| 31st week of 2013 patent applcation highlights part 51 |
| Patent application number | Title | Published |
|---|
| 20130196964 | HETEROCYCLICALLY SUBSTITUTED ARYL COMPOUNDS AS HIF INHIBITORS - The present application relates to novel aryl compounds with heterocyclic substituents, processes for their preparation, their use for treatment and/or prevention of diseases and their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular 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 carried out as monotherapy or also in combination with other medicaments or further therapeutic measures. | 2013-08-01 |
| 20130196965 | CYCLIC AMIDES - The invention relates to a compound of formula (I) | 2013-08-01 |
| 20130196966 | SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS AND METHODS OF CHIRAL SYNTHESIS - Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated. | 2013-08-01 |
| 20130196967 | HETEROCYCLIC COMPOUNDS AS INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compound of formula (I): | 2013-08-01 |
| 20130196968 | DI-AZETIDINYL DIAMIDE AS MONOACYLGLCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 2013-08-01 |
| 20130196969 | DI-AZETIDINYL DIAMIDE AS MONOACYLGLCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 2013-08-01 |
| 20130196970 | AMINO-PYRROLIDINE-AZETIDINE DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: | 2013-08-01 |
| 20130196971 | FATTY ACID SYNTHASE INHIBITORS - This invention relates to the use of imidazole, triazole, and tetrazole 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 imidazoles, triazoles, and tetrazoles in the treatment of cancer. | 2013-08-01 |
| 20130196972 | NOVEL COMPOUND OF A REVERSE-TURN MIMETIC AND A PRODUCTION METHOD AND USE THEREFOR - This invention relates to novel compounds of reverse-turn mimetics, having pyrazino-triazinone as a basic framework, and a method of preparing the same, and the use thereof to treat diseases such as cancer, in particular, acute myeloid leukemia. | 2013-08-01 |
| 20130196973 | BENZODIOXANE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I): | 2013-08-01 |
| 20130196974 | COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS DISEASE - A compound of formula (I) | 2013-08-01 |
| 20130196975 | 5-ALKYNYL-PYRIDINES - The present invention encompasses compounds of general formula (1) | 2013-08-01 |
| 20130196976 | COMPOSITIONS FOR REDUCING BETA-AMYLOID-INDUCED NEUROTOXICITY COMPRISING BETA-SECRETASE INHIBITOR - Disclosed are a composition for reducing beta amyloid-induced neurotoxicity by inhibiting β-secretase activity, comprising a dibenzofuran derivative, and a method for preparing the same. Further disclosed is that the combination of the dibenzofuran derivative with a γ-secretase inhibitor or an anti-inflammatory agent shows higher activity with respect to reducing beta amyloid-induced neurotoxicity. | 2013-08-01 |
| 20130196977 | USE OF ORGANIC COMPOUNDS - The present invention provides methods for the prevention of, delay progression to overt to, or the treatment of diastolic dysfunction or diastolic heart failure which method comprises administering to a warm-blooded animal a therapeutically effective amount of a renin inhibitor, or a pharmaceutically acceptable salt thereof, alone or in combination with
| 2013-08-01 |
| 20130196978 | ALKALOID AMINOESTER DERIVATIVES AND MEDICINAL COMPOSITION THEREOF - Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases. | 2013-08-01 |
| 20130196979 | Bicyclic Heteroaryl Compounds - This invention relates to compounds of the general formula: | 2013-08-01 |
| 20130196980 | DIAGNOSTIC AGENT, DIAGNOSTIC METHOD AND THERAPEUTIC AGENT FOR FIBROMYALGIA - A diagnostic agent and a diagnostic method for appropriately diagnosing fibromyalgia of a specific type, and a therapeutic agent for the aforesaid type include a diagnostic agent for fibromyalgia relating to an anti-voltage-gated potassium channel complex antibody (anti-VGKC complex antibody), said diagnostic agent containing a reagent for detecting the anti-VGKC complex antibody; a diagnostic method using the diagnostic agent; and a therapeutic agent for fibromyalgia relating to the anti-VGKC complex antibody. A diagnostic agent for fibromyalgia relating to an antibody against a voltage-gated potassium channel complex includes a reagent for detecting the antibody against the voltage-gated potassium channel complex; and a therapeutic agent for fibromyalgia relating to an antibody against voltage-gated potassium channel contains an effective amount of an anticonvulsant drug (gabapentine or clonazepam) as the active ingredient. | 2013-08-01 |
| 20130196981 | Synergistic Fungicidal Active Substance Combinations - Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) | 2013-08-01 |
| 20130196982 | MORPHOLINO SUBSTITUTED UREA DERIVATIVES AS MTOR INHIBITORS - The invention relates to compounds of formula (I) | 2013-08-01 |
| 20130196983 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators. | 2013-08-01 |
| 20130196984 | 3-AMINO-5-PHENYL-56-DIHYDRO-2H-[1,4]OXAZINES - The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I | 2013-08-01 |
| 20130196985 | HETEROCYCLIC ALKYNYL BENZENE COMPOUNDS AND MEDICAL COMPOSITIONS AND USES THEREOF - The heterocyclic alkynyl benzene compounds of formula (I), their pharmaceutically acceptable salts and stereoisomers thereof, as well as application in preparing drugs for preventing or treating tumors. The compounds can overcome the clinically induced resistance against Gleevec. | 2013-08-01 |
| 20130196986 | TRIAZOLOPYRAZINONES AS P2X7 RECEPTOR ANTAGONISTS - The invention provides certain 3,7-disubstituted-[1,2,4]triazolo[4,3-a]pyrazin-8(7H)-ones of the Formula (I), and their pharmaceutically acceptable salts, wherein R | 2013-08-01 |
| 20130196987 | MACROCYCLIC COMPOUNDS USEFUL AS PHARMACEUTICALS - The present invention provides compounds, methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis. | 2013-08-01 |
| 20130196988 | Dihydrothienopyrimidines - The present invention relates to dihydrothienopyrimidines, their use as modulators of γ-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with γ-secretase and/or its substrate and therefore modulate the formation of Aβ peptides. | 2013-08-01 |
| 20130196989 | COMPOSITIONS AND METHODS FOR INDUCING CELL DEDIFFERENTIATION - The present invention provides compounds, compositions and methods for dedifferentiating lineage committed mammalian cells into stem cells. The present invention also provides methods of inducing dedifferentiation of lineage committed mammalian cells into stem cells, which can be further differentiated into various lineage committed cells. Methods of identifying additional compounds useful for inducing dedifferentiation of lineage committed cells into stem cells are also provided. | 2013-08-01 |
| 20130196990 | Benzimidazole Derivatives As PI3 Kinase Inhibitors - This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer. | 2013-08-01 |
| 20130196991 | SUBSTITUTED INDOLES, ANTIVIRAL ACTIVE COMPONENT, METHOD FOR PREPARATION AND USE THEREOF - The invention relates to novel antiviral active components of the general formula 1, pharmaceutical composition, antiviral medicament, method for prophylaxis and treatment of viral diseases, particularly caused by hepatisis C viruses (HCV). In the general formula 1 | 2013-08-01 |
| 20130196992 | 1',3'-DISUBSTITUTED-4-PHENY-3,4,5,6-TETRAHYDRO-2H,1'H-[1,4']BIPYRIDINYL-2'- -ONES - The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) | 2013-08-01 |
| 20130196993 | N-HETEROARYL COMPOUNDS - This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to novel N-heteroaryl compounds and the preparation of said compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds. | 2013-08-01 |
| 20130196994 | PDE10 INHIBITORS AND RELATED COMPOSITIONS AND METHODS - Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same. | 2013-08-01 |
| 20130196995 | COMBINATION OF BRIMONIDINE AND TIMOLOL FOR TOPICAL OPHTHALMIC USE - Disclosed are pharmaceutical compositions comprising brimondine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans. | 2013-08-01 |
| 20130196996 | USE OF ISOXAZOLINE COMPOUNDS AND COMPOSITIONS IN BLADDER CANCER - One embodiment provides a method, comprising treating or preventing at least one disease selected from the group consisting of bladder cancer, weight loss accompanying bladder cancer, bone pain accompanying bladder cancer, bladder cancer carcinoma in-situ (CIS), TA stage bladder cancer, T1 stage bladder cancer, T2 stage bladder cancer, T3 stage bladder cancer, T4 stage bladder cancer, lymph node metastasis therefrom, solid organ metastasis therefrom, bony metastasis therefrom, cachexia/anorexia associated with bladder cancer, generalized wasting syndrome associated with bladder cancer, or a combination thereof, by administering to a subject in need thereof one or more compounds described herein, prodrug thereof, salt thereof, or a combination thereof. | 2013-08-01 |
| 20130196997 | DUAL-ACTING OXAZOLE ANTIHYPERTENSIVE AGENTS - In one aspect, the invention relates to compounds having the formula: | 2013-08-01 |
| 20130196998 | SPIRO-CYCLIC AMINE DERIVATIVES AS S1P MODULATORS - The present invention relates to spiro-cyclic amine derivatives of the formula (I) | 2013-08-01 |
| 20130196999 | METHODS OF CONTROLLING NEONICOTINOID RESISTANT APHIDS - The invention relates to a method of controlling aphids that are resistant to neonicotinoid insecticides, using the compound 4,5-dihydro-6-methyl-4-(3-pyridylmethyleneamino)-1,2,4-triazin-3(2H)-one in free form or in agrochemically acceptable salt form as well as the use of compositions comprising said compound to control neonicontinoid resistant insects. In particular the methods relate to controlling neonicotinoid resistant insects in the Aphididae family, that are resistant to one or more neonicotinoid insecticides. Methods of the invention find particular use in controlling neonicotinoid resistant insects in crops of useful plants. Furthermore, the invention extends to methods of controlling plant viruses spread by neonicotinoid resistant insects. | 2013-08-01 |
| 20130197000 | DRUG AND FOOD/DRINK FOR PREVENTING OR IMPROVING CEREBRAL DYSFUNCTION | 2013-08-01 |
| 20130197001 | SUBSTITUTED HETEROCYCLIC COMPOUNDS - The present invention relates to compounds that are late sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): | 2013-08-01 |
| 20130197002 | BRIMONIDINE FOR TREATING VISUAL DISORDERS MEDIATED BY CENTRAL VISUAL PROJECTIONS FROM THE EYE - The present invention relates to a method for treating visual disorders mediated by lateral geniculate nucleus, superior colliculus and the visual cortex by administering to a patient in need of such treatment, compounds acting at the alpha 2 adrenergic receptor. | 2013-08-01 |
| 20130197003 | METHODS AND COMPOSITIONS FOR TREATING OR PREVENTING ERYTHEMA - Methods and products for treating or preventing erythema or a symptom associated with erythema in a subject are described. The methods involve topically applying to an affected skin area a topical aqueous gel composition comprising about 0.01% to about 10% by weight of at least one α-adrenergic receptor agonist and a pharmaceutically acceptable carrier. | 2013-08-01 |
| 20130197004 | Optically Pure Diastereomers of 10-Propargyl-10-Deazaaminopterin and Methods of Using Same for the treatment of cancer - The present invention relates to diastereomers of 10-propargyl-10-deazaminopterin, compositions comprising optically pure diastereomers of 10-propargyl-10-deazaminopterin, in particular the two (R,S) diastereomers about the C10 position. Methods of preparation of these diastereomers, compositions containing them, and their use for the treatment of conditions related to inflammatory disorders and cancer are also disclosed. | 2013-08-01 |
| 20130197005 | Parenteral Formulations Of Dopamine Agonists - This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics. | 2013-08-01 |
| 20130197006 | Non-Starch Based Soft Chewables - The present invention generally relates to soft chewables, especially suitable for delivering active ingredients to animals and processes for the preparation thereof. In various embodiments, the soft chewable comprises a pharmaceutically effective amount of at least one active ingredient, a flavoring agent, a disintegrant a humectant, an antioxidant, a preservative, and water. In accordance with preferred embodiments, the soft chewable is essentially free of starch, oil glycols, waxes, and soy products. | 2013-08-01 |
| 20130197007 | Phenyl-Heteroaryl Derivatives and Methods of Use Thereof - The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof | 2013-08-01 |
| 20130197008 | 3-AMINOCYCLOPENTANECARBOXAMIDES AS CHEMOKINE RECEPTOR AGONISTS - There is provided a compound of Formula I(a) or I(b): | 2013-08-01 |
| 20130197009 | ANTAGONIST FOR MUTANT ANDROGEN RECEPTOR - [Problem] An object of the present invention is to provide a novel anticancer drug which is useful for treating prostate cancer accompanying androgen receptor mutation | 2013-08-01 |
| 20130197011 | Phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones and the use thereof as medicament - Substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones which are glycine transporter-1 (GlyT1) inhibitors. These are useful for the treatment of schizophrenia, Alzheimer's Disease and other neurological and psychiatric disorders. | 2013-08-01 |
| 20130197012 | Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 2013-08-01 |
| 20130197013 | CYCLOPROPYLAMINE DERIVATIVES USEFUL AS LSD1 INHIBITORS - The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection. | 2013-08-01 |
| 20130197014 | PURINONE 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. In addition, reversible inhibitors of Btk are also described. 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. | 2013-08-01 |
| 20130197015 | NOVEL METHOD TO IMPROVE THE SAFETY AND EFFICACY OF CAFFEINE - The present invention relates to methods and compositions for reducing side effects associated with caffeine consumption. The methods comprise administering a Receptor Switcher, such as N-acetyl cysteine, in combination with caffeine. | 2013-08-01 |
| 20130197016 | DOSING REGIMES FOR THE TREATMENT OF OCULAR VASCULAR DISEASE - The use of vascular endothelial growth factor receptor 2 inhibitors or a pharmaceutically acceptable salt thereof for the treatment of ocular vascular disease is provided. Dosing regimes, including once weekly administration, of certain VEGF-R2 inhibitors are provided which deliver therapeutically effective concentrations of the VEGF-R2 compounds in ocular tissues for at least one week for the treatment of ocular vascular disease. | 2013-08-01 |
| 20130197017 | COMBINATIONS COMPRISING A PROTEIN KINASE INHIBITOR BEING A PYRIMIDYLAMINOBENZAMIDE COMPOUND AND A HSP90 INHIBITOR SUCH AS 17-11G - The invention provides a pharmaceutical combination comprising:
| 2013-08-01 |
| 20130197018 | Synergistic Fungicidal Active Substance Combinations - Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) | 2013-08-01 |
| 20130197019 | 1',3'-DISUBSTITUTED-4-PHENYL-3,4,5,6-TETRAHYDRO-2H,1'H-[1,4']BIPYRIDINYL-2- '-ONES - The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) | 2013-08-01 |
| 20130197020 | Method of Providing Sustained Analgesia With Buprenorphine - A method of effectively treating pain in humans is achieved by administering buprenorphine in accordance with first order kinetics over an initial three-day dosing interval, such that a maximum plasma concentration from about 20 pg/ml to about 1052 pg/ml is attained, and thereafter maintaining the administration of buprenorphine for at least an additional two-day dosing interval in accordance with substantially zero order kinetics, such that the patients experience analgesia throughout the at least two-day additional dosing interval. | 2013-08-01 |
| 20130197021 | COMBINATION OF ACTIVE LOADED GRANULES WITH ADDITIONAL ACTIVES - The present invention relates to prolonged release pharmaceutical dosage forms, the manufacture thereof as well as their use for administration to human being | 2013-08-01 |
| 20130197022 | 3-CYANO-QUINOLINE DERIVATIVES WITH ANTIPROLIFERATIVE ACTIVITY - The present invention concerns the compounds of formula | 2013-08-01 |
| 20130197023 | NEUROPROTECTION BY PHARMACOLOGICAL CHAPERONING OF NICOTINIC ACETYLCHOLINE RECEPTORS - A method of ameliorating an endoplasmic reticulum (ER) stress response and/or unfolded protein response (UPR) in cells expressing nicotinic acetylcholine receptors (nAChRs) comprises contacting a cell expressing nAChRs with an effective amount of a ligand for nAChRs. The contacting results in attenuating endogenously expressed ATF6 translocation, expression of XBP1, phosphorylation of eukaryotic initiation factor 2α (peIF2α), increased numbers of ER exit sites, increased trafficking of known associated proteins as well as other proteins such as growth factors and their receptors, changes in abundance of selected mRNA species, and phosphorylation, abundance, or subcellular compartmentalization of other proteins involved with ER stress and/or the UPR, and inhibiting upregulation of CCAAT/Enhancer-Binding Protein Homologous Protein (CHOP) levels in the cells. The method can be used to screen for neuropharmacotherapeutic agents and to treat or prevent neurodegenerative disease, such as amyotrophic lateral sclerosis (ALS), Parkinson's disease, Alzheimer's disease, or cognitive deficiency. | 2013-08-01 |
| 20130197024 | LIQUID FORMULATIONS FOR TREATMENT OF DISEASES OR CONDITIONS - Diseases and conditions associated with tissues of the body, including but not limited to tissues in the eye, can be effectively treated, prevented, inhibited, onset delayed, or regression caused by administering therapeutic agents to those tissues. Described herein are liquid formulations which deliver a variety of therapeutic agents, including but not limited to rapamycin, to a subject for an extended period of time; liquid formulations which form a non-dispersed mass when placed in an aqueous medium of a subject; non-dispersed mass-forming liquid formulations which form a gel or gel-like substance in an aqueous medium; liquid formulations, comprising a therapeutic agent and a plurality of polymers; and methods for delivering therapeutic agents to a subject for an extended period of time using the liquid formulations. The liquid formulation may be placed in an aqueous medium of a subject, including but not limited to via intraocular or periocular administration, or placement proximate to a site of a disease or condition to be treated in a subject. A method may be used to administer rapamycin to treat or prevent angiogenesis, choroidal neovascularization, or age-related macular degeneration, or wet age-related macular degeneration in a subject. The liquid formulations may comprise rapamycin or other therapeutic agents. | 2013-08-01 |
| 20130197025 | A3 ADENOSINE RECEPTOR ALLOSTERIC MODULATORS - The claimed subject matter relates to allosteric modulation of A | 2013-08-01 |
| 20130197026 | COMPOSITION AND METHODS FOR TREATING GLIOBLASTOMA - The disclosure provides methods of treating glioblastoma, methods of screening for compounds that treat glioblastoma, and pharmaceutical compositions useful the treatment of glioblastoma. | 2013-08-01 |
| 20130197027 | HETEROCYCLYL-AZABICYCLO[3.2.1]OCTANE ANALOGS AS SELECTIVE M1 AGONISTS AND METHODS OF MAKING AND USING SAME - In one aspect, the invention relates to compounds which are useful as allosteric or bitopic agonists of the M | 2013-08-01 |
| 20130197028 | nAChRalpha7 Agonists and nAChRalpha7 Antagonists for Treating Ulcerative Colitis (UC) and Crohn's Disease (CD) - Agonists and antagonists of nAChRα7 and their use as therapeutic agents for treating and managing inflammatory bowel diseases (IBD), such as Crohn's disease (CD) and ulcerative colitis (UC), are disclosed. Agonists and antagonists of nAChRα7 and their use as therapeutic agents for treating and managing inflammatory bowel diseases (IBD), such as Crohn's disease (CD) and ulcerative colitis (UC), are disclosed. | 2013-08-01 |
| 20130197029 | CHEMICAL COMPOUNDS - The use of a compound of formula I | 2013-08-01 |
| 20130197030 | Substituted 1,3-Dioxanes and There Uses - The present invention relates to 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 compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer. | 2013-08-01 |
| 20130197031 | DEUTERATED ANALOGS OF PRIDOPIDINE USEFUL AS DOPAMINERGIC STABILIZERS - The present invention provides novel deuterated analogs of Pridopidine, i.e. 4-(3-methanesulfonyl-phenyl)-1-propyl-piperidine. Pridopidine is a drug substance currently in clinical development for the treatment of Huntington's disease. | 2013-08-01 |
| 20130197032 | PHENYLPIPERIDINE COMPOUNDS FOR THE TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS - The present invention relates to a novel use of both enantiomers of the phenylpiperidine derivative OSU6162, i.e. (−) and (+)-OSU6162 as partial agonists on 5-hydroxytryptamine (5hHT) receptors. As a result, both (−) OSU6162 and (+)-OSU6162 may be used for the treatment and/or prevention of one or more diseases associated with a need for modulation of monoaminergic neurotransmitter receptors, wherein at least one of the monoaminergic neurotransmitter receptors is a 5-hydroxytryptamine receptor (5-HT receptor). Thus, said compounds act as stabilizers not only on dopaminergic, but also on serotonergic brain signaling and will act as partial agonists on such monoaminergic neurotransmitter receptors. | 2013-08-01 |
| 20130197033 | PAROXETINE DERIVATIVE - A compound represented by Formula (1), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of paroxetine and has an improved CYP inhibitory effect: | 2013-08-01 |
| 20130197034 | Salts Of Methyl 2-((R)-(3-Chlorophenyl)((R)-1-((S)-2-(Methylamino)-3-((R)-Tetrahydro-2H-P- yran-3-Yl)Propylcarbamoyl)Piperidin-3-Yl)Methoxy)Ethylcarbamate - Mucic acid salts of a compound represented by the following structural formula: | 2013-08-01 |
| 20130197035 | Surgical Adjuvant Composition and Associated Methods of Use - Disclosed herein are surgical adjuvant compositions for ameliorating tissue and cellular necrosis and/or apoptosis. In addition, surgical methods are described which include the use of the adjuvant of the composition to reduce tissue and cellular necrosis and/or apoptosis. | 2013-08-01 |
| 20130197036 | TRANSDERMAL ABSORPTION PREPARATION - Disclosed is a safe, transdermal absorption preparation useful in the treatment of fungal infections, having excellent skin permeability and strong antifungal activity, and greatly contributing to a patient's quality of life. The disclosed transdermal absorption preparation contains 4-{3-[4-(3-{4-[amino(imino)methyl]phenoxy}propyl)-1-piperidinyl]propoxy}benzamidine, or a salt thereof, and a transdermal absorption enhancer. | 2013-08-01 |
| 20130197037 | APOPTOSIS SIGNAL-REGULATING KINASE INHIBITOR - The present invention relates to a compound of formula (I): | 2013-08-01 |
| 20130197038 | Compositions And Methods For Neovascularization - The invention is directed to a method of inducing angiogenesis at a site in an individual in need thereof comprising administering locally to the site an effective amount of one or more agents that induce hypoxia induced factor 1α (HIF-1α). In another aspect, the invention is directed to a method of inducing angiogenesis at a site in an individual in need thereof comprising administering locally to the site an effective amount of one or more agents that induce hypoxia induced factor 1α (HIF-1α) and one or more lysophospholipids. In addition, the invention is directed to methods of generating prevascularized tissue, methods of generating a vascular network in a device and compositions thereof. | 2013-08-01 |
| 20130197039 | Novel Benzyl Sulfonamide Derivatives Useful As MOGAT-2 Inhibitors - The present invention provides compounds of Formula below: | 2013-08-01 |
| 20130197040 | POLYMORPHS OF DALFAMPRIDINE, PREPARATIONS AND USES THEREOF - Provided are polymorphs I to VIII of a dalfampridine or of its solvates, a preparation method therefore, and applications thereof as an active component of a medicine. Said polymorphs Ito VIII of the dalfampridine or of its solvents can be used to prepare formulations for improving the walking speed of patients of multiple sclerosis and for alleviating other symptoms of multiple sclerosis. | 2013-08-01 |
| 20130197041 | GABR-A2 DIAGNOSTIC - The present invention provides a method of selection of a patient, who is a candidate for treatment with an NMDA antagonist drug, such as (S)-1-phenyl-2-(pyridin-2-yl)ethanamine or ketamine, whereby to predict an increased or decreased likelihood of response to the NMDA antagonist. The invention provides a method for determining the sequence of GABR-A2 at any of four single nucleotide polymorphism (SNP) sites known as rs3756007, rs11503016, rs17537359 or rs1372472. The method also provides ARMS primers optimised for determining the sequence at these GABR-A2 SNPs and diagnostic kits comprising suitable primers or probes for determining the particular SNPs. | 2013-08-01 |
| 20130197042 | HDAC INHIBITORS - Compounds of formula (I) inhibit HDAC activity: | 2013-08-01 |
| 20130197043 | USE OF THE FETAL REPROGRAMMING OF A PPAR AGONIST - Disclosed is a novel use of a PPAR δ agonist, and more particularly, a fetal reprogramming effect of a PPAR δ agonist. A PPAR δ agonist adjusts calcium ion during embryo genesis and a early fetal development period to increase slow muscle fiber and to thus improve muscle endurance, thereby improving lipid and glucose metabolism and reprogramming the metabolism of the entire body, thus preventing/inhibiting the occurrence of metabolic diseases, such as obesity and diabetes in an adult body caused by a high-fat diet and a lack of exercise, and improving memory for an adult. | 2013-08-01 |
| 20130197044 | METHODS OF TREATING HEPATORENAL SYNDROME AND HEPATIC ENCEPHALOPATHY WITH THROMBOXANE-A2 RECEPTOR ANTAGONISTS - The present invention is directed to methods of treating hepatorenal syndrome by administration of a therapeutically effective amount of a thromboxane A | 2013-08-01 |
| 20130197045 | SITAXENTAN DERIVATIVE - A compound represented by formula (1-1) or (1-2), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of sitaxentan and has an improved CYP inhibitory effect: | 2013-08-01 |
| 20130197046 | NOVEL P2X7R ANTAGONISTS AND THEIR USE - The present application is directed to novel P2X7R antagonists that are indol-3-carboxamide or azaindole-3-carboxamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity. | 2013-08-01 |
| 20130197048 | METRONIDAZOLE ESTERS FOR TREATING ROSACEA - A compound of formula (I): | 2013-08-01 |
| 20130197049 | COMPOUNDS FOR TREATMENT OF CANCER - The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer. | 2013-08-01 |
| 20130197050 | NOVEL LACTAMS AND USES THEREOF - The present invention provides novel lactams extracted from an alcohol extract of dehulled adlay seeds. The present invention also provides a process for the preparation of the lactams and a method for treating breast cancer in a subject, which method comprises administering to said subject an effective amount of the lactam and a pharmaceutically acceptable carrier or excipient. | 2013-08-01 |
| 20130197051 | KETOROLAC TROMETHAMINE COMPOSITIONS FOR TREATING OR PREVENTING OCULAR PAIN - Compositions comprising ketorolac tromethamine at a therapeutically effective concentration of less than 0.5% are disclosed herein. Methods of treating or preventing ocular pain using said compositions are also disclosed herein. | 2013-08-01 |
| 20130197052 | TRYPTAMINE DERIVATIVES, THEIR PREPARATION AND THEIR USE IN GASTROPATHY - The synthesis and evaluation of gastroprotective effect of different tryptamine derivatives. Tryptamine derivatives have been synthesized by formation of amide or ester with some known anti oxidant molecules. These derivatives show excellent antioxidant property in vitro. Among all the derivatives the compound SEGA (3a), that was prepared by the combination of serotonin with gallic acid shows the greater antioxidant property than the other synthesized compounds both in vivo and in vitro. SEGA(3a) shows the gastroprotective effect against NSAIDs (indomethacin or diclofenac)-induced gastropathy in dose dependent manner and also accelerates the healing from injury. It prevents the NSAIDs-induced mitochondrial oxidative stress in vivo. This derivative prevents NSAID-induced mitochondrial oxidative stress-mediated apoptosis in vivo by preventing the activation of caspase 9 and caspase-3 and restores NSAIDs-mediated collapse of mitochondroial transmembrane potential and dehydrogenase activity. SEGA (3a) plays an important role as an iron chelator as well as intra mitochondrial ROS scavenger. Thus, SEGA (3a) is a potent antioxidant antiapototic molecule, which efficiently prevents NSAID-induced gastropathy and stress or alcohol-mediated gastric damage. | 2013-08-01 |
| 20130197053 | PHARMACEUTICAL COMPOSITION CONTAINING A TRYPTOPHAN DERIVATIVE - Pharmaceutical compositions containing a compound of formula (I) wherein the radicals denote e.g.: R | 2013-08-01 |
| 20130197054 | Composition Based on Vegetable Extract and Methods for the Treatment of Cutaneous Inflammatory Forms, in Particular Psoriasis - The present invention concerns, in one aspect, a composition comprising an extract of beet plant in a biologically active amount and a physiologically acceptable excipient or carrier. The composition of the invention finds application in the dermatological or cosmetic treatment of inflammatory skin affection such as reddening or psoriatic lesions. | 2013-08-01 |
| 20130197055 | INHIBITION OF PCSK9 THROUGH RNAI - The invention relates to various PCSK9 RNAi constructs with gene silencing activities, and uses thereof The construct has a double-stranded region of 19-49 nucleotides, preferably 25, 26, or 27 nucleotides, and preferably blunt-ended The construct has selective minimal modifications to confer an optimal balance of biological activity, toxicity, stability, and target gene specificity The sense strand may be modified such that the construct is not cleaved by Dicer or other RNAse III, and the entire length of the antisense strand is loaded into RISC In addition, the antisense strand may also be modified by 2′-O-methyl groups at the 2nd 5′-end nucleotide to greatly reduce off-target silencing The constructs of the invention largely avoid the interferon response and sequence-independent apoptosis in mammalian cells, exhibits better serum stability, and enhanced target specificity. | 2013-08-01 |
| 20130197056 | NOVEL BIOMARKERS AND TARGETS FOR OVARIAN CARCINOMA - Novel biomarkers and targets associated with ovarian cancer, particularly clear-cell carcinoma, endometrioid carcinoma, and uterine carcinoma, are disclosed. Mutations in genes encoding proteins that form part of the SWI/SNF chromatin remodelling protein complex, including ARID1A, or loss of expression of such proteins, including BAF250a, can be used to evaluate the likelihood endometriosis will progress or transform to cancer, to provide a prognosis for a patient with cancer, to assess whether conventional treatment is likely to be effective against a cancer, and/or in a synthetic lethal screen to identify novel targets and therapeutics for the treatment of cancer. | 2013-08-01 |
| 20130197057 | METHOD FOR REDUCING EXPRESSION OF DOWNREGULATED IN RENAL CELL CARCINOMA IN MALIGNANT GLIOMAS - The present invention relates to novel compositions and therapeutic methods for the treatment of cancer, in particular malignant glioma. The compositions include antisense oligonucleotides or RNAs or vectors encoding them which reduce expression of downregulated in renal cell carcinoma (DRR) in tumor cells, and inhibit malignant glioma cell invasion. | 2013-08-01 |
| 20130197058 | INHIBITING STRIATED MUSCLE ACTIVATOR OF RHO (STARS) TO IMPROVE GLYCEMIC CONTROL - Described are methods of improving glycemic control/improving insulin sensitivity by administering an inhibitor of Striated Muscle Activator of Rho Signaling (STARS) activity, and methods of identifying new compounds for use in the described methods of treatment. | 2013-08-01 |
| 20130197059 | INTEGRIN ANTAGONIST CONJUGATES FOR TARGETED DELIVERY TO CELLS EXPRESSING LFA-1 - The invention relates to compounds of formula I: | 2013-08-01 |
| 20130197060 | MICRORNA PATTERNS FOR THE DIAGNOSIS, PROGNOSIS AND TREATMENT OF MELANOMA - The present invention relates to methods for diagnosing, staging, prognosticating and treating melanoma based on evaluating the expression of specific patterns of oncogenic or suppressive microRNA (miR) molecules in a patient in need thereof. | 2013-08-01 |
| 20130197061 | AGENT FOR SUPPRESSING EXPRESSION OF DOMINANT MUTANT GENE - An RNAi molecule that can selectively and effectively suppress only the expression of a particular dominant mutant gene, while permitting the expression of the wild-type gene or a desired mutant gene, and a design method thereof is presented. | 2013-08-01 |
| 20130197062 | OLIGOMERIC COMPOUNDS COMPRISING TRICYCLIC NUCELOSIDES AND METHODS FOR THEIR USE - The present disclosure provides tricyclic nucleosides, oligomeric compounds comprising at least one of the tricyclic nucleosides and methods of using the oligomeric compounds. The methods provided herein include contacting a cell or administering to an animal at least one of the oligomeric compounds. In certain embodiments, the oligomeric compounds hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA. | 2013-08-01 |
| 20130197063 | USE OF A GROWTH-STIMULATING PROTEIN - This invention relates to the inhibition of a newly discovered growth-stimulating protein in an individual. Further, the invention relates to a method for preventing or treating a cancer, or preventing or treating cancer growth, invasion or metastasis, or preventing or treating other hyperproliferative diseases in an individual, by down regulating the expression of said growth-stimulating protein or by inactivating said protein. Still further, the invention concerns a method for diagnosing cancer or other hyperproliferative diseases in an individual based on said growth-stimulating protein. | 2013-08-01 |
| 20130197064 | METHOD AND COMPOSITION FOR ALVEOLAR EPITHELIAL CELL-SPECIFIC NUCLEIC ACID NUCLEAR IMPORT - One aspect of the invention relates to an isolated nuclear targeting molecule that includes a fragment of a mammalian glycoprotein 36 (gp36, also known as T1-α or podoplanin) gene expressed in type I alveolar epithelial cells. Plasmids containing the isolated nuclear targeting molecule which are useful for affording nuclear uptake of the plasmid DNA in type I alveolar epithelial cells but not type II alveolar epithelial cells, and compositions and host cells containing such plasmids are also disclosed. Use of the plasmids for targeting an exogenous DNA into nuclei of type I alveolar epithelial cells is described herein. | 2013-08-01 |
| 20130197065 | Modulators of Coagulation Factors - The invention provides improved nucleic acid ligands that inhibit coagulation and improved modulators of the nucleic acid ligands to provide ideal modulators of coagulation. These improved nucleic acid ligands and modulators are particularly useful for inhibiting coagulation in a host undergoing a therapeutic regime such as surgery or coronary artery bypass. | 2013-08-01 |
