24th week of 2012 patent applcation highlights part 52 |
Patent application number | Title | Published |
20120149650 | Diphtheria Toxin Variant - The present invention relates to methods and compositions of modified variants of diphtheria toxin (DT) that reduce binding to vascular endothelium or vascular endothelial cells, and therefore, reduce the incidence of Vascular Leak Syndrome. One aspect of the present invention relates to a polypeptide toxophore from a modified DT, wherein the mutation is the substitution or deletion at least one amino acid residue at the amino acid residues 6-8, 28-30 or 289-291 of native DT. Another aspect of the present invention relates to a fusion protein which comprises a modified DT and a non-DT fragment. Another aspect of the present invention relates to the use of modified DT for the treatment of cancer. | 2012-06-14 |
20120149651 | Caveolin peptides and their use as therapeutics - The present invention relates generally to compositions and methods useful for treating various conditions and afflictions, such as inflammation and cancer. More specifically, the present invention relates to compositions and methods of treatment which utilize peptides comprising at least one caveolin scaffolding domain. Even more specifically, the present invention relates to compositions of fusion peptides comprising the antennapedia homeodomain fused to a caveolin scaffolding domain and to methods of using these peptides to treat various conditions and afflictions. | 2012-06-14 |
20120149652 | USE OF PEPTIDES COMPRISING POST-TRANSLATIONAL MODIFICATIONS IN THE TREATMENT OF AUTOIMMUNE PATHOLOGIES - Peptides including post-translational-type modifications, such as phosphorylation or acetylation of one or more amino acids, are provided. Processes for obtaining the peptides, pharmaceutical compositions including the peptides and methods for treating autoimmune diseases using the peptides are also provided. | 2012-06-14 |
20120149653 | MULTIFUNCTIONAL LINKERS AND METHODS FOR THE USE THEREOF - In accordance with the present invention, novel multifunctional compounds have been developed which have orthogonal reactive groups thereon, thereby facilitating preparation of compounds having multiple functional properties (e.g., a targeting moiety and a biologically active moiety). Such constructs are useful for a variety of applications, e.g., for the delivery of biologically compatible materials, and release thereof in active form. Therefore, in accordance with the present invention, there are provided multifunctional linkers of defined structure, as well as various derivatives thereof bearing one or more biologically active components thereon. Also provided in accordance with the present invention are methods for the preparation of such constructs, as well as various uses thereof. | 2012-06-14 |
20120149654 | HUMIC SUBSTANCES AND USES THEREOF IN AGRO-ENVIRONMENT - The present invention relates to the two main categories of humic substances, humic acids and fulvic acids and their use for hindering the propagation and/or contamination with prion infectivity both in agricultural and environmental systems. | 2012-06-14 |
20120149655 | USE OF JASMONATE TO TREAT BLADDER DYSFUNCTION - A formulation or composition contractility comprising jasmonate for modulating bladder and/or treating bladder dysfunction, particularly an overactive bladder in a mammal, particularly a human and use of jasmonate for treating bladder dysfunction is provided. | 2012-06-14 |
20120149656 | WATER SOLUTION OF 20(R) - GINSENOSIDE Rg3 PHARMACEUTICAL COMPOSITION AND PROCESS THEREOF - A preparation of a kind of 20(R)-ginsenoside Rg3 medicinal composition aqueous solution containing ginsenoside Rg3 0.5˜10 mg/ml: add 0.1-5% of ginsenoside solution to 0.1˜30% of adjuvant A, B{circle around (1)}{circle around (2)}{circle around (5)} at the temperature of 40˜100° C., the ratio of these two is 1:1˜300, add water after the solvent is recycled under reduced pressure; another kind of 20(R)-ginsenoside Rg3 medicinal composition aqueous solution contains 0.1˜2 mg/ml of 20 (R) of the ginsenoside Rg3, the preparation: add 0.1˜5% of ginsenoside solution to 20˜65% of adjuvant B{circle around (3)}{circle around (4)} at the temperature of 60˜100° C., main material to adjuvant B=1:100˜400, add water after the solvent is recycled under reduced pressure. The above 20 (R) ginsenoside Rg3 composition aqueous solution and the powder after lyophilizaton can be used to prepare injectable, oral administration and external use, and the bioactivity of these preparations is high, and with the actions of anti cancer, efficacy potentiation and toxicity attenuation effects of the combined chemical or radiation therapy of tumor, enhancement of human immune functions, improvement of human memory, anti fatigue, and detumescence, pain relieving. | 2012-06-14 |
20120149657 | 2'-FLUORO ARABINO NUCLEOSIDES AND USE THEREOF - A method of treating cancer using certain 2′-fluoro arabino nucleosides is provided. Also provided are compounds represented by the formula: (I & A) wherein R is alkyl; and pharmaceutically acceptable salts thereof; and pharmaceutical compositions containing these compounds. | 2012-06-14 |
20120149658 | MODIFIED PECTINS, COMPOSITIONS AND METHODS RELATED THERETO - The present invention provides compositions of modified pectin and methods for preparing and using them. | 2012-06-14 |
20120149659 | COMPOSITIONS AND METHODS FOR DELIVERING AN AGENT TO A WOUND - The invention provides compositions featuring chitosan and methods for using such compositions for the local delivery of biologically active agents to an open fracture, complex wound or other site of infection. Advantageously, the degradation and drug elution profiles of the chitosan compositions can be tailored to the needs of particular patients at the point of care (e.g., in a surgical suite, clinic, physician's office, or other clinical setting). | 2012-06-14 |
20120149660 | NOVEL N-SUBSTITUTED 5-HYDROXYPYROLLINDES AS INHIBITORS OF MDM2-P53 INTERACTIONS - There are provided compounds of formula I | 2012-06-14 |
20120149661 | TETRA-SUBSTITUTED HETEROARYL COMPOUNDS AND THEIR USE AS MDM2 AND/OR MDM4 MODULATORS - The invention relates to tetra-substituted heteroarylic compounds of the formula (I) | 2012-06-14 |
20120149662 | Heterocyclic Compounds as Janus Kinase Inhibitors - The invention provides compounds of formula (I): | 2012-06-14 |
20120149663 | BORONIC ACID COMPOSITIONS AND METHODS RELATED TO CANCER - Disclosed are compounds and methods related to boronic acid derivatives of resveratrol. Certain of these derivatives have enhanced efficacy relative to resveratrol, function as irreversible modulators, and act at the GI/S phase of the cell cycle. | 2012-06-14 |
20120149664 | Transdermal Composition of Phosphatidylcholine and Method for Producing Same - Disclosed is a transdermal composition, which uses high-purity phosphatidylcholine that is most susceptible to oxidation and the like, and which exhibits high stability and high migration into the skin. Specifically, a transdermal composition having good stability and migration into the skin is able to be obtained by preparing a transdermal composition (a colloidal dispersion liquid of phosphatidylcholine) that contains high-purity phosphatidylcholine, carnitine, a polyhydric alcohol and water. Since the transdermal composition does not contain an oleaginous base (an oil component), the transdermal composition has skin compatibility and is thus useful as a therapeutic agent or a cosmetic preparation. In addition, phosphatidylcholine and carnitine have an effect of achieving good migration into the skin and are capable of promoting systemic or local lipid metabolism in subcutaneous adipose tissues. Consequently, the transdermal composition is able to provide a transdermal preparation that is capable of promoting lipolysis in subcutaneous adipose tissues. | 2012-06-14 |
20120149665 | COMBINATION THERAPY FOR TREATING PROLIFERATIVE DISEASES - A pharmaceutical composition of a tubulin polymerisation inhibitor and an mTOR inhibitor and a method of treating proliferative disease with a combination of a tubulin polymerisation inhibitor and an mTOR inhibitor. | 2012-06-14 |
20120149666 | COMPOSITIONS AND METHODS OF TREATMENT FOR INFLAMMATORY DISEASES - Inflammatory bowel diseases are represented by two idiopathic disorders, which include ulcerative colitis and Crohn's disease. Ulcerative colitis is restricted to the colon and involves uncertain and inflammation of the lining (mucosa) of the large intestine. Crohn's disease, on the other hand, can involve the mucosa of the small and/or large intestine and may involve deeper layers of the bowel wall. The present invention is a combination of 5-aminosalicylic acid and one or more antioxidants (e.g., N-acetylcysteine) for treating such inflammatory bowel diseases. | 2012-06-14 |
20120149667 | PHARMACEUTICAL COMPOSITIONS FOR TREATING IBD - A stable and/or synergistic pharmaceutical composition including: a) predinisolone metasulfobenzoate (PMSB) or its acceptable salts, preferably prednisolone metasulfobenzoate sodium and b) 5-ASA, derivatives or pharmaceutically acceptable salts thereof, which is suitable for rectal administration. | 2012-06-14 |
20120149668 | GLUCOCORTICOID RECEPTOR ALLELES AND USES THEREOF - Provided here in are, inter alia, methods of determining whether a patient is resistant or sensitive to glucocorticoid therapy. | 2012-06-14 |
20120149669 | 22-Haloacetoxy-Homopregnacalciferol Analogs and Their Uses - This invention discloses 22-haloacetoxy-homopregnacalciferol analogs and specifically 22-bromoacetoxy-homopregnacalciferol and pharmaceutical uses therefor. This compound exhibits relatively little calcemic activity and does not promote cellular differentiation off HL-60 leukemia cells, but rather kills the cells. This cell death activity is found in small cell lung carcinoma also, but not in prostate cancer cells. This compound thus causes specific cell death in the absence of changes in calcium levels and without general toxicity in an animal. Therefore it might serve as a useful therapy for treatment of some forms of cancer, such as leukemia and lung cancer. | 2012-06-14 |
20120149670 | 17-HYDROXY-17-PENTAFLUOROETHYL-ESTRA-4,9(10)-DIEN-11-ARYL DERIVATIVES, METHOD OF PRODUCTION THEREOF AND USE THEREOF FOR THE TREATMENT OF DISEASES - The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of Formula I with progesterone antagonizing action and method of production thereof, use thereof for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular of fibroids of the uterus (myomas, uterine leiomyoma), endometriosis, heavy menstrual bleeds, meningiomas, hormone-dependent breast cancers and complaints associated with the menopause or for fertility control and emergency contraception. | 2012-06-14 |
20120149671 | 17ALPHA, 21-DIHYDROXYPREGNENE ESTERS AS ANTIANDROGENIC AGENTS - 17α,21-Dihydroxypregna-4,9-diene-3,20-dione and 17α,21-dihydroxypregna-4-ene-3.20-dione 17 and/or 21 esters of having remarkable antiandrogenic activity, and the processes for the preparation thereof. | 2012-06-14 |
20120149672 | METHYLSULFONYLMETHANE (MSM) FOR TREATMENT OF DRUG RESISTANT MICROORGANISMS - Embodiments of the invention relate generally to the use of compositions comprising methylsulfonylmethane (MSM), and one or more therapeutic agents, for the treatment of drug-sensitive and drug resistant microorganisms. In several embodiments, such compositions are effective in treating drug resistant infectious diseases, for example, MRSA. | 2012-06-14 |
20120149673 | INHIBITORS OF STORE OPERATED CALCIUM RELEASE - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity. | 2012-06-14 |
20120149674 | Diaryl Substituted Alkanes - The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. | 2012-06-14 |
20120149675 | 1,2,3-TRIAZOLE-IMIDAZOLECOMPOUNDS - The present invention is concerned with novel 1,2,3-triazole-imidazole compounds of formula (I) | 2012-06-14 |
20120149676 | NOVEL COMPOUNDS - This invention relates to compounds of formula I | 2012-06-14 |
20120149677 | ETHER BENZOTRIAZOLE DERIVATIVES - The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved. | 2012-06-14 |
20120149678 | Organonitro Compounds for Use in Treating Non-Hodgkin's Lymphoma and Leukemia, and Methods Relating Thereto - The invention provides organonitro compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat non-Hodgkin's lymphoma and certain leukemias in a patient. The compounds, compositions, kits, and methods are contemplated to provide a therapeutic benefit in treating non-Hodgkin's lymphoma, chronic lymphocytic leukemia, acute myelogenous leukemia, chronic myelogenous leukemia, and acute lymphoblastic leukemia. Exemplary organonitro compounds described herein include alkyl-substituted and acyl-substituted di-nitroheterocycles. | 2012-06-14 |
20120149679 | Sulfonamide Derivatives - The present invention relates to compounds of the formula | 2012-06-14 |
20120149680 | KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 2012-06-14 |
20120149681 | CYCLOBUTYL SUBSTITUTED PYRROLOPYRIDINE AND PYRROLOPYRIMIDINE DERIVATIVES AS JAK INHIBITORS - The present invention provides cyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I: | 2012-06-14 |
20120149682 | HETEROCYCLIC-SUBSTITUTED PYRROLOPYRIDINES AND PYRROLOPYRIMIDINES AS JAK INHIBITORS - The present invention provides heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines of Formula I: | 2012-06-14 |
20120149683 | SUBSTITUTED AMINOPIPERIDINES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES - The present invention is directed to novel substituted aminopiperidines of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-ÏV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved. | 2012-06-14 |
20120149684 | AKT INHIBITORS - The present invention provides AKT inhibitors of the formula: Formula I The present invention also provides pharmaceutical compositions comprising compounds of Formula I, uses of compounds of Formula I and method of using compounds of Formula I. | 2012-06-14 |
20120149685 | COMPOSITION AND METHOD FOR THE TREATMENT OF TAUOPATHIES - The present invention refers to the use of a specific indolocarbazole compound of general formula (1) or a pharmaceutically-acceptable a salt thereof for the preparation of a pharmaceutical composition for the prevention or treatment of a neurode-generative and/or dementing illness driven by the molecular pathology of microtubule-associate tau such as Alzheimer's disease, frontal lobe dementia, Pick's disease, Parkinson disease with dementia, corticobasal degeneration, argyrophilic grains disease, or supranuclear palsy. A method for treating or preventing such illnesses is also disclosed. Furthermore, methods for the identification of efficacious inhibitors of neurofibrillary degeneration, and methods for the determination of an appropriate dosage of an inhibitor of the PHF-type tau hyperphosphorylation for the treatment of a condition characterized by neurofibrillary pathology are described. | 2012-06-14 |
20120149686 | KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME - The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein. | 2012-06-14 |
20120149687 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 2012-06-14 |
20120149688 | PLATELET ADP RECEPTOR INHIBITORS - Novel compounds of formulae (I) and (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof. | 2012-06-14 |
20120149689 | METHOD OF WEANING FROM HORMONAL TREATMENT OF HORMONE DEPLETION INDUCED VASOMOTOR SYMPTOMS - The invention provides a method to effectively wean a woman from hormonal therapy for treatment of vasomotor symptoms by reducing the dosage of the hormonal agent to zero, while a non-hormonal drug in an amount, which is therapeutically effective for treating vasomotor symptoms, is administered or initiated and continued for one or more periods of durations determined by assessment of the effect of a treatment free period, which follows each period of continuous non-hormonal drug treatment. | 2012-06-14 |
20120149690 | Compositions Comprising Azelastine and Methods of Use Thereof - The present invention provides pharmaceutical compositions comprising azelastine, or a pharmaceutically acceptable salt or ester thereof including azelastine hydrochloride, and optionally one or more additional active agents. Preferred such compositions further comprise one or more pharmaceutically acceptable carriers or excipients that reduce the amount of post-nasal drip, and/or that minimize or mask the unpleasant bitter taste associated with post-nasal drip, of the compositions into the oral cavity, upon intranasal or ocular administration of the compositions. Especially effective excipients used in the compositions of the present invention are hypromellose as a viscosity modifier and sucralose as a taste-masking agent. The invention also provides methods of treating or preventing certain disorders, or symptomatic relief therefrom, by administering the compositions of the invention to a patient, e.g., for the symptomatic relief of allergic rhinitis, non-allergic vasomotor rhinitis, allergic conjunctivitis, as well as other disorders. | 2012-06-14 |
20120149691 | Pyrrolo [1,2-b] Pyridazine Derivatives as Janus Kinase Inhibitors - The invention provides compounds of formula I: | 2012-06-14 |
20120149692 | In Vivo Studies of Crystalline Forms of Meloxicam - The invention is directed to novel crystalline forms of meloxicam. These novel crystalline forms of meloxicam have improved bioavailability, an enhanced rate of dissolution and shorter time to C | 2012-06-14 |
20120149693 | THERAPEUTIC COMPOUNDS - The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C and/or RSK disorders, including diseases and disorders mediated by GPCRs and/or RSKs. | 2012-06-14 |
20120149694 | Substituted piperidines - The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders. | 2012-06-14 |
20120149695 | DIHYDROPYRIMIDINE COMPOUNDS AND PREPARATION METHODS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF - Disclosed are dihydropyrimidine compounds and preparation methods, pharmaceutical compositions and uses thereof. Specifically, the compounds described herein in general formula (I), or their isomers, pharmaceutically acceptable salts or hydrates are provided, wherein each variable has the meaning as defined in the description. Also provided are a process for preparing the compounds of the general formula (I), the use of the compounds, an isomer thereof, a pharmaceutically acceptable salt thereof or a hydrate thereof as a medicament, in particular as a medicament for the treatment and/or prevention of Hepatitis B. | 2012-06-14 |
20120149696 | ETHYLENE DIAMINE MODULATORS OF FATTY ACID HYDROLASE - Certain ethylene diamine compounds of Formula (I) are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed. | 2012-06-14 |
20120149697 | HUMIC SUBSTANCES AND THERAPEUTIC USES THEREOF - The present invention relates to the medical field, in particular to the use of natural organic polyanions, i.e. humic substances, HSs, in the treatment of neurodegenerative diseases, such as Prion disease, Alzheimer's and Parkinson's disease. | 2012-06-14 |
20120149698 | NOUVEL COMPOUNDS - The present invention relates to new CGRP-antagonists of general formulae Ia and Ib | 2012-06-14 |
20120149699 | IMIDAZO[1,2-a]PYRIDINE SULFONAMIDES AS TRPM8 MODULATORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: | 2012-06-14 |
20120149700 | 2-CYANOPHENYL FUSED HETEROCYCLIC COMPOUNDS, AND COMPOSTIONS AND USES THEREOF - Fused heterocyclic compounds are provided according to formula 1: | 2012-06-14 |
20120149701 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS - Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein. | 2012-06-14 |
20120149702 | INHIBITORS OF CELLULAR NECROSIS - The present invention relates to compounds and pharmaceutical preparations and their use in therapy for preventing or treating trauma, ischemia, stroke and degenerative diseases associated with cell death. Methods and compositions of the invention are particularly useful for treating neurological disorders associated with cellular necrosis. | 2012-06-14 |
20120149703 | AZA-SUBSTITUTED SPIRO DERIVATIVES - A compound of the following formula (I) or its pharmaceutically-acceptable salt is provided: | 2012-06-14 |
20120149704 | DISUBSTITUTED BENZAMIDE DERIVATIVES AS GLUCOKINASE (GK) ACTIVATORS - The invention relates to disubstituted benzamide derivatives of the general Formula (I), their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites and polymorphs. The invention also relates to processes for the preparation of the compounds of the invention, pharmaceutical compositions containing the compounds and to methods for treating type II diabetes using the compounds of the invention. | 2012-06-14 |
20120149705 | N-Thio-anthranilamid compounds and their use as pesticides - N-Thio-anthranilamid compounds of formula (I) | 2012-06-14 |
20120149706 | INHIBITION OF P38 KINASE ACTIVITY USING SUBSTITUTED HETEROCYCLIC UREAS - This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases, other than cancer and proteolytic enzyme mediated diseases, other than cancer, and pharmaceutical compositions for use in such therapy. | 2012-06-14 |
20120149707 | ALPHA-ARYLMETHOXYACRYLATE DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME - The present invention relates to an alpha-arylmethoxyacrylate derivative, a preparation method thereof and a pharmaceutical composition comprising the same, and the alpha-arylmethoxyacrylate derivative is inhibitory of HIF, which plays an important role in the regulation of genes associated with energy metabolism, vasomotion, angiogenesis and apoptosis and in the response of cells under hypoxic conditions, so that it can be used for preventing or treating of diseases such as cancer, arthritis, psoriasis, diabetic retinopathy and macular degeneration. | 2012-06-14 |
20120149708 | MODULATORS OF VIRAL TRANSCRIPTION, AND METHODS AND COMPOSITIONS THEREWITH - The present invention is directed to a process for inhibiting the replication of human immunodeficiency virus-1 (HIV-1), by contacting a cell with at least one compound according to Formula I. | 2012-06-14 |
20120149709 | PYRAZINOISOQUINOLINE COMPOUNDS - This invention relates to novel compounds that are pyrazinoisoquinoline derivatives, and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel pyrazinoisoquinoline derivatives that are derivatives of praziquantel. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel. | 2012-06-14 |
20120149710 | SORTASE A INHIBITORS - Bacterial infections, including Methicillin resistant | 2012-06-14 |
20120149711 | PIPERIDINE DERIVATIVES USED AS OREXIN ANTAGONISTS - This invention relates to heteroarylamine methyl substituted piperidine derivatives (I) and their use as antagonists of human orexin. | 2012-06-14 |
20120149712 | Methods for improving kidney function - The invention relates to methods for improving renal (kidney) function. Methods for decreasing blood urea nitrogen (BUN), for increasing glomerular filtration rate (GFR), and for decreasing serum creatinine are also provided. | 2012-06-14 |
20120149713 | ORAL FILMS COMPRISING 7-[4-[4-(2,3-DICHLOROPHENYL) PIPERAZIN-1-L]BUTOXY]-3,4-DIHYDRO-1H-QUINOLIN-2-ONE BASE OR SALTS OR HYDRATES THEREOF - An oral film comprising 7-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy]-3,4-dihydro-1H-quinolin-2-one base or salts or hydrates thereof. | 2012-06-14 |
20120149714 | Effects of Inhibitors of FGFR3 on Gene Transcription - Methods of utilizing biomarkers to identify patients for treatment or to monitor response to treatment are taught herein. Alterations in levels of gene expression of the biomarkers, particularly in response to FGFR3 inhibition, are measured and identifications or adjustments may be made accordingly. | 2012-06-14 |
20120149715 | COMPOUNDS AND METHODS FOR THE TREATMENT OF VIRAL INFECTIONS - High throughput and virtual screening methods are disclosed that can identify potential anti-viral agents. The virtual screening methods identify agents that interact with a viral nucleoprotein binding site. The high throughput methods identify compounds that inhibit viral infection by binding to viral nucleoprotein. Also disclosed are pharmaceutical formulations useful for treating or preventing viral infections, especially influenza A. | 2012-06-14 |
20120149716 | METHODS OF USING AND COMPOSITIONS COMPRISING PDE4 MODULATORS FOR TREATMENT, PREVENTION AND MANAGEMENT OF TUBERCULOSIS - Methods of treating, preventing, and managing tuberculosis and other related disorders are disclosed. The methods comprise the administration of a PDE4 modulator, or a pharmaceutically acceptable salt, solvate, hydrate, clathrate, stereoisomer, or prodrug thereof, optionally in combination with a second active agent and/or other conventional therapies. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in such methods are also disclosed. | 2012-06-14 |
20120149717 | Diarylmethyl Piperazine Derivatives, Preparations Thereof and Uses Thereof - Compounds of general formula: | 2012-06-14 |
20120149718 | Amido Compounds - Compounds of the formula I: | 2012-06-14 |
20120149719 | BITTER TASTE MASKING DOSAGE FORM - A powder-particle dosage form obtained by granulating an excipient and/or a disintegrating agent with a liquid in which a bitter taste masking base is dissolved and/or suspended, and a drug having solubility in water (20° C.) of not higher than 1 g/mL is dissolved or suspended, or a tablet obtained by compressing the powder-particle dosage form could mask bitter taste of a drug. | 2012-06-14 |
20120149720 | VALACYCLOVIR FORMULATIONS - The present invention relates to taste-masked pharmaceutical formulations of valacyclovir. The present invention also relates to process of preparation of valacyclovir suspensions, solutions and dry powder for reconstitution. | 2012-06-14 |
20120149721 | METHYLPYRROLOPYRIMIDINECARBOXAMIDES - The compounds of Formula (I), | 2012-06-14 |
20120149722 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 2012-06-14 |
20120149723 | 5-METHYL-PIPERIDINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS FOR THE TREATMENT OF SLEEP DISORDER - This invention relates to heteroaryloxy 5-methyl substituted piperidine derivatives and their use as pharmaceuticals. | 2012-06-14 |
20120149724 | MODULATING ENDOGENOUS BETA-ENDORPHIN LEVELS - Systemic beta-endorphin can be elevated in response to cutaneous irradiation, including ultraviolet and ionizing radiation. Increases in systemic beta-endorphin levels associated with cutaneous irradiation can be modulated with opiate receptor antagonists, particularly compounds that antagonize opioid receptor binding by beta endorphin. | 2012-06-14 |
20120149726 | Crystal Forms of Kinase Inhibitors - N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N′-(3-fluorophenyl)urea free base and crystallines form thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer. | 2012-06-14 |
20120149727 | PRASUGREL IN NON-CRYSTALLINE FORM AND PHARMACEUTICAL COMPOSITION THEREOF - The present invention relates to prasugrel or a pharmaceutically compatible salt thereof, compositions that contain this active substance and pharmaceutical compositions that contain this active substance or a composition containing this active substance. The present invention further relates to methods for producing the novel compositions. | 2012-06-14 |
20120149728 | NOVEL FUMARATE SALTS OF A HISTAMINE H3 RECEPTOR ANTAGONIST - The disclosure relates to fumarate salts of 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide, to pharmaceutical compositions thereof, processes for making the same, and methods of use thereof. | 2012-06-14 |
20120149729 | METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes. | 2012-06-14 |
20120149730 | METHODS AND COMPOSITIONS USING RACEMIC, (R)-, AND (S)-FEXOFENADINE IN COMBINATION WITH LEUKOTRIENE INHIBITORS - Methods and pharmaceutical compositions employing a terfenadine metabolite and a leukotriene inhibitor for the treatment or prevention of inflammation or allergic disorders, such as asthma, or symptoms thereof. Also included are methods and compositions employing a terfenadine metabolite, a leukotriene inhibitor, and a decongestant for the treatment or prevention of inflammation or allergic disorders, such as asthma, or symptoms thereof. | 2012-06-14 |
20120149731 | NEW MEDICAL USE - The present invention relates to a method of treatment of urticaria comprising administration to a patient in need thereof an amount of the compound 3-(4-{[4-(4-{[3-(3,3-dimethyl-1-piperidinyl) propyl]oxy}phenyl)-1-piperidinyl]carbonyl}-1-naphthalenyl)propanoic acid, | 2012-06-14 |
20120149732 | MULTIFUNCTIONAL LINKERS AND METHODS FOR THE USE THEREOF - In accordance with the present invention, novel multifunctional compounds have been developed which have orthogonal reactive groups thereon, thereby facilitating preparation of compounds having multiple functional properties (e.g., a targeting moiety and a biologically active moiety). Such constructs are useful for a variety of applications, e.g., for the delivery of biologically compatible materials, and release thereof in active form. Therefore, in accordance with the present invention, there are provided multifunctional linkers of defined structure, as well as various derivatives thereof bearing one or more biologically active components thereon. Also provided in accordance with the present invention are methods for the preparation of such constructs, as well as various uses thereof. | 2012-06-14 |
20120149733 | PIPERIDINYL COMPOUND AS A MODULATOR OF CHEMOKINE RECEPTOR ACTIVITY - The present application describes the compound of formula (I): | 2012-06-14 |
20120149734 | AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES - The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved. | 2012-06-14 |
20120149735 | 1,4-Dihydropyridine Derivatives and Their Uses - The present invention relates to 1,4-dihydropyridine derivatives of the formula (I) and their uses in the treatment and/or prevention of diseases and disorders directly or indirectly associated with the modification (increase or decrease) of the activity of the cannabinoid receptor 2 (CB2). | 2012-06-14 |
20120149736 | ENZYME INHIBITORS - Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ═CH— or ═N—; W is —CH═CH— Or —CH | 2012-06-14 |
20120149737 | Therapeutic Aryl-Amido-Aryl Compounds and Their Use - The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-amido-aryl compounds of the following formula (for convenience, collectively referred to herein as “AAA compounds”), which, inter alia, are (selective) retinoic acid receptor α (RARα) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RARα, and in the treatment of diseases and conditions that are mediated by RARα, that are ameliorated by the activation of RARα, etc., including cognitive disorders, memory impairment, memory deficit, senile dementia, Alzheimer's disease, early stage Alzheimer's disease, intermediate stage Alzheimer's disease, late stage Alzheimer's disease, cognitive impairment, and mild cognitive impairment. | 2012-06-14 |
20120149738 | NOVEL INHIBITORS OF PROLIFERATION AND ACTIVATION OF SIGNAL TRANSDUCER AND ACTIVATORS OF TRANSCRIPTION (STATS) - Pyridine compounds effective in modulation STAT3 and/or STAT5 activation are provided that are useful in the prevention and treatment of proliferative disease and conditions including cancer, inflammation and proliferative skin disorders. | 2012-06-14 |
20120149739 | PHARMACEUTICAL DEPOT FOR N-{5-[(CYCLOPROPYLAMINO)CARBONYL]-2-METHYLPHENYL)-3-FLUORO-4-(PYRIDIN-2-Y- LMETHOXY)BENZAMIDE - A pharmaceutical depot comprising (i) N-{5-[(cyclopropylamino)carbonyl]-2-methylphenyl}-3-fluoro-4-(pyridin-2-ylmethoxy)benzamide, or a pharmaceutically-acceptable salt thereof, as a pharmaceutical agent (PA) and (ii) a polymer which degrades to create an acidic microclimate, wherein the PA is released from the polymer upon polymer degradation. | 2012-06-14 |
20120149740 | PHARMACEUTICAL DEPOT FOR N-{5-[(CYCLOPROPYLAMINO)CARBONYL]-2-METHYLPHENYL)-3-FLUORO-4-(PYRIDIN-2-Y- LMETHOXY)BENZAMIDE - A pharmaceutical depot comprising (i) N-{5-[(cyclopropylamino)carbonyl]-2-methylphenyl}-3-fluoro-4-(pyridin-2-ylmethoxy)benzamide, or a pharmaceutically-acceptable salt thereof, as a pharmaceutical agent (PA) and (ii) a polymer which degrades to create an acidic microclimate, wherein the PA is released from the polymer upon polymer degradation. | 2012-06-14 |
20120149741 | TREATMENT OF DUCHENNE MUSCULAR DYSTROPHY - There are provided compounds of Formula (I) wherein three of A | 2012-06-14 |
20120149742 | HETEROCYCLIC DERIVATIVES AS MODULATORS OF ION CHANNELS - The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 2012-06-14 |
20120149743 | Selenophene and Selenazole Carboxylic Acid Derivatives - Derivatives of selenophene and selenazole heterocycles are disclosed. The compounds are useful as inhibitors of D-amino acid oxidase (DAO) and in the treatment of neurodegenerative and psychiatric diseases and disorders. | 2012-06-14 |
20120149744 | ANTI-MITOTIC ANTI-PROLIFERATIVE COMPOUNDS - Substituted triazole compounds and pharmaceutical compositions thereof are presented. Also presented are methods for treating a pathology linked to a hyperproliferative disorder by administering the substituted triazole compounds to a patient in need thereof. | 2012-06-14 |
20120149745 | ANTIMYCOTIC PHARMACEUTICAL COMPOSITION - A pharmaceutical composition which comprises 1) a compound represented by the following general formula (1) and/or a salt thereof; and 2) a ketone such as methyl ethyl ketone. Preferably, the compound represented by the following general formula (1) is luliconazole, where R | 2012-06-14 |
20120149746 | ESTER PRO-DRUGS OF [3-(1-(1H-IMIDAZOL-4-YL)ETHYL)-2-METHYLPHENYL] METHANOL FOR TREATING RETINAL DISEASES - The present invention relates to method of treating retinal diseases in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising a ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals. | 2012-06-14 |
20120149747 | PHARMACEUTICAL COMPOSITIONS COMPRISING (3-(1-(1H-IMIDAZOL-4-YL)ETHYL)-2-METHYLPHENYL)METHANOL - The present invention relates to method of lowering intraocular pressure in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, or enantiomers thereof, or tautomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals. | 2012-06-14 |
20120149748 | Pharmaceutical Cream Compositions and Methods of Use - The present invention provides pharmaceutical cream compositions comprising oxymetazoline and methods for treating rosacea and other skin disorders as described herein using the above cream compositions. | 2012-06-14 |
20120149749 | METHOD OF TREATING THROMBOCYTOPENIA - Invented is a method of treating thrombocytopenia in a human in need thereof which comprises the administration of a therapeutically effective amount of a 3′-{N′-[1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-1,5-dihydropyrazol-4-ylidene]hydrazino}-2′-hydroxybiphenyl-3-carboxylic acid to such human. | 2012-06-14 |
20120149750 | ARYLOAZOL-2-YL CYANOETHYLAMINO COMPOUNDS, METHOD OF MAKING AND METHOD OF USING THEREOF - The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives of formula (I): | 2012-06-14 |