Patents Issued in April 13, 2017
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Publication number: 20170101366Abstract: An integrated process for making di-functional or multi-functional molecules with concurrent light paraffin upgrading is disclosed. The process involves three primary steps: (1) oxidation of an iso-paraffin to alkyl hydroperoxide and alcohol; (2) converting the alkyl hydroperoxide and alcohol to dialkyl peroxide; and (3) coupling functional molecules into di-functional or multi-functional molecules using the dialkyl peroxide as a radical initiator, while the dialkyl peroxide is converted to a tertiary alcohol. The functional molecules include any functional molecule R—X, where R is a hydrocarbyl group and X is a functional group such as —OH, —CN, —C(O)OH, —NH—, or the like.Type: ApplicationFiled: December 22, 2016Publication date: April 13, 2017Inventor: Kun Wang
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Publication number: 20170101367Abstract: This invention relates to a process for operating a gas phase phosgenation plant (100) to form an isocyanate (4) by reacting an amine (2) with phosgene (1), in which the gas phase phosgenation plant is started up by first charging the plant with phosgene. At the same time as, or after the first charge of phosgene, the amine supply devices are rendered inert using a hot inert gas stream (30). Then, amine is admixed for the first time. In this way and by maintaining a pressure drop in the amine and phosgene devices to the mixing zone, the back mixing of phosgene into the amine-containing reactant stream during start-up is prevented.Type: ApplicationFiled: March 24, 2015Publication date: April 13, 2017Applicant: COVESTRO DEUTSCHLAND AGInventors: Thomas Knauf, Wolfgang Lorenz, Friedhelm Steffens, Rainer Bruns, Wolfgang Taube
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Publication number: 20170101368Abstract: The invention relates to a method for preparing isocyanates by the phosgenation of the corresponding amines in which problems resulting from the formation of deposits in apparatuses of the reaction segment during activation (starting) and deactivation (termination) of the method can be prevented by processing measures, in particular ensuring that there is a surplus of phosgene relative to the phosgenating amine during the critical starting and termination steps of the method.Type: ApplicationFiled: March 24, 2015Publication date: April 13, 2017Inventors: Thomas Knauf, Andreas Karl Rausch, Charles Bjoerndahl, Matthias Ehlers, Peter Plathen, Carlos Alvarez Herrero, Francisco Munoz Velasco
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Publication number: 20170101369Abstract: The present disclosure relates to compounds having the Formula (Formula (I)) which are inhibitors of STAT5.Type: ApplicationFiled: May 29, 2015Publication date: April 13, 2017Inventors: Patrick Thomas Gunning, Abbarna A. Cumaraswamy, Andrew Martin Lewis, Mulu Geletu-Heye
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Publication number: 20170101370Abstract: What is described is a compound of formula I wherein R is a linear alkyl of 1 to 12 carbons, or a linear alkenyl or alkynyl of 2 to 12 carbons; L is a linear alkylene or alkenylene of 5 to 18 carbons; X is —CO—O— or —O—CO—; Y is S or O; R1 is a linear or branched alkylene consisting of 1 to 6 carbons; and R2 and R3 are the same or different, consisting of a hydrogen or a linear or branched alkyl consisting of 1 to 6 carbons; and n is 1-6; or a salt, a solvate, or a pharmaceutical formulation thereof.Type: ApplicationFiled: November 9, 2016Publication date: April 13, 2017Inventors: Joseph E. Payne, Padmanabh Chivukula
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Publication number: 20170101371Abstract: A family of amine mining collectors that uses alkoxylates allows for the easy adjustment of solubility and molecular weight useful because anionic and cationic mineral collectors require such varying degrees of solubility and molecular weight. The family of the present invention allows for the optimization of both parameters and an increase in collector efficiency.Type: ApplicationFiled: October 21, 2016Publication date: April 13, 2017Inventor: Thomas P. Daly
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Publication number: 20170101372Abstract: Sweetness receptor antagonists represented by formula (I): wherein each symbol is described herein, are useful for the prophylaxis or treatment of metabolic syndrome, diabetes, obesity and the like.Type: ApplicationFiled: December 23, 2016Publication date: April 13, 2017Applicant: AJINOMOTO CO., INC.Inventors: Yoshiro KITAHARA, Koji OHSUMI, Seiji KITAJIMA, Shimpei OGAWA
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Publication number: 20170101373Abstract: Disclosed is a chromatographic process complex for the refining of krill oil extract including desalting, removal of impurities such as trimethylamine oxide (TMAO), and the production of krill oil products including desalted krill oil extract, polar lipid products having polar lipid contents greater than 50 wt-% on a dry or solvent free basis, neutral lipid streams for biodiesel production and astaxanthin. The refinery includes a continuous desalting zone, a fixed bed polar lipid extraction zone to adsorb neutral lipids and astaxanthin to provide a polar lipid extract stream comprising solvent and polar lipids and being essentially free of neutral lipids and astaxanthin, and an astaxanthin separation zone to recover essentially pure astaxanthin and provide a neutral lipid stream. The enriched products of the krill oil refinery are essentially free of TMAO and salt and provide products which can be used as dietary supplements and as medicinal additives.Type: ApplicationFiled: December 16, 2016Publication date: April 13, 2017Inventors: Anil R. Oroskar, Asha A. Oroskar, Alexander B. Smetana, Slobodan Milasinovic, Xuejun Zang
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Publication number: 20170101374Abstract: The present invention provides a method and process for removing at least a portion of a protonated amine compound that is present as an impurity or a contaminant in a quaternary amine compound. The method of invention is particularly useful in producing highly purified ionic liquids that have quaternary amine moiety as the cationic moiety.Type: ApplicationFiled: October 8, 2015Publication date: April 13, 2017Applicant: CoorsTek Fluorochemicals, Inc.Inventors: Andrew R. Riscoe, Joseph C. Poshusta
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Publication number: 20170101375Abstract: The present invention provides a process and a method for producing a quaternary ammonium cation in an aqueous solution while reducing or preventing formation of a protonated ammonium cation. In particular, the quaternary ammonium cation is produced by adding a base to an aqueous reaction mixture comprising a tertiary amine compound and an alkylating agent.Type: ApplicationFiled: October 8, 2015Publication date: April 13, 2017Applicant: COORSTEK FLUOROCHEMICALS, INC.Inventors: Joseph C. Poshusta, Andrew R. Riscoe
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Publication number: 20170101376Abstract: The present invention relates to a process for the synthesis of molecules that have a pyrrole ring bonded to a diol. In particular, the invention relates to the synthesis of molecules that have the pyrrole ring and a diol derived from serinol by means of a process that does not demand the use of solvents or chemical catalysts. The process consists of a first reaction phase that takes place without any solvents and/or organic diluents, giving rise to an intermediate compound, and a second phase in which the intermediate compound is converted into the required compound by heating the reaction mixture to a temperature ranging from 100° to 200° C. for an interval in the range of 1 to 500 minutes, or by adding a carbon allotrope or its derivatives.Type: ApplicationFiled: June 12, 2015Publication date: April 13, 2017Applicant: Politencnico di MilanoInventors: Vincenzina Barbera, Attilio CITTERIO, Maurizio Stefano GALIMBERTI, Gabriella LEONARDI, Roberto SEBASTIANO, Suresh Udhavrao SHISODIA, Antonio Marco VALERIO
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Publication number: 20170101377Abstract: The present invention is directed towards novel methods of synthesis of molindone, synthesis of the intermediates of molindone, and high-purity compositions of molindone. In particular, the invention relates to the methods of synthesis of molindone through the Mannich reaction.Type: ApplicationFiled: November 30, 2016Publication date: April 13, 2017Applicant: Supernus Pharmaceuticals, Inc.Inventors: Martin HANBAUER, Zarghun NAZIR, Peter HILDEBRAND, Attilia FIGINI, Likan LIANG, Tiziano FUMAGALLI
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Publication number: 20170101378Abstract: The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl) pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.Type: ApplicationFiled: December 21, 2016Publication date: April 13, 2017Inventors: David G. HANGAUER, JR., Debasis PATRA, Jeremy A. CODY, Grant J. PALMER, Paul K. ISBESTER, Jonathon SALSBURY
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Publication number: 20170101379Abstract: Provided herein are pyridone compounds, for example, a compound 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.Type: ApplicationFiled: September 30, 2016Publication date: April 13, 2017Inventors: Robert SULLIVAN, Sara HOWARD, Leah FUNG, Kyle W.H. CHAN, Frank MERCURIO
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Publication number: 20170101380Abstract: Processes are described for the preparation of estrogen receptor modulating compound, (E)-3-(4-((E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid I: and salts thereof, and intermediates useful for the preparation of I.Type: ApplicationFiled: October 6, 2016Publication date: April 13, 2017Applicant: Genentech, Inc.Inventors: Stephan Bachmann, Serena Maria Fantasia, Francis Gosselin, Chong Han, Stefan Hildbrand, Theresa Humphries, Christian Jenny, Ngiap-Kie Lim, Andrew McClory, Christian Moessner, Pankaj Rege, Scott Savage, Haiming Zhang
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Publication number: 20170101381Abstract: A compound having the following structure: or a pharmaceutically acceptable salt or derivative thereof. The compound may be used in the treatment or prevention of a disorder selected from appetite regulation, obesity, metabolic disorders, cachexia, anorexia, pain, inflammation, neurotoxicity, neurotrauma, stroke, multiple sclerosis, spinal cord injury, Parkinson's disease, levodopa-induced dyskinesia, Huntington's disease, Gilles de la Tourette's syndrome, tardive dyskinesia, dystonia, amyotrophic lateral sclerosis, Alzheimer's disease, epilepsy, schizophrenia, anxiety, depression, insomnia, nausea, emesis, alcohol disorders, drug addictions such as opiates, nicotine, cocaine, alcohol and psychostimulants, hypertension, circulatory shock, myocardial reperfusion injury, atherosclerosis, asthma, glaucoma, retinopathy, cancer, inflammatory bowel disease, acute and chronic liver disease such as hepatitis and liver cirrhosis, arthritis and osteoporosis.Type: ApplicationFiled: December 19, 2016Publication date: April 13, 2017Inventors: Carla Patricia da Costa Pereira ROSA, Rita GUSMAO DE NORONHA, Laszlo Erno KISS, Patricio Manuel Vieira Araujo SOARES DA SILVA, Domenico RUSSO, Jorge Bruno Reis WAHNON, William MATON
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Publication number: 20170101382Abstract: Provided are a pyrimidine compound represented by formula (1) having excellent harmful pest-exterminating potency, a harmful pest-exterminating agent comprising the compound and an inert carrier, and a method for exterminating harmful pests whereby the effective dose of the compound is used on harmful pests or on areas where harmful pests grow.Type: ApplicationFiled: March 16, 2015Publication date: April 13, 2017Inventors: Hideki UNEME, Ganesh Balkrishna SALUNKE
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Publication number: 20170101383Abstract: The present invention relates to diaminotriazine compounds of the formula (I) and to their use as herbicides. The present invention also relates to agrochemical compositions for crop protection and to a method for controlling unwanted vegetation. wherein A is phenyl, which is substituted by fluorine in the ortho-position and which may additionally carry 1, 2, 3 or 4 identical or different substituents RA; R1, R2 are inter alia H, OH, S(O)2NH2, ON, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, (C3-C6-cycloalkyl)-C1-C4-alkyl, C1-C6-alkoxy, (C1-C6-alkoxy)-C1-C6-alkyl, (C1-C6-alkyl)-carbonyl, (C1-C6-alkoxy)carbonyl, (C1-C6-alkyl)sulfonyl, (C1-C6-alkylamino)carbonyl, di(C1-C6-alkyl)aminocarbonyl, (C1-C6-alkylamino)sulfonyl, di(C1-C6-alkyl)aminosulfonyl and (C1-C6-alkoxy)sulfonyl, etc.Type: ApplicationFiled: March 27, 2015Publication date: April 13, 2017Applicant: BASF SEInventors: Julia MAJOR, Florian VOGT, Frederick CALO, Thomas SEITZ, Doreen SCHACHTSCHABEL, Trevor William NEWTON, Kristin HANZLIK, Klaus KREUZ, Stefan TRESCH, Johannes HUTZLER
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Publication number: 20170101384Abstract: Disclosed herein are compositions and methods for modulating the androgen receptor.Type: ApplicationFiled: December 19, 2016Publication date: April 13, 2017Inventors: Pamela M. ENGLAND, Robert J. Fletterick, Kristopher Kuchenbecker, Felipe de Jesus Cortez
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Publication number: 20170101385Abstract: The present invention relates to novel isoxazoles, a process for their preparation and their use in the preparation of technical textiles and PPE's (Personal Protective Equipments), namely in the preparation of UV-protective and anti-infective textiles and garments.Type: ApplicationFiled: October 4, 2016Publication date: April 13, 2017Inventors: Acelya AKER, Nuket OCAL, Hikmet Nil ERGINDEMIR, Agamirze HAMITBEYLI
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Publication number: 20170101386Abstract: The present invention relates to 1,2,4-oxadiazole and 1,2,4-thiadiazole compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signaling pathway. The invention also refers to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.Type: ApplicationFiled: October 20, 2016Publication date: April 13, 2017Applicant: Aurigene Discovery Technologies LimitedInventors: Pottayil Govindan Nair Sasikumar, Muralidhara Ramachandra, Seetharamaiah Setty Sudarshan Naremaddepalli
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Publication number: 20170101387Abstract: The present invention relates to 1,3,4-oxadiazole and 1,3,4-thiadiazole compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also refers to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.Type: ApplicationFiled: October 18, 2016Publication date: April 13, 2017Applicant: Aurigene Discovery Technologies LimitedInventors: Pottayil Govindan Nair Sasikumar, Muralidhara Ramachandra, Seetharamaiah Setty Sudarshan Naremaddepalli
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Publication number: 20170101388Abstract: The present invention involves a compound represented by general formula (I), a derivative thereof and a use thereof: wherein R1, R2, R3, R4, R5a, R5b, R5c and X are defined as in the description.Type: ApplicationFiled: December 19, 2016Publication date: April 13, 2017Applicant: XUANZHU PHARMA CO., LTD.Inventor: Frank Wu
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Publication number: 20170101389Abstract: The present disclosure relates to a leveling composition for electrodepositing metals.Type: ApplicationFiled: December 22, 2016Publication date: April 13, 2017Applicant: Shinhao Materials LLCInventors: Yun Zhang, Tao Ma, Peipei Dong
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Publication number: 20170101390Abstract: The present invention relates to a method and apparatus for preparation of lactide using a lactide purification process, comprising introducing an aqueous solution comprising lactic acid into a reactor filled with a catalyst and reacting the same to produce crude lactide vapor; and purifying the crude lactide vapor to produce lactide crystals, wherein a first purification comprises collecting and crystallizing the crude lactide vapor using a first solvent to produce lactide crystals, and separating the lactide crystal from a residue through filtration.Type: ApplicationFiled: October 11, 2016Publication date: April 13, 2017Inventors: Dong Won HWANG, Jong San CHANG, Young Kyu HWANG, U Hwang LEE, Do Young HONG, Su Kyung LEE, Kyung Ho CHO, Pravin Pandharinath UPARE
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Publication number: 20170101391Abstract: Compounds of formula (I) which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals.Type: ApplicationFiled: June 17, 2015Publication date: April 13, 2017Applicant: Bayer Pharma AktiengesellschaftInventors: Keith GRAHAM, Ulrich KLAR, Hans BRIEM, Marion HITCHCOCK, Lars BÄRFACKER, Knut EIS, Volker SCHULZE, Gerhard SIEMEISTER, Wilhelm BONE, Jens SCHRÖDER, Simon HOLTON, Philip LIENAU, René TEMPEL, Helmut SONNENSCHEIN, Jozsef BÁLINT, Heinz GRAUBAUM
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Publication number: 20170101392Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.Type: ApplicationFiled: December 23, 2016Publication date: April 13, 2017Inventors: Qiang Yang, Beth Lorsbach, Gregory Whiteker, Gary Roth, Carl DeAmicis, Daniel I. Knueppel, Ann M. Buysse, Kaitlyn Gray, Xiaoyong Li, Joseck M. Muhuhi, Ronald Ross, JR., David E. Podhorez, Yu Zhang
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Publication number: 20170101393Abstract: 3-(3-Chloro-1H-pyrazol-1-yl)pyridine is prepared by cyclizing 3-hydrazinopyridine-dihydrochloride with commercially available 3-ethoxyacrylonitrile to provide 3-(3-amino-1H-pyrazol-1-yl)pyridine, and by converting the amino group to a chloro group by a Sandmeyer reaction.Type: ApplicationFiled: December 23, 2016Publication date: April 13, 2017Inventors: Xiaoyong LI, Qiang YANG, Gary ROTH, Beth LORSBACH
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Publication number: 20170101394Abstract: A compound having the structure of Formula II, or a stereoisomer, tautomer, or a pharmaceutically acceptable salt thereof: The compound is useful as CFTR modulator. Further, a method of using the compound and pharmaceutical composition comprising the compound are provided for treating diseases in lungs, pancreas, gastrointestinal system, sinuses, reproductive system, and the sweat glands.Type: ApplicationFiled: October 6, 2016Publication date: April 13, 2017Inventor: Lin ZHANG
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Publication number: 20170101395Abstract: A compound having the structure of Formula II, or a stereoisomer, tautomer, or a pharmaceutically acceptable salt thereof: The compound is useful as CFTR modulator. Further, a method of using the compound and pharmaceutical composition comprising the compound are provided for treating diseases in lungs, pancreas, gastrointestinal system, sinuses, reproductive system, and the sweat glands.Type: ApplicationFiled: October 6, 2016Publication date: April 13, 2017Inventor: Lin ZHANG
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Publication number: 20170101396Abstract: The invention relates to new quinoxaline derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: ApplicationFiled: March 26, 2015Publication date: April 13, 2017Applicant: ASTEX THERAPEUTICS LTDInventors: Wim VERMEULEN, Steven Anna HOSTYN, Filip Albert Celine CUYCKENS, Russell Mark JONES, Diego Fernando Domenico BROGGINI
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Publication number: 20170101397Abstract: The invention relates to pyrazolyl substituted tetrahydropyranylsulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: October 7, 2016Publication date: April 13, 2017Applicant: GRÜNENTHAL GMBHInventors: Stefan Schunk, Melanie Reich, René Michael Koenigs
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Publication number: 20170101398Abstract: The invention relates to pyrazolyl substituted tetrahydropyranylsulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: October 7, 2016Publication date: April 13, 2017Applicant: GRÜNENTHAL GMBHInventors: Stefan SCHUNK, Melanie Reich, René Michael Koenigs
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Publication number: 20170101399Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?Type: ApplicationFiled: May 26, 2015Publication date: April 13, 2017Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITEDInventors: Hui LEI, Xin MA, Feng REN, Xichen LIN, Robert W. MARQUIS, JR.
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Publication number: 20170101400Abstract: The invention is directed to methods of inducing apoptosis, arresting cell cycle, or inhibiting cellular proliferation, or any combination thereof, in a tumor cell, by administration of an effective amount of an N-acyl homoserine lactone analog (AHL), optionally in conjunction with a tumor modulating agent such tumor necrosis factor (TNF) related apoptosis inducing ligand (TRAIL) to the patient. Novel bioactive analogs of an N-acyl homoserine lactone are also provided.Type: ApplicationFiled: December 22, 2016Publication date: April 13, 2017Inventors: Vladimir Kravchenko, Richard J. Ulevitch, Kim D. Janda
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Publication number: 20170101401Abstract: The invention relates to compounds of the formula (VIII) wherein the moieties R1, R2, R3, R4, and R5 are as defined in the specification, and salts thereof, as well as their use, methods of use for them, methods of their synthesis, and the like. The compounds are protein tyrosine kinase inhibitors and can be used in the treatment of various cancer diseases and cancer-associated pain.Type: ApplicationFiled: June 3, 2015Publication date: April 13, 2017Applicants: The Arizona Board of Regents, on Behalf of the University of Arizona, Universita' Federico IIInventors: Hong-yu Li, Brendan Frett, Massimo Santoro, Francesca Carlomagno
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Publication number: 20170101402Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, or pharmaceutically acceptable salts thereof, compositions thereof, and methods of their use. The condition or disorder mediated by HDAC comprises a neurodegenerative pathology. Accordingly, also provided is a method of treating a neurodegenerative pathology mediated by HDAC in a subject in need of such a treatment, comprising administering to the subject a therapeutically effective amount of at least one compound, or pharmaceutically acceptable salt thereof, described herein.Type: ApplicationFiled: June 1, 2015Publication date: April 13, 2017Inventors: Celia Dominguez, Ignacio Muñoz-Sanjuán, Christopher A. Luckhurst, Daniel R. Allen, Gilles Raphy, Roland W. Bürli, Perla Breccia, Alan F. Haughan, Grant Wishart, Samantha J. Hughes, Rebeca E. Jarvis, Huw D. Vater, Stephen D. Penrose, Michael Wall, Andrew J. Stott, Elizabeth A. Saville-Stones
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Publication number: 20170101403Abstract: A compound having the structure of Formula II, or a stereoisomer, tautomer, or a pharmaceutically acceptable salt thereof: The compound is useful as CFTR modulator. Further, a method of using the compound and pharmaceutical composition comprising the compound are provided for treating diseases in lungs, pancreas, gastrointestinal system, sinuses, reproductive system, and the sweat glands.Type: ApplicationFiled: October 6, 2016Publication date: April 13, 2017Inventor: Lin ZHANG
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Publication number: 20170101404Abstract: Compounds and compositions for treating, preventing or managing cancer are disclosed. The compositions provided herein comprise SNS-595 and N-desmethyl-SNS-595. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment using the compounds and compositions.Type: ApplicationFiled: May 16, 2016Publication date: April 13, 2017Inventors: Daniel C. Adelman, Marc J. Evanchik, Anantha Sudhakar, Jeffrey William Jacobs, Jeffrey A. Silverman
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Publication number: 20170101405Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjögren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).Type: ApplicationFiled: October 7, 2016Publication date: April 13, 2017Inventors: Rhalid Akkari, Luke Jonathan Alvey, Xavier Marie Bock, Brian S. Brown, Pieter Isabelle Roger Claes, Marlon D. Cowart, Elsa De Lemos, Nicolas Desroy, Béranger Duthion, Gregory A. Gfesser, Romain Luc Marie Gosmini, Christopher Gaëtan Housseman, Koen Karel Jansen, Jianguo Ji, Philip R. Kym, Jean-Michel Lefrancois, Oscar Mammoliti, Christel Jeanne Marie Menet, Nuria Merayo Merayo, Gregory John Robert Newsome, Adeline Marie Elise Palisse, Sachin V. Patel, Matthieu Rafaël Pizzonero, Anurupa Shrestha, Elizabeth C. Swift, Steven Em iel Van der Plas, Xueqing Wang, Ann de Blieck
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Publication number: 20170101406Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, and R4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjögren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).Type: ApplicationFiled: October 7, 2016Publication date: April 13, 2017Inventors: Rhalid Akkari, Luke Jonathan Alvey, Xavier Marie Bock, Pieter Isabelle Roger Claes, Marlon D. Cowart, Elsa De Lemos, Nicolas Desroy, Béranger Duthion, Gregory A. Gfesser, Romain Luc Marie Gosmini, Christopher Gaëtan Housseman, Koen Karel Jansen, Jianguo Ji, Philip R. Kym, Jean-Michel Lefrancois, Oscar Mammoliti, Christel Jeanne Marie Menet, Gregory John Robert Newsome, Adeline Marie Elise Palisse, Sachin V Patel, Mathieu Rafaël Pizzonero, Anurupa Shrestha, Elizabeth C. Swift, Steven Emiel Van der Plas, Xueqing Wang
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Publication number: 20170101407Abstract: The present application relates to novel 6-chloro-substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: April 29, 2015Publication date: April 13, 2017Applicant: Bayer Pharma AktiengesellschaftInventors: Alexandros VAKALOPOULOS, Markus FOLLMANN, Johannes-Peter STASCH, Frank WUNDER, Tobias MARQUARDT, Lisa DIETZ, Dieter LANG, Volkhart Min-Jian LI
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Publication number: 20170101408Abstract: The present disclosure is related to heteroaryl compounds as MEK inhibitors. These compounds include heteroaryl compounds of formula I, their pharmaceutically acceptable salts, combinations with suitable medicament and pharmaceutical compositions thereof. The present disclosure also includes processes of preparation of the compounds and their use in methods of treatment.Type: ApplicationFiled: December 22, 2016Publication date: April 13, 2017Applicant: LUPIN LIMITEDInventors: Bhavesh DAVE, Rakesh Kumar BANERJEE, Samiron PHUKAN, Abhijit Datta KHOJE, Rajkumar HANGARGE, Jitendra Sambhaji JADHAV, Venkata P. PALLE, Rajender Kumar KAMBOJ
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Publication number: 20170101409Abstract: The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula wherein Ar1 is phenyl or a five or six membered heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O?); R1 is lower alkyl, halogen, cyano or cycloalkyl; Ar2 is a five or six membered heteroaryl group, containing one, two, three or four heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O?), or is benzo[b]thiophenyl; R2 is hydrogen, lower alkyl, halogen, cyano, lower alkyl substituted by hydroxyl, lower alkyl substituted by halogen, lower alkyl substituted by amino, lower alkyl substituted by alkoxy, lower alkyl substituted by amide, or is cycloalkyl; X is CH or N; n is 1 or 2; m is 1 or 2; as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereofType: ApplicationFiled: December 22, 2016Publication date: April 13, 2017Applicant: Hoffmann-La Roche Inc.Inventors: Hans Hilpert, Sabine Kolczewski, Roland Humm, Theodor Stoll, Thorsten Muser, Jean-Marc Plancher, Delphine Gaufreteau
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Publication number: 20170101410Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.Type: ApplicationFiled: October 20, 2016Publication date: April 13, 2017Inventors: Theodore M. Kamenecka, Yuanjun He, William Nguyen, Rong Jiang, Xinyi Song, Robert Jason Herr, Qin Jiang
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Publication number: 20170101411Abstract: The invention relates to Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxyamide of general formula (I) which are inhibitors of phosphodiesterase 2, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.Type: ApplicationFiled: October 12, 2016Publication date: April 13, 2017Inventors: Christoph HOENKE, Barbara BERTANI, Marco FERRARA, Giacomo FOSSATI, Sara FRATTINI, Riccardo GIOVANNINI, Scott HOBSON
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Publication number: 20170101412Abstract: Disclosed are chemical entities of formula (I) wherein X, Y, Z, R1, R3, R4, R5 and R6 are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of formula I.Type: ApplicationFiled: June 3, 2015Publication date: April 13, 2017Inventor: Gideon Shapiro
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Publication number: 20170101413Abstract: This invention relates to heterocyclic compounds, which are pyrimidinone derivatives having human neutrophil elastase inhibitory properties, and their use in therapy.Type: ApplicationFiled: June 12, 2014Publication date: April 13, 2017Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Lilian ALCARAZ, Robert Andrew HEALD, Jonathan Mark SUTTON, Elisabetta ARMANI, Carmelida CAPALDI
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Publication number: 20170101414Abstract: An object to be achieved by the present invention is to provide a novel compound having EGFR inhibitory effects and cell growth inhibitory effects, as well as a medication useful for the prevention and/or treatment of cancer based on the EGFR inhibitory effects. The present invention provides a compound represented by Formula (I) below, or a salt thereof.Type: ApplicationFiled: December 19, 2016Publication date: April 13, 2017Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Takao UNO, Katsumasa NONOSHITA, Tadashi SHIMAMURA
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Publication number: 20170101415Abstract: An invention includes a process for the preparation of (S)-2((4R,4aS,6R,7R,7aR,12bS)-7,9-dimethoxy-1,2,3,4,5,6,7,7a-octahydro-4a,7-ethano-4,12-methanobenzofuro[3,2-e]isoquinolin-6-yl)-3,3-dimethylbutan-2-ol.Type: ApplicationFiled: October 12, 2016Publication date: April 13, 2017Applicant: Noramco, Inc.Inventor: Wen-Chun Zhang