Abstract: In some embodiments, provided herein are processes for preparing a compound of Formula C or a salt thereof, as disclosed herein. In some embodiments, provided herein is a compound of Formula I or a pharmaceutically acceptable salt, solvate or hydrate thereof. In some embodiments, provided herein is a solid form of the compound, such as a crystalline form of the compound crystalline Form I.
Type:
Grant
Filed:
October 26, 2017
Date of Patent:
August 17, 2021
Assignees:
Array BioPharma, Inc, Loxo Oncology, Inc.
Inventors:
Qian Zhao, Stacey Spencer, Yutong Jiang, Julia Haas, Charles Todd Eary
Abstract: Described herein are crystalline forms of (R)-3-(2-(trans-4-(2-aminoethylamino)cyclohexyl)acetamido)-2-hydroxy-3,4-dihydro-2H-benzo[e][1,2]oxaborinine-8-carboxylic acid. In some embodiments, the crystalline forms are formulated for treating a subject in need thereof with a bacterial infection.
Type:
Grant
Filed:
March 5, 2018
Date of Patent:
August 17, 2021
Assignee:
VenatoRx Pharmaceuticals, Inc.
Inventors:
Christopher J. Burns, Daniel C. Pevear, Luigi Xerri, Timothy Henkel, Daniel McGarry, Lawrence Rosen, Gerald Brenner, Jean-Baptiste Arlin, Ana Fernandez Casares
Abstract: The present invention relates to novel compounds of general formula (I) wherein the groups X, and R1 to R4 have the meanings given in the description and claims, process for preparing these compounds and their use as for treating, preventing or ameliorating viral infections and their use for treating, preventing or ameliorating diseases which are associated with PLA2G16.
Type:
Grant
Filed:
September 12, 2017
Date of Patent:
August 17, 2021
Assignee:
HAPLOGEN GMBH
Inventors:
Wolfgang Fischl, Mark Whittaker, Christopher John Yarnold, Jean-Francois Pons, Mark Anthony Kerry, Patricia Leonie Amouzegh, Inaki Morao, Peter Neville Ingram, Ewa Iwona Chudyk
Abstract: The present invention relates to substituted indoline derivatives, methods to prevent or treat dengue viral infections by using said compounds and also relates to said compounds for use as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.
Inventors:
Bart Rudolf Romanie Kesteleyn, Jean-François Bonfanti, Erwin Coesemans, Pierre Jean-Marie Bernard Raboisson, Arnaud Didier M Marchand, Dorothée Alice Marie-Eve Bardiot
Abstract: A method for treatment of cardiac dysfunction comprising administering to a subject in need thereof a therapeutically effective amount of at least one of ANAVEX 2-73 or ANAVEX 19-144 or pharmaceutically acceptable salt thereof or combination thereof.
Abstract: The present invention relates generally to proteasome inhibiting ?-lactam compounds useful for the treatment of cancer and neurodegenerative disorders. The invention also provides pharmaceutical compositions and extended release formulations of said compounds, and medical uses of said compounds and/or pharmaceutical compositions to treat cancer and neurodegenerative disorders.
Type:
Grant
Filed:
December 22, 2017
Date of Patent:
July 6, 2021
Assignees:
Philippe Yves-Remy Simon, VITA API
Inventors:
Philippe Yves-Rémy Simon, Henri Oreal, Gérard Audran, Marvin Schulz, Jean-Patrick Joly, Didier Siri, Anouk Siri
Abstract: The present disclosure relates to novel crystalline forms of ozanimod and preparation method thereof. The provided crystalline forms of ozanimod comprise crystalline form CS9, crystalline form CS10 and crystalline form CS11, and can be used for treating autoimmune diseases, particularly used for preparing drugs for treating multiple sclerosis and ulcerative colitis. The crystalline forms of the present disclosure have one or more advantages in solubility, stability, hygroscopicity and processability and provide new and better choices for the preparation of ozanimod drug product, and are very valuable for drug development.
Abstract: The present invention provides water-soluble acetaminophen prodrugs and formulations which may be suitable for parenteral administration. Methods of treating a disease or condition responsive to acetaminophen (such as fever and/or pain) using the acetaminophen prodrugs, as well as kits, unit dosages, and combinations with additional pharmaceutical agent(s) are also provided.
Abstract: The invention provides novel compounds having the general formula (I) wherein R2, R3, R4, R5, R6, R7, R3, R8, R10, R11 and R23 are as described herein, compositions including the compounds and methods of using the compounds.
Type:
Grant
Filed:
September 4, 2018
Date of Patent:
May 25, 2021
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Benoit Hornsperger, Roberto Iacone, Hans P. Maerki, Peter Mohr, Michael Reutlinger
Abstract: A process a process of forming a non-halogenated flame retardant (FR) hindered amine light stabilizer (HALS) cross-linker is disclosed. The process includes forming a mixture that includes a first molecule having a hindered amine group. The first molecule corresponds to a functionalized 2,2,6,6-tetramethylpiperidine (TMP) molecule. The process also includes forming the non-halogenated FR HALS cross-linker via a chemical reaction of the first molecule a second molecule. The second molecule includes a phosphoryl group, a chloride group, and at least one cross-linkable (CL) moiety.
Type:
Grant
Filed:
March 25, 2019
Date of Patent:
May 11, 2021
Assignee:
International Business Machines Corporation
Inventors:
Scott B. King, Brandon M. Kobilka, Joseph Kuczynski, Jason T. Wertz
Abstract: Disclosed herein are substituted pyrazole-pyrimidine compounds of Formula (I) and variants thereof for the treatment, for example, of diseases associated with P2X purinergic receptors. In one embodiment, the P2X3 and/or P2X2/3 antagonists disclosed herein are potentially useful, for example, for the treatment of visceral organ, cardiovascular and pain-related diseases, conditions and disorders.
Type:
Grant
Filed:
December 11, 2017
Date of Patent:
April 27, 2021
Assignee:
Afferent Pharmaceuticals, Inc.
Inventors:
Ronald Charles Hawley, Prabha Ibrahim, Anthony P. Ford, Joel R. Gever
Abstract: Therapeutic compounds containing a phenyl core and amide link(s). Also described are pharmaceutical compositions incorporating the therapeutic compounds and a method for treating cancer with the compounds. These compounds are cytotoxic to stomach, colon, breast, and leukemia cancer cell lines via dual inhibition of Src kinases and tubulin.
Type:
Grant
Filed:
June 4, 2019
Date of Patent:
April 27, 2021
Assignee:
King Abdulaziz University
Inventors:
Moustafa E. El-Araby, Abdelsattar M. Omar, Maan T. Khayat, Dhaval Shah, Martin K. Safo, Azizah M. Malebari, Farid Ahmed
Abstract: A sensor compound and sensor composition comprising the sensor compound are disclosed. The sensor compound includes a metal atom and a mercaptoimidazolyl multidentate ligand. The sensor composition comprises the sensor compound and a metal dichalcogenide.
Type:
Grant
Filed:
March 6, 2020
Date of Patent:
April 20, 2021
Assignee:
CARRIER CORPORATION
Inventors:
Alexander Wei, Aiganym Yermembetova, Benjamin M. Washer
Abstract: The present invention is a method for purifying an NCA, including the steps of: a) dissolving an NCA contaminated with impurities into a solvent which is a good solvent and is not a chlorinated solvent followed by stirring to precipitate an undissolved impurity to afford a suspension, b) adding an acidic filter aid having ability to trap a basic impurity to the obtained suspension followed by filtration and/or forming a fixed bed of the acidic filter aid having ability to trap a basic impurity followed by filtering the suspension to bring the suspension to be in contact with the acidic filter aid having ability to trap a basic impurity, and c) adding the obtained filtrate dropwise to a poor solvent for NCA to crystallize out the NCA in which the impurities are removed. This makes it possible to purify a low-purity NCA conveniently to afford a high-purity NCA.
Abstract: Combination therapy with sorafenib or regorafenib and a phosphoramidate prodrug of troxacitabine with the formula: where Y is C1-C8 straight or branched chain alkyl, X is H, halo, C3-C4cycloalkyl or C1-C4alkyl and Z is H or fluoro, or a pharmaceutically acceptable salt thereof, shows surprising utility in the treatment of liver cancer or liver metastasis.
Type:
Grant
Filed:
August 30, 2019
Date of Patent:
March 30, 2021
Assignee:
Medivir Aktiebolag
Inventors:
Mark Albertella, Anders Eneroth, Björn Klasson, Fredrik Öberg, John Öhd
Abstract: The present invention relates to a compound of general formula (A). The invention provides asynthesis of new 4?-amidotriazole linked podophyllotoxin derivatives of general formulae 8a-z to 9a-z useful as potential anticancer agents against human cancer cell lines and process for the preparation thereof.
Type:
Grant
Filed:
March 10, 2017
Date of Patent:
March 16, 2021
Assignee:
COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
Inventors:
Ahmed Kamal, Velma Ganga Reddy, Ayinampudi Venkata Subbarao, Syed Riyaz, Vadithe Lakshma Nayak, Shaik Taj
Abstract: Disclosed herein are improved formulations for the cabazitaxel. The formulations exhibit increased storage stability relative to other formulations, and are simpler for health care providers to prepare and administer to patients.
Abstract: The present invention relates to the use of a compound containing a moiety of formula (I) as a reagent for linking a compound of formula R1—H which comprises a first functional moiety of formula F1 to a second functional moiety of formula F2 wherein X, X?, Y, R1, F1 and F2 are as defined herein. The present invention also provides related processes and products. The present invention is useful for creating functional conjugate compounds, and specifically conjugates in which at least one of the constituent molecules carries a thiol group.
Type:
Grant
Filed:
December 16, 2019
Date of Patent:
March 2, 2021
Assignee:
UCL BUSINESS LTD
Inventors:
Mark Smith, Stephen Caddick, James Baker, Vijay Chudasama