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09th week of 2018 patent applcation highlights part 26
Patent application numberTitlePublished
20180057460PICOLINAMIDES AS FUNGICIDES - This disclosure relates to picolinamides of Formula I and their use as fungicides.2018-03-01
20180057461PICOLINAMIDES AS FUNGICIDES - This disclosure relates to picolinamides of Formula I and their use as fungicides.2018-03-01
20180057462Substituted 2-difluoromethyl-nicotin(thio)carboxanilide derivatives and their use as fungicides - The present invention relates to novel substituted 2-difluoromethyl-nicotin(thio)carboxanilides derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.2018-03-01
20180057463PICOLINAMIDE N-OXIDE COMPOUNDS WITH FUNGICIDAL ACTIVITY - This disclosure relates to picolinamide N-oxides of Formula I and their use as fungicides.2018-03-01
20180057464PROCESSES FOR PREPARING OLAPARIB - Provided herein are novel processes and methods for making 4-[(3-[(4-cyclopropylcarbonyl)piperazin-1-yl]carbonyl)-4-fluorophenyl]methyl(2H)phthalazin-1-one (Olaparib) and intermediates thereof. Olaparib is a poly ADP ribose polymerase (PARP) inhibitor useful in the treatment of cancers. Benefits of the present disclosure include the use of less toxic compounds and improved yields.2018-03-01
20180057465Inhibitors of Necroptosis - The invention relates to novel heterocyclic compounds of Formula (I) which inhibit necroptosis and methods for their use. The compounds may be useful in the treatment of conditions associated with deregulated necroptosis.2018-03-01
20180057466TRIAZOLE DERIVATIVES AND THEIR USE AS PDE4 ACTIVATORS - Compounds of Formula (I), which are activators of long form cyclic nucleotide phosphodiesterase-4 (PDE4) enzymes, are provided. Methods and uses of these compounds for the treatment or prevention of disorders requiring a reduction of second messenger responses mediated by cyclic 3′,5′-adenosine monophosphate (cAMP) are also described.2018-03-01
20180057467NOVEL TRIAZOLE DERIVATIVES - The present invention relates to novel triazole derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.2018-03-01
20180057468METHOD FOR PREPARING 3-TRIFLUOROMETHYL CHALCONES - Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M2018-03-01
20180057469CRYSTALLINE FORMS OF TYROSINE KINASE INHIBITORS AND THEIR SALTS - The invention relates to various polymorphic forms and amorphous form of sodium 4-((3-(4-cyclo-hexylpiperazin-1-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol-5-yl)amino)benzate, including the polymorphic form A, mixtures of the polymorphs, process for the preparation thereof and the use thereof in a pharmaceutical composition containing thereof.2018-03-01
20180057470COMPOUNDS FOR THERAPEUTIC USE - Chemical entities of Formula (I):2018-03-01
20180057471Two-Electron Donating Phenothiazines and Use Thereof - Compounds for use as electrolyte in a non-aqueous redox battery are provided, including an N-substituted phenothiazine compound according to the formula:2018-03-01
20180057472DERIVATIVES OF SOBETIROME - Ester derivatives of sobetirome with enhanced CNS distribution are disclosed.2018-03-01
20180057473METHOD FOR THE EPOXIDATION OF PROPENE WITH HYDROGEN PEROXIDE - The method for the epoxidation of propene comprises continuously reacting propene with hydrogen peroxide in the presence of a homogeneous epoxidation catalyst in a reaction mixture comprising an aqueous liquid phase and an organic liquid phase using a loop reactor with mixing of the liquid phases, withdrawing aqueous phase from the loop reactor and extracting it by liquid-liquid-extraction using propene as extractant to provide an extract comprising propene and propene oxide.2018-03-01
201800574742,3-Fluorinated Glycosides as Neuraminidase Inhibitors and Their Use as Anti-Virals - Compounds having a structure of Formula I and compositions comprising these compounds are provided. Uses of such compounds and compositions are provided for treatment or prophylaxis of viral infection. In particular, compounds and compositions may be for use in the treatment or prophylaxis of viral influenza.2018-03-01
20180057475Nitroalkene Trolox Derivatives and Methods of Use Thereof In The Treatment And Prevention of Inflammation Related Conditions - The present invention is directed to a class of anti-inflammatory, antioxidant nitroalkene compounds used in biological or biochemical applications to reduce oxidative stress or damage. The nitroalkene compounds described herein further avoid disadvantageous metabolism currently present in this field.2018-03-01
20180057476PRODUCTION OF MESO-LACTIDE, D-LACTIDE AND L-LACTIDE BY BACK BITING OF POLYLACTIDE - Process for increasingly producing D-Lactide and meso lactide by depolymerizing by back biting polylactide (PLA) said process which comprises: 2018-03-01
20180057477HETEROCYCLIC COMPOUNDS AND METHODS FOR THEIR USE - The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2018-03-01
20180057478AMPK-ACTIVATING HETEROCYCLIC COMPOUNDS AND METHODS FOR USING THE SAME - Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure2018-03-01
20180057479Inhibitors of BCR-ABL Mutants and Use Thereof - Inhibitor compounds of Bcr-Abl and Bcr-Abl mutants including Bcr-Abl T315I mutant protein are disclosed. Compositions comprising the inhibitor compounds and methods of using the compounds in the treatment of leukemia such as chronic myelogenous leukemia are also disclosed.2018-03-01
20180057480PYRAZOLYL PYRIMIDINONE COMPOUNDS AS PDE2 INHIBITORS - The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.2018-03-01
20180057481SOLID FORMS OF CENICRIVIROC MESYLATE AND PROCESSES OF MAKING SOLID FORMS OF CENICRIVIROC MESYLATE - The invention relates to solid forms of cenicriviroc mesylate, methods of their preparation, pharmaceutical compositions thereof and methods of their use.2018-03-01
20180057482SYNTHETIC ROUTE TO ANTI-VIRAL AGENTS - The invention provides methods of synthesizing a viral protease inhibitor in high yield, without using expensive catalysts or challenging reaction conditions.2018-03-01
20180057483Novel RAD51 Inhibitors and Uses Thereof - The present invention includes novel RAD51 inhibitors. The compounds of the invention may be useful in preventing or treating cancer in a subject in need thereof. The present invention also includes methods of preventing or treating cancer in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of the invention.2018-03-01
20180057484PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF A PDE10 INHIBITOR - The present invention is directed to an improved process for the preparation of compounds of Formula (II) and Formula (III), which are useful in the inhibition of PDE10. In particular, the present invention is directed to an improved process for the preparation of 1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, which is useful in the inhibition of PDE10.2018-03-01
20180057485BACE1 INHIBITORS - The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.2018-03-01
20180057486HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS - Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.2018-03-01
20180057487NOVEL GLUTAMINASE INHIBITORS - The present disclosure provides compounds of formula (I) to (III) as glutaminase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders involving glutamine.2018-03-01
20180057488COMPOSITIONS AND METHODS FOR INHIBITING KINASES - The present invention provides compounds for the prevention or treatment of cancer or a bacterial or viral infection. Additionally, the present invention provides compositions and methods for using these compounds and compositions in the prevention or treatment of cancer or a bacterial or viral infection in a subject.2018-03-01
201800574891-Amino-triazolo(1,5-A)pyridine-substituted Urea Derivative and Uses Thereof - Provided herein is a compound, 1-(4-(3-amino-[1,2,3]triazolo[1,5-a]pyridin-4-yl)phenyl)-3-(3-chlorophenyl)urea, pharmaceutical compositions thereof and crystal forms thereof. Also provided are particles (e.g., nanoparticles) comprising the compound, and pharmaceutical compositions thereof that are mucus penetrating. Also provided herein are methods and kits for using the compound, and pharmaceutical compositions thereof for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (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.2018-03-01
20180057490BENZOMORPHOLINE AND BENZOMORPHOLINE-SUBSTITUTED COMPOUNDS AS MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION - Compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.2018-03-01
20180057491ISOQUINOLINE AMIDE AND ISOQUINOLINE AMIDE-SUBSTITUTED COMPOUNDS AS MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION - Compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.2018-03-01
20180057492SPECIFIC N AND P ACTIVE MATERIALS FOR ORGANIC PHOTOELECTRIC CONVERSION LAYERS IN ORGANIC PHOTODIODES - The field of the DISCLOSURE lies in active materials for organic image sensors. The present disclosure relates to naphtalene diimide-based molecules and naphtalene diimide dimer-based molecules. The present disclosure relates to transparent N materials and/or to transparent P materials including the molecule(s) according to the present disclosure and their use in absorption layer(s), photoelectric conversion layer(s) and/or an organic image sensor and methods for their synthesis. The present disclosure also relates to photoelectric conversion layer(s) including an active material according to the present disclosure, to a device, including active material(s) according to the present disclosure or photoelectric conversion layer(s) according to the present disclosure. Moreover, the present disclosure relates to an organic image sensor including photoelectric conversion layer(s) according to the present disclosure.2018-03-01
20180057493MORPHINAN DERIVATIVE - A morphinan derivative represented by the following general formula (I):2018-03-01
20180057494TRIAZOLOPYRAZINONE DERIVATIVE USEFUL AS A HUMAN PDE1 INHIBITOR - The present invention provides a compound of Formula I:2018-03-01
201800574958-[3-AMINO-PIPERIDIN-1-YL]-XANTHINES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - The present invention relates to substituted xanthines of general formula2018-03-01
20180057496HETEROCYCLYL LINKED IMIDAZOPYRIDAZINE DERIVATIVES AS PI3KB INHIBITORS - The present invention relates to heterocyclyl linked imidazopyridazine derivatives of Formula (I)2018-03-01
20180057497Pyrazolo[1,5-A][1,3,5]Triazine and Pyrazolo[1,5-A]Pyrimidine Derivatives as CDK Inhibitors - The present invention provides substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors2018-03-01
20180057498CDK INHIBITOR, EUTECTIC CRYSTAL OF MEK INHIBITOR, AND PREPARATION METHOD THEREFOR - The present disclosure relates to novel co-crystals of a CDK inhibitor and an MEK inhibitor and the preparation methods thereof. Specifically, the present disclosure provides hydrates or anhydrates which are named as Form I, Form II and Form III. The novel co-crystals provided in the present disclosure have good stability, low hygroscopicity and high solubility, and have an important value for further optimization and development of the drug.2018-03-01
20180057499PYRAZOLO[1,5-a]PYRIMIDINE COMPOUND - The compounds represented by formulas (I) to (XVIII) or pharmaceutically acceptable salts thereof.2018-03-01
20180057500PYRAZOLE CARBOXAMIDE COMPOUNDS AND METHODS OF USE - Pyrazole carboxamide compounds of Formula I are provided, with various substituents, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.2018-03-01
20180057501FUSED TRICYCLIC PYRIDAZINONE COMPOUNDS USEFUL TO TREAT ORTHOMYXOVIRUS INFECTIONS - The invention provides compounds of Formula (I):2018-03-01
20180057502PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-alpha]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2- ,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF - The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyppyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.2018-03-01
20180057503Pharmaceutically Acceptable Salts and Polymorphic Forms of Hydrocodone Benzoic Acid Enol Ester and Processes for Making Same - Compositions comprising hydrocodone benzoic acid enol ester to form novel prodrugs including hydrocodone benzoic acid enol ester salts, and various polymorphs. Also provided are processes for the preparation of hydrocodone benzoic acid enol ester salts, and various polymorphs.2018-03-01
201800575046-AMIDO DERIVATIVES OF 4,5A-EPOXYMORPHINANS FOR TREATMENT OF PAIN - Compounds of formula:2018-03-01
20180057505BICYCLIC HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF THE PAR-2 SIGNALING PATHWAY - The compounds of formula I, wherein the variables are as defined herein, and pharmaceutically acceptable salts thereof are useful as inhibitors of the PAR-2 signaling pathway. The compounds of formula I and pharmaceutically acceptable compositions comprising such compounds can be employed for treating various diseases, disorders, and conditions.2018-03-01
20180057506FUSED DIHYDRO-4H-PYRAZOLO[5,1-C][1,4]OXAZINYL COMPOUNDS AND ANALOGS FOR TREATING CNS DISORDERS - Disclosed are compounds of Formula (I):2018-03-01
20180057507INHIBITORS OF DUAL LEUCINE ZIPPER (DLK) KINASE FOR THE TREATMENT OF DISEASE - Disclosed herein are compounds which inhibit the kinase activity of dual leucine zipper (DLK) kinase (MAP3K12), pharmaceutical compositions, and methods of treatment of DLK-mediated diseases, such as neurological diseases that result from traumatic injury to central nervous system and peripheral nervous system neurons (e.g. stroke, traumatic brain injury, spinal cord injury), or that result from a chronic neurodegenerative condition (e.g. Alzheimer's disease, frontotemporal dementia, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, spinocerebellar ataxia, progressive supranuclear palsy, Lewy body disease, Kennedy's disease, and other related conditions), from neuropathies resulting from neurological damage (chemotherapy-induced peripheral neuropathy, diabetic neuropathy, and related conditions) and from cognitive disorders caused by pharmacological intervention (e.g. chemotherapy induced cognitive disorder, also known as chemobrain).2018-03-01
20180057508PYRIDO-1,3-OXAZINE-2,4-DIONE COMPOUNDS WITH FUNGICIDAL ACTIVITY - This disclosure relates to pyrido-1,3-oxazine-2,4-diones of Formula I and their use as fungicides.2018-03-01
20180057509ALKYLOXY SUBSTITUTED THIAZOLOQUINOLINES AND THIAZOLONAPHTHYRIDINES - Thiazoloquinolines and thiazolonaphthyridines with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.2018-03-01
20180057510Synthesis and Utility of New Capgroup Largazole Analogs - Analogs of largazole are described herein. Methods of treating cancer, blood disorders, autoimmune disease, and Alzheimer's Disease using largazole analogs and pharmaceutical compositions comprising the same are additionally described herein. Methods for preparing largazole analogs are likewise described.2018-03-01
20180057511ORGANIC ANION LITHIUM IONIC COCRYSTAL COMPOUNDS AND COMPOSITIONS - A cocrystal having the formula LiX.aM, or a solvate or hydrate thereof, wherein X is a conjugate base of an organic acid, M is a neutral organic molecule, and a is from 0.5 to 4, pharmaceutical compositions comprising such cocrystals, cocrystal solvates, or cocrystal hydrates, and methods of preparing such cocrystals, cocrystal solvates, or cocrystal hydrates, and such pharmaceutical compositions.2018-03-01
20180057512ZWITTERIONIC ZINC(II) CARBOXYLATE COMPOUNDS AND THEIR USE - A method of preparing a crystalline zwitterionic zinc(II)-carboxylate compound includes the steps of preparing a mixture of zinc(II) ions and a first pyridyl ligand having three carboxylic acid moieties; subjecting the mixture to conditions under which a precipitate is formed; separating the precipitate; adding a solvent and optionally a second pyridyl ligand to the separated precipitate; subjecting the obtained mixture to conditions under which crystals of the zwitterionic zinc(II)-carboxylate compound are formed; and separating the crystals of the zwitterionic zinc(II)-carboxylate compound. Preferably but not exclusively, the crystalline zwitterionic zinc(II)-carboxylate compound essentially consists of at least one 1D coordination polymer. The compounds are suitable for providing a sensing platform for detecting the presence or amount of target nucleic acid, particularly HIV-1 ds-DNA, with specificity, and, thus, a method of detecting a target nucleic acid sequence in a sample and a kit including the compounds and an oligonucleotide probe are also provided.2018-03-01
20180057513Transition Metal Complexes, Production and Use Thereof - Phosphasalen transition metal complexes are disclosed for use in alkene polymerization to produce polyolefins. The transition metal complexes are represented by the formula:2018-03-01
20180057514SILYLATION OF AROMATIC HETEROCYCLES BY EARTH ABUNDANT TRANSITION-METAL-FREE CATALYSTS - The present invention describes chemical systems and methods for silylating aromatic organic substrates, said system or method comprising or consisting essentially of a mixture of (a) at least one organosilane and (b) at least one strong base, the definition of strong base now also including hydroxide, especially KOH, said system being preferably, but not necessarily substantially free of a transition-metal compound, and said methods comprising contacting a quantity of the organic substrate with a mixture of (a) at least one organosilane and (b) at least one strong base, under conditions sufficient to silylate the aromatic substrate.2018-03-01
20180057515HETEROCYCLIC COMPOUND AND ORGANIC SOLAR CELL COMPRISING SAME - The present specification relates to a heterocyclic compound and an organic solar cell including the same.2018-03-01
20180057516REAGENTS USEFUL FOR SYNTHESIZING RHODAMINE-LABELED OLIGONUCLEOTIDES - The present disclosure provides reagents that can be used to label synthetic oligonucleotides with rhodamine dyes or dye networks that contain rhodamine dyes.2018-03-01
20180057517Metal Tricarbonyl Complexes Comprising Substituted Iminodiactic Acid Ligands and Uses as Radioisotope Tracers - This disclosure relates to compositions comprising substituted iminodiacetic acid ligands and metal tricarbonyl complexes containing the ligands and derivatives thereof. In certain embodiments, the metal tricarbonyl complexes are used as radioisotope tracers such as renal tracers. In certain embodiments, the metal complexes comprise 2018-03-01
20180057518SYNTHETIC MEMBRANE ANCHORS - A construct of the structure F—S2018-03-01
20180057519NON-CALORIC SWEETENERS AND METHODS FOR SYNTHESIZING - Disclosed are steviol glycosides referred to as rebaudioside V and rebaudioside W. Also disclosed are methods for producing rebaudioside M (Reb M), rebaudioside G (Reb G), rebaudioside KA (Reb KA), rebaudioside V (Reb V) and rebaudioside (Reb W).2018-03-01
20180057520NON-CALORIC SWEETENERS AND METHODS FOR SYNTHESIZING - Disclosed are steviol glycosides referred to as rebaudioside V and rebaudioside W. Also disclosed are methods for producing rebaudioside M (Reb M), rebausoside G (Reb G), rebaudioside KA (Reb KA), rebaudioside V (Reb V) and rebaudioside (Reb W).2018-03-01
20180057521NON-CALORIC SWEETENERS AND METHODS FOR SYNTHESIZING - Disclosed are steviol glycosides referred to as rebaudioside V and rebaudioside W. Also disclosed are methods for producing rebaudioside M (Reb M), rebausoside G (Reb G), rebaudioside KA (Reb KA), rebaudioside V (Reb V) and rebaudioside (Reb W).2018-03-01
20180057522NON-CALORIC SWEETENERS AND METHODS FOR SYNTHESIZING - Disclosed are steviol glycosides referred to as rebaudioside V and rebaudioside W. Also disclosed are methods for producing rebaudioside M (Reb M), rebausoside G (Reb G), rebaudioside KA (Reb KA), rebaudioside V (Reb V) and rebaudioside (Reb W).2018-03-01
20180057523PHILLYGENIN GLUCURONIC ACID DERIVATIVE AS WELL AS PREPARATION METHOD AND APPLICATION THEREOF - The present invention provides a novel phillygenin glucuronic acid derivative shown as a general formula (I).2018-03-01
20180057524COMPOUNDS FROM INVASIVE SALVINIAS AND METHODS OF USING THE SAME - In some embodiments, the compositions and methods relate to compounds isolated from plants in the Salviniaceae family, pharmaceutical compositions comprising the same, and methods of using the same.2018-03-01
20180057525SOLID PHASE PEPTIDE SYNTHESIS PROCESSES AND ASSOCIATED SYSTEMS - Systems and processes for performing solid phase peptide synthesis are generally described. Solid phase peptide synthesis is a known process in which amino acid residues are added to peptides that have been immobilized on a solid support. In certain embodiments, the inventive systems and methods can be used to perform solid phase peptide synthesis quickly while maintaining high yields. Certain embodiments relate to processes and systems that may be used to heat, transport, and/or mix reagents in ways that reduce the amount of time required to perform solid phase peptide synthesis.2018-03-01
20180057526NEW DIFLUOROKETAMIDE DERIVATIVES - The invention provides novel compounds having the general formula (I)2018-03-01
20180057527CARBAZOLE COMPOUND HAVING ANTI-VIRUS ACTIVITY - The present invention relates to a carbazole compound having anti-virus activity, and more particularly, to a novel compound selected from the group of consisting of a carbazole compound which shows excellent anti-proliferative efficacy against hepatitis C virus (HCV), a pharmaceutically acceptable salt thereof, a hydrate thereof, and an isomer thereof; an anti-virus pharmaceutical composition including the novel compound as an active ingredient; a pharmaceutical composition for preventing or treating liver diseases caused by hepatitis C virus; and a method of preparing the novel compound.2018-03-01
20180057528INDOLINE COMPOUNDS AS GRANZYME B INHIBITORS - Granzyme B inhibitor compounds, compositions that include the compounds, and methods for using the compounds. The compounds of the invention have advantageous water solubility and effectively inhibit Granzyme B.2018-03-01
20180057529PRO-AMB REVERSE TURN RESTRICTED BIOACTIVE PEPTIDE ANALOGUES - The present invention discloses novel peptides acting as angiotensin II analogue for therapeutic applications. Said peptides can be used for treatment of Alzheimer's and other neurological and cognitive disorders.2018-03-01
20180057530CYCLIC PEPTIDE COMPOUND, AND PREPARATION AND USE THEREOF - The present invention relates to a compound represented by formula (I). The present invention also relates to the use of a compound represented by formula (I) in the treatment of disorders resulting from cell proliferation and/or angiogenesis or disorders associated with or accompanying cell proliferation and/or angiogenesis.2018-03-01
20180057531MUC1-DERIVED PEPTIDE, AND PHARMACEUTICAL COMPOSITION FOR TREATMENT OR PREVENTION OF CANCER, IMMUNITY-INDUCING AGENT AND METHOD FOR MANUFACTURING ANTIGEN PRESENTING CELL USING SAME - The present invention provides a peptide that includes eight or more consecutive amino acid residues of amino acid sequence of one of Sequence ID Nos. 1 to 12 and that consists of eleven or less amino acid residues.2018-03-01
20180057532PEPTIDE HAVING EIGHT AMINO ACID SEQUENCES DERIVED FROM CAGE AND RETAINING ANTICANCER ACTIVITY AND ACTIVITY TO PROMOTE ANTICANCER DRUG SENSITIVITY OF ANTICANCER DRUG-RESISTANT CANCER CELLS - The present invention relates to a peptide having eight amino acid sequences derived from CAGE and retaining anticancer activity and activity to promote anticancer drug sensitivity of anticancer drug resistant cancer cells and, specifically, to a peptide, which has an amino acid sequence of SEQ ID NO: 1 (AQTGTGKT) and thus binds to the CAGE protein, thereby inhibiting an inter-linkage between CAGE and GSK3β, thus exhibiting anticancer activity and activity to promote anticancer drug sensitivity of anticancer drug resistant cancer cells, and to a pharmaceutical composition, containing the peptide, for anticancer use or anticancer drug aiding.2018-03-01
20180057533PEPTIDES CAPABLE OF REACTIVATING p53 MUTANTS - The invention provides peptides that can reactivate p53 mutants efficiently and specifically, as well as methods that allow the identification, selection and isolation of such peptides, in a precise, cost and time effective manner. In particular, there are provided mutant p53 reactivating peptides that can restore the native wild type p53 folding, and hence the tumor suppressor activity, to the mutant p53 protein. Such peptides are useful for treating various conditions and diseases in which p53 is mutated.2018-03-01
20180057534COMPOSITIONS AND METHODS FOR THE TREATMENT OF CAST NEPHROPATHY AND RELATED CONDITIONS - Provided are novel peptides of Formula SEQ ID No. 1:2018-03-01
20180057535COMPOSITIONS FOR PREVENTING AND/OR TREATING AN INFECTION BY AN HIV-1 VIRUS - The present invention relates to an immunogenic composition comprising an antigenic peptide of formula (I) below: Nt-S-X1-X2-X3-K-X4-Ct (I) [SEQ ID N° 1], wherein Nt consists of a peptide having from 0 to 50 amino acids in length, Ct consists of a peptide having from 0 to 50 amino acids in length, each of X1 to X4 consists of an amino acid residue, wherein: (i) X1 means the specific amino acid W or (ii) X1 means any amino acid residue excepted W, (i) X2 means the specific amino acid S or (ii) X2 means any amino acid residue excepted S, (i) X3 means the specific amino acid N or (ii) X3 means any amino acid residue excepted N, (i) X4 means the specific amino acid S or (ii) X4 means any amino acid residue excepted S, with the proviso that three out of the four amino acid residues X1, X2, X3 and X4 mean the specific amino acid defined in their respective meaning (i) above, and the remaining amino acid residue among X1 to X4 means any amino acid residue excepted the specific amino acid residue defined in its meaning (i), for preventing and/or treating an infection of an individual with an HIV-1 virus.2018-03-01
20180057536SELECTIVE DELIVERY MOLECULES AND METHODS OF USE - Disclosed herein is a selective delivery molecule comprising: (a) an acidic sequence (portion A) which is effective to inhibit or prevent the uptake into cells or tissue retention, (b) a molecular transport or retention sequence (portion B), and (c) a linker between portion A and portion B, and (d) at least one cargo moiety.2018-03-01
20180057537ANG (1-7) DERIVATIVE OLIGOPEPTIDES AND METHODS FOR USING AND PRODUCING THE SAME - The present invention provides oligopeptides, in particular, Ang-(1-7) derivatives, and methods for using and producing the same. In one particular embodiment, oligopeptides of the invention have higher blood-brain barrier penetration and/or in vivo half-life compared to the native Ang-(1-7), thereby allowing oligopeptides of the invention to be used in a wide variety of clinical applications including in treatment of cognitive dysfunction and/of impairment.2018-03-01
20180057538POTENT AND HIGHLY SOLUBLE PEGYLATED COMPSTATIN PEPTIDES - The disclosure provides for highly soluble PEGylated compstatin peptides, which exhibit high binding affinities for complement and therapeutic efficacy in vitro. The disclosure further provides for pharmaceutical compositions comprising the PEGylated compstatin peptides, and methods of treatment thereof.2018-03-01
20180057539MULTIMERIZATION OF RECOMBINANT PROTEIN BY FUSION TO A SEQUENCE FROM LAMPREY - The present invention relates to polymerized recombinant proteins, to recombinant nucleic acids coding for the polymerized recombinant proteins, to expression cassettes comprising the recombinant nucleic acids, to host cells transformed by the expression cassettes and to a method for multimerizing a recombinant protein. The polymerized proteins of the invention may be used in pharmaceutical or immunogenic compositions. In particular, the recombinant proteins may be antigens, antibodies or scaffolds. In particular, the polymerized recombinant protein may be an influenza haemagglutinin.2018-03-01
20180057540SIMIAN ADENOVIRUS NUCLEIC ACID-AND AMINO ACID-SEQUENCES, VECTORS CONTAINING SAME, AND USES THEREOF - The present invention relates to novel adenovirus strains with an improved seroprevalence. In one aspect, the present invention relates to isolated polypeptides of adenoviral capsid proteins such as hexon, penton and fiber protein and fragments thereof and polynucleotides encoding the same. Also provided is a vector comprising the isolated polynucleotide according to the invention and adenoviruses comprising the isolated polynucleotides or polypeptides according to the invention and a pharmaceutical composition comprising said vector, adenovirus, polypeptide and/or polynucleotide. The invention also relates to the use of the isolated polypeptides, the isolated polypeptides, the vector, the adenoviruses and/or the pharmaceutical composition for the therapy or prophylaxis of a disease.2018-03-01
20180057541SENECAVIRUS A ANTIGENS AND METHODS OF USE2018-03-01
20180057542THERAGNOSTIC PARTICLES - The present invention provides viral-based nanoparticles for therapeutic and diagnostic use, and methods for making and using the nanoparticles. Specifically, such nanoparticles comprise decoration-competent viral particles shells such as expanded capsids of phages, stabilized with engineered decoration proteins that have been linked to one or more compounds not naturally occurring on a wild type viral capsid.2018-03-01
20180057543PYOLYSIN METHODS AND COMPOSITIONS - Methods for improved cultivation media and culture conditions for 2018-03-01
20180057544MULTIVALENT CD20-BINDING MOLECULES COMPRISING SHIGA TOXIN A SUBUNIT EFFECTOR REGIONS AND ENRICHED COMPOSITIONS THEREOF - The present invention provides multivalent CD20-binding molecules, and compositions thereof, such as enriched compositions comprising large proportions of multivalent CD20-binding molecule relative to monovalent CD20-binding molecule. Certain multivalent CD20-binding molecules of the present invention comprise 1) two or more CD20 binding regions and 2) one or more Shiga toxin effector polypeptide regions derived from an A Subunit of a member of the Shiga toxin family. Certain multivalent CD20-binding molecules of the present invention, and compositions thereof, have uses for selective killing specific cell types and as therapeutics for the treatment of a variety of diseases, including cancers, tumors, and immune disorders. Certain multivalent CD20-binding molecules of the present invention, and compositions thereof, have uses for delivering agents into CD20-expressing cells, including for the intracellular labeling of CD20-expressing cells, collecting diagnostic information, and monitoring the treatment of variety diseases, such as cancers, tumors, and immune disorders which involve CD20-expressing cells.2018-03-01
20180057545EVOLUTION OF BT TOXINS - The disclosure provides amino acid sequence variants of 2018-03-01
20180057546MINIMIZED CYANOBACTERIAL MICROCOMPARTMENT FOR CARBON DIOXIDE FIXATION - A fusion chimeric protein is described herein that can assemble a functional carboxysome core, which is able to fix carbon by taking atmospheric carbon dioxide and converting it into useful caron-containing compounds such as 3-phosphoglycerate (3-PGA).2018-03-01
20180057547DIAGNOSTIC AND THERAPEUTIC EPITOPE, AND TRANSGENIC PLANT - A method of diagnosing coeliac disease, or susceptibility to coeliac disease, in an individual comprising: 2018-03-01
20180057548IMPROVED SILK FIBERS - Methods and compositions are provided for improved proteinaceous block copolymer fibers based on long repeat units having molecular weight of greater than about 10 kDal. Each repeat unit includes more than about 150 amino acid residues that are organized into a number of “quasi-repeat units.” The fibers have improved mechanical properties that better recapitulate those of C the native silk fibers.2018-03-01
20180057549SAXATILIN-FC FUSION PROTEIN AND USE THEREOF - The present invention relates to a saxatilin derivative having an increased half life and a use thereof. The saxatilin derivative of the present invention has thrombolytic ability similar to that of saxatilin, which is the mother protein, a remarkably increased protein half life, and efficiently dissolves, for long period of time, blood clots already formed in blood vessels of an animal model with a FeCl2018-03-01
20180057550METHODS AND COMPOSITIONS FOR REGENERATING TISSUES - Provided are methods for promoting the healing of injuries to tendons and ligaments by administering a NELL1 protein or a nucleic acid encoding a NELL1 protein to a subject in need thereof. Also provided are NELL1 compositions and methods for promoting tissue regeneration, promoting the healing of wounds, and enhancing fibroblast migration, proliferation, or both migration and proliferation.2018-03-01
20180057551ALZHEIMER ABETA PEPTIDE BINDING POLYPEPTIDE - The present disclosure relates to a class of engineered polypeptides having a binding affinity for amyloid β (Aβ) peptides (in the following referred to as Aβ), comprising the amino acid sequence EX2018-03-01
20180057552A PEPTIDE OR COLLECTION OF PEPTIDES DERIVED FROM AMYLOID PRECURSOR PROTEIN - The present invention relates to a peptide or collection of peptides derived from amyloid precursor protein (APP). The present invention also relates to uses of such peptide or collection of peptides, in particular as a diagnostic marker and/or as a drug target.2018-03-01
20180057553CONJUGATE AND USE THEREOF - A technique is provided which enables simple and low-cost purification of biologically active proteins by means of a conjugate of a target substance capturing molecule and a protein which comprises the amino acid sequence in SEQ ID NO:1, or a protein which comprises the amino acid sequence obtained by deleting, substituting or adding one or multiple amino acids in the amino acid sequence in SEQ ID NO: 1 and which has binding activity to a compound having —OH or —OR2018-03-01
20180057554FIBROBLAST GROWTH FACTOR (FGF) 1 MUTANTS AND METHODS OF USE TO REDUCE BLOOD GLUCOSE - The present disclosure provides FGF1 mutant proteins, which include an N-terminal deletion, point mutation(s), or combinations thereof. In some examples, the mutant FGF1 proteins have reduced mitogenic activity. Also provided are nucleic acid molecules that encode such proteins, and vectors and cells that include such nucleic acids. The disclosed FGF1 mutants can reduce blood glucose in a mammal, and in some examples are used to treat a metabolic disorder.2018-03-01
20180057555TARGETING OF CYTOKINE ANTAGONISTS - The present invention relates to a fusion protein, comprising a cytokine antagonist and a targeting moiety, preferably an antibody or anti-body like molecule. In a preferred embodiment, the cytokine antagonist is a modified cytokine which binds to the receptor, but doesn't induce the receptor signalling. The invention relates further to a fusion protein according to the invention for use in treatment of cancer and immune- or inflammation-related disorders.2018-03-01
20180057556CYCLIC GALANIN-ANALOGS AND USES THEREOF - The invention generally relates to the field of medicine and pharmacology. More particularly, it relates to novel analogs of galanin, and the use thereof in therapy. Provided is a cyclic peptide analog of galanin, wherein the galanin analog comprises a (methyl)Lanthionine bridge and wherein the analog has the general formula “X1-X2-X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16-X17-X18-X19-X20-X21-X22-”, or a truncated variant thereof lacking X1 and/or up to 11 of the C-terminal residues, wherein two residues selected from the group consisting of X3, X4, X6, X7, X10 and X13-X19 together form a Lanthionine bridge of the structure Ala-S-Ala, or a methyl Lanthionine bridge of the structure Abu-S-Ala or Ala-S-Abu.2018-03-01
20180057557METHODS AND COMPOSITIONS OF A FOLLICLE STIMULATING HORMONE RECEPTOR IMMUNORECEPTOR OR CHIMERIC ANTIGEN RECEPTOR - The present invention relates to compositions and methods for diagnosing and treating diseases, disorders or conditions associated with dysregulated expression of FSHR. The invention provides novel peptides that specifically bind to Follicle-stimulation hormone receptor (FSHR).2018-03-01
20180057558Synthesis of GLP-1 Peptides - Disclosed are processes for the synthesis of GLP-1 peptides, such as liraglutide and semaglutide, and a process for purifying liraglutide.2018-03-01
20180057559INSULIN ANALOGUES WITH A GLUCOSE-REGULATED CONFORMATIONAL SWITCH - A two-chain insulin analogue contains an A chain modified by (i) a monomeric glucose-binding element at or near its N terminus and (ii) a B chain modified by at or near its C terminus by an element that reversibly binds to the monomeric glucose-binding element such that this linkage is displaceable by glucose. The monomeric glucose-binding element may be phenylboronic acid derivative (optionally halogenated). The B chain may be modified by a diol-containing element derived from a monosaccharide, disaccharide or oligosaccharide, a non-saccharide diol-containing moiety or a α-hydroxycarboxylate-containing moiety. The analogue can be manufactured by trypsin-mediated semi-synthesis. Formulations can be at strengths U-10 to U-1000 in soluble solutions at pH 7.0-8.0 with or without zinc ions at a molar ratio of 0.0-3.0 ions per insulin analogue monomer. A patient with diabetes mellitus may be treated with subcutaneous, intraperitoneal, or oral administration of a physiologically effective amount of the insulin analogue.2018-03-01
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