42nd week of 2013 patent applcation highlights part 52 |
Patent application number | Title | Published |
20130274179 | VIRAL POLYMERASE INHIBITORS - The present invention relates to viral polymerase inhibitors of formula (I) or salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections. | 2013-10-17 |
20130274180 | Pharmaceutical Compositions - Forms and formulations of VX-950 and uses thereof. | 2013-10-17 |
20130274181 | OBESITY-RELATED GENES AND THEIR PROTEINS AND USES THEREOF - The invention provides for methods of treating obesity or an obesity-associated disorder. | 2013-10-17 |
20130274182 | ENGINEERED POLYPEPTIDES HAVING ENHANCED DURATION OF ACTION - Compounds are provided having inter alia good duration of action, high potency and/or convenient dosing regimens including once weekly administration. The compounds are engineered polypeptides which incorporate an albumin binding domain in combination with one or more biologically active polypeptides. Also provided are pharmaceutical compositions and methods of treatment for diseases and disorders including lipodystrophy, dyslipidemia, hyperlipidemia, overweight, obesity, hypothalamic amenorrhea, Alzheimer's disease, leptin deficiency, fatty liver disease or diabetes (including type I and type II). Additional diseases and disorders which can be treated by the compounds and methods described herein include nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD), metabolic syndrome X and Huntington's Disease. | 2013-10-17 |
20130274183 | APPARATUS AND METHOD FOR AUTOMATICALLY SUPPLYING INSULIN BASED ON AMOUNT OF EXERCISE - An apparatus and method for automatically supplying insulin based on exercise amount are provided. The apparatus includes a blood sugar measurer for measuring a blood sugar level of a patient; a controller for, comparing the measured blood sugar level with a predetermined blood sugar level, if the measured blood sugar level is greater than or equal to the predetermined blood sugar level, determining whether a current time is within a blood sugar change time zone, if the measured blood sugar level is equal to or higher than the predetermined blood sugar level, and if the current time does is not within the blood sugar change time zone, acquiring exercise amount information about the patient and determining a dose of insulin to be injected inject into the patient based on the acquired exercise amount information, if the current time does not fall within the blood sugar change time zone; and an insulin injector for injecting the determined dose of insulin into the patient. | 2013-10-17 |
20130274184 | ER STRESS RELIEVERS IN BETA CELL PROTECTION - The present invention is based on the discovery that certain small molecules can relieve ER stress, leading to increased insulin production in beta cells and improved insulin secretion. Methods of treating a disease or disorder in a subject, wherein the disease or disorder is characterized by intracellular endoplasmic reticulum (ER) stress, by administering to the subject, an effective amount of a compound that is an ER stress reliever, are provided herein. | 2013-10-17 |
20130274185 | Pharmaceutical for Pseudo-Exercise Therapy - A pharmaceutical for pseudo-exercise therapy containing an adiponectin receptor 1 agonist compound as an active ingredient and changing the physiological state of muscle to a post-exercise one without applying an exercise stress to the muscle. | 2013-10-17 |
20130274186 | NEURTURIN MOLECULES - Neurturin polypeptides which possess reduced heparin and heparan sulfate binding affinity but retain neurotrophic activity, nucleic acids which encode the neurturin variants and vectors and host cells which express the enhanced neurturin polypeptides. Use of the enhanced neurturin polypeptides, nucleic acids and host cells in the treatment or prevention of disease. | 2013-10-17 |
20130274187 | PEPTIDES AND METHODS OF USING SAME - We describe peptides and their uses for the treatment of autoimmune, inflammatory and metabolic diseases. | 2013-10-17 |
20130274188 | MACROMOLECULE FOR DELIVERING PROTEIN, POLYPEPTIDE OR PEPTIDE DRUGS AND A PRODUCTION METHOD FOR THE SAME, AND A SLOW RELEASE COMPOSITION FOR PROTEIN, POLYPEPTIDE OR PEPTIDE DRUGS AND A PRODUCTION METHOD FOR THE SAME - The present invention relates to a macromolecule for delivering protein, polypeptide or peptide drugs and to a production method for the same, as well as to a slow release composition for protein, polypeptide or peptide drugs comprising the same, and more specifically relates to a polylactic acid derivative compound of Chemical formula 1 of which the numerical average molecular weight is no more than 7000 daltons and to a production method for the same, as well as to a slow release composition for protein, polypeptide or peptide drugs using the same and to a production method for the same. | 2013-10-17 |
20130274189 | VEGF Antagonist Formulations for Intravitreal Administration - Ophthalmic formulations of a vascular endothelial growth factor (VEGF)-specific fusion protein antagonist are provided suitable for intravitreal administration to the eye. The ophthalmic formulations include a stable liquid formulation and a lyophilizable formulation. Preferably, the protein antagonist has an amino acid sequence of SEQ ID NO:4. | 2013-10-17 |
20130274190 | BIOMATERIAL FOR WOUND HEALING AND PREPARATION THEREOF - The present invention provides a biomaterial comprising a scaffold consisting of collagen, hyaluronic acid, and gelatin, which are cross-linked via ethyl-3-[3-dimethylaminopropyl]carbodiimide (EDC) between any two of collagen, hyaluronic acid, and gelatin. The present invention further provides a method for preparing the biomaterial and a method for enhancing wound healing with the biomaterial. | 2013-10-17 |
20130274191 | METHODS AND COMPOSITIONS FOR THERAPEUTIC MODULATION OF ALDOSTERONE LEVELS IN HEART DISEASE - The disclosure describes the contribution of elevated levels of circulating alsosterone to heart disease and other hyperaldosteronic conditions. Since activation of beta-arrestin I (beta.arr-1) by the Angiotensin II (AngII) type 1 receptor (AT1R) mediates AngII-induced aldosterone production, beta-arrestin I (beta.arr-1) is a therapeutic target for heart disease. Specifically, the disclosure provides a beta.arr-1 protein fragment comprising the C-terminus of beta.arr-1 (beta.arr1ct; SEQ ID NO:3), compositions containing this protein fragment, and methods of using this protein fragment to reduce elevated levels of aldosterone in heart disease and other hyperaldosteronic conditions by inhibition of beta-arrestin (beta.arr-1). These compositions and methods are of therapeutic benefit in chronic heart failure and progression to heart failure after myocardial infarction (MI). Additionally, the invention provides an AngII peptide analog (SEQ ID NO:4), compositions containing this analog, and methods of using this analog for stimulation of beta.arr-1 activity and aldosterone production. | 2013-10-17 |
20130274192 | MICROPARTICLES CONTAINING PHYSIOLOGICALLY ACTIVE PEPTIDE, METHOD FOR PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - Disclosed are microparticles containing physiologically active peptides, a method for preparing the same, and a pharmaceutical composition comprising the same. | 2013-10-17 |
20130274193 | TFPI INHIBITORS AND METHODS OF USE - The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, and/or treat a blood coagulation disorder in a subject. | 2013-10-17 |
20130274194 | Factor VIII-Fc Chimeric and Hybrid Polypeptides, and Methods of Use Thereof - The present invention provides methods of administering Factor VIII; methods of administering chimeric and hybrid polypeptides comprising Factor VIII; chimeric and hybrid polypeptides comprising Factor VIII; polynucleotides encoding such chimeric and hybrid polypeptides; cells comprising such polynucleotides; and methods of producing such chimeric and hybrid polypeptides using such cells. | 2013-10-17 |
20130274195 | GENETIC POLYMORPHISMS ASSOCIATED WITH VENOUS THROMBOSIS, METHODS OF DETECTION AND USES THEREOF - The present invention is based on the discovery of genetic polymorphisms that are associated with venous thrombosis. In particular, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by such nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and proteins, and methods of using the nucleic acid and proteins as well as methods of using reagents for their detection. | 2013-10-17 |
20130274196 | METHOD FOR TREATMENT OF INFLAMMATORY DISEASE AND DISORDER - The present disclosure provides a method, composition and kit for treatment of inflammatory disease and disorder using PKC isoform modulators. | 2013-10-17 |
20130274197 | BENZODIAZEPINONE COMPOUNDS USEFUL IN THE TREATMENT OF SKIN CONDITIONS - The present invention provides a family of benzodiazepinone compounds and pharmaceutical compositions thereof. The present invention also provides methods of treating certain skin conditions, e.g., atopic dermatitis, rosacea, or psoriasis, by administering a benzodiazepinone and methods of reducing the proliferation of keratinocyte cells by exposing such cells to a benzodiazepinone. | 2013-10-17 |
20130274198 | TREATING MUC1-EXPRESSING CANCERS WITH COMBINATION THERAPIES - The invention provides method of treating cancers that express MUC1 by the administration of PI3-K inhibitors in combination with MUC1-directed cancer therapies. The PI3-K inhibition may advantageously be combined with peptides that inhibit MUC1 oligomerization, or further with other standard anticancer therapies such as chemo-, radio- and surgical therapies. | 2013-10-17 |
20130274199 | Partial Fragment of REIC/Dkk-3 Gene and Cancer Therapeutic Agent Comprising the Same - This invention provides an inducer of apoptosis in cancer cells comprising a fragment of the REIC/Dkk-3 gene and a cancer therapeutic agent comprising the same. This invention also provides a polynucleotide fragment encoding the REIC/Dkk-3 protein (a) or (b), which encodes a polypeptide having apoptosis activity: (a) a polynucleotide encoding a polypeptide comprising an amino acid sequence of amino acid 1 to any of amino acids 39 to 78 of the amino acid sequence of the REIC/Dkk-3 protein as shown in SEQ ID NO: 2; or (b) a polynucleotide encoding a polypeptide comprising an amino acid sequence derived from the amino acid sequence of amino acid 1 to any of amino acids 39 to 78 of the amino acid sequence of the REIC/Dkk-3 protein as shown in SEQ ID NO: 2 by substitution, deletion, or addition of 1 or several amino acids and having apoptosis activity. | 2013-10-17 |
20130274200 | SELECTIVE ANTICANCER CHIMERIC PEPTIDE - It is an object of the present invention to provide a substance usable as an anticancer agent or DDS, which has intracellular stability, which is capable of evading side effects from functional disorder with respect to normal cells, or which has instantaneous effect. The inventors developed a novel chimeric peptide targeting cancer cells which overexpress EGFR or the like using a binding peptide such as a peptide sequence binding to EGFR, and a lytic peptide sequence, thereby solving such an object. Particularly, by using a chimeric peptide including an EGF receptor-binding peptide or the like and a cytotoxic peptide, this object was solved. | 2013-10-17 |
20130274201 | SELECTIVE ANTICANCER CHIMERIC PEPTIDE - It is an object of the present invention to provide a substance usable as an anticancer agent or DDS, which has intracellular stability, which is capable of evading side effects from functional disorder with respect to normal cells, or which has instantaneous effect. The inventors developed a novel chimeric peptide targeting cancer cells which overexpress EGFR or the like using a binding peptide such as a peptide sequence binding to EGFR, and a lytic peptide sequence, thereby solving such an object. Particularly, by using a chimeric peptide including an EGF receptor-binding peptide or the like and a cytotoxic peptide, this object was solved. | 2013-10-17 |
20130274202 | Peptides for Treating Cancer - The present invention relates to peptide from 4 to 50 amino acids comprising a phosphorylated pYX | 2013-10-17 |
20130274203 | ANTI-SSX-2 T CELL RECEPTORS AND RELATED MATERIALS AND METHODS OF USE - The invention provides an isolated or purified T cell receptor (TCR) having antigenic specificity for synovial sarcoma X Breakpoint (SSX)-2. The invention further provides related polypeptides and proteins, as well as related nucleic acids, recombinant expression vectors, host cells, and populations of cells. Further provided by the invention are antibodies, or an antigen binding portion thereof, and pharmaceutical compositions relating to the TCRs of the invention. Methods of detecting the presence of cancer in a host and methods of treating or preventing cancer in a host are further provided by the invention. | 2013-10-17 |
20130274204 | Agonists of Guanylate Cyclase Useful for the Treatment of Gastrointestinal Disorders, Inflammation, Cancer and Other Disorders - The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer. | 2013-10-17 |
20130274205 | PEPTIDOMIMETIC MACROCYCLES - Provided herein are peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease. | 2013-10-17 |
20130274206 | Compositions and Methods for Promoting Wound Healing and Tissue Regeneration - Provided herein are compositions and methods for use in promoting wound healing and tissue regeneration following tissue injury in a subject. | 2013-10-17 |
20130274207 | Uses of Natriuretic Peptide Constructs - Use of constructs which bind to one or more natriuretic peptide receptors and include a plurality of amino acid residues and at least one amino acid surrogate of formula I: | 2013-10-17 |
20130274208 | Small Peptides And Methods For Treatment Of Chronic Inflammatory Bowel Disease - Methods for treating cutaneous inflammation, are described. Also described is a method for inhibiting the mucous release into airways of a patient, a method for blocking IgE activation of a lymphocyte, a method for stabilizing the cell membrane of a lymphocyte, thereby preventing their further involvement in the increased inflammatory response to an IgE antigen challenge, and a method for inhibiting the migration of T-cells. Such methods involve administering to said patient a therapeutically effective amount of a peptide having the formula f-Met-Leu-X, wherein X is selected from the group consisting of Tyr, Tyr-Phe, Phe-Phe and Phe-Tyr. | 2013-10-17 |
20130274209 | SPRAYABLE PHARMACEUTICAL COMPOSITIONS FOR TOPICAL APPLICATION COMPRISING SUCRALFATE GEL - A pharmaceutical composition is described comprising sucralfate gel, PVA and optionally a vegetable product comprising tocotrienols and tocopherols. In particular, this composition proved to be suitable for being sprayed, and is advantageously used in the treatment of skin lesions, even deep lesions, such as second-degree burns. | 2013-10-17 |
20130274210 | DENDRIMERS WITH A SACCHARIDE ENDING FOR ANTI-INFLAMMATORY PURPOSES - The present invention relates to dendrimers with a monosaccharide, oligosaccharide or polysaccharide terminal group, to their preparation method and their therapeutic uses, notably anti-inflammatory uses. | 2013-10-17 |
20130274211 | BIOCOMPATIBLE, NON-BIODEGRADABLE, NON-TOXIC POLYMER USEFUL FOR NANOPARTICLE PHARMACEUTICAL COMPOSITIONS - The invention relates to a biocompatible, non-biodegradable, and non-toxic polymer of formula (I), comprising of three monomeric units, selected from 1-Vinylpyrrolidne (VP), N-Isopropylactylamide (NIPAM), and ester of Maleic anhydride and Polyethylene glycol (MPEG), cross-linked with a bi-functional vinyl derivative, of high purity and substantially free of respective toxic monomeric contaminants, and a process for preparation thereof. The invention further relates to nanoparticulate pharmaceutical compositions of poorly water-soluble drugs or compounds comprising the polymer of the invention, which are safe, less-toxic and convenient for bedside administration to patients in need thereof. Furthermore, the invention relates to a highly selective method for preparation of nanoparticulate pharmaceutical compositions of poorly water-soluble drugs or compounds. | 2013-10-17 |
20130274212 | Sesterterpene Compounds and Use Thereof - The present invention relates to sesterterpene compounds, to the precursors thereof that are hydrolysable in a living body, or to the pharmaceutically acceptable salts thereof, and also relates to the prevention and treatment efficacy of the sesterterpene compounds with respect to non-insulin dependent diabetes mellitus, diabetic complications (renal failure and foot ulcers caused by diabetes), alcoholic, non-alcoholic, and viral fatty liver diseases, obesity, hyperlipidemia, atherosclerosis, cardiovascular diseases such as atherosclerotic stroke, and cerebropathies (Parkinsonism, schizophrenia and Alzheimer's disease). In addition, the present invention relates to compositions for functional foods, functional beverages, functional cosmetics, and functional feed. | 2013-10-17 |
20130274213 | GLYCOSYLATED AMINOCOUMARINS AND METHODS OF PREPARING AND USES OF SAME - There is provided a method of glycosylating an aminocoumarin compound comprising conjugating a sugar to the 4′-OH position of the core of the aminocoumarin compound. Also provided is an aminocoumarin compound glycosylated at the 4′-OH position of the core of the aminocoumarin compound. Further aspects of this invention provide this compound for use in therapy, more particularly for use as an antibiotic, or in anticancer treatment. | 2013-10-17 |
20130274214 | METHOD FOR TREATING BLEPHARITIS - This invention relates to methods of treating blepharitis. The methods comprise identifying a patient suffering from blepharitis, and topically administering to the eyes of the patient an effective amount of azithromycin and an effective amount of a retinoid. The method is useful in relieving blepharitis signs and symptoms. This invention also relates to a pharmaceutical composition comprising azithromycin and a retinoid such as retinyl palmitate. | 2013-10-17 |
20130274215 | PHARMACEUTICAL COMPOSITIONS TO TREAT FIBROSIS - The present invention provides methods for the prevention, treatment and/or amelioration of fibrosis or fibrotic conditions. The present invention further provides small molecule inhibitors of Wnt- and TGF-p-mediated β-catenin signaling to prevent, treat and/or ameliorate fibrosis or fibrotic conditions. Kits comprising small molecule inhibitors of Wnt- and TGF-p-mediated β-catenin signaling and methods of identifying small molecule inhibitors of Wnt- and TGF-p-mediated β-catenin signaling are also provided. | 2013-10-17 |
20130274216 | TREATMENT FOR MICROBE-INDUCED INFLAMMATORY RESPONSES IN THE EYE - The present invention relates to ophthalmic compositions comprising inhibitors of spleen tyrosine kinase (syk). The compositions are particularly well suited for the treatment of ophthalmic infection such as fungal keratitis. The compositions optionally comprise an antiinfective compound such as an antibacterial or antifungal compound. The present invention also relates to methods for treating fungal keratitis using compositions comprising syk inhibitors. | 2013-10-17 |
20130274217 | Controlled Release Formulations for the Delivery of HIF-1 Inhibitors - Controlled release dosage formulations for the delivery of one or more HIF-1 inhibitors are provided. The controlled release formulations contain one or more HIF-1 inhibitors conjugated to or dispersed in a polymeric vehicle. The one or more HIF-1 inhibitors can be dispersed or encapsulated in a polymeric matrix. In some embodiments, the one or more HIF-1 inhibitors are covalently bound to a polymer, forming a polymer-drug conjugate. Polymeric vehicles can be formed into implants, microparticles, nanoparticles, or combinations thereof. Controlled release HIF-1 formulations provide prolonged therapeutic benefit while lowering side effects by releasing low levels of one or more HIF-1 inhibitors and/or HIF-1 inhibitor conjugates over a prolonged period of time. Controlled release dosage formulations can be used to treat or prevent a disease or disorder in a patient associated with vascularization, including cancer, obesity, and ocular diseases such as wet AMD. | 2013-10-17 |
20130274218 | VIRAL POLYMERASE INHIBITORS - The present invention relates to viral polymerase inhibitors of formula (I) or salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections. | 2013-10-17 |
20130274219 | METHODS FOR TREATING NON-SMALL CELL LUNG CANCER USING 5-AZACYTIDINE - The present disclosure provides methods for treating subjects having non-small cell lung cancer, wherein the methods comprise administering to the subject a cytidine analog, such as 5-azacytidine. Also provided are methods relating to identification and treatment of particular non-small cell lung cancer types sensitive to particular cytidine analogs. | 2013-10-17 |
20130274220 | METHODS, ASSAYS AND COMPOUNDS FOR TREATING BACTERIAL INFECTIONS BY INHIBITING METHYLTHIOINOSINE PHOSPHORYLASE - The present invention discloses methods for treating bacterial infections in a subject comprising administering to the subject a sub-growth inhibiting amount of a 5′-methylthioinosine phosphorylase (MTIP) inhibitor, as well as assays for identifying such inhibitors, and compounds and pharmaceutical compositions comprising the inhibitors. | 2013-10-17 |
20130274221 | ACTIVE INGREDIENT WITH CUTANEOUS APPLICATION OBTAINED FROM METSCHNIKOWIA AGAVES AND USES FOR IMPROVING THE STATE OF THE SKIN - An active ingredient with cutaneous application obtained from | 2013-10-17 |
20130274222 | THREADS OF CROSS-LINKED HYALURONIC ACID AND METHODS OF PREPARATION AND USE THEREOF - This disclosure relates generally to cross-linked hyaluronic acid compositions, threads made from such compositions, methods of making such threads and uses thereof, for example, in aesthetic applications (e.g., facial contouring, soft tissue augmentation products), surgery (e.g., sutures), drug delivery, negative pressure wound therapy, moist wound dressing, and the like. | 2013-10-17 |
20130274223 | METHOD OF APPLYING AN INJECTABLE FILLER - Methods for applying injectable fillers are provided. In some embodiments, the methods can extend effectiveness of the injectable filler. In some embodiments, the methods can provide for an elevated level of effectiveness of the injectable filler. In some embodiments, the methods can prolong the effectiveness of the injectable filler. | 2013-10-17 |
20130274224 | STERILE INJECTABLE AQUEOUS FORMULATION USED IN OPHTHALMOLOGY - The present invention relates to an intraocularly injectable sterile aqueous formulation based on a mixture of hyaluronic acid and alginate, or a salt thereof, used in ophthalmology and having specific viscoelasticity, spreading, covering and ocular tissue adhesion properties and also a high capacity for neutralizing free radicals, said properties enabling said composition to strongly protect the eye tissues. | 2013-10-17 |
20130274225 | METHOD FOR MAKING A POLYSACCHARIDE DIALDEHYDE HAVING HIGH PURITY - A method for making polysaccharide dialdehydes is disclosed, which uses a combination of precipitation and separation steps to purify the polysaccharide dialdehyde formed by oxidation of a polysaccharide with periodate. The method is simple, rapid, and provides a polysaccharide dialdehyde having very low levels of iodine-containing species and a low ash content. The polysaccharide dialdehyde is particularly suitable for preparing hydrogel adhesives for medical applications. | 2013-10-17 |
20130274226 | SILICA NANOPARTICLE AGENT CONJUGATES - The invention provide a silica nanoparticle comprising a non-porous matrix of silicon-oxygen bonds, wherein the matrix comprises organic agents conjugated to silicon or oxygen atoms in the matrix, the organic agents are conjugated to the matrix through linker L groups, wherein the linker L comprises, for example, an ester, urea, thiourea, or thio ether group, and wherein the diameter of the nanoparticle is about 15 nm to about 200 nm. The invention also provides novel methods of making and using the silica nanoparticles described herein. | 2013-10-17 |
20130274227 | 3,5-DIAMINOPYRAZOLE KINASE INHIBITORS - Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition. | 2013-10-17 |
20130274228 | CONCOMITANT DRUG FOR IMPROVING COGNITIVE FUNCTION - The present invention aims to provide a medicament and/or food having a cognitive function improving effect, and a method of improving the cognitive function. | 2013-10-17 |
20130274229 | ENHANCED ANTI-INFLUENZA AGENTS CONJUGATED WITH ANTI-INFLAMMATORY ACTIVITY - Novel dual-targeted, bifunctional anti-influenza drugs formed by conjugation with anti-inflammatory agents are disclosed. Exemplary drugs according to the invention include caffeic acid (CA)-bearing zanamivir (ZA) conjugates ZA-7-CA (1), ZA-7-CA-amide (7) and ZA-7-Nap (43) for simultaneous inhibition of influenza virus neuraminidase and suppression of proinflammatory cytokines. Synthetic methods for preparation of these enhanced anti-influenza conjugate drugs are provided. The synthetic bifunctional ZA conjugates act synergistically towards protection of mice lethally infected by H1N1 or H5N1 influenza viruses. The efficacy of ZA-7-CA, ZA-7-CA-amide and ZA-7-Nap conjugates is much greater than the combination therapy of ZA with anti-inflammatory agents. | 2013-10-17 |
20130274230 | (2-UREIDOACETAMIDO)ALKYL DERIVATIVES AS FORMYL PEPTIDE RECEPTOR 2 MODULATORS - The present invention relates to (2-ureidoacetamido)alkyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2. | 2013-10-17 |
20130274231 | COMPOSITIONS FOR USE IN TREATMENT OF DERMATOLOGICAL DISEASES AND CONDITIONS - Compositions containing an effective dermatological disease-treating or dermatological condition-treating active agent and a pharmaceutically-acceptable carrier or vehicle are disclosed. | 2013-10-17 |
20130274232 | Pharmaceutical Compositions - A pharmaceutical composition for inhalation comprising R(+) budesonide and one bronchodilators, and, optionally, one or more pharmaceutically acceptable excipients. | 2013-10-17 |
20130274233 | MODULATORS OF HEDGEHOG SIGNALING PATHWAY - The invention provides compounds and methods for modulating the Hedgehog signaling pathway. The compounds modulate the translocation and/or accumulation of smoothened to the primary cilia. | 2013-10-17 |
20130274234 | NOVEL 19-NOR-STEROIDS AND THEIR USE FOR TREATING PROGESTERONE- DEPENDENT CONDITIONS - The subject matter of the instant invention is pertinent to the field of treatment of hormone-dependent conditions. New compounds and methods for treating these conditions are disclosed. Embodiments of the instant invention disclose methods for treating endometriosis, dysmenorrhea, breast cancer, uterine fibroids and endometrial hyperproliferation. | 2013-10-17 |
20130274235 | TREATMENT OF MOTOR NEURON DISEASE - Provided herein are methods and compositions for the treatment of motor neuron diseases including, for example, amyotrophic lateral sclerosis. Suitable therapeutic agents include, for example, agents that up-regulate the expression IGF-II or guanine deaminase in a cell. | 2013-10-17 |
20130274236 | FULVESTRANT COMPOSITIONS AND METHODS OF USE - Provided are inclusion complexes comprising fulvestrant and a cyclodextrin. The complexes may be useful for treating various conditions, such as cancer and systemic lupus crythematosus. Also provided are methods of producing the inclusion complexes, methods of using the inclusion complexes in therapy, and kits and unit dosages comprising the complexes. | 2013-10-17 |
20130274237 | COMPOSITION INCLUDING CHLOROPHYLL A AS AN ACTIVE INGREDIENT FOR PREVENTING AND TREATING TH2-MEDIATED IMMUNOLOGICAL DISEASES - The present invention relates to a composition including chlorophyll a as an active ingredient for preventing and treating Th2-mediated immunological diseases. The composition of the present invention is very effective for preventing and treating atopic dermatitis which is one of the Th2-mediated immunological diseases. Chlorophyll a is a natural ingredient used to treat atopic dermatitis and is advantageous in that it causes absolutely no side effects in humans. Further, the composition of the present invention may be applied as a medical composition including chlorophyll a, which has preventive and therapeutic effects for atopic dermatitis, as a food composition, as a cosmetic composition, and for various other products using chlorophyll a, and has excellent marketability. | 2013-10-17 |
20130274238 | Combination Medicaments for Treating Bacterial Infections - Use of a monobactam antibiotic of formula (I) | 2013-10-17 |
20130274239 | POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS - Disclosed are compounds of the following formula: | 2013-10-17 |
20130274240 | FLUORENE COMPOUND AND PHARMACEUTICAL USE THEREOF - The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: | 2013-10-17 |
20130274241 | INDAZOLYL TRIAZOL DERIVATIVES - Compounds of Formula (I) | 2013-10-17 |
20130274242 | SUBSTITUTED PYRIMIDINE COMPOUNDS AND THEIR USE AS SYK INHIBITORS - Compounds of Formula (I) and methods for inhibiting kinases, including spleen tyrosine kinases, are disclosed. Also disclosed are methods for treating a kinase-mediated disease or condition by administering to a subject a therapeutically effective amount of the compound of Formula (I). | 2013-10-17 |
20130274243 | Chemical Compounds - The invention relates to benzimidazole and imidazopyridine derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new Na | 2013-10-17 |
20130274244 | SUBSTITUTED N-(1H-INDAZOL-4-YL)IMIDAZO[1,2-]PYRIDINE-3-CARBOXAMIDE COMPOUNDS AS TYPE III RECEPTOR TYROSINE KINASE INHIBITORS - Compounds of Formula I: and pharmaceutically acceptable salts thereof in which R | 2013-10-17 |
20130274245 | Composition For Prevention of Vasoactivity in the Treatment of Blood Loss and Anemia - The present invention relates to the prevention of cardiovascular and central nervous system side effects in mammals who receive transfusions of hemoglobin based oxygen carriers (HBOC) or stored blood products containing a concentration of hemoglobin sufficient to induce vasoconstriction, by adding a vasoactivity reducing effective amount of one or more phosphodiesterase inhibitors in combination with a calcium channel blocker and/or an alpha agonist, to the circulation, or alternatively to the HBOC or stored blood, thereby preventing the manifestation of vasoactivity attributable to the presence of free tetrameric hemoglobin (Hb). | 2013-10-17 |
20130274246 | Therapeutic Treatment for Metabolic Syndrome, Type 2 Diabetes, Obesity, or Prediabetes - The present invention is directed to a method for treating a patient suffering from the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes, comprising the step of increasing the ratio of dopaminergic neuronal to noradrenergic and/or serotonin neuronal activity within the central nervous system and particularly the hypothalamus of the central nervous system of the patient. | 2013-10-17 |
20130274247 | Mirtazapine as an Appetite Stimulant for Cats - Methods for stimulating appetite in cats in need thereof are disclosed. | 2013-10-17 |
20130274248 | Compound Having Activity Of Blocking NMDA Receptor Channel, and Pharmaceutical Agent Using The Same - [PROBLEMS] To provide a novel compound having NMDA receptor channel blocking activity, and also a pharmaceutical agent comprising the compound. | 2013-10-17 |
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. | 2013-10-17 |
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) | 2013-10-17 |
20130274251 | 2-(2-PHENYLETHENYL) 1,3-BENZODIAZEPINE COMPOUNDS USEFUL FOR THE TREATMENT OF CANCER - The present invention provides compounds of formula (1) acting as protein kinase (PK) and receptor kinase (RK) signaling modulators. The invention further provides methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as anti-cancer agents for preventions and treatments of PK- and RK-related disorders, in particular cancer. (I) wherein A is H or CN; Z is S, SO or S0 | 2013-10-17 |
20130274252 | QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS - The Present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis. | 2013-10-17 |
20130274253 | NOVEL PYRIMIDINE DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL USE THEREOF AS AKT(PKB) PHOSPHORYLATION INHIBITORS - The present invention relates to novel chemical compounds derived from pyrimidines, to the method for preparing same, to the novel intermediates obtained, to the use thereof as drugs, to the pharmaceutical compositions containing same, and to the therapeutic use thereof as AKT inhibitors. | 2013-10-17 |
20130274254 | INHIBITORS OF CYTOCHROME P450 (CYP3A4) - The present application provides for a compound of formula I, and related compounds, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional therapeutic agent. | 2013-10-17 |
20130274255 | HETEROCYCLIC PYRAZOLE COMPOUNDS, METHOD FOR PREPARING THE SAME AND USE THEREOF - The present invention relates to a compound of formula (I): | 2013-10-17 |
20130274256 | NOVEL INHIBITORS OF BACTERIAL BIOFILMS AND RELATED METHODS - Certain multi-cyclic compounds and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms. | 2013-10-17 |
20130274257 | SUBSTITUTED HETEROCYCLES AS JANUS KINASE INHIBITORS - The present invention provides substituted tricyclic heteroaryl compounds, including, for example, pyridoindoles, pyrimidinoindoles and triazinoindoles that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases such as immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 2013-10-17 |
20130274258 | CARBAZOLE AND CARBOLINE DERIVATIVES, AND PREPARATION AND THERAPEUTIC APPLICATIONS THEREOF - Compounds of general formula (I), wherein A, Y, R | 2013-10-17 |
20130274259 | KINASE MODULATION AND INDICATIONS THEREFOR - Compounds, compositions and methods useful for treatment of Flt3-mediated diseases or conditions are provided herewith. Also provided herewith are methods for modulating the receptor protein tyrosine like kinase 3(Flt3). | 2013-10-17 |
20130274260 | NEW COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES - This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1) wherein R | 2013-10-17 |
20130274261 | METHODS FOR TREATING PULMONARY HYPERTENSION - Methods of treating pulmonary hypertension are disclosed. Particular methods comprise the administration of a tryptophan hydroxylase inhibitor and a prostacyclin. Pharmaceutical formulations are also disclosed. | 2013-10-17 |
20130274262 | PHARMACEUTICAL COMPOSITIONS OF LINEZOLID - The present invention relates to stable pharmaceutical compositions comprising linezolid crystalline Form III with one or more pharmaceutically acceptable excipients, wherein the composition retains linezolid in its original crystalline form. | 2013-10-17 |
20130274263 | TUBULIN INHIBITORS | 2013-10-17 |
20130274264 | PIPERAZINO-DIHYDROTHIENOPYRIMIDINE DERIVATIVES - A method for treating diseases associated with the inhibition of phosphodiesterase 4 (PDE4) enzyme in a patient comprising administering to the patient in need thereof a therapeutically effective amount of a dihydrothienopyrimidinesulphoxide of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof | 2013-10-17 |
20130274265 | SUBSTITUTED-QUINOXALINE-TYPE BRIDGED-PIPERIDINE COMPOUNDS AND THE USES THEREOF - Compounds of Formula (I): | 2013-10-17 |
20130274266 | 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) - The present invention relates to novel 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, cerebrovascular amyloid angiopathy, multi-infarct dementia, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid. | 2013-10-17 |
20130274267 | INHIBITORS FOR ANTIVIRAL USE - The present invention relates to the use of potent selective LSD1 inhibitors and LSD1/MAO-B iithibitors for treating or preventing viral infections. Furthermore, the present invention relates to the new use of cyclopropylamine acetamide derivatives or cyclopropylamine derivatives, as defmed herein, for treating or preventing viral infection and treating or preventing reacti - vation of a virus after latency. | 2013-10-17 |
20130274268 | NEW BICYCLIC COMPOUND FOR MODULATING G PROTEIN-COUPLED RECEPTORS - The present invention relates to a bicyclic compound for modulating G protein-coupled receptors. The inventive compound provides preventing or treating a disease associated with the modulation of G protein-coupled receptors, particularly GPR119 G protein-coupled receptors. | 2013-10-17 |
20130274269 | NOVEL SUBSTITUTED ISOQUINOLINE DERIVATIVE - The present invention provides a novel isoquinoline-6-sulfonamide derivative that is useful as a medicine. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt, wherein R | 2013-10-17 |
20130274270 | POLYMORPHS OF 3-CHLORO-4[(2R)-2-(4-CHLOROPHENYL)-4-[(1R)-1-(4-CYANOPHENYL)ETHYL]-1-PIPE- RAZINYL]-BENZONITRILE, PHARMACEUTICAL COMPOSITIONS AND METHOD OF USE COMPRISING SAID POLYMORPHS, AND A PROCESS FOR PREPARING THEM - Polymorphs of 3-chloro-4[(2R)-2-(4-chlorophenyl)-4-[(1R)-1-(4-cyanophenyl)ethyl]-1-piperazinyl]-benzonitrile are disclosed, as well as pharmaceutical compositions comprising said polymorphs, methods of using the polymorphs, and a process for preparing them. | 2013-10-17 |
20130274271 | METHODS AND COMPOSITIONS FOR PREVENTION AND TREATMENTOF CARDIAC HYPERTROPHY - Methods are provided of treating cardiac hypertrophy in a mammalian subject comprising administering to the subject an anti-hypertrophic effective amount of an ion channel TR-PV1 inhibitor. The methods include treatment of a symptom of cardiac hypertrophy in the subject comprises cardiac remodeling, cardiac fibrosis, apoptosis, hypertension, or heart failure | 2013-10-17 |
20130274272 | METHYL/DIFLUOROPHENYL-METHOXY SUBSTITUTED PYRIDINONE-PYRIDINYL COMPOUNDS, METHYL-PYRIDINYL-METHOXY SUBSTITUTED PYRIDINONE-PYRIDINYL COMPOUNDS, AND METHYL-PYRIMIDINYL-METHOXY SUBSTITUTED PYRIDINONE-PYRIDINYL COMPOUNDS - The present disclosure provides methyl/difluorophenyl-methoxy substituted pyridinone-pyridinyl compounds, methyl-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds, and methyl-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): | 2013-10-17 |
20130274273 | Inhibiting Transient Receptor Potential Ion Channel TRPA1 - This disclosure describes a novel compounds and pharmaceutical compositions for inhibiting the TRPA1 ion channel and/or medical conditions related to TRPA1, such as pain. | 2013-10-17 |
20130274274 | SUBSTITUTED PYRIDOPYRIMIDINE COMPOUNDS AND THEIR USE AS FLT3 INHIBITORS - Compounds of Formula (I) and methods for inhibiting kinases, including spleen tyrosine kinases, are disclosed. Also disclosed are methods for treating a kinase-mediated disease or condition by administering to a subject a therapeutically effective amount of the compound of Formula (I). | 2013-10-17 |
20130274275 | 4-PHENYLAMINO-QUINAZOLIN-6-YL-AMIDES - This invention provides quinazoline compounds of the formula: | 2013-10-17 |
20130274276 | METHODS AND COMPOSITIONS FOR DETERMINING VIRUS SUSCEPTIBILITY TO NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS - Methods and compositions for the efficient and accurate determination of HIV susceptibility to a non-nucleoside reverse transcriptase inhibitor (NNRTI) are provided. In certain aspects, the methods involve detecting in a biological sample a nucleic acid encoding an HIV reverse transcriptase that comprises a mutation at codon 188, wherein the presence of the reverse transcriptase-encoding nucleic acid in the biological sample indicates that the HIV has a decreased susceptibility to an NNRTI. In certain embodiments, the HIV also contains one or more secondary mutations in reverse transcriptase. Also provided are methods for selecting a treatment for an HIV patient and methods for determining the selective advantage of a mutation or mutation profile. | 2013-10-17 |
20130274277 | TREATMENT FOR DISCOID LUPUS - Compounds I and II as well as salts and pharmaceutical compositions containing them are useful for treating diseases and/or disorders of the skin, such as cutaneous lupus, for example acute cutaneous lupus erythematosus, subacute cutaneous lupus erythematosus, or discoid lupus erythematosus. In certain embodiments, the compounds are provided in topical compositions. | 2013-10-17 |
20130274278 | IAP INHIBITORS - The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy. | 2013-10-17 |