Abstract: The present invention covers aminoquinolone compounds of general formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8 and n are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and/or prophylaxis of diseases, in particular of diacylglycerol kinase alpha regulated disorders, as a sole agent or in combination with other active ingredients.
Inventors:
Norbert Schmees, Lars Wortmann, Dennis Kirchhoff, Thi Thanh Uyen Nguyen, Nicolas Werbeck, Ulf Bömer, Kirstin Petersen, Christina Kober, Christian Lechner, Dirk Kosemund, Rienk Offringa, Mareike Grees, Benjamin Bader
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: The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof, is useful as an agent for the prophylaxis or treatment of narcolepsy.
Abstract: A new synthetic route to 4,4?-diiodoazobenzene compound using homooxidative cross-coupling of an aryl diazonium salt using a Cu-catalyzed Sandmeyer-style reaction.
Abstract: The present invention provides salts and crystalline forms of Linsitinib (OSI-906; cis-3-[8-amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methyl-cyclobutanol). These forms of Linsitinib provide increased solubility and improved pharmacokinetic profiles for orally administered pharmaceutical formulations. Accordingly, the invention enables improved methods for treating human insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR) mediated conditions.
Abstract: Provided herein are compounds of Formula (I). Methods for the preparation of the compounds of Formula (I) and intermediates useful in the preparation of the compounds of Formula (I) are described herein. The compounds of Formula (I) may be useful as inhibitors of the MYST family of lysine acetyltransferases (KATs) for the treatment of and/or prophylaxis of hyperproliferative diseases, disorders or conditions such as cancer. In particular, the compounds of Formula (I) are useful for the inhibition of KAT6A and KAT6B which are enzymes frequently mutated, overexpressed, amplified and/or translocated in cancer altering their normal expression, activity and function. The use of the compounds of Formula (I) in the manufacture of pharmaceutical compositions or for treating cancers is further described, including for treating cancer in combination with other anti-cancer agents.
Abstract: A compound N?-[(2-chlorobenzoyl)oxy]-1,3-benzothiazole-2-carboximidamide, its synthesis, and its use as an anticancer and/or antimicrobial agent.
Type:
Grant
Filed:
August 29, 2023
Date of Patent:
April 23, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Hany Mohamed Abd El-Lateef Ahmed, Mai Mostafa Khalaf Ali, Amer A. Amer, Doaa Hassan Ahmed Ali, Esam Ajlan Talag Alqurashi, Antar Ahmed Abdelhamid Ahmed
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 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: This disclosure pertains to compounds, the preparation thereof, and the use of these compounds in the treatment of prostate cancer, including metastatic and/or castrate-resistant prostate cancer, in subjects in need thereof.
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.