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10th week of 2013 patent applcation highlights part 44
Patent application numberTitlePublished
20130059784COMBINATION THERAPIES USING CYCLOSPORINE AND AROMATIC CATIONIC PEPTIDES - The invention provides compositions and methods for preventing or treating an ischemia-reperfusion injury, such as occurs during acute myocardial infarction and organ transplant in a mammalian subject. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide or a pharmaceutically acceptable salt thereof, and one or more additional active agents such as cyclosporine.2013-03-07
20130059785Gene and Polypeptide Sequences - The present invention provides a polypeptide comprising (i) a leader sequence, the leader sequence comprising a (a) secretion pre sequence, and (b) the following motif:2013-03-07
20130059786COMPOSITIONS AND METHODS FOR THE TREATMENT OF CARDIAC AND VASCULAR DISEASE - The invention provides methods for the treatment of coronary heart disease, peripheral vascular disease, stroke, and ischemia featuring agents that interfere with the expression or activity of Cthrc1. The invention also provides the use of Cthrc1 peptide as a therapeutic agent for the treatment of acute or chronic cardiac deficiencies. The invention further provides detection and monitoring of Cthrc1 peptide in blood or serum to assess or monitor cardiac function.2013-03-07
20130059787METHODS OF USING HUMAN PROTEIN KINASE C DELTA VIII AS A BIOMARKER - RA treatment can improve cognition; promote neurogenesis; and regulate alternative splicing of genes, particularly by mediating mechanisms of 5′ splice site selection and generation of PKCδ alternatively spliced variants. Expression of PKCδVIII is an indicator of the levels of on-going apoptosis in neurons. In the aging brain, switching the isoform expression to PKCδVIII by RA could shield the cells from neuronal death. The inventors discovered that human PKCδVIII expression is increased in neuronal cancer and decreased in Alzheimer's disease. The data shows that PKCδVIII promotes neuronal survival and increases neurogenesis via Bcl2 and Bcl-xL. In addition, the trans-factor SC35 was found to be crucial in mediating the effects of RA on alternative splicing of PKCδVIII mRNA in neurons. The data described herein indicate that PKCδVIII can be used as a biomarker for neurological diseases such as cancers and Alzheimer's disease and as a tool for monitoring and evaluating treatment.2013-03-07
20130059788PRODOMAIN MODULATORS OF ADAM 10 - The presently disclosed subject matter discloses isolated ADAM 10 modulating peptides and related compounds useful for studying the biological functions of ADAM 10 and for the treatment of diseases such as cancer, neurological disorders, asthma, and allergic responses, and disorders characterized at least in part by the presence of one or more of inflammation, excess cell proliferation, angiogenesis, and excess soluble CD23. In one aspect, the presently disclosed subject matter provides isolated mouse and human ADAM 10 prodomain comprising the sequence set forth in SEQ ID NOs 1-8, or a sequence having at least 95% homology to any of SEQ ID NOs 1-8 and having the functionality of modulating ADAM 10 activity.2013-03-07
20130059789Method for Treating Premature Ejaculation With a Botulinum Neurotoxin - Methods for prolongation of climax time in a patient in need thereof are presented, as are methods for treating premature ejaculation by local administration of a Clostridial neurotoxin, such a 2013-03-07
20130059790PROCESS FOR THE PREPARATION OF A BIOMASS COMPRISING PLANTARICIN AND USES THEREOF IN MEDICAL FIELD - The present invention concerns a process for preparation of a biomass comprising one or a more plantaricins A, N or K in association with the lactic acid bacteria used for the preparation and uses thereof in order to stimulate the barrier function of intestinal cells or human epidermal keratinocytes.2013-03-07
20130059791CRYSTALLINE D-ISOGLUTAMYL-D-TRYPTOPHAN AND THE MONO AMMONIUM SLAT OF D-ISOGLUTAMYL-D-TRYPTOPHAN - A process for making pure crystalline D-isoglutamyl-D-tryptophan is provided which includes the step of deprotecting essentially pure N-tert-butoxycarbonyl-D-isoglutamyl-D-tryptophan or its diester to yield essentially pure D-isoglutamyl-D-tryptophan. A process is also provided for the preparation of pure mono ammonium salt of D-isoglutamyl-D-tryptophan from essentially pure N-tert-butoxycarbonyl-D-isoglutamyl-D-tryptophan. D-isoglutamyl-D-tryptophan, ammonium salt (1:1) is a stable pharmaceutical solid.2013-03-07
20130059792Traceability of Cellular Cycle Ano - The present invention relates to the field of medicine and biology. It concerns a novel test for screening and for therapeutic follow-up in oncology. More particularly, it relates to diagnostic and/or therapeutic tests in oncology and on neurodegenerative diseases. It is a diagnostic test and a prognostic test for various cancers (breast cancer, bladder cancer, ovarian cancer, lung cancer, skin cancer, prostate cancer, colon cancer, liver cancer, glioblastoma, sarcoma, leukemia, etc.) and therapeutics solutions for specific neurodegenerative diseases. More particularly, the invention concerns the use of the LIV21 protein, LIV21 gene and of derivatives thereof as diagnostic and prognostic markers for cancers. The invention therefore concerns the detection of the LIV21 protein with a kit comprising LIV21-specific antibodies.2013-03-07
20130059793EGF RECEPTOR MIMICKING PEPTIDES - Provided are peptides which can mimic the epidermal growth factor receptor (EGFR), e.g., by selectively binding TGF-α and/or EGF. In certain embodiments, the peptides are retro-inverted peptides. The peptides may be used as soluble decoys for TGF-α and/or EGF, and anti-cancer properties of peptides are demonstrated both in vitro and in vivo. The peptides may be administered alone or comprised in a fusion construct, imaging construct, and/or a therapeutic construct, e.g., for the treatment of a cancer.2013-03-07
20130059794ALPHA-FETOPROTEIN "RING AND TAIL" PEPTIDES - The invention relates to compounds that are analogs of a cyclic peptide, cyclo[EKTOVNOGN], AFPep, that has anti-estrotrophic activity. The analogs of the invention include peptides and peptidomimetics that inhibit estrogen receptor-dependent cell proliferation. The compounds of the invention are useful for treating cell proliferative disorders or physiological conditions characterized by undesirable or unwanted estrogen induced cell proliferation, including breast cancer.2013-03-07
20130059795Novel Composition Of Matter For Delivering Lipid-Soluble Materials, And A Method For Producing It - This invention describes a novel composition of matter describing a complex comprising leaf protein and a lipophilic substance(s), along with the method of producing it. Delivery of lipid-soluble materials into the body is challenging because they are generally highly insoluble in water and very subject to oxidative degradation. The inventors have found that leaf protein—the water-soluble proteins derived from plant leaves—can efficiently form a complex with lipophilic materials. This leaf protein—lipid-soluble material complex is an effective carrier of lipophilic substances. As such, the leaf protein—lipid-soluble material complex disclosed herein can be used for the delivery of lipophilic vitamins, fatty acids, caretenoids, lipophilic drugs, and other lipophilic materials. This complex can be used to deliver lipophiles in foods, nutritional and dietary supplements, topical compositions and in pharmaceutical products.2013-03-07
20130059796CYCLOSPORIN COMPOSITIONS - Cyclosporin A compositions are disclosed herein comprising an oil and a surfactant. These are useful in the treatment of dry eye disease.2013-03-07
20130059797Linaclotide for the Treatment of Chronic Constipation - The invention provides methods for treating a patient with chronic constipation by administering a therapeutically effective dose of linaclotide.2013-03-07
20130059798Cell-Permeable Peptide Inhibitors of the JNK Signal Transduction Pathway - The invention provides cell-permeable peptides that bind to JNK proteins and inhibit JNK-mediated effects in JNK-expressing cells.2013-03-07
20130059799AROMATIC-CATIONIC PEPTIDES AND USES OF SAME - The disclosure provides compositions and methods relating to aromatic-cationic peptides. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof. For example, the peptides may be administered to subjects in need of a mitochondrial-targeted antioxidant.2013-03-07
20130059800PYRROLOBENZODIAZEPINES USED TO TREAT PROLIFERATIVE DISEASES - Pyrrolobenzodiazepine dimers I having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and a C2-C3 double bond and either a conjugated double or triple bond at the C2 position or an alkyl group at the C2 position on the other monomer unit, and conjugates of these compounds.2013-03-07
20130059801FATTY ACID AMIDES, COMPOSITIONS AND METHODS OF USE - The invention relates to fatty acid amides; compositions comprising an effective amount of a fatty acid amide; and methods for treating or preventing cancer, a metabolic disease or a neurodegenerative disease comprising the administration of an effective amount of a fatty acid amide.2013-03-07
20130059802BORON-CONTAINING SMALL MOLECULES - This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.2013-03-07
20130059803BORON-CONTAINING SMALL MOLECULES - This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.2013-03-07
20130059804SYNTHESIS OF COMPOUNDS USEFUL AS MODULATORS OF AMYLOID-BETA PRODUCTION - As described herein, the present invention provides methods for preparing compounds useful for treating or lessening the severity of a neurodegenerative disorder. The present invention also provides methods of treating or lessening the severity of such disorders wherein said method comprises administering to a patient a compound of the present invention, or composition thereof. Said method is useful for treating or lessening the severity of, for example, Alzheimer's disease.2013-03-07
20130059805COMPOSITION COMPRISING AN AMORPHOUS NON-CRYSTALLINE GLASS FORM OF AZITHROMYCIN - The invention relates to an amorphous non-crystalline glass form (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-2-ethyl-3,4,10-trihydroxy-3,5,6,8,10,12,14-heptamethyl-15-oxo-11-{[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy}-1-oxa-6-azacyclopentadec-13-yl 2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranoside or azithromycin having an infra-red pattern displaying characteristic relatively broad peaks at approximately 3500 and 1727 cm2013-03-07
20130059806EPIGENETIC CO-REPRESSORS OF THE GAMMA-GLOBIN GENE AND METHODS OF USING SAME - This disclosure describes methods of screening for compounds that disrupt the interaction between DNMT1 and the gamma-globin promoter or between LSD-1 and the gamma-globin promoter. This disclosure describes methods of screening for compounds that de-repress the gamma-globin gene.2013-03-07
20130059807BILE ACID RECYCLING INHIBITORS AND SATIOGENS FOR TREATMENT OF DIABETES, OBESITY, AND INFLAMMATORY GASTROINTESTINAL CONDITIONS - Provided herein are methods of utilizing bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents for the treatment of obesity, diabetes, and inflammatory gastrointestinal conditions.2013-03-07
20130059808AMINOGLYCOSIDE DERIVATIVES - The present invention relates to antimicrobial agents. Some embodiments include compounds, compositions, methods of preparation, and methods of treatment using new aminoglycosides and aminoglycoside derivatives.2013-03-07
20130059809PHARMACEUTICAL COMPOSITIONS COMPRISING FORMS OF 5-AZACYTIDINE - The invention provides novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula:2013-03-07
20130059810PHARMACEUTICAL COMPOSITIONS COMPRISING FORMS OF 5-AZACYTIDINE - The invention provides novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula:2013-03-07
20130059811METHOD FOR TREATING AND PREVENTING ARTHRITIS - Compounds represented by the formula 1:2013-03-07
20130059812COMPOSITION FOR TREATING CHRONIC HEPATITIS B, CONTAINING CLEVUDINE AND ADEFOVIR DIPIVOXIL - The present invention relates to a composition for treating chronic hepatitis B, containing clevudine and adefovir dipivoxil. The combined formulation of the present invention maximizes the effect for treating diseases caused by infection of hepatitis B virus and shows a mutual inhibitory activity against a resistant virus compared with a single-component formulation.2013-03-07
20130059813TREATMENT OF DERMATOLOGICAL CONDITIONS - The present disclosure provides a method for treating dermatological conditions, such as psoriasis, dermatitis, and dandruff. Said conditions are treated by administering to a person a vitamin supplement composition comprising folic acid, vitamin B2013-03-07
20130059814ANTI-INFLAMMATORY DERMATOLOGICAL COMPOSITION COMPRISING CORTICOSTEROIDS AND HYALURONATE FRAGMENTS, AND USES THEREOF - Anti-inflammatory dermatological composition for topical administration, characterized in that it comprises 0.005% to 0.1%, preferably 0.01% to 0.05% by weight of a corticosteroid and 0.1% to 1%, preferably 0.5% to 1% by weight of hyaluronate fragments with an average molecular weight of between 20 and 500 kDa, preferably between 20 and 375 kDa, more preferentially between 20 and 150 kDa.2013-03-07
20130059815NUTRITIONAL COMPOSITIONS CONTAINING HUMAN MILK OLIGOSACCHARIDES AND METHODS FOR USING THE SAME - This disclosure features human milk permeates and compositions containing the same obtained from fractionated whole human milk. The oligosaccharide rich permeate and permeate compositions of the present invention are useful as nutritional supplements for pre-term and full term infants, for establishing or maintaining gut flora and for treating the symptoms of inflammatory bowel disease.2013-03-07
20130059816COMPOSITIONS AND METHODS FOR TREATMENT OF AUTOIMMUNE AND OTHER DISEASE - Provided are methods relating to the use of CDP-therapeutic agent conjugates for the treatment of autoimmune disease, inflammatory disease, or cancer. Also provided are CDP-therapeutic agent conjugates, particles comprising CDP-therapeutic agent conjugates, and compositions comprising CDP-therapeutic agent conjugates.2013-03-07
20130059817COMPOSITION FOR REDUCING ABSORPTION OF DIETARY FAT - This invention relates to compositions for reducing the absorption or bioavailability of lipids in the gastrointestinal tract, and to methods for the preparation and use of these compositions. The compositions comprise a source of dietary fibre together with a cyclodextrin. The compositions of the invention are suitable for use in the prevention and treatment of obesity or hyperlipidaemia.2013-03-07
20130059818CARBOSILANE DENDRIMERS AND THE USE THEREOF AS ANTIVIRAL AGENTS - Highly branched macromolecules synthesized from a polyfunctional core, preferably silicon, or polyphenolic, with a carbosilane structure at its periphery functionalized with groups, preferably anionic, giving to the macromolecule a net negative charge. Furthermore, the invention relates to the procedures for their synthesis and their uses as antiviral agents, antibacterial and antifungal agents.2013-03-07
20130059819INHIBITORS OF FATTY ACID AMIDE HYDROLASE - The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III).2013-03-07
20130059820INOSITOL PYROPHOSPHATES, AND METHODS OF USE THEREOF - The present invention comprises compounds, compositions thereof, and methods capable of delivering modified inositol hexaphosphate (IHP) comprising an internal pyrophosphate ring to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering IHP to the cytoplasm of the red blood cells.2013-03-07
20130059821BICYCLIC ARYL SPHINGOSINE 1-PHOSPHATE ANALOGS - Compounds that have agonist activity at one or more of the SIP receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at SIP receptors.2013-03-07
20130059822Arylfluorophosphate Inhibitors of Intestinal Apical Membrane Sodium/Phosphate Co-Transport - The present invention is directed to fluorophosphates, and pharmaceutical compositions thereof, which are inhibitors of intestinal apical sodium/phosphate co-transport and are useful in the treatment of hyperphosphatemia, in reducing blood phosphate levels, and in treating hypertension.2013-03-07
20130059823Diazeniumdiolate Cyclohexyl Derivatives - A compound having the structure (I) or a pharmaceutically acceptable salt thereof, wherein R2013-03-07
20130059824METHODS FOR TREATING MILD COGNITIVE IMPAIRMENT - Provided herein are PAK inhibitors. Also provided herein are compositions and methods for treating an individual suffering from Mild Cognitive Impairment.2013-03-07
20130059825Antibodies to 25-HYDROXY Vitamin D2 and D3 and Uses Thereof - Provided herein are antigenic molecules that can be used to generate antibodies capable of binding to a vitamin D derivative, such as 25-hydroxyvitamin D2 and/or 25-hydroxyvitamin D3, or a 25-hydroxyvitamin D analog, such as a vitamin D-C22 immunogenic molecule or compound. Antibodies produced using these antigenic molecules, and related antigenic compounds, are also described. In addition, disclosed herein are methods for detecting vitamin D deficiency in a subject, methods for treating a subject suspected of having a vitamin D deficiency, methods for monitoring progression of vitamin D deficiency in a subject, and methods for monitoring treatment of vitamin D deficiency in a subject in need thereof. Also provided are methods and reagents for the detection or quantification of 25-hydroxyvitamin D2 and D3, methods for stabilizing vitamin D analogs, and methods for separating 25-hydroxyvitamin D2 and D3 from vitamin D binding protein in a biological sample.2013-03-07
20130059826Inhalant Formulation Containing Sulfoalkyl Ether Cyclodextrin and Corticosteroid - An inhalable formulation containing SAE-CD and corticosteroid is provided. The formulation is adapted for administration to a subject by nebulization with any known nebulizer. The formulation can be included in a kit. The formulation is administered as an aqueous solution, however, it can be stored as a dry powder, ready-to-use solution, or concentrated composition. The formulation is employed in an improved nebulization system for administering corticosteroid by inhalation. SAE-CD present in the formulation significantly enhances the chemical stability of budesonide. A method of administering the formulation by inhalation is provided. The formulation can also be administered by conventional nasal delivery apparatus.2013-03-07
20130059828PHARMACEUTICAL COMPOSITION - A pharmaceutical composition comprising: (A) an androgen; (B) a cyclic enhancer of the type used in the compositions and methods claimed by U.S. Pat. No. 5,023,252 to Hsieh; and (C) a thickening agent; including, for example, a composition in which the cyclic enhancer is a macrocyclic ester or a macrocyclic ketone; the use of the composition to treat a condition, for example, male hypogonadism, in a patient by applying the composition to the membrane of the patient; and a method for making the composition.2013-03-07
20130059829TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS - A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-β-hydroxysteroid dehydrogenase Type 1 enzyme activity.2013-03-07
20130059830NOVEL PROLYLCARBOXYPEPTIDASE INHIBITORS - Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.2013-03-07
20130059831NOVEL CRYSTAL FORM OF PYRROLIDYLTHIOCARBAPENEM DERIVATIVE - Novel crystals of a pyrrolidylthiocarbapenem derivative having excellent stability is provided. According to the present invention, a crystal of (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3[[(3S,5S)-5-(sulfamoylaminomethyl)pyrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid having a diffraction pattern in powder X-ray diffraction having main peaks at diffraction angles (2θ) of about 6.62, 13.04, 15.44, 16.58, 17.64, 20.88, 23.26, 25.02 and 25.52 (degrees) are provided.2013-03-07
20130059832COMPOUNDS 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.2013-03-07
20130059833PDE10 MODULATORS - The present invention relates to compounds of formula (I)2013-03-07
20130059834PYRROLOPYRAZINE KINASE INHIBITORS - The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I,2013-03-07
20130059835HETEROCYCLYLAMINES AS PI3K INHIBITORS - The present invention provides heterocyclylamine derivatives of Formula I:2013-03-07
20130059836PYRAZOLOPYRIMIDINE COMPOUNDS FOR THE TREATMENT OF CANCER - Compound of Formula (I): are described, along with pharmaceutically acceptable salts thereof, compositions containing the same, and methods of use thereof in the treatment of cancer.2013-03-07
20130059837BENZAZEPINE COMPOUND - Provided is a compound which is useful as an agent for treating or preventing 5-HT2013-03-07
20130059838SUBSTITUTED N-HETEROARYL TETRAHYDRO-ISOQUINOLINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - The present disclosure relates to a series of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I).2013-03-07
20130059839PYRIDYLTHIAZOLE-BASED UREAS AS INHIBITORS OF RHO ASSOCIATED PROTEIN KINASE (ROCK) AND METHODS OF USE - Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed.2013-03-07
20130059840SULFONAMIDO PYRROLIDINE COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF - Described herein are novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.2013-03-07
20130059841THERAPEUTIC COMPOSITIONS AND METHODS - The present invention relates in general to therapeutic compositions and methods of use. In preferred embodiments, the invention relates to the field of eye health. In some embodiments, the invention relates to the prevention and treatment of macular degeneration by administering compounds disclosed herein. In some embodiments, the invention relates to compositions and methods of improving vision.2013-03-07
20130059842MANUFACTURING OF QUICK RELEASE PHARMACEUTICAL COMPOSITONS OF WATER INSOLUBLE DRUGS AND PHARMACEUTICAL COMPOSITIONS OBTAINED BY THE PROCESS OF THE INVENTION - It has been found that pharmaceutical compositions comprising water insoluble drugs can be manufactured and formulated in a manner ensuring fast dissolution in gastric fluid. Advantageously, the manufacturing process provides a significantly improved stability, thus resulting in compositions that may have a longer shelf life than conventionally formulated and processed drugs.2013-03-07
20130059843Thiazolyl- and Oxazolyl-Isoquinolinones and Methods for Using Them - The present invention relates to substituted thiazolyl- and oxazolyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thiazolyl- and oxazolyl-isoquinolinones and to their use in treating various diseases and disorders.2013-03-07
201300598442-PHENYL SUBSTITUTED IMIDAZOTRIAZINONES AS PHOSPHODIESTERASE INHIBITORS - The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.2013-03-07
20130059845BICYCLIC AGONISTS OF GPR131 AND USES THEREOF - The present disclosure relates to compounds that act as agonists of, or otherwise modulate the activity of, GPR131 and to their use in the treatment of various diseases. In particular embodiments, the structure of the compounds is given by Formula I:2013-03-07
20130059846COMPOUNDS 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.2013-03-07
20130059847SUBSTITUTED N-(3-(PYRIMIDIN-4-YL)PHENYL)ACRYLAMIDE ANALOGS AS TYROSINE RECEPTOR KINASE BTK INHIBITORS - In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.2013-03-07
20130059848CANNABINOID-2 AGONISTS - The present specification discloses cannabinoid-2 agonists, compositions comprising such cannabinoid-2 agonists, and methods of treating an individual suffering from a disease by administering compositions comprising such cannabinoid-2 agonists. (Formula I and III)2013-03-07
20130059849AZAINDAZOLES - Herein are disclosed azaindazoles of formula (I)2013-03-07
20130059850AZA-INDOLE DERIVATIVES USEFUL AS MODULATORS OF FAAH - The present invention is directed to certain Aza-Indole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.2013-03-07
20130059851Methods of Diagnosing and Treating Cancer in Patients Having or Developing Resistance to a First Cancer Therapy - A method of identifying a subject having cancer who is likely to benefit from treatment with a combination therapy with a RAF inhibitor and a second inhibitor is provided. A method of treating cancer in a subject in need thereof is also provided and includes administering to the subject an effective amount of a RAF inhibitor and an effective amount of a second inhibitor, wherein the second inhibitor is a MEK inhibitor, a CRAF inhibitor, a CrkL inhibitor or a TPL2/COT inhibitor. A method of identifying a kinase target that confers resistance to a first inhibitor is also provided.2013-03-07
20130059852COMPOUNDS FOR TREATING DISEASE, FOR ADMINISTERING, AND FOR PHARMACEUTICAL COMPOSITIONS - Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).2013-03-07
20130059853BIARYL PHOSPHODIESTERASE INHIBITORS - Novel biaryl compounds with phosphodiesterase inhibitory activity of the general formula (I), wherein R1, R2, R3, X, Y, Z2013-03-07
20130059854Dosage Form for Insertion Into the Mouth - Oral dosage forms as a biodegradable, water soluble film for delivering pharmaceutically active agents, particularly anti-migraine agents to patients through insertion into the mouth of patient and methods for administering pharmaceutically active agents to patients by insertion into the mouth to provide selective uptake of said agents through the mucosa and thus avoiding the gastrointestinal tract.2013-03-07
20130059855CRYSTAL OF DI(ARYLAMINO)ARYL COMPOUND - Provided are crystals of compound A which have properties suitable for industrial production.2013-03-07
20130059856AGONISTS OF GPR131 AND USES THEREOF - Chemical compounds which act as agonists of, or otherwise modulate the activity of, GPR131 are disclosed. Related compositions, formulations and methods of use are also described.2013-03-07
20130059857METHODS AND COMPOSITIONS FOR SAFE AND EFFECTIVE TREATMENT OF TELANGIECTASIA - Improved methods and compositions for safe and effective treatment of telangiectasia or a symptom associated with telangiectasia in a subject are described. The methods involve topically applying to an affected skin area a topical composition comprising about 0.3% to about 10% by weight of brimonidine and a pharmaceutically acceptable carrier.2013-03-07
20130059858BENZOFURANYL ANALOGUES AS GPR119 MODULATORS - Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, where-in A, L, m, n, o, p, R2013-03-07
20130059859PREDICTIVE BIOMARKERS FOR PI3K/AKT KINASE PATHWAY INHIBITOR EFFICACY - A method of predicting the sensitivity of tumor cell growth to inhibition by a PI3K/AKT kinase pathway inhibitor, comprising: determining the localization profile of FOXO3a in a tumor cell, wherein a cytoplasmic localization profile of FOXO3a correlates with sensitivity to inhibition by a PI3K/AKT kinase inhibitor and a nuclear localization profile of FOXO3a correlates with resistance to inhibition by a PI3K/AKT kinase inhibitor.2013-03-07
20130059860NAPHTHALENE CARBOXAMIDE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to naphthalene carboxamide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimers disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.2013-03-07
20130059861METHOD FOR INDUCING TUMOR APOPTOSIS BY INCREASING NITRIC OXIDE LEVELS - The present invention refers to a method for inducing tumor apoptosis by influencing the ROS (reactive oxygen species) signaling pathway in tumor cells. Increasing the level of ROS leads to the selective inactivation of a tumor cell catalase and subsequently to an apoptosis of these cells. The level of ROS can be increased by increasing the level of nitric oxide through inhibition of the enzymes nitric oxide dioxygenase or arginase. According to the present invention inhibitors of the nitric oxide dioxygenase or arginase can be used for the manufacture of a medicament for the treatment of cancer. The present invention further provides a method for identifying compounds which can be used for the treatment of cancer, wherein the method allows to specifically identify compounds which induce apoptosis through the ROS signaling pathway. The present invention also provides a kit for identifying compounds which induce tumor apoptosis by inactivating a catalase on the tumor cell surface.2013-03-07
20130059862Novel 1, 2-Disubstituted Amido-anthraquinone Derivatives, Preparation Method and application thereof - The invention provides a series of novel 1,2-disubstituted amido-anthraquinone derivatives. Further, the invention also provides the preparation method and application of said derivatives, said application comprises: said derivatives with therapeutically effective amount are prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.2013-03-07
20130059863SUBSTITUTED N-HETEROARYL SPIROLACTAM BIPYRROLIDINES, PREPARATION AND THERAPEUTIC USE THEREOF - The present disclosure relates to a series of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I).2013-03-07
20130059864INHIBITING NEUROTRANSMITTER REUPTAKE - This document relates to compounds as well as methods and materials involved in modulating neurotransmitter reuptake. For example, compounds, methods for synthesizing compounds, and methods for inhibiting neurotransmitter reuptake are provided.2013-03-07
20130059865COMPOUNDS HAVING ANTIVIRAL PROPERTIES - The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.2013-03-07
20130059866NOVEL PIPERIDINO-DIHYDROTHIENOPYRIMIDINE SULFOXIDES AND THEIR USE FOR TREATING COPD AND ASTHMA - The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I,2013-03-07
20130059867SALT OF FUSED HETEROCYCLIC DERIVATIVE AND CRYSTAL THEREOF - An objective of the present invention is to improve the solubility of 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid.2013-03-07
20130059868TREATMENT OF GOUT - Sodium 2-(5-bromo-4-(4-cyclopropyl-naphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetate is described. In addition, pharmaceutical compositions and uses such compositions for the treatment of a variety of diseases and conditions.2013-03-07
20130059869METHODS AND COMPOSITIONS FOR TREATING DISORDERS - Compounds and compositions for treating disorders related to TRPA1 are described herein.2013-03-07
20130059870USE OF MYELOPEROXIDASE (MPO) INHIBITORS OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF TO TREAT MULTIPLE SYSYEM ATROPHY (MSA) 938 - The present invention relates to the use of MPO inhibitors for the treatment of multiple system atrophy. The present invention also relates to the use of MPO inhibitors for the treatment of Huntington's disease. The present invention also relates to the use of MPO inhibitors for neuroprotection.2013-03-07
20130059871PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF AMYLOID-RELATED DISEASES - The present invention provides (I) these compounds are useful in prevention and treatment of neurodegenerative disorders, such as Alzheimer's, Parkinson's and Huntington's as well as type II diabetes.2013-03-07
20130059872POLYMORPHS OF ALOGLIPTIN BENZOATE - The present invention provides new amorphous forms of alogliptin benzoate, pharmaceutical compositions comprising same, methods for their preparation and use thereof in treating conditions mediated by DPP-IV, in particular, type 2 diabetes.2013-03-07
20130059873PHARMACEUTICAL COMPOSITIONS AS INHIBITORS OF DIPEPTIDYL PEPTIDASE-IV (DPP-IV) - The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.2013-03-07
20130059874SUBSTITUTED N-PHENYL SPIROLACTAM BIPYRROLIDINES, PREPARATION AND THERAPEUTIC USE THEREOF - The present disclosure relates to a series of substituted N-phenyl spirolactam bipyrrolidines of formula (I).2013-03-07
20130059875METHODS OF TREATING TRAVELER'S DIARRHEA AND HEPATIC ENCEPHALOPATHY - Treatment of traveler's diarrhea using in subjects having hepatic encephalopathy using gastrointestinal specific antibiotics is disclosed. One example of a gastrointestinal specific antibiotic is rifaximin.2013-03-07
20130059876LIQUID NASAL SPRAY CONTAINING LOW-DOSE NALTREXONE - Liquid formulations for administration of naltrexone at low concentrations by the nasal route are described.2013-03-07
20130059877TREATMENT OF SOLID TUMORS WITH RAPAMYCIN DERIVATIVES - Rapamycin derivatives have interesting effects in the treatment of solid tumours, optionally in combination with a chemotherapeutic agent.2013-03-07
20130059878TREATMENT OF DISEASES MODULATED BY A H4 RECEPTOR AGONIST - The invention provides a method for the treatment of H4R modulated diseases and/or conditions comprising administering to the subject an effective amount of a H4R agonist. The invention also provides a method for treating COPD comprising administering to the subject an effective amount of a H4R agonist, a H1R antagonist and an anticholinergic drug. Further, the invention provides a pharmaceutical formulation comprising a H4R agonist, a second active agent and a pharmaceutically acceptable carrier.2013-03-07
20130059879Small Molecule Inhibitors of PFKFB3 and Glycolytic Flux and Their Methods of Use as Anti-Cancer Therapeutics - Small molecule inhibitors of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) having the following formula: Formula (1) are provided herein. Also provided herein are pharmaceutical compositions containing Formula I compounds, together with methods of treating cancer, methods of inhibiting PFK.FB3 enzymatic activity, methods of inhibiting glycolytic flux, and methods of treating tumors by administering an effective amount of a Formula I compound.2013-03-07
20130059880MOXIFLOXACIN HYDROCHLORIDE COMPOUNDS AND INTERMEDIATES AND METHODS FOR MAKING SAME - Methods for producing moxifloxacin hydrochloride compounds having very low levels of impurities are provided. Compounds produced using such methods and pharmaceutical compositions including such compounds are also provided.2013-03-07
20130059881COMPOSITIONS AND METHODS FOR TREATING VIRAL DISEASES - Substituted perhydro pyrrolopyridines and methods for their use in the treatment of viral diseases including hepatitis C viral infections are described herein.2013-03-07
201300598828-Phenylisoquinolines And Pharmaceutical Composition Used In Treatment For Sepsis - A compound is provided. The compound includes a formula of:2013-03-07
20130059883COMPOUNDS AND METHODS - Disclosed are compounds having the formula:2013-03-07
20130059884INHIBITOR OF THE DIFFERENTIATION OF T CELLS INTO TH1 CELLS - The present invention is to provide an inhibitor that inhibits differentiation of T cells into Th1 cells.2013-03-07
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