Abstract: In a process for the synthesis of a nitrile by endothermic catalyzed reaction of ammonia with a hydrocarbon using heating obtained by passing an alternating current through a metallic coil, the endothermic reaction between ammonia and the hydrocarbon takes place in a reactor with direct inductive heating in the reaction zone. The heating is extremely fast, which makes the reaction practically instantaneous.
Type:
Application
Filed:
April 24, 2017
Publication date:
May 16, 2019
Applicant:
HALDOR TOPSØE A/S
Inventors:
Poul Erik HØJLUND NIELSEN, Burcin TEMEL MCKENNA, John Bøgild HANSEN, Rasmus Munksgård NIELSEN
Abstract: Provided are compounds of formula (I), or a stereoisomer, mixture of stereoisomers, deuterated analog, tautomer, solvate or pharmaceutically acceptable salt thereof, compositions, method of making and uses thereof.
Abstract: Provided are a novel water-soluble diacetylene monomer, a composition for photolithography including the novel water-soluble diacetylene monomer and a conductive polymer, and a method of forming micropatterns using the composition. The water-soluble diacetylene monomer may not aggregate even when mixed with a water-soluble conductive polymer. Accordingly, a uniform composition for photolithography can be prepared by mixing a water-soluble conductive polymer with the diacetylene monomer, and micropatterns can be formed using the composition. More particularly, when the composition is formed into a thin film and then is irradiated with light, only light-irradiated portions of the diacetylene monomer are selectively crosslinked due to photopolymerization, thereby resulting in insoluble negative-type micropatterns.
Type:
Application
Filed:
April 26, 2017
Publication date:
May 16, 2019
Applicant:
Industry-University Cooperation Foundation Hanyang University
Inventors:
Jongman KIM, Chanwoo LEE, Taegeun KIM, Kyungchan UH
Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release HNO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.
Type:
Application
Filed:
January 9, 2019
Publication date:
May 16, 2019
Inventors:
John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
Abstract: A copper protective agent is provided. The copper protective agent is represented by a general formula (GI): HS—R (GI); and R is a linear or branched alkyl group having 1 to 20 carbon atoms.
Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
Type:
Application
Filed:
April 13, 2018
Publication date:
May 16, 2019
Inventors:
Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsza H. Tsang
Abstract: The invention relates to new compounds with low cytotoxicity for blocking ubiquitination-proteasome system in diseases. Accordingly, these compounds can be used in treatment of treating disorders including, but not limited to, cancers, neurodegenerative diseases, inflammatory disorders and autoimmune disorders and metabolic disorders.
Abstract: The invention is directed to substituted pyrrolidine derivatives. Specifically, the invention is directed to compounds according to Formula III: wherein A, B, L1, L2, L3, R1, R2, R3, R4, R5, R6, R9, R10, R30, Y1, Y2, z2, z4, z5, and z6 are as defined herein, and salts thereof.
Type:
Application
Filed:
June 7, 2017
Publication date:
May 16, 2019
Inventors:
Jeffrey Michael AXTEN, Mui CHEUNG, Anthony William DEAN, Michael P. DEMARTINO, Hilary Schenck EIDAM, Biswajit KALITA, Raghava Reddy KETHIRI, Rajendra KRISTAM
Abstract: The present invention relates to novel methods for preparing cis-alkoxy-substituted spirocyclic 1-H-pyrrolidine-2,4-dione derivatives and also to novel intermediates and starting compounds, which are passed through or used in the method according to the invention.
Type:
Application
Filed:
April 26, 2017
Publication date:
May 16, 2019
Inventors:
Taraneh FARIDA, Martin LITTMANN, Rafael WARSITZ, Michael ESSER, Albert SCHNATTERER
Abstract: This invention provides novel indole, indazole, benzimidazole, benzotriazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
Type:
Application
Filed:
September 5, 2018
Publication date:
May 16, 2019
Applicant:
University of Tennessee Research Foundation
Inventors:
Ramesh NARAYANAN, Duane D. MILLER, Thamarai PONNUSAMY, Dong-Jin HWANG, Yali HE
Abstract: Deoxynojirimycin and deoxygalactonojirimycin derivatives according to the present invention are N-alkylated D-galacto, D-gluco- or L-ido-deoxynojirimycin with a linear methyloxypentyl group bearing various sidegroups and a non-fused bicyclic aromatic group (“X”) on the methyloxy-carbon. Formula (I), Formula (Ia). These compounds display an increased inhibitory potency towards GCS, and/or an increased inhibitory potency towards GBA2, and/or a decreased inhibitory potency towards GBA1, relative to known deoxynojirimycin derivatives of the same (D-gluco, L-ido or D-galacto) configuration.
Type:
Application
Filed:
January 7, 2019
Publication date:
May 16, 2019
Inventors:
Herman Steven OVERKLEEFT, Stan VAN BOECKEL, Johannes Maria Franciscus Gerardus AERTS, Amar GHISAIDOOBE, Richard VAN DEN BERG
Abstract: Compounds are provided to modulate the C5a receptor. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Type:
Application
Filed:
October 29, 2018
Publication date:
May 16, 2019
Inventors:
Pingchen FAN, Rebecca M. LUI, Venkat Reddy MALI, Rajinder SINGH, Yibin ZENG, Penglie ZHANG
Abstract: There is provided a process for preparing a compound represented by the following general formula (1) or a salt thereof, which comprises exchanging one or more of an amino proton in a compound represented by the following general formula (2) or a salt thereof to deuterium, and after the exchanging, converting a deuterium-exchanged compound of the compound represented by the general formula (2) or a salt thereof into the compound represented by the general formula (1) or a salt thereof: wherein, in the general formula (1), one, or two or more of hydrogen atom may be substituted with their isotope; and in the general formula (2), each of R1 is independently hydrogen atom, tert-butyloxycarbonyl group or benzyloxycarbonyl group, and R2 is independently tert-butyl group, benzyl group, methyl group or ethyl group.
Abstract: The present invention relates to a process for preparing 4-(4-[({[4-chloro-3-(trifluoromethyl)-phenyl]amino}carbonyl)amino]-3-fluorophenoxy}-N-methylpyridine-2-carboxamide, its salts and monohydrate.
Type:
Application
Filed:
January 9, 2019
Publication date:
May 16, 2019
Applicant:
BAYER HEALTHCARE LLC
Inventors:
Juergen STIEHL, Werner HEILMANN, Michael LÖGERS, Joachim REHSE, Michael GOTTFRIED, Saskia WICHMANN
Abstract: A process for preparing the polymorph I of the anhydrate of 2-Chloro-N-(4?-chlorobiphenyl-2-yl)-nicotinamide (boscalid) of the formula I: is provided. The process comprises the steps of: a) dissolving the polymorph II of the anhydrate of boscalid in a first solvent in an amount and at conditions allowing dissolution of the polymorph II of the anhydrate of boscalid; b) combining the resulting solution with water; c) isolating the solid from the solvent mixture; and d) drying the solid to obtain the polymorph I of the anhydrate of boscalid.
Abstract: The present invention provides compounds of Formula (I): P-Ma??(I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
Type:
Application
Filed:
January 11, 2019
Publication date:
May 16, 2019
Inventors:
James R. Corte, Andrew K. Dilger, William R. Ewing, Donald J.P. Pinto, Wu Yang
Abstract: The present application relates to certain substituted imidazole and triazole compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating pain, musculoskeletal inflammation, neuroinflammatory disorders, airway inflammation, itch, dermatitis, colitis and related conditions. The compounds are of Formula (I) where X is N or CH, Z and Y are N or C (but both not N) and R1-R3 are as defined herein.
Type:
Application
Filed:
May 11, 2017
Publication date:
May 16, 2019
Applicant:
Heptares Therapeutics Limited
Inventors:
John Graham Cumming, Frank Xinhe Wu, Karl Henrik Edman, Hongming Chen, Dean Gordon Brown, Roland Werner Burli, Shawn Donald Johnstone, Giles Albert Brown, Benjamin Gerald Tehan, Barry John Teobald, Miles Stuart Congreve
Abstract: 2-substituted benzimidazoles and methods of preparing the same are disclosed. The compositions may include a compound or salt thereof, an acid, and a polar aprotic solvent. The compositions may be used to inhibit corrosion of a metal surface in contact with an aqueous system, and provide enhanced protection against corrosion of metals in the aqueous system.
Type:
Application
Filed:
November 9, 2018
Publication date:
May 16, 2019
Applicant:
Ecolab USA Inc.
Inventors:
Pradeep Cheruku, Suresh R. Sriram, James Joseph Michels
Abstract: The purpose of the present invention is to provide novel compounds having ACC2 selective inhibitory activity. In addition, the present invention provides a pharmaceutical composition comprising the compound. A compound of Formula: or its pharmaceutically acceptable salt, wherein, R1 is substituted or unsubstituted fused aromatic heterocyclyl represented by Formula: wherein, ring B is 5-membered ring, ring C is 6-membered ring; ring A is substituted or unsubstituted non-aromatic carbocycle or the like; -L1- is —O—(CR6R7)m- or the like; -L2- is —O—(CR6R7)n- or the like; each R6 is independently hydrogen or the like; each R7 is independently hydrogen or the like; each m is independently an integer of 0, 1, 2 or 3; each n is independently an integer of 1, 2 or 3; R2 is substituted or unsubstituted alkyl; R3 is hydrogen or substituted or unsubstituted alkyl; R4 is substituted or unsubstituted alkylcarbonyl or the like.
Abstract: The present invention provides a novel crystalline form of Selexipag, Selexipag Form APO-I, which is a methanol solvate of Selexipag, compositions thereof, and the use of this crystalline form in the treatment of pulmonary arterial hypertension.
Type:
Application
Filed:
November 9, 2018
Publication date:
May 16, 2019
Inventors:
Fabio E. S. Souza, Bahareh Khalili, Katherine A. Rantanen, Annyt Bhattacharyya, Jenny L. Gerster, Allan W. Rey
Abstract: The present invention relates to a method for suppressing the immune system in a subject in need thereof, and a method for treating an inflammatory or immune disorder in a subject in need thereof.
Abstract: The present invention provides a 2,4,6-trisubstituted s-triazine compound represented by general formula (I) or pharmaceutically acceptable salts, prodrugs or solvates thereof, a preparation method therefor, and use of these compounds in preparing drugs for preventing or treating diseases associated with protein kinase and vimentin dysregulation, and cell vacuolization, and in particular, drugs for treating or preventing cancer growth and metastasis, tissue fibrosis and atherosclerosis.
Type:
Application
Filed:
May 11, 2017
Publication date:
May 16, 2019
Inventors:
QIZHENG YAO, JIANPING WU, RUIHUAN CHEN, LEI ZHANG, SHINING YAO, LIAN MO, QINGQING ZHANG
Abstract: The present disclosure is directed to oxazoline mono- and hetero-pseudodimer compounds, such as compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof: These compounds are useful for treating pain. The present disclosure also relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of Formula (I) or (II) or a pharmaceutically acceptable salt or solvate thereof.
Abstract: The present invention relates to the use of iminosydnone compounds in processes for the preparation of conjugates of two compounds of interest. The invention further relates to the use of said iminosydnone compounds in a process for releasing a compound of interest. The invention finally relates to novel iminosydnone compounds.
Abstract: The present invention relates to methods of modulating an immune response mediated by a PD-1 signaling pathway and of treating a cancer or an infectious disease. A subject is administered a compound(s) or a pharmaceutically acceptable salt or pharmaceutically acceptable composition thereof of formula (I) In the ring Q is S or O. R1 substituents are an optionally substituted side chain of the amino acid Ser or Thr and R3 substituents are a side chain of the amino acids Asn, Asp, Gln, or Glu. R2 is hydrogen or —CO-Aaa and Aaa is Thr or Ser with a free, amidated or esterified C-terminus. R4 and R5 are independently hydrogen or absent. R6 is hydrogen, alkyl or acyl.
Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicament.
Abstract: The present disclosure provides a reaction of a chlorine-containing compound using a flow reactor which is less restricted by a solvent to be used. In the present disclosure, an organic compound is produced by supplying a reaction substrate having at least one functional group which can react with chlorine and is selected from the group consisting of hydroxy group, a thiol group, an amino group, a carboxyl group, a thiocarboxyl group, and an acid amide group, and a chlorine-containing compound to a flow reactor together with a trialkyl amine having 9 to 40 carbon atoms and an organic solvent, and allowing the reaction substrate and the chlorine-containing compound to react with each other.
Abstract: A group of polyfunctional oxetane-based compounds having a structure as represented by general formula (I) or a product obtained by a reaction between a compound of general formula (I) and epichlorohydrin, an ester compound, or an isocyanate compound. When these polyfunctional oxetane-based compounds are used as cation polymerizable monomers in combination with an epoxy compound, the curing speed is high, and the cured product has highly excellent hardness, flexibility, adherence, and heat resistance.
Abstract: The invention relates to anhydrides, solvates and ethanol hetero-solvates and hydrates of dimethoxy docetaxel or (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propionate of 4-acetoxy-2?-benzoyloxy-5?,20-epoxy-1-hydroxy-7?, 10?-dimethoxy-9-oxo-tax-11-ene-13?-yle, and to the preparation thereof.
Abstract: RhlR modulators including agonist and antagonists which are useful for modulating QS phenotypes in Gram-negative bacteria. Certain compounds of general formula A-W-HG having various carbocyclic ad heterocyclic head groups (HG) and various tail groups (A), where —W— is —CO—NH—, —SO2—NH—, —CO—NH—CH2—, or —SO2—NH—CH2— are RhlR agonists or antagonists. The compounds are useful in methods of modulating quorum sensing in Gram-negative bacteria, particularly in Pseudomonas. Compositions including certain RhlR modulators are useful for decreasing the virulence of Gram-negative bacteria. Pharmaceutical compositions comprising certain RhlR modulators are useful for treatment of infections of Gram-negative bacteria.
Type:
Application
Filed:
April 30, 2017
Publication date:
May 16, 2019
Inventors:
Helen BLACKWELL, Michelle E. BOURSIER, Joseph D. MOORE
Abstract: The present disclosure provides methods to produce 5-(halomethyl)furfural, including 5-(chloromethyl)furfural, by acid-catalyzed conversion of C6 saccharides, including isomers thereof, polymers thereof, and certain derivatives thereof. The methods make use of acids with lower concentrations, and allows for conversion of sugars into 5-(halomethyl)furfural at higher temperatures and faster reaction or residence times.
Type:
Application
Filed:
June 7, 2018
Publication date:
May 16, 2019
Applicant:
MICROMIDAS, INC.
Inventors:
Alex B. WOOD, Makoto N. MASUNO, Ryan L. SMITH, John BISSELL, Dimitri A. HIRSCH-WEIL, Robert Joseph ARAIZA, Daniel R. HENTON, James H. PLONKA
Abstract: Implementations of the disclosed subject matter provide a process for converting biomass into furfural. The process may include subjecting a pentosan-containing biomass material to an acid catalyzed digestion process in a digestion vessel to produce a digested product stream comprising C5-carbohydrates and solids comprising cellulose. The digested product stream may be separated into a liquid product stream and a solid product stream comprising lignin and cellulose. The solids product stream may be contacted with water and an organic solvent, thereby converting at least part of the lignin to a phenolic solvent. The C5-carbohydrate in the liquid product stream may be subjected to a dehydration reaction in the presence of an acid catalyst and a biphasic mixture comprising an aqueous phase and a water-immiscible organic phase, wherein the water-immiscible organic phase includes at least a portion of the phenolic solvent, to produce furfural or a furan derivative.
Type:
Application
Filed:
May 2, 2017
Publication date:
May 16, 2019
Inventors:
Juben Nemchand CHHEDA, Jean Paul Andre Marie Joseph Ghislain LANGE
Abstract: The invention provides a furan-modified compound or oligomer. The compound has a structure represented by Formula I: When formula I represents a compound, x is an integer of 1˜5; A including a group formed of ketone, amido, imide, imido, phenyl ether or enol ether group; G is a direct bond, —O—, —N—, —Ar—NH—(CH2)b—, —Ar—O—(CH2)b—, —Ar—O—(CH2)a—NH—(CH2)b—, —(CH2)a—NH—(CH2)b—, —(CH2)a—O—(CH2)b— or —(CH2)a—CH(OH)—(CH2)b—NH—; Ar is substituted or unsubstituted arylene group; a is an integer of 1 to 5; and b is an integer of 0 to 5.
Type:
Application
Filed:
November 2, 2018
Publication date:
May 16, 2019
Applicant:
INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTE
Abstract: The present invention provides a process for the preparation of (1S)-1,5-anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-D-glucitol which is represented by the following structural formula-1 and its glycerol solvate.
Abstract: A selenium-enriched tea polyphenol selenide, has such a structure as: wherein R1 is alkali metal ion and selenium coordination complex, and R2?H, or A method for preparing the selenium-enriched tea polyphenol selenide, comprises: A) reacting tea polyphenol with at least one inorganic metallic alkali, to obtain tea polyphenol hydroxy acid salt; and B) reacting the tea polyphenol hydroxy acid salt with SeO2, to obtain the selenium-enriched tea polyphenol selenide.
Abstract: The present invention relates to compounds of formula (III) or to compounds of formula (IV) wherein R1, R2, R3 and R4 are as defined in the claims, and their use in therapeutic treatments of 5-lipoxygenase related diseases such as chronic airway inflammatory or dermatological disorders.
Type:
Application
Filed:
August 26, 2016
Publication date:
May 16, 2019
Inventors:
Pascal RICHOMME, Jean-Jacques HELESBEUX, David GUILET, Denis SERAPHIN, Hermann STUPPNER, Birgit WALTENBERGER, Daniela SCHUSTER, Veronika Sophie TEMML, Andreas KOEBERLE, Oliver WERZ
Abstract: The present invention relates to methods for purifying one or two cannabinoid compounds using simulated moving bed chromatography, wherein the cannabinoid compound(s) is/are obtained in the extract and/or the raffmate with the total amount of isomeric impurities being below detection level. In particular, the present invention relates to methods for the purification of cannabidiol, trans-(?)-delta-9-tetrahydrocannabinol, cannabidivarin, trans-(?)-delta-9-tetrahydrocannabivarin and cannabigerol which have been obtained by enantiopure synthesis.
Type:
Application
Filed:
May 13, 2016
Publication date:
May 16, 2019
Inventors:
Harry ERFURT, Maria WEBER, Hans-Jürgen NIEMEYER, Marcus Rudolf GÖTZ, Matthias WINKLER
Abstract: The present invention regards new adipate-type compounds suitable as an intermediate in organic chemistry, a platform chemical for the production of other chemicals, and as a monomer and co-monomer useful for the preparation of polymers and copolymers. The invention also regards the process of preparing the new adipate-type compounds from bio-based raw materials such as sugars.
Abstract: There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
Type:
Application
Filed:
May 4, 2017
Publication date:
May 16, 2019
Inventors:
David K. WILLIAMS, Weifang SHAN, James Aaron BALOG
Abstract: There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
Type:
Application
Filed:
May 4, 2017
Publication date:
May 16, 2019
Inventors:
David K. WILLIAMS, Weifanq SHAN, Liping ZHANG, Emily Charlotte CHERNEY, James Aaron BALOG
Abstract: The present invention provides a polymorph of a benzamide compound and a preparation method and applications thereof. The shown benzamide compound is 3-Bromo-N-[2,4-dichloro-6-[(methylamino)carbonyl]phenyl]-1-(3,5-dichloro-2-pyridinyl)-1H-pyrazole-5-carboxamide. The application of the polymorph of the compound in the preparation of the formulation exhibits excellent effect. The advantages of the polymorph A in aspects such as chemical stability, filterability, solubility, hygroscopicity, melting point, solid density and flowability can have a significant impact on the developments of the production method and a formulation and on the quality and efficacy of a plant treating agent.
Abstract: The present invention provides salts of (E)-N,N-dimethyl-4-((2-((5-((Z)-4,4,4-trifluoro-1-(3-fluoro-1H-indazol-5-yl)-2-phenylbut-1-en-1-yl)pyridin-2-yl)oxy)ethyl)amino)but-2-enamide represented by the formula I and acids, and crystals thereof, possessing a potential to be used as drug substance in pharmaceuticals.
Abstract: The present invention relates to a novel method of preparing a 2-substituted indazole of formula (I) to novel intermediate compounds, and to the use of intermediate compounds for the preparation of said 2-substituted indazole.
Type:
Application
Filed:
April 25, 2017
Publication date:
May 16, 2019
Applicant:
Bayer Pharma Aktiengesellschaft
Inventors:
Tobias THALER, Johannes PLATZEK, Nicolas GUIMOND
Abstract: Novel benzimidazole enantiomeric derivatives, their process of preparation and their therapeutical uses as dual H1 and H4 receptor ligands are disclosed.
Type:
Application
Filed:
November 15, 2018
Publication date:
May 16, 2019
Inventors:
Isabelle BERREBI-BERTRAND, Xavier BILLOT, Thierry CALMELS, Marc CAPET, Stéphane KRIEF, Olivier LABEEUW, Jeanne-Marie LECOMTE, Nicolas LEVOIN, Xavier LIGNEAU, Philippe ROBERT, Jean-Charles SCHWARTZ
Abstract: The present invention relates to novel 5-(hydroxyalkyl)-1-heteroaryl-1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
Type:
Application
Filed:
May 2, 2017
Publication date:
May 16, 2019
Inventors:
Marie-Pierre COLLIN-KRÖPELIN, Peter KOLKHOF, Thomas NEUBAUER, Chantal FÜRSTNER, Elisabeth POOK, Matthias Beat WITTWER, Carsten SCHMECK, Pierre WASNAIRE, Hanna TINEL, Heiko SCHIRMER
Abstract: The present invention relates to novel 5-(carboxamide)-1-pyridinyl-1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
Type:
Application
Filed:
May 2, 2017
Publication date:
May 16, 2019
Inventors:
Marie-Pierre COLLIN-KRÖPELIN, Peter KOLKHOF, Thomas NEUBAUER, Chantal FÜRSTNER, Elisabeth POOK, Matthias Beat WITTWER, Klemens LUSTIG, Anja BUCHMÜLLER, Hanna TINEL, Karoline DRÖBNER, Thomas MONDRITZKI, Heiko SCHIRMER, Axel KRETSCHMER, Carsten SCHMECK, Pierre WASNAIRE, Hana CERNECKA
Abstract: The present invention provides novel inhibitors of MIF tautomerase activity. In certain embodiments, the compounds of the invention are useful in treating or preventing inflammatory and/or auto-immune diseases. In other embodiments, the compounds of the invention are useful in reversing, ameliorating, and/or preventing tumor growth. In yet other embodiments, the compounds of the invention are useful in reversing, ameliorating, and/or preventing angiogenesis.
Abstract: Disclosed herein is the compound (R)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl)acetamido)pyridazin-3-yl)-2-fluorobutyl)-N-methyl-1H-1,2,3-triazole-4-carboxamide, and salt forms and polymorphs thereof demonstrating improved exposure after oral dosing. Methods of inhibition GLS1 activity in a human or animal subject are also provided.
Type:
Application
Filed:
January 7, 2019
Publication date:
May 16, 2019
Inventors:
Philip JONES, Michael J. SOTH, Jason P. BURKE, Kang LE, Gang LIU