Patent classifications
C07C259/06
Inhibitors of histone lysine specific demethylase (LSD1) and histone deacetylases (HDACS)
A series of phenelzine analogs comprising a phenelzine scaffold linked to an aromatic moiety and their use as inhibitors of lysine-specific demethylase 1 (LSD1) and/or one or more histone deacetylases (HDACs) is provided. The presently disclosed phenelzine analogs exhibit potency and selectivity for LSD1 versus MAO and LSD2 enzymes and exhibit bulk, as well as, gene specific histone methylation changes, anti-proliferative activity in several cancer cell lines, and neuroprotection in response to oxidative stress. Accordingly, the presently disclosed phenelzine analogs can be used to treat diseases, conditions, or disorders related to LSD1 and/or HDACs, including, but not limited to, cancers and neurodegenerative diseases.
COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS
The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.
ANTI-FIBROTIC COMPOUNDS AND USE THEREOF
The present invention relates to compounds, compositions and methods for treating fibrosis. In particular, compounds that inhibit or downregulate Sirtuin 1 (SIRT1) activity, which are particularly useful in the treatment of Idiopathic Pulmonary Fibrosis (IPF) are provided.
ANTI-FIBROTIC COMPOUNDS AND USE THEREOF
The present invention relates to compounds, compositions and methods for treating fibrosis. In particular, compounds that inhibit or downregulate Sirtuin 1 (SIRT1) activity, which are particularly useful in the treatment of Idiopathic Pulmonary Fibrosis (IPF) are provided.
HDAC8 inhibitors for treating cancer
Provided herein, inter alia, are compound and methods of treating cancer by inhibiting HDAC8.
HDAC8 inhibitors for treating cancer
Provided herein, inter alia, are compound and methods of treating cancer by inhibiting HDAC8.
IMAGING AND THERAPEUTIC COMPOSITIONS
The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging and therapeutic agents when bound to an appropriate metal centre, particularly for the imaging of tumours.
Compounds for treating infections
The invention relates to hydrazide compounds and their use in medicine, particularly in treating and/or preventing infections caused by a fungus.
Compounds for treating infections
The invention relates to hydrazide compounds and their use in medicine, particularly in treating and/or preventing infections caused by a fungus.
TRNA SYNTHETASE INHIBITORS
Disclosed herein are secondary amine compounds that inhibit tRNA synthetase. The compounds of the invention are useful in inhibiting tRNA synthetase in Gram-negative bacteria and are useful in killing Gram-negative bacteria. The secondary amine compounds of the invention are also useful in the treatment of tuberculosis.