38th week of 2012 patent applcation highlights part 49 |
Patent application number | Title | Published |
20120238538 | MACROCYCLIC AMIDES, PHARMACEUTICAL COMPOSITIONS, PREPARATION METHODS AND USES THEREOF - Macrocyclic amide WH-21091 with antibacterial and antitumor activities, its analogs, preparation methods and uses thereof. The said macrocyclic amides are prepared by microbes of | 2012-09-20 |
20120238539 | NOVEL PIPERAZINE ANALOGS AS BROAD-SPECTRUM INFLUENZA ANTIVIRALS - A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof: | 2012-09-20 |
20120238540 | AMINO-PYRIMIDINE COMPOUNDS AS INHIBITORS OF IKK EPSILON AND/OR TBK1 - The invention relates to certain amino-pyrimidine compounds that inhibit IKK epsilon and/or TBK1, methods of making such compounds, pharmaceutical compositions comprising such compounds, and the use of these compounds in treating a variety of diseases and disorders. | 2012-09-20 |
20120238541 | PHARMACEUTICAL COMPOUNDS - The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer. | 2012-09-20 |
20120238542 | AMINOPYRAZOLOQUINAZOLINES - Compounds of general formula (I) | 2012-09-20 |
20120238543 | Antiviral Compounds - Novel compounds, methods, and compositions for treating various viral infections are described. In some embodiments the novel compounds of the invention are 3-oxo-phenothiazine derivatives; more specific embodiments include 3-oxo-phenothiazine derivatives having substituents at the 1-, 7-, and 9-positions of the phenothiazine parent ring. In other embodiments, the invention provides compositions and methods for treating viral infections, especially HIV. | 2012-09-20 |
20120238544 | THIENO- AND FURO-PYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR - Thieno- and furo-pyrimidine compounds are described, which are useful as H | 2012-09-20 |
20120238545 | TRICYCLIC PYRAZOL AMINE DERIVATIVES - This invention relates to compounds of Formula (I*) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers. | 2012-09-20 |
20120238546 | GAMMA SECRETASE MODULATORS - This invention provides novel compounds that are modulators of gamma secretase. The compounds have the Formula (I): Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of Formula (I). | 2012-09-20 |
20120238547 | 2, 3, 6 - TRIAMINO SUBSTITUTED PYRIDINES AS KV7 (KCNQ) CHANNEL MODULATORS - The present application relates to novel substituted aminopyridine derivatives, to their use in therapy, to pharmaceutical compositions comprising the derivatives, to the use of said derivatives in the manufacture of a medicament, and to therapeutic methods comprising the administration of the derivatives. The present derivatives are useful for treating a disorder responsive to activation of K | 2012-09-20 |
20120238548 | 1,4-OXAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS - The present invention relates to 1,4-Oxazepines of formula I | 2012-09-20 |
20120238549 | Nuclear Hormone Receptor Modulators - The invention provides a compound of Formula (I) | 2012-09-20 |
20120238550 | COMPOUND - There is provided a compound of formula I | 2012-09-20 |
20120238551 | Substituted Phenoxypropylcycloamine Derivatives as Histamine-3 (H3) Receptor Ligands - The present invention provides compounds of formula I: | 2012-09-20 |
20120238552 | PHARMACEUTICAL COMPOSITIONS COMPRISING SORBITAN ESTERS - The present invention relates to a pharmaceutical composition comprising sorbitan esters of carboxylic acids that are useful for the delivery of anti-psychotic drugs. | 2012-09-20 |
20120238553 | NOVEL BENZODIOXOLYL-OXADIAZOLYL-DIAZABICYCLONONANE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel benzodioxolyl-oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention 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 (I). | 2012-09-20 |
20120238554 | SALTS OF POTASSIUM ATP CHANNEL OPENERS AND USES THEREOF - Provided are immediate or prolonged administration of certain salts of K | 2012-09-20 |
20120238555 | Pharmaceutical composition containing irbesartan - This invention relates to pharmaceutical compositions containing irbesartan, providing oral formulations with a high relative amount or concentration of irbesartan. In one embodiment, the present invention provides an oral formulation of irbesartan containing greater than 70% w/w irbesartan. In another embodiment, the invention provides an oral formulation of irbesartan which exhibits a dissolution profile according to which greater than about 85% of the Irbesartan is dissolved within about 30 minutes using USP apparatus 2, placing the tablet in 1000 mL of 0.1N hydrochloric acid at 37° C. with paddle speed of 50 rpm. The formulation can optionally contain at least one additional active ingredient. | 2012-09-20 |
20120238556 | CRYSTALLINE METHYLTHIONINIUM CHLORIDE HYDRATES - Three dihydrate forms B, C and D and a monohydrate form E of methylthioninium chloride are described. Forms B, C, D and E can be prepared under controlled humidity and temperature from methylthioninium chloride with higher water content or conversion of a hydrate. The hydrates can be incorporated in pharmaceutical compositions. | 2012-09-20 |
20120238557 | AMINOTHIAZINE OR AMINOOXAZINE DERIVATIVE HAVING AMINO LINKER - The present invention provide a medicament for treating the diseases induced by production, secretion or deposition of amyloid-β proteins, for example, a compound of the following formula (I) wherein R | 2012-09-20 |
20120238558 | Kinase inhibitors - The present invention relates to drug delivery systems comprising ocular implant, which include organic molecules, capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation, in combination with a polymer, which polymer serves to control, modify, modulate and/or slow the release of the therapeutic component into the environment of the eye in which said composite is placed. | 2012-09-20 |
20120238559 | NOVEL COMPOUNDS - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): | 2012-09-20 |
20120238560 | Oxazine Derivatives and their Use in the Treatment of Neurological Disorders - The invention relates to novel heterocyclic compounds of the formula | 2012-09-20 |
20120238561 | MORPHOLINOTHIAZOLES AS ALPHA 7 POSITIVE ALLOSTERIC MODULATORS - The present invention relates to morpholinothiazole derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulators having the capability to increase the efficacy of nicotinic receptor agonists. | 2012-09-20 |
20120238562 | TREATMENT OF CANCER BY TARGETING MOLECULES THAT INFLUENCE MST1/STK4 SIGNALING - The invention relates to the treatment of prostate cancer. In various embodiments, the invention teaches a method of administering one or more compounds that inhibit a molecule that antagonizes the activity of tumor suppressor Mst1 and Mst2 pathway signaling. In certain embodiments, one or more of the compounds include an mTOR and PI3K inhibitor. | 2012-09-20 |
20120238563 | NOVEL UNSATURATED TETRACYCLIC TETRAHYDROFURAN DERIVATIVES - This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT | 2012-09-20 |
20120238564 | IMIDAZO PYRAZINES - Compounds of formula | 2012-09-20 |
20120238565 | TRIAZOLOPYRIDINE COMPOUNDS AND THEIR USE AS ASK INHIBITORS - The present invention relates to triazolopyridine compounds according to Formula (I), their use as medicament, for treating autoimmune disorders, inflammatory diseases, cardiovascular diseases and/or neurodegenerative diseases and a process for their preparation. | 2012-09-20 |
20120238566 | USE OF CELL AUTOPHAGY (TYPE II CELL APOPTOSIS) INHIBITORS - Use of cell autophagy (type II cell apoptosis) inhibitors for preventing and/or treating avian influenza, injury of lungs caused by avian influenza virus or nanometer materials. The cell autophagy (type II cell apoptosis) inhibitors are selected from 3-methyladenine, SB203580, LY294002, and or wortmannin. The injury of lungs includes acute respiratory distress syndrome. The avian influenza virus is H5N1, H5N2 or H9N2 avian influenza virus. The nanometer materials include PAMAM G3, G4, G5, G5.5, G6, G7, or G8. | 2012-09-20 |
20120238567 | 4,5,6,7-TETRAHYDROBENZO[B]THIOPHENE DERIVATIVES AND THEIR USE AS SIGMA RECEPTOR LIGANDS - The present invention relates to compounds having pharmacological activity towards the sigma (σ) receptor, and more particularly to some 4, 5, 6, 7 tetrahydrobenzo[b]thiophene derivatives, wherein n is selected from 0, 1, 2, 3 or 4; m is selected from 0, 1 or 2; the dotted line represents either a single or a double bond; to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis. | 2012-09-20 |
20120238568 | Pyrido[2,3-b]pyrazin-8-substituted Compounds and Their Use - The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc. | 2012-09-20 |
20120238569 | THIAZOLE AND THIOPHENE COMPOUNDS - Provided herein are compounds of the formula (I): | 2012-09-20 |
20120238570 | INHIBITORS OF THE HEDGEHOG PATHWAY - The present invention is directed to a compound of Formula I | 2012-09-20 |
20120238571 | INDAZOLE DERIVATIVES AS PI 3-KINASE - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): | 2012-09-20 |
20120238572 | USE OF SUBSTITUTED QUINAZOLINE COMPOUNDS IN TREATING ANGIOGENESIS-RELATED DISEASES - Quinazoline derivatives of the following formula: | 2012-09-20 |
20120238573 | PRODRUGS OF [4 [4-(5-AMINOMETHYL-2-FLUORO-PHENYL)-PIPERIDIN-1-YL]-(1H-PYRROLO-PYRIDIN-YL- )-METHANONES AND SYNTHESIS THEREOF - The present invention relates to substituted 2-amino-N-(4-fluoro-3-{1-[1-(alkyl)-1H-indole-3-carbonyl]-piperidin-4-yl}-benzyl)-acetamides (compounds of formula I) | 2012-09-20 |
20120238574 | (1, 1, 1,3,3,3 -HEXAFLUORO-2 HYDROXYPROPAN- 2 -YL) PHENYL DERIVATIVE, PHARMACEUTICAL COMPOSITIONS THEREOF AND THEIR USE FOR THE TREATMENT OF ATHEROSCLEROSIS - The present invention relates to (1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl derivatives having the general formula (I) to pharmaceutical compositions comprising the same and to the use of these (1,1,1,3,3,3-hexafluoro-2-hydroxy-propan-2-yl)phenyl derivatives in the treatment of atherosclerosis. | 2012-09-20 |
20120238575 | ANTIPROLIFERATIVE PYRIMIDYL, FUSED PYRIMIDYL AND PYRIMIDYL HYDRAZONES - The present invention is related to a novel series of pyrimidyl or fused pyrimidyl hydrazones. Compounds of Formula (I) wherein A is selected from the group consisting of Formulas (A1), (A2), (A3), (A4), (A5) are useful for the treatment and/or prevention of a proliferative disease. | 2012-09-20 |
20120238576 | Triazine Derivatives and their Therapeutical Applications - The present invention comprises inter alia compounds as shown in formula (I) or a pharmaceutically acceptable salt thereof. | 2012-09-20 |
20120238577 | PROSTAGLANDIN TRANSPORTER INHIBITORS AND USES THEREOF - Disclosed are compounds for inhibiting prostaglandin transporter (PGT) activity, pharmaceuticals compositions including the compounds, and methods of treating subjects using the compounds. | 2012-09-20 |
20120238578 | COMPOSITIONS USEFUL AS INHIBITORS OF VOLTAGE-GATED SODIUM CHANNELS - The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 2012-09-20 |
20120238579 | New Compounds 806 - The present invention relates to new compounds of formula (I) and to pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof. | 2012-09-20 |
20120238580 | MALEATE SALTS OF 6-(5-CHLORO-2-PYRIDYL)-5-[(4-METHYL-1-PIPERAZINYL)CARBONYLOXY]-7-OXO-6,7-- DIHYDRO-5H-PYRROLO[3,4-b]PYRAZINE - A novel maleate salt of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro- | 2012-09-20 |
20120238581 | INHIBITORS OF DIACYLGLYCEROL O-ACYLTRANSFERASE TYPE 1 ENZYME - Compounds of formula (I), or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. | 2012-09-20 |
20120238582 | QUINAZOLINE DERIVATIVES - Novel quinazolinamide derivatives of the formula (I), in which R | 2012-09-20 |
20120238583 | PHARMACEUTICAL FORMULATIONS OF SUBSTITUTED AZAINDOLEOXOACETIC PIPERAZINE DERIVATIVES WITH PROTEASE INHIBITORS - This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. | 2012-09-20 |
20120238584 | 5-HT1A receptor subtype agonist - The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT | 2012-09-20 |
20120238585 | FATTY ACID ACETYLATED SALICYLATES AND THEIR USES - The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative. | 2012-09-20 |
20120238586 | FATTY ACID ACETYLATED SALICYLATES AND THEIR USES - The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative. | 2012-09-20 |
20120238587 | NOVEL PYRIDOPYRIMIDINE DERIVATIVES AND USE THEREOF - The invention provides novel substituted pyridopyrimidines represented by Formula I or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of the phosphoinositide 3′ OH kinase family (PI3K) for the treatment of inflammatory diseases, cancer, cardiovascular diseases, allergy, asthma and autoimmune disorders. | 2012-09-20 |
20120238588 | 1H-Pyrrolo[2,3-B]Pyridines - Derivatives of pyrrolo[2,3-b]pyridine which are useful as SGK-1 kinase inhibitors are described herein. The invention described herein also describes pharmaceutical compositions containing derivatives of pyrrolo[2,3-b]pyridine and methods of using pyrrolo[2,3-b]pyridine derivatives and pharmaceutical compositions thereof in the treatment of diseases mediated by SGK-1. | 2012-09-20 |
20120238589 | ORGANIC COMPOUNDS - 1- or 2-substituted (6aR,9aS)-3-(phenylamino)-5-6a,7,8,9,9a-hexahydro-5-methyl-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(1H or, 2H)-one compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them. | 2012-09-20 |
20120238590 | COMPOSITIONS FOR TREATING CANCER-RELATED FATIGUE AND METHODS OF SCREENING THEREOF - An animal model has been developed based the understanding that a central mechanism in patients with CTRF is that chemotherapy and/or radiation initiates canonical pathways leading to the development of disrupted sleep architecture, resulting in disruption of REM sleep and fatigue and cognitive dysfunction. Drugs that restore the activity patterns and levels towards normal and/or decrease the pro-inflammatory cytokines associated with the disrupted sleep, should be effective in alleviating one or more symptoms of CTRF. Pentoxifylline was demonstrated to improve activity levels in animals treated with etoposide. | 2012-09-20 |
20120238591 | ACYCLOVIR FORMULATIONS - The present invention relates to acyclovir formulations having improved bioavailability resulting in better efficacy and/or requiring less frequent administration. | 2012-09-20 |
20120238592 | Use and Application of a Pharmaceutical Composition Containing a Mixture of Natural-Origin Heterocylcial Guanidine - Pharmaceutical compositions comprising tricyclic 3,4-propinoperhydropurines and uses thereof for the treatment of facial wrinkling are provided. | 2012-09-20 |
20120238593 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 2012-09-20 |
20120238594 | AZASPIRODECANONE COMPOUNDS - The invention provides novel compounds having the general formula (I) | 2012-09-20 |
20120238595 | THERAPEUTIC COMPOUNDS - The invention provides compounds of formula (I) wherein u, d, v, m, n, R | 2012-09-20 |
20120238596 | FORMULATIONS COMPRISING PALONOSETRON - Pharmaceutical compositions comprising palonosetron and its pharmaceutically acceptable salts, in the form of a ready-to-use solution or a lyophilized form. Specific embodiments of the invention relate to stable pharmaceutical formulations of palonosetron and its pharmaceutically acceptable salts, wherein the formulation does not comprise a chelating agent or an antioxidant. | 2012-09-20 |
20120238597 | Inhibiting EPH B-3 Kinase - EphB3 kinase inhibitor compounds, including certain pyrazolo[1,5-a]pyridine and imidazo[1,2-a]pyridine compounds, inhibit EphB3 kinase. The EphB3 kinase inhibitor compounds can have greater potency for the inhibition of EphB3 kinase than general kinase inhibitors. Pharmaceutical compositions, such as neuroprotective agents, comprising the EphB3 kinase inhibitor compounds are also provided. The EphB3 kinase inhibitor compounds and pharmaceutical compositions are useful, for example, to provide neuroprotection and/or repair of neuronal tissue damaged during an ischemic event, such as a stroke. | 2012-09-20 |
20120238598 | DERIVATIVES OF 7 ALKYNYL-1,8 NAPHTHYRIDONES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS - The disclosure relates to method of treating a disease in which VEGFR-3 is involved, comprising administering a therapeutically effective amount of a compound of the formula | 2012-09-20 |
20120238599 | HETEROCYCLIC COMPOUNDS AS MEK INHIBITORS - The invention provides novel substituted heterocyclic compounds represented by Formula I and Formula II, or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans. | 2012-09-20 |
20120238600 | TROPINONE BENZYLAMINES AS BETA-TRYPTASE INHIBITORS - The present invention discloses and claims a series of substituted tropinone benzylamines of formula (I): | 2012-09-20 |
20120238601 | TREATMENT OF CANCER - The present invention provides compositions of matter, kits and methods for their use in the treatment of cancer. In particular, the invention provides compositions and methods for treating cancer in a subject by inhibiting a poly-ADP-ribose polymerase, as well as providing formulations and modes of administering such compositions. | 2012-09-20 |
20120238602 | PIPERIDINE SULPHONAMIDE DERIVATIVES - The present invention relates to piperidine sulphonamide derivatives of formula | 2012-09-20 |
20120238603 | TREATMENT FOR INFLAMMATORY BOWEL DISEASE - The present invention relates to a method for the treatment of an inflammatory bowel disease by the administration of the compound [4-(5-aminomethyl-2-fluorophenyl)piperidine-1-yl][7-fluoro-1-(2-methoxyethyl)-4-trifluoromethoxy-1H-indol-3-yl]methanone, which may be represented as Formula I: | 2012-09-20 |
20120238604 | CYTOTOXIC COMPOUNDS - The present invention relates to a compound of general formula (I) or a pharmaceutically acceptable salt or solvate or thereof. In particular, the present invention relates to a method treating diseases involving cell proliferation, migration, apoptosis, or adhesion, comprising administering to a human or non-human mammalian patient an effective amount of a compound of general formula (I) or a pharmaceutically acceptable salt or solvate or thereof. | 2012-09-20 |
20120238605 | OTAMIXABAN FOR TREATMENT OF ELDERLY AND RENAL IMPAIRED NON-ST ELEVATION MYOCARDIAL INFARCTION PATIENTS - The invention relates to the use of (2R,3R)-2-(3-carbamimidoyl-benzyl)-3-[4-(1-oxy-pyridin-4-yl)benzoylamino]-butyric acid methyl ester or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for use in non-ST elevation myocardial infarction, said treatment comprising administering a therapeutically effective amount of (2R,3R)-2-(3-Carbamimidoyl-benzyl)-3-[4-(1-oxy-pyridin-4-yl)benzoylamino]-butyric acid methyl ester or a pharmaceutically acceptable salt thereof to a human patient, who is elderly and/or shows renal insufficiency and/or has a low body weight. | 2012-09-20 |
20120238606 | AZILSARTAN ORGANIC AMINE SALTS, PREPARATION METHOD AND USE THEREOF - Azilsartan amine salts, their preparation and method of use are disclosed. Specifically, azilsartan amine salts represented by formula (I), their preparation, pharmaceutical compositions containing a therapeutically effective amount of the compounds and their use for treating hypertension are disclosed. | 2012-09-20 |
20120238607 | SUBSTITUTED 2-ACETAMIDO-5-ARYL-1,2,4-TRIAZOLONES AND USE THEREOF - The present application relates to new, substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders. | 2012-09-20 |
20120238608 | ANGIOTENSIN II RECEPTOR ANTAGONISTS - A compound having the structure wherein R is, for example, Y is selected from the group consisting of 1) R5, 2) —C(R1R2) (C(R3R4))0-1Y1R5, and 3) —C(R1R2)—O—Y1R5; R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is; Y1 is selected from the group consisting of C(O)—O— and P(O)(OR6)—O—; and R6 is hydrogen or CH3, or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension. | 2012-09-20 |
20120238609 | Methods for Treating COPD - Embodiments of the invention include methods and compositions involving aldose reductase inhibitors for treating COPD. | 2012-09-20 |
20120238610 | Use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune/inflammatory diseases associated with toll-like receptor overexpression - Treatment of autoimmune and/or inflammatory diseases associated with overexpression of Toll-like receptor 3 (TLR3) as well as Toll-like receptor 4 (TLR4) and/or TLR3/TLR4 signaling in nonimmune cells, monocytes, macrophages, and/or dendritic cells in association with related pathologies. The use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune and inflammatory diseases associated with TLR3 as well as TLR4 and/or TLR3/TLR4 cellular signaling in association with related pathologies is disclosed. Methods of treating a subject having a disease or condition associated with abnormal TLR-3 as well as TLR-4 and/or TLR3/TLR4 cellular signaling in association with related pathologies are also disclosed. The present disclosure also relates to the treatment of autoimmune-inflammatory pathologies and chemokine and cytokine-mediated diseases associated with TLR overexpression and signaling. The disclosure also relates to pharmaceutical formulations capable of inhibiting the IRF-3/Type 1 IFN/STAT/ISRE/IRF-1 pathway associated with Toll-like receptor overexpression or signaling. | 2012-09-20 |
20120238611 | DUAL-ACTING BENZOIMIDAZOLE ANTIHYPERTENSIVE AGENTS - The invention relates to compounds having the formula: | 2012-09-20 |
20120238612 | POLYMORPHS OF ELTROMBOPAG AND ELTROMBOPAG SALTS AND PROCESSES FOR PREPARATION THEREOF - New polymorphs of Eltrombopag and Eltrombopag ethanolamine salt have been obtained and characterized. These polymorphs and pharmaceutical compositions comprising them are useful, for example, in treating conditions leading to thrombocytopenia. | 2012-09-20 |
20120238613 | SEC-HYDROXYCYCLOHEXYL DERIVATIVES - The invention provides novel compounds having the general formula (I) | 2012-09-20 |
20120238614 | ANTICONVULSANT COMBINATION THERAPY - The present invention is directed to a pharmaceutical composition comprising a Compound (a) of a class of peptide Compounds and at least one further Compound (b) for the prevention, alleviation or/and treatment of epileptic seizures. | 2012-09-20 |
20120238615 | Alpha adrenergic receptor modulators - Compounds are described herein useful for treating diseases and conditions by modulation of one or more alpha adrenergic receptor, in particular the alpha 2C receptor. The compounds can include N-(2,3-substituted phenyl)-3,4-dihydro-2H-pyrrol-5-amine derivatives. Methods of making, using and formulating these compounds are described | 2012-09-20 |
20120238616 | METHODS AND COMPOSITIONS FOR TREATING SLEEP-RELATED BREATHING DISORDERS - Provided herein are methods of treating a sleep-related breathing disorder, such as obstructive sleep apnea, comprising the administration of O-desmethylvenlafaxine or duloxetine. | 2012-09-20 |
20120238617 | MICRORNA EXPRESSION SIGNATURE IN PERIPHERAL BLOOD OF PATIENTS AFFECTED BY HEPATOCARCINOMA OR HEPATIC CIRRHOSIS AND USES THEREOF - A method for diagnosing or prognosticating hepatocellular carcinoma, also in the early stages, or for assessing the risk of developing hepatocellular carcinoma, or for monitoring the effectiveness of an anti-tumour therapy against hepatocellular carcinoma by measuring the expression level of at least one miRNA gene product in a peripheral blood sample or in a biological fluid sample. Said method comprises measuring, in an isolated sample of peripheral blood or biological fluid, the expression level of at least one miRNA gene product, and comparing said measured expression level with a reference level. Such method can also be used to diagnose or assess the risk of developing liver cirrhosis in patients affected by chronic hepatitis, or to prognosticate the evolution of cirrhosis in patients affected by cirrhosis, or to monitor the effectiveness of a pharmacological therapy against liver cirrhosis. | 2012-09-20 |
20120238618 | Pharmaceutical Composition Comprising Anti-miRNA Antisense Oligonucleotides - The invention provides pharmaceutical compositions comprising short single stranded oligonucleotides, of length of between 8 and 26 nucleobases which are complementary to human microRNAs selected from the group consisting of miR19b, miR21, miR122a, miR155 and miR375. The short oligonucleotides are particularly effective at alleviating miRNA repression in vivo. It is found that the incorporation of high affinity nucleotide analogues into the oligonucleotides results in highly effective anti-microRNA molecules which appear to function via the formation of almost irreversible duplexes with the miRNA target, rather than RNA cleavage based mechanisms, such as mechanisms associated with RNaseH or RISC. | 2012-09-20 |
20120238619 | MICRO-RNA FOR THE REGULATION OF CARDIAC APOPTOSIS AND CONTRACTILE FUNCTION - The present invention relates to treating or preventing age-related cardiomyopathy by modulating the expression or activity of a miR-34 family member and/or PNUTS. Methods of treating or preventing age-related cardiomyopathy include administering an inhibitor of miR-34 expression or activity or an agonist of PNUTS expression or activity. Also provided herein are methods of treating or preventing cardiac fibrosis and myocardial infarction by administering an inhibitor of miR-34 expression or activity or an agonist of PNUTS expression or activity. | 2012-09-20 |
20120238620 | TRYPTOPHANYL-tRNA SYNTHETASE-DERIVED POLYPEPTIDES USEFUL FOR THE REGULATION OF ANGIOGENESIS - The invention provides an isolated nucleic acid encoding a polypeptide capable of inhibiting angiogenesis or neovascularization, wherein the nucleic acid comprises a first polynucleotide sequence comprising a coding sequence at least 95 percent identical to a sequence selected from the group consisting of a polynucleotide SEQ ID NO:6, a polynucleotide that encodes a polypeptide of SEQ ID NO:12, and a polynucleotide that encodes a fragment of the polypeptide of SEQ ID NO:12; and wherein the nucleic acid does not encode for the amino acid sequence of amino acids 71-93 of SEQ ID NO:1. Pharmaceutical compositions, vectors, and methods for inhibiting neovascularization or angiogenesis comprising or utilizing the nucleic acids also are provided. | 2012-09-20 |
20120238621 | Oligomer-Calcimimetic Conjugates and Related Compounds - The invention relates to (among other things) oligomer-calcimimetic conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds. | 2012-09-20 |
20120238622 | IRON (III) CITRATE, SUBSTANTIALLY FREE OF BETA-IRON HYDROXIDE OXIDE - This invention provides a method for producing high-purity iron(III) citrate substantially free of beta-iron hydroxide oxide, high-purity iron(III) citrate substantially free of beta-iron hydroxide oxide, and medical uses thereof. | 2012-09-20 |
20120238623 | Inflammation and Autoimmune Disorder Treatment using RARa Selective Agonists - The present specification provides compounds, compositions and methods using such compounds and compositions to treat an autoimmune disorder, inflammation and/or a transplant rejection. | 2012-09-20 |
20120238624 | FORMULATIONS FOR THE TREATMENT OF PAIN - Formulations and methods are provided for the treatment of pain, and neuropathic pain in particular. The formulations are eutectic mixtures of a capsaicinoid and a local anesthetic agent and/or an anti-pruritic agent. | 2012-09-20 |
20120238625 | BIOLOGICALLY ACTIVE OILS - A process for the production of fats or oils and their extracts containing biologically active chemical compounds from a lipid substrate, the process comprising: a) inoculation of a lipid substrate with fungally derived lipolytic enzymes; b) incubating the inoculated substrate for a period of between about 7-120 days at a temperature of between about 4-35° C., at a humidity of between about 75-100%, and c) processing said substrate mixture to obtain a biologically active fat or oil. | 2012-09-20 |
20120238626 | Methods and compositions for promoting the respiratory development of an infant - The present invention relates to methods for promoting respiratory development, reducing the incidence of respiratory distress, bronchopulmonary dysplasia and/or hayfever in an infant by administration of fatty acids and compositions comprising same, wherein the fatty acids are enriched with respect to docosahexaenoic acid (DHA) content. | 2012-09-20 |
20120238627 | N-ACETYL-L-CYSTEINE FOR THE TREATMENT OF ENDOMETRIOSIS - The invention relates to a new prescription of NAC in the treatment of endometriosis and of indications associated with endometriosis, in a human or mammalian animal patient. In addition an effective dose regimen of NAC in the treatment of endometriosis is proposed. In one embodiment of the present invention the prescribed treatment regimen may be used e.g. in order to control the frequency and the intensity of pain symptoms (dysmenorrhea, dyspareunia and acyclic chronic pelvic pain), to reduce the size of endometriotic lesions eventually up to their disappearance, to reduce recurrences after surgery and/or to improve fertility. Side effects of this treatment are virtually absent and, in particular, this treatment does not hinder pregnancy. | 2012-09-20 |
20120238628 | DIHYDRONAPHTHALENE AND NAPHTHALENE DERIVATIVES AS N-FORMYL PEPTIDE RECEPTOR LIKE-1 (FPRL-1) RECEPTOR MODULATORS - The present invention relates to novel dihydronaphthalene and naphthalene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor. | 2012-09-20 |
20120238629 | ADDITION COMPOUNDS OF GUANIDINOACETIC ACID - The present invention provides new addition compounds of guanidinoacetic acid with malic acid, aspartic acid, ascorbic acid, succinic acid, pyruvic acid, fumaric acid, gluconic acid, alpha-ketoglutaric acid, pyroglutamic acid, 3-nicotinic acid, lactic acid, citric acid, maleic acid, acetic acid, formic acid, 2-hydroxybenzoic acid, L-carnitine, acetyl-L-carnitine, taurine, betaine, choline, methionine and lipoic acid as well as in the form of sodium, potassium or calcium guanidinoacetate. These addition compounds have improved physiological and therapeutic properties and are particularly suitable for use as dietary supplements, as animal feeds and in cosmetic or dermatological preparations in which especially the marked stability and good bioavailability of the addition compounds come to the fore. | 2012-09-20 |
20120238630 | COMPOSITIONS COMPRISING NONSTEROIDAL ANTI - INFLAMMATORY DRUGS - The present invention describes liquid compositions comprising pharmaceutically active principles, like scarcely water-soluble, nonsteroidal anti-inflammatory drugs, in particular, but not exclusively, flurbiprofen (FP), processes for their manufacture and their therapeutic use. The liquid compositions comprising FP in association with natural polymers, like xyloglucans (XG), and pharmaceutically acceptable excipients like glycerol, are suitable to be used for pharmaceutical uses and are characterized by good tolerability, therapeutic efficacy, stability and palatability. | 2012-09-20 |
20120238631 | COMPOSITIONS COMPRISING CYCLOHEXYLAMINES AND AMINOADAMANTANES - The invention is directed to formulations of pharmaceutical compounds, such as the Cyclohexylamines and Aminoadamantanes which have antimicrobial properties. In particular, it is directed to aqueous based formulations with reduced amounts of preservatives which allow safe and convenient administration and flexible dosing and which, in the case of oral formulations, are easy to swallow. Optionally, the compositions contain components that provide the requisite stability and shelf life while reducing or avoiding incrustation of the composition around the container closure which leads to leaks and difficulty in opening the container. | 2012-09-20 |
20120238632 | MODULATORS OF RETINOL-RETINOL BINDING PROTEIN (RBP)-TRANSTHYRETIN (TTR) COMPLEX FORMATION - Described herein are methods and compositions for the detection of transthyretin (TTR), retinol binding protein (RBP) and retinol complex formation. The methods and compositions described herein also provide for the screening of modulators of retinol-RBP-TTR complex formation. Furthermore, the methods and compositions provide for therapeutic agents for the treatment and/or prevention of age-related macular degeneration and/or dystrophies. | 2012-09-20 |
20120238633 | HYPOTENSIVE LIPID-CONTAINING BIODEGRADABLE INTRAOCULAR IMPLANTS AND RELATED METHODS - Biocompatible intraocular implants include a prostamide component and a biodegradable polymer that is effective in facilitating release of the prostamide component into an eye for an extended period of time. The prostamide component may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants may be placed in an eye to treat or reduce a at least one symptom of an ocular condition, such as glaucoma. | 2012-09-20 |
20120238634 | INTERLEUKIN-1 AND TUMOR NECROSIS FACTOR-ALPHA MODULATORS; SYNTHESES OF SUCH MODULATORS AND METHODS OF USING SUCH MODULATORS - Described herein are chemical compounds and pharmaceutical compositions, including novel chemical compounds and pharmaceutical compositions thereof, useful in the treatment of various diseases and disease states. Also described are methods of synthesizing natural products and novel, structurally-related chemical compounds. More particularly, disclosed are new analogs of and processes for the preparation of compounds and pharmaceutical compositions thereof useful in the treatment of, for example, inflammation, cancer, multiple myeloma, cachexia, cardiovascular disease, anti-infectious, diabetes, otitis media, sinusitis and transplant rejection. | 2012-09-20 |
20120238635 | Antiseptic Solution of Di(4-Chloro-Phenyldiguanido) Compound and Process Therefor - The present invention relates to a stable antiseptic solution comprising: a di(4-chlorophenyldiguanido) compound or a pharmaceutically acceptable salt thereof, wherein said di(4-chlorophenyldiguanido) compound or a pharmaceutically acceptable salt thereof is a compound of formula (I) or a pharmaceutically acceptable salt thereof. The invention further relates to a process for preparing said antiseptic solution. | 2012-09-20 |
20120238636 | RASAGILINE ORALLY DISINTEGRATING COMPOSITIONS - This invention provides a solid pharmaceutical composition comprising rasagiline or a pharmaceutically acceptable salt of rasagiline, and particles having a non-filamentous microstructure of at least two sugar alcohols. This invention also provides a solid pharmaceutical composition comprising rasagiline or a pharmaceutically acceptable salt of rasagiline, a mixture of a disintegrant, a flow agent and particles having a non-filamentous microstructure of at least two sugar alcohols, a supplemental sugar alcohol, a supplemental flow agent, and a supplemental disintegrant. This invention further provides a method of treating a subject afflicted with Parkinson's disease comprising administering to the subject a therapeutically effective amount of the solid pharmaceutical composition, thereby treating the subject. Finally, this invention provides a process of making such solid pharmaceutical compositions. | 2012-09-20 |
20120238637 | Isolated Extract of Walnuts, Method For Its Obtention And Its Use - The invention refers to an isolated extract of walnuts of high efficiency and stability over time useful for the manufacture of a medicament for the treatment of viral, fungal and bacterial diseases, which is characterized in that it is obtained from a process comprising: i) collecting unripe walnut fruits as raw material; ii) preparing the raw material for the extraction, iii) freezing the raw material prepared in the previous step; iv) drying; v) extracting in a time lower than 10 minutes; vi) filtration; and vii) final packaging. The invention also refers to its use for manufacturing a medicament for the treatment of bacterial, fungal and viral diseases and to a composition comprising it. | 2012-09-20 |