01st week of 2012 patent applcation highlights part 43 |
Patent application number | Title | Published |
20120004206 | INHIBITORS OF THE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME - The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action. | 2012-01-05 |
20120004207 | THERAPEUTIC USES OF DERIVATIVES OF PIPERIDINYL-AND PIPERIDINYL-ALKYL CARBAMATES - Compound corresponding to the general formula (I): | 2012-01-05 |
20120004208 | BENZOYL-PIPERIDINE DERIVATIVES AS DUAL MODULATORS OF THE 5-HT2A AND D3 RECEPTORS - The present invention relates to compounds of the general formula | 2012-01-05 |
20120004209 | 11-Beta-Hydroxysteroid Dehydrogenase Type 1 Active Compounds - A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11β-hydroxy-steroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome. | 2012-01-05 |
20120004210 | SUBSTITUTED QUINAZOLINE COMPOUNDS - The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder. More particularly, this invention is directed to substituted quinazoline compounds useful as selective kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase-mediated disorder, In particular, the methods relate to treating or ameliorating a kinase-mediated disorder including cardiovascular diseases, diabetes, diabetes-associated disorders, inflammatory diseases, immunological disorders, cancer and diseases of the eye such as retinopathies or macular degeneration or other vitreoretinal diseases, and the like. | 2012-01-05 |
20120004211 | 1,2,4-TRIAZOLE DERIVATIVES AS SIGMA RECEPTOR INHIBITORS - The invention relates to the use of compounds having pharmacological activity towards the sigma receptor, and more particularly to 1,2,4-triazole derivatives of formula I | 2012-01-05 |
20120004212 | ORGANIC COMPOUNDS - A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals | 2012-01-05 |
20120004213 | NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE - The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds. | 2012-01-05 |
20120004214 | N-OXIDES OF 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINYL DERIVATIVES USEFUL AS NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl 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. 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. Formula (I) a stereoisomer or a mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein Ar represents an indolyl group, which indolyl may optionally be substituted one or more times with substituents selected from halo, trifluoromethyl, trifluoromethoxy, cyano, nitro, amino, alkyl, hydroxy and alkoxy. | 2012-01-05 |
20120004215 | N-OXIDES OF DIAZABICYCLONONYL PYRIMIDINE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel N-oxides of certain diazabicyclononyl pyrimidine 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. | 2012-01-05 |
20120004216 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 2012-01-05 |
20120004217 | THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN - A compound of formula: | 2012-01-05 |
20120004218 | NOVEL TETRAHYDRO-QUINOLINE DERIVATIVES - A compound of formula (I) | 2012-01-05 |
20120004219 | Method of Inhibition of Respiratory Depression Using Positive Allosteric AMPA Receptor Modulators - The invention is directed to a method for alleviating respiratory depression in a subject as a result of disease of pharmacological agents such as opiates, opioids or barbiturates. The invention also discloses pharmaceutical compositions for use with the method, the composition containing in combination, an analgesic, anaesthetic, or a sedative and a positive allosteric AMPA receptor modulator in an amount sufficient to reduce or inhibit respiratory depression caused by the analgesic, anaesthetic, or sedative. | 2012-01-05 |
20120004220 | SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMS) AND USES THEREOF - Provided herein are compounds of formulae I to II that bind to androgen receptors and/or modulate activity of androgen receptors; and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions. | 2012-01-05 |
20120004221 | Antibacterial Compositions - Compounds of formula (I) have antibacterial activity: | 2012-01-05 |
20120004222 | CB2 RECEPTOR LIGANDS FOR THE TREATMENT OF PAIN - The present invention relates to compounds represented by Formula (I) and Formula (II): | 2012-01-05 |
20120004223 | COMPOUNDS, COMPOSITIONS AND METHODS FOR REDUCING LIPID LEVELS - The present technology relates to compounds of Formulas (V) and (VI) and methods of making and using such compounds. Methods of use include prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Compounds disclosed herein also lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression, inhibit PCSK9 expression, and activate AMP-activated protein kinase. | 2012-01-05 |
20120004224 | Triheterocyclic Compounds and Compositions Thereof - The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus. | 2012-01-05 |
20120004225 | BUMETANIDE, FUROSEMIDE, PIRETANIDE, AZOSEMIDE, AND TORSEMIDE ANALOGS, COMPOSITIONS AND METHODS OF USE - The present invention provides bumetanide, furosemide, piretanide, azosemide, and torsemide analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide, furosemide, piretanide, azosemide, and torsemide analogs and methods for their use. All of these analogs are particularly useful for the treatment and/or prophylaxis of conditions that involve the Na | 2012-01-05 |
20120004226 | Modulators of Muscarinic Receptors - The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases. | 2012-01-05 |
20120004227 | CYCLOHEXANE DERIVATIVE HAVING NPY Y5 RECEPTOR ANTAGONISM - The present invention discloses novel cyclohexane derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), or a pharmaceutically acceptable salt or a solvate thereof: | 2012-01-05 |
20120004228 | Bis Aromatic Compounds for Use as LTC4 Synthase Inhibitors - There is provided compounds of formula I, | 2012-01-05 |
20120004229 | SUBSTITUTED DIKETOPIPERAZINES AND THEIR USE AS OXYTOCIN ANTAGONISTS - Compounds of formula (1) | 2012-01-05 |
20120004230 | IMIDAZOLE DERIVATIVES - The invention relates to imidazole derivatives which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. | 2012-01-05 |
20120004231 | Substituted Pyridazine Derivatives - The present invention is directed to compounds having histamine H | 2012-01-05 |
20120004232 | 2-AMINO-BICYCLO(3.1.0) HEXANE-2, 6-DICARBOXYLIC ESTER DERIVATIVE - A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration | 2012-01-05 |
20120004233 | TRICYCLIC COMPOUNDS AS ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS - Described herein are antagonists of PGD | 2012-01-05 |
20120004234 | PHTHALAZINE-CONTAINING ANTIDIABETIC COMPOUNDS - This invention provides for certain phthalazine-containing compounds of the formula (I) or a pharmaceutically acceptable salt, ester or solvate thereof, wherein G is an optionally substituted N—N containing heteroaryl group and the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders. | 2012-01-05 |
20120004235 | METHODS TO TREAT CANCER - The invention provides methods and pharmaceutical compositions for treating certain cancers with compounds of formula (I) wherein A, B, W, Y, Z, and R | 2012-01-05 |
20120004236 | SUBSTITUTED TRIAZOLO-PYRIDAZINE DERIVATIVES - This invention relates to novel substituted triazolo-pyridazines, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an α1-GABA-A receptor antagonist and/or a α2, α3 and α5 GABA-A receptor agonist. | 2012-01-05 |
20120004237 | SALT OF CD 80 ANTAGONIST - Choline salt of the CD80 antagonist compound 4-(6-fluoro-3-oxo-1,3-dihydro-pyrazolo[4,3-c]cinnolin-2-yl)-N-(2,2-difluoro-ethyl)-benzamide. | 2012-01-05 |
20120004238 | L-methylfolate treatment for psychiatric or neurologic disorders - Provided herein are methods of treating neuropsychiatric disorders or improving the symptoms associated therewith administering a medical food, such as L-methylfolate, to a subject having the disorder. The neuropsychiatric disorder may be an autism spectrum disorder or attention deficit disorder with or without hyperactivity (ADD/ADHD). The L-methylfolate may be administered as an adjunct to other therapeutic agents effective to treat the disorder. The subject preferably may be a child and also may have a single nucleotide polymorphism in the MTHFR gene associated with reduced expression of MTHFR enzyme. Also provided is a method of increasing the de novo synthesis of neurotransmitters in vivo by transporting a methyl-donating compound across the blood-brain barrier in a subject. | 2012-01-05 |
20120004239 | Process for Preparing Quinoxaline Derivatives - The present invention provides an improved process for preparing a compound of formula (IIIA), an intermediate of the synthesis of varenicline. Also, the present invention provides an improved process for preparing varenicline, or a pharmaceutically acceptable salt or solvate thereof. Furthermore, the present invention provides a process for decolorizing varenicline, or a salt or solvate thereof. Still further, the present invention provides a process of preparing varenicline L-tartrate with improved yield. Still further, the present invention relates to the use of compound of formula (V), or a salt or solvate thereof, as a reference marker and reference standard for assessing the purity of varenicline, or a salt or solvate thereof. | 2012-01-05 |
20120004240 | INHIBITORS OF AKT ACTIVITY - The instant invention provides for substituted fused naphthyridine derivatives that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. | 2012-01-05 |
20120004241 | SUCCINATE SALT OF (2R)-METHYL-1-PIPERAZINE - The present invention relates to a process for the preparation of compounds which are therapeutically active in the central nervous system. | 2012-01-05 |
20120004242 | Oligomer-Diarylpiperazine Conjugates - The invention relates to (among other things) oligomer-diarylpiperazine conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated diarylpiperazine compounds. | 2012-01-05 |
20120004243 | AMIDE DERIVATIVES BEARING A CYCLOPROPYLAMINOACARBONYL SUBSTITUENT USEFUL AS CYTOKINE INHIBITORS - The invention concerns a compound of the Formula (I), wherein Qa is heteroaryl and is substituted with halogeno; R1 and R2 are hydrogen; and Qb is phenyl or heteroaryl, and Qb may optionally bear 1 or 2 substituents selected from hydroxy, halogeno and (1-6C)alkyl, or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines. | 2012-01-05 |
20120004244 | Bis Aromatic Compounds for Use as LTC4 Synthase Inhibitors - There is provided compounds of formula I, | 2012-01-05 |
20120004245 | COMPOUNDS FOR THE TREATMENT OF POSTERIOR SEGMENT DISORDERS AND DISEASES - The use of certain urea compounds, for the treatment of retinal disorders associated with pathologic ocular angiogenesis and/or neovascularization is disclosed. | 2012-01-05 |
20120004246 | PURINYL DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS - This invention relates to novel purinyl derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels. | 2012-01-05 |
20120004247 | ORGANIC COMPOUNDS - A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals | 2012-01-05 |
20120004248 | METHODS OF USING A METHYLXANTHINE COMPOUND - The invention relates to compositions and methods for treating various diseases or medical conditions by administering a methylxanthine compound. Specifically, the invention relates to compositions and methods for treating cytochrome oxidase (CcOX) mediated diseases or medical conditions by administering compositions comprising a methyl xanthine compound. | 2012-01-05 |
20120004249 | The polymorph forms of 4-anilinoquinazoline derivatives, the preparation methods and uses thereof - The present invention relates to polymorphic forms of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazolin-6-yl}-acrylamide p-toluenesulfonate with the characteristic X-ray powder diffraction data as stated in the description, preparation methods thereof, pharmaceutical compositions comprising the same and the use thereof. | 2012-01-05 |
20120004250 | PYRIMIDINE CLASSICAL CANNABINOID COMPOUNDS AND RELATED METHODS OF USE - Disclosed are compounds of the formula I: | 2012-01-05 |
20120004251 | USE OF THE PHYTOCANNABINOID CANNABIDIVARIN (CBDV) IN THE TREATMENT OF EPILEPSY - This invention relates to the use of the phytocannabinoid cannabidivarin (CBDV) and combinations of the phytocannabinoid CBDV with tetrahydrocannabivarin (THCV) and cannabidiol (CBD) in the treatment of epilepsy. The invention further relates to the use of the phytocannabinoid CBDV in combination with standard anti-epileptic drugs (SAEDs). Preferably the SAED is one of ethosuximide, valproate or phenobarbital. | 2012-01-05 |
20120004252 | NEW CCR2 RECEPTOR ANTAGONISTS AND USES THEREOF - The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. | 2012-01-05 |
20120004253 | Novel Fused Pyrrolocarbazoles - The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles. | 2012-01-05 |
20120004254 | G PROTEIN-COUPLED RECEPTOR ANTAGONIST AND ITS USE FOR PREVENTING AND TREATING ALZHEIMER'S DISEASE - The invention discloses methods for screening a reagent for treating or preventing Alzheimer's disease or related neurological pathology. A method according to the invention includes the steps of: (a) activating a receptor and determining a first extent of endocytosis of the receptor, wherein the receptor is a G-protein coupled receptor that associates with presenilin-1; (b) activating the receptor under the same conditions as in step (a), in the presence of a candidate reagent, and determining a second extent of endocytosis of the receptor; (c) determining a difference between the first extent of endocytosis and the second extent of endocytosis; and (d) repeating steps (a)-(c), if the difference is less than a threshold. The invention also disclose uses of receptor antagonists for manufacturing medicaments for treating or preventing Alzheimer's disease or related neurological pathology, wherein the receptor antagonists inhibit endocytosis of a G-protein coupled receptor that associates with presenilin-1 during endocytosis. | 2012-01-05 |
20120004255 | DUAL PHASE DRUG RELEASE SYSTEM - The present invention relates to conjugate comprising a carrier substituted with one or more occurrences of a moiety having the structure: | 2012-01-05 |
20120004256 | PARENTERAL FORMULATION OF CLOPIDOGREL - Described herein are ways to solubilize clopidogrel for parenteral administration containing clopidogrel and a diluent NNDMA (N,N-dimethylacetamide); useful in the prevention of platelet aggregation in acute coronary syndrome, acute myocardial infarction or to prevent platelet facilitated thrombosis following coronary angioplasty and/or coronary stenting. | 2012-01-05 |
20120004257 | NOVEL COMPOUNDS - The present applications discloses novel 8-aza-bicyclo[3.2.1]oct-3-yloxy)chromen-2-one derivatives and their use as monoamine neurotransmitter re-uptake inhibitors. In other aspects the applications discloses the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention. | 2012-01-05 |
20120004258 | QUINUCLIDINE CARBONATE SALTS AND MEDICINAL COMPOSITION THEREOF - Quinuclidine carbonate derivatives act as muscarinic receptor antagonists and are effective for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases. | 2012-01-05 |
20120004259 | METHOD OF TREATMENT OR PROPHYLAXIS - The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT | 2012-01-05 |
20120004260 | INHIBITION OF FATTY ACID SYNTHESIS BY IODO-NITROBENZAMIDE COMPOUNDS AND METHODS OF TREATMENT THEREOF - The present invention relates to a method of treating a fatty acid synthesis related disease comprising administering to a patient in need thereof an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis, wherein the fatty acid synthesis related disease is obesity, diabetes, or cardiovascular disease. The present invention also relates to a method of treating a cancer in a subject comprising: (i) identifying a level of fatty acid in a sample from the subject, and (ii) administering an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis in the subject, wherein the administration is based on the level of fatty acid, thereby treating the cancer in the subject. The present invention further relates to a method of treating Her-2 related cancers by administering to a patient in need thereof an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis. | 2012-01-05 |
20120004261 | MIF MODULATORS - The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression. | 2012-01-05 |
20120004262 | PHENYLCYCLOPROPYLAMINE DERIVATIVES AND THEIR MEDICAL USE - The present invention relates to phenylcyclopropylamine derivatives. In particular, pharmaceutical compositions comprising phenylcyclopropylamine derivatives are provided. The compounds of this invention can, inter alia, be used for the treatment and the prevention of cancer as well as neurodegenerative diseases or disorders. | 2012-01-05 |
20120004263 | Compounds for the treatment of pathologies associated with aging and degenerative disorders - The present invention relates to methods of inhibiting one or more signs of aging and/or degenerative disorder in a subject in need of such treatment, which comprise administering, to the subject, an effective amount of one or more of the compounds as set forth herein. “Inhibiting a sign of aging or degenerative disorder” means reducing the risk of occurrence, delaying the onset, slowing the progression, and/or reducing the severity and/or manifestation, of a sign of aging or degenerative disorder, and includes, but is not limited to, preventing the occurrence, development or progression of a sign of aging or degenerative disorder. | 2012-01-05 |
20120004264 | 2-PHENYLPROPIONIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - 4-(trifluoromethanesulfonyloxyphenyl)propionic acid derivatives and pharmaceutical composition containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion. | 2012-01-05 |
20120004265 | Ophthalmic Compositions and Methods of Using the Same - Ophthalmic compositions are provided that comprise or consist essentially of (a) ketotifen or a ketotifen salt, (b) a non-ionic tonicity agent, and (c) water. The concentration of ketotifen or the ketotifen salt is preferably from 0.01% to 0.05%. The non-ionic tonicity agent is preferably glycerol and the concentration of the glycerol is preferably from 4% to 7%. The compositions preferably have an osmolality of from 400 to 875 milliosmoles/Kg. The compositions may also contain an anti-redness agent. Methods of treating allergic conjunctivitis using the ophthalmic compositions and methods of treating dry eye disease using the ophthalmic compositions are also provided. | 2012-01-05 |
20120004266 | DOPAMINE-BETA-HYDROXYLASE GENETIC POLYMORPHISM AND MIGRAINE - The invention provides a method of determining whether or not an individual has a predisposition to migraine including the step of determining whether an isolated nucleic acid obtained from the individual comprises a nucleotide sequence corresponding to at least a fragment of a dopamine β-hydroxylase (DBH) gene promoter, wherein the presence of a −1021C→T single nucleotide polymorphism (SNP) in said nucleotide sequence indicates whether or not said individual has an increased predisposition to migraine compared to an individual without the polymorphism. DBH −1021C/C homozygotes are particularly susceptible to migraine. The −1021T allele may exert a protective effect. The method is particularly suited to detection of a predisposition to migraine with aura in females. The invention also provides a diagnostic kit for detecting a −1021C→T SNP associated with migraine. The method and kit may facilitate selection of individuals for migraine therapy which targets the dopaminergic system. | 2012-01-05 |
20120004267 | APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS - The present invention relates to compounds of Formula (I): | 2012-01-05 |
20120004268 | INSECTICIDAL COMPOSITIONS COMPRISING CYCLIC CARBONYLAMIDINES - Compositions comprising at least one cyclic carbonylamidine of the formula (I) | 2012-01-05 |
20120004269 | Alkynyl Phenyl Derivative Compounds for Treating Ophthalmic Diseases and Disorders - Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions. | 2012-01-05 |
20120004270 | Selective Androgen Receptor Modulators - This invention provides compounds as described herein or pharmaceutically acceptable salte thereof, pharmaceutical compositions comprising a compound as described herein or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor using the compounds or compositions described herein, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) using the compounds and compositions described herein and processes for making compounds described herein and intermediates useful in the preparation of same. | 2012-01-05 |
20120004271 | USE OF VAGINALLY-ADMINISTERED INSULIN SENSITIZING AGENTS - Use of vaginal insulin sensitising agents for the prevention and/or treatment of hyperandrogenism and/or polycystic ovary syndrome and/or related disorders. | 2012-01-05 |
20120004272 | BIOCIDAL COMPOSITION OF 2,6-DIMETHYL-M-DIOXANE-4-OL ACETATE AND METHODS OF USE - Provided are compositions comprising 2,6-dimethyl-m-dioxane-4-ol acetate and a biocidal compound selected from the group consisting of: a biocidal oxazolidine; 1-(3-chloroallyl)-3,5,7-triaza-1-azoniaadamantane; and tris(hydroxymethyl)-nitromethane. The compositions are useful for controlling microorganisms in aqueous or water containing systems. | 2012-01-05 |
20120004273 | GLYT1 TRANSPORTER INHIBITORS AND USES THEREOF IN TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS - Disclosed herein are compounds of formula (I) and: | 2012-01-05 |
20120004274 | USE OF INHIBITORS OF JUN N-TERMINAL KINASES TO TREAT GLAUCOMA - Compositions and methods for lowering IOP and/or providing neuroprotection are disclosed. The compositions and methods are particularly directed to the use inhibitors of Jun N-terminal kinases (JNK) to lower IOP and/or provide neuroprotection. | 2012-01-05 |
20120004275 | SCELETIUM EXTRACT AND USES THEREOF - A composition including as an active ingredient an extract of a plant of the family Mesembryanthemaceae with mesembrenol and mesembrenone as the two major alkaloids present. The invention also relates to the use of the composition as a PDE4 inhibitor and as a serotonin-uptake inhibitor, preferably applied in formulations for the use of the composition as a dual serotonin-uptake inhibitor and PDE4 inhibitor. The invention extends to compositions, such as pharmaceutical compositions or compositions used as dietary supplements, the total alkaloid content of which includes at least 80% (w/w) combined content of mesembrenol and mesembrenone, less than 5% (w/w) mesembrine, and at least 7% (w/w) mesembranol. | 2012-01-05 |
20120004276 | RNA ANTAGONIST COMPOUNDS FOR THE INHIBITION OF EXPRESSION OF MITOCHONDRIAL GLYCEROL-3 PHOSPHATE ACYLTRANSFERASE 1 (MTGPAT1) - The present invention relates to oligomer compounds (oligomers), which target mtGPAT1mRNA in a cell, leading to reduced expression of mtGPAT1. Reduction of mtGPAT1 expression is beneficial for the treatment of certain medical disorders, such as overweight, obesity, fatty liver, hepatosteatosis, non alcoholic fatty liver disease (NAFLD), non alcoholic steatohepatitis (NASH), insulin resistance, and non insulin dependent diabetes mellitus (NIDDM). | 2012-01-05 |
20120004277 | VECTOR(S) CONTAINING AN INDUCIBLE GENE ENCODING A CDK4/CDK6 INHIBITOR USEFUL FOR TREATING NEURODEGENERATIVE DISORDERS OR DISEASES ASSOCIATED WITH AN UNSCHEDULED ACTIVATION OF THE CELL CYCLE - Described are vectors containing (a) a gene encoding (i) a CDK4/CDK6 inhibitor, preferably p16 | 2012-01-05 |
20120004278 | LINC RNAS IN CANCER DIAGNOSIS AND TREATMENT - Long non-coding RNAs (lincRNAs), a relatively recently recognized class of widely transcribed genes, are thought to affect chromatin state and epigenetic regulation, but their mechanisms of action and potential roles in human disease are poorly understood. The present invention shows that long non-coding RNAs in the human HOX loci are systematically dysregulated during breast cancer progression, and that expression levels of the lincRNA termed HOTAIR can predict cancer metastasis. Elevated levels of HOTAIR can lead to altered patterns of Polycomb binding to the genome. These findings indicate that lincRNAs have active roles in modulating the cancer epigenome and may be important targets for cancer diagnosis and therapy. | 2012-01-05 |
20120004279 | COMPOSITIONS AND METHODS FOR MODULATING ACTIVITY OF CAPPED SMALL RNAS - Compositions and methods for modulating transcription by RNA polymerases are described. | 2012-01-05 |
20120004280 | RNA Interference Mediated Inhibition of the High Affinity 1 gE Receptor Alpha Chain (FC Epsilon R1 Alpha) 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 FCεR1α gene expression and/or or activity, and/or modulate a FCεR1α gene expression pathway. Specifically, the invention relates to doublestranded 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 FCεR1α gene expression. | 2012-01-05 |
20120004281 | RNA Interference Mediated Inhibition of the Nerve Growth Factor Beta Chain (NGFB) 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 NGFβ gene expression and/or activity, and/or modulate a NGFβ 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 NGFβ gene expression. | 2012-01-05 |
20120004282 | RNA Interference Mediated Inhibition of the Intercellular Adhesion Molecule 1 (ICAM-1) 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 ICAM-1 gene expression and/or activity, and/or modulate a ICAM-1 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 ICAM-1 gene expression. | 2012-01-05 |
20120004283 | NOVEL SHRNA GENE THERAPY FOR TREATMENT OF ISCHEMIC HEART DISEASE - Short hairpin RNA (shRNA) interference therapy targeting hypoxia inducible factor—lot (HIF-1 α) prolyl-4-hydroxylase protein (HIF-PHD2) is used for treatment of myocardial ischemia. This treatment can be followed noninvasively by molecular imaging. Provided are compositions comprising novel vectors encoding shRNA targeting the HIF-1α and asparaginyl hydroxylase genes. The vectors encoding shRNA are also useful for the treatment of cardiac diseases, peripheral vascular diseases and decubitis ulcers. | 2012-01-05 |
20120004284 | PDK INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF - The invention relates to methods of treating or preventing acquired or congenital mitochondrial diseases or disorders, including treating cell proliferation related disorders or diseases, such as cancer. The invention further relates to pharmaceutical compositions for treating such disorders or diseases. | 2012-01-05 |
20120004285 | ERBB-3 (HER3)-SELECTIVE COMBINATION THERAPY - The invention relates to pharmaceutical compositions for and methods of treatment with HER3-targeted combination therapy. The invention relates to pharmaceutical compositions comprising an oligomer which targets HER3 (and optionally one or more of HER2 and EGFR) mRNA in a cell, leading to reduced expression of HER3 and optionally HER2 and/or EGFR, and a small molecule protein tyrosine kinase inhibitor of one or more receptor tyrosine kinases, leading to inhibition of signaling and/or internalization of receptor dimers into the cell. The combination therapy is beneficial for a range of medical disorders, such hyperproliferative disorders (e.g., cancer). The invention provides methods of treating hyperproliferative disorders with a combination of an oligomer and a protein tyrosine kinase inhibitor. | 2012-01-05 |
20120004286 | LONG-ACTING VETERINARY POLYPEPTIDES AND METHODS OF PRODUCING AND ADMINISTERING SAME - A polypeptide and polynucleotides comprising at least two carboxy-terminal peptides (CTP) of chorionic gonadotrophin attached to a non-human peptide-of-interest are disclosed. Pharmaceutical compositions comprising the non-human polypeptides and polynucleotides of the invention and methods of using both human and non-human polypeptides and polynucleotides are also disclosed. | 2012-01-05 |
20120004287 | THERAPEUTIC AGENT COMPRISING VASOHIBIN - A therapeutic agent containing Vasohibin for diabetic nephropathy, and a therapeutic agent containing Vasohibin for peritoneal sclerosis. Since the therapeutic agent containing Vasohibin of the present invention is a substance in which Vasohibin inhibits angiogenesis in an autocrine manner, the therapeutic agent is effective for inhibiting the progression of diabetic nephropathy and peritoneal sclerosis in which the inhibition in the angiogenesis or the production of cytokine is important, so that the therapeutic agent is suitably used in, for example, the treatment of a disease requiring an action for inhibiting the progression of diabetic nephropathy, and a disease requiring an inhibitory action for peritoneal sclerosis, or the like. | 2012-01-05 |
20120004288 | COMPOUNDS FOR THE MODULATION OF BETA-CATENIN EXPRESSION - The invention relates to oligomer compounds (oligomers), which target beta-catening mRNA in a cell, leading to reduced expression of beta-catenin. Reduction of beta-catenin expression is beneficial for a range of medical disorders, such as hyperproliferative disorders, such as cancer. The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of beta-catenin using said oligomers, including methods of treatment. | 2012-01-05 |
20120004289 | ANNEXIN A11 AND ASSOCIATED GENES AS BIOMARKERS FOR CANCER - The instant invention provides methods and compositions for the diagnosis and treatment of cancer. The invention also provides method and compositions for determining if a subject is, or is at risk of becoming, chemoresistant. | 2012-01-05 |
20120004290 | TREATING CHRONIC FATIGUE SYNDROME AND PROLONGED QT INTERVAL - Chronic fatigue syndrome and prolonged QT interval are treated using one or more different double-stranded ribonucleic acids (dsRNA). | 2012-01-05 |
20120004291 | COMPANION ANIMAL COMPOSITIONS INCLUDING PYRUVIC ACID AND SALTS THEREOF AND METHODS OF USE THEREOF - The invention encompasses pet food compositions and methods for the treatment and/or prevention of diseases or disorders in companion animals, for example, for the treatment or obesity, including administering a pet food composition including pyruvic acid or a salt thereof to a companion animal, or lipoic acid or salt thereof and pyruvic acid or a salt thereof to a companion animal. The invention encompasses pet food compositions and methods for managing weight including administering a pet food composition including pyruvic acid or a salt thereof, or lipoic acid or a salt thereof and pyruvic acid or a salt thereof to a companion animal to a companion animal. | 2012-01-05 |
20120004292 | COMPOSITION FOR INJECTION COMPRISING AN INJECTION MEDICINAL PRODUCT AND A GEL - A composition of an injectable medicinal product and a gel, concentrating the medicinal product on-site to reinforce its action and/or reduce the toxicity of the medicinal product. | 2012-01-05 |
20120004293 | Cancer Cell Targeting Using Nanoparticles - The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries. | 2012-01-05 |
20120004294 | ANTITUMOR COMBINATION COMBINING AVE8062 AND DOCETAXEL - The invention relates to a sequential antitumor combination of AVE8062, or a salt thereof, and docetaxel, characterized in that AVE8062 is administered to a patient in a dose of 10 to 50 mg/m2, and then, on a different day of the week, preferably after a 24-hour interval, docetaxel is administered in a dose of 50 to 120 mg/m2. | 2012-01-05 |
20120004295 | ADMINISTRATION OF 6'-ETHYL LEPIMECTIN, 6'-METHYL LEPIMECTIN OR DERIVATIVES THEREOF FOR TREATING DERMATOLOGICAL DISORDERS IN HUMANS - 6′-ethyl lepimectin, 6′-methyl lepimectin or derivatives thereof are formulated into pharmaceutical compositions useful for the treatment of dermatological conditions in humans, in particular rosacea. | 2012-01-05 |
20120004296 | CHROMAN DERIVATIVES, MEDICAMENTS AND USE IN THERAPY - Novel chroman derivatives and intermediate compounds, compositions containing same, methods for their preparation and uses thereof as therapeutic agents particularly as anti-cancer and chemotherapeutic selective agents are described. | 2012-01-05 |
20120004297 | Agent for alleviating vascular failure - An agent for alleviating, treating and preventing vascular failure and a vascular endothelial cell-protecting agent characterized by containing, as an effective ingredient, at least one active oxygen scavenger such as astaxanthin and tocotrienols; and a food, a drink and an animal feed having an effect of alleviating, treating and preventing vascular failure and an effect of protecting vascular endothelial cells characterized by containing, as the effective ingredient, at least one active oxygen scavenger such as astaxanthin and tocotrienols. | 2012-01-05 |
20120004298 | OPHTHALMIC DEVICES CONTAINING CHEMOKINE ANTAGONISTS - Ionic ophthalmic devices, methods of treating chemoattractant cytokine receptor 2 (CCR2) mediated inflammatory conditions, and methods of making such devices are disclosed herein. | 2012-01-05 |
20120004299 | AZEOTROPE-LIKE COMPOSITIONS OF CIS-1,1,1,4,4,4-HEXAFLUORO-2-BUTENE - This invention relates to azeotrope-like compositions, methods and systems having utility in numerous applications, and in particular, uses for azeotrope-like compositions comprising effective amounts of the compound cis-1,1,1,4,4,4-hexafluoro-2-butene (Z-HFO-1336mzzm), which has the following structure: | 2012-01-05 |
20120004300 | METHODS FOR TREATING BIPOLAR DISORDER - The invention is directed to a method of treating bipolar disorder in a subject, comprising administering a therapeutically effective amount of a carbamate compound, or pharmaceutically acceptable salt or amide thereof. | 2012-01-05 |
20120004301 | METHODS FOR TREATING RESTLESS LEGS SYNDROME - The invention is directed to a method of treating restless legs syndrome in a subject, comprising administering a therapeutically effective amount of a carbamate compound, or pharmaceutically acceptable salt or amide thereof. | 2012-01-05 |
20120004302 | Cosmetic Use of N-Substituted Sulfonyloxybenzylamines and Related Compounds - Cosmetic compositions comprising N-substituted sulfonyloxybenzylamines and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The N-substituted sulfonyloxybenzylamines are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging. | 2012-01-05 |
20120004303 | METHOD OF DISPENSING A TEETHING GEL WITH A METERED DOSE APPLICATOR - A method of treating periodontal pain from teething that uses an applicator to dispense a medicament composition, wherein said applicator dispenses a metered dose of a therapeutic amount of said medicament composition. | 2012-01-05 |
20120004304 | BILE SALT ADJUVANT FOR ANIMALS FOR IMPROVING FAT UTILIZATION EFFICIENCY IN THE BODIES OF ANIMALS, AND ANIMAL FEED COMPRISING SAME - The present invention relates to a bile salt adjuvant for animals for improving fat utilization efficiency in the bodies of the animals, and to animal feed comprising same. More particularly, the present invention relates to a bile salt adjuvant for animals comprising sodium stearoyl-2-lactylate. The adjuvant is used in animal feed to improve fat utilization efficiency in the bodies of livestock when ingested by said livestock, thereby reducing the amount of fat required to be used in animal feed and improving productivity. | 2012-01-05 |
20120004305 | EXTERNAL PREPARATION CONTAINING ANALGESIC/ANTI-INFLAMMATORY AGENT - An external preparation containing the following components (A), (B), (C), and (D):
| 2012-01-05 |