Patent classifications
C07D211/28
CHEMICAL PROBES AND INHIBITORS FOR POLYPEPTIDES OF SARS CORONAVIRUSES
The present invention relates to a compound which can be used in the treatment of infections caused by SARS coronaviruses, e.g. by blocking the active site of the proteases 3CL.sup.pro and PL.sup.pro. The compound can be used as inhibitor or label as such or can be used in screening methods for profiling other inhibitors. Moreover, the present invention relates to a method of producing the compound.
CHEMICAL PROBES AND INHIBITORS FOR POLYPEPTIDES OF SARS CORONAVIRUSES
The present invention relates to a compound which can be used in the treatment of infections caused by SARS coronaviruses, e.g. by blocking the active site of the proteases 3CL.sup.pro and PL.sup.pro. The compound can be used as inhibitor or label as such or can be used in screening methods for profiling other inhibitors. Moreover, the present invention relates to a method of producing the compound.
AGENTS FOR DIFFERENTIATING STEM CELLS AND TREATING CANCER
The present application discloses a method for identifying an agent for the treatment or prevention of cancer or metastatic cancer comprising the steps of contacting stem cell with a potential agent, and identifying an agent that induces differentiation, or inhibits stem cell pluripotency or growth of the stem cell, wherein such agent is determined to be an anti-cancer agent.
4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase
Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells. The compounds can also be used in methods for treating or preventing a 12-lipoxygenase mediated disease or disorder.
4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase
Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells. The compounds can also be used in methods for treating or preventing a 12-lipoxygenase mediated disease or disorder.
K-RAS MODULATORS
Provided herein, inter alia, are methods and compounds for inhibiting K-Ras and for treating cancer.
K-RAS MODULATORS
Provided herein, inter alia, are methods and compounds for inhibiting K-Ras and for treating cancer.
COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF AGENTS
The disclosure features amino lipids and compositions involving the same. Nanoparticle compositions include an amino lipid as well as additional lipids such as phospholipids, structural lipids, PEG lipids, or a combination thereof. Nanoparticle compositions further including therapeutic and/or prophylactic agents such as RNA are useful in the delivery of therapeutic and/or prophylactic agents to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.
COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF AGENTS
The disclosure features amino lipids and compositions involving the same. Nanoparticle compositions include an amino lipid as well as additional lipids such as phospholipids, structural lipids, PEG lipids, or a combination thereof. Nanoparticle compositions further including therapeutic and/or prophylactic agents such as RNA are useful in the delivery of therapeutic and/or prophylactic agents to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.
BIARYL SULFONAMIDE DERIVATIVE HAVING FILOVIRUS CELL ENTRY INHIBITION ACTIVITY
The objective of the present invention is to provide a novel compound inhibiting the entry of a filovirus into a cell, a medical composition, an anti-filovirus agent, or a filovirus entry inhibitor containing the compound, as well as a method for inhibiting a filovirus cell entry process in vitro, a method for treating a filovirus infectious disease, and the like. The objective has been achieved by providing: the compound represented by formula (I) or a hydrate thereof; or a pharmaceutically acceptable salt of the compound or a hydrate thereof.