19th week of 2011 patent applcation highlights part 47 |
Patent application number | Title | Published |
20110112094 | Methods of Treating Pulmonary Hypertension - Methods of treating pulmonary hypertension are disclosed. Particular methods comprise the administration of a tryptophan hydroxylase inhibitor and a prostacyclin. Pharmaceutical formulations are also disclosed. | 2011-05-12 |
20110112096 | PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS - The invention provides novel pyrimidine derivatives of formula (I) and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-IR) or analplastic lymphoma kinase (ALK). | 2011-05-12 |
20110112097 | Substituted imidazoline-2,4-diones, process for preparation thereof, medicaments comprising these compounds and use thereof - The invention relates to compounds of formula (I) wherein the groups R and R′, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs. | 2011-05-12 |
20110112098 | MOLECULES INHIBITING A METABOLIC PATHWAY INVOLVING THE SYK PROTEIN TYROSINE KINASE AND METHOD FOR IDENTIFYING SAID MOLECULES - The present invention relates to the C-13 molecule (methyl 2-{5-[(3-benzyl-4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]-2-furyl}-benzoate) and to organic molecules functionally equivalent to the C-13 molecule, capable of inhibiting the binding of an antibody or antibody fragment with the human Syk protein tyrosine kinase, to the use of these molecules for the production of medicaments for the prevention or treatment of diseases dependent on metabolic pathways involving Syk, and also to a method for identifying such molecules. | 2011-05-12 |
20110112099 | THERAPEUTIC AGENT FOR CANCER RESISTANT TO PROTEASE INHIBITOR - The present invention provides therapeutic agents for a cancer resistant to a protease inhibitor which comprises, as an active ingredient, a benzoyl compound represented by formula (I): | 2011-05-12 |
20110112100 | Hepatitis C Virus Inhibitors - The present invention relates to compounds of the formula (I) | 2011-05-12 |
20110112101 | TREATMENT FOR OCULAR-RELATED DISORDERS - A treatment for ocular related disorders, such as macular degeneration, and preferably age-related macular degeneration, diabetic retinopathy, and diabetic macular edema is disclosed, using a compound of Formula I. | 2011-05-12 |
20110112102 | METHOD OF TREATING CANCER USING A NEUROPEPTIDE Y 5R (NP Y5R) ANTAGONIST - The present invention relates to methods for treating cancer by administering a therapeutically effective amount of compound of formula (I), such as selective NPY5R antagonist MK-0557 (trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro[6-azaisobenzofuran-1(3H), 1′-cyclohexane]-4′-carboxamide), or a pharmaceutically acceptable salt thereof, to a subject in need thereof The methods can further comprise administering a chemotherapeutic agent to the subject in need thereof. | 2011-05-12 |
20110112103 | 5-HYDROXYPYRIMIDINE-4-CARBOXAMIDE COMPOUND - The present invention provides compounds which promote erythropoietin production. Compounds represented by the following general formula (1) or pharmacologically acceptable salts thereof are provided: | 2011-05-12 |
20110112104 | TRICYCLIC COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM. - Compounds of formula (I): | 2011-05-12 |
20110112105 | SUBSTITUTED HETEROCYCLE FUSED GAMMA-CARBOLINES SOLID - The present invention relates to toluenesulfonic acid addition salt crystals of specific substituted heterocycle fused gamma-carbolines, the method of making and using such crystals. | 2011-05-12 |
20110112106 | TRICYCLIC INHIBITORS OF 5-LIPOXYGENASE - Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of 5-lipoxygenase (5-LO). Also described herein are methods of using such 5-LO inhibitors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions, diseases, or disorders. | 2011-05-12 |
20110112107 | SUBSTITUTED 6-(1-PIPERAZINYL)-PYRIDAZINES AS 5-HT6 RECEPTOR ANTAGONISTS - The present invention is concerned with novel substituted 6-(1-piperazinyl)-pyridazines of Formula (I) | 2011-05-12 |
20110112108 | PYRIDAZINE FUNGICIDES - The present invention relates to novel pyridazine derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R | 2011-05-12 |
20110112109 | TRIAZOLONE DERIVATIVES - A compound represented by the following general formula (1) or salts thereof or hydrates of the foregoing: | 2011-05-12 |
20110112110 | ANTIPROLIFERATIVE COMPOUNDS AND THERAPEUTIC USES THEREOF - Inhibitors of the oncogenic tyrosine kinase ALK and of the Bcr-Abl mutant T315I Bcr-Abl, pharmaceutical compositions containing the same and their use for the treatment of hyper-proliferative diseases. | 2011-05-12 |
20110112111 | DRUG COMBINATIONS COMPRISING A DGAT INHIBITOR AND A PPAR-AGONIST - The present invention relates to combinations of a DGAT inhibitor and a peroxisome proliferator-activator receptor (PPAR) agonist or a prodrug thereof. The invention further relates to methods for preparing such combinations, pharmaceutical compositions comprising said combinations as well as the use as a medicament of said combinations. | 2011-05-12 |
20110112112 | APOGOSSYPOLONE DERIVATIVES AS ANTICANCER AGENTS - The disclosure provides compounds and methods of using Apogossypolone derivatives for treating diseases and disorders. In particular, the disclosure provides compounds of Formula I: | 2011-05-12 |
20110112113 | METHODS OF PREDICTING AND TREATING ADVERSE CARDIAC EVENTS - The invention provides methods for treatment of acute coronary syndrome and prediction of adverse cardiac events on the basis of elevations of catalytic iron in biological fluid of a human subject. An embodiment of the invention provides a method for early detection of acute coronary syndrome (ACS) in a human subject at the time of presentation of the chest pain. The method includes analyzing a test sample of the biological fluid for amount of catalytic iron and detecting acute coronary syndrome in the human subject. | 2011-05-12 |
20110112114 | INHIBITORS OF SERINE PROTEASES, PARTICULARLY HEPATITIS C VIRUS NS3 PROTEASE - The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus. | 2011-05-12 |
20110112115 | POLYMERIC MICROEMULSIONS - The invention provides novel self-emulsifying diblock copolymers and novel self-emulsifying compositions comprising an active ingredient and a diblock copolymer characterized in that the diblock copolymer is liquid at a temperature below 50° C. and the composition is non-aqueous and liquid at a temperature below 50° C. | 2011-05-12 |
20110112116 | COMPOSITIONS OF 5-HT3 ANTAGONISTS AND DOPAMINE D2 ANTAGONISTS FOR TREATMENT OF DOPAMINE-ASSOCIATED CHRONIC CONDITIONS - Methods are provided for partial aortic obstruction for cerebral perfusion augmentation in patients suffering from global or focal cerebral ischemia. Alternatively, the methods can be used to partially obstruct aortic blood flow to condition the spinal cord to secrete neuroprotective agents prior to abdominal aortic aneurysm repair. Partial obstruction of a vessel can be accomplished by a device comprising an elongate catheter and a distally mounted expandable member. The expandable member may comprise one or two balloons. Other medical devices, such as an angioplasty, stent, or atherectomy catheter, can be inserted distal the expandable member to provide therapeutic intervention. | 2011-05-12 |
20110112117 | TREATMENT OF HERPES VIRUS RELATED DISEASES - Anti-herpetic material such as 2-aminopurine derivatives, e.g., the aminocyclopropylcarboxylate derivatives of acyclovir, penciclovir, and ganciclovir, are described to prevent or treat autoimmune disease or a disease originating from an abnormal functioning of the sympathetic chain in a human subject. Prolonged use of the anti-herpetic compounds reduces prodrome, vesicle formation and viral shedding. The anti-herpetic compounds may be administered alone or in combination with a compound that reduces the rate of renal excretion of the anti-herpetic compound. The anti-herpetic compounds are particularly useful when administered at a level equivalent in activity to at—least about 150 mg/kg famciclovir per day. | 2011-05-12 |
20110112118 | 2,4-Diaminoquinazolines for Spinal Muscular Atrophy - 2,4-Diaminoquinazolines of formulae I-IV and VI | 2011-05-12 |
20110112119 | AZABICYCLOOCTYL-QUINAZOLONE DERIVATIVES USEFUL AS NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS - This invention relates to novel azabicyclooctyl-quinazolinone 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. | 2011-05-12 |
20110112120 | HETEROMONOCYCLIC COMPOUND AND USE THEREOF - A compound represented by the formula (I): | 2011-05-12 |
20110112121 | Pharmaceutical Compositions and Solid Forms - The present invention relates to pharmaceutical compositions of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide, to the use of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide and compositions of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide in therapeutic applications, especially indications with a dysregulation/overexpression of VEFG, (neo)-vascularisation and VEGF driven angiogenesis and to methods for manufacturing such compositions, the invention further relates to specific forms of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide and to the manufacturing and use of such forms. The present invention also relates to a new process to produce 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide. | 2011-05-12 |
20110112122 | EPIMINOCYCLOALKYL[b] INDOLE DERIVATIVES AS SEROTONIN SUB-TYPE 6 (5-HT6) MODULATORS AND USES THEREOF - The present invention relates to epiminocycloalkyl[b]indole derivatives as serotonin sub-type 6 (5-HT | 2011-05-12 |
20110112123 | Compositions for Intratumoral Administration - The present disclosure describes compositions for intratumoral administration which include a tissue-stabilizing agent and a therapeutic agent. | 2011-05-12 |
20110112124 | FUNGICIDAL COMPOSITIONS - A method of controlling phytopathogenic diseases on useful plants or on propagation material thereof, which comprises applying to the useful plants, the locus thereof or propagation material thereof a combination of components A) and B) in a synergistically effective amount, wherein component A) is a compound of formula (I) wherein R | 2011-05-12 |
20110112125 | Novel hair growth composition - A water-soluble minoxidil composition for topical use significantly enhances the transdermal delivery of the drug in comparison with that of Rogaine. The composition contains minoxidil, water, enhancer, and polymer. The percentage of water in the composition may be up to 95%. | 2011-05-12 |
20110112126 | ENZYME INHIBITING COMPOUNDS - The present invention is directed to compounds that are specifically structured to provide enzyme inhibition. In specific embodiments, the enzyme inhibiting compounds exhibit antifolate activity. Particularly, the inventive compounds are formed of an antifolate residue that is active in inhibiting one or more of TS, DHFR, GAR, FPGS, and AICAR Tfase. The enzyme inhibiting compounds are useful in a variety of methods of treatment, including treating abnormal cell proliferation and treating inflammation. | 2011-05-12 |
20110112127 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, or forms thereof are active on Fms protein kinase, or on Fms and Kit protein kinase, or on Fms and Flt-3 protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Fms protein kinase, Kit protein kinase, or Flt-3 protein kinase including rheumatoid arthritis, osteoarthritis, multiple sclerosis, Alzheimer's disease, Parkinson's disease, glomerulonephritis, interstitial nephritis, Lupus nephritis, tubular necrosis, diabetic nephropathy, renal hypertrophy, acute myeloid leukemia, melanoma, multiple myeloma, metastatic breast cancer, prostate cancer, pancreatic cancer, neurofibromatosis, brain metastases, and gastrointestinal stromal tumors. | 2011-05-12 |
20110112128 | METHOD OF TREATING ILEUS BY PHARMACOLOGICAL ACTIVATION OF CHOLINERGIC RECEPTORS - A method of treating ileus in a subject by administering to the subject an effective amount of a pharmacological agent that increases the activity of cholinergic receptor in a subject. Examples of pharmacological agents are brain muscarinic agonist, cholinergic agonist or cholinesterase inhibitor. The methods of the present invention can be used to treat ileus caused by abdominal surgery, or administration of narcotics or chemotherapeutic agents such as during cancer chemotherapy. | 2011-05-12 |
20110112132 | MEANS FOR THE TREATMENT OF ACUTE AND CHRONIC DISORDERS OF CEREBRAL CIRCULATION, INCLUDING INSULT, BASED ON HYDROGENATED PYRIDO (4,3-B) INDOLES (VARIANTS), PHARMACOLOGICAL MEANS BASED THEREON AND METHOD FOR THE USE THEREOF - A means for the treatment of insult based on hydrogenated pyrido(4,3-b)indoles (variants) of formula (1) or formula (2) a pharmacological means based thereon and a method for the use thereof relate to the use of chemical compounds in the field of medicine and may be used for the treatment of ischemic and hemorrhagic insults and their consequences. | 2011-05-12 |
20110112133 | DIHYDRO PYRROLOQUINOLINE DERIVATIVES - A compound represented by the formula (I) | 2011-05-12 |
20110112134 | Tricyclic Antagonists of Prostaglandin D2 Receptors - Described herein are compounds that are antagonists of PGD | 2011-05-12 |
20110112135 | Imidazo [1,2-A] Pyridine Compounds - This invention relates generally to imidazo[1,2-a]pyridine-based modulators of Liver X receptors (LXRs) having formula (I) and related methods: | 2011-05-12 |
20110112136 | NOVEL PROCESS FOR THE MANUFACTURE OF PHARMACEUTICAL PREPARATIONS - The present invention is related to an improved method for the manufacture of Micro-precipitated Bulk Powder (MBP) containing the active pharmaceutical ingredient Propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3- | 2011-05-12 |
20110112137 | HIV PROTEASE INHIBITOR AND CYTOCHROME P450 INHIBITOR COMBINATIONS - Compositions and methods of treating viral infections are provided. More particularly, compositions including a combination of protease inhibitors and cytochrome p450 enzyme inhibitors are provided. Methods of using the compositions for treatment of diseases or disorders caused by a virus such as HIV infections are also provided. | 2011-05-12 |
20110112138 | MULTI-CYCLIC CINNAMIDE DERIVATIVES - The present invention provides a compound represented by the formula (I): | 2011-05-12 |
20110112139 | NOVEL 8-AZA-BICYCLO[3.2.1]OCTANE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - This invention relates to novel 8-aza-bicyclo[3.2.1]octane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. | 2011-05-12 |
20110112140 | INHIBITOR OF PLASMINOGEN ACTIVATOR INHIBITOR-1 - The present invention relates to a novel compound having plasminogen activator inhibitor-1 (PAI-1) inhibitory activity, and a PAI-1 inhibitor comprising the compound as an active ingredient. The present invention further relates to a pharmaceutical composition that has an inhibitory action on PAI-1 activity and is useful in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. The novel compound is represented by the following general formula. | 2011-05-12 |
20110112141 | CRYSTALS OF LAQUINIMOD SODIUM, AND PROCESS FOR THE MANUFACTURE THEREOF - Disclosed is a process for the preparation of laguinimod sodium which removes the impurities after the salt formation step, thus resulting in crystals of higher purity as well as crystals having improved crystalline characteristics. | 2011-05-12 |
20110112142 | NOVEL ESTROGEN RECEPTOR LIGANDS - The invention provides a pharmaceutical composition comprising 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: wherein R | 2011-05-12 |
20110112143 | ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to new compounds of formula (I) wherein A, B, P, Q, W, R | 2011-05-12 |
20110112144 | METHODS OF PREPARING SUBSTITUTED HETEROCYCLES - The present disclosure relates to methods of preparing substituted thiophenes, which are useful for the treatment and prevention of cancers. Also disclosed are substituted thiophenes made by the methods disclosed herein. | 2011-05-12 |
20110112145 | Salts Of Methyl 2-((R))-(3-Chlorophenyl)((R)-1-((S)-2-(Methylamino)-3((R)-tetrahydro-2H-P- yran-3-YL)Propylcarbamoyl)Piperidin-3-YL)Methoxy)Ethylcarbamate - Disclosed are salts of methyl 2-((R)-(3-chlorophenyl)((R)-1-((S)-2-(methylamino)-3-((R)-tetrahydro-2H-pyran-3-yl)propylcarbamoyl)piperidin-3-yl)methoxy)ethylcarbamate and pharmaceutical compositions containing the same. Also disclosed are processes for the preparation thereof and methods for use thereof. | 2011-05-12 |
20110112146 | CHROMENE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY - The present application describes modulators of MCP-1 or CCR-2 of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W | 2011-05-12 |
20110112147 | INDAZOLONE ANALOGS AS GLYCOGEN SYNTHASE ACTIVATORS - Provided herein are compounds of the formula (I): | 2011-05-12 |
20110112148 | INDOLINE COMPOUNDS - This invention provides new 2,3-dihydro-indole compounds, their use for the treatment or prevention of melatonin-ergic disorders and its compositions. | 2011-05-12 |
20110112149 | EPOTHILONE ANALOGUES, THEIR PHARMACEUTICAL COMPOSITIONS, THEIR USE AND THEIR PREPA RATIONS - The present invention relates to novel 15-membered thiazole lactone or lactam polyketide compounds, their pharmaceutical compositions, their use and their preparations. The disclosed compounds relate to those of general formula I, their preparations and their use for preparing therapeutical compositions used as cell inhibitors. | 2011-05-12 |
20110112150 | USE OF 1-HYDROXY-2-PYRIDONES FOR THE TREATMENT OF SEBORRHEIC DERMATITIS -
Compounds of the formula (I) are disclosed and are suitable for the treatment of seborrheic dermatitis.
| 2011-05-12 |
20110112151 | COMPOUND CAPABLE OF INHIBITING 11-BETA HYDROXYSTERIOD DEHYDROGENASE - There is provided a compound of formula R | 2011-05-12 |
20110112152 | PYRIDONE SULFONAMIDES AND PYRIDONE SULFAMIDES AS MEK INHIBITORS - This invention concerns N-(ortho phenylamino dihydropyridyl)sulfonamides and N-(ortho phenylamino dihydropyridyl), N′-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases. | 2011-05-12 |
20110112153 | USE OF 1-HYDROXY-2-PYRIDONES FOR THE TREATMENT OF SEBORRHEIC DERMATITIS - Compounds of the formula (I) are disclosed and are suitable for the treatment of seborrheic dermatitis. | 2011-05-12 |
20110112154 | Compounds, compositions and methods - Certain substituted sulfonamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure. | 2011-05-12 |
20110112155 | METHODS FOR TREATING CANCER IN PATIENTS HAVING BREAST CANCER RESISTANCE PROTEIN OVEREXPRESSION - A method for treating cancer comprising identifying a mammal that overexpresses breast cancer resistance protein; and administering to said mammal a pharmaceutical composition comprising a therapeutically effective amount of ixabepilone. In one aspect, the mammal is not administered an agent that is susceptible to breast cancer resistance protein overexpression resistance. In another aspect, the cancer is breast and/or lung cancer. | 2011-05-12 |
20110112156 | Bicyclic Derivatives as Modulators of Voltage Gated ION Channels - Bicyclic derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions. | 2011-05-12 |
20110112157 | PROCESS FOR THE PREPARATION OF ZOLMITRIPTAN, SALTS AND SOLVATES THEREOF - The present invention relates to an improved process for the preparation of the active pharmaceutical ingredient zolmitriptan. In particular, it relates to an efficient process for the preparation of zolmitriptan and its pharmaceutically acceptable salts and solvates. | 2011-05-12 |
20110112158 | BENZISOXAZOLE ANALOGS AS GLYCOGEN SYNTHASE ACTIVATORS - Provided herein are compounds of the formula (I): | 2011-05-12 |
20110112159 | SEROTONIN TRANSPORTER GENE AND TREAMENT OF ALCOHOLISM - The gene responsible for encoding SERT has a functional polymorphism at the 5′-regulatory promoter region, which results in two forms, long (L) and short (S). The LL-genotype is hypothesized to play a key role in the early onset of alcohol use. The present invention discloses the differences in treatment and diagnosis based on the L or short genotypes as well as on a single nucleotide polymorphism of the SERT gene, the 3′ UTR SNP rs 1042173. The present invention demonstrates the efficacy of using the drug ondansetron and similar drugs for treatment based on variations in the polymorphisms of the SERT gene as well as methods for diagnosing susceptibility to abuse of alcohol and other addiction-related diseases and disorders. | 2011-05-12 |
20110112160 | TABLET COMPRISING EPROSARTAN MESYLATE - A tablet comprising eprosartan mesylate in only one form of either anhydrous or dihydrate form is described. In another aspect, a tablet is disclosed comprising eprosartan mesylate obtainable by direct compression, wherein eprosartan mesylate is provided in one primary form of being either anhydrous or dihydrate to the extent that the eprosartan mesylate shows a dissolution profile with a variability of dissolution from the different tablet samples of a set of below 30%, preferably below 20% and more preferably below 10% relative standard deviation at all time during dissolution, measured using USP apparatus 2, placing the tablets in 1000 ml 0.1 M hydrochloric acid at 37±0.5° C. with paddle speed of 50 rpm. Further described is a set of samples of tablets, wherein each comprises eprosartan mesylate as an active ingredient, wherein the eprosartan mesylate shows a dissolution profile with a variability of dissolution from different tablet samples of the set of below 30%, preferably below 20% and more preferably below 10% relative standard deviation at all time during dissolution. A tablet can be prepared by using a process, comprising providing eprosartan mesylate in only one primary form of being either anhydrous or dihydrate, optionally subjecting eprosartan mesylate to dry granulation process, and a direct compression while maintaining said only one primary form; or by process comprising mixing eprosartan mesylate in particulate form with excipients or additives, wherein the prepared whole dry formulation or granulation of eprosartan mesylate has a water activity of less than 0.62, preferably less than 0.60 and more preferably less than 0.50, respectively determined at room temperature, and subsequently tabletting. Suitable prophylactic and/or therapeutic uses are also described. | 2011-05-12 |
20110112161 | INDOLE AND INDAZOLE ANALOGS AS GLYCOGEN SYNTHASE ACTIVATORS - Provided herein are compounds of the formula (I): | 2011-05-12 |
20110112162 | SPIRO-OXINDOLE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS - This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. | 2011-05-12 |
20110112163 | CBI DERIVATIVES SUBJECT TO REDUCTIVE ACTIVATION - A unique class of N-acyl O-amino phenol prodrugs of CBI-TMI and CBI-indole | 2011-05-12 |
20110112164 | NOVEL POLYMORPHS AND PROCESSES FOR THEIR PREPARATION - The present invention relates to novel polymorph forms III and IV of sunitinib malate, pharmaceutical compositions comprising the novel polymorphs and the use of the pharmaceutical compositions. The present invention further relates to processes for the preparation of polymorph form I, III and IV of sunitinib malate. | 2011-05-12 |
20110112165 | ATORVASTATIN-ALISKIREN - A new compound in which atorvastatin and aliskiren are covalently bound, salts of this compound, pharmaceutical compositions thereof, as well the use of this compound as a medicament and as an impurity standard are provided. Furthermore, a 0 process for the preparation of a compound in which atorvastatin and aliskiren are covalently bound, a method for analyzing a sample of atorvastatin and/or aliskiren, and a method for determining the retention time on a chromatographic system for atorvastatin and/or aliskiren are provided. | 2011-05-12 |
20110112166 | THERAPEUTIC CYCLOPENTANE DERIVATIVES - Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, are disclosed, wherein B, Y, and A are as described in claims | 2011-05-12 |
20110112167 | THERAPEUTIC AGENTS AND TARGETS - The present invention relates to diagnostic and therapeutic methods in relation to diabetic complications, such as blindness, nephropathy and cardiovascular disease, and inflammatory conditions, such as angina, arthritis, empyema pharyngitis and urinary tract infection. Diagnostic methods involve screening for up regulated expression of decor (Den) or thioredoxin-like protein 19 (TLP 19). Therapeutic methods involve modulation of expression or activity o Den or TLP 19. The invention also relates to screening methods for identifying functional signal sequences to screen for secreted, membrane-bound and exported proteins and cell surface receptors. | 2011-05-12 |
20110112168 | NOVEL SIRNA STRUCTURES - The invention relates to siRNA compounds possessing novel sequences and structural motifs which down-regulate the expression of specific human genes. The invention also relates to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The present invention also provides a method of treating and/or preventing the incidence or severity of various diseases or conditions associated with the genes and/or symptoms associated with such diseases or conditions comprising administering to a subject in need of treatment for such disease or condition and/or symptom the compound or the pharmaceutical composition in a therapeutically effective dose so as to thereby treat the subject. | 2011-05-12 |
20110112169 | RNAi-BASED THERAPEUTICS FOR ALLERGIC RHINITIS AND ASTHMA - The present invention provides compositions comprising one or more RNAi agents (e.g., siRNAs, shRNAs, or RNAi vectors) for the treatment of conditions and diseases mediated by (e.g., featuring IgE-mediated hypersensitivity), as well as systems for identifying RNAi agents effective for this purpose. The compositions are suitable for the treatment of allergic rhinitis and/or asthma. In certain embodiments of the invention the RNAi agent is targeted to a transcript that encodes a protein selected from the group consisting of the FCεRIα chain, the FCεRIβ chain, c-Kit, Lyn, Syk, ICOS, OX40L, CD40, CD80, CD86, Re1A, Re1B, 4-1BB ligand, TLR1, TLR2, TLR3, TLR4, TLR5, TLR6, TLR7, TLR8, TLR9, CD83, SLAM, common γ chain, and COX-2. In addition, the invention provides RNAi agent/delivery agent compositions and methods of use. In certain embodiments of the invention compositions comprising an RNAi agent are delivered by the respiratory route. | 2011-05-12 |
20110112170 | OLIGOMERIC COMPOUNDS COMPRISING BICYCLIC NUCLEOSIDES AND HAVING REDUCED TOXICITY - In certain embodiments, the present invention provides oligomeric compounds having favorable toxicity profiles and therapeutic indexes. Compounds of the present invention comprise bicyclic nucleosides. Certain such bicyclic nucleosides are pyrimidines that do not include a methyl group at the 5-carbon. Oligomeric compounds comprising such nucleosides are less toxic than compounds comprising bicyclic nucleosides that do include a methyl group at the 5-carbon. In certain embodiments, the present invention provides methods of preparing and using such compounds. | 2011-05-12 |
20110112171 | COMPOSITIONS AND THEIR USES DIRECTED TO PTPRU - Disclosed herein are compounds, compositions and methods for modulating the expression of PTPRU in a cell, tissue or animal. Also provided are methods of active target segment validation. Also provided are uses of disclosed compounds and compositions in the manufacture of a medicament for treatment of diseases and disorders. Also provided are methods for the prevention, amelioration and/or treatment of diabetes, obesity, insulin resistance, insulin deficiency, hypercholesterolemia, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hyperfattyacidemia, liver steatosis, steatohepatitis, non-alcoholic steatohepatitis, metabolic syndrome, cardiovascular disease and coronary heart diseaseby administration of antisense compounds targeted to PTPRU. | 2011-05-12 |
20110112172 | SDF-1 Binding Nucleic Acids - The present invention is related to a nucleic acid molecule, preferably binding to SDF-1, selected from the group comprising type A nucleic acid molecules, type B nucleic acid molecules, type C nucleic acid molecules and nucleic acid molecules having a nucleic acid sequence according to any of SEQ ID NO:142, SEQ ID NO:143 or SEQ ID NO:144. | 2011-05-12 |
20110112173 | METHODS AND COMPOSITIONS INVOLVING MICRORNA - The present invention concerns methods and compositions for isolating, enriching, and/or labeling miRNA molecules and for preparing and using arrays or other detection techniques for miRNA analysis. Moreover, the present invention concerns methods and compositions for generating miRNA profiles and employing such profiles for therapeutic, diagnostic, and prognostic applications. | 2011-05-12 |
20110112174 | PEPTIDE BIOSYNTHESIS AND PAIN THERAPY - The invention provides an expression cassette comprising a DNA sequence encoding amino acids 1-99 of human preproenkephalin, a DNA sequence encoding a precursor of a carboxy-amidated peptide flanked by dibasic cleavage sites and optionally a DNA sequence encoding a marker protein (such as Enhanced Green Fluorescent Protein (GFP)) all in operable linkage and under control of a promoter. Where the encoded precursor of a carboxy-amidated peptide is an agonist for an opioid receptor, the invention further provides a method of treating neuropathic pain by administering the gene transfer vector comprising such an expression cassette to a patient. The invention also provides a method for detecting a peptide having a desired effect comprising introducing a library of DNA sequences encoding one or more precursors of carboxy-amidated peptides into host cells; expressing the carboxy-amidated peptides encoded in the library to provide expression products; and screening from the polypeptide expression products for the desired effect. | 2011-05-12 |
20110112175 | PEPTIDE BIOSYNTHESIS AND PAIN THERAPY - The invention provides an expression cassette comprising a DNA sequence encoding amino acids 1-99 of human preproenkephalin, a DNA sequence encoding a precursor of a carboxy-amidated peptide flanked by dibasic cleavage sites and optionally a DNA sequence encoding a marker protein (such as Enhanced Green Fluorescent Protein (GNP)) all in operable linkage and under control of a promoter. Where the encoded precursor of a carboxy-amidated peptide is an agonist for an opioid receptor, the invention further provides a method of treating neuropathic pain by administering the gene transfer vector comprising such an expression cassette to a patient. The invention also provides a method for detecting a peptide having a desired effect comprising introducing a library of DNA sequences encoding one or more precursors of carboxy-amidated peptides into host cells; expressing the carboxy-amidated peptides encoded in the library to provide expression products; and screening from the polypeptide expression products for the desired effect. | 2011-05-12 |
20110112176 | COMPOSITIONS AND METHODS FOR INHIBITING EXPRESSION OF KIF10 GENES - The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of a KIF10 gene. The invention also relates to a pharmaceutical composition comprising the dsRNA or nucleic acid molecules or vectors encoding the same together with a pharmaceutically acceptable carrier; methods for treating diseases caused by the expression of a KIF10 gene using said pharmaceutical composition; and methods for inhibiting the expression of KIF10 in a cell. | 2011-05-12 |
20110112177 | Human G-Protein Coupled Receptor (HETGQ23) - Human G-protein coupled receptor polypeptides and DNA (RNA) encoding such polypeptides and a procedure for producing such polypeptides by recombinant techniques is disclosed. Also disclosed were methods for utilizing such polypeptides for identifying antagonists and agonists to such polypeptides and methods of using the agonists and antagonists therapeutically to treat conditions related to the underexpression and overexpression of the G-protein coupled receptor polypeptides, respectively. Also disclosed are diagnostic methods for detecting a mutation in the G-protein coupled receptor nucleic acid sequences and an altered level of the soluble form of the receptors. | 2011-05-12 |
20110112178 | Compositions And Methods For Inhibiting Expression Of IKK-B Gene - The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of the IKK-B gene, comprising an antisense strand having a nucleotide sequence which is less that 30 nucleotides in length, generally 19-25 nucleotides in length, and which is substantially complementary to at least a part of the IKK-B gene. The invention also relates to a pharmaceutical composition comprising the dsRNA together with a pharmaceutically acceptable carrier; methods for treating diseases caused by the expression or activation of the IKK-B gene using the pharmaceutical composition; and methods for inhibiting the expression of the IKK-B gene in a cell. | 2011-05-12 |
20110112179 | CELL LINE, SYSTEM AND METHOD FOR OPTICAL CONTROL OF SECONDARY MESSENGERS - A variety of methods, devices and compositions are implemented for light-activated molecules. One such method is implemented for generating secondary messengers in a cell. A nucleotide sequence for expressing a chimeric light responsive membrane protein (e.g., rhodopsin) is modified with one or more heterologous receptor subunits {e.g., an adrenergic receptor (alpha1, Beta2)}. The light responsive membrane protein is expressed in a cell for producing a secondary messenger in response t light. | 2011-05-12 |
20110112180 | NOVEL STAT3 PATHWAY INHIBITORS AND CANCER STEM CELL INHIBITORS - The present invention relates to a novel naphtho class of compounds as Stat3 pathway inhibitors and as cancer stem cell inhibitors; to methods of using such compounds to treat cancer; to methods of using such compounds to treat disorders in a mammal related to aberrent Stat3 pathway activity; to pharmaceutical compositions containing such compounds. | 2011-05-12 |
20110112181 | POLYPHENOL COMPOUNDS WITH MODULATING NEUROTRANSMITTER RELEASE - Disclosed is a composition for modulating the release of a neurotransmitter, which includes naturally extracted polyphenols as an active ingredient. The disclosed composition suppresses the formation of a SNARE complex, thereby modulating the release of a neurotransmitter, and thus can be used as a modulator for a reaction within a cell related to the SNARE complex. Such an inhibitor of the SNARE complex formation can be used as a composition for reducing wrinkles and relieving pain. | 2011-05-12 |
20110112182 | DESIGN, SYNTHESIS AND FUNCTIONAL CHARACTERIZATION OF ROTTLERIN ANALOGS - A method of synthesizing rottlerin analogs is described. The synthesis methods described are the first known method of synthesizing rottlerin analogs from commercially-available materials to produce cost effective analogs. Rottlerin analog structures made by the synthesis methods and methods of use for treating a neurological or inflammatory response mediated by protein kinase C (PKC) are further described. | 2011-05-12 |
20110112183 | Oligomer-Bis-Chromonyl Compound Conjugates - The invention provides oligomer-bis-chromonyl compound conjugates. The conjugates of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds. | 2011-05-12 |
20110112184 | COMPOUNDS WITH GLYCIDIC STRUCTURE ACTIVE IN THE THERAPY OF SYSTEMIC AND LOCAL INFLAMMATION - Compounds of the general formula (I) and (II) (including formulae (III) to (V)), wherein X=—CH | 2011-05-12 |
20110112185 | INSECTICIDAL FERMENTATION BROTH FROM ACTINOMYCETES - Methods and compositions are provided for the preparation of insecticidal compositions. | 2011-05-12 |
20110112186 | DIAGNOSTIC METHODS - This invention relates to a method of determining the susceptibility of an individual to statin-induced myopathy, comprising detecting the presence or absence of one or more polymorphisms in the SLCO1B1 gene in a biological sample from an individual, whereby the presence of one or more polymorphisms indicates that the individual has altered susceptibility to statin-induced myopathy. | 2011-05-12 |
20110112187 | Use Of Tranilast And Derivatives Thereof For The Therapy Of Neurological Conditions - The present invention relates to the use of tranilast and derivatives thereof for the preparation of a pharmaceutical composition for treating and/or preventing a neuronal condition where there is a need of neuroprotection and neuroregeneration. The invention furthermore relates to the use of tranilast and derivatives thereof for the in vitro differentiation of neuronal stem cells and the use of such pre-treated cells for stem cell therapy von neurological conditions. | 2011-05-12 |
20110112188 | Treatment of Inflammatory Conditions - The invention relates to methods of inhibiting production and function of 3-deoxyglucosone and other alpha-dicarbonyl sugars in skin thereby treating or prevention various diseases, disorders or conditions. Additionally, the invention relates to treatment of various diseases, disorders or conditions associated with or mediated by oxidative stress since 3DG induces ROS and AGEs, which are associated with the inflammatory response caused by oxidative stress. | 2011-05-12 |
20110112189 | METHODS OF TREATING PAINS ASSOCIATED WITH NEUROMA, NERVE ENTRAPMENT, AND OTHER CONDITIONS - The present disclosure is drawn to methods for treating nerve entrapment pain; neuroma pain; headache associated with neuralgia; connective tissue pain such as iliotibial band pain, blood vessel pain, tendinopathy pain, medial tibial stress syndrome pain, bursitis, etc.; arthritis pain such as osteoarthritis pain or rheumatoid arthritis pain; pain associated with injury such as fracture, severance, break, sprain, strain, tear, point pain, (e.g., trigger point pain or hit point pain), focal pain, or bruise; or combinations of these pains. Specifically, a method for treating various types of pain includes the application of an analgesic system to a skin surface of a subject experiencing the pain and maintaining the analgesic system on the skin surface for a period of time of at least 30 minutes. The analgesic system applied to the skin surface can include a heating component and a local anesthetic formulation which includes at least one local anesthetic. The heating component can be capable of heating the skin surface to a temperature of 36° C. to 42° C. | 2011-05-12 |
20110112190 | ORALLY ACTIVE CURCUMINOID COMPOUNDS - The invention discloses a compound of formula (I) wherein, at least one of R | 2011-05-12 |
20110112191 | OXYLIPINS FROM STEARIDONIC ACID AND GAMMA-LINOLENIC ACID AND METHODS OF MAKING AND USING SAME - Disclosed are novel oxylipins that are derived from γ-linolenic acid (GLA; 18:3n-6) and stearidonic acid (STA or SDA; 18:4n-3), and methods of making and using such oxylipins. Also disclosed is the use of such oxylipins in therapeutic and nutritional or cosmetic applications, and particularly as anti-inflammatory or anti-neurodegenerative compounds. Also disclosed are The invention novel ways of producing long chain polyunsaturated acid (LCPUFA)-rich oils and compositions that contain enhanced and effective amounts of SDA- and/or GLA-derived oxylipins. | 2011-05-12 |
20110112192 | VERFAHREN ZUR GERUCHSEXTINKTION - Use of a pharmaceutically acceptable oxidation or reduction agent for disulfide bridges containing organic compounds for the treatment of odor formation in humans due to the consumption of allium plants or allium plant stuffs. | 2011-05-12 |
20110112193 | BIS-ARYL COMPOUNDS FOR USE AS MEDICAMENTS - There is provided compounds of formula (I), wherein ring A, D | 2011-05-12 |
20110112194 | Medicaments Containing Pantothenic Acid - This invention relates to medicaments and their use in the alleviation of inflammation and pain in joints. | 2011-05-12 |
20110112195 | Potent and Selective Inhibition by Aurinticarboxylic Acid - The severe acute respiratory syndrome virus (SARS) is a coronavirus that instigated regional epidemics in Canada and several Asian countries in 2003. The newly identified SARS coronavirus (SARS-CoV) can be transmitted among humans and cause severe or even fatal illnesses. As preventive vaccine development takes years to complete and adverse reactions have been reported to some veterinary coronaviral vaccines, anti-viral compounds must be relentlessly pursued. In this study, we analyzed the effect of aurintricarboxylic acid (ATA) on SARS-CoV replication in cell culture, and found that ATA could drastically inhibit SARS-CoV replication, with viral production being more than 1000 fold than that in the untreated control. ATA is also shown to be an effective anti-viral for several other viruses, including West Nile Virus and variola virus. | 2011-05-12 |
20110112196 | NRF2 SCREENING ASSAYS AND RELATED METHODS AND COMPOSITIONS - Provided are certain methods of screening, identifying, and evaluating neuroprotective compounds useful for treatment of neurological diseases, such as, e.g., multiple sclerosis (MS). The compounds described upregulate the cellular cytoprotective pathway regulated by Nrf2. Also provided are certain methods of utilizing such compounds in therapy for neurological disease, particularly, for slowing or reducing demyelination, axonal loss, or neuronal and oligodendrocyte death. | 2011-05-12 |
20110112197 | NOVEL CRYSTALLINE FORMS OF (1S,2R)-2-(AMINO METHYL)-N,N-DIETHYL-1-PHENYL CYCLOPROPANE CARBOXAMIDE - The present invention relates to novel crystalline forms of (1S,2R)-2-(amino methyl)-N,N-diethyl-1-phenyl cyclopropane carboxamide. Processes for the preparation of this form, compositions containing the form, and methods of use thereof are also described. | 2011-05-12 |