Patents Issued in May 18, 2017
  • FLEXIBLE TO RIGID NANOPOROUS POLYURETHANE-ACRYLATE (PUAC) TYPE MATERIALS FOR STRUCTURAL AND THERMAL INSULATION APPLICATIONS
    Publication number: 20170137376
    Abstract: Novel urethane-acrylate (UAC) Star monomers and polyurethane-acrylate (PUAC) aerogel polymers derived therefrom are described herein, along with other novel, related monomers and polymers. Also described herein are processes for preparing the UAC Star monomers, the PUAC aerogel polymers, and the other related monomers and polymers. The PUAC and related polymers herein are useful in various applications including in structural and thermal insulation.
    Type: Application
    Filed: October 31, 2016
    Publication date: May 18, 2017
    Inventors: Nicholas Leventis, Chariklia Sotiriou-Leventis, Abhishek Bang
  • METHOD FOR PRODUCING PHENOLIC COMPOUND
    Publication number: 20170137377
    Abstract: Provided is a method for producing a compound represented by formula (2-b), which is useful as an intermediate for producing agricultural chemicals. The method includes a step for obtaining a compound represented by formula (2-a) by oxidizing the compound represented by formula (1) with hydrogen peroxide in the presence of sulfuric acid and/or a C1-6 alkanesulfonic acid that may be halogen-substituted and in the presence of a C2-12 aliphatic carboxylic acid and/or sulfolane. The method also includes a step for obtaining a compound represented by formula (2-b) by nitrating a compound represented by formula (2-a) in the presence of sulfuric acid and/or a C1-6 alkanesulfonic acid that may be halogen-substituted.
    Type: Application
    Filed: June 9, 2015
    Publication date: May 18, 2017
    Inventors: Kazuya UEKI, Toshiyuki KIJI, Hiroaki OKAMOTO
  • Production of Pyrrolidine Derivatives
    Publication number: 20170137378
    Abstract: The present invention relates to a method for the production of a pyrrolidine derivative.
    Type: Application
    Filed: January 30, 2017
    Publication date: May 18, 2017
    Inventors: Bernhard Hirt, Claus Zeyher
  • Composition for the Modulation of the Activity of Non-Structure Proteins
    Publication number: 20170137379
    Abstract: The present invention relates to a composition for the modulation of the activity of non-structure proteins and a compound contained therein.
    Type: Application
    Filed: January 30, 2017
    Publication date: May 18, 2017
    Inventors: Bernhard Hirt, Claus Zeyher, Corinna Gleiser, Lothar Just
  • IONIC LIQUID FILMS WITH MULTIPLE FUNCTIONALITIES FOR SURFACE MODIFICATION OF BIOMEDICAL ALLOYS
    Publication number: 20170137380
    Abstract: The present disclosure relates ionic liquids which are used as lubricants for medical devices. In some aspects, the ionic liquids of the present disclosure can exhibit antimicrobial or host cell integrative activity or a combination of functionalities. In some aspects, the present disclosure also provides devices coated with the ionic liquid.
    Type: Application
    Filed: July 2, 2015
    Publication date: May 18, 2017
    Inventors: Danieli C. RODRIGUES, Izabelle de Mello GINDRI, Clarissa P. FRIZZO, Marcos A.P. MARTINS
  • PREPARATION OF PIPERIDINE-4-CARBOTHIOAMIDE
    Publication number: 20170137381
    Abstract: The present invention describes a novel process for preparing piperidine-4-carbothioamide.
    Type: Application
    Filed: June 8, 2015
    Publication date: May 18, 2017
    Applicant: Bayer CropScience Aktiengesellschaft
    Inventors: Marco BRÜNJES, Mark James FORD
  • QUATERNARY HETEROATOM CONTAINING COMPOUNDS
    Publication number: 20170137382
    Abstract: The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II): comprising treating a compound of Formula (I): with a transition metal catalyst and under alkylation conditions as valence and stability permit.
    Type: Application
    Filed: December 1, 2016
    Publication date: May 18, 2017
    Inventors: Brian M. Stoltz, Scott C Virgil, David E. White, Taiga Yurino, Yiyang Liu, Douglas C. Behenna, Douglas Duquette, Christian Eidamshaus
  • DEUTERATED CFTR POTENTIATORS
    Publication number: 20170137383
    Abstract: This invention relates to compounds of Formula I: and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a CFTR potentiator.
    Type: Application
    Filed: November 22, 2016
    Publication date: May 18, 2017
    Inventor: Adam J. Morgan
  • PROCESS FOR THE PREPARATION OF KINASE INHIBITORS AND INTERMEDIATES THEREOF
    Publication number: 20170137384
    Abstract: Described are processes for the synthesis of certain compounds, useful for treating diseases, e.g. eye disease, such as glaucoma and ocular hypertension, in a subject.
    Type: Application
    Filed: November 17, 2015
    Publication date: May 18, 2017
    Inventors: Jill M. Sturdivant, Mitchell A. deLong, Gilles Chambournier, Michael G. Pamment, Victor Fedij
  • ISOQUINOLINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    Publication number: 20170137385
    Abstract: A compound of formula (I): wherein the substituents are as defined in the description. Medicinal products containing the same which are useful in treating or preventing pathologies which are the result of activation of the RhoA/ROCK pathway and phosphorylation of the myosin light chain.
    Type: Application
    Filed: February 20, 2015
    Publication date: May 18, 2017
    Inventors: Stéfano CHIMENTI, Christine COURCHAY, Aimee DESSINGES, Françoise GELLIBERT, Bertrand GOUMENT, Marc KONNERT, Jean-Louis PEGLION, Christophe POITEVIN, Jean-Paul VILAINE, Nicole VILLENEUVE
  • IBRUTINIB INTERMEDIATE COMPOUNDS, PREPARATION METHODS AND USES THEREOF
    Publication number: 20170137386
    Abstract: The present invention relates to the technical field of ibrutinib, particularly to the technical field of ibrutinib intermediate compounds and preparation methods thereof. The intermediate compounds are represented by formula A, wherein, the dotted line represents a double bond or a single bond between carbon and oxygen.
    Type: Application
    Filed: April 21, 2015
    Publication date: May 18, 2017
    Applicant: ZHEJIANG JIUZHOU PHARMA SCIENCE & TECHNOLOGY CO., LTD.
    Inventors: Yunyu HUA, Xianyi ZHANG, Hongjun GAO, Yuanqiang LI, Daqing CHE
  • PHARMACOLOGICALLY ACTIVE QUINAZOLINEDIONE DERIVATIVES
    Publication number: 20170137387
    Abstract: Compounds of formula (I), wherein R1 through R8 are as defined in the claims, exhibit a positive allosteric GABAB modulator effect and are thus useful as positive allosteric modulators of the GABAB receptor.
    Type: Application
    Filed: May 8, 2015
    Publication date: May 18, 2017
    Inventors: Peteris PRUSIS, Iisa HÖGLUND, Olli TÖRMAKANGAS, Ari HIETANEN, Riina ARVELA, Anniina VESALAINEN, Terhi HEIKKINEN
  • NEPRILYSIN INHIBITORS
    Publication number: 20170137388
    Abstract: In one aspect, the invention relates to compounds having the formula I: where R1-R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: January 30, 2017
    Publication date: May 18, 2017
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Melissa Fleury, Anne-Marie Beausoliel, Adam D. Hughes, Daniel D. Long, Donna A.A. Wilton
  • LINKER MOLECULE FOR MULTIPLEX RECOGNITION BY ATOMIC FORCE MICROSCOPY (AFM)
    Publication number: 20170137389
    Abstract: Some of the embodiments of the present disclosure relate to a compound of the formula, and methods of preparing and using same.
    Type: Application
    Filed: May 7, 2015
    Publication date: May 18, 2017
    Inventors: Peiming ZHANG, Stuart LINDSAY, Saikat MANNA, Subhadip SENAPATI
  • Substituted [1,2,4]triazole and imidazole compounds as fungicides
    Publication number: 20170137390
    Abstract: The present invention relates to compounds of the formula I wherein the variables are defined in the claims and the specification, to their preparation and their use as fungicides.
    Type: Application
    Filed: May 4, 2015
    Publication date: May 18, 2017
    Inventors: Wassilios GRAMMENOS, Nadege BOUDET, Bernd MUELLER, Maria Angelica QUINTERO PALOMAR, Ana ESCRIBANO CUESTA, Erica May Wilson LAUTERWASSER, Jan Klaas LOHMANN, Thomas GROTE, Manuel KRETSCHMER, Ian Robert CRAIG
  • POLYBENZOXAZINE PRECURSOR AND METHOD FOR PREPARING SAME
    Publication number: 20170137391
    Abstract: Disclosed is a polybenzoxazime precursor and a method of preparing the same. The polybenzoxazime precursor is used to prepare a hardened material having improved thermal characteristics, having high thermal and flame-retardant characteristics while maintaining its excellent electrical characteristics, or having high thermal and electrical characteristics, thus being available for use in a copper clad laminate, a semiconductor encapsulate, a printed circuit board, an adhesive, a paint, and a mold.
    Type: Application
    Filed: June 30, 2015
    Publication date: May 18, 2017
    Applicant: KOLON INDUSTRIES, INC.
    Inventors: Hee Jin CHO, Do Kyung SUNG, Ki Hyun PARK, Sang Hun PARK, Hyun Soo KAGN
  • RIBONUCLEOTIDE REDUCTASE INHIBITORS AND METHODS OF USE
    Publication number: 20170137392
    Abstract: Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme, as well as methods of synthesizing these novel compounds. The compounds may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.
    Type: Application
    Filed: January 27, 2017
    Publication date: May 18, 2017
    Inventors: David Horne, Christopher Lincoln
  • ARYL SULTAM DERIVATIVES AS RORc MODULATORS
    Publication number: 20170137393
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, X1, X2, X3, X4, Y, Z, A, R1, R2, R3, R4, R5 R6, R7, R8, R9, R10, R11, R12 and R13 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis, muscular sclerosis and psoriasis.
    Type: Application
    Filed: June 30, 2016
    Publication date: May 18, 2017
    Applicant: Genentech, Inc.
    Inventors: Monique Bodil van Niel, Benjamin Fauber, Emanuela Gancia, Simon Gaines, Alberto Gobbi, Christopher Hurley, Tammy Ladduwahetty, Olivier Rene, David Vesey, Stuart Ward, Paul Winship
  • ALKYLENE OXIDE SEPARATION SYSTEMS, METHODS, AND APPARATUSES
    Publication number: 20170137394
    Abstract: A propylene oxide separation system that comprises a distillation column, a decanter, and water wash system. The distillation column is configured to receive a crude propylene oxide stream, discharge an impurity stream that comprises methanol and water, and discharge a bottoms stream that comprises a majority of the propylene oxide entering in the crude propylene oxide stream. The decanter is configured to receive at least a portion of the impurity stream and a hydrocarbon solvent to provide for formation in the decanter of an organic phase and an aqueous phase. The organic phase comprises propylene oxide and hydrocarbon solvent, and is sent to the distillation column. The aqueous phase comprises a majority weight percent of the methanol and the water entering in the impurity stream. The water wash system is configured to receive and purge the aqueous phase from the propylene oxide separation system.
    Type: Application
    Filed: January 30, 2017
    Publication date: May 18, 2017
    Applicant: Lyondell Chemical Technology, L.P.
    Inventors: Xiangmin Li, Te Chang, David W. Leyshon, Walter S. Dubner, Elizabeth I. Ross-Medgaarden
  • PROCESS FOR THE PRODUCTION OF FURAN AND ITS DERIVATIVES
    Publication number: 20170137395
    Abstract: The present invention provides a process for the production of furan, said process comprising the steps of: i) contacting furfural with a decarbonylation catalyst in a decarbonylation reactor to produce a gaseous decarbonylation reaction product stream comprising furan and carbon monoxide; ii) contacting said gaseous decarbonylation reaction product stream with a solvent stream comprising furfural; iii) absorbing at least a portion of the furan present in the gaseous decarbonylation reaction product stream into the solvent stream to provide a furan-containing solvent stream and a gaseous stream comprising carbon monoxide; iv) separating the furan from the furan containing solvent stream by distillation to provide a first furan stream; and v) using at least a portion of the remaining solvent stream comprising furfural as at least a portion of the furfural provided to the decarbonylation reactor.
    Type: Application
    Filed: March 26, 2015
    Publication date: May 18, 2017
    Inventors: Sipke Hidde WADMAN, Jean Paul Andre Marie Joseph Ghislain LANGE
  • PROCESS FOR THE SELECTIVE OXIDATION OF 5-HYDROXYMETHYLFURFURAL
    Publication number: 20170137396
    Abstract: Process for the selective production of oxidized furan derivatives starting from 5-hydroxymethyl-2-furfural in the presence of a solvent, an oxidation agent, a catalyst, and optionally a base, which process is characterized in that the oxidation process is carried out continuously in flow, and there are provided means for varying reaction parameters.
    Type: Application
    Filed: June 17, 2015
    Publication date: May 18, 2017
    Inventors: Marko Mihovilovic, Michael Schön, Stefan Dochev
  • METHODS FOR PURIFYING 5-(HALOMETHYL)FURFURAL
    Publication number: 20170137397
    Abstract: The present disclosure provides methods for purifying a 5-(halomethyl)furfural composition, including 5-(chloromethyl)furfural, at operating conditions that decrease or minimize the decomposition or degradation of 5-(chloromethyl)furfural during the process. The methods may employ certain solvents, operating conditions, and/or techniques (e.g., gas stripping). The gaseous 5-(halomethyl)furfural produced from the process can be condensed or deposited to yield 5-(halomethyl)furfural in liquid or solid form. The solid 5-(halomethyl)furfural may be amorphous or crystalline.
    Type: Application
    Filed: January 27, 2017
    Publication date: May 18, 2017
    Applicant: MICROMIDAS, INC.
    Inventors: Alex B. WOOD, Shawn M. BROWNING, Makoto N. MASUNO, Ryan L. SMITH, John BISSELL, II
  • OPSIN-BINDING LIGANDS, COMPOSITIONS AND METHODS OF USE
    Publication number: 20170137398
    Abstract: Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.
    Type: Application
    Filed: October 24, 2016
    Publication date: May 18, 2017
    Applicant: BIKAM PHARMACEUTICALS, INC.
    Inventors: David S. Garvey, Gregory J. Larosa, Jeremy R. Greenwood, Leah L. Frye, Tan Quach, Jamie B. Cote, Judd Berman
  • HIGH-PURITY MAGNESIUM LITHOSPERMATE B AND PREPARATION METHOD THEREFOR
    Publication number: 20170137399
    Abstract: The present invention relates to a method for preparing magnesium lithospermate B. The method is characterized in that: magnesium lithospermate B is extracted or purified from a Salvia miltiorrhiza plant material or a Salvia miltiorrhiza extract in the presence of an added magnesium salt. The present invention also relates to a high-purity magnesium lithospermate B product prepared by the method of the present invention, wherein the content of magnesium lithospermate B is more than 95% by weight.
    Type: Application
    Filed: February 9, 2015
    Publication date: May 18, 2017
    Inventors: Lijiang Xuan, Yiping Wang, Weibin Song, Chunguang Chen, Dingxiang Li, Xiaoyu Zhou, Yunlong Gu, Liang Hu, Jing Zhao, Wenwei Xu, Shumei Wang
  • FLAVAGLINE DERIVATIVES
    Publication number: 20170137400
    Abstract: The invention relates to compounds of the following general formula (I) in the form of one of the enantiomers thereof or a mixture of the enantiomers thereof, and the pharmaceutically acceptable salts and/or solvates thereof, especially for the use thereof as a medicament, more specifically in cancer treatment. The invention also relates to pharmaceutical compositions containing same and to the methods for the production thereof.
    Type: Application
    Filed: July 6, 2015
    Publication date: May 18, 2017
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Frédéric MARION, El Bachir KALOUN, Frédéric LIEBY-MULLER, Michel PEREZ, Jean-Philippe ANNEREAU, Laurent CREANCIER
  • Chemokine CXCR4 and CCR5 Receptor Modulators and Uses Related Thereto
    Publication number: 20170137401
    Abstract: The disclosure relates to chemokine receptor modulators and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising compounds disclosed herein or pharmaceutically acceptable salts or prodrugs thereof. In certain embodiments, the compositions disclosed herein are used for managing chemokine related conditions, typically prevention or treatment of viral infections such as HIV or for managing cancer.
    Type: Application
    Filed: May 15, 2015
    Publication date: May 18, 2017
    Applicant: Emory University
    Inventors: Bryan D. Cox, Lawrence J. Wilson, Anthony Prosser, Dennis C. Liotta, James P. Snyder
  • INHIBITORS OF LYSINE SPECIFIC DEMETHYLASE-1
    Publication number: 20170137402
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. 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.
    Type: Application
    Filed: June 26, 2015
    Publication date: May 18, 2017
    Inventors: Young K. Chen, Toufike Kanouni, Jeffrey Alan Stafford, James Marvin Veal
  • REGIOSELECTIVE N-2 ARYLATION OF INDAZOLES
    Publication number: 20170137403
    Abstract: A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.
    Type: Application
    Filed: January 30, 2017
    Publication date: May 18, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Cheol K. Chung, Mark E. Scott, Paul Gerard Bulger, Kevin Michael Belyk, John Limanto, Guy R. Humphrey
  • CRYSTALLINE FORM OF A SUBSTITUTED QUINOLINE COMPOUND AND PHARMACEUTICAL COMPOSITIONS THEREOF
    Publication number: 20170137404
    Abstract: The present invention relates to a crystalline form of N-(3-fluoro-4-((7-(2-hydroxy-2-methylpropoxy)quinolin-4-yl)oxy)phenyl)-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide p-toluenesulfonate, the process for preparing the crystalline form thereof, and pharmaceutical compositions comprising the crystalline form thereof. This invention also relates to a method of using such a crystalline form in the treatment of hyperproliferative diseases in mammals, especially in humans.
    Type: Application
    Filed: November 12, 2016
    Publication date: May 18, 2017
    Applicants: Sunshine Lake Pharma Co., Ltd., Calitor Sciences, LLC
    Inventors: Ning Xi, Mingming Sun
  • COMPOUNDS FOR THE TREATMENT OF HIV
    Publication number: 20170137405
    Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Application
    Filed: February 3, 2017
    Publication date: May 18, 2017
    Inventors: Steven S. Bondy, Carina E. Cannizzaro, Chien-Hung Chou, Randall L. Halcomb, Yunfeng Eric Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
  • ERK INHIBITORS AND USES THEREOF
    Publication number: 20170137406
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Application
    Filed: November 28, 2016
    Publication date: May 18, 2017
    Inventors: Nadia Haq, Deqiang Niu, Russell C. Petter, Lixin Qiao, Juswinder Singh, Zhendong Zhu
  • HETEROCYCLIC COMPOUNDS AND USES THEREOF
    Publication number: 20170137407
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.
    Type: Application
    Filed: October 25, 2016
    Publication date: May 18, 2017
    Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
  • PROCESSES FOR THE PREPARATION OF PYRAZOLE DERIVATIVES USEFUL AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR
    Publication number: 20170137408
    Abstract: The present invention relates to processes for preparing pyrazole derivatives of Formula (I) and salts and pharmaceutical compositions of the salts thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to salts of compounds of Formula (I) and pharmaceutical compositions thereof.
    Type: Application
    Filed: January 9, 2017
    Publication date: May 18, 2017
    Inventors: Ashwin M. Krishnan, Tawfik Gharbaoui
  • Amine Cationic Lipids and Uses Thereof
    Publication number: 20170137409
    Abstract: The present invention relates to lipid compounds and uses thereof. In particular, the compounds include a class of cationic lipids having an amine moiety, such as an amino-amine or an amino-amide moiety. The lipid compounds are useful for in vivo or in vitro delivery of one or more agents (e.g., a polyanionic payload or an antisense payload, such as an RNAi agent).
    Type: Application
    Filed: January 17, 2017
    Publication date: May 18, 2017
    Inventor: Bob Dale BROWN
  • FUSED CYCLOALKYL-PYRIMIDINE COMPOUNDS AND USES THEREOF
    Publication number: 20170137410
    Abstract: Fused cycloalkyl-pyrimidine compounds that are kinase inhibitors, such as multi-kinase inhibitors, are provided. The compounds may be used in a method of treating cancer. Pharmaceutical compositions containing a fused cycloalkyl-pyrimidine compound and a pharmaceutically acceptable carrier are also provided, as are kits containing a fused cycloalkyl-pyrimidine compound or salt thereof and instructions for use, e.g., in a method of treating cancer.
    Type: Application
    Filed: June 26, 2015
    Publication date: May 18, 2017
    Applicant: Medivation Technologies, Inc
    Inventors: Sarvajit CHAKRAVARTY, Roopa RAI, Michael John GREEN, Amantullah ANSARI, Anil Kumar AGARWAL
  • COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY
    Publication number: 20170137411
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Application
    Filed: January 30, 2017
    Publication date: May 18, 2017
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
  • SUBSTITUTED PYRROLIDINES AS FACTOR XIA INHIBITORS FOR THE TREATMENT THROMBOEMBOLIC DISEASES
    Publication number: 20170137412
    Abstract: The present invention provides compounds of the general formula (I), their salts and N-oxides, and solvates and prodrugs thereof (wherein the substituents are as defined in the description). The compounds of the general formula (I) are inhibitors of factor XIa, and are useful in the prevention of and/or therapy for thromboembolic diseases.
    Type: Application
    Filed: January 23, 2017
    Publication date: May 18, 2017
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Akira IMAGAWA, Takashi KONDO, Taihei NISHIYAMA, Steve COURTNEY, Chris YARNOLD, Osamu ICHIHARA, Stuart FLANAGAN
  • NOVEL HALOGEN-SUBSTITUTED COMPOUNDS
    Publication number: 20170137413
    Abstract: The invention relates inter alia to halogen-substituted compounds of the general formula (I) in which the A1-A4, T, W, Q, R1 and Z1-Z3 radicals are as defined in the description. Also described are processes for preparing the compounds of the formula (I). The compounds according to the invention are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.
    Type: Application
    Filed: April 1, 2015
    Publication date: May 18, 2017
    Inventors: MICHAEL MAUE, ANNE DECOR, THOMAS BRETSCHNEIDER (DECEASED), NIKLAS TIM BRETSCHNEIDER (SOLE HEIRS), UTA BRETSCHNEIDER (SOLE HEIRS), JULIA JOHANNA HAHN, WERNER HALLENBACH, REINER FISCHER, HANS-GEORG SCHWARZ, ULRICH GOERGENS, KERSTIN ILG, KLAUS RAMING, JOHANNES KOEBBERLING, WALTER HUEBSCH, ANDREAS TURBERG
  • COMPOUNDS AND THEIR METHODS OF USE
    Publication number: 20170137414
    Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
    Type: Application
    Filed: March 20, 2015
    Publication date: May 18, 2017
    Applicant: AGIOS Pharmaceuticals, Inc.
    Inventors: Giovanni Cianchetta, Rene M. Lemieux, Sheldon Cao, Yue Ding, Zhixiong Ye
  • SULFONAMIDE COMPOUNDS AS VOLTAGE GATED SODIUM CHANNEL MODULATORS
    Publication number: 20170137415
    Abstract: The present invention relates to the compound of Formula (I) wherein the substituents are as described herein, and their use in a medicine for the treatment of diseases, disorders associated with the inhibition of Voltage-gated sodium channels (VGSC) particularly NaV1.7. It further relates to the compounds herein and their pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof useful in treating diseases, disorders, syndromes and/or conditions associated with the inhibition of Voltage-gated sodium channels (VGSC) particularly NaV1.7. The invention also relates to process for the preparation of the compounds of the invention.
    Type: Application
    Filed: March 27, 2015
    Publication date: May 18, 2017
    Inventors: Vidya RAMDAS, Rajeshkumar Maganlal LORIYA, Deepak Sahebrao WALKE, Amit Kumar DAS, Talha Hussain KHAN, Moloy BANERJEE, Venkata P. PALLE, Rajender Kumar KAMBOJ
  • 6-AMINO-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL OR 3-AMINOCHROMAN-7-YL DERIVATIVES
    Publication number: 20170137416
    Abstract: The present invention relates to compounds TAAR receptor antagonists of formula I wherein X, R, L, Ar and R1 are as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric disorders with compounds of formula I.
    Type: Application
    Filed: January 26, 2017
    Publication date: May 18, 2017
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Giuseppe Cecere, Guido Galley, Annick Goergler, Roger Norcross, Philippe Pflieger, Alina Tirla, Philipp Schmid
  • PHENYLPIPERIDINECARBOXAMIDE DERIVATIVES AS FUNGICIDES
    Publication number: 20170137417
    Abstract: Phenylpiperidinecarboxamide derivatives of the formula (I) in which the symbols R1, R2, R3 and R4 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).
    Type: Application
    Filed: March 20, 2015
    Publication date: May 18, 2017
    Applicant: Bayer Cropscience Aktiengesellschaft
    Inventors: STEFAN HILLEBRAND, PIERRE WASNAIRE, ULRIKE WACHENDORFF-NEUMANN, TOMOKI TSUCHIYA
  • SMALL MOLECULAR PROBES, PROCESSES AND USE THEREOF
    Publication number: 20170137418
    Abstract: The present disclosure relates to compounds which function as small molecule fluorescent probes which aid in recognition of specific sequences in DNA and detection of A? aggregates. Probes/dyes of the instant disclosure are specific to AT-rich sequences of DNA and A? aggregates. These small organic dyes/probes are capable of exhibiting switch-on fluorescence and play an important role in fluorescence spectroscopy, diagnostics, imaging and biomedical applications.
    Type: Application
    Filed: April 3, 2015
    Publication date: May 18, 2017
    Applicant: JAWAHARLAL NEHRU CENTRE FOR ADVANCED SCIENTIFIC RESEARCH
    Inventors: Govindaraju Thimmaiah, Nagarjun Narayanaswamy, Kolla Rajasekhar
  • DERIVATIVES OF 2H-PYRAZOLO[4,3-C]QUINOLIN-3(5H)-ONE AND USE THEREOF
    Publication number: 20170137419
    Abstract: The invention relates to compounds of formula (I) or the pharmaceutically acceptable solvates thereof, as well as to the use thereof as a drug.
    Type: Application
    Filed: June 11, 2015
    Publication date: May 18, 2017
    Inventors: Régis Millet, Philippe Chavatte, Pierre Desreumaux, Mathilde Body, Jamal El Bakali
  • PYRIDINO[1,2-A]PYRIMIDONE ANALOGUE USED AS P13K INHIBITOR
    Publication number: 20170137420
    Abstract: Disclosed is a pyridino[1,2-a]pyrimidone analogue used as a PI3K inhibitor. The present invention particularly relates to a compound represented by formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 16, 2015
    Publication date: May 18, 2017
    Inventors: Chengde WU, Tao YU, Shuhui CHEN
  • QUINOLIZINONE DERIVATIVES AS PI3K INHIBITORS
    Publication number: 20170137421
    Abstract: Disclosed are compounds of formula (I), their tautomeric forms, stereoisomers, and pharmaceutically acceptable salts thereof, wherein R1-R4, and n are as defined in the specification, pharmaceutical compositions including a compound, tautomer, stereoisomer, or salt thereof, and methods of treating or preventing diseases or disorders, for example, cancer, that are amenable to treatment or prevention by inhibiting the PI3K enzyme of a subject.
    Type: Application
    Filed: July 1, 2015
    Publication date: May 18, 2017
    Applicant: Lupin Limited
    Inventors: Manojkumar Ramprasad Shukla, Nirmal Kumar Jana, Sachin Jaysing Mahangare, Prashant Popatrao Vidhate, Dipak Raychand Lagad, Anand Jagannath Tarage, Sanjeev Anant Kulkarni, Venkata P. Palle, Rajender Kumar Kamboj
  • ANTIVIRAL DRUGS FOR TREATMENT OF ARENAVIRUS INFECTION
    Publication number: 20170137422
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.
    Type: Application
    Filed: November 16, 2016
    Publication date: May 18, 2017
    Applicant: Kineta Four, LLC
    Inventors: Dongcheng Dai, James R. Burgeson, Sean M. Amberg, Dennis E. Hruby
  • COMPOUNDS ACTING AT MULTIPLE PROSTAGLANDIN RECEPTORS GIVING A GENERAL ANTI-INFLAMMATORY RESPONSE
    Publication number: 20170137423
    Abstract: The present invention provides a compound, that is a 1-({halo-2-[(2-hydrocarbyl or substituted hydrocarbyl)oxy]phenyl}methyl)-(fused bicyclic nitrogen heteroaryl) carboxylic acid or an ester or sulfonamide thereof. The compound may be represented by the following formula Wherein R1, R2, R3, R4 A, X, W, Z and Y are as defined in the specification. The compounds may be administered to treat DP, FP, EP1, TP and/or EP4 receptor-mediated diseases or conditions.
    Type: Application
    Filed: January 13, 2017
    Publication date: May 18, 2017
    Inventors: William R. Carling, Jose L. Martos, Jussi J. Kangasmetsa, Jenny W. Wang, David F. Woodward
  • SUBSTITUTED TRICYCLIC COMPOUNDS AS FGFR INHIBITORS
    Publication number: 20170137424
    Abstract: The present invention relates to tricyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.
    Type: Application
    Filed: January 18, 2017
    Publication date: May 18, 2017
    Inventors: Liangxing Wu, Colin Zhang, Chunhong He, Yaping Sun, Liang Lu, Ding-Quan Qian, Meizhong Xu, Jincong Zhuo, Wenqing Yao
  • TRICYCLIC COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
    Publication number: 20170137425
    Abstract: The disclosure provides compounds of formula I including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic 7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
    Type: Application
    Filed: June 5, 2015
    Publication date: May 18, 2017
    Inventors: Ivar M. MCDONALD, F. Christopher ZUSI, Richard E. OLSON