08th week of 2009 patent applcation highlights part 40 |
Patent application number | Title | Published |
20090048209 | COMPOSITIONS COMPRISING DC-SIGN BLOCKERS AND METHODS OF USING DC-SIGN BLOCKERS FOR PREVENTING OR TREATING DISEASES OF A MAMMAL, INCLUDING VIRAL INFECTIONS - The present invention relates to methods and compositions for preventing or treating diseases of a mammal, including viral infections, wherein at least one symptom of the disease is mediated at least in part by the binding of an effector molecule to a DC-SIGN receptor present on cells of the mammal to be treated. The invention also provides methods of identifying compositions, wherein the compositions are useful for treating mammalian diseases, including viral infections, for which at least one symptom of the disease is mediated at least in part by the specific binding of an effector molecule to a DC-SIGN receptor present on the cells that express the DC-SIGN receptor, belonging to the mammal to be treated. The invention further relates to compositions and methods for targeting subject molecules to cells that express the DC-SIGN receptor. | 2009-02-19 |
20090048210 | AGENT FOR THERAPY OR TREATMENT OF WOUND - The present invention has an object of revealing an epidermis regeneration effect of various chitin derivatives and providing an agent for therapy or treatment for wound which can be clinically used effectively. According to the present invention, it has been evidenced that N-acetyl-D-glucosamine has an effect of promoting proliferation of an epidermis keratinized cell. Accordingly, the present invention provides a proliferation promoting agent for epidermis keratinized cell comprising N-acetyl-D-glucosamine. According to another aspect of the present invention, there is provided a regeneration promoting agent or protecting agent for epithelium, skin or dermis comprising the proliferation promoting agent. Further, a therapeutic agent for wound is provided. | 2009-02-19 |
20090048211 | EXTERNAL PREPARATION COMPOSITION - An external preparation composition used for preventing or treating symptoms or diseases related to dermatopathy caused by dryness, UV rays and aging such as wrinkles and sags of the skin, pigmentation of the skin, skin roughness and coarse texture and skin diseases such as psoriasis, lichen, ichthyosis, keratosis, Darier's disease, pustulosis, acne, eczema and atopic dermatitis. The external preparation composition comprises at least one of acyl glucosamine derivatives represented by the following Formula (I): | 2009-02-19 |
20090048212 | COSMETIC COMPOSITION COMPRISING AN OIL - Cosmetic composition comprising an oil The present invention relates to a composition for making up or caring for the skin in the form of a water-in-oil emulsion comprising an aqueous phase, at least 5% by weight, relative to the total weight of the composition, of a dispersed solid phase and a liquid fatty phase having at least one non-volatile fraction, the said liquid fatty phase comprising at least one first oil chosen from slow volatile oils with an evaporation rate of between 0.002 and 0.05 mg/cm | 2009-02-19 |
20090048213 | Prodrug of cinnamide compound - The present invention provides a most suitable prodrug of a cinnamide compound. The prodrug is represented by Formula (I) | 2009-02-19 |
20090048214 | Methods for Treating Renal Tumors Using 2, 4-Pyrimidinediamine Drug and Prodrug Compounds - The present disclosure provides methods for the inhibiting proliferation of tumor cells, and methods for treating solid tumor cancers in a subject by administration of 2,4-pyrimidinediamine compounds. | 2009-02-19 |
20090048215 | Compositions for Ameliorating a Reduced Higher Brain Function Resulting From Organic Brain Lesions - A composition that has an activity of ameliorating reduced higher brain functions resulting from organic brain lesions, said composition comprising arachidonic acid and/or a compound having arachidonic acid as a constituent fatty acid as well as docosahexaenoic acid and/or a compound having docosahexaenoic acid as a constituent fatty acid. | 2009-02-19 |
20090048216 | INTRAVENOUS AND ORAL DOSING OF A DIRECT-ACTING AND REVERSIBLE P2Y12 INHIBITOR - The invention provides methods and compositions for rapid and reversible inhibition of platelet aggregation in human subjects in need thereof by administering compounds of the formula: | 2009-02-19 |
20090048217 | 17Beta-CYANO-19-NOR-ANDROST-4-ENE DERIVATIVE, ITS USE AND MEDICAMENTS COMPRISING THE DERIVATIVE - The 17β-cyano-19-nor-androst-4-ene derivatives of the present invention possess gestagenic activity. They have the general chemical formula 1, in which Z is selected from the group comprising O, two hydrogen atoms, NOR and NNHSO | 2009-02-19 |
20090048218 | 17Beta-CYANO-18A-HOMO-19-NOR-ANDROST-4-ENE DERIVATIVE, ITS USE AND MEDICAMENTS COMPRISING THE DERIVATIVE - The 17β-cyano-18a-homo-19-nor-androst-4-ene derivatives of the present invention possess gestagenic activity. They have the general chemical formula 1, in which Z is selected from the group comprising O, two hydrogen atoms, NOR and NNHSO | 2009-02-19 |
20090048219 | ORGANIC NITRIC OXIDE DONOR SALTS OF NONSTEROIDAL ANTIINFLAMMATORY COMPOUNDS, COMPOSITIONS AND METHODS OF USE - The invention describes novel organic nitric oxide enhancing salts of nonsteroidal antiinflammatory drugs (NSAIDs) and novel compositions comprising at least one organic nitric oxide enhancing salt of an NSAID, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one organic nitric oxide enhancing salt of an NSAID, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating inflammation, pain and fever; (b) treating gastrointestinal disorders; (c) facilitating wound healing; (d) treating gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; (e) treating inflammatory disease states and/or disorders; (f) treating ophthalmic disorders; (h) treating peripheral vascular diseases; (i) treating diseases resulting from oxidative stress; (j) treating endothelial dysfunctions; and (k) treating diseases caused by endothelial dysfunctions. The organic nitric oxide enhancing compounds that form salts with the NSAIDs are organic nitrates, organic nitrites, nitrosothiols, thionitrites, thionitrates, NONOates, heterocyclic nitric oxide donors and/or nitroxides. The heterocyclic nitric oxide donors are furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5-imines. | 2009-02-19 |
20090048220 | DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS - Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme. | 2009-02-19 |
20090048221 | Conjugates with Anti-Inflammatory Activity - Compounds represented by Formula I: | 2009-02-19 |
20090048222 | Triaza Compound Immunoregulatory Agents - The invention provides certain macrocyclic triaza compounds which down-regulate CD4 expression for use in the treatment of autoimmune diseases and inflammatory diseases or conditions. In a specific embodiment, the invention provides certain naphthalene substituted triaza macrocycles which exhibit high activity for down regulation of CD4 expression. In particular, triaza macrocycles having dansyl groups are provided for use in pharmaceutical compositions. | 2009-02-19 |
20090048223 | Sulfonamide compound - A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; G | 2009-02-19 |
20090048224 | COMPOUNDS AND METHODS OF USE - Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes. | 2009-02-19 |
20090048225 | HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES -
The present invention provides a novel compound of Formula (I) or a pharmaceutically acceptable salt thereof, having 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. | 2009-02-19 |
20090048226 | Inhibitors of caspases - The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1β converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-γ inducing factor-(IGIF), or interferon-γ-(“IFN-γ”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-γ production and methods for treating interleukin-1, apoptosis-, and interferon-γ-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention. | 2009-02-19 |
20090048227 | Substituted-1-Phthalazinamines As Vr- 1 Antagonists - Substituted piperidine 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. | 2009-02-19 |
20090048228 | Heterocycle Derivatives As Histone Deacetylase (Hdac) Inhibitors - The present invention relates to compounds of formula I: | 2009-02-19 |
20090048229 | Methods for promoting wakefulness - The present invention relates to methods of promoting wakefulness in an individual by administering a carbamoyl ester or a pharmaceutically acceptable salt thereof. | 2009-02-19 |
20090048230 | COMPOUNDS AND COMPOSITIONS USEFUL AS CATHEPSIN S INHIBITORS - The present invention relates to the use of a 2-cyanopyrimidine compound of the formula | 2009-02-19 |
20090048231 | SUBSTITUTED PROLINAMIDES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS - The present invention provides new substituted prolinamides of the general formula (I) in which D, L, E, G, J, M, R | 2009-02-19 |
20090048233 | Enhancing the Tolerability of a Seratonin Antagonist and a NSRI, a SNRI or a RIMA by Using Them in Combination - Provided are combinations of pharmaceutical agents capable of eliciting a therapeutic effect. A first therapeutic agent in the combination has 5HT | 2009-02-19 |
20090048234 | Pharmaceutical compositions and methods for preventing, treating, or reversing neuronal dysfunction - The present invention provides compositions and methods for preventing, treating or reversing neuronal dysfunction in a mammal resulting from exposure to organophosphate nerve agents, organophosphate insecticides and incapacitating agents of the central nervous system (CNS); CNS injury, including traumatic brain injury, neurologic complications of cardiac surgery, perinatal asphyxia, and stroke, spinal cord injury, and peripheral nerve injury; and neuronal disorders associated with the loss of motor function including post-polio syndrome, amyotrophic lateral sclerosis, myasthenia gravis, Parkinson's disease and Rett syndrome; neurodegenerative disorders including Alzheimer's disease, mild cognitive impairment and schizophrenia; and cognitive impairment associated with aging. The compositions of the invention preferably comprise in effective amounts (a) at least one acetylcholinesterase inhibitor, (b) at least one compound with anticholinergic properties or both anticholinergic and antiglutamatergic properties, (c) optionally an anticonvulsive compound, and a pharmaceutically acceptable carrier. | 2009-02-19 |
20090048235 | SUBSTITUTED 5-VINYLPHENYL-1-PHENYL-PYRAZOLE CANNABINOID MODULATORS - This invention is directed to a cannabinoid modulator compound of formula (I): | 2009-02-19 |
20090048236 | NEW PHENYLALANINE DERIVATIVES - Specific phenylalanine derivatives or pharmaceutically acceptable salts thereof have an antagonistic effect on the α4 integrins and, therefore, are usable as therapeutic agents or preventive agents for diseases 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. | 2009-02-19 |
20090048237 | COMPOSITIONS AND METHODS FOR PROCEDURAL SEDATION AND ANALGESIA USING ORAL TRANSMUCOSAL DOSAGE FORMS - Dosage forms for procedural sedation and analgesia comprising the combination of an opioid such as sufentanil and a benzodiazepine such as triazolam for administration via the oral transmucosal route and methods for using the same are provided. | 2009-02-19 |
20090048238 | NOVEL BIARYL DERIVATIVES - The invention is concerned with novel biaryl derivatives of formula (I), | 2009-02-19 |
20090048239 | Therapeutic compounds - A class of macrocyclic compounds of formula (I), wherein R | 2009-02-19 |
20090048240 | Antibacterial Agents - This invention provides compositions which are 1,3-oxazinan-2-one compounds of formulae (I) and (II), and oxazolidinone compounds of formula (III): wherein R is a hydrocarbyl group, a heterocyclic group, a hydrocarbyl group having at least one substituent, or a heterocyclic group having at least one hydrocarbyl substituent, wherein the substituent on the hydrocarbyl group or heterocyclic group is selected from the group consisting of a heterocyclic group, an azo group, a cyano group, a nitro group, a fluoro group, a chloro group, a bromo group, an alkoxy group having up to 15 carbon atoms, and a hydrocarbyl group having up to 15 carbon atoms; and R′ and R″ are each independently hydrogen, an alkyl group, an aryl group, a methylaryl group, a carbonyl group, a hydrocarbylamido group, a sulfonyl group, a sulfonamoyl group, a heterocyclic group, a heterocyclic group having at least one substituent, or an aryl group or methylaryl group having at least one substituent, where the substituent on the heterocyclic group, aryl group, or methylaryl group is selected from the group consisting of a heterocyclic group, an azo group, a cyano group, a nitro group, a fluoro group, a chloro group, a bromo group, an alkoxy group having up to 15 carbon atoms, and a hydrocarbyl group having up to 15 carbon atoms. For the oxazolidinone compound of formula (HI), there is a proviso that when one of R′ or R″ is a (3-fluoro)-(4-morpholinyl)-phenyl group, the other of R′ or R″ is not an acetamido group. | 2009-02-19 |
20090048241 | Condensed Imidazole Derivatives as Aromatase Inhibitors - The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R | 2009-02-19 |
20090048242 | (1,10B-DIHYDRO-2-(AMINOALKYL-PHENYL)-5H-PYRAZOLO[1,5 C][1,3]BENZOXAZIN-5-YL)PHENYL METHANONE DERIVATIVES AS HIV VIRAL REPLICATION INHIBITORS - The present invention relates to 5H-pyrazolo[1,5-c][1,3]benzoxazin-5-yl)phenyl methanone derivatives as inhibitors of the viral replication of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present HIV inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS. | 2009-02-19 |
20090048243 | THERAPEUTIC AGENT FOR ATTENTION-DEFICIT HYPERACTIVITY DISORDER - A prophylactic and/or therapeutic drug for AD/HD, containing teniloxazine or an optical isomer thereof, or a pharmaceutically acceptable salt thereof, or a hydrate thereof, as the active ingredient. | 2009-02-19 |
20090048244 | PYRROLOTRIAZINE COMPOUNDS AS KINASE INHIBITORS - The present invention provides compounds of formula I | 2009-02-19 |
20090048245 | Imidazolopyridine compounds useful for the treatment of degenerative and inflammatory diseases - Novel imidazolopyridine compounds are disclosed that have a formula represented by the following: | 2009-02-19 |
20090048246 | COMPOUNDS, COMPOSITIONS AND METHODS FOR REDUCING LIPID LEVELS - Compositions comprising extracts or isolated or purified compounds from plants of the genus | 2009-02-19 |
20090048247 | CONDENSED ISOXALINE DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASE TYPE - IV - The present invention relates to isoxazoline derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. In particular, compounds disclosed herein can be useful in the treatment of AIDS, 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 in a patient, particularly in humans. The present invention also relates to processes for the preparation of disclosed compounds, as well as pharmaceutical compositions thereof, and their use as phosphodiesterase (PDE) type IV inhibitors. | 2009-02-19 |
20090048248 | Octahydropyrano[3,4-C]Pyrrole Tachykinin Receptor Antagonists - The present invention is directed to certain hydropyranopyrrolidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety. | 2009-02-19 |
20090048249 | 3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders - The present invention is directed to novel 3-benzoimidazolyl-pyrazolopyridine compounds of formula (I): | 2009-02-19 |
20090048250 | INDAZOLINONE COMPOSITIONS USEFUL AS KINASE INHIBITORS - The present invention provides compounds of formula I: | 2009-02-19 |
20090048251 | 4-(1H-INDAZOL-5-YL-AMINO)-QUINAZOLINE COMPOUNDS AS ERBB RECEPTOR TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF CANCER - A quinazoline derivative of the Formula I: | 2009-02-19 |
20090048252 | THIAZOLONES FOR USE AS PI3 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using substituted thiazolones. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of substituted thiazolones. | 2009-02-19 |
20090048253 | BENZENOID ANSAMYCIN DERIVATIVE - The present invention provides a benzenoid ansamycin derivative represented by Formula (I) | 2009-02-19 |
20090048254 | SALTS AND POLYMORPHS OF A VEGF-R INHIBITOR - The invention relates to salts and free base forms of N,2-dimethyl-6-[7-(2-morpholinoethoxy)quinolin-4-yloxy]benzofuran-3-carboxamide. The invention further relates to pharmaceutical compositions of these salts and free base forms and methods of treating disorders such as cancer using such compositions. | 2009-02-19 |
20090048255 | PHOSPHODIESTERASE 4 INHIBITORS, INCLUDING N-SUBSTITUTED ANILINE AND DIPHENYLAMINE ANALOGS - PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: | 2009-02-19 |
20090048256 | Pyrazole Compounds Having Cannabinoid Receptor (CB1) Antagonizing Activity - The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: | 2009-02-19 |
20090048257 | COMPOUNDS THAT MODULATE PPAR ACTIVITY, THEIR PREPARATION AND USE - Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPARδ and should be useful for treating conditions mediated by the same. | 2009-02-19 |
20090048258 | Amide Compound - The present invention relate to a compound represented by the formula (I) or (II) | 2009-02-19 |
20090048259 | Phthalazine compounds, compositions and methods of use - The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders such as cancer. | 2009-02-19 |
20090048260 | Use of pyrrolopyrazine derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells - The invention relates to the use of pyrrolopyrazine derivatives for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells, said derivatives being of formula (I): where R2 and R3 independently=H, C1-C6 straight or branched chain optionally-substituted alkyl, R6=an aromatic ring Ar or cycloalkyl, optionally substituted, said cycloalkyl optionally substituted by an aryl group which may equally be substituted, R7=H, C1-C6 alkyl, (alk.) | 2009-02-19 |
20090048261 | Pharmaceutical Composition for Treatment of Ocular Hypertension - The present invention is related to the pharmaceutical industry in general and in particular with the pharmaceutical industry of production of ophthalmic compositions. More specifically, the present invention relates to the pharmaceutical industry of production of ophthalmologic compositions for the treating of ocular hypertension. The advantage of the present invention against the present state of the technique is the fulfilling of a synergic effect of its components for the decreasing of ocular hypertension with no antagonistic effect between its components. The present invention consists of a pharmaceutical composition for the treatment of ocular hypertension characterized by comprising a pharmacologically effective amount of dorzolamide, with a pharmacologically effective amount of timolol and a pharmacologically effective amount of brimonidine. | 2009-02-19 |
20090048262 | COMBINATION OF 10-PROPARGYL-10-DEAZAAMINOPTERIN AND ERLOTINIB FOR THE TREATMENT OF NON-SMALL CELL LUNG CANCER - The present invention relates to compositions comprising a combination of 10-propargyl-10-deazaminopterin and an EGFR Kinase inhibitor, including erlotinib, for treatment of non-small cell lung cancer, and methods of treatment for non-small cell lung cancer in a patient in need thereof comprising administering for combination of 10-propargyl-10-deazaminopterin and an EGFR Kinase inhibitor, including erlotinib, for treatment of non-small cell lung cancer. | 2009-02-19 |
20090048263 | Brain/neuronal cell-protecting agent and therapeutic agent for sleep disorder - A compound represented by the formula (I) or a salt thereof; and an agent for protecting a brain/neuronal cell or a therapeutic agent for sleep disorder comprising the compound or salt: wherein Z represents an oxygen or sulfur; R | 2009-02-19 |
20090048264 | PIPERAZINE AMIDE DERIVATIVES - The invention is concerned with novel piperazine amide derivatives of formula (I) | 2009-02-19 |
20090048265 | NOVEL ANTITUMOR AGENTS AND METHODS OF THEIR USE - Antitumor compounds based on the α1-adrenoceptor antagonist, doxazosin, as well as compositions and methods of use. The disclosed compounds induce apoptosis in cancer cells. | 2009-02-19 |
20090048266 | Effects of Inhibitors of Fgfr3 on Gene Transcription - Methods of utilizing biomarkers to identify patients for treatment or to monitor response to treatment are taught herein. Alterations in levels of gene expression of the biomarkers, particularly in response to FGFR3 inhibition, are measured and identifications or adjustments may be made accordingly. | 2009-02-19 |
20090048267 | MEDICAMENTS FOR THE TREATMENT OR PREVENTION OF FIBROTIC DISEASES - The present invention relates to the use of indolinones of general formula | 2009-02-19 |
20090048268 | ANTI-HISTAMINE COMPOSITIONS AND USE THEREOF - The present invention provides for a storage stable pharmaceutical liquid solution for oral administration having a pharmaceutically effective amount of an antihistamine and having a purity equal to or greater than about 99% by weight-based HPLC assay, residual solvents of less than about 0.5%, and a total impurity of less than about 0.2%. The storage stable solution preferably contains cetirizine. The present invention further provides a process of preparing the storage stable pharmaceutical liquid solution as well as a method of treating a mammal with a therapeutically effective amount of cetirizine in the stable pharmaceutical liquid solution. | 2009-02-19 |
20090048269 | CHEMICAL COMPOUNDS-821 - The invention relates to chemical compounds of the formula (I), | 2009-02-19 |
20090048270 | Compounds, Methods And Devices for Inhibiting Neoproliferative Changes in Blood Vessel Walls - Methods, compositions and devices for inhibiting neoproliferative changes in blood vessel walls or other anatomical structures. One or more compounds of Formula I or I-A set forth herein are administered systemically and/or locally to human or veterinary patients to deter or prevent unwanted proliferative changes in blood vessels or other anatomical structures. The invention may be used to deter or prevent stenosis or restenosis of arteries following angioplasty and/or stent placement. In one embodiment, there is provided an implantable stent or stent graft from which one or more compounds of the present invention will elute or otherwise be delivered into an affected blood vessel wall. | 2009-02-19 |
20090048271 | HETEROCYCLIC COMPOUNDS AND USES AS ANTICANCER AGENTS - Novel compounds having a fused bicyclic heteroaromatic ring system substituted with a heteroaryl five-membered ring are disclosed. The compounds inhibit growth of a variety of types of cancer cells, and are thus useful for treating cancer. Efficacy of these compounds is demonstrated with a system for monitoring cell growth/migration, which shows they are potent inhibitors of growth and/or migration of cancer cells. In addition, compounds of the invention were shown to stop growth of tumors in vivo, and to reduce the size of tumors in vivo. Compositions comprising these compounds, and methods to use these compounds and compositions for treatment of cancers, are disclosed. | 2009-02-19 |
20090048272 | PREPARATION OF PALIPERIDONE - Processes for preparing paliperidone. | 2009-02-19 |
20090048273 | PREMATURE OVULATION PREVENTIVE AGENT - The present invention provides a premature ovulation inhibitor for use in in vitro fertilization or embryo transfer process, which contains a nonpeptidic compound having a gonadotropin releasing hormone antagonistic action. The premature ovulation inhibitor for use in in vitro fertilization or embryo transfer process of the present invention is low toxic, permits oral administration, and has a superior inhibitory effect on premature ovulation in in vitro fertilization or embryo transfer process. | 2009-02-19 |
20090048274 | PYRAZOLO[3,4-d]PYRIMIDINE DERIVATIVES - Disclosed are novel pyrazolo[3,4-d]pyrimidine derivatives that are inhibitors of Raf kinase. These compounds and their pharmaceutically-acceptable salts and esters are anti-proliferative agents useful in the treatment or control of proliferative disorders such as solid tumors, in particular breast tumor, colon tumor, lung tumor, prostate tumor, and melanoma. Also disclosed are a composition and a unit dose formulation comprising such a compound, or a pharmaceutically-acceptable salt or ester thereof, methods for making such compounds, and methods for using such compounds, or their pharmaceutically-acceptable salts or esters, in the treatment of proliferative disorders. | 2009-02-19 |
20090048275 | SOLID FORMS COMPRISING 4-[9-(TETRAHYDRO-FURAN-3-YL)-8-(2,4,6-TRIFLUORO-PHENYLAMINO)-9H-PURIN-2-Y- LAMINO]-CYCLOHEXAN-1-OL, COMPOSITIONS THEREOF, AND USES THEREWITH - Solid forms comprising 4-[9-(tetrahydro-furan-3-yl)-8-(2,4,6-trifluoro-phenylamino)-9H-purin-2-ylamino]-cyclohexan-1-ol, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders are disclosed. | 2009-02-19 |
20090048276 | Inhibitors of Fatty Acid Synthase (Fas) - The instant invention provides for compounds which comprise substituted 3-aryl-4-hydroxyquinolin-2(1H)-ones that inhibit FAS activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting FAS activity by administering the compound to a patient in need of treatment of cancer. | 2009-02-19 |
20090048277 | PYRIDOPYRIMIDONE DERIVATIVES, PREPARATION THEREOF, THERAPEUTIC USE THEREOF - The disclosure relates to pyrido[2,3-d]pyrimidone compounds, to the preparation thereof and to the therapeutic use thereof, wherein said compounds are of general formula (I): | 2009-02-19 |
20090048278 | Novel Quinazoline-2,4-Diamine Derivatives and Their Use as Modulators of Small-Conductance Calcium-Activated Potassium Channels - This invention relates to novel quinazoline-2,4-diamine derivatives useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention. | 2009-02-19 |
20090048279 | QUINAZOLINE ANALOGS AS RECEPTOR TYROSINE KINASE INHIBITORS - This invention provides quinazoline analogs of Formula I: | 2009-02-19 |
20090048280 | Process for the preparation of substituted phenylalanines - Intermediates and synthetic processes for the preparation of substituted phenylalanine-based compounds (e.g., of Formula I) are disclosed: | 2009-02-19 |
20090048281 | Organic Compounds - Compounds of Formula (I); in salt or zwitterionic form wherein R | 2009-02-19 |
20090048282 | PYRIMIDINE SULFONAMIDE ANALOGS AND THEIR USE AS AGONISTS OF THE WNT-BETA-CATENIN CELLULAR MESSAGING SYSTEM - The present invention relates to pyrimidine sulfonamide analogs, methods of making pyrimidine sulfonamide analogs, compositions comprising a pyrimidine sulfonamide analog, and methods for treating canonical Wnt-β-catenin cellular messaging system-related disorders comprising administering to a subject in need thereof an effective amount of a pyrimidine sulfonamide analog. | 2009-02-19 |
20090048283 | Salt of an androgen receptor modulator - The biphthalate salts of compound I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents. | 2009-02-19 |
20090048284 | THERAPEUTIC COMPOUNDS - This invention to antagonists that inhibit transporters and receptors. The invention also relates to partial inhibitors of transporters and receptors that allow partial transport or partial binding of a compound to the transporter or receptor. The invention also relates to compounds that differentially prevent transport or binding through a transporter or to a receptor. The invention also relates to the use of these compounds for treating certain diseases and disorders. | 2009-02-19 |
20090048285 | Pyrrolopyridines Useful in the Treatment of Inflammation - There is provided compounds of formula (I), wherein X | 2009-02-19 |
20090048286 | Inhibitors of Protein Tyrosine Phosphatase 1B - Protein tyrosine phosphatases (PTPases) such as PTP1B can play a role in regulating a wide variety of cellular responses such as insulin signaling. Substituted bicyclic fused-thiophene compounds can inhibit PTP1B and thereby induce greater insulin sensitivity. Accordingly, PTP1B inhibition can provide an alternate treatment for PTPase-mediated disorders such as diabetes. | 2009-02-19 |
20090048287 | Compositions useful for treating gastrointestinal motility disorders - The present invention relates to method of treating a gastrointestinal motility disorder in a subject in need of treatment comprising coadministering to said subject a first amount of a compound having 5-HT | 2009-02-19 |
20090048288 | METHOD OF TREATING STRESS-MEDIATED DEPRESSION - The present invention relates to a method for the treatment of depression comprising administering a therapeutically effective amount of gaboxadol to a patient, wherein the level of one or more inflammatory markers in said patient is increased or abnormal. The present invention also relates to a method for the treatment of stress-mediated depression comprising administering a therapeutically effective amount of gaboxadol to a patient, wherein the level of one or more inflammatory markers is increased or abnormal in said patient. The present invention also relates to a method for the treatment of depression or the amelioration of one or more depressive symptoms comprising administering a therapeutically effective amount of gaboxadol to a patient, wherein the clinical presentation of one or more symptoms of depression are the physiological effect of a general medical condition. Furthermore the present also relates to a method for testing the therapeutic effectiveness of a compound in the treatment of depression or reducing the symptoms of depression comprising measuring the amount of one or more inflammatory markers in a sample from a patient before said compound is administered to the patient and comparing with the amount of said one or more inflammatory markers in a sample from the same patient after administration of said compound to the patient. | 2009-02-19 |
20090048289 | ADMINISTRATION OF TROPISETRON FOR TREATING INFLAMMATORY SKIN DISEASES/DISORDERS - Tropisetron or salt thereof, formulated into diverse pharmaceutical/dermatological compositions, is useful for the treatment of a variety of inflammatory skin disorders/diseases, e.g., eczema, psoriasis, rosacea, acne vulgaris, ulcers, seborrhoeic dermatitis and irritations induced by chemical, physical or mechanical agents, notably rosacea. | 2009-02-19 |
20090048290 | 2S,3R)-N-(2-((3-PYRIDINYL)METHYL)-1-AZABICYCLO[2.2.2]OCT-3-YL-BENZYOFURAN-- 2-CARBOXAMIDE, NOVEL SALT FORMS, AND METHODS OF USE THEREOF - The present invention relates to (2S,3R)—N-(2-((3-pyridinyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzofuran-2-carboxamide, novel salt forms thereof, methods for its preparation, novel intermediates, and methods for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central and autonomic nervous systems. | 2009-02-19 |
20090048291 | Novel Piperidine-4-Acetic Acid Derivatives and Their Use - The present invention is directed to compounds of formula I | 2009-02-19 |
20090048292 | SYNERGISTIC COMBINATION - Pharmaceutical combinations comprising as compound A at least one compound from the group of angiogenesis inhibitors of general formula I | 2009-02-19 |
20090048293 | METHODS FOR TREATING BACILLUS INFECTION - The present invention provides compositions and methods for detecting, treating, and preventing microbial infection, especially infection caused by | 2009-02-19 |
20090048294 | HIF-1 ALPHA ACTIVATING AGENT - The present invention relates to a HIF-1α activator containing clioquinol and its derivatives as an active ingredient. Clioquinol and its derivatives of the invention inhibit HIF-1α (hypoxia-inducible factor-1α) ubiquitination in normoxic cells and thus accumulate HIF-1α. In the meantime, CQ inhibits FIH-I activity and thereby induces transcription activity of the accumulated HIF-1α, resulting in the induction of expressions of HIF-1α target genes VEGF (vascular endothelial growth factor) and EPO (erythropoietin). Therefore, clioquinol and its derivatives can be effectively used as a therapeutic agent for ischemic disease. | 2009-02-19 |
20090048295 | SUBSTITUTED 5,6,7,8-TETRAHYDROQUINOLINE DERIVATIVES, COMPOSITIONS, AND METHODS OF USE THEREOF - Substituted 5,6,7,8-tetrahydroquinoline derivatives, which are C5 | 2009-02-19 |
20090048296 | HIGH CONCENTRATION LOCAL ANESTHETIC FORMULATIONS - A transdermal topical anesthetic formulation, which can be used to ameliorate or inhibit neuropathic pain, has been developed. In the preferred embodiment, the topical anesthetic is a local anesthetic such as lidocaine, most preferably lidocaine free-base in a gel, and the dosage of the local anesthetic is effective in the painful area or immediately adjacent areas, to ameliorate or eliminate the pain. High concentration of local anesthetic in solution in the carrier is used to drive rapid release and uptake of the drug. Relief is typically obtained for a period of several hours. | 2009-02-19 |
20090048297 | 4-AMINO-4-OXOBUTANOYL PEPTIDES AS INHIBITORS OF VIRAL REPLICATION - The invention provides 4-amino-4-oxobutanoyl peptide compounds of Formula I | 2009-02-19 |
20090048298 | Novel acetyl-CoA Carboxylase (ACC) Inhibitors and their use in Diabetes, Obesity and Metabolic Syndrome - The present invention relates to compounds of formula (I) | 2009-02-19 |
20090048299 | Biphenyl compounds useful as muscarinic receptor antagonists - This invention provides compounds of formula I: | 2009-02-19 |
20090048300 | Heterocyclic Compounds - The present invention relates to compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to heterocyclic compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase (HDAC) activities. | 2009-02-19 |
20090048301 | HETEROCYCLIC COMPOUNDS AND THEIR USE AS ANTICANCER AGENTS - The present invention relates to heterocyclic compounds that have anticancer activity, and pharmaceutical compositions that contain such compounds, methods of treating diseases and conditions in mammals using such compounds and composition and methods for their manufacture. | 2009-02-19 |
20090048302 | Methods and compositions for the treatment of conditions related to gastric acid secretion - A method comprising orally administering to a mammal a proton pump inhibitor, or a pharmaceutically acceptable prodrug thereof, and a compound which modulates the activity of the MRP2 or other transporter proteins involved in efflux of a proton pump inhibitor or a prodrug, is disclosed herein, said method being effective for the prevention or treatment of a disease or condition related to gastric acid secretion. This method applied to compounds which both inhibit and stimulate MRP2 activity or activity of other transporter proteins involved in efflux of a proton pump inhibitor or a prodrug. | 2009-02-19 |
20090048303 | Indole-2-carboxamidine derivatives as nmda receptor antago - The present invention relates therefore first to new indole-2-carboxamidine derivatives of formula (I)—wherein the meaning of X is hydrogen or halogen atom, C | 2009-02-19 |
20090048304 | Crystal Form of Besipirdine Chlorhydrate, Process Preparation and Use Thereof - Crystal form of besipirdine chlorhydrate (Form I) corresponding to the Formula (A) below: the aforementioned form being characterized at least by one of the following physico-chemical properties: a) In FTIR, it displays at least the following absorption bands of the infrared spectrum: 778, 1198, 1121, but not the following absorption bands of the infrared spectrum: 3395, 1583, 732, the aforementioned bands being expressed in cm | 2009-02-19 |
20090048305 | Antimicrobial ortho-Fluorophenyl Oxazolidinones For Treatment of Bacterial Infections - The present invention provides certain ortho-fluorophenyl oxazolidinones of the following formula I: | 2009-02-19 |
20090048306 | PYRIDINE DERIVATIVES - The present invention relates to compounds of the formula (I): | 2009-02-19 |
20090048307 | 5-pyridyl-1, 3-azole compounds, process for producing the same and use there of - An optionally N-oxidized compound represented by the formula: | 2009-02-19 |
20090048308 | VLA-4 Antagonists - 4-Thio, 4-sulfinyl and 4-sulfonyl proline derivatives of the present invention are antagonists of the VLA-4 integrin and are useful in the treatment, prevention and suppression of diseases mediated by VLA-4-binding and cell adhesion and activation. Moreover, the compounds of the present invention demonstrate significant receptor occupancy of VLA-4 bearing cells after oral administration and are suitable for once-, twice-, or thrice-a-day oral administration. This invention also relates to compositions containing such compounds and methods of treatment using such compounds. | 2009-02-19 |
20090048309 | N-(2-SUBSTITUTED PHENYL)-N-METHOXYCARBAMATES AND THEIR PREPARATION AND USE THEREOF - The present invention belongs to the field of agricultural fungicide and in particular disclosed N-(2-substituted phenyl)-N-methoxycarbamates and their preparation as well as use. Compounds according to the present invention are shown as the general formula I. | 2009-02-19 |