Patents Issued in December 28, 2017
  • COMPOUNDS FOR AFFINITY CHROMATOGRAPHY AND FOR EXTENDING THE HALF-LIFE OF A THERAPEUTIC AGENT
    Publication number: 20170369448
    Abstract: Compounds useful for affinity chromatography as presented, more particularly for use in affinity chromatography to purify serum albumin, especially human serum albumin (HSA) and fusion proteins thereof. Methods for extending the half-life of therapeutic agents are also presented, particularly therapeutic peptide agents and small molecules, such as by conjugation of compounds described herein to the therapeutic peptide or small molecule, which, upon administration, binds to HSA, thereby providing a prolonged release of the therapeutic agent.
    Type: Application
    Filed: September 7, 2017
    Publication date: December 28, 2017
    Inventors: Peter KUMPALUME, Oliver SCHON, Christine Patricia DONAHUE, Ghotas EVINDAR, David I. ISRAEL, David PAOLELLA, Letian KUAI, Ninad V. PRABHU
  • KINASE INHIBITORS FOR THE TREATMENT OF DISEASE
    Publication number: 20170369449
    Abstract: The invention relates to compounds and their use in the treatment of disease. Novel irreversible inhibitors of wild-type and mutant forms of EGFR, FGFR, ALK, ROS, JAK, BTK, BLK, ITK, TEC, and/or TXK and their use for the treatment of cell proliferation disorders are described.
    Type: Application
    Filed: September 6, 2017
    Publication date: December 28, 2017
    Inventors: Nathanael GRAY, Hwan Geun CHOI, Li TAN
  • ANTIBACTERIAL COMPOUNDS HAVING BROAD SPECTRUM OF ACTIVITY
    Publication number: 20170369450
    Abstract: The present invention relates to novel antibacterial compounds, pharmaceutical compositions containing them and their use as antimicrobials.
    Type: Application
    Filed: December 14, 2015
    Publication date: December 28, 2017
    Applicant: AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.
    Inventors: Rosella OMBRATO, Barbara GAROFALO, Giorgina MANGANO, Alessandra CAPEZZONE DE JOANNON, Gaia CORSO, Claudia CAVARISCHIA, Guido FURLOTTI, Tommaso IACOANGELI
  • METHODS FOR PREPARING FUSED BICYCLIC 2, 4-DIAMINOPYRIMIDINE DERIVATIVES
    Publication number: 20170369451
    Abstract: The present disclosure is directed to improved methods useful for the preparation of, for example, 2-[[5-chloro-2-[[(6S)-6-[4-(2-hydroxyethyl)piperazin-1-yl]-1-methoxy-6,7,8,9-tetrahydro-5Hbenzo[7]annulen-2-yl]amino]pyrimidin-4-yl]amino]-N-methyl-benzamide (CEP-37440).
    Type: Application
    Filed: December 23, 2015
    Publication date: December 28, 2017
    Inventors: Shawn P. ALLWEIN, Roger P. BAKALE, Dale R. MOWREY, Daniel E. PETRILLO, Sander KLUWER
  • Catalysis of Diketopiperazine Synthesis
    Publication number: 20170369452
    Abstract: Provided is a method for the synthesis of N-protected bis-3,6-[4-aminobutyl]-2,5-diketopiperazine including the step of heating a solution of ?-amino protected lysine in the presence of a catalyst selected from the group consisting of sulfuric acid, phosphoric acid, and phosphorus pentoxide.
    Type: Application
    Filed: September 7, 2017
    Publication date: December 28, 2017
    Inventors: John J. Stevenson, Destardi Moye-Sherman
  • PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF
    Publication number: 20170369453
    Abstract: The present disclosure relates generally to derivatives of pyrrolobenzodiazepines and antibody-drug conjugates thereof and to methods of using these conjugates as therapeutics and/or diagnostics.
    Type: Application
    Filed: June 22, 2017
    Publication date: December 28, 2017
    Inventors: Joshua D. THOMAS, Mao YIN, Aleksandr V. YURKOVETSKIY, Patrick R. CONLON, Ahmed HILMY, Eugene W. KELLEHER, Timothy B. LOWINGER, Cheri A. STEVENSON, Shuyi TANG
  • 18F-LABELED TRIAZOLE CONTAINING PSMA INHIBITORS
    Publication number: 20170369454
    Abstract: The present technology is directed to compounds, intermediates thereof, compositions thereof, medicaments thereof, and methods related to the imaging of mammalian tissue overexpressing PSMA. The compounds are of Formula I or a pharmaceutically acceptable salt thereof, wherein one of R1, R2, and R3 is and of Formula IV or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 28, 2017
    Publication date: December 28, 2017
    Inventors: John W. Babich, James M. Kelly, Alejandro Amor-Coarasa, Shashikanth Ponnala
  • COMBINATION OF UV ABSORBER AND PIGMENT FOR PROTECTION OF SUBSTRATES FROM UV/VIS-RADIATION
    Publication number: 20170369455
    Abstract: A coating composition, which contains one or more compounds (A) according to formula (I) and a pigment (B) having a minimum integrated transmittance within the range of 380 to 600 nm, is provided: In formula (I), each R1, R2 and R3 is independently —OR4, R4 being independently hydrogen or a C1 to C24 hydrocarbyl group optionally containing heteroatoms, or C1 to C24 hydrocarbyl groups optionally containing heteroatoms; n is 2, 3, 4 or 5; o is 2, 3, 4 or 5; p is 2, 3, 4 or 5; with the proviso that at least one of R1 and at least one of R2 and at least one of R3 is —OR4. A coating is obtained by applying the coating composition to a substrate for protecting the substrate against UV/Vis-radiation or for stabilizing the substrate against the deleterious influence of UV/Vis-radiation.
    Type: Application
    Filed: December 18, 2015
    Publication date: December 28, 2017
    Applicant: BASF SE
    Inventors: Rolf ALLES, Katharina FRITZSCHE, Wolfgang PETER, Adalbert BRAIG
  • SYNTHESIS OF CYCLOPHANES FOR A SELF-ASSEMBLY REACTION
    Publication number: 20170369456
    Abstract: Disclosed herein is a novel method for preparing cyclophanes, comprising forming a disulfide cyclophane by contacting a linker moiety which includes two or more thiol groups, with a metal salt and an oxidant. The disulfide cyclophane is then desulfurized to form a thiacyclophane comprising thioether bridges. This thiacyclophane optionally may be further desulfurized to form an unsaturated hydrocarbon cyclophane, which can then be reduced to form a saturated hydrocarbon cyclophane. The various cyclophanes can be synthesized in a ring form, such as a dimer, trimer or tetramer etc., or they can be synthesized in a tetrahedral or larger structure. Also disclosed are novel cyclophanes formed by the disclosed method.
    Type: Application
    Filed: September 7, 2017
    Publication date: December 28, 2017
    Applicant: University of Oregon
    Inventors: Darren W. Johnson, Mary Collins
  • Antibacterial Compounds
    Publication number: 20170369457
    Abstract: The present invention relates to the following compounds for use in the treatment of a bacterial infection wherein the integers are as defined in the description. The invention also relates to compounds for use as medicaments, pharmaceutical compositions and some novel compounds.
    Type: Application
    Filed: September 8, 2017
    Publication date: December 28, 2017
    Inventors: Jérôme Émile Georges Guillemont, Magali Motte, Anil Koul, Nacer Lounis
  • METHOD FOR PREVENTION OF PREMATURE POLYMERIZATION
    Publication number: 20170369458
    Abstract: The present invention relates to a method for prevention of premature polymerization during the preparation, purification, transportation and storage of a polymerizable compound with at least one conjugated unsaturated group in the presence of an azine dye-based compound as inhibitor. Further the present invention relates to methods of preparing such inhibitors as well as to the inhibitors itself, as well as to methods of improving solubility and stability of dissolved inhibitors.
    Type: Application
    Filed: September 11, 2017
    Publication date: December 28, 2017
    Applicant: Nitto Europe N.V.
    Inventors: Greet BOSSAERT, Monica GOMES, Bart FORIER
  • THIADIAZOLYL - OXIMINOACETIC ACID DERIVATIVE COMPOUNDS
    Publication number: 20170369459
    Abstract: Thiadiazolyl-oximinoacetic acid derivatives have been synthesized, which are useful in the manufacture of cephalosporin antibiotic compounds. Compound (1) (TATD) is commercially available (CAS No. 76028-96-1). It has now been discovered that the thiadiazolyl-oximinoacetic acid derivative compound (1) (TATD) can be prepared from dimethyl malonate (SM 1, CAS No. 108-59-8) according to methods described herein. The methods provide products having desirable purity.
    Type: Application
    Filed: December 18, 2015
    Publication date: December 28, 2017
    Applicant: Merck Sharp & Dohme Corpl
    Inventors: Kristos Adrian Moshos, Valdas Jurkauskas
  • CARRIER TREATMENT TO IMPROVE CATALYTIC PERFORMANCE OF AN ETHYLENE OXIDE CATALYST
    Publication number: 20170369460
    Abstract: A method for lowering the sodium content of different carriers which may have different physical properties as well as varying degrees of sodium is provided. The method, which lowers the sodium content from the surface, subsurface as well as the binding layer of the carrier, includes contacting a carrier with water. A rinse solution is recovered from the contacting. The rinse solution includes leached sodium from the carrier. The sodium content in the rinse solution is then determined. The contacting, recovering and determining are repeated until a steady state in the sodium content is achieved.
    Type: Application
    Filed: September 11, 2017
    Publication date: December 28, 2017
    Applicant: Scientific Design Company, Inc.
    Inventors: Nabil Rizkalla, Andrzej Rokicki
  • PROFLAVOR DELIVERY POWDERS
    Publication number: 20170369461
    Abstract: Provided herein are formulations of plated powders of acetaldehyde precursors. Also provided herein are methods of making and using the powders.
    Type: Application
    Filed: December 21, 2015
    Publication date: December 28, 2017
    Applicant: Firmenich SA
    Inventors: Valery NORMAND, Rutger M.T. VAN SLEEUWEN
  • Modulation of Bacterial Quorum Sensing with Synthetic Ligands
    Publication number: 20170369462
    Abstract: The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.
    Type: Application
    Filed: September 12, 2017
    Publication date: December 28, 2017
    Inventors: Helen E. BLACKWELL, Grant D. GESKE, Jennifer C. CAMPBELL BUTLER
  • ESTERIFICATION OF 2,5-FURAN-DICARBOXYLIC ACID
    Publication number: 20170369463
    Abstract: A method of making a furan dicarboxylate by means of reacting 2,5-furan dicarboxylic acid (FDCA) with an alcohol or mixture of alcohols in a CO2-predominant atmosphere without the presence of any other acid catalyst is described. The reaction is conducted under conditions that correspond to either supercritical, critical or near-critical temperatures and pressures for the alcohol species and/or CO2 gas.
    Type: Application
    Filed: August 11, 2017
    Publication date: December 28, 2017
    Inventors: Kenneth Stensrud, Padmesh Venkitasubramanian
  • Process for Producing 4-Azidosulfonylphthalic Anhydride
    Publication number: 20170369464
    Abstract: The present disclosure provides a process for the production of 4-azidosulfonylphthalic anhydride. In an embodiment, a process is provided and includes chlorinating 4-sulfophthalic acid trisodium salt (1), under solvent reaction conditions, to form a dissolved 4-chlorosulfonylphthalic anhydride (2) and an insoluble sodium chloride. The process includes first removing the insoluble sodium chloride from the dissolved 4-chlorosulfonylphthalic anhydride to form an isolated 4-chlorosulfonylphthalic anhydride. The process includes reacting, under solvent reaction conditions, the isolated 4-chlorosulfonylphthalic anhydride with sodium azide to form a dissolved 4-azidosulfonylphthalic anhydride and an insoluble sodium chloride. The process includes second removing the insoluble sodium chloride from the dissolved 4-azidosulfonylphthalic anhydride to form an isolated 4-azidosulfonylphthalic anhydride.
    Type: Application
    Filed: December 28, 2015
    Publication date: December 28, 2017
    Inventors: Matthew J. Jansma, Michael F. Gullo, John W. Hull, Jr.
  • SOOTHING PRO-PHEROMONAL COMPOSITION FOR MAMMALS
    Publication number: 20170369465
    Abstract: The invention relates to a compound of general formula (I) (in configuration Z or E) and to pro-pheromonal compositions and formulations comprising said compound, in addition to the uses thereof for soothing purposes for non-human mammals such as sheep, pigs, sheep, cattle, felines, equines and canines.
    Type: Application
    Filed: December 24, 2015
    Publication date: December 28, 2017
    Applicant: Melchior Material And Life Science France
    Inventors: Olivier Guerret, Loic Guilonneau, Samuel Dufour
  • 3-[(BENZO[D][1,3]DIOXOLAN-4-YL)-OXY]-3-ARYLPROPYLAMINE TYPE COMPOUNDS AND APPLICATIONS THEREOF
    Publication number: 20170369466
    Abstract: The present invention relates to 3-[(benzo[d][1,3]dioxolan-4-yl)-oxy]-3-arylpropylamine compounds of formula I or pharmaceutically acceptable salts thereof and use thereof. The compound may be used to prepare an antidepressant agent.
    Type: Application
    Filed: December 24, 2015
    Publication date: December 28, 2017
    Inventors: Qiang Guo, Song Zhao, Zhiqiang Liu, Xiangqing Xu, Guisen Zhang
  • Process for the Preparation of N-Monosubstituted beta-Amino Alcohols
    Publication number: 20170369467
    Abstract: A process is disclosed for the preparation of a compound of formula and/or an addition salt of a proton acid, wherein R1 and R2 independently represent alkyl, cycloalkyl, aryl or aralkyl, each aryl or aralkyl being optionally further substituted with alkyl, alkoxy and/or halogen.
    Type: Application
    Filed: September 8, 2017
    Publication date: December 28, 2017
    Inventors: Dominique Michel, Rudolf Fuchs
  • ANTHROPOD REPELLENT CHEMICALS
    Publication number: 20170369468
    Abstract: Compositions and methods for repelling arthropods. The compositions include a carrier and an arthropod repelling compound, which can be a compound discovered by a novel and complex cheminformatic process to demonstrate repellency behavior across a broad spectrum of arthropods. The compound can be a thiane compound, a pyrrolidone compound, a cyclohexadiene compound, a cyclohexenone compound, a cyclohexene compound, a furanone compound, a pyran compound, a tetrahydropyran compound, a thiazolidine compound, a thiazoline compound, a dihydrothiophene compound, a dithiolane compound, a dithiane compound, an epoxide compound, an oxathiane compound, a cyclopentene compound, a cyclohexane compound, a quinoline compound, an oxazoline compound, a tetrahydropyridine compound, and an imidazolidinone compound, or a combination thereof.
    Type: Application
    Filed: September 1, 2017
    Publication date: December 28, 2017
    Applicant: The Regents of the University of California
    Inventors: Anandasankar Ray, Christine Krause Pham, Sean Michael Boyle
  • COMPOUNDS, COMPOSITIONS AND METHODS
    Publication number: 20170369469
    Abstract: The disclosed subject matter provides certain polymorphic forms of Compound (I) as well as pharmaceutical compositions comprising Compound (I) or such polymorphic forms, and methods of using or making such compounds and pharmaceutical compositions. It has now been discovered that Compound (I) can exist in multiple crystalline forms (polymorphs). One particular crystalline form, Form II, has been found to be more thermodynamically stable and, thus, likely more suitable for bulk preparation and handling than other polymorphic forms. Efficient and economic methods have been developed to prepare Compound (I) and Form II in high purity on a large scale. In animal studies, Form II has demonstrated safety and efficacy in treating depressive disorders and, when micronized, improved absorption compared to non-micronized Form II.
    Type: Application
    Filed: December 18, 2015
    Publication date: December 28, 2017
    Applicants: Cerecor, Inc., Merck Sharp & Dohme Corp.
    Inventors: Reza Mazhari, Djelila Mezaache, Blake M. Paterson, James Vornov, Rachel M. Garner, Todd Nelson
  • Cyclic Compounds and Uses Thereof
    Publication number: 20170369470
    Abstract: The invention generally relates to substituted benzothiophenyl, substituted benzothiazolyl, substituted indolyl and substituted benzoimidazolyl compounds and, more particularly, to a compound represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of a disease or disorder selected from cancer (e.g., lymphoma, such as mantle cell lymphoma), a neurodegenerative disease, inflammatory diseases or an autoimmune system disease (e.g., a T-Cell mediated autoimmune disesase).
    Type: Application
    Filed: December 16, 2015
    Publication date: December 28, 2017
    Inventors: Erkan Baloglu, William Senapedis, Sharon Shacham
  • 5-SUBSTITUTED QUINAZOLINONE DERIVATIVES AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME
    Publication number: 20170369471
    Abstract: Provided are 5-substituted quinazolinone compounds, for example, of formula (I), and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use for treating angiogenesis or cytokine related disorders, and pharmaceutical compositions of these compounds are disclosed.
    Type: Application
    Filed: July 7, 2017
    Publication date: December 28, 2017
    Inventors: George W. Muller, Hon-Wah Man
  • MAP KINASE MODULATORS AND USES THEREOF
    Publication number: 20170369472
    Abstract: The invention provides for novel MAP kinase inhibitors and compositions comprising the same. In some embodiments, the MAP kinase inhibitors are p38? MAP kinase inhibitors. The invention further provides for methods for treatment of diseases comprising administration of MAP kinase inhibitors or compositions comprising MAP kinase inhibitors. In some embodiments, the disease is Alzheimer's Disease, ALS, Huntington's Disease or Parkinson's Disease.
    Type: Application
    Filed: September 7, 2017
    Publication date: December 28, 2017
    Inventors: Ottavio ARANCIO, Daniel Martin WATTERSON, Jeffrey Claude PELLETIER, Saktimayee Mitra ROY
  • PYRROLIDINE DERIVATIVES AS ANGIOTENSIN II TYPE 2 ANTAGONISTS
    Publication number: 20170369473
    Abstract: The invention relates to heterocyclic angiotensin II type 2 (AT2) receptor antagonists of formula (I), and pharmaceutically acceptable salts thereof, ((I) in which all of the variables are as defined in the specification, pharmaceutical compositions thereof,combinations thereof, and their use as medic-aments, particularly for the treatment of neuropathic or inflammatory pain.
    Type: Application
    Filed: January 12, 2016
    Publication date: December 28, 2017
    Inventors: Jane BROWN, Thomas David MCCARTHY, Alan NAYLOR, John Paul WATTS
  • COMPOUNDS, COMPOSITIONS AND METHODS OF USE
    Publication number: 20170369474
    Abstract: Herein, compounds, compositions and methods for modulating inclusion formation and stress granules in cells related to the onset of neurodegenerative diseases, musculoskeletal diseases, cancer, ophthalmological diseases, and viral infections are described.
    Type: Application
    Filed: December 4, 2015
    Publication date: December 28, 2017
    Inventors: Glenn R. Larsen, Manfred Weigele, Joseph P. Vacca
  • Flibanserin Hydrate
    Publication number: 20170369475
    Abstract: The present invention relates to a hydrate of flibanserin, a process for its preparation and to a pharmaceutical composition comprising the hydrate. The invention further relates to the use of said pharmaceutical composition as a medicament in particular for the treatment of hypoactive sexual desire disorder (HSDD).
    Type: Application
    Filed: June 23, 2016
    Publication date: December 28, 2017
    Applicant: Sandoz AG
    Inventors: Andreas Hotter, Hannes Lengauer, Gerhard Widschwenter
  • 2,4-DIAMINO-PYRIMIDINE COMPOUNDS AND METHOD FOR MAKING AND USING THE COMPOUNDS
    Publication number: 20170369476
    Abstract: Compounds within the scope of the present invention have a Formula 1 or a salt or prodrug thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R2 and R3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC50 of from 0.003 ?M to 3.7 ?M; a TAK1 IC50 of from 0.008 ?M to 132 ?M; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.
    Type: Application
    Filed: June 26, 2017
    Publication date: December 28, 2017
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Rose Yen, Jiaxin Yu, Vanessa Taylor, Rajinder Singh
  • 1,3-Dihydroimidazole-2-Thione Derivatives for Use in the Treatment of Pulmonary Arterial Hypertension and Lung Injury
    Publication number: 20170369477
    Abstract: The present invention relates to compounds of formula I: for use in treating pulmonary arterial hypertension and associated conditions, where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkylaryl, alkyloxy, hydroxy, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies hydrogen, alkyl, -alkylaryl or -alkylheteroaryl; X signifies CH2, oxygen atom or sulphur atom; n is 1, 2 or 3, with the proviso that when n is 1, X is not CH2; and the individual (R)- and (S)-enantiomers or mixtures of enantiomers and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: February 14, 2017
    Publication date: December 28, 2017
    Inventors: Patrício Manuel Vieira Araújo SOARES DA SILVA, Maria João Macedo Da Silva BONIFÁCIO
  • 1,3-DIHYDROIMIDAZOLE-2-THIONE DERIVATIVES AS INHIBITORS OF DOPAMINE-BETA-HYDROXYLASE
    Publication number: 20170369478
    Abstract: Compounds of formula I and a method for their preparation are described, where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies -alkyl-aryl or alkyl heteroaryl; X signifies CH2, oxygen atom or sulphur atom; n is 2 or 3; including the individual (R)- and (S)-enantiomers or mixtures of enantiomers thereof; and including pharmaceutically acceptable salts and esters thereof. The compounds have potentially valuable pharmaceutical properties for the treatment of cardiovascular disorders such as hypertension and chronic heart failure.
    Type: Application
    Filed: March 9, 2017
    Publication date: December 28, 2017
    Inventors: Patricio Manuel V. A. Soares Da Silva, David Alexander Learmonth, Alexander Beliaev
  • CYCLIC COMPOUNDS SUBSTITUTED BY A CONDENSED RING SYSTEM
    Publication number: 20170369479
    Abstract: Compounds of formula I defined herein are provided. Uses of these compounds for controlling invertebrate pests, protecting plant propagation material and providing an agricultural and a veterinary composition including the compounds are also described. Compounds for use as intermediate compounds in the preparation of compounds I are also described.
    Type: Application
    Filed: December 21, 2015
    Publication date: December 28, 2017
    Inventors: Pascal Bindschaedler, Gopal Krishna Datta, Wolfgang von Deyn, Franz-Josef Braun
  • COMPOUNDS, COMPOSITIONS, AND METHODS FOR INCREASING CFTR ACTIVITY
    Publication number: 20170369480
    Abstract: The present disclosure is directed to disclosed compounds that increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells.
    Type: Application
    Filed: December 23, 2015
    Publication date: December 28, 2017
    Inventors: Cecilia M. Bastos, Benito Munoz, Bradley Tait
  • Bicyclic PKM2 Activators
    Publication number: 20170369481
    Abstract: Compounds and compositions comprising compounds that activate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that activate PKM2 in the treatment of cancer.
    Type: Application
    Filed: July 10, 2017
    Publication date: December 28, 2017
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders
  • DERIVATIVES OF 5-PHENYL- OR 5-HETEROARYLATHIAZOL-2-CARBOXYLIC AMIDE USEFUL FOR THE TREATMENT OF INTER ALIA CYSTIC FIBROSIS
    Publication number: 20170369482
    Abstract: The present disclosure is based, in part, on the discovery that disclosed compounds such as those having Formula (IIIa), (III), or (IV) can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells.
    Type: Application
    Filed: December 23, 2015
    Publication date: December 28, 2017
    Inventors: Cecilia M. Bastos, Benito Munoz, Bradley Tait
  • ARYL SULFONAMIDES
    Publication number: 20170369483
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: September 6, 2017
    Publication date: December 28, 2017
    Applicant: ChemoCentryx, Inc.
    Inventors: Solomon Ungashe, John J. Wright, Andrew Pennell, Zheng Wei, Anita Melikian
  • IMINOTHIADIAZINE DIOXIDES BEARING AN AMINE-LINKED SUBSTITUENT AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    Publication number: 20170369484
    Abstract: In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R2, ring A, RA, m, ring B, RB, and n are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
    Type: Application
    Filed: January 15, 2016
    Publication date: December 28, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Wen-Lian Wu, Shuwen He, Shawn P. Walsh, Jared N. Cumming
  • HETEROCYCLIC INHIBITORS OF GLUTAMINASE
    Publication number: 20170369485
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.
    Type: Application
    Filed: September 11, 2017
    Publication date: December 28, 2017
    Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy F. Stanton, Eric B. Sjogren
  • GEMINAL SUBSTITUTED QUINUCLIDINE AMIDE COMPOUNDS AS AGONISTS OF ALPHA-7 NICOTONIC ACETYLCHOLINE RECEPTORS
    Publication number: 20170369486
    Abstract: The present invention relates to novel geminal substituted quinuclidine amide compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of ?7-nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.
    Type: Application
    Filed: December 14, 2015
    Publication date: December 28, 2017
    Applicant: AXOVANT SCIENCES GMBH
    Inventors: Raksha ACHARYA, Duane A. BURNETT, Matthew Gregory BURSAVICH, Andrew Simon COOK, Bryce Alden HARRISON, Gerhard KOENIG, Andrew J. MCRINER
  • IMIDAZOPYRIDINES AND IMIDAZOPYRAZINES AS LSD1 INHIBITORS
    Publication number: 20170369487
    Abstract: The present invention is directed to imidazo[1,5-a]pyridine and imidazo[1,5-a]pyrazine derivatives of Formula I, or a pharmaceutically acceptable salt thereof, which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
    Type: Application
    Filed: May 31, 2017
    Publication date: December 28, 2017
    Inventors: Liangxing Wu, Leah C. Konkol, Neil Lajkiewicz, Liang Lu, Meizhong Xu, Wenqing Yao, Zhiyong Yu, Colin Zhang, Chunhong He
  • TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES AS LSD1 INHIBITORS
    Publication number: 20170369488
    Abstract: The present invention is directed to [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-a]pyrazine derivatives of Formula I, or a pharmaceutically acceptable salt thereof, which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
    Type: Application
    Filed: June 5, 2017
    Publication date: December 28, 2017
    Inventors: Liangxing Wu, Xiaozhao Wang, Wenqing Yao, Colin Zhang
  • CK2 INHIBITORS, COMPOSITIONS AND METHODS THEREOF
    Publication number: 20170369489
    Abstract: The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula (I), or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof. For Formula (I) compounds R1, R2, R3, Ar and Z are as defined in the specification. The inventive Formula (I) compounds are inhibitors of CK2 and find utility in any number of therapeutic applications, including but not limited to treatment of proliferative disorders such as cancer, inflammation and immunological disorders.
    Type: Application
    Filed: June 23, 2017
    Publication date: December 28, 2017
    Inventors: Stephen E. WEBBER, Xueliang TAO, Elena BRIN
  • FLUORINATED TETRAHYDRONAPHTHYRIDINYL NONANOIC ACID DERIVATIVES AND USES THEREOF
    Publication number: 20170369490
    Abstract: The present invention relates to fluorinated compounds of formula I and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing the fluorinated compounds of the invention, and methods of treating fibrosis, macular degeneration, diabetic retinopathy (DR), macular edema, diabetic macular edema (DME), and macular edema following retinal vein occlusion (RVO), by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: September 11, 2017
    Publication date: December 28, 2017
    Inventors: Ben C. ASKEW, Takeru FURUYA
  • COMPOUNDS AND METHODS FOR TARGETING HSP90
    Publication number: 20170369491
    Abstract: Described herein are compounds that may selectively bind to Hsp90, methods of using the compounds, and kits including the compounds. The compounds may include detection moieties such as fluorophores that may allow for selective detection of Hsp90 in a sample.
    Type: Application
    Filed: July 18, 2017
    Publication date: December 28, 2017
    Inventors: Timothy Haystead, Philip Floyd Hughes
  • 1,3-SUBSTITUTED 2-AMINO-INDOLE DERIVATIVES AND ANALOGUES USEFUL IN THE TREATMENT OR PREVENTION OF DIABETES MELLITUS, OBESITY, AND INFLAMMATORY BOWEL DISEASE
    Publication number: 20170369492
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein Q, X4, X5, X6, X7, R1, R2, R3 and R8 are as defined in the specification, processes for the preparation of such compounds, pharmaceutical compositions containing them and the use of such compounds in therapy.
    Type: Application
    Filed: June 24, 2015
    Publication date: December 28, 2017
    Inventors: Richard DAVENPORT, Jonathan DUNN, William FARNABY, Duncan HANNAH, David HARRISON, Susanne WRIGHT
  • 6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
    Publication number: 20170369493
    Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.
    Type: Application
    Filed: December 2, 2015
    Publication date: December 28, 2017
    Inventors: Michiel Luc, Maria Van Gool, Manuel Jesús Alcázar-Vaca, Sergio-Alvar Alonso-de Diego, Ana Isabel De Lucas Olivares
  • DRUG FOR TREATING DISORDERS OF CORNEAL EPITHELIUM
    Publication number: 20170369494
    Abstract: A new agent for the treatment of a corneal epithelium disorder, which acts directly on corneal epithelial cells, is provided. Disclosed is an agent for the treatment of a corneal epithelium disorder, the agent comprising a compound of Formula (1) or a salt thereof as an active ingredient: wherein A is an aromatic ring, a heterocyclic ring, or an aliphatic ring; R2, R3, and R4, which may be identical or different, each independently are, for example, a hydrogen atom, a halogen atom; B is an aromatic ring which may have a substituent, a heterocyclic ring which may have a substituent, or an aliphatic ring which may have a substituent; —X—, —Y—, and —Z—, which may be identical or different, each independently are O—, —NH—, —NR5—, —S—, —SO—, —SO2—, —CH2—, —CR6R7—, or —CO—; and —W— is —NR1—, —O—, or —CR8R9—.
    Type: Application
    Filed: December 21, 2015
    Publication date: December 28, 2017
    Applicant: EA PHARMA CO., LTD.
    Inventors: Tohru MIZUSHIMA, Hiroshi IWATA
  • MOLECULAR ISOTOPIC ENGINEERING
    Publication number: 20170369495
    Abstract: The present invention relates to molecular isotopic engineering. The present invention relates to a method or process for preparing a target compound of a statistically defined isotopic composition comprising the step of reacting one or more reactant compounds, wherein each reactant compound is of a statistically defined isotopic composition. The reactant compound is reacted in a chemical process or a biological process thereby generating an isotopic mass balance, or further, an isotopic fractionation to produce the target compound. The present invention also relates to a statistically defined isotopic composition of a target compound. The statistically defined isotopic composition comprises an internal marker, and can be used as, for example, a security feature, an identity indicator, or a purity indicator of the target compound.
    Type: Application
    Filed: December 30, 2015
    Publication date: December 28, 2017
    Inventor: John P. JASPER
  • PYRAZOLO[3,4-D]PYRIMIDIN DERIVATIVE AND ITS USE FOR THE TREATMENT OF LEISHMANIASIS
    Publication number: 20170369496
    Abstract: The compound 3,3,3-trifluoro-N-((1,4-trans)-4-((3-((S)-2-methylmorpholino)-IH-pyrazolo[3,4-d]pyrimidin-6-yl)amino)cyclohexyl)propane-1-sulfonamide having the Formula (I) or a salt thereof, its opposite enantiomer, compositions comprising the compound and its use in the treatment or prevention of leishmaniasis, particularly visceral leishmaniasis.
    Type: Application
    Filed: January 21, 2016
    Publication date: December 28, 2017
    Inventors: Timothy James MILES, Michael George THOMAS
  • IMIDAZOPYRAZINES AS LSD1 INHIBITORS
    Publication number: 20170369497
    Abstract: The present invention is directed to imidazo[1,2-a]pyrazine derivatives of Formula I, or a pharmaceutically acceptable salt thereof, which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
    Type: Application
    Filed: June 5, 2017
    Publication date: December 28, 2017
    Inventors: Liangxing Wu, Joel R. Courter, Chunhong He, Jingwei Li, Liang Lu, Yaping Sun, Xiaozhao Wang, Wenqing Yao, Colin Zhang, Jincong Zhuo