Patents Issued in December 17, 2019
  • Method for preparing acetal carbonyl compound
    Patent number: 10508073
    Abstract: The present application provides a method for preparing acetal carbonyl compound used as an intermediate for producing ethylene glycol, which comprises a step in which a raw material acetal and a raw gas carbon monoxide go through a reactor loaded with a catalyst containing an acidic microporous silicoaluminophosphate molecular sieve, for carrying out a carbonylation reaction. In the method of the present invention, the conversion rate of the raw material acetal is high, and the selectivity of acetal carbonylation is high, and the catalyst life is long, and no additional solvent is needed in the reaction process, and the reaction condition is relatively mild, and the process is continuous, showing the potential for industrial application. Moreover, the product of acetal carbonyl compound can be used for producing ethylene glycol by hydrogenation followed by hydrolysis.
    Type: Grant
    Filed: December 8, 2015
    Date of Patent: December 17, 2019
    Assignee: Dalian Institute of Chemical Physics, Chinese Academy of Sciences
    Inventors: Youming Ni, Wenliang Zhu, Yong Liu, Hongchao Liu, Zhongmin Liu, Miao Yang, Peng Tian
  • Method for purifying (meth)acrylic esters
    Patent number: 10508074
    Abstract: The subject of the invention is a process for recovering/purifying a C1-C4 (meth)acrylic ester from a crude reaction mixture comprising said ester, the process being carried out using a purification system comprising a divided wall column and a decanter, resulting in a simplification of the process and in a high productivity of the ester produced corresponding to the standards in terms of purity. The invention also relates to a process for producing C1-C4 (meth)acrylic ester comprising this recovery/purification process.
    Type: Grant
    Filed: January 3, 2017
    Date of Patent: December 17, 2019
    Assignee: Arkema France
    Inventors: Serge Tretjak, Nathalie Hess, Rose Aguiar, Pierre-Emmanuel Conoir, Christophe Oses
  • Process for preparation of trientine dihydrochloride
    Patent number: 10508075
    Abstract: The present invention provides a process for preparation of trientine dihydrochloride (1) comprising reaction of protected triethylene tetramine with hydrochloric acid in an aqueous system to yield the dihydrochloride salt wherein the formation of inorganic impurities and undesired salts is controlled significantly.
    Type: Grant
    Filed: September 13, 2016
    Date of Patent: December 17, 2019
    Inventors: Mukund Gurjar, Shashikant Joshi, Devising Pardeshi, Mangesh Kamble, Lakindrasing Girase, Samit Mehta
  • Method for resolution of citalopram intermediate 5-cyano diol
    Patent number: 10508076
    Abstract: Provided is a method for resolution of formula 4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxylbutyl]-3-hydroxy-methyl benzonitrile as an enantiomer thereof, comprising the following steps: a salt of (S)-4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxylbutyl]-3-hydroxymethyl benzonitrile with a resolving agent D-(+)di-p-toluoyl tartaric acid was crystallized in a resolving solvent; the method is characterized in that the resolving solvent is an ether solvent. Also provided is a new crystal form of the resolved intermediate.
    Type: Grant
    Filed: February 22, 2019
    Date of Patent: December 17, 2019
    Assignee: Zhejiang huahai Pharmaceuticals Co., Ltd.
    Inventors: Zunjun Liang, Siqi Hu, Caihua Peng, Wenfeng Huang, Qifeng Lu, Guoliang Tu
  • Alpha-cinnamide compounds and compositions as HDAC8 inhibitors
    Patent number: 10508077
    Abstract: The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.
    Type: Grant
    Filed: April 18, 2019
    Date of Patent: December 17, 2019
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Kenneth W. Bair, Nicholas Barczak, Bingsong Han, David R. Lancia, Jr., Cuixian Liu, Matthew W. Martin, Pui Yee Ng, Aleksandra Rudnitskaya, Jennifer R. Thomason, Mary-Margaret Zablocki, Xiaozhang Zheng
  • Compound, photopolymerization initiator comprising said compound, and photosensitive resin composition containing said photopolymerization initiator
    Patent number: 10508078
    Abstract: The purpose of the present invention is to provide: a novel compound which can generate a base and radical upon the irradiation with an active energy ray; a photopolymerization initiator which comprises the novel compound; and a photosensitive resin composition which contains the photopolymerization initiator, has high sensitivity and excellent storage stability, and can be formed into a cured article that does not have a metal-corrosive property. The novel compound is represented by formula (1): (wherein R1 to R6 independently represent a hydrogen atom, a hydroxy group, an alkoxy group, an organic group other than the aforementioned substituents, or the like; X represents a residue having a structure such that n hydrogen atoms are removed from a saturated hydrocarbon containing a ring structure; and n represents an integer of 1 to 6).
    Type: Grant
    Filed: December 7, 2016
    Date of Patent: December 17, 2019
    Assignees: TOKYO UNIVERSITY OF SCIENCE FOUNDATION, NIPPON KAYAKU KABUSHIKI KAISHA
    Inventors: Kiwamu Terada, Kazuyoshi Yamamoto, Koji Arimitsu
  • Method for purification of a CO2 stream
    Patent number: 10508079
    Abstract: A process for removing hydrogen and methanol from a CO2 stream which contains hydrogen and methanol as contaminants, wherein hydrogen and methanol are removed by contacting the CO2 stream with a catalyst which oxidizes hydrogen to water and methanol to carbon dioxide, obtaining a purified CO2 stream.
    Type: Grant
    Filed: September 8, 2016
    Date of Patent: December 17, 2019
    Assignee: Casale SA
    Inventor: Federico Maffietti
  • Process for the preparation of isosulfan blue
    Patent number: 10508080
    Abstract: Isosulfan blue and processes for the preparation thereof are provided. A process is also provided for preparation of the intermediate, 2-chlorobenzaldehyde-5-sulfonic acid, sodium salt of formula (2), used in the preparation thereof and a procedure for the isolation of benzaldehyde-2, 5-disulfonic acid, di-sodium salt of the formula (3). Also provided is a process for the preparation of an isoleuco acid of formula (4), which upon oxidation gives rise to isosulfan blue of pharmaceutical grade which can be used for preparation of pharmaceutical formulations. The isolation and purification procedures provided in the process provide substantially pure isosulfan blue with HPLC purity 99.5% or greater.
    Type: Grant
    Filed: February 1, 2019
    Date of Patent: December 17, 2019
    Assignee: Apicore US LLC
    Inventors: Ravishanker Kovi, Satyam Nampalli, Peter Xavier Tharial
  • Intermediates and methods for synthesizing calicheamicin derivatives
    Patent number: 10508081
    Abstract: The present invention relates to intermediates of Formula I and to methods of synthesizing and purifying calicheamicin derivatives.
    Type: Grant
    Filed: January 12, 2018
    Date of Patent: December 17, 2019
    Assignee: Pfizer Inc.
    Inventors: Robert Wayne Dugger, Leo Joseph Letendre, Vimalkumar Babubhai Patel, Amarnauth Shastrie Prashad, Chunchun Zhang
  • Substituted 6,11-dihydro-5H-benzo[b]carbazoles as inhibitors of ALK and SRPK
    Patent number: 10508082
    Abstract: The application relates to a compound of Formula (I): which modulates the activity of ALK or SRPK, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which ALK or SRPK plays a role.
    Type: Grant
    Filed: September 23, 2016
    Date of Patent: December 17, 2019
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: John Hatcher, Nathanael S. Gray, Hwan Geun Choi, Pasi Janne, Tinghu Zhang
  • Substituted piperidine compound and use thereof
    Patent number: 10508083
    Abstract: Provided is a substituted piperidine compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as a prophylactic or therapeutic agent for narcolepsy.
    Type: Grant
    Filed: February 1, 2017
    Date of Patent: December 17, 2019
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tatsuhiko Fujimoto, Kentaro Rikimaru, Koichiro Fukuda, Hiromichi Sugimoto, Takahiro Matsumoto
  • Method for producing 4,4,7-trifluoro-1,2,3,4-tetrahydro-5H-1-benzazepine compound and intermediate used in the method
    Patent number: 10508084
    Abstract: The present invention provides a method for producing a 4,4,7-trifluoro-1,2,3,4-tetrahydro-5H-1-benzazepine compound which has an superior agonistic activity to an arginine vasopressin V2 receptor and is useful as an active ingredient for a pharmaceutical composition for preventing and/or treating urinary frequency, urinary incontinence, enuresis, central diabetes insipidus, nocturia, nocturnal enuresis, or the like; and useful intermediates for use in the methods. The production method of the present invention is suitable for the industrial production of a medicament, because of a smaller number of steps, a higher yield, and a lower cost, as compared with the methods in the related art.
    Type: Grant
    Filed: March 23, 2018
    Date of Patent: December 17, 2019
    Assignee: TACURION
    Inventors: Souichirou Kawazoe, Takahiro Akiba, Kiichi Sato, Akio Miyafuji, Kazuyoshi Obitsu, Junji Itoh, Shun Hirasawa, Hiroyuki Koshio
  • Compounds and methods for IDO and TDO modulation, and indications therefor
    Patent number: 10508085
    Abstract: Disclosed are compounds of Formula I(a): or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein R4, R5, R6, R7, G1, G2 and Ring A are as described in any of the embodiments described in this disclosure; compositions thereof; and uses thereof.
    Type: Grant
    Filed: September 22, 2017
    Date of Patent: December 17, 2019
    Assignee: Plexxikon Inc.
    Inventors: Jiazhong Zhang, Hannah Powers, Aaron Albers, Phuongly Pham, Guoxian Wu, John Buell, Wayne Spevak, Zuojun Guo, Jack Walleshauser, Ying Zhang
  • PARG inhibitory compounds
    Patent number: 10508086
    Abstract: The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity: wherein R1a, R1b, R1c, R1d, R1e, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.
    Type: Grant
    Filed: December 17, 2015
    Date of Patent: December 17, 2019
    Assignee: Cancer Research Technology Limited
    Inventors: Alison E. McGonagle, Allan M. Jordan, Bohdan Waszkowycz, Colin P. Hutton, Ian D. Waddell, James R. Hitchin, Kate M. Smith, Niall M. Hamilton
  • Crystalline forms of trisodium supramolecular complex comprising valsartan and AHU-377 and methods thereof
    Patent number: 10508087
    Abstract: Novel crystalline forms of trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl) propionate-(S)-3?-methyl-2?-(pentanoyl{2?-(tetrazol-5-ylate)biphenyl-4?-ylmethyl}amino)butyrate] hydrate, methods for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of angiotensin receptor 1 (AT1) blockage and neprilysin (NEP) inhibition, such as heart failure, are disclosed.
    Type: Grant
    Filed: March 18, 2018
    Date of Patent: December 17, 2019
    Assignees: CRYSTAL PHARMATECH CO., LTD., SUZHOU PENGXU PHARMATECH CO., LTD.
    Inventors: Minhua Chen, Yanfeng Zhang, Chaohui Yang, Xiaoyu Zhang
  • Methods using HDAC11 inhibitors
    Patent number: 10508088
    Abstract: The present invention provides methods and uses of inhibitors of histone deacetylase 11 (HDAC11) in the treatment of diseases and/or disorders, such as, for example, cell proliferative diseases.
    Type: Grant
    Filed: November 28, 2018
    Date of Patent: December 17, 2019
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Jennifer Lee, Nicholas Barczak, Jaime A. Escobedo, Chiara Conti, Bingsong Han, David R. Lancia, Jr., Cuixian Liu, Matthew W. Martin, Pui Yee Ng, Aleksandra Rudnitskaya, Jennifer R. Thomason, Xiaozhang Zheng
  • Use of N-(1,3,4-Oxadiazol-2-yl)arylcarboxamides or their salts for controlling unwanted plants in areas of transgenic crop plants being tolerant to HPPD inhibitor herbicides
    Patent number: 10508089
    Abstract: Use of N-(1,3,4-Oxadiazol-2-yl)arylcarboxamides of formula (I) or salts thereof with R, X, A, and Z having the meaning as defined in the description, for controlling unwanted plants in areas of transgenic crop plants being tolerant to HPPD inhibitor herbicides by containing one or more chimeric gene(s) comprising (I) a DNA sequence encoding hydroxyphenylpyruvate dioxygenase (HPPD) derived from a member of a group of organisms consisting of (a) Avena, (b) Pseudomonas, (c) Synechococcoideae, (d) Blepharismidae, (e) Pseudomonas, (f) Picrophilaceae, (g) Kordia, or (II) one or more mutated DNA sequences of HPPD encoding genes of the before defined organisms, preferably from Pseudomonas, or (III) one or more DNA sequences encoding mutated maize (Zea mays) or soybean (Glycine max) HPPD each being mutated as described in WO 2012/021785.
    Type: Grant
    Filed: March 10, 2015
    Date of Patent: December 17, 2019
    Assignee: BASF SE
    Inventors: Fabien Poree, Christian Waldraff, Bernd Laber, Arnim Koehn, Elmar Gatzweiler
  • Sulfonamides as GPR40- and GPR120-agonists
    Patent number: 10508090
    Abstract: The invention relates to compounds acting as agonists of G-protein coupled receptor 120 (GPR120) and/or 40 (GPR40), and having formula (I): Said compounds are useful in the treatment of diseases or disorders modulated by GPR120 and/or GPR40 such as diabetes (particularly type 2 diabetes), impaired oral glucose tolerance, insulin resistance, obesity, obesity related disorders, metabolic syndrome, dyslipidemia, elevated LDL, elevated triglycerides, obesity induced inflammation, osteoporosis and obesity related cardiovascular disorders.
    Type: Grant
    Filed: August 7, 2017
    Date of Patent: December 17, 2019
    Assignee: DOMPÉ FARMACEUTICI S.P.A.
    Inventors: Maria De Pizzol, Anna Sirico, Mara Zippoli, Gianluca Bianchini, Andrea Beccari, Andrea Aramini, Chiara Rossana Maria Liberati
  • Piperazine and piperidine derivatives, their synthesis and use thereof in inhibiting VDAC oligomerization, apoptosis and mitochondria dysfunction
    Patent number: 10508091
    Abstract: Provided herein piperazine and piperidine derivatives, their synthesis and use thereof in inhibiting VDAC oligomerization, apoptosis and mitochondria dysfunction. Also provided methods of treatment of diseases associated with said processes, e.g. Alzheimer's disease.
    Type: Grant
    Filed: September 13, 2016
    Date of Patent: December 17, 2019
    Assignee: THE NATIONAL INSTITUTE FOR BIOTECHNOLOGY IN THE NEGEV LTD.
    Inventors: Varda Shoshan-Barmatz, Arie Lev Gruzman
  • Synthesis of novel analogs of diptoindonesin G, compounds formed thereby, and pharmaceutical compositions containing them
    Patent number: 10508092
    Abstract: Disclosed are unnatural analogs of Diptoindonesin G, methods to make the analogs, pharmaceutical compositions containing the analogs, and methods of using the analogs to inhibit neoplastic cell growth.
    Type: Grant
    Filed: August 29, 2017
    Date of Patent: December 17, 2019
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Wei Xu, Weiping Tang, Jitian Liu, Jill Kolesar
  • Compounds, compositions and methods for treating or preventing a symptom associated with gout or hyperuricemia
    Patent number: 10508093
    Abstract: The inventive subject matter provides compounds, compositions and methods for lowering serum acid (sUA) for the treatment of gout, and having reduced liver toxicity, associated with CYP2C9 metabolic pathway.
    Type: Grant
    Filed: February 5, 2019
    Date of Patent: December 17, 2019
    Assignee: ARTHROSI THERAPEUTICS, INC.
    Inventors: Shunqi Yan, Li-Tain Yeh, Robert Orr
  • Methods for producing ferric maltol compositions from ferrous hydroxides
    Patent number: 10508094
    Abstract: Methods for producing ferric maltol compositions, such as ferric trimaltol, from ferrous hydroxides, are described, as well as ferric maltol compositions produced by these methods and their uses.
    Type: Grant
    Filed: March 31, 2017
    Date of Patent: December 17, 2019
    Assignee: SHIELD TX (UK) LIMITED
    Inventors: Jonathan Joseph Powell, Nuno Jorge Rodrigues Faria
  • Method for producing antibiotic from pleosporaceae ulocladium
    Patent number: 10508095
    Abstract: Fermentation processes that use fungi of the genus Ulocladium for producing novel compounds that include an 8- or 9-membered cyclic structure, wherein an (E)-1,4-dioxo-but-2-ene moiety is embedded in the cyclic structure. The compounds may be used as medicaments, in particular as medicaments for treating and preventing microbial infections, such as infections by multidrug resistant and/or Gram-positive bacteria.
    Type: Grant
    Filed: February 1, 2018
    Date of Patent: December 17, 2019
    Assignee: Koninklijke Nederlandse Akademie van Wetenschappen
    Inventors: Jeroen den Hertog, Gisela Johanna van der Velden, Jelmer Hoeksma
  • Nicotine salts, co-crystals, and salt co-crystal complexes
    Patent number: 10508096
    Abstract: The invention provides certain nicotine salt co-crystals and provides novel polymorphic forms of certain nicotine salts. In particular, certain nicotine salt-co-crystals are described, including nicotine and two different coformers. The invention further provides methods of preparation and characterization of nicotine salts, co-crystals, and salt co-crystals. In addition, tobacco products, including smoking articles, smokeless tobacco products, and electronic smoking articles comprising nicotine salts, co-crystals, and/or salt co-crystals are also provided.
    Type: Grant
    Filed: September 5, 2017
    Date of Patent: December 17, 2019
    Assignee: R.J. Reynolds Tobacco Company
    Inventors: Gary M. Dull, Susana del Rio Gancedo, Judit Galcera Julia
  • Antibacterial compounds and uses thereof
    Patent number: 10508097
    Abstract: The present invention relates to compounds of formula (I) including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of tuberculosis.
    Type: Grant
    Filed: March 7, 2017
    Date of Patent: December 17, 2019
    Assignees: The Global Alliance for TB Drug Development, Inc., Janssen Pharmaceutica NV
    Inventors: Anna Marie Upton, Christopher Blair Cooper, Koenraad Jozef Lodewijk Marcel Andries, Jerome Emile Georges Guillemont, Walter Marcel Mathilde Van den Broeck, Brian Desmond Palmer, Zhenkun Ma
  • Quinazolinones and azaquinazolinones as ubiquitin-specific protease 7 inhibitors
    Patent number: 10508098
    Abstract: The present disclosure relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R4, R4?, X1, Y1, Y2, Y3, Y4, n, and m are described herein.
    Type: Grant
    Filed: November 2, 2018
    Date of Patent: December 17, 2019
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell, David R. Lancia, Jr.
  • Isoquinolin-3-yl carboxamides and preparation and use thereof
    Patent number: 10508099
    Abstract: Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an isoquinoline compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, inflammation, auto-immune diseases and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.
    Type: Grant
    Filed: April 27, 2017
    Date of Patent: December 17, 2019
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, Gopi Kumar Mittapalli, Brian Joseph Hofilena, Joseph Timothy Marakovits, Chandramouli Chiruta, Chi Ching Mak, Jianguo Cao
  • Apoptosis signal-regulating kinase inhibitor
    Patent number: 10508100
    Abstract: The present invention relates to a compound of formula (I): The compound has apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis.
    Type: Grant
    Filed: January 11, 2019
    Date of Patent: December 17, 2019
    Assignee: Gilead Sciences, Inc.
    Inventor: Gregory Notte
  • Protein kinase C inhibitors and methods of their use
    Patent number: 10508101
    Abstract: PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.
    Type: Grant
    Filed: March 15, 2019
    Date of Patent: December 17, 2019
    Assignee: NOVARTIS AG
    Inventors: Michael Joseph Luzzio, Julien Papillon, Michael Scott Visser
  • Inhibitors of cellular necrosis and related methods
    Patent number: 10508102
    Abstract: A compound having the following structure (I): or a pharmaceutically acceptable salt, prodrug, stereoisomer or tautomer thereof, is provided. Related compounds, methods for preparation of the same and uses of the compounds for treatment of various indications, including treatment of necrotic cell diseases and/or inflammation, are also provided.
    Type: Grant
    Filed: February 15, 2018
    Date of Patent: December 17, 2019
    Assignees: President and Fellows of Harvard College, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences
    Inventors: Junying Yuan, Yijun Zhou, Shan Qian, Dawei Ma
  • Benzimidazole-linked indole compound acting as novel divalent IAP antagonist
    Patent number: 10508103
    Abstract: The present invention discloses a benzimidazole-linked indole compound acting as novel divalent IAP antagonist, specifically disclosing the compound shown in formulas (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 27, 2017
    Date of Patent: December 17, 2019
    Assignee: MEDSHINE DISCOVERY INC.
    Inventors: Fei Sun, Charles Z. Ding, Zhe Cai, Wenyuan Qian, Guoping Hu, Jian Li, Shuhui Chen
  • 6-hydroxy-5-(phenyl/heteroarylsulfonyl)pyrimidin-4(1H)-one as APJ agonists
    Patent number: 10508104
    Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.
    Type: Grant
    Filed: June 14, 2017
    Date of Patent: December 17, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: George O. Tora, Heather Finlay, Wen Jiang, Wei Meng, Xiaojun Zhang
  • Indazole compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
    Patent number: 10508105
    Abstract: Indazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease states associated with glutamate dysfunction.
    Type: Grant
    Filed: August 16, 2018
    Date of Patent: December 17, 2019
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Andrew S. Felts, Colleen M. Niswender, Rory A. Capstick, Paul K. Spearing, Sean R. Bollinger
  • Bicyclic BET bromodomain inhibitors and uses thereof
    Patent number: 10508106
    Abstract: The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.
    Type: Grant
    Filed: November 23, 2016
    Date of Patent: December 17, 2019
    Assignees: ConverGene LLC, The United States of America, As Represented by the Secretary, Department of Health and Human Services
    Inventors: Jeffrey William Strovel, Makoto Yoshioka, David J. Maloney, Shyh Ming Yang, Ajit Jadhav, Daniel Jason Urban
  • Morpholine derivative
    Patent number: 10508107
    Abstract: The present invention relates to a compound of formula and to a pharmaceutically suitable acid addition salt thereof with a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1, for the treatment of certain CNS diseases.
    Type: Grant
    Filed: September 13, 2018
    Date of Patent: December 17, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Marius Hoener, Roger Norcross, Philippe Pflieger
  • Tricyclic compounds as inhibitors of mutant IDH enzymes
    Patent number: 10508108
    Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes (I); wherein A is —C(R1)? or —N?; and X is selected from the group consisting of: (II-i), and (II-ii). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
    Type: Grant
    Filed: December 1, 2015
    Date of Patent: December 17, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christian Fischer, Stephane L. Bogen, Matthew L. Childers, Francesc Xavier Fradera Llinas, J. Michael Ellis, Sara Esposite, Dawn M. Hoffman, Chunhui Huang, Solomon D. Kattar, Alexander J. Kim, John W. Lampe, Michelle R. Machacek, Daniel R. McMasters, Dann L. Parker, Jr., Michael H. Reutershan, Nunzio Sciammetta, Pengcheng P. Shao, David L. Sloman, Wanying Sun, Feroze Ujjainwalla, Zhicai Wu, Yang Yu, Craig R. Gibeau
  • Bicyclic compound and use thereof for inhibiting SUV39H2
    Patent number: 10508109
    Abstract: The present invention directs to a compound represented by formula (I).
    Type: Grant
    Filed: September 12, 2016
    Date of Patent: December 17, 2019
    Assignee: ONCOTHERAPY SCIENCE, INC.
    Inventors: Yo Matsuo, Shoji Hisada, Yusuke Nakamura, Anjan Chakrabarti, Manish Rawat, Sanjay Rai, Arvapalli Venkata Satyanarayana, Zhiyong Duan, Arindam Talukdar, Srinivas Ravula, Helene Decornez
  • Process for preparing 1-(4-methanesulfonyl-2-trifluoromethyl-benzyl)-2-methyl-1H-pyrrolo [2,3-B]pyridin-3-yl-acetic acid
    Patent number: 10508110
    Abstract: This invention relates to novel processes for synthesizing [1-(4-Methanesulfonyl-2-trifluoromethyl-benzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl]-acetic acid and to intermediates that are used in such processes.
    Type: Grant
    Filed: September 27, 2016
    Date of Patent: December 17, 2019
    Assignee: NOVARTIS AG
    Inventors: Philipp Lustenberger, Christian Mathes, Zhongbo Fei, Bernard Riss, Thierry Schlama
  • 6-[5-amino-6-(2-ethoxyethoxy)-imidazo[4,5-B]pyridin-3-yl]-nicotinonitrile derivatives and their use as IRAK inhibitors
    Patent number: 10508111
    Abstract: The present invention discloses compounds according to Formula I: wherein R1, R2, and Cy are as defined herein. The present invention relates to compounds inhibiting IRAK family kinases, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory diseases, autoimmune diseases and/or proliferative diseases by administering the compound of the invention.
    Type: Grant
    Filed: October 14, 2016
    Date of Patent: December 17, 2019
    Assignee: GALAPAGOS NV
    Inventors: Reginald Christophe Xavier Brys, Raphaël Jean Joël Geney, Agnès Marie Joncour, Julien Georges Pierre-Olivier Doyon, Frédéric Gilbert Labéguère, Jean-Michel Lefrançois, Oscar Mammoliti, Benoît Antoine Schmitt, Steven Emiel Van Der Plas, Christel Jeanne Marie Menet
  • Intermediate compounds for preparation of praziquantel and processes for preparing the intermediate compounds
    Patent number: 10508112
    Abstract: Intermediate compounds for the preparation of Praziquantel are provided. In particular, the intermediate compounds provided include a compound of formula (IV) and a compound of formula (V). Also provided are processes for preparing the intermediate compounds. Additionally, the raw materials are inexpensive and easy to obtain, the key intermediates are easy to prepare, and the total reaction yield and purity of the obtained target compound Praziquantel is high, so that industrialized mass production of Praziquantel using the intermediate compounds is easy to achieve.
    Type: Grant
    Filed: June 21, 2018
    Date of Patent: December 17, 2019
    Assignees: Zhejiang Hisun Pharmaceutical Co., Ltd., Shanghai Institute of Pharmaceutical Industry
    Inventors: Fuli Zhang, Zhezhou Yang, Rusheng Bao, Weiwei Xu, Hua Bai
  • Inhibitors of tyrosine kinase 2 mediated signaling
    Patent number: 10508113
    Abstract: Disclosed herein are compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4a, R4b, X1, X2, X3, X4, X5, nad n are as defined herein, pharmaeceutical compositions 2C X5, and n are as defined herein, pharmaceutical compositions comprising same, and methods of preparation and use.
    Type: Grant
    Filed: March 12, 2019
    Date of Patent: December 17, 2019
    Assignee: AbbVie Inc.
    Inventors: Maria A. Argiriadi, Eric C. Breinlinger, Ellen Yulin Tsai Chien, Marlon D. Cowart, Kristine E. Frank, Michael M. Friedman, David J. Hardee, J. Martin Herold, Huaqing Liu, Wei Qiu, Marc J. Scanio, Michael R. Schrimpf, Thomas R. Vargo, Stacy A. Van Epps, Matthew P. Webster, Andrew J. Little, Matthew H. Katcher
  • Spiro-isoquinoline-4,4?-piperidine compounds having multimodal activity against pain
    Patent number: 10508114
    Abstract: The present invention relates to compounds having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opiod receptor and more particularly to spiro-isoquinoline-4,4?-piperidine compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
    Type: Grant
    Filed: May 4, 2016
    Date of Patent: December 17, 2019
    Assignee: ESTEVE PHARMACEUTICALS, S.A.
    Inventor: Carmen Almansa-Rosales
  • Toll-like receptor 7 (TLR7) agonists having heteroatom-linked aromatic moieties, conjugates thereof, and methods and uses therefor
    Patent number: 10508115
    Abstract: Compounds having a structure according to formula (I) or (II) where R1, R2, R3, R4, Ar and X1 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.
    Type: Grant
    Filed: August 14, 2018
    Date of Patent: December 17, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Liqi He, Sanjeev Gangwar, Yam B. Poudel, Prasanna Sivaprakasam
  • Click nucleic acid polymers and methods of use
    Patent number: 10508116
    Abstract: Disclosed herein are Click Nucleic Acid Polymers (CNA-polymers) that comprise repeating dimer, trimer and tetramer units. The disclosed polymers can be used for antisense applications, for example, in treatment of “trinucleotide repeat disorders, i.e., Huntington's Disease and the like.
    Type: Grant
    Filed: October 6, 2017
    Date of Patent: December 17, 2019
    Assignee: THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY
    Inventors: Christopher N. Bowman, Weixian Xi, Sankha Pattanayak
  • Solid forms of a toll-like receptor modulator
    Patent number: 10508117
    Abstract: The present invention provides crystalline forms, solvates and hydrates of 4-amino-2-butoxy-8-(3-(pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one, and methods of making.
    Type: Grant
    Filed: December 21, 2018
    Date of Patent: December 17, 2019
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Patricia Andres, Krista Marie Diaz, Valeriya N. Smolenskaya
  • Pyrimidopyrrole compounds, method for preparing the same, pharmaceutical compositions comprising the same and uses thereof
    Patent number: 10508118
    Abstract: The present invention relates to a compound of formula I, a stereoisomer, a prodrug, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, and a process for preparing the same, a pharmaceutical composition comprising the same, and use of the compound in the preparation of medicine preventing and treating tumors, wherein the substituents are as defined in the specification.
    Type: Grant
    Filed: April 25, 2016
    Date of Patent: December 17, 2019
    Assignee: Xiamen University
    Inventors: Xianming Deng, Zhongji Zhuang, Zhou Deng, Xiaoxing Huang, Yan Liu, Ting Zhang, Wei Huang, Qingyan Xu, Zhiyu Hu
  • Pyrazole derivatives useful as 5-lipdxygenase activating protein (FLAP) inhibitors
    Patent number: 10508119
    Abstract: The present application relates to novel compounds of formula (I) to their utility in treating and/or preventing clinical conditions including cardiovascular diseases (CVD), to methods for their therapeutic use, to pharmaceutical compositions containing them and to processes for preparing such compounds.
    Type: Grant
    Filed: November 20, 2018
    Date of Patent: December 17, 2019
    Assignee: ASTRAZENECA AB
    Inventors: Johan Olof Broddefalk, Hans Fredrik Emtenâs, Kenneth Lars Granberg, Malin Anita Lemurell, Daniel Tor Pettersen, Alleyn Thomas Plowright, Lars Johan Andreas Ulander
  • TYK2 inhibitors and uses thereof
    Patent number: 10508120
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
    Type: Grant
    Filed: April 12, 2019
    Date of Patent: December 17, 2019
    Assignee: Nimbus Lakshimi, Inc.
    Inventors: Craig E. Masse, Jeremy Robert Greenwood, Sayan Mondal, Scott D. Cowen, Thomas H. McLean
  • Cortistatin analogues and syntheses and uses thereof
    Patent number: 10508121
    Abstract: Provided herein are compounds of Formula (A), (B), (C), (D) and (E), pharmaceutically acceptable salts, quaternary amine salts, and N-oxides thereof, and pharmaceutical compositions thereof. Compounds of Formula (A), (B), (C), (D), and (E) are contemplated useful as therapeutics for treating a wide variety of conditions, e.g., including but not limited to, conditions associated with angiogenesis and with CDK8 and/or CDK19 kinase activity. Further provided are methods of inhibiting CDK8 and/or CDK19 kinase activity, methods of modulating the ?-catenin pathway, methods of modulating STAT 1 activity, methods of modulating the TGF?/BMP pathway, methods of modulating HIF-1-alpha activity in a cell, and methods of increasing BIM expression to induce apoptosis, using a compound of Formula (A), (B), (C), (D), or (E). Further provided are CDK8 and CDK19 point mutants and methods of use thereof.
    Type: Grant
    Filed: March 5, 2019
    Date of Patent: December 17, 2019
    Assignee: President and Fellows of Harvard College
    Inventors: Matthew D. Shair, Juergen Ramharter, Henry Efrem Pelish, Brian Bor-Jen Liau, Jae Young Ahn
  • Heterocyclic hydroxamic acids as protein deacetylase inhibitors and dual protein deacetylase-protein kinase inhibitors and methods of use thereof
    Patent number: 10508122
    Abstract: The present invention relates to novel hydroxamic acids which are specific histone deacetylase (HDAC) inhibitors and/or TTK/Mps1 kinase inhibitors, including pharmaceutically acceptable salts thereof, which are useful for modulating HDAC and/or TTK/Mps1 kinase activity, pharmaceutical compositions comprising these compounds, and processes for their preparation.
    Type: Grant
    Filed: July 19, 2017
    Date of Patent: December 17, 2019
    Assignee: The Regents of the University of Colorado, A Body Corporate
    Inventors: Xuedong Liu, Gan Zhang, Daniel Chuen-Fong Chan, Anthony D. Piscopio