03rd week of 2012 patent applcation highlights part 44 |
Patent application number | Title | Published |
20120015934 | CYCLOPAMINE LACTAM ANALOGS AND METHODS OF USE THEREOF - The present invention relates to steroidal alkaloids useful in the treatment of hedgehog pathway related disorders, particularly cancer. | 2012-01-19 |
20120015935 | Substituted Tetrahydropyrazolo-Pyrido-Azepine Compounds - The present invention relates to substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 2012-01-19 |
20120015936 | SUBSTITUTED TETRAHYDRONAPHTHALENES, METHOD FOR THE PRODUCTION THEREOF, AND USE THEREOF AS DRUGS - The invention relates to substituted tetrahydronaphthalenes, to derivatives thereof, to physiologically acceptable salts thereof, to physiologically functional derivatives, to the production thereof, to drugs containing at least one substituted tetrahydronaphthalene according to the invention or derivative thereof, and to the use of the substituted tetrahydronaphthalenes according to the invention and to derivatives thereof as MCH antagonists. | 2012-01-19 |
20120015937 | Kinase Inhibitors And Their Uses - The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity. | 2012-01-19 |
20120015938 | 1,4-BENZODIAZEPIN-2-ON DERIVATIVES - The present invention relates to a compound represented by a formula (I): wherein R | 2012-01-19 |
20120015939 | TOPICAL TREATMENT OF NEUROPATHIC PAIN AND METHODS OF DIAGNOSIS - Alpha-2 adrenergic agonists such as clonidine may be used to treat the pain associated with painful diabetic neuropathy (PDN) only in a subset of these patients. Targeted nociceptors (pain fibers) must be functionally expressed in the skin in order for clonidine to have a therapeutic effect. Neuropathies associated with pain differ with respect to the expression of nociceptors in the skin. Clonidine targets alpha-2 adrenergic receptors on the terminals of nociceptors. The presence of the targeted nociceptors may be determined by topical application of a TRPV1 agonist such as capsaicin. Patients who detect the capsaicin as a pain stimulus applied near the painful area have expression in the skin of the requisite targeted nociceptors and the targeted alpha-2 adrenergic receptors. The test is referred to as a capsaicin challenge test. This test significantly improves clinical outcomes in topical neuropathic pain treatment. | 2012-01-19 |
20120015940 | NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION - The present invention relates to a compound of Formula (I): wherein: n is 0 or 1; X is O or CH | 2012-01-19 |
20120015941 | Antibacterial Amide and Sulfonamide Substituted Heterocyclic Urea Compounds - The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided. | 2012-01-19 |
20120015942 | SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I): | 2012-01-19 |
20120015943 | SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I): | 2012-01-19 |
20120015944 | TETRAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I: | 2012-01-19 |
20120015945 | USE OF CB1 ANTAGONISTS AND/OR INVERSE AGONISTS FOR THE PREPARATION OF DRUGS THAT INCREASE MOTOR NEURON EXCITABILITY - Use of a CB1 receptor antagonist and/or inverse agonist, preferably rimonabant, for the preparation of drugs useful for increasing motor neuron excitability in the cerebral cortex and/or in the brain stem and/or at the spinal level, as well as a method for increasing motor neuron excitability through the administration of a CB1 antagonist/inverse agonist receptors, and to the use of a pharmaceutical composition which comprises a CB1 receptor antagonist and/or inverse agonist, preferably rimonabant, for increasing motor neuron excitability in the cerebral cortex and/or in the brain stem and/or at the spinal level. | 2012-01-19 |
20120015946 | INSECTICIDAL COMPOUNDS - A compound of formula (I): wherein A | 2012-01-19 |
20120015947 | Cyclic hydroxylamine as psychoactive compounds - A compound of formula (I): | 2012-01-19 |
20120015948 | TABLET COMPOSITION - A water soluble effervescent disinfecting tablet comprises a chlorinated isocyanurate such as anhydrous sodium dichloroisocyanurate. The tablet also comprises an alkali metal bicarbonate such as sodium bicarbonate, an aliphatic carboxyl acid such as adipidic acid, and a dessicant base such as sodium carbonate. The tablet contains a masking agent, especially isoamyl acetate and/or L-methone in an amount to mask taste and/or odour characteristics of the chlorinated isocyanurate. | 2012-01-19 |
20120015949 | COMPOSITION AND METHOD OF DECREASING RENAL ISCHEMIC DAMAGE - A method of decreasing renal ischemic damage comprising a) identifying an organism having a kidney that is susceptible to renal ischemic damage from an ischemic event; and b) administering to the organism one or more than one effective dose of an agent prior to the ischemic event; where administering to the organism the one or more than one effective dose of the agent serves to at least partially protect the organism's kidney from damage during a subsequent ischemic event. A composition for decreasing renal ischemic damage comprising one or more than one phosphodiesterase inhibitor, and one or more than one HMG-CoA reductase inhibitor. | 2012-01-19 |
20120015950 | CARBAMATE DERIVATIVES OF ALKYL-HETEROCYCLES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - Compound corresponding to general formula (I): in which R | 2012-01-19 |
20120015951 | Polymorphs of Brimonidine Pamoate - A brimonidine pamoate polymorph exhibits characteristics disclosed herein. The polymorph is included in a composition, device, or implant for use in the treatment or control of elevated intraocular pressure or in the neuroprotection of components of a neurological tissue to prevent progressive degeneration of such components. In particular, such a composition, device, or implant can be used to provide neuroprotection to cells and components of the optic nerve system. | 2012-01-19 |
20120015952 | Inhibitors of NF-KB - The invention relates to compounds of formulae (1) and (2): | 2012-01-19 |
20120015953 | METHODS AND COMPOSITIONS FOR THE TREATMENT OF ALLERGY - The present invention relates to compositions comprising an antagonist of the histamine H1 receptor and a compatible antagonist of the histamine H4 receptor. The antagonist compounds are selected to prevent the H4 receptor antagonist from interfering with the H1 receptor antagonist's suppression of acute phase allergic responses in a patient. The present invention also relates to compositions comprising a mast cell stabilizer and a compatible antagonist of the histamine H4 receptor. | 2012-01-19 |
20120015954 | THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN - A compound of formula: | 2012-01-19 |
20120015955 | F, G, H, I and K Crystal Forms of Imatinib Mesylate - The invention relates to the F-crystal form, G-crystal form, H-crystal form, I-crystal form and K-crystal form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide, certain processes for their preparation, pharmaceutical compositions containing these crystal forms, their use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, and their use as an intermediate or for the preparation of pharmaceutical preparations for use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, especially humans. | 2012-01-19 |
20120015956 | DEUTERIUM-ENRICHED DASATINIB - The present application describes deuterium-enriched dasatinib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 2012-01-19 |
20120015957 | PIPERAZINYL DERIVATIVES USEFUL AS MODULATORS OF THE NEUROPEPTIDE Y2 RECEPTOR - The present invention is directed to piperidinyl and piperazinyl derivatives of formula (I) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor. | 2012-01-19 |
20120015958 | 1-(4-UREIDOBENZOYL)PIPERAZINE DERIVATIVES - The present invention relates to 1-(4-ureidobenzoyl)piperazine derivatives having the general Formula I (We bring to your attention that formula I is not provided on this electronic version as it is provided in the abstract of the paper copy) Wherein R | 2012-01-19 |
20120015959 | HETEROCYCLIC COMPOUNDS AS AUTOTAXIN INHIBITORS - Compounds of the formula (I), in which Het, R, X, Y, R | 2012-01-19 |
20120015960 | CHEMICAL INHIBITOR OF P53-SNAIL BINDING AND PHARMACEUTICAL COMPOSITION FOR TREATING CANCER DISEASE CONTAINING SAME AS ITS ACTIVE INGREDIENT - Provided are compounds for inhibiting Snail-p53 binding and therapeutic agents for cancer including the compounds as an effective component. The Snail-p53 binding inhibitors induce expression of p53 in K-Ras mutant cell lines, thereby enabling effective treatment or prevention of K-Ras mutant cancer, such as, pancreatic cancer, lung cancer, cholangioma, and colon cancer, of which diagnosis or treatment is not easy. | 2012-01-19 |
20120015961 | ISOTHIOUREA DERIVATIVES OR ISOUREA DERIVATIVES HAVING BACE1 INHIBITORY ACTIVITY - The present invention provides, for example, a compound of the following formula (I): | 2012-01-19 |
20120015962 | PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS - Compounds of the formula I or II: | 2012-01-19 |
20120015963 | NOVEL PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS - The present disclosure is directed to novel compounds of Formula (I) | 2012-01-19 |
20120015964 | QUINAZOLINONES AS INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA - Compounds that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3Kδ plays a role in leukocyte function, using the compounds also are disclosed. | 2012-01-19 |
20120015965 | PHARMACEUTICAL COMPOSITION COMPRISING N-[3-CHLORO-4-[(3-FLUOROPHENYL)METHOXY] PHENYL]-6-[5[[[2-(METHYLSULFONYL) ETHYL]AMINO]METHYL]-2-FURYL]-4- QUINAZOLINAMINE - The present invention relates to a pharmaceutical composition comprising N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine as active pharmaceutical ingredient and a process of preparing such composition. | 2012-01-19 |
20120015966 | PPAR ACTIVE COMPOUNDS - Compounds are described that are active on at least one of PPARα, PPARδ, and PPARγ, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPARα, PPARδ, and PPARγ. | 2012-01-19 |
20120015967 | PYRIMIDINE AND PYRIDINE DERIVATIVES AS POSH AND POSH-AP INHIBITORS - Pyridine and pyrimidine derivatives inhibit ubiquitination of human polypeptides, particularly of POSH and POSH-associated proteins such as HERPUD1, and can be used as medicaments for treatment of viral infections caused by virus such as HIV and for treatment of neurological disorders or diseases. | 2012-01-19 |
20120015968 | USE OF PYRIMIDYLAMINOBENZAMIDE DERIVATIVES FOR THE TREATMENT OF DISORDERS MEDIATED BY THE LEUCINE ZIPPER-AND STERILE ALPHA MOTIF-CONTAINING KINASE (ZAK) - The invention relates to the use of a pyrimidylaminobenzamide derivative of formula I | 2012-01-19 |
20120015969 | NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION - The present invention relates to a compound of Formula (I): wherein: R | 2012-01-19 |
20120015970 | NEW AZACYCLIC COMPOUNDS - The invention provides novel compounds having the general formula (I) | 2012-01-19 |
20120015971 | OPHTHALMIC COMPOSITION COMPRISING ASCOMYCIN - This invention relates to topical ophthalmic compositions comprising an ascomycin e.g. for the treatment of inflammatory diseases such as blepharitis. | 2012-01-19 |
20120015972 | INDOLIZINE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES - The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level and the like. That is, the present invention relates to indolizine derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, salts thereof or the like. In the formula, ring U represents aryl or heteroaryl; R | 2012-01-19 |
20120015973 | MEK MUTATIONS CONFERRING RESISTANCE TO MEK INHIBITORS - The present invention relates to methods, compositions and kits concerning resistance to treatment with an anti-cancer agent, specifically an inhibitor of MEK. In particular embodiments, the invention concerns mutations in a MEK sequence that confer resistance to a MEK inhibitor. Identification of such mutations in a MEK sequence allows the identification and design of second-generation MEK inhibitors. Methods and kits for detecting the presence of a mutant MEK sequence in a sample are also provided. | 2012-01-19 |
20120015974 | IMIDAZOPYRIDINE INHIBITORS OF IAP - The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: | 2012-01-19 |
20120015975 | FUSED HETEROCYCLIC COMPOUND AND USE THEREOF - A fused heterocyclic compound of formula (1): wherein, A | 2012-01-19 |
20120015976 | AUTOTAXIN INHIBITORS - The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers. | 2012-01-19 |
20120015977 | QUINOLINONE DERIVATIVES USEFUL FOR THE TREATMENT OF CNS DISORDERS - The present invention relates to novel quinolinone derivatives (I), efficacious in animal models of CNS disorders and, as such, valuable candidates for the prevention or treatment of CNS (Central Nervous System) diseases or disorders. In other aspects the invention relates to pharmaceutical compositions comprising the quinolinone derivatives of the invention and to the use of these compounds for therapeutic applications. | 2012-01-19 |
20120015978 | THERAPEUTIC AGENTS FOR OCULAR HYPERTENSION - This invention provides well defined 6-alkyl or hydroxyalkyl- | 2012-01-19 |
20120015979 | Compounds for Modulating TRPV3 Function - The present application relates to compounds and methods for treating pain and other conditions related to TRPV3. | 2012-01-19 |
20120015980 | ANTHRANILIC DIAMIDE DERIVATIVES - The present invention relates to novel anthranilic acid derivatives of the general formula (I) | 2012-01-19 |
20120015981 | Active compound combinations - The present invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) the compound 3-(difluoromethyl)-1-methyl-N-(3′,4′,5′-trifluorobiphenyl-2-yl)-1H-pyrazole-4-carboxamide of formula (I) and/or the compound 3-(difluoromethyl)-1-methyl-N-(2′.4′.5′-trifluorobiphenyl-2-yl)-1H-pyrazole-4-carboxamide of formula (II) and (B) at least one azolylmethyloxirane of formula (III). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed. | 2012-01-19 |
20120015982 | Thiazolidinedione analogues - The present invention relates to thiazolidinedione analogues that are useful for treating metabolic inflammation mediated diseases such as diabetes. | 2012-01-19 |
20120015983 | Synthesis and Novel Salt Forms of (R)-3-((E)-pyrrolidin-3-yl)vinyl)-5-tetrahydropyran-4-yloxy)pyridine - The present invention relates to (R)-3-((E)-2-(pyrrolidin-3-yl)vinyl)-5-(tetrahydropyran-4-yloxy)pyridine, its salt forms, and to processes for the commercial-scale production of these compounds in sufficient purity and quality for use in pharmaceutical compositions. | 2012-01-19 |
20120015984 | Granulate Formulation of Pirfenidone and Pharmaceutically Acceptable Excipients - A capsule formulation of pirfenidone is provided that includes pharmaceutically acceptable excipients. In one embodiment, this capsule formulation is capable of sustaining desirable pharmacokinetic responses in a patient. Further provided are methods of treating fibrotic conditions and other cytokine-mediated disorders by administering pirfenidone capsules of such formulation to a patient in need. | 2012-01-19 |
20120015985 | Methods of Administering Pirfenidone Therapy - The present invention relates to methods involving avoiding adverse drug interactions with fluvoxamine and pirfenidone or other moderate to strong inhibitors of CYP enzymes. | 2012-01-19 |
20120015986 | SALTS OF DEHYDROACETIC ACID AS A PYRITHIONE STABILIZER IN PLASTICS - The invention provides a method for preventing discoloration of pyrithione-containing materials, in particular plastic materials or other material such as paints, coatings, adhesives or textiles which are exposed to an outdoor environment. The method is likewise suited for preventing discoloration of other pyrithione-containing materials such as personal care compositions like shampoos. A discoloration inhibitor that includes dehydroacetic acid or a salt thereof is added to the pyrithione-containing material. The discoloration is prevented without the addition of a cyclic organic phosphoric acid ester or an organic phosphite. Use of the discoloration inhibitor does not interfere with the antimicrobial effect of the pyrithione. | 2012-01-19 |
20120015987 | NOVEL POLYMORPH OF ATAZANAVIR SULFATE - The present invention provides a novel crystalline form of atazanavir sulfate, process for its preparation and to pharmaceutical composition containing it. In accordance with the present invention atazanavir sulfate was dissolved in methanol, to the solution was added ethyl acetate, the solid obtained was collected by filtration and dried to give atazanavir sulfate crystalline form H1. | 2012-01-19 |
20120015988 | Sulfone Compounds Which Modulate The CB2 Receptor - Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain. | 2012-01-19 |
20120015989 | LINKED MYC-MAX SMALL MOLECULE INHIBITORS - Provided herein are compounds and compositions for interfering with the association of Myc and Max. These compounds and compositions are useful in methods for inhibiting growth or proliferation of a cell. Methods of inhibiting growth or proliferation of a cell comprise contacting the cell with an amount of a compound that interferes with Myc and Max association effective to inhibit growth or proliferation of the cell. | 2012-01-19 |
20120015990 | TASPASE1 INHIBITORS AND THEIR USES - Provided herein are small molecule inhibitors of Taspase1 and methods of using the small molecule inhibitors of Taspase1 to treat neoplasm in subjects in need thereof. | 2012-01-19 |
20120015991 | POLYCYCLIC ANTAGONISTS OF LYSOPHOSPHATIDIC ACID RECEPTORS - Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases. | 2012-01-19 |
20120015992 | Napthalene-Based Inhibitors of Anti-Apoptotic Proteins - Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: | 2012-01-19 |
20120015993 | Novel Pharmaceutical Forms, and Methods of Making and Using the Same - Crystalline salts, polymorphs, solvates, and hydrates of bicalutamide, 5-fluorouracil, donepezil, anastrozole, nelfinavir, mirtazapine, lansoprazole, and tamsulosin, or derivatives thereof are provided by the subject invention. Methods of making and using the same are also provided. | 2012-01-19 |
20120015994 | (2,5-DIOXOIMIDAZOLIDIN-I-YL)-N-HYDROXY-ACETAMIDES AS METALLOPROTEINASE INHIBITORS - The invention provides compounds of the formula (I) | 2012-01-19 |
20120015995 | BENDAMUSTINE ANIONIC-CATIOINIC CYCLOPOLYSACCHARIDE COMPOSITIONS - The present invention is directed to pharmaceutical compositions including: (a) bendamustine, (b) a first charged cyclopolysaccharide, and (c) a stabilizing agent which is a second charged cyclopolysaccharide having a charge opposite to that of the first charged cyclopolysaccharide. The composition provides unexpectedly desirable stability in reactive environments such as plasma, coupled with unexpectedly desirable anticancer activity. The compositions are suitable for injection or infusion into patients in need for treatment with bendamustine. | 2012-01-19 |
20120015996 | ANTIFUNGAL MEDICINAL COMPOSITIONS - An object of the present invention is to provide a medicinal composition useful for external application in the treatment of a fungal infection reaching the lower part of a thick keratin layer. Provided is an antifungal medicinal composition, comprising: (1) a film-forming agent; (2) a water-soluble plasticizer in a form of a solid or a paste at 20° C. at 1 atm; and (3) an antifungal compound represented by a general formula (1) and/or a physiologically acceptable salt thereof. | 2012-01-19 |
20120015997 | PHARMACEUTICAL COMPOSITION FOR EXTERNAL USE - Provided is a pharmaceutical composition for external use, including: (i) a compound represented by structural formula (2) and/or a salt thereof; and (ii) N-methyl-2-pyrrolidone. | 2012-01-19 |
20120015998 | PHOTOTHERAPY METHODS AND DEVICES COMPRISING EMISSIVE ARYL-HETEROARYL COMPOUNDS - Disclosed herein are compounds represented by a formula: R | 2012-01-19 |
20120015999 | FORMULATIONS OF (R)-1-(2,2-DIFLUOROBENZO[D] [1,3] DIOXOL-5-YL)-N-(1-(2,3-DIHYDROXYPROPYL)-6-FLUORO-2-(1-HYDROXY-2-METHYLPRO- PAN-2-YL)-1H-INDOL-5-YL)CYCLOPROPANECARBOXAMIDE - The present invention relates to formulations of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), pharmaceutical packs or kits thereof, and methods of treatment therewith. | 2012-01-19 |
20120016000 | METHOD TO ASSAY PHOSPHOLIPID AND TRIGLYCERIDE TRANSFER ACTIVITY OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN - The present invention is directed to a method for identifying an antagonist compound of microsomal triglyceride transfer protein (MTP), wherein the antagonist at least partially inhibits triglyceride transfer activity while not significantly inhibiting phospholipids transfer activity of MTP. In particular, the present invention is directed to assays for phospholipid (PL) and triglyceride (TG) transfer activity having considerably improved sensitivity. In addition, antagonist compounds that modulate the lipid transfer activity of MTP are provided. Kits for measuring the lipid transfer activity of MTP are also provided by the present invention. | 2012-01-19 |
20120016001 | SUCCINIMIDE DERIVATIVES AS OCULAR HYPOTENSIVE AGENTS - The present invention provides methods and pharmaceutical compositions for treating ocular disorders associated with elevated intraocular pressure, such as glaucoma, by administering antiepileptic or anti-convulsant compounds of the succinimide family, in particular compounds of formula I and/or II as defined herein. | 2012-01-19 |
20120016002 | Patient Selection and Therapeutic Methods Using Markers of Prostaglandin Metabolism - Disclosed herein are methods related generally to a patient selection process for identifying individuals for treatment of cancer, inflammation, pain, and/or related conditions. | 2012-01-19 |
20120016003 | POT1 ALTERNATIVE SPLICING VARIANTS - The present invention provides methods and compositions for diagnosis and treatment of carcinomas with aberrant expression patterns of POT 1. The invention also provides methods of identifying compounds that may modulate the cellular expression of POT 1. The invention further provides methods for treating subjects suffering from or at risk of developing a colorectal carcinoma. | 2012-01-19 |
20120016004 | COMPOSITIONS FOR INHIBITING GENE EXPRESSION AND USES THEREOF - The inventors have examined the means for providing more efficacious gene expression blocking compounds. The inventors have discovered new structural features that surprisingly improve the efficacy of gene expression blocking molecules. These features include the presence of multiple 3′ ends and a linker at the 5′ ends. Surprisingly, these features improve the efficacy of the gene expression blocking compounds in a manner that decreases the compound's biologic instability. Even more surprisingly, this effect has been found to be applicable to both DNA and RNA oligonucleotide-based compounds and to have application in traditional antisense and RNAi technologies. | 2012-01-19 |
20120016005 | PHAGOCYTIC CELL DELIVERY OF RNAI - The present invention provides a particulate delivery system for delivering an RNAi construct to phagocytic cells such as macrophages, comprising various configurations of a complex comprising a phagocytic cell-targeting moiety and an RNAi construct. The invention further provides methods of making the delivery system, and their uses, such as treating phagocytic cell-associated disease conditions. | 2012-01-19 |
20120016006 | Compositions And Methods For Increasing Cellular Uptake Of RNAi Via SID-1 - The invention relates to a double-stranded ribonucleic acid (dsRNA) targeting a Systemic RNA Interference Defective-1 (SID-I) gene, and methods of using the dsRNA to inhibit expression of SID-1. | 2012-01-19 |
20120016007 | SMALL INTERFERENCE RNA COMPLEX WITH INCREASED INTRACELLULAR TRANSMISSION CAPACITY - A multiplex siRNA complex and a multifunctional nucleic acid structure complex, which have enhanced intracellular delivery capacity are provided. The siRNA complex and the multifunctional nucleic acid structure complex have a novel structure which can be chemically synthesized in an easy manner for a conventional shRNA system for inhibiting the expression of a plurality of genes, while they can inhibit the expression of a plurality of genes at the same time at increased efficiency compared to the conventional siRNA. Also, they have high intracellular delivery capacity and can specifically inhibit the expression of target genes without causing a nonspecific antiviral response, and thus are highly useful as siRNA mechanism-mediated therapeutic agents for treating cancer or viral infection. In addition, the multifunctional nucleic acid structure complex can comprise, in addition to siRNAs, functional oligonucleotides, such as miRNA, antagomiR, an antisense oligonucleotide, an aptamer and ribozyme, and thus can perform various functions at the same time. | 2012-01-19 |
20120016008 | ISOLATED GENOMIC POLYNUCLEOTIDE FRAGMENTS FROM THE p15 REGION OF CHROMOSOME 11 ENCODING HUMAN RIBOSOMAL PROTEIN L26 (RIBO26) - Provided herein are isolated genomic polynucleotide fragments from the from the p15 region of chromosome 11 encoding human ribosomal protein L26 (RIBO26) and methods of use. | 2012-01-19 |
20120016009 | Optimized Methods For Delivery Of DSRNA Targeting The PCSK9 Gene - This invention relates to optimized methods for treating diseases caused by PCSK9 gene expression. | 2012-01-19 |
20120016010 | RNA Interference Mediated Inhibition of BTB and CNC Homology 1, Basic Leucine Zipper Transcription Factor 1 (BACH1) Gene Expression Using Short Interfering Nucleic Acid (siNA) - The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of Bach1 gene expression and/or activity, and/or modulate a Bach1 gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against Bach1 gene expression. | 2012-01-19 |
20120016011 | RNA Interference Mediated Inhibition of Connective Tissue Growth Factor (CTGF) Gene Expression Using Short Interfering Nucleic Acid (siNA) - The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of CTGF gene expression and/or activity, and/or modulate a CTGF gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against CTGF gene expression. | 2012-01-19 |
20120016012 | RNAi MOLECULE TARGETING THYMIDYLATE SYNTHASE AND APPLICATION THEREOF - This invention provides a novel RNAi molecule that can significantly potentiate antitumor effects of a 5-FU antitumor agent. The RNAi molecule comprises the nucleotide sequence shown in SEQ ID NO: 2. The invention also provides an antitumor agent comprising such RNAi molecule and a 5-FU antitumor agent. | 2012-01-19 |
20120016013 | ANTI-CANCER OLIGODEOXYNUCLEOTIDES - It is disclosed herein that suppressive OD Ns are of use for preventing or delaying the formation of a tumor, reducing the risk of developing a tumor, treating a tumor, preventing conversion of a benign to a malignant lesion, or preventing metastasis. In some embodiments, methods are disclosed herein for treating, preventing or reducing the risk of developing a tumor, such as esophageal, gastrointestinal, liver, lung, skin and colon tumors or a mesothelioma. Generally, the methods disclosed herein include selecting a subject for treatment and administering to the subject a therapeutically effective amount of one or more suppressive ODN. In some examples, additional agents can also be administered to the subject of interest. | 2012-01-19 |
20120016014 | BENZOTHIOPHENE CARBOXAMIDE COMPOUNDS, COMPOSITION AND APPLICATIONS THEREOF - The present invention provides benzothiophene carboxamide compounds of formula I, their polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts and formulations thereof, which are useful as COX-2 inhibitors and PfENR inhibitors. | 2012-01-19 |
20120016015 | ALDEHYDE CONJUGATED FLAVONOID PREPARATIONS - There is provided a method of conjugating a polymer containing a free aldehyde group with a flavonoid in the presence of an acid catalyst, such that the polymer is conjugated to the C6 or C8 position of the flavonoid A ring. The resulting conjugates may be used to form delivery vehicles to deliver high doses of flavonoids, and may also be used as delivery vehicles to deliver an additional bioactive agent. | 2012-01-19 |
20120016016 | METHODS AND COMPOSITIONS FOR TREATING COMPLICATIONS OF DIABETES AND VASCULAR DISEASES USING FLAVONES - Disclosed herein, inter alia, are methods and compositions for treating a complication of diabetes or a vascular disease using a 5-desoxy-flavone and/or 5-desoxy-flavonol. | 2012-01-19 |
20120016017 | PHARMACEUTICAL COMPOSITION FOR TREATING OR PREVENTING CANCER - The present invention relates to a compound of the formula I: | 2012-01-19 |
20120016018 | COMPOSITION FOR INDUCING MULTIPLE NUCLEAR DIVISION OF CELLS - The present invention relates to the novel use of a composition comprising a compound of the formula I: | 2012-01-19 |
20120016019 | PHARMACEUTICAL COMPOSITION FOR TREATING OR PREVENTING CANCER - The present invention relates to a compound of the formula I: | 2012-01-19 |
20120016020 | SOLID DISPERSION OF ALPHA-KETOAMIDE DERIVATIVES - A solid dispersion comprising ((1S)-1-((((1S)-1-benzyl-2,3-dioxo-3-(cyclopropylamino)propyl)amino)carbonyl)-3-methylbutyl)carbamic acid 5-methoxy-3-oxapentyl ester made amorphous in the presence of a water-soluble cellulosic polymer has improved storage stability. The solid dispersion also has improved solubility for an improved bioavailability. | 2012-01-19 |
20120016021 | METHODS OF TREATING FRAGILE X SYNDROME, DOWN'S SYNDROME, AUTISM AND RELATED DISORDERS - Disclosed herein are methods of treating fragile X syndrome, fragile X-associated tremor/ataxia syndrome, Down's syndrome and other forms of mental retardation, and/or autism comprising administering a GABA | 2012-01-19 |
20120016022 | AGROCHEMICAL COMPOSITION FOR PEST CONTROL AND PEST CONTROL METHOD - The invention has as its object the provision of an agrochemical composition for pest control, by which an excellent control effect is achieved on pests, hyposensitive mites having reduced sensitivity to chemicals and eggs of the mites, and other pests of all stages of growth than the mites even when the composition is applied in a small amount, and a pest control method. | 2012-01-19 |
20120016024 | Water-In-Oil Emulsion Composition - The present invention provides a water-in-oil emulsion composition that provides a post-application elastic feeling, softness, and a moisturizing effect and that is excellent in emulsion stability while it is a composition with a high internal-aqueous-phase proportion, which allows the makeup to stay on nicely because of its uniform applicability and provides a refreshing effect on the skin when used as a pre-makeup emulsion. The water-in-oil emulsion composition of the present invention is characterized by comprising the below-described components (A) (B) and (C), and satisfying the below-described conditions (1) and (2). Components: (A) glycerol isostearate and/or glycerol oleate, (B) an aqueous component, (C) an oil component containing an isoparaffin having 20 carbon atoms or less. Conditions: (1) The internal-aqueous-phase proportion, which is obtained by dividing the mass of the aqueous component (B) by the sum of the mass of the aqueous component (B) and the mass of the oil component (C), is 68% or higher, (2) The amount of glycerol monoisostearate and/or glycerol monooleate contained in component (A) is 85 mass % or higher with respect to the total amount of (A). | 2012-01-19 |
20120016025 | PERHYDROLASES FOR ENZYMATIC PERACID GENERATION - Disclosed herein are variants enzymes that are structurally classified as CE-7 enzymes and have perhydrolysis activity. Also disclosed herein is a process for producing peroxycarboxylic acids from carboxylic acid esters using the aforementioned variant enzymes as well as methods and compositions comprising the variant enzymes. Further, disinfectant formulations comprising the peroxycarboxylic acids produced by the processes described herein are provided. | 2012-01-19 |
20120016026 | Compositions containing non-polar compounds - Provided are compositions and methods for producing stable foods and beverages that contain high concentrations of additives such as essential fatty acids, including omega-3 fatty acids, omega-6 fatty acids, conjugated fatty acids, and other fatty acids; phytochemicals, including phytosterols and carotenoids; oil soluble vitamins; alpha lipoic acid; other oils; and coenzymes, including Coenzyme Q10, and other oil-based additives. | 2012-01-19 |
20120016027 | Composition and Method for Improved Lens Comfort - The present invention relates to methods of preventing ocular discomfort, improving ocular comfort or ameliorating decrease in ocular comfort during wearing of an ophthalmic device (such as a contact lens), that include the administration of compositions comprising fatty acids, such as omega-3 and/or -6 fatty acids. The present invention also relates to fatty acid compositions suitable for use in the methods of the present invention. | 2012-01-19 |
20120016028 | METHOD OF PREPARING AN UNSATURATED FATTY ACID DRY CONCENTRATE - There is provided a method of preparing an unsaturated fatty acid dry concentrate, wherein a substance comprising at least one unsaturated fatty acid is applied on a biologically inert matrix having a large surface area and is subsequently dried, as well as a composition comprising at least one unsaturated fatty acid and foods, beverages, drugs comprising this composition. | 2012-01-19 |
20120016029 | ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS - Described herein are compounds that are antagonists of PGD | 2012-01-19 |
20120016030 | METHOXYPOLYETHYLENE GLYCOL THIOESTER CHELATE AND USES THEREOF - The present invention is directed generally to protecting cells, tissues and organs against the damaging effects of ionizing or other damaging agents associated with radiation or chemotherapy, or degenerative diseases or processes of various organs that elicit the production of free radicals or oxidants such as peroxides, superoxide anions, hydroxyl radicals or nitric oxides, or heavy metal cations. More particularly, the present invention is concerned with methoxypolyethylene glycol thioester chelate methyl esters that are useful as protectors against tissue damage by penetrating the cell membrane to remove electrons from free radical oxidants and remove heavy metals that may react with peroxides to produce the reactive hydroxyl radical, or remove Ca | 2012-01-19 |
20120016031 | BIPHENYL COMPOUND SELECTIVE AGONISTS OF GAMMA RAR RECEPTORS - Biphenyl compounds having the formula (I): | 2012-01-19 |
20120016032 | Cosmetic Composition Containing Calcium Citrate And N-Acylated Aminoalcohol Derivative To Prevent Dry Skin And Signs Of Cutaneous Ageing - Cosmetic compositions comprising calcium citrate and at least one N-acylated aminoalcohol according to formula (I). | 2012-01-19 |
20120016033 | Small Molecule Antagonists of Phosphatidylinositol-3,4,5-Triphosphate (PIP3) and Uses Thereof - Disclosed are new members of a class of non-lipid small molecule inhibitors which interfere with the interaction between phosphoinositol-3,4,5-triphosphate (PIP3) and pleckstrin homology (PH) domains. These molecules target a broad range of PIP3-dependent signaling events in vitro and exert significant anti-tumor activity in vivo, with improved activity and selectivity toward particular PH domains. The small molecule inhibitors of the invention can be used alone or together with tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) or other cancer medicament to treat cancer. Small molecule inhibitors of the invention act synergistically in combination with TRAIL and with other Akt inhibitors in treating cancer. Pharmaceutical compositions and methods for treating cancer are provided. | 2012-01-19 |
20120016034 | Polymorphic Form Of N-(S)-(3,4-Difluoro-2-(2-Fluoro-4-Iodophenylamino)-6-Methoxyphenyl)-1-(2,- 3-Dihydroxypropyl)Cyclopropane-1-Sulfonamide And Uses Thereof - Disclosed herein, in certain embodiments, is a crystalline polymorph form A of N-(S)-(3,4-difluoro-2 -(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide. Further disclosed herein, in certain embodiments, are pharmaceutical compositions comprising the crystalline polymorph form A of N-(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl) -1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide. | 2012-01-19 |