| Entries |
| Document | Title | Date |
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| 20080214525 | Alkyl 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; R | 09-04-2008 |
| 20080234254 | Inhibitors 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 |
| 20080249082 | Use 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 autism | 10-09-2008 |
| 20080255096 | Phantom 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 |
| 20080255097 | Methods 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 GABA | 10-16-2008 |
| 20080275030 | Methods 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 |
| 20080280884 | Mixed 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 |
| 20080280885 | Methods 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 |
| 20080280886 | SUBSTITUTED 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 |
| 20080293698 | Methods 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 |
| 20080293699 | Inhibitors 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 |
| 20080318934 | Diazepinoes - 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 |
| 20090005366 | DEUTERIUM-ENRICHED OLANZAPINE - The present application describes deuterium-enriched olanzapine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 01-01-2009 |
| 20090012064 | Compositions 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 |
| 20090018119 | USE 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 |
| 20090023712 | Pharmaceutical 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 |
| 20090029972 | Dibenzodiazepinone 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 conditions | 01-29-2009 |
| 20090029973 | FUSED HETEROCYCLIC COMPOUND - The present invention relates to a compound represented by the formula: | 01-29-2009 |
| 20090036431 | Cytotoxic 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 |
| 20090054412 | Treatment 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 |
| 20090062262 | NON STEROIDAL GLUCOCORTICOID RECEPTOR MODULATORS - The present invention relates to compounds having general Formula (I) or a pharmaceutically acceptable salt thereof. In this formula R | 03-05-2009 |
| 20090069306 | PROCESS 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 |
| 20090093466 | Carboxamide 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 |
| 20090105228 | Heterocyclic benzodiazepine cgrp receptor antagonists - Compounds of formula I: | 04-23-2009 |
| 20090105229 | PURINE DERIVATIVES AS KINASE INHIBITORS - The present invention provides kinase inhibitors of Formula I. | 04-23-2009 |
| 20090124606 | Composition 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 |
| 20090124607 | Novel 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 |
| 20090137563 | PROCESS 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 |
| 20090137564 | 5-[(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 |
| 20090149449 | PYRROLOBENZODIAZEPINE DERIVATIVES, COMPOSITIONS COMPRISING THE SAME AND METHODS RELATED THERETO - Disclosed are compounds of Formula I | 06-11-2009 |
| 20090156583 | Tricyclic Amide Derivatives - The present invention relates to compounds of formula I | 06-18-2009 |
| 20090170837 | METHODS 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 |
| 20090186878 | CRYSTALLINE 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 |
| 20090186879 | TRICYCLIC COMPOUNDS AND USE THEREOF - There is provided a compound of the formula (I′): | 07-23-2009 |
| 20090209525 | ENABLING 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 |
| 20090215751 | Use 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 GABA | 08-27-2009 |
| 20090221559 | BENZODIAZEPINES 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 |
| 20090221560 | Pharmaceutical 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 |
| 20090239849 | Aryl-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 |
| 20090258863 | Method 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 |
| 20090270373 | TREATMENT 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 |
| 20090281090 | BIOMARKERS 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 |
| 20090281091 | METHODS 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 |
| 20090318426 | USE 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 |
| 20090325937 | Pyridazine 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 |
| 20090325938 | 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). | 12-31-2009 |
| 20100004225 | CONTROLLED 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 |
| 20100004226 | STEREOSPECIFIC 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 |
| 20100041643 | THIENOTRIAZOLODIAZEPINE COMPOUND AND MEDICINAL USE THEREOF - [Solving means] A thienotriazolodiazepine compound of the following formula (I) | 02-18-2010 |
| 20100056499 | 3-AMINO-1-ARYLPROPYL AZAINDOLES AND USES THEREOF - The present invention provides compounds of the formula: | 03-04-2010 |
| 20100069372 | COMPOSITIONS 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 |
| 20100075955 | SHORT-ACTING BENZODIAZEPINE SALTS AND THEIR POLYMORPHIC FORMS - The invention relates to esylate salts of the compound of formula (I): | 03-25-2010 |
| 20100081647 | SHORT-ACTING BENZODIAZEPINE SALTS AND THEIR POLYMORPHIC FORMS - The invention relates to besylate salts of the compound of formula (I): | 04-01-2010 |
| 20100093704 | NOVEL 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 |
| 20100113425 | PYRROLOBENZODIAZEPINES - Compounds of the formula I: | 05-06-2010 |
| 20100113426 | Intranasal 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 |
| 20100113427 | COMPOSITIONS 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-HT | 05-06-2010 |
| 20100120751 | SPIRO-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 I | 05-13-2010 |
| 20100120752 | MUSCARINIC 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 (M | 05-13-2010 |
| 20100125066 | ALKYLCYCLOHEXYLETHERS 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 I | 05-20-2010 |
| 20100130478 | SUSTAINED 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 |
| 20100130479 | Gabaergic 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 |
| 20100130480 | BENZOQUINOLINE 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 |
| 20100130481 | ANTICONVULSANT 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 |
| 20100137286 | ARYLCYCLOHEXYLETHERS 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 I | 06-03-2010 |
| 20100144714 | DERIVATIVES 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 R | 06-10-2010 |
| 20100152170 | Benzazole 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 |
| 20100168085 | Dopamine 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 |
| 20100168086 | 7,8,10,10A-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 |
| 20100190775 | PYRIMIDODIAZEPINONE DERIVATIVE - The invention provides a pyrimidodiazepinone derivative represented by the general formula (I) | 07-29-2010 |
| 20100190776 | Thiazoline 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 |
| 20100204214 | HISTAMINE 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 |
| 20100210631 | SUBSTITUTED 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 |
| 20100234358 | NERAMEXANE 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 |
| 20100234359 | TREATMENT 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 |
| 20100234360 | 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. | 09-16-2010 |
| 20100261710 | HDAC 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 |
| 20100261711 | SELECTIVE 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 |
| 20100261712 | HEMATOPOIETIC 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 |
| 20100261713 | PHARMACEUTICAL 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 |
| 20100286127 | ANTITUMOR 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 |
| 20100298304 | DIAGNOSIS 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 |
| 20100311732 | NOVEL 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 |
| 20100324027 | DIAZAHOMOADAMANTANE 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 |
| 20110015186 | METHODS 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 |
| 20110021507 | INHIBITING 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 M | 01-27-2011 |
| 20110028456 | Solid 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 |
| 20110028457 | PHARMACEUTICAL 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 |
| 20110028458 | INHIBITION 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 |
| 20110034442 | Use 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 serotonin | 02-10-2011 |
| 20110046116 | SEDATIVE 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 |
| 20110046117 | COMPOSITIONS 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-HT | 02-24-2011 |
| 20110077238 | METHODS 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 |
| 20110118237 | Isoxazoline 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 |
| 20110124633 | Heterocyclic Compounds, Methods of Making Them and Their Use in Therapy - In part, the present invention is directed to antibacterial compounds. | 05-26-2011 |
| 20110152251 | COMPOUNDS 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 |
| 20110160191 | NEW 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 |
| 20110160192 | BIARYL 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 C | 06-30-2011 |
| 20110166128 | Diaryldiazepine Prodrugs for the Treatment of Neurological and Psychological Disorders - The present invention provides prodrug compounds of diaryldiazepine drug compounds. | 07-07-2011 |
| 20110172210 | METHOD 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 |
| 20110178068 | Quaternary 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 X | 07-21-2011 |
| 20110190275 | C2-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 |
| 20110201600 | CHALCONE 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 R | 08-18-2011 |
| 20110207721 | PURINE DERIVATIVES AS KINASE INHIBITORS - The present invention provides kinase inhibitors of Formula I. | 08-25-2011 |
| 20110224195 | HETEROCYCLIC 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 |
| 20110245237 | ARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES - The present invention is concerned with aryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I | 10-06-2011 |
| 20110251183 | ARYL-/HETEROARYL-CYCLOHEXENYL-TETRAAZABENZO[E]AZULENES - The present invention is concerned with aryl-/heteroaryl-cyclohexenyl-tetraazabenzo[e]azulenes of formula I | 10-13-2011 |
| 20110263573 | HETEROBIARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES - The present invention relates to heterobiaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I | 10-27-2011 |
| 20110263574 | PIRENZEPINE 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 |
| 20110281852 | Pharmaceutical 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 |
| 20110281853 | COMPOSITIONS 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 |
| 20110294791 | PIRENZEPINE 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 |
| 20110294792 | PURINE DERIVATIVES AS KINASE INHIBITORS - The present invention provides kinase inhibitors of Formula I. | 12-01-2011 |
| 20110301152 | NICOTINIC 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 |
| 20110312946 | COMBINATION 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 |
| 20110319394 | FUSED 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 |
| 20110319395 | Pharmaceutical 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 |
| 20120022051 | RAPID 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 |
| 20120028964 | PHARMACEUTICAL 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 |
| 20120058993 | Stable Suspension Formulation - A physicochemically stable aqueous composition including clozapine suspension. | 03-08-2012 |
| 20120077804 | Small 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 |
| 20120115852 | HETEROCYCLIC COMPOUNDS AS AUTOTAXIN INHIBITORS - Compounds of the formula (I), in which R, R | 05-10-2012 |
| 20120122851 | PHARMACEUTICAL 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 |
| 20120122852 | TRICYCLIC 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 |
| 20120142675 | Methods 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 |
| 20120172352 | PYRAZOLINE 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 |
| 20120184536 | COMPOSITIONS 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 |
| 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 |
| 20120202796 | METHOD 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 |
| 20120202797 | SUBSTITUTED [(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-HT | 08-09-2012 |
| 20120202798 | COMPOSITIONS 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 |
| 20120202799 | Condensed Azepine Derivatives As Bromodomain Inhibitors - Benzodiazepine compounds of formula (I) | 08-09-2012 |
| 20120208800 | Bromodomain 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 |
| 20120220573 | Benzodiazepine 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 |
| 20120225865 | ARYLCYCLOHEXYLETHERS 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 I | 09-06-2012 |
| 20120232065 | DIHYDRO-OXAZOLOBENZODIAZEPINONE COMPOUNDS, A PROCESS FOR THERE PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - Compounds of formula (I): | 09-13-2012 |
| 20120232066 | COMPOSITIONS FOR REDUCING RISK OF ADVERSE EVENTS CAUSED BY DRUG-DRUG INTERACTIONS - The present disclosure provides a composition comprising a GABA | 09-13-2012 |
| 20120238552 | PHARMACEUTICAL 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 |
| 20120264745 | METHODS 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 |
| 20120277221 | SELECTIVE 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 |
| 20120283249 | Novel 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 |
| 20120283250 | Methods 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 |
| 20120295892 | GABAERGIC 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 |
| 20120295893 | COMPOSITIONS 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 |
| 20120302554 | PHANTOM 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 |
| 20120322793 | PROTEIN KINASE INHIBITORS - In one aspect, the invention provides compounds of Formula I | 12-20-2012 |
| 20130023524 | TRICYCLIC 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 R | 01-24-2013 |
| 20130040940 | MERCAPTOAMIDINE DERIVATIVES AND METHODS OF USE - Compounds of formula (I) | 02-14-2013 |
| 20130065885 | ORAL 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 |
| 20130072477 | TREATMENT 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 |
| 20130079334 | Compositions 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 |
| 20130079335 | Benzotriazolodiazepine Compounds Inhibitors Of Bromodomains - Benzodiazepine compounds, pharmaceutical compositions containing such compounds and to their use in therapy. | 03-28-2013 |
| 20130085136 | NOVEL 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 |
| 20130109679 | HETEROCYCLIC COMPOUNDS CONTAINING AN INDOLE CORE | 05-02-2013 |
| 20130131048 | NOVEL 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 |
| 20130137680 | HETEROCYCLIC COMPOUNDS CONTAINING A PYRROLOPYRIDINE OR BENZIMIDAZOLE CORE - The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salt thereof, wherein R | 05-30-2013 |
| 20130143872 | INJECTABLE 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 |
| 20130150350 | Derivatives 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, R | 06-13-2013 |
| 20130150351 | METHODS 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 |
| 20130158016 | ANESTHETIC 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 |
| 20130172328 | FUSED 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 |
| 20130184264 | Compositions 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 |
| 20130184265 | Prodrugs of Secondary Amine Compounds - The present invention relates to compounds of Formula I: | 07-18-2013 |
| 20130190299 | METHODS AND COMPOSITIONS FOR TREATMENT OF MULTIPLE SCLEROSIS - Methods and formulations for the treatment of multiple sclerosis with drugs with affinity for both serotonergic 5-HT | 07-25-2013 |
| 20130210813 | Male Contraceptive Compositions and Methods of Use - The invention relates to compositions and methods for effecting male contraception. | 08-15-2013 |
| 20130217681 | METHOD 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 |
| 20130261109 | ANTITUMOR AGENT - The invention provides a method of inhibiting binding between acetylated histone and a bromodomain-containing protein in a mammal, as well as a method of shrinking or killing of cancer cells expressing a bromodomain-containing protein or inhibiting the growth of cancer cells expressing a bromodomain-containing protein in a mammal. The methods involve administering an effective amount of (S)-2-[4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]-N-(4-hydroxyphenyl)acetamide or a dihydrate thereof to the mammal. | 10-03-2013 |
| 20130267503 | PHARMACEUTICAL COMPOSITIONS COMPRISING FATTY ACID ESTERS - The present invention relates to an injectable, pharmaceutical composition comprising a C | 10-10-2013 |
| 20130267504 | PHARMACEUTICAL COMPOSITIONS COMPRISING FATTY GLYCEROL ESTERS - The present invention relates to a pharmaceutical composition comprising glycerol esters of a fatty acid, wherein the compositions are useful for the delivery of anti-psychotic drugs. | 10-10-2013 |
| 20130267505 | PHARMACEUTICAL COMPOSITIONS COMPRISING BENZYL ALCOHOL - The present invention relates to a pharmaceutical composition comprising benzyl alcohol and polyoxyethylene derivatives of sorbitan esters of carboxylic acids that are useful for the delivery of anti-psychotic drugs. | 10-10-2013 |
| 20130267506 | THERAPEUTIC COMPOSITIONS FOR DIABETIC SYMMETRICAL POLYNEUROPATHY - Compositions for therapy of a diabetic symmetrical polyneuropathy a subject in need thereof, the compositions comprising: an effective amount of a muscarinic acetylcholine receptor antagonist exemplified by pirenzepine, telenzepine, atropine, or derivatives thereof or salts thereof or analogs thereof or derivatives thereof, and a pharmacologically acceptable carrier. The composition may be injectable or alternatively, may be applied topically or alternatively, may be delivered orally. A suitable topical composition may comprise a lotion, a cream, a gel, or a viscous fluid. The muscarinic acetylcholine receptor antagonist may be a muscarinic acetylcholine receptor antagonist salt or a muscarinic acetylcholine receptor antagonist derivative or a muscarinic acetylcholine receptor antagonist analog. | 10-10-2013 |
| 20130267507 | NOVEL ANTIFUNGAL 5,6-DIHYDRO-4H-PYRROLO[1,2-a][1,4]-BENZODIAZEPINES AND 6H-PYRROLO[1,2-a][1,4]BENZODIAZEPINES SUBSTITUTED WITH BICYCLIC BENZENE DERIVATIVES - The present invention is concerned with novel antifungal 5,6-dihydro-4H-pyrrolo-[1,2-a][1,4]benzodiazepines and 6H-pyrrolo[1,2-a][1,4]benzodiazepines substituted with bicyclic benzene derivatives of Formula (I) | 10-10-2013 |
| 20130274249 | SUBSTITUTED 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 useful for the prevention, alleviation, and curing of, for example, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases. | 10-17-2013 |
| 20130274250 | NOVEL ANTIFUNGAL 5,6-DIHYDRO-4H-PYRROLO[1,2-a][1,4]-BENZODIAZEPINES AND 6H-PYRROLO[1,2-a][1,4]BENZODIAZEPINES SUBSTITUTED WITH BENZENE DERIVATIVES - The present invention is concerned with novel antifungal 5,6-dihydro-4H-pyrrolo-[1,2-a][1,4]benzodiazepines and 6H-pyrrolo[1,2-a][1,4]benzodiazepines of Formula (I) | 10-17-2013 |
| 20130281439 | TOSYLATE SALT OF CYCLOPROPANECARBOXYLIC ACID 4-(6-CHLORO-3-METHYL-4, 10-DIHYDRO-3H-2,3,4,9-TETRABENZO[F]AZULENE-9-CARBONYL)-2-FLUOROBENZYLAMID- E - The invention provides cyclopropanecarboxylic acid 4-(6-chloro-3-methyl-4,10-dihydro-3H-2,3,4,9-tetraazabenzo[f]azulene-9-carbonyl)-2-fluoro-benzylamide para-toluenesulphonate, pharmaceutical compositions containing it, and its use in therapy. | 10-24-2013 |
| 20130281440 | DDX3 AS A BIOMARKER FOR CANCER AND METHODS RELATED THERETO - The invention encompasses methods for treating or preventing diseases and disorders associated abnormal cell growth, for example, treating or preventing cancer or tumor growth, by administering to a subject in need thereof a composition comprising a therapeutically or prophylactically effective amount of a compound that downregulates DDX3, for example a fused diimidazodiazepine ring compound or a pharmaceutically acceptable salt thereof. The invention also encompasses the use of DDX3 as a biomarker for diagnostic and treatment purposes, for example, to identify a hyperproliferative disorder susceptible to treatment by down regulation of DDX3. | 10-24-2013 |
| 20130281441 | DIAZEPINEDIONE DERIVATIVE - A diazepinedione derivative represented by the formula (I) or a pharmacologically acceptable salt thereof is used as a P2X | 10-24-2013 |
| 20130317011 | DIARYL ETHER LINKED PYRROLO [2,1-c][1,4] BENZODIAZEPINE HYBRIDS AND PROCESS FOR THE PREPARATION THEREOF - The present invention provides a compound of general formula A, useful as potential anticancer agents against eleven human cancer cell lines. The present invention further provides a process for the preparation of diaryl ether linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates attached through different alkane spacers of general formula A. | 11-28-2013 |
| 20130324520 | RXRG MODULATORS FOR THE TREATMENT OF CANCER - The present invention provides methods for treating cancer using modulators of retinoid X receptor gamma (RXRG). The ability of RXRG antagonists to disrupt the association of complexes comprising RXRG is demonstrated. | 12-05-2013 |
| 20130338149 | SEDATIVE 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. | 12-19-2013 |
| 20130345201 | PHARMACEUTICAL 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. | 12-26-2013 |
| 20130345202 | Flumazenil Complexes, Compositions Comprising Same And Uses Thereof - Soluble complexes of flumazenil, methods for the preparation thereof, pharmaceutical compositions including same and use of the compositions for alleviating or counteracting the various types of hypersomnia, drowsiness, residual effects associated with the administration of sleep/hypnotic drugs, alcohol intoxication or hepatic encephalopathy. | 12-26-2013 |
| 20140018352 | 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. | 01-16-2014 |
| 20140018353 | METHOD OF TREATING B-CELL MALIGNANT CANCERS AND T-CELL MALIGNANT CANCERS USING THIENOTRIAZOLODIAZEPINE COMPOUNDS - A method of treating B-cell malignant cancers or T-cell malignant cancers in a mammal by administering to a patient a pharmaceutically acceptable amount of a composition comprising (S)-2-[4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo-[4,3-a][1,4]diazepin-6-yl]-N-(4-hydroxyphenyl)acetamide. The B-cell malignant cancers include diffuse large B-cell lymphoma and splenic marginal zone lymphoma. The T-cell malignant cancers include anaplastic large T-cell lymphoma. | 01-16-2014 |
| 20140045827 | NOVEL ANTIFUNGAL 5,6-DIHYDRO-4H-PYRROLO[1,2-a][1,4]BENZO-DIAZEPINES AND 6H-PYRROLO[1,2-a][1,4]BENZODIAZEPINES SUBSTITUTED WITH HETEROCYCLIC DERIVATIVES - The present invention is concerned with novel antifungal 5,6-dihydro-4H-pyrrolo-[1,2-a][1,4]benzodiazepines and 6H-pyrrolo[1,2-a][1,4]benzodiazepines substituted with heterocyclic derivatives of Formula (I) | 02-13-2014 |
| 20140051689 | Polycyclic Agents for the Treatment of Respiratory Syncytial Virus Infections - Compounds of formula (I), and their use as in the treatment of infections involving viruses of the Pneumovirinae sub-family (RSV) are disclosed. In the formula ring (A) may be phenyl, pyridyl etc., (B-C) may be CH | 02-20-2014 |
| 20140057902 | Diazepinone derivatives - The invention relates to compound of the formula I | 02-27-2014 |
| 20140066435 | PYRROLOBENZODIAZEPINES USED TO TREAT PROLIFERATIVE DISEASES - Pyrrolobenzodiazepine dimers having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and a C2-C3 double bond and either a conjugated double or triple bond at the C2 position or an alkyl group at the C2 position on the other monomer unit, and conjugates of these compounds. | 03-06-2014 |
| 20140073633 | 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. | 03-13-2014 |
| 20140080813 | TRICYCLIC QUINOLINE AND QUINOXALINE DERIVATIVES - The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT | 03-20-2014 |
| 20140080814 | TRICYCLIC QUINOLINE AND QUINOXALINE DERIVATIVES - The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT | 03-20-2014 |
| 20140080815 | DOSING REGIMEN FOR SEDATION WITH CNS 7056 (REMIMAZOLAM) - The invention relates to a dosing regimen for sedation with the fast-acting benzodiazepine CNS 7056 in combination with an opioid, in particular fentanyl, whereas CNS 7056 is given in a dose of 2 to 10 mg, preferably between 4 and 9 mg and most preferably between 5 and 8 mg. | 03-20-2014 |
| 20140080816 | TRICYCLIC QUINOLINE AND QUINOXALINE DERIVATIVES - The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT | 03-20-2014 |
| 20140088089 | CYTOTOXIC BENZODIAZEPINE DERIVATIVES AND METHODS OF PREPARATION - The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds, such as those in formulas (V)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The present invention is further directed to methods of preparing a conjugate of a cell-binding agent and a cytotoxic compound. The methods comprise the use of an imine reactive compound to enable efficient conjugations of cytotoxic compounds with cell binding agents. | 03-27-2014 |
| 20140094452 | Rapid 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. | 04-03-2014 |
| 20140107106 | THERAPEUTIC AGENTS, AND METHODS OF MAKING AND USING THE SAME - In part, the present invention is directed to antibacterial compounds. | 04-17-2014 |
| 20140107107 | PHARMACEUTICAL FORMULATION CONTAINING THIENOTRIAZOLODIAZEPINE COMPOUNDS - A solid dispersion comprising an amorphous thienotriazolodiazepine compound of the Formula ( | 04-17-2014 |
| 20140107108 | COMPOSITIONS COMPRISING ALPRAZOLAM FOR TREATING PRIMARY INSOMNIA AND INSOMNIA ASSOCIATED 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. | 04-17-2014 |
| 20140128377 | METHODS OF TREATING REFRACTORY REPETITIVE SEIZURES - The present invention is directed to the use of a class of peptide Compounds for prevention, alleviation or/and treatment of refractory Status epilepticus. | 05-08-2014 |
| 20140128378 | METHODS OF TREATING EPILEPTOGENESIS - The present invention is directed to the use of a class of peptide Compounds for prevention, alleviation or/and treatment of refractory Status epilepticus. | 05-08-2014 |
| 20140135316 | BROMODOMAIN INHIBITORS AND USES THEREOF - The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders. | 05-15-2014 |
| 20140142090 | UNSYMMETRICAL PYRROLOBENZODIAZEPINE-DIMERS FOR TREATMENT OF PROLIFERATIVE DISEASES - The present invention is directed to novel pyrrolobenzodiazepine dimers and methods of using the dimers in the treatment of proliferative diseases. | 05-22-2014 |
| 20140155388 | METHODS AND COMPOSITIONS FOR SELF-REGULATED RELEASE OF ACTIVE PHARMACEUTICAL INGREDIENT - An abuse deterrent pharmaceutical composition including a pharmaceutically active ingredient; an acid soluble ingredient; and a buffering ingredient; wherein the acid soluble ingredient and the buffering ingredient retard release of the active pharmaceutical ingredient when the composition is ingested in excess of an intended dosage. | 06-05-2014 |
| 20140163013 | PROPHYLACTIC OR THERAPEUTIC AGENT FOR NEUROPATHIC PAIN ASSOCIATED WITH GUILLAIN-BARRE SYNDROME | 06-12-2014 |
| 20140163014 | BENZODIAZEPINE AND PYRIDODIAZEPINE DERIVATIVES - The present application relates to benzodiazepine and pyridodiazepine derivatives of formula (I) | 06-12-2014 |
| 20140171422 | PYRIMIDODIAZEPINONE COMPOUND - Provided are a compound represented by general formula (I), or the pharmaceutically acceptable salt thereof, | 06-19-2014 |
| 20140206674 | COMBINATIONS WITH 2-AMINOETHANESULFONIC ACID - The invention relates to a pharmaceutical combination of 2-aminoethanesulfonic acid with a pharmaceutical agent such as an antihypertensive agent and the use of 2-aminoethanesulfonic acid in a method to lower the bilirubin level in the blood. | 07-24-2014 |
| 20140235621 | HEMATOPOIETIC 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. | 08-21-2014 |
| 20140243321 | BIOORTHOGONAL MONOMERS CAPABLE OF DIMERIZING AND TARGETING BROMODOMAINS, AND METHODS OF USING SAME - Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins. | 08-28-2014 |
| 20140243322 | BIVALENT BROMODOMAIN LIGANDS, AND METHODS OF USING SAME - Described herein are compounds capable of modulating one or more biomolecules substantially simultaneously, e.g., modulating two or more binding domains (e.g., bromodomains) on a protein or on different proteins. | 08-28-2014 |
| 20140275042 | TRICYCLIC AND TETRACYCLIC SYSTEMS ACTING UPON THE VASCULAR AND CENTRAL NERVOUS SYSTEMS - Tricyclic and tetracyclic derivatives of benzodiazepine, pyridodiazepine, and pyrimidodiazepine fused with 1,4-dihydropyridine derivatives are disclosed. The present derivatives can be obtained from derivatives containing a dihydropyridine ring reacting with compounds of the ortho-phenyldiamine, ortho-diaminopyridine, and ortho-diaminopyrimidine type, as well as some subsequent transformations and, tricyclic and tetracyclic derivatives can be obtained with a diazepine or diazepinone nucleus fused to a 1,4-dihydropyridine nucleus, having a substituted or unsubstituted ring of benzene, pyridine or pyrimidine. The present derivatives exhibit vascular and central nervous system therapeutic activity. | 09-18-2014 |
| 20140296218 | SUPER-ENHANCERS AND METHODS OF USE THEREOF - The present invention relates in some aspects to super-enhancers and related compositions, methods, and agents that are useful for modulating expression of cell type-specific genes that are required for maintenance of cell identity (e.g., embryonic stem cell identity) or maintenance of a disease state (e.g., cancer). | 10-02-2014 |
| 20140296219 | COMPOUNDS 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. | 10-02-2014 |
| 20140315894 | ANTI-CANCER COMPOUNDS TARGETING RAL GTPASES AND METHODS OF USING THE SAME - The invention provides methods of inhibiting the growth or metastasis of a cancer in a mammal by inhibiting a Ral GTPase in the mammal. The invention also provides small molecule inhibitors of Ral GTPases useful in the methods of the invention and pharmaceutical compositions containing the therapeutically effective compounds of the invention, and methods of using the same. | 10-23-2014 |
| 20140323472 | METHODS 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. | 10-30-2014 |
| 20140329804 | NOVEL PHOSPHODIESTERASE INHIBITORS AND USES THEREOF - The invention provides for novel benzonaphthyridine derivatives and compositions comprising novel benzonaphthyridine derivatives. In some embodiments, the compounds are phosphodiesterase inhibitors. The invention further provides for methods for inhibition of phosphodiesterase comprising contacting phosphodiesterase with novel benzonaphthyridine derivatives or compositions comprising novel benzonaphthyridine derivatives. The invention further provides for methods for treatment of neurodegenerative diseases, increasing memory or long term potentiation with novel benzonaphthyridine derivatives or compositions comprising novel benzonaphthyridine derivatives. In some embodiments, the phosphodiesterase is PDE5. | 11-06-2014 |
| 20140336183 | Compositions And Method For Treatment Of Ischemic Neuronal Reperfusion Injury - A method and composition for the treatment of ischemic neuronal reperfusion injury are provided. The composition may include at least a benzodiazepine class material. In another form, the composition may include at least two components selected from the group consisting of an antagonist of the type 3 ryanodine receptor, an NMDA blocker (antagonist), and a benzodiazepine class material which can be administered for ischemic neuronal reperfusion injury. In one form, all three components may be used. | 11-13-2014 |
| 20140357625 | DIAZEPINONE DERIVATIVES - The invention relates to compound of the formula I | 12-04-2014 |
| 20140371210 | METHODS AND COMPOSITIONS FOR RAPID TRANSBUCCAL DELIVERY OF ACTIVE AGENTS - A method of rapid transbuccal delivery of an active agent into the bloodstream is provided. The method can include providing a pharmaceutical composition comprising the active agent, resin and a volatile solvent and, optionally, water. In some embodiments, the method achieves a Tmax 60 minutes or less, an onset of therapeutic effect of 60 minutes or less, and/or achieves therapeutic serum levels of the active agent within 60 minutes or less. Related compositions also are provided. | 12-18-2014 |
| 20140378443 | Novel Compositions and Methods of Treating HIV-1 Infections Using Same - The present invention includes novel compositions useful for preventing or treating an HIV-1 infection in a subject in need thereof. The present invention further includes a novel method of preventing or treating an HIV-1 infection in a subject in need thereof, the method comprising administering to the subject an effective amount of a compound of the invention. In one embodiment, the subject is further administered at least one additional therapeutic agent. | 12-25-2014 |
| 20150011536 | ANTITUMOR AZA-BENZO [F] AZULEN DERIVATIVE, METHOD FOR PREPARING SAME, AND USE THEREOF - The present invention relates to the field of pharmaceutical chemistry, and particularly to an aza-benzo[f]azulen derivative (I) and an antitumor effect thereof Pharmacological tests show that the compound of the present invention has in vitro and in vivo antitumor activities, and can be developed into clinical drugs for treating or controlling diseases such as stomach cancer, lung cancer, liver cancer, breast cancer, colon cancer, prostate cancer, and oral cancer. | 01-08-2015 |
| 20150045352 | COMPOSITIONS 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) | 02-12-2015 |
| 20150080384 | METHODS 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. | 03-19-2015 |
| 20150087636 | Inhibition of DUX4 Expression Using Bromodomain and Extra-Terminal Domain Protein Inhibitors (BETi) - The use of BETi as a potential treatment for FSHD is provided. Specifically, the use of BETi, and particularly selective BETi for BRD4, are shown to inhibit DUX4 expression which is expected to result in a decrease in the severity of symptoms of FSHD. Further, the treatments are shown to work when pulsed as opposed to continuous. This allows for a BETi to be supplied to a human in a pulse, and then allows the human to not need any additional treatment for a window at least as long as the one of the treatment pulse. | 03-26-2015 |
| 20150099741 | DIAGNOSING AND TREATING PATIENTS HAVING PSYCHIATRIC DISORDERS - Disclosed are methods and kits for diagnosing, prognosing, and treating patients having psychiatric disorders. The methods may include assessing whether a patient has a treatment resistant psychiatric disorder or assessing whether the patient is likely to develop a treatment resistant psychiatric disorder. The methods may include detecting genetic markers such as the single nucleotide polymorphism (SNP) in genes present in a genomic nucleic acid sample from the patient, and/or receiving, as a caregiver, the results of tests indicating whether the genetic markers are present in the genomic nucleic acid sample from the patient. The methods may include administering treatment to the patient, for example, based on the detected genetic markers, and administering treatment may include administering new antipsychotic drugs (APDs) that are trace amine-associated receptor 1 (TAAR1) agonists. | 04-09-2015 |
| 20150099742 | PHANTOM 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. | 04-09-2015 |
| 20150111880 | UNSYMMETRICAL PYRROLOBENZODIAZEPINE-DIMERS FOR TREATMENT OF PROLIFERATIVE DISEASES - A compound with the formula I: | 04-23-2015 |
| 20150126495 | PYRROLOBENZODIAZEPINES - A compound of formula (I) or a salt or solvate thereof, wherein the dotted double bond indicates the presence of a single or double bond between C2 and C3; R | 05-07-2015 |
| 20150126496 | DIAGNOSIS 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. | 05-07-2015 |
| 20150133434 | Compositions and Methods for Reactivating Latent Immunodeficiency Virus - The present disclosure provides compositions and methods for reactivating latent immunodeficiency vims. The methods generally involve contacting an HIV-infected cell in which HIV is latent with an agent that binds a bromodomain (BRD) in the cell. Latently infected cells contain replication-competent integrated HIV-1 genomes that are blocked at the transcriptional level, resulting in the absence of viral protein expression. The present disclosure provides methods for reducing the reservoir of latent immunodeficiency virus in an individual. | 05-14-2015 |
| 20150133435 | PYRROLOBENZODIAZEPINES - Pyrrolobenzodiazepine (PBDs) having a (1-methyl-1H-pyrrol-3-yl)phenyl based amino residue were found to be highly effective compounds having improved cytotoxicity ad DNA binding properties. | 05-14-2015 |
| 20150133436 | Bromodomain 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. | 05-14-2015 |
| 20150148338 | COMPOSITIONS COMPRISING SHORT-ACTING BENZODIAZEPINES - A composition is provided with a benzodiazepine and at least one hygroscopic excipient, in particular lactose and/or dextran. | 05-28-2015 |
| 20150290215 | METHODS 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. | 10-15-2015 |
| 20150315196 | UNSYMMETRICAL PYRROLOBENZODIAZEPINES-DIMERS FOR USE IN THE TREATMENT OF PROLIFERATIVE AND AUTOIMMUNE DISEASES - A compound of formula I: | 11-05-2015 |
| 20150320763 | TRICYCLIC 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. | 11-12-2015 |
| 20150328231 | PREVENTIVE OR THERAPEUTIC AGENT FOR PAIN ASSOCIATED WITH HERPES ZOSTER IN ACUTE PHASE | 11-19-2015 |
| 20150335656 | ANTITUMOR AGENT - The invention provides a method of inhibiting binding between acetylated histone and a bromodomain-containing protein in a mammal, as well as a method of shrinking or killing of cancer cells expressing a bromodomain-containing protein or inhibiting the growth of cancer cells expressing a bromodomain-containing protein in a mammal. The methods involve administering an effective amount of (S)-2-[4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]-N-(4-hydroxyphenyl)acetamide or a dihydrate thereof to the mammal. | 11-26-2015 |
| 20150342960 | DRUG COMBINATIONS FOR TREATMENT OF MELANOMA AND OTHER CANCERS - Presented herein are methods of treating cancer, for example, RAFi-resistant melanoma, using a combination of a bromodomain inhibitor such as JQ1, together with either a MEK inhibitor (e.g., MEKi) or a BRAF inhibitor (e.g., RAFi). These combinations were identified from candidate combinations produced by a cell type-specific, quantitative network model of signaling in cells (e.g., melanoma) to predict cellular response to untested combinatorial perturbations. | 12-03-2015 |
| 20150352038 | A DOSAGE FORM FOR ADMINISTERING AN ACTIVE PRINCIPLE FOR ACCELERATED SLEEP INDUCTION AND/OR FOR TREATING SLEEP DISORDERS AND/OR FOR TREATING A CENTRAL NERVOUS SYSTEM DISORDER - A dosage form for oral administration, via the mucous membranes, of an active principle for accelerated sleep induction and/or for treating sleep disorders and/or for treating a central nervous system disorder, the active principle being lipophilic or amphiphilic and being in a dissolved state that is stable and complete in a hydro-alcoholic solution having 35% to 70% by weight of ethanol and 30% to 65% by weight of water, generating nanostructures of the active principle under consideration within the hydro-alcoholic solution, thereby enabling the active principle to cross the blood-brain barrier, the active principle being in base and/or salt form and belonging to the chemical families of sleep inducers or modulators of lipophilic or amphiphilic type and of molecular weight that is less than 1000 Da, the active principle being selected from the families of Imidazopyridines, including Zolpidem, the family of Cyclopyrrolones, including Eszopiclone, the family of Pyrazolopyrimidines, including Zaleplon, the family of Benzodiazepines, including Midazolam and Brotizolam, the family of H1-antihistamine sedatives, including Doxylamine and Cyproheptadine, and/or the family of Melatonin and Melatonin agonists, including Melatonin, Ramelteon, and Agomelatine, the volume of the hydro-alcoholic solution being less than or equal to 2 mL, and the active principle being present at a dosage that is less than or equal to 8 mg, all of the active principle being absorbed in transmucosal manner via the mucous membranes of the floor of the oral cavity, in particular via the gums/cheeks, via the gum area, via the cheeks, or under the tongue. | 12-10-2015 |
| 20150359756 | USE OF CANNABINOIDS IN THE TREATMENT OF EPILEPSY - The present disclosure relates to the use of cannabidiol (CBD) in the treatment of absence seizures. In particular, the disclosure relates to the use of CBD for reducing absence seizures in patients suffering with etiologies that include: Lennox-Gastaut Syndrome; Tuberous Sclerosis Complex; Dravet Syndrome; Doose Syndrome; CDKL5; Dup15q; Jeavons syndrome; Myoclonic Absence Epilepsy; Neuronal ceroid lipofuscinoses (NCL) and brain abnormalities. The disclosure further relates to the use of CBD in combination with one or more anti-epileptic drugs (AEDs). | 12-17-2015 |
| 20150366877 | METHODS OF TREATMENT OF HUMAN CYTOMEGALOVIRUS INFECTION AND DISEASES WITH BROMODOMAIN INHIBITORS - Methods of inhibiting replication of human cytomegalovirus (HCMV) are disclosed. In various configurations, these methods comprise administering a therapeutically effective amount of a bromodomain inhibitor to a subject in need thereof. Bromodomain inhibitors including methyltriazolodiazepine-related compounds, 3,5-dimethylisoxazole-related compounds, 3-methyldihydroquinazolinone-related compounds, N-acetyl-2-methyltetrahydroquinoline-related compounds, quinazolone-related compounds, diazobenzene-related compounds, and triazolopyridazine-related compounds can be used to inhibit viral replication. | 12-24-2015 |
| 20150376208 | MK2 INHIBITORS AND USES THEREOF - The present invention provides compounds, compositions thereof, and methods of using the same. | 12-31-2015 |
| 20160002225 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that inhibit Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 01-07-2016 |
| 20160016954 | TRICYCLIC QUINOLINE AND QUINOXALINE DERIVATIVES - The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT | 01-21-2016 |
| 20160024011 | Multi-API Loading Prodrugs - The present invention accomplishes this by having multiple molecules of parent drugs attached to carrier moieties and by extending the period during which the parent drug is released and absorbed after administration to the patient and providing a longer duration of action per dose than the parent drug itself. Prodrug conjugates are suitable for sustained delivery of heteroaryl, lactam-amide-, imide-, sulfonamide-, carbamate-, urea-, benzamide-, acylaniline-, cyclic amide- and tertiary amine-containing parent drugs that are substituted at the amide nitrogen or oxygen atom with labile aldehyde-linked prodrug moieties. The carrier groups of the prodrugs can be hydrophobic to reduce the polarity and solubility of the parent drug under physiological conditions. | 01-28-2016 |
| 20160024073 | GAMMA-SECRETASE MODULATORS - There are provided, imer alia, compounds and methods for lowering total AB peptide production by inhibiting the catalytic activity of gamma-secretase. Since all of the major AB peptide variants, including the pathogenic AB42 as known in the art, are ultimately generated by gamma-secretase-mediated proteolysis of APP-C99 (i.e., the beta-secretase-mediated cleavage product of the amyloid protein precursor IAPPI), one approach to therapeutic intervention (e.g., intervention in Alzheimer's Disease, AD) relates to lowering total AB peptide production by inhibiting the catalytic activity of gamma-secretase. | 01-28-2016 |
| 20160024096 | METHODS AND COMPOSITIONS FOR INHIBITION OF BROMODOMAIN-CONTAINING PROTEINS - The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, 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. | 01-28-2016 |
| 20160032390 | SCHIZOPHRENIA-ASSOCIATED GENETIC LOCI IDENTIFIED IN GENOME WIDE ASSOCIATION STUDIES AND METHODS OF USE THEREOF - Compositions and methods for the identification of agents useful for the treatment of neurological disorders, including schizophrenia, are provided. | 02-04-2016 |
| 20160038508 | PHARMACEUTICAL 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. | 02-11-2016 |
| 20160045504 | COMPOSITIONS AND METHODS FOR TREATMENT OF LEUKEMIA - The invention relates generally to effective treatment leukemia. In particular, the present invention provides compositions and methods to inhibit the interaction of menin with MLL and MLL-fusion oncoproteins, and well as systems and methods to screen for such compositions. | 02-18-2016 |
| 20160052929 | BENZODIAZEPINE AND PYRIDODIAZEPINE DERIVATIVES - The present application relates to benzodiazepine and pyridodiazepine derivatives of formula (I) | 02-25-2016 |
| 20160058872 | IMIDE-BASED MODULATORS OF PROTEOLYSIS AND ASSOCIATED METHODS OF USE - The description relates to imide-based compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type. | 03-03-2016 |
| 20160060702 | METHODS, KITS, AND DEVICES FOR DIAGNOSING, PROGNOSING, AND TREATING PSYCHIATRIC DISORDERS IN A PATIENT - Disclosed are methods, kits, and devices for diagnosing and treating psychiatric, disorders and the symptoms thereof. The methods, kits, and devices relate to identifying genetic markers that may be utilized to diagnose and/or prognose a patient and treat the diagnosed and/or prognosed patient by administering a drug the patient based on the genetic marker having been identified. Genetic markers identified in the methods may include HTR2C polymorphisms such as a polymorphism resulting in a Cys23Ser amino acid substitution, an rs3813929 (−759C/T) polymorphism, and an rs518147 (−697G/C) polymorphism). | 03-03-2016 |
| 20160074415 | METHODS OF TREATMENT AND PHARMACEUTICAL COMPOSITIONS USING AN SGLT-2 INHIBITOR AND A NEUROLEPTIC AGENT - The invention relates to methods for preventing, slowing the progression of, delaying or treating metabolic disorders induced in patients by the treatment with neuroleptic agents comprising administering to the patients an SGLT2 inhibitor. | 03-17-2016 |
| 20160083386 | SUBSTITUTED BRIDGED UREA ANALOGS AS SIRTUIN MODULATORS - Provided herein are novel substituted bridged urea and related analogs and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 03-24-2016 |
| 20160083391 | TRICYCLIC PIPERAZINE DERIVATIVE - Disclosed are compounds useful as inhibitors of Phosphodiesterase 1 (PDE1), compositions thereof, and methods of using the same. | 03-24-2016 |
| 20160089379 | TREATMENT OF NEUROLOGICAL AND OTHER DISORDERS - Methods and implants for treating neurological, muscular and other cells having an electrical potential, with an infusion of antagonists or inverse agonists (such as flumazenil for the benzodiazepine receptor, or naltrexone for the opiate receptor or other antagonist for other receptor) at rates that are so low that only a small percentage of receptors have the antagonist effect at any one time. | 03-31-2016 |
| 20160106680 | Abuse Deterrent Immediate Release Formulation - The present invention relates to an immediate release orally administrable abuse-deterrent pharmaceutical formulation comprising: at least one pharmaceutically active ingredient susceptible to abuse; at least one gelling polymeric compound selected from the group consisting of: polysaccharides, sugars, sugar derived alcohols, starches, starch derivatives, cellulose derivatives, Carrageenan, pectin, sodium alginate, gellan gum, xanthan gum, poloxamer, Carbopol®, PolyOx®, povidone, hydroxypropyl methylcellulose (HPMC), hypermellose, and combinations thereof; at least one disintegrant and optionally at least one surfactant, wherein said formulation exhibit properties related to deterring the abuse, via injection or nasal inhalation when being tampered and exposed to aqueous, alcoholic, acidic and basic media. | 04-21-2016 |
| 20160106756 | BENZODIAZEPINES FOR TREATING SMALL CELL LUNG CANCER - The present invention relates to the use of a benzodiazepine compound, and its use in the treatment of cancer, particularly small cell lung cancer. | 04-21-2016 |
| 20160120877 | PHARMACEUTICAL COMPOSITIONS FOR SUSTAINED DELIVERY OF BENZODIAZEPINE ANTAGONISTS - The present invention relates to sustained release formulations of benzodiazepine antagonists and their use. | 05-05-2016 |
| 20160130282 | MERCAPTOAMIDINE DERIVATIVES AND METHODS OF USE - Compounds of formula (I) | 05-12-2016 |
| 20160152612 | NOVEL PHOSPHODIESTERASE INHIBITORS AND USES THEREOF | 06-02-2016 |
| 20160158245 | PHARMACEUTICAL FORMULATION CONTAINING THIENOTRIAZOLODIAZEPINE COMPOUNDS - A method of treating lymphoblastic leukemia, acute myeloid leukemia, BCR-ABL positive acute lymphoblastic leukemia or CD34 positive acute myeloid leukemia comprising the step of administering to a patient a pharmaceutically acceptable amount of a composition comprising a thienotriazolodiazepine compound according to Formula (1) as a solid dispersion wherein X is a halogen, R | 06-09-2016 |
| 20160158246 | METHOD OF TREATING DIFFUSE LARGE B-CELL LYMPHOMA (DLBCL) USING A BET-BROMODOMAIN INHIBITOR - A method of treating diffuse large B-cell lymphoma comprising administering to a patient a pharmaceutically acceptable amount of a composition comprising a thienotriazolodiazepine compound, said thienotriazolodiazepine compound being represented by Formula (I), wherein R | 06-09-2016 |
| 20160158248 | METHODS AND SYSTEMS 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. | 06-09-2016 |
| 20160159795 | DIAZEPINONE DERIVATIVES - The invention relates to compound of the formula I | 06-09-2016 |
| 20160176881 | SHORT-ACTING BENZODIAZEPINE SALTS AND THEIR POLYMORPHIC FORMS | 06-23-2016 |
| 20160199388 | METHODS AND COMPOSITIONS FOR SELF-REGULATED RELEASE OF ACTIVE PHARMACEUTICAL INGREDIENT | 07-14-2016 |
| 20160375032 | METHOD OF TREATING NON-SMALL-CELL LUNG CANCER USING PHARMACEUTICAL FORMULATION CONTAINING THIENOTRIAZOLODIAZEPINE COMPOUNDS - A method of treating non-small cell lung cancer in a mammal by administering to a patient a pharmaceutically acceptable amount of a compound being a thienotriazolodiazepine compound of the Formula (1) wherein R | 12-29-2016 |
| 20220133740 | VALPROIC ACID COMPOUNDS AND WNT AGONISTS FOR TREATING EAR DISORDERS - The present invention provides methods for treating diseases and disorders of the ear with valproic acid compounds and Wnt agonists. The present invention further provides kits for the same. | 05-05-2022 |
