28th week of 2015 patent applcation highlights part 17 |
Patent application number | Title | Published |
20150191427 | INHIBITORS OF HISTONE DEACETYLASE - The present invention relates to compounds of formula (I) or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein X | 2015-07-09 |
20150191428 | FLUOROPICOLINOYL FLUORIDES AND PROCESSES FOR THEIR PREPARATION - Provided herein are fluoropicolinoyl fluorides and processes for their preparation. In some embodiments, provided herein is a process for the preparation of 5-fluoro-6-aryl-picolinoyl fluorides from chloropicolinoyl chlorides. | 2015-07-09 |
20150191429 | Process for the Preparation of 6-(7-((1-Aminocyclopropyl)Methoxy)-6-Methoxyquinolin-4-Yloxy)-N-Methyl-1-- Naphthamide and Synthetic Intermediates Thereof - A process for the preparation in high yields and purity of the compound 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide of formula (I) and of the pharmaceutically acceptable salts thereof is described. The process has various advantages over those previously described, in particular it avoids the use of acyl azide intermediates and their Curtius rearrangement. Novel intermediates useful for the preparation of compound (I) are also described. | 2015-07-09 |
20150191430 | CONJUGATES OF HUPERZINE AND ANALOGS THEREOF - Compounds and compositions for treating neurodegenerative diseases are described. The compounds include a therapeutic agent covalently linked with huperzine or an analog thereof through a linker. Methods of preparing the compounds are described. Methods of treating a neurodegenerative disease by administering compounds and compositions including a therapeutic agent covalently linked with huperzine or an analog thereof are described. Methods for delivering a therapeutic agent by administering the therapeutic agent covalently linked to huperzine or an analog thereof are described. | 2015-07-09 |
20150191431 | N-[4-(Quinolin-4-yloxy)cyclohexyl(methyl)](hetero)arylcarboxamides as androgen receptor antagonists, production and use thereof as medicinal products - The invention relates to N-[4-(quinolin-4-yloxy)cyclohexyl(methyl)](hetero)arylcarboxamides, intermediates and methods for their production, use thereof for treating and/or preventing diseases and use thereof for producing medicinal products and use thereof for treating and/or preventing diseases, especially of hyperproliferative diseases. | 2015-07-09 |
20150191432 | PRMT5 INHIBITORS AND USES THEREOF - Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described. | 2015-07-09 |
20150191433 | PROCESSES FOR THE PREPARATION OF PESTICIDAL COMPOUNDS - The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds. | 2015-07-09 |
20150191434 | 3-CYCLOHEXENYL AND CYCLOHEXYL SUBSTITUTED INDOLE AND INDAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF - The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions. | 2015-07-09 |
20150191435 | DUAL-ACTING IMIDAZOLE ANTIHYPERTENSIVE AGENTS - The invention is directed to compounds having the formula: | 2015-07-09 |
20150191436 | N1-SULFONYL-5-FLUOROPYRIMIDINONE DERIVATIVES - This present disclosure is related to the field of N1-sulfonyl-5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides. | 2015-07-09 |
20150191437 | PROCESS FOR PREPARING ANTIVIRAL COMPOUNDS - This disclosure is directed to: (a) processes for preparing compounds and salts thereof that, inter alia, are useful for inhibiting hepatitis C virus (HCV); (b) intermediates useful for the preparation of the compounds and salts; (c) pharmaceutical compositions comprising the compounds or salts; and (d) methods of use of such compositions. | 2015-07-09 |
20150191438 | PREPARATION AND PHARMACEUTICALS OF BIPHENYL BENZAMIDE-DERIVED DERIVATIVES - The present invention provides a biphenyl benzamide-derived derivatives, which structure is selected from formula I or formula II | 2015-07-09 |
20150191439 | INHIBITORS TARGETING DRUG-RESISTANT INFLUENZA A - Provided are compounds according to formula (Ia) or (Ib) as described herein, that are capable of modulating the activity of influenza viruses (e.g., influenza A virus), for example, via interaction with the M2 transmembrane protein, and other similar viroporins. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds according to according to formulas (Ia′) or (Ib), as described herein. | 2015-07-09 |
20150191440 | ALKYLENE OXIDE PRODUCTION - A process for preparing an alkylene oxide comprising contacting an alkyl phenyl hydroperoxide with an alkene in an epoxidation reaction to obtain an alkylene oxide and an alkyl phenyl alcohol, wherein the alkyl phenyl hydroperoxide is prepared by a process comprising reacting an alkyl aryl compound and oxygen to produce a reaction mixture comprising alkyl phenyl hydroperoxide, alkyl aryl compound and oxygen; separating at least a part of the reaction mixture into a product stream comprising alkyl phenyl hydroperoxide and an alkyl aryl compound stream; mixing at least a part of the alkyl aryl compound stream with a basic aqueous solution; separating at least a part of the mixture of alkyl aryl compound and basic aqueous solution with the help of a coalescer to obtain an organic phase containing alkyl aryl compound, and an aqueous phase; and recycling at least a part of the organic phase to the reacting step. | 2015-07-09 |
20150191441 | PROCESS FOR THE PREPARATION OF KARANJA OIL-BASED EPOXY AND ACYLOXY COMPOUNDS AS LUBRICANT BASESTOCKS - The present invention relates to preparation of epoxy karanja oil, epoxy karanja fatty acid methyl esters and their acylated derivatives. Accordingly karanja oil and karanja fatty acid methyl esters were epoxidised using performic acid method. Karanja oil and its fatty acid methyl esters were also hydroxylated to prepare their acyloxy derivatives (C | 2015-07-09 |
20150191442 | ALKYLENE EPOXIDATION WITH MESOPOROUS CATALYSTS - A process for epoxidizing an olefin comprising contacting an olefin with an oxidant in the presence of an insoluble oxidation catalyst in a solvent system comprising an organic water-miscible solvent to form an alkylene oxide. The insoluble oxidation catalyst comprises a metal, preferably selected from the group consisting of tungsten, cerium, and niobium. The metal is directly incorporated within a solid mesoporous silicate support, such as one selected from the group consisting of KIT-5, KIT-6, and TUD-1. | 2015-07-09 |
20150191443 | GRISEOFULVIN DERIVATIVES - The present invention relates to compounds of the following general formula (I), or to a pharmaceutically acceptable salt thereof, as well as to the uses thereof as a drug, in particular for treating cancerous or precancerous hyperproliferative conditions, and to the pharmaceutical compositions containing same. | 2015-07-09 |
20150191444 | HETEROATOM CONTAINING CYCLIC DIMERS - The present invention provides cyclic dimers of alpha acids and polymers derived therefrom. Also provided are processes for preparing and methods of using the cyclic dimers and the polymers derived from the cyclic dimers. | 2015-07-09 |
20150191445 | ACYL-HYDRAZONE AND OXADIAZOLE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AND USES THEREOF - The present invention relates to acyl-hydrazone compounds, in particular 3,4,5-trimethoxyphenyl-hydrazide derivatives, as well as the oxadiazole analogs thereof and other similar compounds, and to the pharmaceutical use of the same for the treatment of various diseases associated with cell proliferation, such as leukemias, including acute lymphoblastic leukemia (ALL), tumours and inflammation. Acyl-hydrazones have been obtained having activity similar to that of the compound used as a standard in experiments (colchicine). The greater selectivity of the compounds according to the invention is an important feature, associated with fewer side effects than the pharmaceuticals used at present in clinical treatments. The synthetised acyl-hydrazones, more particularly the compounds 02 and 07, exhibited important antileukemic activity, which suggests 02 and 07 as candidates to pharmaceutical prototypes, or to pharmaceuticals for the treatment of leukemias, in particular acute lymphoblastic leukemia (ALL), tumours and other proliferative diseases, such as inflammation. The action mechanism of the most active compounds was determined by using DNA microarrays and subsequent tests indicated by the chip, besides selectivity studies in healthy human lymphocytes. | 2015-07-09 |
20150191446 | SELENO-COMPOUNDS AND THERAPEUTIC USES THEREOF - Compounds and compositions, useful as antioxidants and in particular to selenium containing compounds of formula (I): wherein n is 1, 2, or 3; m is 2, 3, 4, or 5; and each R] is independently-(optionally substituted C1-C3 alkylene)p-OH, where p is 0 or 1, or a salt thereof. These seleno-compounds may be used in the treatment of diseases or conditions associated with increased levels of oxidants produced by myeloperoxidase (MPA), such as for instance, atherosclerosis and diabetes. | 2015-07-09 |
20150191447 | Process for Preparing Pyridyl-Substituted Pyrazoles - The present invention relates to a process for preparing 1-pyridyl-substituted pyrazoles, comprising the reaction of acetyleneketones with pyridylhydrazine derivatives to give 1-pyridyl-substituted dihydro-1H-pyrazoles, the further reaction thereof with elimination of water to give 1-pyridyl-substituted trihalomethylpyrazoles, and the further processing thereof. | 2015-07-09 |
20150191448 | PROCESSES FOR THE PREPARATION OF PESTICIDAL COMPOUNDS - The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds. | 2015-07-09 |
20150191449 | SYNTHESIS OF THIOHYDANTOINS - A novel synthesis of the anti-androgen, A52, which has been found to be useful in the treatment of prostate cancer, is provided. A52 as well as structurally related analogs may be prepared via the inventive route. This new synthetic scheme may be used to prepare kilogram scale quantities of pure A52. | 2015-07-09 |
20150191450 | ISOQUINOLINE-5-CARBOXAMIDE DERIVATIVE HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASE - A compound selected from the group consisting of an isoquinoline-5-carboxamide derivative of formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate and a solvate thereof is effective for the prevention or treatment of diseases associated with abnormal cell growth, which are caused by abnormal activation of a protein kinases. | 2015-07-09 |
20150191451 | 4-(AZACYCLOALKYL)BENZENE-1,3-DIOL COMPOUNDS AS TYROSINASE INHIBITORS, PROCESS FOR THE PREPARATION THEREOF AND USE THEREOF IN HUMAN MEDICINE AND IN COSMETICS - 4-(Azacycloalkyl)benzene-1,3-diol compounds are described corresponding to general formula (I) below: | 2015-07-09 |
20150191452 | Selective NR2B Antagonists - The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system. | 2015-07-09 |
20150191453 | ASYMMETRICAL REVERSIBLE NEUROMUSCULAR BLOCKING AGENTS OF ULTRA-SHORT, SHORT, OR INTERMEDIATE DURATION - We describe ultra-short, short, and intermediate duration neuromuscular blocking compounds, reversible by cysteine or similar compounds, that are bisquaternary diesters of chlorofumaric, fumaric, or maleic acids where the quaternary groups are very different, creating a highly asymmetrical molecule where one quaternary includes an isoquinolinium ring system and the other includes a morpholinium, piperidinium, piperazinium, or pyrrolidinium system, pharmaceutical compositions, methods to use such compounds and compositions, and kits. | 2015-07-09 |
20150191454 | MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH) and related disorders; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD). | 2015-07-09 |
20150191455 | PYRAZOLYL SUBSTITUTED CARBONIC ACID DERIVATIVES AS MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH) and related disorders; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD). | 2015-07-09 |
20150191456 | AMIDE DERIVATIVE AND USE OF THE SAME AS STABILITY INDEX OF A LULICONAZOLE PHARMACEUTICAL FORMULATION - An object is to establish an index to prepare a stable pharmaceutical formulation by specifying a related substance of luliconazole which appears depending on the type of a selected solvent in the luliconazole pharmaceutical formulation and which is different from the SE form and the Z form. Disclosed is an amide derivative of luliconazole. | 2015-07-09 |
20150191457 | BISARYL (THIO)MORPHOLINE DERIVATIVES AS S1P MODULATORS - The present invention relates to bisaryl (thio)morpholine derivatives of the formula (I) wherein R1 is an aryl substitutent selected from phenyl, pyridyl, pyrimidinyl, biphenyl and naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino, —SO | 2015-07-09 |
20150191458 | TRIAZOLE CARBOXAMIDES AND USES THEREOF - The invention relates to compounds of formula | 2015-07-09 |
20150191459 | CATHEPSIN INHIBITORS - The present invention is directed to inhibitors of cathepsins and the methods for using and making such inhibitors. | 2015-07-09 |
20150191460 | N-(3-heteroarylaryl)-4-arylarylcarboxamides and Analogs as Hedgehog Pathway Inhibitors and Use Thereof - Disclosed are novel N-(3-heteroarylaryl)-4-arylarylcarboxamides and analogs thereof, represented by the Formula I: wherein C cyclic group, D | 2015-07-09 |
20150191461 | PYRAZOLYL DERIVATIVES AS SYK INHIBITORS - The present invention provides novel pyrazole derivatives of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer. | 2015-07-09 |
20150191462 | PYRROLIDINE DERIVATIVES AND THEIR USE AS COMPLEMENT PATHWAY MODULATORS - The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as complement alternative inhibitors for the treatment of ocular diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 2015-07-09 |
20150191463 | DIFLUOROMETHYLENE COMPOUND - The present invention relates to a compound having an URAT1 inhibitory activity, and to an URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition containing the compound. | 2015-07-09 |
20150191464 | HETEROARYL SUBSTITUTED NICOTINAMIDE COMPOUNDS - Disclosed are compounds of Formula (I) | 2015-07-09 |
20150191465 | AZAINDOLE DERIVATIVES - Disclosed are compounds of Formula 1, | 2015-07-09 |
20150191466 | TROPOMYOSIN-RELATED KINASE (TRK) INHIBITORS - Tropomyosin-related kinase inhibitors (Trk inhibitors) are small molecule compounds useful in the treatment of disease. Trk inhibitors can be used as pharmaceutical agents and in pharmaceutical compositions. Trk inhibitors are useful in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and/or cancer, and are particularly useful in the treatment of osteoarthritis (OA), pain, and pain associated with OA. Trk inhibitors are also useful for inhibiting tropomyosin-related kinase A (TrkA), tropomyosin-related kinase B (TrkB), tropomyosin-related kinase C (TrkC), and/or c-FMS (the cellular receptor for colony stimulating factor-1 (CSF-1)). | 2015-07-09 |
20150191467 | AGONISTS OF SRC HOMOLOGY-2 CONTAINING PROTEIN TYROSINE PHOSPHATASE-1 AND TREATMENT METHODS USING THE SAME - The present invention provides new compounds of formula I, II or III, which have Src homology-2 containing protein tyrosine phosphatase-1 (SHP-1) agonist activity. Also provided are treatment methods using the compounds of formula I, II or III. | 2015-07-09 |
20150191468 | INHIBITORS OF INFLUENZA VIRUSES REPLICATION - Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): | 2015-07-09 |
20150191469 | COMPOUNDS AND METHODS FOR TREATING HIV - Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV). | 2015-07-09 |
20150191470 | CRYSTALLINE BIPYRIDINIUM RADICAL COMPLEXES AND USES THEREOF - Described herein are methods of generating 4,4′-bipyridinium radical cations (BIPY | 2015-07-09 |
20150191471 | COMPOUNDS AND METHODS FOR TARGETING HSP90 - Described herein are compounds that may selectively bind to Hsp90, methods of using the compounds, and kits including the compounds. The compounds may include detection moieties such as fluorophores that may allow for selective detection of Hsp90 in a sample. | 2015-07-09 |
20150191472 | COMPOSITIONS AND METHODS FOR INHIBITING VIRAL POLYMERASE - Provided are compounds of Formula I: | 2015-07-09 |
20150191473 | PROTEIN KINASE INHIBITORS - The present invention relates to a novel family of inhibitors of protein kinases. In particular, the present invention relates to inhibitors of the members of the Tec and Src protein kinase families. | 2015-07-09 |
20150191474 | FUSED HETEROCYCLIC COMPOUND - The fused heterocyclic compound represented by formula (1) has excellent effectiveness in pest control. | 2015-07-09 |
20150191475 | Ticagrelor Adducts With Divalent Metal Salts - The present invention relates to amorphous adducts of ticagrelor with divalent metal salts useful in the treatment or prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease. | 2015-07-09 |
20150191476 | Imidazotriazinone Compounds - The present invention provides imidazotriazinone compounds which are inhibitors of phosphodiesterase 9 and pharmaceutically acceptable salt thereof. The present invention further provides processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of PDE9 associated diseases or disorders in mammals, including humans. | 2015-07-09 |
20150191477 | Fluoride Processing Method - The invention relates to methods for processing [ | 2015-07-09 |
20150191478 | FUSED RING COMPOUND CONTAINING FURAN OR SALT THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING SAME - The present invention provides a fused ring compound containing furan or a pharmaceutically acceptable salt thereof, a method for preparing same, a pharmaceutical composition comprising same, and a use thereof. The fused ring compound containing furan or a pharmaceutically acceptable salt thereof inhibits the activity of phosphatidylinositol 3-kinase (PI3K) and can therefore be used in a pharmaceutical composition for treating and preventing respiratory diseases, inflammatory diseases, proliferative diseases, cardiovascular diseases, or central nervous system diseases which occur due to the over-activation of PI3K. | 2015-07-09 |
20150191479 | DIHYDROFURO PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: | 2015-07-09 |
20150191480 | BENZODIOXOLE DERIVATIVE AND PREPARATION METHOD AND USE THEREOF - Provided in the present invention are novel benzodioxole derivatives and preparation methods thereof. These compounds represented by formula (I) or pharmaceutically acceptable salts thereof have acetylcholinesterase inhibitory activity, so can be used in the treatment or prevention of Alzheimer's disease. The definitions of R | 2015-07-09 |
20150191481 | HETEROCYCLIC FLAVONE DERIVATIVES, COMPOSITIONS, AND METHODS RELATED THERETO - In certain embodiments, the disclosure relates to heterocyclic flavone derivatives, such as those described by formula provided herein, pharmaceutical compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of 5 treating or preventing diseases or conditions related to BDNF and TrkB activity, such as depression, stroke, Rett syndrome, Parkinson's disease, and Alzheimer's disease by administering effective amounts of pharmaceutical compositions comprising compounds disclosed herein to a subject in need thereof. | 2015-07-09 |
20150191482 | Imidazopyrazine Derivatives as Modulators of TNF Activity - A series of imidazo[1,2-α]pyrazine derivatives, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorder; and oncological disorders. | 2015-07-09 |
20150191483 | PYRROLIDINYL SULFONE RORGAMMA MODULATORS - Described are RORγ modulators of the formula (I), | 2015-07-09 |
20150191484 | NOVEL COMPOUNDS HAVING A TETRACYCLIC IRIDOID SKELTON AND AN ANTI-TRYPANOSOMAL AGENT COMPRISING THE SAME AS AN ACTIVE INGREDIENT - The present invention provides anti-trypanosomal agent for treating, preventing Trypanosomiasis of mammals, which comprises a compound having the tetracyclic iridoid skeleton represented by a general formula (I). | 2015-07-09 |
20150191485 | Process for Preparing Enantiomerically Enriched Oxamides - The present invention relates to a chiral oxamide of formula (I) useful as an intermediate in the preparation of dorzolamide, and to the preparation thereof. The invention also relates to the preparation of dorzolamide, to the hydrochloride salt thereof, and to the active ingredient contained in a drug useful in the treatment of glaucoma, by means of the intermediate of formula (I). | 2015-07-09 |
20150191486 | HETEROCYCLIC COMPOUND AND USE THEREOF - Compounds represented by the formulas | 2015-07-09 |
20150191487 | TETRAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I: | 2015-07-09 |
20150191488 | METHODS FOR THE ACYLATION OF MAYTANSINOL - Disclosed is a method of preparing an amino acid ester of maytansinol by reacting maytansinol with an N-carboxyanhydride of an amino acid (NCA) in the presence of a drying agent. Also disclosed is an improved method of preparing an amino acid ester of maytansinol in which a nucleophile is added to the reaction mixture after completion of the reaction between maytansinol and an N-carboxyanhydride of an amino acid. | 2015-07-09 |
20150191489 | IMIDAZO BICYCLIC IMMINIUM COMPOUNDS AS ANTITUMOR AGENTS - Compounds of formula I: | 2015-07-09 |
20150191490 | MITOTIC KINESIN INHIBTORS AND METHODS OF USE THEREOF - This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders. | 2015-07-09 |
20150191491 | PREPARATION METHOD OF ZEOLITIC IMIDAZOLATE FRAMEWORK-90 IN WATER-BASED SYSTEM - The present invention provides a preparation method of Zeolitic Imidazolate Framework-90 (ZIF-90) in water-based system, which uses pure water as a solvent, and the reaction is carried out at room temperature. In addition, the present invention provides a preparation method of ZIF-90, and the particle size and the uniformity of the obtained ZIF-90 are controllable by addition of adjuvant or additive (Polyvinylpyrrolidone). | 2015-07-09 |
20150191492 | ARGINASE INHIBITORS AS THERAPEUTICS - Compounds according to Formula I are potent inhibitors of Arginase I and II activity: | 2015-07-09 |
20150191493 | NEW PROCESS FOR PREPARING ARYLBORANES BY ARYLATION OF ORGANOBORON COMPOUNDS - A new process for the preparation of an arylborane compound, by arylation of a B—H bond, which includes a step (1) of contacting an arenediazonium salt or a heteroarenediazonium salt with an organoboron compound containing at least one B—H bond, in a reaction medium containing a solvent, in the absence of base, in the absence or in the presence of an activating agent, for the preparation of an arylborane compound, and a possible step (2) of recovery and purification of the arylborane compound obtained at the step (1), the arylborane being in particular an aminoarylborane, and a possible step (3) of refunctionalization of the arylborane obtained at step (1) or (2) for the preparation of aryl boronic derivatives or arylborates. | 2015-07-09 |
20150191494 | TETRAHYDROISOQUINOLINES AND INTERMEDIATES THEREFOR - Disclosed are processes for preparing tetrahydroisoquinolines, intermediates useful in the preparation of tetrahydroisoquinolines, processes for preparing such intermediates, and a crystalline form of 6-[(4S)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. Also disclosed are pharmaceutical compositions comprising tetrahydroisoquinolines, methods of using tetrahydroisoquinolines in the treatment of depression and other conditions and methods for obtaining the crystalline form. | 2015-07-09 |
20150191495 | ANTIDIABETIC TRICYCLIC COMPOUNDS - Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia. | 2015-07-09 |
20150191496 | (R)-3-((3S,4S)-3-FLUORO-4-(4-HYDROXYPHENYL)PIPERIDIN-1-YL)-1-(4-METHYLBENZ- YL)PYRROLIDIN-2-ONE AND ITS PRODRUGS FOR THE TREATMENT OF PSYCHIATRIC DISORDERS - The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the NR2B NMDA receptor and may be useful for the treatment of various disorders of the central nervous system. | 2015-07-09 |
20150191497 | NOVEL PHOSPHORUS 2-PYRONE DERIVATIVE AND PREPARATION METHOD THEREOF - Provided are a novel phosphorus 2-pyrone derivative and a preparation method thereof. The phosphorus 2-pyrone derivative according to the present invention is capable of being efficiently synthesized by treating an alkyl hydrogen alkynylphosphonate derivative and an alkyne derivative with a minimal amount of a gold catalyst. | 2015-07-09 |
20150191498 | METHOD FOR DECOMPOSING PLANT BIOMASS, AND METHOD FOR PRODUCING GLUCOSE - A plant biomass; a solid catalyst which can catalyze the hydrolysis of the biomass; and a method for hydrolyzing a plant biomass, which is characterized by a step of heating a mixture containing an inorganic acid and water and which has high glucose yield and high glucose selectivity. As the inorganic acid, hydrochloric acid can be used. The pH value is adjusted to 1.0 to 4.0. As the solid catalyst, activated carbon or the like can be used. | 2015-07-09 |
20150191499 | COMPOSITIONS COMPRISING C5 AND C6 OLIGOSACCHARIDES - Compositions comprising C5 and C6 saccharides of varying degrees of polymerization and low levels of undesirable impurities, such as compounds containing sulfur, nitrogen, or metals, are disclosed. | 2015-07-09 |
20150191500 | COMPOSITIONS COMPRISING C5 AND C6 OLIGOSACCHARIDES - Compositions comprising C5 and C6 saccharides of varying degrees of polymerization and low levels of undesirable impurities, such as compounds containing sulfur, nitrogen, or metals, are disclosed. | 2015-07-09 |
20150191501 | ADVANCED GLYCATION END PRODUCT ANALOGUES - Disclosed are processes for the production of composition comprising one or more fructose amino acids, said process comprising the steps of: (a) providing plant material derived from a botanical source selected from plants of the families Solanaceae, Compositae, (Asteraceae), Guttiferae, Umbelliferae, Papaveraceae, Vitidaceae or Acanthaceae; (b) extracting one or more fructose amino acid(s) from said plant material; and optionally (c) detecting the presence and/or measuring the amount of said fructose amino acid(s) in the extract of step (b). | 2015-07-09 |
20150191502 | OPTICALLY PURE BENZYL-4-CHLOROPHENYL-C-GLUCOSIDE DERIVATIVE - The present invention belongs to the field of pharmaceutical technology, more specifically relates to optically pure benzyl-4-chlorophenyl-C-glucoside derivatives represented by formulae (II) and (III), a process for preparing these compounds and intermediates thereof, a pharmaceutical formulation and a pharmaceutical composition containing these compounds, and the use of the optically pure benzyl-4-chlorophenyl-C-glucoside derivative as a sodium glucose co-transporter (SGLT) inhibitor in manufacture of a medicament for treating and/or preventing diabetes mellitus (including insulin-dependent diabetes mellitus and non-insulin-dependent diabetes mellitus) or diabetes-associated diseases (including insulin resistance disease and obesity) | 2015-07-09 |
20150191503 | ORGANIC COMPOUNDS - This invention relates to sphingoglycolipid analogues, compositions comprising these compounds, processes for preparing the compounds, and methods of treating or preventing diseases or conditions using the compounds, such as diseases or conditions relating to infection, atopic disorders, autoimmune disease, diabetes or cancer. | 2015-07-09 |
20150191504 | PREPARATION METHOD OF DEGLYCOSYLATED GINSENOSIDES - The present invention provides a preparation method of deglycosylated ginsenosides, which uses the supercritical fluid technology to conduct the deglycosylation of ginsenosides extract in supercritical solvent under preset pressure and temperature conditions. Under the same operational conditions, the deglycosylated ginsenosides extract and solvent at supercritical state are input into an adsorption tank at the preset volume flow rate ratio for the adsorption of ginsenosides. Then, the adsorbed ginsenosides are applied with gradient eluent by using the ethanol solution. Finally, the pressure is lowered for the separation and purification of ginsenosides to get the deglycosylated ginsenosides of high concentration. | 2015-07-09 |
20150191505 | SURFACE NEUTRALIZATION OF APATITE - The present invention discloses methods of neutralizing apatite surfaces, for example during chromatography and before protein elution. | 2015-07-09 |
20150191506 | ADSORBENT CONSISTING OF CARRIER WHICH BOUND WITH POLYPEPTIDE COMPRISING B-DOMAIN MUTANT DERIVED FROM PROTEIN A - It is an object of the present invention to provide an affinity chromatographic adsorbent using temperature-responsive protein A, wherein the adsorbent is capable of improving the culture productivity of the temperature-responsive protein A and the stability of the temperature-responsive protein A in cell disruption solution. According to the present invention, there is provided an adsorbent consisting of a carrier, to which a polypeptide comprising a tag peptide, a linker sequence, and a B-domain mutant derived from protein A from the N-terminal side thereof binds, wherein the linker sequence is an amino acid sequence that does not comprise a Val-Pro-Arg sequence and is composed of 7 to 12 amino acid residues; and the binding property of the B-domain mutant derived from protein A to an immunoglobulin can vary depending on temperature under conditions of pH 5 to 9 and a temperature of lower than 60° C. | 2015-07-09 |
20150191507 | CYCLIC PENTADEPSIPEPTIDE DERIVATIVE AND FUSARIUM STRAIN PRODUCING THE SAME - Disclosed is a | 2015-07-09 |
20150191508 | Selective Delivery of Molecules into Cells or Marking of Cells in Diseased Tissue Regions Using Environmentally Sensitive Transmembrane Peptide - A polypeptide with a predominantly hydrophobic sequence long enough to span a membrane lipid bilayer as a transmembrane helix (TM) and comprising one or more dissociable groups inserts across a membrane spontaneously in a pH-dependant fashion placing one terminus inside cell. The polypeptide conjugated with various functional moieties delivers and accumulates them at cell membrane with low extracellular pH. The functional moiety conjugated with polypeptide terminus placed inside cell are translocated through the cell membrane in cytosol. The peptide and its variants or non-peptide analogs can be used to deliver therapeutic, prophylactic, diagnostic, imaging, gene regulation, cell regulation, or immunologic agents to or inside of cells in vitro or in vivo in tissue at low extracellular pH. | 2015-07-09 |
20150191509 | Compositions and Methods for the Treatment or Prevention of Hepatitis B Virus Infection - Disclosed are yeast-based immunotherapeutic compositions, hepatitis B virus (HBV) antigens, and fusion proteins for the treatment and/or prevention of HBV infection and symptoms thereof, as well as methods of using the yeast-based immunotherapeutic compositions, HBV antigens, and fusion proteins for the prophylactic and/or therapeutic treatment of HBV and/or symptoms thereof. | 2015-07-09 |
20150191510 | POLYPEPTIDES AND IMMUNIZING COMPOSITIONS CONTAINING BURKHOLDERIA POLYPEPTIDES AND METHODS OF USE - This disclosure provides isolated polypeptides isolatable from a | 2015-07-09 |
20150191511 | Genetically Modified Organisms to Produce Organic Compounds - Disclosed herein are embodiments for a genetically modified organism or cell line; a composition containing the same; and a method of harvesting at least one organic compound from an organism or cell line genetically engineered with an added gene for at least one carbon-fixing protein and at least one proton-pump protein. | 2015-07-09 |
20150191512 | RECOMBINANT BACTERIAL LIPOCALIN BLC AND USES THEREOF - The present inventors have solved the crystal structure of an | 2015-07-09 |
20150191513 | STABILISED PROTEINS FOR IMMUNISING AGAINST STAPHYLOCOCCUS AUREUS - Elimination of disulphide bond formation of cysteine-containing | 2015-07-09 |
20150191514 | HYR1-DERIVED COMPOSITIONS AND METHODS OF TREATMENT USING SAME - The disclosure features isolated polypeptides of Hyr1. The disclosure further features vaccines and antibodies useful in treating or preventing candidiasis or | 2015-07-09 |
20150191515 | Compositions and Methods for Modulating Biomass Productivity - The disclosure generally relates to methods and materials for modulating cell productivity. In particular, the present disclosure provides polynucleotides encoding transcription factor proteins that when overexpressed in microrganisms result in increased in productivity, such as increased biomass productivity. Also disclosed are methods of using the genetically engineered host strains to modulate or increase productivity of host cells such as, for example, algal or heterokont cells. Genetically engineered host cells, such as algal and heterokont cells having increased biomass productivity and bioproducts derived from such host cells are also disclosed. | 2015-07-09 |
20150191516 | LY6K EPITOPE PEPTIDES FOR TH1 CELLS AND VACCINES CONTAINING THE SAME - Isolated LY6K-derived epitope peptides having Th1 cell inducibility are disclosed herein. Such peptides can be recognized by MHC class II molecules and induce Th1 cells. In preferred embodiments, such a peptide of the present invention can be promiscuously bind to MHC class II molecules and induce LY6K-specific cytotoxic T lymphocytes (CTLs) in addition to Th1 cells. Such peptides are thus suitable for use in enhancing immune response in a subject, and accordingly find use in cancer immunotherapy, in particular, as cancer vaccines. Also disclosed herein are polynucleotides that encode any of the aforementioned peptides, APCs and Th1 cells induced by such peptides and methods of induction associated therewith. Pharmaceutical compositions that comprise any of the aforementioned components as active ingredients find use in the treatment and/or prevention of cancers or tumors. | 2015-07-09 |
20150191517 | NOVEL SODIUM CHANNEL BLOCKING PEPTIDES AND THE USE THEREOF - The present invention relates to C-terminal modified Protoxin II peptides that selectively inhibit the Nav1.7 sodium channel; the present invention also relates to pharmaceutical compositions useful for prophylactic or therapeutic treatment of a disorder responsive to the blockade of sodium ion channels, especially Nav1.7 sodium ion channels; the present invention further provides methods of treating a disorder responsive to the blockade of sodium channels, and particularly Nav1.7 sodium channels, in a mammal suffering from excess activity of said channels. | 2015-07-09 |
20150191518 | NOVEL MALARIA TRANSMISSION-BLOCKING VACCINES - Immunogenic compositions, vaccines, constructions, host cells, and vectors that include or express one or more PfGAP50 antigen or fragment thereof. The vaccine may include an adjuvant, a pharmaceutically acceptable salt, an excipient, a preservative, a binder or a pharmaceutically acceptable liquid. | 2015-07-09 |
20150191519 | VECTORS ENCODING A PARALYTIC PEPTIDE - The invention relates to a low molecular weight peptide isolated from the submaxiliary saliva glands of shrews of the species | 2015-07-09 |
20150191520 | Complement split product C4d for the treatment of inflammatory conditions - The present invention relates to a pharmaceutical composition comprising complement split product C4d for use in treating an inflammatory condition, such as graft rejection, graft versus host disease, an autoimmune disease or atopy. The C4d to be used may be a multimer. Accordingly, also C4d multimers and their use in medicine, like the treatment of inflammatory conditions, is provided. Furthermore, the present invention provides a protein complex comprising C4d interacting with its ILT4 receptor. This protein complex may be used in screening methodsAlso antibodies specifically binding to the C4d multimer or the C4d/ILT4-protein complex are subject of the present invention. | 2015-07-09 |
20150191521 | DOMINANT NEGATIVE TRANSCRIPTION FACTOR FOR ANTAGONIZING ONCOGENIC TRANSCRIPTION FACTORS VIA MULTIMERIZATION - The present invention teaches compositions, methods and kits for treating or preventing cancer in a subject by using a dominant negative transcription factor and/or a multimerization adaptor. The invention teaches that the dominant negative transcription factor can antagonize an oncogenic transcription activator and can cause cell cycle arrest and cell death in a cancer cell. The invention further teaches delivering the inventive compositions by a variety of mechanisms, including: transfection, a virus-based system, and using a protein-transduction-domain moiety fused to the inventive dominant negative transcription factor. | 2015-07-09 |
20150191522 | COMPOSITIONS FOR PRESERVING INSULIN-PRODUCING CELLS AND INSULIN PRODUCTION AND TREATING DIABETES - Nuclear Transport Modifiers such as cSN50 and cSN50.1, afford in vivo islet protection following a 2-day course of intense treatment in autoimmune diabetes-prone, non-obese diabetic (NOD) mice, a widely used model of Type 1 diabetes (T1D), which resulted in a diabetes-free state for one year without apparent toxicity and the need to use insulin. cSN50 precipitously reduces the accumulation of islet-destructive autoreactive lymphocytes while enhancing activation-induced cell death of T and B lymphocytes derived from NOD mice. cSN50 attenuated pro-inflammatory cytokine and chemokine production in immune cells in this model of human T1D. cSN50 also provides cytoprotection of beta cells, therefore preserving residual insulin-producing capacity. Because intracellular delivery of a Nuclear Transport Modifier peptide such as cSN50 and cSN50.1 can result in lowering of fasting blood glucose levels and may ameliorate (e.g., reduce, eliminate) insulin resistance, the compositions, methods and cells described herein can also be used for treating Type 2 diabetes (T2D). | 2015-07-09 |
20150191523 | TOLL-LIKE RECEPTORS - The present invention relates to toll-like receptors, to cells comprising such toll-like receptors, to methods for the detection of immunostimulatory oligodeoxynucleotides wherein such methods use such toll-like receptors, to immunostimulatory oligodeoxynucleotides detected by use of this method, to the use of such immunostimulatory oligodeoxynucleotides in medicine and to vaccines comprising such immunostimulatory oligodeoxynucleotides. | 2015-07-09 |
20150191524 | ENGINEERING T CELL RECEPTORS - The use of model T cell receptors (TCRs) as scaffolds for in vitro engineering of novel specificities is provided. TCRs with de novo binding to a specific peptide-major histocompatibility complex (MHC) product can be isolated by: 1) mutagenizing a T cell receptor protein coding sequence to generate a variegated population of mutants (a library), 2) selection of the library of TCR mutants with the specific peptide-MHC, using a process of directed evolution and a “display” methodology (e.g., yeast, phage, mammalian cell) and the peptide-MHC ligand. The process can be repeated to identify TCR variants with improved affinity for the selecting peptide-MHC ligand. | 2015-07-09 |
20150191525 | OX40L FUSION PROTEIN FOR THE IMMUNOTHERAPY OF TUMORS OF VETERINARY ANIMALS - Provided is an isolated recombinant polypeptide comprising an immunoglobulin domain and a canine OX40L extracellular domain polypeptide fragment or a biological equivalent thereof and compositions comprising: an isolated recombinant polypeptide comprising an immunoglobulin domain and a canine OX40L extracellular domain polypeptide fragment; and a pharmaceutically acceptable carrier. Also provided are methods for treating or ameliorating the symptoms of cancer in a canine comprising administering an effective amount of the isolated recombinant polypeptide of the disclosure and/or a composition of the disclosure to a canine in need thereof. | 2015-07-09 |
20150191526 | CELL LINE EXPRESSING SINGLE CHAIN FACTOR VIII POLYPEPTIDES AND USES THEREOF - The present invention provides cell lines for producing single chain FVIII polypeptides, e.g., chimeric single chain FVIII polypeptides, methods of producing single chain FVIII polypeptides, single chain FVIII polypeptides, and methods of treating Hemophilia A with a single chain Factor VIII polypeptide. | 2015-07-09 |