08th week of 2010 patent applcation highlights part 55 |
Patent application number | Title | Published |
20100048519 | METHODS OF TREATMENT FOR ULCERATIVE COLITIS USING AMINOSALICYLATE - Disclosed herein is a new treatment for ulcerative colitis in male mammalian subjects. Further disclosed are increased dosages of an aminosalicylate composition for treatment of moderate ulcerative colitis in male mammalian subjects. | 2010-02-25 |
20100048520 | RIFAXIMIN ANTI-RECTAL DYSFUNCTION PREPARATION - The present invention relates to compositions and methods for treating rectal disorders. | 2010-02-25 |
20100048521 | COMBINATION OF A GLUCO-KORTICOID AND BETA-CYCLODEXTRIN CONJUGATED VITAMIN A-DERIVATE COMPLEX - The present invention is related to a pharmaceutical combination of a glucocorticoid and a β-cyclodextrin conjugated vitamin A derivative complex as well as a pharmaceutical composition comprising the same. The combination and the composition of the invention can be used for reducing or eliminating skin atrophy induced by treatment with glucocorticoids (GC). Also comprised is a method for reducing or eliminating skin atrophy induced by GC treatment. Furthermore the invention concerns a kit comprising a glucocorticoid and a β-cyclodextrin conjugated vitamin A derivative complex. | 2010-02-25 |
20100048522 | Method Of Treating Otic Infections With Moxifloxacin Compositions - Ophthalmic, otic and nasal compositions containing a new class of antibiotics (e.g., moxifloxacin) are disclosed. The compositions preferably also contain one or more anti-inflammatory agents. The compositions may be utilized to treat ophthalmic, otic and nasal conditions by topically applying the compositions to the affected tissues. | 2010-02-25 |
20100048523 | Compounds, Compositions and Methods for Treating Hormone-Dependent Maladies - A composition and method of using are provided, which composition includes: at least one compound selected from the group including a compound having formula (I), a salt thereof, a prodrug thereof, a compound having formula (II), a salt thereof, a prodrug thereof, and a combination thereof, the compounds being described herein, and a combination thereof, and at least one pharmaceutically acceptable carrier; wherein the composition is suitable for administration to a mammal. Methods of using the compound are also provided. | 2010-02-25 |
20100048524 | Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity - Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3β-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3β-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer. | 2010-02-25 |
20100048525 | ANDROGEN TREATMENT IN FEMALES - The present invention is directed to a method of improving ovarian reserve in a human female with diminished ovarian reserve as measured by the female's anti-Müllerian hormone level. The method may include evaluating a first anti-Müllerian hormone level of the female, administering dehydroepiandrosterone to the female for at least about one month, and evaluating a second anti-Müllerian hormone level of the female, wherein the second anti-Müllerian hormone level is greater than the first anti-Müllerian hormone level. | 2010-02-25 |
20100048526 | PHARMACEUTICAL COMPOSITION FOR TRANSDERMAL OR TRANSMUCOUS ADMINISTRATION - The present invention relates to a novel pharmaceutical composition for transdermal or transmucous administration of at least one active substance, and comprising especially a fatty acid as a percutaneous absorption promoter, at least one alcoholic vehicle and also a stabilizer capable of stabilizing the fatty acid in the said pharmaceutical composition. | 2010-02-25 |
20100048527 | Methods and compositions for the non-surgical removal of fat - Compositions and methods useful in the non-surgical removal of localized fat deposits in patients in need thereof using pharmacologically active detergents are disclosed. The pharmacologically active detergent compositions can additionally include anti-inflammatory agents, analgesics, dispersion agents and pharmaceutically acceptable excipients but do not contain phosphotidylcholine. The pharmacologically active detergent compositions are useful for treating localized accumulations of fat including lower eyelid fat herniation, lipodystrophy and fat deposits associated with cellulite and do not require surgical procedures such as liposuction. | 2010-02-25 |
20100048528 | HETEROCYCLIC COMPOUNDS AS INHIBITORS OF BETA-LACTAMASES - This invention discloses and claims methods for inhibiting bacterial β-lactamases and treating bacterial infections by inhibiting bacterial β-lactamases in man or an animal comprising administering a therapeutically effective amount to said man or said animal of a compound, or pharmaceutically acceptable salt thereof, of formula (I) either alone or in combination with a β-lactamine antibiotic wherein said combination can be administered separately, together or spaced out over time. Pharmaceutical compositions comprising a compound of formula (I), or a combination of a compound of formula (I) and a therapeutically effective amount of a β-lactamine antibiotic, and a pharmaceutically acceptable carrier are also disclosed and claimed. | 2010-02-25 |
20100048529 | New 2-Azetidinone Derivatives Useful In The Treatment Of Hyperlipidaemic Conditions - The invention relates to compounds of formula (I) and pharmaceutically acceptable salts, solvates, and prodrugs thereof, and to their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia. The invention also relates to processes for their manufacture and pharmaceutical compositions containing them. | 2010-02-25 |
20100048530 | New 2-Azetidinone Derivatives As Cholesterol Absorption Inhibitors For The Treatment Of Hyperlipidaemic Conditions - The invention relates to 2-azetidinone derivatives of formula (I), including pharmaceutically acceptable salts, solvates and prodrugs thereof. The compounds inhibit cholesterol absorption and are useful in the treatment of hyperlipidaemic conditions. The invention also relates to processes for their manufacture and to pharmaceutical compositions containing them. | 2010-02-25 |
20100048531 | GlyT1 RECEPTOR ANTAGONISTS - The present invention relates to a compound of formula I | 2010-02-25 |
20100048532 | Benzimidazole Derivatives as Selective Acid Pump Inhibitors - This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R | 2010-02-25 |
20100048533 | LESTAURTINIB CRYSTALLINE FORM 1, CRYSTALLINE LESTAURIMIB ANHYDRATE AND AMORPHOUS LESTAURIMIB - Lestaurtinib Crystalline Form 1, isolated crystalline lestaurtinib anhydrate and amorphous lestaurtinib, processes to reproducibly make them and methods of treating patients using them. | 2010-02-25 |
20100048534 | CRYSTALLINE LESTAURTINIB HYDRATES AND CRYSTALLINE LESTAURTINIB HEMIHYDRATE HEMIACETONITRILEATE AND CRYSTALLINE LESTAURTINIB HEMIHYDRATE HEMITETRAHYDROFURANATE - Crystalline lestaurtinib hydrates and crystalline lestaurtinib hemihydrate hemicetonitrileate and crystalline lestaurtinib hemihydrate hemitetrahydrofuranate, processes to reproducibly make them and methods of treating patients using them are disclosed. | 2010-02-25 |
20100048535 | Method and dosage regimens for eliminating a chemical substance in blood - A method of reducing the concentration of a chemical or drug substance in the blood plasma that targets the same or similar receptors as the normal neurotransmitters in the central or peripheral nervous system includes titrating an initial peak concentration of the chemical or drug substance in the blood for a predefined dosing period, titrating a lowest concentration level of the chemical or drug substance in the blood immediately before the end of the dosing period, and providing a plurality of subsequent dosing periods where each subsequent dosing period requires administration of a dosing amount of the chemical or drug substance and titrating of the peak concentration and the lowest concentration level to ensure that the lowest concentration level of the chemical or drug substance in the blood plasma for the subsequent dosing period is decreased by not more than five percent of the lowest concentration level of the previous dosing period and where the plurality of dosing periods added together extends the method for seventy days or more. | 2010-02-25 |
20100048536 | Novel Substituted Diaryl Azepine Derivatives as Integrin Ligands - The invention relates to novel compounds which bind to integrin receptors, their use as ligands of integrin receptors, in particular as ligands of the α | 2010-02-25 |
20100048537 | HETEROARYL DERIVATIVES - The present invention relates to a compound represented by formula [1] or a pharmaceutically acceptable salt thereof: | 2010-02-25 |
20100048538 | Therapeutical Uses of Eslicarbazepine - New applications of eslicarbazepine and eslicarbazepine acetate in the treatment of intractable conditions, selected from epilepsy, central and peripheric nervous system disorders, affective disorders, schizoaffective disorders, bipolar disorders, attention disorders, anxiety disorders, neurophatic pain and neuropathic pain-related disorders, sensorimotor disorders, vestibular disorders, and nervous function alterations in degenerative and post-ischemic diseases. Preferably the intractable condition is, at least in part, caused by an overexpression of P-gp or MRP. | 2010-02-25 |
20100048539 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to beat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFRα and PDGFRβ kinases. Formula (I). | 2010-02-25 |
20100048540 | Heterocyclic N-Oxides as Hypoxic Selective Protein Kinase Inhibitors - The invention relates to novel heterocyclic N-oxides which are useful as hypoxic selective cytotoxic agents that mediate and/or inhibit cell proliferation, for example, through the activity of protein kinases. The invention is further related to pharmaceutical compositions containing such compounds and compositions, and to methods of treating cancer as well as other disease states associated with unwanted ahgiogenesis and/or cellular proliferation by administering effective amounts of such compounds. | 2010-02-25 |
20100048541 | SUBSTITUTED LACTAMS AS INHIBITORS OF ABETA PROTEIN PRODUCTION - This invention relates to novel lactams of Formula (I): | 2010-02-25 |
20100048542 | METHODS AND COMPOSITIONS FOR TREATING PRIMARY AND SECONDARY TUMORS OF THE CENTRAL NERVOUS SYSTEM (CNS) - Methods and compositions for the treatment and/or prophylaxis and/or suppression of primary and/or secondary tumors of the central nervous system (brain and spinal cord, eyes) in mammalian subjects are disclosed, wherein an effective dose of a methylol transfer agent such as Taurolidine and/or Taurultam and/or a bioequivalent is administered to a mammalian subject suffering from, or at risk of growth of, tumors of the central nervous system. Furthermore, methods for local application of Taurolidine and/or Taurultam and/or a bioequivalent in solution are disclosed using microdialysis methods, irrigation methods, implantion methods and angiographic methods. | 2010-02-25 |
20100048543 | PYRIMIDINE COMPOUNDS HAVING TIES (TEK) INHIBITORY ACTIVITY - The invention relates to a compound of the Formula I | 2010-02-25 |
20100048544 | PYRROLO (3, 2, 1-IJ) QUINOLINE-4-ONE-DERIVATIVES FOR TREATING TUBERCULOSIS - Tricyclic nitrogen-containing compounds of Formula (I) or pharmaceutically acceptable salts and/or N-oxides thereof: | 2010-02-25 |
20100048545 | Compounds and Compositions for Use in the Prevention and Treatment of Disorders of Fat Metabolism and Obesity - The invention relates to 4-hydroxyisoleucine, isomers, analogs, lactones, salts, and prodrugs thereof, to processes for their preparation, and to pharmaceutical compositions comprising the same. More particularly, the invention relates to the use of those compounds in the prevention and treatment of disorders of fat metabolism and related syndromes. The invention further relates to the use of those compounds in the prevention and treatment of obesity and related syndromes including, but not limited to, the cosmetic treatment of a mammal in order to effect a cosmetically beneficial loss of body weight, and more particularly loss of body fat. | 2010-02-25 |
20100048546 | FUNGICIDAL COMBINATIONS COMPRISING A GLYOXALIC ACID METHYL ESTER-O-METHYLOXIME DERIVATIVES - The present invention relates to a method of combating phytopathogenic disease on crop plants by applying to the crop plants and/or the locus thereof an effective amount of a combination of
| 2010-02-25 |
20100048547 | PI 3-KINASE INHIBITORS AND METHODS OF THEIR USE - Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases, including proliferative diseases, inflammatory and obstructive airways diseases, allergic conditions, autoimmune and cardiovascular diseases. | 2010-02-25 |
20100048548 | IMINO-OXAZOLIDINES AND USE THEREOF - The present invention relates to novel iminooxazolidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular thromboembolic disorders. | 2010-02-25 |
20100048549 | Peptidomimetics selective for the somatostatin receptor subtypes 1 and/or 4 - The invention relates to (hetero)arylsulfonylamino based peptidomimetics of formula (I), wherein A, D, E, J, Q1 R1, R2, R3, p and j are defined as disclosed, or a pharmaceutically acceptable salt or ester thereof. Compounds of formula (I) possess high affinity and selectivity for the somatostatin receptor subtypes sst | 2010-02-25 |
20100048550 | SELECTIVE TR-BETA 1 AGONIST - The present invention relates to novel compounds of general formula (I) which are thyroid receptor ligands and are preferably selective for the thyroid hormone receptor beta(TR-Beta). Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them. | 2010-02-25 |
20100048551 | Tricyclic Compounds Useful as Inhibitors of Kinases - The present invention provides inhibitors of kinases, specifically IκB kinases, JAK1, JAK2, JAK3 and TYK2. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting said kinase activity by administering the compound to a patient in need of treatment for myeloproliferative disorders, cancer or NF-κB-mediated diseases. | 2010-02-25 |
20100048552 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, Bcr-Abl(T315I), ALK, BLK, BMX, BRK, C-kit, c-RAF, CSK, c-SRC, EGFR, Fes, FGFR3, Flt3, Fms, Fyn, IGF-1R, IR, JAK(2), JAK(3), KDR, Lck, NLK, p70S6K, PDGFRα, Ros, SAPK2α, SGK, SIK, Syk, Tie2 and TrkB kinases. | 2010-02-25 |
20100048553 | Spirocyclic Cyclohexane Compounds - Spirocyclic cyclohexane compounds corresponding to formula I | 2010-02-25 |
20100048554 | Spirocyclic Cyclohexane Compounds - Spirocyclic cyclohexane compounds corresponding to formula I | 2010-02-25 |
20100048555 | IMIDAZOTHIAZOLE DERIVATIVES AS MARK INHIBITORS - Compounds of formula (I): are inhibitors of MARK, and hence useful for treatment of disorders involving 10 hyperphosphorylation of tau. | 2010-02-25 |
20100048556 | QUINOXALINE DERIVATIVES - The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I) | 2010-02-25 |
20100048557 | Triazolopyridine JAK Inhibitor Compounds and Methods - A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R | 2010-02-25 |
20100048558 | THIENOPYRIDINES - The invention relates to novel thienopyridine derivatives of formula (I), wherein R1, R2, R3, R4 and Y have the meaning cited in claim | 2010-02-25 |
20100048559 | PYRIDO(3,2-d)PYRIDMIDINES USEFUL FOR TREATING VIRAL INFECTIONS - This invention provides pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (I), wherein: R | 2010-02-25 |
20100048560 | PYRAZOLO PYRIDINE DERIVATIVES AS NADPH OXIDASE INHIBITORS - The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase). | 2010-02-25 |
20100048561 | QUINAZOLINES FOR PDK1 INHIBITION - The invention provides quinazoline compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions. | 2010-02-25 |
20100048562 | ORGANIC COMPOUNDS - The present invention provides a compound of formula I: | 2010-02-25 |
20100048563 | SUBSTITUTED INDOLEPYRIDINIUM AS ANTI-INFECTIVE COMPOUNDS - The present invention concerns the compounds of formula (I) | 2010-02-25 |
20100048564 | FUSED BICYCLIC HETEROARYL DERIVATIVE - The present invention relates to a novel fused bicyclic heteroaryl derivative or a pharmacologically acceptable salt thereof, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) γ. | 2010-02-25 |
20100048565 | BENZIMIDAZOLE DERIVATIVES - Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related conditions or disorders. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, immune response regulation and cell proliferation. The subject compounds are 2-amino-imidazole derivatives. | 2010-02-25 |
20100048566 | ANTIBACTERIAL QUINOLINE DERIVATIVES - The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): | 2010-02-25 |
20100048567 | Inhibitors of syk and JAK protein kinases - The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 2010-02-25 |
20100048568 | PYRIMIDINE HYDRAZIDE COMPOUNDS AS PGDS INHIBITORS - This invention is directed to a compound of formula (I): | 2010-02-25 |
20100048569 | DIAZOLE DERIVATIVES - The present invention relates to diazole derivatives of the general formula | 2010-02-25 |
20100048570 | THIAZOLIDINE DERIVATIVES AND METHODS FOR THE PREPARATION THEREOF - The present invention relates to novel 2-carbonyl-3-acyl-1,3-thiazolidines having a β-amino group on the acyl chain, in free, prodrug form or pharmaceutically acceptable salt thereof, including their enantiomers, diastereomers and racemates, as efficient inhibitors against DPP-IV. The invention further relates to the pharmaceutical compositions comprising the disclosed compounds. The present invention also relates to methods for preparing the disclosed compounds and for treating DPP-IV-mediated diseases. | 2010-02-25 |
20100048571 | Organic Compounds - The present disclosure relates to XIAP inhibitor compound of the formula I: | 2010-02-25 |
20100048572 | NAPHTHALENONE COMPOUNDS EXHIBITING PROLYL HYDROXYLASE INHIBITORY ACTIVITY, COMPOSITIONS, AND USES THEREOF - Compounds of Formula I and Formula II are useful as inhibitors of HIF prolyl hydroxylases. Compounds of Formula I and Formula II have the following structures: | 2010-02-25 |
20100048573 | Methods of Inhibiting Bacterial Virulence and Compounds Relating Thereto - The present invention relates to compounds and methods for the treatment of bacterial infections. Because their mechanism of action does not involve killing of bacteria or inhibiting their growth, the potential for these compounds to induce drug resistance in bacteria is minimized. Through inhibiting bacterial virulence, the present invention provides a novel means of treating bacterial infections. | 2010-02-25 |
20100048574 | NOVEL HETEROCYCLIC NF-kB INHIBITORS - The present invention relates to compounds of the general formula (II): | 2010-02-25 |
20100048575 | NOVEL TETRACYCLIC INHIBITORS OF CYSTEINE PROTEASES, THE PHARMACEUTICAL COMPOSITIONS THEREOF AND THEIR THERAPEUTIC APPLICATIONS - The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use: Formula (I) wherein R3, R4, R5, R6, Y, Het1, T, U, V, W, X, Ru, Rv and Rw are as defined in claim | 2010-02-25 |
20100048576 | PYRIDOPYRAZINES AND DERIVATIVES THEREOF AS ALK AND c-MET INHIBITORS - The present invention provides a compound of Formula I | 2010-02-25 |
20100048577 | Method for treating benign prostate hyperplasia using resveratrol - The invention relates to the discovery that resveratrol, and substituted forms of resveratrol, are effective in alleviating benign prostate hyperplasia. Formulations containing the resveratrol or resveratrol derivative, lack omega-3 fatty acids, and also contain no other compounds which activate SIRT1 and PGCα. | 2010-02-25 |
20100048578 | HYDRAZIDE COMPOUND AND HARMFUL ARTHROPOD-CONTROLLING AGENT CONTAINING THE SAME - Disclosed is a hydrazine compound represented by the formula (1) below, which has an excellent control activity against a harmful arthropod. (1) (In the formula, R | 2010-02-25 |
20100048579 | PYRIDAZINE-, PYRIDINE- AND PYRANE-DERIVATIVES AS GPBAR1 AGONISTS - A compound of formula (I) wherein the substituents have various meanings, optionally in salt and/or solvate form, and their use as pharmaceuticals. | 2010-02-25 |
20100048580 | HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES - The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases | 2010-02-25 |
20100048581 | THIAZOLYL COMPOUNDS USEFUL AS KINASE INHIBITORS - The invention provides compounds of formula I [INSERT CHEMICAL STRUCTURE HERE] (I) and pharmaceutically acceptable salts thereof. The formula I thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease. | 2010-02-25 |
20100048582 | HETEROCYCLIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5HT6 RECEPTOR - The invention relates to compounds of the formula (I) | 2010-02-25 |
20100048583 | Novel Heterocyclic NF-kB Inhibitors - The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, | 2010-02-25 |
20100048584 | PYRIDYL DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS - Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): | 2010-02-25 |
20100048585 | QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS - Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide form thereof, wherein R | 2010-02-25 |
20100048586 | MULTIFUNCTIONAL BIOACTIVE COMPOUNDS - The present invention discloses multifunctional bioactive compounds of formula (I) constituted of an immunoregulatory portion linked to a stabilizer moiety and pharmaceutical compositions thereof useful in the treatment of immune disorders and hemopoietic disorders such as immune cytopema, multiple myeloma, chronic lymphoid leucosis, lymphocytic lymphomas, lymphosarcomas. | 2010-02-25 |
20100048587 | CYSTEINE AND CYSTINE BIOISOSTERES TO TREAT SCHIZOPHRENIA AND REDUCE DRUG CRAVINGS - The present invention provides cysteine and cystine bioisosteres for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing such bioisosteres and methods of using the bioisosteres for treatment of schizophrenia and drug addiction. | 2010-02-25 |
20100048588 | AMINOCARBONYL-DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I) | 2010-02-25 |
20100048589 | Cold Menthol Receptor Antagonists - 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: | 2010-02-25 |
20100048590 | N-(3-AMINO-2-HYDROXY-PROPYL) SUBSTITUTED ALKYLAMIDE COMPOUNDS - Disclosed are compounds of the formula (I): | 2010-02-25 |
20100048591 | CHEMICAL COMPOUNDS AND PROCESSES - The present invention relates generally to chemical compounds and methods for their use and preparation. In particular, the invention relates to chemical compounds which may possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds. | 2010-02-25 |
20100048592 | Use of sodium channel blockers for the management of musculoskeletal pain - The invention provides methods for managing musculoskeletal pain. The compounds useful in the methods of the invention are blockers of sodium ion channels, and in particular compounds that bind to the SS1 or SS2 extracellular mouth of the a-subunit thereof. Particularly useful compounds are saxitoxin and its derivatives and analogues and tetrodotoxin and its derivatives and analogues. | 2010-02-25 |
20100048593 | DEAZAFLAVIN COMPOUNDS AND METHODS OF USE THEREOF - The present invention features 5-deazaflavin compounds, pharmaceutical compositions of 5-deazaflavin compounds and methods of treating a patient suffering from cancer, the method comprising administering to a patient one or more 5-deazaflavin compounds of the invention. | 2010-02-25 |
20100048594 | USE OF CYTOHESIN INHIBITORS FOR CHEMICALLY INDUCING LONGEVITY - The invention relates to compounds selected from among the group comprising general formulas (1), (2), (3), and/or (4) and/or the enantiomers, diastereomers, and derivatives thereof, and the pharmaceutically acceptable salts thereof for producing a medicament used for therapeutically and/or preventively treating disease and pathological conditions linked to regulation of the insulin and/or insulin-like growth factor (IGF) signalling pathway and/or for chemically inducing longevity. | 2010-02-25 |
20100048595 | USE OF ARCHAEA TO MODULATE THE NUTRIENT HARVESTING FUNCTIONS OF THE GASTROINTESTINAL MICROBIOTA - The invention generally relates to the use of archaea to modulate nutrient harvesting in a subject. In particular, the invention provides methods that use archaea to modulate the nutrient harvesting functions of the microbiota in the subject's gastrointestinal tract. | 2010-02-25 |
20100048596 | Indole Derivatives as Antitumoral Compounds - Antitumoural compounds of general formula (I); wherein Ar is an heterocyclic group of formula (a) and R | 2010-02-25 |
20100048597 | Organic Compounds and Their Uses - The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases. | 2010-02-25 |
20100048598 | TOPICAL COMPOSITIONS COMPRISING 5-ALPHA REDUCTASE INHIBITORS - The present invention relates to topical compositions comprising 5α-reductase inhibitors. The present invention also includes processes for preparation of such topical compositions and methods of using them. | 2010-02-25 |
20100048599 | Compounds As Kinase Inhibitors - The present invention relates to compounds of Formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with angiogenesis, such as cancers associated with protein tyrosine kinases, to their use as medicaments for use in the production of inhibition of tyrosine kinases reducing effects in warm-blooded animals such as humans. | 2010-02-25 |
20100048600 | NOVEL BENZIMIDAZOLE DERIVATIVES - The present invention relates to a compound of the formula (I): | 2010-02-25 |
20100048601 | HYDROCHLORIDE SALTS OF 8-[-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one AND PREPARATION PROCESS THEREFOR - Disclosed are hydrochloride and tosylate crystalline salt forms of (5S,8S)-8-S[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I and methods of preparing the same. | 2010-02-25 |
20100048603 | BROAD-SPECTRUM ANTI-CANCER TREATMENT BASED ON IMINOCAMPTOTHECIN DERIVATIVES - A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of a cancer or tumor pathology selected from the group consisting of head and neck carcinoma, pancreas carcinoma, melanoma, bladder carcinoma, mesothelioma and epidermoid skin carcinoma. | 2010-02-25 |
20100048604 | Ligands for Aldoketoreductases - The present invention relates to compounds useful for detecting the activity of human aldoketoreductase 1Cs, compounds useful for competitively inhibiting human aldoketoreductase 1Cs and compounds useful for treating human aldoketoreductase 1C-related cancers, as well as pharmaceutical compositions and methods of manufacture thereof. | 2010-02-25 |
20100048606 | 10-Substituted Cytisine Derivatives and Methods of Use Thereof - The present invention relates to substituted cytisine compounds that are useful in treating diseases impacted by a nicotinic ACh receptor. One aspect of the invention relates to 10-substituted cytisine compounds. In certain instances, the cytisine is substituted in the 10-position by an alkyl, aryl or aralkyl group. The present invention also relates to a pharmaceutical composition comprises the substituted cytisine compound or the 10-substituted cytisine compound. The invention also relates to a method of modulation a nicotinic ACh receptor in a mammal, comprising the step of administering to a mammal in need thereof a therapeutically effective amount of a substituted cytisine. In certain instances, the substituted cytisine is a 10-substituted cytisine. Another aspect of the present invention relates a method of treating a disease impacted by a nicotinic ACh receptor, comprising the step of administering to a mammal in need thereof a therapeutically effective amount of a substituted cytisine. In certain instances, the substituted cytisine is a 10-substituted cytisine. | 2010-02-25 |
20100048607 | FORMULATIONS COMPRISING PALONOSETRON - Pharmaceutical compositions comprising palonosetron and its pharmaceutically acceptable salts, in the form of a ready-to-use solution or a lyophilized form. Specific embodiments of the invention relate to stable pharmaceutical formulations of palonosetron and its pharmaceutically acceptable salts, wherein the formulation does not comprise a chelating agent or an antioxidant. | 2010-02-25 |
20100048608 | Histone Deacetylase Inhibitors for the Treatment of Ocular Neovascular or Edematous Disorders and Diseases - Ophthalmic compositions containing HDAC inhibitors and their use for treating ocular neovascular or edematous diseases and disorders are disclosed. | 2010-02-25 |
20100048609 | PHARMACEUTICAL DOSAGE FORMS FOR (+)-1,4-DIHYDRO-7-[(3S,4S)-3-METHOXY-4-(METHYLAMINO)-1-PYRROLIDINYL]-4-OX- O-1-(2-THIAZOLYL)-1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACID - Provided herein are light protective pharmaceutical packages for enantiomerically pme (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid. In certain embodiments, the pharmaceutical packages comprise a glass vial containing SNS-595 drug product within a secondary container. | 2010-02-25 |
20100048610 | CARBINOL DERIVATIVES HAVING CYCLIC LINKER - [Object] To provide a novel LXRβ agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. | 2010-02-25 |
20100048611 | TETRAHYDROPYRROLOPYRIDINE, TETRAHYDROPYRAZOLOPYRIDINE, TETRAHYDRO-IMIDAZOPYRIDINE AND TETRAHYDROTRIAZOLOPYRIDINE DERIVATIVES AND USE THEREOF - The invention relates to novel tetrahydropyrrolopyridine, tetrahydropyrazolopyridine, tetrahydroimidazopyridine and tetrahydrotriazolopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders | 2010-02-25 |
20100048612 | BICYCLIC HETEROCYCLES AS CANNABINOID-1 RECEPTOR MODULATORS - The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formula: | 2010-02-25 |
20100048613 | POLYMORPHIC FORM OF GRANISETRON HYDROCHLORIDE AND METHODS OF MAKING THE SAME - Crystalline granisetron hydrochloride characterized by a powder x-ray diffraction pattern with peaks at about 14.3, 20.4, and 23.0±0.2 degrees two-theta and process of making the same are disclosed. | 2010-02-25 |
20100048614 | THERAPEUTIC USES OF BICYCLIC LIGANDS OF SIGMA 2 RECEPTOR - A series of N-substituted 9-azabicyclo[3.3.1]nonan-3α-yl phenylcarbamate analogs are disclosed, as well as methods of their preparation. Their affinities for sigma (σ1 and σ2) receptors are described. Two new compounds, N-(9-(4-aminobutyl)-9-azabicyclo[3.3.1]nonan-3α-yl)-N′-(2-methoxy-5-methylphenyl)carbamate and N-(9-(6-aminohexyl)-9-azabicyclo[3.3.1]nonan-3α-yl)-N′-(2-methoxy-5-methylphenyl)carbamate, are shown to have a high affinity and selectivity for σ2 versus σ1 receptors. Among the disclosed compounds are biotinylated and fluorescent analogs. These compounds can serve as probes to the σ2 receptor. In addition, some disclosed compounds can induce apoptotic cell death by both caspase-dependent and caspase-independent mechanisms, and are effective for treatment of tumors. The compounds can be used as chemotherapeutics or chemosensitizers in the treatment of a wide variety of solid tumors. | 2010-02-25 |
20100048615 | COMBINATIONS COMPRISING ANTIMUSCARINIC AGENTS AND PDE4 INHIBITORS - Combinations comprising (a) a PDE4 inhibitor and (b) an antagonist of M3 muscarinic receptors which is 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid are useful, e.g., for the treatment of respiratory disease, e.g., asthma or chronic obstructive pulmonary diseases. | 2010-02-25 |
20100048616 | COMBINATIONS COMPRISING ANTIMUSCARINIC AGENTS AND PDE4 INHIBITORS - A combination which comprises (a) a PDE4 inhibitor and (b) an antagonist of M3 muscarinic receptors which is (3R)-1-phenethyl-3-(9H-xanthene-9carbonyloxy)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid. | 2010-02-25 |
20100048617 | COMPOUNDS - The present invention relates to substituted 3-Aminopyrazole compounds of formula (I) | 2010-02-25 |
20100048618 | Derivatives of 8-epiblechnic Acid and their Effects on Down-Regulation of Endothelin (ETA) receptor mRNA - The present application discloses derivatives of 8-epiblechnic acid and use thereof in treating a disease related to endothelin receptor A or endothelin-1 (ET-1) over-expression, such as hypertension, cancer, atherosclerosis, and myocardial infarction. | 2010-02-25 |
20100048619 | Cold Menthol Receptor Antagonists - 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: | 2010-02-25 |
20100048620 | COMPOSITION FOR TREATMENT OF UNDIFFERENTIATED GASTRIC CANCER - Disclosed are: a therapeutic agent, a kit and a treatment method for undifferentiated gastric cancer; and a pharmaceutical composition, a kit and a treatment method which are more effective on a living organism having at least one cell selected from the group consisting of a cell overexpressing FGFR2 and a cell expressing a mutant FGFR2. A combination of a FGFR2 inhibitor and a therapeutic substance for gastric cancer is more effective on undifferentiated gastric cancer. The combination of a FGFR2 inhibitor and a therapeutic substance for gastric cancer is more effective on a living organism having at least one cell selected from the group consisting of a cell overexpressing FGFR2 and a cell expressing a mutant FGFR2. | 2010-02-25 |