Abstract: Substituted naphthyl p38? mitogen-activated protein kinase inhibitors, pharmaceutical compositions thereof, and the use of the substituted naphthyl p38? mitogen-activated protein kinase inhibitors and pharmaceutical compositions thereof for treating diseases are disclosed.
Abstract: A 2-((1H-indazol-5-yl)methylene)hydrazinecarbothioamide compound, its synthesis, and its use as a tyrosine kinase inhibitor. In particular, the synthesis of the 2-((1H-indazol-5-yl)methylene)hydrazinecarbothioamide compound as shown below. This compound has a high efficacy of inhibiting mushroom tyrosinase enzyme, and is a potent inhibitor of tyrosinase that can be used as an inhibitor of skin hyperpigmentation as well as an inhibitor of fruit and vegetable browning.
Abstract: The present invention covers aminothiazole compounds of general formula (I), in which R1, R2, R3 and R4 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 zeta (DGK?) regulated disorders, as a sole agent or in combination with other active ingredients.
Inventors:
Norbert Schmees, Ulrike Roehn, Dennis Kirchhoff, Kirstin Petersen, Mareike Grees, Nicolas Werbeck, Benjamin Bader, Rienk Offringa, Corinna Link
Abstract: Provided herein are lipid compounds that can be used in combination with other lipid components, such as neutral lipids, cholesterol and polymer conjugated lipids, to form lipid nanoparticles for delivery of therapeutic agents (e.g., nucleic acid molecules) for therapeutic or prophylactic purposes, including vaccination. Also provided herein are lipid nanoparticle compositions comprising said lipid compounds.
Abstract: The invention provides novel 6-heterocyclyl-4-morpholin-4-yl-pyridine-2-one compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for using such compounds in treatment of diseases including cancer, diabetes, inflammatory disease, neurodegenerative disorders, cardiovascular disorders and viral infections; wherein R1, R2, R3 and A are as defined in the specification.
Type:
Grant
Filed:
October 14, 2021
Date of Patent:
April 23, 2024
Assignee:
Sprint Bioscience AB
Inventors:
Jessica Martinsson, Martin Andersson, Johan Lindström, Rickard Forsblom, Fredrik Rahm, Tobias Ginman, Jenny Viklund
Abstract: Described herein are methods of treating metastatic castration-sensitive prostate cancer with anti-androgens, including but not limited to, 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide.
Abstract: A group of tropomyosin receptor kinase inhibitors including an amido-phenoxy-indazole structure fragment. These compounds show potent inhibitory effects on various oncogenic kinases, especially TRK, and thus can be used to treat tumors or cancers.
Type:
Grant
Filed:
September 3, 2019
Date of Patent:
April 9, 2024
Assignee:
TYLIGAND BIOSCIENCE (SHANGHAI) LIMITED
Inventors:
Boyu Zhong, Tony Yantao Zhang, Yiju Cao, Guangming Chen
Abstract: Provided herein are pharmaceutical compositions that comprise myrcene, optionally in admixture with cannabinoids and other terpenes, typically substantially free of THC and THCA, for targeting TRPV1 receptors. Also provided are methods of using the pharmaceutical compositions to desensitize TRPV1 receptors in order to treat pain, cardiovascular diseases such as cardiac hypertrophy, overactive bladder, and chronic cough.
Abstract: Linker-drug compounds and antibody-drug conjugates that bind to human oncology targets are disclosed. The linker-drug compounds and antibody-drug conjugates comprise a splicing modulator drug moiety. The disclosure further relates to methods and compositions for use in the treatment of neoplastic disorders by administering the antibody-drug conjugates provided herein. In an embodiment, the splicing modulator comprises a pladienolide or a pladienolide derivative.
Type:
Grant
Filed:
May 3, 2022
Date of Patent:
April 2, 2024
Assignee:
EISAI R&D MANAGEMENT CO., LTD.
Inventors:
Ermira Pazolli, Silvia Buonamici, Thiwanka Samarakoon, Sudeep Prajapati, Nathan Fishkin, James Palacino, Michael Seiler, Ping Zhu, Andrew Cook, Peter Smith, Xiang Liu, Shelby Ellery, Dominic Reynolds, Lihua Yu, Zhenhua Wu, Shouyong Peng, Nicholas Calandra, Megan Sheehan, Yonghong Xiao
Abstract: Provided are methods for prophylaxis or therapy for an RNA virus infection. The methods involve modulating the Type I interferon pathway in RNA virus infected cells of an individual. The Type I interferon pathway is modulated by administering one or more agents to virus infected cells that inhibit the expression and/or function of METTL3 or inhibit expression and/or function of YTHDF1, YTHDF2 or YTHDF3.
Abstract: The invention relates to a (S)-3-[1-Methylpyrrolidin-2-yl]pyridine analogues thereof, precursors thereof, or its derivatives, for the use as a pharmaceutical in form of a substance as a colloid of fine solid and/or liquid particles in a fluid. 1. According to the invention the substance is dispensed in form of a parenteral administration into a human and/or animal body.
Abstract: The present invention relates to a pharmaceutically compatible iron chelator or a prodrug thereof for use in treating and/or preventing cancer in a subject suspected or known to comprise hypoxic cancer cells, and use in treatment and/or prevention of a human papillomavirus (HPV) related lesion. The present invention further relates to a use of an iron chelator or prodrug thereof for inducing senescence in a cancer cell, preferably a hypoxic cancer cell; and to a method for inducing an irreversible proliferation arrest in cancer cells comprising a) contacting said cancer cells with an iron chelator or prodrug thereof and, thereby, b) inducing an irreversible proliferation arrest in said cancer cells.
Type:
Grant
Filed:
November 23, 2018
Date of Patent:
March 19, 2024
Assignee:
Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts
Inventors:
Felix Hoppe-Seyler, Julia A. Braun, Karin Hoppe-Seyler
Abstract: The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.
Type:
Grant
Filed:
April 23, 2021
Date of Patent:
March 5, 2024
Assignee:
VALO HEALTH, INC.
Inventors:
Kenneth W. Bair, Nicholas Barczak, Bingsong Han, David R. Lancia, Jr., Cuixian Liu, Matthew W. Martin, Pui Yee Ng, Aleksandra Rudnitskaya, Jennifer R. Thomason, Mary-Margaret Zablocki, Xiaozhang Zheng
Abstract: Disclosed herein are methods of treating a cancer characterized by expressing a mutant form of a RAS protein. Some embodiments relate to treatment of cancer by administering Plinabulin to a subject in need thereof.