| 10th week of 2009 patent applcation highlights part 63 |
| Patent application number | Title | Published |
|---|
| 20090062198 | Maurotoxin, PI1 and HSTX1 derivatives - Derivatives of Maurotoxin (MTX) in which the native disulfide bridge pattern (Cys3-Cys24, Cys9-Cys29, Cys19, Cys31-Cys34) has been disrupted are useful for the treatment of pathologies associated with dysfunctioning and/or activation of Ca | 2009-03-05 |
| 20090062199 | Nogo Receptor Polypeptides and Polypeptide Fragments and Uses Thereof - Nogo receptor 1 (NgR1) is a leucine rich repeat protein that forms part of a signaling complex that modulates axon regeneration. Previous studies have shown that the entire LRR region of Nogo receptor-1, including the C-terminal cap of LRR, LRRCT, is needed for ligand binding, and that the adjacent CT stalk of the Nogo receptor-1 contributes to interaction with its co-receptors. The present invention is directed to the use of certain Nogo receptor-1 and Nogo receptor-2 polypeptides and polypeptide fragments for promoting neurite outgrowth, neuronal survival, and axonal regeneration in CNS neurons. The invention features molecules and methods useful for inhibiting neurite outgrowth inhibition, promoting neuronal survival, and/or promoting axonal regeneration in CNS neurons. | 2009-03-05 |
| 20090062200 | VEGF-Binding Fusion Proteins and Therapeutic Uses Thereof - Nucleic acid molecules encoding fusion proteins which bind and inhibit vascular endothelial growth factor (VEGF). The VEGF-binding fusion proteins are therapeutically useful for treating VEGF-associated conditions and diseases, and are specifically designed for local administration to specific organs, tissues, and/or cells. | 2009-03-05 |
| 20090062201 | INTEGRIN BINDING MOTIF CONTAINING PEPTIDES AND METHODS OF TREATING SKELETAL DISEASES - Peptide sequences comprising 10 to 50 amino acids are disclosed. The sequences are characterized by containing at least one of an integrin binding motif such as an RGD sequence, a glycosaminoglycan binding motif, and a calcium binding motif, and the remainder of amino acids contiguous with the RGD sequence in matrix extracellular phosphoglycoprotein. The sequences may be formulated for injection or dispersed in toothpaste or a mouthwash or gum patch and administered to enhance bone/tooth growth and/or reduce excessive urinary phosphate loss from the body. | 2009-03-05 |
| 20090062202 | METHODS OF TREATING AND PREVENTING PRESSURE ULCERS WITH INTRADERMAL AND TRANSDERMAL DELIVERY OF CALCITONIN GENE-RELATED PEPTIDE (CGRP) - A method of treating ischemic skin pressure ulcers and helping such ulcers heal has the steps of a. debriding the ulcer as necessary to produce a clean, largely uncontaminated surface; and b. applying calcitonin gene-related peptide (CGRP) intradermally or transdermally to the periphery of the ulcer, the CGRP being administered at a dose below a vascular-affecting threshold, thereby enhancing ulcer healing with the anti-ischemic and tissue-healing properties of the CGRP. Also provided is a method of preventing, pressure ulcers of the skin in individuals prone thereto with the steps of a. providing a container with contents comprising CGRP and a vehicle, the CGRP container further comprising connectors for connection to an iontophoresis controller; b. connecting the CGRP container to the iontophoresis controller; c. applying the CGRP container to a body location known to be prone to pressure ulcers; and d. performing an electronic program for forcing CGRP through the skin. | 2009-03-05 |
| 20090062203 | DIPEPTIDYL PEPTIDASE IV INHIBITORS FOR THE TREATMENT OF SCHIZOPHRENIA AND DEPRESSION - A method for therapeutically treating an animal, including a human, for psychosomatic, depressive and neuropsychiatric diseases, such as anxiety, depression, insomnia, schizophrenia, epilepsy, spasm and chronic pain. Administration of a suitable DP IV inhibitor causes the reduction of activity in the enzyme dipeptidyl peptidase (DP IV or CD 26) or of DP IV-like enzyme activity in the brain of mammals and leads as a causal consequence to a reduced degradation of the neuropeptide Y (NPY) and similar substrates by DP IV and DP IV-like enzymes. Such treatment will result in a reduction or delay in the decrease of the concentration of functionally active neuronal NPY (1-36). As a consequence of the resulting enhanced stability of the endogenous NPY (1-36) caused by the inhibition of DP IV activity, NPY activity is prolonged thereby resulting among other things in functionally active NPY Y1 receptor activity thereby facilitating antidepressive, anxiolytic, analgesic, antihypertension and other neurological effects. | 2009-03-05 |
| 20090062204 | COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING GASTROENTERIC DISEASES - A model system to study extracellular enteric bacterial pathogen (e.g., | 2009-03-05 |
| 20090062205 | Reconstitution Medium For Protein and Peptide Formulations - Compositions useful for reconstitution of concentrated formulations containing protein/peptide pharmaceuticals are provided. The composition generally includes one or more lipids, as well as one or more alcohols that promote and stabilize the formation of (a) lipid molecular assemblies with greater protein encapsulation; (b) protein-lipid complexes and (c) protein and lipid solutions. The reconstitution medium improves the protein-lipid association that in turn alters the pharmaceutical properties. | 2009-03-05 |
| 20090062206 | Urodilatin Cancer Treatment - Urodilatin, a peptide formed in the kidney, has significant anticancer effects eliminating two-thirds of cancer cells within 24 hours. | 2009-03-05 |
| 20090062207 | Methods and compositions for the treatment of gastrointestinal disorders - The present invention features compositions and related methods for treating IBS and other gastrointestinal disorders and conditions (e.g., gastrointestinal motility disorders, functional gastrointestinal disorders, gastroesophageal reflux disease (GERD), duodenogastric reflux, Crohn's disease, ulcerative colitis, Inflammatory bowel disease, functional heartburn, dyspepsia (including functional dyspepsia or nonulcer dyspepsia), gastroparesis, chronic intestinal pseudo-obstruction (or colonic pseudo-obstruction), and disorders and conditions associated with constipation, e.g., constipation associated with use of opiate pain killers, post-surgical constipation (post-operative ileus), and constipation associated with neuropathic disorders as well as other conditions and disorders using peptides and other agents that activate the guanylate cyclase C (GC-C) receptor. | 2009-03-05 |
| 20090062208 | Methods for maintaining blood-brain barrier integrity in hypertensive subjects using a delta-PKC inhibitor - Methods for maintaining the integrity of the blood-brain barrier are described. Compounds that act to inhibit the action of the delta isozyme of protein kinase C (PKC) to prevent disruption of the blood-brain barrier in hypertensive subjects are described, to, in one embodiment, decrease the likelihood of hypertension-induced stroke or hypertension-induced encephalopathy. | 2009-03-05 |
| 20090062209 | METHODS OF USE OF EPSILON INHIBITOR COMPOUNDS FOR THE ATTENUATION OF PAIN - The disclosure herein relates to modified εPKC inhibitory peptides, methods of generating such peptides, and method for using εPKC inhibitory peptides for the treatment of pain. | 2009-03-05 |
| 20090062210 | Methods for promoting erythropoiesis - The present invention provides methods, compounds, pharmaceutical compositions, and kits for the augmentation of erythropoiesis by potentiating erythropoietin-induced differentiation with angiotensinogen, angiotensin I (AI), AI analogues, AI fragments and analogues thereof, angiotensin II analogues, AII fragments or analogues thereof or AII AT | 2009-03-05 |
| 20090062211 | CONOPEPTIDES AND METHODS OF USE - Isolation, synthesis and therapeutic use of conotoxin and conophan compounds and related compositions including a new class of conopeptides including the modified amino acid D-γ-hydro-oxyvalinie (D-Hyv=V*) are described herein. These isolated peptides are the first known example of a naturally occurring polypeptide chain containing D-Hyv. The active peptides, termed γ-Hydroxyconophans are heavily hydroxylated small peptides. These peptides contain a definitive structural motif which is a double modification of the polypeptide chain (γ-D-OH-Hyv-Trp). | 2009-03-05 |
| 20090062212 | Peptide analogs that are potent and selective for human neurotensin preceptor subtype 2 - Neurotensin analogs selective for neurotensin receptor subtype 2 are described. These include hexapeptides (NT(8-13)) and pentapeptides (NT(9-13)) having a D-3,1-naphthyl-alanine, D-3,2-naphthyl-alanine, an alanine derivative such as cyclohexylalanine, or 1,2,3,4-tetrahydroisoquinoline at position 11. Methods of treating pain by administering these neurotensin analogs are also described. | 2009-03-05 |
| 20090062213 | Small Molecule Inhibitors of PDZ Interactions - The present invention relates to compositions for use in the modulation of PDZ domain interactions with cognate ligands. Methods of assessing and characterizing PDZ domain interactions from various polypeptides also are provided. | 2009-03-05 |
| 20090062214 | Left-Side Glucose Lipid a Analogue - A compound having excellent macrophage activity inhibitory action, which is represented by the general following formula: | 2009-03-05 |
| 20090062215 | APPLICATION OF D-PSICOSE TO SUPPRESSION OF ABNORMAL CIRCADIAN INCREASE IN BLOOD GLUCOSE LEVEL - A novel use of D-psicose (for suppressing the abnormal intra-day increase of blood glucose level) is provided. A composition containing D-psicose as the active component and for use in suppressing the abnormal intra-day increase of plasma glucose concentration. The composition is a composition in blend with D-psicose and/or a derivative thereof. The composition is in a form selected from sweeteners, seasonings, food additives, food materials, food and drink products, health food and drink products, pharmaceutical products, and feeds and blended with D-psicose, and/or a derivative thereof as the active component, for use in preventing and therapeutically treating diseases requiring the saving of insufficient insulin, the amelioration of insulin sensitivity and the amelioration of hyperglycemia, and/or diseases of which the symptoms can be ameliorated via the suppression of the abnormal intra-day increase of plasma glucose concentration or of which the onset can be prevented via the suppression thereof, such as diabetes mellitus, occult diabetic states, obesity, hyperglycemia, and/or arteriosclerosis. A method for using D-psicose in suppressing the abnormal intra-day increase of plasma glucose concentration, comprising giving D-psicose at given times to suppress the abnormal increase of plasma glucose concentration throughout the day. | 2009-03-05 |
| 20090062216 | BUTANOL EXTRACT OF BIDENS PILOSA - A method of treating a Th1-mediated disorder includes administering to a subject in need of the treatment an effective amount of a compound of the formula I: | 2009-03-05 |
| 20090062217 | Promoter For The Production Of Hyaluronic Acid Containing Ginsenoside Compound K - There are provided a promoter containing ginsenoside compound K for the production of hyaluronic acid, and more particularly, a new efficacy of 20-O-β-D-glucopyranosyl-20(S)-protopanaxadiol (compound K), a chief metabolite of ginseng saponin, to increase the expression of hyaluronic acid synthase gene in human cell and thereby to promote the production of hyaluronic acid, and an anti-aging agent containing the promoter for the production of hyaluronic acid as an effective ingredient. | 2009-03-05 |
| 20090062218 | MACROLONE COMPOUNDS - A compound of formula (I) | 2009-03-05 |
| 20090062219 | DRUGS FOR THE TREATMENT AND/OR PROPHYLAXIS OF GASTROPARESIS SYMPTOM - The present invention provides a therapeutic and/or preventive agent against gastroparesis symptom which is appropriate for continuous medication and which comprises a compound represented by formula (1): | 2009-03-05 |
| 20090062220 | DEUTERIUM-ENRICHED AZITHROMYCIN - The present application describes deuterium-enriched azithromycin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 2009-03-05 |
| 20090062221 | Azithromycin for treatment of skin disorders - Azithromycin has increased efficacy in treating acne and other skin conditions when administered systemically at low doses, below those previously known to produce a clinical antibiotic effect. | 2009-03-05 |
| 20090062222 | Methods for Sensitizing Cancer Cells to Inhibitors - The present invention is based on the discovery that inactivation of the heat shock response in cancer cells significantly enhances their sensitivity to proteasome and Hsp90 inhibitors. The inventors have discovered novel compounds which exhibit low toxicity, inhibit the heat shock protein response and sensitize cancer cells to anti-cancer therapies. In general, the heat shock protein inhibitors of the present invention share a common structure, namely a 2H-benzo[a]quinolizine tricyclic ring. Also encompassed are methods for a high throughput screen to identify heat shock inhibitors that sensitize cancer cells to anti-cancer therapies. | 2009-03-05 |
| 20090062223 | AMINO TRICYCLIC-NUCLEOSIDE COMPOUNDS, COMPOSITIONS, AND METHODS OF USE - Provided are compounds of Formula (I) or a pharmaceutically acceptable salt or solvate thereof. The compounds and compositions are useful for treating viral infections caused by the Flaviviridae family of viruses. | 2009-03-05 |
| 20090062224 | Therapeutic use of cpg oligodeoxynucleotide for skin disease - Disclosed is the therapeutic use of CpG oligodeoxynucleotides for skin diseases. The CpG oligodeoxynucleotides (CpG ODNs) of the present invention show excellent immunoactive effects against skin diseases in both cases of CpG ODNs with a phosphorothioate backbone and CpG ODNs with a phosphodiester backbone. | 2009-03-05 |
| 20090062225 | COMPOSITIONS AND METHODS FOR INHIBITING EXPRESSION OF A GENE FROM THE JC VIRUS - The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of a gene from the JC Virus (JC virus genome), comprising an antisense strand having a nucleotide sequence which is less that 30 nucleotides in length, generally 19-25 nucleotides in length, and which is substantially complementary to at least a part of a gene from the JC Virus. The invention also relates to a pharmaceutical composition comprising the dsRNA together with a pharmaceutically acceptable carrier; methods for treating diseases caused by JC virus expression and the expression of a gene from the JC Virus using the pharmaceutical composition; and methods for inhibiting the expression of a gene from the JC Virus in a cell. | 2009-03-05 |
| 20090062226 | Method and Compositions for Inhibiting MAGE Protein Interaction With KAP-1 - Method for inhibiting tumor cell formation or tumor cell growth, and method for inducing apoptosis in sperms, the method comprising administering to a patient in need thereof an antagonist that inhibits the binding of MAGE protein to KAP-1, thereby inhibiting MAGE gene function. Also disclosed are pharmaceutical compositions comprising the same, and method for screening a substance that inhibits MAGE protein binding to KAP-1. | 2009-03-05 |
| 20090062227 | METHODS AND COMPOSITIONS FOR INDUCING APOPTOSIS BY STIMULATING ER STRESS - The present invention provides a method for inducing apoptosis in selected cells by aggravating ER-stress. The aggravation of ER-stress is achieved in a specific manner by inhibiting SERCA (sarcoplasmic/endoplasmic reticulum calcium ATPase), leading to elevated level of cytoplasmic calcium concentration, yet without inhibiting the activity of COX-2 (cyclooxygenase-2) or triggering the release of histamine. Induction of apoptosis may be enhanced by first inducing or further aggravating ER-stress through inhibition of proteasome or proteases. Also provided are compounds and compositions useful as ER-stress aggravating agents, methods for screening, selecting, identifying and designing the same and methods for treating diseased conditions by inducing apoptosis through specific and selective aggravation of ER-stress. | 2009-03-05 |
| 20090062228 | piRNA and uses related thereto - The invention relates to small single stranded RNAs and analogs thereof (collectively “piRNA” herein), compositions comprising such piRNAs, and their uses in regulating target gene expression or as markers for certain disease states. | 2009-03-05 |
| 20090062229 | METHOD AND COMPOSITION FOR REDUCING THE EXPRESSION OF ROCK-II - Methods and compositions for reducing the expression of Rho-associated, coiled-coil containing protein kinase 2 (ROCK-II) are provided. | 2009-03-05 |
| 20090062230 | NOVEL CATIONIC 17 ALPHA-SUBSTITUTED-ESTRADIOL DERIVATIVES USEFUL AS ANTI-CANCER AGENT - The present invention provides a novel series of cationic, lipid-based, 17α-substituted-estradiol derivatives. The present invention further provides a process for the preparation of a novel series of 17α-substituted-estradiol derivatives. The invention also provides information about highly selective anticancer activities of these molecules in estrogen responsive cell lines. The compound elicits high level of toxicity to gynecological cancer cell lines such as MCF-7, T47D (estrogen receptor positive cell lines), MDA-MB-468 (estrogen receptor knock-out cell line), Hela (cervical cancer). The present class of cationic lipid-based, estradiol derivatives is likely to find specific use in developing target specifically deliverable anticancer drugs for the treatment of gynecological cancers that are most prevalent in women population irrespective of ethnicity. | 2009-03-05 |
| 20090062231 | Appetite Suppressant Composition and Method of Appetite Suppression - The present invention provides an appetite suppressant composition including alginate, hydroxycitric acid, and piperine. The present invention also provides an appetite suppressant composition including alginate, hydroxycitric acid, and garcinol. The present invention further provides a method of suppressing appetite utilizing an appetite suppressant composition for creating an immediate and sustained feeling of satiety; reducing total cholesterol, glucose, insulin, and triglyceride levels; and preventing gastric reflux. | 2009-03-05 |
| 20090062232 | High-Purity Xylooligosaccharide Compositions - To provide a high-purity xylooligosaccharide composition while preventing the formation of UV-absorbing substances and coloring matters. | 2009-03-05 |
| 20090062233 | Modified starch material of biocompatible hemostasis - A modified starch material for biocompatible hemostasis, biocompatible adhesion prevention, tissue healing promotion, absorbable surgical wound sealing and tissue bonding, when applied as a biocompatible modified starch to the tissue of animals. The modified starch material produces hemostasis, reduces bleeding of the wound, extravasation of blood and tissue exudation, preserves the wound surface or the wound in relative wetness or dryness, inhibits the growth of bacteria and inflammatory response, minimizes tissue inflammation, and relieves patient pain. Any excess modified starch not involved in hemostatic activity is readily dissolved and rinsed away through saline irrigation during operation. After treatment of surgical wounds, combat wounds, trauma and emergency wounds, the modified starch hemostatic material is rapidly absorbed by the body without the complications associated with gauze and bandage removal. | 2009-03-05 |
| 20090062234 | SUBSTITUTED ORGANOPOLYSILOXANES AND USE THEREOF - The invention relates to new compounds of Formula (1): wherein Q is selected from CXYR′ and RC(Z) wherein Z is selected from oxygen, hydrogen, OH, NR | 2009-03-05 |
| 20090062235 | Inhibitors of Dipeptidylpeptidase IV - The present invention relates to inhibitors of post-proline cleaving enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention are improved over those in the prior art by selection of particular classes of sidechains in the P1 and/or P2 position of the inhibitor that contain a carboxylic acid moiety. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease. | 2009-03-05 |
| 20090062236 | Programmable genotoxic agents and uses therefor - The compositions and methods disclosed herein provide heterobifunctional programmable genotoxic compounds that can be designed to kill selected cells present in a heterogenous cell population. The present compounds comprise a first agent that inflicts damage on cellular DNA, and a second agent that attracts a macromolecular cell component such as a protein, which in turn shields genomic lesions from repair. Unrepaired lesions therefore persist in the cellular genome and contribute to the death of selected cells. In contrast, lesions formed in nonselected cells, which lack the cell component, are unshielded and thus are repaired. As a result, compounds described herein are less toxic to nonselected cells. Compounds of this invention can be designed to cause the selective killing of transformed cells, viral-infected cells and the like. | 2009-03-05 |
| 20090062237 | EVALUATING IMMUNE COMPETENCE - This document relates to methods and materials involved in evaluating immune competence in a subject. For example, methods and materials for evaluating immune competence in a subject to BK virus (BKV) are provided. Also provided are isolated peptides, compositions, and methods useful for evaluating whether or not a subject is BKV immunocompetent. Also provided are methods for treating BK virus nephropathy in a subject that is BKV immune incompetent. | 2009-03-05 |
| 20090062238 | METHOD FOR TREATMENT OF NEUROPATHIC PAIN - Compounds and methods useful for preventing and treating pain, e.g., neuropathic pain, in a subject in need thereof are provided. The compounds can be “S1P modulating” agents that are capable of inducing a detectable change in S1P receptor activity. | 2009-03-05 |
| 20090062239 | THROMBIN RECEPTOR ANTAGONISTS AS PROPHYLAXIS TO COMPLICATIONS FROM CARDIOPULMONARY SURGERY - Disclosed herein are methods of preventing, inhibiting, or ameliorating complications associated with cardiopulmonary bypass surgery by the use of a thrombin receptor antagonist compound. Among the thrombin receptor antagonist compounds useful in these methods are those of Formulas I and II, described herein. Examples of such thrombin receptor antagonists include: | 2009-03-05 |
| 20090062240 | Pharmaceutical combinations containing an inhibitor of platelet aggregation and a fibrate - The present invention relates to a novel pharmaceutical combination, containing an inhibitor of platelet aggregation and a fÊbrate, where the inhibitor of platelet aggregation is preferably either aspirin or clopidogreL Such a pharmaceutical combination of an inhibitor of platelet aggregation and a fÊbrate is expected to be useful in the treatment and/or prevention of myocardial infarction (heart attack), cardiac arrest, peripheral vascular disease (including symptomatic carotid artery disease), congestive heart failure, ischemic heart disease, angina pectoris (including unstable angina), sudden cardiac death, unstable angina, as well as cerebrovascular events such as cerebral infarction, cerebral thrombosis, cerebral ischemia and transient ischemic attack, disorders related to bypass operations (angioplasty), fitting of endovascular prostheses and restenosis, and inflammatory disorders, including arthritic conditions such as rheumatoid arthritis and osteoarthritis, as well as asthma or related airway or respiratory inflammatory disorders. | 2009-03-05 |
| 20090062241 | Highly porous, fast-disintegrating solid dosage form and its way of manufacturing comprising the preparation of a powder and a freezedrying step - The invention relates to a method of manufacture of fast-disintegrating solid dosage forms, characterized in that one or more structure building components in mixed solid powder form are dosed into cavities of blister packs or moulds, the remaining components dissolved in water dosed and added to the powder to form a moistened, plasticized mass, frozen to below −20° C. , and the water sublimed in high vacuum. In this way solid dosage forms are obtainable with a similar porous structure as usually result from freeze-drying processes, but the process requires much less water, which means considerably less time and less energy. | 2009-03-05 |
| 20090062242 | METHODS AND COMPOSITIONS FOR TREATING GASTROINTESTINAL CONDITIONS - Methods and compositions for treating a condition involving gastrointestinal symptoms comprising administering to a patient in need of such treatment an effective amount of a P-glycoprotein substrate, wherein the P-glycoprotein substrate is a compound exhibiting an efflux inhibition ratio (EIR) of greater than or equal to 0.4, wherein the P-glycoprotein substrate is administered in a manner to minimize bioavailability. | 2009-03-05 |
| 20090062243 | Lupane-Type Triterpenoids Modified at 30-Position and Analogues Thereof - The present invention comprises lupine-type triterpenoids that inhibit cell proliferations, in particular cancer and conditions associated with cancer. For example, associated malignancies include ovarian cancer, cervical cancer, breast cancer, colorectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases. Thus, the present invention also comprising pharmaceutical formulations comprising the compounds and methods of using the compounds and formulations to inhibit cancer and treat, prevent, or inhibit the foregoing diseases. | 2009-03-05 |
| 20090062244 | PHARMACEUTICAL COMPOSITION - Topical composition for enhanced local and systemic delivery of poorly soluble biologically active compounds, comprises of non-volatile solvent or mixture of solvents to dissolve active component, and moisture absorbent or mixture of sorbents to prevent precipitation or crystallization of insoluble material after application | 2009-03-05 |
| 20090062245 | Modulation of Neurodegenerative Diseases Through The Progesterone Receptor - Methods for modulating hormonal pathways involving the progesterone receptor in a subject with a neurodegenerative disorder, are provided. Progesterone receptor activity is modulated by administering an effective amount of an progesterone receptor modulating pharmacological agent to a subject such that the progesterone receptor modulating pharmacological agent interacts with the progesterone receptor and alters the expression of a protein associated with the neurodegenerative disease. | 2009-03-05 |
| 20090062246 | THERAPEUTIC TREATMENT-014 - A combination, comprising N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide, or a pharmaceutically acceptable salt thereof, and an aromatase inhibitor or an estrogen receptor down-regulator is described. The combination is expected to be useful in the treatment of cancer. | 2009-03-05 |
| 20090062247 | METHODS FOR INHIBITING TGF-beta - The present invention provides methods for inhibiting or blocking TGF-β activity in cells and/or tissues expressing TGF-β comprising, contacting cells and/or tissues expressing TGF-β with an amount of cholesterol or cholesterol derivative effective to inhibit the activity of TGF-β. The present invention further provides a method for treating a condition associated with overactivity of TGF-β or negative regulation in normal physiology by TGF-β in a subject in need of treatment, comprising contacting cells and/or tissue overexpressing TGF-β in the subject with an amount of cholesterol or cholesterol derivative effective to inhibit activity of TGF-β thereby treating the condition. In a preferred embodiment, the cholesterol derivative is oxidized 7-DHC. | 2009-03-05 |
| 20090062248 | OPTIMIZING MIFEPRISTONE LEVELS IN PLASMA SERUM OF PATIENTS SUFFERING FROM MENTAL DISORDERS TREATABLE WITH GLUCOCORTICOID RECEPTOR ANTAGONISTS - The present invention provides a method for optimizing levels of mifepristone in a patient suffering from a mental disorder amenable to treatment by mifepristone. The method comprises the steps of treating the patient with seven or more daily doses of mifepristone over a period of seven or more days; testing the serum levels of the patient to determine whether the blood levels of mifepristone are greater than 1300 ng/mL; and adjusting the daily dose of the patient to achieve mifepristone blood levels greater than 1300 ng/mL. | 2009-03-05 |
| 20090062249 | METHODS FOR REDUCING OR PREVENTING TRANSPLANT REJECTION IN THE EYE AND INTRAOCULAR IMPLANTS FOR USE THEREFOR - Methods for reducing or preventing transplant rejection in the eye of an individual are described, comprising: a) performing an ocular transplant procedure; and b) implanting in the eye a bioerodible drug delivery system comprising an immunosuppressive agent and a bioerodible polymer. | 2009-03-05 |
| 20090062250 | Analogs of Benzoquinone-Containing Ansamycins and Methods of Use Thereof - The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present invention provides analogs of benzoquinone-containing ansamycins where the benzoquinone is reduced to a hydroquinone and trapped by reaction with a suitable acid, preferably ones that increase the solubility and air stability of the resulting 17-ammonium hydroquinone ansamycin analog. | 2009-03-05 |
| 20090062251 | Novel Compounds 002 - Compounds of Formulae I, or pharmaceutically acceptable salts thereof: | 2009-03-05 |
| 20090062252 | THERAPEUTIC ISOXAZOLE COMPOUNDS - The invention provides a compound of formula I: | 2009-03-05 |
| 20090062253 | HETEROCYCLODIAZEPINE CANNABINOID RECEPTOR MODULATORS FOR TREATMENT OF DISEASE - The present invention relates to compounds and methods useful as modulators of CB2 for the treatment or prevention of disease states including, but not limited to pain, autoimmune disease, malabsorption syndrome, pulmonary disease, osteoporosis, muscle spasm in cancer, neuromuscular disorder, and atherosclerosis progression. | 2009-03-05 |
| 20090062254 | Acute Treatment of Headache with Phenothiazine Antipsychotics - Methods of treating headache with antipsychotics are provided. A kit for treating headache is also provided, comprising an antipsychotic and a device for rapid delivery of the antipsychotic. | 2009-03-05 |
| 20090062255 | TUMOR-TARGETING EVALUATION METHODOLOGY AND COMPOUNDS RELATED THERETO - The invention relates to a method for evaluating a chemotherapeutic potential of a candidate molecule. In evaluating the candidate molecule, the candidate molecule is tested for its ability to inhibit the in vitro growth of a cancer cell; to bind a cellular receptor produced by a cancer cell, wherein said receptor, such as a peripheral benzodiazepine receptor, is produced in a greater amount by said cancer cell than by a normal cell; and to inhibit the activity of at least one protein member of the MAPK pathway. The invention further relates to dibenzodiazepinone analogues and derivatives thereof. | 2009-03-05 |
| 20090062256 | LACTAMS SUBSTITUTED BY CYCLIC SUCCINATES AS INHIBITORS OF Abeta PROTEIN PRODUCTION - This invention relates to novel lactams having the Formula (I): | 2009-03-05 |
| 20090062257 | DEUTERIUM-ENRICHED VARENICLINE - The present application describes deuterium-enriched varenicline, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 2009-03-05 |
| 20090062258 | FUSED PYRIMIDINE DERIVATIVE AND USE THEREOF - The present invention provides a compound represented by the formula (I) and a salt thereof | 2009-03-05 |
| 20090062259 | Bezothiazol Derivatives as Beta2 Adrenoreceptor Agonists - The present invention relates to compounds according to formula (I), a process for preparing them, the intermediate compounds of the process and the use of the compounds in the manufacture of a medicament for use in treating diseases such as ARDS, pulmonary emphysema, bronchitis, bronchiectasis, COPD, asthma and rhinitis. The compounds are beta adrenoreceptor agonists. | 2009-03-05 |
| 20090062260 | COMPOUNDS AND COMPOSITIONS AS LXR MODULATORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs). | 2009-03-05 |
| 20090062261 | NITROGEN-CONTAINING HETEROCYCLE DERIVATIVES SUBSTITUTED WITH CYCLIC GROUP - It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. | 2009-03-05 |
| 20090062262 | NON STEROIDAL GLUCOCORTICOID RECEPTOR MODULATORS - The present invention relates to compounds having general Formula (I) or a pharmaceutically acceptable salt thereof. In this formula R | 2009-03-05 |
| 20090062263 | 4-Hydroxy-5,6-dihydro-1H-pyridin-2-one compounds - The invention is directed to 4-hydroxy-5,6-dihydro-1H-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus. | 2009-03-05 |
| 20090062264 | SALTS OF POTASSIUM ATP CHANNEL OPENERS AND USES THEREOF - Provided are immediate or prolonged administration of certain salts of K | 2009-03-05 |
| 20090062265 | Pyrrolo-Quinoxalinone Derivatives as Antibacterials - Tricyclic nitrogen containing compounds and their use as antibacterials. | 2009-03-05 |
| 20090062266 | OXAZOLIDINONE COMPOUNDS, AND COMPOSITIONS AND METHODS RELATED THERETO - The invention provides new oxazolidinone compounds of formula (I) wherein A is certain heterocycles optionally substituted; R | 2009-03-05 |
| 20090062267 | L-ALANINE DERIVATIVES AS a5beta1 ANTAGONISTS - The present invention relates to compounds that inhibit a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins. | 2009-03-05 |
| 20090062268 | NOVEL INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) - A compound having the structure set forth in Formula (I): | 2009-03-05 |
| 20090062269 | Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment - The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included. | 2009-03-05 |
| 20090062270 | SPIRO 2,4 PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES - The present invention provides methods of treating or preventing autoimmune diseases with spiro 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lupus erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms. | 2009-03-05 |
| 20090062271 | Antithrombotic Diamides - This application relates to a compound of formula I (or a pharmaceutically acceptable salt of the compound) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor. | 2009-03-05 |
| 20090062272 | IMIDAZOQUINOLINYL SULFONAMIDES - Imidazoquinolinyl, imidazopyridinyl, and imidazonaphthyridinyl sulfonamide compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed. | 2009-03-05 |
| 20090062273 | 3-H-pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same. - The invention relates to 3-H-pyrazolopyridines according to the general formula (I): | 2009-03-05 |
| 20090062274 | Pyridopyrimidinone inhibitors of pi3kalpha - The invention is directed to Compounds of Formula I and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds. | 2009-03-05 |
| 20090062275 | N-Substituted Imidazopyridine c-Kit Inhibitors - Compounds represented by Formula (I): | 2009-03-05 |
| 20090062276 | PYRIDOPYRIMIDINE PROTEIN TYROSINE PHOSPHATASE INHIBITORS - The present invention comprises pyridopyrimidinediamine compounds of the general formula I: | 2009-03-05 |
| 20090062277 | PHOSPHODIESTERASE 10 INHIBITORS - The present invention is directed to certain compounds useful as phosphodiesterase 10 (PDE10) inhibitors that have the formula | 2009-03-05 |
| 20090062278 | 5- OR 6-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION - The present invention concerns 5- or 6-substituted-benzimidazole derivatives having inhibitory activity on the replication of the respiratory syncytial virus and having the formula | 2009-03-05 |
| 20090062279 | HETEROCYCLIC COMPOUNDS, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS, IN PARTICULAR AS ANTI-ALZHEIMER AGENTS - The invention is related to compound which comprises at least one radical C═Y, Y being O or S, and an oxidable and non protonable nitrogen atom N wherein the distance (d) between the at least one carbon atom of the radical group C═Y and the nitrogen atom, when oxidized, is comprised between 0.3 and 0.8 nanometers. The invention is related to new heterocyclic compounds defined by formula G, their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of neurodegenerative or Alzheimer disease. | 2009-03-05 |
| 20090062280 | Ophthalmic Compositions for Treating Ocular Hypertension - This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans. | 2009-03-05 |
| 20090062281 | 3-QUINOLINECARBONITRILE PROTEIN KINASE INHIBITORS - This invention provides a compound of Formula 1 | 2009-03-05 |
| 20090062282 | Substituted Amino-Pyrimidones and Uses Thereof - This invention relates to novel compounds having the structural formula Ia or formula Ib below: (Ia, Ib), and their pharmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of Aβ related pathologies such as cognitive impairment, Alzheimer Disease, neurodegeneration and dementia. | 2009-03-05 |
| 20090062283 | DEUTERIUM-ENRICHED LINEZOLID - The present application describes deuterium-enriched linezolid, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 2009-03-05 |
| 20090062284 | Thio-Substituted Biarylmethanesulfinyl Derivatives - The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted biaryl-methanesulfinyl acetamides of Formula (I): | 2009-03-05 |
| 20090062285 | SULFUR-CONTAINING COMPOUND, METHOD OF PREPARATION AND PHARMACEUTICAL USES THEREOF - The invention relates to a sulfur-containing compound and the preparation thereof. The invention also relates to the uses of the sulfur-containing compound in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2. This invention also describes a series of chemical analogues of the said sulfur-containing compound and the preparation of these compounds. | 2009-03-05 |
| 20090062286 | Crystal Structure of SMYD3 Protein - The invention relates to SMYD3 methyltransferase (SMYD3), SMYD3 binding pockets or SMYD3-like binding pockets. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to SMYD3 methyltransferase protein, complexes of SMYD3 methyltransferase protein, homologues thereof, or SMYD3-like protein or protein complexes. | 2009-03-05 |
| 20090062287 | SUBSTITUTED BIARYL COMPOUNDS AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I): | 2009-03-05 |
| 20090062288 | PYRROLOTRIAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS AND METHODS OF TREATING KINASE-ASSOCIATED CONDITIONS THEREWITH - The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition. | 2009-03-05 |
| 20090062289 | IMMUNOMODULATING OXOPYRRAZOLOCINNOLINES AS CD 80 INHIBITORS - N-(1-Aza-bicyclo[2.2.2]oct-3-yl)-4-(6,9-difluoro-3-oxo-1,3-dihydro-pyrazolo[4,3-c]cinnolin-2-yl)-benzamide is a CD80 antagonist, useful in the treatment of dieases which benefit from immuno-inhibition. | 2009-03-05 |
| 20090062290 | HETEROCYCLES AS POTASSIUM CHANNEL MODULATORS - Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions. | 2009-03-05 |
| 20090062291 | PHOSPHODIESTERASE 10 INHIBITORS - The present invention is directed to compounds, useful as PDE10 inhibitors, having the formula | 2009-03-05 |
| 20090062292 | Tetrahydropteridines useful as inhibitors of protein kinases - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 2009-03-05 |
| 20090062293 | 1,4-Substituted Piperazine Derivatives - A compound represented by the formula (I): | 2009-03-05 |
| 20090062294 | HETEROARYL-SUBSTITUTED UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE - Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis). | 2009-03-05 |
| 20090062295 | Pharmaceutical Products - Pharmaceutical products comprising 6-[4-(4-pyridylamino)phenyl]-4,5-dihydro-3(2H)-pyridazinone or a salt thereof, or a hydrate thereof or a solvate thereof as an active ingredient, wherein production of hydrazine is substantially suppressed is provided. | 2009-03-05 |
| 20090062296 | Prostaglandin derivatives - Nitroderivatives of prostaglandin amides having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension. | 2009-03-05 |
| 20090062297 | Hydroxyalkylarylamide Derivatives - The present invention relates to a novel class of hydroxyalkylarylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo. | 2009-03-05 |
