52nd week of 2013 patent applcation highlights part 51 |
Patent application number | Title | Published |
20130345143 | MODULATION OF p62 FUNCTION THROUGH THE PB1 DOMAIN - Provided are methods, compositions, and kits employing a molecule that exhibits a function of the PB | 2013-12-26 |
20130345144 | Use of ID4 for Diagnosis and Treatment of Cancer - Methods for diagnosis and treatment of cancer using ID4 are disclosed. Specifically, epigenetic inactivation of ID4 in colorectal carcinomas and breast correlates with poor differentiation and unfavorable prognosis. Further, aberrant hypermethylation of ID4 gene promoter region increases risk of metastasis in colorectal and breast cancer. | 2013-12-26 |
20130345145 | ATIP3 AND BIOLOGICALLY ACTIVE FRAGMENTS THEREOF FOR USE IN THE TREATMENT OF CANCER - The present invention concerns a combination of (i) a polypeptide comprising ATIP3 or a biologically active fragment thereof, and (ii) a chemotherapeutic drug that is an antimitotic agent, for simultaneous or sequential use in the treatment of a patient suffering from cancer, e.g. a triple-negative breast cancer. The present invention also relates to a polypeptide comprising ATIP3 or a biologically active fragment thereof, for use in sustaining drug effect, increasing or restoring or enhancing sensitivity of a patient suffering from cancer to a chemotherapeutic drug that is an anti-mitotic agent. The present invention further provides biologically active polypeptides that comprise or consist of fragments of ATIP3, and antibodies binding thereto. | 2013-12-26 |
20130345146 | NEAR-INFRARED ELECTROMAGNETIC MODIFICATION OF CELLULAR STEADY-STATE MEMBRANE POTENTIALS - Systems and methods are disclosed herein for applying near-infrared optical energies and dosimetries to alter the bioenergetic steady-state trans-membrane and mitochondrial potentials (ΔΨ-steady) of all irradiated cells through an optical depolarization effect. This depolarization causes a concomitant decrease in the absolute value of the trans-membrane potentials ΔΨ of the irradiated mitochondrial and plasma membranes. Many cellular anabolic reactions and drug-resistance mechanisms can be rendered less functional and/or mitigated by a decrease in a membrane potential ΔΨ, the affiliated weakening of the proton motive force Δp, and the associated lowered phosphorylation potential ΔGp. Within the area of irradiation exposure, the decrease in membrane potentials ΔΨ will occur in bacterial, fungal and mammalian cells in unison. This membrane depolarization provides the ability to potentiate antimicrobial, antifungal and/or antineoplastic drugs against only targeted undesirable cells. | 2013-12-26 |
20130345147 | PREVENTION AND TREATMENT OF OCULAR SIDE EFFECTS WITH A CYCLOSPORIN - Therapeutic methods are disclosed herein. | 2013-12-26 |
20130345148 | PREVENTION AND TREATMENT OF OCULAR SIDE EFFECTS WITH A CYCLOSPORIN - Therapeutic methods are disclosed herein. | 2013-12-26 |
20130345149 | SILICONE-BASED OPHTHALMIC FORMULATIONS - Compositions, products and methods including silicone based excipients are provided. The compositions, products and methods of the present invention are particularly useful for the treatment of ophthalmic diseases. | 2013-12-26 |
20130345150 | OPHTHALMIC COMPOSITION - An ophthalmic composition comprising a polyaphron dispersion. | 2013-12-26 |
20130345151 | PREPARATION FOR ORAL ADMINISTRATION COMPRISES QUERCETIN GLYCOSIDE AND A WATER BASED SOLVENT EXTRACT OF CARTILAGE CONTAINING CHONDROITIN SULFATE - It is an object of the present invention to provide a preparation for oral administration in which the bitter taste derived from quercetin glycoside is improved. | 2013-12-26 |
20130345152 | COMPOSITIONS COMPRISING RECOMBINANT COWPOX VIRUS PROTEIN CPXV014 - Disclosed herein are expression vectors that encode cowpox virus protein CPXV014 and homologs thereof that are useful in inhibiting CD3/CD28 mediated T cell stimulation. Further disclosed are polypeptide compositions comprising CPXV014 and homologs thereof as well as methods of inhibiting CD3/CD28 mediated T cell stimulation using the polypeptide compositions. | 2013-12-26 |
20130345153 | TOPICAL PREVENTATIVE MEDICAMENT AGAINST BURNS-RELATED SYSTEMIC INFLAMMATORY RESPONSE SYNDROME - A topical preventative medicament against burns-related systemic inflammatory response syndrome containing a low-molecular-weight chaperone as the main active ingredient. | 2013-12-26 |
20130345154 | Gap Junction-Enhancing Agents for Treatment of Necrotizing Enterocolitis and Inflammatory Bowel Disease - The present invention relates to methods of reducing the risk of occurrence of, and/or treating, necrotizing enterocolitis (“NEC”) or inflammatory bowel disease (“IBD”) comprising administering, to a subject in need of such treatment, an effective amount of a gap junction enhancing agent (“GJEA”), for example a peptide (“GJP”) or peptide analog (“GJPA”). It is based, at least in part, on the discovery that greater functionality of gap junctions between enterocytes increases their rate of migration and reduces the severity of intestinal inflammation. | 2013-12-26 |
20130345155 | MODULATORS FOR SIRT6 AND ASSAYS FOR SCREENING SAME - Method for identifying a modulator of Sirt6, PfSir2a, or Sirt7 deacylase activity, wherein a fatty-acylated substrate containing an acyl-lysine moiety and an indicator moiety is contacted with Sirt6, PfSir2a, or Sirt7 in the presence of a candidate compound under conditions for Sirt6, PfSir2a, or Sirt7 to deacylate the substrate, wherein the acyl is a hydrophobic fatty acyl group containing a hydrocarbon group having at least three carbon atoms connected by carbon-carbon bonds; contacting the deacylated substrate with a cleavage agent that cleaves the linkage between the lysine and indicator moiety to generate a detectable signal; and correlating a quantified Sirt6, PfSir2a, or Sirt7 deacylase activity therefrom. Modulating compounds of Sirt6, PfSir2a, or Sirt7 deacylase activity are also described, as are pharmaceutical compositions thereof, methods of treatment by administration of the modulating compounds, and kits for practicing the method. | 2013-12-26 |
20130345156 | AQUEOUS SOLUTION OF 20(R)-GINSENOSIDE RG3 PHARMACEUTICAL COMPOSITION AND PROCESS THEREOF - A preparation of a kind of 20(R)-ginsenoside Rg3 medicinal composition aqueous solution containing ginsenoside Rg3 0.5˜10 mg/ml: add 0.1-5% of ginsenoside solution to 0.1˜30% of adjuvant A, B{circle around (1)}{circle around (2)}{circle around (5)} at the temperature of 40˜100° C., the ratio of these two is 1:1˜300, add water after the solvent is recycled under reduced pressure; another kind of 20(R)-ginsenoside Rg3 medicinal composition aqueous solution contains 0.1˜2 mg/ml of 20 (R) of the ginsenoside Rg3, the preparation: add 0.1˜5% of ginsenoside solution to 20˜65% of adjuvant B{circle around (3)}{circle around (4)} at the temperature of 60˜100° C., main material to adjuvant B=1:100˜400, add water after the solvent is recycled under reduced pressure. The above 20 (R) ginsenoside Rg3 composition aqueous solution and the powder after lyophilizaton can be used to prepare injectable, oral administration and external use, and the bioactivity of these preparations is high, and with the actions of anti cancer, efficacy potentiation and toxicity attenuation effects of the combined chemical or radiation therapy of tumor, enhancement of human immune functions, improvement of human memory, anti fatigue, and detumescence, pain relieving. | 2013-12-26 |
20130345157 | HYDROXYL, KETO, AND GLUCURONIDE DERIVATIVES OF 3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROP- ANENITRILE - The present invention provides hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile. | 2013-12-26 |
20130345158 | COMPOSITION FOR PROMOTING HEMATOGENESIS CONTAINING QUERCETIN 3-O-beta-(2''-GALLOYL)-RHAMNOPYRANOSIDE AS ACTIVE INGREDIENT - This invention relates to a composition for promoting hematopoiesis and for treating, preventing or alleviating cytopenia or bone marrow failure comprising quercetin 3-O-β-(2″-galloyl)-rhamnopyranoside (QGR) as active ingredient. The present active compound QGR (i) increases dose dependently the mRNA expression of cytokines involved in hematopoiesis including stem cell factor, granulocyte-macrophage colony stimulating factor and erythropoietin from mouse bone marrow mononuclear cells, (ii) promotes the formation of burst forming unit-erythroid and colony forming unit-fibroblast, (iii) stimulates the generation of cells positive for TER-119, a specific marker of mouse erythroid precursors, (iv) promotes erythropoiesis, leukopoiesis, thrombopoiesis, and hemoglobin production in bone marrow failure mouse model, (v) stimulates the formation of hematopoietic stem/progenitor cells and mesenchymal stem/progenitor cells, (vi) stimulates megakaryocyte formation surrounding the blood system of damaged bone marrow, osteoid formation and bone marrow restoration through a recovery of damaged bone marrow microenvironment. The QGR of the present invention can be used for promoting hematopoiesis and treating cytopenia or bone marrow failure. | 2013-12-26 |
20130345159 | PURIFIED CARDIOGENIN ISOMER AND RELATED METHODS - A cardiogenin major isomer is obtained from a methanol extract of | 2013-12-26 |
20130345160 | GLYCYRRHIZIN HIGH-CONCENTRATION PREPARATION - To provide a glycyrrhizin/aminoacetic acid/cysteine combination drug containing an active ingredient in high concentration and excelling in stability and safety. Stability at compounding of active ingredient in high concentration has been improved by avoiding the addition of sulfite salts having been used as a stabilizer in existing products. As glycyrrhizin high-concentration preparations, there is provided a drug composition comprising 8 to 16 mg/mL of glycyrrhizin, 3 to 6 mg/mL of cysteine and 80 to 160 mg/mL of aminoacetic acid wherein no sulfite salts are added as an additive, and pH is 6 to 7. | 2013-12-26 |
20130345161 | Methods of Treating Breast Cancer With Taxane Therapy - The application describes methods for screening subjects with breast cancer to determine if the breast cancer will be responsive to a breast cancer therapy including a taxane or a taxane derivative. The application also describes methods for treating subjects with breast cancer by screening them for the likelihood of the effectiveness of treating the cancer with a therapy including a taxane or a taxane derivative and administering the therapy in subjects when it is found that a taxane or a taxane derivative is likely to be effective. | 2013-12-26 |
20130345162 | NOVEL ANTI-VIRAL THERAPEUTIC - Anti-viral therapeutics for use in viral targets having VPg unlinkase activity, including the broad class of picornaviruses, and therapeutic methods directed at suppression of such activity are provided. Such anti-viral therapies for use against human rhinovirus, for example, are particularly desirable as they would lessen both the severity and duration of upper respiratory distress in both normal and asthmatic individuals. Assays and purification protocols for detecting and purifying VPg unlinkase are also provided. | 2013-12-26 |
20130345163 | BIOLOGICAL MARKER FOR INFLAMMATION - Inflammatory state in a subject is assayed by determining the level of expression of A | 2013-12-26 |
20130345164 | TREATMENTS FOR CELLULAR PROLIFERATIVE DISORDERS AND IDENTIFICATION THEREOF - This invention concerns methods of identifying treatments for treating various disorders and related computer products and systems. Also disclosed are methods for treating cellular proliferative disorders and use of compounds identified for such treatment. | 2013-12-26 |
20130345165 | COMBINATION THERAPEUTIC COMPOSITION - Embodiments disclosed in the present application relate to a composition that can include a hepatitis C viral nucleoside polymerase inhibitor, or pharmaceutically acceptable salt or prodrug thereof, a hepatitis C viral protease inhibitor, or pharmaceutically acceptable salt or prodrug thereof, and a hepatitis C viral non-nucleoside polymerase inhibitor, or pharmaceutically acceptable salt or prodrug thereof. Additional embodiments disclosed relate to methods for treating a disease condition such as a hepatitis C virus infection, liver fibrosis and/or impaired liver function with a hepatitis C viral nucleoside polymerase inhibitor, or pharmaceutically acceptable salt or prodrug thereof, a hepatitis C viral protease inhibitor, or pharmaceutically acceptable salt or prodrug thereof, and a hepatitis C viral non-nucleoside polymerase inhibitor, or pharmaceutically acceptable salt or prodrug thereof. | 2013-12-26 |
20130345166 | METHODS OF TREATING HEPATIC ENCEPHALOPATHY - The application describes treatment of hepatic encephalopathy using gastrointestinal specific antibiotics. One example of a gastrointestinal specific antibiotic is rifaximin. The instant application also provides methods for determining if a subject has a neurological condition or hepatic encephalopathy by determining the critical flicker frequency and/or the venous ammonia level of the subject at two or more time points. The invention further provides methods for treating these subjects. | 2013-12-26 |
20130345167 | HYPERSULFATED DISACCHARIDE FORMULATIONS - Hypersulfated disaccharides with utility in asthma or asthma related disorders are disclosed. The compounds are formulated with agents that enhance the oral delivery of the hypersulfated disaccharides. The delivery agents are selected from the group consisting of natural or synthetic polymers having ionic side chains as well as other compounds or types of compounds that improve the bioavailability of the disaccharides relative to delivery of the drug without such agents. The hypersulfated disaccharides are made from heparin or salts thereof. | 2013-12-26 |
20130345168 | COSMETIC COMPOSITION FOR PREVENTING SKIN AGING CONTAINING CHITOOLIGOSACCHARIDES - The present invention relates to a composition for preventing skin aging containing chitooligosaccharides as an active ingredient. The invention provides a cosmetic composition for preventing skin aging caused by UV rays containing chitooligosaccharides of 1-3 kDa, 3-5 kDa or 5-10 kDa molecular weight as an active ingredient. | 2013-12-26 |
20130345169 | Article Suitable for Oral Administration - A material which contains a lipophilic component having a pungent taste or flavor such as a spicy component (e.g., a capsaicin) and a bitter component (e.g., a turmeric extract), in which the pungent taste and/or flavor of the lipophilic component can be reduced effectively, and in which the separation among components contained therein is not caused; a method for producing the material; a composition such as a food, a beverage, a cosmetic and a medicine, which contains the material; and a liquid composition having such a form that the material is dispersed in water. | 2013-12-26 |
20130345170 | Ear Pieces Having an Antimicrobial Treatment - A hearing aid, ear bud, ear plug, and hands-free headset are provided that may include one or more surfaces coated with an antimicrobial treatment, which may include a silane quaternary ammonium salt and isopropyl alcohol. The silane quaternary ammonium salt may include an unreacted organofunctional silane to promote bonding to the surfaces of the ear piece, such as 3-(trimethoxysilyl) propyldimethyloctadecyl ammonium chloride. Methods are also provided for coating, or otherwise integrating the antimicrobial treatment on or within a hearing aid, ear bud, ear plug, and hands-free headset. | 2013-12-26 |
20130345171 | TREATMENT AND PREVENTION OF CARDIOVASCULAR DISEASE AND THROMBOSIS - Provided herein are compositions for the treatment and/or prevention of cardiovascular disease (CVD), and methods of application and use thereof. In particular, the present invention provides treatment and/or prevention of cardiovascular disease with compounds that inhibit the production of TMA in the gut, such as 3,3-dimethyl-1-butanol (DMB) or other compounds represented by Formula I or as shown in FIGS. | 2013-12-26 |
20130345172 | CYCLIC BORONIC ACID ESTER DERIVATIVES AND THERAPEUTIC USES THEREOF - Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to 1 cyclic boronic acid ester derivatives and their use as therapeutic agents. | 2013-12-26 |
20130345173 | INHIBITORS OF FATTY ACID AMIDE HYDROLASE - Provided herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof, or mixtures thereof, wherein Z | 2013-12-26 |
20130345174 | PROTEASOME INHIBITOR DELANZOMIB FOR USE IN THE TREATMENT OF LUPUS - The present invention provides a method for treating lupus in a subject, comprising the step of administering to the subject Compound A. | 2013-12-26 |
20130345175 | Methods for Improving Diabetes Management - A method for determining the levels of biomarkers, specifically, advanced glycation end products (AGEs) and oxidation products (Ops) in a biological sample such as a plasma ultrafiltrate, is used to determine a patient's risk and/or rate of developing diabetes related nephropathy. The preferred biomarkers to measure include N | 2013-12-26 |
20130345176 | NOVEL ESTERS OF 4, 9-DIHYDROXY-NAPHTHO [2, 3-b] FURANS FOR DISEASE THERAPIES - The present invention discloses esters of 4,9-dihydroxy-naphtho[2,3-b]furans and methods of making and using the same. The present invention also discloses conversion of the esters into therapeutically active 4,9-dihydroxy-naphtho[2,3-b]furans in vivo. The present invention furthermore discloses pharmaceutical compositions comprising the esters of 4,9-dihydroxy-naphtho[2,3-b]furans for the treatment of various indications including proliferative diseases. | 2013-12-26 |
20130345177 | Oleyl Phosphocholine for the Treatment of Mycosis - The present invention relates to the use of oleyl phosphocholine (C18:1-PC), or OlPC,for the treatment of mycosis, and especially for the treatment of mycosis such as mycosis caused by pathogens belonging to a genus selected from the group consisting of | 2013-12-26 |
20130345178 | 8-AZA Tetracycline Compounds - The present invention is directed to a compound represented by Structural Formula (I): | 2013-12-26 |
20130345179 | Substituted tetracycline compounds for treatment of inflammatory skin disorders - Methods and compositions for the treatment of skin disorders (e.g., acne, rosacea) are described. | 2013-12-26 |
20130345180 | 2,4- DIAMINOPYRIMIDINE DERIVATIVES - There are provided compounds of formula I | 2013-12-26 |
20130345181 | PYRROLOPYRIDINEAMINO DERIVATIVES AS MPS1 INHIBITORS - The present invention relates to the use of certain pyrrolopyridineamino derivatives (hereinafter referred to as “PPA derivatives”), particularly 1H-pyrrolo[3,2-c]pyridine-6-amino derivatives, to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps kinase itself. In particular, the present invention relates to PPA derivatives for use as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of the PPA derivatives, and pharmaceutical compositions comprising them. Formula (I) | 2013-12-26 |
20130345182 | STABLE COMPOSITION COMPRISING CHOLESTEROL-LOWERING AGENTS, ANTIHYPERTENSIVE AGENTS AND ANTIPLATLET AGENTS - The present invention relates to a stable composition for providing substances with different types of activity, such as cholesterol lowering agents, antihypertensive agents and antiplatelet agents, which substantially reduce the dosage required to prevent cardiovascular events. | 2013-12-26 |
20130345183 | INTRAVENOUS FORMULATION WITH WATER-SOLUBLE COCRYSTALS OF ACETYLSALICYLIC ACID AND THEANINE - A method of treating rheumatoid arthritis using a water-soluble cocrystal composition contains a quantity of acetylsalicylic acid and a quantity of a theanine enantiomer selected from an alpha variant of theanine or a beta variant of theanine or other form of theanine. | 2013-12-26 |
20130345184 | PHARMACEUTICAL SOLID STATE FORMS-2 - The invention provides and describes solid state 17α-ethynyl-5α-androstane-3α,17β-diol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-5α-androstane-3α,17β-diol include Form III anhydrate and Form I solvate. The invention further relates to solid and suspension formulations containing 17α-ethynyl-5α-androstane-3α,17β-diol in a described solid state form and use of the formulations to treat cancers or precancers such as prostate cancer or breast cancer in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-5α-androstane-3α,17β-diol and uses of such formulations in treating the described conditions. | 2013-12-26 |
20130345185 | Ophthalmic Compositions - The embodiments disclosed herein relate to ophthalmic compositions comprising calcineurin inhibitors or mTOR inhibitors, and more particularly to methods for treating an ocular disease and/or condition using the disclosed compositions. According to aspects illustrated herein, there is provided a pharmaceutical composition that includes a calcineurin inhibitor or an mTOR inhibitor; a first surfactant with an HLB index greater than about 10; and a second surfactant with an HLB index of greater than about 13, wherein an absolute difference between the HLB index of the first surfactant and the HLB index of the second surfactant is greater than about 3, and wherein the composition forms mixed micelles. | 2013-12-26 |
20130345186 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS - Chemical entities that are novel compounds, pharmaceutical compositions and methods of treatment of cancer are described. | 2013-12-26 |
20130345187 | METHOD FOR PRE-SCREENING AND CORRELATION OF UNDERLYING SCARB1 GENE VARIATION TO INFERTILITY IN WOMEN AND THERAPEUTIC USE OF PROGESTATIONAL AND OTHER MEDICATIONS IN TREATMENT - A method of genotyping women experiencing infertility for non-physical reasons in order to identify the presence of the rs4238001 and/or rs10846744 mutation of the SCARB1 gene and, upon identifying the presence of one or both genetic mutations, administering a tailored therapeutic regimen to restore fertility by either one or a combination of 1) mediating the flux of cholesterol resulting from the mutation by therapeutic use of the cholesterol medication probucol and/or other cholesterol altering medications, and/or 2) amplifying the presence of hormone progesterone by therapeutic use of progestational and progestin medications. | 2013-12-26 |
20130345188 | Preparation and Uses of Obeticholic Acid - The present invention relates to obeticholic acid: | 2013-12-26 |
20130345189 | METALLOINSERTOR COMPLEXES TARGETED TO DNA MISMATCHES - A composition including a Rh or Ru metalloinsertor complex specifically targets mismatch repair (MMR)-deficient cells. Selective cytotoxicity is induced in MMR-deficient cells upon uptake of the inventive metalloinsertor complexes. | 2013-12-26 |
20130345190 | ISOXAZOLE BETA-LACTAMASE INHIBITORS - β-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D β-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed. | 2013-12-26 |
20130345191 | 1,2,4-TRIAZINE-6-CARBOXAMIDE KINASE INHIBITORS - Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity. | 2013-12-26 |
20130345192 | HETEROCYCLIC TYROSINE KINASE INHIBITORS - The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same. | 2013-12-26 |
20130345193 | 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. | 2013-12-26 |
20130345194 | SUBSTITUTED CYCLOPENTYL-AZINES AS CASR-ACTIVE COMPOUNDS - The invention relates to compounds of general Formula (I), Wherein R | 2013-12-26 |
20130345195 | BENZODIOXANE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I): | 2013-12-26 |
20130345196 | PHENOXY THIOPHENE SULFONAMIDES AND OTHER COMPOUNDS FOR USE AS INHIBITORS OF BACTERIAL GLUCURONIDASE - This invention relates generally to compounds that are glucuronidase inhibitors. The glucuronidase inhibitors include phenoxy thiophene sulfonamides, and other compounds such as pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls. These compounds include nialamide, isocarboxazid, phenelzine, amoxapine, loxapine and mefloquine. Also compositions including one or more of such compounds for use in inhibiting glucuronidase and methods of using one or more of such compounds for selective inhibition of bacterial β-glucuronidase. These compounds may be used as a co-drug in combination with the anticancer drug CPT-11. Also a method for screening compounds to determine their usefulness in reducing diarrhea associated with irinotecan chemotherapy. | 2013-12-26 |
20130345197 | AZAINDOLES USEFUL AS INHIBITORS OF JAK AND OTHER PROTEIN KINASES - The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 2013-12-26 |
20130345198 | PROCESS FOR THE PREPARATION OF (S)-(+)- OR (R)-(-)-10-HYDROXY DIHYDRODIBENZ[B,F]AZEPINES BY ENANTIOSELECTIVE REDUCTION OF 10,11-DIHYDRO-10-OXO-5H-DIBENZ[B,F]AZEPINES AND POLYMORPHS THEREOF - The present invention provides a novel process for the preparation of substituted optically pure (S)-(+)- or (R)-(−)-10-hydroxy-dihydrodibenz[b,f]azepines or derivatives thereof, starting from 10,11-dihydro-10-oxo-5H-dibenz[b,f]azepines using boronate esters or their derivatives. The present invention also provides use of thus prepared (S)-(+)- or (R)-(−)-10-hydroxy-dihydrodibenz[b,f]azepines for the preparation of their ester such as (S)-(−)-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide or (R)-(+)-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide. The present invention also provides novel solid state crystalline forms J | 2013-12-26 |
20130345199 | 1-[M-CARBOXAMIDO(HETERO)ARYL-METHYL]-PIPERIDINE-4-CARBOXAMIDE DERIVATIVES - The present invention relates to 1-[m-Carboxamido(hetero)aryl-methyl]-piperidine-4-carboxamide derivatives of formula (I) | 2013-12-26 |
20130345200 | INDOLES - Herein are disclosed indoles of formula (I) | 2013-12-26 |
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. | 2013-12-26 |
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. | 2013-12-26 |
20130345203 | SUBSTITUTED BICYCLIC ALKOXY PYRAZOLE ANALOGS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS - In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2013-12-26 |
20130345204 | SUBSTITUTED BICYCLIC CYCLOALKYL PYRAZOLE LACTAM ANALOGS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS - In one aspect, the invention relates to substituted bicyclic cycloalkyl pyrazole lactam analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2013-12-26 |
20130345205 | SUBSTITUTED BICYCLIC ARALKYL PYRAZOLE LACTAM ANALOGS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS - In one aspect, the invention relates to substituted bicyclic aralkyl pyrazole lactam analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2013-12-26 |
20130345206 | SUBSTITUTED BICYCLIC ALKOXY PYRAZOLE ANALOGS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS - In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2013-12-26 |
20130345207 | BENZYL-OXATHIAZINE DERIVATIVES SUBSTITUTED WITH ADAMANTANE AND NORADAMANTANE, MEDICAMENTS CONTAINING SAID COMPOUNDS AND USE THEREOF - The invention relates to compounds of formula (I) and to the physiologically compatible salts thereof. Said compounds are suitable, for example, for treating hyperglycemia. | 2013-12-26 |
20130345208 | ION CHANNEL MODULATORS AND METHODS OF USE - In general, the invention relates to novel 4-phenylpyrimidine compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels and/or calcium channels for the treatment of pain. | 2013-12-26 |
20130345209 | AMINOTRIAZOLOPYRIDINE FOR USE IN THE TREATMENT OF INFLAMMATION, AND PHARMACEUTICAL COMPOSITIONS THEREOF - The present invention relates to the compound according to Formula I, and to its use in medicine, in particular in the treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. In particular, the compound inhibits JAK a family of tyrosine kinases, and more particularly JAK1. The present invention also provides pharmaceutical compositions comprising the compound, methods for the prophylaxis and/or treatment of diseases involving inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons by administering the compound. | 2013-12-26 |
20130345210 | LOCAL TOPICAL ADMINISTRATION FORMULATIONS CONTAINING INDOXACARB - The present invention provides formulations and methods useful in the control of ectoparasites on a domestic animal, using a formulation comprising Indoxacarb and a veterinarily acceptable carrier that is applied topically to 10% or less of the total surface area of a domestic animal. Other embodiments include these formulations also including one or more additional pesticides such as fipronil. | 2013-12-26 |
20130345211 | Pyridine Compounds as Sodium Channel Blockers - The invention relates to substituted pyridine compounds of Formula I: (I) or a pharmaceutically acceptable salt, prodrug, or solvate thereof wherein A | 2013-12-26 |
20130345212 | QUINOLINONE DERIVATIVES - The present invention relates to compounds of the formula (I), | 2013-12-26 |
20130345213 | SUBSTITUTED MORPHOLINES AS MODULATORS FOR THE CALCIUM SENSING RECEPTOR - Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors of Formula (I). | 2013-12-26 |
20130345214 | Lipoxygenase Inhibitors - The disclosure provides bisindole suitable for inhibiting lipoxygenases or Aβ-formation, and treating associated diseases, such as Alzheimer's disease. The bisindoles are indolo[2,3-b]carbazole derivatives, and may be administered to a patient as part of a pharmaceutical formulation. | 2013-12-26 |
20130345215 | PYRAZOLOPYRIMIDONE AND PYRAZOLOPYRIDONE INHIBITORS OF TANKYRASE - There are provided compounds of the formula | 2013-12-26 |
20130345216 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS - Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein. | 2013-12-26 |
20130345217 | COMBINATIONS OF PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND CHEMOTHERAPEUTIC AGENTS, AND METHODS OF USE - Combinations of PI3K inhibitor compounds having Formulas I and II and chemotherapeutic agents, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for treating hyperproliferative disorders such as cancer. Methods of using such combinations for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 2013-12-26 |
20130345218 | INHIBITORS OF INFLUENZA VIRUSES REPLICATION - Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): | 2013-12-26 |
20130345219 | TRIAZINONE AND DIAZINONE DERIVATIVES USEFUL AS HSP90 INHIBITORS - The present invention relates to compounds according to formulae (IA) to (ID) and compositions that inhibit the activity of Hsp90. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a compound of the invention, or a composition comprising such a compound. | 2013-12-26 |
20130345220 | COMPOUNDS AND COMPOSITIONS AS LXR MODULATORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs). | 2013-12-26 |
20130345221 | ISOXAZOLE DERIVATIVES - The invention relates to new isoxazoline compounds of formula | 2013-12-26 |
20130345222 | IDENTIFICATION OF HUMAN T2R RECEPTORS THAT RESPOND TO BITTER COMPOUNDS THAT ELICIT THE BITTER TASTE IN COMPOSITIONS, AND THE USE THEREOF IN ASSAYS TO IDENTIFY COMPOUNDS THAT INHIBIT (BLOCK) BITTER TASTE IN COMPOSITIONS AND USE THEREOF - The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals. | 2013-12-26 |
20130345223 | COMPOUNDS AND METHODS FOR TREATING TUBERCULOSIS INFECTION - The present invention provides compounds which are potent inhibitors against Lpd activity, PDH activity, and/or the growth of | 2013-12-26 |
20130345224 | IMIDAZO[1,2-B][1,2,4]TRIAZINES AS C-MET INHIBITORS - The present invention relates to imidazo[1,2-b][1,2,4]triazines that are inhibitors of c-Met and are useful in the treatment of c-Met associated diseases including cancer. | 2013-12-26 |
20130345225 | DIAZABENZO[DE] ANTHRACEN-3-ONE COMPOUNDS AND METHODS FOR INHIBITING PARP - The present invention relates to diazabenzo[de]anthracen-3-one compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein. | 2013-12-26 |
20130345226 | PYRROLOPYRAZONE INHIBITORS OF TANKYRASE - There are provided compounds of the formula | 2013-12-26 |
20130345227 | PYRIDO [2, 3 - B] PYRAZINE DERIVATIVES AND THEIR THERAPEUTICAL USES - The present invention relates to novel pyrido[2,3-b]pyrazine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors. | 2013-12-26 |
20130345228 | 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) - The present invention relates to novel 3,4-dihydro-pyrrolo[1,2-a]pyrazin- | 2013-12-26 |
20130345229 | Compositions and Methods for the Treatment of Nasal Conditions - The invention provides compositions and methods for treating nasal congestion. The provided compositions and methods utilize low concentrations of selective α-2 adrenergic receptor agonists. The compositions preferably include brimonidine. | 2013-12-26 |
20130345230 | METHODS AND COMPOSITIONS FOR MODULATING CALCIUM CHANNELS - The present invention relates to methods and compositions for modulating calcium channels. In particular, the present invention provides methods and compositions for modulating (e.g., disrupting) Cav1.3a calcium channels for research and therapeutic methods (e.g., treating dopaminergic diseases and conditions). | 2013-12-26 |
20130345231 | ANTICANCER THERAPEUTIC AGENTS - The invention described herein pertains to anticancer therapeutic agents that exhibit preferential cytotoxicity to malignant cells that express a cancer specific isoform of proliferating cell nuclear antigen (caPCNA) compared to cytotoxicity to comparable non-malignant cells, pharmaceutical compositions comprising the agents, and their use in cancer therapy. | 2013-12-26 |
20130345232 | METHODS AND COMPOSITIONS FOR TREATING A SUBJECT FOR A LYMPHATIC MALFORMATION - Methods of treating lymphatic malformations using a phosphodiesterase type 5 inhibitor are provided. Pharmaceutical compositions and kits comprising phosphodiesterase type 5 inhibitors are also provided. | 2013-12-26 |
20130345233 | INHIBITORS OF PROTEIN KINASES - Compounds of general Formula (I): | 2013-12-26 |
20130345234 | FGFR AND LIGANDS THEREOF AS BIOMARKERS FOR BREAST CANCER IN HR POSITIVE SUBJECTS - The present invention describes methods for diagnosing, treating and determining the prognosis of breast cancer HR+ patient, the methods including detecting the amplification of one or more biomarkers comprising a FGFR ligand such as FGF3, FGF4, FGF19, and/or a FGFR, such as for example FGFR1 in a subject; determining an FGFR1 inhibitor for treating the subject based on the amplification of the one or more biomarkers in the subject; administering to the subject in need thereof the FGFR1 inhibitor and using the one or more biomarkers to indicate prognosis of the subject treated with the FGFR1 inhibitor. | 2013-12-26 |
20130345235 | PHENOXY THIOPHENE SULFONAMIDES AND THEIR USE AS INHIBITORS OF GLUCURONIDASE - This invention relates generally to compounds that are glucuronidase inhibitors. Glucuronidase inhibitors described include phenoxy thiophene sulfonamides. Other compounds, for instance pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls, are also contemplated. Also contemplated are compositions including one or more of such compounds for use inhibiting glucuronidase and methods of using one or more of such compounds as a co-drug to be used in combination with the anticancer drug CPT-11. | 2013-12-26 |
20130345236 | PHARMACEUTICAL COMPOSITIONS PROVIDING ENHANCED DRUG CONCENTRATIONS - A drug in a solubility-improved form is combined with a concentration-enhancing polymer in a sufficient amount so that the combination provides substantially enhanced drug concentration in a use environment relative to a control comprising the same amount of the same solubility-improved form of drug without the concentration-enhancing polymer. | 2013-12-26 |
20130345237 | ARYL-SUBSTITUTED IMIDAZOLES - The compounds of the invention are antagonists of MDM2 and MDMX, with excellent specificity for MDM2 and MDMX over other proteins, and with selective binding affinity to MDMX over MDM2. The compounds can therefore regulate p53 activity and treat a variety of cancers. 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. | 2013-12-26 |
20130345238 | METHOD OF USING DIKETOPIPERAZINES AND COMPOSITION CONTAINING THEM - The invention provides a method of inhibiting the effects of platelet activating factor (PAF). For instance, a disease or condition mediated by PAF (particularly inflammation) can be treated or platelet aggregation can be inhibited. The invention also provides a method of inhibiting the production and/or release of interleukin 8 (IL-8) by cells. The effects of PAF and the production and/or release of IL-8 are inhibited according to the invention by a compound of the formula: | 2013-12-26 |
20130345239 | NOVEL CRYSTALLINE FORM - This invention relates to a new crystalline form of the succinate salt of the epithelial sodium channel (ENaC) blocker 3-(3-{2-[(E)-3,5-Diamino-6-chloro-pyrazine-2-carbonylimino]-1,3,8-triaza-spiro[4.5]decane-8-carbonyl}-benzenesulfonylamino)-propionic acid dipropylcarbamoylmethyl ester, pharmaceutical compositions comprising said crystalline form, uses of said crystalline form and pharmaceutical compositions, and methods for preparing said crystalline form. | 2013-12-26 |
20130345240 | 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. | 2013-12-26 |
20130345241 | DIHYDROOXAZOL-2-AMINE DERIVATIVES - The invention relates to compounds of formula | 2013-12-26 |
20130345242 | HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF E1 ACTIVATING ENZYMES - This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia. | 2013-12-26 |