02nd week of 2011 patent applcation highlights part 45 |
Patent application number | Title | Published |
20110009371 | SYNTHESIS OF TETRACYCLINES AND ANALOGUES THEREOF - The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals. | 2011-01-13 |
20110009372 | Compounds and compositions - The invention provides compositions comprising formula 1 steroids, e.g., 16α-bromo-3β-hydroxy-5α-androstan-17-one hemihydrate and one or more excipients, including compositions that comprise a liquid formulation comprising less than about 3% v/v water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16α-bromo-3β-hydroxy-5α-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using the compounds. The invention also provides methods to make and use these immunomodulatory compositions and formulations. | 2011-01-13 |
20110009373 | COMPOSITION COMPRISING A COMBINATION OF AN AROMATASE INHIBITOR, A PROGESTIN AND AN OESTROGEN AND ITS USE FOR THE TREATMENT OF ENDOMETRIOSIS - The invention relates to a method of treating endometriosis using a combination of an aromatase inhibitor, a progestin and an oestrogen. The invention also relates to pharmaceutical formulations comprising said combination. | 2011-01-13 |
20110009374 | METHOD OF WOUND HEALING AND SCAR MODULATION - The invention relates to methods of promoting wound healing and reducing scar formation by administration of corticosteroids, and pharmaceutical compositions comprising corticosteroids. | 2011-01-13 |
20110009375 | FUSIDIC ACID REGIMENS FOR TREATMENT OF BACTERIAL INFECTIONS - Novel dosing regimens for the treatment and prevention of bacterial infections using fusidic acid are described. The use of a high loading dose of fusidic acid, followed by moderate maintenance doses of the drug, have been found to prevent development of drug-resistant strains of bacteria, to increase the effective spectrum of the drug, and to avoid nausea and vomiting associated with a prolonged course of therapy of high amounts of the drug. | 2011-01-13 |
20110009376 | PROPHYLACTIC OR THERAPEUTIC AGENT FOR EYE DISEASE ACCOMPANIED BY OPTIC NERVE DISORDER - The present invention provides a novel pharmaceutical use of 2-phenyl-1,2-benzisoselenazol-3(2H)-one or a salt thereof. 2-Phenyl-1,2-benzisoselenazol-3(2H)-one or a salt thereof exhibits an excellent suppressive effect on retinal ganglion cell death in a pharmacological test using rats, and is therefore useful as a prophylactic or therapeutic agent for an eye disease accompanied by optic nerve disorder. | 2011-01-13 |
20110009377 | AZETIDINE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPY - The invention relates to azetidine derivatives having the formula (I): | 2011-01-13 |
20110009378 | Heterocyclic compounds, pharmaceutical compositions containing them, and their use in therapy - The present invention relates to heterocyclic compounds of the formula (I) | 2011-01-13 |
20110009379 | INDOLINONE COMPOUND - [Problems] A compound, which is useful as an active ingredient for a pharmaceutical composition, for example a pharmaceutical composition for treating constipation-type irritable bowel syndrome, atonic constipation and/or functional gastrointestinal disorder, is provided. | 2011-01-13 |
20110009380 | QUINOLINE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR - The present invention relates to novel quinoline compounds. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT | 2011-01-13 |
20110009381 | SOLUBILIZED THIAZOLOPYRIDINES - Provided herein are novel sirtuin-modulating compounds Structural Formula (I): and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 2011-01-13 |
20110009382 | Substituted Benzimidazoles, Benzothiazoles and Benzoxazoles - Substituted benzimidazoles, benzothiazoles and benzoxazoles, processes for their preparation, pharmaceutical compostions containing these compounds and the use of these compounds for treating or inhibiting disorders or disease states mediated at least in part by bradykinin receptor 1 (BR1). | 2011-01-13 |
20110009383 | METHOD OF TREATING MIXED LINEAGE LEUKEMIA GENE-REARRANGED ACUTE LYMPHOBLASTIC LEUKEMIAS - The present invention relates to a method of treating a warm-blooded animal, especially a human, having Mixed Lineage Leukemia (MLL rearranged ALL) comprising administering to said animal a therapeutically effective amount of a staurosporine derivative, especially PKC412 or a pharmaceutically acceptable salt thereof, alone or in combination with further therapeutic measures, for example, those defined herein; to the use of a staurosporine derivative for the preparation of a medicament for the treatment of MLL rearranged ALL; and to a commercial package comprising a staurosporine derivative together with instructions for its use in the treatment of MLL rearranged ALL. | 2011-01-13 |
20110009384 | FUSED RING COMPOUNDS AS PARTIAL AGONISTS OF PPAR-GAMMA - The present invention provides an agent for the prophylaxis or treatment of diabetes, which has a superior hypoglycemic action, and is associated with a fewer side effects such as body weight gain and the like. | 2011-01-13 |
20110009385 | COMPOUNDS - A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, | 2011-01-13 |
20110009386 | FURO[3, 2-B] PYRR0L-3-0NES AS CATHESPIN S INHIBITORS - A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, | 2011-01-13 |
20110009387 | HISTONE H2AX (HH2AX) BIOMARKER FOR FTI SENSITIVITY - The present invention relates e.g., to methods for predicting cellular sensitivity to farnesyl protein transferase inhibitors, such as lonafarnib; manumycin A; FTI-276; L-744832; BMS-214662; tipifarnib; BMS-316810K. The methods involve determining if malignant cells exhibit increased expression. of phosphorylated histone H2Ax following contact of one or more of said cells with said inhibitor. | 2011-01-13 |
20110009388 | Formulations and Methods of Administration of Cephalotaxines, Including Homoharringtonine - The present invention is directed to compositions and methods for the treatment of patients with cephalotaxines, for example, homoharringtonine. The invention is also directed to improvements in the purity, manufacturing process, formulation and administration of homoharringtonine for the treatment of cancer and other aberrant cellular diseases. The invention also provides methods and compositions for antiparasitic, antifungal, antiviral and antibacterial treatments. | 2011-01-13 |
20110009389 | IMIDAZOLE DERIVATIVE, THEIR PRODUCTION AND USE - There is provided an imidazole derivative useful as a thrombosis treating agent, which is represented by the formula (I): | 2011-01-13 |
20110009390 | 2-OXO-2- (2-PHENYL-5,6,7,8-TETRAHYDRO-INDOLIZIN-3-YL) -ACETAMIDE DERIVATIVES AND RELATED COMPOUNDS AS ANTIFUNGAL AGENTS - The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof: wherein: R1, R2, R3, R4, R5, R6, R7, R8, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in the manufacture of medicaments for use in the prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides. | 2011-01-13 |
20110009391 | TETRAHYDROQUINOXALINE UREA DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION - The present invention relates to tetrahydroquinoxaline urea derivatives, to their preparation and to their therapeutic application. | 2011-01-13 |
20110009392 | GAMMA SECRETASE MODULATORS - In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions. | 2011-01-13 |
20110009393 | Novel Soluble 1,4 Benzodiazepine Compounds and Stable Salts Thereof - The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and related compounds and methods of using benzodiazepine derivatives and related compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like. | 2011-01-13 |
20110009394 | TRICYCLIC NITROGEN COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS - Tricyclic nitrogen containing compounds and their use as antibacterials. | 2011-01-13 |
20110009395 | BACE INHIBITORS - The present invention provides BACE inhibitors of Formula I: | 2011-01-13 |
20110009396 | TRICYCLIC COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS - The present invention provides compounds represented by formula 1: | 2011-01-13 |
20110009397 | TRIAZONE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound. | 2011-01-13 |
20110009398 | p27 Protein Inducer - The present invention provides a p27 protein inducing agent comprising a compound represented by general formula (11) below or pharmaceutically acceptable salt thereof as an active ingredient: | 2011-01-13 |
20110009399 | ORGANIC COMPOUNDS - The application relates to trisubstituted piperidines of the general formula (I) and their salts, preferably their pharmaceutically acceptable salts, in which R | 2011-01-13 |
20110009400 | BICYCLIC DERIVATIVES OF AZABICYCLIC CARBOXAMIDES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The disclosure relates to compounds of formula (I): | 2011-01-13 |
20110009401 | 2-AZA-BICYCLO[2.2.1]HEPTANE DERIVATIVES - The invention relates to novel 2-aza-bicyclo[2.2.1]heptane derivatives of formula (I), | 2011-01-13 |
20110009402 | Cyclic Inhibitors of 11Beta-Hydroxysteroid Dehydrogenase 1 - The invention relates to novel compounds of the Formula Ik, Im | 2011-01-13 |
20110009403 | 2-MORPHOLINYLPURINES AS INHIBITORS OF PI3K - The present invention relates to purine compounds that are useful as kinase inhibitors. More particularly, the present invention relates to purine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with mTOR kinases. | 2011-01-13 |
20110009404 | 4-ARYL-2-ANILINO-PYRIMIDINES - The present invention relates to compounds of Formula (Ia) or (Ib), the N-oxide forms, pharmaceutically acceptable addition salts, quaternary amines, stereoisomers, tautomers, racemics, metabolites, prodrugs, hydrates, or solvates thereof, | 2011-01-13 |
20110009405 | PYRIMIDINYL AND 1,3,5-TRIAZINYL BENZIMIDAZOLES AND THEIR USE IN CANCER THERAPY - Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazoles of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs. | 2011-01-13 |
20110009406 | TETRAHYDRO-1H-PYRROLO FUSED PYRIDONES - The present invention relates to tetrahydro-1H-pyrrolo fused pyridone compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions. | 2011-01-13 |
20110009407 | PYRIDINONE ANTAGONISTS OF ALPHA-4 INTEGRINS - The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: | 2011-01-13 |
20110009408 | METHODS FOR IDENTIFIYING INHIBITORS AGAINST VIRUSES THAT USE A CLASS I FUSION PROTEIN - The invention concerns the generation of a three dimensional model of the six helix bundle (6HB) complexed with an inhibitor and the use of that model to identify, screen and/or develop inhibitors against viruses that use a class I fusion protein. Such inhibitors of viruses that use a class I fusion protein may be effective for treating, for example, respiratory infections by Respiratory Syncytial Virus (RSV). | 2011-01-13 |
20110009409 | DUAL-ACTING PYRAZOLE ANTIHYPERTENSIVE AGENTS - In one aspect, the invention relates to compounds having the formula: | 2011-01-13 |
20110009410 | APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS - The present invention relates to compounds of Formula (I): | 2011-01-13 |
20110009411 | THERAPEUTIC COMPOSITIONS AND THE USE THEREOF - The invention includes methods, compositions, and kits useful for treating a viral infection by coadministering 6-(3-chloro-2-fluorobenzyl)-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable salt thereof, with lopinavir or a pharmaceutically acceptable salt thereof. | 2011-01-13 |
20110009412 | MACROPHAGE MIGRATION INHIBITORY FACTOR ANTAGONISTS AND METHODS OF USING SAME - Methods of inhibiting one or more biological activities of Macrophage migration inhibitory factor (MIF) polypeptides are provided using an MIF inhibitory compound. The methods include therapeutic methods for treating cancers and inflammatory diseases. | 2011-01-13 |
20110009413 | CYCLIC TRIAZO AND DIAZO SODIUM CHANNEL BLOCKERS - Compounds of general structure in which X and Y are each N or C with at least one of X and Y being N; Z is a single bond or an optionally substituted linking group R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when RI is hydrogen or ═NH when R1 is a substituent group; or N* is a group NRaRb where Ra and Rb are independently H or an alkyl group; or N* is an optionally substituted piperazinyl ring; and A is an optionally substituted heterocyclic or carbocyclic ring system which may be linked to the triazo/diazo ring through R2 to form a fused multicyclic ring; are indicated as suitable for treatment of disorders in mammals that are susceptible to sodium channel blockers and antifolates, and particularly disorders such epilepsy, multiple sclerosis, glaucoma and uevitis, cerebral traumas and cerebral ischaemias, stroke, head injury, spinal cord injury, surgical trauma, neurodegenerative disorders, motorneurone disease, Alzheimer's disease, Parkinson's disease, chronic inflammatory pain, neuropathic pain, migraine, bipolar disorder, mood, anxiety and cognitive disorders, schizophrenia and trigeminal autonomic cephalalgias; for treatment of mammalian cancers; and for treatment of malaria. | 2011-01-13 |
20110009414 | HETEROCYCLIC DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS - Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise, for example, administering to a mammal in need thereof a compound of formula (II): | 2011-01-13 |
20110009415 | Thienopyridazine Compounds, Their Preparations, Pharmaceutical Compositions And Uses - The present invention relates to thienopyridazine compounds of formula (I), their pharmaceutically acceptable salts or hydrates, wherein R1 and R2 are independently H or C1-4 alkyl, R3 is a saturated or unsaturated 5- or 6-membered ring containing N, S or O, or its optical isomers, R4 is a halophenyl monosubstituted or disubstituted at any position. The present invention provides the preparation methods of these compounds, pharmaceutical compositions containing these compounds and the uses of these compounds, particularly in treating cancer. | 2011-01-13 |
20110009416 | PH INDEPENDENT FORMULATIONS OF 6-(5-CHLORO-2-PYRIDYL)-5-[(4-METHYL-1-PIPERAZINYL)CARBONYLOXY]-7-OXO-6,7-- DIHYDRO-5H-PYRROLO[3,4-b]PYRAZINE - Pharmaceutical compositions of zopiclone [(6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine)] that render the aqueous solubility/dissolution of the free base independent of the pH of the gastrointestinal tract are disclosed. The compositions are useful for oral administration. | 2011-01-13 |
20110009417 | PYRIDOPYRAZINONES DERIVATIVES INSULIN SECRETION STIMULATORS, METHODS FOR OBTAINING THEM AND USE THEREOF FOR THE TREATMENT OF DIABETES - The present invention relates to pyridopyrazinone derivatives of formula (I), wherein X, Y, Z, W, A and R1 are as defined in claim 1, as insulin secretion stimulators. The invention also relates to the preparation and use of these pyridopyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated. | 2011-01-13 |
20110009418 | THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN - The present invention discloses compounds of formula: | 2011-01-13 |
20110009419 | Enantiomers of 2'-Fluoralkyl-6-nitroquipazine as Serotonin Transporter Positron Emission Tomography Imaging Agents and Antidepressant Therapeutics - Racemic mixtures and individual enantiomers of fluorine-18 or carbon-11 radiolabelled 2′-alkyl-6-nitroquipazine ligands are serotonin transporter (SERT) tracers for positron emission tomography (PET) imaging. The non-radioactive ligand forms possess therapeutic antidepressant in vitro and in vivo pharmacological binding profiles in rodent brain and cells expressing human serotonin transporter (hSERT). Twelve 2′-alkyl-6-nitroquipazine ligands potently bind in sub-nanomolar concentrations to the pre-synaptic SERT binding site where established antidepressant drugs bind and inhibit the re-uptake of the neurotransmitter serotonin (5-HT). In vivo tracer studies in rats as well as monkey PET scan trial have demonstrated the fluorine-18 and carbon-11 positron radionuclide labeled tracers perform as quantitative tracers of specific binding the SERT protein in live brain. | 2011-01-13 |
20110009420 | Histamine H3 Receptor Ligands - The present invention provides compounds of the formula | 2011-01-13 |
20110009421 | COMPOUND HAVING 6-MEMBERED AROMATIC RING - An object of the present invention is to provide an agent for preventing or treating schizophrenia or the like, wherein the compound of the present invention has GPRS2 agonist activity. | 2011-01-13 |
20110009422 | 1- [2-(2,4-DIMETHYLPHENYLSULFANYL)-PHENYL] PIPERAZINE AS A COMPOUND WITH COMBINED SEROTONIN REUPTAKE, 5-HT3 AND 5-HT1A ACTIVITY FOR THE TREATMENT OF PAIN OR RESIDUAL SYMPTOMS IN DEPRESSION RELATING TO SLEEP AND COGNITION - The use of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine in the treatment of pain and residual symptoms in depression is provided. | 2011-01-13 |
20110009423 | PHENYL-PIPERAZINE DERIVATIVES AS SEROTONIN REUPTAKE INHIBITORS - The invention provides compounds represented by the general formula I | 2011-01-13 |
20110009424 | Co-Crystals and Pharmaceutical Compositions Comprising the same - The invention relates to co-crystals and compositions each comprising VX-950 and a co-crystal former selected from the group consisting of 3-methoxy-4-hydroxybenzoic acid, 2,4-dihydroxybenzoic acid, and 2,5-dihydroxybenzoic acid. Also within the scope of this invention are methods of making and using the same. | 2011-01-13 |
20110009425 | TETRAHYDROTHIENO PYRIDINES - The present invention relates to tetrahydrothienopyridine compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions. | 2011-01-13 |
20110009426 | 5,6-BISARYL-2-PYRIDINE-CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATION THEREOF AS UROTENSIN II RECEPTOR ANTAGONISTS - The present invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists. | 2011-01-13 |
20110009427 | ARYL PYRIMIDINE DERIVATIVES, PREPARATION METHODS AND PHARMACEUTICAL USES THEREOF - The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof. Various substituents in the formula (I) are as defined in the specification. The present invention also relates to a pharmaceutical composition comprising the compound of formula (I), the preparation method of compound of formula (I), and the use of the compound for the preparation of a medicament for treating and/or preventing human peroxisome proliferators activated receptor δ (hPPARδ)-associated diseases and risk factors. | 2011-01-13 |
20110009428 | NOVEL ANDROGENS - The compounds of the subject invention have a structure according to formula I: | 2011-01-13 |
20110009429 | HETEROCYCLIC COMPOUNDS AS INHIBITORS OF CXCR2 - The present invention relates to compounds of formula (I) | 2011-01-13 |
20110009430 | METHODS AND COMPOSITIONS FOR TREATING PAIN - The present application relates to compounds and methods for treating pain, incontinence and other conditions. | 2011-01-13 |
20110009431 | COMPOSITIONS AND METHODS FOR TREATING FIBROPROLIFERATIVE DISORDERS - The present invention relates, in general, to fibroproliferative disorders, and, in particular, to methods and compositions for treating fibroproliferative disorders by administering to a mammal in need of treatment pharmacologically effective doses of a phosphodiesterase inhibitor, such as pentoxifylline, and an anti-oxidant which is a precursor of glutathione, such as N-acetyl-cysteine, or their derivatives or metabolites. | 2011-01-13 |
20110009432 | PYRID-2YL FUSED HETEROCYCLIC COMPOUNDS, AND COMPOSITIONS AND USES THEREOF - Fused heterocyclic compounds are provided according to formula 1a or 1b: | 2011-01-13 |
20110009433 | BICYCLIC PYRROLE COMPOUND - Disclosed is a compound composed of an easily-handleable crystal form and having storage stability that is practical enough to be used as an active ingredient of a pharmaceutical product. Specifically disclosed is 6-[(3R)-3-aminopiperidin-1-yl]-5-(2-chloro-5-fluorobenzyl)-1,3-dimethyl-1H-pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione monohydro chloride hemihydrate. | 2011-01-13 |
20110009434 | CRYSTALS OF ISOPROPYL ESTER OF N-(2,6-DICHLOROBENZOYL)-4-[6-(METHYLAMINO)METHYL -1-METHYL-2,4-DIOXO-1,4-DIHYDROQUINAZOLINE-3(2H)-YL]-L- PHENYLALANINE HYDROCHLORIDE, PRODUCTION METHOD THEREOF AND USE THEREOF - Crystals of isopropyl ester of N-(2,6-dichlorobenzoyl)-4-[6-(methylamino)methyl-1-methyl-2,4-dioxo-1,4-dihydroquinazoline-3(2H)-yl]-L-phenylalanine hydrochloride are useful as α4 integrin inhibitors. | 2011-01-13 |
20110009435 | HETERO BICYCLIC CARBOXAMIDE DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS - The present invention relates to compounds of Formula I | 2011-01-13 |
20110009436 | NOVEL THERAPEUTIC USES OF ADRENERGIC ALPHA-1 RECEPTOR ANTAGONISTS - The disclosure relates to methods of using an adrenergic α-1 receptor antagonist or its pharmaceutically acceptable salts for treating and/or preventing interstitial cystitis, overactive bladder or detrusor overactivity. | 2011-01-13 |
20110009437 | CARBOXAMIDE-HETEROARYL DERIVATIVES FOR THE TREATMENT OF DIABETES - Novel heterocyclic compounds of the formula I | 2011-01-13 |
20110009438 | SUBSTITUTED ISOXAZOLINE COMPOUND AND PEST CONTROL AGENT - There is provided a novel pest control agent, particularly an insecticide or miticide. A substituted isoxazoline compound of General Formula (1): | 2011-01-13 |
20110009439 | INDENE DERIVATIVES AS PHARMACEUTICAL AGENTS - Compounds of formula (Ia): | 2011-01-13 |
20110009440 | GLYT1 TRANSPORTER INHIBITORS AND USES THEREOF IN TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS - Compounds of formula (I) or a salt thereof are provided: | 2011-01-13 |
20110009441 | IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS - The present invention relates to novel compounds, in particular novel imidazo[1,2-a]piridine derivatives according to Formula (I). The compounds according to the invention are positive allosteric modulators of metabotropic receptors-sub-type 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. | 2011-01-13 |
20110009442 | METHODS FOR STEREOSELECTIVE REDUCTION - The invention is directed to a method to reduce a C—C double bond of an enone of a steroidal compound to produce a mixture of β ketone product and α ketone product, comprising treating a solution or suspension of the steroidal compound in a solvent with hydrogen gas in the presence of a catalyst and a substituted pyridine. | 2011-01-13 |
20110009443 | Pyrazolospiroketone Acetyl-Coa Carboxylase Inhibitors - The invention provides compounds of Formula (1) or a pharmaceutically acceptable salt of said compound, wherein R | 2011-01-13 |
20110009444 | N-AZABICYCLIC CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - This disclosure relates to compounds of formula (I): | 2011-01-13 |
20110009445 | NEUROPROTECTANTS - Methods of protecting cells against cytotoxic insults are provided. The methods involve administering a composition including a CpG oligonucleotide to a subject. The methods are applicable to the protection of neural and non-neural cells. For example, methods of protecting a neural cell against excitotoxic brain injury are provided. Methods for preparing medicaments for the prophylactic treatment of excitotoxic injury, ischemia and/or hypoxia are also provided. Also provided are compositions for use in the described methods. | 2011-01-13 |
20110009446 | OLIGOMER-GUANIDINE CLASS CONJUGATES - The invention relates to (among other things) oligomer-guanidine class conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds. | 2011-01-13 |
20110009447 | Substituted Benzoic Acid Amides and Use thereof for the Inhibition of Angiogenesis - Substituted benzoic acid amides of formula (I) and their use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis as well as their intermediate products for the production of benzoic acid amides are described. | 2011-01-13 |
20110009448 | Compound - A compound having Formula I | 2011-01-13 |
20110009449 | N-ARYL-N-PIPERIDIN-4-YL-PROPIONAMIDE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - This invention relates to N-aryl-N-piperidin-4-yl-propionamide derivatives for use as monoamine neurotransmitter re-uptake inhibitors. | 2011-01-13 |
20110009450 | Crystalline form of benzothiophene compound and process for preparation thereof - Crystalline raloxifene hydrochloride in hydrated form, particularly the monohydrate, processes for its preparation, pharmaceutical compositions comprising it and uses thereof. | 2011-01-13 |
20110009451 | Controlled delivery system - The present invention relates to novel anesthetic compositions containing a non-polymeric carrier material and an anesthetic, where the compositions are suitable for providing a sustained local anesthesia without an initial burst and having a duration for about 24 hours or longer. Certain compositions are also provided that include a first anesthetic and a second anesthetic. In such compositions, the second anesthetic is a solvent for the first anesthetic and provides an initial anesthetic effect upon administration to a subject. The non-polymeric carrier may optionally be a high viscosity liquid carrier material such as a suitable sugar ester. The compositions can further include one or more additional ingredients including active and inactive materials. Methods of using the compositions of the invention to produce a sustained anesthetic effect at a site in a subject are also provided. Preferably the composition contains bupivacaine and a sugar ester such as saib. | 2011-01-13 |
20110009452 | HYDROXYALKANYL AMIDES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY - The application describes modulators of MIP-1α or CCR-1 of the formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein ring A, T, V, R | 2011-01-13 |
20110009453 | S1P3 RECEPTOR INHIBITORS FOR TREATING INFLAMMATION - Disclosed herein are compositions and methods for treating inflammation using S1 P3 receptor inhibitors. | 2011-01-13 |
20110009454 | COMPOSITION FOR AGRICULTURAL USE FOR CONTROLLING OR PREVENTING PLANT DISEASES CAUSED BY PLANT PATHOGENS - Disclosed is a composition for agricultural use, which is used for controlling or preventing plant diseases caused by plant pathogens. The composition for agricultural use contains a compound represented by formula (1), a salt thereof or a hydrate of the compound or the salt. (1) [In the formula, Z represents an oxygen atom, a sulfur atom or NR | 2011-01-13 |
20110009455 | 5-Oxo-2,3,4,5-tetrahydro-benzo[b]oxepine-4-carboxylic acid amides and 2,3-Dihydro-benzo[b]oxepine-4-carboxylic acid amides for treatment and prevention of Diabetes Typ 1 and 2 - The present invention relates to novel compounds of general formula (I) | 2011-01-13 |
20110009456 | Compounds, Compositions and Methods for Treatment and Prevention of Orthopoxvirus Infections and Associated Diseases - Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus. | 2011-01-13 |
20110009457 | Aminobenzamide Derivatives as Useful Agents for Controlling Animal Parasistes - The invention relates to a composition comprising at least one aminobenzamide compound or a salt thereof for controlling animal parasites, veterinary pharmaceutical compositions comprising at least one aminobenzamide of formula (I) for preventing infection with diseases transmitted through parasites, its use for the preparation of a veterinary pharmaceutical for controlling animal parasites, and a method for preventing infection with diseases transmitted through parasites. | 2011-01-13 |
20110009458 | STABLE FORMULATIONS OF THIADIAZOLE DERIVATIVE - The present invention provides formulation parameters and manufacturing conditions for stable pharmaceutical compositions comprising N-{4-(2,2-dimethyl-propionyl)-(5R)-5-[(2-ethylamino-ethanesulfonylamino)-methyl]-5-phenyl-4,5-dihydro-[1,3,4]thiadiazol-2-yl}-2,2-dimethyl-propionamide that minimize undesirable chiral conversion to the less active S enantiomeric form. | 2011-01-13 |
20110009459 | EPOTHILONE DERIVATIVES - Epothilone derivatives of Formula (I) and their use as a pharmaceutical. | 2011-01-13 |
20110009460 | COMPOSITIONS AND METHODS FOR TREATING AMYOTROPHIC LATERAL SCLEROSIS - Pharmaceutical compositions of dexpramipexole and methods of using such compositions for the treatment of ALS are disclosed. | 2011-01-13 |
20110009461 | 2-AZA-BICYCLO[3.3.0]OCTANE DERIVATIVES - The invention relates to 2-aza-bicyclo[3.3.0]octane derivatives of Formula (I) wherein A, B, and R | 2011-01-13 |
20110009462 | STABLE, SYNERGISTIC MIXTURES - The present invention relates to storage-stable, synergistically acting combinations comprising glutaraldehyde (GDA) and 2-methyl-2H-isothiazol-3-one (methylisothiazolinone, MIT) and, where appropriate, 2-bromo-2-nitropropane-1,3-diol (bronopol) and/or other active substances for protecting industrials materials. | 2011-01-13 |
20110009463 | GERANYLGERANYL TRANSFERASE INHIBITORS AND METHODS OF MAKING AND USING THE SAME - The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylation in an organism using the same. | 2011-01-13 |
20110009464 | IMMUNE SYSTEM STIMULATION BY LIGHT THERAPY INDUCED APOPTOTIC CELL DEATH IN ABNORMAL TISSUE - The efficacy of light activated therapy treatment is enhanced by stimulating the immune system of the patient substantially above the pre-therapy level. Abnormal tissue that is destroyed by the light activated therapy releases factors that stimulate the immune system, leading to systemic reductions in abnormal tissue (i.e., reduction beyond the area treated using light), so long as the light therapy conditions favor apoptosis over necrosis. The volume of abnormal tissue destroyed is maximized to the extent possible, reducing tumor load, which reduces an amount of immunosuppressive factors in the body, enabling stimulation of the immune system to be successful. | 2011-01-13 |
20110009465 | 3-PHENOXYMETHYLPYRROLIDINE COMPOUNDS - In one aspect, the invention relates to compounds of formula I: | 2011-01-13 |
20110009466 | METHODS OF INCREASING GENE EXPRESSION THROUGH RNA PROTECTION - This invention relates to the use of one or more RNA target protectors to inhibit the binding of an RNA, e.g., small RNA, to a target RNA (e.g., a target mRNA), thus increasing the stability of the target RNA and its function (e.g., increasing the gene expression of the gene corresponding to a target mRNA). An RNA target protector may be, for example, an oligonucleotide, e.g., a morpholino, or a small molecule. The invention further relates to the treatment of a human patient in need thereof with one or more RNA target protectors. | 2011-01-13 |
20110009467 | Methods to Increase or Decrease Bone Density - The SOST gene gives rise to sclerostin, a protein that leads to apoptosis of bone progenitor cells. The invention provides antagonists to the sclerostin protein, and methods for identifying new sclerostin antagonists. The invention also provides molecules that can depress expression of the SOST gene, as well as methods for identifying such molecules. Such molecules and antagonists are useful for increasing bone mineralization in mammals, for example, in the treatment of osteoporosis. | 2011-01-13 |
20110009468 | MIRNA, SIRNA AND USE THEREOF IN THERAPY - The present invention relates to a mixture of molecules comprising at least one miRNA and at least one siRNA, or at least two miRNAs, or at least two siRNAs for inducing hematopoietic differentiation or for treating leukemia wherein the miRNA is able to modulate hematopoietic differentiation and/or to act as oncosuppressor, and the siRNA is able to modulate hematopoietic differentiation or to inhibit the expression of a fusion product deriving from a chromosomic translocation associated to leukemia. | 2011-01-13 |
20110009469 | COMPOSITIONS AND METHODS OF TREATING NEOPLASIA - The present invention provides compositions and methods featuring microRNA polynucleotides for the diagnosis, treatment or prevention of neoplasia. | 2011-01-13 |
20110009470 | Nucleic acid external skin formulation - The present invention provides a nucleic acid external skin formulation having a high skin permeability and which is prepared from a polymeric nucleic acid having a high molecular weight and sodium alginate. The nucleic acid external skin formulation is highly skin permeable and delivers its active ingredient nucleic acid to the affected area efficiently. The nucleic acid used may be smaller in amount, and thus, the formulation is also superior in safety and cost. The working mechanism thereof is different from that of the low-molecular weight compounds currently used as an active ingredient for skin anti-inflammatory agents, and thus, the formulation may be applicable to cases where such low-molecular weight medicines are less effective. | 2011-01-13 |