Abstract: A method of transforming biomass into lactic acid using modified beta zeolites is disclosed. The one-step preparation process of preparing catalyst in the invention is mild, economical and convenient. The biomass used as precursor is economic and easy to get. Meanwhile, the reaction process doesn't need to be protected by noble gases with high pressure. The catalyst can be reused and the yield of lactic acid is high.
Abstract: Process for preparing (meth)acrylates of the formula (I) CH2?C(R1)—CO—O—R2 ??(I) in which R1 is hydrogen or methyl and R2 is a saturated or unsaturated, linear or branched, aliphatic or cyclic alkyl radical having 6 to 22 carbon atoms, or a (C6-C14)-aryl-(C1-C8)-alkyl radical; by reacting a (meth)acrylate of the formula II CH2?C(R1)—CO—OR3 ??(II) with an alcohol of the formula (III) HO—R2 ??(III) in the presence of an amount of a suitable catalyst which catalyses the reaction and of an amount of a phenolic polymerization inhibitor or a combination of two or more phenolic polymerization inhibitors which is sufficient to inhibit undesired polymerization; the reaction being undertaken with input or introduction into the reaction mixture resulting from the reaction of an amount of oxygen or of an oxygenous gas mixture sufficient to inhibit undesired polymerization, and the process is characterized in that the specific total oxygen input is less than or equal to 1.
Type:
Application
Filed:
October 27, 2015
Publication date:
February 18, 2016
Applicant:
Evonik Roehm GmbH
Inventors:
Joachim KNEBEL, Ralf MERBACH, Guido PROTZMANN, Klaus GOTTMANN, John HIRSH, Gerold SCHMITT, Dieter TESSMER, Wilhelm KARNBROCK, Wolfgang KLESSE, Volker KERSCHER
Abstract: A process for the preparation of vinyl acetate by a heterogeneously catalysed, continuous gas-phase reaction of ethylene, acetic acid and oxygen in a reactor, where process heat liberated during the reaction is removed from the reactor by means of heat exchange with water, generating intrinsic steam, the product mixture leaving the reactor and comprising ethylene, vinyl acetate, acetic acid, water, carbon dioxide and inert gases is separated by distillation using one or more azeotrope columns and/or one or more pure distillation columns, wherein at least one azeotrope column and/or pure distillation column contains packings, and intrinsic steam is used at least partially for introducing energy into the thus-equipped azeotrope columns and/or pure distillation columns.
Type:
Application
Filed:
March 26, 2014
Publication date:
February 18, 2016
Applicant:
Wacker Chemie AG
Inventors:
Mehmet GUENALTAY, Peter SCHULTHEISS, Heribert WESTERMAYER
Abstract: Provided is a process for making (2-nitro)alkyl (meth)acrylate compounds of formula I: wherein n, R, R1, R2, R3, R4, R6, R7, and n are as defined herein, by a transesterification reaction between a nitroalcohol compound and a (meth)acrylate compound in the presence of a transesterification catalyst and a free radical inhibitor.
Type:
Application
Filed:
February 18, 2014
Publication date:
February 18, 2016
Inventors:
Muhunthan SATHIOSATHAM, Robert WILCZYNSKI
Abstract: Methods and compounds for treating neurological and other disorders are provided. Included is the administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for a TrkB receptor molecule, optionally optionally in combination with a TrkA and/or TrkC receptor molecule.
Abstract: The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
Type:
Application
Filed:
April 4, 2014
Publication date:
February 18, 2016
Inventors:
Jonathan Z. Sexton, Jay E. Brenman, David L. Musso
Abstract: The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms.
Abstract: Provided is a styrenated phenol compound represented by Formula 1 in which styrenated phenol and hydroxylamine bind to each other: In Formula 1, n is one of integers of 1 to 3, and R1 and R2 are each hydrogen or one of C1 to C4 alkyl groups. The styrenated phenol compound may maintain curing stimulation property and plasticity, and prevent discoloration when being mixed with a curing agent for an epoxy paint, thereby enhancing exterior quality and storage stability of a product.
Type:
Application
Filed:
September 17, 2014
Publication date:
February 18, 2016
Applicant:
KOREA KUMHO PETROCHEMICAL CO., LTD.
Inventors:
Kee Yoon Roh, Jung Hee Jang, Je Young Park, Jin Eok Kim
Abstract: The present invention relates to compounds which are suitable as synthesis precursors for the production of electronically active materials for use in organic electroluminescence devices.
Type:
Application
Filed:
February 24, 2014
Publication date:
February 18, 2016
Inventors:
PHILIPP STOESSEL, Amir Hossain PARHAM, Anja JATSCH
Abstract: An amidine compound represented by formula (1) wherein R1, R2, R3, R4 and R5 are the same or different and represent a C1 to C5 alkyl group optionally having one or more halogen atoms or the like; R6 and R7 are a hydrogen atom or the like; R8 and R9 are the same or different and represent a C1 to C3 alkyl group optionally having one or more halogen atoms or the like; and R10 and R11 are the same or different and represent a C1 to C6 alkyl group optionally having one or more halogen atoms or the like, has an excellent control effect on plant diseases.
Abstract: Xylylene dicarbamate contains impurities represented by formulas (1) to (4) below at a ratio of less than 100 ppm as a total amount thereof on a mass basis. (In the above-described formulas (1) to (4), R represents a monovalent hydrocarbon group.
Type:
Application
Filed:
March 28, 2014
Publication date:
February 18, 2016
Inventors:
Koji TAKAMATSU, Hideki SONE, Masaaki SASAKI
Abstract: Provided is a compound that allows easy introduction of a pentafluorosulfanylaryl group into a compound of interest. A diaryliodonium salt is represented by the general formula (d) shown below: In this formula, k is 1 or 2, R1 is an alkyl group having 1 or 2 carbon atoms, m is an integer of 0 to 4, R2 is a straight or branched alkyl group having 1 to 4 carbon atoms, n is an integer of 0 to 5, and A? is a counter anion.
Abstract: Since biomass is always accompanied by caustic inorganic materials, we have found that the formation of the anion salt of ?-hydroxysulfonic acid represent the largest “loss” of the ?-hydroxysulfonic acid in the potential reversible acid pretreatment process. By titrating the ?-hydroxysulfonic acid salt with strong mineral acid and then reverting the alfa-hydroxysulfonic acid as its primary components, the acid components can be recovered substantially quantitatively.
Type:
Application
Filed:
August 13, 2015
Publication date:
February 18, 2016
Inventors:
Robert Lawrence BLACKBOURN, Paul Richard WEIDER, Dennis Shane BORISKI
Abstract: It is an object of the present invention to provide a medicament for preventing or treating hyperphosphatemia. Solution: A compound represented by a general formula (I) or a pharmacologically acceptable salt thereof. [In the formula, R1: a methyl group or the like, R2: a hydrogen atom or the like, R3: a hydrogen atom or the like, A: a cyclohexyl ring or the like, X: CH or the like, Y: CH or the like, Z: CH or the like, and n: 2 or the like.
Abstract: The disclosed subject matter provides N-hydroxymethanesulfonamide compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure.
Type:
Application
Filed:
October 29, 2015
Publication date:
February 18, 2016
Inventors:
Vincent Jacob Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
Abstract: The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
Type:
Application
Filed:
October 30, 2015
Publication date:
February 18, 2016
Inventors:
John P. Toscano, Art Sutton, Vincent Jacob Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
Abstract: The present invention relates to a new method for the preparation of (3S,3S?) 4,4?-disulfanediylbis(3-aminobutane 1-sulfonic acid) in five steps from (S)-ethyl 2-(benzyloxycarbonylamino)-4-(neopentyloxysulfonyl)butanoate A.
Type:
Application
Filed:
October 27, 2015
Publication date:
February 18, 2016
Inventors:
Fabrice BALAVOINE, Jonathan MADEC, Jean-Marie SCHNEIDER, Gerard COQUEREL, Nicolas COUVRAT, Yohann CARTIGNY, Marie-Noelle PETIT
Abstract: The present invention relates to a process for preparing a compound of the formulae (Ia) or (Ib), or a mixture thereof, wherein R1 and R2 independently of one another are hydrogen, C1-C10-alkyl, C1-C10-haloalkyl, C3-C10-cycloalkyl, C3-C10-halocycloalkyl, C2-C10-alkenyl, C2-C10-haloalkenyl or together represent an aliphatic chain, or the like; A? is HSO4? or 1/2 SO42?; the process comprising the reaction of a sulfide of formula SR1R2 with hydroxylamineO-sulfonic acid of formula; wherein the reaction is carried out in an aqueous medium in the presence of a base.
Type:
Application
Filed:
March 27, 2014
Publication date:
February 18, 2016
Applicant:
BASF SE
Inventors:
Timo FRASSETTO, Harald JOCKERS, Christopher KORADIN, Thomas ZIERKE, Karsten KOERBER
Abstract: The invention provides a method of assessing the appropriate therapeutic dose of 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid to administer to a patient in need thereof. It is determined whether a patient has a particular metabolizer genotype. If the patient does not have a particular genotype, 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid, or a pharmaceutically acceptable salt thereof is administered at a standard dose. If the patient has the poor metaboliser genotype, either 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid, or a pharmaceutically acceptable salt thereof, is administered at a dose below that of the standard therapeutic dose; or is not dosed at all.
Type:
Application
Filed:
April 19, 2013
Publication date:
February 18, 2016
Applicant:
Novartis AG
Inventors:
Hubert BORELL, Anne GARDIN, Yi JIN, Eric LEGANGNEUX, Mike UFER
Abstract: Certain biphenyic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.
Type:
Application
Filed:
October 28, 2015
Publication date:
February 18, 2016
Inventors:
Nicholas I. Carruthers, Wenying Chai, Jill A. Jablonowski, Chandravadan R. Shah, Brock T. Shireman, Devin M. Swanson, Vi Tran, Victoria Wong
Abstract: Novel forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt designated Form XX, Form XXI, Form XXII, Form XXIII, Form XXIV, Form XXV, Form XXVI, Form XXVII, Form XXVIII, Form XXIX, and Form XXX, characterized by their X-ray powder diffraction, solid-state NMR, and/or Raman spectroscopy are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease.
Type:
Application
Filed:
October 27, 2015
Publication date:
February 18, 2016
Inventors:
Joseph Francis Krzyzaniak, George Michael Laurence, Aeri Park, Kevin Quackenbush, Marie Louise Reynolds, Peter Robert Rose, Timothy Andrew Woods
Abstract: There are provided inter alia compounds of formula (I) wherein R1, R2, R3, R4a and R4b are as defined in the specification and their use in therapy, especially in the treatment of bacterial (e.g. pneumococcal) infections.
Type:
Application
Filed:
October 30, 2015
Publication date:
February 18, 2016
Inventors:
Peter William Andrew, Rana Lonnen, Mafalda Pires Damaso, Fritz-Frieder Frickel, Simon Christopher Hirst, Mark William Davies, Daniel Hamza
Abstract: The present invention provides novel indoline compounds, derivatives of Formula 1 and salts thereof; which can be effectively used for the preparation of a1-adrenoceptor antagonists, Silodosin and its pharmaceutically acceptable salts.
Abstract: In one aspect, the invention relates to PRMT5 inhibitors, including optionally substituted N-alkyl-9H-carbazole analogs, derivatives thereof, and related compounds; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation and benign hematologic diseases using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Type:
Application
Filed:
March 15, 2014
Publication date:
February 18, 2016
Inventors:
Robert A. BAIOCCHI, Chenglong LI, Hongshan LAI, Said SIF
Abstract: Compounds of general formula (I) and compositions comprising compounds of general formula (I) that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.
Type:
Application
Filed:
March 13, 2014
Publication date:
February 18, 2016
Inventors:
Giovanni Cianchetta, Janeta Popovici-Muller, Robert Zahler, Sheldon Cao, Xiaolei Wang, Zhixiong Ye
Abstract: Methods of producing a sulfilimine compound, such as N-cyano-S-methyl-S-[1-(6-trifluoromethyl-3-pyridinyl)ethyl]sulfilimine or other substituted sulfilimine compound. The method includes combining a sulfide compound, cyanamide, a hypochlorite compound, and a base, and oxidizing the sulfide compound to form the sulfilimine compound. The sulfide compound may include a 2-trifluoromethyl-5-(1-substituted)alkyl-thiopyridine compound. The base may include sodium hydroxide. A buffer, such as a phosphate buffer, may, optionally, be used in the reaction.
Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.
Type:
Application
Filed:
March 21, 2014
Publication date:
February 18, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Anthony Ogawa, Scott Edmondson, Mark Erion, Santhosh Neelamkavil, Zhuyan Guo, Rudrajit Mal, Jiafang He, Weiguo Liu, Ellen K. Vande Bunte
Abstract: The subject invention provides a mixture of Crystalline Laquinimod sodium particles, wherein (i) ?90% of the total amount by volume of the laquinimod sodium particles have a size of ?40 ?m or (ii) ?50% of the total amount by volume of the laquinimod sodium particles have a size of ?15 ?m and wherein: a) the mixture has a bulk density of 0.2-0.4 g/mL; b) the mixture has a tapped density of 0.40-0.7 g/mL; c) an amount of heavy metal in the mixture is no more than 20 ppm relative to the amount by weight of laquinimod sodium; d) an amount of MCQ in the mixture is no more than 0.15% relative to the amount of laquinimod sodium as measured by HPLC; e) an amount of MCQCA in the mixture is no more than 0.15% relative to the amount of laquinimod sodium as measured by HPLC; or f) an amount of MCQME in the mixture is no more than 0.12% relative to the amount of laquinimod sodium as measured by HPLC.
Type:
Application
Filed:
March 14, 2014
Publication date:
February 18, 2016
Applicant:
Teva Pharmaceutical Industries Ltd.
Inventors:
Anton FEWNKEL, Avital LAZER, Vladimir IOFFE, Karl-Erik JANSSON, Ulf Tomas FRISTEDT
Abstract: The present invention relates to the use of compounds of general formula wherein R1 is phenyl or pyridinyl, which are optionally substituted by halogen, cyano or lower alkyl substituted by halogen, or is dihydro-pyran-4-yl; R2 is hydrogen or lower alkyl; R3 is —(CHR)n-phenyl, optionally substituted by lower alkoxy or S(O)2-lower alkyl, or is heterocycloalkyl, optionally substituted by ?O and lower alkyl, or is —(CH2)n-five or six membered heteroaryl, optionally substituted by lower alkyl, or is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, —NR—S(O)2-lower alkyl, —(CH2)n-cycloalkyl or —(CH2)n—S(O)2-lower alkyl; or R2 and R3 form together with the N-atom to which they are attached a heterocycloalkyl ring, selected from the group consisting of 1,1-dioxo-thiomorpholinyl, morpholinyl, or pyrrolidinyl, optionally substituted by hydroxyl; R is hydrogen or lower alkyl; n is 0, 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture
Type:
Application
Filed:
October 29, 2015
Publication date:
February 18, 2016
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Simona M. Ceccarelli, Ravi Jagasia, Roland Jakob-Roetne, Rainer E. Martin, Juergen Wichmann
Abstract: Disclosed herein is a compound for use in a composition applied to a blood vessel, wherein the compound softens and/or disrupts the crystalline matrix of calcified plaque. Methods of treatment comprising applying the disclosed composition are also disclosed. Plaque-softening compounds are also disclosed.
Type:
Application
Filed:
January 31, 2014
Publication date:
February 18, 2016
Applicant:
Alumend, LLC
Inventors:
Barbara R. Haberer, Therese J. Downey, Ronald E. Utecht, Jeffrey E. Elbert
Abstract: There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin.
Type:
Application
Filed:
March 17, 2014
Publication date:
February 18, 2016
Inventors:
Kevin Michael SHORT, Son Minh PHAM, David Charles WILLIAMS
Abstract: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Type:
Application
Filed:
October 20, 2015
Publication date:
February 18, 2016
Inventors:
David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
Abstract: The present disclosure relates to a novel active compound having the formula Ia: solid preparations, uses and methods for the treatment or prevention of respiratory diseases comprising said compound as well as process of preparation thereof.
Type:
Application
Filed:
March 12, 2014
Publication date:
February 18, 2016
Applicant:
Universite Laval
Inventors:
Evelyne ISRAEL-ASSAYAG, Pierre LAVALLEE, Yvon CORMIER, Bildad NYAMBURA
Abstract: A method for obtaining solutions that contain 1,2,4-triazole-5-one (OTA) in concentrated sulphuric acid, includes using 3-amino-1,2,4-triazole (ATA) as a precursor of OTA. There is also provided a method for preparing 3-nitro-1,2,4-triazole-5-one (4) (ONTA) from the solutions.
Type:
Application
Filed:
April 4, 2014
Publication date:
February 18, 2016
Inventors:
Grégoire HERVE, Guy JACOB, Guy CAGNON, Jean-Marc BOUCHEZ
Abstract: The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein: R1 is alkyl, Cl, F or Br; R2 is H or F; R3 is selected from H and alkyl; R4 is selected from H and C(O)R6; R5 is H; or R4 and R5 are linked to form a heterocyclic group which is optionally substituted with one or more R10 groups; R6 is selected from R7, OR7 and NR8R9; R7, R8 and R9 are each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocyclyl and aryl, each of which is optionally substituted with one or more R10 groups; each R10 is independently selected from halogen, OH, CN, NO2, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO-alkyl, CO-aryl, NH2, NH-alkyl, N(alkyl)2, CF3, alkyl and alkoxy; X and Z are each independently CR11, and Y is selected from CR11 and N; and R11 is H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.
Abstract: Sonic Hedgehog modulators and methods of use thereof are provided for.
Type:
Application
Filed:
March 23, 2015
Publication date:
February 18, 2016
Inventors:
Sara Buhrlage, Chris Dockendorff, Mike Foley, Han-Je Kim, Andrew Germain, Lawrence MacPherson, Partha Pratim Nag, Stuart Schreiber, Amal Ting, Michel Weiwer, Willmen Youngsaye
Abstract: An object is to find a substance which inhibits IL-2 production. IL-2 production can be inhibited by a compound represented by the following formula (I): wherein R1 to R4 and A are as defined in the present specification, or a pharmaceutically acceptable salt thereof.
Abstract: An object is to provide a novel compound which has a glycogen synthase activation ability, but activates a receptor PPAR to a low degree and is highly safe.
Abstract: The present invention discloses eight new diterpenoids, i.e. Dysongensins A to H, extracted from the leaves and twigs of Dysoxylum hongkongense, wherein AMBROX® which is applicable in the perfume industry is prepared from Dysongensin A via a series of chemical reactions, and the cytotoxicity of Dysongensins A to H against human cancer cell lines and their antiviral and anti-inflammatory activities are determined. Therefore, in the present invention, AMBROX® prepared from Dysongensin A is a new idea for application as an odorous compound in the perfume industry, and the novel diterpenoids can be prepared as a pharmaceutical compositions and/or a drug having antiviral, anti-inflammatory and/or anti-cancer activities.
Abstract: The present invention is in the field of pharmaceuticals and chemical industries. In particular, the present invention relates to new anticancer agents based on miliusane compounds. The present invention also includes its preparation and application method for treating cancer.
Abstract: The present invention provides a phenyl C-glucoside derivative containing a deoxyglucose structure as represented by formula I, preparation method thereof, a pharmaceutical composition comprising the same, and uses thereof in the preparation of medicaments for treating diabetes, wherein substituents R1-R7 are as defined in the specification. The present invention also provides a method for synthesizing the phenyl C-glucoside derivative containing a deoxyglucose structure and an intermediate product. The method has advantages of being simple to manage and of low cost, which is suitable for large-scale industrial production. The present invention further provides a cocrystal of (1S)-1-[4-chloro-3-(4-ethoxybenzyl)phenyl]-1,6-dideoxy-D-glucose and L-proline, and preparation method and uses thereof.
Type:
Application
Filed:
December 5, 2013
Publication date:
February 18, 2016
Applicant:
Tianjin Institute of Pharmaceutical Research
Abstract: The present application provides novel inhibitors of indoleamine 2,3-dioxygenase-1 and/or indoleamine 2,3-dioxygenase-2 and/or tryptophan 2,3-dioxygenase, metabolites thereof, and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. A therapeutically effective amount of one or more of the compounds of formula (I) is useful in treating diseases resulting from dysregulation of the kynurenine pathway. Compounds of formula (I) act by inhibiting the enzymatic activity or expression of indoleamine 2,3-dioxygenase-1 and/or indoleamine 2,3-dioxygenase-2 and/or tryptophan 2,3-dioxygenase.
Type:
Application
Filed:
March 12, 2014
Publication date:
February 18, 2016
Inventors:
Monali Banerjee, Sandip Middya, Ritesh Shrivastava, Sushil Raina, Arjun Surya, Dharmendra B. Yadav, Veejendra K. Yadav, Kamal Kishore Kapoor, Aranapakam Venkatesan, Roger A. Smith, Scott K. Thompson
Abstract: The present invention provides compounds, pharmaceutical compositions, methods of inhibiting ROR? activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such compounds and pharmaceutical compositions.
Type:
Application
Filed:
July 31, 2014
Publication date:
February 18, 2016
Inventors:
Mark Edward Schnute, Göran Mattias Wennerstål, James Robert Blinn, Neelu Kaila, James Richard Kiefer, JR., Scot Richard Mente, Ravi G. Kurumbail, Marvin Jay Meyers, Atli Thorarensen, Li Xing, Christoph Wolfgang Zapf, Edouard Zamaratski, Andrew Christopher Flick, Peter Jones
Abstract: The present invention relates to novel biologically active glutarimide derivatives of general formula I or pharmaceutically acceptable salts thereof, their use as an agent for the treatment of upper respiratory tract diseases, pharmaceutical compositions comprising the glutarimide derivatives of general formula I, methods for preparing the glutarimide derivatives of general formula I by heating a dicarboxylic acid monoamide of general formula II with a dehydrating agent.
Type:
Application
Filed:
April 10, 2014
Publication date:
February 18, 2016
Inventors:
Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova
Abstract: The present invention is directed to compounds of Formula I: wherein X is CR1 or N; Y is CR2 or N; Z is NH or O; R1 is alkoxy, triazolyl, oxazolyl, isoxazolyl, oxadiazolyl, or pyrimidinyl; R2 is H, alkyl, or halo; R3 is H, alkyl, alkoxy, halo, triazolyl, oxazolyl, or pyrimidinyl; R4 is alkyl; R5 is pyridyl; benzoxazolyl; pyrimidinyl; pyridazinyl; quinoxalinyl; pyrazinyl; or quinazolinyl; wherein the pyridyl; benzoxazolyl; pyrimidinyl; pyridazinyl; quinoxalinyl; pyrazinyl; or quinazolinyl is optionally substituted with one or two substituents independently selected from the group consisting of alkyl, halo, or phenyl; and R6 is H or alkyl. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods using the compounds of the invention are also within the scope of the invention.
Type:
Application
Filed:
March 12, 2014
Publication date:
February 18, 2016
Inventors:
Heather R. COATE, Curt A. DVORAK, Cathy PREVILLE, Brock T. SHIREMAN
Abstract: The present invention relates to compounds of Formula (I), and solvates, hydrates, and pharmaceutically acceptable salts thereof, wherein ring A, R1, R5 and R6 are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
Type:
Application
Filed:
March 13, 2014
Publication date:
February 18, 2016
Inventors:
Wenying Chai, Charlotte Deckhut, Curt A. Dvorak, Wendy Eccles, James P. Edwards, Steven D. Goldberg, Paul J. Krawczuk, Alec D. Lebsack, Jing Liu, Virginia M. Tanis, Kyle T. Tarantino
Abstract: Compounds represented by the formulas wherein each symbol is as defined in the specification, and a prodrug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.
Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
Type:
Application
Filed:
October 30, 2015
Publication date:
February 18, 2016
Inventors:
Carl R. ILLIG, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
Abstract: The present disclosure relates generally to crystalline forms of anhydrous D-glucitol, 1-deoxy-1-(methylamino)-, 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxyazetidin-1- yl)-4-oxo-3-quinolinecarboyxlate, compositions comprising the same, and methods of making the same. Delafloxacin is an fluoroquinolone antibiotic with the chemical structure and the chemical name 1-deoxy-1-(methylamino)-, 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxyazetidin-1-yl)-4-oxo-3-quinolinecarboyxlate. Studies have indicated the existence of three anhydrous polymorphs of delafloxacin, as well as a trihydrate and methanol and ethanol solvates.
Abstract: Compounds of formula (I), which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals.
Type:
Application
Filed:
March 20, 2014
Publication date:
February 18, 2016
Inventors:
Marion HITCHCOCK, Anne MENGEL, Christoph-Stephan HILGER, Lars BÄRFACKER, Hans BRIEM, Gerhard SIEMEISTER, Amaury Ernesto FERNANDEZ-MONTALVAN, Jens SCHRÖDER, Simon HOLTON, Cornelia PREUßE, Ursula MÖNNING