05th week of 2014 patent applcation highlights part 51 |
Patent application number | Title | Published |
20140031284 | NEUREGULIN VARIANTS AND METHODS OF SCREENING AND USING THEREOF - The present invention provides polypeptide variants of neuregulin-1β (NRG-1β) that have enhanced or decreased binding affinity to ErbB3 and/or ErbB4. The invention also provides methods of screening and producing polypeptide variants of NRG-1β and methods of using polypeptide variants of NRG-1β for treating diseases. | 2014-01-30 |
20140031285 | PHOTODEGRADABLE GROUPS FOR TUNABLE POLYMERIC MATERIALS - Here, we present a photodegradable microparticle system that can be employed to entrap and deliver bioactive proteins to cells during culture. By using a photosensitive delivery system, experimenters can achieve a wide variety of spatiotemporally regulated release profiles with a single microparticle formulation, thereby enabling one to probe many questions as to how protein presentation can be manipulated to regulate cell function. Photodegradable microparticles were synthesized via inverse suspension polymerization with a mean diameter of 22 μm, and degradation was demonstrated upon exposure to several irradiation conditions. The protein-loaded depots were incorporated into cell cultures and release of bioactive protein was quantified during the photodegradation process. This phototriggered release allowed for the delivery of TGF-β1 to stimulate PE25 cells and for the delivery of fluorescently labeled Annexin V to assay apoptotic 3T3 fibroblasts during culture. By incorporating these photoresponsive protein delivery depots into cell culture, new types of experiments are now possible to test hypotheses about how individual or multiple soluble factors might affect cell function when presented in a uniform, temporally varying, or gradient manner. | 2014-01-30 |
20140031286 | Angiotensin (1-7) Dosage Forms and Uses Thereof - The present invention provides angiotensin (1-7) pharmaceutical compositions, dosage forms, and methods for their use, and methods for treating or limiting development of acquired immune deficiency syndrome. | 2014-01-30 |
20140031287 | COMPOUNDS, METHODS AND FORMULATIONS FOR THE ORAL DELIVERY OF A GLUCAGON-LIKE PEPTIDE (GLP-1) COMPOUND OR A MELANOCORTIN-4 RECEPTOR (MIC4) AGONIST PEPTIDE - The present invention relates to novel compounds, methods, and formulations useful for the oral delivery of a GLP-1 compound or an MC4 agonist peptide. | 2014-01-30 |
20140031288 | NOVEL COMPOSITION FOR TUMOR GROWTH CONTROL - The invention describes a pharmaceutical composition comprising at least compound selected from the group of demethylating agents and HDAC inhibitors and at least one somatostatin analog or dopamine agonist for the treatment of a tumor which expresses a somatostatin and/or dopamine receptor. | 2014-01-30 |
20140031289 | POLY(ORGANOPHOSPHAZENE) CONTAINING DEGRADATION CONTROLLABLE IONIC GROUP, PREPARATION METHOD THEREOF AND USE THEREOF - The present invention relates to a thermosensitive phosphazene-based polymer having a degradation controllable ionic group, a use thereof, and a use thereof as a material for delivering bioactive substances. The phosphazene-based polymer according to the present invention has the thermosensitivity of showing the temperature-dependent sol-gel phase transition. Thus, it forms a gel phase at the body temperature when it is injected into the body to make it easy to control the release of bioactive substances such as drugs, and has the functional groups capable of making chemical bonds such as ionic bond, covalent bond, coordinate bond, etc. with drugs and thus is excellent in bearing the drugs. Since it can control the degradation rate depending on the kind of ionic group, it can selectively control the release time depending on the characteristics of drugs. Furthermore, it has an excellent biocompatibility and thus is very useful as a material for delivery of bioactive substances such as drugs, etc. | 2014-01-30 |
20140031290 | NOVEL GLP-1 RECEPTOR STABILIZERS AND MODULATORS - Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided. | 2014-01-30 |
20140031291 | PP2A REGULATORY SUBUNIT MODIFICATION IN DISEASE - Disclosed herein are methods for the diagnosis, detection, and treatment of cardiovascular disease and symptoms thereof in a subject. Disclosed herein are methods of diagnosing ischemic heart disease, non-ischemic heart disease, myocardial infarction, tachy-pacing induced non-ischemic heart disease, heart failure, and catecholaminergic-induced arrhythmia and symptoms thereof in a subject. Disclosed herein are methods of screening the efficacy of a pharmaceutical agent for treating cardiovascular disease and symptoms thereof in a subject. Disclosed herein are methods of identifying a subject eligible for a cardiovascular disease treatment clinical trial | 2014-01-30 |
20140031292 | Yeast Cell Surface Display of Proteins and Uses Thereof - The present invention provides a genetic method of tethering polypeptides to the yeast cell wall in a form accessible for binding to macromolecules. Combining this method with fluorescence-activated cell sorting provides a means of selecting proteins with increased or decreased affinity for another molecule, altered specificity, or conditional binding. As one embodiment, attaching an scFv antibody fragment to the Aga2p agglutinin effectively mimics the cell surface display of antibodies by B cells in the immune system for affinity maturation in vivo. As another embodiment, T cell receptor mutants can be isolated by this method that are efficiently displayed on the yeast cell surface, providing a means of altering T cell receptor binding affinity and specificity by library screening. | 2014-01-30 |
20140031293 | THERAPEUTIC AGENTS WITH IMPROVED FIBRINOGEN BINDING - Therapeutic agents with improved fibrinogen binding properties are described. The agents are suitable for use as artificial platelets, or for formation of biogels. Methods and intermediates for producing the agents, cross-linking agents for use in the methods, and biogels formed from, or comprising the agents, are also described. | 2014-01-30 |
20140031294 | RECOMBINANT TRANSFERRIN MUTANTS - The present invention provides a recombinant protein comprising the sequence of a transferrin mutant, wherein Ser415 is mutated to an amino acid which does not allow glycosylation at Asn413 and/or wherein Thr613 is mutated to an amino acid which does not allow glycosylation as Asn611. It also provides polynucleotides encoding the same and methods of making and using said recombinant protein. | 2014-01-30 |
20140031295 | Recombinant C7 and Methods of Use - The present disclosure provides methods of treating epidermolysis bullosa, and/or preventing, preventing the progression of, or delaying the onset of one or more symptom associated with scarring, e.g., of blisters, in subjects with epidermolysis bullosa through chronic systemic administration of collagen 7. | 2014-01-30 |
20140031296 | NEW SYNTHETIC PEPTIDES AND THEIR USE - The present invention relates to new peptides and to use thereof, in particular for treatment and/or prevention of infections, inflammations, pain, wounds, scar and/or tumours. | 2014-01-30 |
20140031297 | COMPOUNDS FOR ENZYME INHIBITION - Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles. | 2014-01-30 |
20140031298 | Compositions and Methods for Localized Therapy of the Eye - Compositions, and methods of using such compositions, useful for injection into the posterior segments of human or animal eyes are provided. Such compositions include small particles of a poorly soluble therapeutic agent that facilitates formation of concentrated regions of the therapeutic agent in the retinal pigmented epithelium of an eye. The particles are formed by combining a therapeutic agent with an ophthalmically acceptable polymer component. The particles have sizes less than about 3000 nanometers, and in some cases, less than about 200 nanometers. One example of a composition includes particles of triamcinolone acetonide and hyaluronic acid have a size less than about 3000 nanometers. | 2014-01-30 |
20140031299 | NUTRITIONAL SUPPLEMENTS AND ASSOCIATED TREATMENT METHODS - A nutritional supplement, comprising a combination of resveratrol, nicotinic acid or a nicotinic acid precursor, and D-ribose in nutritionally effective amounts; and wherein the combination is configured to increase Sirtuin 1 enzymatic activity and to initiate increased NAD+ production for sustaining said Sirtuin 1 enzymatic activity. In some examples the nutritional supplement is configured to target a certain physiologic stress and is delivered in treatments including a resveratrol dose of 30 mg per day, a nicotinic acid or nicotinic acid precursor dose of 30 mg per day, and a D-ribose dose of 3 grams per day. | 2014-01-30 |
20140031300 | BENZYLBENZENE DERIVATIVES AND METHODS OF USE - Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition. | 2014-01-30 |
20140031301 | PHARMACEUTICAL COMPOSITION, METHODS FOR TREATING AND USES THEREOF - The invention relates to the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia using a SGLT-2 inhibitor. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions. | 2014-01-30 |
20140031302 | POCHOXIME CONJUGATES USEFUL FOR THE TREATMENT OF HSP90 RELATED PATHOLOGIES - The present invention includes novel derivatives, analogs, and intermediates of the natural products radicicol, pochonins, pochoximes, and their syntheses. The present invention also provides a pharmaceutical composition comprising the present compound and the use of the compound as inhibitors of kinases and of the enzyme family known as heat shock protein 90 (HSP90). | 2014-01-30 |
20140031303 | Bioactive hybrid of ionic/polyhydroxyl, lipophilic and covalently reactive moieties and method of use - A combination of the following three structures in a single molecule imparts a surprisingly broad range of beneficial effects in promoting and maintaining health. First, a strongly hydrophilic moiety, either a cation or anion or a polyhydroxyl group, with two or preferably three or more hydroxyl groups. Second, a lipophilic group, such as an alkyl chain of at least 8 carbons, and preferentially more, up to 18 or even 30-odd atoms in the chain. And third, a covalently reactive group, preferably with a strong tendency for binding to biosurfaces and biomolecules such as proteins, cell membranes, and/or nucleic acids, such as an epoxide, an acid anhydride, isocyanate or other reactive group(s) as herein defined. | 2014-01-30 |
20140031304 | ANTI-CHOLESTEROLEMIC COMPOUNDS AND METHODS OF USE - The present invention provides novel compounds with hypocholesteremic activity from crude | 2014-01-30 |
20140031305 | ANHYDROUS FOAMING COMPOSITION - The subject-matter of the present invention is an anhydrous cosmetic composition comprising, in a physiologically acceptable medium: —at least one nonionic surfactant, at least one anionic surfactant, at least 25% of at least one filler. The article is partially or completely soluble in water and it constitutes a foaming product used for cleansing the skin and hair and/or removing makeup from the skin and/or as scrubbing product. | 2014-01-30 |
20140031306 | SINGLE DOSE ORAL FORMULATIONS AND METHODS FOR TREATMENT OF CATS WITH ECTOPARASITICIDAL SPINOSAD - This invention provides a single-dose oral formulation of spinosad for the extended control of a | 2014-01-30 |
20140031307 | ANTI-INFLAMMATORY MACROLIDES - The invention provides novel compounds and compositions and methods for making and using the compounds and compositions. | 2014-01-30 |
20140031308 | BENCHMARKS FOR NORMAL CELL IDENTIFICATION - Provided herein are methods, compositions, and kits for determining cell signaling profiles in normal cells and comparing the cell signaling profiles of normal cells to cell signaling profiles from a test sample. | 2014-01-30 |
20140031309 | Beta-L-N4 Hydroxycytosine Deoxynucleosides and their use as Pharmaceutical Agents in the Prophylaxis or Therapy of Viral Diseases - The invention relates to ss-L-N4-hydroxycytosine nucleo-sides, pharmaceutical agents comprising same, and to the use of said ss-f31 L-N4-hydroxycytosine nucleosides and pharmaceutical agents in the prophylaxis or therapy of an infection caused by hepatitis B virus (HBV) or human immunodeficiency virus (HIV). The invention also relates to a method for the preparation of said ss-L-nucleoside and analogs. | 2014-01-30 |
20140031310 | PHARMACEUTICAL COMPOSITIONS AND METHODS FOR MAKING AND USING THEM - In alternative embodiments the invention provides compositions, e.g., pharmaceutical compositions and preparations, formulations, kits and other products of manufacture, e.g., exemplary drug combinations packaged together or separately in blister packs, lidded blisters or blister cards, or wrapped in paper, plastic or cellophane wrappers (e.g., a shrink wrap), comprising combinations of beneficial ingredients that in alternative embodiments are serviceable as therapies or palliatives for treating, preventing or improving conditions, states and disease symptoms involving the use of targeted protein kinase inhibitors such as Multi-Kinase Inhibitors (MKIs) or Epidermal Growth Factor Receptor (EGFR) Inhibitors (EGFRIs), or the use of other oral oncolytics, such as capcitabine or erlotinib, known to be associated with drug-induced dermatological toxicity, e.g., in the amelioration or treatment of a cancer, a dermatitis, a rosacea, an eczema, an ichthyosis, or a related condition; and methods for making and using these compositions; and methods for making and using these compositions. | 2014-01-30 |
20140031311 | TREATMENT OF REYNAUD'S DISEASE - A method of treating a patient inflicted with Reynaud's Disease including the step of injecting into the back of the patient's hand an effective amount of a hyaluronic product, thereby creating a glove-like insulation to decrease the blood vessel vasospasm. | 2014-01-30 |
20140031312 | COMPOSITIONS AND FORMULATIONS OF GLUCOSAMINE FOR TRANSDERMAL AND TRANSMUCOSAL ADMINISTRATION - Disclosed are compositions and formulations comprising glucosamine or a pharmaceutically acceptable salt thereof for use in the treatment of joint conditions and adapted for use in a bath or soak or bath beads, powders, salts, and oils, kits, and methods of treatment using the same. Also disclosed are lozenges, suppositories, patches, and topical creams comprising glucosamine or a pharmaceutically acceptable salt thereof for use in the treatment of joint conditions and methods of treatment using the same. In some embodiments the joint conditions include osteoarthritis. | 2014-01-30 |
20140031313 | Mimicking the Metabolic Effects of Caloric Restriction by Administration of Glucose Anti-Metabolites - Methods of maintaining and/or attenuating a decline in the quality of life of a mammal comprising the step of administering to the mammal a composition comprising an effective amount of mannoheptulose wherein the effective amount of mannoheptulose provides a dosage to the mammal on a daily basis from about 0.001 gram per kilogram of body weight of the mammal to about 1 gram per kilogram of body weight of the mammal. | 2014-01-30 |
20140031314 | METHOD OF PREPARATION OF CHITIN AND ACTIVE PRINCIPLE COMPLEXES AND COMPLEXES OBTAINED - The present invention relates to chitin nanofibrils complexes in association with at least one negatively charged polymer and one or more active ingredients; pharmaceutical or cosmetic compositions comprising such complexes, kit for concomitant or sequential administration comprising said compositions in a form suitable for topical administration and in a form suitable for oral administration, and uses thereof. | 2014-01-30 |
20140031315 | POLYSACCHARIDE COMPOSITIONS AND METHODS OF USE FOR THE TREATMENT AND PREVENTION OF DISORDERS ASSOCIATED WITH PROGENITOR CELL MOBILIZATION - Polysaccharide preparations lacking substantial anticoagulant activity are provided herein. Methods of making and using such preparations are provided. | 2014-01-30 |
20140031316 | POLYSACCHARIDES COMPRISING TWO ANTITHROMBIN III-BINDING SITES, PREPARATION THEREOF AND USE THEREOF AS ANTITHROMBOTIC MEDICAMENTS - The invention relates to sulphated polysaccharides which have the general structure of the constituent polysaccharides of heparin and which have a molecular weight of less than 8000 Daltons, comprising two antithrombin III-binding hexasaccharide sequences corresponding to formula (I) in which: R1 represents an OH group when the hexasaccharide of formula (I) is located at the reducing end of the polysaccharide, or else R1 represents a bond with another saccharide unit of said polysaccharide; R2 represents a hydrogen atom when the hexasaccharide of formula (I) is located at the non-reducing end of the polysaccharide, in which case the bond between carbon atoms 4 and 5 of the first saccharide unit of said hexasaccharide is a double bond, or else R2 represents a bond with another saccharide unit of said polysaccharide, in which case the bond between carbon atoms 4 and 5 of the first saccharide unit is a single bond. Preparation thereof, use thereof as antithrombotic medicaments, and also use thereof in a method for analysing a sample of a heparin derivative. | 2014-01-30 |
20140031317 | NOVEL 2-SUBSTITUTED BENZIMIDAZOLES AS SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMS) - The present invention is directed to a novel 2-substituted benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor. | 2014-01-30 |
20140031318 | SOLID FORMS OF (R)-2-(5-(2-(3-ETHYLUREIDO)-6-FLUORO-7-(TETRAHYDROFURAN-2-YL)-1H-BENZO[d]- IMIDAZOL-5-YL)PYRIMIDIN-2-YL)PROPAN-2-YL DIHYDROGEN PHOSPHATE AND SALTS THEREOF - The invention relates to solid forms of the Formula (I) | 2014-01-30 |
20140031319 | METHODS FOR SYNTHESIZING AND PURIFYING AMINOALKYL TETRACYCLINE COMPOUNDS - Methods for the synthesis and purification of 9-amino alkyl tetracycline compounds are described. | 2014-01-30 |
20140031320 | Anti-Thrombotic Compounds - New compounds, namely, (7aS,2′S)-2-oxoclopidogrel and its pharmaceutically acceptable salts thereof are disclosed for treatment or prophylaxis of thrombo-embolism and/or cardiovascular diseases. | 2014-01-30 |
20140031321 | METHOD OF INDUCING NEGATIVE CHEMOTAXIS - The current invention is directed to methods of inducing the negative chemotaxis of a migratory cell comprising contacting the cell with a compound selected from the group consisting of idebenone, benazepril, rolipram, moxonidine, lamivudine, loxoprofen, terbinafine, synephrine, 6-aminoindazole, and a Vitamin D analog, or a pharmaceutically acceptable salt of any of thereof. | 2014-01-30 |
20140031322 | MEDICINE COMPOSITION CONTAINING VITAMIN D AND METFORMIN - A medicine composition contains vitamin D and metformin, wherein vitamin D comprises vitamin D2, vitamin D3, alphacalcidol, calcifediol, calcitriol, and dihydrotachysterol. The composition can be used in the preparation of a medicine for treating and/or preventing a polyp and cancer in large intestine. | 2014-01-30 |
20140031323 | TRANSDERMAL HORMONE COMPOSITION AND COMBINED STATIC-CYCLIC DELIVERY - The various embodiments of the present invention relate to a human identical flowable hormone composition dispersed in a cream or gel contained in the novel “Smart” metered dose applicator, which facilitates numerous patient specific dosing options, dose titration, as well as continuous and variable dosing. The composition is designed for transdermal usage for consumers who follow a specified dosage protocol resulting in static and cyclic variations on serum hormone levels over a 28 day cycle stretched over the span of a month. The regimen is modeled after nature, in an attempt to replicate temporal variations in serum progesterone and estradiol hormone levels of premenopausal females with healthy hormone cycles. A dispenser is also disclosed for flowable cream-base medicaments, specifically; a unidirectional rotatable platform attached to a screw that is slipped into a barrel where it is secured in place and it joins the said components that house an elevator. | 2014-01-30 |
20140031324 | COMPOUND COMPOSITION FOR INHALATION USED FOR TREATING ASTHMA - A compound composition for inhalation comprising β2 receptor agonist and corticosteriod is provided in the present invention. The composition is used as a reliever for a patient with asthma or chronic obstructive pulmonary disease, or a controller in eccentric way, and can reduce drug acute resistance of β2 receptor agonist. | 2014-01-30 |
20140031325 | COMBINATION THERAPY WITH LENALIDOMIDE AND A CDK INHIBITOR FOR TREATING MULTIPLE MYELOMA - Provided herein are methods for the treatment of multiple myeloma, wherein the methods comprise administration of lenalidomide and administration of a second active agent such as a CDK inhibitor. | 2014-01-30 |
20140031326 | METHODS FOR THE TREATMENT OF FIBROMYALGIA AND CHRONIC FATIGUE SYNDROME - The invention relates to methods for the treatment of fibromyalgia and chronic fatigue syndrome by administration of a transdermally applied androgen composition. The treatment is both safe and effective for treating fibromyalgia-related pain and fatigue, as well as chronic fatigue syndrome. | 2014-01-30 |
20140031327 | NON-SURGICAL METHOD OF TREATMENT FOR CATARACT - The invention provides inhibitors of α-crystallin aggregation and methods of using α-crystallin aggregation inhibitors to, e.g., treat or prevent cataracts in a subject having or at risk of developing cataracts. The invention further provides high throughput methods of screening compounds for modulation of protein thermal stability, the method comprising contacting a protein with each of a plurality of test compounds; and (b) measuring the melting transition (T | 2014-01-30 |
20140031328 | Gallium compounds and methods of use to treat inflammatory bowel disease - Provided are formulations and methods for treating inflammatory bowel disease, including Crohn's disease, ulcerative colitis, and Johne's disease. The formulations provided comprise pharmaceutically acceptable gallium compounds; the methods provided comprise means of using such formulations in the treatment of inflammatory bowel disease and closely related disorders. | 2014-01-30 |
20140031329 | SUBSTITUTED DIHYDROPYRAZOLONES FOR TREATING CARDIOVASCULAR AND HEMATOLOGICAL DISEASES - The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing. | 2014-01-30 |
20140031330 | ARYL SULTAM DERIVATIVES AS RORc MODULATORS - Compounds of the formula I: | 2014-01-30 |
20140031331 | AMINOTETRALINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to aminotetraline derivatives of the formula (I) | 2014-01-30 |
20140031332 | Biomarkers for Sensitive Detection of Statin-Induced Muscle Toxicity - The present invention inter alia provides a method, and uses thereof, of predicting statin-induced muscle toxicity or its complications, such as myalgia, myopathy and rhabdomyolysis, by detecting the lipid concentrations or lipid ratios of a biological sample and comparing it to a control. This method has identified lipid markers that are more specific and sensitive in detecting these statin-induced muscle toxicity than the currently utilized clinical markers. Also provided is an antibody towards said lipids, and the use thereof for predicting, diagnosing, statin-induced muscle toxicity. The invention additionally relates to kits comprising lipids and/or an antibody thereto, for use in the prediction and/or diagnosis of statin-induced muscle toxicity. | 2014-01-30 |
20140031333 | COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS - The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFRα, PDGFRβ) kinases. | 2014-01-30 |
20140031334 | DERIVATIVES OF 4-PIPERAZIN-1-YL-4-BENZO[B]THIOPHENE SUITABLE FOR THE TREATMENT OF CNS DISORDERS - A heterocyclic compound or a salt thereof represented by the formula (1): | 2014-01-30 |
20140031335 | CYCLOALKENYL ARYL DERIVATIVES FOR CETP INHIBITOR - The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the present invention show the effect of CETP activity inhibition. It means that the compounds can increase HDL-cholesterol and decrease LDL-cholesterol. | 2014-01-30 |
20140031336 | Tetrahydroquinoline Derivatives Useful As Bromodomain Inhibitors - Tetrahydroquinoline compounds, pharmaceutical compositions containing such compounds and their use in therapy. | 2014-01-30 |
20140031337 | AZOLOTRIAZINONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS - The present application provides compounds that are useful as MCHR1 antagonists, especially for the treatment of obesity, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I | 2014-01-30 |
20140031338 | INHIBITORS OF VIRAL REPLICATION, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES - The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV. | 2014-01-30 |
20140031339 | INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I): | 2014-01-30 |
20140031340 | 5-Amino-Oxazepine and 5-Amino-Thiazepane Compounds as Beta Secretase Antagonists and Methods of Use - The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula (I); wherein variables A | 2014-01-30 |
20140031341 | MODULATORS AND METHODS FOR THE TREATMENT OF ROSACEA - An in vitro method of screening candidate compounds for the preventive or curative treatment of rosacea is described. The method can include determining the capacity of a compound to modulate the expression or activity of the Transient Receptor Potential (TRPs), as well as the use of modulators of the expression or activity of this transcription factor for the treatment of rosacea. The method can also include in vitro diagnosis or prognosis of this pathology. | 2014-01-30 |
20140031342 | 6,7-DIHYDROIMIDAZO [2,1-b] [1,3]OXAZINE BACTERICIDES - The present invention provides a novel 6,7-dihydroimidazo[2,1-b][1,3]oxazine compound that has excellent bactericidal action against tubercle bacilli, multidrug-resistant tubercle bacilli, and atypical acid-fast bacilli. Specifically, the present invention provides a compound represented by Formula (1): | 2014-01-30 |
20140031343 | DRUG COMBINATIONS CONTAINING PDE4 INHIBITORS AND NSAIDS - Drug combinations which contain a PDE4-inhibitor and a non-steroidal anti-inflammatory drug (NSAID), processes for preparing them, and their use in treating in particular respiratory complaints such as COPD, chronic sinusitis, and asthma. The PDE4 inhibitors of the drug combinations include compounds of general formula 1 | 2014-01-30 |
20140031344 | AZEPINE INHIBITORS OF JANUS KINASES - The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 2014-01-30 |
20140031345 | QUINAZOLINES AS POTASSIUM ION CHANNEL INHIBITORS - A compound of formula I | 2014-01-30 |
20140031346 | 5,6-DIHYDRO-1H-PYRIDIN-2-ONE COMPOUNDS - The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I | 2014-01-30 |
20140031347 | 1,2,4-OXADIAZOLE DERIVATIVES AS DRUGS MODULATING THE GLP-1 PEPTIDE RECEPTOR - The present invention relates to the use of a compound of formula (I): | 2014-01-30 |
20140031348 | HETEROARYL SULFONAMIDES AND CCR2/CCR9 - Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists. | 2014-01-30 |
20140031349 | INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL - The present invention provides compounds of Formula I | 2014-01-30 |
20140031350 | 2,4-Pyrimidinediamine Compounds and Their Uses - The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades. | 2014-01-30 |
20140031351 | Macrocyclic Compounds as ALK, FAK and JAK2 Inhibitors - The present invention provides compounds of Formula I | 2014-01-30 |
20140031352 | SOLID FORMS OF TYROSINE KINASE INHIBITORS, PROCESS FOR THE PREPARATION AND THEIR PHARMACEUTICAL COMPOSITION THEREOF - The present invention generally relates to solid forms of tyrosine kinase inhibitors, in particular combinations of tyrosine kinase inhibitors with anti-oxidative acids, processes for its preparation and a pharmaceutical compositions containing the same. | 2014-01-30 |
20140031353 | COMPOUND AS ANTAGONIST OF LYSOPHOSPHATIDIC ACID RECEPTOR, COMPOSITION, AND USE THEREOF - The present invention relates to a compound as antagonist of LPA receptor, and a pharmaceutical composition comprising the same. The present invention also relates to the use of the compound and the composition, and a method of using the compound to treat, prevent or diagnose diseases, disorders or conditions associated with one or more of the LPA receptors. | 2014-01-30 |
20140031354 | Protein Kinase Inhibitors - The present invention relates to compounds of Formula I: | 2014-01-30 |
20140031355 | HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity. The present invention also enables methods for treating cancers that are mediated, dependent on or associated with pi 105 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. | 2014-01-30 |
20140031356 | THERAPY FOR LEUKEMIA - A pharmaceutically acceptable composition and method for leukemia therapy in a patient in need of such therapy. The composition contains, as the only active agents, the combination of (a) an inhibitor of c-Fos, (b) an inhibitor of Dusp-1, and (c) an inhibitor of BCR-ABL tyrosine kinase. The composition is administered to the patient in a dosing regimen for a period sufficient to provide therapy for leukemia. | 2014-01-30 |
20140031357 | ASYMMETRICALLY SUBSTITUTED ANTHRAPYRIDAZONE DERIVATIVES AS CYTOSTATICS - The invention relates to the new, asymmetrically substituted derivatives of 2,7-dihydro-3H-dibenzo[de,h]cinnoline-3,7-dione and their use as cytostatics exhibiting activity against tumor cells, especially against cells with multidrug resistance (MDR). In particular, the invention concerns derivatives of 2,7-dihydro-3H-dibenzo[de,h]cinnoline-3,7-dione represented by the general formula (I). | 2014-01-30 |
20140031358 | QUINAZOLINEDIONES AND THEIR USE - The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts or prodrugs thereof, which inhibit the poly(ADP-ribose) polymerases (PARP) and therefore are useful for treating diseases, disorders, and conditions related to PARP. The present invention also discloses pharmaceutical compositions comprising a compound of formula (I), and methods of using such compounds to inhibit PARP enzymes, and to treat diseases, disorders, and conditions related to PARP. | 2014-01-30 |
20140031359 | Method Of Treating Metabolic Disorders And Depression With Dopamine Receptor Agonists - This invention relates to methods and formulations for treating metabolic disorders and depression. In some embodiments, the methods comprise administering a dopamine receptor agonist and an anti-depressant. | 2014-01-30 |
20140031360 | BICYCLIC COMPOUNDS AS PIM INHIBITORS - The invention relates to bicyclic compounds of formula (1′), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer. | 2014-01-30 |
20140031361 | INHIBITORS OF PROTEIN KINASES - The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 2014-01-30 |
20140031362 | TRI - AND TETRACYCLIC PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS AS ANTINEOPLASTIC AGENT - The present invention relates to compounds of following general formula (I): and to the pharmaceutically acceptable salts of same, the tautomers of same, the stereoisomers or mixture of stereoisomers in any proportions of same, such as a mixture of enantiomers, notably a racemic mixture, as well as to methods for preparing same and uses of same, notably as an antineoplastic agent. | 2014-01-30 |
20140031363 | NMDA Receptor Antagonists for Neuroprotection - Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: | 2014-01-30 |
20140031364 | PHENYL-ISOXAZOL DERIVATIVES AND PREPARATION PROCESS THEREOF - Disclosed are a phenyl-isoxazol derivative compound, which is useful as a treatment material for virus infection, especially, infection of an influenza virus, or its pharmaceutically acceptable derivative, a preparation method thereof, and an illness treatment pharmaceutical composition including the compound as an active ingredient. | 2014-01-30 |
20140031365 | USE OF A POLYMORPH OF FLIBANSERIN FOR TREATING DISEASE - The invention relates to the polymorph A of flibanserin, to a technical process for the preparation thereof, as well as to the use thereof for preparing medicaments. | 2014-01-30 |
20140031366 | AZOLE PHARMACEUTICAL FORMULATIONS FOR PARENTERAL ADMINISTRATION AND METHODS FOR PREPARING AND USING THE SAME AS TREATMENT OF DISEASES SENSITIVE TO AZOLE COMPOUNDS - A parenteral azole composition comprises a first solvent, made of benzyl alcohol and/or an acidified alcohol such as ethanol, and a lipophilic component such as PEG400, and the azole, or triazole, such as itraconazole or posaconazole dissolved in this first composite solvent vehicle that is essentially free of surfactants, particularly non-ionic surfactants, and has low levels of water, preferably less than 5% water. The composition may be further diluted with an infusion fluid, such as normal saline or 5% or 10% dextrose in water, before infusion into an immunocompromized mammal, preferably a human. The composition is useful for the treatment and suppression of infections caused by microbes such as yeast and molds that are sensitive to azoles, but it may be extended to dissolve other pharmaceutically active agents that can be used to treat other types of infectious diseases or other ailments, such as malignant and autoimmune diseases. | 2014-01-30 |
20140031368 | SELECTIVE HDAC INHIBITORS - This disclosure is related to compounds having the structure | 2014-01-30 |
20140031369 | N-CYCLOPROPYL-N-PIPERIDINYL-AMIDE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USES THEREOF - The present invention relates to compounds of general formula I, | 2014-01-30 |
20140031370 | AMIDE DERIVATIVES, PROCESS FOR PREPARATION THEREOF AND USE THEREOF AS INSECTICIDE - A compound represented by Formula (1): | 2014-01-30 |
20140031371 | POLY AROMATIC SODIUM CHANNEL BLOCKERS - Polyaromatic sodium channel blockers represented by the formula: | 2014-01-30 |
20140031372 | CICLETANINE IN COMBINATION WITH ORAL ANTIDIABETIC AND/OR BLOOD LIPID-LOWERING AGENTS AS A COMBINATION THERAPY FOR DIABETES AND METABOLIC SYNDROME - Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and/or preventing complications in patients with diabetes and/or metabolic syndrome. More particularly, aspects of the present invention are related to using a combination of cicletanine and an oral antidiabetic agent for treating and/or preventing complications (including microalbuminuria, nephropathies, retinopathies and other complications) in patients with diabetes or metabolic syndrome. | 2014-01-30 |
20140031373 | PYRIMIDINE DERIVATIVES AND USE THEREOF AS PESTICIDES - The present invention relates to novel substituted pyrimidine derivatives, to processes for preparing these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators. | 2014-01-30 |
20140031374 | TRIAZOLE DERIVATIVES AS WNT SIGNALING PATHWAY INHIBITORS - The present invention relates to compounds of formula (I), to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy: Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway and increased presence of nuclear β-catenin. For example, these may be used in preventing and/or retarding proliferation of tumor cells and metastasis, for example carcinomas such as colon carcinomas. | 2014-01-30 |
20140031375 | A1 ADENOSINE RECEPTOR ANTAGONISTS - This invention relates to compounds of formula (I), Wherein R | 2014-01-30 |
20140031376 | IMINOPROPENE COMPOUND AND USE THEREOF - The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition. | 2014-01-30 |
20140031377 | MULTICOMPONENT CRYSTALLINE SYSTEM OF ROSUVASTATIN CALCIUM SALT AND VANILLIN - A novel solid form of Rosuvastatin comprises as the active ingredient a salt of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)-amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid] and vanillin or vanillin derivatives. The crystal comprising the two components, and minor amounts of water, shows improved properties such as crystallization behavior stability and decreased hydroscopic behavior. | 2014-01-30 |
20140031378 | INSECTICIDAL SPIRONINDANE DERIVATIVES - An insecticidal compound of formula I | 2014-01-30 |
20140031379 | Camsylate Salt - A camsylate salt of (1r,1′R,4R)-4-methoxy-5″-methyl-6′-[5-(prop-1-yn-1-yl)pyridin-3-yl]-3′H-dispiro[cyclohexane-1,2′-inden-1′2′-imidazole]-4″-amine, pharmaceutical compositions containing the salt and therapeutic uses of the salt for treating Aβ-related pathologies such as Alzheimer's Disease, Down's syndrome, β-amyloid angiopathy and conditions such as dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. | 2014-01-30 |
20140031382 | DOSAGE FORM CONTAINING OXYCODONE AND NALOXONE - The present invention concerns a dosage form comprising oxycodone and naloxone which is characterized by specific in vivo parameters such as t | 2014-01-30 |
20140031383 | METHODS FOR TREATMENT OF MELANOMA - The present invention is directed to methods for treatment of melanoma using an inhibitor of dihydroorotate dehydrogenase (DHODH) and to combination therapies that involve administering to a subject an inhibitor of oncogenic BRAF (e.g. BRAF(V600E)), as well as an inhibitor of dihydroorotate dehydrogenase (DHODH). Assays for identifying compounds useful for the treatment of melanoma are also provided. The methods herein are directed to screening for compounds or agents that inhibit neural crest progenitor formation in a zebra fish model of melanoma. | 2014-01-30 |
20140031384 | THERAPEUTIC AGENT FOR TUMOR - A therapeutic agent for tumor for combined use of a compound or pharmaceutically acceptable salt thereof represented by Formula (I) and a compound represented by Formula (II): | 2014-01-30 |
20140031385 | THERAPEUTIC PYRAZOLYL THIENOPYRIDINES - The present invention provides for compounds of Formula I, and pharmaceutically acceptable salts thereof, | 2014-01-30 |
20140031386 | NOVEL ANTI-PLATELET COMPOUND ADDITION SALT - The present invention relates to a use of haloid acid salt and sulfonate of a compound of formula I and a salt of the compound of formula I in preparation of medicament for preventing or treating diseases caused by thrombosis or embolism. The present invention provides acid addition salts, especially haloid acid and sulfonic acid addition salts of a compound of formula I having high inhibition effect on platelet aggregation, and preparation method of the same, a medicament comprising the same, and a use and/or method for preventing or treating diseases caused by thrombosis or embolism. | 2014-01-30 |