35th week of 2014 patent applcation highlights part 57 |
Patent application number | Title | Published |
20140243302 | BRIDGED BICYCLIC COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS - Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions. | 2014-08-28 |
20140243303 | SPIROCYCLIC MOLECULES AS PROTEIN KINASE INHIBITORS - The present invention relates to spirocyclic compounds of formula I, namely spirocyclic (1H-pyrazol-4-yl)-3-(1-(2,6-dichloro-3-fiuorophenyl)ethoxy)pyridin-2-amines having protein kinase inhibitory activity, and methods of synthesizing and using such compounds. Preferred compounds are c-Met and/or ALK inhibitors useful for the treatment of abnormal cell growth, such as cancers. | 2014-08-28 |
20140243304 | INHALABLE AZTREONAM LYSINATE FORMULATION FOR TREATMENT AND PREVENTION OF PULMONARY BACTERIAL INFECTIONS - A method and a composition for treatment of pulmonary bacterial infections caused by gram-negative bacteria suitable for treatment of infection caused by | 2014-08-28 |
20140243305 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 2014-08-28 |
20140243306 | NOVEL PYRROLO PYRIMIDINE DERIVATIVES - The present invention describes new pyrrolo pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel pyrrolo pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors. | 2014-08-28 |
20140243307 | PYRAZOLE AZETIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to pyrazole azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 2014-08-28 |
20140243308 | SUBSTITUTED IMIDAZOPYRIDAZINES AND BENZIMIDAZOLES AS INHIBITORS OF FGFR3 - The present invention relates to substituted imidazopyridazines and substituted benzimidazoles, as well as pharmaceutical compositions comprising the same, which are FGFR3 inhibitors useful in the treatment of cancer and other diseases. | 2014-08-28 |
20140243309 | CYCLOALKYLNITRILE PYRAZOLE CARBOXAMIDES AS JANUS KINASE INHIBITORS - The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer. | 2014-08-28 |
20140243310 | BICYCLIC COMPOUND - The present invention provides a compound represented by the formula (I): | 2014-08-28 |
20140243311 | NOVEL OCTAHYDROTHIENOQUINOLINE DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING DERIVATIVE, AND USE OF THESE - The present invention provides compounds represented by the general formula (I): or pharmaceutical acceptable salts thereof, wherein R | 2014-08-28 |
20140243312 | PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES - Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them. | 2014-08-28 |
20140243313 | TRICYCLIC COMPOUNDS USEFUL AS NEUROGENIC AND NEUROPROTECTIVE AGENTS - The invention disclosed herein is direct to compounds of Formula I and pharmaceutically acceptable salts thereof, which are useful in treating neurodegenerative diseases and promoting the generation or survival of neurons in the mammalian brain. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula I or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to a method of promoting the generation or survival of neurons in a patient in need thereof in neurodegenerative and related diseases. | 2014-08-28 |
20140243314 | QUINOLINONE CARBOXAMIDE INHIBITORS OF ENDOTHELIAL LIPASE - The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments. | 2014-08-28 |
20140243315 | PYRROLOPYRIMIDINE COMPOUNDS FOR THE TREATMENT OF CANCER - The ectopic expression of Mer receptor tyrosine kinase (Mer) has been identified as a tumor cell survival gene product in Acute Lymphoblastic Leukemia (ALL) cells and a potential cause of ALL chemoresistance. Hence, we investigated whether the development of small molecule Mer inhibitors was possible. A first aspect of the present invention is a compound (sometimes referred to as an “active compound” herein) of Formula I, IA, or IB. | 2014-08-28 |
20140243316 | Tetrahydroimidazo(1,5-D)[1,4]Oxazepine Derivative - A compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof works as an mGluR2 antagonist, and is applicable as a therapeutic agent for neurological disorders related to glutamate dysfunction and diseases involving the mGluR2, such as Alzheimer's disease: | 2014-08-28 |
20140243317 | DIBENZOTHIAZEPINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CNS DISORDERS - A compound of formula I: | 2014-08-28 |
20140243318 | SALTS AND POLYMORPHS OF 8-FLUORO-2--1,3,4,5-TETRAHYDRO-6H-AZEPINO[5,4,3-CD]INDOL-6-ONE - The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer. | 2014-08-28 |
20140243319 | TREATMENTS TARGETING GAMMA-SYNUCLEIN EXPRESSION LEVELS - A combination treatment taking advantage of the synergistic effect of inhibiting γ-synuclein expression and chemotherapeutic agents to provide improved treatment of cancers, preferably stage III/IV cancers. A method for identifying improved cancer treatments. | 2014-08-28 |
20140243320 | NOVEL COMPOUND HAVING PARP INHIBITORY ACTIVITY - A compound represented by the following general formula (1) or a salt thereof. R | 2014-08-28 |
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. | 2014-08-28 |
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. | 2014-08-28 |
20140243324 | USE OF HEMATOPOIETIC GROWTH FACTOR MIMETICS - The present invention relates to uses of small molecule mimetics of hematopoietic growth factors. In particular the present invention relates to uses of small molecule mimetics of erythropoietin. | 2014-08-28 |
20140243325 | 1,3-Oxazines as Bace1 and/or Bace2 Inhibitors - The present invention provides 4-(3-Amino-phenyl)-5,6-dihydro-4H-[1,3]oxazin-2-ylamines of formula I | 2014-08-28 |
20140243326 | Synergistic Insecticidal Mixtures - The invention relates to insecticide mixtures comprising thiodicarb and at least one other known active ingredient from the category of chloronicotinyls, as well as the use of these mixtures to control animal pests. | 2014-08-28 |
20140243327 | RIMINOPHENAZINES WITH 2-(HETEROARYL) AMINO SUBSTITUENTS AND THEIR ANTI-MICROBIAL ACTIVITY - The present invention relates to riminophenazines having heteroaromatic substitutions, including those with 2-heteroaryl-amino substituents, to their preparation, and to their use as drugs for treating | 2014-08-28 |
20140243328 | IMIDAZOPYRIDINE DERIVATIVES, PROCESS FOR PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to compounds corresponding to formula (I): | 2014-08-28 |
20140243329 | SULFAMIDES AS TRPM8 MODULATORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: | 2014-08-28 |
20140243330 | PHOSPHOINOSITIDE 3-KINASE INHIBITOR WITH A ZINC BINDING MOIETY - The invention provides a compound of Formula I, | 2014-08-28 |
20140243331 | INHIBITORS OF INV(16) LEUKEMIA - This invention describes the development of targeted small molecule inhibitors of the inv(16) fusion, the causative agent in ˜12% of acute myeloid leukemia (AML). The inv(16) fusion results in expression of the CBFβ-SMMHC fusion protein in the blood cells of afflicted patients. The present invention provides compounds which inhibit the function of both CBFβ and the CBFβ-SMMHC fusion. These compounds block the growth of an inv(16) leukemia cell line as well as increase its apoptosis, while showing minimal effects against non inv(16) cell lines. As a mechanism to develop inhibitors with selectivity for the CBFβ-SMMHC fusion protein, the present invention further provides dimeric derivatives of these compounds which show both increased potency as well as selectivity for CBFβ-SMMHC. These compounds show potent inhibition of an inv(16) leukemia cell line with minimal effects on non inv(16) cell lines. Analysis of the pharmacokinetics of the developed compounds has made it possible to improve the lifetime of the compound in the plasma of mice to a level commensurate with long-term treatment. | 2014-08-28 |
20140243332 | METHODS OF TREATING CANCERS CHARACTERIZED BY ABERRENT ROS1 ACTIVITY - Disclosed herein are methods of treating cancers characterized by aberrant ROS1 activity by administering an effective amount of foretinib (N1′-[3-fluoro-4-[[6-methoxy-7-(3-morpholinopropoxy)-4-quinolyl]oxy]phenyl]-N1-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide), including methods of identifying mutations in the kinase domain of ROS1 that indicate resistance to crizotinib, but sensitivity to foretinib. | 2014-08-28 |
20140243333 | SYNTHESIS OF FUNCTIONALIZED OCTAHYDRO-ISOQUINOLIN-1-ONE-8-CARBOXYLIC ESTERS AND ANALOGS, AND THERAPEUTIC METHODS - A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject. | 2014-08-28 |
20140243334 | SUBSTITUTED HYDOXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I): | 2014-08-28 |
20140243335 | SUBSTITUTED HYDOXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I): | 2014-08-28 |
20140243336 | 2-Pyridyl Carboxamide-Containing Spleen Tyrosine Kinase (SYK) Inhibitors - The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase. | 2014-08-28 |
20140243337 | Phenyl Carboxamide-Containing Spleen Tyrosine Kinase (SYK) Inhibitors - The invention provides certain phenyl carboxamide-containing compounds of the Formula (I); or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase. | 2014-08-28 |
20140243338 | PHENYLPYRAZOLE DERIVATIVES AS POTENT ROCK1 AND ROCK2 INHIBITORS - The present invention provides compounds of Formula (I): | 2014-08-28 |
20140243339 | COMBINATIONS VEGF(R) INHIBITORS AND HEPATOCYTE GROWTH FACTOR (C-MET) INHIBITORS FOR THE TREATMENT OF CANCER - This invention is in the field of pharmaceutical agents and specifically relates to compounds, compositions, uses and methods for treating cancer, by combining VEGF(R) inhibitors and inhibitors of HGF/SF:c-Met. | 2014-08-28 |
20140243340 | CYTOCHROME P450 OXIDASE INHIBITORS AND USES THEREOF - The present invention features compounds of formula I | 2014-08-28 |
20140243341 | BROAD-SPECTRUM ANTIVIRALS AGAINST 3C OR 3C-LIKE PROTEASES OF PICORNAVIRUS-LIKE SUPERCLUSTER: PICORNAVIRUSES, CALICIVIRUSES AND CORONAVIRUSES - Antiviral protease inhibitors, including peptidyl aldehydes, peptidyl α-ketoamides, peptidyl bisulfite salts, and peptidyl heterocycles, are disclosed, along with related antiviral compounds, and methods of using the same to treat or prevent viral infection and disease. The compounds possess broad-spectrum activity against viruses that belong to the picornavirus-like supercluster, which include important human and animal pathogens including noroviruses, enteroviruses, poliovirus, foot-and-mouth disease virus, hepatitis A virus, human rhinovirus (cause of common cold), human coronavirus (another cause of common cold), transmissible gastroenteritis virus, murine hepatitis virus, feline infectious peritonitis virus, and severe acute respiratory syndrome coronavirus. | 2014-08-28 |
20140243342 | COMPOSITIONS AND METHODS FOR PROPHYLAXIS AND THERAPY FOR MENIERES DISEASE - Provided are articles of manufacture, compositions and methods for prophylaxis and/or therapy for disorders involving dizziness and/or vertigo. The articles of manufacture and compositions contain lamotrigine and/or bupropion and pharmaceutically acceptable salts thereof. The compositions include pharmaceutical compositions which are intended to alleviate dizziness and/or vertigo. In certain aspects the disclosure includes articles of manufacture and kits which include printed material which provides an indication that the articles or compositions are intended to be used for prophylaxis and/or therapy of Meniere's disease or a symptom thereof. | 2014-08-28 |
20140243343 | CYCLIC TRIAZO SODIUM CHANNEL BLOCKERS - The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The compounds are of formula I: | 2014-08-28 |
20140243344 | COMBINATION ALS THERAPY - Provided is a method for treating ALS in a subject, comprising administering to the subject a therapeutically effective amount of riluzole and a therapeutically effective amount of CK-2017357. Also provided are methods of reducing the variability of riluzole exposure (e.g., C | 2014-08-28 |
20140243345 | SELECTIVE HDAC3 INHIBITORS - Provided herein are HDAC3 inhibitors, as well as methods of treatment comprising administering these compounds to a subject in need thereof. | 2014-08-28 |
20140243346 | IP RECEPTOR AGONIST HETEROCYCLIC COMPOUNDS - The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed. Examples of compounds of the invention include the compounds according to Formula Ia, or a pharmaceutically acceptable salt thereof, and the compounds of the examples. | 2014-08-28 |
20140243347 | SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS - The present invention relates to substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them. | 2014-08-28 |
20140243348 | COMPOSITIONS AND METHODS FOR TREATING HERPES VIRUSES - Compositions and methods that are useful for the treatment of herpesvirus infection (including herpes simplex virii) are disclosed. Methods for identifying compounds useful for the treatment of herpesvirus infection are also disclosed. | 2014-08-28 |
20140243349 | GAMMA-DIKETONES AS WNT/BETA -CATENIN SIGNALING PATHWAY ACTIVATORS - The present disclosure provides γ-diketones or analogs thereof, that activate Wnt/β-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases. | 2014-08-28 |
20140243350 | USE OF SEROTONIN RECEPTOR AGONISTS FOR TREATMENT OF MOVEMENT DISORDERS - The present invention relates to the combined use of compounds which are activators of the KCNQ family potassium ion channels and compounds which are serotonin 5-HT1 receptor agonists. The combined use of KCNQ channel activators and 5-HT1 receptor agonists is useful in the treatment of for example movement disorders. The present invention further relates to pharmaceutical compositions, methods of treatments and kits of parts. | 2014-08-28 |
20140243351 | DRUG FOR THE TREATMENT OF ALLERGIC RHINITIS COMPRISING PGD2 ANTAGONIST AND HISTAMINE ANTAGONIST - A medicament for treating allergic rhinitis, characterized in that (A) a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof, is combined with (B) at least one compound selected from the group consisting of cetirizine, fexofenadine, and loratadine, or a pharmaceutically acceptable salt thereof. Since the effects of the medicament for treating allergic rhinitis of the present invention surpass the sum of the effects of single dose of each of the agents against the allergic rhinitis, the medicament is useful as a medicament for treating allergic rhinitis having potent effects. | 2014-08-28 |
20140243352 | METHODS FOR TREATING DIABETIC COMPLICATIONS WITH CARBAMOYLOXY ARYLALKANOYL ARYLPIPERAZINE COMPOUNDS - A pharmaceutical composition that includes a carbamoyloxy arylalkanoyl arylpiperazine compound and effectively prevents or treats diabetic nephropathy, diabetic neuropathy, diabetic vascular complications, hyperlipidemia, coronary artery disease, or inflammation. | 2014-08-28 |
20140243353 | 5- OR 6-SUBSTITUTED 3-HYDROXY-2(1H)-PYRIDINONES AS D-AMINO ACID OXIDASE (DAAO) INHIBITORS IN THERAPY OF DISEASES SUCH AS SCHIZOPHRENIA, COGNITIVE DISORDER AND PAID - The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R | 2014-08-28 |
20140243354 | COMBINATIONS OF INDIGO NATURALIS AND BERBERINE AND USES THEREOF - Methods and composition for treating or preventing an inflammatory dermatological disease or condition, such as psoriasis, in a subject are described. The methods involve topical applications to the subject a therapeutically effective amount of a composition comprising at least one indigo naturalis composition, beberine and a pharmaceutically acceptable carrier. | 2014-08-28 |
20140243355 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. 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. | 2014-08-28 |
20140243356 | USE OF TRANSLATIONAL PROFILING TO IDENTIFY TARGET MOLECULES FOR THERAPEUTIC TREATMENT - The present invention provides methods of identifying an agent that modulates an oncogenic signaling pathway in a biological sample by generating a translational profile of gene translational levels in the biological sample. The present invention also provides diagnostic and therapeutic methods using the translational profiling methods described herein. | 2014-08-28 |
20140243357 | SUBSTITUTED PYRAZOLO[3,4-D]PYRIMIDINES AND USES THEREOF - Presented herein are novel therapeutic compounds and methods of using the same for the treatment of cancers. | 2014-08-28 |
20140243358 | METHOD OF PREVENTING AND TREATING HEPATIC DISEASE USING A2B ADENOSINE RECEPTOR ANTAGONISTS - The invention is related to methods of preventing and treating hepatic fibrosis using A | 2014-08-28 |
20140243359 | ADENINE DERIVATIVES HAVING IMMUNOMODULATING ANTI-INFLAMMATORY AND ANALGESIC ACTIVITY - The compound 2-[1-(6-aminopurin-9-yl)-2-oxoethoxy]prop-2-enal of formula (I), its monohydrate of formula (II), or its corresponding cyclic monohydrate of formula (III), in which the stereochemical chiral center indicated with an asterisk can be R (Rectus), S (Sinister) or racemic, including the tautomers of the adenine ring and the pharmaceutically acceptable salts, are used in the treatment of inflammatory disorders or of pain disorders. | 2014-08-28 |
20140243360 | Heteroaryl Substituted Pyrrolo[2,3-B] Pyridines And Pyrrolo[2,3-B] Pyrimidines As Janus Kinase Inhibitors - The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 2014-08-28 |
20140243361 | POLYMORPHS OF ARRY-380, A SELECTIVE HERB2 INHIBITOR AND PHARMACEUTICAL COMPOSITIONS CONTIANING THEM - Polymorphs of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine are provided herein. Processes for preparing the polymorphs and pharmaceutical composition comprising the polymorphs are also disclosed. | 2014-08-28 |
20140243362 | SULFONAMIDE COMPOUNDS AND THEIR USE IN THE MODULATION RETINOID-RELATED ORPHAN RECEPTOR - The present invention is directed to novel retinoid-related orphan receptor gamma (RORγ) modulators of formula (I), processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by RORγ | 2014-08-28 |
20140243363 | METHODS AND COMPOSITIONS FOR TREATING ANXIETY DISORDERS OR SYMPTOMS THEREOF - The present invention relates to methods and compositions for reducing distress dysfunction, including emotional and physical distress. The invention entails co-administration of at least one Receptor Switcher and at least one Endorphin Enhancer. Additionally, at least one Synergistic Enhance and/or at least one Exogenous Opioid are also administered to enhance or prolong the therapeutic effects. | 2014-08-28 |
20140243364 | ENHANCED STABILITY OF NOVEL LIQUID COMPOSITIONS - The present invention relates to compositions of pharmaceutical agents in combination with additional pharmaceutical agents in a mixture of polyethylene glycol, polyvinylpyrrolidone, and propylene glycol and a process of making the compositions. | 2014-08-28 |
20140243365 | COMPOUNDS MODULATING C-FMS AND/OR C-KIT ACTIVITY AND USES THEREFOR - Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof. | 2014-08-28 |
20140243366 | COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity. | 2014-08-28 |
20140243367 | ANTIVIRAL DRUGS FOR TREATMENT OF ARENAVIRUS INFECTION - Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever. | 2014-08-28 |
20140243368 | PIPERIDINYL ALKYNE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to piperidinyl alkyne compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the piperidinyl alkyne compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 2014-08-28 |
20140243369 | SYNTHESIS OF A GLYCOSYLTRANSFERASE INHIBITOR - Process for the preparation of animinosugar, and the intermediates thereof, having known activity as a glycosyltransferase inhibitor and used, for example, in the treatment of Gaucher's disease. | 2014-08-28 |
20140243370 | Pyrano[3,2-D][1,3]thiazole as glycosidase inhibitors - Novel compounds of formula (I) | 2014-08-28 |
20140243371 | MICROBIOCIDAL PYRAZOLE DERIVATIVES - The present invention relates to compounds of formula (I) wherein R | 2014-08-28 |
20140243372 | BENZOIC ACID DERIVATIVE MDM2 INHIBITOR FOR THE TREATMENT OF CANCER - The present invention provides a MDM2 inhibitor compound, or a pharmaceutically acceptable salt thereof, which compound is useful as a therapeutic agent, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contains the MDM2 inhibitor. | 2014-08-28 |
20140243373 | CYCLIC AMINE DERIVATIVES AS EP4 RECEPTOR AGONISTS - There is described a group of novel cyclic amine derivative compounds having an EP | 2014-08-28 |
20140243374 | Novel Sulfonamides - This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of γ-secretase. | 2014-08-28 |
20140243375 | ISOXAZOLINE DERIVATIVES AS INSECTICIDAL COMPOUNDS - The present invention provides compounds of formula I wherein G | 2014-08-28 |
20140243376 | O-AMINO BENZONITRILE COMPOUNDS, METHOD FOR PREPARING SAME AND USES THEREOF - It relates to an anthranilonitrile compound, and to the process for preparing the said anthranilonitrile compound, and to its use. The anthranilonitrile compound has a chemical general formula (I). The compound of the general formula (I) has excellent pesticidal activity, can be used to control pests, and has more than 98% of mortality in 3 days to diamondback moth and pink borer. | 2014-08-28 |
20140243377 | DEUTERIUM-ENRICHED PIOGLITAZONE - The present application describes deuterium-enriched pioglitazone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 2014-08-28 |
20140243378 | Compositions and Methods for the Treatment of Muscular Disease, and Related Screening Methods - Disclosed are methods of treating a muscle disease and improving normal muscle function by administering a therapeutically effective amount of an isoprenoid antibiotic. Also disclosed are methods of upregulating hnRNP L and hnRNP L targets by administering a therapeutically effective amount of an isoprenoid antibiotic. Methods of screening compounds for use in treating muscle disease and improving muscle function are also described. | 2014-08-28 |
20140243379 | ADHESIVE MIXTURE FOR TRANSDERMAL DELIVERY OF HIGHLY PLASTICIZING DRUGS - Transdermal drug delivery patches and methods of their production are described. The patches can be made such that the accommodate highly plasticizing drugs such as selegiline and/or the use of protonated forms of various drugs. | 2014-08-28 |
20140243380 | COMBINATION THERAPY WITH NITRATED LIPIDS AND INHIBITORS OF THE RENIN-ANGIOTENSIN-ALDOSTERONE SYSTEM - The present technology provides compositions and methods for treating chronic kidney disease, end-stage renal disease, or diabetic nephropathy. The compositions comprise a nitrated lipid and an inhibitor of the renin-angiotensin-aldosterone system. The methods comprise administering a nitrated lipid in combination with an inhibitor of the renin-angiotensin-aldosterone system to a subject in need thereof, in an amount effective to treat diabetic nephropathy, chronic kidney disease, and/or end-stage renal disease. The use of a nitrated lipid with an inhibitor of the renin-angiotensin-aldosterone system exhibits a synergistic effect in treating chronic kidney disease and diabetic nephropathy. | 2014-08-28 |
20140243381 | FURYL AND THIENYL TRIAZOLE DERIVATIVES AND THERAPEUTIC USES THEREOF - Nitric oxide biosynthesis-inhibiting anti-inflammatory and anti-microbial compounds of Formula (3) and Formula (4) wherein R1 and R2 are independently selected from optionally substituted thienyl, optionally substituted furyl, optionally substituted —CH═CH-thienyl and optionally substituted provided that R2 is substituted with as nitro group | 2014-08-28 |
20140243382 | INHIBITORS OF C-FMS KINASE - The invention is directed to compounds of Formula I: | 2014-08-28 |
20140243383 | PHARMACEUTICAL COMPOSITIONS OF SILODOSIN - The present invention discloses a stable pharmaceutical composition comprising: (a) plurality of granules comprising silodosin or salts thereof and one or more pharmaceutical excipients; and (b) an extragranular portion comprising one or more lubricants and optionally one or more surfactants, wherein the granules are free of partially pregelatinized starch. | 2014-08-28 |
20140243384 | USE OF MELATONIN FOR TREATING AND/OR PREVENTING MUCOSITIS - The present invention relates to the use of a composition comprising melatonin or a derivative thereof at a proportion of 2.5% to 5% w/v for preparing a pharmaceutical composition for treating and/or preventing mucositis. The mucositis is preferably caused by radiotherapy and/or chemotherapy and preferably refers to oral mucositis. | 2014-08-28 |
20140243385 | Dithiol Compounds, Derivatives, and Uses Therefor - Dithiol compounds and derivatives thereof are disclosed. The agents are useful for treating ocular disease, especially presbyopia and cataract. Also disclosed are novel mercaptan compounds, particularly those including a photolabile protecting group, as well as methods of using the compounds for the prevention and treatment of ocular damage and disease. | 2014-08-28 |
20140243386 | PHARMACEUTICAL COMPOSITION COMPRISING ROTIGOTINE SALTS (ACID OR NA), ESPECIALLY FOR IONTOPHORESIS - The present invention relates to new salts of 6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol (rotigotine), their use as a medicament, for example for the treatment of CNS disorders like Parkinson Disease, RLS, fibromyalgia and/or depression, in particular through electromotive administration. The present invention relates to pharmaceutical formulations suitable for iontophoresis that provide enhanced iontophoretic delivery of rotigotine to at least one target tissue. The formulations are further characterized by good to excellent solubility of the salts in aqueous solutions. | 2014-08-28 |
20140243387 | METHODS FOR IMPROVING CARDIAC CONTRACTILITY - The present invention relates to regulation of cardiac contractile function. The present invention is based on the discovery that microRNAs contribute to the loss of cardiac contractility. Specifically, miR-25 binds to SERCA2a which results in a loss of function and interferes with Ca | 2014-08-28 |
20140243388 | ANTISENSE OLIGONUCLEOTIDES THAT TARGET A CRYPTIC SPLICE SITE IN USH1C AS A THERAPEUTIC FOR USHER SYNDROME - The present invention provides a method for treating Usher's syndrome in a human subject including administering to the human subject an oligonucleotide having 8 to 30 linked nucleosides having a nucleobase sequence comprising a complementary region comprising at least 8 contiguous nucleobases complementary to a target region of equal length within exon 3 of an Usher RNA transcript. | 2014-08-28 |
20140243389 | COMPOSITIONS COMPRISING EICOSAPENTAENOIC ACID AND MIPOMERSEN AND METHODS OF USE THEREOF - The present invention relates to, inter alia, pharmaceutical compositions comprising a polyunsaturated fatty acid and to methods of using the same to treat or prevent cardiovascular-related diseases. | 2014-08-28 |
20140243390 | NOVEL KIF5B-RET FUSION MOLECULES AND USES THEREOF - Novel RET fusion molecules and uses are disclosed. | 2014-08-28 |
20140243391 | PHOSPHOLIPID-DETERGENT CONJUGATES AND USES THEREOF - The invention relates to novel compounds, in particular novel O-substituted phospholipids that are useful for the in vitro and in vivo delivery of drugs as well as nucleic acids into cells. The invention also relates to pharmaceutical compositions and supramolecular complexes comprising said compounds and the use of these compounds in therapeutic treatment, in particular in gene therapy. | 2014-08-28 |
20140243392 | MicroRNA-Based Methods and Assays for Osteosarcoma - Provided are methods and compositions useful in the diagnosis, treatment, and monitoring of osteosarcoma. Antisense to certain microRNA (miRNA) found to be associated with cancer stem cells (CSCs) or tumor-initiating cells (TICs) of osteosarcoma are useful to suppress tumor growth and metastasis, and prolong survival. Antisense oligonucleotides to miR-133a are synergistic in combination with standard chemotherapy such as cisplatin in the treatment of osteosarcoma. | 2014-08-28 |
20140243393 | METHODS OF DIAGNOSING AND TREATING MOTOR NEURON DISEASES - Use of an agent which upregulates an activity or amount of miRNA-9 or miRNA-9* is disclosed for the preparation of a medicament for the treatment of a motor neuron disease (MND). | 2014-08-28 |
20140243394 | Compositions and Methods for Inhibiting Expression of a Gene from the Ebola Virus - The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of a gene from the Ebola virus. | 2014-08-28 |
20140243395 | SPRAY SYSTEM FOR PRODUCTION OF A MATRIX FORMED IN SITU - A spray system for production of a matrix formed in situ is described, which comprises at least one lipophilic component comprising at least one polymer based on glycolic acid and lactic acid and at least one biocompatible solvent having an X log P3 value of less than 0.2, and at least one hydrophilic component, wherein the at least two components are present separately from each other prior to use and are not mixed until or in the course of spraying, with components forming a film when sprayed onto human tissue. | 2014-08-28 |
20140243396 | METHOD OF TREATING MUCOEPIDERMOID CARCINOMA - Imidazoquinolines, as set forth in formula (I), are useful for inhibiting growth or proliferation of mucoepidermoid carcinoma cells. The therapeutic and prophylactic treatments provided by this invention are practiced by administering to a patient in need thereof an amount of a compound of formula (I) that is effective to inhibit growth or proliferation of the mucoepidermoid carcinoma cells. | 2014-08-28 |
20140243397 | CXCR4 INHIBITING CARRIERS FOR NUCLEIC ACID DELIVERY - The present invention generally relates to carriers including polymers and lipids that comprise a CXCR4 inhibiting moiety. More specifically, these carriers are biodegradable and can be bioreducible polymers that comprise a CXCR4 inhibiting moiety. These carriers can be suitable for delivery of nucleic acids to cells. These carriers and pharmaceutical compositions can be used to treat various conditions including cancers and inflammation conditions. | 2014-08-28 |
20140243398 | IRS MODULATORS - This invention is directed to a general method for the chronic treatment, potential cure, or prevention of various metabolic and related diseases in people, including diabetes, by modulating IRS2 activity in cells and tissues in the body. IRS1 and IRS2 are part of the insulin or insulin-like growth factor signaling pathway. By upregulating the levels or functional activity of IRS2, insulin is used more efficiently by the body to control nutrient levels. By upregulating IRS2 levels or functional activity in pancreatic β-cells, glucose sensing and insulin secretion are enhanced. | 2014-08-28 |
20140243399 | ENGINEERED NUCLEIC ACIDS AND METHODS OF USE THEREOF - Provided are compositions and methods for delivering biological moieties such as modified nucleic acids into cells to modulate protein expression. Such compositions and methods include the use of modified messenger RNAs, and are useful to treat or prevent diseases, disorders or conditions, or to improve a subject's heath or wellbeing. | 2014-08-28 |
20140243400 | COMPOSITIONS COMPRISING CITRIC ACID AND MALIC ACID AND METHODS AND USES THEREOF - The invention relates to compositions comprising at least about 500 mg of citric acid; at least about 500 mg of malic acid; and at least about 100 mg of N-acetylcysteine, or at least about 100 mg of α-lipoic acid, or a mixture thereof and methods for use of the compositions thereof. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2014-08-28 |
20140243401 | METHODS OF SCREENING COMPOUNDS THAT ARE CYTOTOXIC TO TUMOR CELLS AND METHODS OF TREATING TUMOR CELLS USING SUCH COMPOUND - The invention relates to methods of screening to find compounds that are cytotoxic to tumor cells and methods of treating tumor cells using these compounds. In particular, the invention relates to methods of screening for compounds that inhibit mammalian mitochondrial fatty acid synthase (mmFAS) and methods of treating tumor cells using mmFAS inhibitors. This invention also provides methods for inhibiting or preventing cancer cell survival by the administration of mitochondrial fatty acid synthase (FAS) inhibitors. Specifically, this invention describes a method for prohibiting or delaying the development of cancer, the growth of cancer or invasion of cancer from pre-malignant (noninvasive) lesions, or metastasis of cancer based upon the findings that this method compromises energy balance in cancer cells, in turn compromising their basic functions and causing their cell death. Compositions of matter containing mitochondrial FAS inhibition activity are also provided, as well as applications based upon the requisite role of mitochondrial FAS in cancer cell homeostasis. | 2014-08-28 |
20140243402 | Artemisinins in the Clinical and Veterinary Management of Kinetoplastid Infextions - The invention relates to the treatment of kintoplastid infections by administering a pharmaceutical composition containing an extract from the plant | 2014-08-28 |