12th week of 2016 patent applcation highlights part 22 |
Patent application number | Title | Published |
20160083360 | PROCESS FOR THE EPOXIDATION OF OLEFINS - The subject invention is related to a process for the epoxidation of olefin with peroxide, comprising reacting peroxide with olefin in the presence a solvent, wherein the solvent has Hansen Solubility Parameters (HSPs) of δ | 2016-03-24 |
20160083361 | INHIBITORS OF THE IRE-1/XBP-1 PATHWAY AND METHODS OF USING THEREOF - Disclosed are XBP-1/IRE-1 inhibitors having formula disclosed herein. Methods of making and using these inhibitors for the treatment of cancer, in particular B cell cancers, are also disclosed. Also disclosed is a genetic XBP-1-knockout cancer mouse model. In still further aspects, the disclosed subject matter relates to methods for treating oncological and inflammatory disorders in a patient. For example, disclosed herein are methods whereby an effective amount of a compound or composition disclosed herein is administered to a patient having an oncological disorder, for example B-cell chronic lymphocytic leukemia (CLL), and who is in need of treatment thereof. XBP-1 deficiency causes leukemic cells to acquire phenotypes that are disadvantageous for their survival, such as compromised BCR signaling capability and increased surface expression of S1 P1. | 2016-03-24 |
20160083362 | TRICYCLIC SULPHONAMIDE COMPOUNDS AND METHODS OF MAKING AND USING SAME - The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2. | 2016-03-24 |
20160083363 | Substituted Indoles as Selective Protease Activated Receptor 4 (PAR-4) Antagonists - Embodiments of the invention include substituted indole compounds and compositions thereof to inhibit protease activated receptor-4. Also described are methods of preparation of compositions and methods for treating diseases related to thrombotic disorders by administration of the composition. | 2016-03-24 |
20160083364 | Phenanthridine Derivatives, Preparation Methods and Uses Thereof - The present invention relates to the pharmaceutical field, in particular to a phenanthridine derivative as shown in general formula (1) | 2016-03-24 |
20160083365 | QUINOLINONE PYRIMIDINES COMPOSITIONS 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: | 2016-03-24 |
20160083366 | 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: | 2016-03-24 |
20160083367 | PYRIDINYL 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: | 2016-03-24 |
20160083368 | THERAPEUTIC COMPOUNDS - Compounds of formula I: | 2016-03-24 |
20160083369 | HETEROCYCLIC COMPOUNDS AND USE THEREOF - Heterocyclic compounds of Formula (I) shown herein. Also disclosed are pharmaceutical compositions containing the heterocyclic compounds and methods of using the heterocyclic compounds to mobilize hematopoietic stem cells and endothelial progenitor cells into the peripheral circulation. Further provided are methods for treating tissue injury, cancer, inflammatory disease, and autoimmune disease with the heterocyclic compounds. | 2016-03-24 |
20160083370 | SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF - Provided herein are novel heteroaryl compounds, pharmaceutically acceptable salts and pharmaceutical formulations thereof for selectively inhibiting serotonin reuptake and/or acting as 5-HT | 2016-03-24 |
20160083371 | 1-ARYL-1-HYDROXY-2,3-DIAMINO-PROPYL AMINES, 1-HETEROARYL-1-HYDROXY-2,3-DIAMINO-PROPYL AMINES AND RELATED COMPOUNDS HAVING ANALGESIC AND/OR IMMUNO STIMULANT ACTIVITY - Compounds of the formula | 2016-03-24 |
20160083372 | NEPRILYSIN INHIBITORS - In one aspect, the invention relates to compounds having the formula: | 2016-03-24 |
20160083373 | METHOD FOR PREPARING AFATINIB AND INTERMEDIATE THEREOF - Revealed in the present invention is a method for preparing Afatinib (I): using 2-nitrile-4-[4-(N,N-dimethylamino)-I-oxo-2-buten-I-yl]amino-5-[(S)-(tetrahydrofuran-3-yl)oxy]aniline (II) and 4-fluoro-3-chloroaniline (III) as starting materials, and respectively performing a condensation and cyclization reaction with N,N-dimethylformamide dimethyl acetal (IV) to prepare Afatinib (I), wherein the method significantly reduces the manufacturing steps of Afatinib and greatly lower the costs. In addition, also provided in the present invention is a method for preparing an intermediate of Afatinib, wherein the method has a stable process, uses readily available starting materials, has a low cost, and all the reactions are classic reactions, suitable for meeting amplification requirements in the industry. | 2016-03-24 |
20160083374 | AMORPHOUS FORM OF CANAGLIFLOZIN AND PROCESS FOR PREPARING THEREOF - The present invention provides invention relates to stable amorphous form of Canagliflozin. The invention also provides the processes for the preparation of an amorphous form of Canagliflozin; and pharmaceutical compositions comprising therapeutically effective amount of an amorphous form of Canagliflozin, use of said composition for treatment of diabetes, obesity and diabetic complications, especially in type-2 diabetes. | 2016-03-24 |
20160083375 | THIAZOLYL- OR THIADIAZOLYL-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS KINASE INHIBITORS - Compounds having the following formula: | 2016-03-24 |
20160083376 | CERTAIN PROTEIN KINASE INHIBITORS - Disclosed herein are protein kinase inhibitors, more particularly pyridazine derivatives and pharmaceutical compositions thereof, and method of use thereof. | 2016-03-24 |
20160083377 | BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY - The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R | 2016-03-24 |
20160083378 | NOVEL PROCESSES FOR THE MANUFACTURE OF PROPANE-1-SULFONIC ACID (3-[5-(4-CHLORO-PHENYL)-1H-PYRROLO[2,3-b]PYRIDINE-3-CARBONYL]-2,4-DIFLUOR- O-PHENYL)-AMIDE - According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 | 2016-03-24 |
20160083379 | HISTONE DEMETHYLASE INHIBITORS - The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of 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. | 2016-03-24 |
20160083380 | OXIMINO DERIVATIVES FOR THE TREATMENT OF DYSLIPIDEMIA - Compounds of the general formula (I), including their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds and the intermediates involved in their preparation. | 2016-03-24 |
20160083381 | POLYMORPH FORMS - The present invention relates to novel crystal forms of 2-amino-N-[2-(3a-(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl)-1-(R)-benzyloxymethyl-2-oxo-ethyl]-isobutyramide L-tartrate. More particularly, the invention relates to polymorph forms, and to processes for the preparation of compositions containing and to uses of such polymorph forms. | 2016-03-24 |
20160083382 | COMPOUNDS FOR INHIBITING DRUG-RESISTANT STRAINS OF HIV-1 INTEGRASE - A method of inhibiting drug-resistant HIV-1 integrase in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof, having a structure of: | 2016-03-24 |
20160083383 | Novel 6-fused heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis B virus infection - The invention provides novel compounds having the general formula: | 2016-03-24 |
20160083384 | SALTS AND CRYSTALLINE FORMS OF AN APOPTOSIS-INDUCING AGENT - Salts and crystalline forms of 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}-sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer. | 2016-03-24 |
20160083385 | PYRAZINOISOQUINOLINE COMPOUNDS - This invention in one embodiment is directed to a compound of Formula Ia; | 2016-03-24 |
20160083386 | SUBSTITUTED BRIDGED UREA ANALOGS AS SIRTUIN MODULATORS - Provided herein are novel substituted bridged urea and related analogs and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 2016-03-24 |
20160083387 | SHIP1 MODULATORS AND METHODS RELATED THERETO - Compounds of formula (I): where R | 2016-03-24 |
20160083388 | NOVEL MODULATORS OF NRF2 AND USES THEREOF - There is provided modulators of Nrf2 protein which comprises a compound which binds at least one of the BTB domain, IVR domain and Kelch domain of Keap1 protein, activating or inhibiting Nrf2. There is also provided pharmaceutical compositions containing the modulators, as well as uses and method of use of the modulators for the treatment of conditions. | 2016-03-24 |
20160083389 | PROCESS OF PREPARING ALCAFTADINE - The present invention relates to an improved process of preparing substantially pure alcaftadine comprising reacting substantially pure compound of structural formula VIII with more than 20 moles of oxidizing reagent in an organic solvent to obtain alcaftadine: | 2016-03-24 |
20160083390 | ORGANIC COMPOUNDS - Optionally substituted 3-(thio, sulfinyl or sulfonyl)-7,8-dihydro-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one or a substituted 3-(thio, sulfinyl or sulfonyl)-7,8,9-trihydro-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them. | 2016-03-24 |
20160083391 | TRICYCLIC PIPERAZINE DERIVATIVE - Disclosed are compounds useful as inhibitors of Phosphodiesterase 1 (PDE1), compositions thereof, and methods of using the same. | 2016-03-24 |
20160083392 | Fused heterocyclic compounds as protein kinase inhibitors - The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby. | 2016-03-24 |
20160083393 | COMPOUNDS FOR TREATMENT OF PAIN - The aspects of the disclosed embodiments are directed to novel compounds, specifically, quaternary ammonium derivatives of tertiary amine containing opioid drug compounds such as hydrocodone, hydromorphone and oxycodone, formulations containing said. compounds or pharmaceutically acceptable salts thereof, which are capable of providing controlled release of the opioid drug upon administration to a patient in order to treat pain. | 2016-03-24 |
20160083394 | ANTIVIRAL COMPOUNDS - The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds. | 2016-03-24 |
20160083395 | ANTIVIRAL COMPOUNDS - The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds. | 2016-03-24 |
20160083396 | SYNTHESIS OF ISOHEXIDE DICARBAMATES AND DERIVATIVES THEREOF - Isohexide dicarbamates and a method of preparing the same are described. The method involves reacting a mixture of an isohexide and a cynate salt in a non-aqueous solvent, with a miscible acid having a pKa of about 3.7 or less. The isohexide dicarbamates can serve as precursor materials from which various derivative compounds can be synthesized. | 2016-03-24 |
20160083397 | PARTHENOLIDE DERIVATIVES AND THEIR MODULATION OF PROCESSES CONTROLLED BY REGULATED TRANSLATION - The present invention provides parthenolide derivatives. In particular, the present invention provides parthenolide derivatives that modulate processes controlled by regulated mRNA translation and have anticancer activity. | 2016-03-24 |
20160083398 | DIARYLETHENE COMPOUNDS AND USES THEREOF - A compound according to Formula IA and IB, reversibly convertible under photochromic and electrochromic conditions between a ring-open isomer A and a ring-closed isomer B is provided. For substitutent groups, Z is N, O or S; each R | 2016-03-24 |
20160083399 | MULTICYCLIC COMPOUNDS AND METHODS OF USE THEREOF - Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia. | 2016-03-24 |
20160083400 | TRICYCLIC GUANIDINE DERIVATIVE - Disclosed are compounds useful as inhibitors of Phosphodiesterase 1 (PDE1), compositions thereof, and methods of using the same. | 2016-03-24 |
20160083401 | ARYLQUINAZOLINES - The invention relates to novel compounds of the formula (I) which can be used for the inhibition of serine-threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. | 2016-03-24 |
20160083402 | ORGANOBORON COMPOUNDS AND METHODS OF MAKING ORGANOBORON COMPOUNDS - Embodiments of the present disclosure provide for methods of making an organoboron compound, organoboron compounds, and the like. | 2016-03-24 |
20160083403 | Boron-Containing Diacylhydrazine Compounds - The present disclosure provides boron-containing diacylhydrazines having Formula I: | 2016-03-24 |
20160083404 | Heterocyclic Compound, Light-Emitting Element, Light-Emitting Device, Electronic Device, and Lighting Device - Provided are a heterocyclic compound which emits blue light and is represented by General Formula (G | 2016-03-24 |
20160083405 | TANTALUM- OR VANADIUM-CONTAINING FILM FORMING COMPOSITIONS AND VAPOR DEPOSITION OF TANTALUM- OR VANADIUM-CONTAINING FILMS - Tantalum- or Vanadium-containing film forming compositions are disclosed as well as methods of synthesizing the same and methods of forming Tantalum- or Vanadium-containing films on one or more substrates via vapor deposition processes using the disclosed Tantalum- or Vanadium-containing film forming compositions. The disclosed Tantalum- or Vanadium-containing film forming compositions comprising a precursor having the formula M(R | 2016-03-24 |
20160083406 | EXTRACTION SOLVENT CONTROL FOR REDUCING STABLE EMULSIONS - Disclosed herein are methods for recovering diphosphonite-containing compounds from mixtures comprising organic mononitriles and organic dinitriles, using liquid-liquid extraction. Also disclosed are treatments to enhance extractability of the diphosphonite-containing compounds. | 2016-03-24 |
20160083407 | NUCLEOTIDE ANALOGS - Disclosed herein, inter alia, are acyclic nucleotide analogs and methods of using an acyclic nucleotide analog for treating and/or ameliorating a papillomavirus infection. | 2016-03-24 |
20160083408 | ARSENIC COMPLEXES FOR POTENTIAL DIAGNOSTIC APPLICATIONS - The present invention provides radioactive arsenic complexes useful in diagnostic and therapeutic applications and methods for forming those arsenic complexes. | 2016-03-24 |
20160083409 | METHOD FOR THE PREPARATION OF alpha-SUBSTITUTED ACRYL ALDEHYDES - The invention discloses simple and rapid method for the preparation of α-substituted acryl aldehydes. More particularly, the invention discloses a method for the preparation of α-substituted acryl aldehydes via a gold-catalysed [1,3] rearrangement of the allenyl ethers with a record turnover frequency of 4600 h | 2016-03-24 |
20160083410 | METAL OXALATE HYDRATE BODY HAVING A CERTAIN SHAPE, PREPARATION METHOD THEREOF, AND METAL OXIDE/CARBON COMPOSITE BODY PREPARED FROM THE SAME - The present invention relates to a metal oxalate hydrate body having a certain shape, a preparation method thereof, and a metal oxide/carbon composite body prepared by using the metal oxalate hydrate body. In the present invention, the metal oxalate body, whose shape is diversely controlled, and the metal oxide/carbon composite body therefrom are provided. | 2016-03-24 |
20160083411 | ANTIDIABETIC ENOLIC GLUCOSIDE OF PHENYLPYRUVIC ACID - There is provided an antidiabetic enolic glucoside of phenylpyruvic acid and derivatives thereof for use as medicaments, especially normoglycemic agents, i.e. for lowering blood glucose levels to normal levels in mammals that are obese, pre-diabetic or have diabetes, obesity and/or syndrome X. Hence the compounds of the present invention help to manage blood sugar levels, i.e. helping the body by balancing the blood sugar levels; helping to keep balanced blood glucose levels, particularly in humans with diabetes; aiding by enhancing the glucose uptake by the cells and by reducing sugar levels, thus improving or restoring the glucose tolerance; optimizing the glycemic response; normalizing the glucose tolerance. | 2016-03-24 |
20160083412 | KETOLIDE COMPOUNDS - The invention relates to ketolide compounds of Formula (1) and their pharmaceutically acceptable salts, solvates, hydrates, polymorphs and stereoisomers having antimicrobial activity. The invention also provides pharmaceutical compositions containing the compounds of invention and methods of treating or preventing microbial infections with the compounds of invention, wherein, T is —C*H(R | 2016-03-24 |
20160083413 | 2'-CHLORO NUCLEOSIDE ANALOGS FOR HCV INFECTION - Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2′-chloro nucleosides according to Formula 2001: | 2016-03-24 |
20160083414 | PHOSPHORAMIDITE BUILDING BLOCKS FOR SUGAR-CONJUGATED OLIGONUCLEOTIDES - Novel nucleoside phosphoramidite building blocks for preparation of synthetic oligonucleotides containing at least one phosphotriester linkage conjugated to a monosaccharide and synthetic processes for making the same are disclosed. Furthermore, oligomeric compounds are prepared using said building blocks, preferably followed by removal of protecting groups to provide monosaccharide-conjugated oligonucleotides. | 2016-03-24 |
20160083415 | Crystalline Anhydrate Forms Of A Pharmaceutical - The invention provides and describes solid state 17α-ethynyl-androst-5-ene-3β,7β,17β-triol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-androst-5-ene-3β,7β,17β-triol include Form I anhydrate and Form IV and Form V solvates. The invention further relates to solid and suspension formulations containing 17α-ethynyl-androst-5-ene-3β,7β,17β-triol in a described solid state form and use of the formulations to treat hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, and autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-androst-5-ene-3β,7β,17β-triol and uses of such formulations in treating the described conditions. | 2016-03-24 |
20160083416 | PROCESS FOR PRODUCING A SOLID FORM OF ABIRATERONE ACETATE - The present invention relates to a process for the preparation of 17-substituted steroids and, more particularly, to an improved method of preparing micro size abiraterone or derivatives thereof in high yield and purity by means of a spherical agglomeration process. | 2016-03-24 |
20160083417 | 19-NOR C3, 3-DISUBSTITUTED C21-C-BOUND HETEROARYL STEROIDS AND METHODS OF USE THEREOF - Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein, | 2016-03-24 |
20160083418 | 19-NOR NEUROACTIVE STEROIDS AND METHODS OF USE THEREOF - Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, and status epilepticus. | 2016-03-24 |
20160083419 | METHOD FOR PURIFYING ANTIBODY PROTEIN - A method for purifying a biologically active substance from a solution mixture containing impurities and the biologically active substance, in which an ion exchange chromatography carrier comprising a matrix and a copolymer containing at least N-isopropylacrylamide as a monomer unit and immobilized to a surface of the matrix is used, and the solution mixture is allowed to flow through a container storing the carrier at a uniform temperature, thereby recovering the biologically active substance. | 2016-03-24 |
20160083420 | DERIVATIVES OF DOLASTATIN 10 AND AURISTATINS - The present invention concerns a compound of following formula (I) where: —R | 2016-03-24 |
20160083421 | COMPUNDS FOR ENZYME INHIBITION - Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles. | 2016-03-24 |
20160083422 | INDOLINE 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. | 2016-03-24 |
20160083423 | NEW COMPOUNDS HAVING TRIPLE ACTIVITIES OF THROMBOLYSIS, ANTITHROMBOTIC AND RADICAL SCAVENGING, AND SYNTHESIS, NANO-STRUCTURE AND USE THEREOF - The present invention relates to a compound simultaneously having triple activities of thrombolysis, antithrombosis and free radical scavenging, as well as the preparation method, composition, and applications thereof. The compound is represented by the formula I shown below: | 2016-03-24 |
20160083424 | COMPOSITIONS AND METHODS FOR TARGETING ANTIGEN-PRESENTING CELLS - The present invention relates to compositions and method for targeting antigen presenting cells. In particular, the present invention relates to targeting peptides and methods of using the peptides to target molecules of interest to dendritic cells. | 2016-03-24 |
20160083425 | Proprotein Convertase Subtilisin Kexin Type 9 (PCSK9) Allosteric Binding Ligands To Modulate Serum Low Density Lipoprotein (LDL) Levels - This invention is related to the field of hypercholesterolemia. In particular, the invention provides compositions and methods to modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9 using synthetic ligands and/or synthetic ligand derivative sequences of 3-8 amino acids ranging between 350-2,000 Da. Altering the conformation of PCSK9 affects the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for ligands which can raise LDL levels. | 2016-03-24 |
20160083426 | NON-BENZENOID AROMATIC SYSTEMS FOR IMAGING, MONITORING AND THERAPY - This invention is directed to non-benzenoid aromatic compounds. Other aspects include methods of using non-benzenoid aromatic compounds for imaging and phototherapeutic uses thereof. Non-benzenoid compounds provided herein generally have one or more substituent groups which allow tailoring of the spectral properties or provide photoreactivity or targeting ability. | 2016-03-24 |
20160083427 | CYCLIC CATIONIC PEPTIDES WITH ANTIBMICROBIAL ACTIVITY - A series of cationic cyclic peptides, useful for the treatment of infectious diseases in both human and veterinary clinical/surgical environment are described herein. The peptides of the invention have a length of 15 to 21 amino acids, and show a sequence A-B-C-D-C′-B′-A′, wherein units A and A′ correspond to —NH | 2016-03-24 |
20160083428 | INHIBITORS OF THE Eph-A RECEPTOR AND USES THEREOF - Eph A receptor inhibitor peptides, and particularly Eph A4 receptor inhibitor peptides, are provided. The peptides comprise a sequence derived from the G-H loop of ephrin A4. Further, pharmaceutical compositions comprising said peptides and use thereof in treating, ameliorating or preventing diseases associated with memory formation are provided. | 2016-03-24 |
20160083429 | COMPOSITIONS AND METHODS FOR ENDOTOXIN NEUTRALIZATION - Peptide therapeutic agents are provided that bind to lipid A and neutralize the injurious effects of endotoxin. | 2016-03-24 |
20160083430 | PEPTIDE AND PEPTIDOMIMETIC INHIBITORS - The present invention provides inhibitors and/or antagonists of plasma kallikrein. Also provided are methods of utilizing the inhibitors as therapeutics. | 2016-03-24 |
20160083431 | LYOPHILISATE CONTAINING A CYCLIC PEPTIDE OF FORMULA X1-GQRETPEGAEAKPWY-X2 - Cyclic peptide of formula | 2016-03-24 |
20160083432 | CRYSTALLINE FORM OF CYCLOSPORIN A, METHODS OF PREPARATION, AND METHODS FOR USE THEREOF - The present invention relates generally to crystalline forms of cyclosporin A and particularly to a newly identified form of cyclosporin A. The invention further relates to methods for its preparation and to methods for treating certain ocular disorders. | 2016-03-24 |
20160083433 | TEMPLATE-DIRECTED GAMMAPNA SYNTHESIS PROCESS AND GAMMAPNA TARGETING COMPOUNDS - Described herein are recognition modules that bind specifically to a template nucleic acid and which ligate together in a reducing environment to produce a gamma peptide nucleic acid (γPNA) oligomer. Also provided are methods of synthesizing a γPNA oligomer on a template using the recognition modules. | 2016-03-24 |
20160083434 | DIVALENT NUCLEOBASE COMPOUNDS AND USES THEREFOR - Described herein are novel divalent nucleobases that each bind two nucleic acid strands, matched or mismatched when incorporated into a nucleic acid or nucleic acid analog backbone (a genetic recognition reagent, or genetic recognition reagent). In one embodiment, the genetic recognition reagent is a peptide nucleic acid (PNA) or gamma PNA (?PNA) oligomer. Uses of the divalent nucleobases and monomers and genetic recognition reagents containing the divalent nucleobases also are provided. | 2016-03-24 |
20160083435 | VACCINES AND METHODS TO TREAT LYME DISEASE IN DOGS - The instant invention provides an immunogenic composition comprising an antigenic fragment of OspA protein of | 2016-03-24 |
20160083436 | Non-Natural Consensus Albumin Binding Domains - Non-natural albumin binding domains, polynucleotides encoding thereof and methods of making and using these domains and polynucleotides are useful in controlling the half-life of therapeutic molecules for patients. | 2016-03-24 |
20160083437 | COMPOSITION COMPRISING RECOMBINANT FUSION PROTEIN OF PATHOGENIC ANTIGEN PROTEIN AND FLAGELLIN OF VIBRIO VULNIFICUS FOR PREVENTING, ALLEVIATING, OR TREATING AGING - The present invention relates to a composition for preventing, improving, or treating aging, wherein the composition comprises a recombinant protein of flagellin, which is the constituent of | 2016-03-24 |
20160083438 | Plasmodium falciparum antigens - The invention relates to antigens, associated with sterile immunity, and methods of their use, in an immunogenic formulation to confer an immune response against | 2016-03-24 |
20160083439 | NOVEL VACCINES AGAINST APICOMPLEXAN PATHOGENS - The technology provided herein generally relates to novel fusion proteins suitable as human and/or animal vaccines against parasites or pathogens of the phylum Apicomplexa. In particular, the present disclosure relates to novel fusion proteins as a basis for vaccines against | 2016-03-24 |
20160083440 | FOLLISTATIN IN TREATING DUCHENNE MUSCULAR DYSTROPHY - The present invention provides, among other things, methods and compositions for treating muscular dystrophy, in particular, Duchenne muscular dystrophy (DMD). In some embodiments, a method according to the present invention includes administering to an individual who is suffering from or susceptible to DMD an effective amount of a recombinant follistatin protein such that at least one symptom or feature of DMD is reduced in intensity, severity, or frequency, or has delayed onset. | 2016-03-24 |
20160083441 | Development of Protein-Based Biotherapeutics That Penetrate Cell-Membrane and Induce Anti-Cancer Effect - Cell-Permeable Trefoil Factor 1 (CP-TFF1) in Gastrointestinal Track (GIT) Cancer, Polynucleotides Encoding The Same, and Anti-Cancer Compositions Comprising The Same - The present study investigated the use of macromolecule intracellular transduction technology (MITT) to deliver biologically active TFF1 protein into gastric cancer cells both in vitro and in vivo. Proteins engineered to enter cancer cells are supposed to suppress cell proliferation and survival, consistent with its role as a tumor suppressor. The invention has developed new hydrophobic CPP-advanced MTDs (aMTDs) for high solubility/yield and cell-/tissue-permeability of the recombinant therapeutic fusion proteins. The TFF1 protein has been fused to aMTD165 and solubilization domains (SDs), and tested their therapeutic applicability as a gastric cancer-specific protein-based anti-cancer agent. Treatment with CP-TFF1 in gastric cancer cells reduced cancer cell viability (60%˜80% in 10 μM treatment), inhibited cell migration (approximately 50%). Furthermore, CP-TFF1 significantly inhibited the tumor growth during the treatment and the effect persisted for at least 3 weeks after the treatment was terminated (90% inhibition at day 42) in a xenografts model which were subcutaneously implanted with tumor block of gastric cancer cells (MKN45). In the present invention, CP-TFF1 recombinant protein showed the potential of novel protein therapies against gastric cancer. | 2016-03-24 |
20160083442 | INHIBITORS OF THE T CELL-SPECIFIC ALTERNATIVE P38 ACTIVATION PATHWAY AND METHODS OF USE - In T lymphocytes, p38 mitogen activated protein kinase (MAPK) can be activated through an alternative pathway that involves phosphorylation at tyrosine 323. Disclosed herein is the identification of a minimal region of the growth arrest and DNA damage-inducible alpha (Gadd45α) protein that is required for binding to and inhibition of tyrosine 323-phosphorylated p38 in T cells. The disclosed Gadd45α polypeptides inhibit proliferation of T cells in response to T cell receptor stimulation, inhibit differentiation of T cells into Th1 or Th17 cells, inhibit the production of proinflammatory cytokines, and reduce tumor formation and growth of inflammatory cancers, such as pancreatic cancer. | 2016-03-24 |
20160083443 | IMMUNOMODULATORY COMPOSITIONS AND METHODS FOR TREATING DISEASE WITH MODIFIED HOST DEFENSE PEPTIDES - Compositions and methods are provided for modulating an immune response in a vertebrate subject. Compositions and methods can comprise administering a modified host defense peptide to the vertebrate subject in an amount effective to activate the immune response in the vertebrate subject, wherein the modified host defense peptide is inverted in amino acid sequence from an amino terminus to a carboxy terminus or modified to one or more | 2016-03-24 |
20160083444 | Novel Feline Erythropoietin Receptor Agonists - The present specification discloses erythropoietin receptor agonists, compositions and medicaments comprising such erythropoietin receptor agonists, methods and uses for such erythropoietin receptor agonists and compositions and medicaments, and methods and uses for erythropoietin receptor agonists and compositions and medicaments for treating an anemia. | 2016-03-24 |
20160083445 | NOVEL POLYPEPTIDES - The present invention relates to an isolated polypeptide comprising (a) the amino acid sequence set forth in SEQ ID NO: 2; or (b) an amino acid sequence that is at least 95% identical to SEQ ID NO: 2, and to therapeutic treatments based thereon. | 2016-03-24 |
20160083446 | HIGHLY SOLUBLE LEPTINS - The disclosure provides chimeric polypeptides and nucleic acid molecules encoding chimeric polypeptides. Also provided are pharmaceutical compositions and methods of treatment for diseases and disorders including lipodystrophy, dyslipidemia, hyperlipidemia, overweight, obesity, hypothalamic amenorrhea, Alzheimer's disease, leptin deficiency, fatty liver disease or diabetes (including type I and type II). Additional diseases and disorders which can be treated by the compounds and methods described herein include nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD), metabolic syndrome X and Huntington's Disease. | 2016-03-24 |
20160083447 | DOUBLE-ACYLATED GLP-1 DERIVATIVES - The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 27 of GLP-1(7-37) (SEQ ID NO: 1); a second K residue at a position corresponding to position T of GLP-1(7-37), where T is an integer in the range of 7-37 except 18 and 27; and a maximum of ten amino acid changes as compared to GLP-1(7-37); wherein the first K residue is designated K | 2016-03-24 |
20160083448 | SITE 2 INSULIN ANALOGUES - An insulin analogue contains one or more modifications at a distinct protein surface comprising one or more of the residues at position B13, B17, A12, A13, and/or A17. Formulations of the above analogues at successive strengths U-100 to U-1000 in soluble solutions a at least pH value in the range 6.8-8.0 either in the presence of zinc ions at a molar ratio of 2.2-10 zinc ions per six insulin analogue monomers or in the presence of fewer than 1 zinc ions per six insulin analogue monomers. Use of the above formulation in an insulin pump functionally integrated with a continuous glucose monitor and computer-based control algorithm as a closed-loop system. A method of treating a patient with diabetes mellitus comprises administering a physiologically effective amount of the insulin analogue to a patient by means of intravenous, intraperitoneal, or subcutaneous injection. | 2016-03-24 |
20160083449 | T CELL IMMUNOTHERAPY SPECIFIC FOR WT-1 - The present disclosure provides high affinity and enhanced affinity T cell receptors specific for human Wilms tumor protein 1 (WT-1) epitopes for use in treating diseases or disorders, such as cancer cells that overexpress WT-1. | 2016-03-24 |
20160083450 | HUMAN PROTEIN SCAFFOLD WITH CONTROLLED SERUM PHARMACOKINETICS - This invention provides constructs comprising a protein scaffold, wherein the scaffold comprises Domain III, Domain IIIa, or Domain IIIb of human serum albumin or a polypeptide having substantial sequence identity to the Domain III, the Domain IIIa, or the Domain IIIb; and a targeting moiety in covalent linkage to the protein scaffold; and a therapeutic moiety and/or an imaging moiety in covalent linkage to the protein scaffold. The scaffold can be modified to tune the serum pharmacokinetics of the construct. In addition to methods of making the constructs, therapeutic, imaging and diagnostic uses of the constructs are also provided. | 2016-03-24 |
20160083451 | METHODS AND SYSTEMS FOR ZINC DELIVERY USING INTRINSIC FACTOR OR HAPTOCORRIN - Improved delivery of zinc using haptocorrin or intrinsic factor modified to include a zinc binding sequence that can outcompete dietary zinc inhibitors such as phytin. Known zinc binding sequences can be assayed to determine competitiveness with respect to phytin and, if successful, incorporated into the B | 2016-03-24 |
20160083452 | Isolation and Purification of Antibodies Using Protein A Affinity Chromatography - Disclosed herein are methods for the isolation and purification of antibodies wherein the use of an affinity chromatographic step results in an antibody composition sufficiently pure for pharmaceutical uses. The methods described herein comprise pH viral reduction/inactivation, ultrafiltration/diafiltration, affinity chromatography, preferably Protein A affinity, ion exchange chromatography, and hydrophobic chromatography. Further, the present invention is directed toward pharmaceutical compositions comprising one or more antibodies of the present invention. | 2016-03-24 |
20160083453 | SEPARATION OF RECOMBINANT POLYCLONAL ANTIBODY MULTIMERS WITH MINIMAL SEPARATION OF MONOMERS - The invention provides a method for removing multimers from a preparation of recombinant polyclonal antibodies (rpAbs) while maintaining the ratio of monomers within a narrow range. The invention provides a method of separating recombinant polyclonal antibody multimers with minimal separation of monomers comprising subjecting a mixture comprising a plurality of monoclonal antibodies to at least one separation process selected from the group consisting of multi-modal chromatography, apatite chromatography, and hydrophobic interaction chromatography thereby producing an antibody monomer preparation that is substantially free of multimers. | 2016-03-24 |
20160083454 | CONTINUOUS MULTISTEP PROCESS FOR PURIFYING ANTIBODIES - The invention provides a three-step chromatography process for small and large-scale purification of proteins, specifically monoclonal antibodies, using only four buffer solutions made from a mother solution. | 2016-03-24 |
20160083455 | ANTIVIRAL AGENT AGAINST ANIMAL VIRUSES - Disclosed herein is an antiviral agent against animal viruses. The antiviral agent contains a protein or a nucleic acid sequence encoding the protein, as an active ingredient, the protein having binding ability and degrading ability to foreign nucleic acid chains invaded in an animal cell and that has no cytotoxicity to the animal cell itself. Disclosed herein is further an antiviral animal cell containing the protein according to the present invention, or the nucleic acid sequence encoding the protein. The antiviral agent and antiviral animal cell exhibit advantageous effects in that they se | 2016-03-24 |
20160083456 | COMPOSITION AND METHODS BASED ON NEUTRALIZING ANTIBODIES DELIVERED INTRANASALLY FOR ENHANCED THERAPEUTIC EFFICACY - The present invention provides methods for treatment or prophylaxis of viruses, particularly influenza virus, by administration of agents, particularly neutralizing antibodies or active fragments thereof, directly to the respiratory tract, including by intranasal or inhalation administration. The invention provides compositions suitable for intranasal or inhalation treatment and administration. The invention includes methods for treatment or prophylaxis combining intranasal or inhalation administration with intraperitoneal or intravenous administration of antibodies. | 2016-03-24 |
20160083457 | METHODS AND COMPOSITIONS FOR THE TREATMENT AND/OR PROPHYLAXIS OF CLOSTRIDIUM DIFFICILE ASSOCIATED DISEASE - The present invention relates to methods and compositions for the treatment and/or prophylaxis of | 2016-03-24 |
20160083458 | ANTI-LIPOARABINOMANNAN ANTIBODY AND IMMUNOASSAY FOR ACID-FAST BACILLARY INFECTION USING THE ANTIBODY - The present invention provides a monoclonal antibody that specifically binds to acid-fast bacillary lipoarabinomannan, particularly tubercle bacillary lipoarabinomannan, the antibody being set forth below:
| 2016-03-24 |
20160083459 | Anti-Inflammatory Antibodies and Uses Therefor - The invention provides antibodies that inhibit activation of complement, which may be used to treat various inflammatory diseases or disorders. | 2016-03-24 |