| 45th week of 2011 patent applcation highlights part 43 |
| Patent application number | Title | Published |
|---|
| 20110275617 | OPHTHALMIC COMPOSITION - The present invention provides an ophthalmic composition comprising a hyperbranched polymer. The ophthalmic compositions may also comprise carbonic anhydrase inhibitors, wherein the hyperbranched polymer increases the aqueous solubility of the carbonic anhydrase inhibitor, and increases corneal permeation of the active agent. The ophthalmic compositions may also comprise non-ionic surfactants, such as polysorbate, hydroxypropyl methyl cellulose or hydroxyethyl cellulose, and beta-blockers, such as carteolol, levobunolol, betaxolol, metipranolol, timolol or propranolol. | 2011-11-10 |
| 20110275618 | NOVEL LOW CONCENTRATION MELOXICAM TABLETS - The invention relates to a solid tablet that is directly-compressed of powder, comprising meloxicam and one or more excipients which are homogenously dispersed within the tablet that can be broken into two, three or four units with each unit containing equal amounts of the active ingredient, meloxicam. | 2011-11-10 |
| 20110275619 | INHIBITORS OF BACE1 AND METHODS FOR TREATING ALZHEIMER'S DISEASE - Inhibitors of BACE1 and compositions containing them are described. Use of the inhibitors and compositions containing them to treat Alzheimer's disease are described. | 2011-11-10 |
| 20110275620 | Method for preventing or treating a disease related to the glucocorticoid receptor - A method for preventing or treating a disease related to the glucocorticoid receptor involving administering a pharmacologically effective amount of a 1,2-hydroquinoline compound. | 2011-11-10 |
| 20110275621 | HIV INTEGRASE INHIBITORS - Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: | 2011-11-10 |
| 20110275622 | BI-FUNCTIONAL QUINOLINE ANALOGS - Provided are compounds of Formula I: | 2011-11-10 |
| 20110275623 | BI-FUNCTIONAL PYRAZOLOPYRIDINE COMPOUNDS - This invention provides compounds of the formula: | 2011-11-10 |
| 20110275624 | INDOLE AND BENZOMORPHOLINE DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to novel compounds, in particular novel indole and benzomorpholine derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved. | 2011-11-10 |
| 20110275625 | Heteroaryl Diamide Compounds Useful as MMP-13 Inhibitors - Disclosed are compounds and compositions of the formula (I) as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula (I). | 2011-11-10 |
| 20110275626 | FORMULATION FOR ORAL TRANSMUCOSAL ADMINISTRATION OF ANALGESIC AND/OR ANTISPASMODIC MOLECULES - A formulation for oral transmucosal administration of at least one active principle with antispasmodic and/or analgesic effect, including the active principle in base form and/or in salt form, an aqueous alcohol solution titrating at least 35° alcohol by weight, the active principle being present in a state of stable and complete dissolution in the aqueous alcohol solution. Also, a method of preparing this formulation and its use for treating spastic crises. | 2011-11-10 |
| 20110275627 | INDOLIZINE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I): | 2011-11-10 |
| 20110275628 | NOVEL PYRAZOLE-3-CARBOXAMIDE DERIVATIVE HAVING 5-HT2B RECEPTOR ANTAGONIST ACTIVITY - Disclosed is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, which is useful as a selective antagonist of a 5-HT | 2011-11-10 |
| 20110275629 | Pyridazino-pyridinone Compounds and Methods of Use - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I | 2011-11-10 |
| 20110275630 | ISOINDOLINONE KINASE INHIBITORS - Compounds having the formula: | 2011-11-10 |
| 20110275631 | Heteroaryl Substituted Indole Compounds Useful as MMP-13 Inhibitors - Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I. | 2011-11-10 |
| 20110275632 | Method for preventing or treating a disease related to the glucocorticoid receptor - A method for preventing or treating a disease related to the glucocorticoid receptor involving administering a pharmacologically effective amount of a 1,2-dihydroquinoline compound. | 2011-11-10 |
| 20110275633 | 2,4-DIAMINOPYRIMIDINE DERIVATES AS PTK2- INHIBITORS FOR THE TREATMENT OF ABNORMAL CELL GROWTH - The present invention encompasses compounds of general formula (1) wherein R | 2011-11-10 |
| 20110275634 | DUAL-ACTING PYRAZOLE ANTIHYPERTENSIVE AGENTS - In one aspect, the invention relates to compounds having the formula: | 2011-11-10 |
| 20110275635 | SMALL MOLECULE INHIBITORS OF NADS, NAMNAT, AND NMNAT - Small molecule inhibitors of bacterial nicotinamide adenine dinucleotide synthetase (NADs), bacterial nicotinic acid mononucleotide adenylyltransferase (NaMNAT), and human nicotinamide mononucleotide adenylyltransferase (NMNAT) are provided, as well as methods of making and using the inhibitors. | 2011-11-10 |
| 20110275636 | DESAZADESFERROTHIOCIN AND DESAZADESFERROTHIOCIN POLYETHER ANALOGUES AS METAL CHELATION AGENTS - Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity. | 2011-11-10 |
| 20110275637 | PIPERAZINE DERIVATIVES AND THEIR USE AS LEPTIN RECEPTOR MODULATORS - The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias. | 2011-11-10 |
| 20110275638 | PIPERAZINE DERIVATIVES AND THEIR USE AS LEPTIN RECEPTOR MODULATORS - The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias. | 2011-11-10 |
| 20110275639 | C5aR ANTAGONISTS - Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors. | 2011-11-10 |
| 20110275640 | Preventives or remedies for alzheimer's disease, or amyloid protein fibril-formation inhibitors, which include a nitrogen-containing heteroaryl compound - The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: | 2011-11-10 |
| 20110275641 | Preventives or remedies for Alzheimer's disease, or amyloid protein fibril-formation inhibitors, which include a nitrogen-containing heteroaryl compound - The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: | 2011-11-10 |
| 20110275642 | NEW METHOD FOR OBTAINING 5-AMINO 2,3-DIHYDROPHTHALAZINE-1,4-DIONE ALKALI METAL SALTS AND THEIR USE IN MEDICINE - The invention is related to a method for preparing 5-amino-2,3-dihydrophthalazine-1,4-dione salt with alkali metals of the formula II wherein 5-nitro-2,3-dihydrophthalazine-1,4-dione is solved in water solution of MOH1 where M has the below mentioned meaning, with formation of solution of 5-nitro-2,3-dihydrophthalazine-1,4-dione alkali metal salt, which is catalytically transformed into 5-amino-2,3-dihydrophthalazine-1,4-dione salt at the temperature 40-900C by means of hydrogen under the pressure 1-4 MPa in at the presence of a transition metal catalyst (Pt, Pd) on activated carbon, and separation of crystalline 5-amino-2,3-dihydrophthalazine-1,4-dione salt is performed by water solution diluting with lower alcohol or cyclic lower ether with cooling to the temperature −5° C. to −15° C., providing that there is used 5-nitro-2,3-dihydrophthalazine-1,4-dione formed in the reaction of anhydride of 3-nitrophthalic acid with hydrazine hydrate in anhydrous acetic acid at the temperature 100-110° C. with distilling the mixture of acetic acid and water off. There was also presented a pharmaceutical composition containing such obtained 5-amino-2,3-dihydrophthalazine-1,4-dione salt with alkali metals and its application in medicine. There was also presented new use of 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt for production of a drug for treatment of heart diseases, pancreas diseases and diabetes as well as application of sodium salt optionally in combination with lithium salt for treatment of the nervous system diseases. Besides, the methods of treatment of these diseases were also presented. Formula II where M represents Li, Na, K | 2011-11-10 |
| 20110275643 | AROYLQUINOLINE COMPOUNDS - A serious of nitro heterocyclic derivatives including a structure of formula (I) are provided. In formula (I), P, Q and R1 to R8 are defined in the specification. The derivatives disclosed in the present invention are characterized in inhibiting tubulin polymerization, and treating cancers and other tubulin polymerization-related disorders with a suitable pharmaceutical acceptable carrier. | 2011-11-10 |
| 20110275644 | BIOLOGICAL MARKERS PREDICTIVE OF ANTI-CANCER RESPONSE TO INSULIN-LIKE GROWTH FACTOR-1 RECEPTOR KINASE INHIBITORS - The present invention provides diagnostic methods for predicting the effectiveness of treatment of a cancer patient with an IGF-1R kinase inhibitor that inhibits both IGF-1R and IR kinases. Methods are provided for identifying patients with cancer who are likely to benefit from treatment with an IGF-1R kinase inhibitor that inhibits both IGF-1R and IR kinases. Methods are also provided for identifying patients with cancer who are likely to benefit from treatment with an IGF-1R kinase inhibitor that inhibits both IGF-1R and IR kinases, but who would likely not respond to therapy with an anti-IGF-1R antibody. Methods are also provided for identifying patients with cancer who are more likely to benefit from treatment with anti-IGF-1R antibody. Improved methods for treating cancer patients with IGF-1R kinase inhibitors that incorporate these methods are also provided. | 2011-11-10 |
| 20110275645 | Small Molecules for Inhibition of Protein Kinases - The invention provides compounds that inhibit protein kinases, prodrugs of the compounds, intermediates and methods of synthesizing the compounds and/or prodrugs, pharmaceutical compositions including the compounds and/or prodrugs and methods of using the compounds and/or prodrugs in a variety of contexts, including, for example, in the treatment and/or prevention of various diseases that are responsive to protein kinase inhibition and/or that are mediated, at least in part, by inappropriate kinase activity. | 2011-11-10 |
| 20110275646 | Novel Compounds for Treatment of Cancer and Disorders Associated with Angiogenesis Function - Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating gene expression. | 2011-11-10 |
| 20110275647 | PYRIMIDIN-4-(3H)-ONE DERIVATIVES - The present invention relates to a compound represented by a formula (I): or a pharmaceutically acceptable salt thereof, wherein R | 2011-11-10 |
| 20110275648 | FLURBIPROFEN ANALOGS AND METHODS OF USE IN TREATING CANCER - Flurbiprofen analog compounds having an amino acid derivatized at the flurbiprofen alkanoic acid carboxyl group and terminating at an ester or amide group are effective in inhibiting cancer cells in vitro and inhibiting the growth of cancers in viva. The compounds and pharmaceutical compositions containing them are particularly useful for the treatment of lung, pancreatic and head and neck cancers. | 2011-11-10 |
| 20110275649 | Combination therapy for the prevention of statin induced diabetes - Novel combinations comprising HMG CoA reductase inhibitors, or statins, with partial fatty acid oxidation inhibitors (pFOXi), and methods for their use, are disclosed. These combinations are useful in preventing or reducing the risk of developing diabetes which results from therapy with a statin. | 2011-11-10 |
| 20110275650 | METHODS AND COMPOSITIONS RELATED TO TARGETING MONOACYLGLYCEROL LIPASE - This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat conditions that are associated with or linked to endocannabinoid signaling. The invention additionally provides methods of treating cancer or inhibiting tumor growth by targeting MAGL with MAGL specific inhibitors. The invention further provides methods of screening for MAGL inhibitors with improved biochemical and pharmaceutical properties. | 2011-11-10 |
| 20110275651 | FUSED RING HETEROARYL KINASE INHIBITORS - Provided herein are fused ring heteroaryl compounds useful in a variety of methods, including reducing the activity of certain kinases and treating certain disease states. | 2011-11-10 |
| 20110275652 | 2,2-BIS-(HYDROXYMETHYL)CYCLOPROPYLIDENEMETHYL-PURINES AND -PYRIMIDINES AS ANTIVIRAL AGENTS - Compounds which are active against viruses have the following formulas: | 2011-11-10 |
| 20110275653 | HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. | 2011-11-10 |
| 20110275654 | LONG TERM TREATMENT OF HIV-INFECTION WITH TMC278 - This invention relates to the use of a parenteral formulation comprising an anti-virally effective amount of TMC278 or a pharmaceutically acceptable acid-addition salt thereof, and a carrier, for the manufacture of a medicament for the treatment of a subject being infected with HIV, wherein the formulation is to be administered intermittently at a time interval of at least one week. | 2011-11-10 |
| 20110275655 | PYRIMIDINECARBOXAMIDE DERIVATIVES AS INHIBITORS OF SYK KINASE - The present invention relates to the compound of formula (I): | 2011-11-10 |
| 20110275656 | 3H-Imidazo [4, 5-C] Pyridine- 6 -Carboxamides As Anti-Inflammatory Agents - There are provided compounds of formula (I), wherein R | 2011-11-10 |
| 20110275657 | MELANOCORTIN RECEPTOR MODULATORS, PROCESS FOR PREPARING THEM AND USE THERE IN HUMAN MEDICINE AND COSMETICS - Melanocortin receptor modulators, processes for preparing them and use thereof in human medicine and cosmetics are described. Melanocortin receptor modulators corresponding to formula (I): | 2011-11-10 |
| 20110275658 | OPIOID-CONTAINING ORAL PHARMACEUTICAL COMPOSITIONS AND METHODS - The present invention provides sustained-release oral pharmaceutical compositions and methods of use. The sustained-release oral pharmaceutical compositions include an opioid (including salts thereof) and a salt of a non-steroidal anti-inflammatory drug (NSAID). | 2011-11-10 |
| 20110275659 | Tacrolimus For Improved Treatment Of Transplant Patients - An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form. | 2011-11-10 |
| 20110275660 | BETA CARBOLINE SULPHONYLUREA DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS - The invention is directed to β-carboline sulphonylurea derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, inflammation, osteoarthritis, and rheumatoid arthritis. Pharmaceutical compositions and methods of use are also included. | 2011-11-10 |
| 20110275661 | TRICYCLIC NITROGEN COMPOUNDS USED AS ANTIBACTERIALS - The present invention relates to tricyclic nitrogen containing compounds of Formula (I): | 2011-11-10 |
| 20110275662 | METHODS OF IMPROVING SKIN QUALITY - Methods of improving skin quality are disclosed. Generally, the methods include topically administering an IRM compound to a treatment area of skin for a period of time and in an amount effective for improving the quality of the skin. Suitable IRM compound compounds include agonists of one or more TLRs. | 2011-11-10 |
| 20110275663 | N-Acylthiourea and N-Acylurea Inhibitors of the Hedgehog Protein Signalling Pathway - The present invention relates to the use of acylthiourea or acylurea derivatives for the treatment of pathologies involving a tissue dysfunction associated with a deregulation of the Hedgehog protein signalling pathway, and also to novel acylthiourea or acylurea derivatives as such, to their use as a medicinal product, and to pharmaceutical compositions containing them. | 2011-11-10 |
| 20110275664 | Method for treating drug and behavioral addictions - The present invention is directed to the use of ibudilast for treating addictions, including drug and behavioral addictions. In particular, ibudilast is used to diminish the dopamine-mediated reward associated with addictions and to treat withdrawal syndromes after discontinuance of addictive drug use or behavior. In addition, methods are provided for preventing or inhibiting relapse in human subjects having a history of methamphetamine addiction or dependence by the administration of an effective amount of ibudilast. | 2011-11-10 |
| 20110275665 | GLUCOKINASE ACTIVATORS - Compounds are provided for use with hexokinases that comprise: | 2011-11-10 |
| 20110275666 | ACTIVATED BLOOD COAGULATION FACTOR X (FXA) INHIBITOR - An object of the present invention is to provide an activated blood coagulation factor X (FXa) inhibitor that reduces the risk of bleeding caused by the treatment of thromboembolism. The present invention provides an oral anticoagulant agent comprising a compound represented by the following formula (1): | 2011-11-10 |
| 20110275667 | COMPOSITIONS USEFUL FOR TREATING GASTROESOPHAGEAL REFLUX DISEASE - The present invention relates to a method of treating GERD in a human subject in need of treatment. The method comprises orally administering to said subject an effective amount of a thieno[3,2-b]pyridine compound of Structural Formula I or a pharmaceutically acceptable salt or N-oxide derivative thereof, wherein the effective amount is from about one to about three daily doses of the compound and the dose is from about 0.2 mg to about 0.5 mg. | 2011-11-10 |
| 20110275668 | Compound with antimalarial activity and antimalarial drug containing the same as active ingredient - Compounds with high antimalarial activity; and antimalarial drugs containing the same as an active ingredient. There are provided compounds with antimalarial activity represented by the chemical formula: (wherein R | 2011-11-10 |
| 20110275669 | Novel pyrroles having hypolipidemic hypocholesteremic activities, process for their preparation and pharmaceutical compositions containing them and their use in medicine - The present invention relates to compounds of the general formula (I) | 2011-11-10 |
| 20110275670 | New Compounds VII - The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias. | 2011-11-10 |
| 20110275671 | DIHYDROINDOLINONE DERIVATIVES - Disclosed are dihydroindolone compounds which can modulate the activity of protein tyrosine kinases, a method for preparing the same, and pharmaceutical compositions comprising the same. Also disclosed are use of such compounds and pharmaceutical compositions thereof in the treatment and/or prophylaxis of protein tyrosine kinase associated diseases in an organism, particularly in the treatment and/or prophylaxis of tumors and fibroblast proliferation associated diseases. | 2011-11-10 |
| 20110275672 | METHODS FOR TREATING CANCERS USING POLYMORPHIC FORMS OF 3-(4-AMINO-1-OXO-1,3 DIHYDRO-ISOINDOL-2-YL)-PIPERIDINE-2,6-DIONE - Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed. | 2011-11-10 |
| 20110275673 | INHIBITORS OF SPHINGOSINE KINASE 1 - The invention relates to compounds of Formula (I). Compounds of the present invention are inhibitors of sphingosine kinase 3, and are useful in the treatment of various disorders and conditions, such as inflammatory disorders. | 2011-11-10 |
| 20110275674 | Small Molecules Modulator of Epigenetic Regulation and Their Therapeutic Applications - Disclosed are methods and compositions for modulating the function of transcription factors, especially transcription factors that recruit epigenetic regulators (histone modifying enzymes) to specific DNA promoters. The targeted transcription factors include but are not limited to the myocyte enhancing factor (MEF2), the forkhead/winged helix transcription factor FOXP3 and the transcription factor GATA3. Also disclosed are small molecule modulators of MEF2 and its associated factors that include but not limited to histone deacetylases (HDACs), p300/CBP and Cabin1 and the therapeutic applications thereof. | 2011-11-10 |
| 20110275675 | Antimicrobial Dental Materials - Dental material which contains an antimicrobial active ingredient according to general formula (I), | 2011-11-10 |
| 20110275676 | Triazole-substituted anthranilamides as pesticides - The present invention constitutes new, triazole-substituted anthranilamides of the general formula (I), | 2011-11-10 |
| 20110275677 | INDOLE COMPOUNDS BEARING ARYL OR HETEROARYL GROUPS HAVING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR BIOLOGICAL ACTIVITY - The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as sphingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors. | 2011-11-10 |
| 20110275678 | New Pyridine Derivatives as Leptin Receptor Modulator Mimetics - The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias. | 2011-11-10 |
| 20110275679 | FLUPIRTINE HYDROCHLORIDE MALEIC ACID COCRYSTAL - The invention relates to crystalline forms of flupirtine, particularly to 1:1 flupirtine hydrochloride maleic acid cocrystal. The preparation and characterization of 1:1 flupirtine hydrochloride maleic acid cocrystal is described. The invention also relates to the therapeutic use of the flupirtine hydrochloride maleic acid cocrystal to treat nervous system disorders, pain disorders, and musculoskeletal disorders and to pharmaceutical compositions containing the cocrystal. | 2011-11-10 |
| 20110275680 | NOXEL OXIME DERIVATIVES OF 3, 5-SECO-4-NOR-CHOLESTANE, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, AND METHOD FOR PREPARING SAME - The invention relates to novel chemical compounds, in particular oxime derivatives of 3,5-seco-4-nor-cholestane, to the application thereof as drugs, in particular cytoprotective drugs, and more particularly as neuroprotective, cardioprotective and/or hepatoprotective drugs. | 2011-11-10 |
| 20110275681 | NOVEL SOLID FORMS OF EPALRESTAT - The invention relates to novel crystalline salts of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid and a novel betaine cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel crystalline salts and cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel crystalline salts and cocrystal and the therapeutic use of the novel crystalline salts and cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, inhibiting aldose reductase, and affording cardioprotection in patients who may be non-diabetic. | 2011-11-10 |
| 20110275682 | NOVEL CHOLINE COCRYSTAL OF EPALRESTAT - The invention relates to a novel choline cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel choline cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel choline cocrystal and the therapeutic use of the novel choline cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, treating and/or preventing homocystinuria reducing levels of homocysteine in blood serum, inhibiting aldose reductase, and affording cardioprotection in non-diabetic patients. | 2011-11-10 |
| 20110275683 | Selenophene and Selenazole Carboxylic Acid Derivatives - Derivatives of selenophene and selenazole heterocycles are disclosed. The compounds are useful as inhibitors of D-amino acid oxidase (DAO) and in the treatment of neurodegenerative and psychiatric diseases and disorders. | 2011-11-10 |
| 20110275684 | NOVEL BENZOTRIAZOLE DERIVATIVES USEFUL FOR THE TREATMENT OF CNS DISORDERS - The present invention relates to novel benzotriazole derivatives, 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 benzotriazole derivatives of the invention and to the use of these compounds for therapeutic applications. | 2011-11-10 |
| 20110275685 | SALT AND POLYMORPHS OF A KINESIN INHIBITOR COMPOUND - The present invention relates to salts, polymorphs and hydrates of the kinesin inhibitor compound N-((S)-3-amino-4-fluorobutyl)-N-((R)-1-(1-benzlyl-4-(2,5-difluorophenyl)-1H-imidazol-2-yl)-2,2-dimethylpropyl)-2-hydroxyacetamide, processes to prepare such salts, polymorphs and hydrates and a liquid formulation comprising at least one of these salts, polymorphs and hydrates. | 2011-11-10 |
| 20110275686 | NANOPARTICLE CARRIER SYSTEMS BASED ON POLY(DL-LACTIC-CO-GLYCOLIC ACID) (PLGA) FOR PHOTODYNAMIC THERAPY (PDT) - Compositions, which are stable in storage, and a method of production of pharmaceutical based nanoparticulate formulations for clinical use in photodynamic therapy comprising a hydrophobic photosensitizer, poly(lactic-co-glycolic) acid and stabilizing agents are provided. These nanoparticulate pharmaceutical formulations provide therapeutically effective amounts of photosensitizer for parenteral administration. In particular, tetrapyrrole derivatives can be used as photosensitizers, whose efficacy and safety are enhanced by such nanoparticulate formulations. It also teaches the method of preparing PLGA-based nanoparticles under sterile conditions. In one of the preferred embodiments of the present invention PLGA-based nanoparticles have a mean particle size less than 500 nm and the photosensitizer is temoporfin, 5,10,15,20-tetrakis(3-hydroxyphenyl)-chlorin (mTHPC). In another embodiment, the photosensitizer 2,3-dihydroxy-5,10,15,20-tetrakis(3-hydroxyphenyl)-chlorin (mTHPD-OH) is formulated as a nanoparticle for parenteral administration. Yet, in another embodiment preferred photosensitizer is 5,10,15,20-tetrakis(3-hydroxyphenyl)-porphyrin (mTHPP). The formulations can be used for treating hyperplasic and neoplasic conditions, inflammatory problems, and more specifically to target tumor cells. | 2011-11-10 |
| 20110275687 | SAXAGLIPTIN INTERMEDIATES, SAXAGLIPTIN POLYMORPHS, AND PROCESSES FOR PREPARATION THEREOF - The invention provides Saxagliptin Schiff bases, polymorphs of Saxagliptin and (1S,3S,5S)-2-[(2S)-2-propan-2-ylideneamino-2-(3-hydroxy-1-adamantyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile, processes for preparing Saxagliptin hydrates, and pharmaceutical compositions thereof. | 2011-11-10 |
| 20110275688 | KETOROLAC COMPOSITIONS FOR CORNEAL WOUND HEALING - The present invention is directed to an aqueous ophthalmic solution comprising an effective amount of ketorolac which comprises carboxymethyl cellulose which promotes epithelial wound healing in a patient's cornea. | 2011-11-10 |
| 20110275689 | Preparation of 3-Pyrrole Substituted 2-Indolinone Derivatives - The present invention relates to novel intermediates and further to the use of said intermediates in processes for the preparation of indolinone derivatives, in particular 3-pyrrole substituted 2-indolinones having amide moieties on the pyrrole ring. Such compounds are useful in die treatment of abnormal cell growth, such as cancer, in mammals. | 2011-11-10 |
| 20110275690 | NEW CRYSTAL FORM OF SUNITINIB MALATE - A process for the preparation of a new crystal form of sunitinib malate, along with pharmaceuticals comprising the same are described. | 2011-11-10 |
| 20110275691 | METHODS OF TREATING HEADACHES USING 5-HT AGONISTS IN COMBINATION WITH LONG-ACTING NSAIDS - The invention is directed to methods and compositions that can be used in the treatment of headaches. In particular, methods and compositions are described involving the combination of a long-acting NSAID and a 5-HT1 | 2011-11-10 |
| 20110275692 | SUBSTITUTED GAMMA LACTAMS AS THERAPEUTIC AGENTS - A compound comprising | 2011-11-10 |
| 20110275693 | Pharmaceutical Compositions Comprising 2-Oxo-1-Pyrrolidine Derivatives - The present invention relates to an immediate release formulation of pharmaceutical compounds. | 2011-11-10 |
| 20110275694 | 3-(PHENOXYPHENYLMETHYL)PYRROLIDINE COMPOUNDS - In one aspect, the invention relates to compounds of formula I: | 2011-11-10 |
| 20110275695 | CRYSTALLINE FORMS OF ZOTEPINE HYDROCHLORIDE - The invention relates to crystalline forms of zotepine hydrochloride, including the crystalline hydrochloride salt of zotepine and two cocrystals of zotepine hydrochloride with benzoic acid. The preparation and characterization of these crystalline forms of zotepine hydrochloride is described. The invention also relates to the therapeutic use of the crystalline forms of zotepine hydrochloride to treat central nervous system disorders and to pharmaceutical compositions containing them. | 2011-11-10 |
| 20110275696 | Thioxanthone-Based Autophagy Inhibitor Therapies to Treat Cancer - The present specification provides compositions comprising a thioxanthone-based autophagy inhibitor and/or a cancer therapeutic autophagy inducing compound, pharmaceutical kits comprising these compositions, and methods of treating cancer using such compounds, compositions and kits. Additionally, the present specification provides methods of treating cancer using a thioxanthone-based autophagy inhibitor and a radiotherapy. | 2011-11-10 |
| 20110275697 | REGULATION OF CYCLIN D - The present invention provides methods for modulating the level or activity of cyclin D by inhibiting EGLN2 expression or activity. The methods are particularly useful for treating or preventing a disorder associated with elevated cyclin D levels or activity, such as cancer. | 2011-11-10 |
| 20110275698 | "TEST AND TREAT" STRATEGY FOR TREATING TRANSFORMING HPV INFECTION - The invention is concerned with a “test and treat” method of screening and directly treating female subjects having transforming or abnormal human papillomavirus (HPV) infection. | 2011-11-10 |
| 20110275699 | Treatment For Obesity And Diabetes - The present disclosure relates to strategies aimed at treating/preventing obesity and diabetes. In particular, obesity is a major public health problem, associated with detrimental metabolic consequences such as diabetes, cardiovascular disease, stroke, osteoarthritis and even some types of cancer. Thus, application of DNA-PK inhibitors, that has been connected to the signaling pathway involved in the formation of fat from carbohydrate in the liver, could potentially be a pharmacological target for regulation of obesity and diabetes due to a diet high in carbohydrates. Therefore, the invention finds application in the fields of obesity, diabetes, and lipogenesis research and therapy. | 2011-11-10 |
| 20110275700 | BIODEGRADABLE POLYKETAL POLYMERS AND METHODS FOR THEIR FORMATION AND USE - The present invention relates to biodegradable biocompatible polyketals, methods for their preparation, and methods for treating animals by administration of biodegradable biocompatible polyketals. In one aspect, a method for forming the biodegradable biocompatible polyketals comprises combining a glycol-specific oxidizing agent with a polysaccharide to form an aldehyde intermediate, which is combined with a reducing agent to form the biodegradable biocompatible polyketal. The resultant biodegradable biocompatible polyketals can be chemically modified to incorporate additional hydrophilic moieties. A method for treating animals includes the administration of the biodegradable biocompatible polyketal in which biologically active compounds or diagnostic labels can be disposed. | 2011-11-10 |
| 20110275701 | ANTI-THROMBIN APTAMER FORMULATIONS AND METHODS FOR USE - The invention relates to the formulation, dosing, administration and use of an aptamer antagonist therapeutic that binds to thrombin. | 2011-11-10 |
| 20110275702 | Novel DNA Nanostructures that Promote Cell-Cell Interaction and Use Thereof - The present invention provides a ligand-nucleic acid nanostructure that promotes cell-cell interaction. Specially, the invention provides a ligand-nucleic acid nanostructure for treating tumor in a mammal. The methods of using and making the composition comprising a ligand-nucleic acid nanostructure are also provided. | 2011-11-10 |
| 20110275703 | SUBSTITUTED SPIROKETAL DERIVATIVES AND USE THEREOF AS THERAPEUTIC DRUG FOR DIABETES - The present invention provides a compound represented by Formula (II): | 2011-11-10 |
| 20110275704 | Stable Formulations for Lyophilizing Therapeutic Particles - The present disclosure generally relates to lyophilized pharmaceutical compositions comprising polymeric nanoparticles which, upon reconstitution, have low levels of greater than 10 micron size particles. Other aspects of the invention include methods of making such nanoparticles. | 2011-11-10 |
| 20110275705 | STABLE INJECTABLE OIL-IN-WATER DOCETAXEL NANOEMULSION - The present invention describes Stable injectable oil-in-water Docetaxel nanoemulsion composition having Docetaxel concentrations as high as 20 mg/ml, devoid of hypersensitivity reaction and fluid retention. It employs Synthetic triglycerides, and DSPE PEG-2000, Natural phosphatides, Polyhydric alcohol and Water for injection. In another embodiment lyophilised products with added Cryoprotectants have been described which on reconstitution gives nanoemulsion suitable for parenteral administration. | 2011-11-10 |
| 20110275706 | Pharmaceutical Compositions Containing Lipase Inhibitors - A pharmaceutical composition comprises at least one inhibitor of lipases, preferably an inhibitor of gastrointestinal and pancreatic lipases, such as orlistat, at least one surfactant, and at least one dispersant. | 2011-11-10 |
| 20110275707 | SUBSTITUTED AFPO (6-ARYL-4H-FURO[3,2-C]PYRAN-4-ONE) DERIVATIVES AS ANTI-CANCER AGENTS - Compounds of Formulas I are described, along with methods of using such compounds for the treatment of cancer and pharmaceutical formulations thereof. | 2011-11-10 |
| 20110275708 | POLYCYCLIC COMPOUNDS AND METHODS RELATED THERETO - The invention relates to a novel compound of formula I or pharmaceutically acceptable salts thereof as well as pharmaceutical, nutraceutical, and botanical drug compositions and therapeutic methods related thereto. In certain embodiments, the compounds are used for the treatment of abnormal cell growth, hyperproliferative disorders, and inflammatory diseases in mammals. In other embodiments, the invention encompasses methods to isolate and synthesize the compounds. | 2011-11-10 |
| 20110275709 | TELLURIUM-CONTAINING COMPOUNDS FOR AFFECTING MALE'S FERTILITY FOLLOWING CHEMOTHERAPY AND/OR RADIOTHERAPY - Use of tellurium-containing compounds for maintaining and/or augmenting fertility in a male subject following chemotherapy and/or radiotherapy is disclosed. The tellurium-containing compound is utilized in combination with a chemotherapeutic agent and/or radiation, such that the male subject treated by the chemotherapeutic agent and/or radiation and by the tellurium-containing compound is instructed to refrain from conceptive sex for a pre-determined time period, following the chemotherapy and/or radiotherapy, during which conception is undesired. | 2011-11-10 |
| 20110275710 | Agricultural Pesticide Formulations and Process for Making the Same - The present invention provides an agricultural pesticide formulation of reduced toxicity and high dispersibility, and a process for making the same. | 2011-11-10 |
| 20110275711 | METHOD FOR TREATING MACULAR EDEMA - Provided is a method for treating macular edema in a mammalian subject, comprising administering an effective amount of a fatty acid derivative to the subject in need thereof. The method of the present invention can effectively treat macular edema in a non-invasive manner. In one embodiment of the present invention, the fatty acid derivative is isopropyl unoprostone. | 2011-11-10 |
| 20110275712 | Oil In Water Emulsion Cosmetic Composition For Skin - An oil in water emulsion cosmetic composition for skin, in which vitamin A and its derivatives are stably incorporated and which has superior feeling in use (skin familiarity or feeling of skin absorption, feeling of efficacy after application) and base composition stability (emulsion stability) with the passage of time. The oil in water emulsion cosmetic composition for skin comprises, relative to the total amount of the cosmetic composition, (a) from 0.01 to 4% by mass of vitamin A and its derivative, (b) from 0.6 to 4% by mass of a nonionic surfactant comprising three of (b-1) sorbitan tristearate, (b-2) polyethylene glycol stearate with from 20 to 120 mols of polyethylene glycol added thereto, (b-3) glyceryl stearate having an HLB of from 5 to 8, and (c) from 1 to 10% by mass of a higher alcohol having from 14 to 24 carbon atoms, wherein the blend ratio (by mass) of component (b-1) to component (b) is from 0.1 to 0.8. | 2011-11-10 |
| 20110275713 | Acetylated amino acids as Anti-platelet agents, Nutritional And Vitamin Supplements - This invention relates to pharmaceutical compounds and nutritional supplements that are acetylated derivatives of naturally occurring amino acids and acetylated derivatives of peptides derived from naturally occurring amino acids containing hydroxyl groups. They are as useful as anti-platelet drugs, and as nutritional supplements. | 2011-11-10 |
| 20110275714 | Use Of Cationic Surfactants As Acaricidal Agents - This invention relates to a use of a composition for protecting against mites and ticks containing cationic surfactants such as ethyl-Nα-lauroyl-L-arginate HCl (LAE). It has been found that cationic surfactants such as ethyl-N | 2011-11-10 |
| 20110275715 | METHOD FOR TREATING RETINAL DISEASE - The present application provides a method for treating a retinal disease in a patient in need thereof, which comprises administering at least three drops of an ophthalmic composition comprising a fatty acid derivative as an active ingredient in an eye of the patient per day. | 2011-11-10 |
| 20110275716 | COMPOSITION AND METHOD FOR TREATMENT OF DIABETES - The present invention relates to a method of treating an incretin related disease such as diabetes, obesity and the like by delivery of butyric acid, bile acid, long chain fatty acid, or glutamine to the colon by bypassing the upper digestive tract. | 2011-11-10 |
