25th week of 2017 patent applcation highlights part 27 |
Patent application number | Title | Published |
20170174655 | VITAMIN D RECEPTOR-COREGULATOR INHIBITORS - Described herein are compounds, pharmaceutical compositions and methods for inhibiting the expression of a vitamin D receptor target gene, inhibiting interactions between the vitamin D receptor and at least one vitamin D receptor coactivator, for treating cancer in a subject, and for inhibiting angiogenesis in a subject. | 2017-06-22 |
20170174656 | HISTONE DEMETHYLASE INHIBITORS - The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like. | 2017-06-22 |
20170174657 | 1H-INDAZOLE-3-CARBOXAMIDE COMPOUNDS AS GLYCOGEN SYNTHASE KINASE 3 BETA INHIBITORS - The present invention relates to the 1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta (GSK-3β) inhibitors and to their use in the treatment of GSK-3β-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; (viii) epilepsies; and (ix) neuropathic pain. | 2017-06-22 |
20170174658 | PYRIDIN-2(1H)-ONE QUINOLINONE DERIVATIVES AS MUTANT-ISOCITRATE DEHYDROGENASE INHIBITORS - The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: | 2017-06-22 |
20170174659 | PYRAZINES MODULATORS OF GPR6 - The present invention provides compounds of formula I: | 2017-06-22 |
20170174660 | HEAT SHOCK PROTEIN 70 (HSP-70) RECEPTOR LIGANDS - Inducible HSP70 is overexpressed in a wide spectrum of human tumors and its expression correlates with metastasis and poor outcomes to radiation and chemotherapy in patients. Identification of small molecule inhibitors of HSP70 pose a new therapy to cancer treatment. HS72, a benzimidazole piperidinyl carboxamide has been identified as an allosteric inhibitor for HSP70 and has demonstrated good tumor growth inhibition in vivo. | 2017-06-22 |
20170174661 | SALT FORMS AND POLYMORPHS OF (R)-1-(4-(6-(2-(4-(3,3-DIFLUOROCYCLOBUTOXY)-6-METHYLPYRIDIN-2-YL)ACETAMID- O) PYRIDAZIN-3-YL)-2-FLUOROBUTYL)-N-METHYL-1H-1,2,3-TRIAZOLE-4-CARBOXAMIDE - Disclosed herein is the compound (R)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl)acetamido)pyridazin-3-yl)-2-fluorobutyl)-N-methyl-1H-1,2,3-triazole-4-carboxamide, and salt forms and polymorphs thereof demonstrating improved exposure after oral dosing. Methods of inhibition GLS1 activity in a human or animal subject are also provided. | 2017-06-22 |
20170174662 | CRYSTALLINE AND AMORPHOUS FORMS OF OLAPARIB - Disclosed are a novel crystalline form and an amorphous form of Olaparib, and the process for their preparation. | 2017-06-22 |
20170174663 | HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS - The present invention encompasses compounds of the formula (I) | 2017-06-22 |
20170174664 | SUBSTITUTED 3-(5-MEMBERED UNSATURATED HETEROCYCLYL-1, 3-DIHYDRO-INDOL-2-ONE'S AND DERIVATIVES THEREOF AS KINASE INHIBITORS - The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. | 2017-06-22 |
20170174665 | POTENT SOLUBLE EPOXIDE HYDROLASE INHIBITORS - The invention discloses a new series of inhibitors of soluble epoxide hydrolase (sEH) with improved physical properties that enhance their druglikeness to treat sEH associated diseases such as chronic diabetic neuropathic pain. | 2017-06-22 |
20170174666 | PYRAZOLONE COMPOUNDS AND USES THEREOF - The invention disclosed herein is directed to compounds of Formula I [Formula should be entered here] and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, acute or chronic myeloid leukemia, melanoma, and other cancers. The invention also includes pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to methods of treating prostate, breast, ovarian, liver, kidney, colon, pancreatic, human chronic lymphocytic leukemia, acute or chronic myeloid leukemia, melanoma and other cancers. The invention disclosed herein is further directed to methods of treating prostate, breast, ovarian, liver, kidney, colon, pancreatic, human chronic lymphocytic leukemia, acute or chronic myeloid leukemia, melanoma and other cancers through the administration of a therapeutically effective amount of a selective PPARα antagonist. The compounds and pharmaceutical compositions of the invention are also useful in the treatment of viral infections, such as HCV infections and HIV infections. | 2017-06-22 |
20170174667 | CYANOAMINO (AZA)BENZOFURAN COMPOUNDS FOR THE TREATMENT OF HEPATITIS C - Compounds of Formula (I), including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV: (I) | 2017-06-22 |
20170174668 | SULFOXIMINE SUBSTITUTED QUINAZOLINES FOR PHARMACEUTICAL COMPOSITIONS - This invention relates to novel sulfoximine substituted quinazoline derivatives of formula (I), wherein Ar, R | 2017-06-22 |
20170174669 | POCHOXIME CONJUGATES USEFUL FOR THE TREATMENT OF HSP90 RELATED PATHOLOGIES - The present invention includes novel derivatives, analogs, and intermediates of the natural products radicicol, pochonins, pochoximes, and their syntheses. The present invention also provides a pharmaceutical composition comprising the present compound and the use of the compound as inhibitors of kinases and of the enzyme family known as heat shock protein 90 (HSP90). | 2017-06-22 |
20170174670 | COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISEASES - Compounds, and compositions, methods, and uses thereof, are described herein for treating neurodegenerative diseases and disorders. In particular, vasopressin receptor modulators, and compositions, methods and uses thereof, are described herein for treating neuropsychiatric aspects of neurodegenerative diseases such as Huntington's Disease, Parkinson's Disease, and Alzheimer's Disease. | 2017-06-22 |
20170174671 | HETEROCYCLIC 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. | 2017-06-22 |
20170174672 | FUSED (HETERO)CYCLIC COMPOUNDS AS S1P MODULATORS - The invention relates to (hetero)cyclic compounds as S1P modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment, alleviation or prevention of diseases or disorders mediated by an S1P receptor. | 2017-06-22 |
20170174673 | PYRIDAZINE COMPOUNDS AS JAK INHIBITORS - In one aspect, the invention provides a compound according to formula I, as well as tautomers, pharmaceutically acceptable salts, and hydrates thereof. Pharmaceutical compositions, methods of inhibiting Janus kinases (JAKs), and methods for treating a condition or disorder mediated at least in part by JAK kinase activity are also described. | 2017-06-22 |
20170174674 | HYDROXYALKYLAMINE- and HYDROXYCYCLOALKYLAMINE-SUBSTITUTED DIAMINE-ARYLSULFONAMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS - Disclosed are compounds of Formula A, or a salt thereof: | 2017-06-22 |
20170174675 | Modulators of Cystic Fibrosis Transmembrane Conductance Regulator - The present invention relates to modulators of cystic fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating CFTR mediated diseases using such modulators. | 2017-06-22 |
20170174676 | CHLORINATED NAPTHALENETETRACARBOXYLIC ACID DERIVATIVES, PREPARATION THEREOF AND USE THEREOF IN ORGANIC ELECTRONICS - The present invention relates to chlorinated naphthalenetetracarboxylic acid derivatives, preparation thereof and use thereof as charge transport materials, exciton transport materials or emitter materials. | 2017-06-22 |
20170174677 | TETRAHYDROPYRIDOPYRAZINES MODULATORS OF GPR6 - The present invention provides compounds of formula I: | 2017-06-22 |
20170174678 | NOVEL ANTIVIRAL COMPOUNDS AND METHODS USING SAME - The present invention includes bicyclic compounds that are useful in preventing or treating viral infections, such as viral infections caused by a filovirus, arenavirus, rhabdovirus, paramyxovirus, and/or retrovirus. The present invention further includes compositions comprising such compounds, and methods of treating a viral infection in a subject using such compounds. | 2017-06-22 |
20170174679 | HETEROCYCLIC 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. | 2017-06-22 |
20170174680 | P2X7 MODULATORS - The present invention is directed to a compound of Formula (I) or (Ia) | 2017-06-22 |
20170174681 | Pyrazolopyridine Derivatives, Preparation Process Therefor And Therapeutic Use Thereof - The invention relates to FGF-inhibiting pyrazolopyrimidine derivatives of general formula (I) | 2017-06-22 |
20170174682 | HETEROCYCLIC COMPOUND - Provided is a compound or a salt thereof, which has an excellent JAK inhibitory action, and is useful as a prophylactic or therapeutic agent for autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's syndrome, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like. The present invention relates to a compound represented by the formula (I) | 2017-06-22 |
20170174683 | ANTIBACTERIAL CYCLOPENTA[C]PYRROLE SUBSTITUTED 3,4-DIHYDRO-1H-[1,8]NAPHTHYRIDINONES - The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds. | 2017-06-22 |
20170174684 | ERGOLINE COMPOUNDS AND USES THEREOF - Provided herein are ergoline compounds and pharmaceutical compositions thereof. In some embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT | 2017-06-22 |
20170174685 | ERGOLINE COMPOUNDS AND USES THEREOF - Provided herein are ergoline compounds and pharmaceutical compositions thereof. In some embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT | 2017-06-22 |
20170174686 | PROCESS FOR PREPARATION OF SODIUM (2S, 5R)-6-(BENZYLOXY)-7-OXO-1,6-DIAZABICYCLO[3.2.1]OCTANE-2-CARBOXYLATE | 2017-06-22 |
20170174687 | FUSED QUINOLINE COMPUNDS AS PI3K, mTOR INHIBITORS - (Formula I), The present invention relates to the compounds of formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with cancers associated with protein kinases, to their use as medicaments for use in the production of inhibition of mTor, pi3k reducing effects in warm-blooded animals such as humans. | 2017-06-22 |
20170174688 | Substituted Indoles - The invention provides for compounds of formula (I) | 2017-06-22 |
20170174689 | SUBSTITUTED INDOLE MCL-1 INHIBITORS - The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein. | 2017-06-22 |
20170174690 | SUBSTITUTED 4,5,6,7-TETRAHYDRO-PYRAZOLO[1,5-a]PYRAZINE DERIVATIVES AND 5,6,7,8-TETRAHYDRO-4H-PYRAZOLO[1,5-a][1,4]DIAZEPINE DERIVATIVES AS ROS1 INHIBITORS - The present invention relates to substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrazine derivatives and 5,6,7,8-tetrahydro-4H-pyrazolo[1,5-a][1,4]diazepine derivatives of formula (I) | 2017-06-22 |
20170174691 | Protein Kinase Conjugates and Inhibitors - The invention relates to protein conjugates that contain a protein kinase containing a cysteine residue in the ATP binding site and an inhibitor that is covalently and irreversibly bonded to said cysteine residue, such that the activity of the protein kinase is irreversibly inhibited. The invention also relates to compounds that irreversibly inhibit protein kinases. | 2017-06-22 |
20170174692 | INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7) - The present invention provides novel compounds described herein, such as of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject. | 2017-06-22 |
20170174693 | SOLUBLE GUANYLATE CYCLASE STIMULATORS - The invention provides compounds of the Formula (I) | 2017-06-22 |
20170174694 | PYRROLOPYRIMIDINE COMPOUNDS, USE AS INHIBITORS OF THE KINASE LRRK2, AND METHODS FOR PREPARATION THEREOF - The present disclosure is concerned with certain pyrrolopyrimidine compounds that are capable of inhibiting certain protein kinases, and especially the leucine-rich repeat kinase 2 (LRRK2) protein. Compounds of the present disclosure can be used to treat a number of disorders caused by or associated with abnormal LRRK2 kinase activity. Compounds of the present disclosure can be used to treat disorders including neurodegenerative diseases such as Parkinson's disease; precancerous conditions and cancer; autoimmune disorders such as Crohn's disease, rheumatoid arthritis and psoriasis; and leprosy (Hansen's disease). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2017-06-22 |
20170174695 | NEW SPIRO[3H-INDOLE-3,2'-PYRROLIDIN]-2(1H)-ONE COMPOUNDS AND DERIVATIVES AS MDM2-P53 INHIBITORS - The present invention encompasses compounds of formula (I) | 2017-06-22 |
20170174696 | 6H-FURO[2,3-E]INDOLE COMPOUNDS FOR THE TREATMENT OF HEPATITIS C - Compounds of Formula I, including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 2017-06-22 |
20170174697 | BENZIMIDAZOLE DERIVATIVES AS ERBB TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF CANCER - Provided herein are benzimidazole derivatives, for example, of Formula (I), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease. | 2017-06-22 |
20170174698 | METHOD FOR THE SYNTHESIS OF PRIMARY ISOHEXIDE AMINES - A method for synthesizing a primary amine, having the steps of: a) providing at least one dianhydrohexitol, and b) aminating the dianhydrohexitol by reacting same with ammonia, the amination being performed by heterogeneous catalysis using a hydrogenation catalyst in the presence of hydrogen. | 2017-06-22 |
20170174699 | COMPOUNDS FOR THE TREATMENT OF CANCER AND INFLAMMATORY DISEASE - Provided herein are compounds that inhibit the phosphorylation of MAPK and thus are useful in compositions and methods for treating cancer and inflammatory disease. | 2017-06-22 |
20170174700 | Biotin Derivatives - Biotin derivatives, methods of using the biotin derivatives and kits comprising the biotin derivatives. | 2017-06-22 |
20170174701 | CYCLIC CARBONATE MONOMER CONTAINING DOUBLE-SULFUR FIVE-MEMBERED RING FUNCTIONAL GROUP, AND PREPARATION METHOD THEREOF - Disclosed are a cyclic carbonate monomer containing a double-sulfur five-membered ring functional group, and preparation method thereof. The cyclic carbonate monomer can be simply and efficiently synthesized without protection and deprotection processes. The cyclic carbonate monomer of the present invention can be utilized to obtain polycarbonate having a controllable molecular weight and molecular weight distribution via ring opening polymerization, and has biodegradability and reduction-sensitive reversible crosslinking properties. The present invention can be used in a carrier having controllably released drug, a biological tissue scaffold or a biochip. | 2017-06-22 |
20170174702 | BROMODOMAIN-INHIBITING COMPOUNDS AND PHARMACEUTICAL COMPOSITION COMPRISING SAME FOR PREVENTING OR TREATING A CANCER - Provided is a novel compound having bromodomain and extra terminal domain (BET) protein inhibiting activities, and a pharmaceutical composition comprising the same which can be useful for prevention or treatment of precancerous transformation or cancer. | 2017-06-22 |
20170174703 | QUINOLINE DERIVATIVES AS SMO INHIBITORS - Disclosed are quinoline derivatives as hedgehog pathway inhibitors, especially as SMO inhibitors. Compounds of the present invention can be used in treating diseases relating to hedgehog pathway including cancer. | 2017-06-22 |
20170174704 | QUINOXALINE COMPOUNDS AND USES THEREOF - This invention provides compounds of formula I and subsets thereof: wherein T, J, R, R | 2017-06-22 |
20170174705 | CONDENSED CYCLIC COMPOUND, COMPOSITION INCLUDING THE CONDENSED CYCLIC COMPOUND, ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE CONDENSED CYCLIC COMPOUND, AND METHOD OF MANUFACTURING THE ORGANIC LIGHT-EMITTING DEVICE - A condensed cyclic compound represented by Formula (1): | 2017-06-22 |
20170174706 | SPIRO-OXAZINES, INDOLINONES AND PREPARATION THEREOF - The present invention relates to novel spiro-oxazine analogues of Formula-I and Indolinone compounds of Formula-II or positional isomers, or stereoisomers, or derivatives, or pharmaceutically acceptable salt thereof. Formula-I Formula-II Further the invention provides transition-metal free multicomponent reaction (MCR) process for the preparation of said compounds of Formula-I and II using aryne precursor, N-substituted isatin and N-heteroaromatic compound as the nucleophile, under mild condition leading to formation of desired complex of spiro-oxazine analogues (I) and indolinone analogues (II) in high yield and selectivity. | 2017-06-22 |
20170174707 | HETEROCYCLE-SUBSTITUTED BICYCLIC AZOLE PESTICIDES - Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, | 2017-06-22 |
20170174708 | PENTACYCLIC PYRIDOINDOLOBENZO[b,e]DIAZEPINES AND THIAZEPINES FOR TREATING CNS DISORDERS - The present invention discloses pyridoinolobenzo[b,e]diazepine and thiazepine derivatives of Formula 1, | 2017-06-22 |
20170174709 | TRICYCLIC BENZOXABOROLES AS ANTIBACTERIAL AGENTS - The present invention provides a tricyclic compound represented by general formula (I), a pharmaceutical salt thereof, or a stereoisomer thereof exhibits excellent antibacterial activity against Gram-negative bacteria resistant bacteria thereof, and also being excellent in terms of safety. Furthermore, the present invention provides production processes, pharmaceutical compositions comprising a tricyclic compound, a pharmaceutically acceptable salt thereof, or a stereoisomer thereof as an active ingredient and use thereof as a pharmaceutical agent. The compounds of the present invention are useful for the treatment and/or prevention of disease such as complicated urinary tract infections (cUTIs), nosocomial pneumonia, intra-abdominal infections (IAIs) or bacteremia. | 2017-06-22 |
20170174710 | COMPOUNDS THAT ARE S1P MODULATING AGENTS AND/OR ATX MODULATING AGENTS - Compounds of formula (I) can modulate the activity of one or more S1P receptors and/or the activity of autotaxin (ATX). | 2017-06-22 |
20170174711 | ACID GENERATOR AND COMPOSITION - Acid generators and compositions are disclosed. Such acid generators and compositions are applicable to functional materials such as adhesives, sealant or antireflection coating (ARC). | 2017-06-22 |
20170174712 | Silicon-containing azodicarboxamides, their preparation and use - A silicon-containing azodicarboxamide is obtainable by reacting an azodicarboxy compound with an aminosilane. The silicon-containing azodicarboxamides are suitable for use in cable sheathing, hoses, drive belts, conveyor belts, roll coverings, footwear soles, ring seals and damping elements. | 2017-06-22 |
20170174713 | TANK-BINDING KINASE INHIBITOR COMPOUNDS - Compounds having the following formula (I) and methods of their use and preparation are disclosed: | 2017-06-22 |
20170174714 | PROCESS OF PREPARING CYCLIC PHOSPHONATE ESTER, CYCLIC PHOSPHONATE ESTER PREPARED THEREFROM AND INDUSTRIAL APPLICATIONS CONTAINING THE SAME - There is provided herein a process for preparing cyclic phosphonate ester comprising reacting a glycol with at least one of phosphonic acid and phosphinic acid in the presence of a solvent. There is also provided a flame retardant comprising the cyclic phosphonate ester and industrial applications containing a flame retardant effective amount of the cyclic phosphonate ester. | 2017-06-22 |
20170174715 | BIDENTATE DIPHOSPHORAMIDITES WITH A PIPERAZINE GROUP AS LIGANDS FOR HYDROFORMYLATION - The invention relates to Rh, Ru, Co and Ir complexes comprising bidentate diphosphoramidites as ligands and to the use thereof as catalysts for the hydroformylation of olefins. The invention also relates to a process for preparing an aldehyde from an olefin using the complexes or ligands mentioned. | 2017-06-22 |
20170174716 | FUMARATE-CO-RELEASING MOLECULE HYBRIDS, THEIR USE IN THE TREATMENT OF INFLAMMATORY OR CARDIOVASCULAR DISEASES AND THEIR PROCESS OF PREPARATION - The present invention relates to hybrid fumarate-CO-releasing molecules capable of increasing heme oxygenase-1 (HO-1) activity and HO-1 protein expression and simultaneously releasing CO, their synthesis and their use in therapeutic applications, in particular their use in the treatment of inflammatory or cardiovascular diseases. | 2017-06-22 |
20170174717 | METHOD OF SEPARATING BETANIN FROM RED QUINOA BY SUPERCRITICAL FLUID FRACTIONATION - The present invention relates to a method of separating betanin from red quinoa by supercritical fluid fractionation, including: mixing an extract of red quinoa with an ethanol/water mixture to obtain a mixture of red quinoa/ethanol/water; and separating betanin from the mixture of red quinoa/ethanol/water by supercritical fluid fractionation, which operates under a pressure between 2300 to 4400 psi at a temperature between 35 to 65° C. for a period of time between 15 to 90 minutes. | 2017-06-22 |
20170174718 | SUBSTITUTED 4-PHENYL PYRIDINE COMPOUNDS AS NON-SYSTEMIC TGR5 AGONISTS - The invention relates to non-systemic TGR5 agonist useful in the treatment of chemotherapy-induced diarrhea, diabetes, Type II diabetes, gestational diabetes, impaired fasting glucose, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity, metabolic syndrome, ulcerative colitis, Crohn's disease, disorders associated with parenteral nutrition especially during short bowel syndrome, and irritable bowel syndrome (IBS), and other TGR5 associated diseases and disorders, having the Formula: | 2017-06-22 |
20170174719 | PROCESS FOR THE PURIFICATION OF FLUTICASONE PROPIONATE USING A KETONE SOLVENT AND WATER AS ANTI-SOLVENT - The present disclosure relates to an improved process for the purification of fluticasone propionate by: a) dissolving fluticasone propionate in a ketone solvent to produce a mixture, b) heating the mixture slowly for 1-2 hours to get a clear solution, c) adding water to the step (b) solution at 50-60° C., d) cooling to −5° C. to 10° C., and e) isolating fluticasone propionate. | 2017-06-22 |
20170174720 | CATIONIC STEROIDAL ANTIMICROBIAL SALTS - Disclosed herein are acid addition salts of cationic steroidal antimicrobials (“CSAs” or “ceragenins”) and methods of making the same. Particularly advantageous salt forms are identified, such as 1,5-naphthalenedisulfonic acid addition salts and sulfate addition salts. The acid addition salts may be formulated for treating subjects with ailments responsive to CSAs, including but not limited to treating bacterial infections. Accordingly, some embodiments include formulations and methods of administering acid addition salts of CSAs. | 2017-06-22 |
20170174721 | BUFFER SYSTEM FOR PROTEIN PURIFICATION - A method for purifying a protein using a simplified, sodium chloride-free buffer system that consists of two components (acid and base pairs) for appropriate solution pH control; and a third component for ionic strength control, where the third component is the sodium salt conjugate base. | 2017-06-22 |
20170174722 | LLP2A-BISPHOSPHONATE CONJUGATES FOR OSTEOPOROSIS TREATMENT - The present invention provides compounds and pharmaceutical compositions of a peptidomimetic ligand, e.g. LLP2A, conjugated with a bisphosphonate drug, e.g. Alendronate. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of osteoporosis and for the promotion of bone growth due to their specificity for the α | 2017-06-22 |
20170174723 | BI-TERMINAL PEGYLATED INTEGRIN-BINDING PEPTIDES AND METHODS OF USE THEREOF - The present invention provides bi-terminal PEGylated peptide conjugates that target an integrin such as α | 2017-06-22 |
20170174724 | BIOLOGICALLY ACTIVE PEPTIDES - A peptide or peptide derivative comprising:
| 2017-06-22 |
20170174725 | PROCESSES FOR THE PREPARATION OF OXYTOCIN ANALOGUES - Provided herein is a process for the preparation of oxytocin receptor agonists that have the potential to be used for the treatment of neurological disorders. | 2017-06-22 |
20170174726 | STABILIZED PEPTOID-PEPTIDE HYBRIDS AND USES THEREOF - The current invention pertains to stabilized peptoids or peptoid-peptide hybrids. The peptoids or peptoid-peptide hybrids are stabilized by side chain-side to side chain linkages and/or backbone cyclization. The current invention also provides a positional library scanning method for identification of peptoids or peptoid-peptide hybrids having a desired biological activity. | 2017-06-22 |
20170174727 | TFPI INHIBITORS AND METHODS OF USE - The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. Peptide complexes also are provided. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, treat a blood coagulation disorder in a subject, purify TFPI, and identify a TFPI-binding compound. | 2017-06-22 |
20170174728 | Soluble Forms of Hendra and Nipah Virus G Glycoprotein - This invention relates to soluble forms of G glycoprotein from Hendra and Nipah virus. In particular, this invention relates to compositions comprising soluble forms of G glycoprotein from Hendra and Nipah virus and also to diagnostic and therapeutic methods using the soluble forms of G glycoprotein from Hendra and Nipah virus. Further, the invention relates to therapeutic antibodies including neutralizing antibodies, and vaccines for the prevention and treatment of infection by Hendra and Nipah viruses. | 2017-06-22 |
20170174729 | MODIFICATION OF CUPREDOXIN DERIVED PEPTIDES AND METHODS OF USE THEREOF - The present invention provides modified cupredoxin derived peptides with pharmacologic activity that have improved pharmacokinetic properties, and methods to use them to treat mammals suffering from various conditions related to the pharmacologic activities. Modifications of the cupredoxin derived peptides include amino acid sequence variants and structural derivations that increase the plasma half-life of the peptide, increase the specific activity of the pharmacologic activity, decrease immunogenicity, and decrease the biotransformation of the peptides. The modified cupredoxin derived peptides can be used in methods to treat mammals for cancer, conditions related to inappropriate angiogenesis, viral and bacterial infections, and specifically HIV and malaria, conditions related to ephrin signaling, and to deliver cargo compounds, including diagnostic compounds, to cancer cell | 2017-06-22 |
20170174730 | BLUE LIGHT-ACTIVATED ION CHANNEL MOLECULES AND USES THEREOF - The invention, in some aspects relates to light-activated ion channel polypeptides and encoding nucleic acids and also relates in part to compositions comprising light-activated ion channel polypeptides and methods using light-activated ion channel polypeptides to alter cell activity and function. | 2017-06-22 |
20170174731 | TOXIC PEPTIDE PRODUCTION, PEPTIDE EXPRESSION IN PLANTS AND COMBINATIONS OF CYSTEINE RICH PEPTIDES - New insecticidal proteins, nucleotides, peptides, their expression in plants, methods of producing the peptides, new processes, production techniques, new peptides, new formulations, and new organisms, a process which increases the insecticidal peptide production yield from yeast expression systems. The present invention is also related and discloses selected endotoxins we call cysteine rich insecticidal peptides (CRIPS) which are peptides derived from | 2017-06-22 |
20170174732 | NANOBODY-FLOURESCENT PROTEIN FUSION - We describe the rational structure-based design of monomeric and dimeric forms of a nanobody-enhanced GFP (termed vsfGFP) that demonstrates ˜1.3-fold higher brightness than sfGFP in a monomeric form and ˜2.5-fold higher brightness in a dimeric form. These new vsfGFP variants demonstrate high stability and brightness in both bacterial and eukaryotic cells and are thus ideal for in vivo imaging applications. The combination of higher brightness, facile folding, stable expression, and tunable dimerization makes them ideal partners in essentially all in vitro applications already described for fluorescent proteins, including antibody fusion-based molecular probes, for which the higher brightness and tunable dimerization provide distinct advantages. Furthermore, the vsfGFP variants retain folding properties of sfGFP that enable bright fluorescence in oxidizing environments such as the bacterial periplasm. In particular, periplasmic expression enables the general construction of functional, fluorescent single domain antibody fusions, markedly enhancing the breadth and utility and reducing the cost of these molecular probes. Generalization of the vGFP strategy should provide similar improvements to other fluorescent proteins and may be extendable to higher order (and thus higher brightness) complexes. | 2017-06-22 |
20170174733 | CHAGASIN-BASED SCAFFOLD COMPOSITIONS, METHODS, AND USES - Provided are novel, non-naturally occurring chagasin scaffold proteins derived from chagasin or chagasin-like protease inhibitor proteins. Also provided are libraries of non-naturally occurring chagasin scaffold proteins and methods of using such libraries to generate non-naturally occurring chagasin scaffold proteins that specifically bind to a target ligand. The present invention further provides methods of using non-naturally occurring chagasin protein scaffold that bind to a target ligand, including diagnostic and therapeutic compositions and methods. The invention also provides novel non-naturally occurring chagasin scaffold proteins that specifically bind low density lipoprotein receptor-related protein 6 (LRP6) and novel non-naturally occurring chagasin scaffold proteins that specifically bind vascular endothelial growth factor (VEGF). | 2017-06-22 |
20170174734 | DR6 Receptor Mediates the Leukemia Differentiation Activity of Angiocidin: A Potent Anti-Tumor Peptide - The present invention provides compositions and methods of treating cancer by inducing the cellular differentiation activity of angiocidin. | 2017-06-22 |
20170174735 | COMPOSITIONS AND METHODS RELATING TO THE TREATMENT OF DISEASES - The present invention relates to compositions and methods for promoting the induction of a cell-mediated immune response (such as that mediated by Th1 cells) and the suppression of a humoral or allergic immune response (such as that mediated by Th2 and Th17 cells). In particular, the invention relates to compositions and methods for preventing or treating allergy, such as food allergy, and associated allergic diseases, and conditions where an exaggerated Th17 response plays a detrimental role. The invention further extends to the use of the compositions of the invention in the treatment and/or prophylaxis of allergy and associated allergic diseases and also of cancer. | 2017-06-22 |
20170174736 | LONG-ACTING RECOMBINANT HUMAN FOLLICLE-STIMULATING HORMONE-FC FUSION PROTEIN - Recombinant Fc fusion proteins of human follicle-stimulating hormone (hFSH) with in vivo biological activities comparable to those of human follicle-stimulating hormone are disclosed. A recombinant hFSH-Fc fusion protein comprises β subunit of hFSH (hFSH β), CTP, α subunit of hFSH (hFSH α), a flexible peptide linker, and human IgG2 Fe variant (vIgG2Fc). A method is also disclosed to make such fusion proteins at good expression levels. These recombinant hFSH-Fc fusion proteins of the present disclosure exhibit sufficient biological activities and prolonged plasma half-lives, leading to improved pharmacokinetics and pharmacodynamics. Thus, a lower dosage may be used and/or better or different therapeutic efficacies with less side effects may be achieved. A method for the application of the recombinant hFSH-Fc fusion proteins in the treatment and/or prevention of human infertility is also disclosed. | 2017-06-22 |
20170174737 | CHROMATOGRAPHY PROCESS FOR PURIFICATION OF INSULIN AND INSULIN ANALOGS - A process is described for purifying insulin and insulin analogs that comprises use of two or more orthogonal chromatographic purification steps in tandem following enzymatic digestion of the propeptide-insulin precursor to remove specific product impurities, improve process consistency, and increase process redundancy in the purification of the insulin or insulin analog, e.g., insulin lispro. | 2017-06-22 |
20170174738 | ALPHA- AND GAMMA-MSH ANALOGUES - The present invention provides peptide analogues of α-MSH and γ-MSH, comprising the amino acid sequence of human α-MSH or γ-MSH, or variants thereof, and having a branched amino acid probe in the N-terminal part of the peptide. | 2017-06-22 |
20170174739 | Protein-Based Molecular Temperature Switch - A region of the TRPM8 protein that functions as a temperature switch (FIG. | 2017-06-22 |
20170174740 | KV2.1 CHANNEL-DERIVED PEPTIDES AND METHODS OF USE - Peptides capable of interfering with the Kv2.1-mediated apoptotic K | 2017-06-22 |
20170174741 | COMBINATORIAL GAMMA 9 DELTA 2 T CELL RECEPTOR CHAIN EXCHANGE - The current invention provides methods to identify γ9δ2T-cell receptors (γ9δ2TCR) that mediate anti-tumour responses. Surprisingly, it was now found that the CDR3 regions of the γ9-T-cell receptor chain and the δ2-T-Cell receptor chain MICR chain) are of importance. Based on these findings, combinatorial-γδTCR-chain-exchange (CTE) is proposed as an efficient method for identifying γ9δ2TCRs that mediate anti-tumour responses. Using the method of the invention, specific sequences of the respective γ9TCR and δ2TCR chains were identified that mediate anti-tumour responses. Hence, the invention further provides for specific γ9δ2TCRs, or fragments thereof, that may be used e.g. in diagnostics or treatment of cancer. The invention further provides for nucleic acid sequences, genetic constructs and retroviral vectors that can be used to express the γ9δ2TCRs according to the invention. | 2017-06-22 |
20170174742 | TMIGD2 AND ITS DERIVATIVES AS BLOCKERS OR BINDERS OF CANCER-EXPRESSED HHLA2 FOR IMMUNOTHERAPIES - Provided are methods of treating an HHLA2-bearing tumor in a subject with a fusion protein comprising an IgV-like domain of a TMIGD2 sufficient to treat the HHLA2-bearing tumor. A fusion protein comprising an IgV-like domain of a TMIGD2 and related compositions and encoding nucleic acids are also provided. | 2017-06-22 |
20170174743 | POLYPEPTIDES, CELLS, AND METHODS INVOLVING ENGINEERED CD16 - This disclosure describes, generally, a modified form of CD 16, genetically-modified cells that express the modified CD 16, and methods that involve the genetically-modified cells. The modified form of CD 16 can exhibit increased anti-tumor and/or anti- viral activity due, at least in part, to reduced susceptibility to ADAM17-mediated shedding upon NK cell stimulation. | 2017-06-22 |
20170174744 | NEW METHOD FOR TREATING MELANOMA - The present invention relates to a TNFα blocking agent for use in the treatment and prevention of melanoma in a subject in whom melanoma cells express MHCI and in whom stroma cells exhibit TNF expression. | 2017-06-22 |
20170174745 | MULTIVALENT HETEROMULTIMER SCAFFOLD DESIGN AND CONSTRUCTS - Provided herein are multifunctional heteromer proteins. In specific embodiments is a heteromultimer that comprises: at least two monomeric proteins, wherein each monomeric protein comprises at least one cargo polypeptide, attached to a transporter polypeptide, such that said monomeric proteins associate to form the heteromultimer. These therapeutically novel molecules comprise monomers that function as scaffolds for the conjugation or fusion of therapeutic molecular entities resulting in the creation of bispecific or multivalent molecular species. | 2017-06-22 |
20170174746 | Recombinant Bacterium and Uses Thereof - The present invention relates to a recombinant bacterium expressing an antigen that is translocated to the cytosol of a host organism, and uses thereof. To this end, the present invention provides a recombinant bacterium comprising a nucleic acid encoding an antigen that is translocated to the cytosol of a host cell utilizing Type Ill secretion system. The recombinant bacterium is generally chosen from intracellular pathogens that reside in the phagosome and fail to induce rapid T cell activation. The translocated antigen may be a viral antigen, a bacterial antigen, or a tumour antigen. Methods of imparting immunity using the recombinant bacterium are also provided. | 2017-06-22 |
20170174747 | Methods and Apparatus for Creating Particle Derivatives of HDL with Reduced Lipid Content - The present invention is directed to systems, apparatus and methods for creating derivatives of at least one form of HDL without substantially affecting LDL. These derivatives of HDL are particles with reduced lipid content, particularly reduced cholesterol content. These particles have the capacity to bind cholesterol and are administered to a patient to enhance cellular cholesterol efflux and reduce cholesterol levels in cells, tissues, organs, and blood vessels. The present method is useful for treating atherogenic vascular disease and may be combined with other therapies such as statins, inhibitors of cholesterol absorption, niacin, anti-inflammatories, exercise and dietary restriction. | 2017-06-22 |
20170174748 | SERUM ALBUMIN-BINDING FIBRONECTIN TYPE III DOMAINS - The present invention relates to polypeptides which include tenth fibronectin type III domains ( | 2017-06-22 |
20170174749 | MIMETIC PEPTIDES DERIVED FROM COLLAGEN TYPE IV AND THEIR USE FOR TREATING ANGIOGENESIS- AND LYMPHANGIOGENESIS- DEPENDENT DISEASES - Mimetic peptides having anti-angiogenic and anti-tumorigenic properties and methods of their use for treating cancer, ocular diseases, such as age-related macular degeneration, and other-angiogenesis-dependent diseases are disclosed. More particularly, active non-cysteine analogs (mimetics), which exhibit anti-angiogenic activity in endothelial cell proliferation, migration, adhesion, and tube formation assays, anti-migratory activity in human breast cancer cells in vitro, anti-angiogenic and anti-tumorigenic activity in vivo in breast cancer xenograft models, and age-related macular degeneration models are disclosed. The presently disclosed mimetic peptides also exhibit anti-lymphangiogenic and directly anti-tumorigenic properties. | 2017-06-22 |
20170174750 | Peptide Inhibitors of BCR-ABL Oligomerization - In one aspect, the invention relates to peptides comprising the Bcr-Abl coiled-coil oligomerization domain and an alpha helix stabilizing moiety, mutant forms thereof, truncated forms thereof, derivatives thereof, and related peptides, which are useful as inhibitors of the Bcr-Abl chimeric protein; pharmaceutical compositions comprising the compounds; and methods of treating hyperproliferative disorders associated with Bcr-Abl using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2017-06-22 |
20170174751 | IMMUNOGENETIC RESTRICTION ON ELICITATION OF ANTIBODIES - The present invention provides structural determinants important for binding to the stem domain of the HA protein of influenza virus, and methods of use thereof for production of high affinity neutralizing influenza virus antibodies based upon these determinants. The present invention further provides tools for determining the efficacy of an influenza virus vaccine. The present invention further provides a molecular signature useful for determining the efficacy of an influenza virus vaccine in a subject, or for predicting prior immunologic exposure or antigen responsiveness to vaccine or influenza virus infection. | 2017-06-22 |
20170174752 | ANTIBODIES DIRECTED TO RICIN TOXIN - The invention provides a pharmaceutical composition comprising as an active ingredient a combination of three isolated monoclonal antibodies or any antigen-binding fragment thereof which bind ricin toxin and neutralize its toxic effects, and a pharmaceutically acceptable carrier, excipient or diluent. The invention also provides a method of prophylaxis, treatment or amelioration of ricin toxin poisoning including administering to a subject in need thereof a therapeutically effective amount of the pharmaceutical composition. | 2017-06-22 |
20170174753 | METHOD FOR TREATING BREAST CANCER - Breast cancer cells lacking ER protein expression, PgR protein expression and/or showing absence of HER2 protein over-expression (i.e., triple-negative breast cancer cells, basal-like) can be efficiently targeted with an anti-KAAG1 antibody and killed upon delivery of a therapeutic moiety. Antibodies and antigen binding fragments that specifically binds to KAAG1 may thus be used for the, detection and therapeutic treatment of breast cancer cells that are negative for at least one of these markers. The use of antibody conjugates in the treatment of triple-negative breast cancer and/or basal-like breast cancer is disclosed herein. | 2017-06-22 |
20170174754 | ANTI-CGRP COMPOSITIONS AND USE THEREOF - The present invention is directed to antibodies and fragments thereof having binding specificity for CGRP. Another embodiment of this invention relates to the antibodies described herein, and binding fragments thereof, comprising the sequences of the V | 2017-06-22 |