| 19th week of 2013 patent applcation highlights part 46 |
| Patent application number | Title | Published |
|---|
| 20130116194 | COSMETIC COMPOSITION FOR RESTORING LIPIDIC LAYER OF THE STRATUM CORNEUM IN ORTHORHOMBIC - The present invention refers to a cosmetic composition of the oil-in-glycol type comprising (a) at least one sucrose non-ionic surfactant or derivatives thereof, (b) at least one fatty alcohol, (c) at least one glycol and (d) at least one ingredient selected from aminoacid and/or peptide, as well as associated uses, products and methods. The composition of the invention is capable of restoring the cutaneous barrier, reorganizing the lipidic layer of the stratum corneum in orthorhombic, conceding hydration, renewal and cellular energization in the long run. In a particular embodiment, said composition can be used simultaneously as an emulsifying system for preparing cosmetic products, for example, in the preparation of creams, lotions, etc. | 2013-05-09 |
| 20130116195 | Binding ligand linked drug delivery conjugates of tubulysins - Described herein are compounds, pharmaceutical compositions, and methods for treating pathogenic cell populations. Kits including the compounds or pharmaceutical compositions are described. The compounds described herein include conjugates of tubulysins and folates. The conjugates also include a releasable bivalent linker. | 2013-05-09 |
| 20130116196 | MUSCLE FATIGUE SUBSTANCE CYTOKINES AND METHODS OF INHIBITING TUMOR GROWTH THEREWITH - Compositions and methods for inhibiting tumor growth and tumor cell proliferation are provided. In general, the cytokines useful with the present invention are selected from the group consisting of LIX (or CXCL | 2013-05-09 |
| 20130116197 | MODIFIED BINDING PROTEINS INHIBITING THE VEGF-A RECEPTOR INTERACTION - The present invention relates to binding proteins specific for VEGF-A, in particular to recombinant binding proteins comprising a polyethylene glycol moiety and a binding domain, which inhibits VEGF-Axxx binding to VEGFR-2. Examples of such recombinant binding proteins are proteins which comprise an ankyrin repeat domain with the desired binding specificity, and a polyethylene glycol moiety. The binding proteins are useful in the treatment of cancer and other pathological conditions, e.g. eye diseases such as age-related macular degeneration. | 2013-05-09 |
| 20130116198 | Compositions for Regenerating Defective or Absent Myocardium - Compositions of the invention for regenerating defective or absent myocardium comprise an emulsified or injectable extracellular matrix composition. The composition may also include an extracellular matrix scaffold component of any formulation, and further include added cells, proteins, or other components to optimize the regenerative process and restore cardiac function. | 2013-05-09 |
| 20130116199 | Agonists of Guanylate Cyclase Useful For the Treatment of Gastrointestinal Disorders, Inflammation, Cancer and Other Disorders - The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer. | 2013-05-09 |
| 20130116200 | Treatment of Vascular Complications of Diabetes - A peptide consisting of 7-17 amino acids and including the adjacent hexamer TX | 2013-05-09 |
| 20130116201 | USE OF PEPTIDES AS TRANSPORTERS INTENDED FOR THE INTERNALIZATION OF MOLECULES OF INTEREST INTO TARGET CELLS - The method pertains to a peptide including the amino acid sequence SEQ ID NO: 1, or a peptide including an amino acid sequence having 93%, in particular 95%, particularly 98% sequence identity homology with the sequence SEQ ID NO: 1, in order to obtain a transporter intended for the internalization of a molecule of diagnostic or therapeutic interest into the target cells. | 2013-05-09 |
| 20130116202 | NGNA COMPOSITIONS AND METHODS OF USE - The present invention relates to the field of viral disorders, and in particular to the use of natural compounds to inhibit viruses and viral infection. Compositions comprising NGNA are provided for treating or preventing viral infections, such as those causing the common cold. | 2013-05-09 |
| 20130116203 | ISOTHIOCYNATES AND GLUCOSINOLATE COMPOUNDS AND ANTI-TUMOR COMPOSITIONS CONTAINING SAME - The present invention provides glucosinolate and isothiocyanate compounds and related methods for synthesizing these compounds and analogs. In certain embodiments, these glucosinolate and isothiocyanate compounds are useful and chemopreventive and or chemotherapeutic agents. | 2013-05-09 |
| 20130116204 | (METHYLSULFONYL) ETHYL BENZENE ISOINDOLINE DERIVATIVES AND THEIR PHARMACEUTICAL USES - Provided are (methylsulfonyl)ethyl benzene isoindoline compounds, and pharmaceutically acceptable salts, solvates, or stereoisomers thereof. Methods of use and pharmaceutical compositions of these compounds are also disclosed. | 2013-05-09 |
| 20130116205 | COMPOSITION CONTAINING IRIDOIDS AND USES THEREOF - Composition containing iridoids such as morroniside and loganin, the use thereof in preparing medicaments for preventing and treating neurologic demyelinating diseases, and the method thereof in treating diseases related to neurologic demyelinating lesions are disclosed by the present application. | 2013-05-09 |
| 20130116206 | QUINOLINE DERIVATIVES USED AS PET IMAGING AGENTS - There is provided compounds of formula (I), wherein R | 2013-05-09 |
| 20130116207 | Compositions and Methods for Treating Cancer - Provided herein are compounds used to inhibit the deamination enzyme responsible for the inactivation of therapeutic compounds, and methods of using them. | 2013-05-09 |
| 20130116208 | ADMINISTRATION OF A NEDD8-ACTIVATING ENZYME INHIBITOR AND HYPOMETHYLATING AGENT - The present disclosure relates to methods for the treatment of cancer in patients in recognized need of such treatment. The methods comprise administering to such a patient an NAE inhibitor or a pharmaceutically acceptable salt thereof, such as ((1S,2S,4R)-4-(4-((1S)-2,3-dihydro-1H-inden-1-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate (MLN4924) or {(1S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyclopentyl}methyl sulfamate (I-216), and a hypomethylating agent or a pharmaceutically acceptable salt thereof, such as azacitidine or decitabine. Also disclosed are medicaments for use in the treatment of cancer. | 2013-05-09 |
| 20130116209 | METHOD FOR SELECTION OF CHEMOTHERAPEUTIC AGENTS FOR ADENOCARCINOMA CANCER - The subject invention relates to determining the presence and level of hENT1 expression in tumor tissue that is appropriate for gemcitabine therapy, and more importantly, the level of hENT1 expression that signifies that treatment with a gemcitabine derivative is a more appropriate strategy. | 2013-05-09 |
| 20130116210 | CONTROLLED RELEASE ANTIMICROBIAL COMPOSITIONS AND METHODS FOR THE TREATMENT OF OTIC DISORDERS - Disclosed herein are compositions and methods for the treatment of otic diseases or conditions with antimicrobial agent compositions and formulations administered locally to an individual afflicted with an otic disease or condition, through direct application of these compositions and formulations onto or via perfusion into the targeted auris structure(s). | 2013-05-09 |
| 20130116211 | Novel Salts Of Boswellic Acids And Selectively Enriched Boswellic Acids And Processes For The Same - New salts or ion-pair complexes obtained by a reaction between boswellic acids or selectively enriched 3-O-acetyl-11-keto-β-boswellic acid (AKBA) or 11-keto-β-boswellic acid (KBA) compounds obtained through a new improved process, and an organic amine, more particularly with glucosamine. These salts or ion pair complexes are useful in nutraceuticals and in food supplements for anti-inflammatory and analgesic treatment of joints and cancer prevention or cancer therapeutic agents. These salts or ion pair complexes could also be used in cosmetic or pharmaceutical composition for external treatment of body parts or organs to treat inflammatory diseases or cancer. | 2013-05-09 |
| 20130116212 | OIL-BASED GEL-LIKE COMPOSITION - There is provided a gel-forming agent which is easily prepared and has all of high safety in the living body and the environment, good gel-forming capability, excellent use feeling, and good handleability. | 2013-05-09 |
| 20130116213 | NOVEL FUSED PYRIMIDINE DERIVATIVES FOR INHIBITION OF TYROSINE KINASE ACTIVITY - The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient. | 2013-05-09 |
| 20130116214 | HETEROCYCLIC RING COMPOUND - The present invention provides a compound having a muscle cell or adipocyte differentiation regulating action, useful for the prophylaxis or treatment of diseases such as diabetes, obesity, dyslipidemia and the like, and the like, and having superior efficacy. | 2013-05-09 |
| 20130116215 | COMBINATION THERAPIES FOR TREATING NEUROLOGICAL DISORDERS - The invention features novel pharmaceutical combinations useful for the treatment of neurological diseases, specifically neurodegenerative diseases. The novel pharmaceutical combinations of the invention demonstrate additive or synergistic effect in silico and in vivo. The invention also relates to methods of treatment of neurological and neurodegenerative diseases including the pharmaceutical combinations of the invention. | 2013-05-09 |
| 20130116216 | TRANSGLUTAMINASE TG2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF - Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents. | 2013-05-09 |
| 20130116217 | NEUROPROTECTION AND MYELIN REPAIR USING NESTORONE.RTM. - Methods for treating neurodegeneration and/or myelination in patients are disclosed comprising treating the patient with a progestin compound which exerts binding to progesterone receptors and elicits progesterone-receptor-induced biological responses without interacting with the androgen receptor and without inducing androgen or glucocorticoid biological responses at a dosage sufficient to prevent or reduce neurodegeneration. The progestin compound preferably comprises 16-methylene-17α-acetoxy-19-norpregn-4-ene-3,20-dione, and the methods include combining the progestin compound with an estrogen compound to provide both contraception and treatment for myelin repair and neurodegeneration, and include effects on stroke and TBI. | 2013-05-09 |
| 20130116218 | METHODS AND COMPOSITIONS OF BILE ACIDS - Methods and compositions are provided for treating metabolic disorders by modulating bile acid levels. Generally, the methods and compositions can modulate bile acid levels, such as serum bile acid levels, to treat a metabolic disorder. In one embodiment, a method of modulating a bile acid level includes measuring a bile acid level and delivering a composition effective to modulate the bile acid level. A method for modulating a bile acid profile includes comparing a bile acid profile to a target profile and delivering a bile acid cocktail to increase bile acid levels. In another embodiment, a pharmaceutical composition for increasing bile acid levels includes a bile acid cocktail effective to increase bile acid levels. The composition is further useful as part of an implantable system. | 2013-05-09 |
| 20130116219 | ANTIMICROBIAL CARBOLINE COMPOUNDS - The invention provides compositions comprising carboline compounds for treating infections such as viral conjunctivitis. The invention also provides methods for treating of other infections, including ocular infections. More particularly, the present invention relates to compositions comprising carboline compounds for the treatment of ocular infections such as viral conjunctivitis, particularly those caused by adenovirus | 2013-05-09 |
| 20130116220 | Polymeric Pheromone Formulation and Method of Use to Calm Stress-Related Behavior in Mammals over an Extended Period of Time - Pheromone compositions comprising a combination of squalene, linoleic acid and 1-docosanol are described, along with methods of using the pheromone compositions to modify behavior in mammals. The compositions are useful for behavior modification in mammals that exhibit undesirable or harmful stress-related behaviors. | 2013-05-09 |
| 20130116221 | THEOBROMINE FOR INCREASING HDL-CHOLESTEROL - Theobromine for use in the treatment of increasing HDL-cholesterol and/or increasing the ratio HDL-cholesterol:LDL-cholesterol in humans and the use of theobromine for increasing HDL-cholesterol in humans, and/or for increasing the ratio HDL-C/LDL-C, and compositions comprising theobromine. | 2013-05-09 |
| 20130116222 | Dermal Delivery Compositions and Methods - A composition for transdermal delivery of a progestin for progestin hormone therapy is disclosed. Also disclosed is a transdermal delivery device comprising the composition. For progestin-only hormone therapy, the composition contains an anti-oxidant and does not contain an estrogen. For therapy involving a progestin and an estrogen, the composition contains the progestin, the estrogen and an additional anti-oxidant. Methods of improving the stability of progestin-containing compositions comprising oxidative agents are also disclosed. The methods comprise including one or more anti-oxidants in the compositions. | 2013-05-09 |
| 20130116223 | MEDICINAL COSMETIC LIPOATROPHY - Methods relating to local injections of corticosteroids are provided. More specifically intralesional injections of corticosteroids and preferably Triamcinolone and its derivatives are suitable to produce medicaments to be injected in the subcutaneous fat at deep levels to provoke cosmetic lipoatrophy of small fat deposits on the face and body. | 2013-05-09 |
| 20130116224 | Method and Composition for Treatment of Tumors - A method for ameliorating tumors which result from high or increased activity of Gli by treating a human subject evidencing tumor growth by treating the subject with a deactivating effective amount of CTC-96 to reduce or inhibit tumor growth. | 2013-05-09 |
| 20130116225 | METHOD FOR TREATING HEMATOLOGICAL CANCERS - Methods and compositions for treating hematological cancer are disclosed, including refractory or resistant hematological cancer. | 2013-05-09 |
| 20130116226 | METHOD FOR TREATING ESOPHAGEAL CANCER - Methods and compositions for treating gastric and esophageal cancers are disclosed. | 2013-05-09 |
| 20130116227 | BIARYL AMIDE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R | 2013-05-09 |
| 20130116228 | THIAZOLES AND PYRAZOLES USEFUL AS KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention. | 2013-05-09 |
| 20130116229 | NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A - The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. | 2013-05-09 |
| 20130116230 | 3-AMINOPYRROLIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTORS - The present invention relates to 3-aminopyrrolidine derivatives of the formula I: | 2013-05-09 |
| 20130116231 | TYROSINE KINASE INHIBITORS - The present invention relates to 1,4-dihydropyridazinone derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals. | 2013-05-09 |
| 20130116232 | ESTROGEN RECEPTOR MODULATORS AND USES THEREOF - Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors. | 2013-05-09 |
| 20130116233 | NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A - The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. | 2013-05-09 |
| 20130116234 | ARYL-QUINOLINE DERIVATIVES - The invention provides novel compounds having the general formula (I) | 2013-05-09 |
| 20130116235 | HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS - Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X | 2013-05-09 |
| 20130116236 | NOVEL [1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES - The invention relates to a compound of formula (I) | 2013-05-09 |
| 20130116237 | [6,6] AND [6,7]-BICYCLIC GPR119 G PROTEIN-COUPLED RECEPTOR AGONISTS - Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: | 2013-05-09 |
| 20130116238 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 2013-05-09 |
| 20130116239 | IVABRADINE-CONTAINING PHARMACEUTICAL COMPOSITION WITH MODIFIED RELEASE - The present invention relates to pharmaceutical compositions with delayed release which contain ivabradine adipate as active substance. The present invention furthermore relates to processes for the preparation of this composition and certain salts of ivabradine. | 2013-05-09 |
| 20130116240 | INDOLE COMPOUNDS AND PHARMACEUTICAL USE THEREOF - Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. | 2013-05-09 |
| 20130116241 | NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A - The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. | 2013-05-09 |
| 20130116242 | METHOD OF TREATMENT OF HORMONE DEPLETION INDUCED VASOMOTOR - The invention provides a method to effectively wean a woman from hormone therapy for treatment of vasomotor symptoms by reducing the dosage of the hormonal agent to zero, while a non-hormonal drug in an amount, which is therapeutically effective for treating vasomotor symptoms, is administered or initiated and continued for a limited period of a duration between 3 and 8 months. | 2013-05-09 |
| 20130116243 | INHIBITORS OF AKT ACTIVITY - The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer. | 2013-05-09 |
| 20130116244 | PHARMACEUTICAL POWDER COMPOSITIONS - The present invention provides a powder composition for the buccal delivery comprising a drug compound, a muco-adhesive agent and a dispersing agent Suitable compounds drugs include benzodiazepine compounds. Suitable muco-adhesive agents include those selected from (t) esters and salts of alginic acid and (it) hydroxyethyl cellulose. Suitable dispersing agents include those selected from ethylene oxide-propylene oxide copolymers. | 2013-05-09 |
| 20130116245 | ALKYLATED PIPERAZINE COMPOUNDS - Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 2013-05-09 |
| 20130116246 | 8-FLUOROPHTHALAZIN-1(2H)-ONE COMPOUNDS - 8-Fluorophthalazin-1(2h)-one compounds of Formula II where one or two of X | 2013-05-09 |
| 20130116247 | IRE-1alpha INHIBITORS - Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts there-of. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies. | 2013-05-09 |
| 20130116248 | SUBSTITUTED IMIDAZOQUINOLINE DERIVATIVES AS KINASE INHIBITORS - The present invention relates to substituted imidazo[4,5-c]quinoline derivatives, the compounds of formula (I), wherein R | 2013-05-09 |
| 20130116249 | INDOLIZINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to compounds corresponding to formula (I): | 2013-05-09 |
| 20130116250 | IMIDAZOPYRIDINE DERIVATIVES, PROCESS FOR PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to compounds corresponding to formula (I): | 2013-05-09 |
| 20130116251 | Novel HSP90 Inhibitor - Disclosed is a triazole derivative(s) represented by the general formula (1) below or a pharmacologically acceptable salt(s) thereof. Also disclosed are a prodrug(s) of such a triazole derivative(s) and an HSP90 inhibitor(s) containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkynyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or alkyl group or the like.) | 2013-05-09 |
| 20130116252 | Novel HSP90 Inhibitor - Disclosed is a triazole derivative(s) represented by the general formula (1) below or a pharmacologically acceptable salt(s) thereof. Also disclosed are a prodrug(s) of such a triazole derivative(s) and an HSP90 inhibitor(s) containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkynyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or alkyl group or the like.) | 2013-05-09 |
| 20130116253 | Novel HSP90 Inhibitor - Disclosed is a triazole derivative(s) represented by the general formula (1) below or a pharmacologically acceptable salt(s) thereof. Also disclosed are a prodrug(s) of such a triazole derivative(s) and an HSP90 inhibitor(s) containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkynyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or alkyl group or the like.) | 2013-05-09 |
| 20130116254 | COMPOSITIONS AND METHODS FOR LOWERING INTRAOCULAR PRESSURE - Disclosed herein are compositions for lowering intraocular pressure (IOP) of an eye comprising a combination of the IOP-lowering agents bimatoprost, brimonidine, and timolol. Further disclosed are methods for reducing IOP in the eye of a subject. | 2013-05-09 |
| 20130116255 | 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. | 2013-05-09 |
| 20130116256 | HEXENONE COMPOUNDS AND MEDICAL USE THEREOF - The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof; to a composition comprising a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluent; and also to use of a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, or preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, or preventing or treating a disease or disorder associated with cardiomyocyte apoptosis. | 2013-05-09 |
| 20130116257 | METHOD FOR TREATING A PULMONARY HYPERTENSION CONDITION - A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years. | 2013-05-09 |
| 20130116258 | ANDROGEN RECEPTOR MODULATORS AND USES THEREOF - Described herein are compounds that are androgen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such androgen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon androgen receptors. | 2013-05-09 |
| 20130116259 | COMBINATION THERAPY FOR TREATING OR PREVENTING AN INFLAMMATORY SKIN DISORDER - Methods and compositions for improved treatment and prevention of an inflammatory skin disorder or a sign and/or symptom associated with the skin disorder are described. The methods involve topical application to the skin a combination of a therapeutically effective amount of an α2 adrenergic receptor agonist, such as brimonidine, and a therapeutically effective amount of a non-steroidal anti-inflammatory agent, such as diclofenac. | 2013-05-09 |
| 20130116260 | FUSED HETEROAROMATIC PYRROLIDINONES AS SYK INHIBITORS - Disclosed are compounds of Formula 1, | 2013-05-09 |
| 20130116261 | NANOPARTICLES FOR ENCAPSULATION OF COMPOUNDS, THE PRODUCTION AND USES THEREOF - The present invention relates to nanoparticles for the encapsulation of compounds, the obtaining and uses thereof. The nanoparticles comprise a zein matrix and a basic amino acid. Said nanoparticles can encapsulate a water-soluble or fat-soluble biologically active compound. It is applicable in the food, pharmaceutical and cosmetic sectors and in the nanotechnology sector. | 2013-05-09 |
| 20130116262 | BICYCLIC PIPERAZINE COMPOUNDS - Bicyclic piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 2013-05-09 |
| 20130116263 | PAK INHIBITORS FOR THE TREATMENT OF CELL PROLIFERATIVE DISORDERS - Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of cell proliferative disorders and/or CNS disorders. | 2013-05-09 |
| 20130116264 | Novel Hetaryl (thio)carboxamide Compounds for Controlling Invertebrate Pests - The present invention relates to hetaryl (thio)carboxamide compounds of formula I, to the tautomers and N-oxides thereof and to the salts thereof: | 2013-05-09 |
| 20130116265 | COMPOUND FOR INHIBITING TYPE 5 PHOSPHODIESTERASE AND PREPARATION METHOD THEREOF - The present invention discloses a compound of formula (I) and citrate thereof as type 5 phosphodiesterase inhibitor, a preparation method thereof, and a pharmaceutical composition including the compound of formula (I) and citrate thereof. The experimental results of the present invention prove that the compound of formula (I) and citrate thereof can inhibit activity of type 5 phosphodiesterase, and can be used for treating erectile dysfunction, inhibiting platelet aggregation and treating thrombosis, decreasing pulmonary hypertension and treating cardiovascular diseases, treating asthma and treating diabetes gastroparesis. | 2013-05-09 |
| 20130116266 | QUINAZOLINONES AS INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA - Compounds that inhibit P13Kδ activity, including compounds that selectively inhibit P13Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (P13Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which P13Kδ plays a role in leukocyte function, using the compounds also are disclosed. | 2013-05-09 |
| 20130116267 | Role of PI3K P110 Delta Signaling in Retroviral Infection and Replication - The invention includes compositions and methods for regulating PI3K p110 delta as an anti-retroviral therapy. The invention includes a method of inhibiting p110 delta, a component of PI3K p110 delta signaling pathway, or any combination thereof in a cell as an anti-retroviral therapeutic approach for treating a retroviral infection, for example HTV. The invention includes a method of modulating PI3K p110 delta in a cell infected with a retrovirus by contacting the cell with an effective amount of a composition comprising an inhibitor of PI3K P110 delta. | 2013-05-09 |
| 20130116268 | USE OF MODIFIED PYRIMIDINE COMPOUNDS TO PROMOTE STEM CELL MIGRATION AND PROLIFERATION - Disclosed herein are methods and materials for improving vision. Particularly exemplified herein are pyrimidine compounds that serve to proliferate retinal stem cells. | 2013-05-09 |
| 20130116269 | CYCLIC N,N'-DIARYLTHIOUREAS AND N,N'-DIARYLUREAS - ANDROGEN RECEPTOR ANTAGONISTS, ANTICANCER AGENT, METHOD FOR PREPARATION AND USE THEREOF - The present invention relates to novel cyclic N,N′-diarylureas and N,N′-diarylthioureas—androgen receptor antagonists, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of cancerous diseases, among them prostate cancer. | 2013-05-09 |
| 20130116270 | NOVEL COMPOUNDS - The invention relates to novel spirocyclic derivatives with affinity for Ca.,2.2 calcium channels and which are capable of interfering with Ca | 2013-05-09 |
| 20130116271 | TACROLIMUS-CONTAINING OIL-IN-WATER TYPE CREAMY COMPOSITION - The purpose is to provide a tacrolimus-containing pharmaceutical composition which is a creamy preparation for external application having good feeling upon use and has high stability of a main ingredient contained therein (high main ingredient residual ratio), and allows easy control of skin concentration of the main ingredient. | 2013-05-09 |
| 20130116272 | HETEROCYCLIC FUSED PHENANTHROLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to heterocyclic fused phenanthrolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 2013-05-09 |
| 20130116273 | BETA CARBOLINE DERIVATIVES USEFUL IN THE TREATMENT OF PROLIFERATIVE DISORDERS - The invention provides novel beta-carboline derivatives of formulae (Ia) and (Ib) useful in the treatment of proliferative disorders including cancer, intermediates used in their preparation, processes for preparing the same and uses thereof. | 2013-05-09 |
| 20130116274 | THERAPEUTIC COMBINATIONS CONTAINING RILUZOLE - Disclosed is a method of treating melanoma in a mammal comprising administering (a) a therapeutically effective amount of an inhibitor of metabotropic glutamate receptor 1 (GRM1); and (b) a therapeutically effective amount of an inhibitor of at least one downstream signaling target of GRM1. Also disclosed are compositions and kits for treating melanoma comprising (a) a therapeutically effective amount of an inhibitor of GRM1; and (b) a therapeutically effective amount of an inhibitor of at least one downstream signaling target of GRM1. | 2013-05-09 |
| 20130116275 | INHIBITORS OF HIF AND ANGIOGENESIS - Inhibitors of the Hypoxia Inducible Factor (HIF) and angiogenesis and their methods of use including the treatment of cancer, hypoxia related pathologies, disorders leading to ischemia, for example stroke and ischemic heart disease, and non-cancerous angiogenic diseases are provided. | 2013-05-09 |
| 20130116276 | New use of neferine - The present invention reveals a new use of neferine. Neferine regulates M8 and V1 subtype of transient receptor potential ion channel (TRPM8 and TRPV1), respectively, in mammalians, including humans, and can be used for preparing medicaments for treating disease related to said ion channel (such as hyperalgesia, Parkinson's disease, painful bladder syndrome, chronic obstructive pulmonary disease, and tumor of skin, prostate, mammary gland, lung, colon, etc). The potency of neferine in the present invention is higher than that of hexahydrothymol. | 2013-05-09 |
| 20130116277 | ALDO-KETO REDUCTASE SUBFAMILY 1C3 (AKR1C3) INHIBITORS - The present invention relates to a novel class of AKR1C3 inhibitors, to compositions containing them, to methods for their preparation, and to methods of use thereof. The AKR1C3 inhibitors may be useful in the treatment of, for example, prostate cancer, benign prostate hyperplasia (BPH), lung cancer, acne, seborrhea, hirsuitism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, uterine cancer, uterine fibroids, endometriosis, myeloma and leiomyoma. | 2013-05-09 |
| 20130116278 | ANTIMICROBIAL AGENTS - The invention provides a compound of formula (I): or a salt or prodrug thereof, wherein R | 2013-05-09 |
| 20130116279 | BICYCLIC HETEROARYL INHIBITORS OF PDE4 - The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators. | 2013-05-09 |
| 20130116280 | Fusion protein comprising C-terminal domain of RET protein and use thereof as a diagnosing marker - A fusion protein including N-terminal domain of a fusion partner at N-terminal and C-terminal domain of RET protein at C-terminal, a fusion gene encoding the fusion protein, and a use of the fusion protein or the fusion gene as a diagnosing marker for a cancer, are provided. | 2013-05-09 |
| 20130116281 | Multiphoton Activable Quinoline Derivatives, Their Preparation and Their Uses - The present invention relates to multiphoton activable organic compounds responding to the following formula (I). The present invention also relates to a method of synthesizing the compounds of the invention, to an aqueous solution comprising at least one compound of the invention, and to their specific uses. The present invention also concerns a method of liberating organic ligands, said method involving the step of irradiating a compound according to the invention. | 2013-05-09 |
| 20130116282 | BUCKWHEAT EXTRACT ENRICHED IN D-FAGOMINE - The buckwheat extract comprises a extract of buckwheat which are enriched in | 2013-05-09 |
| 20130116283 | Substituted indole derivatives - Substituted indole derivatives, processes for the preparation thereof, medicinal products and pharmaceutical compositions containing these compounds and the use of substituted indole derivatives to treat pain and other conditions and for other medical purposes. | 2013-05-09 |
| 20130116284 | LIPOIC ACID AND NITROXIDE DERIVATIVES AND USES THEREOF - Provided are bifunctional compounds comprising a poly(ADP-ribose) polymerase (PARP) inhibitor moiety and a reactive oxygen species (ROS) scavenger moiety, more particularly, a lipoic acid or cyclic nitroxide derivative, covalently attached either directly or via a linker, as well as pharmaceutical compositions comprising them. The compounds and pharmaceutical compositions are useful for prevention, treatment, or management of diseases, disorders and conditions associated with elevated PARP activity or expression. | 2013-05-09 |
| 20130116285 | Chemical Compounds - The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula 10 (I):(I) or a pharmaceutically acceptable salt thereof, wherein Z, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain. | 2013-05-09 |
| 20130116286 | DROXIDOPA AND PHARMACEUTICAL COMPOSITION THEREOF FOR THE TREATMENT OF NEURALLY MEDIATED HYPOTENSION - The present invention is directed to methods of treating neurally mediated hypotension. In particular, the invention provides pharmaceutical compositions comprising droxidopa alone, or in combination with one or more further active ingredients, that can be administered to a patient for the treatment of neurally mediated hypotension. | 2013-05-09 |
| 20130116287 | FUNGICIDE HYDROXIMOYL-HETEROCYCLES DERIVATIVES - The present invention relates to hydroximoyl-heterocycle derivatives of formula (I) | 2013-05-09 |
| 20130116288 | Selective Androgen Receptor Modulators - This invention provides compounds of formulas I, Ia, Ib, Ic, Id, Ie, If or Ig or salts thereof, pharmaceutical compositions comprising a compound of formulas I, Ia, Ib, Ic, Id, If or Ig and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of formulas I, Ia, Ib, Ic, Id, Ie, If or Ig and intermediates useful in the preparation of same. | 2013-05-09 |
| 20130116289 | 5-(BIPHENYL-4-YL)-3-PHENYL-1,2,4-OXADIAZOLYL DERIVATIVES AS LIGANDS ON THE SPHINGOSINE 1-PHOSPHATE(SIP)RECEPTORS - The present invention provides compounds of Formula (I), as selective S1P1 inhibitors, as well as their use for treating multiple sclerosis and other diseases. | 2013-05-09 |
| 20130116290 | Use of Dipeptidyl Peptidase IV Effectors for Normalizing the Blood Glucose Level in Mammals - The present invention comprises the use of activity-reducing effectors of dipeptidyl peptidase (DP IV) and DP IV-analogous enzyme activity in the blood of a mammal to lower elevated post-prandial and basal blood glucose levels in mammalian organisms. The invention further comprises the use of activity-reducing effectors of dipeptidyl peptidase (DP IV) and DP IV-analogous enzyme activity in the blood of a mammal to increase the half-life of incretins in vivo. | 2013-05-09 |
| 20130116291 | ASSOCIATION OF XANTHINE OXIDASE INHIBITORS AND STATINS AND USE THEREOF - The present invention relates to the association of active principles, i.e. of a xanthine oxidase inhibitor with one or more HMG CoA reductase inhibitors, pharmaceutical compositions comprising said active principles, for use in a human or veterinary therapeutic treatment, and methods for the preparation thereof. | 2013-05-09 |
| 20130116292 | NEURORESTORATION WITH R(+) PRAMIPEXOLE - Formulations and methods of use thereof for restoring neuronal, muscular (cardiac and striated) and/or retinal tissue function in children and adults afflicted with chronic neurodegenerative diseases, such as neurodegenerative movement disorders and ataxias, seizure disorders, motor neuron diseases, and inflammatory demyelinating disorders, are described herein. Examples of disorders include Alzheimer's disease (AD), Parkinson's disease (PD), and amyotrophic lateral sclerosis (ALS). The method involves administering a pharmaceutical composition containing an effective amount of a tetrahydrobenzathiazole, preferably a formulation consisting substantially of the R(+) enantiomer of pramipexole. R(+) pramipexole is generally administered in doses ranging from 0.1-300 mg/kg/daily, preferably 0.5-50 mg/kg/daily, and most preferably 1-10 mg/kg/daily for oral administration. Daily total doses administered orally are typically between 10 mg and 500 mg. Alternatively, R(+) pramipexole can be administered parenterally to humans with acute brain injury in single doses between 10 mg and 100 mg, and/or by continuous intravenous infusions between 10 mg/day and 500 mg/day. | 2013-05-09 |
| 20130116293 | High-Throughput Methods for Determining Pharmacological Levels of Plasma D-Serine - Described herein are high-throughput methods of monitoring D-serine levels in plasma. The assay involves the use of strong cation solid phase extraction (SPE) to isolate D-serine from plasma, followed by quantitation of D-serine using the D-amino acid oxidase-(DAAO-) catalyzed reaction. Also described are methods of screening for compounds that act as DAAO inhibitors. | 2013-05-09 |
