46th week of 2008 patent applcation highlights part 46 |
Patent application number | Title | Published |
20080280845 | Compositions and Their Uses Directed to Ptpru - Disclosed herein are compounds, compositions and methods for modulating the expression of PTPRU in a cell, tissue or animal. Also provided are methods of active target segment validation. Also provided are uses of disclosed compounds and compositions in the manufacture of a medicament for treatment of diseases and disorders. Also provided are methods for the prevention, amelioration and/or treatment of diabetes, obesity, insulin resistance, insulin deficiency, hypercholesterolemia, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hyperfattyacidemia, liver steatosis, steatohepatitis, non-alcoholic steatohepatitis, metabolic syndrome, cardiovascular disease and coronary heart disease by administration of antisense compounds targeted to PTPRU. | 2008-11-13 |
20080280846 | 2', 3'-DIDEOXYNUCLEOSIDE ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRIDAE INFECTIONS - A method for the treatment or prevention of Flaviviridae infections, in particular, hepatitis C virus infection, in a host, and in particular, a human, is provided that includes administering an effective amount of a β-L- or β-D-2′,3′-dideoxynucleoside or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable diluent or excipient. | 2008-11-13 |
20080280847 | PIT-1 AND VASCULAR CALCIFICATION - The present invention relates to methods and compositions comprising small interfering RNAs (siRNAs) to identify nucleotides encoding proteins involved in the co-transport of inorganic phosphate in vascular tissues. Specifically, it relates to the identification of Pit-1 and Pit-2 as key proteins involved in vascular calcification, the deposition of calcium phosphate, in blood vessels. The nucleic acids encoding specific siRNAs and vectors encoding these siRNAs are useful as tools to specifically inhibit the expression of Pit-1, Pit-2, or related proteins in various primary and stably-transformed cell lines, and as tools to explore the roles and functional relationships of these proteins involved in vascular calcification. In addition, they may be useful directly as therapeutic agents in humans delivered to sites of vascular calcification. | 2008-11-13 |
20080280848 | Structures of Active Guide Rna Molecules and Method of Selection - The present invention relates to methods and compositions for modulating RNA silencing efficiency by providing selective RISC (RNA-induced silencing complex) formation. The present invention also relates to methods for identifying nucleic acids and/or determining their structures. | 2008-11-13 |
20080280849 | Synergic Combinations Comprising a Quinoline Compound and Other Hiv Infection Therapeutic Agents - The invention relates to a combination comprising a quinoline compound or its sail, according to general formula (I) and at least one HIV infection therapeutic agent selected from the group consisting of entry inhibitors, reverse-transcriptase inhibitors, strand-transfer inhibitors, protease inhibitors, and maturation inhibitors. Said combination has therapeutic synergy in the treatment of an HIV infection compared with the quinoline compound, or HIV infection therapeutic agent alone. | 2008-11-13 |
20080280850 | Methods and Compositions for Treating Flaviviruses, Pestiviruses and Hepacivirus - A method and composition for treating a host infected with flavivirus, pestivirus or hepacivirus comprising administering an effective flavivirus, pestivirus or hepacivirus treatment amount of a described base-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided. | 2008-11-13 |
20080280851 | Oral Dosage Forms of Gemcitabine Derivatives - The present invention relates to oral dosage forms of certain long chain saturated and monounsaturated fatty acid derivatives of 2′,2′-difluorodeoxycytidine (Gemcitabine). In particular, the present invention relates to the use of the said gemcitabine derivatives or a pharmaceutical acceptable salt thereof for preparing an oral dosage form ameliorating compliance in treatment of cancer. | 2008-11-13 |
20080280852 | Composition Containing Fermentable Polysaccharides - The present invention relates to a composition to a nutritional composition comprising 0.1 to 15 gram fermentable e partially hydrolysed gum having a degree of polymerisation between 10 and 300 per 100 gram dry weight of the composition and 0.1 to 15 gram fermentable, indigestible polysaccharide other than a hydrolysed gum having a DP between 10 and 300 per 100 gram dry weight of the composition. | 2008-11-13 |
20080280853 | COMPOSITIONS FOR REDUCING, AMELIORATING, TREATING, OR PREVENTING CONDITION OF DRY EYE AND METHODS OF MAKING AND USING SAME - Compositions for relief, treatment, or prevention of a condition of dry eye comprise alginate, at least a polyol, and a pharmaceutically acceptable carrier, wherein the compositions have pH in the range from about 5 to about 7.5. In some embodiment, the compositions can further include a chelating agent, a buffering system or agent, an organic acid, or combinations thereof. | 2008-11-13 |
20080280854 | PREVENTING OR REDUCING OXIDATIVE STRESS OR OXIDATIVE CELL INJURY - A water-soluble cellulose derivative is useful for preventing or reducing oxidative stress or oxidative cell injury in tissues of an animal and in particular for regulating Stearoyl-CoA Desaturase-1 gene expression and/or ATPF1 gene expression in non-adipose tissues of the animal. | 2008-11-13 |
20080280855 | Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles - The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. | 2008-11-13 |
20080280856 | Fibroblast Activation Protein Inhibitor Compounds and Methods - Amino terminus-blocked peptide boronate compounds of Formulas I and II are useful for inhibiting Fibroblast Activation Protein (FAP) and other proteases, and for treating disorders mediated by FAP. Methods of using the amino terminus blocked peptide boronate compounds, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 2008-11-13 |
20080280857 | CGRP receptor antagonists - The present invention is directed to compounds of Formula I: | 2008-11-13 |
20080280858 | METHOD OF CREATING CRYSTALLINE SUBSTANCES - Process for preparing a cocrystal of an active substance and a cocrystal former, the process involving precipitating the active substance and the cocrystal former together from solution or suspension, in the presence of a supercritical or near-critical fluid, in particular using a GAS, SAS, SEDS or SAS-EM process. The invention also provides a cocrystal prepared using such a process, and its use as a seed crystal in a subsequent process for precipitating a cocrystal of an active substance and a cocrystal former. | 2008-11-13 |
20080280859 | GEMINI VITAMIN D3 COMPOUNDS AND METHODS OF USE THEREOF - The invention provides Gemini vitamin D | 2008-11-13 |
20080280860 | Use of Vitamin D Compounds to Treat Endometriosis - The use of vitamin D compounds in the treatment or prevention of endometriosis, methods for the treatment or prevention of endometriosis by administering a vitamin D compound, and compounds for use therein. | 2008-11-13 |
20080280861 | Method of Female Contraception and a Kit For Use Therein - The invention is concerned with a method of contraception in a female mammal of childbearing capability. The method has two alternating phases—a preservation phase and a shedding phase—and has at least two sequences of (a) a preservation phase of 3-12 months involving continuous oral administration to the female of dosage units containing: (i) an estrogen selected from 17β-estradiol, esters of 17β-estradiol and combinations thereof, in an amount equivalent to a daily oral dosage of 2.2-5 mg 17β-estradiol, and (ii) a progestogen in an amount equivalent to a daily oral dosage of 30-750 μg levonorgestrel; and (b) a shedding phase of 4-12 days during which no progestogen is administered. The invention also relates to a contraceptive kit having one or more packaging units that are separately packaged, individually removable oral dosage units for use in the aforementioned contraceptive method. | 2008-11-13 |
20080280862 | Methods, compositions, and kits for the treatment of pain - The invention features methods, compositions, and kits for the treatment of pain. | 2008-11-13 |
20080280863 | COMPOSITIONS FOR THE TREATMENT OF INFLAMMATORY DISORDERS - The invention features methods and compositions for the treatment of immunoinflammatory disorders. | 2008-11-13 |
20080280864 | Novel C-17-Heteroaryl Steroidal Cyp17 Inhibitors/Antiandrogens, 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 CYP 17 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. | 2008-11-13 |
20080280865 | WATER-IN-OIL TYPE EMULSIFIED COMPOSITION - Water-in-oil type emulsified compositions with a high silicone oil content which are excellent in emulsification stability and whose sticky feeling has been improved may be obtained by incorporating a specific (A) N-long chain acyl neutral amino acid ester, (B) a silicone oil, and (C) water therein. | 2008-11-13 |
20080280866 | Method of Treating or Sepsis - Provided is a method of treating trauma or sepsis comprising: administering an effective amount of one or both of a SOC channel-selective inhibitor or a SphK inhibitor to an animal at risk of inflammation-mediated organ damage from trauma or sepsis. | 2008-11-13 |
20080280867 | COMBINATION THERAPY WITH PARP INHIBITORS - The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with temozolomide (TMZ). | 2008-11-13 |
20080280868 | Pyridine Derivatives and Their Use as Cb2 Receptor Modulators - The present invention relates to novel pyridine derivatives such as compounds of the formula (I): | 2008-11-13 |
20080280869 | Pyrazole or Triazole Compounds and Their Use for the Manufacture of a Medicament for Treating Somatic Mutation-Related Diseases - The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA. | 2008-11-13 |
20080280870 | Beta-Lactamyl Phenylalanine, Cysteine, and Serine Vasopressin Antagonists - Substituted 2-(azetidin-2-on-1-yl)alkoxyalkylalkanoic acids and 2-(azetidin-2-on-1-yl)arylalkylalkanoic acids, and analogs and derivatives thereof are described. Methods for using the described compounds, and pharmaceutical compositions thereof, to treat disease states responsive to antagonism of one or more vasopressin receptors are also described. | 2008-11-13 |
20080280871 | 5-Phenyl-4-Methyl-Thiazol-2-Yl-Amine Derivatives as Inhibitors of Phosphatidylin Ositol 3 Kinase Enzymes (PI13) For Treatment of Inflammatory Diseases - in free or salt form, wherein R | 2008-11-13 |
20080280872 | Benzamide Derivatives and Their Use as Glucokinase Activating Agents - Compounds of Formula (I): wherein: R | 2008-11-13 |
20080280873 | Biaryl Substituted Pyrazinones as Sodium Channel Blockers - Biaryl substituted pyrazinone compounds 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, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. | 2008-11-13 |
20080280874 | Phenoxy Benzamide Compounds with Utility in the Treatment of Type 2 Diabetes and Obesity - Compounds of Formula (I): | 2008-11-13 |
20080280875 | FUSED PHENYL AMIDO HETEROCYCLIC COMPOUNDS - The present invention relates to a compound of formula (I): | 2008-11-13 |
20080280876 | Novel oxadiazole compounds - Novel oxadiazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions as agonists or antagonists of the S1P family of G protein-coupled receptors for treating diseases associated with modulation of S1P family receptor activity, in particular by affording a beneficial immunosuppressive effect are disclosed. | 2008-11-13 |
20080280877 | Azetidines - The invention relates to EP2 antagonist azetidines of formula (I) | 2008-11-13 |
20080280878 | Methods and Compositions for Treating Chronic Lymphocytic Leukemia - Novel method of treating chronic lymphocytic leukemia by the administering of HSP90 inhibitors, particularly ansamycins, more particularly I 7-allylamino-I 7-demethoxygetdanarnycin (17-AAG). | 2008-11-13 |
20080280879 | SUBSTITUTED HETEROCYCLIC DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS - Compounds of the general Formula I, wherein X | 2008-11-13 |
20080280880 | Staurosporine Derivatives for Use in Alveolar Rhabdomyosarcoma - This invention relates to staurosporine derivatives are effective when used in combination with ionizing radiation for the delay of progression or treatment of a proliferative disease, especially a disease associated with a PAX/FKHR translocation including a PAX3/FKHR translocation and a PAX7/FKHR translocation, more especially a solid tumor disease such as a Sarcoma, most especially an Alveolar Rhabdomyosarcoma. | 2008-11-13 |
20080280881 | MORPHOLINYL CONTAINING BENZIMIDAZOLES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION - The present invention concerns morpholinyl containing benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula | 2008-11-13 |
20080280882 | Novel Substituted Diazabicyclo Derivatives and Their Use as Monoamine Neurotransmitter Re-Uptake Inhibitors - This invention relates to novel substituted diazabicyclo derivatives useful as monoamine neurotransmitter re-uptake inhibitors. | 2008-11-13 |
20080280883 | Muscarinic Receptor Antagonists - This present invention generally relates to muscarinic receptor antagonists which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors. | 2008-11-13 |
20080280884 | Mixed Solvate of Olanzapine, Method for Preparing It and Method for Preparing Form I of Olanzapine Therefrom - Said mixed solvate is a solvate of olanzapine/water/tetrahydrofuran in the proportion 1:1:1/2 (I). The method for preparing said solvate comprises treating a crude anhydrous olanzapine with a mixture of tetrahydrofuran/water. The method for preparing Form I of olanzapine includes desolvating the mixed solvate of formula I, by means of drying, in vacuo and under temperature-controlled conditions. | 2008-11-13 |
20080280885 | Methods for Treating Anxiety Related Disorders - The present invention relates to methods of and compositions for treating and relieving symptoms and disease associated with indications caused by a physiological drive to alleviate a sensation of anxiety. In one treatment method, methods of, and compositions for, modulating the expression of certain GABAA receptor subunits are used to treat anxiety-related disorders and depressive disorders associated with physiological tolerance to endogenous neurosteroids. | 2008-11-13 |
20080280886 | SUBSTITUTED UREAS - Disclosed herein are urea-based 5-HT receptor modulators, pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and medical use of such compounds for the treatment and/or management of 5-HT receptor-mediated disorders. | 2008-11-13 |
20080280887 | Selected Cgrp-Antagonists, Processes for Preparing Them and Their Use as Pharmaceutical Compositions - The invention relates to CGRP-antagonists of general formula (I), wherein R | 2008-11-13 |
20080280888 | Antibiotics Derivatives - The invention relates to antibiotic derivatives of formula I | 2008-11-13 |
20080280889 | Inhibitors of Akt Activity - The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration (if the compounds of the invention. | 2008-11-13 |
20080280890 | HYDROXYLAMINE COMPOUNDS AND METHODS OF THEIR USE - The present disclosure provides compounds that include hydroxylamines of formula I or II, pharmaceutical compositions, and methods for their use. The methods utilize hydroxylamine compounds and/or their pharmaceutical compositions for the treatment of angiogenesis, hepatitis, complement-mediated pathologies, drusen-mediated pathologies, macular degeneration and certain other ophthalmic conditions, inflammation, arthritis, and related diseases and for the inhibition of complement activation. | 2008-11-13 |
20080280891 | Anti-cancer agents and uses thereof - The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: | 2008-11-13 |
20080280892 | Compounds - Tricyclic nitrogen containing compounds and their use as antibacterials. | 2008-11-13 |
20080280893 | SUBSTITUTED-DIHYDRO[1,4]OXAZINO[2,3,4-hi]INDAZOLE DERIVATIVES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS - The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor. | 2008-11-13 |
20080280894 | DIHYDRO[1,4]OXAZINO[2,3,4-hi]INDAZOLE DERIVATIVES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS - The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor. | 2008-11-13 |
20080280895 | 5-Amino-4-Hydroxy-7-(1H-Indolmethyl)-8-Methylnonamide Derivatives as Renin Inhibitors for the Treatment of Hypertension - The application relates to novel alkanamides of the general formula (I) where X is —CH | 2008-11-13 |
20080280896 | Dipyrrole Compounds, Compositions, and Methods For Treating Cancer or Viral Diseases - The present invention relates to novel Dipyrrole Compounds, compositions comprising a Dipyrrole Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Dipyrrole Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus. The invention also provides screening assays for compounds that can be used in combination with Dipyrrole Compounds for the treatment of cancer or neoplastic disease, inhibition of cancer cell growth, or treatment of viral infections. | 2008-11-13 |
20080280897 | Aerosol Formulation for Inhalation - The present invention relates to a propellant-free aerosol formulation which contains one or more compounds of general formula 1. | 2008-11-13 |
20080280898 | Spiro-piperidine derivatives - The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. | 2008-11-13 |
20080280899 | Inhibitors of Akt Activity - The present invention is directed to compounds which contain substituted napthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention. | 2008-11-13 |
20080280900 | BICYCLIC PYRIMIDINE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS - Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing thienopyrimidine or oxoquinazoline derivatives are disclosed of the general formula (1) or formula (2) where X is a linker and Y is an aromatic moiety or N(R5)(R6). | 2008-11-13 |
20080280901 | Pharmaceutical Composition for Preventing and Treating Metabolic Bone Diseases Containing Alpha-Arylmethoxyacrylate Derivatives - The present invention relates to a use of a specific alpha-arylmethoxyacrylate derivative, or its pharmacologically acceptable salt or solvate for preventing and treating metabolic bone diseases. | 2008-11-13 |
20080280902 | Inhibitors of Checkpoint Kinases - The instant invention provides for compounds which comprise substituted quinolinones that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer. | 2008-11-13 |
20080280903 | Apoptosis Inhibitors - The present invention provides compounds that act as selective agents to protect against unintentional cell death or tissue damage and can relieve side effects of cancer treatment such as, for example, oral mucositis, hair loss, diarrhea due to damage to the gastrointestinal epithelium, and myelosuppression. In addition, these compounds can be used to prevent premature cell death when the cell death is caused by signals from damaged cells, for example, signals generated as the result of a traumatic incident or an ischemic episode. | 2008-11-13 |
20080280904 | N-Substituted Pyridinone or Pyrimidinone Compounds Useful as Soluble Epoxide Hydrolase Inhibitors - Disclosed are compounds active against soluble epoxide hydrolase (sEH), compositions thereof and methods of using and making same. | 2008-11-13 |
20080280905 | UREA ANTAGONISTS OF P2Y1 RECEPTOR USEFUL IN THE TREATMENT OF THROMBOTIC CONDITIONS - The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y | 2008-11-13 |
20080280906 | Imidazolyl-Pyrimidine Compounds for Use in the Treatment of Proliferative Disorders - Compounds of formula (I): | 2008-11-13 |
20080280907 | Triazolophthalazines - The compounds of formula (I) | 2008-11-13 |
20080280908 | NAPHTHYL(ETHYL) ACETAMIDES - This disclosure relates to novel melatonin analogues or naphthyl(ethyl)acetamides, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a dual melatoninergic agonist and serotoninergic antagonist. | 2008-11-13 |
20080280909 | NEW PHENYLALANINE DERIVATIVES - Phenylalanine derivatives of the following formula, analogues thereof and pharmaceutically acceptable salts thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning α4 integrin in which α4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection. | 2008-11-13 |
20080280910 | PHTHALAZINONE DERIVATIVES - A compound of the formula (I): | 2008-11-13 |
20080280911 | Cinnoline Compounds as Inhibitors of Phosphodiesterase Type IV (Pde4) - There are provided according to the invention novel compounds of formula (I) | 2008-11-13 |
20080280912 | Novel Diazabicycylic Aryl Derivatives and Their Medical Use - This invention relates to novel diazabicyclic aryl derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 2008-11-13 |
20080280913 | TETRAHYDROTRIAZOLOPYRAZINE DERIVATIVES AND USES THEREOF - This invention relates to novel substituted tetrahydrotriazolopyrazines and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an enzyme inhibitor of dipeptidyl-peptidase IV (DPP-IV). | 2008-11-13 |
20080280914 | Intravenous Formulations of Pde Inhibitors - The invention relates to a novel pharmaceutical dosage form of PDE 5 inhibitors for intravenous administration and the use thereof for the treatment of diseases. | 2008-11-13 |
20080280915 | Insecticidal n-substituted (heteroaryl)alkyl sulfilimines - N-Substituted (heteroaryl)alkyl sulfilimines are effective at controlling insects. | 2008-11-13 |
20080280916 | PYRIDAZINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS - Methods of treating an SCD-mediated skin disorder or condition in a mammal, preferably a human include administering to a mammal in need thereof a compound of formula (I): | 2008-11-13 |
20080280917 | Nitrogen-Containing heterocyclyl ketones and methods of use - Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes. | 2008-11-13 |
20080280918 | Pyridazin-3(2H)-One Derivatives and Their Use as Pde4 Inhibitors - The invention relates to new therapeutically useful pyridazin-3(2H)-one derivatives of Formula (I) and to pharmaceutical compositions containing them. These compounds are potent and selective inhibitors of phosphodiesterase 4 (PDE4) and are thus useful in the treatment, prevention or suppression of pathological conditions, diseases and disorders known to be susceptible of being improved by inhibition of PDE4 such as asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatilis, psoriasis or irritable bowel disease. | 2008-11-13 |
20080280919 | QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING AFFINITY FOR 5HT1-TYPE RECEPTORS - Disclosed are methods for use of compounds of formula (I) in combination with other active substances in the treatment of CNS disorders such as depression or anxiety. | 2008-11-13 |
20080280920 | Plasminogen Activator Inhibitor-1 Inhibitors - Inhibitors of plasminogen activator inhibitor-1 (PAI-I) are provided, which may also act as anti cancer agents, of formulae (I-V). | 2008-11-13 |
20080280921 | Amorphous Aripiprazole and Process for the Preparation thereof - Morphologically stabilized amorphous aripiprazole and process for preparing the same. | 2008-11-13 |
20080280922 | Intermittent Dosing Regimen For Overweight and Obese Subjects - The present invention concerns an intermittent dosing regimen for the treatment of obesity or the reduction of body weight wherein a pharmaceutical composition containing an apoB secretion/MTP inhibitor is administered to a subject in need thereof for a period of time, then withheld for a period of time, and again administered for a period of time. The intermittent regimen may be repeated depending on the response in the subject that is being sought. | 2008-11-13 |
20080280923 | 1-Benzylindole-2-Carboxamide Derivatives - The present invention relates to i-benzylindole-2-carboxamide derivatives of formula I, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to pharmaceutical compositions comprising said 1-benzylindole-2-carboxamide derivatives and to their use in therapy, particularly for the treatment of obesity or nicotine dependence. | 2008-11-13 |
20080280924 | PYRIDINE AND PYRIMIDINE DERIVATIVES AS MGLUR2 ANTAGONISTS - The present invention relates to compounds of formula (I) | 2008-11-13 |
20080280925 | Amines as Small Molecule Inhibitors - The present invention relates to compounds that are useful as inhibitors of protein arginine methyltransferase that have a formula selected from Formula (I), Formula (II) and Formula (III), as well as racemic mixtures, diastereomers, enantiomers and tautomers thereof and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof as defined herein. Said compound are useful as inhibitors of PRMTs and/or CARM-I. The invention further relates to compositions comprising such compounds and methods for their use. | 2008-11-13 |
20080280926 | Phosphodiesterase Inhibitors - The present invention relates to purine derivatives, which can be used as selective phosphodiesterase (PDE) type IV inhibitors. Compounds disclosed herein can be useful in the treatment of asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases especially in humans. Also provided are processes for the preparation of disclosed compounds, pharmaceutical composition containing the disclosed compounds and their use as selective phosphodiesterase (PDE) type IV inhibitors. | 2008-11-13 |
20080280927 | 3-(DIHYDRO-1H-PYRAZOLO[4,3-D]PYRIMIDIN-5-YL)-4-PROPOXYBENZENESULFONAMIDE DERIVATIVES AND METHODS OF USE - This invention relates to novel 3-(dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxybenzenesulfonamide compounds, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of cyclic guanosine 3′,5′-monophosphate specific phosphodiesterase (cGMP-specific PDE), in particular PDE5. | 2008-11-13 |
20080280928 | Pyrrolopyrimidine and Pyrrolopyridine Derivatives Substituted with a Cyclic Amino Group As Crf Antagonists - [PROBLEM TO BE SOLVED] An object of the present invention is to provide an antagonist against CRF receptors and/or an agonist for δ receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal diseases, drug dependence, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, pain, etc.
| 2008-11-13 |
20080280929 | Antifungal Wallboards and Building Materials and Methods for the Production Thereof - The present invention relates to, inter alia, methods for the treatment of wallboards and the treated wallboards. In particular, the invention relates to the treatment of wallboards with a fungicidally effective amount of a strobilurin or strobilurin-type fungicide. In a particular embodiment the fungicide is azoxystrobin. The invention also provides for the treatment of wallboards and building materials with combinations of fungicides present in synergistic amounts. | 2008-11-13 |
20080280930 | Pyrimidinone Compounds and Preparation and Use Thereof - Disclosed are pyrimidinone compounds having formula (I), a preparation and use thereof. The compounds are inhibitors of HMG-CoA reductase, and therefore have antivirus activities and are useful for preventing and treating cardiovascular and cerebrovascular disorders, senile dementia, diabetes mellitus, osteoporosis and tumors, and enhancing immune functions in a subject, and especially useful for treating diseases associated with hyperlipaemia. | 2008-11-13 |
20080280931 | POLYMORPHS OF SUCCINATE SALT OF 2-[6-(3-AMINO-PIPERIDIN-1-YL)-3-METHYL-2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN-1-YLMETHY]-4-FLUOR-BENZONITRILE AND METHODS OF USE THEREFOR - Compositions comprising the succinate salt of 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile (referred to herein as Compound I) which has the formula: | 2008-11-13 |
20080280932 | COMPOSITIONS AND METHODS FOR TREATING VASCULAR, AUTOIMMUNE, AND INFLAMMATORY DISEASES - The disclosure provides methods and compositions for the treatment of vascular, autoimmune and inflammatory diseases using a combination of an inosine monophosphate dehydrogenase (IMPDH) inhibitor and a HMG CoA reductase inhibitor. | 2008-11-13 |
20080280933 | BENZIMIDAZOLYL COMPOUNDS - Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I | 2008-11-13 |
20080280934 | Method of Preparing Porphyrin Derivatives, Porphyrin Derivatives, Uses Thereof and Pharmaceutical Compositions - Method of preparing a porphyrin derivative starting from a meso-substituted porphyrin compound. According to the invention, the meso-substituted porphyrin compound used is a meso-(2′-cyanovinyl)-substituted porphyrin compound, wherein said meso-(2′-cyanovinyl)-substituted porphyrin compound, in a form in which its porphyrin ring is complexed with a bivalent metal ion is converted, in the present of an acid for which | 2008-11-13 |
20080280935 | Process to Prepare Camptothecin Derivatives - A process is provided for the preparation of camptothecin derivatives, such as irinotecan, in a one-pot operation. | 2008-11-13 |
20080280936 | Morphinan Compounds - This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ | 2008-11-13 |
20080280937 | Ligand Conjugates of Vinca Alkaloids, Analogs, and Derivatives - Described herein are compounds, pharmaceutical compositions and methods for treating pathogenic cell populations in a patient. The compounds described herein include conjugates of cytotoxic drugs and vitamin receptor binding ligands. The conjugates also include a linker that is formed from one or more spacer linkers, heteroatom linkers, and releasable linkers. | 2008-11-13 |
20080280938 | Screening Method - The present invention provides a medicament for preventing/treating cancer, comprising a tacrine compound, or a compound promoting the binding between the tacrine compound and a protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1. | 2008-11-13 |
20080280939 | Combination of Organic Compounds - The invention relates to a pharmaceutical combinations comprising an AT1 receptor blocker or pharmaceutically acceptable salts thereof and a mTOR inhibiting agent, e.g. rapamycin or a rapamycin derivative, optionally in the presence of a pharmaceutically acceptable carrier. | 2008-11-13 |
20080280940 | Rapamycin Derivative or an Impdh Inhibitor For Treating Polycystic Kidney Disease - A method for treating polycystic kidney disease, comprising administering to a subject in need thereof a therapeutical effective amount of an inosine-5′-monophosphate dehydrogenase inhibitor or a rapamycin derivative. | 2008-11-13 |
20080280941 | 8-Phenoxy-Gamma Carboline Derivatives - Compounds of Formula I and corresponding pharmaceutical compositions are disclosed. | 2008-11-13 |
20080280942 | Tetrahydro-Beta-Carbolin-Sulfonamide Derivatives as 5-Ht6 Ligands - The present invention relates to new tetrahydro-β-carbolin-sulfonamide derivatives of general formula (I), optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their racemates or in form of a mixture of at least two of their stereoisomers, preferably enantiomers or diastereomers, in any mixing ratio, or corresponding physiologically acceptable salts or corresponding solvates. These compounds are suitable as pharmacologically active agents in a medicament for the prophylaxis and/or treatment of disorders or diseases related to 5-HT | 2008-11-13 |
20080280943 | METHODS AND PACKAGES TO ENHANCE SAFETY WHEN USING IMIQUIMOD TO TREAT CHILDREN DIAGNOSED WITH SKIN DISORDERS - Pharmaceutical packages and methods for enhancing the safety of imiquimod when used to treat children affected by skin disorders are disclosed. More particularly, the safety profile of imiquimod use is enhanced by providing information to the children, guardians of the children, including parents and health care professionals, that systemic absorption of imiquimod and other effects may be observed when imiquimod therapy is used to treat children of between about 2 and about 12 years of age. Examples of systemic absorption include a serum imiquimod concentrations of less than about 2 ng/mL, a decrease in median white blood cell count by about 1.4*10 | 2008-11-13 |
20080280944 | Imidazo[1,2-A]Pyridine Derivatives For The Treatment Of Silent Gastro-Esophageal Reflux - The present invention relates to a new method of treatment of sleep disturbance due to silent gastro-esophageal reflux. In particular, the present invention relates to the use of certain imidazo (1,2-a)pyridines derivatives (I) in said treatment. | 2008-11-13 |