20th week of 2016 patent applcation highlights part 23 |
Patent application number | Title | Published |
20160137570 | MULTI-FUNCTIONAL PHENOLIC RESINS - Disclosed herein are compositions and methods of making phenolic compounds and phenolic resins. The resins include multifunctional epoxies, amino glycidyl derivatives, alkanoate derivatives, alkyl ether derivatives, and multi-functional amines prepared from hydroxymethyl derivatives of novolac resin. | 2016-05-19 |
20160137571 | ALKYL POLY GLYCOL-ETHERS AND THEIR SYNTHESIS - Processes for producing long chain ethers by reacting a long chain secondary alcohol, a long chain alkoxide, or a combination thereof with at least one epoxide. The long chain ether may comprise a long chain ether alcohol, a long chain ether alcoholate, or a combination thereof. The long chain ether alcoholate may be either protonated to provide the long chain ether alcohol or reacted with an alkyl halide to provide a long chain capped ether. Long chain ether compositions are also disclosed herein. | 2016-05-19 |
20160137572 | FLUORINATED AROMATIC COMPOUND, METHOD FOR ITS PRODUCTION, CURABLE MATERIAL, ITS CURED PRODUCT, AND OPTICAL MEMBER - To provide a novel fluorinated aromatic compound having at least two carbon-carbon unsaturated bonds, a method for its production, a curable material comprising the fluorinated aromatic compound, a cured product thereof, and an optical member. The fluorinated aromatic compound is represented by formula (A), wherein n is an integer of 0 to 6, a is an integer of 0 to 5, b is an integer of 0 to 4, c is an integer of 0 to 4, a+c+n is 2 to 6, a+b is 2 to 9, Z is a single bond, —O—, —S—, —CO—, —C(CH | 2016-05-19 |
20160137573 | METHODS AND CATALYST SYSTEMS FOR CARBON DIOXIDE CONVERSION - Disclosed herein are embodiments of a heterogeneous catalyst system and methods of using the same to convert CO | 2016-05-19 |
20160137574 | Reducing Hydrogen Iodide Content in Carbonylation Processes - Processes for producing acetic acid wherein at least one process vent stream is treated in an absorber column that utilizes a scrubber solvent, e.g., acetic acid, methanol, and/or methyl acetate to remove hydrogen iodide therefrom. | 2016-05-19 |
20160137575 | PROCESSES FOR PRODUCING ACETIC ACID FROM A REACTION MEDIUM HAVING LOW ETHYL IODIDE CONTENT - A process for producing high purity acetic acid from a carbonylation reaction, wherein the carbonylation reaction is carried out while maintaining a low ethyl iodide content in the reaction medium. The ethyl iodide concentration may be maintained by removing acetaldehyde from the reaction medium and/or by adjusting at least one A) hydrogen partial pressure in the reactor, B) methyl acetate concentration of the reaction medium; and/or C) methyl iodide concentration of the reaction medium. | 2016-05-19 |
20160137576 | Processes for Producing an Acetic Acid Product Having Low Butyl Acetate Content - A process for producing an acetic acid product having low butyl acetate content via a carbonylation reaction. The carbonylation reaction is carried out at a temperature from 100 to 300° C., a hydrogen partial pressure from 0.3 to 2 atm, and a rhodium catalyst concentration from 100 to 3000 wppm, based on the weight of the reaction medium. The butyl acetate concentration in the acetic acid product may be controlled by removing acetaldehyde from a stream derived from the reaction medium and/or by adjusting at least one of reaction temperature, hydrogen partial pressure, and metal catalyst concentration. | 2016-05-19 |
20160137577 | Process for Flashing A Reaction Medium Comprising Lithium Acetate - A process for producing acetic acid is disclosed, in which the methyl iodide concentration is maintained in the vapor product stream formed in a flashing step. The process includes introducing a lithium compound into the reactor and maintaining a concentration of lithium acetate in the reaction medium is in an amount from 0.3 to 0.7 wt. %. The reaction medium is fed forward to the flashing step. The methyl iodide concentration in the vapor product stream ranges from 24 to less than 36 wt. %, based on the weight of the vapor product stream. The vapor product stream is distilled in a first column to obtain an acetic acid product stream comprising acetic acid and hydrogen iodide in an amount of less than or equal to 300 wppm and/or methyl iodide in an amount from 0.1 to 6 wt. %. | 2016-05-19 |
20160137578 | PROCESSES FOR IMPROVING ACETIC ACID YIELD BY REMOVING IRON - In a process for improving a carbonylation process, iron is removed to maintain an effective Space Time Yield (STY) of the rhodium catalyst of at least 80% of the maximum STY. The process comprises carbonylating methanol in a reactor in a reaction medium comprising water, a rhodium catalyst, methyl iodide and a halide salt, separating a portion of the reaction medium in a flash vessel to form a less volatile stream and a vapor product stream comprising acetic acid, recycling a liquid stream to the reactor, wherein the liquid stream comprises a portion of the less volatile stream and wherein the liquid stream comprises iron, and removing a portion of the iron from the liquid stream to maintain an effective STY of the rhodium catalyst of at least 80% of the maximum STY. | 2016-05-19 |
20160137579 | PROCESS FOR THE PREPARATION OF BENZENE DERIVATIVES FROM FURAN DERIVATIVES - Benzene derivatives of the formula (I); | 2016-05-19 |
20160137580 | PROCESS FOR THE SELECTIVE HYDROGENATION OF VEGETABLE OILS - This invention relates to a process for the selective hydrogenation of vegetable oils. In particular the invention relates to a process for the hydrogenation of vegetable oils which is capable of selectively converting polyunsaturated fatty acids into mono-unsaturated fatty acids and products obtained therefrom. The vegetable oils obtained from the process according to the invention have in particular a high mono-unsaturated fatty acids content and are particularly suitable for use as raw materials for the synthesis of chemical intermediates. | 2016-05-19 |
20160137581 | Processes for Producing Acetic Acid With Decanter Control - A process for producing acetic acid comprising the steps of carbonylating methanol in a reaction medium to form a crude acetic acid product; conveying the crude acetic acid product to a flash vessel at a flash flow rate; flashing the crude acetic acid product to form a first vapor stream comprising acetic acid and a liquid residue stream comprising metal catalyst and halide salt; separating the flashed vapor stream to form a second vapor stream comprising methyl iodide a sidedraw comprising purified acetic acid and water, and a liquid residue stream. The process further comprises the steps of condensing at least a portion of the second vapor stream to form at least one liquid phase and refluxing to the light ends column at least a portion of the at least one liquid phase at a reflux rate. The reflux rate is adjusted based on changes in the flash flow rate. | 2016-05-19 |
20160137582 | Method for Producing Polyol Esters - A process for preparing polyol esters by reacting polyols with linear or branched aliphatic monocarboxylic acids having 3 to 20 carbon atoms, is characterized in that a mixture of the starting compounds is allowed to react in the presence of a Lewis acid containing at least one element of groups 4 to 14 of the periodic table of the elements as a catalyst and in the presence of an adsorbent with removal of the water formed, and then the crude ester obtained is aftertreated by adding a further adsorbent which is an acidic activated carbon having a pH of 1 to 6.5. | 2016-05-19 |
20160137583 | METHOD FOR PRODUCING ALPHA-HYDROXYCARBOXYLIC ACID ESTERS - The present invention relates to a process for the production of alpha-hydroxycarboxylic esters by means of alcoholysis of the corresponding alpha-hydroxycarboxamide under heterogeneous catalysis. | 2016-05-19 |
20160137584 | PROCESSES AND INTERMEDIATES FOR PREPARING a,w -DICARBOXYLIC ACID-TERMINATED DIALKANE ETHERS - The present disclosure provides a process for the preparation of compounds of formula (III), | 2016-05-19 |
20160137585 | COMPOSITIONS AND METHODS FOR GLUCOSE TRANSPORT INHIBITION - Glucose deprivation is an attractive strategy in cancer research and treatment. Cancer cells upregulate glucose uptake and metabolism for maintaining accelerated growth and proliferation rates. Specifically blocking these processes is likely to provide new insights to the role of glucose transport and metabolism in tumorigenesis, as well as in apoptosis. As solid tumors outgrow the surrounding vasculature, they encounter microenvironments with a limited supply of nutrients leading to a glucose deprived environment in some regions of the tumor. Cancer cells living in the glucose deprived environment undergo changes to prevent glucose deprivation-induced apoptosis. Knowing how cancer cells evade apoptosis induction is also likely to yield valuable information and knowledge of how to overcome the resistance to apoptosis induction in cancer cells. Disclosed herein are novel anticancer compounds that inhibit basal glucose transport, resulting in tumor suppression and new methods for the study of glucose deprivation in animal cancer research. | 2016-05-19 |
20160137586 | POROUS DIACETYLENE PARTICLES, SYNTHESIS METHOD THEREOF - Provided are a radial porous diacetylene particle, which is synthesized by ion-bonding a diacetylene-containing dicarboxylic acid or diamine monomer represented by Formula 1 above with a diamine or dicarboxylic acid monomer represented by Formula 2 above, and a method of manufacturing the same. | 2016-05-19 |
20160137587 | TRANSITION-METAL-FREE N-ARYLATION OF TERTIARY AMINES USING ARYNES - The present invention relates to transition-metal-free process for the synthesis of tertiary arylamines comprises coupling reaction between arynes and N,N-dimethyl aniline compounds in presence of 18-crown-6, KF and THF. | 2016-05-19 |
20160137588 | INHIBITORS OF COGNITIVE DECLINE - Compounds that are central nervous system drug candidates for the treatment of cognitive decline and, more particularly, Alzheimer's disease are provided. Methods of treating, inhibiting, and/or abatement of cognitive decline and/or Alzheimer's disease with a compound or pharmaceutically acceptable salt of the invention are also provided. Also provided are methods of preparing the compounds/compositions of the invention. | 2016-05-19 |
20160137589 | USE OF 4-[ETHYL(DIMETHYL)AMMONIO]BUTANOATE IN THE TREATMENT OF CARDIOVASCULAR DISEASE - New compound 4-[ethyl(dimethyl)ammonio]butanoate, method of preparation thereof and use in the treatment of cardiovascular disease. | 2016-05-19 |
20160137590 | THERMAL CONVERSION VESSEL USED IN A PROCESS FOR AMIDIFICATION OF ACETONE CYANOHYDRIN - The invention relates to a thermal conversion vessel ( | 2016-05-19 |
20160137591 | PREPARATION OF CHEMICALS, MONOMERS AND POLYMERS FROM PLANT OILS - Methods for forming a compound from a plant oil compound having a carboxylic acid group attached to an organic group are provided. The method can include performing an aminolysis reaction between the plant oil compound and a hydroxyl-containing amine compound to form a functionalized plant oil compound having an amide bond; and functionalizing the hydroxyl group to have a polyerizable vinyl group or a norbornene group to form a polyerizable plant oil compound having the amide bond and an ester bond. | 2016-05-19 |
20160137592 | NOVEL COMPOUNDS ADVANTAGEOUS IN THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISEASES AND DISORDERS - A series of novel amides showing broad pharmaceutical activity. Compounds described herein are effective as anticonvulsants, chemical countermeasures, and analgesics. Such compounds also show, neuroprotective/neuroreparative effects and activity against spinal muscular atrophy. Such pharmaceutically active compounds show utility in the treatment of central nervous system (“CNS”) diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, neurodegenerative diseases (e.g., Parkinson's disease, Alzheimer's, ALS, and Huntington's disease) spasticity, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), and/or traumatic brain and/or spinal cord injuries. | 2016-05-19 |
20160137593 | Cationic Lipids for Therapeutic Agent Delivery Formulations - Here described are compounds of formula I: | 2016-05-19 |
20160137594 | HDAC INHIBITORS - Compounds of formula (I) inhibit HDAC activity: | 2016-05-19 |
20160137595 | IDO INHIBITORS - There are disclosed compounds of formula (I) that modulate or inhibit the enzymatic activity of indoleamine 2,3-di-oxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention. | 2016-05-19 |
20160137596 | METHOD FOR PURIFYING ACRYLAMIDE ALKYL SULFONIC ACID - A method for purifying acrylamide alkyl sulfonic acid comprises: (1) making a material A evenly mixed and contacted with a solvent C, an amount of the material A exceeding a solubility of the material A in the solvent C under the condition where the material A is located, therefore the material A is not completely dissolved by the solvent C; (2) keeping the material A even mixed and contacted with the solvent C for at least 5 minutes; (3) performing a solid-liquid separation to obtain a solid, namely, a purified product B with impurities reduced. In the purifying method according to the invention, the material does not need to be completely dissolved, therefore less solvent is used, and the steps of dissolving the material by increasing temperature, separating out by decreasing temperature or removing the solvent are eliminated, so cost is reduced, efficiency is improved, and operations are simplified. | 2016-05-19 |
20160137597 | SPECIFIC SULFONATE COMPOUNDS THAT CAN BE USED AS ELECTROLYTE SOLVENT FOR LITHIUM BATTERIES - The invention relates to sulfonate compounds with the following formula (I): | 2016-05-19 |
20160137598 | SYNTHESIS OF CYCLOPHANES FROM A SELF-ASSEMBLY REACTION - Disclosed herein is a novel method for preparing cyclophanes, comprising forming a disulfide cyclophane by contacting a linker moiety which includes two or more thiol groups, with a metal salt and an oxidant. The disulfide cyclophane is then desulfurized to form a thiacyclophane comprising thioether bridges. This thiacyclophane optionally may be further desulfurized to form an unsaturated hydrocarbon cyclophane, which can then be reduced to form a saturated hydrocarbon cyclophane. The various cyclophanes can be synthesized in a ring form, such as a dimer, trimer or tetramer etc., or they can be synthesized in a tetrahedral or larger structure. Also disclosed are novel cyclophanes formed by the disclosed method. | 2016-05-19 |
20160137599 | 2-METHYLTHIOPYRROLIDINES AND THEIR USE FOR MODULATING BACTERIAL QUORUM SENSING - Compounds of Formula (I) are disclosed herein and their use in inhibiting quorum sensing in bacteria. | 2016-05-19 |
20160137600 | Pyrrole Derivatives as Alpha 7 nAChR Modulators - Disclosed are compounds of the formula (I), wherein R | 2016-05-19 |
20160137601 | METHOD FOR PROVIDING STABLE ISOINDOLE DERIVATIVES - Method for producing an isoindole derivative, the isoindole derivative obtainable by the methods, a methods for stabilizing an isoindole derivative, and methods for detection and/or quantification of macromolecules. | 2016-05-19 |
20160137602 | NOVEL PROCESSES FOR THE PREPARATION OF PROSTAGLANDIN AMIDES - The subject of the invention is process for the preparation of the prostaglandin amides of the general formula I, | 2016-05-19 |
20160137603 | PROCESS FOR THE PREPARATION OF CERTAIN SUBSTITUTED SULFILIMINES - Cyano-substituted sulfilimines are produced efficiently and in high yield from the corresponding sulfides, cyanamide and hypochlorite by adding the sulfide to a solution of the cyanamide and hypochlorite in the presence of a nitrile solvent while maintaining the pH from about 8 to about 12. | 2016-05-19 |
20160137604 | PURIFICATION OF INTERMEDIATES USED IN THE PREPARATION OF HETEROBIFUNCTIONAL LINKERS - The present invention is directed to a method of separating a monocarboxylic represented by the following stmctural formula: (I) from a dicarboxylic acid represented by the following structural fonnula: (II) using silica chromatography. | 2016-05-19 |
20160137605 | SELECTIVE PLACEMENT OF CARBON NANOTUBES VIA COULOMBIC ATTRACTION OF OPPOSITELY CHARGED CARBON NANOTUBES AND SELF-ASSEMBLED MONOLAYERS - A method of forming a structure having selectively placed carbon nanotubes, a method of making charged carbon nanotubes, a bi-functional precursor, and a structure having a high density carbon nanotube layer with minimal bundling. Carbon nanotubes are selectively placed on a substrate having two regions. The first region has an isoelectric point exceeding the second region's isoelectric point. The substrate is immersed in a solution of a bi-functional precursor having anchoring and charged ends. The anchoring end bonds to the first region to form a self-assembled monolayer having a charged end. The substrate with charged monolayer is immersed in a solution of carbon nanotubes having an opposite charge to form a carbon nanotube layer on the self-assembled monolayer. The charged carbon nanotubes are made by functionalization or coating with an ionic surfactant. | 2016-05-19 |
20160137606 | NOVEL PYRIDINE DERIVATIVES - The invention relates to a compound of formula (I) | 2016-05-19 |
20160137607 | Autophagy Inhibitors - The present invention relates to compounds of formulas III and V that are useful as pharmaceutical agents, particularly as autophagy inhibitors. | 2016-05-19 |
20160137608 | SUBSTITUTED BENZOAZEPINES AS TOLL-LIKE RECEPTOR MODULATORS - Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease. | 2016-05-19 |
20160137609 | PYRAZOLE DERIVATIVES AS ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF - Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described. Formula (I). | 2016-05-19 |
20160137610 | Compounds that Modulate EGFR Activity and Methods for Treating or Preventing Conditions Therewith - Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith. | 2016-05-19 |
20160137611 | PREPARATION METHOD FOR ACRYLATE COMPOUND - The present invention relates to a method for preparing an acrylate compound. The acrylate compound has a structure as shown in formula (I). The method includes: subjecting a compound with a structure of formula (II) or a mixture of compounds with structures of formula (I) and formula (II), and a catalyst to a contact reaction in the absence of an anhydride, and removing the resulting methanol by pressure reduced distillation during the contact reaction process. In the formulas (I) and (II), R is selected from one of: an alkoxy with a carbon number of 1-5, a substituent-containing phenoxyl with a carbon number of 6-20, a substituent-containing heteroaryloxy with a carbon number of 4-20, a substituent-containing heteroaryloxymethyl with a carbon number of 4-20, a substituent-containing phenoxymethyl with a carbon number of 5-20, and a substituent-containing alkyl with a carbon number of 2-20. According to the method for preparing an acrylate compound provided in the invention, the conversion rate and selectivity of the reaction can be substantially improved. | 2016-05-19 |
20160137612 | PROCESS FOR PREPARING 4,6-BIS (ARYLOXY) PYRIMIDINE DERIVATIVES - Process for preparing 4,6-bis(aryloxy)pyrimidine derivatives A process is provided for preparing 4,6-bis(aryloxy)pyrimidine derivatives. The process is conducted in water as reaction medium and catalyzed by one or more tertiary-amine catalyst(s). It has been found that a water based reaction substantially free of organic solvents can be carried out providing excellent yields by the addition of one or more tertiary-amine catalysts to the reaction medium. This provides a clean reaction and produces the desired product in high yields. | 2016-05-19 |
20160137613 | NOVEL ANTI-INFLAMMATORY AGENTS - Disclosed are novel compounds that are useful in regulating the expression of interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1), and their use in the treatment and/or prevention of cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s). Also, disclosed are compositions comprising the novel compounds, as well as methods for their preparation. | 2016-05-19 |
20160137614 | FORMATION OF N-PROTECTED BIS-3,6- (4-AMINOBUTYL) -2, 5-DIKETOPIPERAZINE THROUGH A CYCLIC ALPHA-N-PROTECTED AMINO ESTER - A method for the synthesis of N-protected 3,6-aminoalkyl-2,5-diketopiperazines is provided. The method includes obtaining a cyclic α-N protected active amino ester and adding it to a mixture of an amine catalyst in an organic solvent. | 2016-05-19 |
20160137615 | Process for Manufacturing 4-Propargylated Amino-Benzoxazinones - The present invention relates to a process for manufacturing 4-propargylated amino-benzoxazinones of formula (I), | 2016-05-19 |
20160137616 | BICYCLIC 1,3,4-OXADIAZOLE DERIVATIVES AS SPHINGOSINE-1-PHOSPHATE RECEPTORS' MODULATORS - The present invention relates to bicyclic 1,3,4-oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 2016-05-19 |
20160137617 | NEW MACROCYCLIC AMIDINOUREA DERIVATIVES, METHODS OF PREPARATION AND USES THEREOF AS CHITINASE INHIBITORS - The present invention relates to macrocyclic amidinourea derivatives of formula 8, methods of preparation and uses thereof, pharmaceutical compositions in particular to be used as chitinase inhibitors in the treatment of a fungal infection. | 2016-05-19 |
20160137618 | Macrocyclic Urea Derivatives as Inhibitors of TAFIa, Their Preparation and Their Use as Pharmaceuticals - The present invention relates to macrocydic urea derivatives of the formula I (I) in which R1, R2, R3, V and Y are as defined below. The compounds of the formula I are inhibitors of the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor). The invention further relates to the process for the preparation of the compounds of formula I and to the use thereof as medicaments. | 2016-05-19 |
20160137619 | Thiazole Inner Salt Compounds, and Preparation Methods and Uses Thereof - The present invention pertains to field of pharmaceutical chemicals, and relates to thiazole inner salt compounds, preparation methods and uses thereof. Specifically, the present invention relates to a compound of Formula I, hydrates or pharmaceutically acceptable salts thereof. The compound of Formula I of the present invention is a potent cross-linking protein cleavage agent, has a stable structure, good physical and chemical properties, and good pharmacological activities, and is suitable for large scale production to obtain samples with stable, controllable and reliable quality, thereby being suitable for pharmaceutical development. | 2016-05-19 |
20160137620 | Phenyl-Piperazine Derivatives As Serotonin Reuptake Inhibitors - The invention provides compounds represented by the general formula I | 2016-05-19 |
20160137621 | PROCESS FOR THE PREPARATION OF TRAVOPROST - The crystalline compound of formula (III) | 2016-05-19 |
20160137622 | AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES - The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved. | 2016-05-19 |
20160137623 | METHOD FOR SEPARATING FLAVONOID SUBSTANCES IN CAMELLIA NITIDISSIMA CHI BASED ON A MAGNETIC NANOPARTICLES-PAMAM NANO COMPOSITES - The present invention discloses a method for separating flavonoid substances in | 2016-05-19 |
20160137624 | PROCESS FOR PREPARING PYRIDYLPYRAZOLE COMPOUNDS AND DERIVATIVES THEREOF FROM PYRIDYLHYDRAZINE - The present invention relates to a process for preparing pyridylpyrazole compounds of the formula (I) | 2016-05-19 |
20160137625 | 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. | 2016-05-19 |
20160137626 | BICYCLIC AROMATIC CARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS - The present disclosure describes bicyclic aromatic carboxamide derivatives, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases. | 2016-05-19 |
20160137627 | DERIVATIVES OF 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, PREPARATION AND THERAPEUTIC USE THEREOF - The invention relates to compounds corresponding to formula (I), in the form of the base or of an acid-addition salt: | 2016-05-19 |
20160137628 | Aurora A Kinase Inhibitor - The present invention provides an aminopyridine compound, or a pharmaceutically acceptable salt thereof, that inhibits Aurora A and, therefore may be useful in treating cancer. | 2016-05-19 |
20160137629 | COMPOUNDS FOR BINDING TO THE PLATELET SPECIFIC GLYCOPROTEIN IIb/IIIa AND THEIR USE FOR IMAGING OF THROMBI - The present invention relates to novel fluorine containing compounds, methods for their preparation, the intermediates of the synthesis, their use as diagnostic agents, especially for imaging of thrombi. The invention relates to positron emission tomography (PET) agents and associated precursor reagents, and methods for producing such radiolaveled agents for imaging of thrombi in a mammalian body. More particularly, the invention relates to small nonpeptide, high-affinity, specific-binding glycoprotein 11b/IIIa antagonists for imaging of thrombi. | 2016-05-19 |
20160137630 | INDUCTION OF GATA2 BY HDAC1 AND HDAC2 INHIBITORS - Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with Gata2 deficiency, particularly diseases or disorders that involve any type of HDAC1 and/or HDAC2 expression. Such diseases include acute myeloid leukemia (AML); familial myelodysplastic syndrome (MDS); leukemia; sickle-cell anemia; beta-thalassemia; monocytopenia and mycobacterial infections; dendritic cell, nonocyte, B, and natural killer lymphoid deficiency; Emberger syndrome; asymptomatic neurocognitive impairment; mild neurocognitive disorder; and HIV-associated dementia. | 2016-05-19 |
20160137631 | 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. | 2016-05-19 |
20160137632 | BENZAMIDE DERIVATIVES AS MODULATORS OF THE FOLLICLE STIMULATING HORMONE - Novel benzamide derivatives of formula (I) | 2016-05-19 |
20160137633 | PHARMACEUTICAL COMPOSITION FOR TREATING DIABETES - Provided is a compound represented by the following general formula (I), or a pharmaceutically acceptable salt thereof. This novel compound has a glycogen-synthase activation ability, but activates a receptor PPAR to a low degree and is highly safe. | 2016-05-19 |
20160137634 | Chemical Compounds - The invention concerns compounds of Formula (I) | 2016-05-19 |
20160137635 | THE (S)-ENANTIOMER OF MEPAZINE - The present invention relates to the (S)-enantiomer of mepazine, its applicability in therapy, a pharmacological composition comprising (S)-mepazine, and processes for the preparation of (S)-mepazine and one of its intermediates. | 2016-05-19 |
20160137636 | Bicyclic Sulfonamide Compounds as Sodium Channel Inhibitors - The present invention provides compounds of Formula I or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention. | 2016-05-19 |
20160137637 | 2,3-DIHYDROBENZOFURAN-5YL COMPOUNDS AS DYRK KINASE INHIBITORS - The present invention relates to compounds of below Formula (I), physiologically functional derivatives or salts thereof, where the groups R | 2016-05-19 |
20160137638 | Crystalline Form of (R)-7-Chloro-N-(Quinuclidin-3-YL)benzo[B]thiophene-2-Carboxamide Hydrochloride Monohydrate - Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described. | 2016-05-19 |
20160137639 | TRIAZOLE-ISOXAZOLE COMPOUND AND MEDICAL USE THEREOF - A compound represented by Formula [I]: | 2016-05-19 |
20160137640 | FIVE-MEMBER-HETEROCYCLE FUSED PYRIDINE COMPOUNDS, METHOD OF PRODUCING THE SAME, AND USE THEREOF - This invention provides a class of five-member-heterocycle fused pyridine compounds as shown below in Formula (X), pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, a method of producing the same, pharmaceutical compositions containing the compound, and use of the compounds in preparing medicament for preventing and/or treating diseases and tumours associated with abnormal protein tyrosine kinase. | 2016-05-19 |
20160137641 | PYRROLOQUINOLINE QUINONE LITHIUM SALT CRYSTAL AND PREPARATION METHOD AND APPLICATION THEREOF - The present invention provides pyrroloquinoline quinone lithium salt crystal and a preparation method and application thereof. Characteristic absorption peaks appear when the diffraction angles are 6.222±0.2°, 7.379±0.2°, 7.941±0.2°, 23.631±0.2°, 24.044±0.2°, 25.497±0.2°, 27.541±0.2°, 30.736±0.2°, and 32.306±0.2° degrees in a powder X-ray diffraction pattern of the pyrroloquinoline quinine lithium salt crystal. The maximum value of thermal absorption of the pyrroloquinoline quinine lithium salt crystal appears between 90° C. and 96° C. through differential scanning calorimetry. Peaks appear when infrared spectroscopy of the pyrroloquinoline quinine lithium salt crystal is at 3396.03 cm | 2016-05-19 |
20160137642 | SUBSTITUTED PYRAZOLYLPYRAZOLE DERIVATIVE AND USE OF SAME AS HERBICIDE - Provided is a compound capable of effectively control worst weeds of higher leaf stages that present practical problems. A specific pyrazolylpyrazole derivative of formula (I) is disclosed that is able to solve the above-mentioned problems. | 2016-05-19 |
20160137643 | 1,7-NAPHTHYRIDINE DERIVATIVES - The present invention relates to compounds of general formula I wherein R | 2016-05-19 |
20160137644 | METHOD FOR PRODUCING TRICYCLIC HETEROCYCLIC COMPOUND - It is an object of the present invention to provide a method for producing a high-purity tricyclic heterocyclic compound represented by formula (I), which is useful as a production intermediate for a pharmaceutical agent, wherein the method is an efficient production method with short steps and with a high yield, which does not use, as raw materials, expensive bromopyruvate and highly harmful copper chromite, and does not need silica gel column chromatography that generates, as by-products, large quantities of waste. The present invention relates to production of Compound (I) by the following method. | 2016-05-19 |
20160137645 | COMPOUNDS USEFUL FOR PRODUCING AN OPTICALLY ACTIVE DIAZABICYCLOOCTANE COMPOUND - An optically active (2S,5R)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxylic acid compound defined by the following formula (F): | 2016-05-19 |
20160137646 | Novel Compounds and Uses Thereof - The present invention provides novel compounds of any one of Formulae (I)-(IV), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of any one of Formulae (I)-(IV) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor signaling pathway (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof. | 2016-05-19 |
20160137647 | SUBSTITUTED BENZOXAZOLES - The invention relates to substituted benzoxazoles and to processes for their preparation and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular disorders, preferably of thrombotic or thromboembolic disorders. | 2016-05-19 |
20160137648 | TETRAAZA-CYCLOPENTA[A]INDENYL DERIVATIVES - The present invention provides compounds of Formula (I) as M1 receptor positive allosteric modulators for the treatment of diseases mediated by the muscarinic M1 mediator. | 2016-05-19 |
20160137649 | PYRROLO-PYRROLE CARBAMATE AND RELATED ORGANIC COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND MEDICAL USES THEREOF - The invention provides pyrrolo-pyrrole carbamate and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., solid tumor cancer, obesity, Down's syndrome, Alzheimer's disease, or pain, in a patient. The octahydropyrrolo pyrrole carbamates could be derived from hexafluoroisopropanol, N,N-disuccinimide and such. The activity of carbamates in MAGL, FAAH, and ABHD6 assays are also described. | 2016-05-19 |
20160137650 | IMIDAZO[1,2-B][1,2,4]TRIAZINES AS C-MET INHIBITORS - The present invention relates to imidazo[1,2-b][1,2,4]triazines that are inhibitors of c-Met and are useful in the treatment of c-Met associated diseases including cancer. | 2016-05-19 |
20160137651 | PYRAZOLOPYRIMIDINE COMPOUNDS - The present teachings provide a compound represented by the following structural formula: (Formula (I)); or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof. | 2016-05-19 |
20160137652 | IMMUNOREGULATORY AGENTS - Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided. | 2016-05-19 |
20160137653 | IMMUNOREGULATORY AGENTS - Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided. | 2016-05-19 |
20160137654 | CRYSTALLINE FORM OF (S)-N-(5-((R)-2-(2,5-DIFLUOROPHENYL)-PYRROLIDIN-1-YL)-PYRAZOLO[1,5-A]PYRI- MIDIN-3-YL)-3-HYDROXYPYRROLIDINE-1-CARBOXAMIDE HYDROGEN SULFATE - A novel crystalline form of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or | 2016-05-19 |
20160137655 | PROCESSES FOR MAKING HYDROCODONE, HYDROMORPHONE AND THEIR DERIVATIVES - Improved processes for making hydrocodone and hydromorphone as well as their 8,14-dihydrothebaine and 8,14-dihydrooripavine derivatives and salts are disclosed. | 2016-05-19 |
20160137656 | PROCESSES FOR MAKING HYDROCODONE, HYDROMORPHONE AND THEIR DERIVATIVES - Improved processes for making hydrocodone and hydromorphone as well as their 8,14-dihydrothebaine and 8,14-dihydrooripavine derivatives and salts are disclosed. | 2016-05-19 |
20160137657 | Polymorphic Forms of Naltrexone - This invention relates to the discovery of novel polymorphic forms of naltrexone, including solvates, hydrates, anhydrous and other crystalline forms and combinations thereof. These novel forms of naltrexone impart advantages in pharmaceutical formulations incorporating them, including sustained release, or long acting, formulations. | 2016-05-19 |
20160137658 | POLYMORPHIC FORMS OF ICOTINIB MALEATE AND USES THEREOF - Provided are Icotinib maleate (the compound of Formula I) and polymorph forms thereof, and methods of preparing and using them. | 2016-05-19 |
20160137659 | CHROMANE AND CHROMENE DERIVATIVES AND THEIR USE AS CRAC MODULATORS - The invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine for the treatment of diseases, disorders associated with the modulation of calcium release-activated calcium (CRAC) channel. The invention also relates to pharmaceutical compositions containing such compounds in treating diseases disorders associated with calcium release-activated calcium (CRAC) channel modulators. | 2016-05-19 |
20160137660 | PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES - The present invention provides compounds of formula (I), | 2016-05-19 |
20160137661 | SYNTHETIC PROCESS FOR PREPARATION OF MACROCYCLIC C1-KETO ANALOGS OF HALICHONDRIN B AND INTERMEDIATES USEFUL THEREIN INCLUDING INTERMEDIATES CONTAINING -SO2-(P-TOLYL) GROUPS - Disclosed is a compound of formula 1, or a pharmaceutically acceptable salt thereof, where R | 2016-05-19 |
20160137662 | COMPOSITIONS AND METHODS FOR TREATING CANCER - Provided herein, inter alia, are compositions and methods useful for treating hyperproliferative diseases, including cancer and non-malignant hyperproliferative diseases. | 2016-05-19 |
20160137663 | NOVEL SESQUITERPENOID STAT3 INHIBITORS - The present disclosure provides a method of purifying pharmaceutical compositions consisting essentially of STAT3 inhibitors from a mixture of compounds, pharmaceutical compositions comprising STAT3 inhibitors used to inhibit STAT3 in tumor cells, and certain pharmaceutically acceptable salts thereof, and methods of use. | 2016-05-19 |
20160137664 | THIENO [2,3-b] PYRIDINES AS MULTIDRUG RESISTANCE MODULATORS - The thieno[2,3-b]pyridines of general formula (I), | 2016-05-19 |
20160137665 | COMPOSITIONS COMPRISING THIENOPYRIMIDINE AND THIENOPYRIDINE COMPOUNDS AND METHODS OF USE THEREOF - The present disclosure relates generally to thienopyrimidine and thienopyridine compounds and methods of use thereof. In particular embodiments, the present disclosure provides compositions comprising thienopyrimidine and thienopyridine compounds of Formula 2: | 2016-05-19 |
20160137666 | SUBSTITUTED CYCLOPENTA[4,5]OXAZOLO[3,2-a]PYRIDO[1,2-d]PYRAZINES AS HIV INTEGRASE INHIBITORS - The present invention is to provide a novel compound (I) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. | 2016-05-19 |
20160137667 | Piperidinone Derivatives as MDM2 Inhibitors for the Treatment of Cancer - The present invention provides MDM2 inhibitor compounds of Formula I, | 2016-05-19 |
20160137668 | 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. | 2016-05-19 |
20160137669 | PREPARATION OF GRIGNARD REAGENTS USING A FLUIDIZED BED - The present invention relates to a process of preparing a Grignard reagent comprising reacting magnesium particulates in a fluid bed reactor. The present invention further relates to a continuous process comprising fluidizing magnesium particulates in a reactor, forming the Grignard reagent continuously, and reacting the Grignard reagent with a substrate. | 2016-05-19 |