14th week of 2010 patent applcation highlights part 41 |
Patent application number | Title | Published |
20100087418 | BENZOXAZEPINE DERIVATIVES AND USE THEREOF - Compounds represented by the general formula (I): | 2010-04-08 |
20100087419 | HIV INTEGRASE INHIBITORS - Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: | 2010-04-08 |
20100087420 | Heterotricyclic Metalloprotease Inhibitors - The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors. | 2010-04-08 |
20100087421 | METHOD TO DETERMINE THE RISK FOR SIDE EFFECTS OF AN SSRI TREATMENT IN A PERSON - A new method is found to determine an increased risk for side effects of an SSRI treatment in a person by genotyping the person for the presence of the 102 C/C DNA sequence in the 5-HT | 2010-04-08 |
20100087422 | TREATMENT OF ADHD - A method is described for treating attention deficit hyperactivity disorder (ADHD), by administering to the individual an anti-epileptic mood stabiliser at a dose which is sub-therapeutic for mood stabilisation, optionally in combination with a psychostimulant. Also described is a method of improving reading comprehension and/or fluency in an individual suffering from learning difficulties which method comprises administering to the individual an anti-epileptic mood stabiliser. | 2010-04-08 |
20100087423 | NEW BENZAMIDE DERIVATIVES AS BRADYKININ ANTAGONISTS - The present invention relates to new phenylsulfamoyl benzamide derivatives of formula (I) | 2010-04-08 |
20100087424 | TRICYCLIC NITROGEN CONTAINING HETEROCYCLES AS ANTIBACTERIAL AGENTS - Tricyclic nitrogen containing compounds and their use as antibacterials. | 2010-04-08 |
20100087425 | Substituted N-Arylsulfonylheterocyclic Amines As Gamma-Secretase Inhibitors - This invention discloses novel gamma secretase inhibitors of the formula: | 2010-04-08 |
20100087426 | PROCESS AND INTERMEDIATES FOR THE SYNTHESIS OF 8-[-METHYL]-8-PHENYL-1,7-DIAZA-SPIRO[4.5]DECAN-2-ONE COMPOUNDS - This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations. | 2010-04-08 |
20100087427 | PYRROLIDINE DERIVATIVES FOR THE TREATMENT OF A DISEASE DEPENDING ON THE ACTIVITY OF RENIN - Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I | 2010-04-08 |
20100087428 | Novel Potassium Channel Blockers - The present invention provides a compound of formula (I) | 2010-04-08 |
20100087429 | SPIRO-TRICYCLIC RING COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I | 2010-04-08 |
20100087430 | NOVEL BENZOFURAN POTASSIUM CHANNEL BLOCKERS AND USES THEREOF - The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of K | 2010-04-08 |
20100087431 | TRIAZOLYL AMINOPYRIMIDINE COMPOUNDS - The present invention provides triazolyl aminopyrimidine compounds useful in the treatment of cancer. | 2010-04-08 |
20100087432 | PYRROLE DERIVATIVES HAVING CRTH2 RECEPTOR ANTAGONIST ACTIVITY - There are provided according to the invention compounds of formula (I) as CRTh2 antagonists. In free or salt form, wherein R | 2010-04-08 |
20100087433 | Methods of inhibiting tryptophan hydroxylase - Compounds, compositions and methods of treating serotonin-mediated diseases and disorders are disclosed. | 2010-04-08 |
20100087434 | NK-1 and Serotonin Transporter Inhibitors - The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both. | 2010-04-08 |
20100087435 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 2010-04-08 |
20100087436 | METHOD OF PREVENTING OR TREATING ORGAN, HEMATOPOIETIC STEM CELL OR BONE MARROW TRANSPLANT REJECTION - Methods of preventing or treating organ, hematopoietic stem cell or bone marrow transplant rejection are disclosed. | 2010-04-08 |
20100087437 | Novel Potassium Channel Blockers - The present invention provides a compound of formula (I) | 2010-04-08 |
20100087438 | New Potassium Channel Blockers - The present invention provides a compound of formula (I) | 2010-04-08 |
20100087439 | NOVEL PREVENTIVE AND/OR THERAPEUTIC AGENT FOR NEUROPATHIC PAIN - The present invention relates to an agent for preventing and/or treating neuropathic pain comprising a 2-[(substituted-inden-7-yloxy)methyl]morpholine of the formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient. The invention is useful for providing an excellent agent for preventing and/or treating neuropathic pain, and particularly useful for providing an agent for preventing and/or treating allodynia, hyperalgesia, hyperesthesia, spontaneous pain, cancer pain, trigeminal neuralgia, phantom limb pain, postherpetic neuralgia, fibromyalgia, low back/leg pain, thalamic pain, entrapment (compressive) peripheral neuropathy, atypical facial pain, pain accompanying spinal cord injury, pain accompanying multiple sclerosis, pain accompanying chemotherapy-induced neuropathy, cancer pain on which an analgesic effect of a narcotic analgesic such as morphine is insufficient, pain accompanying diabetic neuropathy, and the like. | 2010-04-08 |
20100087440 | Phosphatidylinositol 3-Kinase Inhibitors and Methods of Their Use - The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases. | 2010-04-08 |
20100087441 | Prognostic Method - A method for prognosing a rheumatoid arthritis phenotype using the outcomes of selected single nucleotide polymorphisms (SNPs) and clinical variables. A method for genotyping multiple rheumatoid arthritis associated genetic variations comprising use of a DNA microrarray. A microarray for use in the described methods. | 2010-04-08 |
20100087442 | DIKETOHYDRAZINE DERIVATIVE COMPOUNDS AND DRUGS CONTAINING THE COMPOUNDS AS THE ACTIVE INGREDIENT - The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). | 2010-04-08 |
20100087443 | 9-SUBSTITUTED-8-OXO-ADENINE COMPOUNDS AS TOLL-LIKE RECEPTOR (TLR7) MODULATORS - The present invention provides compounds of formula | 2010-04-08 |
20100087444 | IMATINIB MESYLATE - There is provided a solid dispersion of imatinib mesylate that includes imatinib mesylate and a pharmaceutically acceptable carrier, wherein said carrier is a cellulose derivative. Also provided is a process for making a solid dispersion and a process for making imatinib. | 2010-04-08 |
20100087445 | ARYL PIPERAZINE DERIVATIVES USEFUL FOR THE TREATMENT OF NEUROPSYCHIATRY DISORDERS - This invention provides novel aryl piperazine derivatives represented by Formula (I) having medical utility, in particular as modulators of dopamine and serotonin receptors, preferably the D | 2010-04-08 |
20100087446 | 2-SUBSTITUTED INDOLE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS - 2-Substituted indole derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. | 2010-04-08 |
20100087447 | PHARMACEUTICAL COMPOSITION COMPRISING PYRAZINE DERIVATIVE, AND METHOD OF USING PYRAZINE DERIVATIVE IN COMBINATION - Disclosed is a pharmaceutical composition comprising a pyrazine derivative represented by the general formula: | 2010-04-08 |
20100087448 | Dihydropyrimidine Compounds and Their Uses in Preparation of Medicaments for Treating and Preventing Antiviral Diseases - The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof, to a process for preparing the compound of formula (I), and to use of the compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof as a medicament, in particular as a medicament for the treatment and prevention of type B hepatitis. | 2010-04-08 |
20100087449 | HETEROARYLAMIDE PYRIMIDONE COMPOUNDS - The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: | 2010-04-08 |
20100087450 | ORGANIC COMPOUNDS - The present invention relates to a new use of phosphodiesterase 1 (PDE1) inhibitors for the treatment and/or prophylaxis of narcolepsy. | 2010-04-08 |
20100087451 | POLYMORPH B OF N--N-METHYL-ACETAMIDE - The present invention relates to a novel polymorph of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-acetamide, processes for its preparation, its use as a medicament, its use in the manufacture of a medicament, and pharmaceutical compositions comprising the novel polymorph. | 2010-04-08 |
20100087452 | PYRIDYL-TRIAZOLOPYRIMIDINE DERIVATIVE OR ITS SALT, PESTICIDE CONTAINING IT AND ITS PRODUCTION PROCESS - To provide a novel pesticide. The present invention provides a pesticide containing a pyridyl-triazolopyrimidine derivative represented by the formula (I) or its salt as an active ingredient: wherein R | 2010-04-08 |
20100087453 | COMPOUNDS, SCREENS, AND METHODS OF TREATMENT - The present invention features compounds of Formula (I), pharmaceutical compositions, methods of synthesis, and methods for treating diseases and conditions associated with cellular necrosis. Screening assays for identifying compounds useful for treating these conditions are also described. | 2010-04-08 |
20100087454 | MUCOSAL BIOADHESIVE SLOW RELEASE CARRIER FOR DELIVERING ACTIVE PRINCIPLES - A mucosal bioadhesive slow release carrier comprising an active principle, which can release the active principal for a duration of longer than 20 hours. This bioadhesive carrier contains at least one bioadhesive natural protein of vegetal origin and preferably a pea protein from the genus | 2010-04-08 |
20100087455 | SUBSTITUTED XANTHINE COMPOUNDS - The present invention relates to new substituted xanthine-based agents, pharmaceutical compositions thereof, and methods of use thereof. | 2010-04-08 |
20100087456 | PYRIDOPYRIMIDINONE INHIBITORS OF PI3K-ALPHA and mTOR - The invention is directed to Compounds of Formula I: | 2010-04-08 |
20100087457 | DOSAGES AND METHODS FOR THE TREATMENT OF CANCER - In general, the invention relates to a pharmaceutical dose having (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride as the active ingredient that upon administration to a subject provides a C | 2010-04-08 |
20100087458 | METHOD OF TREATING MELANOMA - Disclosed is (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride effective as a cytotoxic agent. (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride is useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, and in particular to its use in treating melanoma. | 2010-04-08 |
20100087459 | FORMS OF LAPATINIB COMPOUNDS AND PROCESSES FOR THE PREPARATION THEREOF - The present invention provides novel crystalline and amorphous lapatinib compounds and processes for preparing them | 2010-04-08 |
20100087460 | ARYLAMIDE PYRIMIDONE DERIVATIVES - The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: | 2010-04-08 |
20100087461 | ARYLAMIDE PYRIMIDONE COMPOUNDS - The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: | 2010-04-08 |
20100087462 | METHODS FOR PREDICTING AND DETECTING INTOLERANCE TO AN HYPOLIPIDEMIC AGENT - The invention describes methods and tools for the identification of drug intolerance into subjects receiving an hypolipidemic agent. The invention further describes methods and tools for the prediction of drug intolerance in subjects in need of hypolipidemic agents. Some aspects of the invention are based on the assessment of the subject plasma glycerol concentrations. Some aspects of the invention are based on the assessment of the subject HDL-triglycerides concentration. Some other aspects are based on the identification of hepatic lipase gene variants in a subject genome. | 2010-04-08 |
20100087463 | PHARMACEUTICAL COMPOSITIONS COMPRISING NILOTINIB OR ITS SALT - A pharmaceutical composition, especially capsules. comprising granules containing nilotinib or a salt thereof with at least one pharmaceutically acceptable excipient. The granules may be produced by a wet granulation process. | 2010-04-08 |
20100087464 | PROTEIN KINASE INHIBITORS AND METHODS FOR USING THEREOF - The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of TrkA, TrkB, TrkC, Abl, Bcr-Abl, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKCα, Raf, ROCK-II, Rsk1, and SGK kinases, or a combination thereof. | 2010-04-08 |
20100087465 | HETEROCYCLIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS - Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control. The compounds of the invention are orally active. | 2010-04-08 |
20100087466 | NOVEL SMALL MOLECULE DNAK INHIBITORS - Methods of inhibiting HSP70 proteins, agents causing the inhibition of HSP70 proteins, and the effects of such inhibition on cell proliferation. Anti-microbial agents comprising small molecules, or pharmaceutical salts thereof, disclosed herein and further methods of use thereof are also disclosed. The disclosed small molecules, or pharmaceutical salts thereof, are effective in inhibiting microbial chaperone activity in microbes, such as homologs of HSP70. The disclosed small molecules, or pharmaceutical salts thereof, are also effective for the therapeutic treatment of cancer. | 2010-04-08 |
20100087467 | Compositions Useful As Inhibitors of Protein Kinases - The present invention provides compounds of formula I: | 2010-04-08 |
20100087468 | MODULATORS OF PPAR AND METHODS OF THEIR PREPARATION - The present invention is directed to certain novel compounds represented by Formula (I) and pharmaceutically acceptable salts, solvates, hydrates and prodrugs thereof. The present invention is also directed to methods of making and using such compounds and pharmaceutical compositions containing such compounds to treat or control a number of diseases mediated by PPAR such as glucose metabolism, lipid metabolism and insulin secretion, specifically Type 2 diabetes, hyperinsulinemia, hyperlipidemia, hyperuricemia, hypercholesteremia, atherosclerosis, one or more risk factors for cardiovascular disease, Syndrome X, hypertriglyceridemia, hyperglycemia, obesity and eating disorders. | 2010-04-08 |
20100087469 | Natural product derivatives with antimalarial activity - The present invention provides new chemical compositions with desirable biological activity and toxicity profiles for the enhanced treatment of malaria. | 2010-04-08 |
20100087470 | Buprenorphine-Wafer for Drug Substitution Therapy - The present invention relates to oral pharmaceutical dosage forms comprising buprenorphine with the dosage form releasing buprenorphine instantly upon oral, preferably sublingual, application of the dosage form. The present invention also relates to the use of such dosage forms for treating pain in a human or animal or for drug substitution therapy in drug-dependent human subjects. | 2010-04-08 |
20100087471 | INDOLE AND INDOLINE DERIVATIVES AND METHODS OF USE THEREOF - The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) | 2010-04-08 |
20100087473 | FREEZE-DRIED INJECTABLE PHARMACEUTICAL COMBINATION OF SEMISYNTHETIC VINCA ALKALOIDS AND CARBOHYDRATE STABLE AT ROOM TEMPERATURE - This invention relates to pharmaceutical compositions consisting of a semisynthetic derivative of vinca alkaloid, stable at room temperature, in which said derivative is present in the form of a freeze dried product obtained in the presence of at least one carbohydrate. | 2010-04-08 |
20100087474 | MATERIALS AND METHODS FOR ENHANCED DEGRADATION OF MUTANT PROTEINS ASSOCIATED WITH HUMAN DISEASE - The invention features compositions and methods that are useful for treating or preventing a protein conformation disease in a subject by enhancing the degradation of misfolded proteins in vivo. | 2010-04-08 |
20100087475 | PHARMACEUTICAL COMPOUNDS - This application describes substituted 1,3,4,6,7,11b-hexahydro-benzo(a)quinolizine compounds, pharmaceutical compositions containing them, processes for making them and their therapeutic methods. | 2010-04-08 |
20100087476 | PHARMACEUTICAL COMPOUNDS - This application describes methods of treatment and/or prophylaxis of asthma that involve administration of dihydrotetrabenazine, and isomers and/or pharmaceutically acceptable salts thereof. | 2010-04-08 |
20100087477 | SELECTIVE GLYCOSIDASE INHIBITORS - The present invention provides glucoimidazole derivatives and methods of making them. The compounds can be used to inhibit the activity of O-GlcNAcase enzymes, including both bacterial OGA (bOGA) and human OGA (hOGA) and can be selective, showing low inhibition of hexosaminidases. The compounds can be used to study the role of the O-GlcNAcase modification in human or animal cells. Furthermore the compounds can have therapeutic uses in the treatment of diseases mediated by the activity of O-GlcNAcase enzymes including type II diabetes, Alzheimers disease, and cancer. | 2010-04-08 |
20100087478 | HIF-1 Inhibitors - HIF-1 inhibitors and methods of their use are provided. In particular, 2,2-dimethylbenzopyran based compounds and methods of their use, for example in the treatment or prevention of hypoxia-related pathologies are provided. | 2010-04-08 |
20100087479 | Compositions Useful as Inhibitors of Voltage-Gated Sodium Channels - The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 2010-04-08 |
20100087480 | SUBSTITUTED PHENYLMETHYL BICYCLOCARBOXYAMIDE COMPOUNDS - This invention provides a compound of the formula (I). These compounds are useful for the treatment of disease conditions caused by overactivation of the VR1 receptor such as pain, or the like in mammal. This invention also provides a pharmaceutical composition comprising the above compound. | 2010-04-08 |
20100087481 | ORAL PHARMACEUTICAL FORMULATIONS FOR ANTIDIABETIC COMPOUNDS - Oral pharmaceutical preparations of salts and polymorphs of a compound useful in the treatment of inflammatory and metabolic conditions and diseases are provided herein. The oral pharmaceutical preparation is useful for the treatment or prevention of conditions and disorders associated with energy homeostasis such as type II diabetes, lipid metabolism, adipocyte differentiation and inflammation. | 2010-04-08 |
20100087482 | Method for Treating Gefitinib Resistant Cancer - The present invention is directed to methods for the treatment of gefitinib and/or erlotinib resistant cancer. An individual with cancer is monitored for cancer progression following treatment with gefitinib and/or erlotinib. Progression of the cancer is indicative that the cancer is resistant to gefitinib and/or erlotinib. Once progression of cancer is noted, the subject is administered a pharmaceutical composition comprising an irreversible epidermal growth factor receptor (EGFR) inhibitor. In preferred embodiments, the irreversible EGFR inhibitor is EKB-569, HKI-272 and HKI-357. | 2010-04-08 |
20100087483 | Aminosulfonyl Substituted 4-(Aminomethyl)-Piperidine Benzamides As 5HT 4-Antagonists - The present invention is concerned with novel compounds of formula (I) having 5HT | 2010-04-08 |
20100087484 | AMINOALKOXY ARYL SULFONAMIDE COMPOUNDS AND THEIR USE AS 5-HT6 LIGANDS - The present invention relates to novel aminoalkoxy arylsulfonamide compounds of the formula (I), their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. These compounds are useful in the treatment of various disorders that are related to 5-HT | 2010-04-08 |
20100087485 | 4-AMINOPIPERIDINE DERIVATIVES - The present invention relates to compounds of the formula (I) | 2010-04-08 |
20100087486 | METHODS FOR USING TGF-B RECEPTOR INHIBITORS OR ACTIVIN-LIKE KINASE (ALK) 5 INHIBITORS A-83-01 AND SB-431542 TO TREAT EYE DISEASE AND WOUND HEALING CONDITIONS - A pharmaceutical composition useful in the prevention of subconjunctival scarring that may occur after glaucoma filtration surgery comprising an effective amount of an activin receptor-like kinase 5 inhibitor. Also disclosed is a method of treating corneal haze and subconjunctival scarring that may develop after ocular surgery comprising applying an amount of a pharmaceutical composition including an activin receptor-like kinase 5 inhibitor. | 2010-04-08 |
20100087487 | 3-CYANO-4-(4-TETRAHYDROPYRAN-PHENYL)-PYRIDIN-2-ONE DERIVATIVES - The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate 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 such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved. | 2010-04-08 |
20100087488 | Physiologically Acceptable Salts of 3-[(2--1-methyl-1H-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionic acid ethyl ester - The invention relates to new salt forms of the active substance ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-propionate. | 2010-04-08 |
20100087489 | Phenyl and Benzodioxinyl Substituted Indazoles Derivatives - A compound of formula Ia: | 2010-04-08 |
20100087490 | Dosage Units of 3-(6-(1-(2,2-Difluorobenzo[D] [1,3] Dioxol-5-YL) Cyclopropanecarboxamido)-3-Methylpyridin-2-YL)Benzoic Acid - The present invention relates to formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in Form I, pharmaceutical packs or kits thereof, and methods of treatment therewith. | 2010-04-08 |
20100087491 | POLYCYCLIC COMPOUNDS - The invention relates to novel diaryl oxadiazole compounds of Formula I: | 2010-04-08 |
20100087492 | SYSTEMIC TREATMENT OF BLOOD-SUCKING AND BLOOD-CONSUMING PARASITES BY ORAL ADMINISTRATION OF A PARASITICIDAL AGENT - Pharmaceutically acceptable single parasiticidal agent compositions of imidacloprid for oral delivery to mammals to systemically control targeted blood-sucking or blood-consuming parasites, such as fleas, ticks and certain species of helminthes and scabies. | 2010-04-08 |
20100087493 | METHOD FOR IMPROVING THE PHARMACOKINETICS OF DRUGS METABOLIZED BY UGT2B10 - A method for modifying the pharmacokinetics of a pharmacologically active agent that undergoes direct N-glucuronidation by UDP-glucuronosyltransferase isoenzyme UGT2B10 in a human subject comprising administering an effective amount of an UGT2B10 modulator to said human subject. A method for identifying compounds which are directly metabolized by UGT2B10 or which act as UGT2B10 modulators is also disclosed. | 2010-04-08 |
20100087494 | FUNGICIDE N-(3-PHENYLPROPYL) CARBOXAMIDE DERIVATIVES - A compound of general formula (I): | 2010-04-08 |
20100087495 | PHENYL DERIVATIVES AND THEIR USE AS IMMUNOMODULATORS - The invention relates to phenyl derivatives of formula (I), their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. | 2010-04-08 |
20100087496 | NOVEL CINNAMIC AMIDE DERIVATIVES USEFUL AS ION CHANNEL MODULATORS - This invention relates to novel cinnamic amide derivatives that are found to be potent modulators of ion channels and, as such, they are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to modulation of ion channels. | 2010-04-08 |
20100087497 | Benzimidazole Anthelmintic Compositions - The present invention provides a veterinary anthelmintic composition that includes: at least 10% w/v of a benzimidazole anthlemintic; and b) a water-immiscible solvent system, which comprises a lactone solvent, an essential oil, and surfactant. | 2010-04-08 |
20100087498 | USE OF BIOTIN TO PREVENT PHOTOAGING - Use of biotin, preferably in a combination of biotin and (-)-epigallocatechin gallate (EGCG) in a specific ratio, to prevent sunlight-induced aging (photoaging) of the skin. | 2010-04-08 |
20100087499 | PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING TEMOZOLOMIDE AND MULTI-TARGETED KINASE INHIBITORS - The present invention provides formulations, kits and methods useful for treating cell proliferative disorder. In particular, the formulations, kits and methods include temozolomide (TMZ) in combination with a multi-targeted kinase inhibitor. | 2010-04-08 |
20100087500 | Methods and Compositions for Treatment of Acute Heart Failure - The present disclosure provides methods and compositions for treating acute heart failure, by administering to a subject in need thereof a therapeutically effective amount of an AICA riboside analog or a pharmaceutically acceptable salt or prodrug thereof. | 2010-04-08 |
20100087501 | Highly Bioavailable Composition Containing Eprosartan-Poloxamer Complex or 2-(7-Chloro-5-Methyl-4-Oxo-3-Phenyl-4,5-Dihydro-3H-Pyridazine (4,5-b)Indol-1-yl)-N,N-Dimethylacetamide - Poloxamer Complex - A composition including an association complex of a pharmaceutical composition and one or more polyethylene-polypropylene glycol block copolymers (poloxamers) is provided. The pharmaceutical composition may include a member selected from the group consisting of (a) an association complex of an eprosartan composition including eprosartan or a pharmaceutically acceptable salt of eprosartan and (b) the non-zwitterionic compound 2-(7-chloro-5-methyl-4-oxo-3-phenyl-4,S dihydro-3H-pyridazino(4,S-b)indol-1-yl)N,N-dimethylacetamide (NZ). | 2010-04-08 |
20100087502 | Indazoles Used To Treat Estrogen Receptor Beta Mediated Disorders - The present invention relates to novel indazole derivatives having pharmacological activity, processes for their preparation, compositions containing them and uses of these compounds in the treatment of estrogen receptor beta mediated diseases. | 2010-04-08 |
20100087503 | KETOROLAC TROMETHAMINE COMPOSITIONS FOR TREATING OR PREVENTING OCULAR PAIN - The present invention provides an aqueous ophthalmic solution comprising an effective amount of ketorolac which comprises carboxymethyl cellulose in an aqueous solution which provides increased visual acuity in users and wherein said concentration of carboxymethyl cellulose is selected to provide an increased absorption of ketorolac in the eye of a patient which is at least 130% greater than the absorption of a comparative aqueous ketorolac ophthalmic solution having the same concentration of ketorolac. | 2010-04-08 |
20100087504 | Use of Diindolylmethane (DIM) Compounds and Derivatives as Neuroprotective Agents - Presented herein are diindolylmethane derivative compounds useful for the prevention and or treatment of neurological conditions, including neurological conditions related to neuroinflammation. One such neurological condition is Parkinson's disease. | 2010-04-08 |
20100087505 | Compounds Having Aryl-Sulphonamidic Structure Useful As Metalloproteases Inhibitors - The invention relates to aryl-sulphonamido compounds endowed with inhibitory activity against metallo proteases MMP, having formula (I) below | 2010-04-08 |
20100087506 | CYCLIC AMINE COMPOUND - Provision of a compound having a superior androgen receptor regulating action. | 2010-04-08 |
20100087507 | USE OF RPN2 GENE EXPRESSION INHIBITOR - The present invention uses an RPN2 gene expression inhibitor as a cancer cell growth inhibitor, which further includes a drug showing an anti-cancer action if desired, and is administered in combination with atelocollagen if desired. In addition, the present invention is an anti-cancer agent including such cancer cell growth inhibitor. | 2010-04-08 |
20100087508 | Compositions and Methods for Inhibiting Expression of Eg5 and VEGF Genes - This invention relates to compositions containing double-stranded ribonucleic acid (dsRNA) in a SNALP formulation, and methods of using the compositions to inhibit the expression of the Eg5 and Vascular Endothelial Growth Factor (VEGF), and methods of using the compositions to treat pathological processes mediated by Eg5 and VEGF expression, such as cancer. | 2010-04-08 |
20100087509 | Methods, Agents, and Compound Screening Assays for Inducing Differentiation of Undifferentiated Mammalian Cells into Osteoblasts - The present invention relates to methods, agents and compound screening assays for inducing differentiation of undifferentiated mammalian cells into osteoblasts. The invention thus provides a method, comprising contacting a compound with a polypeptide comprising an amino acid sequence selected from the group consisting of SEQ ID No: 194-309; and measuring a compound-polypeptide property related to the differentiation of said cells. The invention further relates to a bone formation enhancing pharmaceutical composition, and the use thereof in treating and/or preventing a disease involving a systemic or local decrease in mean bone density in a subject. Furthermore, the invention relates to a method for the in vitro production of bone tissue. | 2010-04-08 |
20100087510 | Novel Adaptor protein that binds to mammalian toll-like receptor 3 and gene thereof - A novel adaptor protein and its gene are provided. The novel adaptor protein has a property of binding to mammalian Toll-like receptor 3, which controls type I interferon production that is effective for prevention/treatment of viral infectious disease such as hepatitis B, hepatitis C, and the like, treatment of tumors, and the other purposes. Novel adaptor protein TICAM-1, which has an amino acid sequence set forth in SEQ ID NO: 2 or 4, specifically binds to the mammalian Toll-like receptor 3 and induces production of type I interferon. A mutant of the adaptor protein TICAM-1 has similar properties, provided that it has TIR domain (an amino acid sequence ranging from 394-position to 532-position in the amino acid sequence set forth in SEQ ID NO: 2 or an amino acid sequence ranging 396-position to 534-position in the amino acid sequence set forth in SEQ ID NO: 4). The gene is a gene encoding the adaptor protein TICAM-1. | 2010-04-08 |
20100087511 | SPINAL MUSCULAR ATROPHY (SMA) TREATMENT VIA TARGETING OF SMN2 SPLICE SITE INHIBITORY SEQUENCES - The present invention is directed to methods and compositions capable of blocking the inhibitory effect of a newly-identified intronic inhibitory sequence element, named ISS-N1 (for “intronic splicing silencer”), located in the SMN2 gene. The compositions and methods of the instant invention include oligonucleotide reagents (e.g., oligoribonucleotides) that effectively target the SMN2 ISS-N1 site in the SMN2 pre-mRNA, thereby modulating the splicing of SMN2 pre-mRNA to include exon 7 in the processed transcript. The ISS-N1 blocking agents of the invention cause elevated expression of SMN protein, thus compensating for the loss of SMN protein expression commonly observed in subjects with spinal muscular atrophy (SMA). | 2010-04-08 |
20100087512 | MICRORNA MOLECULES | 2010-04-08 |
20100087513 | MICRORNA MOLECULES | 2010-04-08 |
20100087514 | METHOD AND MEANS FOR TREATMENT OF OSTEOARTHRITIS - The present invention relates to in vivo and in vitro methods, agents and compound screening assays for inducing anabolic stimulation of chondrocytes, including cartilage formation enhancing pharmaceutical compositions, and the use thereof in treating and/or preventing a disease involving a systemic or local decrease in mean cartilage thickness in a subject. | 2010-04-08 |
20100087515 | IKK-BETA SERINE-THREONINE PROTEIN KINASE INHIBITORS - Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: Formula (A) and (B) wherein R | 2010-04-08 |
20100087516 | ANTIBACTERIAL MACROLACTIN A THAT BACILLUS POLYFERMENTICUS KJS-2 PRODUCED IN - The present invention relates to uses of Macrolactin A produced by | 2010-04-08 |
20100087517 | PRODRUGS OF SUBSTITUTED 1,3-DIOXANES AND THEIR USES - The present invention relates to prodrugs of compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The prodrugs of the compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer. | 2010-04-08 |
20100087518 | DELTA 9 - TETRAHYDROCANNABINOL PROCESSING - The present invention provides a process for handling Δ9-THC, which comprises preparing a solution of Δ9-THC in a solvent which exists as a gas at room temperature and atmospheric pressure. The invention also provides solutions of Δ9-THC in the solvent and solid preparations of Δ9-THC. | 2010-04-08 |