Abstract: The present disclosure relates to a compound of formula (Ia), (Ib), (IIa), and (IIb): which are useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.
Type:
Grant
Filed:
November 25, 2019
Date of Patent:
May 28, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Michael Graupe, John O. Link, Roland D. Saito, Scott D. Schroeder, Dimitrios Stefanidis, Winston C. Tse, Jennifer R. Zhang
Abstract: The present invention relates to a solid pharmaceutical preparation comprising ?-lipoic acid, dicalcium phosphate and a binder. The solid pharmaceutical preparation has an improved stability and thereby improved bioavailability.
Abstract: This invention relates to novel salts and crystal forms of 2-[3-({1-[2-(dimethylamino)ethyl]-2-(2,2-dimethylpropyl)-1H-1,3-benzodiazol-5-yl}sulfonyl)azetidin-1-yl]ethan-1-ol, simply abbreviated as Compound A, which is a selective CB2 receptor agonist. The present invention provides a salt of Compound A, a crystal form thereof, a method for preparing the said salt and a pharmaceutical composition thereof and its use. The salts of Compound A of the present invention show good pharmaceutical formulation properties such as high aqueous solubility, good crystallinity, high melting point, good chemical and physical stability, or non-deliquescent.
Abstract: The invention discloses compositions and methods comprising enriched Bisdemethoxycurcumin (BDMC) present not less than 20% w/w for use in inhibiting Receptor for Advanced Glycation End-Products (RAGE) expression in a subject with chronic-inflammatory condition. The composition further comprises ?-amyrin palmitate (BAP). The invention also includes disclose the use of the above composition in the management of chronic inflammatory condition in a subject.
Type:
Grant
Filed:
December 16, 2021
Date of Patent:
April 16, 2024
Assignee:
Sami-Sabinsa Group Limited
Inventors:
Muhammed Majeed, Kalyanam Nagabhushanam, Lakshmi Mundkur
Abstract: RAS modulating compounds and methods of using the same are provided. The compounds find use in modulating the activity of a target RAS in a sample. The target RAS can be a mutant RAS that is implicated in a disease of interest. In some cases, the subject compounds can inhibit the growth of cancer cells whose progression is driven by kRAS or a mutated kRAS. Methods of treating a subject for a RAS driven disease including administering a therapeutically effective amount of the subject compound are provided. Also provided are pharmaceutical compositions and kits which include the subject compounds.
Type:
Grant
Filed:
August 6, 2019
Date of Patent:
April 2, 2024
Assignee:
Tosk, Inc.
Inventors:
Annie L. Lennek, Stephen D. Yanofsky, Brian D. Frenzel, Solomon B. Ungashe, William A. Garland, Philip Liaw
Abstract: Disclosed herein are pyrazole pyrimidine compounds that modulate and/or inhibit hematopoietic progenitor kinase 1, as well as methods of making such compounds and therapeutic methods of using same.
Type:
Grant
Filed:
March 14, 2022
Date of Patent:
March 5, 2024
Assignee:
RAPT Therapeutics, Inc.
Inventors:
Cyril Bucher, Adrian Dukes, Blanca Gomez, Hannah Haley, Dennis Hu, Jeffrey J. Jackson, Michelle Yoo Min Ko, Paul Leger, Anqi Ma, Andrew A. Ng, Daniel Poon, Omar Robles, Anton Shakhmin, Grant Shibuya, Parcharee Tivitmahaisoon, Vi-Anh Vu, David J. Wustrow, Mikhail Zibinsky
Abstract: The present invention relates to a series of compounds having a structural benzothiazole-benzamide core with capacity to inhibit the LRRK2 enzyme, due to which the invention also relates to the use of these compounds for treating neurodegenerative diseases in which this enzyme is involved, such as Parkinson's Disease or Alzheimer's Disease.
Type:
Grant
Filed:
August 8, 2019
Date of Patent:
February 27, 2024
Assignee:
CONSEJO SUPERIOR DE INVESTIGACIONES CIENTÍFICAS
Inventors:
Ana Martinez Gil, Carmen Gil Ayuso-Gontan, Josefa Zaldivar Diaz De Bonilla, Rocio Benitez Fernandez
Abstract: The application relates to N-(4-fluoro-3-(6-(3-methylpyridin-2-yl)-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)phenyl)-2,4-dimethyloxazole-5-carboxamide (Compound I) fumaric acid co-crystals and X-ray amorphous complexes of Compound (I) and fumaric acid. The application also provides methods of making the same; pharmaceutical compositions comprising them; and their use in treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a kinetoplastid parasite, such as leishmaniasis, human African trypanosomiasis and Chagas disease.
Type:
Grant
Filed:
October 8, 2019
Date of Patent:
February 6, 2024
Assignee:
NOVARTIS AG
Inventors:
Yudong Cao, Siyi Jiang, Hongyong Kim, Andreas Kordikowski, Irene Xia, Bo Yu, Jing Zhang, Yi Zhao
Abstract: The present invention relates to a compound according to general formula (I), which acts as an inhibitor of PqsR (the currently only known receptor for the Pseudomonas Quinolone Signal (PQS)); to a pharmaceutical composition containing one or more of the compound(s) of the invention; to a combination preparation containing at least one compound of the invention and at least one further active pharmaceutical ingredient; and to uses of said compound(s), including the use as a medicament, e.g. the use in the treatment or prophylaxis of a bacterial infection, especially a Pseudomonas aeruginosa or Burkholderia infection.
Type:
Grant
Filed:
July 3, 2019
Date of Patent:
January 30, 2024
Assignee:
Helmholtz-Zentrum Für Infektionsforschung GmbH
Inventors:
Ahmed S. A. Ahmed, Martin Empting, Mostafa Hamed, Rolf W. Hartmann, Jörg Haupenthal, Thomas Hesterkamp, Ahmed A. M. Kamal, Christine K. Maurer, Teresa Röhrig, Christian Schütz, Samir Yahiaoui, Michael Zender
Abstract: The present disclosure relates to novel compounds for use in therapeutic treatment of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.
Type:
Grant
Filed:
December 21, 2021
Date of Patent:
January 23, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Daniel H. Byun, Zhenhong R. Cai, Eda Y. Canales, Laurent P. Debien, Timothy R. Hansen, Richard Huang, Petr Jansa, Rick A. Lee, Jennifer A. Loyer-Drew, Ryan McFadden, Michael L. Mitchell, Hyung-Jung Pyun, Roland D. Saito, Michael S. Sangi, Adam J. Schrier, Marina E. Shatskikh, James G. Taylor, Joshua J. Van Veldhuizen, Lianhong Xu
Abstract: The present disclosure relates to the discovery that certain ocular diseases may be treated using Edonentan crystalline forms. Specific Edonentan crystalline form can be used alone or in combination with an intra-ocular pressure (TOP) reducing agent, a neuroprotective agent, or an anti-VEGF agent. Using Edonentan crystalline forms, alone or in combination with an additional agent, provides increased perfusion to the retina or reduced IOP in certain ocular diseases and reduces damage to retinal cells.
Type:
Grant
Filed:
August 2, 2022
Date of Patent:
January 16, 2024
Assignee:
Perfuse Therapeutics, Inc.
Inventors:
Sevgi Gurkan, David Floyd, Zhongli Ding
Abstract: The present invention is related to the inhibition of the formation of Streptococci biofilms through the inhibition of glucosyl transferase (Gtf). Compounds, compositions and methods for inhibiting Streptococcus biofilm formation, as well as for preventing, inhibiting and/or treating the formation of dental caries, and methods of identifying compounds that prevent, inhibit and/or treat the formation of dental caries are provided.
Type:
Grant
Filed:
April 3, 2019
Date of Patent:
January 9, 2024
Assignee:
UAB Research Foundation
Inventors:
Sadanandan E. Velu, Hui Wu, Qiong Zhang, Bhavitavya Nijampatnam
Abstract: The disclosure provides methods, treatments and materials for enhancing the effect of an adenosine A2 receptor agonist in the treatment, mitigation or prophylaxis of a disease or condition characterized by inotropic and/or lusitropic dysfunction, and/or enhancing adenosine A2 receptor function in the treatment, mitigation or prophylaxis of a disease or condition characterized by impaired adenosine A2 receptor function, comprising administration of an effective amount of a PDE1 inhibitor to a patient in need thereof, for example a patient suffering from heart failure.
Type:
Grant
Filed:
January 31, 2019
Date of Patent:
December 12, 2023
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
David Kass, Toru Hashimoto, Lawrence Wennogle, Joseph Hendrick, Robert Davis
Abstract: There is provided a compound of formula (I), wherein R1, R2, R3, Q1, Q2, Q3, X, A and n are as defined herein, which compounds are useful in the treatment of diseases characterised by impaired signalling of neurotrophins and/or other trophic factors, such as Alzheimer's disease and the like.
Abstract: The present invention relates to novel compounds of formula I: which have the properties of CDK8/19 inhibitors, to a pharmaceutical composition comprising said compounds, and to use thereof as a medicine for treating diseases and disorders.
Type:
Grant
Filed:
July 31, 2019
Date of Patent:
December 12, 2023
Inventors:
Aleksei Leonidovich Mindich, Anna Jur'evna Chestnova, Mariia Andreevna Kasatkina, Andrei Ivanovich Alafinov, Aleksei Sergeevich Gavrilov, Anton Aleksandrovich Evdokimov, Liliana Vyacheslavovna Lenshmidt, Elena Aleksandrovna Maksimenko, Mariia Sergeevna Mishina, Sergei Aleksandrovich Silonov, Evgenii Jur'evich Smirnov, Pavel Andreevich Iakovlev, Dmitry Valentinovich Morozov
Abstract: Disclosed herein are methods for treating or limiting development of cardiovascular disease-related neurological disorders by administering a compound of general formula (I), as defined herein.
Type:
Grant
Filed:
May 10, 2019
Date of Patent:
December 5, 2023
Assignee:
Arizona Board of Regents on Behalf of the University of Arizona
Inventors:
Sachin Suresh Jadhav, Kevin Gaffney, Kathleen E. Rodgers, Maira Soto
Abstract: The present disclosure relates to a pharmaceutical composition comprising ibrutinib as an effective ingredient for preventing or treating neurodegenerative brain disease. Ibrutinib according to the present disclosure inhibits LPS-induced proinflammatory cytokine levels and BV2 microglial cell migration. In addition, ibrutinib treatment significantly reduced LPS-mediated microglial and astroglial activation. Ibrutinib treatment significantly diminished AP plaque numbers, tau hyperphosphorylation, and tau kinase CDK5 phosphorylation. Moreover, ibrutinib treatment enhances memory and thus can be used as a therapeutic agent for prevention or treatment of neurodegenerative brain disease.
Type:
Grant
Filed:
April 26, 2019
Date of Patent:
November 28, 2023
Assignee:
DAEGU GYEONGBUK INSTITUTE OF SCIENCE AND TECHNOLOGY
Inventors:
Hyang Sook Hoe, Jeoung Yeon Kim, Hye Yeon Nam, Ju Young Lee, Young Pyo Nam, Ri Jin Kang, Hyun Ju Lee
Abstract: Provided are crystalline forms of (R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-2-(oxetan-3-yl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-5-yl)-1H-1,2,3-triazole-4-carboxamide, pharmaceutical compositions, methods of use and methods of making thereof.
Type:
Grant
Filed:
October 15, 2019
Date of Patent:
November 21, 2023
Assignee:
BIOGEN MA INC.
Inventors:
Fengmei Zheng, Anton Peterson, Kalyan Vasudevan, Chaomin Li, Daniel B. Patience, Yiqing Lin
Abstract: Provided herein are compounds of formula (I?): or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein Y2, Y3, L1, L2, X1, X2, X3, X4, X5, Q1, R1, R2, Rk, Rm, and Rn are as defined elsewhere herein. Also provided herein are methods of preparing compounds of formula (I?). Also provided herein are methods of inhibiting GYS1 and methods of treating a GYS1-mediated disease, disorder, or condition in an individual in need thereof.
Type:
Grant
Filed:
March 14, 2022
Date of Patent:
November 14, 2023
Assignee:
MAZE THERAPEUTICS, INC.
Inventors:
David John Morgans, Jr., Kevin Mellem, Hannah L. Powers, Patrick Sang Tae Lee, Walter Won, Christopher Joseph Sinz