Abstract: Disclosed are methods for the treatment of cancer in patients in need of such treatment. The methods comprise administering to such a patient an Aurora kinase inhibitor such as 4-{[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino}-2-methoxybenzoic acid or a pharmaceutically acceptable salt in combination with a platin. Also disclosed are medicaments for use in the treatment of cancer.
Abstract: The invention provides a compound of formula (I): wherein Ring A, Q, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, X, a, b, c and d are as defined in the specification, useful for inhibiting the activity of SHP2.
Inventors:
Tadashi Shimamura, Ryo Kato, Risako Miura, Takashi Mita, Takahiro Ogawa, Yufu Sagara, Christopher Norbert Johnson, Steven Howard, James Edward Harvey Day, Jeffrey David St. Denis, John Walter Liebeschuetz
Abstract: An L-lysine salt of 4-chloro-5-[4-(2,6-dichlorophenyl)sulfonylpiperazin-1-yl]-1-benzofuran-2-carboxylic acid and forms thereof are provided. Also provided are pharmaceutical or veterinary compositions comprising this L-lysine salt and their use for treating a number of diseases.
Abstract: Compounds of formula (I) wherein A, W, R3b, Z and p have the meaning according to the claims, can be employed, inter alia, for the treatment of taupathies and Alzheimer's disease.
Type:
Grant
Filed:
August 22, 2019
Date of Patent:
June 25, 2024
Assignee:
Asceneuron SA
Inventors:
Anna Quattropani, Grant Wishart, Santosh S. Kulkarni, Paul Rakesh
Abstract: The present invention relates to certain substituted heterocondensed pyridone analogues of formula (I) which modulate the activity of Isocitrate Dehydrogenase (IDH). The compounds of this invention are therefore useful in treating diseases caused by mutated IDH1 and/or mutated IDH2 enzyme and/or IDH1 wild type enzyme, in particular cancer, cell proliferative disorders and immune-related disorders. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
Type:
Grant
Filed:
May 16, 2019
Date of Patent:
June 25, 2024
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Elena Casale, Francesco Casuscelli, Teresa Disingrini, Paola Magnaghi, Beatrice Malgesini, Ilaria Motto, Stefano Nuvoloni
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 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: 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.