| 07th week of 2013 patent applcation highlights part 45 |
| Patent application number | Title | Published |
|---|
| 20130040923 | INTRANASAL LOWER DOSAGE STRENGTH TESTOSTERONE GEL FORMULATIONS AND USE THEREOF FOR TREATING ANORGASMIA OR HYPOACTIVE SEXUAL DESIRE DISORDER - The present invention relates to lower dosage strength pernasal testosterone gel formulations for intranasal administration and treatment methods for using the lower dosage strength pernasal testosterone gel formulations for treating a female subject with anorgasmia and/or hypoactive sexual desire disorder. | 2013-02-14 |
| 20130040924 | BRIDGED POLYCYCLIC COMPOUND BASED COMPOSITIONS FOR THE INHIBITION AND AMELIORATION OF DISEASE - A pharmaceutically active agent, a pharmaceutically active agent carrier and method of use thereof are described. In some embodiments, a system may include a composition. The composition may include one or more bridged polycyclic compounds. At least one of the bridged polycyclic compounds may include at least two cyclic groups, and at least two pharmaceutically active agents may be associated with the bridged polycyclic compound. In some embodiments, a bridged polycyclic compound may be pharmaceutically active. In some embodiments, a bridged polycyclic compound may be function as a carrier for pharmaceutically active agents. | 2013-02-14 |
| 20130040925 | OSMIUM (II) ARENE AZO ANTI-CANCER COMPLEXES - The present invention relates to the use of certain osmium containing complexes such as cytotoxic agents particularly for the treatment of cancer. There is also provided novel osmium containing complexes, as well as pharmaceutical formulations comprising such complexes. | 2013-02-14 |
| 20130040926 | NOVEL COMPOUND - There is provided a compound which is (a) a pyrimidine sulfonamide of formula (I) or (b) a pharmaceutically acceptable salt thereof, crystalline forms of the compound, processes for obtaining the compound, pharmaceutical intermediates used in the manufacture of the compound, and pharmaceutical compositions containing the compound. | 2013-02-14 |
| 20130040927 | CHOLESTEROL ABSORPTION INHIBITOR AND OMEGA 3 FATTY ACIDS FOR THE REDUCTION OF CHOLESTEROL AND FOR THE PREVENTION OR REDUCTION OF CARDIOVASCULAR, CARDIAC AND VASCULAR EVENTS - A composition and a method of treatment for the reduction of risk factors for cardiovascular disease utilizing a combination of lipid lowering cholesterol absorption inhibitors, e.g. azetidinones, with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight including a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DPA) and Docosahexaenoic acid (DHA) in a weight ratio of EPA:DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA represent about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition are taught. | 2013-02-14 |
| 20130040928 | NITROGEN HETEROCYCLE DERIVATIVES, PREPARATION THEREOF AND APPLICATION THEREOF IN HUMAN THERAPEUTICS - The present invention relates to compounds having general formula I characterised in that | 2013-02-14 |
| 20130040929 | NOVEL 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. | 2013-02-14 |
| 20130040930 | NOVEL AMIDE DERIVATIVE AND USE THEREOF AS MEDICINE - Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) | 2013-02-14 |
| 20130040931 | Amino Heteroaryl Compounds as Beta-Secretase Modulators and Methods of Use - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein ring A, B | 2013-02-14 |
| 20130040932 | SUBSTITUTED ARYL SULFONE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS - A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. | 2013-02-14 |
| 20130040933 | AZAINDOLES AS JANUS KINASE INHIBITORS - The present invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof. Compounds of formula I are inhibitors of Janus kinases and as such are useful for the treatment of various diseases and conditions mediated by said enzymes, such as rheumatoid arthritis, asthma, COPD, ALS, and the like. | 2013-02-14 |
| 20130040934 | SPIROCYCLIC COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS AND DIAGNOSTIC PROBES - The invention relates to new triazines (G=Q=U are N), pyrimidines (two out of G, Q and U are N), and pyridopyrimidines (one of G and U together with R2 forms an anullated pyridine ring) of formula (I) carrying a spirocyclic substituent, wherein E | 2013-02-14 |
| 20130040935 | CYCLIC KETO-ENOLS FOR THERAPY - The invention relates to 5′-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of tumour disorders. | 2013-02-14 |
| 20130040936 | 1,4-OXAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS - This invention relates to compounds of the formula | 2013-02-14 |
| 20130040937 | INHIBITORS FOR TREATING AND PREVENTING HEART FAILURE IN FELINES - The present invention relates to an I | 2013-02-14 |
| 20130040938 | COMPOSITIIONS FOR TREATING COGNITIVE DISORDERS - Disclosed herein is a pharmaceutical composition comprising a cholinesterase inhibitor and compound of the following formula: | 2013-02-14 |
| 20130040939 | Oral Suspension Formulations of Esclicarbazepine Acetate - An oral suspension formulation comprising eslicarbazepine acetate and a pharmaceutically acceptable liquid vehicle. | 2013-02-14 |
| 20130040940 | MERCAPTOAMIDINE DERIVATIVES AND METHODS OF USE - Compounds of formula (I) | 2013-02-14 |
| 20130040941 | BENZODIAZEPINE COMPOUND AND PHARMACEUTICAL COMPOSITION - The present invention provides a novel benzodiazepine compound that blocks the I | 2013-02-14 |
| 20130040942 | SALTS OF POTASSIUM ATP CHANNEL OPENERS AND USES THEREOF - Provided are immediate or prolonged administration of certain salts of K | 2013-02-14 |
| 20130040943 | TRICYCLIC PYRIDYL-VINYL PYRROLES AS PAR1 INHIBITORS - This disclosure relates to compounds of formula I: | 2013-02-14 |
| 20130040944 | MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION - Pyrrole compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction. | 2013-02-14 |
| 20130040945 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS - Chemical entities that are arctigenin derivatives, pharmaceutical compositions and methods of treatment of cancer are described. | 2013-02-14 |
| 20130040946 | SUBSTITUTED IMIDAZOPYRIMIDINES AND TRIAZOLOPYRIMIDINES - The invention relates to substituted imidazo- and triazolopyrimidines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of haematological disorders, preferably of leucopenias and neutropenias. | 2013-02-14 |
| 20130040947 | TRKB AGONISTS AND METHODS OF USE - Compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering a 7,8-di-hydroxyflavone derivative with modified flavone or heterocyclic ring to a subject in need thereof. Methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided. | 2013-02-14 |
| 20130040948 | NOVEL BENZODIOXOLE PIPERAZINE COMPOUNDS - The present invention is concerned with novel dual modulators of the 5-HT | 2013-02-14 |
| 20130040949 | TYPE II RAF KINASE INHIBITORS - The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions. | 2013-02-14 |
| 20130040950 | MULTISUBSTITUTED AROMATIC COMPOUNDS AS INHIBITORS OF THROMBIN - There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin. | 2013-02-14 |
| 20130040951 | PROPHYLACTIC OR THERAPEUTIC AGENT FOR CANCER - A compound represented by the formula (I): | 2013-02-14 |
| 20130040952 | INFLUENZA VIRUS INHIBITORS THAT DISRUPT NUCLEOPROTEIN TRIMERIZATION - Methods for identifying agents capable of disrupting a salt bridge in an influenza A virus nucleoprotein corresponding to the E339 . . . R416 salt bridge in SEQ ID NO:1, and thus the trimerization of the NP protein; and uses of such agents, e.g., small molecules and peptides, for inhibiting influenza virus replication and treating infection caused by influenza virus. | 2013-02-14 |
| 20130040953 | PROMOTION OF WOUND HEALING - The present invention provides compositions and methods that promote wound healing in a subject with a cutaneous injury. In particular, the present invention provides systemic and/or local administration of one or more compositions that cause ganglioside depletion (e.g., glucosylceramide synthase (GCS) inhibitors) for the treatment of cutaneous wounds. | 2013-02-14 |
| 20130040954 | PLEUROMUTILIN DERIVATIVES FOR THE TREATMENT OF DISEASES MEDIATED BY MICROBES - Pleuromutilin derivative compounds of the following formula, and uses thereof for the treatment of diseases mediated by microbes, are disclosed: | 2013-02-14 |
| 20130040955 | 6-CYCLOALKYL-PYRAZOLOPYRIMIDINONES FOR THE TREATMENT OF CNS DISORDERS - The invention relates to novel pyrazolopyrimidinones according to formula (I). | 2013-02-14 |
| 20130040956 | PROCESS FOR THE PREPARATION OF STABLE, CRYSTALLINE (6S)-N(5)-METHYL-5,6,7,8-TETRAHYDROFOLIC ACID - A process for the preparation of the stable, amorphous calcium salt of (6S)-N(5)-methyl-5,6,7,8-tetrahydrofolic acid of the formula V, | 2013-02-14 |
| 20130040957 | Deuterium-Enriched Pyrimidine Compounds and Derivatives - The present invention is concerned with deuterium-enriched pyrimidine compounds of formula I, their derivatives, enantiomers, diastereomers, solvates and pharmaceutical salts thereof, | 2013-02-14 |
| 20130040958 | IMATINIB MESYLATE PREPARATION PROCEDURE - Methods for making Imatinib mesylate of formula (I): | 2013-02-14 |
| 20130040959 | Heterocyclic Quinolizine Derived M1 Receptor Positive Allosteric Modulators - The present invention is directed to novel 3-oxo-2,3-dihydropyrazolo[4,3-c]quinolizine derived compounds of generic formula (I) or a pharmaceutically acceptable salt thereof, 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 Alzheimer's 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. | 2013-02-14 |
| 20130040960 | OPHTHALMIC GEL OF GATIFLOXACIN AND PREPARATION METHOD THEREOF - An ophthalmic gel of gatifloxacin and the preparation method thereof are disclosed. The gel comprises gatifloxacin or its pharmaceutical salts, matrix and water. Said matrix is one or more selected from carbomer, mixture of carbomer and HPMC, and sodium hyaluronate. | 2013-02-14 |
| 20130040961 | OLIGOMER MODIFIED DIAROMATIC SUBSTITUTED COMPOUNDS - Disclosed are compounds comprising diaromatic substituted compound residues, namely the anti-viral (anti-HIV) drug delavirdine, covalently attached via a linkage to water-soluble, non-peptidic oligomers, specifically to poly(ethylene glycol) PEG) oligomers. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over non-oligomer modified diaromatic substituted compounds. | 2013-02-14 |
| 20130040962 | P38 MAP Kinase Inhibitors - There is provided a compound of formula (I): wherein: J represents (A): or (B): compositions comprising same, processes for preparing said compounds and use thereof in treatment, particularly in the treatment of inflammatory disease, such as asthma, COPD and 15 rheumatoid arthritis. | 2013-02-14 |
| 20130040963 | Compounds, Compositions and Methods of Using Same for Modulating Uric Acid Levels - Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid. | 2013-02-14 |
| 20130040964 | 1,2,3-TRIAZOLE-BASED PEPTIDOMIMETIC INTEGRIN INHIBITORS FOR THE DIAGNOSIS AND THERAPY OF TUMORS - The present invention refers to the field of chemical compounds bearing a 1,2,3-triazole ring of formula (I) and possessing guanidino and carboxylic groups or their isosteres, their preparation by Cu-catalyzed “click-chemistry”, and medical-diagnostic use in pathologies where angiogenesis is altered, for example pathologic conditions of tumor origin, tumor metastasis, osteoporosis, and rheumatoid arthritis. | 2013-02-14 |
| 20130040965 | AMINOTETRALIN COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS - The invention provides aminotetralin compounds of formula (I): | 2013-02-14 |
| 20130040966 | PHARMACEUTICAL FORMULATIONS CONTAINING DOPAMINE RECEPTOR LIGANDS - The present invention relates to stable and bioavailable immediate release formulations comprising dopamine receptor ligands. Methods of treating various disorders by administering the formulations are also described. | 2013-02-14 |
| 20130040967 | 4'-DEMETHYLEPIPODOPHYLLOTOXIN DERIVATIVE, PREPARATION METHOD AND USE THEREOF - A 4′-demethylepipodophyllotoxin derivative of formula(III) having anti-tumor activity is provided. After the activation of hydroxyl in position C4 of 4′-demethylepipodophyllotoxin, tetramethylpyrazine is introduced by transamination to obtain the 4′-demethylepipodophyllotoxin derivative which is preferably used to inhibit gastric cancer line BGC-823. | 2013-02-14 |
| 20130040968 | FAT OR OIL COMPOSITION - Provided is an oil or fat composition, including a vitamin B1 derivative or a salt thereof at a content of 44 to 8,000 ppm in terms of thiamine and having a hydroxyl value of 9 to 100 mg-KOH/g, in which the content C (ppm) of the vitamin B1 derivative or the salt thereof in terms of thiamine and the hydroxyl value X (mg-KOH/g) satisfy a relationship of the following expression (1): | 2013-02-14 |
| 20130040969 | Fungicidal Mixtures Based on Azolopyrimmidinylamines - Fungicidal mixtures based on azolopyrimidinylamines. | 2013-02-14 |
| 20130040970 | Co-Crystals Of A Triazolo [4,5-D] Pyrimide Platelet Aggregation Inhibitor - The present invention relates to novel co-crystal forms of the compound of formula (I); wherein the co-former molecule is selected from glycolic acid, salicylic acid, decanoic (capric) acid, gentisic acid (2,5-dihydroxybenzoic acid), glutaric acid, vanillic acid (4-hydroxy-3-methoxybenzoic acid), succinic acid, malonic acid or maltol (3-hydroxy-2-methyl-4-pyrone); and to processes for their preparation, to pharmaceutical compositions containing such co-crystals, to the use of such co-crystals in the manufacture of a medicament for use in the prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of a co-crystal of the compound of formula (I). | 2013-02-14 |
| 20130040971 | 6-CYCLOALKYL-PYRAZOLOPYRIMIDINONES FOR THE TREATMENT OF CNS DISORDERS - The invention relates to novel pyrazolopyrimidinones according to formula (I) | 2013-02-14 |
| 20130040972 | USE OF c-Src INHIBITORS IN COMBINATION WITH A PYRIMIDYLAMINOBENZAMIDE COMPOUND FOR THE TREATMENT OF LEUKEMIA - The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) a pyrimidylaminobenzamide compound; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukemia, especially chronic myelogenous leukemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Btk kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, in combination with a pyrimidylaminobenzamide compound, in particular 4-Methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl]benzamide. | 2013-02-14 |
| 20130040973 | JAK PI3K/mTOR COMBINATION THERAPY - Provided herein is a combination therapy comprising a JAK kinase inhibitor and a dual PI3K/mTOR inhibitor, as well as methods of treating various cancers through the use of such a combination therapy. | 2013-02-14 |
| 20130040974 | PIPERIDINE INHIBITORS OF JANUS KINASE 3 - The present invention relates to new piperidine inhibitors of Janus kinase 3 activity, pharmaceutical compositions thereof, and methods of use thereof. | 2013-02-14 |
| 20130040975 | GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO - GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: | 2013-02-14 |
| 20130040976 | INDAZOLE INHIBITORS OF THE WNT SIGNAL PATHWAY AND THERAPEUTIC USES THEREOF - Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 2013-02-14 |
| 20130040977 | Pro-Neurogenic Compounds - This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like. | 2013-02-14 |
| 20130040978 | SPIRO ISOXAZOLINE COMPOUNDS AS SSTR5 ANTAGONISTS - Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety. | 2013-02-14 |
| 20130040979 | CCR1 INHIBITORS USEFUL FOR THE TREAMENT OF MULTIPLE MYELOMA AND OTHER DISORDERS - The invention relates to the use of inhibitors of CCR1 for the treatment of cancers and osteolytic bone disorders. In some embodiments, the invention relates to methods for the treatment of multiple myeloma, smoldering multiple myeloma and secondary bone cancers. | 2013-02-14 |
| 20130040980 | CCI-779 CONCENTRATE FORMULATIONS - This invention provides CCI-779 cosolvent concentrates which are useful in preparing a parenteral formulation of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) following admixture with a diluent. | 2013-02-14 |
| 20130040981 | Pyridylvinylpyrazoloquinolines as PAR1 inhibitors - The disclosure relates to compounds of formula I: | 2013-02-14 |
| 20130040982 | ORAL SUSTAINED RELEASE FORMULATION OF HUPERZINE A - Sustained-release formulations comprising huperzine A are disclosed herein. The formulations are for oral administration, and contain a carrier which comprises native albumin. Unit dosage forms of the formulations, and kits comprising such unit dosage forms are also disclosed herein. Methods utilizing the formulations for treating a medical condition treatable by huperzine A are also disclosed herein, as well as processes for preparing the formulations, and uses of huperzine A and albumin in the manufacture of a medicament. | 2013-02-14 |
| 20130040983 | RAF KINASE INHIBITORS - Described herein are compounds, pharmaceutical compositions and methods for the inhibition of RAF kinae mediated signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human disease and disorders. | 2013-02-14 |
| 20130040984 | 7-(lH-PYRAZOL-4-YL)-1,6-NAPHTHYRIDINE COMPOUNDS AS SYK INHIBITORS - The present invention relates to a compound of formula (I): | 2013-02-14 |
| 20130040985 | CHROMEN-2-ONE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - The present application discloses novel 8-aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the application discloses the use of these compounds, a method for therapy and to pharmaceutical compositions comprising these compounds. | 2013-02-14 |
| 20130040986 | Modulators of Cystic Fibrosis Transmembrane Conductance Regulator - The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR. | 2013-02-14 |
| 20130040987 | Stereoisomeric Compounds and Methods for the Treatment of Gastrointestinal and Central Nervous System Disorders - The subject invention provides stereoisomeric compounds of formula (X): | 2013-02-14 |
| 20130040988 | 3-AMINO-PYRIDINE DERIVATIVES FOR THE TREATMENT OF METABOLIC DISORDERS - Compounds represented by the general formula (1): | 2013-02-14 |
| 20130040989 | 1-CYCLOPROPYL-8-METHYL-7-[5-METHYL-6-(METHYLAMINO)-3-PYRIDINYL]-4-OXO-1,4-- DIHYDRO-3-QUINOLINECARBOXYLIC ACID SALTS - There is provided a salt of 1-cyclopropyl-8-methyl-7-[5-methyl-6-(methylamino)-3-pyridinyl]-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid selected from the group consisting of citrate, hemi-fumarate, maleate, L-tartrate, mesylate, hydrochloride, potassium, and sodium salts. | 2013-02-14 |
| 20130040990 | SYNTHESIS OF DGJNAc FROM D-GLUCURONOLACTONE AND USE TO INHIBIT ALPHA-N-ACETYLGALACTOSAMINIDASES - A convenient and scalable synthesis of DGJNAc ID from D-glucuronolactone in an overall yield of 20% is provided. DGJNAc is the first highly potent and specific competitive inhibitor of GalNAcases. DGJNAc ID is also a competitive inhibitor of -hexosaminidases. Synthesis and activity of L-DGJNAc IL is also shown. The use of DGJNAc as a potent and specific inhibitor of GalNAcases will allow useful investigation and treatment of a number of diseases, including Schindler Disease. | 2013-02-14 |
| 20130040991 | PHARMACEUTICAL COMPOSITION COMPRISING GEMFIBROZIL AND CYP2C8 AND/OR OATP SUBSTRATE DRUG SUCH AS REPAGLINIDE - The invention provides gemfibrozil for use in adjusting the effect of a CYP2C8 and/or OATP substrate drug, wherein gemfibrozil is administered in an amount of less than 1200 mg/day. The invention also provided a pharmaceutical composition comprising gemfibrozil providing a significant improvement to the plasma profiles of a CYP2C8 and/or OATP substrate drug in a mammal. | 2013-02-14 |
| 20130040992 | Substituted 2, 6-Diamino-3, 5-Dicyano-4-Aryl-Pyridines And Their Use As Adenosine-Receptor-Selective Ligands - The present invention relates to substituted 2,6-diamino-3,5-dicyano-4-arylpyridines of the formula (I) | 2013-02-14 |
| 20130040993 | FUNGICIDE HYDROXIMOYL-HETEROCYCLES DERIVATIVES - The present invention relates to hydroximoyl-heterocycle derivatives, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. | 2013-02-14 |
| 20130040994 | Methods of Treatment Using Allosteric Processing Inhibitors for Matrix Metalloproteinases - The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues. The present invention also relates to the use of small-molecule allosteric processing inhibitors for the treatment of diseases mediated by inappropriate matrix metalloproteinase (MMP) activity. | 2013-02-14 |
| 20130040995 | NOVEL COMPOUNDS - There is provided inter alia a compound of formula (I): | 2013-02-14 |
| 20130040996 | COMPOSITION FOR TREATING ATHEROSCLEROSIS AND A PREPARATION METHOD THEREOF - Disclosed are a composition for preventing and treating atherosclerosis which includes chalcone compound. In particular, the chalcone compound bound with 2-hydroxyl in ring A and 4′-methyoxy in ring B has versatile therapeutic potentials on anti-atherosclerosis by acting as PPARγ inducer, p44/42 MAPK inhibitor and cell cycle blocker and does not show toxicity to human aortic smooth muscle cells (HASMCs). In addition, the chalcone compound exhibits synergistic effect with the PPARγ ligand (rosiglitazone) to inhibit cell proliferation and the upregulation of cyclin D1, cyclin D3, interleukin-1β (IL-1β) and interleukin-6 (IL-6) induced by oxidized low density lipoprotein (Ox-LDL). | 2013-02-14 |
| 20130040997 | NOVEL PYRIDINE CARBOXYLIC ACID BASED COMPOUND USED AS A P2X1 AND P2X3 RECEPTOR ANTAGONIST, A PRODUCTION METHOD FOR THE SAME AND A COMPOSITION COMPRISING THE SAME - Provided are a novel pyridine carboxylic acid based compound used as a P2X | 2013-02-14 |
| 20130040998 | FLUORINATED HDAC INHIBITORS AND USES THEREOF - Fluorinated deacetylase inhibitors of the general formulae (I), (II), and (III): and pharmaceutically acceptable salts thereof, as described herein, are useful as inhibitors of histone deacetylases or other deacetylases, and thus are useful for the treatment of various diseases and disorders associated with acetylase activity as described herein (e.g., cancer, neurodegenerative diseases, inflammatory diseases). | 2013-02-14 |
| 20130040999 | NEW COMPOUNDS FOR ALLEVIATION, PREVENTION OR TREATMENT OF OSTEOPOROSIS, THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - The present invention provides novel compounds of Chemical Formula I, a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, a preparation thereof and a composition for the alleviation, prevention or treatment of osteoporosis, comprising thereof in an effective amount, and a method for alleviating, preventing or treating osteoporosis. | 2013-02-14 |
| 20130041000 | NOVEL AZOLE COMPOUND - Azole compounds represented by formula I: | 2013-02-14 |
| 20130041001 | VALSARTAN DERIVATIVES CARRYING NITROGEN OXIDE DONORS FOR THE TREATMENT OF VASCULAR AND METABOLIC DISEASES - Nitrate esters and diazeniumdiolate derivatives of valsartanamide are described. They have valuable properties in the treatment of vascular and metabolic diseases. | 2013-02-14 |
| 20130041002 | DENIBULIN DI-HYDROCHLORIDE - MN-029 di-hydrochloride (MN-029.2HCl, Formula 2) is a potent vascular targeting agent. | 2013-02-14 |
| 20130041003 | Bendamustine Pharmaceutical Compositions - The present invention provides pharmaceutical formulations of lyophilized bendamustine suitable for pharmaceutical use. The present invention further provides methods of producing lyophilized bendamustine. The pharmaceutical formulations can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases. | 2013-02-14 |
| 20130041004 | Liquid Formulations Of Bendamustine - Stable liquid formulations of bendamustine, and pharmaceutically acceptable salts thereof, and polar aprotic solvents, are described. | 2013-02-14 |
| 20130041005 | PHARMACEUTICAL COMPOSITIONS COMPRISING NEUROPILIN INHIBITORS, AND THEIR USE FOR THE PREVENTION AND/OR TREATMENT OF ANGIOGENIC DISORDERS AND CANCERS - The present invention relates to a compound of general formula (I), | 2013-02-14 |
| 20130041006 | PHARMACEUTICAL COMPOSITION FOR INTRACELLAR ACIDIFICATION WITH CIS-UROCANIC ACID - A pharmaceutically acceptable agent able to acidify the cell cytoplasm for the manufacture of a pharmaceutical composition useful for causing immunosuppression in a person or animal, where an effective amount of the agent is administered in an essentially non-dissociated form to the person or animal, and where the agent is admixed with a carrier to adjust the pH of the composition to the pH range 6.1 to 7.0. A pharmaceutical composition is also disclosed. | 2013-02-14 |
| 20130041007 | Selective Androgen Receptor Modulators - This invention provides compounds of Formula (I), (Ia), (Ib), (Ic), (II), (IIa) or (III) and or salts thereof, pharmaceutical compositions comprising a compound of Formula (I), (Ia), (Ib), (Ic), (II), (IIa) or (III) and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type II diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of Formula (I), (Ia), (Ib), (Ic), (II), (IIa) or (III) and intermediates useful in the preparation of same. | 2013-02-14 |
| 20130041008 | COMPOUNDS FOR ENZYME INHIBITION - One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention. | 2013-02-14 |
| 20130041009 | Methods and means for increasing resistance to cell damage - Methods are provided to increase resistance to cell damage in a subject. The increase in resistance to cell damage in a subject in the subject is accomplished by decreasing activity of eEF2 kinase in the subject. The eEF2 kinase activity can be decreased by decreasing the amount of functional eEF2 kinase produced by the subject, including contacting the eEF2 kinase with a compound that inhibits phosphorylation of eEF2 kinase substrate or decreasing the amount of functional eEF2 kinase is decreased by reducing expression of a gene encoding the eEF2 kinase. | 2013-02-14 |
| 20130041010 | COMPOSITIONS AND METHODS FOR THE SPECIFIC INHIBITION OF GENE EXPRESSION BY DSRNA CONTAINING MODIFIED NUCLEOTIDES - The invention features compositions and methods that are useful for reducing the expression or activity of a specified gene in eukaryotic cell. | 2013-02-14 |
| 20130041011 | BASE MODIFIED BICYCLIC NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM - Provided herein are novel base modified bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, novel pyrimidine bicyclic nucleosides are provided wherein each pyrimidine base is substituted at the 5 position with an optionally substituted, aromatic or heteroaromatic ring system comprising from 5 to 7 ring atoms selected from C, N, O and S. In certain embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA. | 2013-02-14 |
| 20130041012 | NEW ISOFORM OF BRUTON'S TYROSINE KINASE (BTK) PROTEIN - The use of compounds is described which are capable of functionally blocking at least one of the genes chosen from the group composed of EphAI, EphA2, EphA8, EphB2, CSF1R, VEGFR2, RAMP2, RAMP3, CLRN1, MAPK4, PIK3C2A, PIK3CG, GSK3alpha, GSK3beta, IRAK3, DAPK1, JAK1, PIM1, TRB3, BTG1, LATS1, LIMK2, MYLK, PAK1, PAK2, CDC2, BTK, PNRC2, NCOA4, NR2C1, TPR, RBBP8, TRPC7, FXYD1, ERNI, PRSS16, RPS3, CCL23 and SERPINE1, for the manufacture of a medicament destined to diminish the resistance to chemotherapeutic drugs in the therapeutic treatment of epithelial tumour pathologies. Also described is a method for the determination of the drug resistance in tumour cells, as well as a method for the identification of tumour stem cells. | 2013-02-14 |
| 20130041013 | ISOFORM OF BRUTON'S TYROSINE KINASE (BTK) PROTEIN - The use of compounds is described which are capable of functionally blocking at least one of the genes chosen from the group composed of EphA1, EphA2, EphA8, EphB2, CSF1R, VEGFR2, RAMP2, RAMP3, CLRN1, MAPK4, PIK3C2A, PIK3CG, GSK3alpha, GSK3beta, IRAK3, DAPK1, JAK1, PIM1, TRB3, BTG1, LATS1, LIMK2, MYLK, PAK1, PAK2, CDC2, BTK, PNRC2, NCOA4, NR2C1, TPR, RBBP8, TRPC7, FXYD1, ERNI, PRSS16, RPS3, CCL23 and SERPINE1, for the manufacture of a medicament destined to diminish the resistance to chemotherapeutic drugs in the therapeutic treatment of epithelial tumour pathologies. Also described is a method for the determination of the drug resistance in tumour cells, as well as a method for the identification of tumour stem cells. | 2013-02-14 |
| 20130041014 | ISOFORM OF BRUTON'S TYROSINE KINASE (BTK) PROTEIN - The use of compounds is described which are capable of functionally blocking at least one of the genes chosen from the group composed of EphAl, EphA2, EphA8, EphB2, CSF1R, VEGFR2, RAMP2, RAMP3, CLRN1, MAPK4, PIK3C2A, PIK3CG, GSK3alpha, GSK3beta, IRAK3, DAPK1, JAK1, PIM1, TRB3, BTG1, LATS1, LIMK2, MYLK, PAK1, PAK2, CDC2, BTK, PNRC2, NCOA4, NR2C1, TPR, RBBP8, TRPC7, FXYD1, ERNI, PRSS16, RPS3, CCL23 and SERPINE1, for the manufacture of a medicament destined to diminish the resistance to chemotherapeutic drugs in the therapeutic treatment of epithelial tumour pathologies. Also described is a method for the determination of the drug resistance in tumour cells, as well as a method for the identification of tumour stem cells. | 2013-02-14 |
| 20130041015 | Use of the Lactosylceramide Synthase Isoform B1,4GALT-V as a Biomarker for Cancer - In one aspect, B1,4GalT-V, an isoform of the enzyme lactosylceramide synthase, is provided as a biomarker for cancer. Also provided are methods and compositions directed at cancers characterized by the overexpression or upregulation of the lactosylceramide synthase isoform B1,4GalT-V. | 2013-02-14 |
| 20130041016 | Compositions and Methods for Preventing and Treating Cancer via Modulating UBE1L, ISG215 and/or UBP43 - Compositions and methods of using compositions that induce UBE1L or a ubiquitin-like protein ISG15, or inhibit a deconjugase UBP43 to degrade oncogenic proteins and enhance apoptosis of cancer (neoplastic) or pre-cancerous (pre-neoplastic) cells are provided. Methods for the prevention or treatment of cancer via administration of these compositions are also provided. | 2013-02-14 |
| 20130041017 | SIRNA-BASED THERAPY OF FIBRODYPLASIA OSSIFICANS PROGRESSIVA (FOP) - This invention is directed to mutated Activin A type I receptor proteins (ACVR1) and isolated nucleic acids encoding same. The invention also relates to compositions and methods for siRNA-based regulation of mutated ACVR1 expression in the treatment of Fibrodysplasia Ossificans Progressiva (FOP). | 2013-02-14 |
| 20130041018 | METHOD OF TREATING ACUTE MYELOGENOUS LEUKEMIA - A method of treating acute myelogenous leukemia (AML) in a subject in need thereof is carried out by administering the subject an active compound in an amount effective to treat the leukemia. The active compound comprises FdUMP[10] or a pharmaceutically acceptable salt thereof. | 2013-02-14 |
| 20130041019 | SDF-1 Binding Nucleic Acids - The present invention is related to an L nucleic acid that binds to an SDF-1. | 2013-02-14 |
| 20130041020 | Methods of Control and Prophylaxis of Inflammation and Mitigation of Inflammatory Conditions in Companion Animals - The invention relates to methods of control and prophylaxis of inflammation and mitigation of inflammatory conditions, particularly arthritis and joint pain, in companion animals, e.g., dogs or cats, comprising administering a diet comprising lipoic acid. | 2013-02-14 |
| 20130041021 | METHODS OF IMPROVING THE PHARMACOKINETICS OF DOXEPIN - Methods of improving the pharmacokinetics of doxepin in a patient. | 2013-02-14 |
| 20130041022 | Glyceollins Suppress Androgen-Responsive Prostate Cancer - The present disclosure demonstrates the molecular effects of glyceollins on human prostate cancer cell LNCaP to further elucidate its potential effects on prostate cancer prevention. The glyceollins inhibited LNCaP cell growth similar to that of the soy isoflavone genistein. The growth inhibitory effects of the glyceollins appeared to be due to an inhibition on G1/S progression and correlated with an up-regulation of cyclin-dependent kinase inhibitor A1 and B1 mRNA and protein levels. By contrast, genistein only up-regulates cyclin-dependent kinase inhibitor A1. In addition, glyceollin treatments led to down-regulated mRNA levels for androgen responsive genes. In contrast to genistein, this effect of glyceollins on androgen responsive genes appeared to be mediated through modulation of an estrogen- but not androgen-mediated pathway. Hence, the glyceollins exerted multiple effects on LNCaP cells that may be considered cancer preventive and the mechanisms of action appeared to be different from other soy-derived phytochemicals. | 2013-02-14 |
