| 27th week of 2013 patent applcation highlights part 51 |
| Patent application number | Title | Published |
|---|
| 20130172288 | Process for the simultaneous substitution and crosslinking of a polysaccharide via its hydroxyl functional groups - A process for the simultaneous substitution and crosslinking of a polysaccharide via its hydroxyl functional groups, in an aqueous phase, which includes the following steps:
| 2013-07-04 |
| 20130172289 | METHOD FOR THE PREPARATION OF SODIUM CHONDROITIN SULPHATE - The present invention concerns a method for obtaining sodium chondroitin sulphate from cartilage, notably of avian origin, as well as a sodium chondroitin sulphate preparation. | 2013-07-04 |
| 20130172290 | TREATMENT OF POLYSACCARIDES WITH DIALDEHYDES - A process for treating a polysaccharide with a dialdehyde in the presence of from 10 to 40 weight percent of water, based on the total weight of polysaccharide and water, is beneficially conducted in a mixing device characterized by a FROUDE number FR | 2013-07-04 |
| 20130172291 | RETINAL CYCLODEXTRIN ACETALS AND HEMIACETALS FOR TREATING SKIN COMPLEXION DISORDER - The present invention discloses certain polyene cyclodextrin acetals and hemiacetals that are effective in providing skin clarification, which is useful for the treatment of acne, and skin disfigurements and skin darkening resulting from acne; skin darkening from cancer, diabetes, radiation treatments, chemotherapy, and sun-burn; mitochondrial and DNA dysfunction; age spots; loss of cellular antioxidants; skin changes associated with aging including collagen loss, loss of skin pliability, loss of skin suppleness, skin wrinkles and fine lines, oxidation, damage from radiation, damage from free radicals, and damage from UV; dry skin; xerosis; ichthyosis; dandruff; brownish spots; keratoses; melasma; lentigines; liver spots; skin pigmentation including pigmented spots, dark circles under the eyes, darkened skin, and blemishes; oily skin; warts; eczema; pruritic skin; psoriasis; inflammatory dermatoses; topical inflammation; disturbed keratinization; scalp dryness, and combinations thereof. | 2013-07-04 |
| 20130172292 | FUSED HETEROCYCLIC COMPOUNDS - The present invention provides a compound which has the effect of PDE 10A inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound represented by the formula (1′): wherein, Ring A′ represents an optionally substituted pyridine ring, an optionally substituted pyridazine ring, a pyrimidine ring, or 10 a pyrazine ring, R1′ represents (1) wherein, R | 2013-07-04 |
| 20130172293 | DRUG AGAINST CENTRAL NERVOUS SYSTEM INFLAMMATION - An objective of the present invention is to provide a novel method with an effect of alleviating central nervous system inflammation. The present invention provides a drug against central nervous system inflammation containing a plasmalogen. More preferably, the present invention provides a drug against central nervous system inflammation containing a plasmalogen extracted from a biological tissue (preferably an avian tissue) that mainly contains an ethanolamine plasmalogen and a choline plasmalogen. | 2013-07-04 |
| 20130172294 | Treatment with VB-201 - Unit dosage forms comprising between 1 mg and 100 mg VB-201 and a pharmaceutically acceptable carrier, and formulated for oral administration, are disclosed herein, as well as treatment regimens comprising oral administration of VB-201 once or twice daily for treating an inflammatory disease or disorder. | 2013-07-04 |
| 20130172295 | PROCESS FOR PREPARATION OF HIV PROTEASE INHIBITORS - A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed | 2013-07-04 |
| 20130172296 | METHOD OF ACTIVATION OF OXAZAPHOSPHORINES - The present invention provides a method of hydroxylating or oxidizing a compound of interest in a subject (e.g., a cytotoxic oxazaphosphorine prodrug), by administering the compound of interest to the subject; and concurrently administering the subject a metalloporphyrin in an amount effective to hydroxylate or oxidize the compound of interest in the subject. | 2013-07-04 |
| 20130172297 | Treatment of Autoimmune Diseases - Disclosed is the use of a compound of formula I wherein X is O, S, SO or SO | 2013-07-04 |
| 20130172298 | Okadaella Gastrococcus and Cancer - The present invention provides compositions, methods of manufacture, process and uses for diagnosing, preventing, inhibiting, and treating the development and proliferation of diseases and disorders associated with | 2013-07-04 |
| 20130172299 | Combination Therapy for Treatment of Bone and Mineral Disorders for Patients with Impaired Renal Function - The field of the present invention relates to novel and improved therapies for treatment of complications associated with impaired renal function. More specifically, the present invention relates to evaluating the effects of a novel renal multivitamin on Vitamin D levels, EPO dose, inflammatory (e.g., C-reactive protein) and other biomarkers in an end stage renal disease (ESRD) population on hemodialysis (HD). | 2013-07-04 |
| 20130172300 | NEW HORMONAL COMPOSITION AND ITS USE - A method of preventing estrogen deficiencies and osteoporosis in menopausal women by continuously orally administering without interruption to menopausal women in need thereof an amount of 0.3 to 3 mg of 17β-estradiol or esters thereof and 0.3 to 1.25 mg of nomegestrol or esters thereof in an amount sufficient to prevent said problems. | 2013-07-04 |
| 20130172301 | BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS - This invention provides compounds of formula I: | 2013-07-04 |
| 20130172302 | QUINUCLIDINE ESTERS OF 1-AZAHETEROCYCLYLACETIC ACID AS ANTIMUSCARINIC AGENTS, PROCESS FOR THEIR PREPARATION AND MEDICINAL COMPOSITIONS THEREOF - Compounds of formula (I): | 2013-07-04 |
| 20130172303 | ROFLUMILAST COMPOSITIONS FOR THE TREATMENT OF COPD - The present invention relates to pharmaceutical compositions comprising roflumilast in combination with a corticosteroid and/or a leukotriene receptor antagonist. The invention also relates to the use of such compositions for the treatment of Chronic Obstructive Pulmonary Disorder (COPD). | 2013-07-04 |
| 20130172305 | Acute Treatment of Social Phobia - Methods and compositions for the treatment of social phobia are provided, including administering a therapeutically effective amount of an androsta-4,16-dien-3-ol steroid to an individual in need of treatment and a pharmaceutical composition for the treatment of social phobia having a therapeutically effective amount of an androsta-4,16-dien-3-ol steroid. Therapeutically effective amounts may be, for example, between about 100 picograms and about 100 micrograms, or between about 1 nanogram and about 10 microgram, or between about 10 nanograms and about 1 microgram of an androsta-4,16-dien-3-ol steroid. Administration of the androsta-4,16-dien-3-ol compound is preferably intranasal administration to the nasal passages and the vomeronasal organ of the individual. A preferred androsta-4,16-dien-3-ol steroid is [3β]-androsta-4,16-dien-3-ol. In some embodiments of the methods, both [3β}-androsta-4,16-dien-3-ol and [3α]-androsta-4,16-dien-3-ol are administered to a patient, and are included in a pharmaceutical composition for the treatment of social phobia. | 2013-07-04 |
| 20130172306 | USE OF AN ESTROGEN DERIVATIVE FOR THE MANUFACTURE OF PHARMACEUTICAL COMPOSITIONS USEFUL FOR THE TREATMENT AND/OR PREVENTION OF PSYCHIATRIC DISEASES AND FOR THE TREATMENT AND PREVENTION OF SAID DISEASES - The object of the invention is the use of 17-alpha-estradiol of formula (I) and its derivatives for the treatment and/or prevention of psychiatric clinical pictures. According to the invention, 17-alpha-estradiol and its derivatives can be used preferably as antidepressant drugs, especially preferably as quick-acting antidepressant drugs. According to the invention, 17-alpha-estradiol of formula (I) and its derivatives can also be used for the treatment and/or prevention of postpartum depression, post-menopausal depression, anxiety, schizophrenia, memory disturbance associated with depression or bipolar depression. | 2013-07-04 |
| 20130172307 | 5a-ANDROSTANE (ALKYL)-3b, 5, 6b-TRIOL INJECTION AND PREPARATION METHOD THEREFOR - A 5α-androstane-3β,5,6β-triol injection and its preparation are disclosed. The injection uses hydroxypropyl-β-cyclodextrin as a solubilizing agent and the active ingredient is present at a weight ratio of 1-20:40-500 to the hydroxypropyl-β-cyclodextrin. The injection may also comprise, by weight, 1-100 parts of at least one isotonic adjusting agent, 0-200 parts of at least one freeze drying filler, and 0-2000 parts of at least one solvent. The preparation method comprises dissolving hydroxypropyl-β-cyclodextrin solution, 5α-androstane-3β,5,6β-triol and at least one additional soluble excipient in water for injection in sequence to obtain a raw injection solution, and subjecting the raw injection solution to decolorization, depyrogenation, filtration and sterilization to obtain the injection, Drying the filtrate yields a solid for injection. | 2013-07-04 |
| 20130172308 | ANTIMICROBIAL AGENTS - The present invention relates to ruthenium complexes, and in particular di- and multi-nuclear ruthenium complexes which may be used as antimicrobial agents. The invention also relates to pharmaceutical compositions comprising such complexes, and methods for their use in treating or preventing microbial infections. | 2013-07-04 |
| 20130172309 | COMPOSITIONS AND METHODS FOR THE IDENTIFICATION OF A CARBAPANEMASE GENE - Compositions and methods for the rapid and sensitive detection of a carbapenemase in a sample are provided. The compositions include novel primer and probe compositions for use in detecting the presence of this enzyme in a sample, particularly using PCR methods. These primers and probe sets can be used in amplification methods (such as PCR, particularly quantitative PCR) and packaged into kits for use in amplification methods for the purpose of detecting carbapenemase in a test sample, particularly a patient sample, particularly a direct sample. Thus, in one embodiment, the present invention provides for novel oligonucleotide primers set forth in SEQ ID NOs:1, 2, 4, 5, 7, 8, 14, 15, 17, 18, and 20, and the novel oligonucleotide probe sequences set forth in SEQ ID NOs:3, 6, 9, 16, and 19. These sequences can be used in a method of detecting carbapenemase in a sample. | 2013-07-04 |
| 20130172310 | BENZAMIDES AND RELATED INHIBITORS OF FACTOR XA - Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders. | 2013-07-04 |
| 20130172311 | Substituted heterocyclyl benzyl pyrazoles, and use thereof - The present application relates to novel substituted 1-[3-(heterocyclyl)benzyl]-1H-pyrazole derivatives, to processes for preparation thereof, to use thereof for treatment and/or prevention of diseases and to use thereof for production of medicaments for treatment and/or prevention of diseases, more particularly for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures. | 2013-07-04 |
| 20130172312 | Azetidine Derivatives - Azetidine derivatives of which the following is exemplary | 2013-07-04 |
| 20130172313 | Carbapenem Antibacterials with Gram-Negative Activity - The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. | 2013-07-04 |
| 20130172314 | PYRAZOLO[3,4-d]PYRIMIDINE AND PYRROLO[2,3-d]PYRIMIDINE COMPOUNDS AS KINASE INHIBITORS - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 2013-07-04 |
| 20130172315 | SUBSTITUTED ANILINES AS CCR(4) ANTAGONISTS - Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer. | 2013-07-04 |
| 20130172316 | New azetidine derivatives, pharmaceutical compositions and uses thereof - The invention relates to new azetidine derivatives of the formula I | 2013-07-04 |
| 20130172317 | TRIAZINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION HAVING AN ANALGESIC ACTIVITY COMPRISING THE SAME - The present invention provides novel compounds having a P2X | 2013-07-04 |
| 20130172318 | ANTI-INFLAMMATORY AGENTS - Disclosed herein are methods of preventing or treating inflammatory diseases using 3-aminolactam compounds, each with aromatic “tail groups”. Compounds as defined by formulae (I) and (I′), and the medical uses of the compounds, are described herein. | 2013-07-04 |
| 20130172319 | Alpha-AminoCycloLactam Ligands for G-Protein Coupled Receptors, and Methods of Using Same - The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs). | 2013-07-04 |
| 20130172320 | PYRIDO [4,3-B] INDOLE AND PYRIDO [3,4-B] INDOLE DERIVATIVES AND METHODS OF USE - This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 2013-07-04 |
| 20130172321 | Compositions Comprising Nicotinic Agonists and Methods of Using Same - The disclosure is directed at least in part to compositions and methods comprising nicotinic agonists for treating e.g., nervous system disorders, in particular, to combination therapies that include a nicotinic agonist (for example, nicotine) and a nicotinic acetylcholine receptor desensitization inhibitor (for example, opipramol). | 2013-07-04 |
| 20130172322 | BENZAZEPINE DERIVATIVES USEFUL FOR TREATMENT OF 5HT2C RECEPTOR ASSOCIATED DISEASES - The present invention relates to certain 1-substituted-2,3,4,5-tetrahydro-3-benzazepine derivatives of Formula (I), that are modulators of the 5HT2C receptor. Accordingly, compounds of the present invention are useful for the prophylaxis or treatment of 5HT2C receptor associated diseases, conditions or disorders, such as, obesity and related disorders. | 2013-07-04 |
| 20130172323 | PYRIDAZINONES AS GPR119 AGONISTS - The present invention relates to pyridazinone derivatives of general formula I, wherein the groups A, G and R | 2013-07-04 |
| 20130172324 | METHOD FOR TREATING CARDIOVASCULAR DISEASES USING RHO KINASE INHIBITOR COMPOUNDS - This invention is directed to methods of preventing or treating diseases or conditions associated with excessive cell proliferation, remodeling, inflammation, and vasoconstriction. Particularly, this invention is directed to methods of treating cardiovascular diseases or conditions such as stent restenosis and thrombosis, vascular thrombosis, cerebral vasospasm, atherosclerosis, systemic hypertension, cardiac hypertrophy, and sexual dysfunction. The method comprises identifying a subject in need of the treatment, and administering to the subject an effective amount of a novel Rho kinase inhibitor compound to treat the disease. | 2013-07-04 |
| 20130172325 | NOVEL HOMOPIPERAZINE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS AND PHARMACEUTICAL USE THEREOF - The invention relates to compounds of general formula (I) wherein R | 2013-07-04 |
| 20130172326 | DERIVATIVES OF HETEROARYLSULFONAMIDES, THEIR PREPARATION AND THEIR APPLICATION IN HUMAN THERAPY - The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C | 2013-07-04 |
| 20130172327 | SUBSTITUTED N- [1-CYANO-2- (PHENYL) ETHYL] -2-AZABICYCLO [2.2.1] HEPTANE-3-CARBOXAMIDE INHIBITORS OF CATHEPSIN C - Disclosed are N-1-cyano-2-(phenyl)ethyl)-2-azabicyclo[2.2.1]heptane-3-carboxamides of formula I | 2013-07-04 |
| 20130172328 | FUSED HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASES (PDES) INHIBITORS - The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I): | 2013-07-04 |
| 20130172329 | NOVEL SOLID FORMS - The instant invention relates to novel solid forms of the compound of formula (I) | 2013-07-04 |
| 20130172330 | Chemokine Receptor Modulators - The invention provides compounds of Formula (I) | 2013-07-04 |
| 20130172331 | NOVEL OXAZINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE - The invention relates to novel oxazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, | 2013-07-04 |
| 20130172332 | COMPOSITIONS AND METHODS FOR BONE FORMATION AND MODELING - The present disclosure is directed to methods of identifying a compound that binds to or interacts with a protein receptor involved in bone formation. Specifically, the disclosure is directed to methods of identifying a compound that regulates a Wnt pathway in a cell by binding to or interacting with cavities in proteins such as LRP5, LRP 6 and/or frizzled receptor and interfering with receptor binding to other proteins in a Wnt pathway. The present disclosure is further directed to methods and compositions that comprise an identified compound for treating or preventing a disease in a mammal in which Wnt pathway suppression plays a role. | 2013-07-04 |
| 20130172333 | FORMULATION AND DOSING OF HSP90 INHIBITORY COMPOUNDS - Provided is a pharmaceutical composition comprising a pharmaceutically acceptable organic solvent, a pharmaceutically acceptable surfactant, and a compound according to the following formula: wherein the variables are defined herein. Optionally, the pharmaceutical composition further comprises a co-solvent. Also provided is a method of using the pharmaceutical composition disclosed herein for the treatment of a patient in need thereof. | 2013-07-04 |
| 20130172334 | TRPV1 ANTAGONISTS - Disclosed herein are compounds of formula (I): | 2013-07-04 |
| 20130172335 | 2,3-DIARYL- OR HETEROARYL-SUBSTITUTED 1,1,1-TRIFLUORO-2-HYDROXYPROPYL COMPOUNDS - The present invention relates to compounds of formula I | 2013-07-04 |
| 20130172336 | 4-ANILINOFURO[2,3-B]QUINOLINE DERIVATIVES, THEIR PREPARATION PROCESSES, AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME - Disclosed herein are novel 4-anilinofuro[2,3-b]quinoline derivatives of formula (I): | 2013-07-04 |
| 20130172337 | Imidazo[4,5-c]quinolines as DNA-PK inhibitors - The invention relates to compounds of the formulae (I) and (II) in which R1, R2, R3, R4, R5, R8, X and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I). | 2013-07-04 |
| 20130172338 | OXYGEN LINKED PYRIMIDINE DERIVATIVES - The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine 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 kinases. | 2013-07-04 |
| 20130172339 | SULFONAMIDE COMPOUNDS - A compound of formula (I), wherein A is S, O or a double bond, and L is a substituted thiazolyl, phenyl or pyridyl. The compound is useful for the treatment of inflammation and cancer. | 2013-07-04 |
| 20130172340 | SUBSTITUTED 2-(9H-PURIN-9-YL) ACETIC ACID ANALOGUES AS INHIBITORS OF STAT3 - In one aspect, the invention relates to substituted purine analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2013-07-04 |
| 20130172341 | FUSED PYRAZOLE DERIVATIVES AS NOVEL ERK INHIBITORS - Disclosed are the ERK inhibitors of Formula (I): (Formula (I)) and the pharmaceutically acceptable salts thereof. All substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of Formula (I). | 2013-07-04 |
| 20130172342 | BENZIMIDAZOLE DERIVATIVES AS SELECTIVE BLOCKERS OF PERSISTENT SODIUM CURRENT - The present invention is directed to methods of treating diseases or conditions mediated by elevated persistent sodium channel, such as ocular disorders, pain, multiple sclerosis, and seizure disorders utilizing a compound of Formula I | 2013-07-04 |
| 20130172343 | Derivatives of 1H-isoindol-3-amine, 1H-iso-aza-indol-3amine, 3,4-dihydroisoquinolin-1-amine, and 1,4-dihydroisoquinolin-3-amine as Beta-secretase Inhibitors - 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: (I). In another embodiment, the compounds have a general Formula II: (II). In another embodiment, the compounds have a general Formula III: (III). Variables A | 2013-07-04 |
| 20130172344 | 4-OXOQUINOLINE COMPOUND AND USE THEREOF AS HIV INTEGRASE INHIBITOR - An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I] | 2013-07-04 |
| 20130172345 | 1-ACYL-4-(PHENOXY, BENZYLOXY, OR PHENYLAMINO)-1,2,3,4-TETRAHYDROQUINOLINE DERIVATIVES - Disclosed is a low-molecular-weight compound having an EPO production-promoting activity and/or a hemoglobin expression-enhancing activity. Specifically disclosed is an EPO production promoter and/or a hemoglobin expression enhancer comprising a 1-acyl-4-(phenoxy, benzyloxy or phenylamino)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by the general formula (1); | 2013-07-04 |
| 20130172346 | USE OF KYNURENIC ACID AMIDE DERIVATIVES FOR THE TREATMENT OF HUNTINGTON'S DISEASE - The invention is directed to kynurenic acid analogues and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing said compounds for treating the symptoms of Huntington's disease and preventing the development of the symptoms. | 2013-07-04 |
| 20130172347 | 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. | 2013-07-04 |
| 20130172348 | NOVEL AND SELECTIVE CCR2 ANTAGONISTS - The present invention relates to novel and selective antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD as well as pain. | 2013-07-04 |
| 20130172349 | INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE - Compounds of formula I | 2013-07-04 |
| 20130172350 | PYRIMIDINE COMPOUNDS AND THEIR USES - Pyrimidine compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof, are useful are useful as PDE4 inhibitors and are useful for treating PDE4 mediated diseases and in the treatment of immunological diseases, inflammation, pain disorder, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; atherosclerosis; cancer; cachexia; ischemic-induced cell damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; ARDS; psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; asthma; COPD; bone resorption diseases; multiple sclerosis; sepsis; septic shock; toxic shock syndrome and fever. | 2013-07-04 |
| 20130172351 | Dihydropyrazoles - Novel dihydropyrazole derivatives of formula (I) | 2013-07-04 |
| 20130172352 | 5-MEMBERED HETEROCYCLE-BASED P38 KINASE INHIBITORS - Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38α, and p38β kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders. | 2013-07-04 |
| 20130172353 | 3-PHENYL-5-UREIDOISOTHIAZOLE-4-CARBOXIMIDE AND 3-AMINO-5-PHENYLISOTHIAZOLE DERIVATIVES AS KINASE INHIBITORS - This invention is directed to a compound of Formula I | 2013-07-04 |
| 20130172354 | HETEROARYL COMPOUNDS AND THEIR USES - The present invention provides a compound of formula (I): | 2013-07-04 |
| 20130172355 | SULFUR-CONTAINING COMPOUND, METHOD OF PREPARATION AND PHARMACEUTICAL USES THEREOF - The invention relates to a sulfur-containing compound and the preparation thereof. The invention also relates to the uses of the sulfur-containing compound in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2. This invention also describes a series of chemical analogues of the said sulfur-containing compound and the preparation of these compounds. | 2013-07-04 |
| 20130172356 | COMBINATION OF EGCG OR METHYLATED EGCG AND A PDE INHIBITOR - Disclosed is a medicament characterized by the combination of: epigallocatechin gallate, methylated epigallocatechin gallate, or a pharmacologically permitted salt thereof; and a phosphodiesterase inhibitor. | 2013-07-04 |
| 20130172357 | Compositions and Methods for Treatment of Glaucoma - The invention provides α-2 adrenergic receptor agonist compositions and methods for treating glaucoma and other intraocular conditions. The preferred α-2 agonist used in the inventive compositions and methods is dexmedetomidine. | 2013-07-04 |
| 20130172358 | Compounds, Formulations, and Methods for Treating or Preventing Inflammatory Skin Disorders - In methods, compounds, and topical formulations for treatment of inflammatory skin disorders incorporating compounds represented by the formulas below: | 2013-07-04 |
| 20130172359 | Compounds, Formulations, and Methods for Treating or Preventing Inflammatory Skin Disorders - In methods, compounds, and topical formulations for treatment of inflammatory skin disorders incorporating compounds represented by the formulas below: | 2013-07-04 |
| 20130172360 | DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE AS MEDICAMENT - The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same. | 2013-07-04 |
| 20130172361 | ASSAYS AND METHODS FOR SELECTING A TREATMENT REGIMEN FOR A SUBJECT WITH DEPRESSION - Disclosed herein are novel assays, systems and kits for selecting a treatment regimen for a subject with depression by identifying at least one nucleic acid polymorphism, e.g., but not limited to, at the MTHFR, MTR, or MTRR locus, and/or determining expression levels of peripheral biomarkers (e.g., SAM, SAH, and 4-HNE) in a test sample from a human subject. These biomarkers can be used to determine the effectiveness of treating a depressed subject with a folate-containing compound (alone or as an adjunct to an antidepressant). Additionally, these biomarkers can be used to select an appropriate treatment regimen for subjects with treatment-resistant depression (e.g., resistant to at least one selective serotonin reuptake inhibitor). Methods and compositions for treating a subject with depression and/or determining or improving the effectiveness of an antidepressant drug taken by a subject are also provided herein. | 2013-07-04 |
| 20130172362 | Imidazothiazole Derivatives Having Proline Ring Structure - Compounds that inhibit interaction between murine double minute 2 (Mdm2) protein and p53 protein and that exhibit anti-tumor activity are provided. Compounds provided by the present disclosure include imidazothiazole derivatives that inhibit interaction between Mdm2 protein and p53 protein and exhibit anti-tumor activity. | 2013-07-04 |
| 20130172363 | NOVEL BENZENESULFONAMIDE COMPOUNDS, METHOD FOR SYNTHESIZING SAME, AND USE THEREOF IN MEDICINE AS WELL AS IN COSMETICS - Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions. | 2013-07-04 |
| 20130172364 | PROPARGYL-TRIFLUOROMETHOXY-AMINOBENZOTHIAZOLE DERIVATIVES, THEIR PREPARATION AND USE - Disclosed are novel derivatives of propargyl-trifluoromethoxy-amino-benzothiazole which are effective in treating neurologic disorders, including Parkinson's disease and multiple sclerosis. | 2013-07-04 |
| 20130172365 | ARYLOSULFONAMIDES FOR THE TREATMENT OF CNS DISEASES - Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system. | 2013-07-04 |
| 20130172366 | BRIDGED HETEROCYCLIC COMPOUNDS AND METHODS OF USE - This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 2013-07-04 |
| 20130172367 | 2-Alkyl-Cycloalk(en)yl-Carboxamides | 2013-07-04 |
| 20130172368 | Methods for Treating Hyperuricemia in Patients with Gout Using Halofenate or Halogenic Acid and A Second Urate-Lowering Agent - Disclosed herein are pharmaceutical compositions, methods and kits for lowering the serum uric acid level of a subject and for the treatment of a condition associated with elevated serum uric acid levels comprising administering a composition comprising a first urate-lowering agent and a second urate-lowering agent. In some aspects the first urate-lowering agent is (−)-halofenate, (−)-halofenic acid, or a pharmaceutically acceptable salts thereof. In some aspects the second urate-lowering agent is an inhibitor of uric acid production, a uricosuric agent, a uricase, or a pharmaceutically acceptable salt thereof. | 2013-07-04 |
| 20130172369 | PROCESSES FOR THE PREPARATION OF DIPYRIDAMOLE - The present invention relates to the active pharmaceutical ingredient dipyridamole. In particular, it relates to efficient processes for the preparation of dipyridamole which are amenable to large scale commercial production and provide the required product with improved yield and purity. The present invention also relates to a novel crystallization method for the purification of dipyridamole. | 2013-07-04 |
| 20130172370 | PHARMACEUTICAL COMPOSITION FOR USE IN THE TREATMENT OF GLAUCOMA - The present invention relates to a compound which is an antagonist of CXCR3 or an inhibitor of the CXCR3 receptor expression for the treatment of glaucoma. | 2013-07-04 |
| 20130172371 | Methods of Treating Cancer Using Pyridopyrimidinone Inhibitors of PI3K and mTOR in Combination with Autophagy Inhibitors - The invention provides compounds of Formula I: | 2013-07-04 |
| 20130172372 | RING-FUSED 4-AMINOPYRIMIDINES AND USE THEREOF AS STIMULATORS OF SOLUABLE GUANYLATE CYCLASES - The present application relates to novel fused 4-aminopyrimidines, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for the treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders. | 2013-07-04 |
| 20130172373 | QUINAZOLINE COMPOUNDS - Provided are certain quinazoline compounds, compositions thereof and methods of use thereof. These quinazoline compounds can effectively inhibit the overexpression and/or overactivity of epidermal growth factor receptor (EGFR). | 2013-07-04 |
| 20130172374 | SOLID COMPOSITION FOR CONTROLLED RELEASE OF IONIZABLE ACTIVE AGENTS WITH POOR AQUEOUS SOLUBILITY AT LOW PH AND METHODS OF USE THEREOF - A novel solid composition and methods for making and using the solid composition are provided. The solid composition comprises: (a) at least one active agent with a solubility of less than about 0.3 mg/ml in an aqueous solution with a pH of at most about 6.8 at a temperature of about 37° C.; and (b) a hydrophilic polymer matrix composition comprising: i) a hydrophilic polymer selected from the group consisting of METHOCEL™, POLYOX™ WSR 1105 and combinations thereof; and optionally ii) a hydrophobic polymer selected from the group consisting of Ethocel 20 premium; and (c) an alkalizer selected from the group consisting of calcium carbonate, magnesium oxide heavy and sodium bicarbonate; wherein the composition provides at least about 70% release of the active between about 7 to about 12 hours following oral administration. | 2013-07-04 |
| 20130172375 | PHARMACEUTICAL COMPOSITION - The present invention relates to a pharmaceutical composition comprising a solid dispersion of a drug. In the composition, the drug is in substantially amorphous form. | 2013-07-04 |
| 20130172376 | SOLID DOSAGE FORMS OF (S)-ETHYL 2-AMINO-3-(4-(2-AMINO-6-((R)-1-(4-CHLORO-2-(3-METHYL-1H-PYRAZOL-1-YL)PHEN- YL)-2,2,2-TRIFLUOROETHOXY)PYRIMIDIN-4-YL)PHENYL)PROPANOATE - Solid pharmaceutical dosage forms comprising (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate (telotristat) are disclosed, as well as methods of making them and compositions useful in their manufacture. | 2013-07-04 |
| 20130172377 | ADMINISTRATION OF DIPEPTIDYL PEPTIDASE INHIBITORS - Pharmaceutical compositions and methods comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile or a pharmaceutically acceptable salt thereof administered once weekly. | 2013-07-04 |
| 20130172378 | Combination of BRAF and VEGF Inhibitors - A novel combination comprising the VEGFR inhibitor 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, with a B-Raf inhibitor, particularly N-(3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl)-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of VEGFR and/or B-Raf is beneficial. | 2013-07-04 |
| 20130172379 | Combined Acetylcholinesterase Inhibitor and Quaternary Ammonium Antimuscarinic Therapy to Alter Progression of Cognitive Diseases - A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression. In one preferred embodiment, the disease is dementia with Lewy Bodies. New formulations for quaternary ammonium anti-cholinergic muscarinic receptor antagonists are also disclosed. | 2013-07-04 |
| 20130172380 | METHOD OF RESTORING THE INCRETIN EFFECT - The present invention relates to methods of treating metabolic syndrome, Type 2 diabetes mellitus, atherogenic dyslipidemia and/or obesity. The present invention also relates to methods of restoring the incretin effect, to restoring physiologic control of glucagon levels, to restoring first-phase insulin secretion, and to restoring the physiologic glucose-dependent insulin secretion. The methods of the present invention comprise administration of a selective κ-receptor antagonist, such as guanidinylated naltrindole (GNTI), or pharmaceutically acceptable derivatives thereof to a subject in need thereof. | 2013-07-04 |
| 20130172381 | ORAL DOSAGE FORMS FOR OXYGEN-CONTAINING ACTIVE AGENTS AND OXYL-CONTAINING POLYMER - The disclosed invention is drawn to pharmaceutical tablets that provide delivery of active agents having at least three oxygen-containing groups, as well as a second active ingredient. Non-limiting examples of three oxygen-containing group active agents include guaifenesin, codeine, hydrocodone, and their pharmaceutically acceptable salts. In one embodiment, a pharmaceutical tablet for oral administration once every 12 hours is provided. The tablet includes a first active agent that is a tri-oxy active agent, a second active agent, and a release rate controlling non-ionic oxyl-containing hydrophilic polymer. The total oxyl content of the hydrophilic polymer in the tablet is about 4×10 | 2013-07-04 |
| 20130172383 | TREATMENT OF FIBROSING DISORDERS - A method for treating liver-associated fibrosing disorders or lupus, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula | 2013-07-04 |
| 20130172384 | FATTY ACID SYNTHASE INHIBITORS - This invention relates to the use of triazolone and triazolethione derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones and triazolethiones in the treatment of cancer. | 2013-07-04 |
| 20130172385 | ANTHELMINTICS FOR PREVENTING PARASITIC INFECTIONS IN HUMANS AND ANIMALS - The present invention relates to compositions comprising certain active compounds which are suitable as repellents, and to their use for preventing an infection of humans or of animals by the infectious states of parasitic flatworms (platyhelminths). | 2013-07-04 |
| 20130172386 | 5-HT2B RECEPTOR ANTAGONISTS - The present invention relates to novel fluorinated piperidine derivatives having antagonistic activity at the 5-HT | 2013-07-04 |
| 20130172387 | METHOD AND COMPOSITION FOR PROLONGING ANALGESIC EFFECT OF LOCAL ANESTHETIC - Disclosed herein is a method for prolonging analgesic effect of a membrane permeable local anesthetic in a subject in need thereof. The method uses cinnamaldehyde as an adjuvant which, when administered prior to or simultaneously with the administration of a local anesthetic, prolongs the analgesic effect of the local anesthetic. Also disclosed herein is a method for providing analgesic effect in a subject in need thereof. The method uses cinnamaldehyde as an analgesic compound which, when administered alone to the subject in an analgesically effective amount, provides the analgesic effect. | 2013-07-04 |
| 20130172388 | NOVEL CANNABINOID RECEPTOR 2 (CB2) INVERSE AGONISTS AND THERAPEUTIC POTENTIAL FOR MULTIPLE MYELOMA AND OSTEOPOROSIS BONE DISEASES - Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: | 2013-07-04 |
| 20130172389 | BENZIMIDAZOLE DERIVATIVES AS SELECTIVE BLOCKERS OF PERSISTENT SODIUM CURRENT - The present invention is directed to a compound of Formula I | 2013-07-04 |
