention provides administration of muscarinic receptor antagonists (e.g., M2-selective muscarinic receptor blockers), administered alone or in combination with other therapeutic agents (e.g., beta-adrenergic receptor blockers) to treat and/or prevent atrial fibrillation.11-17-2011
20110281852Pharmaceutical compositions containing berberine for treatment or prevention of weight gain and obesity associated with anti-psychotic drugs - The compositions and methods disclosed herein are of use for the treatment and prevention of weight gain and obesity. In particular, the compositions and methods include treatment of weight gain and obesity with berberine and/or berberine analogs alone or in combination thereof to cause a reduction in an individual's weight or prevent weight gain or obesity. In certain embodiments, the weight gain and obesity are associated with administration of anti-psychotic drugs. In an alternative embodiment, the compositions and methods provide berberine or berberine analogs alone or for coadministration with an anti-psychotic agent. In an additional embodiment, the compositions and methods further include a natural product. The usefulness of the present invention is that berberine and berberine analogs do not have synergistic effects with other drugs and administration results in few side effects. Such characteristics of berberine or berberine analogs are a great improvement able to support the widespread use of the compositions and methods of the present invention as therapeutics for the treatment and prevention of weight gain and obesity.11-17-2011
20110028456Solid Pharmaceutical Dosage Form - A pharmaceutical composition comprising a solid unit dosage form comprising: one or more of pharmaceutically active ingredients selected from valacyclovir, olanzapine, voriconazole, topotecan, artesunate, amodiaquine, guggulosterone, ramipril, telmisartan, tibolone, atorvastatin, simvastatin, amlodipine, ezetimibe, fenofibrate, tacrolimus, valgancyclovir, valsartan, clopidrogel, estradiol, trenbolone, efavirenz, metformin, pseudoephedrine, verapamil, felodipine, valproic acid/sodium valproate, mesalamine, hydrochlorothiazide, levosulpiride, nelfinavir, cefixime and cefpodoxime proxetil in combination with a water insoluble polymer and/or a water soluble polymer. Methods for making the pharmaceutical composition are also disclosed.02-03-2011
20110301152NICOTINIC RECEPTOR AGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES - Nicotine receptor agonists or analogs or derivatives thereof for treating inflammatory pulmonary diseases, and pharmaceutical compositions including nicotine receptor agonists or analogs or derivatives thereof. Compounds of formula wherein R1, R2, Xa and Ya are as defined herein are also provided.12-08-2011
20090005367COMPOSITION AND METHOD FOR TREATING ALCOHOLISM AND OTHER SUBSTANCE ADDICTIONS - Disclosed are pharmaceutical compositions comprising a benzodiazepine, an alcohol aversive agent, and an abuse aversive agent, and methods of use in preventing alcohol or cocaine abuse.01-01-2009
20130023524TRICYCLIC INDAZOLE COMPOUND, METHOD OF PREPARATION AND PHARMACEUTICAL COMPOSITION CONTAINING IT - Tricyclic indazole compound and its pharmaceutically acceptable salts of acid addition, use thereof, method and intermediates for preparing them, and a pharmaceutical composition containing them. The tricyclic indazole compound has the following general Formula (I): in which R01-24-2013
20110294791PIRENZEPINE AS AN AGENT IN CANCER TREATMENT - The present invention generally relates to the neuroprotective activity of condensed diazepinones, e.g. condensed benzodiazepinones such as pirenzepine or compounds which are metabolized to condensed benzodiazepinones such as olanzapine. These compounds are suitable as co-medicaments for the prevention and/or treatment of drug-induced neurotoxic effects in general and neurotoxic side effects during cancer treatments with cytostatic drugs such as platinum-derivatives, e.g. cis-, carbo- and oxaliplatin, taxanes, bleomycin, cyclophosphamide and vincristine etc. Further, these compounds have an intrinsic anti-cancer activity on their own due to PARP-1 inhibition, which prevents NADH depletion in oxidative metabolism of healthy cells thus preventing the shift to anoxygenic, glycolytic metabolism present in many types of tumour cells thus eliminating this crucial metabolic advantage favoring tumour growth. These results exploit the fact of differential PARP-1 expression between many cancer cells and healthy tissues.12-01-2011
20110294792PURINE DERIVATIVES AS KINASE INHIBITORS - The present invention provides kinase inhibitors of Formula I.12-01-2011
20100120752MUSCARINIC AGONISTS TO TREAT IMPULSE CONTROL DISORDERS - The invention relates to a novel use of compounds and pharmaceutically acceptable salts thereof, which are muscarinic, for example muscarine-1 (M05-13-2010
20090258863Method for treatment of amyotrophic lateral sclerosis using talampanel - A method of treating a human patient afflicted with amyotrophic lateral sclerosis (ALS) comprising periodically administering to the human patient for a therapeutically effective duration a pharmaceutical composition comprising an amount of talampanel therapeutically effective to provide a benefit to the human patient, thereby treating the human patient.10-15-2009
20090170837METHODS FOR TREATING RAS DRIVEN CANCER IN A SUBJECT - The invention relates to the discovery that the dibenzodiazepinone analogues have growth inhibiting activities on tumorigenic cells that are driven by expression of RAS or mutated RAS. Thus the invention includes methods for inhibiting the activity of RAS using dibenzodiazepinone analogues; methods for inhibiting the growth of a RAS driven cancer cell using dibenzodiazepinone analogues; methods for inhibiting the growth of a RAS driven cancer using dibenzodiazepinone analogues; and methods for treating a subject having a RAS driven cancer using dibenzodiazepinone analogues.07-02-2009
20100125066ALKYLCYCLOHEXYLETHERS OF DIHYDROTETRAAZABENZOAZULENES - The present invention is concerned with alkylcyclohexylethers of dihydro-tetraazabenzoazulenes, i.e. alkylcyclohexylethers of 5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulene s of formula I05-20-2010
20080207599Use of Selective Chloride Channel Modulators to Treat Methamphetamine Abuse - The invention relates to methods of and treatments for using pharmaceutical compositions from a class of compounds that directly or indirectly selectively modulates GABA08-28-2008
20090281090BIOMARKERS FOR THE PREDICTION OF RESPONSIVENESS TO CLOZAPINE TREATMENT - This invention provides methods to predict the likelihood of suicidal or self-destructive behaviour in a patient during treatment. The method employs the detection of a VNTR polymorphism in the 3′-UTR of the dopamine transporter gene (SLC6A3). Patients with nine or fewer repeats are considered poor responders to clozapine. Nine or fewer repeats in the SLC6A3 gene have been correlated with poor expression of the SLC6A3 gene. Also provided are methods of treatment based on the presence or absence of this polymorphism or surrogate markers thereof. Also provided are kits to use in the methods of the invention.11-12-2009
20110172210METHOD FOR TITRATING CLOZAPINE - Method for titrating clozapine in treatment of psychotic disorders in a human patient in need of treatment with clozapine including administering once-a-day controlled release clozapine to the human patient titrating to a therapeutic dose of clozapine within a period of less than one week, or administering controlled release clozapine to the patient at an initial dose of at least 37.5 mg and titrating to a therapeutic dose within a period of less than ten days.07-14-2011
20100113427COMPOSITIONS OF 5-HT3 ANTAGONISTS AND DOPAMINE D2 ANTAGONISTS FOR TREATMENT OF DOPAMINE-ASSOCIATED CHRONIC CONDITIONS - The present invention provides novel compositions comprising a combination of a 5-HT05-06-2010
20120295893COMPOSITIONS AND METHODS OF COUNTERACTING RESIDUAL SEDATIVE EFFECTS OF SLEEP/ HYPNOTIC DRUGS - The present invention provides pharmaceutical compositions comprising a flumazenil, and methods of alleviating or counteracting residual effects (e.g. drowsiness) associated with the administration of sleep/hypnotic drugs or alleviating effects of alcohol intoxication, using self administration modes of delivery.11-22-2012
20100144714DERIVATIVES OF IMIDAZO PYRIMIDO AND DIAZEPINE PYRIMIDINE-DIONE, AND USE THEREOF AS A DRUG - The present invention relates to new derivatives of imidazo, pyrimido and diazepine-pyrimidine-dione of the general formula (I) in which R06-10-2010
20100093704NOVEL PSYCHOTROPIC AGENTS HAVING GLUTAMATE NMDA ACTIVITY - The invention provides novel compounds and pharmaceutical compositions for the treatment of psychological and/or psychiatric diseases or disorders.04-15-2010
20080275030Methods and Compositions for the Delivery of a Therapeutic Agent - The present invention provides a liquid pharmaceutical composition comprising a therapeutic agent and an alkoxy-polyethylene glycol, for example, methoxy-polyethylene glycol, for administration of the therapeutic agent to the mammal. The compositions can be applied to a membrane, for example, a nasal membrane during intranasal administration. The invention also provides methods of administering such compositions to a mammal.11-06-2008
20100130479Gabaergic Agents to Treat Memory Deficits - The present invention provides molecules and methods for the prevention and/or treatment of memory deficit related conditions and/or enhancement of cognition. In a preferred embodiment, the invention includes compounds, salts and prodrugs thereof for the prevention and/or treatment of these conditions.05-27-2010
20080280886SUBSTITUTED UREAS - Disclosed herein are urea-based 5-HT receptor modulators, pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and medical use of such compounds for the treatment and/or management of 5-HT receptor-mediated disorders.11-13-2008
20080280884Mixed Solvate of Olanzapine, Method for Preparing It and Method for Preparing Form I of Olanzapine Therefrom - Said mixed solvate is a solvate of olanzapine/water/tetrahydrofuran in the proportion 1:1:1/2 (I). The method for preparing said solvate comprises treating a crude anhydrous olanzapine with a mixture of tetrahydrofuran/water. The method for preparing Form I of olanzapine includes desolvating the mixed solvate of formula I, by means of drying, in vacuo and under temperature-controlled conditions.11-13-2008
20080280885Methods for Treating Anxiety Related Disorders - The present invention relates to methods of and compositions for treating and relieving symptoms and disease associated with indications caused by a physiological drive to alleviate a sensation of anxiety. In one treatment method, methods of, and compositions for, modulating the expression of certain GABAA receptor subunits are used to treat anxiety-related disorders and depressive disorders associated with physiological tolerance to endogenous neurosteroids.11-13-2008
20100137286ARYLCYCLOHEXYLETHERS OF DIHYDROTETRAAZABENZOAZULENES - The present invention is concerned with arylcyclohexylethers of dihydro-tetraazabenzoazulenes, i.e. arylcyclohexylethers of 5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I06-03-2010
20120142675Methods for Treating Diseases of the Retina - Disclosed herein is a method of treating disorders of the retina comprising administering to a patient in need of such treatment a compound selected from the group consisting of olanzapine, certain of its metabolites, clozapine, and n-desmethyl clozapine.06-07-2012
20110207721PURINE DERIVATIVES AS KINASE INHIBITORS - The present invention provides kinase inhibitors of Formula I.08-25-2011
20100004226STEREOSPECIFIC ANXIOLYTIC AND ANTICONVULSANT AGENTS WITH REDUCED MUSCLE-RELAXANT, SEDATIVE-HYPNOTIC AND ATAXIC EFFECTS - The present invention provides compositions and methods of using stereospecific benzodiazepine derivatives, their salts and prodrugs for the treatment of anxiolytic or convulsant disorders having the side effects of reduced alcohol craving in human alcoholics and a concomitant reduced sedative, hypnotic, muscle relaxant and ataxic side-effects. The invention further provides pharmaceutical compositions for treatment of anxiolytic and convulsant disorders in subjects in need thereof, comprising a compound, prodrug or a salt having a chemical structure represented by any one of Formula I-IV, VI-XI, XV-XVIII and XX-XXI and a pharmaceutically-acceptable carrier.01-07-2010
20100004225CONTROLLED RELEASE AURAL PRESSURE MODULATOR COMPOSITIONS AND METHODS FOR THE TREATMENT OF OTIC DISORDERS - Disclosed herein are compositions and methods for the treatment of otic diseases or conditions with aural pressure modulating agent compositions and formulations administered locally to an individual afflicted with an otic disease or condition, through direct application of these compositions and formulations onto or via perfusion into the targeted auris structure(s).01-07-2010
20090186878CRYSTALLINE FORMS OF A FARNESYL DIBENZODIAZEPINONE - The present invention relates to crystalline forms of ECO-4601 and the processes for providing them. The invention further relates to pharmaceutical compositions comprising the crystalline forms and to methods of use of the crystalline forms as pharmaceuticals.07-23-2009
20080318934Diazepinoes - The invention relates to compounds of the formula (I), to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumours and/or diseases in the development or course of which kinases are involved.12-25-2008
20090325938CONTROLLED-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).12-31-2009
20090325937Pyridazine Compounds as Glycogen Synthase Kinase 3 Inhibitors - Disclosed are pyridazine compounds of the formula I which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds:12-31-2009
20130217681METHOD AND COMPOSITION FOR WEIGHT-GAIN MANAGEMENT - Presented herein is a methodology for reducing weight in obese subjects and in patients receiving various medical treatments that are accompanied with weight gain. The methodology allows for management of weight gain, management of triglyceride levels and weight reduction in obese subjects.08-22-2013
20090023712Pharmaceutical Compositions for the Treatment of Attention Deficit Hyperactivity Disorder Comprising Flibanserin - The invention relates to new pharmaceutical compositions for the treatment of Attention Deficit Hyperactivity Disorder (ADHD) and methods for the preparation thereof. In a preferred embodiment, the instant invention is directed to pharmaceutical combinations comprising flibanserin as one active ingredient in combination with at least one additional active ingredient for the treatment ADHD and methods for the preparation thereof.01-22-2009
20090062262NON STEROIDAL GLUCOCORTICOID RECEPTOR MODULATORS - The present invention relates to compounds having general Formula (I) or a pharmaceutically acceptable salt thereof. In this formula R03-05-2009
20090054412Treatment of Sleep Disorders - A method for treating various types of insomnia is provided using 7-chloro-3-(5-dimethylaminomethyl-[1,2,4]oxadiazol-3-yl)-5methyl-4,5-dihydro-imidazol[1,5,-a][1,4]benzodiazepine-6-one or its pharmaceutically acceptable salt.02-26-2009
20090105229PURINE DERIVATIVES AS KINASE INHIBITORS - The present invention provides kinase inhibitors of Formula I.04-23-2009
20090105228Heterocyclic benzodiazepine cgrp receptor antagonists - Compounds of formula I:04-23-2009
20090018119USE OF N-DESMETHYLCLOZAPINE TO TREAT HUMAN NEUROPSYCHIATRIC DISEASE - Disclosed herein is a method to treat neuropsychiatric diseases including psychosis, affective disorders, dementia, neuropathic pain, and glaucoma. Treatment is carried out by administering a therapeutically effective amount of N-desmethylclozapine to a patient suffering from a neuropsychiatric disease.01-15-2009
20120077804Small Molecule Inhibitors of RNA Silencing - The present invention provides compositions and formulations that contain active compounds as RNAi inhibitors. These compositions and formulations are useful for controlling insects and pests including mosquitoes and agricultural pests.03-29-2012
20090239849Aryl-Fused Spirocyclic Compounds - The present invention relates to a novel class of aryl-fused spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.09-24-2009
20090209525ENABLING METHODS TO IDENTIFY ALLOSTERIC MODULATORS OF RECEPTOR ACTIVITY - A method developed to identify receptor modulators, involving providing a mutant receptor, wherein said mutant receptor has a mutation that alters the activity of said mutant receptor compared to a wild type receptor; contacting said mutant receptor with a candidate compound; and determining whether said candidate compound modulates the activity of said mutant receptor.08-20-2009
20100261712HEMATOPOIETIC NEOPLASM CHEMOTHERAPY - A method and medicament for treating mixed lineage leukemia; translocated mixed lineage leukemia; translocated mixed lineage leukemia based acute myelogenous leukemia; translocated mixed lineage leukemia based acute lymphoid leukemia; a non-MLL based chronic myeloproliferative disorder, or non-MLL based acute lymphoid leukemia is provided.10-14-2010
20100261710HDAC Inhibitors - The present invention provides hydroxamic acid compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the hydroxamic acid compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of the present invention.10-14-2010
20100261713PHARMACEUTICAL FORMULATION CONTAINING IRRITANT - Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse; and an effective amount of an irritant to impart an irritating sensation to an abuser upon administration of said dosage form after tampering.10-14-2010
20100261711SELECTIVE ANTICONVULSANT AGENTS AND THEIR USES - In preferred embodiments, the present invention provides methods of treatment and pharmaceutical compositions for the suppression, alleviation and prevention of seizures. The preferred embodiments of the present invention further relate to methods of treatment and pharmaceutical compositions using benzodiazepine derivatives that provide suppression, alleviation and prevention of seizures with reduced sedative and ataxic side effects.10-14-2010
20110201600CHALCONE LINKED PYRROLO[2,1-C][1, 4]BENZODIAZEPINE HYBRIDS AS POTENTIAL ANTICANCER AGENTS AND PROCESS FOR THE PREPARATION THEREOF - The present invention relates to chalcone linked pyrrolo[2,1-c][1,4]benzodiazepine hybrids and a process for the preparation there of. More particularly it relates to 7-Methoxy-8-{n[4-1-(2 or 4-substituted phenyl)-3-(4-hydroxy-3-methoxyphenyl)-2-propen-1-one]alkyl}-oxy}-(11aS)-1,2,3,11a-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one and 7-Methoxy-8-{n[-3-(4-hydroxy-3-methoxyphenyl)-1-(2,4-alkyl-3-quinolyl)-2-propen-1-one]alkyl}-oxy-(11aS)-1,2,3,11a-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one with aliphatic chain length variations useful as anticancer (antitumour) agent. The general structural formula of these chalcone linked pyrrolo[2,1-c][1,4]benzodiazepines hybrids is given below. wherein R08-18-2011
20100069372COMPOSITIONS AND METHODS FOR MODULATING POLY(ADP-RIBOSE) POLYMERASE ACTIVITY - The present invention is based, in part, on assays we conducted that revealed compounds that modulate (e.g., inhibit) PARP-1 and are therefore useful in treating or preventing diseases characterized by abnormal PARP-1 activity (e.g., undesirable PARP-1 activity).03-18-2010
20090137563PROCESS FOR THE PREPARTION OF OLANZAPINE - The invention relates to a process for the preparation of 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno-[2,3-b][1,5]benzodiazepine (olanzapine) of the formula (I) by reacting 4-amino-2-methyl-10H-thieno [2,3-b][1/5]benzodiazepine hydrochloride of the formula (II) with N-methylpiperazine in an organic solvent, which comprises carrying out the reaction in the mixture of toluene and 1,3-dimethyl-2-imidazolidinone. The invention also encompasses new 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno [2,3-b][1,5]benzodiazepine dihydrochloride trihydrate of the formula (IB), the preparation thereof and pharmaceutical compositions comprising said new compound.05-28-2009
200901375645-[(3,3,3-Trifluoro-2-hydroxy-1-arylpropyl)amino]-1H-quinolin-2-ones, A Process for Their Production and Their Use as Anti-inflammatory Agents - The present invention relates to compounds of formula I,05-28-2009
20130131048NOVEL PSYCHOTROPIC AGENTS HAVING GLUTAMATE NMDA ACTIVITY - The invention provides novel compounds and pharmaceutical compositions for the treatment of psychological and/or psychiatric diseases or disorders.05-23-2013
20130137680HETEROCYCLIC COMPOUNDS CONTAINING A PYRROLOPYRIDINE OR BENZIMIDAZOLE CORE - The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salt thereof, wherein R05-30-2013
20110245237ARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES - The present invention is concerned with aryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I10-06-2011
20110178068Quaternary Ammonium Salt Prodrugs - The invention provides a method of sustained delivery of a tertiary amine-containing parent drug comprising administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile quaternary ammonium salts of tertiary amine-containing parent drugs (or tertiary imine-containing parent drugs) that are derivatized through aldehyde-linked prodrug moieties that reduce the solubility of the prodrug compound at a reference pH as compared to the parent drug. The physical, chemical and solubility properties of these derivatives can be further modulated by the choice of counterion X07-21-2011
201000564993-AMINO-1-ARYLPROPYL AZAINDOLES AND USES THEREOF - The present invention provides compounds of the formula:03-04-2010
20090215751Use of Selective Chloride Channel Modulators to Treat Alcohol and/or Stimulant Substance Abuse - The invention relates to methods of and treatments for using pharmaceutical compositions from a class of compounds that directly or indirectly selectively modulates GABA08-27-2009
20110152251COMPOUNDS FOR MODULATING TLR2 - The present invention is directed to methods, kits, and uses of inhibitors of LCMV mediated NF-κB activation to treat viral infections and inflammatory conditions.06-23-2011
20110251183ARYL-/HETEROARYL-CYCLOHEXENYL-TETRAAZABENZO[E]AZULENES - The present invention is concerned with aryl-/heteroaryl-cyclohexenyl-tetraazabenzo[e]azulenes of formula I10-13-2011
20100130481ANTICONVULSANT AND ANXIOLYTIC METHODS OF USING RECEPTOR SUBTYPE SELECTIVE AGENTS - Methods of using orally active benzodiazepine derivatives and their salts are disclosed. These compounds and their salts have anticonvulsant and anxiolytic activity with reduced sedative, hypnotic, muscle relaxant, or ataxic effects.05-27-2010
20110077238METHODS AND COMPOSITIONS FOR DETERRING ABUSE - Effective methods and compositions to deter abuse of pharmaceutical products (e.g., orally administered pharmaceutical products) including but not limited to immediate release, sustained or extended release and delayed release formulations for drugs subject to abuse comprising at least 10% by weight hydroxypropylcellulose; polyethylene oxide; and a disintegrant selected from the group consisting of crospovidone, sodium starch glycolate and croscarmellose sodium; wherein the ratio of hydroxypropylcellulose to polyethylene oxide on a weight basis is between about 10:1 and 1:10.03-31-2011
20100120751SPIRO-5,6-DIHYDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENES - The present invention is concerned with spiro-dihydrotetraazabenzoazulenes, i.e. spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I05-13-2010
20080249082Use of Memantine (Namenda) to Treat Autism, Compulsivity and Impulsivity - The present invention relates to the treatment of compulsive, impulsive and pervasive developmental disorders. More particularly, the methods described herein comprise administration of memantine to an individual suffering from such a disorder in an amount effective to relieve one or more symptoms of said disorder. In particularly preferred aspects, the invention is directed to the use of memantine for the treatment of autism10-09-2008
20100113426Intranasal Benzodiazepine Compositions - A pharmaceutical composition for intranasal administration to a mammal. The pharmaceutical composition comprises an effective amount of a benzodiazepine or pharmaceutically acceptable salt thereof; and a nasal carrier. In some embodiments, the pharmaceutical composition when administered intranasally produces a rapid physiological response. Pharmaceutical compositions may also include at least one or more sweeteners, flavoring agents, or masking agents or combinations thereof.05-06-2010
20100113425PYRROLOBENZODIAZEPINES - Compounds of the formula I:05-06-2010
20090005366DEUTERIUM-ENRICHED OLANZAPINE - The present application describes deuterium-enriched olanzapine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.01-01-2009
20090029973FUSED HETEROCYCLIC COMPOUND - The present invention relates to a compound represented by the formula:01-29-2009
20120302554PHANTOM PHENOMENA TREATMENT - The present invention relates to a substance for the treatment of the phantom phenomena of tinnitus and/or phantom pain, a method for the diagnosis and for the treatment of these phantom phenomena.11-29-2012
20100311732NOVEL HETEROCYCLIC COMPOUNDS - 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 the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising compounds of Formula I and methods of treating or preventing one or more conditions that may be regulated or normalized via inhibition of dipeptidyl peptidase IV (DPP-IV).12-09-2010
20120202799Condensed Azepine Derivatives As Bromodomain Inhibitors - Benzodiazepine compounds of formula (I)08-09-2012
20120202798COMPOSITIONS CONTROLLING pH RANGE OF RELEASE AND/OR RELEASE RATE - The present invention provides a composition controlling a pH range of release and/or a release rate, which contains (i) a thienotriazolodiazepine compound of the formula (I)08-09-2012
20080255097Methods for the Treatment of Substance Abuse and Dependence - The present invention relates to methods of and compositions for treating and relieving symptoms and disease associated with indications caused by a physiological drive to alleviate a sensation of anxiety. More specifically, the present invention relates to methods of and compositions for treating and relieving symptoms associated with substance abuse and withdrawal. The present invention relates to methods of and compositions for treating and relieving symptoms associated with addiction to antidepressants, opiates, nicotine or marijuana. In one method, a patient is treated with a composition that directly or indirectly modulates GABA10-16-2008
20110028457PHARMACEUTICAL PREPARATION COMPRISING PERMETHYLATED CYCLODEXTRIN - The invention relates to a pharmaceutical preparation for applying a pharmaceutical agent. According to the invention, the preparation contains: a) a pharmaceutical agent which has an aromatic group or an aromatic part and the molecule of which has a maximum diameter of ≦2 nm; b) a permethylated cyclodextrin having a degree of substitution of 3 methyl groups per glucopyranose unit. The permethylated cyclodextrin and the pharmaceutical agent form a complex.02-03-2011
20110028458INHIBITION OF CELL MIGRATION BY A FARNESYLATED DIBENZODIAZEPINONE - The invention relates to the discovery that dibenzodiazepinone analogues have cell migration inhibiting activities on neoplastic and endothelial cells. The migration of neoplastic cells from various tumor types, such as a glioma tumor that may comprise an EGF and/or PTEN mutation, or a Ras-, Raf, or EGFR-mediated tumor, may be inhibited when contacted by the dibenzodiazepinone analogues of the present invention. The invention includes methods for inhibiting migration of a cell in a subject, by contacting a cell with a dibenzodiazepinone analogue of the present invention.02-03-2011
20100286127ANTITUMOR AGENT - The present invention relates to a novel antitumor agent containing a compound that inhibits binding between acetylated histone and a bromodomain-containing protein, preferably a thienotriazolodiazepine compound represented by the following formula (I)11-11-2010
20110263573HETEROBIARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES - The present invention relates to heterobiaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I10-27-2011
20110118237Isoxazoline linked pyrrolo[2,1-c][1,4]benzodiazepine hybrids as potential anticancer agents and the process for preparation thereof - The present invention provides compounds of general formula (5a-d) and (9a-h) useful as potential antitumour agents against human cancer cell lines. The present invention also provides a process for the preparation of pyrrolo [2,1-c][1,4]benzodiazepine hybrids of general formula (5a-d) and (9a-h).05-19-2011
20100298304DIAGNOSIS AND TREATMENT OF AUTISM SPECTRUM DISORDERS - The invention relates to methods for diagnosis and treatment of autism spectrum disorders, particularly for autism spectrum disorders characterized by increased head size (circumference) and deficits in social behavior.11-25-2010
20100190776Thiazoline and Oxazoline Derivatives and Their Methods of Use - The invention relates to a series of thiazoline and oxazoline derivatives, compositions thereof, and methods of treating conditions and disorders using such compounds.07-29-2010
20110190275C2-FLUORO SUBSTITUTED PIPERAZINE LINKED PYRROLO[2,1-C][1,4] BENZODIAZEPINE DIMERS AND A PROCESS FOR THE PREPARATION THEREOF - The present invention provides a compounds of general formula IXa-d, useful as potential antitumour agents and pharmaceutical composition comprising these compounds exhibits binding affinity with calf thymus (CT) DNA at a molar ratio of 1:5 in aqueous sodium phosphate buffer at pH of 7.00. The present invention further provides a process for the preparation of C2-Fluoro substituted piperazine linked pyrrolo[2,1c][1-4], benzodiazepine of formula (IX).08-04-2011
20110263574PIRENZEPINE AS OTOPROTECTIVE AGENT - The present invention generally relates to the otoprotective activity of condensed diazepinones, e.g. condensed benzodiazepines such as pirenzepine or compounds which are metabolized to condensed benzodiazepinones such as olanzapine. These compounds are suitable as medicaments for the prevention and/or treatment of otic diseases, e.g. diseases associated with loss of hearing.10-27-2011
20080293698Methods and Compositions for Treating Arg - The invention provides dilute and concentrated, aqueous, pharmaceutical compositions comprising gamma-hydroxybutyric acid or pharmaceutically acceptable salts thereof; gamma-butyryl lactone; 1,4-butanediol; 4-hydroxyl pentanoic acid or pharmaceutically acceptable salts thereof; 4-hydroxyl pentanoic acid lactone, or combinations thereof, and a coloring agent and/or flavoring agent that is useful in preventing sexual assault or date rape. Methods of treating conditions responsive to the administration of gamma-hydroxyl butyric acid and/or its pharmaceutically acceptable salts; gamma-butyryl lactone; 1,4-butanediol; 4-hydroxyl pentanoic acid and/or its pharmaceutically acceptable salts; and 4-hydroxyl pentanoic acid lactone are also described. The invention provides methods for treating patients with acquired resistance to GABAnergic agents.11-27-2008
20110039834NOVEL PHARMACEUTICAL COMPOSITIONS FOR OPTIMIZING SUBSTITUTION TREATMENTS AND EXTENDING THE PHARMACOPOEIA TO GLOBAL TREATMENT OF ADDICTIONS - The present invention relates to the field of life needs and more particularly to the therapeutic field.02-17-2011
20090221560Pharmaceutical Formulation - This invention relates to a stable pharmaceutical formulation containing olanzapine. The composition comprises olanzapine or a pharmaceutically acceptable salt thereof, one or more suitable pharmaceutical excipients and a compound of formula (I) and/or a compound of formula (II): or a pharmaceutically acceptable salt thereof.09-03-2009
20100168085Dopamine and agonists and antagonists thereof for modulation of suppressive activity of CD4+CD25+ regulatory T cells - Compositions and methods for modulation of the suppressive activity of CD4+CD25+regulatory T cells (Treg) on CD4+CD25− effector T cells (Teff) are provided. An agent selected from: (i) dopamine; (ii) a dopamine precursor; (iii) a D1-R agonist; (iv) a D2-R antagonist; (v) a combination of (i) and (ii); or (vi) a combination of (i), (ii) or (iii) with (iv), down-regulates the suppressive activity of Treg and is useful for treatment of cancer. An agent selected from (i) a dopamine D2-R agonist, (ii) a dopamine D1-R antagonist, and (iii) a combination of (i) and (ii), up-regulates the suppressive activity of Treg and is useful for treatment of an autoimmune disease or for controlling graft rejection in tissue/organ transplantation.07-01-2010
20100190775PYRIMIDODIAZEPINONE DERIVATIVE - The invention provides a pyrimidodiazepinone derivative represented by the general formula (I)07-29-2010
20110319395Pharmaceutical Formulation of Olanzapine - A pharmaceutical formulation comprising a homogeneous mixture of (a) olanzapine or a pharmaceutically acceptable salt thereof as an active ingredient, (b) a monosaccharide and/or oligosaccharide, (c) a polysaccharide and, optionally, further ingredients.12-29-2011
20120208800Bromodomain Inhibitors For Treating Autoimmune And Inflammatory Diseases - The use of compounds in the treatment of autoimmune and inflammatory diseases or conditions, pharmaceutical compositions containing such compounds and to methods for identifying compounds for use in the treatment of such diseases or conditions.08-16-2012
20090029972Dibenzodiazepinone Analogues, Processes for Their Production and Their Use as Pharmaceuticals - The invention relates to biologically active dibenzodiazepinone analogs represented by Formula I, to methods of producing them, and their use in the preparation of medicaments for the treatment of neoplastic conditions01-29-2009
20110166128Diaryldiazepine Prodrugs for the Treatment of Neurological and Psychological Disorders - The present invention provides prodrug compounds of diaryldiazepine drug compounds.07-07-2011
20120022051RAPID ONSET LIQUID MIDAZOLAM COMPOSITION FOR BUCCAL ADMINISTRATION - This application discloses liquid compositions for administration to a patient comprising midazolam and a pharmaceutically acceptable carrier, wherein the pH of the composition is about 6 or higher, the composition comprises less than about 200 mg/ml cyclodextrin, and at least about 50% of the midazolam is present in solution. Uses of these compositions are also disclosed.01-26-2012
20120058993Stable Suspension Formulation - A physicochemically stable aqueous composition including clozapine suspension.03-08-2012
20120115852HETEROCYCLIC COMPOUNDS AS AUTOTAXIN INHIBITORS - Compounds of the formula (I), in which R, R05-10-2012
20120122852TRICYCLIC N-HETEROARYL-CARBOXAMIDE DERIVATIVES CONTAINING A BENZIMIDAZOLE UNIT, METHOD FOR PREPARING SAME AND THEIR THERAPEUTIC USE - The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I):05-17-2012
20120122851PHARMACEUTICAL PREPARATION AND DELIVERY SYSTEM - The present invention relates to unique delivery systems and the use of an imidazobenzodiazepine derivative, such as flumazenil either alone or in combination with other receptor antagonists in the treatment of disease or medical disorders.05-17-2012
20120232066COMPOSITIONS FOR REDUCING RISK OF ADVERSE EVENTS CAUSED BY DRUG-DRUG INTERACTIONS - The present disclosure provides a composition comprising a GABA09-13-2012
20120232065DIHYDRO-OXAZOLOBENZODIAZEPINONE COMPOUNDS, A PROCESS FOR THERE PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - Compounds of formula (I):09-13-2012
20120172352PYRAZOLINE DIONE DERIVATIVES AS NADPH OXIDASE INHIBITORS - The present invention is related to pyrazoline dione derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).07-05-2012
20120220573Benzodiazepine Bromodomain Inhibitor - The present invention relates to a benzodiazepine compound of formula (I), processes for its preparation, pharmaceutical compositions containing such a compound and to its use in therapy.08-30-2012
20110124633Heterocyclic Compounds, Methods of Making Them and Their Use in Therapy - In part, the present invention is directed to antibacterial compounds.05-26-2011
20120264745METHODS AND COMPOSITIONS FOR THE DELIVERY OF A THERAPEUTIC AGENT - The present invention provides a liquid pharmaceutical composition comprising a therapeutic agent and an alkoxy-polyethylene glycol, for example, methoxy-polyethylene glycol, for administration of the therapeutic agent to the mammal. The compositions can be applied to a membrane, for example, a nasal membrane during intranasal administration. The invention also provides methods of administering such compositions to a mammal.10-18-2012
20110046117COMPOSITIONS OF 5-HT3 ANTAGONISTS AND DOPAMINE D2 ANTAGONISTS FOR TREATMENT OF DOPAMINE-ASSOCIATED CHRONIC CONDITIONS - The present invention provides novel compositions comprising a combination of a 5-HT02-24-2011
20110046116SEDATIVE FOR USE DURING EYE SURGERY - A drug for sedating a patient, and especially a smoker, during eye surgery. The drug includes a sedative such as midazolam in a mix with nicotine. The mixture is injected into the patient prior to the eye surgery.02-24-2011
20120322793PROTEIN KINASE INHIBITORS - In one aspect, the invention provides compounds of Formula I12-20-2012
20100234360Methods 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.09-16-2010
20100234359TREATMENT OF SLEEP DISORDERS - The use of 7-chloro-3-(5-dimethylaminomethyl-[1,2,4]oxadiazol-3-yl)-5methyl 4,5-dihydro-imidazol[1,5,-a][1,4]benzodiazepine-6-one or its pharmaceutically acceptable salt for treating various types of insomnia.09-16-2010
20100234358NERAMEXANE FOR THE TREATMENT OF NYSTAGMUS - The present invention relates to the treatment of an individual diagnosed with nystagmus comprising administering to the individual an effective amount of a 1-aminoalkylcyclohexane derivative, for example neramexane or a pharmaceutically acceptable salt thereof, such as neramexane mesylate.09-16-2010
20100204214HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF - Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.08-12-2010
20110319394FUSED HETEROCYCLIC COMPOUNDS - The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I):12-29-2011
201001680867,8,10,10A-TETRAHYDRO-6H-BENZO[C]CHROMEN-9(6AH)-ONE MODULATORS OF CANNABINOID RECEPTORS - The present invention relates to new 7,8,10,10a-tetrahydro-6H-benzo[c]chromen-9(6aH)-one modulators of cannabinoid receptors, pharmaceutical compositions thereof, and methods of use thereof.07-01-2010
20100130480BENZOQUINOLINE INHIBITORS OF VESICULAR MONOAMINE TRANSPORTER 2 - The present invention relates to new benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions thereof, and methods of use thereof.05-27-2010
20100130478SUSTAINED RELEASE FORMULATIONS OF PSYCHOACTIVE DRUGS - This invention provides biodegradable, sustained-release pharmaceutical compositions of a psychoactive drug formulated with biocompatible, biodegradable tyrosine-derived polyarylates.05-27-2010
20110160192BIARYL AMINO ACIDS AND THEIR USE IN DNA BINDING OLIGOMERS - Compounds of formula (I): Z′-CO-A-B—NH-Z (I) wherein: Z is H or an amino protecting group; Z′ is OH, a protected or activated hydroxyl group or Cl; A is an optionally substituted C06-30-2011
20110160191NEW FUSED POLYCYCLIC COMPOUNDS HAVING A HETEROCYCLIC RING(S) AND PHARMACEUTICAL USE THEREOF - The present invention provides a fused polycyclic compound of the following formula, analogues thereof and pharmaceutically acceptable salts thereof; and agents for increasing the sugar-transporting capacity, hypoglycemic agents and pharmaceutical compositions containing the above compounds. This fused polycyclic compound has high medicinal properties and few side-effects, and a therapeutic effect on diabetes.06-30-2011
20080255096Phantom Phenomena Treatment - The present invention relates to a substance for the treatment of the phantom phenomena of acute tinnitus and/or phantom pain, a method for the diagnosis and for the treatment of these phantom phenomena.10-16-2008
20080234254Inhibitors of Histone Deacetylase - The present invention relates to a benzamide derivative comprising a head, spacer and cap group wherein the spacer includes a benzene ring substituted with an additional spacer and wherein the additional spacer is an unsaturated group.09-25-2008
20130172328FUSED HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASES (PDES) INHIBITORS - The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):07-04-2013
20130143872INJECTABLE FORMULATION OF A REVERSE TRANSCRIPTASE INHIBITOR FOR THE TREATMENT CANCER - This invention relates to a composition formulated into a parenteral or injectable dosage form for the treatment of cancer, more particularly, this invention relates to a composition formulated into a parenteral dosage form suitable for administration in and around cancerous tissue, the composition including: a pharmaceutically acceptable solvent including from 20% to 100% ethanol (V/V); and a reverse transcriptase inhibitor exhibiting an anti-cancer effect, dissolved in the solvent.06-06-2013
20090221559BENZODIAZEPINES AS HCV INHIBITORS - The present invention relates to the use of benzodiazepines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to benzodiazepine compounds per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceutical compositions comprising them, and combinations of said compounds with other anti-HCV agents.09-03-2009
20080214525Alkyl 4- [4- (5-Oxo-2,3,5, 11A-Tetrahydo-5H-Pyrrolo [2, 1-C] [1,4] Benzodiazepine-8-Yloxy) -Butyrylamino]-1H-Pyrrole-2-Carboxylate Derivatives and Related Compounds For the Treatment of a Proliferative Disease - A compound of formula (I); or a salt or solvate thereof, wherein: the dotted line indicates the optional presence of a double bond between C2 and C3; R09-04-2008
20110224195HETEROCYCLIC COMPOUNDS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES - The present invention is directed to substituted six-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as obesity and diabetes, particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.09-15-2011
20130150350Derivatives of 1-Phenyl-1,5-Dihydro-Benzo[B] [1,4]Diazepine-2,4-Dione as Inhibitors of HIV Replication - Compounds of formula (I) wherein m, R06-13-2013
20110275616Combination Analgesic Employing Opioid and Neutral Antagonist - Methods of utilizing an opioid agonist in a mammalian subject in a manner that inhibits peripheral effects of the opioid agonist are described. The methods comprise administering the opioid agonist in an amount sufficient to confer analgesia the subject and co-administering a neutral opioid antagonist or pharmaceutically acceptable isomorph or pharmaceutically acceptable salt thereof in an amount sufficient to substantially inhibit peripheral effects and insufficient to block substantial central effects of the opioid agonist in the subject.11-10-2011
20120277221SELECTIVE SEROTONIN 2A/2C RECEPTOR INVERSE AGONISTS AS THERAPEUTICS FOR NEURODEGENERATIVE DISEASES - Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.11-01-2012
20130150351METHODS AND COMPOSITIONS FOR TREATING A SUBJECT FOR CENTRAL NERVOUS SYSTEM (CNS) INJURY - Methods for treating a central nervous system (CNS) injury in a subject are provided. As of the methods include administering to the subject an effective amount of gamma aminobutyric acid (GABA) receptor signaling inhibitor to treat the subject for the CNS injury. Also provided are compositions useful in embodiments of the methods. Methods and compositions of the invention find use in the treatment of a variety of different CNS injuries, including but not limited to, treating a subject for CNS injury associated with the occurrence of stroke.06-13-2013
20120283250Methods and Compositions for Determining Hypersusceptibility of HIV-1 to Non-Nucleoside Reverse Transcriptase Inhibitors - This invention relates to methods for determining hypersusceptibility of HIV-1 viruses to non-nucleoside reverse transcriptase inhibitors (NNRTIs) based on the viral genotypes. The methods generally comprise detecting, in a gene encoding reverse transcriptase of the HIV-1, the presence of a mutation at codon 65, 69, or 74 alone or in combination with one or more mutations at certain other codons. Combinations of mutations associated with hypersusceptibility to NNRTIs are also disclosed.11-08-2012
20120283249Novel 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.11-08-2012
20130158016ANESTHETIC ASSOCIATION, ANESTHETIC COMPOSITION, AND ANESTHETIC MEDICAMENT FOR VETERINARY USE - The present invention relates to a new association of active ingredients working as anesthetic and pre-anesthetic formulated in a composition containing anesthetics and analgesics suitable for use in surgical and pre-surgical procedures and others which require sedation, tranquilization, chemical restraint and pre-anesthetic medication. More specifically the present invention relates to a new association comprising the active ingredients ketamine, preferably the isomer S-ketamine(+), midazolam and tramadol, formulated in true solution for parenteral use. The present invention also contemplates an anesthetic drug for veterinary use for parenteral use.06-20-2013
20130184265Prodrugs of Secondary Amine Compounds - The present invention relates to compounds of Formula I:07-18-2013
20130184264Compositions And Methods For Treating Neoplasia, Inflammatory Disease And Other Disorders - The invention features compositions and methods for treating or preventing a neoplasia. More specifically, the invention provides compositions and methods for disrupting the interaction of a BET family polypeptide comprising a bromodomain with chromatin (e.g., disrupting a bromodomain interaction with an acetyl-lysine modification present on a histone N-terminal tail).07-18-2013
20090281091METHODS FOR MODULATING BLADDER FUNCTION - This invention provides methods and pharmaceutical compositions for modulating bladder function, and in particular for maintaining bladder control or treating urinary incontinence.11-12-2009
20110312946COMBINATION THERAPY FOR THE TREATMENT OF DIABETES - The present invention provides methods of treating, reducing, preventing, or inhibiting symptoms of diabetes and/or lowering plasma levels of HbA1c by co-administration of therapeutic or subtherapeutic doses of telenzepine and sertraline to a subject in need thereof.12-22-2011
20130190299METHODS AND COMPOSITIONS FOR TREATMENT OF MULTIPLE SCLEROSIS - Methods and formulations for the treatment of multiple sclerosis with drugs with affinity for both serotonergic 5-HT07-25-2013
20120028964PHARMACEUTICAL COMBINATION - The present invention relates to a pharmaceutical combination for the treatment of schizophrenia and acute manic episodes associated with bipolar disorders, which comprises a compound which is active on a trace amine-associated receptor 1 (TAAR1 agonist) and an antipsychotic drug. This combination can reduce metabolic side effects which appear if using an antipsychotic drug alone.02-02-2012
20120295892GABAERGIC RECEPTOR SUBTYPE SELECTIVE LIGANDS AND THEIR USES - Described herein are α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands, pharmaceutical compositions, and methods of use of such ligands and compositions in treatment of anxiety disorders, epilepsy and schizophrenia with reduced sedative and ataxic side effects. In embodiments, such as α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands lack ester linkages and may be thus relatively insensitive to hydrolysis by esterases.11-22-2012
20130210813Male Contraceptive Compositions and Methods of Use - The invention relates to compositions and methods for effecting male contraception.08-15-2013

Patent applications in class Tricyclo ring system having the seven-membered hetero ring as one of the cyclos