Abstract: A method of producing ?-caprolactam from 3-oxoadipic acid includes: step 1 of mixing at least one selected from the group consisting of 3-oxoadipic acid and salts thereof with a catalyst and a solvent in the presence of hydrogen to produce 3-hydroxyadipic acid; and step 2 of reacting the 3-hydroxyadipic acid which is a product of step 1, a salt or carboxylic acid derivative thereof, or a mixture of these with hydrogen and ammonia.
Abstract: Disclosed is the use of fluorinated cyclic dinucleotides and pharmaceutically acceptable salts thereof as an adjuvant for the preparation of an oral vaccine. Further disclosed is the use of fluorinated cyclic dinucleotides and pharmaceutically acceptable salts thereof for enhancing the immune response to an orally administered vaccine.
Type:
Grant
Filed:
September 18, 2018
Date of Patent:
July 23, 2019
Assignees:
Brock University, National Research Council of Canada
Inventors:
Hongbin Yan, Wangxue Chen, Rhonda Kuo Lee
Abstract: The present invention relates to a new route of synthesis to obtain pharmaceutically acceptable Vismodegib. In addition, besides the synthesis also suitable pharmaceutical compositions and the use of the compound for the treatment of basal-cell carcinomas are disclosed.
Type:
Grant
Filed:
March 26, 2018
Date of Patent:
July 9, 2019
Assignee:
AZAD PHARMACEUTICAL INGREDIENTS AG
Inventors:
Christian Manfred Frech, Pasquale Gabriele Grieco, Christine Aebersold, Patrick Müller, Jan-Erik Ingenhoff, Miriam Oberholzer, Viktorya Rstakyan, Roman Gerber Aeschbacher
Abstract: Described are cancer therapies and anti-cancer compounds. In particular, disclosed are inhibitors of ACK1 tyrosine kinase and their use in the treatment of cancer. Methods of screening for new ACK1 tyrosine kinase inhibitors are also disclosed. In specific example, compound having Formula I are disclosed.
Type:
Grant
Filed:
August 2, 2016
Date of Patent:
July 2, 2019
Assignee:
H. Lee Moffitt Cancer Center and Research Institute, Inc.
Inventors:
Nupam P. Mahajan, Kiran N. Mahajan, Nicholas J. Lawrence, Harshani R. Lawrence
Abstract: Disclosed are a compound, a stereisomer and a tautomer thereof, a pharmaceutically acceptable salt thereof, and a solvate or a prodrug thereof, which can be used for preventing or treating a ROR? mediated disease. The compound has the structural formula (I).
Type:
Grant
Filed:
January 22, 2016
Date of Patent:
June 18, 2019
Assignee:
Beijing Hanmi Pharmaceutical Co., Ltd.
Inventors:
Hai Xue, Tao Zhao, Mi Young Cha, Maengsup Kim
Abstract: The present invention relates to the use of a compound of formula (I), a pharmaceutically acceptable salt thereof, a solvate thereof, or a pharmaceutical composition containing the same in reducing uric acid level, preventing or reducing inflammations, and preventing or treating uratic or gouty diseases. In particular, the present invention relates to the use of a compound of formula (I), a pharmaceutically acceptable salt thereof, a solvate thereof, or a pharmaceutical composition containing the same in the manufacture of a medicament for the treatment or prevention of hyperuricemia, gout, gouty inflammations, pain and uric acid nephropathy. R1 represents hydrogen, C1-4 alkyl or the like. R2 represents C1-10 alkyl or the like. R3 represents halogen or the like.
Type:
Grant
Filed:
January 28, 2016
Date of Patent:
June 18, 2019
Assignee:
SHANTON PHARMA CO., LTD
Inventors:
Qian Zhang, Zhenhua Huang, Jinrong Liu, Shuangshuang Chi
Abstract: This document provides compounds, compositions, and methods for treating cancers including renal cancer (e.g., renal cell carcinoma) as well as ovarian, breast, prostate, colon, pancreatic, bladder, liver, lung, and thyroid cancers and melanoma. For example, compounds, compositions, and methods for using one or more inhibitors of SCD1 to treat renal cell carcinoma (e.g., clear cell renal cell carcinoma (ccRCC)), thyroid cancer, or liver cancer; or to increase the efficacy of treatment for the same.
Type:
Grant
Filed:
August 7, 2015
Date of Patent:
May 28, 2019
Assignee:
Mayo Foundation for Medical Education and Research
Inventors:
John A. Copland, III, Han W. Tun, Thomas R. Caulfield, Christina Von Roemeling, Laura Ann Marlow
Abstract: Compounds of Formula (A?), (B?), (C?), (D?), (E?), (A?), (B?), (C?), (D?), (E?), (G1), and (G2) are useful as therapeutics for treating a wide variety of conditions in a host such as a human, e.g., including but not limited to, conditions associated with angiogenesis and/or which are mediated by CDK8 and/or CDK19 kinase activity. Also provided are methods of modulating the ?-catenin pathway, methods of modulating STAT1 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 an effective amount of a compound of Formula (A?), (B?), (C?), (D?), (E?), (A?), (B?), (C?), (D?), (E?), (G1), or (G2).
Type:
Grant
Filed:
December 22, 2017
Date of Patent:
April 30, 2019
Assignee:
President and Fellows of Harvard College
Abstract: The present invention relates to a liquid pharmaceutical composition suitable for parenteral administration comprising: a) pemetrexed diacid; b) at least one organic amine; c) at least one antioxidant; d) 10-200 mg/ml of propylene glycol; and e) one or more parenteral solvents, wherein the preparation thereof is conducted in an atmosphere of inert gas and wherein the organic amine(s) is present in an amount sufficient to reach a pH of the composition in the range from 8.3 to 9.1.
Abstract: The present invention relates to novel substituted ethylenediaminetetraacetic acid bisamide derivatives, their complexes with Mn(II) ion and the use thereof as contrast agents for Magnetic Resonance Imaging (MRI) analysis.
Type:
Grant
Filed:
February 25, 2016
Date of Patent:
April 23, 2019
Assignee:
Bracco Imaging S.P.A.
Inventors:
Zsolt Baranyai, Zoltán Garda, Simona Ghiani, Ferenc Krisztián Kálmán, László Krusper, Alessandro Maiocchi, Gyula Tircsó, Imre Toth
Abstract: The present invention provides compounds and compositions that inhibit Factor XIa or kallikrein and methods of using these compounds and composition.
Type:
Grant
Filed:
April 11, 2018
Date of Patent:
April 16, 2019
Assignee:
eXIthera Pharmaceuticals, Inc.
Inventors:
Robert A. Chrusciel, Robert C. Gadwood, Neil J. Hayward, Michael J. Melnick, Manuel A. Navia, Toni J. Poel, Frans L. Stassen, Catherine A. Stewart
Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein R1, R2, Rc, and Rd have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of bromodomains. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various bromodomain-mediated disorders.
Type:
Grant
Filed:
May 10, 2017
Date of Patent:
April 16, 2019
Assignees:
GENENTECH, INC., CONSTELLATION PHARMACEUTICALS, INC.
Inventors:
Brian K. Albrecht, Steven F. Bellon, Daniel J. Burdick, Alexandre Cote, Terry Crawford, Les A. Dakin, Vickie Hsiao-Wei Tsui, Michael Charles Hewitt, Yves LeBlanc, Steven R. Magnuson, Christopher G. Nasveschuk, F. Anthony Romero, Yong Tang, Alexander M. Taylor, Shumei Wang
Abstract: The present invention provides taxanes compounds with a formula (I) or formula (II) structure, a method for preparing the compounds, as well as the use of the compositions containing the compounds, pharmaceutically acceptable salts and solvates thereof as active ingredients in manufacturing oral antitumor medicaments, In formula (I), R1 is —COR6, —COOR6 or —CONR7aR7b; R2 is a C1-C6 alkyl, a C1-C6 alkenyl, a substituted hydrocarbon group, a heterocyclic group, an aromatic group or a substituted aromatic group; R3 is —OR6, —OCOOR6, —OCOSR6 or —OCONR7aR7b; R4 is —OR6, —OCOOR6, —OCOSR6, —OCONR7aR7b or H; wherein, R6 is a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group; R7a and R7b are respectively hydrogen, a hydrocarbon group, a substituted hydrocarbon group or a heterocyclic group.
Abstract: Embodiments of small molecule inhibitors of hypoxia inducible factor 1 (HIF-1) and pharmaceutical compositions thereof are disclosed. The disclosed compounds suppress HIF-1 activity by inhibiting the interaction between the HIF-1 ? subunit and transcriptional co-activator protein p300. Embodiments of methods for making and using the small molecule inhibitors are also disclosed.
Type:
Grant
Filed:
April 6, 2016
Date of Patent:
April 2, 2019
Assignee:
The United States of America, as represented by the Secretary, Department of Health and Human Services
Inventors:
Kirk R. Gustafson, Martin J. Schnermann, Susanna T. S. Chan, Paresma R. Patel, William D. Figg, James B. McMahon
Abstract: According to the present invention, differently from well-known production methods, with the use of a different starting material, Ullmann condensation which may decrease the yield with an increase of a production scale can be avoided and thus 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one can be provided safely and stably with high reaction yield.
Abstract: The invention relates to ligands and complexes of metal ions with the ligands useful in various applications, including therapeutic and diagnostic applications.
Type:
Grant
Filed:
March 7, 2018
Date of Patent:
March 26, 2019
Assignee:
LUMIPHORE, INC.
Inventors:
David Tatum, Jide Xu, Darren Magda, Nathaniel Butlin
Abstract: The present invention relates to bis(sulfonamide) compounds and pharmaceutically acceptable salts thereof. The present invention also relates to pharmaceutical compositions comprising these compounds and to their use as a medicament for the treatment and/or prevention of a disease, disorder or condition in which modulation of microsomal prostaglandin E synthase-1 activity is beneficial, such as pain, inflammation and cancer.
Type:
Grant
Filed:
November 24, 2015
Date of Patent:
March 12, 2019
Assignee:
Arcturum Real Estate AB
Inventors:
Peter Söderman, Mats A. Svensson, Annika Kers, Liselott Öhberg, Katharina Högdin, Andreas Hettman, Jesper Hallberg, Maria Ek, Johan Bylund, Johan Nord
Abstract: The present invention relates to a compound of formula (I), provided that this compound is not caffeine, for use in the treatment of myotonic dystrophy type 1 and type 2. The present invention also relates to compositions comprising the compound of formula (I). The present invention further relates to new compounds which are dimers of compounds of formula (I).
Type:
Grant
Filed:
November 13, 2015
Date of Patent:
March 12, 2019
Assignees:
Universitat de Valencia, Institut Quimic de Sarria Cets Fundacio Privada, Institut Univ. de Ciencia I Tecnologia, S.A.
Inventors:
Ruben Artero Allepuz, Josep Castells Boliart, José Ignacio Borrell Bilbao, Beatriz Llamusi Troísi, Ariadna Bargiela Schönbrunn, Piotr Konieczny, Marta Pascual Gilabert, Jordi Teixidó Closa, Roger Estrada Tejedor, Alejandro López González
Abstract: The present invention provides, inter alia, compounds capable of inhibiting NF-?B. Pharmaceutical compositions containing and methods of using the compounds are also provided herein.
Abstract: The present invention relates to pharmaceutical compounds of the Formula (I), or a pharmaceutically acceptable salt or composition thereof, and methods of their use for the treatment of pain, respiratory conditions, as well as inhibiting the Transient Receptor Potential A1 ion channel (TRPA1).