18th week of 2016 patent applcation highlights part 23 |
Patent application number | Title | Published |
20160122299 | INITIATOR NANOCONSTITUENTS FOR ELASTOMER CROSSLINKING AND RELATED METHODS AND ARTICLES - An initiator nanoconstituent comprises a nanoparticle covalently bonded to a group having a free radical. The nanoparticle may be bonded to the group via an ether group or an amide group. The initiator nanoconstituent may be formed in situ, in a mixture comprising an elastomer material to be crosslinked. The initiator nanoconstituent is formed from an organic nanoconstituent compound that includes the nanoparticle and an organic group that does not include a free radical at the time the mixture is formed. At least one chemical bond of the organic nanoconstituent compound may be ruptured, in situ, to form the initiator nanoconstituent, which may then bond with polymer molecules of the elastomer material and form a crosslinked elastomer material. Downhole tools or components thereof may include such crosslinked elastomer material. | 2016-05-05 |
20160122300 | ACETYLCHOLINESTERASE INHIBITOR COMPOUNDS AND 5HT4 SEROTONERGIC RECEPTOR AGONISTS, WITH PROMNSIA EFFECT, METHODS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME - Compounds are provided according to Formula (I) | 2016-05-05 |
20160122301 | LIQUID CRYSTAL COMPOSITION AND LIQUID CRYSTAL DISPLAY DEVICE - A liquid crystal composition satisfying at least one of characteristics such as a high maximum temperature of a nematic phase, a low minimum temperature of the nematic phase, a small viscosity, a suitable optical anisotropy, a large negative dielectric anisotropy, a large specific resistance, a high stability to ultraviolet light and a high stability to heat, or a liquid crystal composition having a suitable balance regarding at least two of the characteristics. | 2016-05-05 |
20160122302 | Mammalian and Bacterial Nitric Oxide Synthase Inhibitors - Compounds and related methods for inhibition of mammalian and bacterial nitric oxide synthase. | 2016-05-05 |
20160122303 | Biocatalyzed synthesis of the optically pure (R) and (S) 3-methyl-1,2,3,4-tetrahydroquinoline and their use as chiral synthons for the preparation of the antithrombic (21R)- and (21S)-argatroban - The present invention relates to the biocatalyzed synthesis of enantiomerically pure (3R) and (3S)-methyl-1,2,3,4-tetrahydroquinoline. Said enantiomerically pure compounds are useful as chiral synthons in organic synthesis and, in particular, for the preparation of diastereomerically pure (21R) and (21S)-agratroban and its analogues. New compounds used as intermediates in the process of the invention are also disclosed. | 2016-05-05 |
20160122304 | METHOD FOR THE PRODUCTION OF 3,5-BIS(FLUOROALKYL)PYRAZOLE DERIVATIVES - The present invention describes a novel method for preparing 3,5-bis(fluoroalkyl)pyrazole derivatives. | 2016-05-05 |
20160122305 | Topical Compositions and Methods of Use Thereof - The invention is generally directed to compositions useful for improving the aesthetic appearance of human skin and the use of those compounds for improving the appearance of human skin, including improving skin tone, reducing the appearance of dark circles under the eyes, and reducing inflammation in the skin. The compositions typically comprise adrenergic receptor agonists. | 2016-05-05 |
20160122306 | DENDRIMER LIKE AMINO AMIDES POSSESSING SODIUM CHANNEL BLOCKER ACTIVITY FOR THE TREATMENT OF DRY EYE AND OTHER MUCOSAL DISEASES - Sodium channel blockers represented by the formula: | 2016-05-05 |
20160122307 | PERHYDROQUINOXALINE DERIVATIVES - The present invention relates to perhydroquinoxaline compounds according to the general formula (1), their use as a medicament, in particular as analgesic, antipruritic and anti-inflammatory agents, and their preparation. | 2016-05-05 |
20160122308 | RIBONUCLEOTIDE REDUCTASE INHIBITORS AND METHODS OF USE - Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme, as well as methods of synthesizing these novel compounds. The compounds may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases. | 2016-05-05 |
20160122309 | EPOXIDATION METHODS - A method for the epoxidation of alkylenes is provided. The method makes use of an epoxidation catalyst comprising a support, silver, manganese and greater than 35 ppm sodium. The catalyst is produced by a method comprising impregnating the support with manganese prior to impregnating the support with sodium and impregnating the support with silver prior to, at the same time as, or after impregnation with manganese. A method for using the alkylene oxides for the production of 1,2-diols, 1,2-carbonates, 1,2-diol ethers is also provided. | 2016-05-05 |
20160122310 | PROCESS FOR THE MANUFACTURE OF EPOXY-MONOMERS AND EPOXIDES - A process for manufacturing epoxy monomers and/or epoxides in high yields and useful quality and chemical stability by dehydrochlorination of the corresponding chlorohydrins with an alkaline agent, producing the corresponding side product dry salt in a high purity, characterized in that the process comprises the following steps: a. Reaction of the chlorohydrins with the alkaline agent to form corresponding epoxides and the corresponding precipitated chloride salt; b. Dehydration, and optionally completing the reaction, of the reaction mixture of step (a), by use of an azeotropic agent, added to step (b) or generated in situ in step (a), resulting in the producing of a dehydrated reaction mixture; c. Separating the resulting chloride salt by filtration from the dehydrated reaction mixture (b) and d. Isolating the epoxide from the filtered liquid fraction. | 2016-05-05 |
20160122311 | SYNTHESIS OF COUMALIC ACID - A method to prepare coumalic acid comprising (a) heating a solution in dichloroethane of malic acid and sulfuric acid or a solution in dichloroethane of malic acid and a perfluorosulfonic acid or (b) adding an acid comprising sulfuric acid or a perfluorosulfonic acid to a solution of malic acid in dichloroethane to yield a solution that is heated for a period of time so as to convert the malic acid into a major amount of coumalic acid and, optionally, a minor amount of fumaric acid. | 2016-05-05 |
20160122312 | ANTI-VIRAL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF - Disclosed herein are compounds, pharmaceutical compositions, and methods for the treatment of viral infection, including RNA viral infection, as well as compounds, pharmaceutical compositions, and methods for modulating the RIG-I pathway in a subject and/or in cells. These compounds are isoflavone derivatives, typically substituted at the 3-position with an aryl group and at the 7-position with a heterofunctional group. | 2016-05-05 |
20160122313 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF DIABETES - The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for treating or preventing diabetes may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of metabolic syndrome, insulin resistance, glucose intolerance, hyperinsulinemia, diabetes mellitus, diabetes insipidus, hyperglycemia and diabetic complications. | 2016-05-05 |
20160122314 | HISTONE DEMETHYLASE INHIBITORS - The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted imidazole-pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase enzymes. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like. | 2016-05-05 |
20160122315 | CRYSTALLINE IMATINIB MESYLATE PROCESS - The present invention relates to a process for preparation of crystalline non-needle shaped Form-SA of Imatinib mesylate (I). | 2016-05-05 |
20160122316 | SERINE/THREONINE KINASE INHIBITORS - Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 2016-05-05 |
20160122317 | 1-SULFONYL PIPERIDINE DERIVATIVES AS MODULATORS OF PROKINETICIN RECEPTORS | 2016-05-05 |
20160122318 | ISOINDOLINE INHIBITORS OF ROR-GAMMA - Provided are novel compounds of Formula (I): | 2016-05-05 |
20160122319 | CYCLIC AMINOMETHYL PYRIMIDINE DERIVATIVE - The present invention provides a cyclic aminomethyl pyrimidine derivative and a pharmaceutically acceptable salt thereof with high selectivity for dopamine D | 2016-05-05 |
20160122320 | USEFUL COMBINATIONS OF MONOBACTAM ANTIBIOTICS WITH BETA-LACTAMASE INHIBITORS - A pharmaceutical composition, comprising a combination of an antibiotically active compound of the formula (I): with a β-lactamase inhibitor of one of the formulae (II) to (XIII) are active against Gram-negative bacteria, in particular such bacteria which have become resistant against antibiotics such as aztreonam, carumonam and tigemonam. Optionally the compositions may comprise another β-lactamase inhibitor of one of the formulae (II) to (XIII), particularly of formula (V) or formula (VI). | 2016-05-05 |
20160122321 | Carboxamide Compounds and Methods for Using the Same - Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure | 2016-05-05 |
20160122322 | AZETIDINYLOXYPHENYLPYRROLIDINE COMPOUNDS - The invention provides certain azetidinyloxyphenylpyrrolidine compounds, particularly compounds of formula I wherein R is hydrogen or methyl, and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat overactive bladder. | 2016-05-05 |
20160122323 | INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7) - The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma, lung cancer), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject. | 2016-05-05 |
20160122324 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf. | 2016-05-05 |
20160122325 | Hydroxyalkyl-substituted phenyltriazole derivatives and uses thereof - The present invention relates to novel 5-(hydroxyalkyl)-1-phenyl-1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular and renal diseases. | 2016-05-05 |
20160122326 | TRIAZOLE COMPOUNDS AND THEIR USE AS GAMMA SECRETASE MODULATORS - The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. The invention also relates to pharmaceutical compositions comprising these compounds, to processes for making these compounds, and to their use as medicaments for treatment and/or prevention of Aβ-related diseases. | 2016-05-05 |
20160122327 | STROBILURIN TYPE COMPOUNDS FOR COMBATING PHYTOPATHOGENIC FUNGI - The present invention relates to novel strobilurine type compounds I, processes for preparing these compounds, a use of compounds of the formula I and/or their agriculturally useful salts for controlling phytopathogenic fungi, to compositions comprising at least one such compound, to plant health applications, and to seeds coated with at least one such compound. | 2016-05-05 |
20160122328 | METHOD FOR PRODUCING AZOLE DERIVATIVE - In the present invention, a compound (I) is reacted with a base selected from the group consisting of a metal alkoxide, a metal hydride compound, an alkali metal, an organometallic compound of an alkali metal, an alkali metal amide, an alkali metal carbonate salt, an alkali earth metal carbonate salt, and a mixture of these to produce a compound (II). Thereafter, this reaction solution is mixed with a compound (III) and a sulfonium compound or a sulfoxonium compound in the presence of a base to obtain an azole derivative (V). | 2016-05-05 |
20160122329 | CRYSTALLINE FORMS OF AFATINIB DI-MALEATE - The present disclosure encompasses crystalline forms of Afatininb di-maleate and methods of their use. | 2016-05-05 |
20160122330 | PIPERIDINYL BENZOIMIDAZOLE DERIVATIVES AS MPGE-1 INHIBITORS - The compounds (R)-1-(5-chloro-6-methyl-1-(6-(trifluoromethyl)pyridin-2-yl)-1H-benzo[d]imidazol-2-yl)-N-(tetrahydrofuran-3-yl)piperidine-4-carboxamide and (R)-1-(6-chloro-1-methyl-1-(6-(trifluoromethyl)pyridin-2-yl)-1H-benzo[d]imidazol-2-yl)-N-(tetrahydrofuran-3-yl)piperidine-4-carboxamide, as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising any one of these compounds. The compounds are useful for the treatment and/or prevention of a disorder selected from an inflammatory disease; an autoimmune disease; pain; a breathing disorder; cancer; a cardiovascular disease; a neurodegenerative disease; a bone disease; a disorder due to familial adenomatous polyposis (FAP) condition; overactive bladder; fever; and inflammation-related anorexia. | 2016-05-05 |
20160122331 | SUBSTITUTED TETRAHYDROPYRANS AND METHOD OF USE - Compounds of formula (I) | 2016-05-05 |
20160122332 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF NEUROLOGICAL DISORDERS - The invention relates to the compounds of formula I and formula IA or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I and formula IA; and methods for treating or preventing neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of epilepsy, bipolar disorder, trigeminal neuralgia, attention-deficit hyperactivity disorder (ADHD), schizophrenia, neuropathic pain, seizures, bipolar disorder, mania, phantom limb syndrome, complex regional pain syndrome, paroxysmal extreme pain disorder, neuromyotonia, intermittent explosive disorder, borderline personality disorder, Myotonia congenita and post-traumatic stress disorder. | 2016-05-05 |
20160122333 | MULTISUBSTITUTED AROMATIC COMPOUNDS AS INHIBITORS OF THROMBIN - There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin. | 2016-05-05 |
20160122334 | INHIBITORS OF C-FMS KINASE - The invention is directed to compounds of Formula I: | 2016-05-05 |
20160122335 | AMIDE SUBSTITUTED THIAZOLES AS MODULATORS OF RORyt - The present invention comprises compounds of Formula I. | 2016-05-05 |
20160122336 | TRIFLUOROMETHYL ALCOHOLS AS MODULATORS OF RORyt - The present invention comprises compounds of Formula I. | 2016-05-05 |
20160122337 | 2-HETEROARYL CARBOXAMIDES - The invention relates to novel 2-heteroaryl carboxamides and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory. | 2016-05-05 |
20160122338 | NOVEL PHOTOCHROMIC TETRAHYDROINDOLIZINES - Photochromic tetrahydroindolizines (THIs) bearing dihydroisoquinoline derivatives as heterocyclic bases and central fluorene groups have been synthesized via different chemical and photochemical pathways. Three alternative pathways for the synthesis of the target photochromic THI-based pyridazinopyrrolo[1,2-b]isoquinolines via in situ trapping with hydrazine hydrate are also provided. High product yields are obtained using different Sonogashira-mediated coupling reactions provided herein. Low temperature multichannel UV-vis and flash photolysis techniques were used to detect the photochromic and kinetic properties of the synthesized system. | 2016-05-05 |
20160122339 | [1,2,4] TRIAZOL [4,3-A] PYRIDINE DERIVATIVE, PREPARATION METHOD THEREFOR OR MEDICAL APPLICATION THEREOF - Provided are [1,2,4]triazol[4,3-a]pyridine derivatives as shown in the general formula (I), a preparation method therefor, and a pharmaceutical composition containing the derivative, wherein the pharmaceutical composition is used as a therapeutic agent, and especially used as a c-Met inhibitor and an immunosuppressant. Each substituent in the general formula (I) is the same as that defined in the specification. | 2016-05-05 |
20160122340 | HISTONE DEACETYLASE INHIBITORS BASED ON DERIVATIVES OF TRICYCLIC POLYHYDROACRIDINE AND ANALOGS POSSESSING FUSED SATURATED FIVE-AND-SEVEN-MEMBERED RINGS - The present invention refers to compounds of formula (I): | 2016-05-05 |
20160122341 | 3-ARYL-SUBSTITUTED IMIDAZO[1,2-A]PYRIDINES AND THEIR USE - The present application relates to novel 3-aryl-substituted imidazo[1,2-a]pyridines, 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 treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders. | 2016-05-05 |
20160122342 | ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS - This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers. | 2016-05-05 |
20160122343 | Novel Pyridopyrimidinone Compounds for Modulating the Catalytic Activity of Histone Lysine Demethylases (KDMs) - The present invention provides a compound of Formula (I) being capable of modulating the activity of histone lysine demethylase (KDM), pharmaceutical compositions thereof, methods to prepare the said compounds, and the use of such compounds as a medicament. The compound of Formula (I) acts as KDM inhibitor with marked potency, thereby having an outstanding potential for a pharmaceutical intervention of cancer and any other diseases related to KDM dysregulation. | 2016-05-05 |
20160122344 | Novel 6,7-dihydrobenzo[a]quinolizin-2-one derivatives for the treatment and prophylaxis of hepatitis B virus infection - The invention provides novel compounds having the general formula: | 2016-05-05 |
20160122345 | DIHYDROPYRROLOPYRIDINE INHIBITORS OF ROR-GAMMA - Provided are novel compounds of Formula (I): | 2016-05-05 |
20160122346 | NOVEL 1,3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE DERIVATIVES SUBSTITUTED WITH HETEROCYCLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS - The present invention is concerned with novel 1,3-dihydro-2H-benzimidazol-2-one derivatives substituted with heterocycles having formula (I) | 2016-05-05 |
20160122347 | 4,6-DIAMINOPYRIMIDINE STIMULATORS OF SOLUBLE GUANYLATE CYCLASE - The present invention relates to new 4,6-diaminopyrimidine stimulators of soluble guanylate cyclase, pharmaceutical compositions thereof, and methods of use thereof. | 2016-05-05 |
20160122348 | COMPOUNDS AND ANTI-TUMOR NQO1 SUBSTRATES - Compounds of Formula (I) can be selectively lethal toward a variety of different cancer cell types. The compounds are useful for the management, treatment, control or adjunct treatment of diseases, where the selective lethality is beneficial in chemotherapeutic therapy. | 2016-05-05 |
20160122349 | MORPHINAN DERIVATIVE - The present invention relates to a morphinan derivative represented by the following general formula (I), wherein R | 2016-05-05 |
20160122350 | PROCESS FOR THE PREPARATION OF CHIRAL TERT-BUTYL 4-((1R,2S,5R)-6-(BENZYLOXY)-7-OXO-1,6-DIAZABICYCLO[3.2.1]OCTANE-2-CARBOXA- MIDO)PIPERIDINE-1-CARBOXYLATE DERIVATIVES AND (2S,5R)-7-OXO-N-PIPERIDIN-4-YL-6-(SULFOXY)-1,6-DIAZABICYCLO[3.2.1]OCTANE-- 2-CARBOXAMIDE - A process for the preparation of N-protected 6-(piperidin-4-ylcarbamoyl)piperidin-3-yl sulfonates of Formula (III): which comprises contacting a lactone of Formula (II): with an azacycloalkylamine of formula (II-Am): followed by contact with a sulfonyl halide of formula (II-Su): R | 2016-05-05 |
20160122351 | Substituted Pyrimidinium Compounds and Derivatives for Combating Animal Pests - Substituted pyrimidinium compounds of the general formula (I) and their uses for combating animal pests | 2016-05-05 |
20160122352 | POLYMORPHS - The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament. | 2016-05-05 |
20160122353 | HETEROCYCLIC COMPOUNDS AS PEST CONTROL AGENTS - The present application relates to the use of known and novel heterocyclic compounds for controlling animal pests, to novel heterocyclic compounds, to processes for preparation thereof and to the use thereof for controlling animal pests. | 2016-05-05 |
20160122354 | PROCESS FOR THE PREPARATION OF (3R,4R)-4-METHYL-3-(METHYL-7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL-AMINO)- -OXO-1-PIPERIDINEPROPANENITRILE AND ITS SALTS - The present invention relates to an improved 7H-pyrrolo[2,3-d]pyrimidin-4-yl-amino)-β-oxo-1-piperidine propanenitrile compound of formula-1 and its pharmaceutically acceptable salts. | 2016-05-05 |
20160122355 | CRYSTALLINE FORMS OF PEMETREXED DIACID AND MANUFACTURING PROCESSES THEREFOR - Crystalline forms of pemetrexed diacid are provided (Forms 1 and 2) which are readily produced for either laboratory-scale or industrial scale. Processes for the preparation of Forms 1 and 2 are also provided. | 2016-05-05 |
20160122356 | METHODS FOR THE PREPARATION OF RIBOSIDES - Provided are methods of preparing compounds and pharmaceutical compositions for treating Filoviridae virus infections The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections. | 2016-05-05 |
20160122357 | PYRIMIDO-DIAZEPINONE KINASE SCAFFOLD COMPOUNDS AND METHODS OF TREATING DISORDERS - The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), polo kinase 1, 2, 3, or 4, Ack1, Ack2, Abl, DCAMKL1, ABL1, Abl mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions. | 2016-05-05 |
20160122358 | NOVEL SUBSTITUTED PYRAZOLO-PIPERAZINES AS CASEIN KINASE 1 D/E INHIBITORS - The invention provides compounds of Formula (I): | 2016-05-05 |
20160122359 | SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF - Disclosed are compounds having enhanced potency in the modulation of NMD A receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed. | 2016-05-05 |
20160122360 | TETRAHYDRO-2H-PYRANO[3,2-C]ISOCHROMENE-6-ONES AND ANALOGS FOR THE TREATMENT OF INFLAMMATORY DISORDERS - The present invention relates to 2,3,4,4a-tetrahydro-3,4,8,10-tetrahydroxy-2-(hydroxymethyl)-9-methoxypyrano[3,2-c]isochromen-6(10bH)-one analogs of the Formula I, wherein, R, R′ and R″ are as herein described. In addition, the invention relates to methods of using compounds for treating or preventing various inflammatory disorders such as rheumatoid arthritis, inflammatory bowel disease, psoriasis, asthma and chronic obstructive pulmonary disorder. | 2016-05-05 |
20160122361 | PYRIMIDINE COMPOUNDS AS KINASE INHIBITORS - This disclosure relates to compounds, methods for their preparation, pharmaceutical compositions including these compounds and methods for the treatment of cellular proliferative disorders, including, but not limited to, cancer. | 2016-05-05 |
20160122362 | INHIBITORS OF PLASMODIUM FALCIPARUM EQUILIBRATIVE NUCLEOSIDE TRANSPORTER TYPE I AS ANTI-PARASITIC COMPOUNDS - Inhibitors of | 2016-05-05 |
20160122363 | NOVEL 6-BRIDGED HETEROARYLDIHYDROPYRIMIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION - The invention provides novel compounds having the general formula: | 2016-05-05 |
20160122364 | NOVEL GAK MODULATORS - The present invention relates to a class of novel isothiazolo[4,3-b]pyridine derivatives and a method for their preparation, as well as to pharmaceutical compositions comprising one or more of said isothiazolo[4,3-b]pyridine derivatives and one or more pharmaceutically acceptable excipients. The present invention further relates to the use of said novel isothiazolo[4,3-b]pyridine derivatives as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, cell-proliferative and neurodegenerative diseases. | 2016-05-05 |
20160122365 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. | 2016-05-05 |
20160122366 | BORONIC ACID INHIBITORS OF HIV PROTEASE - Protease inhibitors, particularly aspartyl protease inhibitors, and more particularly HIV protease inhibitors which are boronated to enhance activity or to enhance entry into cells. Compounds, prodrugs and salts thereof of this invention contain phenylboronate groups, in particular p-B(OH) | 2016-05-05 |
20160122367 | ANTIBACTERIAL POWDERS BASED ON ANIONIC SILICON OR TITANIUM DIOXIDE ADSORBED WITH PHARMACEUTICALLY ACTIVE CATIONS - The present invention relates to a dioxide silicon or titanium derivative of formula (I): (MO | 2016-05-05 |
20160122368 | CHROMATOGRAPHIC MATERIAL AND METHOD FOR PREPARATION THEREOF - A chromatographic material comprising a zwitterionic ligand covalently bound to a substrate, the ligand preferably has a formula II: | 2016-05-05 |
20160122369 | NOVEL AMINO-SILYL AMINE COMPOUND, METHOD FOR PREPARING THE SAME AND SILICON-CONTAINING THIN-FILM USING THE SAME - Provided are a novel amino-silyl amine compound, a method for preparing the same, and a silicon-containing thin-film using the same, wherein the amino-silyl amine compound has thermal stability and high volatility and is maintained in a liquid state at room temperature and under a pressure where handling is easy to thereby form a silicon-containing thin-film having high purity and excellent physical and electrical properties by various deposition methods. | 2016-05-05 |
20160122370 | BIMETALLIC COMPLEX COMPRISING CYCLOPENTADIENYL AND AMIDINE LIGANDS - The present invention relates to a new bimetallic complex of the formula (1) wherein: M is a group 4-6 metal R | 2016-05-05 |
20160122371 | LIGAND COMPOUND, CATALYST SYSTEM FOR OLEFIN OLIGOMERAZATION, AND METHOD FOR OLEFIN OLIGOMERIZATION USING THE SAME - This disclosure relates to a ligand compound, a catalyst system for olefin oligomerization, and a method for olefin oligomerization using the same. The catalyst system for olefin oligomerization according to the present invention has excellent catalytic activity, and yet, exhibits high selectivity to 1-hexene and 1-octene, thus enabling efficient preparation of alpha-olefin. | 2016-05-05 |
20160122372 | TRICYCLIC NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM - The present invention provides novel tricyclic nucleosides and oligomeric compounds prepared therefrom. Incorporation of one or more of the tricyclic nucleosides into an oligomeric compound is expected to enhance one or more properties of the oligomeric compound. Such oligomeric compounds can also be included in double stranded compositions. In certain embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA. | 2016-05-05 |
20160122373 | AN EFFICIENT PROCESS FOR SEPARATION OF DIASTEREOMERS OF 9-[(R)-2-[[(R,S)-[[(S)-1-(ISOPROPOXYCARBONYL)ETHYL]AMINO]-PHENOXYPHOSPHIN- YL] METHOXY]PROPYL]ADENINE - The present invention relates to an efficient process for the separation of diastereomers of 9-[(R)-2-[[(R,S)-[[(S)-1-(Isopropoxycarbonyl)ethyl]amino]-phenoxyphosphinyl]methoxy]propyl]adenine and to a process for preparing 9-[(R)-2-[[(R)-[[(S)-1-(Isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine and 9-[(R)-2-[[(S)-[[(S)-1-(Isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine. | 2016-05-05 |
20160122374 | METHODS FOR TREATING FILOVIRIDAE VIRUS INFECTIONS - Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula IV: | 2016-05-05 |
20160122375 | IMMOBILIZED METATHESIS TUNGSTEN CATALYSTS AND USE THEREOF IN OLEFIN METATHESIS - Compound of formula (I) wherein M is W; R | 2016-05-05 |
20160122376 | RUTHENIUM- OR OSMIUM-BASED COMPLEX CATALYSTS - The present invention provides novel ruthenium or osmium based complex structures with a unique combination of ligands comprising a Schiff-base type ligand, a N-heterocyclic carbene ligand and a CO ligand which can be prepared according to two different routes involving easily accessible starting materials and which represent excellent catalysts for hydrogenating unsaturated compounds, oligomers and polymers, in particular at unforeseeably low temperatures. | 2016-05-05 |
20160122377 | LIPID-BASED PLATINUM-N-HETEROCYCLIC CARBENE COMPOUNDS AND NANOPARTICLES - The present disclosure is in relation to the field of nanotechnology and cancer therapeutics. In particular, the present disclosure relates to carbene compounds, particularly platinum containing carbenes and corresponding nanoparticles thereof. The disclosure further relates to synthesis of said platinum containing carbenes, nanoparticles and compositions comprising said platinum containing carbenes/nanoparticles. The disclosure also relates to methods of managing cancer by employing aforesaid platinum based compounds, nanoparticles and compositions. | 2016-05-05 |
20160122378 | METHOD FOR PRODUCING BETA-HEMATIN CRYSTAL COMPRISING STEP OF HEATING - This invention provides a method of preparing a β-hematin crystal comprising a step of heating, the β-hematin crystal obtained by such method, and a vaccine adjuvant composition containing the β-hematin crystal. The β-hematin crystal has a needle-like morphology, it has an average particle size of 0.6 to 1.2 μm, and it exhibits main peaks characteristics for angles of diffraction (2θ) of 7.4°, 12.2°, 21.6°, and 24.1° in an X-ray diffraction pattern obtained by powder X-ray diffractometry with Cu—Kα rays (with each peak including a plus-minus 0.2° diffraction angle). | 2016-05-05 |
20160122379 | Renewable aromatics from lignocellulosic lignin - The present invention provides novel and improved processes for treating a lignocellulosic biomass or technical lignin using ionic liquids to obtain lignin breakdown products and polysaccharide biomass components. Recycling of ionic liquids can be included in the methods of the invention. | 2016-05-05 |
20160122380 | CYCLIC PHOSPHONATE SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES - The present invention relates to Cyclic Phosphonate Substituted Nucleoside Derivatives of Formula (I): (structure) and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein, as well as to compositions and methods of using the Cyclic Phosphonate Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient. | 2016-05-05 |
20160122381 | METHOD OF PREPARATION OF ANTIVIRAL COMPOUNDS AND USEFUL INTERMEDIATES THEREOF - The invention is directed to processes for synthesizing bicyclic nucleoside antiviral compounds and for synthesizing the intermediates used in the process. The invention is also directed to novel intermediate compounds useful in the process. The antiviral compounds are useful in the treatment of herpes zoster (i.e., varicella zoster virus, VZV, shingles) and for the prevention of post herpetic neuralgia (PHN) resulting from this viral infection. | 2016-05-05 |
20160122382 | PROCESSES FOR THE PREPARATION OF DEHYDROEPIANDROSTERONE AND ITS INTERMEDIATES - The present application relates to a regioselective and stereoselective processes for the preparation of dehydroepiandrosterone (DHEA) and processes for its intermediates. | 2016-05-05 |
20160122383 | Peptide Ligation - The invention relates to a process for introducing a thiol group a to a carbonyl group in a side chain of a protected a-amino acid, said protected a-amino acid having protecting groups on both the α-amine group and the a-carboxyl group. The process comprises a) if the side chain contains a functional group comprising a heteroatom bearing a hydrogen atom, protecting said functional group; b) treating the protected amino acid with a base of sufficient strength to abstract a hydrogen atom a to the carbonyl group, so as to form an anion; c) treating the anion with a reagent of structure Pr-S-L in which L is a leaving group and Pr is a thiol-protecting group, so as to introduce a Pr-S- group a to the carbonyl group; and d) converting the Pr-S- group to an H-S-(thiol) group. This process may be used to prepare ligated peptides. | 2016-05-05 |
20160122384 | Method For Purifying Antibody - The present invention relates to a method of purifying an antibody with high purity and high quality by removing impurities by sequential use of a cation-exchange column, a culture supernatant multilayer filter and an anion-exchange column without using a protein-A column that is an affinity chromatography column which is generally used for antibody purification. | 2016-05-05 |
20160122385 | METHODS OF INCREASING PROTEIN PURITY USING PROTEIN A BASED CHROMATOGRAPHY - The present invention provides methods for increasing purity of an Fc-containing protein by removing protein aggregates during the Protein A chromatography step used during the purification of the Fc-containing protein. | 2016-05-05 |
20160122386 | V1A RECEPTOR AGONISTS - Compounds of formula (I), salts thereof, and compositions and uses thereof are described. The compounds are useful as V1a vasopressin agonists, for the treatment of, e.g., complications of cirrhosis, including bacterial peritonitis, HRS2 and refractory ascites. | 2016-05-05 |
20160122387 | Angiotensin Peptide and Pharmaceutical Compositions for Disease Treatment - The present invention relates to the peptide (arg0) n-angiotensin-(1-7) [(arg0) n-Ang-(1-7)], where n is 1 to 10 (Xaa-Asp-Arg-Val-Tyr-Ile-His-Pro; SEQ ID NO:1 where Xaa represents 1 to 10 L-Arg residues), which is produced by inserting at least one arginine amino acid at the amino terminal position of Ang-(1-7), as well as pharmaceutical compositions containing this peptide and the use thereof for the treatment or prevention of diseases or disorders that are due or associated with reduced nitric oxide production. Non-limiting examples of these diseases or disorders are cardiopulmonary and liver diseases, vascular disorders, metabolic disorders, neural disorders, genito-urinary tract disorders, skeletal muscle disorders, kidney disorders, skin disorders, alopecia or tumors. The peptide is able to cause, for example, dilation of aortic and mesenteric vessels, reduction of mean arterial blood pressure, decrease of body weight gain, blockade of the development of visceral adiposity, reduced serum and liver cholesterol levels, the normalization of glucose intolerance and insulin resistance, and an anti-proliferative effect. The peptides of the invention, such as (arg0) n-Ang-(1-7), optionally can be associated with a carrier system or controlled drug release system. | 2016-05-05 |
20160122388 | CONOTOXIN PEPTIDES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF - The present disclosure describes analog conotoxin peptides of the α-contoxin peptide RgIA. These analog conotoxin peptides block the α9α10 subtype of the nicotinic acetylcholine receptor (nAChR) and can be used for treating pain, inflammatory conditions, inflammation, and/or cancer. | 2016-05-05 |
20160122389 | PEPTIDES WITH ANTAGONISTIC ACTIVITIES AGAINST NATURAL CXCR4 - A peptide effective in blocking the CXC-chemokine receptor 4 (CXCR4) mediated HIV-1 NL4-3 (X4-tropic) infection with an IC | 2016-05-05 |
20160122390 | A BIOMIMETIC PEPTIDE AND BIODEGRADABLE DELIVERY PLATFORM FOR THE TREATMENT OF ANGIOGENESIS- AND LYMPHANGIOGENESIS-DEPENDENT DISEASES - Mimetic peptides having anti-angiogenic and anti-tumorigenic properties and methods of their use for treating cancer, ocular diseases, such as age-related macular degeneration, and other-angiogenesis-dependent diseases are disclosed. More particularly, an isolated peptide comprising the amino acid sequence LRRFSTAPFAFIDINDVINF, which exhibits anti-angiogenic activity in endothelial cell proliferation, migration, adhesion, and tube formation assays, anti-migratory activity in human breast cancer cells in vitro, anti-angiogenic and anti-tumorigenic activity in vivo in breast cancer xenograft models, and age-related macular degeneration models is disclosed. The isolate peptide also exhibits anti-lymphangiogenic and directly anti-tumorigenic properties. | 2016-05-05 |
20160122391 | SHORT BETA-DEFENSIN-DERIVED PEPTIDES - The invention is directed to β-defensin-derived peptides and their use in modulating the activity of hematopoietic cells, particularly hematopoietic stem cells and progenitor cells. Specifically, the invention provides compositions and methods useful for promoting mobilization and transplantation of hematopoietic stem cells and progenitor cells. The invention further provides compositions and methods useful in the treatment of cancer. | 2016-05-05 |
20160122392 | POLYPEPTIDES FOR USE IN SELF-ASSEMBLING PROTEIN NANOSTRUCTURES - Synthetic nanostructures, polypeptides that are useful, for example, in making synthetic nanostructures, and methods for using such synthetic nanostructures are disclosed herein. | 2016-05-05 |
20160122393 | POLYPEPTIDES HAVING NUCLEIC ACID BINDING ACTIVITY - Polynucleotides having nucleic acid binding activity are provided. Methods of stabilizing a nucleic acid duplex are provided. Methods of promoting the annealing of complementary nucleic acid strands are provided. Methods of increasing the processivity of a DNA polymerase are provided. Methods of enhancing the activity of a nucleic acid modification enzyme are provided. Fusion proteins are provided. Methods of using fusion proteins are provided. Kits are provided. | 2016-05-05 |
20160122394 | FC RECEPTOR (FcRn) BINDING PEPTIDES AND USES THEREOF - The invention provided herein includes isolated polypeptides that specifically block the interaction between neonatal Fc receptor (FcRn) and albumin. Blocking the interaction treats diseases and conditions caused by increased amounts of albumin or modified albumin that possesses pathogenic properties wherein it is deemed desirable to decrease albumin levels. Accordingly, also provided are methods of using these isolated polypeptides to treat various diseases and conditions caused by increased amounts of albumin or modified albumin that possesses pathogenic properties. The invention provided herein also includes isolated polypeptides capable of binding to a non-IgG and non-albumin competitive site on an FcRn alpha 3 domain. These can be useful for tracking FcRn without inhibiting IgG or albumin binding or function. Accordingly, the invention also includes methods and systems to track FcRn without inhibiting IgG or albumin binding or function. | 2016-05-05 |
20160122395 | Immunogenic compositions and a process for producing same - The present invention provides a modified HIV envelope glycoprotein (Env) antigen or a lipid containing vehicle comprising same. The Env antigen comprises one of a second site suppressor mutation in residue 674 of the membrane proximal ectodomain region (MPER) of HIV gp41; a second site suppressor mutation which ablates a glycosylation site in the variable region (V1) region of gp120; or a second site suppressor mutation ablating a glycosylation site in the V1 region of gp120 and a second site suppressor mutation in residue 674 of the MPER of HIV gp41. It is preferred that the lipid containing vehicle is a HIVLP. | 2016-05-05 |
20160122396 | THERAPEUTIC HPV16 VACCINES - Provided is designer nucleic acid constructs and polypeptides that can be used as therapeutic vaccines against HPV16. | 2016-05-05 |
20160122397 | REPLIKIN-BASED COMPOUNDS FOR PREVENTION AND TREATMENT OF INFLUENZA AND METHODS OF DIFFERENTIATING INFECTIVITY AND LETHALITY IN INFLUENZA - The present invention provides methods of differentiating the infectivity and lethality of isolates of influenza virus and provides compounds for diagnosing, preventing, and treating outbreaks of influenza virus including compounds for diagnosing, preventing, and treating across different strains of influenza virus. | 2016-05-05 |
20160122398 | RECOMBINANT RSV ANTIGENS - This disclosure provides recombinant respiratory syncytial virus (RSV) antigens and methods for making and using them, including immunogenic compositions (e.g., vaccines) for the treatment and/or prevention of RSV infection. | 2016-05-05 |