32nd week of 2012 patent applcation highlights part 43 |
Patent application number | Title | Published |
20120202797 | SUBSTITUTED [(5H-PYRROLO[2,1-c][1,4]BENZODIAZEPIN-11-YL)PIPERAZIN-1-YL]-2,2-DIMETHYLP- ROPANOIC ACID COMPOUNDS AS DUAL ACTIVITY H1 INVERSE AGONISTS/5-HT2A ANTAGONISTS - A dual H1/5-HT | 2012-08-09 |
20120202798 | COMPOSITIONS CONTROLLING pH RANGE OF RELEASE AND/OR RELEASE RATE - The present invention provides a composition controlling a pH range of release and/or a release rate, which contains (i) a thienotriazolodiazepine compound of the formula (I) | 2012-08-09 |
20120202799 | Condensed Azepine Derivatives As Bromodomain Inhibitors - Benzodiazepine compounds of formula (I) | 2012-08-09 |
20120202800 | DUAL SMALL MOLECULE INHIBITORS OF CANCER AND ANGIOGENESIS - The present invention provides analogs and derivatives of thalidomide which inhibit cancer and angiogenesis. The present invention further provides compounds which disrupt microtubule polymerization. The present further provides methods of treating cancers comprising mutant p53. | 2012-08-09 |
20120202801 | METHODS FOR TREATING BREAST CANCER - Methods for treating breast cancer involving the administration of a compound that selectively inhibits pathological production of human vascular endothelial growth factor (VEGF) are described. The compound can be administered as a single agent therapy or in combination with one or more additional therapies to a human in need of such treatment. | 2012-08-09 |
20120202802 | SPIROCYCLIC COMPOUNDS AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY - The present application describes modulators of chemokine receptor activity of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed. | 2012-08-09 |
20120202803 | N-[3-(5-AMINO-3,3A,7,7A-TETRAHYDRO-1H-2,4-DIOXA-6-AZA-INDEN-7-YL)-PHENYL]-- AMIDES AS BACE1 AND/OR BACE2 INHIBITORS - The present invention relates to N-[3-(5-Amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides of formula I | 2012-08-09 |
20120202804 | FUSED AMINODIHYDRO-OXAZINE DERIVATIVES - A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C | 2012-08-09 |
20120202805 | PI3K (delta) SELECTIVE INHIBITORS - Novel PI3K, especially PI3K delta isoform, selective inhibitors are disclosed. The compounds are useful in treating disorders related to abnormal PI3K or PI3Kδ activities such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. | 2012-08-09 |
20120202806 | Novel Pyrimidine- And Triazine-Hepcidine Antagonists - The present invention relates to new hepcidin antagonists, pharmaceutical compositions containing them and the use thereof as a drug, in particular for the treatment of iron metabolism disorders such as, in particular, iron deficiency diseases and anaemia, in particular anaemia associated with chronic inflammatory disease (ACD: anaemia of chronic disease and AI: anaemia of inflammation). | 2012-08-09 |
20120202807 | AZABICYCLOALKANE DERIVATIVES, PREPARATION THEREOF AND USE THEREOF IN THERAPY - The invention relates to compounds of the general formula (I): | 2012-08-09 |
20120202808 | NOVEL THIOPHENEDIAMINE DERIVATIVE HAVING UREA STRUCTURE - A compound of formula (1): | 2012-08-09 |
20120202809 | NOVEL N-PYRIMIDIN-4-YL-3-AMINO-PYRROLO[3,4-C]PYRAZOLE DERIVATIVES AS PKC KINASE INHIBITORS - The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: | 2012-08-09 |
20120202810 | SUBSTITUTED 4-AMINOCYCLOHEXANE DERIVATIVES - The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions. | 2012-08-09 |
20120202811 | NOVEL COMPOUNDS - Compounds of formula (I) | 2012-08-09 |
20120202812 | HETEROARYLS AND USES THEREOF - This invention provides compounds of formula I: | 2012-08-09 |
20120202813 | TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound. | 2012-08-09 |
20120202814 | COMPOUNDS WITH DDX3 INHIBITORY ACTIVITY AND USES THEREOF - The present invention relates to the medical use of the compound of formula 1, 2, 3 or 4: | 2012-08-09 |
20120202815 | HETEROBICYCLE-SUBSTITUTED AZOLYL BENZENE FUNGICIDES - Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, | 2012-08-09 |
20120202816 | NOVEL COMPOUNDS - The present invention discloses a novel thyroid like compounds of formula (I), wherein R | 2012-08-09 |
20120202817 | COMPOUNDS HAVING 4-PYRIDYLALKYLTHIO GROUP AS A SUBSTITUENT - A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: | 2012-08-09 |
20120202818 | UREIDOPHENYL SUBSTITUTED TRIAZINE DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS - The present invention provides Uredophenyl substituted triazine derivatives and provides methods of using these compounds to modulate protein kinases and methods of using these compounds to treat protein kinase mediated diseases and conditions. | 2012-08-09 |
20120202819 | COMBINATION THERAPY USING A BETA 3 ADRENERGIC RECEPTOR AGONISTS AND AN ANTIMUSCARINIC AGENT - Described herein is an improved method of treating overactive bladder, wherein the method comprises administering to a patient in need thereof a beta 3 adrenergic receptor agonist, an antimuscarinic agent, and an optional selective M | 2012-08-09 |
20120202820 | PHARMACEUTICAL COMPOSITION HAVING THE ACTIVE SUBSTANCES METFORMIN AND SITAGLIPTIN OR VILDAGLIPTIN - The present invention relates to a pharmaceutical composition that comprises the active substance metformin in combination with one of the active substances sitagliptin or vildagliptin. The present invention further relates to a method of production of said pharmaceutical composition. | 2012-08-09 |
20120202821 | CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS - Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT | 2012-08-09 |
20120202822 | COMBINATION - The present invention relates to a method of treating cancer in a mammal and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a novel combination comprising the MEK inhibitor: N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethy; -2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, and the PI3 kinase inhibitor: 2,4-difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl}benzenesulfonamide, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same, and methods of using such combinations in the treatment of cancer. | 2012-08-09 |
20120202823 | Multi-API Loading Prodrugs - The present invention accomplishes this by having multiple molecules of parent drugs attached to carrier moieties and by extending the period during which the parent drug is released and absorbed after administration to the patient and providing a longer duration of action per dose than the parent drug itself. Prodrug conjugates are suitable for sustained delivery of heteroaryl, lactam- amide-, imide-, sulfonamide-, carbamate-, urea-, benzamide-, acylaniline-, cyclic amide- and tertiary amine-containing parent drugs that are substituted at the amide nitrogen or oxygen atom with labile aldehyde-linked prodrug moieties. The carrier groups of the prodrugs can be hydrophobic to reduce the polarity and solubility of the parent drug under physiological conditions. | 2012-08-09 |
20120202825 | Soluble Salts of Thieno [2,3-d] Pyrimidine Derivatives - The present invention is directed to novel salts of thieno[2,3-d]pyrimidine derivatives, including 4-(2-fluorophenyl)-6-methyl-2-(piperazin-1-yl)thieno[2,3-d]pyrimidine salts. The present invention is also directed to compositions including such polymorphs and methods for using such salts, e.g., in the treatment of gastrointestinal and/or genitourinary disorders. | 2012-08-09 |
20120202826 | Tetrahydropyrrolopyrimidinediones And Their Use In Therapy - The subject invention provides compounds of formula (I): | 2012-08-09 |
20120202827 | SULFOXIDE DERIVATIVES FOR THE TREATMENT OF TUMORS - Sulfoxide derivatives of the formula Ia to Im as described, and pharmaceutically usable salts, solvates, enantiomers, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for the treatment of tumours. | 2012-08-09 |
20120202828 | FUSED AMINODIHYDROPYRIMIDONE DERIVATIVES - A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C | 2012-08-09 |
20120202829 | 6-Cycloalkyl-pyrazolopyrimidinones for the Treatment of CNS Disorders - The invention relates to novel 6-Cycloalkyl-pyrazolopyrimidinones according to formula (I). | 2012-08-09 |
20120202830 | SUBSTITUTED XANTHINE DERIVATIVES - This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial. | 2012-08-09 |
20120202831 | Pharmaceutical Formulation - The invention relates to a pharmaceutical formulation including, as an active principle, the compound of formula (I) | 2012-08-09 |
20120202832 | KINASE INHIBITORS, PRODRUG FORMS THEREOF AND THEIR USE IN THERAPY - The invention provides kinase inhibitors of Formula I: | 2012-08-09 |
20120202833 | TRICYCLIC PYRAZOLOPYRIMIDINE DERIVATIVES - A pyrazolopyrimidine compound represented by formula (1) that inhibits the function of HSP90 as a chaperone protein and that has antitumor activity, a medicament comprising a compound represented by formula (1), a pharmaceutical composition comprising a compound represented by formula (1), and a method for treating cancer using a compound represented by formula (1). | 2012-08-09 |
20120202834 | GLUCAGON RECEPTOR MODULATORS - The present invention provides a compound of Formula (I) | 2012-08-09 |
20120202835 | COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof. | 2012-08-09 |
20120202836 | METHOD OF TREATING PROLIFERATIVE DISORDERS AND OTHER PATHOLOGICAL CONDITIONS MEDIATED BY BCR-ABL, C-KIT, DDR1, DDR2 OR PDGF-R KINASE ACTIVITY - The present invention relates to a regimen for the administration of a pyrimidylaminobenzamide of formula I as defined herein for the treatment of proliferative disorders, particularly solid and liquid tumors, and other pathological conditions mediated by the Bcr-AbI oncoprotein, the cell transmembrane tyrosine kinase receptor c-Kit, DDR1 (discoidin domain receptor 1), DDR2 (discoidin domain receptor 2) or PDGF-R (platelet derived growth factor receptor) kinase activity. | 2012-08-09 |
20120202837 | SPIROCYCLIC PIPERIDINE DERIVATIVES USEFUL AS RENIN INHIBITORS - Renin inhibitors which are spirocyclic piperidine derivatives, of formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof, wherein: n, for each instance in which it occurs, is independently 0, 1, or 2; W is a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring, A is (i) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring or (ii) a first five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring which is fused to a second five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring, V is —(C═O)—, —CH | 2012-08-09 |
20120202840 | Use of Flubendazole and Vinca Alkaloids for Treatment of Hematological Diseases - Provided are methods for treating a hematological malignancy comprising administering an effective amount of flubendazole alone or in combination with a vinca alkaloid. Also provided are compositions and kits comprising an effective amount of flubendazole and/or a vinca alkaloid for use in the methods of the disclosure. | 2012-08-09 |
20120202841 | Topical Compositions Comprising Ascomycins - The present invention relates to a composition for topical administration comprising an ascomycin and a carrier vehicle comprising means to retain water in the outer skin layer and means to hinder water evaporating from the skin. | 2012-08-09 |
20120202842 | 2-HETEROARYLCARBOXYLIC ACID AMIDES - The invention relates to novel 2-heteroarylcarboxamides, processes for their preparation, and their use for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory. | 2012-08-09 |
20120202843 | H3K27me3 and Cancer - Methods of diagnosing and monitoring cancers and precancerous lesions associated with human papillomavirus (HPV), by detecting abnormal levels of lysine (K)-specific demethylase 6A (KDM6A), KDM6B, or trimethylated Histone H3 Lys27 (H3K27me3). | 2012-08-09 |
20120202844 | Crystal Forms of Kinase Inhibitors - Citrate salts of N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N′-(3-fluorophenyl)urea and crystalline forms thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer. | 2012-08-09 |
20120202845 | DIURETICS - A compound having the structure formula (I) or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension. | 2012-08-09 |
20120202846 | MOLECULAR TARGET OF NEUROTOXICITY - The present invention relates to the fields of biology, genetics and medicine. In particular it concerns new methods for the detection, characterisation and/or treatment (or management) of neurodegenerative diseases, particularly amyotrophic lateral sclerosis. The invention equally concerns methods for identifying or screening compounds active in these diseases. The invention further concerns the compounds, genes, cells, plasmids or compositions useful for implementing the hereinabove methods. In particular, the invention describes the role of PDE4B in these diseases and its use as a therapeutic, diagnostic or experimental target. | 2012-08-09 |
20120202847 | Novel Tetrahydroisoquinoline Compounds - The present invention relates to a compound or a pharmacologically acceptable salt thereof having an excellent DGAT inhibitory effect and feeding suppressant effect. The present invention provides trans-6-[3-(2,4-difluoro-phenyl)-ureido]-3,4-dihydro-1H-isoquinoline-2-carboxylic acid 4-carboxymethyl-cyclohexyl ester, trans-6-[3-(2-chloro-phenyl)-ureido]-3,4-dihydro-1H-isoquinoline-2-carboxylic acid 4-carboxymethyl-cyclohexyl ester, trans-6-[3-(2,3-difluoro-phenyl)-ureido]-3,4-dihydro-1H-isoquinoline-2-carboxylic acid 4-carboxymethyl-cyclohexyl ester, trans-6-[3-(2,5-difluoro-phenyl)-ureido]-3,4-dihydro-1H-isoquinoline-2-carboxylic acid 4-carboxymethyl-cyclohexyl ester, trans-6-[3-(2,6-difluoro-phenyl)-ureido]-3,4-dihydro-1H-isoquinoline-2-carboxylic acid 4-carboxymethyl-cyclohexyl ester, or the like, or a pharmacologically acceptable salt thereof. | 2012-08-09 |
20120202848 | THERAPY OF AUTOIMMUNE COLITIS USING A TIP60 INHIBITOR - This invention is in the fields of immunology and autoimmunity. More particularly it concerns methods of treating patients with compounds which are useful agents for inhibiting the functions of TIP60 in the treatment of an individual suffering, for example, from ulcerative colitis and other irritable bowel diseases. | 2012-08-09 |
20120202849 | PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT/PROPHYLAXIS OF NON-ALCOHOLIC FATTY LIVER DISEASE - Disclosed herein is a novel synergistic pharmaceutical composition comprising hydroxychloroquine with insulin sensitizing agents and lipid lowering agents such as statins along with pharmaceutical excipients/carriers useful in treating Non-Alcoholic Fatty Liver Disease. | 2012-08-09 |
20120202850 | METHOD FOR TREATING THROMBOSIS AND INHIBITING PLATELET AGGREGATION WITH 21-(S)-ARGATROBAN - A method for inhibiting coagulation including administering to a patient in need thereof a pharmaceutical composition containing 21-(S)-Argatroban and/or a pharmaceutically acceptable salt thereof. Compared with 21-(R)-Argatroban, 21-(S)-Argatroban significantly prolongs coagulation time of whole blood (CT), recalcification time (RT), kaolin partial thromboplastin time (APTT), pro-time prothrombin time (PT), thrombin time (TT), and reduces platelet adhesion rate and platelet aggregation rate in healthy dogs. Therefore, 21-(S)-Argatroban has a stronger effect for inhibiting coagulation and reducing therapeutically effective dose and is suitable for use in a method for treatment and/or prevention of thrombosis and inhibiting platelet aggregation. | 2012-08-09 |
20120202851 | PIM KINASE INHIBITORS AND METHODS OF THEIR USE - The present invention relates to new compounds of Formulas I and II, their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the inhibition of Pim kinase activity and/or the prophylaxis or treatment of cancer. | 2012-08-09 |
20120202852 | HETEROCYCLE AMIDE T-TYPE CALCIUM CHANNEL ANTAGONISTS - The present invention is directed to heterocycle amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved. | 2012-08-09 |
20120202853 | SUBSTITUTED PYRAZOLES AS ESTROGEN RECEPTOR LIGANDS - The invention provides a compound of formula (I) wherein G is a pyrazole ring as defined in the specification and R | 2012-08-09 |
20120202854 | 4-SUBSTITUTED PHENOXYPHENYLACETIC ACID DERIVATIVES - Compounds of formula (I): | 2012-08-09 |
20120202855 | METHODS FOR TREATING HYPERLIPIDEMIA WITH INTERMEDIATE RELEASE NICOTINIC ACID COMPOSITIONS HAVING UNIQUE BIOPHARMACEUTICAL CHARACTERISTICS - Methods for treating hyperlipidemia with intermediate release nicotinic acid formulations having unique biopharmaceutical characteristics, without causing drug-induced hepatotoxicity to a level which would require discontinuation of the therapy, are disclosed. According to the methods of the present invention, the intermediate nicotinic acid formulations are administered as a single dose once-a-day during the evening or at night. While the methods of the present invention contemplate administering the intermediate release nicotinic acid formulations at any time during a 24 hour period, it is preferable to administer them as a single dose during the evening or at night between about 6:00 pm. and 12:00 a.m., preferably between about 8:00 p.m. and 12:00 a.m., and most preferably between about 8:00 p.m. and 10:00 p.m. | 2012-08-09 |
20120202856 | SUBSTITUTED BENZIMDAZOLE DERIVATIVES USEFUL AS TRPM8 RECEPTOR MODULATORS - The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold. | 2012-08-09 |
20120202857 | NOVEL SALTS AND POLYMORPHS OF DESAZADESFERRITHIOCIN POLYETHER ANALOGUES AS METAL CHELATION AGENTS - Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity. | 2012-08-09 |
20120202858 | Solid Pharmaceutical Dosage Form - A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10. | 2012-08-09 |
20120202859 | Macrocyclic Inhibitors of Hepatitis C Virus - Inhibitors of HCV replication of formula (I) | 2012-08-09 |
20120202860 | Analgesic Compounds, Compositions and Uses Thereof - The invention relates to compounds, compositions, and methods for diminishing pain in a subject in need thereof comprising administering the compounds and compositions herein described. | 2012-08-09 |
20120202861 | NOVEL ESTROGEN RECEPTOR LIGANDS - The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. Formula (I) wherein R | 2012-08-09 |
20120202862 | Substituted carbamoylmethylamino acetic acid derivatives as novel NEP inhibitors - The present invention provides a compound of formula I; | 2012-08-09 |
20120202863 | Compositions and methods for treatment of glaucoma - The invention provides α-2 adrenergic receptor agonist compositions and methods for treating glaucoma and other intraocular conditions. The preferred α-2 agonist used in the inventive compositions and methods is dexmedetomidine at near alkaline pH and extremely low concentrations. | 2012-08-09 |
20120202864 | Compositions and Methods for Treatment of Glaucoma - The invention provides α-2 adrenergic receptor agonist compositions and methods for treating glaucoma and other intraocular conditions. The preferred α-2 agonist used in the inventive compositions and methods is dexmedetomidine at acidic pH and extremely low concentrations. | 2012-08-09 |
20120202865 | SUBSTITUTED-ARYL-(IMIDAZOLE)-METHYL)-PHENYL COMPOUNDS AS SUBTYPE SELECTIVE MODULATORS OF ALPHA 2B AND/OR ALPHA 2C ADRENERGIC RECEPTORS - A compound having selective modulating activity at the alpha 2B and or alpha 2C adrenergic receptor subtypes is represented by the general Formula 1: | 2012-08-09 |
20120202866 | BUCCAL, POLAR AND NON-POLAR SPRAY CONTAINING ONDANSETRON - Buccal aerosol sprays or capsules using polar and non-polar solvents have now been developed which provide ondansetron for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, ondansetron, and optional flavoring agent; formulation II: aqueous polar solvent, ondansetron, optionally flavoring agent, and propellant; formulation III: non-polar solvent, ondansetron, and optional flavoring agent; formulation IV: non-polar solvent, ondansetron, optional flavoring agent, and propellant; formulation V: a mixture of a polar solvent and a non-polar solvent, ondansetron, and optional flavoring agent; formulation VI: a mixture of a polar solvent and a non-polar solvent, ondansetron, optional flavoring agent, and propellant. | 2012-08-09 |
20120202867 | NOVEL MICROBIOCIDES - Compounds of formula (I), in which the substituents are as defined in claim | 2012-08-09 |
20120202868 | METHOD FOR TREATMENT OF BRONCHIAL ASTHMA - The present invention relates to a method for the treatment of bronchial asthma and chronic obstructive pulmonary disease (COPD) comprising administering to the patient suffering from asthama and COPD an effective dose of carbazole derivatives or salt thereof, optionally along with pharmaceutically acceptable excipients.
| 2012-08-09 |
20120202869 | Antidepressant Oral Pharmaceutical Compositions - The invention provides a pharmaceutical composition of duloxetine or its pharmaceutically equivalent derivatives like salts, isomers, complexes, polymorphs, hydrates or esters thereof and at least one buffering agent. The duloxetine or its pharmaceutically equivalent derivative is present from about 2 mg to approximately 200 mg; and the buffering agent is present in an amount of approximately 0.1 mEq to approximately 2.5 mEq per mg of duloxetine. Also provided is a method for treating of major depressive disorder and or diabetic peripheral neuropathic pain comprising administering to a mammal in need of such treatment a therapeutically effective amount of a composition. | 2012-08-09 |
20120202870 | TREATMENT OF INFLAMMATORY DISEASES USING MIR-124 - Methods of treating, reducing the risk of developing, or delaying the onset of an inflammatory disease are disclosed. The methods involved providing a subject with or at risk of developing an inflammatory disease and administering to the subject an effective amount of a first therapeutic composition comprising miR-124. Further provided are methods of diagnosing a subject with or at risk of developing an inflammatory disease. | 2012-08-09 |
20120202871 | CATIONIC LIPIDS AND METHODS FOR THE DELIVERY OF THERAPEUTIC AGENTS - The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art. | 2012-08-09 |
20120202872 | METHODS AND COMPOSITIONS FOR THE DIAGNOSIS AND PROGNOSIS OF CERVICAL INTRAEPITHELIAL NEOPLASIA AND CERVICAL CANCER - The invention provides methods and compositions for the diagnosis and prognosis of cervical intraepithelial neoplasia and cervical cancer. The methods comprise the step of determining the expression levels or genetic status of specific miRNAs. | 2012-08-09 |
20120202873 | RNAi Probes Targeting Cancer-Related Proteins - RNAi sequences that are useful as therapeutics in the treatment of cancers of various types, including prostate cancer, sarcomas such as osteosarcoma, renal cell carcinoma, breast cancer, bladder cancer, lung cancer, colon cancer, ovarian cancer, anaplastic large cell lymphoma and melanoma; and Alzheimer's disease. These sequences target clusterin, IGFBP-5, IGFBP-2, both IGFBP-2 and -5 simultaneously, Mitf, and B-raf. The invention further provides for the use of these RNAi sequences in the treatment of cancers of various types, including prostate cancer, sarcomas such as osteosarcoma, renal cell carcinoma, breast cancer, bladder cancer, lung cancer, colon cancer, ovarian cancer, anaplastic large cell lymphoma and melanoma; and Alzheimer's disease, and a method of treating such conditions through the administration of the RNA molecules with RNAi activity to an individual, including a human individual in need of such treatment. | 2012-08-09 |
20120202874 | ANTISENSE OLIGONUCLEOTIDE MODULATION OF STAT3 EXPRESSION - Compounds, compositions and methods are provided for inhibiting the expression of human STAT3. The compositions comprise antisense oligonucleotides targeted to nucleic acids encoding STAT3. Methods of using these oligonucleotides for inhibition of STAT3 expression and for promotion of apoptosis are provided. Methods for treatment of diseases, particularly inflammatory diseases and cancers, associated with overexpression or constitutive activation of STAT3 or insufficient apoptosis are also provided. | 2012-08-09 |
20120202875 | Method Of Treatment - The present invention relates to methods for treatment or prevention of autoimmune and inflammatory diseases and conditions by inhibiting or modifying histone demethylation. In a further aspect the invention relates to a method for identifying agents useful in said methods of treatment. The invention particularly describes the role of certain histone demethylase enzymes in these diseases and conditions and their use as therapeutic and screening targets. | 2012-08-09 |
20120202876 | METHODS OF TREATING DISEASES WITH PROANTHOCYANIDIN OLIGOMERS SUCH AS CROFELEMER - Disclosed herein are methods of treating diseases including gastrointestinal disorders, such as secretory diarrheas, with the proanthocyanidin oligomer, crofelemer. Also disclosed is the anti-secretory effect of crofelemer on Calcium-activated chloride channels (CaCC) and Cystic fibrosis transmembrane conductance regulator (CFTR). | 2012-08-09 |
20120202877 | ANTI-INFLUENZA AGENTS - The present invention relates to compounds that selectively inhibit influenza A virus group (1) sialidases and are therefore potential anti-influenza agents. | 2012-08-09 |
20120202878 | METHOD FOR TREATING PSORIASIS - A method for treating psoriasis including the steps of applying an isothiocyanate functional surfactant to an area affected by psoriasis, wherein the isothiocyanate functional surfactant comprises at least one isothiocyanate functional group associated with an aliphatic and/or aromatic carbon atom of the isothiocyanate functional surfactant. | 2012-08-09 |
20120202879 | MICROBIOLOGICALLY SOUND AND STABLE SOLUTIONS OF GAMMA-HYDROXYBUTYRATE SALT FOR THE TREATMENT OF NARCOLEPSY - Disclosed are formulations of gamma-hydroxybutyrate in an aqueous medium that are resistant to microbial growth. Also disclosed are formulations of gammahydroxybutyrate that are also resistant to the conversion into GBL. Disclosed are methods to treat sleep disorders, including narcolepsy, with these stable formulations of GHB. The present invention also provides methods to treat alcohol and opiate withdrawal, reduced levels of growth hormone, increased intracranial pressure, and physical pain in a patient. | 2012-08-09 |
20120202880 | MICROBIOLOGICALLY SOUND AND STABLE SOLUTIONS OF GAMMA-HYDROXYBUTYRATE SALT FOR THE TREATMENT OF NARCOLEPSY - Disclosed are formulations of gamma-hydroxybutyrate in an aqueous medium that are resistant to microbial growth. Also disclosed are formulations of gammahydroxybutyrate that are also resistant to the conversion into GBL. Disclosed are methods to treat sleep disorders, including narcolepsy, with these stable formulations of GHB. The present invention also provides methods to treat alcohol and opiate withdrawal, reduced levels of growth hormone, increased intracranial pressure, and physical pain in a patient. | 2012-08-09 |
20120202881 | Novel NIDDM Regimen - The present invention relates to the use of a short-acting oral hypoglycemic agent and to a novel regimen in the treatment of type 2 diabetes in which the endogenous secretion of insulin is stimulated in connection with meals by administering in connection with the meals a short-acting oral hypoglycaemic agent. Also, the present invention relates to a method of achieving significantly improvement in the glycaemic control by a combined use of repaglinide and metformin in NIDDM patients poorly controlled on metformin alone. | 2012-08-09 |
20120202882 | PERMEATION ENHANCERS FOR TOPICAL FORMULATIONS - A composition to be used as a permeation enhancer is provided. The composition may be added to topical cosmetics or pharmaceutical formulations that are topically applied. The composition comprises about 0.05-5% w/w of one or more phospholipids, 1-20% w/w of one or more oils having essential fatty acids, behenic acid, and oleic acid, 0.1-3% w/w of one or more skin lipids, and 1-10% w/w of a butter having linoleic acid and linolenic acid. One of the oils used in the composition is Pracaxi oil. | 2012-08-09 |
20120202883 | EFFECTS OF IDH1 AND IDH2 MUTATIONS ON THE CELLULAR METABOLOME - Point mutations of the NADP | 2012-08-09 |
20120202884 | INHIBITORS OF CXCR1/2 AS ADJUVANTS IN THE TRANSPLANT OF PANCREATIC ISLETS - The invention relates to CXCR1 and/or CXCR2 inhibitors for the preparation of a medicament for use as an adjuvant in the transplant of pancreatic islets in Type 1 diabetes patients. In particular, the compounds that can be used according to the invention have the following formula (I) in which R and R′ are as defined in the description. | 2012-08-09 |
20120202885 | METHODS, ASSAYS AND COMPOSITIONS FOR TREATING RETINOL-RELATED DISEASES - Described herein are methods and compositions for treating certain retinol-related diseases and conditions by modulation of transthyretin (TTR) and retinol binding protein (RBP) availability in the subject. For example, the methods and compositions provide for therapeutic agents for the treatment and/or prevention of age-related macular degeneration and/or dystrophies, metabolic disorders, idiopathic intracranial hypertension, hyperostosis, and protein misfolding and aggregation diseases. The compositions disclosed may be used as single agent therapy or in combination with other agents or therapies. In addition, described herein are methods and assays for selecting appropriate agents that can modulate the TTR and RBP availability in a subject. | 2012-08-09 |
20120202886 | METHOD OF ENHANCING HAIR GROWTH - Methods and compositions for stimulating the growth of hair are disclosed wherein said compositions include a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I | 2012-08-09 |
20120202887 | Facially Amphiphilic Polyaryl and Polyarylalkynyl Polymers and Oligomers and Uses Thereof - The present invention discloses methods of use of facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, including, but not limited to, pharmaceutical uses of the polymers and oligomers as antimicrobial agents and as antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, compositions of the novel polymers and oligomers, including pharmaceutical compositions, and methods of designing and synthesizing the facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers. | 2012-08-09 |
20120202888 | BIOMARKERS OF PROSTATE CANCER AND PREDICTING MORTALITY - Measurement of circulating C-peptide levels is useful for the prognostic evaluation of subjects, in particular for the prediction of adverse clinical outcomes, e.g., mortality, and the detection of fatal prostate cancer. | 2012-08-09 |
20120202889 | PRODUCTION METHOD FOR ASTAXANTHIN-CONTAINING COMPOSITION - The present invention relates to a method for reducing the relative ratio of 3-hydroxy-3′,4′-didehydro- β, Ψ-caroten-4-one (HDCO) to astaxanthin in a composition containing astaxanthin and HDCO by contacting the composition with an acidic medium having a pH of 3 or less and/or a basic medium having a pH of 9 or greater, and also relates to a method for producing an astaxanthin-containing composition which includes reducing the relative ratio of HDCO by the above method. By means of the method of the present invention, the relative ratio of HDCO, the biological function of which is not known, in an astaxanthin-containing composition can be easily reduced. | 2012-08-09 |
20120202890 | POLYMER-CARBOHYDRATE-LIPID CONJUGATES - The invention comprises compounds, methods of making, and methods of using. The compounds may have a backbone and three appended functional groups: one lipid, one hydrophilic polymer, and one carbohydrate. Specific functional groups may be selected for specific applications in formulating pharmaceuticals, cosmetics, nutriceuticals, and the like. A variety of linkers between the backbone and functional groups may also be selected to optimize performance. | 2012-08-09 |
20120202891 | Cannabinoid-Containing Compositions and Methods for Their Use - This invention relates to cannabinoid-containing compositions, particularly cannabinoid-containing gel formulations and methods for the treatment of traumatic injury, e.g., strains, sprains and contusions, and disease conditions, e.g., arthritis, particularly osteoarthritis. The methods involve topically applying a cannabinoid or a cannabinoid-containing composition to a subject's skin near, or distant from, the area of the injury or the area affected by the disease condition, e.g., an arthritic joint. The cannabinoid-containing composition is preferably a pharmaceutically acceptable gel containing a therapeutically effective amount of a cannabinoid sufficient to alleviate the symptoms associate with the injury or disease condition. | 2012-08-09 |
20120202892 | Cannabinoid-Containing Compositions and Methods for Their Use - This invention relates to cannabinoid-containing compositions, particularly cannabinoid-containing gel formulations and methods for the treatment of traumatic injury, e.g., strains, sprains and contusions, and disease conditions, e.g., arthritis, particularly osteoarthritis. The methods involve topically applying a cannabinoid or a cannabinoid-containing composition to a subject's skin near, or distant from, the area of the injury or the area affected by the disease condition, e.g., an arthritic joint. The cannabinoid-containing composition is preferably a pharmaceutically acceptable gel containing a therapeutically effective amount of a cannabinoid sufficient to alleviate the symptoms associate with the injury or disease condition. | 2012-08-09 |
20120202893 | Method Of Manufacturing A Purified Product Of Alkyl-Modified Polydimethylsiloxane, A Cosmetic Raw Material, And Cosmetics - To provide a method for manufacturing a purified product of an alkyl-modified polydimethylsiloxane that is practically odorless and compatible with other cosmetic raw materials. The manufacturing method comprises the steps of: [A] synthesizing an alkyl-modified polydimethylsiloxane by subjecting a hydrosilyl-containing polydimethylsiloxane and an C2-C30 α-olefin to a hydrosilation reaction, and [B] subjecting the crude alkyl-modified polydimethylsiloxane obtained in Step [A] to a treatment of rendering it odorless by a hydrogenation reaction in the presence of a hydrogenation catalyst in an organic solvent (c) that is essentially free of active hydrogen atoms and has a boiling point equal to or greater than 70° C. | 2012-08-09 |
20120202894 | Rapidly Soluble Solid Pharmaceutical Preparations Containing Amphiphilic Copolymers Based On Polyethers In Combination With Hydrophilic Polymers - Dosage forms comprising formulations of sparingly water-soluble active ingredients in a polymer matrix composed of amphiphilic polyether copolymers and of at least one hydrophilic polymer, in which the sparingly water-soluble active ingredient is present in amorphous form in the polymer matrix. | 2012-08-09 |
20120202895 | PASTE COMPOSITION AND COSMETIC CONTAINING IT - The present invention has an object to provide a paste composition having a high thickening effect to an oil material such as a silicone oil and giving a silky and light feeling without poor spreading properties and without such feelings as an oily, a sticky, and an oil-film feeling and an object to provide a cosmetic containing it; wherein the paste composition comprises (I) an organopolysiloxane obtained by an addition polymerization of a polysiloxane mixture containing (i) one or more organohydrogen polysiloxane and (ii) one or more organopolysiloxane having an aliphatic unsaturated group and (II) at least one oil material that is a liquid at 25° C., selected from a silicone oil, a hydrocarbon oil, an ester oil, a natural plant and animal oil, and a semi-synthetic oil. | 2012-08-09 |
20120202896 | COMPOSITION INCLUDING A COPOLYAMIDE AND A CROSS-LINKED POLYOLEFIN - The invention relates to a composition including: 45 to 95 wt % of a semi-aromatic copolyamide containing at least two separate units having the following general formulation: A/X.T, where A is selected from among a unit obtained from an amino acid, a unit obtained from a lactam, and a twit having the formula (diamine Ca).(diacid Cb), and XT denotes a unit obtained from the polycondensation of a diamine in Cx and from terephthalic acid, with x being the number of carbon atoms of the diamine in Cx, said copolyamide having a polymoleoularity index, noted Ip, of less than or equal to 3.5, measured by gel permeation chromatography, and an amino chain end content of between 0.020 mcg/g and 0.058 mcg/g; and 5 to 55 wt % of at least one cross-linked polyolefin. The invention also relates to a method for preparing said composition and to the uses thereof. | 2012-08-09 |
20120202897 | METHOD OF PURIFYING A GAS - A method of purifying gas obtained by gasification of a biomass feedstock. The gas which contains carbon monoxide, carbon dioxide, hydrogen, hydrocarbons and mixtures thereof can be freed from impurities, such as hydrogen sulphide, hydrogen chloride, ammonia, carbonyl sulphide, hydrogen cyanide and mixtures thereof, by contacting the gas with an acidic aqueous wash solution of transition metal ions capable of binding to sulphide ions, by binding a significant portion of the hydrogen sulphide impurities contained in the gas into practically insoluble transition metal sulphide compounds to remove hydrogen sulphide impurities from the gas; and by separating the thus obtained purified gas from the aqueous solution. The purified gas is suitable for production of hydrocarbon compositions by, for example the Fischer-Tropsch process. | 2012-08-09 |
20120202898 | METHOD FOR OBTAINING A MULTIMETALLIC SULFUREOUS CATALYST AND USE THEREOF IN A METHOD FOR PRODUCING HIGHER ALCOHOLS BY CATALYTIC CONVERSION OF SYNTHESIS GAS - The present invention relates to a sulphided multi-metallic catalyst, the process for obtaining it by sulphidation of a multi-metallic solid and use thereof in a process for producing higher alcohols (C | 2012-08-09 |
20120202899 | PRODUCTION OF HYDROCARBONS - A process for producing hydrocarbons and, optionally, oxygenates of hydrocarbons is provided. A synthesis gas comprises hydrogen, carbon monoxide and N-containing contaminants selected from the group consisting of HCN, NH | 2012-08-09 |